Free Russia: 2016

Tuesday, September 27, 2016

Nix Lice Control

Generic Name: permethrin topical (per METH rin)

Brand Names: Elimite, Lice Bedding Spray, Nix Complete Lice Treatment System, Nix Cream Rinse, Nix Lice Control, RID Home Lice Control Spray for Surfaces

What is Nix Lice Control (permethrin topical)?

Permethrin is an anti-parasite medication.

Permethrin topical (for the skin) is used to treat head lice and scabies.

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

What is the most important information I should know about Nix Lice Control (permethrin topical)?

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

Do not take this medication by mouth. It is for use only on the skin, hair, fabrics, or other surfaces. Do not apply permethrin topical to open cuts or wounds. Do not use this medication if you are allergic to permethrin or to chrysanthemums. For the most complete treatment of lice or scabies and to prevent reinfection, you must treat your environment (clothing, bedding, pillows, furniture, hats, hair brushes and accessories, etc) at the same time you treat your body.

Avoid sexual or intimate contact with others until your lice or scabies infection has cleared up. Avoid sharing hair brushes, combs, hair accessories, hats, clothing, bed linens, and other articles of personal use. Lice and scabies infections are highly contagious.

What should I discuss with my healthcare provider before using Nix Lice Control (permethrin topical)?

Do not use this medication if you are allergic to permethrin or to chrysanthemums. FDA pregnancy category B. Permethrin topical is not expected to be harmful to an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant during treatment. Permethrin can pass into breast milk and may harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby. Do not use this medication on an infant younger than 2 months without the advice of a doctor.

How should I use Nix Lice Control (permethrin topical)?

Do not take this medication by mouth. It is for use only on the skin, hair, fabrics, or other surfaces.

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

You may need to shake the medication before each use. Follow the directions on the medicine label. Do not apply permethrin topical to open cuts or wounds.

To treat scabies:

Make sure your skin is clean and dry. Apply a thin layer of permethrin topical to all body parts from the neck down to the soles of the feet. Rub in completely. Leave the medication on for 8 to 14 hours, then wash it off completely.

When using permethrin topical on an infant, also apply the medication to the scalp, temples, and forehead. Avoid applying close to the eyes, nose, mouth, or genitals.

If your condition does not clear up within 14 days after applying permethrin topical, use another application.

To treat head lice:

When using the shampoo, apply it to dry hair only. Cover all hair completely and leave the shampoo in for 10 minutes. Then work into a lather using warm water and rinse out thoroughly.

When using the cream rinse, wash your hair using shampoo only (no conditioner or 2-in-1 shampoo). Rinse thoroughly and towel dry the hair, leaving it damp. Apply enough of the cream rinse to completely saturate all hair. Leave the cream rinse in your hair for 10 minutes.

Use a towel or washcloth to protect your eyes while the medication is left in your hair.

Use a second application if lice are still seen 7 days after your first treatment.

You may also use a nit comb to remove lice eggs from the hair. Your hair should be slightly damp while using a nit comb. Work on only one section of hair at a time, combing through 1- to 2-inch strands from the scalp to the ends.

Rinse the nit comb often during use. Place removed nits into a sealed plastic bag and throw it into the trash to prevent re-infestation.

Check the scalp again daily to make sure all nits have been removed.

To treat pubic lice (crabs):

Wash and dry the treatment area. Apply permethrin topical to all pubic hair and any surrounding hairs on the thighs and around the anus.

Avoid getting this medication inside the rectum or vagina.

Leave the medication in for 10 minutes. Then work into a lather using warm water and rinse out thoroughly.

You may also use a nit comb to remove lice eggs from pubic hair (hair should be slightly damp).

All sexual partners should also be treated to prevent re-infestation of crabs.

To prevent reinfection, wash all clothing, hats, bed clothes, bed linens, and towels in hot water and dry in high heat. Dry-clean any non-washable clothing. Hair brushes, combs, and hair accessories should be soaked in hot water for at least 10 minutes.

Use permethrin surface spray to disinfect non-washable items such as:

furniture;

mattresses and pillows;

stuffed toys;

hats, gloves, and scarves;

headphones or headbands;

the inside of a bike helmet; or

seats and carpets inside your car.

Stuffed toys or pillows that cannot be washed should be sealed in air-tight plastic bags for 4 weeks.

Vacuum all rugs and carpets and throw away the vacuum cleaner bag.

For the most complete treatment of lice or scabies, you must treat your environment (clothing, bedding, etc) at the same time you treat your body. Store permethrin topical at room temperature away from moisture and heat.

What happens if I miss a dose?

Since permethrin topical is usually needed only once, you are not likely to be on a dosing schedule. Wait at least 7 days before using a second application.

What happens if I overdose?

Seek emergency medical attention if you think you have used too much of this medicine.

Symptoms of a permethrin topical overdose are unknown.

What should I avoid while using Nix Lice Control (permethrin topical)?

Avoid getting this medication in your mouth or eyes. If it does get into any of these areas, rinse with water.

Do not use other medicated skin products unless your doctor has told you to.

Nix Lice Control (permethrin topical) side effects

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat. Call your doctor at once if you have severe burning, stinging, redness, or swelling after applying permethrin topical.

Less serious side effects may include:

itching or mild skin rash;

mild burning, stinging, or redness; or

numbness or tingling where the medication was applied.

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.

What other drugs will affect Nix Lice Control (permethrin topical)?

It is not likely that other drugs you take orally or inject will have an effect on topically applied permethrin. But many drugs can interact with each other. 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 Nix Lice Control resources

Nix Lice Control Side Effects (in more detail)
Nix Lice Control Use in Pregnancy & Breastfeeding
Nix Lice Control Support Group
0 Reviews for Nix Lice Control - Add your own review/rating

Acticin Cream MedFacts Consumer Leaflet (Wolters Kluwer)

Acticin Topical Advanced Consumer (Micromedex) - Includes Dosage Information

Elimite Prescribing Information (FDA)

Compare Nix Lice Control with other medications

Head Lice
Lice
Scabies

Where can I get more information?

Your pharmacist has additional information about permethrin topical written for health professionals that you may read.

See also: Nix Lice Control side effects (in more detail)

Nizoral A-D Topical

Generic Name: ketoconazole (Topical route)

kee-toe-KON-a-zole

Commonly used brand name(s)

In the U.S.

Extina

Nizoral

Nizoral A-D

Xolegel

In Canada

Ketoderm

Available Dosage Forms:

Shampoo

Foam

Gel/Jelly

Solution

Cream

Therapeutic Class: Antifungal

Chemical Class: Imidazole

Uses For Nizoral A-D

Ketoconazole is used to treat infections caused by a fungus or yeast. It works by killing the fungus or yeast or preventing its growth.

Ketoconazole cream is used to treat:

Athlete's foot (tinea pedis; ringworm of the foot);

Ringworm of the body (tinea corporis);

Ringworm of the groin (tinea cruris; jock itch);

Seborrheic dermatitis;

"Sun fungus" (tinea versicolor; pityriasis versicolor); and

Yeast infection of the skin (cutaneous candidiasis).

Ketoconazole foam or gel is used to treat seborrheic dermatitis (scaly areas on your skin or scalp).

Ketoconazole 1% shampoo is used to treat dandruff.

Ketoconazole 2% shampoo is used to treat "sun fungus" (tinea versicolor; pityriasis versicolor).

This medicine may also be used for other fungus infections of the skin as determined by your doctor.

Most forms of this medicine are available only with your doctor's prescription. Some forms are available without a prescription. However, your doctor may have special instructions on the proper use for your medical condition.

Before Using Nizoral A-D

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 have not been performed on the relationship of age to the effects of ketoconazole topical in children younger than 12 years of age. Safety and efficacy have not been established.

Geriatric

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of ketoconazole topical in the elderly. However, some elderly patients may be more sensitive to the side effects of this medicine.

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. 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.

Proper Use of ketoconazole

This section provides information on the proper use of a number of products that contain ketoconazole. It may not be specific to Nizoral A-D. 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, nose, mouth, or vagina. 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.

For patients using the cream:

Apply enough cream to cover the affected and surrounding skin areas, and rub in gently.

To help clear up your infection completely, it is very important that you keep using the cream for the full time of treatment, even if your symptoms begin to clear up after a few days. Since fungus or yeast infections may be very slow to clear up, you may have to continue using this medicine every day for up to several weeks. If you stop using this medicine too soon, your symptoms may return. Do not miss any doses.

For patients using the foam:

Wash your hands before and after using this medicine.

Do not spray the foam directly on your hand because it will begin to melt as soon as it touches your skin. Instead, spray the foam into the cap of the medicine can or other cool surface. Then dip your fingertips into the foam to pick up small amounts of the medicine, and apply to the affected skin areas. Gently massage the foam into your skin until it disappears.

If you are treating skin areas with hair, such as your scalp, move any hair away so the foam can be applied directly to the affected skin.

This medicine is flammable. Do not use it near heat, an open flame, or while smoking. Do not puncture, break, or burn the medicine can.

For patients using the gel:

Wash your hands before and after using this medicine.

Apply enough ketoconazole gel to cover the affected and surrounding skin areas, and rub in gently with your fingertips.

After applying this medicine, do not wash the affected area for at least 3 hours.

Cosmetics (makeup or sunscreens) may be used on the treated skin areas no sooner than 20 minutes after this medicine is applied.

This medicine may be flammable. Do not use it near heat, an open flame, or while smoking.

For patients using the 1% shampoo:

Wet your hair and scalp well with water.

Apply enough shampoo to work up a good lather and gently massage it over your entire scalp.

Rinse your hair and scalp with warm water.

Repeat application.

Rinse your hair and scalp well with warm water, and dry your hair.

For patients using the 2% shampoo:

Wet your hair and scalp well with water.

Apply the shampoo to the skin of the affected area and a wide margin surrounding this area.

Work up a good lather and leave it in place for 5 minutes.

Rinse your hair and scalp well with warm water, and dry your hair.

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 cream dosage form:
- For cutaneous candidiasis, tinea corporis, tinea cruris, tinea pedis, or pityriasis versicolor:
  - Adults—Apply to the affected area of the skin and the surrounding area once a day.
  - Children—Use and dose must be determined by your doctor.
- For seborrheic dermatitis:
  - Adults—Apply to the affected area of the skin and the surrounding area two times per day.
  - Children—Use and dose must be determined by your doctor.

For foam dosage form:
- For seborrheic dermatitis:
  - Adults—Apply to the affected area of the skin and the surrounding area two times per day for 4 weeks.
  - Children—Use and dose must be determined by your doctor.

For gel dosage form:
- For seborrheic dermatitis:
  - Adults, teenagers, and children 12 years of age and older—Apply to the affected area of the skin and the surrounding area once a day for 2 weeks.
  - Children younger than 12 years of age—Use and dose must be determined by your doctor.

For 1% shampoo dosage form:
- For dandruff:
  - Adults—Use every 3 or 4 days for up to 8 weeks. Then use only as needed to keep dandruff under control.
  - Children—Use and dose must be determined by your doctor.

For 2% shampoo dosage form:
- For pityriasis versicolor:
  - Adults—Use once.
  - 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

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 Nizoral A-D

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 check you for any problems or unwanted effects that may be caused by this medicine.

Do not use this medicine for a skin problem that has not been checked by your doctor.

If your skin problem does not improve within 2 weeks for cutaneous candidiasis, pityriasis versicolor, tinea corporis, or tinea cruris; or 4 weeks for seborrheic dermatitis; or 4 to 6 weeks for tinea pedis, or if it becomes worse, check with your doctor.

Good health habits are also required for patients using the cream form of this medicine to help clear up your infection completely and to help make sure it does not return.

For patients using the cream for athlete's foot (tinea pedis; ringworm of the foot), the following instructions will help keep the feet cool and dry:

Avoid wearing socks made from wool or synthetic materials (e.g., rayon or nylon). Instead, wear clean, cotton socks and change them daily or more often if your feet sweat a lot.

Wear sandals or well-ventilated shoes (e.g., shoes with holes).

Use a bland, absorbent powder (e.g., talcum powder) or an antifungal powder between the toes, on the feet, and in socks and shoes one or two times a day. It is best to use the powder between the times you use the cream.

If you have any questions about these instructions, check with your doctor.

For patients using the cream for ringworm of the groin (tinea cruris; jock itch), the following instructions will help reduce chafing and irritation and will also help keep the groin area cool and dry:

Avoid wearing underwear that is tight-fitting or made from synthetic materials (e.g., rayon or nylon). Instead, wear loose-fitting, cotton underwear.

Use a bland, absorbent powder (e.g., talcum powder) or an antifungal powder on the skin. It is best to use the powder between the times you use ketoconazole cream.

If you have any questions about these instructions, check with your doctor.

The foam form of this medicine may make your skin more sensitive to sunlight. Use a sunscreen when you are outdoors. Avoid sunlamps and tanning beds.

This medicine may cause a serious type of allergic reaction called anaphylaxis. Anaphylaxis can be life-threatening and requires immediate medical attention. Call your doctor right away if you have a rash; itching; hoarseness; trouble breathing; trouble swallowing; or any swelling of your hands, face, or mouth while you are using this medicine.

Tell your doctor if you have the following symptoms while using the ketoconazole 2% shampoo: hair discoloration, abnormal hair texture, removal of the curl from permanently waved hair, hair loss, itching, burning sensation of the skin, or blistering, peeling, or redness of the skin.

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.

Nizoral A-D 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:

Less common—For cream, shampoo, foam, or gel

Itching, stinging, burning, or irritation not present before use of this medicine

Rare—For cream, foam, or gel

Acne

bleeding from sore in the mouth

blistering, crusting, irritation, itching, or reddening of the skin

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

cracked, dry, or scaly skin

discoloration of the fingernails or toenails

dizziness

eye dryness, irritation, or swelling

red rash with watery, yellow-colored, or pus filled blisters with or without thick yellow to honey-colored crusts

skin dryness, pain, rash, redness, or swelling

sore in the mouth or on the gums

swelling of the face

Rare—For shampoo

Hair loss and irritation

Incidence not known—For gel

Pain

Incidence not known—For shampoo

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

burning sensation of the skin

burning, itching, redness, skin rash, swelling, or soreness at the application site

discoloration of the hair

dry skin

fast heartbeat

fever

hives

hoarseness

irritation

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

joint pain, stiffness, or swelling

rash

shortness of breath

swelling of the eyelids, face, lips, hands, or feet

thinning of the hair

tightness in the chest

troubled breathing or swallowing

wheezing

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—For shampoo or gel

Dryness or oiliness of the hair and scalp

headache

Rare—For shampoo

Abnormal hair texture

mild dryness of the skin

scalp pustules

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: Nizoral A-D Topical side effects (in more detail)

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Compare Nizoral A-D Topical with other medications

Cutaneous Candidiasis
Dandruff
Seborrheic Dermatitis
Tinea Corporis
Tinea Cruris
Tinea Pedis
Tinea Versicolor

Nolvadex

Generic Name: Tamoxifen Citrate
Class: Antineoplastic Agents
VA Class: AN500
Chemical Name: 2-Hydroxy-1,2,3-propanetricarboxylate-(Z)-2-[4-(1,2-diphyl-1-butenyl)phenoxy]-N,Ndimethyl ethanamine
Molecular Formula: C₂₆H₂₉NO•C₆H₈O₇
CAS Number: 54965-24-1

For women with ductal carcinoma in situ (DCIS) and women at high risk for breast cancer: serious and life-threatening events associated with tamoxifen in the risk reduction setting include uterine malignancies, stroke, and pulmonary embolism.^a Incidence rates for these events have been estimated from the NSABP P-1 trial (median length of follow-up 6.9 years).^a

Uterine malignancies consist of both endometrial adenocarcinoma (incidence rate per 1000 women-years of 2.2 for tamoxifen versus 0.71 for placebo) and uterine sarcoma (incidence rate per 1000 women-years of 0.17 for tamoxifen versus 0 for placebo).

For stroke, the incidence rate per 1000 women-years was 1.43 for tamoxifen versus 1 for placebo.^a

For pulmonary embolism, the incidence rate per 1000 women-years was 0.75 for tamoxifen versus 0.25 for placebo.^a

Health care providers should discuss the potential benefits versus the potential risks of these serious events with women at high risk of breast cancer and women with DCIS considering tamoxifen to reduce their risk of developing breast cancer.^a

The benefits of tamoxifen outweigh its risks in women already diagnosed with breast cancer.^a

Introduction

A nonsteroidal estrogen agonist-antagonist; an antineoplastic agent.¹²⁸

Uses for Nolvadex

Breast Cancer

An adjuvant to surgery and radiation therapy for the treatment of breast cancer in women with negative axillary lymph nodes and in postmenopausal women with positive axillary lymph nodes.¹¹⁰ ¹²¹ ¹²⁸ ¹³⁰ ¹³³ ¹³⁶ ¹⁹⁴ ¹⁹⁵ ¹⁹⁶ ¹⁹⁸ ²⁰⁴ ²⁰⁵ ²⁵³ ²⁵⁴ ²⁵⁸ Also reduces the occurrence of contralateral breast cancer in these women.¹²⁸ ²⁵³ ²⁵⁴ ²⁵⁸

Reduction of risk of invasive breast cancer in patients with DCIS following surgery and radiation therapy.^a

Palliative treatment of metastatic breast cancer in men and women.¹²⁸ An alternative to ovarian ablative therapy (oopherectomy or radiation) in premenopausal women.¹²⁸ ¹³³ ¹⁵⁸ ¹⁵⁹ ¹⁶⁰ ¹⁶¹ ¹⁶² ¹⁶³ ¹⁶⁴ ¹⁶⁵ ¹⁶⁶ ¹⁶⁷ ¹⁶⁸ ¹⁶⁹ ¹⁸³

Reduction in the incidence of breast cancer in women at high risk for developing the disease.¹²⁸ ²⁹³

Albright’s Syndrome

Has been used to reduce the frequency of vaginal bleeding episodes and to reduce the rate of increase in bone age in girls with Albright’s syndrome (McCune-Albright syndrome†) and precocious puberty.^a

Long-term effects not established.^a

Nolvadex Dosage and Administration

General

Consult specialized references for procedures for proper handling and disposal of antineoplastic drugs.

Administration

Administered orally as a single daily dose or in divided doses; dosages exceeding 20 mg daily should be given in divided doses (morning and evening).¹²⁸

Initiate therapy during menstruation when used to reduce the incidence of breast cancer in sexually active women.^a In women with menstrual irregularity, a negative β-human chorionic gonadotropin test immediately prior to therapy is sufficient.^a

Dosage

Available as tamoxifen citrate; dosage expressed in terms of tamoxifen.¹²⁸

Adults

Breast Cancer

Adjuvant Therapy

Oral

20–40 mg daily.¹⁰⁰ ¹⁰² ¹¹⁰ ¹²¹ ¹²⁸ ¹²⁹ ¹³⁰ ¹⁹⁴ ¹⁹⁵ ¹⁹⁶ ²⁰⁵ Current data from clinical studies support 5 years of adjuvant therapy.¹²⁸ ¹⁹⁴ ¹⁹⁵ ¹⁹⁶ ²⁵³ ²⁵⁴ ²⁵⁶ ²⁵⁷ ²⁹¹ ³²⁸

Ductal Carcinoma in Situ

Oral

20 mg daily for 5 years.^a

Metastatic Breast Cancer

Oral

20–40 mg daily.¹²⁸

Reduction in the Incidence of Breast Cancer in Women at High Risk

Oral

20 mg daily for 5 years.¹²⁸ ²⁷⁰ ²⁸⁴ ²⁹¹

Prescribing Limits

Adults

Breast Cancer

Adjuvant Therapy

Oral

No evidence that dosages >20 mg daily are more effective.¹¹² ¹²⁸

Cautions for Nolvadex

Contraindications

Known hypersensitivity to tamoxifen or any ingredient in the formulation.¹²⁸

When used in women with DCIS and women at high risk for breast cancer, history of DVT or pulmonary embolism.^a

When used in women with DCIS and women at high risk for breast cancer, concurrent anticoagulant therapy with a warfarin derivative.^a ²⁷⁸ ²⁹³ ³⁰⁹

Warnings/Precautions

Warnings

Hypercalcemia

Hypercalcemia reported in patients with metastatic breast cancer who have bone metastases.¹²⁸ ¹²⁹ If hypercalcemia occurs, take appropriate measures; if severe, discontinue tamoxifen.¹²⁸

Effects on the Uterus

Increased incidence of uterine malignancies, sometimes fatal, reported.¹²⁸ ³³⁰ Most uterine malignancies have been classified as adenocarcinoma of the endometrium; rare uterine sarcomas also reported.¹²⁸ ³³⁰ (See Boxed Warning.) Gynecologic symptoms (i.e., menstrual irregularities, abnormal vaginal bleeding, changes in vaginal discharge, pelvic pain or pressure) should be promptly evaluated.¹²⁸ ¹⁶³ ¹⁸³

Endometrial changes, including hyperplasias and polyps, endometriosis and uterine fibroids reported.¹²⁸ ¹⁸⁰ ²⁵⁸ ²⁵⁹ ²⁷⁴ Ovarian cysts reported in a small number of premenopausal women with advanced breast cancer.¹²⁸

Cardiovascular Effects

Increased incidence of thromboembolic events, including DVT¹²⁸ ²⁹³ and pulmonary embolism; ²⁶⁹ ²⁷⁰ ²⁹³ stroke also reported.¹²⁸ ²⁶⁹ ²⁷⁷ ²⁹³ Some cases of stroke and pulmonary emboli have been fatal.¹²⁸ (See Boxed Warning.) Concomitant use with chemotherapy may increase incidence of these events.¹²⁸

Hepatic Effects

Liver cancer reported.¹²⁸

Changes in AST, ALT, bilirubin and/or alkaline phosphatase concentrations reported; severe hepatic abnormalities including fatty changes in the liver, cholestasis, hepatitis, and hepatic necrosis (some fatal) reported rarely.¹²⁸

Ocular Effects

Visual disturbances, decrement in color vision perception, corneal changes, cataracts, optic neuritis, retinal vein thrombosis, intraretinal crystals, posterior subcapsular opacities, and/or retinopathy reported.¹²⁸ ¹⁹⁰ ¹⁹¹ ¹⁹² ¹⁹³ ²⁵⁸ ²⁶⁸ ³²⁶

Fetal/Neonatal Morbidity and Mortality

May cause fetal harm.¹²⁸ If inadvertently used during pregnancy or if patient becomes pregnant, apprise of potential fetal hazard, including possible long-term risk of a diethylstilbestrol-like syndrome.¹²⁸

General Precautions

Hematologic Effects

Thrombocytopenia, neutropenia, pancytopenia, and leukopenia reported; caution in patients with leukopenia or thrombocytopenia.¹²⁸ Periodic CBCs, including platelet count recommended.¹²⁸

Specific Populations

Pregnancy

Category D.¹²⁸ (See Fetal/Neonatal Morbidity and Mortality under Cautions.)

Lactation

Not known whether tamoxifen is distributed into milk.¹²⁸ Discontinue nursing or the drug because of potential risk to nursing infant.¹²⁸

Pediatric Use

Safety and efficacy in girls 2–10 years of age with Albright’s syndrome and precocious puberty not studied beyond 1 year; long-term effects not established and continued monitoring recommended.^a (See Special Populations under Pharmacokinetics.)

Geriatric Use

No substantial differences in safety and efficacy relative to younger adults.^a

Common Adverse Effects

Hot flashes, vaginal discharge, menstrual irregularities, weight loss.¹²⁸

Interactions for Nolvadex

A substrate of CYP3A, 2C9, 2D6.^a

Effect of tamoxifen on drugs that require mixed function oxidases for activation unknown.^a

Cytotoxic Agents

Increased risk of thromboembolic events.¹²⁸

Specific Drugs

Drug	Interaction	Comments
Aminoglutethimide	Decreased plasma tamoxifen and N-desmethyltamoxifen concentrations¹²⁸
Anticoagulants (e.g., warfarin)	Enhanced warfarin effects¹²⁸ ¹⁷⁰ ¹⁷¹ ¹⁷²	Careful monitoring of PT is recommended¹²⁸ ¹⁷⁰ ¹⁷¹ ¹⁷² When used in women with DCIS or at high risk for breast cancer, concomitant use contraindicated^a
Bromocriptine	Increased plasma tamoxifen and N-desmethyltamoxifen concentrations¹²⁸
Cyclosporine	Competitively inhibited formation of N-desmethyltamoxifen in vitro^a	Clinicial importance unknown^a
Diltiazem	Competitively inhibited formation of N-desmethyltamoxifen in vitro^a	Clinicial importance unknown^a
Erythromycin	Competitively inhibited formation of N-desmethyltamoxifen in vitro^a	Clinicial importance unknown^a
Letrozole	Decreased plasma letrozole concentrations^a
Medroxyprogesterone	Decreased plasma N-desmethyltamoxifen concentrations but did not reduce plasma tamoxifen concentrations^a
Nifedipine	Competitively inhibited formation of N-desmethyltamoxifen in vitro^a	Clinicial importance unknown^a
Phenobarbital	Decreased plasma tamoxifen concentrations¹²⁸	Clinical importance unknown¹²⁸
Rifampin	Decreased plasma tamoxifen and N-desmethyltamoxifen concentrations^a

Nolvadex Pharmacokinetics

Absorption

Bioavailability

Absorbed slowly following oral administration; peak serum concentrations of tamoxifen occur about 3–6 hours after a single dose.¹²⁸ ¹³⁷ ¹³⁸ ¹³⁹ ¹⁴⁰ ¹⁴¹

Plasma Concentrations

Steady-state concentrations of tamoxifen are attained after 3–4 weeks and those of N-desmethyltamoxifen, an active metabolite, are attained after 3–8 weeks.¹²⁸ ¹³⁷ ¹⁴⁰ ¹⁴³ ¹⁴⁵

Distribution

Extent

Not fully characterized.¹²⁸

Not known whether tamoxifen is distributed into milk.¹²⁸

Elimination

Metabolism

Rapidly and extensively metabolized.²⁶ ²⁸ ¹⁴⁰ ¹⁴² ¹⁴³ ¹⁴⁴ ¹⁴⁵ ¹⁴⁶ ¹⁴⁸ ¹⁴⁹ ¹⁵⁰ ¹⁵¹ The major metabolite, N-desmethyltamoxifen,¹²⁸ ¹⁴⁰ ¹⁴³ ¹⁴⁴ ¹⁴⁵ ¹⁴⁶ ¹⁴⁸ ¹⁵⁰ ¹⁵¹ has biologic activity similar to that of the parent drug.¹²⁸

Elimination Route

Excreted principally in feces as polar conjugates.¹²⁸

Half-life

Tamoxifen: 5–7 days.²⁸ ¹³⁷ ¹³⁹ ¹⁴⁵

N-Desmethyltamoxifen: 9–14 days.¹²⁸ ¹³⁹ ¹⁴⁵

Special Populations

Clearance higher in female children 2–10 years of age than in women; exposure to N-desmethyltamoxifen in these pediatric patients similar to adults.^a

Stability

Storage

Oral

Tablets

Well-closed, light-resistant containers 20–25°C.¹²⁸

ActionsActions

Acts as an estrogen antagonist on breast tissue and in the CNS and as an estrogen agonist on endometrium, bone, and lipids.³¹¹

In breast epithelial tissue, increases production of inhibitory factors and decreases production of stimulatory factors that influence breast cell growth.²⁷¹ ²⁸⁶ ²⁸⁷ ³²³

Reduces bone resorption and bone turnover.²⁶⁵ ²⁶⁶ ²⁶⁷ ³¹⁶

Decreases total and LDL-cholesterol concentrations.³¹⁸ ³¹⁹ ³²⁰ Less favorably, decreases HDL-cholesterol concentrations and increases triglyceride concentrations.³¹⁸ ³¹⁹ ³²⁰

Acts as an estrogen agonist on the uterus and exhibits proliferative and tumor-promoting effects on the endometrium.³¹¹

Advice to Patients

Importance of receiving routine gynecologic care and of immediately informing clinician if any new breast lumps or abnormal gynecologic symptoms, including abnormal vaginal bleeding, change in vaginal discharge, menstrual irregularities, or pelvic pain/pressure occur.¹²⁸ ¹⁶³ ¹⁸³

Importance of informing clinician of any changes in vision.¹²⁸ ¹⁹⁰ ¹⁹¹ ¹⁹² ¹⁹³ ²⁵⁸ ²⁶⁸

Importance of immediately informing clinician of unexplained shortness of breath or leg swelling/tenderness.¹²⁸

Importance of periodic monitoring, including liver function test monitoring and blood counts.¹²⁸

Advise patients at high risk of breast cancer that tamoxifen may decrease the incidence of breast cancer, but may not eliminate the risk of the disease.¹²⁸

Importance of women informing clinicians immediately if they are or plan to become pregnant; importance of avoiding pregnancy during therapy;¹¹⁹ ¹²⁸ ²⁴³ importance of using effective nonhormonal contraception while receiving tamoxifen and for 2 months after discontinuing the drug.^a Necessity of advising pregnant patients of the risk to the fetus.¹²⁸

Importance of reading the medication guide; the guide is for women using tamoxifen to lower their risk of breast cancer or with DCIS.¹²⁸

Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs.¹²⁸

Importance of women informing clinicians if they are or plan to breast-feed.¹²⁸

Importance of informing patients of other important precautionary information.¹²⁸ (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Tamoxifen Citrate
Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	Tablets	10 mg (of tamoxifen)*	Nolvadex	AstraZeneca
			Tamoxifen Citrate Tablets	Aegis, Andrx, Barr, Mylan, Roxane, Teva
		20 mg (of tamoxifen)*	Nolvadex	AstraZeneca
			Tamoxifen Citrate Tablets	Aegis, Andrx, Barr, Mylan, Roxane, Teva

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 03/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Nolvadex 20MG Tablets (ASTRAZENECA): 30/$120.99 or 60/$239.98

Tamoxifen Citrate 20MG Tablets (TEVA PHARMACEUTICALS USA): 30/$21.99 or 90/$49.97

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions July 2006. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

References

Only references cited for selected revisions after 1984 are available electronically.

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201. McGuire WL. Adjuvant therapy of node-negative breast cancer. N Engl J Med. 1989; 320:525-7. [PubMed 2915655]

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204. Anon. Tamoxifen for node-negative breast cancer. FDA Drug Bull. 1990; 20:5.

205. Bianco AR, De Placido S, Gallo C et al. Adjuvant therapy with tamoxifen in operable breast cancer. Lancet. 1988; 2:1095-9. [IDIS 247823] [PubMed 2903322]

206. McGuire WL. Adjuvant therapy of node-negative breast cancer: another point of view. J Natl Cancer Inst. 1988; 80:1075-6. [PubMed 3411619]

207. Pritchard KI. Systemic adjuvant therapy for node-negative breast cancer: proven or premature? Ann Intern Med. 1989; 111:1-4. Editorial.

Nizoral

Generic Name: Ketoconazole
Class: Azoles
VA Class: AM700
CAS Number: 65277-42-1

Oral ketoconazole has been associated with hepatoxicity, including some fatalities.²⁶³ Inform patients of the risk and monitor closely.²⁶³

Concomitant use with cisapride or with astemizole or terfenadine (drugs no longer commercially available in the US) is contraindicated.²⁶³ Pharmacokinetic interactions can occur and serious cardiovascular events have been reported with concomitant use.²⁶³ VT, VF, and torsades de pointes have been reported in patients receiving concomitant cisapride; death, VT, and torsades de pointes have been reported in patients receiving concomitant terfenadine.²⁶³ (See Interactions.)

Introduction

Antifungal; azole (imidazole derivative).¹²⁷ ²²²

Uses for Nizoral

Blastomycosis

Treatment of North American blastomycosis caused by Blastomyces dermatitidis.²¹³ ²²⁰ ²³⁴ ²³⁸ ²⁶³ ²⁶⁴ ²⁸⁸ ²⁹⁰ ²⁹¹ ²⁹² ²⁹⁹ ³⁰⁰

Drugs of choice are IV amphotericin B (especially for severe infections and those involving the CNS) or oral itraconazole;²³⁴ ²³⁸ ²⁶⁴ ²⁸⁸ ²⁹⁰ ²⁹² ²⁹⁶ ²⁹⁷ ²⁹⁸ ²⁹⁹ ³³² ³³³ fluconazole and ketoconazole are considered alternatives.²³⁸ ²⁶⁴ ²⁸⁸ ²⁹⁰ ²⁹² ²⁹⁶ ²⁹⁷ ²⁹⁹

Oral ketoconazole usually has been effective when used in immunocompetent individuals with mild to moderate pulmonary or extrapulmonary blastomycosis.²¹³ ²²⁰ ²⁹⁰ ²⁹¹ ²⁹² ²⁹⁷ Consider that treatment failures have been reported when ketoconazole was used for treatment of cutaneous or pulmonary blastomycosis in individuals who had asymptomatic or subclinical CNS involvement at the time of the initial diagnosis.²¹¹ ²⁹⁵ ²⁹⁶ (See Meningitis and Other CNS Infections under Cautions.)

Candida Infections

Treatment of candidiasis, candiduria, chronic mucocutaneous candidiasis, or oropharyngeal and esophageal candidiasis.²¹² ²³⁸ ²⁶³ ²⁷⁹ ²⁹¹ ²⁹² ³²⁰ ³²² ³²³ ³²⁶ ³²⁸ ³²⁹ ³³¹ ³³⁴ ³⁴¹

Has been used for treatment of uncomplicated vulvovaginal candidiasis†.³⁴⁰ ³⁴³ ³⁴⁴ Not a drug of choice for initial treatment; single-dose fluconazole is the only oral regimen included in current CDC recommendations for treatment of uncomplicated vulvovaginal candidiasis.²⁷⁰ ²⁷² Recommended by CDC and others as one of several alternatives for maintenance treatment of recurrent vulvovaginal candidiasis† in women with a history of recurrent infections.²⁷⁰ ²⁷¹ ³⁴⁰ ³⁴³ ³⁴⁴ ³⁴⁶

Chromomycosis

Treatment of chromomycosis (chromoblastomycosis) caused by Phialophora.²⁶³ ²⁸⁸ ³³⁵ A response may not be attained in those with more extensive disease.³³⁵

Optimum regimens for chromomycosis have not been identified.²⁸⁸ ³³⁵ Flucytosine may be a drug of choice used alone or in conjunction with another antifungal (e.g., IV amphotericin B, oral itraconazole, oral ketoconazole).²⁸⁸ ³³⁵

Coccidioidomycosis

Treatment of mild to moderate coccidioidomycosis caused by Coccidioides immitis.²³⁸ ²⁶³ ²⁸⁰ ²⁹⁰ ²⁹¹ ²⁹² ²⁹³ ³⁰³ ³⁰⁴ ³⁰⁵ ³²⁷

Drugs of choice are IV amphotericin B (especially for severe infections and those in immunocompromised patients including HIV-infected individuals) or oral fluconazole; itraconazole and ketoconazole are considered alternatives.²³⁴ ²³⁸ ²⁷⁹ ²⁸⁰ ²⁸⁸ ²⁹⁰ ²⁹² ²⁹³

Dermatophytoses

Treatment of certain dermatophytoses of the skin, scalp, and nails, including tinea capitis (scalp ringworm), tinea corporis (ringworm of the body), tinea cruris (jock itch; groin ringworm), tinea pedis (athlete’s foot, foot ringworm), tinea manuum (hand ringworm), and tinea unguium (onychomycosis; nail ringworm) caused by Epidermophyton, Microsporum, or Trichophyton.²⁶³ ²⁹¹ ³²⁴ ³²⁵

Used for severe recalcitrant cutaneous dermatophyte infections in patients who have not responded to topical therapy or have not responded to or are unable to take other oral antifungals (e.g., griseofulvin).²⁶³

Tinea corporis and tinea cruris generally can be effectively treated using a topical antifungal; an oral antifungal may be necessary if the disease is extensive, dermatophyte folliculitis is present, the infection does not respond to topical therapy, or the patient is immunocompromised or has a coexisting disease.³⁵² ³⁵³ ³⁵⁶ ³⁵⁷ ³⁵⁸ ³⁶⁰ Tinea capitis and tinea barbae generally are treated using an oral antifungal.³²⁵ ³⁵³ ³⁵⁹

While topical antifungals usually are effective for treatment of uncomplicated tinea manuum and tinea pedis,³⁵³ ³⁵⁶ ³⁵⁸ ³⁶⁰ an oral antifungal usually is necessary for treatment of severe, chronic, or recalcitrant tinea pedis, for treatment of chronic moccasin-type (dry-type) tinea pedis, and for treatment of tinea unguium (onychomycosis).³⁵³ ³⁵⁷ ³⁵⁸ ³⁶⁰

Histoplasmosis

Treatment of histoplasmosis caused by Histoplasma capsulatum.²¹³ ²³⁸ ²⁶³ ²⁸⁸ ²⁹⁰ ²⁹¹ ²⁹² ²⁹³ ³⁷⁵

Drugs of choice are IV amphotericin B (especially for life-threatening infections including those in HIV-infected individuals) or oral itraconazole; ketoconazole and fluconazole are considered alternatives.²³⁸ ²⁷⁹ ²⁸⁰ ²⁹⁰ ²⁹¹ ²⁹² ³⁷⁵

Paracoccidioidomycosis

Treatment of paracoccidioidomycosis (South American blastomycosis) caused by Paracoccidioides brasiliensis.²³⁸ ²⁶³ ²⁸⁸ ²⁹¹ ³¹¹ ³³⁵

Drug of choice for initial treatment of severe infections is IV amphotericin B;²³⁸ ²⁸⁸ ²⁹¹ ²⁹³ ³¹⁰ ³¹¹ ³³⁵ oral azole antifungals (e.g., ketoconazole, itraconazole) can be used in patients with less severe infections.²³⁸ ²⁸⁸ ²⁹¹ ³³⁵

Pityriasis (Tinea) Versicolor

Has been effective for treatment of pityriasis (tinea) versicolor†, a superficial infection caused by Malassezia furfur (Pityrosporum orbiculare or P. ovale).²³⁴ ³⁵⁴ ³⁵⁵

Pityriasis (tinea) versicolor generally can be treated topically with an imidazole-derivative azole antifungal (e.g., clotrimazole, econazole, ketoconazole, miconazole, oxiconazole, sulconazole), an allylamine antifungal (e.g., terbinafine), ciclopirox olamine, or certain other topical therapies (e.g., selenium sulfide 2.5%).²³⁴ ³²⁴ ³⁵² ³⁵⁴ ³⁵⁵ ³⁵⁷ An oral antifungal (e.g., itraconazole, ketoconazole) may be indicated, with or without a topical agent, in patients who have extensive or severe infections or who fail to respond to or have frequent relapses with topical therapy.³²⁴ ³⁵⁴ ³⁵⁵ ³⁵⁷

Acanthamoeba Infections

Has been used in conjunction with a topical anti-infective (e.g., miconazole, neomycin, metronidazole, propamidine isethionate) in the treatment of Acanthamoeba keratitis†.¹³⁴ ¹³⁵ ¹³⁶ ¹³⁷ ¹³⁸ ¹³⁹ ¹⁴⁰ ²²⁶ Optimum therapy for Acanthamoeba keratitis remains to be clearly established, but prolonged local and systemic therapy with multiple anti-infectives and often surgical treatment (e.g., penetrating keratoplasty) usually required.¹³⁴ ¹³⁵ ¹³⁶ ¹³⁷ ¹³⁸ ¹³⁹ ¹⁴⁰

A regimen of oral ketoconazole, rifampin, and co-trimoxazole has been used for treatment of chronic Acanthamoeba meningitis† in several immunocompetent children.¹⁸⁷ ²²⁵ (See Meningitis and Other CNS Infections under Cautions.)

Leishmaniasis

Has been used for treatment of cutaneous or mucocutaneous leishmaniasis† caused by various Leishmania spp. (e.g., Leishmania major†, L. mexicana†, L. panamensis†, L. braziliensis†, L. tropica†).²⁰³ ²⁰⁴ ²⁰⁵ ²⁰⁶ ²⁰⁷ ²⁰⁸ ²⁰⁹ ²³⁴ ²⁵⁰ ³¹⁴ ³¹⁶ ³¹⁷ Usual drugs of choice are pentavalent antimony compounds (e.g., sodium stibogluconate or meglumine antimonate [drugs not commercially available in the US]).²²⁵ ²³⁴ ³¹⁷ ³¹⁹ Preferred alternatives or additional drugs of choice are IV amphotericin B (conventional or liposomal formulations) and parenteral pentamidine; other alternatives include oral azole antifungals (e.g., itraconazole, ketoconazole) or topical paromomycin (for cutaneous leishmaniasis when there is a low potential for mucosal spread).²²⁵ ²³⁴ ³¹⁹

Has been used in a limited number of patients for treatment of antimony-resistant visceral leishmaniasis (kala-azar) caused by L. donovani†,²⁶¹ ²⁶² ³¹⁵ ³¹⁷ ³¹⁸ but may be less effective in these infections than in the treatment of cutaneous leishmaniasis.²⁶¹ ²⁶² ³¹⁷ Usual drugs of choice for initial treatment of visceral leishmaniasis are pentavalent antimony compounds, but resistance and treatment failures are becoming increasingly common;²⁸⁸ ³¹⁷ IV amphotericin B and pentamidine are considered alternatives.²⁸⁸ ³¹⁷ ³¹⁹

Prostate Cancer

Because of ketoconazole’s ability to inhibit testicular and adrenal steroid synthesis, the drug has been used in the treatment of advanced prostatic carcinoma†.¹⁰⁶ ¹⁰⁷ ¹⁰⁸ ¹⁵¹ ¹⁷⁹ ¹⁸⁰ ¹⁸¹ ¹⁸² ¹⁸³ ¹⁸⁴ ²⁸⁴ ²⁸⁵ ²⁸⁶ ³⁶⁸ ³⁶⁹

Cushing’s Syndrome

Has been used effectively for palliative treatment of Cushing’s syndrome† (hypercortisolism), including adrenocortical hyperfunction associated with adrenal or pituitary adenoma or ectopic corticotropin-secreting tumors.¹¹² ¹¹³ ¹¹⁴ ¹⁵¹ ¹⁵⁴ ²²⁴ ³⁴²

Has been used in a limited number of geriatric patients ≥75 years of age for treatment of corticotropin-dependent Cushing’s syndrome; may provide an effective alternative in patients who cannot tolerate surgical treatment.³⁴²

Hirsutism and Precocious Puberty

Has been used with some success in a limited number of patients for treatment of dysfunctional hirsutism†.¹¹⁵ ³⁷⁰

Has been used in a limited number of boys for treatment of precocious puberty†.¹¹⁶ ¹⁸⁵ ¹⁸⁶

Hypercalcemia

Has been used with some success for treatment of hypercalcemia in adults with sarcoidosis†.³⁶³ ³⁶⁴ ³⁶⁵ ³⁶⁶ Has reduced serum calcium concentrations in some, but not all, patients with sarcoidosis-associated hypercalcemia;³⁶⁴ ³⁶⁵ ³⁶⁶ hypercalcemia and increased serum 1,25-dihydroxyvitamin D concentrations may recur when ketoconazole dosage is decreased or the drug discontinued.³⁶⁵ ³⁶⁶

Has been effective in a few adolescents for treatment of tuberculosis-associated hypercalcemia†.³⁶⁷

Nizoral Dosage and Administration

Administration

Oral Administration

Administer orally.²⁶³

To ensure absorption in patients with achlorhydria, each 200-mg ketoconazole tablet should be dissolved in 4 mL of 0.2N hydrochloric acid solution²⁶³ or taken with 200 mL of 0.1N hydrochloric acid.^a The resultant solution should be administered via a plastic or glass straw to avoid contact with the teeth, and a glass of water should be administered immediately after the solution.²⁶³ Alternatively, some clinicians recommend that each 200 mg of ketoconazole be given with ≥680 mg of glutamic acid hydrochloride.¹⁹⁸ ¹⁹⁹ Other clinicians suggest that each 200 mg of ketoconazole be administered with an acidic beverage (e.g., Coca-Cola, Pepsi)²⁷³ or the dose dissolved in 60 mL of citrus juice to ensure absorption; however, this strategy may not be adequate in all patients with achlorhydria and patients should be monitored closely for therapeutic failure.²⁷³

Dosage

Pediatric Patients

General Pediatric Dosage

Treatment of Fungal Infections

Oral

Children >2 years of age: 3.3–6.6 mg/kg once daily has been used.²³⁴ ²⁶³

Adults

General Adult Dosage

Treatment of Fungal Infections

Oral

200 mg once daily.²⁶³ Dosage may be increased to 400 mg once daily for severe infections or if the expected clinical response is not achieved.²⁶³

Blastomycosis

Oral

Some clinicians suggest 400 mg once or twice daily.²¹³ ²²⁰ ²³⁸ ²⁸⁸ ²⁹⁰ ²⁹² ²⁹⁶ ²⁹⁹ ³⁰¹ ³²⁷ ³⁷⁵ Treatment usually continued for 6–12 months.^a

Candidiasis

Oropharyngeal and Esophageal Candidiasis

Oral

200–400 mg daily.²³⁸ ²⁷⁹

Vulvovaginal Candidiasis†

Oral

Treatment of uncomplicated vulvovaginal candidiasis† in nonpregnant women: 200–400 mg twice daily for 5 days.³⁴⁰ ³⁴³ ³⁴⁴

When used as a maintenance regimen to reduce the frequency of recurrent episodes of vulvovaginal candidiasis† in women who have received an initial intensive antifungal regimen (i.e., 7–14 days of an intravaginal azole antifungal or a 2-dose fluconazole regimen), ketoconazole has been given in a dosage of 100 mg once daily for up to 6 months.²⁷⁰ ³⁴⁰ ³⁴¹ ³⁴³ ³⁴⁴ ³⁴⁶

Chromomycosis

Oral

200–400 mg daily.³³⁵ Treatment usually continued for 6–12 months.

Coccidioidomycosis

Oral

400 mg once or twice daily.²¹³ ²²⁰ ²³⁸ ²⁸⁸ ²⁹⁰ ²⁹² ²⁹⁶ ²⁹⁹ ³⁰¹ ³²⁷ ³⁷⁵ Treatment usually continued for 6–12 months.

Dermatophytoses

Oral

200–400 mg daily has been given for 1–2 months.^a Infections involving glabrous skin require a minimum of 4 weeks of treatment; palmar and plantar infections may respond more slowly.²⁶³ Tinea unguium (onychomycosis) may require ≥6–12 months of treatment.^a

Histoplasmosis

Oral

400 mg once or twice daily.²¹³ ²²⁰ ²³⁸ ²⁸⁸ ²⁹⁰ ²⁹² ²⁹⁶ ²⁹⁹ ³⁰¹ ³²⁷ ³⁷⁵ A dosage of 200 mg once or twice daily also has been used.³⁷⁵

A minimum of 6 months of therapy usually required, but 2–6 months has been effective in some patients.^a

Paracocciodioidomycosis

Oral

200–400 mg daily.³³⁵

A minimum of 6 months of therapy usually required, but 2–6 months has been effective in some patients.^a

Leishmaniasis†

Cutaneous and Mucocutaneous Leishmaniasis†

Oral

400–600 mg daily for 4–8 weeks has been used.²⁰³ ²⁰⁴ ²⁰⁷ ²⁰⁸ ³¹⁷

Visceral Leishmaniasis (Kala-Azar)†

Oral

400–600 mg daily for 4–8 weeks has been used.³¹⁵ ³¹⁷ ³¹⁸

Prostate Cancer†

Oral

400 mg every 8 hours has been used for treatment of prostatic carcinoma†¹⁰⁶ ¹⁰⁸ ¹⁸⁰ ¹⁸¹ ¹⁸² ¹⁸³ ²⁸⁵ or as an adjunct in the management of disseminated intravascular coagulation (DIC) associated with prostatic carcinoma†.¹⁵² ¹⁷⁸ Risk of depressed adrenocortical function at this high dosage should be considered.²⁶³ (See Endocrine and Metabolic Effects under Cautions.)

Cautions for Nizoral

Contraindications

Hypersensitivity to ketoconazole.²⁶³

Concomitant use with certain drugs metabolized by CYP3A4 isoenzymes (e.g., astemizole [no longer commercially available in the US], cisapride, midazolam, terfenadine [no longer commercially available in the US], triazolam).²⁶³ (See Specific Drugs under Interactions.)

Warnings/Precautions

Warnings

Hepatic Effects

Hepatotoxicity (usually the hepatocellular type) has been reported.¹⁶⁴ ¹⁶⁵ ¹⁶⁶ ¹⁶⁷ ¹⁶⁸ ¹⁶⁹ ¹⁷⁰ ¹⁹¹ ¹⁹² ¹⁹³ ²⁶³

Symptomatic hepatotoxicity usually is apparent within the first few months of ketoconazole therapy (median 28 days),⁵⁰ ⁶¹ ¹⁶⁴ ¹⁶⁷ ¹⁶⁸ ¹⁶⁹ ¹⁷⁰ ¹⁸⁸ ¹⁸⁹ ¹⁹⁰ ¹⁹¹ ¹⁹² ²⁶³ but occasionally may be apparent within 3–7 days of initiation of therapy.¹⁶⁴ ¹⁶⁶ ¹⁶⁷ ¹⁹¹ ¹⁹² ²⁶³ Although ketoconazole-induced hepatotoxicity usually is reversible following discontinuance of the drug,⁵⁰ ¹⁶⁴ ¹⁶⁵ ¹⁶⁶ ¹⁶⁷ ¹⁸⁸ ¹⁸⁹ ¹⁹⁰ ¹⁹¹ ¹⁹² ²⁶³ recovery may take several months;¹⁶⁴ ¹⁶⁵ ¹⁶⁷ ¹⁸⁸ ¹⁹⁰ ²⁶³ rarely, death has occurred.¹⁶⁴ ¹⁶⁵ ¹⁶⁷ ¹⁶⁸ ¹⁶⁹ ¹⁷⁰ ¹⁹¹ ¹⁹² ¹⁹³ ²⁶³

Most cases of hepatotoxicity have been reported in patients receiving the drug for tinea unguium (onychomycosis);⁵⁰ ¹⁶⁷ ¹⁶⁸ ¹⁶⁹ ¹⁸⁸ ¹⁸⁹ ¹⁹⁰ ¹⁹¹ ¹⁹² ¹⁹³ ²⁶³ many others were receiving the drug for chronic, refractory dermatophytoses.¹⁶⁷ ¹⁹¹ ¹⁹² Several cases of ketoconazole-induced hepatitis have been reported in children.¹⁶⁵ ¹⁶⁷ ¹⁸⁹ ¹⁹¹ ¹⁹² ²⁶³

Monitor closely for clinical and biochemical signs of hepatotoxicity.¹⁶⁴ ¹⁶⁶ ¹⁶⁷ ¹⁶⁹ ¹⁷⁰ ¹⁹² ²⁶³ Perform liver function tests (e.g., serum AST, ALT, alkaline phosphatase, γ-glutamyltransferase [γ-glutamyltranspeptidase, GGT, GGTP], bilirubin) prior to and frequently (e.g., biweekly during the first 2 months of therapy and monthly or bimonthly thereafter) during therapy, particularly in those receiving prolonged therapy, those receiving other potentially hepatotoxic drugs, and those with a history of hepatic disease.¹⁶⁴ ¹⁶⁶ ¹⁶⁷ ¹⁶⁹ ¹⁷⁰ ¹⁸⁸ ¹⁸⁹ ¹⁹⁰ ¹⁹³ ²⁶³

Minor, asymptomatic elevations in liver function test results may return to pretreatment concentrations during continued ketoconazole therapy.¹⁶⁴ ¹⁶⁷ ¹⁹¹ ¹⁹² ¹⁹³ If liver function test results are substantially elevated or if such abnormalities persist, worsen, or are accompanied by other manifestations of hepatic dysfunction, ketoconazole should be discontinued.¹⁶⁴ ¹⁶⁷ ¹⁶⁸ ¹⁶⁹ ¹⁷⁰ ¹⁸⁹ ¹⁹⁰ ¹⁹¹ ¹⁹²

Sensitivity Reactions

Hypersensitivity Reactions

Anaphylaxis and urticaria reported rarely.¹⁰² ²⁶³

General Precautions

Endocrine and Metabolic Effects

Ketoconazole can inhibit testosterone synthesis and transient decreases in serum testosterone may occur;¹⁰⁹ ¹¹⁰ ¹⁵¹ ¹⁷⁴ ²⁶³ concentrations usually return to baseline values after the drug is discontinued.²⁶³ Testosterone concentrations are impaired with ketoconazole dosage of 800 mg daily and abolished with dosage of 1.6 g daily.²⁶³

Ketoconazole may inhibit cortisol synthesis, particularly in patients receiving relatively high daily dosage or divided daily dosing.¹⁰⁹ ¹¹² ¹¹³ ¹¹⁴ ¹⁵¹ ¹⁵⁴ ¹⁵⁶ ¹⁵⁷ ¹⁵⁸ ¹⁵⁹ ¹⁶⁶ ¹⁷³ ¹⁹² ²²⁹ ²³⁰ The adrenocortical response to corticotropin (ACTH) may be at least transiently diminished and a reduction in urinary free and serum cortisol concentrations may occur.¹⁰⁹ ¹¹⁰ ¹¹² ¹¹³ ¹¹⁴ ¹⁵¹ ¹⁵⁴ ¹⁵⁶ ¹⁵⁷ ¹⁵⁸ ¹⁵⁹ ¹⁶⁶ ¹⁷³ ¹⁹² Adrenocortical insufficiency has been reported only rarely.¹⁰⁹ ¹⁵⁹ ¹⁶⁰ ¹⁶⁶ ¹⁷³ ¹⁹² ²²⁹ Adrenocortical hypofunction generally is reversible following discontinuance of the drug,¹⁵⁴ ¹⁵⁶ ¹⁵⁷ ¹⁶⁶ but rarely may be persistent.¹⁵⁹

To minimize the risk of possible endocrine and metabolic effects, dosages greater than those usually recommended should not be used.²⁶³

Meningitis and Other CNS Infections

Because CSF concentrations of ketoconazole are unpredictable following oral administration, the drug should not be used alone to treat CNS fungal infections, including candidal, coccidioidal, or cryptococcal meningitis.²⁶³ ²⁹¹ ³⁰² ³³⁰

Specific Populations

Pregnancy

Category C.²⁶³

Lactation

Probably distributed into human milk.²⁶³ Discontinue nursing or the drug.²⁶³

Pediatric Use

Use in pediatric patients only when potential benefits justify possible risks.²⁶³ Has not been systematically studied in children of any age,²⁶³ but has been used in a limited number of children >2 years of age.²⁶³ There is essentially no information available to date on use in children <2 years of age.²⁶³

Common Adverse Effects

GI effects (nausea, vomiting), hepatic effects, pruritus.²⁶³

Interactions for Nizoral

Inhibits CYP3A4.²⁶³

Drugs Metabolized by Hepatic Microsomal Enzymes

Pharmacokinetic interactions likely with drugs that are substrates of CYP3A4.²⁶³

Hepatotoxic Drugs

Monitor closely if used concomitantly with other potentially hepatotoxic drugs, especially in patients requiring prolonged therapy or with a history of liver disease.²⁶³ (See Hepatic Effects under Cautions.)

Specific Drugs

Drug	Interaction	Comments
Alcohol	Disulfiram reactions (flushing, rash, peripheral edema, nausea, headache) have occurred rarely in patients who ingested alcohol while receiving ketoconazole;²⁶³ ²⁶⁷ ²⁶⁸ usually resolved within a few hours²⁶³	Some clinicians recommend that alcohol be avoided during and for 48 hours after discontinuance of ketoconazole therapy²⁶⁷
Antacids	Because gastric acidity is necessary for dissolution and absorption of ketoconazole, concomitant administration of antacids may decrease absorption of the antifungal²⁶³	Administer antacids at least 2 hours after ketoconazole²⁶³
Anticoagulants, oral (warfarin)	Possible enhanced anticoagulant effects²⁶³	Monitor PT or other appropriate tests closely; adjust anticoagulant dosage if necessary²⁶³
Anticonvulsants (phenytoin)	Possible pharmacokinetic interaction with changes in metabolism of one or both drugs²⁶³	Monitor serum concentrations if used concomitantly²⁶³
Antidiabetic agents, sulfonylureas	Increased plasma concentrations of the antidiabetic agent and symptoms of hypoglycemia reported with other azoles (e.g., itraconazole)²⁶³ ^b	Consider the possibility that hypoglycemia may occur when ketoconazole used concomitantly with antidiabetic agents²⁶³
Antihistamines (astemizole, loratadine, terfenadine)	Aztemizole and terfenadine (drugs no longer commercially available in the US): Pharmacokinetic interaction and potential for serious or life-threatening reactions (e.g., cardiac arrhythmias, prolonged QT interval)²⁵² ²⁵³ ²⁵⁴ ²⁵⁵ ²⁵⁶ ²⁵⁷ ²⁵⁹ ²⁶⁰ ²⁶³ ²⁸⁷ Loratadine: Increased plasma concentrations and AUCs of loratadine and its active metabolite, but no evidence of changes in QT interval or incidence of adverse effects²⁶³	Aztemizole and terfenadine: Concomitant use contraindicated²⁵² ²⁵⁴ ²⁶³ ²⁶⁵
Antimycobacterials (rifampin, isoniazid)	Rifampin: Decreased serum concentrations of ketoconazole¹¹¹ ¹⁴¹ ²²¹ ²⁶³ Isoniazid: May affect ketoconazole serum concentrations¹¹¹ ²⁶³	Do not use concomitantly with rifampin or isoniazid²⁶³
Benzodiazepines (midazolam, triazolam)	Increased plasma concentrations of midazolam or triazolam; possible prolonged sedative and hypnotic effects of the drugs²⁶³	Ketoconazole should not be used concomitantly with midazolam or triazolam²⁶³ Special precaution is required if parenteral midazolam is used in patients receiving ketoconazole because the sedative effects of midazolam may be prolonged²⁶³
Cisapride	Increased cisapride plasma concentrations and increased risk of adverse effects (e.g., cardiovascular effects)²⁶³ ²⁷⁶	Concomitant use contraindicated²⁶³
Digoxin	Increased plasma concentrations of digoxin reported; causative relationship unclear²⁶³	Closely monitor digoxin concentrations in patients receiving ketoconazole²⁶³
Histamine H₂-receptor antagonists (e.g., cimetidine, ranitidine)	Because gastric acidity is necessary for dissolution and absorption of ketoconazole, concomitant administration of histamine H₂-receptor antagonists may decrease absorption of the antifungal ²⁶³	Administer H₂-receptor antagonist at least 2 hours after ketoconazole²⁶³
Immunosuppressive agents (cyclosporine, methylprednisolone, prednisone, tacrolimus)	Cyclosporine or tacrolimus: Increased concentrations of the immunosuppressive agent¹⁴² ¹⁴³ ¹⁴⁴ ²⁶³ ³⁷² Methylprednisolone or prednisone: Increased concentrations of the corticosteroid and possible enhanced adrenal suppression²²⁷ ²²⁸ ²³² ²³³	Cyclosporine or tacrolimus: Use with caution and monitor concentrations of the immunosuppressive agent if possible; adjust cyclosporine or tacrolimus dosage if needed when ketoconazole is initiated or discontinued¹⁴⁶ ²⁶³ Methylprednisolone or prednisolone: Adjust dosage of the corticosteroid as needed²²⁷ ²²⁸ ²⁶³
Paclitaxel	In vitro evidence that ketoconazole can inhibit metabolism of paclitaxel²⁶⁹	Clinical importance unclear; use concomitantly with caution²⁶⁹
Sucralfate	Possible decreased absorption of ketoconazole³⁶²	Administer sucralfate at least 2 hours after ketoconazole³⁶²
Theophylline	Conflicting data;¹⁴⁷ ¹⁵⁰ possible decreased theophylline concentrations¹⁴⁷	Pending further accumulation of data, monitor serum theophylline concentrations and adjust theophylline dosage if necessary when ketoconazole is initiated or discontinued in patients receiving theophylline¹⁴⁷

Nizoral Pharmacokinetics

Absorption

Bioavailability

Rapidly absorbed from GI tract;¹⁶² ¹⁶³ peak plasma concentrations attained within 1–2 hours.¹⁴⁹ ¹⁶² ²⁶³

Ketoconazole must be dissolved in gastric secretions and converted to the hydrochloride salt prior to absorption from the stomach.^a Bioavailability depends on the pH of the gastric contents in the stomach; an increase in pH results in decreased absorption of the drug.^a (See Absorption: Special Populations.)

Food

Effect of food on rate and extent of GI absorption of ketoconazole has not been clearly determined.¹⁶²

Plasma Concentrations

Considerable interindividual variations in peak plasma concentrations and AUCs have been reported.^a

Special Populations

Oral bioavailability may be decreased in patients with achlorhydria,^a including those with HIV-associated gastric hypochlorhydria.¹⁹⁸ ²⁰⁰ Concomitant administration of dilute hydrochloric acid solution usually normalizes absorption of the drug in these patients.¹⁹⁸ Concomitant administration of an acidic beverage may increase bioavailability in some individuals.²⁷³ (See Oral Administration under Dosage and Administration.)

Distribution

Extent

Distributed into urine, bile, saliva, sebum, cerumen, and synovial fluid.^a

May be distributed into CSF following oral administration, but CNS penetration is unpredictable and has generally been considered to be minimal.^a

Not known whether crosses the placenta in humans; crosses the placenta in rats.^a Distributed into milk of dogs; probably distributed into human milk.^a

Plasma Protein Binding

84–99% bound to plasma proteins, primarily albumin.²⁶³ ^a

Elimination

Metabolism

Partially metabolized in the liver to several inactive metabolites by oxidation and degradation of the imidazole and piperazine rings, by oxidative O-dealkylation, and by aromatic hydroxylation.^a

Elimination Route

Major route of elimination of ketoconazole and its metabolites appears to be excretion into the feces via the bile.^a

In fasting adults with normal renal function, approximately 57% of a single 200-mg oral dose is excreted in feces within 4 days (20–65% of this is unchanged drug); approximately 13% of the dose is excreted in urine within 4 days (2–4% of this is unchanged drug).^a

Half-life

Plasma concentrations appear to decline in a biphasic manner with a half-life of approximately 2 hours in the initial phase and 8 hours in the terminal phase.²⁶³

Special Populations

Plasma concentrations and half-life not substantially affected by renal or hep

Tuesday, September 27, 2016

Nix Lice Control

What is Nix Lice Control (permethrin topical)?

What is the most important information I should know about Nix Lice Control (permethrin topical)?

What should I discuss with my healthcare provider before using Nix Lice Control (permethrin topical)?

How should I use Nix Lice Control (permethrin topical)?

What happens if I miss a dose?

What happens if I overdose?

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Nix Lice Control (permethrin topical) side effects

What other drugs will affect Nix Lice Control (permethrin topical)?

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Nizoral A-D Topical

Commonly used brand name(s)

Uses For Nizoral A-D

Before Using Nizoral A-D

Allergies

Pediatric

Geriatric

Pregnancy

Breast Feeding

Interactions with Medicines

Interactions with Food/Tobacco/Alcohol

Proper Use of ketoconazole

Dosing

Missed Dose

Storage

Precautions While Using Nizoral A-D

Nizoral A-D Side Effects

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Nolvadex

Introduction

Uses for Nolvadex

Breast Cancer

Albright’s Syndrome

Nolvadex Dosage and Administration

General

Administration

Dosage

Adults

Breast Cancer

Adjuvant Therapy

Ductal Carcinoma in Situ

Metastatic Breast Cancer

Reduction in the Incidence of Breast Cancer in Women at High Risk

Prescribing Limits

Adults

Breast Cancer

Adjuvant Therapy

Cautions for Nolvadex

Contraindications

Warnings/Precautions

Warnings

Hypercalcemia

Effects on the Uterus

Cardiovascular Effects

Hepatic Effects

Ocular Effects

Fetal/Neonatal Morbidity and Mortality

General Precautions

Hematologic Effects

Specific Populations

Pregnancy

Lactation

Pediatric Use

Geriatric Use

Common Adverse Effects

Interactions for Nolvadex

Cytotoxic Agents

Specific Drugs

Nolvadex Pharmacokinetics

Absorption

Bioavailability

Plasma Concentrations

Distribution

Extent

Elimination