Estradiol Implant 100mg (Organon Laboratories Ltd)

1. Name Of The Medicinal Product

ESTRADIOL IMPLANT 100mg 

2. Qualitative And Quantitative Composition

Each implant contains 100mg estradiol.

3. Pharmaceutical Form

Implant

4. Clinical Particulars

4.1 Therapeutic Indications

Hormone replacement therapy for estrogen deficiency symptoms in postmenopausal women.

Prevention of osteoporosis in postmenopausal women at high risk of future fractures who are intolerant of, or contraindicated for, other medicinal products approved for the prevention of osteoporosis.

4.2 Posology And Method Of Administration

Dosage and Administration

Dose

Adults: 25 - 100 mg

Estradiol implants are available in strengths of 25, 50 and 100mg. For initiation and continuation of treatment of postmenopausal symptoms, the lowest effective dose for the shortest duration (see also section 4.4) should be used. In most patients, implantation of a 25mg dose provides relief of symptoms and prevents osteoporosis. Some patients may require 50 mg or even higher doses initially.

If possible, subsequent doses should be reduced stepwise (for example, 100mg to 50mg to 25mg), eventually using 25mg as a maintenance dose. Frequency of replacement depends on the duration of activity of the implants administered and the severity of the symptoms. Patients require a further implant when symptoms return, usually every 4 to 8 months.

Use of a progestagen

Women with an intact uterus:

Because of the sustained absorption of estradiol, the endometrium of post-menopausal or ovariectomised women is liable to progressive hypertrophy. Therefore, in women with an intact uterus, additional administration of a progestagen is recommended, for 12-14 days in each cycle, to prevent endometrial hyperplasia.

When the patient no longer requires or seeks re-implantation with estradiol pellets, it is recommended that, in those women with an intact uterus, cyclical administration of an oral progestagen should be continued until there is a cessation of withdrawal bleeding, in order to prevent the possibility of continued endometrial stimulation.

Hysterectomised women:

Unless there is a previous diagnosis of endometriosis, it is not recommended to add a progestagen in hysterectomised women.

Administration

Estradiol implants should be inserted subcutaneously, (either by means of a trocar and cannula or in the wound at the time of laparotomy), into an area where there is relatively little movement or blood supply, such as the lower abdominal wall or the buttock. Insertion is made under local anaesthesia and the wound is closed either with an adhesive dressing or a fine suture.

Full aseptic 'no touch' technique should be adopted.

Removal of the implant

Since the implant consists entirely of estradiol without any auxilliary ingredients, it is biodegradable and no removal procedure is required. In the rare event that removal of the implant should be necessary, the implant may be located by palpation or, if not successful, by Magnetic Resonance Imaging. This technique can identify the implant by its size and structure. The implant can then be precisely located by insertion of a localiser wire with the tip ending at the implant. After locating the implant, it can be removed following a small incision under local anaesthetic.

Starting/switching treatment

An Estradiol implant may be inserted immediately in women experiencing a surgical menopause.

In women not taking HRT or who are changing from a continuous-combined HRT product, an Estradiol implant may be inserted at any time. In women who are switching from a sequential HRT regimen, the implant should be inserted right after the withdrawal bleeding has ended.

4.3 Contraindications

• Known, past or suspected breast cancer.

• Known or suspected estrogen-dependent malignant tumours (e.g endometrial cancer).

• Undiagnosed genital bleeding.

• Untreated endometrial hyperplasia.

• Previous idiopathic or current venous thromboembolism (deep venous thrombosis, pulmonary embolism).

• Active or recent arterial thromboembolic disease (e.g. angina, myocardial infarction).

• Acute liver disease, or a history of liver disease as long as liver function tests have failed to return to normal

• Known hypersensitivity to the active substance.

• Porphyria.

4.4 Special Warnings And Precautions For Use

For the treatment of postmenopausal symptoms, HRT should only be initiated for symptoms that adversely affect quality of life. In all cases, a careful appraisal of the risks and benefits should be undertaken at least annually and HRT should only be continued as long as the benefit outweighs the risk.

Medical examination/follow-up

Before initiating or reinstituting HRT, a complete personal and family medical history should be taken. Physical (including pelvic and breast) examination should be guided by this and by the contraindications (section 4.3) and warnings for use (section 4.4). During treatment, periodic check-ups are recommended of a frequency and nature adapted to the individual woman. Women should be advised what changes in their breasts should be reported to their doctor or nurse (see “Breast cancer” below). Investigations, including mammography, should be carried out in accordance with currently accepted screening practices, modified to the clinical needs of the individual.

Conditions which need supervision

If any of the following conditions are present, have occurred previously, and/or have been aggravated during pregnancy or previous hormone treatment, the patient should be closely supervised. It should be taken into account that these conditions may recur or be aggravated during treatment with Estradiol implants, in particular:

• Leiomyoma (uterine fibroids) or endometriosis.

• A history of, or risk factors for, thromboembolic disorders (see below).

• Risk factors for estrogen dependent tumours, e.g. 1^st degree heredity for breast cancer.

• Hypertension.

• Liver disorders (e.g. liver adenoma).

• Diabetes mellitus with or without vascular involvement.

• Cholelithiasis.

• Migraine or (severe) headache.

• Systemic lupus erythematosus.

• A history of endometrial hyperplasia (see below)

• Epilepsy.

• Asthma.

• Otosclerosis.

Reasons for immediate withdrawal of therapy:

Therapy should be discontinued in case a contra-indication is discovered and in the following situations:

• Jaundice or deterioration in liver function.

• Significant increase in blood pressure.

• New onset of migraine-type headache.

• Pregnancy.

Endometrial hyperplasia

• The risk of endometrial hyperplasia and carcinoma is increased when estrogens are administered alone for prolonged periods (see section 4.8). The addition of a progestagen for at least 12 days of the cycle in non-hysterectomised women greatly reduces this risk.

• The endometrial safety of Estradiol implants with the addition of progestagen in women with an intact uterus has not been studied in clinical trials.

• Break-through bleeding and spotting may occur during the first months of treatment. If break-through bleeding or spotting appears after some time on therapy, or continues after treatment has been discontinued, the reason should be investigated, which may include endometrial biopsy to exclude endometrial malignancy.

• Unopposed estrogen stimulation may lead to premalignant or malignant transformation in the residual foci of endometriosis. Therefore, the addition of progestagens to estrogen replacement therapy should be considered in women who have undergone hysterectomy because of endometriosis if they are known to have residual endometriosis (but see above).

Breast cancer

A randomised placebo-controlled trial, the Women's Health Initiative Study (WHI), and epidemiological studies, including the Million Women Study (MWS), have reported an increased risk of breast cancer in women taking estrogens, estrogen-progestagen combinations or tibolone for HRT for several years (see section 4.8). For all HRT, an excess risk becomes apparent within a few years of use and increases with duration of use but returns to baseline within a few (at most five) years after stopping treatment.

In the MWS, the relative risk of breast cancer with conjugated equine estrogens (CEE) or estradiol (E2) was greater when a progestagen was added, either sequentially or continuously, and regardless of type of progestagen. There was no evidence of a difference in risk between the different routes of administration.

In the WHI Study, the continuous combined conjugated equine estrogen and medroxyprogesterone acetate (CEE + MPA) product used was associated with breast cancers that were slightly larger in size and more frequently had local lymph node metastases compared to placebo.

HRT, especially estrogen-progestagen combined treatment, increases the density of mammographic images which may adversely affect the radiological detection of breast cancer.

Ovarian cancer

Long-term (at least 5 to 10 years) use of estrogen-only HRT products in hysterectomised women has been associated with an increased risk of ovarian cancer in some epidemiological studies. It is uncertain whether long-term use of combined HRT confers a different risk than estrogen-only products.

Venous thromboembolism

• HRT is associated with a higher risk of developing venous thromboembolism (VTE) i.e. deep vein thrombosis or pulmonary embolism. One randomised controlled trial and epidemiological studies found a 2-3 fold higher risk for users compared with non-users. For non-users, it is estimated that the number of cases of VTE that will occur over a 5 year period is about 3 per 1000 women aged 50-59 years and 8 per 1000 women aged between 60-69 years. It is estimated that in healthy women who use HRT for 5 years, the number of additional cases of VTE over a 5 year period will be between 2 and 6 (best estimate = 4) per 1000 women aged 50-59 years and between 5 and 15 (best estimate = 9) per 1000 women aged 60-69 years. The occurrence of such an event is more likely in the first year of HRT use than later.

• Generally recognised risk factors for VTE include a personal or family history, severe obesity (Body Mass Index >30 kg/m²) and systemic lupus erythematosus (SLE). There is no consensus about the possible role of varicose veins in VTE.

• Patients with a history of VTE or known thrombophilic states have an increased risk of VTE. HRT may add to this risk. Personal or strong family history of thromboembolism or recurrent spontaneous abortion should be investigated in order to exclude a thrombophilic predisposition. Until a thorough evaluation of thrombophilic factors has been made or anticoagulant treatment initiated, use of HRT in such patients should be viewed as contraindicated. Those women already on anticoagulant treatment require careful consideration of the benefit-risk of use of HRT.

• The risk of VTE may be temporarily increased with prolonged immobilisation, major trauma or major surgery. As in all postoperative patients, scrupulous attention should be given to prophylactic measures to prevent VTE following surgery. Where prolonged immobilisation is liable to follow elective surgery, particularly abdominal or orthopaedic surgery to the lower limbs, consideration should be given to temporarily stopping HRT 4 to 6 weeks earlier if possible. Treatment should not be restarted until the woman is completely mobilised.

• If VTE develops after initiating therapy the drug should be discontinued. Patients should be told to contact their doctors immediately when they are aware of a potential thromboembolic symptom (eg, painful swelling of a leg, sudden pain in the chest, dyspnea).

Coronary artery disease (CAD)

There is no evidence from randomised controlled trials of cardiovascular benefit with continuous combined conjugated estrogens and medroxyprogesterone acetate (MPA). Two large clinical trials (WHI and HERS i.e. Heart and Estrogen/progestin Replacement Study) showed a possible increased risk of cardiovascular morbidity in the first year of use and no overall benefit. For other HRT products there are only limited data from randomised controlled trials examining effects in cardiovascular morbidity or mortality. Therefore, it is uncertain whether these findings also extend to other HRT products.

Stroke

One large randomised clinical trial (WHI-trial) found, as a secondary outcome, an increased risk of ischaemic stroke in healthy women during treatment with continuous combined conjugated estrogens and MPA. For women who do not use HRT, it is estimated that the number of cases of stroke that will occur over a 5 year period is about 3 per 1000 women aged 50-59 years and 11 per 1000 women aged 60-69 years. It is estimated that for women who use conjugated estrogens and MPA for 5 years, the number of additional cases will be between 0 and 3 (best estimate = 1) per 1000 users aged 50-59 years and between 1 and 9 (best estimate = 4) per 1000 users aged 60-69 years. It is unknown whether the increased risk also extends to other HRT products.

Other conditions

• Estrogens may cause fluid retention, and therefore patients with cardiac or renal dysfunction should be carefully observed. Patients with terminal renal insufficiency should be closely observed, since it is expected that the level of the circulating active ingredient in Estradiol implants is increased.

• Women with pre-existing hypertriglyceridemia should be followed closely during estrogen replacement or hormone replacement therapy, since rare cases of large increases of plasma triglycerides leading to pancreatitis have been reported with estrogen therapy in this condition.

• Estrogens increase thyroid binding globulin (TBG), leading to increased circulating total thyroid hormone, as measured by protein-bound iodine (PBI), T4 levels (by column or by radio-immunoassay) or T3 levels (by radio-immunoassay). T3 resin uptake is decreased, reflecting the elevated TBG. Free T4 and free T3 concentrations are unaltered. Other binding proteins may be elevated in serum, i.e. corticoid binding globulin (CBG), sex-hormone-binding globulin (SHBG) leading to increased circulating corticosteroids and sex steroids, respectively. Free or biological active hormone concentrations are unchanged. Other plasma proteins may be increased (angiotensinogen/renin substrate, alpha-I-antitrypsin, ceruloplasmin).

• There is no conclusive evidence for improvement of cognitive function. There is some evidence from the WHI trial of increased risk of probable dementia in women who start using continuous combined CEE and MPA after the age of 65. It is unknown whether the findings apply to younger post-menopausal women or other HRT products.

4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction

The metabolism of estrogens may be increased by concomitant use of substances known to induce drug-metabolising enzymes, specifically cytochrome P450 enzymes, such as anticonvulsants (e.g. phenobarbital, phenytoin, carbamezapine) and anti-infectives (e.g. rifampicin, rifabutin, nevirapine, efavirenz). Ritonavir and nelfinavir, although known as strong inhibitors, by contrast exhibit inducing properties when used concomitantly with steroid hormones. Herbal preparations containing St John's wort (Hypericum Perforatum) may induce the metabolism of estrogens.

Since Estradiol implants are administered parentally, the first-pass effect in the liver is avoided and, thus, parentally administered estrogens might be less affected than oral hormones by enzyme inducers.

Clinically, an increased metabolism of estrogens and progestagens may lead to decreased effect and changes in the uterine bleeding profile.

4.6 Pregnancy And Lactation

Estradiol implants are not indicated during pregnancy. If pregnancy occurs during medication with Estradiol implants treatment should be withdrawn immediately. The results of most epidemiological studies to date relevant to inadvertent foetal exposure to estrogens indicate no teratogenic or foetotoxic effects.

Estradiol implants are not indicated during lactation.

4.7 Effects On Ability To Drive And Use Machines

As far as known Estradiol implants have no effect on alertness or concentration.

4.8 Undesirable Effects

The following adverse reactions have been associated with estrogen therapy in general.

Genito-urinary tract:

Intermenstrual bleeding, increase in the size of the uterine fibromyomata, endometrial proliferation, excessive production of cervical mucus, aggravation of endometriosis, pre-menstrual like syndrome.

Endometrial cancer

In women with an intact uterus, the risk of endometrial hyperplasia and endometrial cancer increases with increasing duration of use of unopposed estrogens. According to data from epidemiological studies, the best estimate of the risk is that for women not using HRT, about 5 in every 1000 are expected to have endometrial cancer diagnosed between the ages of 50 and 65. Depending on the duration of treatment and estrogen dose, the reported increase in endometrial cancer risk among unopposed estrogen users varies from 2- to 12-fold greater compared with non-users. Adding a progestagen to estrogen-only therapy greatly reduces this increased risk.

Breast:

Tenderness, pain, enlargement, secretion.

Breast cancer

According to evidence from a large number of epidemiological studies and one randomised placebo-controlled trial, the Women's Health Initiative (WHI), the overall risk of breast cancer increases with increasing duration of HRT use in current or recent HRT users.

For estrogen-only HRT, estimates of relative risk (RR) from a reanalysis of original data from 51 epidemiological studies (in which >80% of HRT use was estrogen-only HRT) and from the epidemiological Million Women Study (MWS) are similar at 1.35 (95%CI 1.21 – 1.49) and 1.30 (95%CI 1.21 – 1.40), respectively.

For estrogen plus progestagen combined HRT, several epidemiological studies have reported an overall higher risk for breast cancer than with estrogens alone.

The MWS reported that, compared to never users, the use of various types of estrogen-progestagen combined HRT was associated with a higher risk of breast cancer (RR = 2.00, 95%CI: 1.88 – 2.12) than use of estrogens alone (RR = 1.30, 95%CI: 1.21 – 1.40) or use of tibolone (RR=1.45; 95%CI 1.25-1.68).

The WHI trial reported a risk estimate of 1.24 (95%CI 1.01 – 1.54) after 5.6 years of use of estrogen-progestagen combined HRT (CEE + MPA) in all users compared with placebo.

The absolute risks calculated from the MWS and the WHI trial are presented below:

The MWS has estimated, from the known average incidence of breast cancer in developed countries, that:

Ø For women not using HRT, about 32 in every 1000 are expected to have breast cancer diagnosed between the ages of 50 and 64 years.

Ø For 1000 current or recent users of HRT, the number of additional cases during the corresponding period will be

Ø For users of estrogen-only replacement therapy

• between 0 and 3 (best estimate = 1.5) for 5 years' use

• between 3 and 7 (best estimate = 5) for 10 years' use.

Ø For users of estrogen plus progestagen combined HRT,

• between 5 and 7 (best estimate = 6) for 5 years' use

• between 18 and 20 (best estimate = 19) for 10 years' use.

The WHI trial estimated that after 5.6 years of follow-up of women between the ages of 50 and 79 years, an additional 8 cases of invasive breast cancer would be due to estrogen-progestagen combined HRT (CEE + MPA) per 10,000 women years.

According to calculations from the trial data, it is estimated that:

Ø For 1000 women in the placebo group,

• about 16 cases of invasive breast cancer would be diagnosed in 5 years.

Ø For 1000 women who used estrogen + progestagen combined HRT (CEE + MPA), the number of additional cases would be

• between 0 and 9 (best estimate = 4) for 5 years' use.

The number of additional cases of breast cancer in women who use HRT is broadly similar for women who start HRT irrespective of age at start of use (between the ages of 45-65) (see section 4.4).

Gastro-intestinal tract:

Nausea, vomiting, cholelithiasis, cholestatic jaundice, gall bladder disease.Changes in liver function.

Cardiovascular system:

Venous thromboembolism, i.e. deep leg or pelvic venous thrombosis and pulmonary embolism, is more frequent among hormone replacement therapy users than among non-users. For further information, see section 4.3 Contraindications and 4.4 Special warnings and precautions for use.

Myocardial infarction and stroke, thrombosis, rise of blood pressure.

Skin and subcutaneous disorders:

Chloasma, erythema nodosum, erythema multiforme, vascular purpura, rash.

Eyes:

Discomfort of the cornea if contact lenses are used.

CNS:

Headache, migraine, mood changes. Probable dementia (see section 4.4).

Metabolic:

Sodium and water retention, reduced glucose tolerance, and change in body weight.

High dosages and/or prolonged use of estrogens may cause psychotic disturbances.

Prolonged exposure to estrogens may increase risk of development of cardiac and renal disease, estrogen-dependant neoplasms benign and malignant, e.g. melanoma, otosclerosis, multiple sclerosis and systemic lupus erythematosus.

4.9 Overdose

Acute overdose with Estradiol implants is not known to occur.

With chronic use supraphysiological levels of estradiol can be found, however these do not generally result in adverse symptoms, signs or metabolic effects. None the less it would seem prudent in the circumstances to withhold further implantation or other administration of exogenous estrogens until estradiol levels have fallen to within the pre-menopausal physiological range.

5. Pharmacological Properties

5.1 Pharmacodynamic Properties

Estradiol/Estradiol valerate: The active ingredient, synthetic 17-estradiol is chemically and biologically identical to endogenous human estradiol. It substitutes for the loss of estrogen production in menopausal women, and alleviates menopausal symptoms. Estrogens prevent bone loss following menopause or ovariectomy.

Clinical Trial Information

• Relief of estrogen-deficiency symtoms and bleeding patterns

Relief of menopausal symptoms was achieved usually during the first week of treatment.

• Prevention of osteoporosis

- Estrogen deficiency at menopause is associated with an increasing bone turnover and decline in bone mass. The effect of estrogens on bone mineral density is dose-dependent. Protection appears to be effective for as long as treatment is continued. After discontinuation of HRT, bone mass is lost at a rate similar to that in untreated women.

- Evidence from the WHI trial and meta-analysed trials shows that current use of HRT, alone or in combination with a progestagen – given to predominantly healthy women – reduces the risk of hip, vertebral, and other osteoporotic fractures. HRT may also prevent fractures in women with low bone density and/or established osteoporosis, but the evidence for that is limited.

- Studies have reported significant increases in bone mineral density at spine and hip after treatment with Estradiol implants (25-100 mg every 6 months) for 1 to 15.5 years.

5.2 Pharmacokinetic Properties

After insertion of an Estradiol implant 100mg, into the subcutaneous fat the estradiol plasma level reaches its maximum of about 550 pmol/l in a few weeks and shows a slow and gradual decline to about 300 pmol/l at 6 months. As with other estrogens, there are large interindividual differences in estradiol levels, but intraindividual variability appears to be small. Unlike oral estrogen therapy, subcutaneous administration bypasses the gastrointestinal tract, where estradiol is converted to estrone and avoids the first-pass effect of the liver. Therefore more unconjugated estradiol is observed and the liver is less burdened.

The transport, metabolism, and excretion of estradiol released from the implants are comparable to those of endogenous estradiol. Thus, about 38 per cent of circulatory estradiol will be bound to SHBG, 60 per cent is bound to albumin, and only 2-3 per cent is free. The main metabolic end products are estriol and 2-hydroxyestrone, which are synthesised after conversion of estradiol to estrone. Most of the estradiol is excreted by the kidneys, mainly after conjugation with glucuronic and sulphuric acid. There is a significant enterohepatic circulation of estradiol and its metabolites. Most of the conjugated biliary estrogens undergo hydrolysis in the intestines after which they are reabsorbed. Therefore, only a small part of the administered estradiol will ultimately be lost in the faeces.

After long-term treatment, accumulation may occur (with doses of 50 mg or more, especially when reimplantation is performed after periods of less than 6 months), but in most cases there is only a moderate increase and levels remain well within the normal premenopausal range. However, in rare cases (mainly with implantation intervals of only 3 or 4 months) plasma levels may rise above 1750 pmol/l. There are some indications that supraphysiological levels occur most frequently in women with a history of depression or surgical castration.

5.3 Preclinical Safety Data

There are no preclinical data of relevance to the prescriber which are additional to that included in other sections of the SPC.

6. Pharmaceutical Particulars

6.1 List Of Excipients

Estradiol implants contain no auxiliary ingredients.

6.2 Incompatibilities

None known.

6.3 Shelf Life

5 years.

6.4 Special Precautions For Storage

Do not store above 25°C. Store in the original package.

6.5 Nature And Contents Of Container

Each sterile implant is supplied singly, in a sealed glass tube.

6.6 Special Precautions For Disposal And Other Handling

Full aseptic 'no-touch' technique should be used.

Administrative Data

7. Marketing Authorisation Holder

Organon Laboratories Limited, Cambridge Science Park, Milton Road, Cambridge, CB4 0FL, U.K.

8. Marketing Authorisation Number(S)

0065/5076R

9. Date Of First Authorisation/Renewal Of The Authorisation

31/8/87 Renewed 06/07/1995

10. Date Of Revision Of The Text

May 2005

Ref: US06ESTRADIOL100v1.1

tolterodine

tol-TER-oh-deen TAR-trate

Commonly used brand name(s)

In the U.S.

• Detrol


• Detrol LA

Available Dosage Forms:

• Capsule, Extended Release


• Tablet

Therapeutic Class: Urinary Antispasmodic

Pharmacologic Class: Tolterodine

Uses For tolterodine

Tolterodine is used to treat symptoms of an overactive bladder, such as incontinence (loss of bladder control) or a frequent need to urinate.

Tolterodine belongs to the group of medicines called antispasmodics. It helps decrease muscle spasms of the bladder and the frequent urge to urinate caused by these spasms.

tolterodine is available only with your doctor's prescription.

Before Using tolterodine

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For tolterodine, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to tolterodine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Appropriate studies performed to date have not demonstrated that tolterodine is useful in children.

Geriatric

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of tolterodine in the elderly. However, elderly patients are more likely to have age-related kidney or liver problems, which may require an adjustment in the dose for patients receiving tolterodine.

Pregnancy

	Pregnancy Category	Explanation
All Trimesters	C	Animal studies have shown an adverse effect and there are no adequate studies in pregnant women OR no animal studies have been conducted and there are no adequate studies in pregnant women.

Breast Feeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking tolterodine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using tolterodine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.

• Potassium

Using tolterodine with any of the following medicines may cause an increased risk of certain side effects, but using both drugs may be the best treatment for you. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

• Amiodarone


• Clarithromycin


• Cyclosporine


• Donepezil


• Erythromycin


• Galantamine


• Itraconazole


• Ketoconazole


• Miconazole


• Propafenone


• Quinidine


• Rivastigmine


• Vinblastine


• Warfarin

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other Medical Problems

The presence of other medical problems may affect the use of tolterodine. Make sure you tell your doctor if you have any other medical problems, especially:

• Heart rhythm problems (e.g., QT prolongation), or history of or


• Intestinal or stomach problems (e.g., blockage, intestinal atony, pyloric stenosis) or


• Myasthenia gravis (severe muscle weakness) or


• Narrow-angle glaucoma, controlled or


• Urinary problems (e.g., blockage)—Use with caution. May make these conditions worse.

• Kidney disease or


• Liver disease (including cirrhosis)—Use with caution. The effects may be increased because of slower removal of the medicine from the body.

• Liver disease, severe—Use is not recommended for patients taking tolterodine extended-release capsules.

• Narrow-angle glaucoma, uncontrolled or


• Stomach problems (e.g., gastric retention) or


• Urinary retention (hard to pass urine)—Should not be used in patients with these conditions.

Proper Use of tolterodine

Take tolterodine only as directed. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered. To do so may increase the chance of side effects. Also, do not change your dose without checking first with your doctor.

tolterodine comes with a patient information insert. It is very important that you read and understand this information. Be sure to ask your doctor about anything you do not understand.

You may take tolterodine with or without food.

Swallow the extended-release capsule whole with water. Do not crush, open, or chew it.

Take tolterodine at the same time each day.

Dosing

The dose of tolterodine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of tolterodine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For bladder problems:
  
  • For oral dosage form (tablets):
    
    • Adults—At first, 2 milligrams (mg) two times a day. Your doctor may adjust your dose if needed.
    
    
    • Children—Use and dose must be determined by your doctor.
    
    
  
  
  • For oral dosage form (extended-release capsules):
    
    • Adults—4 milligrams (mg) once a day. Your doctor may adjust your dose if needed.
    
    
    • Children—Use and dose must be determined by your doctor.
    
    
  
  

Missed Dose

If you miss a dose of tolterodine, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Precautions While Using tolterodine

It is very important that your doctor check your progress at regular visits. This will allow your doctor to see if the medicine is working properly and to decide if you should continue to take it.

Tolterodine may cause serious types of allergic reactions, including anaphylaxis and angioedema. Anaphylaxis and angioedema can be life-threatening and require immediate medical attention. Stop using tolterodine and call your doctor right away if you have a rash; itching; hoarseness; lightheadedness, dizziness, or fainting; trouble breathing; trouble swallowing; or any swelling of your hands, face, mouth, or throat after using tolterodine.

tolterodine may cause some people to become dizzy, drowsy, or have blurred vision. Make sure you know how you react to tolterodine before you drive, use machines, or do anything else that could be dangerous if you are dizzy, not alert, or not able to see well.

tolterodine may cause dryness in the mouth, nose, and throat. For temporary relief of mouth dryness, use sugarless candy or gum, melt bits of ice in your mouth, or use a saliva substitute. However, if your mouth continues to feel dry for more than 2 weeks, check with your medical doctor or dentist. Continuing dryness of the mouth may increase the chance of dental disease, including tooth decay, gum disease, and fungus infections.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements.

tolterodine Side Effects

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

More common

• Abnormal vision, including difficulty with adjusting to distances


• bloody or cloudy urine


• difficult, burning, or painful urination


• frequent urge to urinate

Less common

• Chest pain


• chills


• cough


• diarrhea


• fever


• general feeling of discomfort or illness


• headache


• joint pain


• loss of appetite


• muscle aches and pains


• nausea


• pain or tenderness around the eyes and cheekbones


• shivering


• shortness of breath or troubled breathing


• sore throat


• stuffy or runny nose


• sweating


• tightness of the chest or wheezing


• trouble with sleeping


• vomiting

Incidence not known

• Being forgetful


• bloating or swelling of the face, arms, hands, ankles, lower legs, or feet


• confusion about identity, place, and time


• difficulty with swallowing


• dizziness


• fast, pounding, or irregular heartbeat or pulse


• hives


• itching


• large, hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or sex organs


• mood or mental changes


• puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue


• rapid weight gain


• seeing, hearing, or feeling things that are not there


• skin rash


• tingling of the hands or feet


• unusual tiredness or weakness


• unusual weight gain or loss

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

• Abdominal or stomach pain


• constipation


• drowsiness


• dry eyes


• dry mouth


• upset stomach

Less common

• Acid or sour stomach


• belching


• blurred vision


• difficulty with moving


• dizziness or lightheadedness


• dry skin


• fear or nervousness


• feeling of constant movement of self or surroundings


• heartburn


• indigestion


• sensation of spinning


• sleepiness or unusual drowsiness


• stomach discomfort


• weight gain

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

See also: tolterodine side effects (in more detail)

The information contained in the Thomson Reuters Micromedex products as delivered by Drugs.com is intended as an educational aid only. It is not intended as medical advice for individual conditions or treatment. It is not a substitute for a medical exam, nor does it replace the need for services provided by medical professionals. Talk to your doctor, nurse or pharmacist before taking any prescription or over the counter drugs (including any herbal medicines or supplements) or following any treatment or regimen. Only your doctor, nurse, or pharmacist can provide you with advice on what is safe and effective for you.

The use of the Thomson Reuters Healthcare products is at your sole risk. These products are provided "AS IS" and "as available" for use, without warranties of any kind, either express or implied. Thomson Reuters Healthcare and Drugs.com make no representation or warranty as to the accuracy, reliability, timeliness, usefulness or completeness of any of the information contained in the products. Additionally, THOMSON REUTERS HEALTHCARE MAKES NO REPRESENTATION OR WARRANTIES AS TO THE OPINIONS OR OTHER SERVICE OR DATA YOU MAY ACCESS, DOWNLOAD OR USE AS A RESULT OF USE OF THE THOMSON REUTERS HEALTHCARE PRODUCTS. ALL IMPLIED WARRANTIES OF MERCHANTABILITY AND FITNESS FOR A PARTICULAR PURPOSE OR USE ARE HEREBY EXCLUDED. Thomson Reuters Healthcare does not assume any responsibility or risk for your use of the Thomson Reuters Healthcare products.

More tolterodine resources

• Tolterodine Side Effects (in more detail)
• Tolterodine Use in Pregnancy & Breastfeeding
• Tolterodine Drug Interactions
• Tolterodine Support Group
• 19 Reviews for Tolterodine - Add your own review/rating

• Tolterodine MedFacts Consumer Leaflet (Wolters Kluwer)


• Detrol Prescribing Information (FDA)


• Detrol Monograph (AHFS DI)


• Detrol Consumer Overview


• Detrol LA Prescribing Information (FDA)


• Detrol LA Extended-Release Capsules MedFacts Consumer Leaflet (Wolters Kluwer)

Compare tolterodine with other medications

• Overactive Bladder
• Urinary Incontinence

Acyclovir IV Infusion

DESCRIPTION

Acyclovir is an antiviral drug active against herpes viruses. Acyclovir Injection is a formulation for intravenous administration. Acyclovir Injection is a sterile solution containing acyclovir 25 mg/mL. Acyclovir Injection is available in 20 mL and 40 mL vials, with each mL containing acyclovir sodium equivalent to 25 mg acyclovir. The pH has been adjusted with sodium hydroxide and if necessary, hydrochloric acid to fall in the range of 10.7 to 11.7. Dilution in any appropriate intravenous solution must be performed before infusion (see DOSAGE AND ADMINISTRATION: Method of Preparation and Administration). Each 20 mL vial contains 500 mg of acyclovir and 49 mg of sodium, and each 40 mL vial contains 1000 mg acyclovir and 98 mg of sodium.

The chemical name of acyclovir is 9-[(2-Hydroxyethoxy)methyl]guanine sodium. The molecular formula of acyclovir is C8H10N5O3 Na and it has the following structural formula:

Acyclovir sodium is a white, crystalline powder with a molecular weight of 247.19, and solubility in water at 25°C exceeding 100 mg/mL. At physiologic pH, acyclovir exists as the un-ionized form with a molecular weight of 225.21 and a maximum solubility of 2.5 mg/mL in water at 37°C. The pka’s of acyclovir are 2.27 and 9.25.

VIROLOGY

Mechanism of Antiviral Action

Acyclovir is a synthetic purine nucleoside analogue with in vitro and in vivo inhibitory activity against herpes simplex virus types 1 (HSV-1), 2 (HSV-2), and varicella-zoster virus (VZV).

The inhibitory activity of acyclovir is highly selective due to its affinity for the enzyme thymidine kinase (TK) encoded by HSV and VZV. This viral enzyme converts acyclovir into acyclovir monophosphate, a nucleotide analogue. The monophosphate is further converted into diphosphate by cellular guanylate kinase and into triphosphate by a number of cellular enzymes. In vitro, acyclovir triphosphate stops replication of herpes viral DNA. This is accomplished in three ways: 1) competitive inhibition of viral DNA polymerase, 2) incorporation into and termination of the growing viral DNA chain, and 3) inactivation of the viral DNA polymerase. The greater antiviral activity of acyclovir against HSV compared to VZV is due to its more efficient phosphorylation by the viral TK.

Antiviral Activities

The quantitative relationship between the in vitro susceptibility of herpes viruses to antivirals and the clinical response to therapy has not been established in humans, and virus-sensitivity testing has not been standardized. Sensitivity testing results, expressed as the concentration of drug required to inhibit by 50% the growth of virus in cell culture (IC50) vary greatly depending upon a number of factors.

Using plaque-reduction assays, the IC50 against herpes simplex virus isolates ranges from 0.02 to 13.5 mcg/mL for HSV-1 and from 0.01 to 9.9 mcg/mL for HSV-2. The IC50 for acyclovir against most laboratory strains and clinical isolates of VZV ranges from 0.12 to 10.8 mcg/mL. Acyclovir also demonstrates activity against the Oka vaccine strain of VZV with a mean IC50 of 1.35 mcg/mL.

Drug Resistance

Resistance of HSV and VZV to acyclovir can result from qualitative and quantitative changes in the viral TK and/or DNA polymerase. Clinical isolates of HSV and VZV with reduced susceptibility to acyclovir have been recovered from immunocompromised patients, especially with advanced HIV infection. While most of the acyclovir-resistant mutants isolated thus far from such patients have been found to be TK-deficient mutants, other mutants involving the viral TK gene (TK partial and TK altered) and DNA polymerase have been isolated. TK-negative mutants may cause severe disease in infants and immunocompromised adults. The possibility of viral resistance to acyclovir should be considered in patients who show poor clinical response during therapy.

CLINICAL PHARMACOLOGY

Pharmacokinetics

The pharmacokinetics of acyclovir after intravenous administration have been evaluated in adult patients with normal renal function during Phase 1/2 studies after single doses ranging from 0.5 to 15 mg/kg and after multiple doses ranging from 2.5 to 15 mg/kg every 8 hours. Proportionality between dose and plasma levels is seen after single doses or at steady state after multiple dosing. Average steady-state peak and trough concentrations from 1-hour infusions administered every 8 hours are given in Table 1.

Table 1: Acyclovir  Peak and Trough Concentrations at Steady State

Dosage Regimen	CSS max	CSS trough
5 mg/kg q 8 hr (n = 8)	9.8 mcg/ml range: 5.5 to 13.8	0.7 mcg/ml range: 0.2 to 1.0
10 mg/kg q 8 hr (n = 7)	22.9 mcg/ml range: 14.1 to 44.1	1.9 mcg/ml range: 0.5 to 2.9

Concentrations achieved in the cerebrospinal fluid are approximately 50% of plasma values. Plasma protein binding is relatively low (9% to 33%) and drug interactions involving binding site displacement are not anticipated.

Renal excretion of unchanged drug is the major route of acyclovir elimination accounting for 62% to 91% of the dose.

The only major urinary metabolite detected is 9-carboxymethoxymethylguanine accounting for up to 14.1% of the dose in patients with normal renal function.

The half-life and total body clearance of acyclovir are dependent on renal function as shown in Table 2.

Table 2: Acyclovir Half-life and Total Body Clearance

Creatine Clearance (mL/min/1.73 m2)	Half-Life (h)	Total Body Clearance
		(mL/min/1.73 m2)	(mL/min/mg)
>80	2.5	327	5.1
50 - 80	3.0	248	3.9
15 - 50	3.5	190	3.4
0 (Anuric)	19.5	29	0.5

Special Populations

Adults With Impaired Renal Function

Acyclovir was administered at a dose of 2.5 mg/kg to 6 adult patients with severe renal failure. The peak and trough plasma levels during the 47 hours preceding hemodialysis were 8.5 mcg/mL and 0.7 mcg/mL, respectively.

Consult DOSAGE AND ADMINISTRATION section for recommended adjustments in dosing based upon creatinine clearance.

Pediatrics

Acyclovir pharmacokinetics were determined in 16 pediatric patients with normal renal function ranging in age from 3 months to 16 years at doses of approximately 10 mg/kg and 20 mg/kg every 8 hours (Table 3). Concentrations achieved at these regimens are similar to those in adults receiving 5 mg/kg and 10 mg/kg every 8 hours, respectively (Table 1). Acyclovir pharmacokinetics were determined in 12 patients ranging in age from birth to 3 months at doses of 5 mg/kg, 10 mg/kg, and 15 mg/kg every 8 hours (Table 3).

Table 3: Acyclovir Pharmacokinetics in Pediatric Patients (Mean ± SD)

Parameter	Birth to 3 Months of Age (n = 12)	3 Months to 12 Months of Age (n = 16)
CL (mL/min/kg)	4.46 ± 1.61	8.44 ± 2.92
VDSS (L/kg)	1.08 ± 0.35	1.01 ± 0.28
Elimination Half-life (h)	3.80 ± 1.19	2.36 ± 0.97

Geriatrics

Acyclovir plasma concentrations are higher in geriatric patients compared to younger adults, in part due to age-related changes in renal function. Dosage reduction may be required in geriatric patients with underlying renal impairment (see PRECAUTIONS: Geriatric Use).

Drug Interactions

Coadministration of probenecid with acyclovir has been shown to increase the mean acyclovir half life and the area under the concentration-time curve. Urinary excretion and renal clearance were correspondingly reduced.

Clinical Trials

Herpes Simplex Infections in Immunocompromised Patients

A multicenter trial of acyclovir injection at a dose of 250 mg/m2 every 8 hours (750 mg/m2/day) for 7 days was conducted in 98 immunocompromised patients (73 adults and 25 children) with orofacial, esophageal, genital, and other localized infections (52 treated with acyclovir and 46 with placebo). Acyclovir decreased virus excretion, reduced pain, and promoted healing of lesions.

Initial Episodes of Herpes Genitalis

In placebo-controlled trials, 58 patients with initial genital herpes were treated with intravenous acyclovir 5 mg/kg or placebo (27 patients treated with acyclovir and 31 treated with placebo) every 8 hours for 5 days. Acyclovir decreased the duration of viral excretion, new lesion formation, and duration of vesicles, and promoted healing of lesions.

Herpes Simplex Encephalitis

Sixty-two patients ages 6 months to 79 years with brain biopsy-proven herpes simplex encephalitis were randomized to receive either acyclovir (10 mg/kg every 8 hours) or vidarabine (15 mg/kg/day) for 10 days (28 were treated with acyclovir and 34 with vidarabine). Overall mortality at 12 months for patients treated with acyclovir was 25% compared to 59% for patients treated with vidarabine. The proportion of patients treated with acyclovir functioning normally or with only mild sequelae (e.g., decreased attention span) was 32% compared to 12% of patients treated with vidarabine.

Patients less than 30 years of age and those who had the least severe neurologic involvement at time of entry into study had the best outcome with treatment with acyclovir. An additional controlled study performed in Europe demonstrated similar findings.

Neonatal Herpes Simplex Virus Infection

Two hundred and two infants with neonatal herpes simplex infections were randomized to receive either acyclovir 10 mg/kg every 8 hours (n = 107) or vidarabine 30 mg/kg/day (n = 95) for 10 days. Outcomes are presented in Table 4.

Table 4: Mortality at 1 Year

HSV Disease Classification	Treatment Group
*SEM refers to localized infection with disease limited to skin, eye, and/or mouth.
+CNS refers to infection of the central nervous system with compatible neurologic and CSF findings.
++DISS refers to visceral organ involvement such as hepatitis or pneumonitis with or without CNS involvement.
	Acyclovir (n = 107)	Vidarabine (n = 95)
SEM* (n = 85)	0/54	0/31
CNS+ (n = 71)	5/35	5/36
DISS++ (n = 46)	11/18	14/28

Rates of neurologic sequelae at 1 year were comparable between the treatment groups.

Varicella-Zoster Infections in Immunocompromised Patients

A multicenter trial of acyclovir injection at a dose of 500 mg/m2 every 8 hours for 7 days was conducted in immunocompromised patients with zoster infections (shingles). Ninety-four (94) patients were evaluated (52 patients were treated with acyclovir and 42 with placebo). Acyclovir was superior to placebo as measured by reductions in cutaneous dissemination and visceral dissemination.

INDICATIONS AND USAGE

Herpes Simplex Infections in lmmunocompromised Patients

Acyclovir Injection is indicated for the treatment of initial and recurrent mucosal and cutaneous herpes simplex (HSV-1 and HSV-2) in immunocompromised patients.

Initial Episodes of Herpes Genitalis

Acyclovir Injection is indicated for the treatment of severe initial clinical episodes of herpes genitalis in immunocompetent patients.

Herpes Simplex Encephalitis

Acyclovir Injection is indicated for the treatment of herpes simplex encephalitis.

Neonatal Herpes Simplex Virus Infection

Acyclovir Injection is indicated for the treatment of neonatal herpes infections.

Varicella-Zoster Infections in lmmunocompromised Patients

Acyclovir Injection is indicated for the treatment of varicella-zoster (shingles) infections in immunocompromised patients.

CONTRAINDICATIONS

Acyclovir Injection is contraindicated for patients who develop hypersensitivity to acyclovir or valacyclovir.

WARNINGS

Acyclovir Injection is intended for intravenous infusion only, and should not be administered topically, intramuscularly, orally, subcutaneously, or in the eye. Intravenous infusions must be given over a period of at least 1 hour to reduce the risk of renal tubular damage (see PRECAUTIONS and DOSAGE AND ADMINISTRATION).

Renal failure, in some cases resulting in death, has been observed with acyclovir therapy (see ADVERSE REACTIONS: Observed During Clinical Practice and OVERDOSAGE).

Thrombotic thrombocytopenic purpura/hemolytic uremic syndrome (TTP/HUS), which has resulted in death, has occurred in immunocompromised patients receiving acyclovir therapy.

PRECAUTIONS

General

Precipitation of acyclovir crystals in renal tubules can occur if the maximum solubility of free acyclovir (2.5 mg/mL at 37°C in water) is exceeded or if the drug is administered by bolus injection. Ensuing renal tubular damage can produce acute renal failure.

Abnormal renal function (decreased creatinine clearance) can occur as a result of acyclovir administration and depends on the state of the patient’s hydration, other treatments, and the rate of drug administration. Concomitant use of other nephrotoxic drugs, pre-existing renal disease, and dehydration make further renal impairment with acyclovir more likely. Administration of acyclovir by intravenous infusion must be accompanied by adequate hydration.

When dosage adjustments are required, they should be based on estimated creatinine clearance (see DOSAGE AND ADMINISTRATION).

Approximately 1% of patients receiving intravenous acyclovir have manifested encephalopathic changes characterized by either lethargy, obtundation, tremors, confusion, hallucinations, agitation, seizures, or coma. Acyclovir should be used with caution in those patients who have underlying neurologic abnormalities and those with serious renal, hepatic, or electrolyte abnormalities, or significant hypoxia.

Drug Interactions

See CLINICAL PHARMACOLOGY: Pharmacokinetics.

Carcinogenesis, Mutagenesis, Impairment of Fertility

The data presented below include references to peak steady-state plasma acyclovir concentrations observed in humans treated with 30 mg/kg/day (10 mg/kg every 8 hours, dosing appropriate for treatment of herpes zoster or herpes encephalitis), or 15 mg/kg/day (5 mg/kg every 8 hours, dosing appropriate for treatment of primary genital herpes or herpes simplex infections in immunocompromised patients). Plasma drug concentrations in animal studies are expressed as multiples of human exposure to acyclovir at the higher and lower dosing schedules (see CLINICAL PHARMACOLOGY: Pharmacokinetics).

Acyclovir was tested in lifetime bioassays in rats and mice at single daily doses of up to 450 mg/kg administered by gavage. There was no statistically significant difference in the incidence of tumors between treated and control animals, nor did acyclovir shorten the latency of tumors. At 450 mg/kg/day, plasma concentrations in both the mouse and rat bioassay were lower than concentrations in humans.

Acyclovir was tested in 16 in vitro and in vivo genetic toxicity assays. Acyclovir was positive in 5 of the assays. Acyclovir did not impair fertility or reproduction in mice (450 mg/kg/day, PO) or in rats (25 mg/kg/day, SC). In the mouse study, plasma levels were the same as human levels, while in the rat study, they were 1 to 2 times human levels. At higher doses (50 mg/kg/day, SC) in rats and rabbits (1 to 2 and 1 to 3 times human levels, respectively) implantation efficacy, but not litter size, was decreased. In a rat peri- and post-natal study at 50 mg/kg/day, SC, there was a statistically significant decrease in group mean numbers of corpora lutea, total implantation sites, and live fetuses.

No testicular abnormalities were seen in dogs given 50 mg/kg/day, IV for 1 month (1 to 3 times human levels) or in dogs given 60 mg/kg/day orally for 1 year (the same as human levels). Testicular atrophy and aspermatogenesis were observed in rats and dogs at higher dose levels.

Pregnancy

Teratogenic Effects

Pregnancy Category B

Acyclovir administered during organogenesis was not teratogenic in the mouse (450 mg/kg/day, PO), rabbit (50 mg/kg/day, SC and IV), or rat (50 mg/kg/day, SC).

These exposures resulted in plasma levels the same as, 4 and 9, and 1 and 2 times, respectively, human levels. There are no adequate and well-controlled studies in pregnant women. A prospective epidemiologic registry of acyclovir use during pregnancy was established in 1984 and completed in April 1999. There were 749 pregnancies followed in women exposed to systemic acyclovir during the first trimester of pregnancy resulting in 756 outcomes. The occurrence rate of birth defects approximates that found in the general population. However, the small size of the registry is insufficient to evaluate the risk for less common defects or to permit reliable or definitive conclusions regarding the safety of acyclovir in pregnant women and their developing fetuses. Acyclovir should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Nursing Mothers

Acyclovir concentrations have been documented in breast milk in 2 women following oral administration of acyclovir and ranged from 0.6 to 4.1 times corresponding plasma levels. These concentrations would potentially expose the nursing infant to a dose of acyclovir up to 0.3 mg/kg/day. Acyclovir should be administered to a nursing mother with caution and only when indicated.

Pediatric Use

See DOSAGE AND ADMINISTRATION.

Geriatric Use

Clinical studies of acyclovir did not include sufficient numbers of patients aged 65 and over to determine whether they respond differently from younger patients. Other reported clinical experience has identified differences in the severity of CNS adverse events between elderly and younger patients (see ADVERSE REACTIONS: Observed During Clinical Practice). In general, dose selection for an elderly patient should be cautious, reflecting the greater frequency of decreased renal function, and of concomitant disease or other drug therapy. This drug is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and it may be useful to monitor renal function.

ADVERSE REACTIONS

The adverse reactions listed below have been observed in controlled and uncontrolled clinical trials in approximately 700 patients who received acyclovir at ~5 mg/kg (250 mg/m2) 3 times daily, and approximately 300 patients who received ~10 mg/kg (500 mg/m2) 3 times daily.

The most frequent adverse reactions reported during administration of acyclovir were inflammation or phlebitis at the injection site in approximately 9% of the patients, and transient elevations of serum creatinine or BUN in 5% to 10% (the higher incidence occurred usually following rapid [less than 10 minutes] intravenous infusion). Nausea and/or vomiting occurred in approximately 7% of the patients (the majority occurring in nonhospitalized patients who received 10 mg/kg). Itching, rash, or hives occurred in approximately 2% of patients. Elevation of transaminases occurred in 1% to 2% of patients.

The following hematologic abnormalities occurred at a frequency of less than 1%: anemia, neutropenia, thrombocytopenia, thrombocytosis, leukocytosis, and neutrophilia. In addition, anorexia and hematuria were observed.

Observed During Clinical Practice

In addition to adverse events reported from clinical trials, the following events have been identified during post-approval use of acyclovir injection in clinical practice. Because they are reported voluntarily from a population of unknown size, estimates of frequency cannot be made. These events have been chosen for inclusion due to either their seriousness, frequency of reporting, potential causal connection to acyclovir or a combination of these factors.

General: Anaphylaxis, angioedema, fatigue, fever, headache, pain and peripheral edema.

Digestive: Abdominal pain, diarrhea, gastrointestinal distress, nausea.

Cardiovascular: Hypotension.

Hematologic and Lymphatic: Disseminated intravascular coagulation, hemolysis, leukocytoclastic vasculitis, leukopenia, lymphadenopathy.

Hepatobiliary Tract and Pancreas: Elevated liver function tests, hepatitis, hyperbilirubinemia, jaundice.

Musculoskeletal: Myalgia.

Nervous: Aggressive behavior, agitation, ataxia, coma, confusion, delirium, dizziness, dysarthria, encephalopathy, hallucinations, obtundation, paresthesia, psychosis, seizure, somnolence, tremor. These symptoms may be marked, particularly in older adults (see PRECAUTIONS).

Skin: Alopecia, erythema multiforme, photosensitive rash, pruritus, rash, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria. Severe local inflammatory reactions, including tissue necrosis, have occurred following infusion of acyclovir into extravascular tissues.

Special Senses: Visual abnormalities.

Urogenital: Renal failure, elevated blood urea nitrogen, elevated creatinine (see WARNINGS).

OVERDOSAGE

Overdoses involving ingestions of up to 20 g have been reported. Adverse events that have been reported in association with overdosage include agitation, coma, seizures, and lethargy. Precipitation of acyclovir in renal tubules may occur when the solubility (2.5 mg/mL) is exceeded in the intratubular fluid. Overdosage has been reported following bolus injections or inappropriately high doses, and in patients whose fluid and electrolyte balance was not properly monitored. This has resulted in elevated BUN and serum creatinine, and subsequent renal failure. In the event of acute renal failure and anuria, the patient may benefit from hemodialysis until renal function is restored (see DOSAGE AND ADMINISTRATION).

DOSAGE AND ADMINISTRATION

CAUTION – RAPID OR BOLUS INTRAVENOUS INJECTION MUST BE AVOIDED (see WARNINGS and PRECAUTIONS).

INTRAMUSCULAR OR SUBCUTANEOUS INJECTION MUST BE AVOIDED (see WARNINGS).

Therapy should be initiated as early as possible following onset of signs and symptoms of herpes infections. A maximum dose equivalent to 20 mg/kg every 8 hours should not be exceeded for any patient.

Dosage

Herpes Simplex Infections: Mucosal and Cutaneous Herpes Simplex (HSV-1 and HSV-2) Infections in lmmunocompromised Patients:

 

Adults and Adolescents (12 years of age and older): 5 mg/kg infused at a constant rate over 1 hour, every 8 hours for 7 days.

 

Pediatrics (Under 12 years of age): 10 mg/kg infused at a constant rate over 1 hour, every 8 hours for 7 days.

Severe Initial Clinical Episodes of Herpes Genitalis:

 

Adults and Adolescents (12 years of age and older): 5 mg/kg infused at a constant rate over 1 hour, every 8 hours for 5 days.

Herpes Simplex Encephalitis:

 

Adults and Adolescents (12 years of age and older): 10 mg/kg infused at a constant rate over 1 hour, every 8 hours for 10 days.

 

Pediatrics (3 months to 12 years of age): 20 mg/kg infused at a constant rate over 1 hour, every 8 hours for 10 days.

Neonatal Herpes Simplex Virus Infections (Birth to 3 months): 10 mg/kg infused at a constant rate over 1 hour, every 8 hours for 10 days. In neonatal herpes simplex infections, doses of 15 mg/kg or 20 mg/kg (infused at a constant rate over 1 hour every 8 hours) have been used; the safety and efficacy of these doses are not known.

Varicella Zoster Infections: Zoster in Immunocompromised Patients:

 

Adults and Adolescents (12 years of age and older): 10 mg/kg infused at a constant rate over 1 hour, every 8 hours for 7 days.

 

Pediatrics (under 12 years of age): 20 mg/kg infused at a constant rate over 1 hour, every 8 hours for 7 days.

Obese Patients: Obese patients should be dosed at the recommended adult dose using Ideal Body Weight.

Patients with Acute or Chronic Renal Impairment: Refer to DOSAGE AND ADMINISTRATION section for recommended doses, and adjust the dosing interval as indicated in Table 5.

Table 5: Dosage Adjustments for Patients with Renal Impairment

Creatine Clearance (mL/min/1.73 m2)	Percent of Recommended Dose	Dosing Interval (hours)
>50	100%	8
25 - 50	100%	12
10 - 25	100%	24
0 - 10	50%	24

 

Hemodialysis: For patients who require dialysis, the mean plasma half-life of acyclovir during hemodialysis is approximately 5 hours. This results in a 60% decrease in plasma concentrations following a 6-hour dialysis period. Therefore, the patient’s dosing schedule should be adjusted so that an additional dose is administered after each dialysis.

 

Peritoneal Dialysis: No supplemental dose appears to be necessary after adjustment of the dosing interval.

Method of Preparation: Each 20 mL vial contains acyclovir sodium equivalent to 500 mg of acyclovir as a sterile aqueous solution. Each 40 mL vial contains acyclovir sodium equivalent to 1000 mg or 1 g of acyclovir as a sterile aqueous solution. The solution in the vial is ready for further dilution prior to infusion.

Administration

The calculated dose should then be removed and added to any appropriate intravenous solution at a volume selected for administration during each 1-hour infusion. Infusion concentrations of approximately 7 mg/mL or lower are recommended. In clinical studies, the average 70-kg adult received between 60 and 150 mL of fluid per dose. Higher concentrations (e.g., 10 mg/mL) may produce phlebitis or inflammation at the injection site upon inadvertent extravasation. Standard, commercially available electrolyte and glucose solutions are suitable for intravenous administration; biologic or colloidal fluids (e.g., blood products, protein solutions, etc.) are not recommended.

Once diluted for administration, each dose should be used within 24 hours.

Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.

HOW SUPPLIED

Acyclovir Injection is supplied as sterile vials, each containing acyclovir sodium equivalent to 500 mg of acyclovir for intravenous administration in 20 mL of water for injection, tray of 10 (NDC 61703-311-21). Each mL contains acyclovir 25 mg/mL.

Acyclovir Injection is supplied as sterile vials, each containing acyclovir sodium equivalent to 1000 mg of acyclovir for intravenous administration in 40 mL of water for injection, tray of 10 (NDC 61703-311-43). Each mL contains acyclovir 25 mg/mL.

Store between 15° to 25°C (59° and 77°F).

Manufactured for:

Mayne Pharma ( USA) Inc.

Paramus, NJ  07652

By: Mayne Pharma Pty Ltd

Mulgrave VIC 3170

Australia

Rev. February 2004

480162

ACYCLOVIR  acyclovir  solution

Product Information Product Type HUMAN PRESCRIPTION DRUG NDC Product Code (Source) 61703-311 Route of Administration INTRAVENOUS DEA Schedule

INGREDIENTS Name (Active Moiety) Type Strength acyclovir sodium (acyclovir ) Active 500 MILLIGRAM  In 1 MILLILITER sodium hydroxide Inactive   hydrochloric acid Inactive

Product Characteristics Color      Score      Shape Size Flavor Imprint Code Contains

Packaging # NDC Package Description Multilevel Packaging 1 61703-311-21 10 VIAL In 1 TRAY contains a VIAL 1 20 mL (MILLILITER) In 1 VIAL This package is contained within the TRAY (61703-311-21) 2 61703-311-43 10 VIAL In 1 TRAY contains a VIAL 2 40 mL (MILLILITER) In 1 VIAL This package is contained within the TRAY (61703-311-43)

Revised: 01/2006Mayne Pharma (USA) Inc.

More Acyclovir IV Infusion resources

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• Drug Images
• Acyclovir IV Infusion Drug Interactions
• Acyclovir IV Infusion Support Group
• 26 Reviews for Acyclovir - Add your own review/rating

Compare Acyclovir IV Infusion with other medications

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cholecalciferol

Generic Name: cholecalciferol (vitamin D3) (KOE le kal SIF e role)

Brand names: D 1000 IU, D3-5, D3-50, Delta D3, Vitamin D3, ...show all 15 brand names.D400, Enfamil D-Vi-Sol, Maximum D3, Carlson D, D2000, Replesta, Liquid Vitamin D-3, Thera-D 2000, Thera-D 4000, Thera-D Rapid Repletion

What is cholecalciferol?

Cholecalciferol is a vitamin D3. Vitamin D is important for the absorption of calcium from the stomach and for the functioning of calcium in the body.

Cholecalciferol is used to treat or prevent many conditions caused by a lack of vitamin D, especially conditions of the skin or bones.

Cholecalciferol may also be used for other purposes not listed in this medication guide.

What is the most important information I should know about cholecalciferol?

Do not use this medication if you have ever had an allergic reaction to vitamin D, or if you have high levels of calcium or vitamin D in your blood, or if you have any condition that makes it hard for your body to absorb nutrients from food (malabsorption).

Before taking cholecalciferol, tell your doctor if you are allergic to any drugs, or if you have heart disease, kidney disease, or an electrolyte imbalance.

Do not take other vitamin or mineral supplements unless your doctor has told you to.

Avoid using calcium supplements or antacids without your doctor's advice. Use only the specific type of supplement or antacid your doctor recommends. Tell your doctor about all your prescription and over-the-counter medications, vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start a new medication without telling your doctor.

Seek emergency medical attention if you think you have used too much of this medicine. An overdose of vitamin D can cause serious or life-threatening side effects.

Overdose symptoms may include headache, weakness, drowsiness, dry mouth, nausea, vomiting, constipation, muscle or bone pain, metallic taste in the mouth, weight loss, itchy skin, changes in heart rate, loss of interest in sex, confusion, unusual thoughts or behavior, severe pain in your upper stomach spreading to your back, or fainting.

What should I discuss with my healthcare provider before taking cholecalciferol?

Do not use this medication if you have ever had an allergic reaction to vitamin D, or if you have:

• 
  

  high levels of calcium in your blood (hypercalcemia);

  
  


• 
  

  high levels of vitamin D in your body (hypervitaminosis D); or

  
  


• 
  

  any condition that makes it hard for your body to absorb nutrients from food (malabsorption).

  
  

If you have any of these other conditions, you may need a dose adjustment or special tests to safely use cholecalciferol:

• 
  

  heart disease;

  
  


• 
  

  kidney disease; or

  
  


• 
  

  an electrolyte imbalance.

  
  

Your cholecalciferol dose needs may change if you are pregnant or breast-feeding. Tell your doctor if you are pregnant or plan to become pregnant during treatment, or if you are breast-feeding a baby.

How should I take cholecalciferol?

Take this medication exactly as directed on the label, or as prescribed by your doctor. Do not take it in larger amounts or for longer than recommended.

Your doctor may occasionally change your dose to make sure you get the best results from this medication.

Measure liquid medicine with a special dose-measuring spoon or cup, not a regular table spoon. If you do not have a dose-measuring device, ask your pharmacist for one.

Cholecalciferol is only part of a complete program of treatment that may also include a special diet. It is very important to follow the diet plan created for you by your doctor or nutrition counselor. You should become very familiar with the list of foods you must eat or avoid to help control your condition.

Store this medication at room temperature away from moisture, light, and heat.

See also: Cholecalciferol dosage (in more detail)

What happens if I miss a dose?

Take the missed dose as soon as you remember. If it is almost time for your next dose, wait until then to take the medicine and skip the missed dose. Do not take extra medicine to make up the missed dose.

What happens if I overdose?

Seek emergency medical attention if you think you have used too much of this medicine. An overdose of vitamin D can cause serious or life-threatening side effects.

Overdose symptoms may include headache, weakness, drowsiness, dry mouth, nausea, vomiting, constipation, muscle or bone pain, metallic taste in the mouth, weight loss, itchy skin, changes in heart rate, loss of interest in sex, confusion, unusual thoughts or behavior, severe pain in your upper stomach spreading to your back, or fainting.

What should I avoid while taking cholecalciferol?

Do not take other vitamin or mineral supplements unless your doctor has told you to.

Avoid using calcium supplements or antacids without your doctor's advice. Use only the specific type of supplement or antacid your doctor recommends.

Cholecalciferol side effects

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Stop taking cholecalciferol and call your doctor at once if you have a serious side effect such as:

• 
  

  thinking problems, changes in behavior, feeling irritable;

  
  


• 
  

  urinating more than usual;

  
  


• 
  

  chest pain, feeling short of breath; or

  
  


• 
  

  early signs of vitamin D overdose (weakness, metallic taste in your mouth, weight loss, muscle or bone pain, constipation, nausea, and vomiting).

  
  

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Cholecalciferol Dosing Information

Usual Adult Dose for Vitamin D Insufficiency:

400 to 1000 international units orally once a day.

Usual Adult Dose for Vitamin D Deficiency:

1000 international units orally once a day.

Usual Adult Dose for Prevention of Falls:

800 international units orally every day (with calcium).

Usual Geriatric Dose for Prevention of Fractures:

For patients over 65 years of age:

100,000 international units orally every 4 months

Usual Pediatric Dose for Vitamin D Insufficiency:

Neonates, infants and children: 200 international units orally once daily.

Alternate dosing:

Premature neonates: 400 to 800 international units orally once daily or 150 to 400 international units/kg/day.

Breastfed neonates and infants (fully or partially breastfed): 400 international units orally once daily beginning in the first few days of life. Continue supplementation until the infant is weaned to greater than or equal to 1000 ml/day or 1 qt/day of vitamin D fortified formula or whole milk (after 12 months of age).

Formula fed neonates and infants ingesting less than 1000 ml of vitamin D fortified formula: 400 international units orally once daily.

Children ingesting less than 1000 ml of vitamin D fortified milk: 400 international units orally once daily.

Adolescents without adequate intake: 400 international units orally once daily.

Children with increased risk of vitamin D deficiency (chronic fat malabsorption, maintained on chronic antiseizure medications): Higher doses may be required; use laboratory testing [25(OH)D, PTH, bone mineral status] to evaluate.

Usual Pediatric Dose for Vitamin D Deficiency:

Treatment of Vitamin D deficiency and/or rickets:

Infants 1 to 12 months: 1000 to 5000 international units/day for 2 to 3 months; once radiologic evidence of healing is observed, dose should be decreased to 400 international units/day.

Children older than 12 months: 5000 to 10,000 international units/day for 2 to 3 months; once radiologic evidence of healing is observed, dose should be decreased to 400 international units/day.

Children with increased risk of vitamin D deficiency (chronic fat malabsorption, maintained on chronic antiseizure medications): Higher doses may be required; use laboratory testing [25(OH)D, PTH, bone mineral status] to evaluate.
Note: If poor compliance, single high dose may be used or repeated periodically.

Treatment of Vitamin D insufficiency or deficiency associated with CKD (stages 2 to 5, 5D): serum 25 hydroxyvitamin D [25(OH)D] level less than or equal to 30 ng/mL:

Serum 25(OH)D level 16 to 30 ng/mL: Children: 2000 international units/day for 3 months or 50,000 international units every month for 3 months.

Serum 25(OH)D level 5 to 15 ng/mL: Children: 4000 international units/day for 12 weeks or 50,000 international units every other week for 12 weeks.

Serum 25(OH)D level less than 5 ng/mL: Children: 8000 international units/day for 4 weeks then 4000 international units/day for 2 months for total therapy of 3 months or 50,000 international units/week for 4 weeks followed by 50,000 international units 2 times/month for a total therapy of 3 months.

Maintenance dose [once repletion accomplished; serum 25(OH)D level greater than 30 ng/mL]: 200 to 1000 international units/day.

Dosage adjustment: Monitor serum 25(OH)D, corrected total calcium and phosphorus levels 1 month following initiation of therapy, every 3 months during therapy and with any Vitamin D dose change.

Prevention and treatment of Vitamin D Deficiency in cystic fibrosis:

Recommended daily intake:

Infants less than 1 year: 400 international units/day.

Children older than 1 year: 400 to 800 international units/day.

Alternate dosing:

Infants less than 1 year: 8000 international units/week.

Children older than 1 year: 800 international units/day.

Note: If serum 25 hydroxyvitamin D [25(OH)D] level remains less than or equal to 30 ng/mL (75 nmol/L) and patient compliance established; then medium dose regimen may be used:

Medium Dose Regimen:

Patients less than 5 years: 12,000 international units/week for 12 weeks.

Patients 5 years or older: 50,000 international units/week for 12 weeks.

Note: If repeat 25 hydroxyvitamin D [25(OH)D] level remains less than or equal to 30 ng/mL (75 nmol/L) and patient compliance established; then high dose regimen may be used:

High Dose Regimen:

Patient less than 5 years: 12,000 international units twice weekly for 12 weeks.

Patient 5 years or older: 50,000 international units twice weekly for 12 weeks.

What other drugs will affect cholecalciferol?

Before taking cholecalciferol, tell your doctor if you are taking any of the following medicines:

• 
  

  seizure medication;

  
  


• 
  

  cholestyramine (Prevalite, Questran);

  
  


• 
  

  colestipol (Colestid);

  
  


• 
  

  steroids (prednisone and others);

  
  


• 
  

  digoxin (digitalis, Lanoxin); or

  
  


• 
  

  a diuretic (water pill) such as chlorothiazide (Diuril), hydrochlorothiazide (HCTZ, HydroDiuril, Hyzaar, Lopressor, Vasoretic, Zestoretic), chlorthalidone (Hygroton, Thalitone), indapamide (Lozol), metolazone (Mykrox, Zaroxolyn), and others.

  
  

This list is not complete and there may be other drugs that can interact with cholecalciferol. Tell your doctor about all your prescription and over-the-counter medications, vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start a new medication without telling your doctor.

More cholecalciferol resources

• Cholecalciferol Side Effects (in more detail)
• Cholecalciferol Dosage
• Cholecalciferol Use in Pregnancy & Breastfeeding
• Cholecalciferol Drug Interactions
• Cholecalciferol Support Group
• 0 Reviews for Cholecalciferol - Add your own review/rating

• Delta D3 Advanced Consumer (Micromedex) - Includes Dosage Information

Compare cholecalciferol with other medications

• Prevention of Falls
• Prevention of Fractures
• Vitamin D Deficiency
• Vitamin D Insufficiency

Where can I get more information?

• Your pharmacist can provide more information about cholecalciferol.

See also: cholecalciferol side effects (in more detail)

Ectosone Mild-Lotion

Generic Name: betamethasone valerate (Topical application route)

bay-ta-METH-a-sone VAL-er-ate

Commonly used brand name(s)

In the U.S.

• Betamethacot


• Beta-Val


• Luxiq


• Qualisone


• Valisone

In Canada

• Betacort Scalp Lotion


• Betnovate


• Betnovate-1/2


• Celestoderm-V


• Celestoderm-V/2


• Ectosone Mild-Lotion


• Ectosone Regular-Cream


• Ectosone Regular-Lotion


• Ectosone Scalp Lotion


• Metaderm Mild


• Metaderm Regular


• Novo-Betamet

Available Dosage Forms:

• Gel/Jelly


• Ointment


• Lotion


• Cream


• Foam

Therapeutic Class: Corticosteroid, Intermediate

Pharmacologic Class: Betamethasone

Uses For Ectosone Mild-Lotion

Betamethasone topical is used to help relieve redness, itching, swelling, or other discomfort caused by skin conditions. Betamethasone foam is used for scalp problems. This medicine is a corticosteroid (cortisone-like medicine or steroid).

This medicine is available only with your doctor's prescription.

Before Using Ectosone Mild-Lotion

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Appropriate studies performed to date have not demonstrated pediatric-specific problems that would limit the usefulness of betamethasone topical in the pediatric population. However, because of this medicine's toxicity, it should be used with caution. Children may absorb large amounts through the skin, which can cause serious side effects. If your child is using this medicine, follow your doctor's instructions very carefully. For the foam form, safety and efficacy have not been established.

Geriatric

No information is available on the relationship of age to the effects of betamethasone topical in geriatric patients.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. Tell your healthcare professional if you are taking any other prescription or nonprescription (over-the-counter [OTC]) medicine.

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other Medical Problems

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

• Cushing's syndrome (adrenal gland disorder) or


• Diabetes or


• Hyperglycemia (high blood sugar) or


• Intracranial hypertension (increased pressure in the head)—Use with caution. May make these conditions worse.

• Infection of the skin at or near the place of application or


• Large sores, broken skin, or severe skin injury at the place of application—The chance of side effects may be increased.

Proper Use of betamethasone

This section provides information on the proper use of a number of products that contain betamethasone. It may not be specific to Ectosone Mild-Lotion. Please read with care.

It is very important that you use this medicine only as directed by your doctor. Do not use more of it, do not use it more often, and do not use it for a longer time than your doctor ordered. To do so may cause unwanted side effects or skin irritation.

This medicine is for use on the skin only. Do not get it in your eyes. Do not use it on skin areas that have cuts, scrapes, or burns. If it does get on these areas, rinse it off right away with water.

This medicine should only be used for skin conditions that your doctor is treating. Check with your doctor before using it for other conditions, especially if you think that an infection may be present. This medicine should not be used to treat certain kinds of skin infections or conditions, such as severe burns.

To use cream, lotion, or ointment:

• Wash your hands with soap and water before and after using this medicine.


• Apply a thin layer of this medicine to the affected area of the skin. Rub it in gently.


• With the lotion, protect the skin from water, clothing, or anything that causes rubbing until the medicine has dried. Also, shake the lotion well before using it.


• Do not bandage or otherwise wrap the skin being treated unless directed to do so by your doctor.


• If the medicine is applied to the diaper area of an infant, do not use tight-fitting diapers or plastic pants unless directed to do so by your doctor.


• If your doctor ordered an occlusive dressing or airtight covering to be applied over the medicine, make sure you know how to apply it. Occlusive dressings increase the amount of medicine absorbed through your skin, so use them only as directed. If you have any questions about this, check with your doctor.

To use the foam:

• This medicine comes with a patient information insert. Read and follow the instructions carefully.


• Wash your hands with soap and water before and after using this medicine.


• Turn the can upside down and place a small amount of medicine in a saucer or any cool, clean surface. Do not put the foam directly in your hands. This will melt the foam immediately upon contact with warm skin.


• Move the hair away and put a small amount of the foam on the affected areas of the scalp. Massage it in gently until the medicine has dried.


• Do not wash or rinse the treated areas immediately after applying the medicine.


• Do not use this medicine near heat, open flame, or while smoking.

Dosing

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For redness, itching, and swelling of the skin:
  
  • For topical dosage forms (cream and ointment):
    
    • Adults—Apply to the affected area of the skin one to three times per day.
    
    
    • Children—Use and dose must be determined by your doctor.
    
    
  
  
  • For topical dosage form (lotion):
    
    • Adults—Apply a few drops to the affected area of the skin two times per day (morning and evening).
    
    
    • Children—Use and dose must be determined by your doctor.
    
    
  
  


• For scalp problems:
  
  • For topical dosage form (foam):
    
    • Adults—Apply to the affected area of the scalp two times per day (once in the morning and once at night).
    
    
    • Children—Use and dose must be determined by your doctor.
    
    
  
  

Missed Dose

If you miss a dose of this medicine, apply it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule.

Storage

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Store the can of the foam at room temperature, away from heat and direct light. Do not freeze. Do not keep this medicine inside a car where it could be exposed to extreme heat or cold. Do not poke holes in the canister or throw it into a fire, even if the canister is empty.

Precautions While Using Ectosone Mild-Lotion

It is very important that your doctor check the progress of you or your child at regular visits for any unwanted effects that may be caused by this medicine.

If your or your child's symptoms do not improve within a few days, or if they become worse, check with your doctor.

Using too much of this medicine or using it for a long time may increase your risk of having adrenal gland problems. The risk is greater for children and patients who use large amounts for a long time. Talk to your doctor if you or your child have more than one of these symptoms while you are using this medicine: blurred vision; dizziness or fainting; a fast, irregular, or pounding heartbeat; increased thirst or urination; irritability; or unusual tiredness or weakness.

Stop using this medicine and check with your doctor right away if you or your child have a skin rash, burning, stinging, swelling, or irritation on the skin.

Do not use cosmetics or other skin care products on the treated areas.

Ectosone Mild-Lotion Side Effects

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

More common

• Burning, itching, or stinging at the application site

Less common

• Hair loss


• thinning of the hair

Incidence not known

• Blistering, burning, crusting, dryness, or flaking of the skin


• irritation


• itching, scaling, severe redness, soreness, or swelling of the skin


• redness and scaling around the mouth


• thinning of the skin with easy bruising, especially when used on where the skin folds together (e.g. between the fingers)

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

Less common

• Acne or pimples


• burning, crawling, itching, numbness, prickling, "pins and needles", or tingling feelings

Incidence not known

• Burning and itching of the skin with pinhead-sized red blisters


• burning, itching, and pain in hairy areas, or pus at the root of the hair


• increased hair growth on the forehead, back, arms, and legs


• lightening of normal skin color


• lightening of treated areas of dark skin


• reddish purple lines on the arms, face, legs, trunk, or groin


• softening of the skin

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

The information contained in the Thomson Reuters Micromedex products as delivered by Drugs.com is intended as an educational aid only. It is not intended as medical advice for individual conditions or treatment. It is not a substitute for a medical exam, nor does it replace the need for services provided by medical professionals. Talk to your doctor, nurse or pharmacist before taking any prescription or over the counter drugs (including any herbal medicines or supplements) or following any treatment or regimen. Only your doctor, nurse, or pharmacist can provide you with advice on what is safe and effective for you.

The use of the Thomson Reuters Healthcare products is at your sole risk. These products are provided "AS IS" and "as available" for use, without warranties of any kind, either express or implied. Thomson Reuters Healthcare and Drugs.com make no representation or warranty as to the accuracy, reliability, timeliness, usefulness or completeness of any of the information contained in the products. Additionally, THOMSON REUTERS HEALTHCARE MAKES NO REPRESENTATION OR WARRANTIES AS TO THE OPINIONS OR OTHER SERVICE OR DATA YOU MAY ACCESS, DOWNLOAD OR USE AS A RESULT OF USE OF THE THOMSON REUTERS HEALTHCARE PRODUCTS. ALL IMPLIED WARRANTIES OF MERCHANTABILITY AND FITNESS FOR A PARTICULAR PURPOSE OR USE ARE HEREBY EXCLUDED. Thomson Reuters Healthcare does not assume any responsibility or risk for your use of the Thomson Reuters Healthcare products.

More Ectosone Mild-Lotion resources

• Ectosone Mild-Lotion Use in Pregnancy & Breastfeeding
• Ectosone Mild-Lotion Drug Interactions
• Ectosone Mild-Lotion Support Group
• 13 Reviews for Ectosone-Lotion - Add your own review/rating

Compare Ectosone Mild-Lotion with other medications

• Atopic Dermatitis
• Dermatitis
• Dermatological Disorders
• Lichen Planus
• Lichen Sclerosus