1.KELOMPOK 2

2. MIKOSIS SuperficialisInter- ProfundaDermatofitosisNon mediate SubcutisSistemikDermatofitosisTinea capitisPitiriasisKandidiasisMisetoma AktinomikosisTinea barbaeversikolor Aspergillosis Kromomikosis Nokardiosis Tinea corporisPiedra hitam Sporotrikosis Histoplasmosis( T. imbrikata & Piedra putih Fikomikosis -KriptokokosisT. favosa )Tinea nigrasubkutan KoksidioidomikosisTinea manumpalmarisRinosporodiosis Blastomikosis Tinea pedisOtomikosis Fikomikosis -Tinea krurissistemik Tinea unguium 3. Description of the contents 4. Antifungal Agents Polyene antibiotic The polyene antibiotics bind with sterols in the fungal cell membrane, principally ergosterol. This causes the cells contents to leak out and the cell dies. Animal cells contain cholesterol instead of ergosterol and so they are much less susceptible. Nystatin Amphotericin B (may be administered liposomally) Natamycin Rimocidin Filipin Pimaricin 5. Nystatin: The first antibiotic against fungi Like many other antimycotics and antibiotics, nystatin is of bacterial origin. It was isolated from Streptomyces noursei in 1950 by Elizabeth Lee Hazen and Rachel Fuller Brown, who were doing research for the Division of Laboratories and Research of the New York State Department of Health. The soil sample where they discovered nystatin, was from the garden of Hazens friends called Nourses, therefore the strain was called noursei. Hazen and Brown named nystatin after the New York State Public Health Department (now known as the Wadsworth Center) in 1954. The two scientists donated the royalties from their invention, over $13 million dollars, to the nonprofit Research Corporation for the advancement of academic scientific study. Elizabeth Lee Hazen and Rachel Fuller Brown were inducted into the National Inventors Hall of Fame in 1994. 6. Antifungal Agents Imidazole and triazoleThe imidazole and triazole groups of antifungal drugsinhibit the enzyme cytochrome P450 14-demethylase.This enzyme converts lanosterol to ergosterol, and isrequired in fungal cell membrane synthesis. These drugsalso block steroid synthesis in humans. Imidazoles: MiconazoleBifonazole KetoconazoleButoconazole ClotrimazoleEconazole Mebendazole Fenticonazole Isoconazole Oxiconazole Sertaconazole Sulconazole Thiabendazole Tiaconazole 7. Antifungal Agents The triazoles are newer, and areless toxic and more effective: Fluconazole Itraconazole Ravuconazole Posaconazole Voriconazole 8. Antifungal Agents Allylamines Allylamines inhibit the enzyme squalene epoxidase, another enzyme required for ergosterol synthesis: Terbinafine - marketed as Lamisil Amorolfine Naftifine Butenafine 9. Antifungal Agents Echinocandin Echinocandins inhibit the synthesis of glucan in the cell wall, probably via the enzyme 1,3- glucan synthase: Anidulafungin Caspofungin Micafungin 10. Antifungal Agents Others: Flucytosine is an antimetabolite. Griseofulvin binds to polymerized microtubulesand inhibits fungal mitosis; It is derived from themold Penicillium griseofulvum. Fluocinonide Salicylic Acid (topical) Tinactin or Tolnaftate Potassium Iodide 11. Anti jamur untuk infeksi sistemik1. AMFOTERISIN B Bersifat fungistatik /fungisidaltergantung dosis & sensivitivitas jamur 12. Farmakokinetika Absorpsi melalui saluran cernasedikit. T 24 - 48 jam. Kadar mantap dicapai setelahbeberapa bulan. Dapat melewati plasenta,CSS &vitreus. Ekskresi melalui ginjal lambat sekali. 13. Efek sampingInfus kulit panas, keringatan, sakitkepala, demam, flebitis ,penurunanfungsi ginjal > 80% pasien ,dll.Derajat kerusakan ginjal tergantungdosis.Efek toksik ginjal dapat ditekan denganpemberian bersama flusitosin. 14. Indikasi1. Terapi awal infeksi jamur yang mengancam kehidupan2. Koksidiomikosis,Aspergilosis, kandidiosis dll.3. Obat terpilih (Drug of choice) untuk Blastomikosis. 15. Perhatian1. Selama pengobatan pasien harus di rawat di rumah sakit2. Monitoring ketat urinalisis, darah dan kimia darah (K,Mg,ureum dan kreatinin) menjelang tercapai dosis optimal3. Bila terjadi insuffisiensi ginjal,terapi stop 16. 2. FLUSITOSIN Spektrum sempit Efektif untuk kriptokokosis,kandidiasis, Aspergilosis Bila diberikan bersamaAmfoterisin B bersifatsupraaditif. 17. Efek samping Toksisitas < amfoterisin B Dapat menimbulkan anemia, leukopenia dan trombositopenia Tidak bersifat nefrotoksik. Keamanan pada ibu hamil belum terbukti. 18. 3. Imidazol & Triazol Spektrum luas Terdiri dari : ketokonazol, mikonazol,fluokonazol , dll. Banyak digunakan sebagai anti jamursistemik. Vorikonazol relatif baru, tosisitas lebih rendah. 19. ANTI JAMUR UNTUK INFEKSIDERMATOFIT & MUKOKUTAN1. Griseofulvin in vitro efektif terhadap berbagai jenis jamur. Absorpsi melalui sal cerna kurang baik Efek samping : Leukopenia & granulo sitopenia. Sediaan tablet 125 mg & 500mg 20. ANTI JAMUR UNTUK INFEKSIDERMATOFIT & MUKOKUTAN2. Imidazol & triazol3. Tolnaftat4. Nistatin Mekanisme kerja : Nistatin + sterol perubahan permeabilitas membran sel sel kehilangan berbagai molekul kecil 21. Nistatin Merupakan antibiotik polien. Mekanisme kerja : berikatan denganergosterol pada membran jamur,permeabilitas meningkat, sel jamur mati. Indikasi : kandidiasis kulit, selaput lendir,dan saluran cerna. Efek samping : jarang ditemukan, mual,muntah, diare ringan 22. ANTI JAMUR LAIN Asam benzoat & as salisilat(whitfield) 2 : 1 Asam benzoat fungistatik Asam salisilat keratolitik Asam undesilenat Haloprogin 23. PERTIMBANGAN TERAPI Infeksi berat gol imidazol Lesi hiperkeratosis kuku antijamur topikal + zat keratolitik Infeksi jamur dgn tandaradanghebat anti jamur +kortikosteroid Tinea versikolor seleniumsulfid 24. ANTELMENTIKObat untuk memberantas atau mengurangiinfestasi cacing dalam lumen usus ataujaringan tubuhAntelmentik lama kurang amankurang efektifAntelmentik baru lebih aman & efektif rasa tidak mengganggu, sebagian dapat diberikan oral, dosis tunggal. 25. Jenis infestasi cacing Cacing tambang (ankilostomiasis) Cacing kremi (enterobiasis) Cacing gelang (askariasis) Cacing Pita (taeniasis) Filaria (W bancrofti, B malayi, Loaloa (filariasis) dll. 26. 1. Dietilkarbamazin Obat pilihan pertama untukfilariasis Dapat menghilangkanmikrofilaria W bacrofti, B malayi, loa loa dari peredaran darah. 27. DietilkarbamazinMekanisme kerja :1.Menurunkan aktivitas otot cacingparalisis2.Menyebabkan perubahan padapermukaan membran mikrofilariasehingga mudah dihancurkan. 28. Efek sampingRelatif aman pada dosis terapiPusing,gangguan sal cerna, sakit kepaladll.Reaksi alergi karena matinya parasitdan substansi yang dilepaskan olehmikrofilaria yang hancur. 29. 2. Piperazin Efektif terhadap A. lumbricoides &E vermicularis Mekanisme kerja : Blokade respon otot cacingterhadap asetil kolin paralisis Cacing mudah dikeluarkan olehperistaltik usus,cacing keluar 1-3hari setelah pengobatan. 30. 3. Pirantel Pamoat Untuk : caing kremi, gelang,tambang. Mekanisme kerja : depolarisasi ototcacing dan meningkatkan frekuensiimpuls Cacing mati dalam keadaan spastis 31. Pirantel Pamoat Absorpsi kurang baik, ekskresisebagian besar melalui tinja Efek non terapi: keluhan saluran cerna,demam & sakit kepala Kontra indikasi : wanita hamil,Usia < 2 tahunPemberian bersama piperazin 32. Pirantel Pamoat Obat terpilih untuk : askariasis,ankilostomiasis, enterobiasis &strongiloidiasis Sediaan : tablet 125mg, 250 mgDosis 10 mg/kgBB, dosis tunggal 33. Antelmentik 34. 4. Mebendazol Spektrum paling luas, obat terpilihuntuk enterobiasis & trichuriasis.Mekanisme kerja : menyebabkan kerusakan struktursubseluler & menghambat sekresiasetilkolinesterase cacing. Menghambat ambilan glukosa secarairreversibel. 35. Antelmentik lain Levamisol Niklosamid Niridazol Prazikuantel Ivermektin, dll. 36. TERAPI PILIHAN HelminthTreatment of ChoiceAscaris Albendazole, Mebendazole PlumbricoidespamoatE. vermicularis Albendazole, Mebendazole, PHookworms pamoatTrichuris trichiura Albendazole Mebendazole, PFilaria pamoatMebendazole, albendazoleDietilcarbamazineCutaneus larvaThiabendazol (topical), ivermectin,migrans AlbendazolS. stercoralisIvermectin, Thiabendazoleect 37. Rational Use of Antimalarial Drugs1. Choice of Antimalarial Drugs: Control symptoms: chloroquine Cerebral malaria: chloroquine phosphate, quinine bimuriate, artemisinin injection Chloroquine-resistant falciparum malaria: quinine, mefloquine, artemisinin Dormant hypnozoite stages : pyrimethamine + primaquine Prophylaxis: pyrimethamine, chloroquine2. Combination therapy: chloroquine + primaquine: symptom stages pyrimethamine + primaquine: dormant hypnozoite stages Combination of drugs with different mechanisms: therapeutic effect, resistance 38. Drug ClassificationClassified by their selective actions on different phases of the parasite life cycle:1. Tissue schizonticides(): eliminate developing or dormant() liver forms.2. Blood schizonticides: act on erythrocytic parasites.3. Gametocides(): kill sexual stages and prevent transmission to mosquitoes.No one available agent can reliably effect a radical cures. 39. Anti-amebiasis Drugs Amebiasis is infection with Entamoeba histolytic. Amebiasis is transmitted through gastrointestinaltract. Ameba has two stages of development: cyst() and trophozoite().Cysts small intestine little trophozoites (ileocecum)cysts (colon) asymptomatic intestinal infection,source of infectionbig trophozoites (tissues of intestine) intestinalamebiasis extraintestinal infection 40. CHLOROQUINE A synthetic 4-aminoquinoline formulated as thephosphate salt for oral use. Pharmacokinetics Rapidly and almost completely absorbed from thegastrointestinal tract. Very large apparent volume of distribution of 100-1000 L/kg. Necessitate the use of a loading dose to rapidlyachieve effective serum concentrations. Slowly released from tissues and metabolized. Principally excreted in the urine. 41. Pharmacological Effects1. Antimalarial action: highly effective blood schizonticide. Moderately effective against gametocytes of P vivax, P ovale, and P malariae but not against those of P falciparum. not active against liver stage parasites. Mechanism: plasmodium aggregates chloroquine. chloroquine incorporated into DNA chain of plasmodium inhibit proliferation. chloroquine prevents the polymerization() of the hemoglobin() breakdown product, heme(), into hemozoin() and thus eliciting parasite toxicity due to the buildup of free heme. pH plasmodium protease activity Resistance: very common among strains of P falciparum and uncommon but increasing for P vivax. The mechanism of resisitance to chloroquine is resistant strains excretes drug more rapidly.2. Killing Amibic trophozoites : chloroquine reaches high liver concentrations.3. Immunosuppression action: 42. Clinical Uses1. Treatment: nonfalciparum and sensitive falciparum malaria. Primaquine() must be added for the radical cure of P vivax and P ovale, because chloroquine does not eliminate dormant liver forms of these species.2. Chemoprophylaxis: for without resistant falciparum malaria in malarious regions.3. Amebic liver abscess(): not effective in the treatment of intestinal or other extrahepatic amebiasis. 43. Adverse Effects and Cautions Usually very well tolerated, even with prolonged use. Pruritus() is common. Nausea, vomiting, abdominal pain, headache,anorexia(), malaise(), blurring ofvision(), and urticaria() are uncommon. Dosing after meals may reduce some adverse effects. Rare reactions include hemolysis in G6PD-deficientpersons, impaired hearing, confusion, psychosis,seizures, hypotension, ECG changes. teratogenesis 44. Metronidazole A nitroimidazole(). The nitro group ofmetronidazole is chemically reduced inanaerobic() bacteria and sensitiveprotozoans. Reactive reduction products appearto be responsible for antimicrobial activity. Pharmacokinetics Oral metronidazole is readily absorbed andpermeates all tissues by simple diffusion. Protein binding is low (