KETOCONAZOLE
Drugs in Pregnancy and Lactation.
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Name: KETOCONAZOLE
Class: Antifungal
Risk Factor: CM
Fetal Risk Summary
Ketoconazole is a synthetic, broad-spectrum antifungal agent. The antimycotic agent is embryotoxic (1) and teratogenic (1,2) in rats, producing syndactyly and oligodactyly at a dose of 80 mg/g/day (10 times the maximum recommended human dose), a maternally toxic dose. Ketoconazole has been used, apparently without fetal harm, for the treatment of vaginal candidiasis occurring during pregnancy (3).
In a surveillance study of Michigan Medicaid recipients involving 229,101 completed pregnancies conducted between 1985 and 1992, 20 newborns had been exposed to oral ketoconazole during the 1st trimester (F. Rosa, personal communication, FDA, 1993). No major birth defects were observed (one expected). Since this study, the FDA has received six reports of limb defects (F. Rosa, personal communication, FDA, 1996).
Limb malformations were also reported in a 1985 abstract (4). A Turkish woman had used ketoconazole, 200 mg daily, during the first 7 weeks of gestation. Hydrops fetalis was diagnosed at 29 weeks' gestation and she delivered a female infant at 30.5 weeks'. The infant, with a normal karyotype (46,XX), had multiple anomalies of the limbs (further details not specified).
Women infected with human immunodeficiency virus frequently have vaginal candidiasis. Maternal symptoms, such as pruritus, may require treatment and in these cases, therapeutic and prophylactic ketoconazole regimens are recommended, even though the fungal infection has little perinatal significance (5).
Ketoconazole inhibits steroidogenesis in fungal cells. In humans, high doses, such as those above 400 mg/day, impair testosterone and cortisol synthesis (6,7,8 and 9). Because of this effect, ketoconazole has been used in the treatment of hypercortisolism (10). A review summarizing the treatment of 67 cases of Cushing's syndrome occurring during pregnancy did not find any cases treated with ketoconazole (10). A 1990 report, however, described a ketoconazole-treated 36-year-old pregnant woman with Cushing's syndrome (11). The pregnancy, in addition to Cushing's syndrome, was complicated by hypertension, the onset of gestational diabetes mellitus at 9 weeks' gestation, and intrauterine growth retardation. Ketoconazole, 200 mg every 8 hours, was started at 32 weeks' gestation and continued for 5 weeks because of maternal clinical deterioration resulting from the sustained hypercortisolism. Rapid clinical improvement was noted in the mother after therapy was begun. A growth-retarded, 2080-g, but otherwise normal, female infant was delivered by elective cesarean section at 37 weeks. The Apgar scores were 9 and 9 at 1 and 5 minutes, respectively. No clinical or biochemical evidence of adrenal insufficiency was found in the newborn. The infant's basal cortisol and adrenocorticotropic hormone levels, 306 nmol/L and 8.1 pmol/L, respectively, were normal. The child was growing normally at 18 months of age.
Breast Feeding Summary
No reports describing the use of ketoconazole during human lactation or measuring the amount, if any, of the drug excreted into milk have been located. Although citing no data, the manufacturer states that ketoconazole is probably excreted into milk (1). Moreover, two other azole fungicides (fluconazole and itraconazole) are excreted into breast milk; thus, the passage of ketoconazole into milk should be expected. The effects on the nursing infant from exposure to drug in the milk are unknown.
References
- Product information. Nizoral. Janssen Pharmaceutics, 1997.
- Nishikawa S, Hara T, Miyazaki H, Ohguro Y. Reproduction studies of KW-1414 in rats and rabbits. Clin Report 1984;18:1433–88. As cited in Shepard TH. Catalog of Teratogenic Agents. 6th ed. Baltimore, MD:Johns Hopkins University Press, 1989:1075.
- Luscher KP, Schneitter J, Vogt HP. Frequency of candidiasis during pregnancy and therapy with ketokonazol ovula. Schweiz Rundsch Med Prax 1987;76:1285–7.
- Lind J. Limb malformations in a case of hydrops fetalis with ketoconazole use during pregnancy (abstract). Arch Gynecol 1985;237(Suppl):398.
- Minkoff HL. Care of pregnant women infected with human immunodeficiency virus. JAMA 1987;258:2714–7.
- Hobbs ER. Coccidioidomycosis. Dermatol Clin 1989;7:227–39.
- Pont A, Williams PL, Loose DS, Feldman D, Reitz RE, Bochra C, Stevens DA. Ketoconazole blocks adrenal steroid synthesis. Ann Intern Med 1982;97:370–2.
- Engelhardt D, Mann K, Hormann R, Braun S, Karl HJ. Ketoconazole inhibits cortisol secretion of an adrenal adenoma in vivo and in vitro. Klin Wochenschr 1983;61:373–5.
- Divers MJ. Ketoconazole treatment of Cushing's syndrome in pregnancy. Am J Obstet Gynecol 1990;163:1101.
- Aron DC, Schnall AM, Sheeler LR. Cushing's syndrome and pregnancy. Am J Obstet Gynecol 1990;162:244–52.
- Amado JA, Pesquera C, Gonzalez EM, Otero M, Freijanes J, Alvarez A. Successful treatment with ketoconazole of Cushing's syndrome in pregnancy. Postgrad Med J 1990;66:221–3.
Q&A about Ketoconazole
If Ketoconazole 200mg does not work on me, should i use a stronger Ketoconazole with more mg's?
Ketoconazole is very lipophilic (fat loving), which leads to accumulation in fatty tissues. The less toxic and more effective triazole compounds fluconazole and itraconazole have largely replaced ketoconazole for internal use. Ketoconazole is best absorbed at highly acidic levels, so antacids or other causes of decreased stomach acid levels will lower the drug's efficacy when taken orally.
Since I don't know what you have I cannot suggest you to go in for a higher dose of it or no cause if you do so it might lead to side effects which are greater and also toxicity. I advise you to go to a doctor and get it checked. It is possible that the fungal infection which you have is resistant to the ketoconazole and most probably your doctor will suggest that you change your medicine or he will give you a combination of medicines.BUT DO NOT INCREASE THE MGS(WEIGHT/DOSE) WITHOUT CONSULTING A PHYSICIAN.
HI
iam a pharmacist and i have assignment in medicinal chemistry in the differences between ketoconazole and fluconazole in SAR(structure activity relation ship)
thnxx
Ketoconazole is very lipophilic, which leads to accumulation in fatty tissues. The less toxic and more effective triazole compounds fluconazole and itraconazole have largely replaced ketoconazole for internal use. Ketoconazole is best absorbed at highly acidic levels, so antacids or other causes of decreased stomach acid levels will lower the drug's efficacy when taken orally.
http://en.wikipedia.org/wiki/Ketoconazol...
Fluconazole (INN) (IPA: [fluˈkɒnəzoʊl]) is a triazole antifungal drug used in the treatment and prevention of superficial and systemic fungal infections. It is commonly marketed under the trade name Diflucan (Pfizer).
Mode of action
Like other imidazole- and triazole-class antifungals, fluconazole inhibits the fungal cytochrome P450 enzyme 14α-demethylase. Mammalian demethylase activity is much less sensitive to fluconazole than fungal demethylase. This inhibition prevents the conversion of lanosterol to ergosterol, an essential component of the fungal cell wall, and subsequent accumulation of 14α-methyl sterols. Fluconazole is primarily fungistatic, however may be fungicidal against certain organisms in a dose-dependent manner.
http://en.wikipedia.org/wiki/Fluconazole
It's now a fact that a lot of people with major clinical depression suffer from high levels of cortisol. Ketoconazole works by blocking cortisol levels, so they are not irregularly high. I guess what I am asking is that I have tests saying my cortisol is high, could my psychiatrist prescribe Ketoconazole to lower my cortisol levels to treat my major clinical depression if she or he wanted to?
Let's find out, shall we?
IN THIS SITUATION I HAVE TO TAKE THE ORAL KETOCONAZOLE, SO STOPPING THE MED IS NOT AN OPTION. I KNOW SOMEONE IN THIS WORLD HAS GOT RID OF THIS SIDE EFFECT BEFORE. WHEN TAKING KETOCONAZOLE I GET RASHES, PATCHES OF DRY SKIN, AND EXTREMELY DRY SKIN. THE SKIN THING IS MY ONLY PROBLEM, BUT IT'S DESTROYING MY LIFE. THERE HAS TO BE SOME KIND OF CREAM OR MEDICATION TO MAKE MY SKIN NORMAL AGAIN WHILE I CONTINUE TO TAKE ORAL KETOCONAZOLE. PLEASE, PLEASE, PLEASE HELP ME FIGURE THIS OUT. IF IT HELPS AT ALL THE ORAL KETOCONAZOLE IS MAKING MY HAIR GROW BACK.
I got this cream from my doctor for a rash on my arm. I was just curious if I could use it on cold sores.
Cold sores are outbreaks of herpes, which is a virus not a fungus, so no it won't work!
What you are after for cold sores is something such as zovirax or valtrex/valacyclovir/acyclovir, either oral or a cream (oral tablets works best).
Candida 3. Treatment by ketoconazole. 3yrs old. Anyone know when to be concerned?
Good luck!
She was taking this for the skin. Should she go to the doctor or she could wait and the side effects will ware off?
It's insoluble in water, it's soluble in more non-polar solvent.
Is it bad to take this medication for a long time? Is because I buy this medication every two weeks and I never stop taking it since one time a doctor told me to take it and is because my yeast infection keeps coming back and I can't afford to go to the doctor everytime I get an yeast infection.