Flashcards in Anti-metabolits and TB drugs Deck (19):
Sulfonamides affect the _______ step of tetrahydrofolic acid synthesis whereas trimethoprim affect the ________ step
What compound do sulfonamide antimicrobial drugs try to mimic to compete for the active site of dihydropteroate synthetase?
Para-Aminobenzoic acid (PABA)
*bacteria have to form folic acid, we get it from diet
What two folate synthesis enzymes are the target of inhibition?
1st step- Dihydropteroate synthetase
2nd step- Dihydrofolate reductase
What are the two most common Sulfonamide antibiotics?
-Sulfamethoxazole (inhibits 1st step, systemic use)
-Silver sulfadiaxine (used as a topical usually in burns)
Which sulfamethoxazole is bacteriostatic, no longer used as a mono therapy and is a competitive inhibitor of dihydropteroate synthetase?
Which combination drug is the first line treatment for Pneumocystis jiroveci (carinii) Pneumonia?
*synergistic 1 part trimethoprim to 5 parts sulfamethoxazole
What are the 3 extra bacterial defenses mycobacterium posses?
1. High lipid content of cell wall
2. Efflux pumps in cell membrane (pump out harmful chemicals)
3. Hide inside patient cells (mycobacterium avium)
Which drug is the first line agent for TB and leprosy treatment and is a prophylactic drug for Meningococcal infection?
*4 R's (RNA pol inhib, Revs CYP450, Red fluids, Rapid resistance on its own)
Used as a TB prophylaxis, which drug must be activated by the TB catalase-oxidase enzyme, decreases mycolic acid synthesis and can be neurotoxic?
*Neuron and hepatocyte injuries, Disulfiram like rxn with alcohol
Which drug requires acidic pH to activate, is a mycolic acid inhibitor should not be used in pregnancy and can cause hepatotoxicity and gout?
Which drug is bacteriostatic, decreases carbohydrate polymerization by inhibiting arbinosol transferase, crosses the BBB and can cause blindness?
Which drug inhibits the 30 s subunit and can cause ototoxicity and deafness?
*dont use in pregnancy
Which drug inhibits mycobacterial ATP synthase and may cause headache or arthralgias?
*used for multi-drug resistant TB
Which drug is a 50S inhibitor and may result in prolonged QT and acute cholestatic hepatitis?
Which drug inhibits bacterial dihydrofolate synthesis and is used for leprosy and prophylaxis against pneumocystis jirovecii?
What are the two major mycobacterium related diseases?
2-Leprosy or Hansen's disease
What is the prophylactic treatment of choice and for how long for latent or asymptomatic TB patients?
Isoniazid for 9 months
For an active TB infection, what is the treatment of choice?
-2 months isoniazid, rifampin, ethambutol and pyrazinamide
-4 months isoniazid and rifampin
*2 with 4, 4 with 2