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ANTIJAMUR, ANTIMALARIA DAN ANTIHELMINTIKYesi AstriDepartemen Farmakologi dan FarmasiFakultas Kedokteran Universitas Muhammadiyah Palembang... ANTIJAMUR ...(ANTIFUNGAL)Drugs that affect fungal membranes1. Amphotericin B (Fungizone) a. Structure and mechanism of action-is an antibiotic that binds to ergosterol (a major componenet of fungal cell membranes) and alters membrane to allow leakage of cellular contents.b. Pharmacologic properties-poorly absorbed from the gastrointestinal tract and; has poor penetration into the CNS.-eliminated predominantly through the biliary route.- Can be detected in urine for weeks after cessation of therapy.c. Therapeutic usesis used to treat most severe fungal infection, including those caused by Candida albicants, Histoplasma capsulatum, Cryptococcus neoformans, especially in immunocompromised patients.Is the most effective antifungal agent and is usually the drug of choise for major systemic infections. In some cases, combination therapy with flucytosine is advantageous.2.Ketonazole, miconazole, clotrimazole, and fluconazole

a. General propertiesare imidazole derivates that block the synthesis of ergosterol by inhibiting the cytochrome P-450-mediated sterol 14-demethylase.Are broad-spectrum antifungals; also inhibit many gram-positive bacteria and some protozoa.Ketonazole (Nizoral)-can be administered orally; elevation of gastric pH impairs absorption. It does not penetrate CSF.-Is extensively bond to plasma protein. -Most commonly causes gastric upset (3%-20% of patients). Itching, rashes, and headaches are observed in 1% of patients.-Is useful for treatment of mucocutaneous candidiasis, histoplasmosis, and paraccoccidioidomycosis as well as dermatophyte infections.Miconazole (Monistat)

-is available for IV administration, but this is associated with a high incidence of adverse effects (phlebitis, pruritus, nausea, and anemia). It is generally used only when amphotericin B is contraindicated.- Is available for topical application, which is associated with high incidence of burning and itching. Can be used for tinea pedis, ringworm, and cutaneous and vulvovaginal candidiasis. d. Clotrimazole (Lotrimin, Mycelex) and terconazole (Terazol)are available for topical application and are useful for many dermatophyte infections.

e. Fluconazole (Diflucan)-is available for I or oral administration.-Is useful for oropharyngeal, isopharyngeal, and systemic candidiasis. Also used for acute and maintenance therapy of cryptococcalmeningitis.

3. Nystatin

-is a polyene antibiotic similar in structure and mechanism of action to amphotericin B.- is too toxic for systemic administration. Is not absorbed from the gastrointestinal tract; oral preparations can be used prophylactically with tetracycline to prevent superinfection of the intestine.Other antifungal agents1. Griseofulvin (Fulvicin, Grisactin)-binds to microtubules and prevents spindle formation and mitosis in fungi. Also binds filament proteins such as keratin. The drug accumulates in skin, hair, and nails.-adequately absorbed after oral administration -administered as oral therapy for dermatophyte infections.-used for long-term therapy of hair and nail infections.Flucytosine (Ancobon)Is actively transported into fungal cells and is converted to 5-fluorouracil and subsequently to 5-fluorodeoxyyuridylic acid, which is an inhibitor of pyrimidine and nucleic acid synthesis. Human cells lack the ability to convert large amounts of flucytosine to the uracil form.Is well-absorbed afer oral administration; penetrates many tissues, including the CNS.Is rarely used as a single drug, but often is used in combination with other antifungal agents.... ANTIMALARIA ...KLASIFIKASI ANTIMALARIASkizontosid jaringan pencegahan kausatif, pencegahan relapsSkizontosid darah pengobatan supresi dan klinikGametosid membunuh gametosid di eritrositSporontosid menghambat perkembangan gametosid, tapi tidak membunuhnyaAntimalaria yang TersediaKlorokuinPirimetaminPrimakuinKinaMeflokuinProguanilArtemisinAtovakuon

Prinsip Kemoprofilaksis dan Terapi MalariaEndemis atau tidaknya suatu daerah sehingga dapat diketahui strain yang resistenAdanya P. ovale dan P. Vivax, yang sering menyebabkan relapsKehamilanReaksi intoleransi

... ContMalaria akut akibat P.falcifarum, P.vivax, P.ovale dan P.malariae skizontosid darah (klorokuin dan kina)Ditambahkan Primakuin untuk infeksi akibat P.vivax dan P.ovale.... ContKemoprofilaksis malaria : skizontosid darah (klorokuin), dosis dewasa 500mg/minggu (anak-anak : 5mg/kgBB), dimulai 1 minggu sebelum memasuki daerah endemis, selama di lokasi dan berakhir 4 minggu setelah meninggalkan lokasi.Untuk daerah endemis yang diketahui resisten terhadap klorokuin kombinasi pirimetamin dan sulfadoksin (dosis tunggal 3 tablet)... ContPengobatan pada wanita hamil :- trimester 1 : klorokuin atau proguanil- trimester 2 dan 3 : klorokuin/proguanil/meflokuin... ANTIHELMINTIK ...ANTIHELMINTIKMekanisme kerja obat :- Lokal: mengeluarkan cacing dari saluran cerna- Sistemik: mengeradikasi cacingAntihelmintik yang ideal :1. efektif dan aman2. praktis pemakaiannya (oral, dosis tunggal)3. stabil pada jangka waktu tertentuBENZIMIDAZOLDerivat mebendazol, albendazol, tiabendazolMekanisme kerja :1. menghambat polimerase mikrotubulus parasit2. menghambat fumarat reduktase mitokondria

... ContIndikasi 1. Tiabendazol kutaneus larva migran2. Mebendazol askariasis, enterobiasis, trikuriasis3. Albendazol nematoda, kista hidatid, neurosistiserkosis ... Cont... Cont Prazikuantel meningkatkan permeabilitas membran terhadap Ca kontraksi dan paralisis spastis.Menyebabkan kerusakan tegumen Indikasi : skistosomiasis, klonorsiasis, taniasis

... ContPirantel PamoatMenghambat depolarisasi neuromuskular paralisis spastikIndikasi : askariasis dan enterobiasis, A.duodenale, N.americanus, T.trichiura

...thank you...TUGASAmoksisilin Ceftriaxon CefiximTetrasiklin Vancomicin SkizontosidGametosidKetokonazolMebendazol Pirantel Pamoat

AsiklovirAmphotericin BIvermektin Prazikuantel NistatinKloramfenikolRifampisinEritromisinMetronidazolKarbapenem

PETUNJUKTULISKAN PROFIL FARMAKOKINETIK, MELIPUTI : ABSORPSI, DISTRIBUSI, METABOLISME DAN EKSKRESI

TULISKAN PROFIL FARMAKODINAMIK, MELIPUTI : MEKANISME KERJA, EFEK SAMPING, INTERAKSI OBAT, DOSIS