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Anti Fungal drugs, Pharmacology III, Unit-3 Download Notes PDF BPharmacy 6th Semester 2022
π BP602T Pharmacology III
Title: |
Anti Fungal drugs, Pharmacology III, Unit-3 |
Course: | BPharmacy |
Semester/Year: | 6th Semester |
Subject: | BP602T Pharmacology III |
Session: | 2022 |
Category: | Notes |
Pharmacology BPharmacy BPharm 6th Semester Important Exam Notes |
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ANTI-FUNGALAGENTβ’ These are drugs used for superficial anddeep(systemic)fungal infections. β’ Fungal infections are mostly associatedwiththeuseofbroad-spectrum antibiotics, corticosteroids, anticancer/immunosuppressant drugs, catheters andimplantsandemergence of AIDS. β’ As a result of breakdown of host defencemechanismsbythe above agents, saprophytic (live andfeedondead)fungi easily invade living tissue.
Classification of drugs:
1. Antibiotics
A. Polyenes: Amphotericin B (AMB), NystatinB. Echinocandins: Caspofungin, MicafunginC. Heterocyclic benzofuran: Griseofulvin
2. Antimetabolite: Flucytosine (5-FC)
3. Azoles
A. Imidazoles
Topical: Clotrimazole, Econazole, Miconazole, OxiconazoleSystemic: Ketoconazole
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B. Triazoles: Fluconazole, Itraconazole, Voriconazole.4. Allylamine: Terbinafine
5. Other topical agents:
Tolnaftate, Undecylenic acid, Benzoicacid,Butenafine, Sodium thiosulfate. Amphotericin B (AMB)
β’ Obtained from Streptomyces nodosus. β’ Amphotericin has two parts:
A- lipophilic (non-polar) and B- hydrophilic(polar)β’ When amphotericin binds with the fungal cell membrane,it makes a special channel (micropore), andincreasethecell membrane permeability, so that thehydrophilicportion of drug can penetrate easily andresult inthecellcontents comes out (ions, amino acidsandotherwater-soluble substances). β’ When the lipid portion of AmphotericinBbindstofungalcell membrane, it is called βmicroporeβ. β’ Given orally (50β100 mg QID) for intestinalmoniliasis; also topically for vaginitis, otomycosis,etc. β’ active against a wide range of yeastsandDownloaded from HK Technical PGIMS (pgims.hktechnical.com)
fungiβCandida albicans, Histoplasmacapsulatum,Cryptococcus neoformans, Leishmaniaetc. Adverse effects:
1. Acute reaction: on infusion causes chills, fever, aches,nausea, vomiting and dyspnoea (Shortnessof breath).2. Thrombophlebitis (inflammatory processintheveindue to clot formation) of the injectedvein. 3. Long-term toxicity: Nephrotoxicity
4. CNS toxicity: intrathecal (Spinal cord) injectioncausesheadache, vomiting, nerve palsies, etc. Uses: Amphotericin B can be appliedtopicallyfororal,vaginal and cutaneous candidiasis andotomycosis.β’ Used in Febrile neutropenia
β’ Used in Leishmaniasis (an infectioncausedbyleishmania parasite)
β’ Conventional formulation of AMB (C-AMB):
For systemic mycosis, C-AMB is availableasdrypowder along with deoxycholate(DOC)forextemporaneous dispersion before use. β’ Liposomal amphotericin B (L-AMB): β’ It has been produced to improve tolerabilityofi.v.infusion of AMB, reduce its toxicityandachievetargeted delivery. It consists of 10%AMBincorporatedin liposomes made up of lecithinandotherDownloaded from HK Technical PGIMS (pgims.hktechnical.com)
biodegradable phospholipids. Nystatin
β’ Obtained from S. noursei. β’ Similar to Amphotericin in antifungal action. β’ Due to high systemic toxicity, usedonlylocallyinsuperficial candidiasis. β’ AE: Nausea and bad taste in mouth. β’ Used in vaginitis, oral thrush, corneal, conjunctivalandcutaneous candidiasis, diarrhoea. β’ Dosage: MYCOSTATIN 5 lakh U tab (1mg=2000U).Caspofungin
β’ active mainly against Candida and Aspergillusstrains.β’ MOA: inhibits the synthesis of Ξ²-1, 3-glucan, whichisaunique component, responsible for toughnessoffungalcell wall. As a result cell wall disrupt. β’ It is not absorbed orally; has to be infusedi.v. β’ Uses: deep and invasive candidiasis, esophagealcandidiasis.
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β’ Dose: 70 mg loading dose infusedi.v. over1hour,followed by 50 mg i.v. daily. Griseofulvin
β’ Obtained from Penicilliumgriseofulvum. β’ It is fungistatic against Epidermophyton, Trichophyton,Microsporum, etc. β’ MOA: It interferes with mitosisβmultinucleatedandstunted fungal hyphae are produced under itsaction.Italso causes abnormal metaphase configurations. β’ AE: Headache, g.i.t. disturbances, rashes, photoallergy.β’ Uses: used orally only for dermatophytosis. β’ Dose: 125β250 mg QID with meals, usedfor
Scalp 4 weeks
Palm, soles 6 to 8 weeks
Finger nails 6 to 8 months
Toe nails 10 to 12 months
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Imidazoles and Triazoles:
β’ They are broad spectrumantifungal drugscoveringdermatophytes, candida, other fungi involvedindeepmycosis, Nocardia and Leishmania. β’ They inhibit the fungal cytochromeP450enzymeβlanosterol 14- demethylaseβ whichisrequiredforergosterol synthesis. Thus leadingtomembraneabnormalities in the fungus. Clotrimazole:
β’ Effective in the topical treatment of tineainfectionslikeringworm, athletesβ foot, otomycosis andoral/cutaneous/vaginal candidiasis. β’ Dose: SURFAZ, CLODERM1% lotion, cream, powder.Econazole:
β’ Similar to clotrimazole; penetrates superficial layersofthe skin and is highly effective indermatophytosis,otomycosis, oral thrush.
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β’ Dose: ECONAZOLE 1% oint. Miconazole:
β’ Highly efficacious (>90% cure rate) drugfortinea,pityriasis versicolor (yeast infectionof theskin),otomycosis, cutaneous and vulvovaginal candidiasis.β’ AE: vaginal irritation, pelvic cramps. Ketoconazole (KTZ):
β’ First orally effective broad-spectrumantifungal drug,useful in both dermatophytosis and deepmycosis. β’ Dose is 200 mg OD or BD, used in shampoo. β’ AE: hormonal effects, gynaecomastia, lossofhair,menstrual irregularities.
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Fluconazole:
β’ Has a wider range of activity than KTZ. β’ Used in cryptococcal meningitis, systemicandmucosalcandidiasis. β’ AE: nausea, vomiting, abdominal pain, rashandheadache.β’ Uses: can be taken orally as well as i.v. (insevereinfections). β’ Used in vaginal candidiasis, oropharyngeal candidiasis,tinea infections and cutaneous candidiasis.
Itraconazole:
β’ Orally active triazole antifungal moreefficaciousthanKTZ or fluconazole. β’ Well tolerated in doses below 200 mg/day. β’ Dizziness, pruritus, headache and hypokalaemiaaretheother common side effects.
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Posaconazole :
β’ This recently introduced broad-spectrumtriazolehasmore potent antifungal activity andistheonlyazolewhich has shown efficacy in mucormycosis. Terbinafine
β’ Orally and topically active drug against dermatophytesand Candida. β’ Fungicidal in nature. β’ It acts as a non-competitive inhibitor of βsqualeneepoxidaseβ
, an early step enzymeinergosterolbiosynthesis by fungi. β’ Side effects: gastric upset, rashes, tastedisturbance,hepatic dysfunction, haematological disorder andseverecutaneous reaction. β’ Uses: Terbinafine applied topically as 1%creamtwicedaily is indicated in localized tinea pedis/ cruris/corporis(infection between toes, rashes in groin) andpityriasisversicolor.
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