Life-extension drugs

+44 (808) 189 0019
Life-extension drugs
Can not find medication you need on our site? Let us know and we'll supply you any drug you wish!

Nizoral Review Article

 

FungiNizoral having generic name Ketoconazole is an anti-fungal agent available in white tablets. It is basically used for the treatment of systemic fungal infections such as candidiasis, chronic mucocutaneous candidiasis, oral thrush, candiduria, blastomycosis, coccidioidomycosis, histoplasmosis, chromomycosis, and paracoccidioidomycosis. It belongs to the class fluconazole. It is recommended not to use this drug for meningitis fungus as it penetrates poorly into cerebral spinal fluid. It is also use for the treatment of severe recalcitrant cutaneous dermatophyte infections. The recommended dosage of this medication is of 3.3 to 6.6 mg per kg. Minimum treatment duration is of 4 weeks. It is found that this drug may cause serious damage to liver.

Fungal Infections

Fungi (Kingdom Myceetae) are a group of organisms that are somewhat hard to describe. They are considered a group between groups, because of the sharing of characteristics between different organisms. For instance, some fungi are single- celled (like many bacteria are), while some are as large as plants. Some reproduce by fission (asexual reproduction), while others reproduce sexually. Continue reading...

Dosage Packing Price Add to basket
Nizoral Dandruff Shampoo 100 ml USD 26.00 Add to Basket
45 g 3 tubes USD 19.00 Add to Basket
90 g 6 tubes USD 47.00 Add to Basket

Fungi exist almost everywhere. In fact, some of them live as parasites inside the body of host organisms. They are a group of microbes considered to be a major medical concern because of the wide variety of infections and diseases that they cause. Some may be minor itches, but some can even be life threatening. Because of this, several drugs to fight off fungi have been developed. One such drug is Nizoral.

Nizoral (Ketoconazole)

Nizoral is an antifungal agent belonging to the azoles, subclass imidazoles. It can be used either as a prophylactic agent or for treatment; and either via topical or oral route. It is prescribed for several fungal infections affecting the mouth, gastrointestinal tract (GIT), bladder, skin, hair, nails, and other parts of the body. Its molecular formula is C26H28Cl2N4O4.



Nizoral is a drug that has long established its effectiveness. In a review by Hume and Kerkeing (1983), it was shown that Nizoral use is effective in treating several fungal conditions.

Nizoral possesses antifungal activity against a wide variety of fungi. Topically, it is used for the treatment of dermatophyte infections like tinea pedis (foot), tine versicolor (skin), tinea manuum (hand), tinea capitis (head), tinea ungulum (nails) and tinea corporis. These dermatophyte infections are caused by fungi belonging to the Trichosporon, Epidermophyton and Microsporon spp.

Onchomycosis: A fungal infection of the nails
Seborrheic dermatitis: A fungal infection of the hair
Stratigos et al. in 2008 found that Nizoral is effective in the treatment of seborrheic dermatitis. In a study by Zaias and Drachman (1983), it was found that long-term use of Nizoral cream can effectively manage onychomycosis (nail fungal infection). See the figures on the right for these conditions.








Nizoral is an effective broad spectrum antifungal agent (Thienpont, et al., 1979). It is useful for the treatment of vaginal candidiasis (caused by Candida spp like C. albicans, C. tropicalis, C. parapsilosis and C. glabrata), dermatophyte infections not responding to topical treatment, and systemic infections like blastomycosis (Blastomyces dermatitidis), histoplasmosis (Histoplasma capsulatum), coccidioidomycosis (Coccidioides spp.), paracoccidioidomycosis (Paracoccidioides brasiliensis) and systemic candidiasis.

Nizoral is also used as a prophylactic therapy for immunocompromised patients (people who have a lower immune response, thus have a higher susceptibility for infection). Nizoral is effective in preventing possible fungal infections associated with these patients. In a study made by Estey and colleagues (1984), they found that Nizoral is an effective prophylactic agent for patients who are suffering from leukemia.

Mechanism of action

As an antifungal belonging to the azole group, Nizoral acts on the cell wall synthesis of fungi. The fungi cell wall is made up of ergosterol, a type of cholesterol. Ergosterol is synthesized from lanosterol, through the action of a microsomal CYP450 enzyme called 14-α-sterol demethylase enzyme. Impairment of the synthesis of ergosterol is lethal to fungi – it causes a variety of effects like:
a) accumulation of 14-α-methylsterol that subsequently disrupts the integrity of the fungal cell wall;
b) impairment of membrane-bound enzymes;
c) inhibition of the electron transport chain;
d) increasing of the permeability of the cell membrane.

Anti-Androgen and Anti-Glucocorticoid

Aside from its antifungal effects, Nizoral is also known for its anti-androgenic effects, and also as a potent inhibitor of glucocorticoid synthesis.

Androgens and glucocorticoids are compounds that are structurally similar to cholesterol – they possess a steroid nucleus. They are synthesized through the use of several enzymes found in the body, which act on cholesterol. As mentioned, Nizoral inhibits the synthesis of ergosterol, another compound similar to cholesterol. Because Nizoral inhibits enzymes that act on cholesterol, other compounds synthesized from cholesterol are also blocked, such as androgen and glucocorticoids. This results to a decrease amount of these compounds in the body. This was shown by Pont et al. in 1982, observing that glucocorticoids were virtually blocked after just 4 hours of 400 and 600mg dose administration.

In the synthesis of androgen and glucocorticoids, Nizoral specifically inhibits the enzymes P450c11, P450c17, C17, 20-lyase, and 3β-hydroxysteroid dehydrogenase, which are responsible for the cholesteorol side chain cleavage step. Though other azole antifungals have the same mechanism of action, it was found that Nizoral alone has the highest effect on human cholesterol enzymes. Other azoles are more selective for fungal enzymes.

Though these side effects are viewed as negative (due to the development of gynecomastia in men), it has found some other medical use. For example, in a study made by Evans and colleagues (2004), it was found that Nizoral is effective in preventing postoperative penile erections after surgery. This is due to the inhibition of testosterone, a type of androgen (Pont et al., 1982).

Another non fungal indication of Nizoral is the management of Cushing’s syndrome. Cushing’s syndrome is a hormonal disorder that is caused by high amounts of glucocorticoids in the body. The high levels of glucocorticoids may be caused by exogenous intake (drugs) or tumors. Because Nizoral inhibits glucocorticoid synthesis, it is effective in managing Cushing’s syndrome. According to Loli, Berselli and Tagliaferri (1986), Nizoral specifically inhibits adrenal 11β-hydroxlyase and 17,20-lyase, leading to a decrease in glucocorticoid levels.

Another condition that is currently being studied is androgenic alopecia. In a study by Pierard-Franchimont et al. (1998), it was found that Nizoral may be effective in the long term treatment of this condition. These findings were also reported by Rogers and Avram (2008).



References

ESTEY, E., MAKSYMIUK, A., SMITH, T., ET AL. 1984. Infection Prophylaxis in Acute Leukemia. Retrieved from
http://archinte.ama-assn.org/cgi/content/abstract/144/8/1562

EVANS, K.C., PETERSON, A.C., RUIZ, H.E. & COSTABILE, R.A. 2004. Use of oral ketoconazole to prevent postoperative erections following penile surgery. Retrieved from
http://www.nature.com/ijir/journal/v16/n4/full/3901160a.html

HUME, A.L. & KERKERING, T.M. 1983. Ketoconazole. Retrieved from
http://www.theannals.com/content/17/3/169.short

LOLI, P., BERSELLI, M.E. & TAGLIAFERRI, M. 1986. Use of ketoconazole in the treatment of Cushing's syndrome. Retrieved from
http://www.ncbi.nlm.nih.gov/pubmed/3023421

PIERARD-FRANCHIMONT, C., DE DONCKER, P. & Pierard, G.E. 1998. Ketoconazole Shampoo: Effect of Long-Term Use in Androgenic Alopecia. Retrieved from
http://content.karger.com/ProdukteDB/produkte.asp?Aktion=ShowAbstract&ProduktNr=224164&Ausgabe=225575&ArtikelNr=17954

PONT, A., WILLIAMS, P.L., LOOSE, D.S., ET AL. 1982. Ketoconazole Blocks Adrenal Steroid Synthesis. Retrieved from
http://www.annals.org/content/97/3/370.short

PONT, A., WILLIAMS, P.L., SALMAN, A., ET AL. 1982. Ketoconazole Blocks Testosterone Synthesis. Retrieved from
http://archinte.ama-assn.org/cgi/content/abstract/142/12/2137

STRATIGOS, J.D., ANTONIOU, C.H.R., KATSAMBAS, A., ET AL. 2008. Ketoconazole 2% cream versus hydrocortisone 1% cream in the treatment of seborrheic dermatitis: A double-blind comparative study. Retrieved from
http://www.sciencedirect.com/science/article/pii/S0190962288702443

THIENPONT, D., VAN CUTSEM, J., GERVEN, F., ET AL. 1979. Ketoconazole — a new broad spectrum orally active antimycotic. Retrieved from
http://www.springerlink.com/content/pjq373h9143w0336/

REGERS, N.E. & AVRAM M.R. Medical treatments for male and female pattern hair loss. Retrieved from
http://www.ncbi.nlm.nih.gov/pubmed/18793935

ZAIAS, N. & DRACHMAN, D. A method for the determination of drug effectiveness in onychomycosis: Trials with ketoconazole and griseofulvin ultramicrosize. Retrieved from
http://www.sciencedirect.com/science/article/pii/S0190962283702082


 

My BasketMy Basket

Antifungals
Nizoral
Nizoral Review Article


Buy here


Nizoral prescribing information


Newsletter subscription


Product search

Product list

- ACARBOSE
- ACCUPRIL
- ACIPHEX
- ACTOS
- ACYCLOVIR
- ADALAT
- ADAMANTAN
- AERIUS
- ALENDRONATE
- ALLEGRA
- ALLOPURINOL
- AMANTADINE
- AMARYL
- AMINOGUANIDINE
- AMITRIPTYLINE
- ARAVA
- AREDIA
- ARICEPT
- ARIMIDEX
- ASTRAGALOSIDE IV
- ATORVASTATIN
- AUGMENTIN
- AVAPRO
- AVASTIN
- AVEMAR IMMUNE BOOSTER
- AZARGA
- AZOPT
- B-VITAMIN COMPLEX
- B-VITAMIN COMPLEX FORTE
- B6 VITAMIN
- BENICAR
- BONIVA
- BROMOCRIPTINE
- BURDOCK ROOT OIL
- CAFFEINE COMPLEX
- CALCITRIO
- CAMPTO
- CASODEX
- CAVINTON
- CENTROPHENOXINE
- CIALIS
- CIPROBAY
- CLIMAGEST
- CLOMID
- CLOTRIMAZOLE, BIFONAZOLE
- COAXIL
- COENZYME Q10
- COMBIVIR
- COMPETACT
- COMTAN
- COVEREX
- COVERSYL
- COZAAR
- CRESTOR
- CYCLOASTRAGENOL (TA-65 ACTIVE SUBSTANCE)
- CYMBALTA
- D3 VITAMIN
- DEPAKOTE
- DEPO-MEDROL
- DEPRENYL
- DIABENOL
- DIFLUCAN
- DOXYCYCLINE
- E VITAMIN
- ECHINACEA/ VIT. C 1000/ ZINC
- EFFEXOR
- ELDEPRYL
- EULEXIN
- EVISTA
- EXELON
- FARESTON
- FAT BURNER
- FEMARA
- FISH OIL
- FLOMAX
- FLUCONAZOLE
- FOLIC ACID
- FOSAMAX
- GALVUS
- GLEEVEC, GLIVEC
- GLUCOBAY
- GLUCOBENE
- GLUCONORM
- GLUCOPHAGE, GLUCOPHAGE XR
- IBUPROFEN
- IMATINIB
- IMIGRAN
- IMUNOVIR
- INULIN
- IODIDE (KI)
- IODINE WATER
- IRESSA
- ISOPRINOSINE
- JANUMET
- JANUVIA
- JUMEX
- K-2 VITAMIN
- KALETRA
- LAMISIL
- LESCOL
- LEUZEA ROOT
- LEVAQUIN, LEVOFLOXACIN
- LIFE EXTENDING KIT
- LIPITOR
- LIPOIC ACID
- LOTENSIN
- MACA VIBE
- MADOPAR
- MEGACE
- MELATONIN
- MEMANTINE
- METFORMIN
- METOPROLOL
- MILGAMMA
- MIRAPEXIN
- MOBIC
- MOVALIS
- MUMIJO (MUMIO)
- NADH
- NEUPRO
- NEXIUM
- NIZORAL
- NOLVADEX
- NOOTROPIL
- NOOTROPYL
- NORVASC
- ORUNGAL
- OSELTAMIVIR
- PANTOCRIN
- PIKAMILON (PICAMILON)
- PIRACETAM
- PLAVIX
- PRECOSE
- PROSCAR
- PUMPKINSEED OIL
- RALOXIFENE
- RAPAMYCIN
- RED WINE HIGH IN RESVERATROL
- RESVERATROL
- REVALID CAPSULES
- REVALID CREAM
- REVALID HAIR TONIC
- REVALID SHAMPOO AND CONDITIONER
- REYATAZ
- RHODIOLA ROOT
- RHODIOLA TABLETS
- ROSUVASTATIN
- RUTIN
- SCHISANDRA
- SEA-BUCKTHORN
- SELEGILIN
- SELENIUM
- SEROQUEL
- SINEMET
- SINGULAIR
- SPORANOX
- STABLON
- SUSTIVA
- TAMIFLU
- TAMOXIFEN (ZITAZONIUM)
- TASMAR
- TELFAST
- THIOGAMMA (LIPOIC ACID)
- TOLCAPONE
- TOPAMAX
- TRITICO
- TRUVADA
- VALDOXAN
- VEPESID
- VFEND (VORICONAZOLE)
- VIAGRA
- VINPOCETINE
- VINPOTROPILE
- VIREAD
- XALATAN
- XELODA
- XENICAL
- XYLOMETAZOLINE / OTRIVIN
- ZETIA
- ZIAGEN
- ZINC (ZN)
- ZITHROMAX
- ZOCOR
- ZOFRAN
- ZOVIRAX
- ZYPREXA
- ZYRTEC

You are located on a secure website.
Customer data is for our internal use only and will be treated as confidential.

eXTReMe Tracker