(kee toe kon' na zole)
P Â - Caution when used during pregnancy
L Â - Caution when used during lactation
|Indication & Dosage||Oral
Adult:Â 200 mg once daily. Increase to 400 mg once daily if clinical response is insufficient. Treatment duration: 14 days and for at least 1 wk after symptoms have cleared and cultures have become negative.
Child:Â â‰¥2 yr: 3.3-6.6 mg/kg daily as a single dose. Treatment duration: 1-2 wk forÂ candidiasis; at least 4 wk in recalcitrnt dermatophyte infections and up to 6 mth for otherÂ systemic mycoses.Â
ChronicÂ vaginal candidiasis
Adult:Â 400 mg once daily for 5 days.
Adult:Â As 2% cream: Apply to the affected area bid for 4 wk or until clinical clearing. As 2% foam: Apply to the affected area bid for 4 wk. As 1 or 2% shampoo: Apply on the scalp twice wkly for 2-4 wk; continue for a few days until symptoms disappear. For prophylaxis: 2% shampoo is used once every 1-2 wk.
Skin fungal infections
Adult:Â As 2% cream: Apply 1-2 times daily to cover affected and surrounding area until at least a few days after disappearance of symptoms. For treatment of pityriasis versicolor: As 2% shampoo: Apply on the skin once daily for up to 5 days. For prophylaxis: 2% shampoo is used once daily for a max of 3 days before exposure to sunshine.Â
Adult:Â As 2% cream: Apply 1-2 times daily to cover affected and surrounding area until at least a few days after disappearance of symptoms. For treatment of pityriasis versicolor: As 2% shampoo: Apply on the skin once daily for up to 5 days. For prophylaxis: 2% shampoo is used once daily for a max of 3 days before exposure to sunshine.
|Administration||Should be taken with
|Contraindications||Hypersensitivity; preexisting liver disease, porphyria. Concurrent use with cisapride, terfenadine or astemizole.|
|Special Precautions||Hepatic impairment; monitor liver function regularly. Pregnancy, lactation. Predisposition to adrenocortical insufficiency. Discontinue treatment if there is persistent or worsening of liver enzyme elevation.|
|Adverse Drug Reactions||GI disturbances e.g. nausea and vomiting; rash, dermatitis,
burning sensation, pruritus; headache, dizziness, somnolence, fever and chills; thrombocytopenia; gynaecomastia, impotence; raised intracranial pressure;
photophobia; transient elevations in LFTs.
Potentially Fatal:Â Hepatotoxicity.
|Drug Interactions||Reduced absorption with antimuscarinics, antacids, H2-blockers, PPIs, sucralfate. Reduced plasma concentrations with rifampicin,
isoniazid, efavirenz, nevirapine or phenytoin. May reduce concentrations of isoniazid and rifampicin. May increase plasma concentrations of CYP3A4 substrates
such as benzodiazepines, mirtazapine, nefazodone, tacrolimus, oral anticoagulants, rosiglitazone, sertindole, sildenafil. Disulfiram-like reaction with
alcohol. May reduce efficacy of oral contraceptives. Avoid concurrent use with clopidogrel.
Potentially Fatal:Â Increased risk of cardiac arrhythmias with astemizole, cisapride, pimozide, quinidine or nilotinib. May reduce metabolism of conviptan; avoid concurrent usage. Increased risk of dofetilide toxicity when used together.Â Please consult detailed drug interactions before prescribing.
|Pregnancy Category (US FDA)||Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.|
|Storage||Oral:Â Store at 15-25Â°C (59-77Â°F).Â Topical/Cutaneous:Â Store below 25Â°C (77Â°F).|
|Pharmacology||Ketoconazole interferes with biosynthesis of triglycerides and phopholipids by blocking fungal cytochrome P450, thus altering cell
membrane permeability in susceptible fungi. It also inhibits other fungal enzymes resulting in the accumulation of toxic concentrations of hydrogen
Absorption:Â Variably absorbed from the GIT (oral), may be increased with decreasing gastric pH. Minimally absorbed systemically (topical or vaginal). Peak plasma concentrations after 2 hr (oral).
Distribution:Â Widely distributed, CSF (poor penetration); enters breast milk. Protein-binding: >90%, mainly to albumin.
Metabolism:Â Hepatic; converted to inactive metabolites.
Excretion:Â Via faeces (as metabolites and unchanged drug), via urine; 2 hr (initial half-life), 8 hr (terminal half-life).
|ATC Classification||D01AC08 - ketoconazole ; Belongs to the class of imidazole and
triazole derivatives for topical use. Used in the treatment of fungal infection.Â
J02AB02 - ketoconazole ; Belongs to the class of systemic imidazole derivative antimycotics. Used in the treatment of mycotic infections.Â
G01AF11 - ketoconazole ; Belongs to the class of imidazole derivative antiinfectives. Used in the treatment of gynecological infections.
|Brand Name||Manufacturer/Marketer||Composition||Dosage Form||Pack Size & Price|
|Dancel||Incepta Pharmaceuticals Limited||Ketoconazole 2% Shampoo||Shampoo||100ml:MRP 230 Tk|
|Dancel 60 ml||Incepta Pharmaceuticals Limited||Ketoconazole 2% Shampoo||Shampoo||60ml:MRP 175 Tk|
|KETOCON||Opsonin Pharma Limited||Ketoconazole 20mg/gm (2%) shampoo||Shampoo||60ml: 175.00 MRP|
|KETOCON 200||Opsonin Pharma Limited||Ketoconazole 200mg||Tablet||30's: 240.00 MRP|
|KETOFUN||Amico Laboratories Ltd.||Ketoconazole 200mg||Tablet||30's: 249.90 MRP|
|KETORAL||Square Pharmaceuticals Ltd.||Ketoconazole 200mg||Tablet||4x10's: 362.40 MRP|
|KETOZOL||Aristopharma Ltd.||Ketoconazole 20mg/gm (2%) shampoo||Shampoo||60ml: 175.00 MRP|
|NIZODER||UniDerma Pharmaceuticals Ltd.||Ketoconazole 20mg/gm (2%) shampoo||Shampoo||100ml: 230.00 MRP|
|NIZODER 2%||UniDerma Pharmaceuticals Ltd.||Ketoconazole 2% (20mg/gm)||Cream||15gm: 50.00 MRP|
Ketoconazole may cause liver damage, sometimes serious enough to require liver transplantation or to cause death. Tell your doctor if you drink or have ever drunk large amounts of alcohol and if you have or have ever had liver disease.
If you experience any of the following symptoms, call your doctor immediately: extreme tiredness, loss of appetite, weight loss, nausea, vomiting, yellowing of the skin or eyes, dark yellow urine, pale stools, pain in the upper right part of the stomach, fever, or rash.
Ketoconazole can cause QT prolongation (an irregular heart rhythm that can lead to fainting, loss of consciousness, seizures, or sudden death). Do not take dofetilide (Tikosyn), pimozide (Orap), quinidine (Quinidex, Quinaglute), or cisapride (Propulsid; no longer available in the US), while you are taking ketoconazole. If you experience any of the following symptoms, stop taking ketoconazole and call your doctor immediately: fast, pounding, or irregular heartbeat; fainting; loss of consciousness.
Keep all appointments with your doctor and the laboratory. Your doctor will order certain tests to check your body's response to ketoconazole.
Your doctor will give you the manufacturer's patient information sheet (Medication Guide) when you begin treatment with ketoconazole and each time you refill your prescription. Read the information carefully and ask your doctor if you have any questions. You can also visit the Food and Drug Administration (FDA) website (http://www.fda.gov/Drugs/DrugSafety/ucm085729.htm) or the manufacturer's website to obtain the Medication Guide.
Talk to your doctor about the risk(s) of taking ketoconazole.
Why is this medication prescribed?
Ketoconazole is used to treat fungal infections when other medications are not available or could not be tolerated. Ketoconazole is in a class of antifungals called imidazoles. It works by slowing the growth of fungi that cause infection.
Ketoconazole cream is used to treat tinea corporis (ringworm; fungal skin infection that causes a red scaly rash on different parts of the body), tinea cruris (jock itch; fungal infection of the skin in the groin or buttocks), tinea pedis (athlete's foot; fungal infection of the skin on the feet and between the toes), tinea versicolor (fungal infection of the skin that causes brown or light colored spots on the chest, back, arms, legs, or neck), and yeast infections of the skin. Prescription ketoconazole shampoo is used to treat tinea versicolor. Over-the-counter ketoconazole shampoo is used to control flaking, scaling, and itching of the scalp caused by dandruff. Ketoconazole is in a class of antifungal medications called imidazoles. It works by slowing the growth of fungi that cause infection.
How should this medicine be used?
Ketoconazole may come as a tablet to take by mouth. It is usually taken once a day. To help you remember to take ketoconazole, take it at around the same time every day. Follow the directions on your prescription label carefully, and ask your doctor to explain any part you do not understand. Take ketoconazole exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.
Your doctor may increase your dose if your condition does not improve.
You may need to take ketoconazole for several weeks or months to cure your infection completely. Your doctor will probably order laboratory tests to be sure your infection has been treated completely. Continue to take ketoconazole until your doctor tells you that you should stop, even if you feel better. Do not stop taking ketoconazole without talking to your doctor. If you stop taking ketoconazole too soon, your infection may come back after a short time.
Ketoconazole also comes as a cream and a shampoo to apply to the skin. Over-the-counter ketoconazole comes as a shampoo to apply to the scalp. Ketoconazole cream is usually applied once a day for 2 to 6 weeks. Prescription ketoconazole shampoo is usually applied one time to treat the infection. Over-the-counter ketoconazole shampoo is usually used every 3 to 4 days for up to 8 weeks, and then used as needed to control dandruff. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Use ketoconazole exactly as directed. Do not use more or less of it or use it more often than prescribed by your doctor.
One treatment with prescription ketoconazole shampoo may successfully treat your tinea versicolor infection. However, it may take several months for your skin color to return to normal, especially if your skin is exposed to sunlight. After your infection is treated, there is a chance that you will develop another tinea versicolor infection.
If you are using over-the-counter ketoconazole shampoo to treat dandruff, your symptoms should improve during the first 2 to 4 weeks of your treatment. Call your doctor if your symptoms do not improve during this time or if your symptoms get worse at any time during your treatment.
If you are using ketoconazole cream, your symptoms should improve at the beginning of your treatment. Continue to use ketoconazole cream even if you are feeling well. If you stop using ketoconazole cream too soon, your infection may not be completely cured and your symptoms may return.
Ketoconazole cream and shampoos are only for use on the skin or scalp. Do not let ketoconazole cream or shampoo get into your eyes or mouth, and do not swallow the medication. If you do get ketoconazole cream or shampoo in your eyes, wash them with plenty of water.
To use the cream, apply enough cream to cover the affected area and all of the skin around it.
To use the prescription shampoo, follow these steps:
Use a small amount of water to wet your skin in the area where you will apply ketoconazole shampoo.
Apply the shampoo to the affected skin and a large area around it.
Use your fingers to rub the shampoo until it forms a lather.
Leave the shampoo on your skin for 5 minutes.
- Rinse the shampoo off of your skin with water.
To use the over-the-counter shampoo, follow these steps:
Be sure that your scalp is not broken, cut, or irritated. Do not use ketoconazole shampoo if your scalp is broken or irritated.
Wet your hair thoroughly.
Apply the shampoo to your hair.
Use your fingers to rub the shampoo until it forms a lather.
Rinse all of the shampoo out of your hair with plenty of water.
Repeat steps 2 to 5.
Other uses for this medicine
Ketoconazole cream and shampoo are also sometimes used to treat dandruff and seborrheic dermatitis (condition that causes flaking of the skin). Ketoconazole cream is sometimes used to treat tinea manuum (fungal infection of the skin on the hands). Ketoconazole cream is also sometimes used with other medications to treat skin conditions that are often worsened by fungal infection such as diaper rash, eczema (skin irritation caused by allergies), impetigo (blisters caused by a bacterial infection), and psoriasis (a lifelong skin condition). Talk to your doctor about the possible risks of using this drug for your condition.
This medication may be prescribed for other uses; ask your doctor for more information.
What special precautions should I follow?
Before taking ketoconazole,
- tell your doctor if you are allergic to ketoconazole or any other medications or any of the ingredients in ketoconazole tablets. Ask your pharmacist or check the Medication Guide for a list of the ingredients.
- tell your doctor if you are taking alprazolam, eplerenone, ergot alkaloids such as ergotamine and dihydroergotamine, lovastatin, midazolam, nisoldipine, simvastatin, and triazolam . Your doctor will probably tell you not to take ketoconazole if you are taking one or more of these medications or any of the medications listed in the IMPORTANT WARNING section.
- tell your doctorÂ what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking. Be sure to mention the medications listed in the IMPORTANT WARNING section and any of the following: antacids; anticoagulants Â such as warfarin; bosentan; buspirone; busulfan; carbamazepine; cilostazol; calcium channel blockers such as amlodipine, diltiazem, felodipine, nicardipine, nifedipine, and verapamil; clarithromycin; clopidogrel; cancer medications such as docetaxel, paclitaxel, vincristine, vinblastine, and vinorelbine; immunosuppressants such as cyclosporine, sirolimus, and tacrolimus; diazepam; digoxin; erythromycin; fentanyl; HIV medications such as indinavir, nevirapine, ritonavir, and saquinavir; loratadine; medications for diabetes; medications for erectile dysfunction such as sildenafil, tadalafil, and vardenafil; medications for indigestion, heartburn, or ulcers such as cimetidine, famotidine, lansoprazole, nizatidine, omeprazole, and ranitidine; medications for irritable bowel disease, motion sickness, Parkinson's disease, ulcers, or urinary problems; methadone; methylprednisolone; phenytoin; medications to treat tuberculosis such as isoniazid, rifabutin, rifampin; quinine; sucralfate; tamoxifen; telithromycin; tolterodine; and trazodone . Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
- tell your doctor if you have or have ever had the conditions mentioned in the IMPORTANT WARNING section or adrenal insufficiency (condition in which the adrenal glands do not make enough steroid hormones).
- tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant while taking ketoconazole, call your doctor. Do not breast-feed while you are taking ketoconazole.
- if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking ketoconazole.
- do not drink any alcoholic beverages (including wine, beer, and medications that contain alcohol such as cough syrup) while taking ketoconazole. You may experience unpleasant symptoms such as flushing, rash, nausea, headache, and swelling of the hands, feet, ankles, or lower legs if you drink alcohol while you are taking ketoconazole.
What special dietary instructions should I follow?
Unless your doctor tells you otherwise, continue your normal diet.
What should I do if I forget a dose?
Take the missed dose as soon as you remember it. However, if it is almost time for the next dose, skip the missed dose and continue your regular dosing schedule. Do not take a double dose to make up for a missed one.
What side effects can this medication cause?
Ketoconazole may cause side effects. Tell your doctor if either of these symptoms is severe or does not go away:
Some side effects can be serious. The following symptoms are uncommon, but if you experience any of them or those listed in the IMPORTANT WARNING section, call your doctor immediately:
difficulty breathing or swallowing
swelling of the lips or tongue
tiredness or weakness
A small number of patients who were taking high doses of ketoconazole for prostate cancer died soon after they began taking the medication. It is not known whether they died because of their disease or their treatment with ketoconazole or for other reasons. Talk to your doctor about the risks of taking ketoconazole.
Ketoconazole may cause a decrease in the number of sperm (male reproductive cells) produced, especially if it is taken at high doses. Talk to your doctor about the risks of taking this medication if you are a man and would like to have children.
Ketoconazole may cause other side effects. Call your doctor if you have any unusual problems while taking this medication.
What should I know about storage and disposal of this medication?
Keep this medication in the container it came in, tightly closed, and out of reach of children. Store it at room temperature and away from excess heat and moisture (not in the bathroom). Throw away any medication that is outdated or no longer needed. Talk to your pharmacist about the proper disposal of your medication.
In case of emergency/overdose
In case of overdose,Â consult your doctor. If the victim has collapsed or is not breathing, consult local medical emergency services.
What other information should I know?
Keep all appointments with your doctor and the laboratory. Your doctor will order certain lab tests to check your response to this medicine.
Do not let anyone else use your medication. If you still have symptoms and need further treatment, consult your doctor.
It is important for you to keep a written list of all of the prescription and nonprescription (over-the-counter) medicines you are taking, as well as any products such as vitamins, minerals, or other dietary supplements. You should bring this list with you each time you visit a doctor or if you are admitted to a hospital. It is also important information to carry with you in case of emergencies.
Ref:Â Â U.S. National Library of Medicine.
This information is provided for reference only and not a replacement for and should only be used in conjunction with full consultation with a registered medical practitioner. It may not contain all the available information you require and cannot substitute professional medical care, nor does it take into account all individual circumstances. Although great effort has been made to ensure content accuracy, mph-bd shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise.