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level: Level 1 of Antitubercular agents

Questions and Answers List

level questions: Level 1 of Antitubercular agents

QuestionAnswer
1 TB has been plaguing humans for __ years 2 Discovered mycobacterium tuberculosis 3 Discovered Streptomycin1) 4000 2 Robert Koch, 1905 (Nobel Laureate) 3 Selman Waksman, 1952 (Nobel Laureate)
1 In the year 1938 discovered: 2 sulfone derivative (4,4-diaminodiphenylsulfone) treatement of leprosy (Mycobacteriumleprae), antimalarial> too toxic in high dosages1 Sulfanilamide-bacteriostatic properties 2 Dapsone
1 aminoglycoside antibiotic, Waksman et al. in 1944 > modern era of anti-TB tx 2 (PAS) 3 Introduced in 1952 4 (synthetic) 5 ( semisynthetic)1 Streptomycin 2 P-aminosalicylic acid 3 Isoniazid 4 Ethambutol 5 Rifampin
1 Can be used only for infected patients who do not have TB (latent TB infection) 2 standard medical practice 3 Choice of antiTB drugs depends on:1 Monotherapy 2 Combination therapy 3) a. Location of dx (pulmonary, urogenital, GI, neural) b. Results of susceptibility tests c. Pattern of resistance in the locality d. Physical condition and age of the patient e. Toxicities of ind. agent
Nonpharmacologic Therapy Aim:1 Prevent Spread of TB 2 Return the patient to a state of normal weight and wellbeing 3 Surgery may be needed to remove destroyed lung tissue, tuberculomas and certain extrapulmonary lesions
1 These drugs have high antitubercular efficacy; are used routinely 2 These drugs have either low antitubercular efficacy or higher toxicity or both; are used as reserved drugs1 First Line Drugs 2 Second Line Drugs
1 First Line Drugs (AntiTB)1 Isoniazid 2 Rifampicin 3 Pyrazinamide 4 Ethambutol 5 Streptomycin
Second Line Drugs (AntiTB)1 Para-aminosalicylic acid (PAS) 2 Kanamycin 3 Amikacin 4 Ethionamide 5 Prothionamide 6 Fluoroquinolones (Oflo, levo, moxi, Ciprofloxacin)
It is a prodrug and is converted into active form inside mycobacterium cellIsoniazid ( Isonicotinic acid hydrazide, isonicotinyl hydrazide, INH)
Isoniazid (Isonicotinic acid hydrazide, isonicotinyl hydrazide, INH) SIDE EFFECTS:1 Inducer of Lupus, Inhibitor of CYTP450 2 Neuropathy (Peripheral) 3 Hepatotoxicity, Hemolysis in G6PD Deficiency
1 Isoniazid is an analog of __ 2 Adverse Effects of Isoniazid 3 Adverse effects happen because Isoniazid competes with __ for the enzyme __ 4 Prevents Neurotoxicity even in higher doses of Isoniazid, but routine use is not mandatory. 5 Is treated with Vitamin B6 100mg / day.1 Pyridoxine (Vitamin B6) - a potent anti tubercular drug 2 a) peripheral neuritis b) Neurological manifestations: Paresthesia, Numbness, Mental disturbances, Optic neuritis, Convulsions c) Hepatitis (potentially fatal) - Due to Pyridoxine (Vit B6 Deficiency) 3 Pyridoxal phosphate, Apoptryptophanase 4 Vitamin B6 10 mg / day 5 Isoniazid Neurotoxicity
1 Isoniazid can potentiate the adverse effects of __ 2 Slow/ Fast Acetylators are particularly At risk from Isoniazid1 Difenin (Nystagmus, Ataxia) - Isoniazid inhibits metabolism of Difenin 2) Slow Acetylators
used in combination with other agents because resistance develops rapidly must be enzymatically hydrolyzed to Pyrazinoic acid (active form) 1st line drug for short term treatmentPyrazinamide (Pyrazinecarboxamide, PZA)
Pyrazinamide Side Effects1 Hepatotoxicity 2 Hyperuricemia 3 Gout like Arthralgia 4 Others: Rash, Vomiting, Anemia, Lupus, Seizures, Photodermatitis
active only in dividing mycobacteria S/E: Optic neuritis ↓ visual acuity loss of ability to discriminate red and green colorsEthambutol, (+)-2,2-ethylenediimino)-d-1-butanol dihydrochloride, EMB
structural analog of isoniazid 2-substitution enhances activity in the thioisonicotamide series used in the tx of Isoniazid-resistant TB S/E: Gastric irritation, hepatoxicity, peripheral neuropathies, optic neuritisEthionamide , 2-Ethylthioisonicotinamide
acts as a competitive inhibitor for p-aminobenzoic acid in folate biosynthesis S/E: Severe gastric irritationPara-aminosalicylic acid (4-aminosalicylic acid)
basic red dye used in the treatment of leprosy (Hansen's dx), including dapsone-resistant forms S/E: GI intolerance, hyperpigmentation, ichtyosis, dryness, rash, pruritusClofazimine (Lamprene)