Protein synthesis inhibitor นายรุจิภาส ชื่นชมกิจ 633070085-3

Monk 1.Bind to 30s ribosomal and alter protein synthesis -> cell death
Macrolides(Erythromycin)

:
Ex. Aminoglycosides
- aerobic gram neg. (E.Coli, Klebsiella app.), Mycobacterium(2nd - Erythromycin, same as penicillin G
Line :streptomycin) Roxithromycin, + M.pneumonia, H.Influenza
-polycations -> pharmacokinetics : oral administration can't Azithromycin, +Clamydia trachomatis
absorb adequately, (usually IV) Clarithromycin+ H.pylori
-Inadequate in CSF,Lung
-bind 50s ribosomal -> inhibit translocation
-High concentration at renal cortex,
(Transpeptidation)
inner ears
-Excrete rapidly by kidneys. -food interfere absorption except
->It has to diffuse through porin clarithromycin)
channel which depend on O2 -metabolized and inhibit CYP3A4 except
and can be inhibited by anaerobic and azithromycin
acidity Adverse: epigastric distress from
-Post antibiotic effect: bactericidal activity persist after
erythromycin, Jaundice
concentration fall below MIC
-Once daily dose (except:pregnancy, neonate, endocarditis)
-MOA: bind 30s subunit, premature termination of translation, Clindamycin
incorporation of incorrect amino acid ->abnormal or ใช้แทนcloxacillin and dicloxacillin
nonfunctional protein -MOA: same as erythomycin
-gram pos. Cocci
-ex. Gentamicin, Amikacin, Streptomycin, Neomycin
-anaerobe
Clinical Use: Acute pyelonephritis, Bacterial endocarditis
Adverse: GI disturbance
(combine with penicillin), TB
Adverse: Nephrotoxicity, Ototoxicity

Mao 2.Affect function of 30s and 50s ribosomal ->

reversible inhibition of protein synthesis
Ex.
Miscellaneous antibiotics
Chloramphenicol
-Metronidazole

:
-bind 50s subunit
-inhibit peptidyl transferase -MOA: cytotoxic(Free radical)
-inhibit mitochondrial protein synthesis in mammalian -> BM -> - metabolized by liver
infection, Anemia, Bleeding -potent against anaerobe ex. Clostridium
-high dose in neonate: Gray baby difficile colitis (previous antibiotic use causing
-Gram pos.+neg. , rickettsiae
overgrowth of C.diffisile, it can secrete
-Clinical Use : Meningitis, Topical conjunctivitis
exotoxins making necrotizing inflammation at
Tetracycline/Doxycycline colon mucosa (Diarrhea, abdominal pain).
-bind 30s subunit, blocking access of amino acyl-tRNA to Stool exam; mucous, WBC, RBC. Treatment:
mRNA-ribosome cpx Stop using ATB or using metronidazole and
-Gram neg. rod : Vibrio Cholrae. vancomycin
-Spirochetes, Rickettsial -antiprotozoal agent: E.hist, Giardiasis
-bind to divalent/trivalent ex. Milk, antacid, to form no
Lambia, T. vaginalis
absorbable cheatles
-Adverse: N/V, epigastric distress,
-bind bone, teeth
-metabolized by liver abdominal cramp, dizziness, numbness,
-Adverse: GI discomfort, discoloration and hypoplasia of teeth, disulfiram like reaction(ถ้ากินเหล้าพร้อมยา)
hepatotoxicity, photo toxicity, dizziness