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ADME/SE B-lactams

antibiotic side effects and ADME

QuestionAnswer
Aminoglycoside ADME Poor absorption, Poor CNS, and lung penetration, renal excretion
Aminoglycosides SE Nephrotoxicity accumulates in proximal tubules (dose and duration,and renal) Ototoxcity (duration, agent)
Aminoglycoside Streptomycin isolated from Streptomyces
Penicillin isolated by Flemming from Staphyloccus
Penicillin Structure 6-aminopenicillanic Acid ( Penicilloic Acid- hapten)
Natural Penicillins ADME PEN G acid labile(increased con in elderly), good distribution, renal excretion
Penicillinase resistant ADME Nafcillin (IV), Good distribution, Naficillin hepatic elimination
Aminopenicillins ADME Good absorption, good distribution, renal elimination
Carboxypenicillins ADME Poor absorption (IV), renal & hepatic combo elimination***
Penicillin SE GI irritation, diarrhea (ampicillin), rash (ampicilin & amoxicillin), hematologic, CNS distrubances
Type I hypersensitivity Immediate mediated by IgE (2-20 min)
Type II hypersensitivity Mediated by IgG &IgM, cytotoxic AB directed against penicillin haptens on RBS surface (methacillin)
Type III hypersensitivity Mediated by IgG occur 1-3 weeks after therapy(Ab-antigen complex deposit) and see as serum sickness, fever, aches, pains
Tupe IV hypersensitivity Delayed reaction involve lymphocytes and machrophages, skin peeling reactions
Cephalosporine parent structure 7-aminocephalosporanic acid-B-lactam and a dihydrothiazine
Cephalosporin 1st ADME Acid stable highly absorbed, good distribution, renal elimination
Cephalosporin 2nd ADME Acid stable, good absorption, good distribution, renal elimination
Cephalosporin 3rd ADME Good absorption, Good CNS penetrationm renal elimination
Cephalosporins 4th ADME Good absorption, Good distribution, renal elimination
Carbapenems ADME Poor oral ABS (IV), well distribution,renal elimination
Carbapenems (Imipenem) SE Neurotoxic-due to GABA receptor causing seizures(risks-renal impairment, elderly, CNS condition)
Azetronam ADME Poor oral absorption, well distributed but poor CNS penetration, renal elimination
Azetronam SE Well tolerated
FLuoroquinolone history Naldixic acid ID in 1962 as a bi-product of Chloroquin synthesis (poor pk)
Cipro SAR Addition of a fluorine at #7 increased binging affinity at target site with 7-piperazinyl substituent-excellent tissue penetration
Fluoroquinolones ADME Excellent absorption, excellent distribution (CNS penetration not great), renal filtration and tubular secretion
Fluoroquinolone SE GI, CNS, rash, Increase transaminases, Glucose abnormalities, QTc prolongation, tendonitis, photosensitivity
Vancomycin history Found from Norcardia orientalis in indonesia and india-huge tricyclic glycopeptide
Vancomycin ADME Poor oral absorption, Wide distribution (CSF limited), 70 renal excretion via glomerular filtration other ?
Vancomycin SE Phlebitis and pain (slow rate and dilute), Red man syndrome (slow infusion, benadril), nephrotoxicity, Ototoxcity
Synercid ADME Poor oral absorption, Wide distribution, active metabolites (3A4 DI) ,
Synercid SE Phlebis (severe) requires placement of central line, arthralgia, myalgia, increased hepatic enzymes, N/V, rash
Linezolid ADME Good oral absorption, well distributed, metabolized via non-enzyme oxidation to aminoethoxyacetic acid and hydroxyethyl glycine, urine elimination
Linezolid SE GI, HA, elevation of hepatic transaminase, reversible bone marrow suppression
Daptomycin ADME Poor oral absorption, low lung penetration due ti inactivation via surfactants, 80 renal elimination
Daptomycin SE GI, HA, elevation in creatine phosphokinase, increase in hepatic transaminases (caution statins)
Created by: liza001
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