Comprehensive Exam - Pharmacology Flashcards
Cephalosporins
mechanism same as penicillins, more resistant to B-lactamase
Adverse effects: cross sensitivity with penicillin
Renal excretion generally
penicillins
Bind to PBPs and inhibit transpeptidase reaction and cross linking of peptidoglycans.
CSF: enter inflamed meninges.
Excretion: renal (exceptions: ampicillin, naficillin = biliary)
Adverse effects: hypersensitivity reaction (mild-severe), diarrhea, superinfections
Aminoglycosides
Bind to 30S subunit & interfere with initiation of protein synthesis. Cause incorporation of wrong amino acids.
Renally excreted
Adverse effects: Renal toxicity (reversible), Cochlear toxicity (irreversible), Vestibular toxicity (reversible)
examples: gentamicin, neomycin
Tetracyclines
block tRNA from binding to 30S subunit, preventing addition of new amino acid.
Renal excretion
Adverse effects: bind to calcifying teeth and bone, hepatotoxicity for pregnant women, nephotoxicity, phototoxicity
Macrolides
Examples: erythromycin
Bind 50S subunit, block peptidyl transferase.
Adverse effects: ototoxicity (high doses), cholestatic jaundice
Clindamycin
Binds 50S subunit.
Adverse effects: superinfection by C. difficile
Sulfonamides
Examples: sulfamethoxazole
inhibit dihydropteroate synthase, decrease folic acid
Renal excretion, cause crystaluria, displace other drugs from albumin
Adverse effect: skin rashes/ Stevens-Johnson syndrome, kernicterus in neonates
Trimethoprim
Inhibits bacterial dihydrofolate reductase
Adverse effects: cause folate deficiency in pregnant women
Floroquinolones
Examples: Ciprofloxacin
Inhibits DNA gyrase
Chelates metals, post antibiotic effect
Toxicity: CNS problems if taken with coffee, phototoxicity, arthropathy in children
Isoniazid
Inhibits synthesis of mycolic acid.
High concentration in CSF
Toxicity: hepatitis (risk is high > 50 years), peripheral neuropathy (prevented by B6)
Used for TB prophylaxis
Rifampin
Binds to DNA dependent RNA polymerase and inhibits transcription.
Toxicity: hepatitis, hypersensitivity reaction, discoloration of body fluids
Tuberculosis
Ethambutol
Blocks arabinosyl transferase (cell wall synthesis)
Enters CSF
Toxicity: optic neuritis, acute gout
Pyrazinamide
Pyrasinoic acid inhibits growth
Enters CSF
Toxicity: Acute gout
Chloramphenicol
toxicity: gray baby syndrome
Vancomycin
Red man syndrome (infusion related toxicity due to histamine release)
Otitis media
S. pnumonia, H. influenzae
Drug of choice: amoxicillin
Resistance by beta-lactamase: amoxicillin + clavulanate
If diarrhea, switch to Cefprozil (2nd gen cephalosporin)
Surgical prophylaxis
IV administation 2 hrs before surgery.
S. aureus, S. epidermis
Cephazolin (1st generation cephalosporin). Severe penicillin allergy or MRSA: Vancomycin
Colorectal & appendectomy: Add oral antibiotics as well due to increased risk of infection
Community Acquired Pneumonia
S. pneumoniae
Erythromycin
Requiring hospitalization: Erythromycin + Cefotaxime (3rd generation cephalosporin)
For neuropenic patients: levofloxacin
Gonorrhea
Ceftriaxone (3rd gen cephalosporin)
Severe penicillin allergy: Ciprofloxacin
Traveller’s diarrhea
Ciprofloxacin