klasifikasi kemoterapi blok 5
DESCRIPTION
iiTRANSCRIPT
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Klasifikasi kemoterapi
dr. Elly Nurus Sakinah
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Kemoterapi
• Antibakteri• Antimycobacterial• Antifungal• Antiviral• Antiprotozoa• Antihelminth• Antikanker
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Anti Bakteri
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INTRODUCTION
• Antimikroba: obat pembasmi mikroba
• Antibiotik : zat-zat kimia yang dihasilkan oleh fungi dan bakteri yang menghambat atau membunuh mikroba jenis lain.
• Toksisitas selektif
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Mekanisme kerja antibakteri
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MEKANISME KERJA
1. Mengganggu metabolisme sel• Sulfonamid, Trimetoprim
2. Menghambat sintesis dinding sel• Penisilin, Sefalosporin
3. Mengganggu permeabilitas membran sel• Polimiksin
4. Menghambat sintesis protein• Aminoglikosida, Makrolida, Tetrasiklin, Kloramfenikol
5. Menghambat sintesis atau merusak asam nukleat• Rifampisin, kuinolon
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Obserrvasi Invitro
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Klasifikasi
• Aktivitas kerja:1. BAKTERIOSTATIK2. BAKTERISID
• Spektrum:–Broad spectrum–Narrow spectrum
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MEKANISME RESISTENSI
• Menginaktivasi enzim yang merusak obat• Mengurangi akumulasi obat membran sel
bakteri impermeabel thd obat• Perubahan tempat ikatan• Perkembangan jalur metabolik alternatif
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Penggunaan Antibiotik Secara Rasional
1. Tepat indikasi1. Profilaksis2. Terapeutik
1. Empiris: data epidemiologis bakteri2. Terarah: >>>efektif, aman, spektrum sempit
2. Tepat penderita3. Tepat obat4. Tepat dosis5. Waspada terhadap “AE”
(kejadian yang tidak diinginkan, efek samping obat)
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PENGHAMBAT SINTESIS DINDING SEL• GOLONGAN BETA
LAKTAMPENISILIN, SEFALOSPORINMekanisme kerjaantibiotika β laktam memiliki cincin β laktam mencegah ikatan silang diantara rantai polimer peptidoglikan hambat sintesis dinding selBAKTERISID
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PENISILIN
• ADME:– A: di usus terganggu makanan kec. Amoksisilin– D: bebas ke seluruh tubuh, plasenta tapi tidak
teratogenik– M: tidak bermakna– E: ginjal
• EFEK SAMPING: hipersensitivitas, diare, nefritis, neurotoksisitas, gangguan pembekuan darah
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PENISILIN
• Resistensi :– Aktivitas β laktamase– Penurunan permeabilitas terhadp obat– Perubahan protein pengikat penisilin
• OBAT PENTING : Amoksisilin , Ampisilin
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Penicillins : Spectrum of activity and clinical use Natural Penicillins
Anti-Staphyllococcal penicillins
Aminopenicillins
Aminopenicillins plus beta-lactamaseinhibitor
Anti-pseudomonal penicillins
Anti-pseudomonal penicillins plus betalactamase inhibitor
Penicillin GPenicillin V
Oxacillin, Dicloxacillin, Methicillin, Nafcillin
Ampicillin, Amoxicillin
Amoxi-Clavulinic acid, Ampicillin-Sulbactam
Piperacillin, Ticarcillin
Pip-Tazobactam, Ticar-Clavulinic acid
gram-positivebacteria except Staphyllococcus
Resist degradation by penicillinase.Useful for treating S. aureus.No added benefit in treating Strep. species
Extended antimicrobial spectrum.Gram negatives: E. coli, Proteus, Salmonella, Haemophilus, M. catarrhalis, Klebsiella, Neisseria, Enterobacter, Bactoroides.
Used as first line therapy for acute otitis media and sinusitis.
Active against Pseudomonas, E. coli, klebsiella, enterobacter, serratia and B. fragilis.Lower activity against gram positivesOften used with aminoglycosides when treating pseudomonal infections
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Cephalosporins : Spectrum of activity and clinical use
First generation
Second generation
Third generation
Fourth generation
Fifth generation
Cefazolin, Cephalexin
Cefuroxime, Cefaclor
Cefotaxime, Ceftriaxone, CeftazidimeCefixime
Cefepime, Sulperazon
Ceftibiprole
Most gram positive cocci (Strep, S. aureus), E. coli, Proteus, Klebsiella.
Increased activity against H. flu, enterobacter, Neisseria, proteus, E. coli, klebsiella, M. catarrhalis, anaerobes and B. fragilis.
gram negative > gram positive.Useful for meningitis.Ceftriaxone used for highly resistant and multi drug resistant strep pneumo along with vancomycin
Active against Strep, Staph (mssa), aerobic gram negatives (enterobacter, e. coli, klebsiella, proteus and pseudomonas)
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SEFALOSPORIN
• Sebagian besar diberikan intravena, krn absorbsi oral jelek
• Per oral : sefadroksil, sefuroksim, sefiksim.• Efek samping: alergi, perdarahan (akibat efek
anti vitamin K)• Resistensi mirip penisilin
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1. Menghambat sintesis dinding sel▫ Beta lactam:
Penicillin Cephalosporins Monobactam Carbapenem
▫ Vancomycin▫ Bacitracin▫ Daptomycin (new)
2. Meningkatkan permeabilitas membran▫ Polymyxin
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PENGHAMBAT METABOLISME SEL
Mek. Kerja:Kompetisi dg PABA hambat enz.dihidropteroat sintetaseimpermeabel thd as.folatsintesis DNA terganggu
SpektrumBAKTERIOSTATIKEnterobakter, klamidia, pneumocystis
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SULFONAMID• ADME– A: oral cukup baik– D: ke seluruh tubuh, CSS, Plasenta, ASI berikatan
dengan albumin– M: di hati– E :ginjal
• EFEK SAMPING: kristaluria, hipersensitivitas, gangguan darah, kernicterus,potensiasi obat.
• KI neonatus, bayi<2bl, kehamilan
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APLIKASI TERAPEUTIK SULFONAMID
• TOPIKAL: sulfasetamid, sulfadiazin perak combustio
• Trakoma : sulfasetamid topikal dan sistemik atau tetrasiklin
• ISK : kotrimoksazol
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TRIMETOPRIM
• MK inhibitir dihidrofolat reduktase• Spektrum mirip sulfametoksazol, tapi 20-50
kali lebih poten• Resistensi afinitas obat menurun• ADME mirip sulfametoksazol• ES defisiensi folat anemia megaloblastik,
leukopenia, dan granulositopenia.
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KOTRIMOKSAZOLE
• Kombinasi trimetropim dengan sulfametoksazole, BAKTERISID
• MK sinergistik• Spektrum lebih luas dibanding tunggal• Resistensi lebih jarang dibanding tunggal• ESkulit, GIT, SJS• Dosis: 2 dd 2 tab (sulf 400mg+trim 80) selama
3-7 hari
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Adverse effect
• Severe allergic reactions : Anaphylaxis
• Cutaneous reactions– Toxic epidermal
necrolysis or Steven-Johnson syndrome
• Myelosuppression• Hemolytic anemia, esp
in patients with G-6PD deficiency
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PENGHAMBAT SINTESIS ASAM NUKLEAT
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Fluoroquinolones• Ciprofloxacin (IV ;PO/Topical) Ofloxacin (Floxin; Topical), Levofloxacin
(Levaquin; IV ; Oral).
• Synthetic derivatives of nalidixic acid.
• Inhibits DNA gyrase, causing permanent DNA cleavage.
• Pharmacokinetics▫ Excellent bioavailability▫ Excellent tissue penetration : Wide distribution - CSF, saliva, bone, cartilage
• Resistance:▫ DNA Gyrase mutations ▫ Cellular membrane efflux mechanisms.▫ Decreased number of porins in target cells.
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Fluoroquinolones
• Adverse effects.– Headache, dizziness, nausea, lightheadedness– Limit use in pregnancy, nursing mothers, and
children < 18.– Drug interactions: may increase levels of
theophylline, warfarin, caffeine and cyclosporine. – Absorption decreased when taken with cations.– Arthralgias - 1%.
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Protein Synthesis Inhibitors
• Target the bacterial ribosome.• Bacterial – 70S (50S/30S)• Mammalian – 80S (60S/40S)
– High levels may interact with mammalian ribosomes.
• 50S binders - Macrolides, Clindamycin, Chloramphenicol, Streptogramins.
• 30S binders - Aminoglycosides, Tetracyclines• Mupirocin
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PENGHAMBAT SINTESIS PROTEIN
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Macrolides
• First generation– Erythromycin
• Second generation– Azithromycin, Clarithromycin– Ketolide : Telithromycin
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Aminoglycosides• Neomycin , Gentamicin ,Tobramycin, Amikacin• Binds the 30S subunit.• Only active against anaerobes because an oxygen dependent
system is required to transport the molecules into the cell.• Synergism with cell wall inhibitors is seen because they
increase the permeability of the cell.• Post antibiotic effect
– Persistent suppression of bacterial growth that occurs after the drug has been removed
– Gram negative bacilli and Staphyllococcus aureus
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INTERAKSI OBAT
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EFEK SAMPINGTETRASIKLI N : GIGI COKLATAMINOGLIKOSIDA : OTOTOKSIK
NEFROTOKSIK
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ANTI MALARIA• Profilaksis Proguanil• Prevent Relaps
Primaquine• Blood Schizontizide :
• Rapidly acting Klorokuin, Kuinin & derivatnya, artemisinin, atovaquone
• Slower acting antifolate, antibiotic
• Gametocytocides klorokuin, kuinin
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Obat Skizontisid DarahKlorokuin Kuinin Meflokuin
Cara kerja
-Hambat polimerisasi hem-Alkalinisasi vakuola mak-Penurunan sintesis DNA
Pengaruhi sintesis DNA
Seperti kuinin
Spektrum
-Pengobatan malaria falcifarum eritrositik-Amebiasis ekstraintestinal
Untuk jenis malaria yang resisten dengan obat lain
Menekan bentuk P.falcifarum
FK Oral,vol distribusi yang besarDealkilasi oleh enzim hati, ekresi dalam urine asam
Oral,terdistribusi seluruh tubuhAlkalinasi urine eksresi
Oral,ditimbun dihati dan paruT½ panjang. Mb luas,eksresi feses
ES Do rendah: kecilDo :efek toksik
Kinkonisme(sindrom mual, muntah, tinitus dan vertigo)Tes Coombs+ berhenti
Do mual,muntah disorientasi, halusinasi,depresiKx e-kardiografi jk+ kuinin/ penyekatβ
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Primakuin
• Skizontisid Jaringan Cara Kerja: belum diketahui Spektrum: - efektif fase eksoeritrositer jaringan.
- penyembuhan radikal malaria P.vivax dan P.Ovale yang menetap dihati
FK: - Oral dan tidak ditimbun jaringan
- Cepat dioksidasi dan metabolit lewat urine ES: ~Anemia Hemolitik defisiensi G6PD
~Nyeri lambung jika dikombinasi dengan klorokuin
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ANTI VIRUS
Berdasar tempat hambatannya,dibagi menjadi:
1. obat yang menstop virus biar ndak melekat sama sel hospes
2. obat yang menghambat sintesis asam nukleat
3. inhibitor protease
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ACYCLOVIR• Efektif terhadap VZV dan
HSV• Timidin kinase dari virus
mengubah asiklovir menjadi monofosfat fosforilase dari sel hospesasikloguanin trifosfat hambat polimerase dan sintesis DNA virus
• Toksik selektif• Bisa topikal, oral, dan
parenteral• ES : iritasi lokal, gangguan
GIT