Farmakologi Obat Antibiotik
Farmakologi Obat Antibiotik
Farmakologi Obat Antibiotik
Soluble in body
Stable in body
Selectively toxic
Consistent Toxicity
Non-allergic
Bacterial resistance difficult to develop
Umur simpan yang panjang
Reasonable cost
Terms/Concepts of Antimicrobial Agent
• Selective Toxicity
• Spectrum of Activity
• Mode of Action
• Side Effects
• Resistance
Selective Toxicity
• Concentration that eliminates pathogen
– Therapeutic dosage level
• Concentration that causes damage to host
– Toxic dosage level
PENGGOLONGAN ANTIBIOTIK
BERDASARKAN DAYA KERJANYA
• ZAT BAKTERISIDA, pada dosis biasa berkhasiat mematikan
kuman
1. Zat yang bekerja pada fase tumbuh (penisilin, sefalosporin,
polipeptida, rifampisin, asam nalidiksat, kuinolon)
2. Zat yang berkerja terhadap fase I stirahat
(aminoglikosida, nitrofurantoin, INH, klotrimoksazol)
• ZAT BAKTERIOSTATIK, pada dosis biasa terutama
berkhasiat menghentikan pertumbuhan dan perbanyakan
kuman (Sulfonamida, kloramfenikol, tetrasiklin, makrolida,
linkomisin)
Prinsip Penggunaan Antibiotik
• A. Berdasarkan penyebab infeksi: Dari hasil
pemeriksaan mikrobiologis, pemberian antibiotika tanpa
pemeriksaan mikrobiologis dapat didasarkan pada
educate guess.
• B. Berdasarkan faktor pasien: Fungsi ginjal dan hati,
riwayat alergi, daya tahan terhadap infeksi, daya tahan
terhadap obat, usia, wanita hamil dan menyusui.
PENGGOLONGAN ANTIBIOTIK
BERDASARKAN Spectrum of Activity
• Rentang mikroorganisme yang dipengaruhi oleh
agen
• Spektrum luas
• Jangkauan luas, mis. baik gram-pos & gram-neg
• Digunakan saat agen bakteri infektif aktif tidak
diidentifikasi secara tepat.
– Spektrum sempit
• Jumlah terbatas, atau kelompok bakteri tertentu
• Digunakan untuk mencegah perkembangan resistensi
• Kurang mempengaruhi flora bakteri normal
Spectrum
1. Cell Wall
2. Cell membrane
3. Protein synthesis
4. Nucleic Acid Synthesis
5. Antimetabolites
Some clinically important antibiotics
Site or mode of
Antibiotic Producer organism Activity
action
Penicillin Penicillium chrysogenum Gram-positive bacteria Wall synthesis
penicillin
– Chemical characteristics
– Spectrum of activity
– Development of bacterial resistance
• Methicillin
– Penicillinase resistant
– resistance by an different mechanism developed
• Ampicillin
– broad spectrum ( gram-neg & gram-pos)
– acid resistant, i.e. oral administration
β-lactam Antibiotics
Cephalosporins
• Produced by fungi, Cephalosporium
• ring similar to penicillins
– so action similar to penicillins
• Originally for gram-positive cocci
• Used when
– infecting bacterial strain is reistant due to penicillinase
– when allergy or toxicity to penicillin present
• Broader spectrum
• few serious side effects
– Local irritation at injection site
– Nausea, vomiting, diarrhea
– Penicillin allergic persons can also be sensitive (~15%)
Antibiotics
• Bacitracin
– Produced by Bacillus licheniformis
– Small polypeptide
– Inhibits cell wall formation Luka tembak
– Used on lesions & wounds because:
• Poorly absorbed in body luka
• Toxic to kidneys
• Vancomycin
– Streptomyces
– Very narrow spectrum
– Used against Staphylococcus that is resistant to penicillin
– Vancomycin resistance is now developing
dihasilkan
Cell Wall -
Antimycobacterial
• Isoniazid (INH)
– Inhibits synthesis of mycolic acid in cell wall of
Mycobacteria
• Tuberculosis
resistance mencegah
– Administered with other antibiotics to prevent
• Ethambutanol
development of
– Inhibits incorporation of mycolic acid into cell wall
• Rifampin (inhibits mRNA synthesis)
– Hits alternative target in cell
• Isoniazid Complications
translokasi
lon
• Ciprofloxacin
• Menghambat DNA girase (topoisomerase II)
Sulfa
• Analog PABA
• Menghambat terbentuknya THF (carrier
karbon yang digunakan dalam sintesis A, G,
T dan M)
3. SELEKSI ANTIBIOTIK
ANTIBIOTIKA APAKAH YANG PALING TEPAT ?