ANTI BIOTIK II -...
Transcript of ANTI BIOTIK II -...
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ANTI
MIKROBA
II
TIM FARMAKOLOGI
FKH UB 2019
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ANTI PARASIT
ANTI FUNGAL
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ANTI PARASITIC DRUG
•Anthelmintic
•AntiprotozoaENDOPARACITIDES
• InsectisidaECTOPARACITIDES
• Endo dan ectoENDECTOCIDES
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ANTHELMINTIC
WATER INSOLUBLE
• Suspension, pasta, granule
SOLUBLE
• Inject, oral, topical
PARTICLE SIZE
• Small : mudah diabsorbsi GI tract
• Large
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GOL. BENZIMIDAZOLE
– Bekerja dengan mempengaruhi metabolisme energi cacing
– Umumnya diakhiri dengan –azole
– Albendazole, mebendazole, tinidazole, Thiabendazole
– Efek samping : relatif jarang, vomite, diare, lethargy
– Masing2 obat memiliki keefektifan terhadap cacing tertentu
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– Resistensi small strongyles (horses) & abomasal
trichostrongylus (sheep)
– Punya efek antiinflamasi & anti fungi
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– Broad spectrum : roundworms, lungworms,
tapeworms &adult flukes of Fasciola hepatica
– ternak
– Efek : hepatotoksisitas & teratogenik
– KI : hewan bunting
ALBENDAZOLE
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– Broad spectrum
– Efek anthelmintik : nematoda, Thricuris sp,
Thricostrongylus sp, u/ cestoda efeknya bervariasi
– KI : Tidak boleh diberikan utk hewan bunting
(embriotoksik & teratogenik)
– Hati2 penggunaan pada hewan sirosis
MEBENDAZOLE
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– Biasa dipakai utk kuda, produk utk anjing umumnya kombinasi
– Menyebabkan Liver toxicity, kombinasi dengan diethylcarbamazine: heartworm, not used anymore
– Small animal, food animal,
horses, birds, reptiles
– Lungworm & Liver fluke: 10
– 14 days
– Bisa utk Giardiasis yg
resisten metronidazole
– Bisa utk hewan laktasi
OXIBENDAZOLE FENBENBENDAZOLE
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PRAZIQUANTEL
– Schistosomiasis dan cercaria
– Mekanisme :
Peningkatan permeabilitas membran sel
nematoda
Gangguan Ca shg terjadi kontraksi
muskulus
Paralisis dan kematian cacing
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PYRANTEL
– Nematoda : ascaris, strongylus, hookworm
– Embryonic effect
– Aman utk hewan laktasi
– pyrantel embonat spastic (tetany) paralyzing
agent obstruksi usus akibat overload cacing
– Cacing keluar bersama feses & muntah
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PIPERAZINE
– Efektif utk Ascaris, tidak untuk tapeworms, whipworms, hookworm, protozoa
– KI : hewan bunting
– Mekanisme :
Gangguan permeabilitas membran & hambatan asetilkolin
Hiperpolarisasi, hambatan GABA pd
otot cacing
Paralisa & kematian cacing
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– Hambat neuromuscular transmission parasit, ekspulsi parasit
– (GABA) agonis pembukaan saluran klorida, hiperpolarisasi saraf dan paralisis parasit. Cacingdikeluarkan oleh gerakan enteric
– Hanya efektif sbg ascarids
– Tidak membunuh tapeworms, whipworms,hookworm, protozoa
– tidak boleh digunakan pada hewan dengan infestasi berat, khususnya anak kuda ascarid-impaction colic atau perforasi usus.
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MACROCYCLIC LACTONES
(AVERMECTIN)
– Milbemycin &
avermectin
– Endo &ectoparasites,
tdk efektif u/ cestodes
or trematodes
Obat berikatan dengan
glutamat-gate Cl ion channel ion pd otot cacing
Gangguan regulasi ion
fluks membran sel
Paralisis
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– Avermectins (ivermectinlike drugs)
– Milbemycins (milbemycin, doramectin, &
moxidectin)
– KI pada anjing yg memiliki mutasi pada mdr
gene 1 gene deletion non fungsional P
glycoprotein (transporter, transmembrane
efflux pump) neurotoksisitas
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https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1636591/pdf/cvj47pg1165.pdf
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– Isolasi actinomycete Streptomyces
avermitilis
– 50 - 300 μg/kg PO, SC
– Tidak punya efek antibakteri / antifungal
– heartworm preventative : 6 μg/kg PO
once a month
– Penggunaan lebih luas pd hewan ternak
IVERMECTIN
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– Sintetik avermectin, topical parasitisides, toksisitas rendah
– Neurotoksik pd parasit mempengaruhi glutamate-gated
chloride ion channels.
– Paralisis dan kematian parasit disebabkan oleh peningkatan
permeabilitas terhadap ion klorida dan hiperpolarisasi sel
saraf. Obat-obatan ini juga mempotensiasi saluran klorida
lainnya, termasuk yang dijaga oleh GABA.
SELAMECTIN
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– Setelah aplikasi topikal, selamektin memiliki
afinitas tinggi untuk kelenjar sebaceous dan
kulit.
– Waktu paruh terminal selamektin : 11 hari
(anjing) dan 8 hari (kucing)
– Anjing : Heartworm, fleas, ear mites,
sarcoptes mange, beberapa caplak tertentu
– Kucing : heratworm, roundworm, hookworm,
fleas, ear mites
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– Efektif terhadap psoroptic & sarcoptic mange
– Sediaan 60 or 120 mg/mL spot-on solution.
– Kelinci mite infestations 12 mg/kg
– Penggunaan umumnya 1 bulan sekali
– Kitten umur > 8 mgu
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IMIDAZOTHIAZOLES
– Levamisole, Tetramisole
– Ruminant, poultry
– ascarids, strongyles (paling efektif), whipworms, and
hookworms
– Hambat neuromuskular junction paralisis keluar
bersama feses
– Efek imunomodulasi treatment colon cancer,
rheumatoid arthritis (anti inflamasi)
– Sediaan umumnya kombinasi dg Niclosamide utk
tapeworm
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NICLOSAMIDE
– Efektif utk tapeworm
– Digunakan pada poultry, perikanan
– Sediaan kombinasi dg Levamisole, albendazole
– Aman digunakan pada hewan bunting, hewan muda
– Niclosamide hambat uptake glukosa, fosforilasi oxidative & anaerobic metabolism pada tapeworm
– Efek lain : Hambat H. Pylori; aktivitas kuat thd methicillin-resistant S aureus (MRSA)
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TREATMENT UTK
HEARTWORM
DAILY ORAL
– Diethycarbamazine
– Gunakan selama banyak
ditemukan vektor
– Sediaan kombinasi dg
oxfendazole
MONTHLY ORAL
– Ivermectin
– Milbemycine oxime
Hambat L3, preventif
MONTHLY TOPICAL
– Moxidectin +
imidacloprid (insektisida)
– KI : hewan sakit
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– Melarsomine (anti trypanosoma ) diberikan
pada otot antara Lumbal 3 & 5
– Microfilaricid, konsentrasi maks arsenic darah
dicapai dlm 11 menit (2,5 mg/kg IM)
– Tidak boleh diberikan pd kucing
ADULT HEARTWORM
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– Less toxic dibandingkan thiacetarsamide
– SE : coughing, gagging, lethargy
– Nephrotoxicity & hepatotoxicity
– Tidak direkomendasikan pada hewan dg lage stage /
caval syndrome (large numbers of adult heartworms in
the right ventricle, right atrium, and vena cava).
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ANTI EKTOPARASIT
TIPE
Dips
Spray
Powder
Spot on
Injeksi
Oral
Pour on
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JENIS BAHAN AKTIF
– Chlorinated Hydrocarbons
– Organophosphates
– Carbamates
– Pyrethrins and pyrethroids
– Formamidines
– Imidacloprid
– Fipronil
– Nitenpyram
– Insect Growth Regulators
– Insect Repellents
– Rotenone
– D-limonene
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– Kontak insektisida dg ektoparasit, beracun pada
saluran cerna parasit
– Shampoo anjing
– harmful side effects in people & pets
gunakan pelindung
– Jangan digunakan pd cats, puppies <3 weeks,
lactating animals, food animals.
CHLORINATED
HYDROCARBONS
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– Jenis : Coumaphos, cythidates, cythioat,
diazinon
– Hambat AchE Ach meningkat
overstimulation produces muscle tremors
paralysis (ataxia, loss of motor control).
– Keracunan pd hewan & manusia (OPS)
ORGANOFOSFAT & CARBAMAT
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cythioat Coumaphos
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– Pyrethrins : natural plant products, derivat bunga chrysanthemum
– Pyrethroids : synthetic pyrethrins
– Sangat aman; quick kill
– Adulticide, insecticide/miticide
– Kombinasi dg imidacloprid & pyriproxyfen
– Mempengaruhi membran sel parasit gangguan sodium channel delays polarization paralisis
PYRETHRINS & PYRETHROIDS
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– Non sistemik acaricid dan insecticid
– Aktivitas agonist alfa adrenergik hambat
monoamin oksidase paralisis insekta
– Bahaya bagi mamalia minimal, u/ anjing
demodicosis
– Dipping
AMITRAZ
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– Insektisida broad spectrum
– Disrupt CNS insekta blocking channel GABA-
gate chloride & glutamat-gate chloride (GluCl)
hipereksitasi
FIPRONIL
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– Toksik pd ikan & babi
– “Derris Powder” (derived
from derris root)
ROTENON
– Dari citrus peel
– Aktivitas insektisida
rendah, bau enak,
kombinasi
D-Limonene
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ANTI PROTOZOA DARAH & SAL CERNA
– Allopurinol (Leishmaniosis)
– Doxycycline (Erhliciosis,
Anaplasmosis)
– Imidocarb (babesiosis,
trypanosomiasis)
– Azytrhromycine (Babesiosis)
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ANTI COCCIDIOSIS
– Poultry
– Thiamine antagonist
– Hambat transporter thiamin
Eimeria mencegah uptake
glukosa
– mengganggu proses reproduksi
aseksual Eimeria sp.
AMPROLIUM
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– mengganggu fungsi mitokondria
Eimeria kematian pada semua
tahap perkembangan sel Eimeria
sp. (reproduksi seksual maupun
aseksual).
– Dicampur air minum
TOLTRAZURIL
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– sulfadiazine, sulfadimethylpirimidine, sulfaquinoxaline,
sulfamonomethoxine, sulfadimethoxine
– efektif untuk Eimeria yang menyerang usus halus (E.
acervulina, E. maxima, E. necratix, E. brunetti, E. mitis).
– Potensi sulfanamide meningkat 10 kali
dikombinasikan golongan diamino pyrimidine
(trimetoprim, pyrimethamin)
GOL SULFONAMIDE
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ANTI FUNGAL
– Nystatin
– Amphotericin B
– Natamycin
– Rimocidin
– Filipin
– Pimaricin
POLYENE
ANTIBIOTIK
– Berikatan dg sterol (ergosterol)
membran sel jamur sel jamur
pecah
– sel hewan tdk mengandung
ergosterol tp kolesterol
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– Hambat enzim sitokrom P450 14α-demethylase.
– Enzim ini mengubah lanosterol menjadiergosterol, dan diperlukan dalam sintesismembran sel jamur.
– Gol ini juga memblokir sintesis steroid padamanusia.
IMIDAZOLE & TRIAZOLE
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– Imidazoles:
– Miconazole Bifonazole
– Ketoconazole Oxiconazole
– Butoconazole Fenticonazole
– Econazole Isoconazole
– Sertaconazole
– Sulconazole
– Tiaconazole
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TRIAZOLE are newer, less toxic and more
effective:
– Fluconazole
– Itraconazole
– Ravuconazole
– Posaconazole
– Voriconazole