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Antimycobacterial Drugs

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40 Questions

What is isoniazid effective against?

Both rapidly growing bacilli and intracellular organisms

What is the main reason for resistance to isoniazid?

Chromosomal mutations

Why is absorption of isoniazid impaired?

When taken with food, particularly high-fat meals

What is the mechanism of inactivation of isoniazid in the body?

N-acetylation and hydrolysis

What is the difference between fast and slow acetylators of isoniazid?

Fast acetylators have a shorter half-life

What is the primary route of excretion of isoniazid?

Glomerular filtration and secretion

What is the enzyme required for the activation of pyrazinamide?

Pyrazinamidase

What is the reason for usually discontinuing pyrazinamide after 2 months of a 6-month regimen?

Because most of the clinical benefit occurs early in treatment

What is the primary organ responsible for the excretion of ethambutol and its metabolites?

Kidneys

Why is ethambutol used in combination with other antitubercular drugs?

Pending culture and susceptibility data

Why is rifampin not given as a single agent in the treatment of active tuberculosis?

Because resistant strains rapidly emerge during monotherapy

What is the mechanism of action of rifampin?

It interacts with the β subunit of mycobacterial DNA-dependent RNA polymerase

What is the common side effect of pyrazinamide?

Uric acid retention

What is the limitation of ethambutol in the treatment of tuberculous meningitis?

Penetration into the CNS is variable

Which of the following is rifampin effective against?

Both gram-positive and gram-negative organisms

What is the cause of resistance to rifampin?

Mutations in the bacterial DNA-dependent RNA polymerase gene

What is the effect of rifampin on hepatic cytochrome P450 enzymes?

It induces their activity

What is the fate of rifampin after oral administration?

It is distributed to all body fluids and organs and undergoes enterohepatic recycling

Which mechanism of action does para-aminosalicylic acid work through?

Inhibition of folic acid

What is the primary concern when using capreomycin for the treatment of MDR-TB?

Nephrotoxicity and ototoxicity

Which drug is primarily excreted unchanged in the urine?

Cycloserine

What is the primary effect of cycloserine on the bacterial cell wall?

Disruption of D-alanine incorporation

Which of the following drugs is a structural analog of isoniazid?

Ethionamide

Which of the following drugs is not typically used for the treatment of MDR-TB?

Isoniazid

What is the primary mechanism of action of dapsone in inhibiting bacteria?

Inhibiting dihydropteroate synthase in the folate synthesis pathway

Why should rifampin be avoided when taking the agent mentioned?

Because it is a strong CYP3A4 inducer

What is the primary site of concentration of dapsone in the body?

Skin

What is a common adverse reaction of dapsone, especially in patients with glucose-6-phosphate dehydrogenase deficiency?

Hemolysis

What is the primary route of elimination of dapsone and its metabolites?

Urine

What is another disease that dapsone is used to treat, besides leprosy?

Pneumonia caused by Pneumocystis jirovecii

What is the primary organ responsible for the metabolism of ethionamide?

Liver

What is the primary mechanism of action of bedaquiline?

Inhibiting the ATP synthase

What is a common adverse effect of ethionamide?

Nausea and vomiting

Which of the following fluoroquinolones is effective against multidrug-resistant tuberculosis?

Moxifloxacin

What is the primary reason for preferring azithromycin over clarithromycin in certain patients?

Azithromycin is less likely to interact with other drugs

What is the boxed warning associated with bedaquiline?

QT prolongation

Which of the following macrolides is a substrate and inhibitor of cytochrome P450 enzymes?

Clarithromycin

What is the primary route of administration of bedaquiline?

Oral

Which of the following is a common laboratory abnormality associated with bedaquiline therapy?

Elevated liver enzymes

What is the primary indication for bedaquiline?

Treatment of MDR-TB

Learn about the mechanisms of resistance to Isoniazid, a drug used to treat tuberculosis. Understand how chromosomal mutations, including KatG and InhA, lead to resistance and how cross-resistance occurs with ethionamide. Test your knowledge of tuberculosis chemotherapy.

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