Pharmacology Flashcards
Selegiline class, mechanism
MAO-B inhibitor, MAO-B metabolizes dopamine, slows the breakdown of dopamine
MAO-A inhibitors mechanism
preferentially slows the breakdown of norepinephrine and serotonin
Levidopa mechanism
dopamine precursor, increases circulating dopamine levels in the striatum
(given in combination with carbidopa, peripheral decarboxylase inhibitor, increases peripheral DA)
Three dopamine receptor agonists
bromocriptine
ropinirole
pramipexole
Benztropine and trihexyphenidyl drug class
antimuscarinic agents
Common sulfa drugs
Sulgonylureas: glyburide
NSAIDs: celecoxib
Diuretics: chlorthalidone, furosemide, bumetanide, (-amide, -ide)
Anticonvulsants: Zonisamide, Topiramate
Others: Bosentan, defetilide, dronedarone
Drug that damages DNA by forming toxic free radical metabolites
Metronidazole
Aminopenicillins and spectrum
Amoxicillin, ampicillin (penicillinase-sensitive)
H.influenzae H.pylori E.coli Listeria Proteus Salmonella Shigella enterococci Triple-therapy for H.pylori Early stage or young Lyme Disease coverage in asplenic or dental procedure
Drugs that Interrupt Cell Wall Synthesis
Glycopeptides (peptidoglycan synthesis) Penicillins + Antipseudomonals Cephalosporins Carbapenems Monobactams
Penicillinase-resistant penicillins + Spectrum
Dicloxacillin
Nafcillin
Oxacillin
S.aureus (naf for staph) except MRSA
Drugs that interrupt folic acid synthesis
Sulfonamides
Trimethoprim
Antipseudomonals
Piperacillin, Ticarcillin
Same mechanism of penicillins with coverage for Pseudomonas and gram negative rods
Add a B-lactamase inhibitor
Drugs that inhibit prokaryotic enzymes topoisomerase II and IV, DNA gyrase
Fluoroquinolones (ciprofloxacin, etc)
B-lactamase inhibitors
Clavulanic Acid
Sulbactam
Taxobactam
Mechanism of penicillin
Bind penicillin-binding proteins (transpeptidases), block transpeptidase cross-linking of peptidoglycan in the cell wall, activate autolytic enzymes
Mechanism of Cephalosporins
B-lactam drugs that inhibit cell wall synthesis and peptidoglycan cross-linking
Coverage of penicillin
Gram positive organisms (S.pneumo, S.pyo, Actino)
Gram negative cocci (N.menin)
Spirochetes (T.pallidum)
1st generation cephalosporins + spectrum
Cefazolin, cephalexin
Gram positive cocci + Proteus, E.coli, Klebsiella
Pre-surgical prophylaxis
2nd generation cephalosporins + spectrum
cefoxitin, cefaclor, cefuroxime
1st gen + Haemophilis inf, Enterobacter, Neisseria, Serratia
3rd generation cephalosporins + spectrum
ceftriaxone (meningitis, gonorrhea, Lyme)
cefotaxime
ceftazidime (Pseudomonas)
serious gram negative infections resistant to other B-lactams
4th generation cephalosporins + spectrum
Cefepime
Pseudomonas
5th generation cephalosporins + spectrum
Ceftaroline
broad gram + and gram - including MRSA, not pseudomonas
Resistance to cephalosporins is based on
Structural change in penicillin-binding proteins (transpeptidases)
Vancomycin mechanism and clinical use
Inhibits cell wall peptidoglycan formation by binding D-ala-D-ala, not susceptible to B-lactamases
Gram positive only
Carbapenems mechanism and clinical use
inhibit cell wall synthesis, administer imipenam with cilastatin to decrease renal tubule inactivation
Use in life-threatening infections or after drug failure due to severe side effects: GI distress, skin rash, CNS toxicity/seizures
Amphotericin B mechanism and use
Bind ergosterol –> pores in membrane
Systemic mycoses or Intrathecally for fungal meningitis
Supplement K+ and Mg2+
Nystatin mechanism and use
Bind ergosterol –> pores in membrane
Topical use only: oral candidiasis, diaper rash, vaginal
Azoles mechanism and use
Inhibit fungal ergosterol synthesis via 14-a-demethylase/P450 enzyme
Local/less serious systemic mycoses:
- chronic suppression of cryptococcal in AIDS
- chronic suppression candidal infections
- topical fungal infections
- SE testosterone inhibition, liver dysfunction
Echinocandins drugs, mechanism, use
-fungin
Inhibit cell wall synthesis of B-glucan
Invasive aspergillosis, candida
- SE GI upset, flushing (histamine)
Flucytosine mechanism, use
Inhibit DNA/RNA synthesis by conversion to 5-fluorouracil by cytosine deaminase
Use for systemic infections in combination with amphotericin B
- SE: bone marrow suppression
Griseofulvin mechanism, use
Interferes with microtubule function, disrupts mitosis, deposits in keratin containing tissues (nails)
Oral treatment of superficial infections, inhibits growth of dermatophytes (tinea, ringworm)
- SE: teratogenic, carcinogenic, confusion, headaches, increased P-450 and warfarin metabolism
Oseltamivir, Zanamivir mechanism, use
Inhibit influenza NEURAMINIDASE –>
Decrease release of progeny
Use in first 48 hours
Treat/prevent Influenza A & B
Acyclovir, Famciclovir, Valacyclovir mechanism, use
Inhibit viral DNA polymerase by chain termination
(Guanosine analogs monophosphorylated by viral thymidine kinase –> mechanism of resistance)
Use for HSV and VZV, weak EBV
Prophylaxis in immunocompromised, no effect on latent
Valacyclovir = prodrug acyclovir (better oral bioavailbility)
- SE crystalline nephropathy, acute renal failure
(prevent with hydration)
Ganciclovir mechanism, use
Inhibit viral DNA polymerase by chain termination
(Guanosine analog 5’ monophosphate formed by CMV viral kinase –> mechanism of resistance)
Use for CMV, especially in immunicompromised
Valgancyclovir = prodrug ganciclovir (better oral bioavailability)
- SE leukopenia, neutropenia, thrombocytopenia, renal toxicity, more toxic to host than acyclovir
Foscarnet mechanism, use
Viral DNA/RNA polymerase inhibitor, HIV reverse transcriptase inhibitor, binds to pyrophosphate-binding site or enzyme
Use in CMV retinitis if ganciclovir fails, in acyclovir-resistant HSV
- SE nephrotoxicity, electrolyte abnormalities can lead to seizures
CYP450 Inhibitors
Increase warfarin effect –> increase bleeding
PICK EGS (protease inhib, isoniazid, cimetidine, erythromycin, grapefruit juice, sulfonamides)
Acetaminophen, Azoles, Amiodarone, Cimetidine, Clarithromycin, Cranberry juice, Fluoroquinolones, Fluoxetine, Ginkgo biloba, Grapefruit, Isoniazid, Omeprazole, Ritonavir, Thyroid Hormone
CYP450 Inducers
Decrease warfarin effect –> Clotting risk
Carbamezapine Cyclophosphamide Ginseng Griseofulvin Modafinil OCPs Phenobarbital + other barbs Phenytoin Rifampin St. John's wort
Cholestyramine interaction with warfarin
Binds warfarin in intestine –> reduces uptake
High risk of drug-induced lupus
Hydralazine Procainamide Isoniazid Minocycline Quinidine
Sulfonylureas, meglitinides mechanism, class, side effects
Mechanism: Inhibit B-cell K-atp channels, increase insulin secretion
“Insulin secretagogues” glyburide, glimipride, glipizide
Repaglinite, Metaglinide
SE: HYPOGLYCEMIA, weight gain
Metformin mechanism, class, side effects
Mechanism: Stimulate AMPK, decrease glucose production, decrease hepatic gluconeogenesis, decrease insulin resistance
“Biguanides”
SE: lactic acidosis
check creatinine before use
Pioglitazone mechanism, class, side effects
Mechanism: activate transcription regulator PPAR-y, decrease insulin resistance
“Thiazolidinediones”
SE: fluid retention, heart failure, weight gain
Exenatide, liragluitide mechanism, class, side effects
Mechanism: increase glucose-dependent insulin secretion, decrease glucagon secretion, delay gastric emptying
“GLP-1 agonists”
SE: Pancreatitis
Sitagliptin, saxagliptin mechanism, class, side effects
Mechanism: Increase endogenous GLP-1 and GIP levels
“DPP4 inhibitors”
SE: nasopharyngitis
acarbose, miglitol mechanism, class, side effects
Mechanism: reduce intestinal disaccharide absorption
“a-glucosidase inhibitors “
SE: diarrhea, flatulence