nsaids (mefenamic acid/asam mefenamat)
TRANSCRIPT
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Kelompok IVKetua :1. Raditiya Yoharni
10. Dwi Melliza2. Ferry Zulfachmi 11. Monica Anandita3. Rizky Jaya Amal 12. Marsillina4. Muhammad Deni Ansa 13. Ozza Mutiara
Vonna5. Rahmat Risky Jayusni 14. Cut Sandra
Ardilla6. Taufiq Andrian 15. Hilda Annisa7. Sayed Ikramullah 16. Mardhatillah8. Irwan Avianda 17. Evine9. Indah Sabrina
By PresenterMedia.com
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NSAIDs ( Non-Steroid Anti-inflamasi Drugs
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Pendahuluan
• NSAID sering disebut sebagai aspirin-like drugs
• Gol. Obat ini menghambat enzim COX sehingga
konversi asam arakidonat PGG2 terganggu
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Biosintesis Prostaglandin
Trauma/luka pada sel
Gang, membran selenzim fosofilipase
Asam ArakidonatEnzim Lipooksigenase Enzim COX
Hidroperoksid OAINSEndoperoksid PGG2
PGE2,PGF2,PGD2 Leukotrien Tromboksan A2
Prostaksiklin
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Asam Mefenamat (Mefix)Struktur Kimiawi
• Rumus Molekul : C15H15NO2
• Berat Molekul : 241.29
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Farmakokinetik
• Diabsorbsi pertama kali dari lambung dan usus selanjutnya obat akan melalui hati
diserap darah dan dibawa oleh darah sampai ke tempat kerjanya
• Half-Life = 2 jam
• Puncak Plasma Waktu: 2-4 jam (1 g dosis)
• Puncak Plasma Konsentrasi: 10 mcg / mL (1 g dosis)
• Terikat kuat pada protein plasma
•Metabolism: Hepatic oxidation/conjugation
•Enzymes inhibited: Cyclooxygenase
Excretion: urine 66% (single dose); feces 20-25%
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Farmakodinamik• Menghambat sintesis prostaglandin dalam jaringan tubuh dengan menghambat minimal 2 isoenzim siklooksigenase, siklooksigenase-1 (COX- 1) dan -2 (COX-2)• Dapat menghambat kemotaksis• Mungkin mengubah aktivitas limfosit T memproduksi limfokin dan pengurangan vasodilatasi akibat peradangan• Mengurangi aktivitas sitokin pro inflamasi Ex : TNF, IL-1• Dapat menghambat agregasi neutrofil
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Dosis dan indikasi• Sediaan : Caps. 250mg, Tab. 500mg.•Dewasa :
• Nyeri akut : awal 500mg PO, selanjutnya 250mg PO q6hr PRN Max 7 hari• Disminero primer : awal 500mg PO, selanjutnya 250mg PO q6hr PRN Max 7 hari• Pemberian : gunakan setelah makan utk menghindari E.S pada GI• Utk Dis.Primer : gunakan saat onset nyeri dan perdarahan terjadi
•Pediatric:
• Nyeri akut Dan dismero primer : <14 years old: Not recommended
• > 14 th : sama seperti dewasa
•Geriatri
• Nyeri akut : sama seperti dewasa
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Kontraindikasi dan Waspada!!!
• Resiko Cardiovaskular• Hipotesa ketidak seimbangan prostasiklin dan tromboksan A2
• Resiko Gastrointestinal(GI)
Black Box Warning
Kontraindikasi Perhatian!!!• Hipersensitivitas - Anemia• acetyl-salicylic acid (ASA) Alergi - Bronko spasme• Ulkus/Inflamasi GI - Retensi Cairan• Late pregnancy - Kerusakan Hepar & Renal
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Tingkat ratio kejadian kardiovaskular
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Efek Samping & Interaksi obat
• Peningkatan LFTs
> 10%
1-10%• Abdominal pain - pyrosis• Anorexia - gastritis• Diarrhea - flatulence• Nausea - constipation
- steatorrheaUpper GI ulcers, gross bleeding/perforation (1% of patients treated for 3-6 mth and 2-4% of those treated for 1 yo)
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Efek Samping<1%
• Leukopenia• Eosinophilia• Thrombocytopenic purpura• Agranulocytosis• Pancytopenia• Bone marrow hypoplasia• Renal failure
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Interaksi obatTerhadap antikoagulan harus diperhatikan!!!
• warfarin• heparin
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