Ketoconazole did not show any signs of mutagenic potential when evaluated using the dominant lethal mutation test or the Ames Salmonella microsomal activator assay. Ketoconazole was not carcinogenic in an 18-month, oral study in Swiss albino mice or a 24-month oral carcinogenicity study in Wistar rats at dose levels of 5, 20 and 80 mg/kg/ day. The high dose in these studies was approximately 1× (mouse) or 2× (rat) the clinical dose in humans based on a mg/m2 comparison.
Ketoconazole has been shown to be teratogenic (syndactylia and oligodactylia) in the rat when given in the diet at 80 mg/kg/day (2 times the maximum recommended human dose, based on body surface area comparisons). However, these effects may be related to maternal toxicity, evidence of which also was seen at this and higher dose levels.
There are no adequate and well controlled studies in pregnant women. Ketoconazole tablets should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Ketoconazole has also been found to be embryotoxic in the rat when given in the diet at doses higher than 80 mg/kg during the first trimester of gestation.
In addition, dystocia (difficult labor) was noted in rats administered oral ketoconazole during the third trimester of gestation. This occurred when ketoconazole was administered at doses higher than 10 mg/kg (about one fourth the maximum human dose, based on body surface area comparison).
Ketoconazole has been shown to be excreted in the milk. Mothers who are under treatment with ketoconazole tablets should not breast feed.
Ketoconazole tablets have not been systematically studied in children of any age, and essentially no information is available on children under 2 years. Ketoconazole tablets should not be used in pediatric patients unless the potential benefit outweighs the risks.
Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
The following adverse reactions were reported in clinical trials:
Immune System Disorders: anaphylactoid reaction
Endocrine Disorders: gynecomastia
Metabolism and Nutrition Disorders: alcohol intolerance, anorexia, hyperlipidemia, increased appetite
Psychiatric Disorders: insomnia, nervousness
Nervous System Disorders: headache, dizziness, paresthesia, somnolence
Eye Disorders: photophobia
Vascular Disorders: orthostatic hypotension
Respiratory, Thoracic and Mediastinal Disorders: epistaxis
Gastrointestinal Disorders: vomiting, diarrhea, nausea, constipation, abdominal pain, abdominal pain upper, dry mouth, dysgeusia, dyspepsia, flatulence, tongue discoloration
Hepatobiliary Disorders: hepatitis, jaundice, hepatic function abnormal
Skin and Subcutaneous Tissues Disorders: erythema multiforme, rash, dermatitis, erythema, urticaria, pruritus, alopecia, xeroderma
Musculoskeletal and Connective Tissue Disorders: myalgia
Reproductive System and Breast Disorders: menstrual disorder
General Disorders and Administration Site Conditions: asthenia, fatigue, hot flush, malaise, edema peripheral, pyrexia, chills
Investigations: platelet count decreased.
The following adverse reactions have been identified during postapproval use of ketoconazole tablets. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.
The following adverse reactions were reported during post-marketing experience:
Blood and Lymphatic System Disorders: thrombocytopenia
Immune System Disorders: allergic conditions including anaphylactic shock, anaphylactic reaction, angioneurotic edema
Endocrine Disorders: adrenocortical insufficiency
Nervous System Disorders: reversible intracranial pressure increased (e.g. papilloedema, fontanelle bulging in infants)
Hepatobiliary Disorders: serious hepatotoxicity including hepatitis cholestatic, biopsyconfirmed hepatic necrosis, cirrhosis, hepatic failure including cases resulting in transplantation or death
Skin and Subcutaneous Tissue Disorders: acute generalized exanthematous pustulosis, photosensitivity
Musculoskeletal and Connective Tissue Disorders: arthralgia
Reproductive System and Breast Disorders: erectile dysfunction; with doses higher than the recommended therapeutic dose of 200 or 400mg daily, azoospermia.
In the event of acute accidental overdose, treatment consists of supportive and symptomatic measures. Within the first hour after ingestion, activated charcoal may be administered.
There should be laboratory as well as clinical documentation of infection prior to starting ketoconazole therapy. The usual duration of therapy for systemic infection is 6 months. Treatment should be continued until active fungal infection has subsided.
The recommended starting dose of ketoconazole tablets is a single daily administration of 200 mg (one tablet). If clinical responsiveness is insufficient within the expected time, the dose of ketoconazole tablets may be increased to 400 mg (two tablets) once daily.
In small numbers of children over 2 years of age, a single daily dose of 3.3 to 6.6 mg/kg has been used. Ketoconazole tablets have not been studied in children under 2 years of age.
Ketoconazole tablets USP, 200 mg are white to off-white round, flat tablets, one side scored and engraved with “T” above the score and “57″ below the score. The other side is plain. They are supplied in bottles of 30 tablets (NDC 33261-0739-30).
Store at 20°- 25°C (68°- 77°F) [See USP Controlled Room Temperature].
Protect from moisture.
Keep out of reach of children.
Mfd. by: Taro Pharmaceutical Industries Ltd., Haifa Bay, Israel 26110
Dist. by: Taro Pharmaceuticals U.S.A., Inc. , Hawthorne, NY 10532
Repackaged By :
Aidarex Pharmaceuticals LLC,
Corona, CA 92880
Revised: August, 2013
MEDICATION GUIDE Ketoconazole Tablets USP, 200 mg
What is the most important information I should know about ketoconazole tablets USP?
Ketoconazole tablets is not the only medicine available to treat fungal infections and should only be used when other medicines are not right for you. Talk to your healthcare provider to find out if ketoconazole tablets are right for you.
Ketoconazole tablets USP can cause serious side effects, including:
- liver problems (hepatotoxicity). Some people who were treated with ketoconazole the active ingredient in ketoconazole tablets, had serious liver problems that led to death or the need for a liver transplant. Call your healthcare provider right away if you have any of the following symptoms:
- loss of appetite or start losing weight (anorexia)
- nausea or vomiting
- feel tired
- stomach pain or tenderness
- dark urine or light colored stools
- yellowing of your skin or the whites of your eyes
- fever or rash
- changes in the electrical activity of your heart called QT prolongation. QT prolongation can cause irregular heart beats that can be life threatening. This can happen when ketoconazole tablets are taken with certain medicines, such as dofetilide, quinidine, pimozide, and cisapride. Talk to your healthcare provider about other medicines you are taking before you start taking ketoconazole tablets. Tell your healthcare provider right away if you feel faint, lightheaded, dizzy, or feel your heart beating irregularly or fast. These may be symptoms related to QT prolongation.
What are ketoconazole tablets USP?
- Ketoconazole tablets are prescription medicine used to treat serious fungal infections including: blastomycosis, coccidioidomycosis, histoplasmosis, chromomycosis, and paracoccidioidomycosis.
- Ketoconazole tablets are not for people with fungal nail infections.
- Ketoconazole tablets have not been approved for the treatment of advanced prostate cancer or Cushing’s syndrome. The safety and efficacy have not been established.
- Ketoconazole tablets should only be used in children if prescribed by the healthcare provider who has determined that the benefits outweigh the risks.
Who should not take ketoconazole tablets USP?
- Do not take ketoconazole tablets if you:
- have liver problems
- take simvastatin, and lovastatin. Ketoconazole tablets when taken with these medicines may cause muscle problems.
- take eplerenone, dihydroergotamine, ergotamine, and nisoldipine.
- take triazolam, midazolam, or alprazolam. Taking ketoconazole tablets with these medicines may make you very drowsy and make your drowsiness last longer.
- are allergic to ketoconazole or any of the ingredients in ketoconazole tablets. See the end of this Medication Guide for a complete list of ingredients in ketoconazole tablets.
Before you take ketoconazole tablets USP, tell your healthcare provider if you:
- have had an abnormal heart rhythm tracing (ECG) or anyone in your family have or have had a heart problem called “congenital long QT syndrome”.
- have adrenal insufficiency.
- are pregnant or plan to become pregnant. It is not known if ketoconazole tablets will harm your unborn baby.
- are breastfeeding or plan to breastfeed. Ketoconazole tablets can pass into your breast milk. You and your healthcare provider should decide if you will take ketoconazole tablets or breastfeed. You should NOT do both.
Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.
Using ketoconazole tablets with certain other medicines may affect each other. Using ketoconazole tablets with other medicines can cause serious side effects.
How should I take ketoconazole tablets USP?
- Take ketoconazole tablets 1 time each day.
- Do not stop taking ketoconazole tablets without first talking to your healthcare provider.
What should I avoid while taking ketoconazole tablets USP?
- Do not drink alcohol while taking ketoconazole tablets.
What are the possible side effects of ketoconazole tablets USP?
Ketoconazole tablets may cause serious side effects, including:
- See “What is the most important information I should know about ketoconazole tablets USP?”
- adrenal insufficiency. Adrenal insufficiency is a condition in which the adrenal glands do not make enough steroid hormones. Ketoconazole tablets may cause adrenal insufficiency if you take a high dose. Your healthcare provider will follow you closely if you have adrenal insufficiency or if you are taking prednisone or other similar medicines for long periods of time. Call your healthcare provider right away if you have symptoms of adrenal insufficiency such as tiredness, weakness, dizziness, nausea, and vomiting.
- serious allergic reactions. Some people can have a serious allergic reaction to ketoconazole tablets. Stop taking ketoconazole tablets and go to the nearest hospital emergency room right away if you get a rash, itching, hives, fever, swelling of the lips or tongue, chest pain, or have trouble breathing. These could be signs of a serious allergic reaction.
- muscle problems. Taking certain medicines with ketoconazole tablets may cause muscle problems. See “Who should not take ketoconazole tablets USP?”
The most common side effects of ketoconazole tablets include nausea, headache, diarrhea, stomach pain, and abnormal liver function tests.
These are not all the possible side effects of ketoconazole tablets. For more information, ask your healthcare provider or pharmacist.
Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
How should I store ketoconazole tablets USP?
- Store ketoconazole tablets at room temperature between 68°F to 77°F (20°C to 25°C).
- Keep ketoconazole tablets dry.
General information about the safe and effective use of ketoconazole tablets USP.
Medications are sometimes prescribed for purposes other than those listed in a Medication Guide. Do not use ketoconazole tablets for a condition for which it was not prescribed. Do not give ketoconazole tablets to other people, even if they have the same symptoms that you have. It may harm them.
This Medication Guide summarizes the most important information about ketoconazole tablets.
If you would like more information, talk to your healthcare provider. You can ask your pharmacist or healthcare provider for information about ketoconazole tablets that is written for health professionals.
What are the ingredients in ketoconazole tablets USP, 200 mg?
Active ingredient: ketoconazole.
Inactive ingredients: colloidal silicon dioxide, corn starch, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and povidone.
This Medication Guide has been approved by the U.S. Food and Drug Administration
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