Drug Mechanisms Flashcards
Beta-lactam antibiotic MOA
inhibition of transpeptidase
Causes acute allergic interstitial nephritis
Methicillin
Bulky R groups
Anti-Staph Penicillin
Nono-allergic skin rash
amoxicillin ampicillin
Not affected by food absorption
Amoxicillin
Ticarcillin SE
Excessive Na+ - problematic for CHF pts
Prolonged bleeding time
Rapidly broken down by dehydropeptidases found in the renal tubule - Cilastatin inhibits this enzyme
Imipenem
Cefazolin SE
EtOH Intolerance, Bleeding Disorder
Prophylaxis for surgery to prevent S. aureus infection
Cefazolin
Chloramphenicol MOA
binds the 50S Subunit, blocks peptidyltransferase binding
Chloramphenicol resistance is d/t
acetyltransferase production
Gray Baby Syndrome
Chloramphenicol
Drug of choice for Mycoplasma pneumonia (or Tetracycline), Legionella pneumonia
Macrolide
Macrolide MOA
Reversibly binds 50S Subunit & prevents translocation & polypeptide chain growth
tissue concentrations exceed plasma by 10-100X - DO NOT USE FOR BACTEREMIA
Azithromycin
MAC in AIDS pts
Clarithromycin
Absorption decreased by Ca and antacids
Tetracycline
Tetracycline SE
Drug-Ca Complex: Tooth discoloration, Bone deformities or growth inhibition;
Fanconi Syndrome: renal damage d/t renal acidosis; Sensitivity to Sunlight
Tetracycline MOA
binding the 30S Subunit & blocking aa-tRNA binding
Aminoglycoside MOA
irreversibly bind 30S Subunit, causing: inhibition of protein synthesis, ribosome disassembly, misreading of mRNA & mutant protein production
Aminoglycoside SE
Ototoxicity, Nephrotoxicity, Neuromuscular block
Sulfonamide MOA
Competitive inhibition of Dihydropteroate Synthase (converts PABA to Dihydropteroic Acid)
Trimethoprim MOA
Inhibits bacterial Dihydrofolate reductase
converts dihydrofolate to tetrahydrofolate
burns/burn management
Opthalmological ointments for conjunctivitis & Chlamydia trachomatis
Sulfonamide
Fluoroquinolone MOA
target DNA gyrase & DNA topoisomerase IV to prevent supercoiling
Sulfonamide SE
Crystaluria (drink fluids), Hemolytic anemia in pts w/ G6PD deficiency, Bone dyscrasias, Anemia in pts w/ AIDS or cancer
Kernicterus
Sulfonamide SE
Cartilage Damage: blackbox warning,
Fluoroquinolone
Inhibits bacterial cell wall synthesis by binding the D-ala-D-ala peptidoglycan pentapeptide, inhibiting formation of peptidoglycan
Vancomycin MOA
Red Man Syndrome
Vancomycin
Clindamycin MOA
Binds 50S Subunit to inhibit bacterial protein synthesis
Nitrofurantoin mOA
Reduced forms damage DNA, more active at acidic pH
Polymyxin B MOA
Interact w/ cell membrane phospholipids & disrupt cell membrane permeability, causking leakage of intracellular components
Quinupristin/Dalfopristin MOA
Binds 50S subunit at a site different than Macrolides
Bacitracin MOA
Inhibits cell wall formation by interfering w/ the lipid that carries peptidoglycan subunits to the site of cell wall formation
Metronidazole MOA
Reduction of drug to compounds & free radicals that bind to intracellular macromolecules, & cause bacterial DNA damage
Linezolid MOA
Binds 50S subunit & prevents formation of the 70S translational initiation complex
Daptomycin moA
depolarizing bacterial cell membranes which leads to loss of membrane potential, K+ efflux, & cell death
Vanco -resistance
Daptomycin, Quinupristin/Dalfopristin
Isoniazid MOA
interferes w/ cell wall mycolic acid biosynthesis, since mycolic acid is unique to Mycobacteria
Isoniazid SE
Peripheral Neuropathy, Hepatitis
Rifampin MOA
inhibition of RNA transcription by binding to beta-subunit of DNA-dependent RNA pol
Rifampin SE
Reddish-orange urine, saliva, sweat, & tears
Pyrazinamide SE
Nongouty Polyarthralgia:
Dapsone MOA
inhibits folic acid synthesis
Dapsone SE
Hemolytic anemia, Methemoglobinemia,
Sulfone Syndrome
Clofazimine MOA
binds to Mycobacterial DNA & interferes w/ growth
Clofazimine SE
Pigmentation of Skin
Amphotericin B MOA
Binds sterols (ergosterol) in fungal cell membrane causing increased pore/channel permeabilit
Inhibition of 14-alpha-demethylase, causing demethylation of lanosterol MOA
Ketoconazole, Miconazole, Fluconazole, Itraconazole
Endocrinologic Abnormalities
Ketoconazole
Cryptococcosis in AIDS pts (indefinitely)
Fluconazole
Histoplasmosis in AIDS pts
Itraconazole
disrupts cell’s mitotic spindle structure, arresting cell division in metaphase, deposited in keratin precursor cells
Griseofulvin MOA
Nystatin MOA
Binds sterols (ergosterol) in fungal cell membrane, increased permeabiliity
Tolnaftate & Terbinafine HCl MOA
interfere w/ sterold biosynthesis by inhibiting Squalene Monooxygenase, resulting in decreased synthesis of ergosterol
Caspofungin MOA
Inhibits synthesis of beta-1,3-D-glucan, an essential polysaccharide component of the cell wall of filmentous fungi
Invasive Aspergillosis, Esophageal Candidiasis in pts refractory to Amphotericin B or Itraconazole
Caspofungin
Immune Globulin Tx
Measles & Hep A Prevention
Hep B & Measles Prophylaxis
RSV in high risk infants
Palivizumab
Palivizumab MOA
mAb to the F protein of RSV
Amantadine MOA
blocks viral penetration of host cells & uncoating, inhibits release of infectious nucleic acid into cell cytoplasm, by buffering the pH of endosomes, Blocks M2 viral protein channels required for nucleocapsid release
Amantadine Tx
Influenza A
Zanamivir & Oseltamivir MOA
inhibition of Influenza virua NA, decreasing release & causing viral aggregat
Zanamivir & Oseltamivir Tx
all strains of Influenza A & B
Ribavirin MOA
affects cellular nucleotide pool & inhibits viral RNA pol & viral mRNA synthesis (higher affinity for viral RNA pol than cellular RNA pol)
Ribavirin Tx
Children: RSV Tx of LRTI
Adults: chronic hepatitis C
Trifluridine MOA
Analog, inhibits viral DNA synthesis by causing chain termination after being incorporated into DNA strand
Trifluridine Tx
HSV-1 & HSV-2 keratoconjunctivitis & keratitis
Trifluridine SE
Visual Haze: burning or stinging
Acyclovir Tx
Genital warts, Systemic HSV, VZV in children
Ganciclovir SE
Teratogenic, carcinogenic
Granulocytopenia, Thrombocytopenia
Severe Myelosuppression
Ganciclovir Tx
CMV retinitis, Life- or Sight-threatening CMV infections
Foscarnet Tx
CMV retinitis in AIDS pts
Interferon alpha-2b MOA
inhibition of viral protein synthesis & viral replication by acting as an inducer of proteins that inhibits the translation fo viral mRNA to protein - 2’5’ oligo adenylate synthetase, protein kinase, phosphodiesterase
Interferon alpha-2b Tx
Cutaneous warts, Chronic Hep B, Chronic Hep C w/ Ribavirin, anti-cancer effects