antibiotic side effects and ADME Flashcards

renal elimination
Terms Definitions
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)
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