Ketoconazole(kee toe kon' na zole) | Nizoral |
| Category | Stimulate/DHT reducer |
| Parameter |
Effect |
Result on hair growth |
| DHT |  | GOOD |
| 5a-reductases |  | UNKNOWN |
| PGD2 | | UNKNOWN |
| PGE2 | | UNKNOWN |
| PGF2 | | UNKNOWN |
| CRTH2 | | UNKNOWN |
Where to buy
Information
| Description |
Ketoconazole is thought to disrupt DHT pathways in the scalp and reduce inflammation.
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| Typical Results |
Moderate regrowth alone and when used in conjuction with other treatments good to excellent regrowth.
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| Typical Dosages |
Three times a week to daily, can cause scalp irritation if used too often.
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| Significant Side Effects |
Scalp irritation
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| Pharmacology Pharmacodynamics |
Ketoconazole, a synthetic imidazole antifungal, is effective for superficial fungal infections, genital candidosis and chronic mucocutaneous candidosis, and has been used in immunocompromised patients and advanced prostatic carcinoma. Absorption of ketoconazole is variable after oral administration, with large variability in peak serum concentrations. Antacids reduce, and food or dilute hydrochloric acid increase, absorption. Renal failure and bone marrow transplantation are associated with reduced absorption. Ketoconazole is not absorbed systemically after topical administration, and minimally absorbed from the vagina. Distribution of ketoconazole varies according to the tissue sampled, the underlying disease and the dose and duration of treatment. Ketoconazole does not cross the intact blood-brain barrier, and crosses to only a limited extent in fungal meningitis. Urinary concentrations of ketoconazole are usually low, but vaginal and vaginal tissue concentrations correlate with those in serum. Seminal fluid concentrations are inadequate for treatment of epididymitis. Ketoconazole is 83.7% plasma protein (mainly albumin) bound, and 15.3% is erythrocyte bound, resulting in only 1% of free drug. Animal studies indicate strong binding to the cytochrome P-450 mono-oxygenase complex. Extensive metabolism to inactive metabolites occurs, the products being mainly excreted in the faeces. Saturable hepatic first-pass metabolism is probable. The half-life of ketoconazole is dose-dependent, increases during long term treatment, suggesting auto-inhibition of metabolism. The kinetics after oral administration fit a 2-compartment model. Drug interactions of theoretical, if not practical, significance include warfarin, chlordiazepoxide, methylprednisolone, cyclosporin and drugs known to induce microsomal enzymes. In each case, some dosage adjustment for ketoconazole, or the interacting drug, may be required.
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Clinical Studies
| Clinical Studies | Abstract |
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Ketocazole as an adjunct to finasteride in the treatment of androgenetic alopecia in men.
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Dihydrotestosterone (DHT) binding to androgen receptors (AR) in hair follicles is commonly accepted as the first step leading to the miniaturizing of follicles associated with androgenetic alopecia (AGA). Testosterone is converted to DHT by the enzyme 5alpha-reductase. Finasateride a 5alpha-reducase inhibitor blocks the production of DHT and is currently used to treat AGA. The inhibition is not complete but a reduction of DHT systemically and in the scalp is accomplished. Ketoconazole has been clinically shown to be effective in the treatment of AGA. In this paper, evidence is presented to support the hypothesis that ketoconazole 2% shampoo has a local disruption of the DHT pathway. It is proposed that using ketoconazole 2% shampoo as an adjunct to finasteride treatment could lead to a more complete inhibition of DHT and thus better treat AGA.
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Reversal of androgenetic alopecia by topical ketoconzole: relevance of anti-androgenic activity.
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Ketoconazole (KCZ), an imidazole anti-fungal agent, is known to be effective for the treatment of seborrheic dermatitis and dandruff. In addition, 2% ketoconazole shampoo was found to improve hair density and the size and proportion of anagen follicles in androgenetic alopecia (AGA) and, in combination with finasteride, to have an additive effect for AGA. Six Japanese males from 23 to 51 years old were enrolled in this study with their written informed consent. They presented with grade II vertex to IVa AGA according to the Hamilton–Norwood classification. The subjects applied topical 2% ketoconazole lotion (Nizoral®) almost every day during or immediately after hair washing with their own unmedicated shampoos. When they revisited our clinic every several months, clinical pictures were obtained to determine the efficacy of the treatment. Two of the men, one 23 years old with grade II vertex and the other 25 years old with Va AGA, showed remarkable hair regrowth after 6 and 10 months, respectively. The 23-year-old male stopped using ketoconazole and 3 months later hair loss recurrence on the vertex was noted. When he started using ketoconazole again during shampooing, hairs on the vertex grew again after 3 months. These findings constitute evidence of the clinical efficacy of ketoconazole for AGA. A 41-year-old male showed a slight increase in vertex hair growth after 1 year. Other three of the men, 31, 38 and 51 years old did not show significant improvement.
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Ketoconazole shampoo: effect of long-term use in androgenic alopecia.
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BACKGROUND:
The pathogenesis of androgenic alopecia is not fully understood. A microbial-driven inflammatory reaction abutting on the hair follicles might participate in the hair status anomaly.
OBJECTIVE:
The aim of our study was to determine if ketoconazole (KCZ) which is active against the scalp microflora and shows some intrinsic anti-inflammatory activity might improve alopecia.
METHOD:
The effect of 2% KCZ shampoo was compared to that of an unmedicated shampoo used in combination with or without 2% minoxidil therapy.
RESULTS:
Hair density and size and proportion of anagen follicles were improved almost similarly by both KCZ and minoxidil regimens. The sebum casual level appeared to be decreased by KCZ.
CONCLUSION:
Comparative data suggest that there may be a significant action of KCZ upon the course of androgenic alopecia and that Malassezia spp. may play a role in the inflammatory reaction. The clinical significance of the results awaits further controlled study in a larger group of subjects.
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Comparative efficacy of various treatment regimens for androgenetic alopecia in men.
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Our understanding of the aetiology of androgenetic alopecia (AGA) has substantially increased in recent years. As a result, several treatment modalities have been tried with promising results especially in early stages of AGA. However, as far as has been ascertained, there is no comprehensive study comparing the efficacy of these agents alone and in combination with each other. One hundered male patients with AGA of Hamilton grades II to IV were enrolled in an open, randomized, parallel-group study, designed to evaluate and compare the efficacy of oral finasteride (1 mg per day), topical 2% minoxidil solution and topical 2% ketoconazole shampoo alone and in combination. They were randomized into four groups. Group I (30 patients) was administered oral finasteride, Group II (36 patients) was given a combination of finasteride and topical minoxidil, Group III (24 patients) applied minoxidil alone and Group IV (10 patients) was administered finasteride with topical ketoconazole. Treatment efficacy was assessed on the basis of patient and physician assessment scores and global photographic review during the study period of one year. At the end of one year, hair growth was observed in all the groups with best results recorded with a combination of finasteride and minoxidil (Group II) followed by groups IV, I and III. Subjects receiving finasteride alone or in combination with minoxidil or ketoconazole showed statistically significant improvement (p<0.05) over minoxidil only recipients. No signifcant side-effects related to the drugs were observed. In conclusion, it is inferred that the therapeutic efficacy is enhanced by combining the two drugs acting on different aetiological aspects of AGA.
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Ketoconazole shampoo: effect of long-term use in androgenic alopecia.
|
BACKGROUND:
The pathogenesis of androgenic alopecia is not fully understood. A microbial-driven inflammatory reaction abutting on the hair follicles might participate in the hair status anomaly.
OBJECTIVE:
The aim of our study was to determine if ketoconazole (KCZ) which is active against the scalp microflora and shows some intrinsic anti-inflammatory activity might improve alopecia.
METHOD:
The effect of 2% KCZ shampoo was compared to that of an unmedicated shampoo used in combination with or without 2% minoxidil therapy.
RESULTS:
Hair density and size and proportion of anagen follicles were improved almost similarly by both KCZ and minoxidil regimens. The sebum casual level appeared to be decreased by KCZ.
CONCLUSION:
Comparative data suggest that there may be a significant action of KCZ upon the course of androgenic alopecia and that Malassezia spp. may play a role in the inflammatory reaction. The clinical significance of the results awaits further controlled study in a larger group of subjects
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Topical application of ketoconazole stimulates hair growth in C3H/HeN mice.
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Ketoconazole (KCZ) is an imidazole anti-fungal agent that is also effective in topical applications for treating seborrheic dermatitis and dandruff. Recently, topical use of 2% KCZ shampoo has been reported to have had a clinically therapeutic effect on androgenetic alopecia. The present study was conducted with the purpose of quantitatively examining the stimulatory effect of KCZ on hair growth in a mouse model. Coat hairs on the dorsal skin of seven week-old male C3H/HeN mice were gently clipped, and either 2% KCZ solution in 95% ethanol or a vehicle solution was topically applied once daily for three weeks. The clipped area was photographed, and the ratio of re-grown coat area was then calculated. The results demonstrated that 2% KCZ had a macroscopically significant stimulatory effect compared with the vehicle group (p < 0.01, n=10). Repeated experiments showed similar effects, confirming the efficacy of KCZ as a hair growth stimulant. Although the therapeutic mechanism of topical KCZ for hair growth is unclear, our results suggest that topical applications of the substance are useful for treating seborrheic dermatitis accompanied by hair regression or male pattern hair loss.
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