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Modern Pharmacology

Antifungal Medication : Classification, Side effects

An Antifungal medication, also known as an antimycotic medication, is a pharmaceutical fungicide or fungistatic used to treat and prevent mycosis such as athlete’s foot, ringworm, candidiasis (thrush), serious systemic infections such as cryptococcal meningitis, and other.

Causes

CLASSIFICATION :-

  1. Antibiotics
  • Polyenes: Amphotericin B (AMB), Nystatin, Hamycin
  • Echinocandins: Caspofungin, Micafungin, Anidulafungin
  • Heterocyclic benzofuran: Griseofulvin

2. Antimetabolite Flucytosine (5-FC)

3. Azoles

A. Imidazoles

  • Topical: Clotrimazole, Econazole, Miconazole, Oxiconazole
  • Systemic: Ketoconazole

B. Triazoles (systemic)

Fluconazole, Itraconazole, Voriconazole, Posaconazole

4. Allylamine

Terbinafine

5. Other topical agents

Tolnaftate, Undecylenic acid, Benzoic acid, Quiniodochlor, Ciclopirox olamine, Butenafine, Sod. thiosulfate.

Side effects :-

Apart from side effects like altered estrogen levels and liver damage, many Antifungal medicines can cause allergic reactions in people.

For example: The azole group of drugs is known to have caused anaphylaxis.

Drugs knowledge in detail

antibioptics as antifungal

  • Polyenes

The polyenes bind to ergosterol in the fungal cell membrane and thus weakens it, causing leakage of K+ and Na+ ions, which may contribute to fungal cell death.

Amphotericin B, nystatin, and natamycin are examples of polyene antimycotics. They are a subgroup of macrolides.

Amphotericin B is an antifungal medication used for serious fungal infections and leishmaniasis. The fungal infection it is used to treat include aspergillosis, blastomycosis, candidiasis, coccidioidomycosis, and cryptococcosis. For certain infections it is given with flucytosine .

It is typically given by injection into a vein.

Nystatin sold under the brand name Mycostatin among others, is an antifungal medication. It is used to treat Candida infections of the skin including diaper rash, thrush, esophageal candidiasis, and vaginal yeast infections. It may also be used to prevent candidiasis in those who are at high risk. Nystatin may be used by mouth, in the vagina, or applied to the skin.

Hamycin It is a heptaene antifungal compound rather similar in chemical structure to amphotericin B except that it has an additional aromatic group bonded to the molecule. When pure, hamycin is a yellow, powdered solid.

  • Echinocandins

This is a new class of antifungal drugs that inhibit the synthesis of B-glucan in the fungal cell wall .The class has been termed the “penicillin of antifungals”.

Caspofungin (brand name Cancidas worldwide) is a lipopeptide antifungal drug. It works by inhibiting the enzyme (1-3)-B-D glucan synthase and thereby disturbing the integrity of the fungal cell wall. Caspofungin was the first inhibitor of fungal (1-3)-B-D glucan synthesis to be approved by the United States Food and Drug Administration.

Caspofungin is administered intravenously.

Micafungin (trade name Mycamine) used to treat and prevent invasive fungal infections including candidemia, abscesses and esophageal candidiasis. It inhibits the production of beta-1,3-glucan, an essential component of fungal cell walls. Micafungin is administered intravenously.

Anidulafungin is a semisynthetic echinocandin used as an antifungal drug. It may also have application in treating invasive Aspergillus infection when used in combination with Voriconazole.

  • Benzofuran derivatives

are an important heterocyclic compounds that are possess vital biological activities such as antidepressant, anticancer, antiviral, antifungal, antioxidant, anti-psychotic etc.

Benzofurans presents in various natural products with various physiological, pharmacological and toxic properties.

Griseofulvin is used to treat infections such as ringworm, athlete’s foot, jock itch, and fungal infections of the scalp, fingernails, or toenails.

Antimetabolites

These are drugs used in cancer chemotherapy. Cancer cells divide more rapidly compared to normal cells so antimetabolites affect cancer cell replication more than they affect normal cell replication.

Flucytosine, also known as 5-fluorocytosine (5 FC), is an antifungal medication. It is specifically used, together with amphotericin B, for serious Candida infections and cryptococcosis. It may be used by itself or with other antifungals for chromomycosis. Flucytosine is used by mouth and by injection into a vein.

Triazole /azole

Triazoles agents, which are now the most commonly used azoles, include fluconazole, itraconazole, econazole, terconazole, butoconazole, and tioconazole. Newer triazoles (ie, voriconazole, posaconazole, ravuconazole) are active against fluconazole-resistant strains of Candida.

  • Azoleimidazole and benzimidazole scaffolds are extremely versatile and have featured a number of clinically used drugs such as antihistaminic, antiulcer, antihypertensive, antibacterial, antifungal, antiparasitic, antiemetic, anticancer, antiviral, and other therapeutic agents with high therapeutic potency and market..

TOPICAL

Clotrimazole is an antifungal medicine.

It’s used to treat skin infections caused by a fungus (yeast). Clotrimazole treats different types of fungal infections including: athlete’s foot.

Econazole is used to treat skin infections such as athlete’s foot, jock itch, and ringworm.

Miconazole is used to treat vaginal yeast infections. Miconazole reduces vaginal burning, itching, and discharge that may occur with this condition. It works by stopping the growth of yeast (fungus) that causes the infection.

SYSTEMATIC

Ketoconazole should be used only when you cannot use other antifungal medications.

Ketoconazole can cause serious harm to your liver that may result in liver transplant or cause death.

  • Trizolesfluconazole this includes candidiasis, blastomycosis, coccidiodomycosis, cryptococcosis, histoplasmosis, dermatophytosis, and pityriasis versicolor.

Itraconazole This includes infections in any part of the body including the lungs, mouth or throat, toenails, or fingernails. Some brands of itraconazole are not for use in treating fungal infections of the fingernails or toenails.

Voriconazole is a triazole antifungal medication used to treat serious fungal infections. It is used to treat invasive fungal infections that are generally seen in patients who are immunocompromised. These include invasive candidiasis, invasive aspergillosis, and emerging fungal infections.

Allylamine Antifungal

An antifungal agent used to treat infections of the Tinea, Trichophyton, and Epidermophyton species. An allylamine antifungal used to treat dermatophyte infections of toenails and fingernails as well as other fungal skin infections.

Terbinafine tablets are used to treat infections caused by fungus that affect the fingernails or toenails. Terbinafine oral granules are used to treat a fungal infection of scalp hair follicles in children who are at least 4 years old.

Topical agents

Tolnaftate is a synthetic thiocarbamate used as an anti-fungal agent .

It is supplied as a cream, powder, spray, and liquid aerosol. Tolnaftate is used to treat fungal conditions such as jock itch, athlete’s foot and ringworm.

Undecylenic acid is an active ingredient in medications for skin infections, and to relieve itching, burning, and irritation associated with skin problems.

For example, it is used against fungal skin infections, such as athlete’s foot, ringworm, tinea cruris, or other generalized infections by Candida albicans.

Benzoic acid derivatives produced a similar pattern of antifungal properties as observed for C. lunatus but resulted in six moderately active compounds.

Quiniodochlor is an anti-amoebic, antibacterial and antifungal agent used to treat a variety of infections caused by amoeba, bacteria, and fungi. The topical form of this medicine is used to treat skin infections

Ciclopirox is a synthetic antifungal agent for topical dermatologic treatment of superficial mycoses. It is most useful against Tinea versicolor. It is sold under many brand names worldwide.

By Bhawna Tourani

Belonging to Ajmer, Rajasthan. Currently persuading B.A.M.S. 3rd Prof. From Gaur Brahman Ayurvedic College. My Strong point is in Ayurvedic Portion so will help you in that. While Studying Ayurveda for last 2 years i developed hobby about learning about Ayurvedic medicines, also good at reading.

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