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RS Pharmacology
Respiratory System Pharmacology- Anti- TB
| Question | Answer |
|---|---|
| First line anti-tuberculous agents: | Isoniazid (INH) Rifampin “Rifadin” or “Rimactane” Ethambutal Streptomycin Pyrazinamide Island Rivers Establish Shoddy Palms |
| Secondary or Second Line Drugs used as anti-tuberculous agents: | Ethionamide Capreomycin Cycloserine Para-Amino-Salicylic Acid (PAS) Amikacin Flouroquinolones Linezolid Rifabutin Rifapentine Earthworms Create Creepy Pumpkins And Ferrets List Robotic Robots |
| Most active anti-TB drug: | Isoniazid |
| General characteristics of Isonazid: | Small molecule, water soluble, Structurally related to Pyridoxine Prodrug, activated by KatG, the mycobacterial catalase peroxidase |
| MOA of Isonazid: | Blocks mycolic acid synthesis-consequently mycobacterial cell wall synthesis- bactericidal effect in growing TB cells Widely distributed, penetrates into macrophages Metabolized by acetylation |
| Resistance of Tb to Isonazid: | 1 in 10^6 when used alone 1 in 10^12 when used in combination |
| Side effects of Isonazid use: | Hepatitis-1% Anorexia N,V Jaundice Neuropathy:10-20% Neurotoxicity: Memory loss, Psychosis,Seizures Tinnitus GIT effects Interactions |
| Neuropathy is more likely to occur in: | Slow acetylators Malnutrition AIDS Alcoholics DM Uremia Due to pyridoxine deficiency |
| Rifampin was isolated from: | Stretomyces miditerranei |
| Rifampin is effective in cases of: | Gram+ve and –ve bacteria Mycobacteria Enterococci Chlamydia |
| MOA of rifampin: | Binds to the beta subunit of bacterial DNA-dependant RNA polymerase and therefore inhibits RNA synthesis Bactericidal Widely distributed Hepatic metabolism - enterohepatic recirculation |
| What are the clinical uses of Rifampin? | TB Leprosy Meningococcal Carrier State Prophylaxis in H.influenzae. Staph osteomyelitis and valve endocarditis. |
| In Jordan it is available only in | MOH Ministry of Health |
| Rifampin toxicity can cause: | Orange color to secretions( tears, urine, sweat). Nephritis Rashes Hepatitis Flu-like syndrome Liver Enzyme Inducer- lower serum levels of many drugs |
| Uses of streptomycin: | Anti-tuberculus agent. Plague Tuleremia Brucellosis Endocarditis |
| Streptomycin toxicity causes: | Allergy: Fever, Rashes Pain, after i.m injection Vestibular toxicity---- Irreversible Nephrotoxicity |
| What are the Indications for Secondary or Second- Line Drugs? | 1) Resistance to first –line drugs 2) Failure of clinical response to conventional therapy 3) Occurrence of serious treatment-limiting adverse drug reactions 4) When expert guidance is available to deal with the toxic effects |
| MOA of Ethionamide: | Related to Isoniazid Blocks mycolic acid synthesis |
| How is Ethionamide administered? | Orally |
| Disadvantages of taking Ethionamide: | Poorly tolerated: Severe GIT irritation Neurotoxic Hepatotoxic |
| MOA of Capreomycin: | Peptide protein synthesis inhibitor |
| Administration of Capreomycin via: | Injection |
| Disadvantages of taking Capreomycin: | Nephrotoxic, ototoxic Local pain and sterile abscesses may occur |
| MOA of Cycloserine: | Inhibits cell wall synthesis |
| Disadvantages of taking Cycloserine: | Peripheral neuropathy CNS toxicity including depression and psychotic reactions |
| MOA of Para-Amino-Salicylic Acid (PAS): | Folate synthesis antagonist |
| Dosage of PAS: | 8-12 gm/day |
| Advantages of taking PAS: | Well absorbed Widely distributed, except CNS Excreted in urine |
| Disadvantages of taking PAS: | GI toxicity Hypersensitivity reactions Crystalluria |
| Uses of Amikacin: | Multidrug-resistant strains Atypical mycobacteria |
| Use of Florquinone: | Combination, because resistance develops rapidly when used alone |
| When is Linezolid used? | For multi-drug resistant strains \LAST resort |
| Side effects of Linezolid use: | Bone marrow suppression Irreversible peripheral and optic neuropathy |
| MOA of Rifabutin and Rifapentine | Related to Rifampin. Inhibit bacterial RNA polymerase. Both, like Rifampin, are inducers for CYP P450 enzymes. But Rifabutin is a less potent inducer |
| Rifabutin is indicated in place of Rifampin in | the treatment of TB in HIV-infected patients receiving protease inhibitor or nonnucleoside reverse transcriptase inhibitor |
| Drugs used in the cases of Atypical Mycobacteria | M.tuberculosis complex: Erythromycin Sulphonamides Tetracycline M.avium complex: Important and common cause of disseminated TB in late stages of AIDS Azithromycin or Clarithromycin Ethambutal & Ciprofloxacin |
| Stats for TB: | Annually, 9 million cases recorded 5% of these are drug-resistant tuberculosis Forty-nine percent of those with XDR-TB died compared to 19 percent of patients with ordinary MDR-TB |
Created by:
Ulaisl
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