Antituberculous 1
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This document discusses anti-tuberculosis drugs, including first-line drugs like isoniazid, rifampicin, ethambutol, and pyrazinamide as well as second-line drugs. It describes the mechanisms of action, pharmacokinetics, and adverse effects of isoniazid, rifampicin, ethambutol, and pyrazinamide. It also discusses multi-drug therapy, drug resistance including MDR-TB and XDR-TB, and measures to improve treatment compliance like directly observed therapy.
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This document discusses various antimycobacterial drugs used to treat tuberculosis. It begins by describing tuberculosis and its clinical features. It then discusses first-line drugs including isoniazid, rifampin, ethambutol, and pyrazinamide. For each drug, it covers mechanisms of action, pharmacokinetics, adverse effects, drug interactions, and dosing. It also briefly discusses second-line drugs used when first-line treatment fails or bacteria develop resistance. Throughout, it provides detailed information on the individual drugs used in standard combination therapy to treat tuberculosis.
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Rifampicin is a rifamycin antibiotic derived from soil mold. It was discovered in 1959 and is highly effective against Mycobacterium leprae. Rifampicin is well absorbed orally and distributed throughout the body, including crossing the blood-brain barrier. It is metabolized in the liver and excreted in both urine and bile. Its mechanism of action involves preventing mRNA and protein synthesis. A single monthly 600mg dose of Rifampicin is highly effective against leprosy due to its strong bactericidal properties. Common side effects include discoloration of bodily fluids and gastrointestinal issues. It is generally safe in pregnancy. Resistance can develop via mutations in the rpoB gene.
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This document provides information about tuberculosis (TB) and anti-tubercular drugs. It discusses how TB is caused by Mycobacterium tuberculosis and spreads through droplets from coughing or sneezing. Common symptoms include low-grade fever, night sweats, and cough. First-line drugs to treat TB include isoniazid, rifampin, pyrazinamide, ethambutol, and streptomycin. Second-line drugs are used to treat multi-drug resistant TB. Treatment involves a two month intensive initial phase followed by a four to six month continuation phase to prevent relapse. Directly observed treatment is recommended to ensure patient compliance and treatment success.
Antitubercular agents
Antitubercular antibiotics
Tuberculosis is caused by either mycobacterium tuberculosis (in Humans) or by mycobacterium bovis (in animals)
Tuberculosis is a disease of respiratory transmission.
A person gets infected when it comes in contact with the environmental contaminated with viable tubercle Bacilli.
This bacilli are expelled by coughing , sneezing , shouting and singing of a patient with active tuberculosis.
Tubercles are formed in the infected organs during the course of the disease , hence the disease is known as tuberculosis.
Main symptoms are :- cough, tachycardia ,respiratory failure, cynosis (Bluish or greyish colour of the skin, nails, lips or around the eyes.)
The agents or antibiotics which are used to treat tuberculosis these are known as the antitubercular antibiotics.
Drugs includes :-
Rifampicin , streptomycin , cycloserine , capreomycin sulfate and Refabutin
Rifampicine
Orally active bactericidal semi synthetic derivative of Rifamycin B.
This antibiotic is produced by the streptomyces Mediterranei.
It is the first line agent.
Mechanism of Action :-
DNA-dependent-RNA polymerase (DDRP) enzyme is required for the synthesis of RNA.
- Rifampicin binds to Beta subunit of enzyme DDRP and make it inactive.
- so it causes inhibition of bacterial RNA synthesis.
hence there is tuberculocidal effect
SAR
Free OH group is required at C-1, C-8, C-21, and C- 23 .
These group must be in one plane.
Opening of ring will destroy the activity of antibiotic.
Rifampicin is active against both Gram Negative and Gram Positive Bacteria.
resistance is developed when mutation occurs in beta subunit of DDRP.
bacterial resistance develop rapidly if rifampicin taken alone, though the combination with Isoniazid or ethambutol are preferable used.
Adverse effects :
Nausea, Vomiting, headache, erythema, nervousness, emotional disturbances , pulmonary edema, increased cardiac output and cardiac arrythmias
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Tuberculosis is caused by Mycobacterium tuberculosis and was once incurable but now treatable with anti-tubercular drugs. These drugs are classified as primary/standard or secondary/reserve drugs and include isoniazid, rifampicin, streptomycin, pyrazinamide, ethambutol, para-aminosalicylic acid, thiacetazone, capreomycin, kanamycin, ethionamide, and cycloserine. The primary drugs are bactericidal while the secondary drugs treat multi-drug resistant strains. A standard short-term regimen involves taking isoniazid, rifampicin, ethambutol, and pyrazinamide daily for 2 months
Rifampicin in leprosy
Rifampicin is a rifamycin antibiotic derived from soil mold. It was discovered in 1959 and is highly effective against Mycobacterium leprae. Rifampicin is well absorbed orally and distributed throughout the body, including crossing the blood-brain barrier. It is metabolized in the liver and excreted in both urine and bile. Its mechanism of action involves preventing mRNA and protein synthesis. A single monthly 600mg dose of Rifampicin is highly effective against leprosy due to its strong bactericidal properties. Common side effects include discoloration of bodily fluids and gastrointestinal issues. It is generally safe in pregnancy. Resistance can develop via mutations in the rpoB gene.
Anti tubercular drugs
Tuberculosis is caused by Mycobacterium tuberculosis, an acid-fast bacillus. Treatment involves multidrug therapy with first-line drugs like isoniazid, rifampin, pyrazinamide, and ethambutol over 6-24 months to prevent drug resistance. Second-line drugs are used in special cases but have higher toxicity. Standard WHO treatment schedules involve an intensive initial phase with multiple drugs followed by a continuation phase with fewer drugs to fully treat both intracellular and extracellular bacteria. Adverse effects from these anti-tubercular drugs require monitoring.
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This document provides information about tuberculosis (TB) and anti-tubercular drugs. It discusses how TB is caused by Mycobacterium tuberculosis and spreads through droplets from coughing or sneezing. Common symptoms include low-grade fever, night sweats, and cough. First-line drugs to treat TB include isoniazid, rifampin, pyrazinamide, ethambutol, and streptomycin. Second-line drugs are used to treat multi-drug resistant TB. Treatment involves a two month intensive initial phase followed by a four to six month continuation phase to prevent relapse. Directly observed treatment is recommended to ensure patient compliance and treatment success.
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Antitubercular antibiotics
Tuberculosis is caused by either mycobacterium tuberculosis (in Humans) or by mycobacterium bovis (in animals)
Tuberculosis is a disease of respiratory transmission.
A person gets infected when it comes in contact with the environmental contaminated with viable tubercle Bacilli.
This bacilli are expelled by coughing , sneezing , shouting and singing of a patient with active tuberculosis.
Tubercles are formed in the infected organs during the course of the disease , hence the disease is known as tuberculosis.
Main symptoms are :- cough, tachycardia ,respiratory failure, cynosis (Bluish or greyish colour of the skin, nails, lips or around the eyes.)
The agents or antibiotics which are used to treat tuberculosis these are known as the antitubercular antibiotics.
Drugs includes :-
Rifampicin , streptomycin , cycloserine , capreomycin sulfate and Refabutin
Rifampicine
Orally active bactericidal semi synthetic derivative of Rifamycin B.
This antibiotic is produced by the streptomyces Mediterranei.
It is the first line agent.
Mechanism of Action :-
DNA-dependent-RNA polymerase (DDRP) enzyme is required for the synthesis of RNA.
- Rifampicin binds to Beta subunit of enzyme DDRP and make it inactive.
- so it causes inhibition of bacterial RNA synthesis.
hence there is tuberculocidal effect
SAR
Free OH group is required at C-1, C-8, C-21, and C- 23 .
These group must be in one plane.
Opening of ring will destroy the activity of antibiotic.
Rifampicin is active against both Gram Negative and Gram Positive Bacteria.
resistance is developed when mutation occurs in beta subunit of DDRP.
bacterial resistance develop rapidly if rifampicin taken alone, though the combination with Isoniazid or ethambutol are preferable used.
Adverse effects :
Nausea, Vomiting, headache, erythema, nervousness, emotional disturbances , pulmonary edema, increased cardiac output and cardiac arrythmias
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Tuberculosis is caused by Mycobacterium tuberculosis. There are several drugs used to treat tuberculosis, classified as first-line and second-line drugs. First-line drugs include isoniazid, rifampin, pyrazinamide, and ethambutol, which form the core of the standard treatment regimen. Second-line drugs are used when there is resistance or intolerance to first-line drugs, and include fluoroquinolones, aminoglycosides, ethionamide, and cycloserine. All drugs have potential adverse effects and many drug-drug interactions that require monitoring during treatment.
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- The patient is experiencing drowsiness and dizziness while taking standard four-drug antimycobacterial therapy including isoniazid, rifampin, pyrazinamide, and ethambutol.
- Rifampin is known to cause adverse effects like headache, dizziness, and gastrointestinal upset.
- The symptoms reported by the patient are consistent with an adverse reaction to rifampin.
Drugtherapy of tuberculosis DR. KARTIK
1. Tuberculosis is a chronic infectious disease caused by the bacterium Mycobacterium tuberculosis that primarily affects the lungs.
2. It is difficult to treat due to the slow growth of the bacteria and its ability to become dormant. The first line drugs used for treatment are isoniazid, rifampin, pyrazinamide, and ethambutol.
3. These drugs have high efficacy against the bacteria but resistance can develop, requiring second line treatments with more side effects to be used. Proper treatment duration and compliance with the drug regimen is important to cure tuberculosis.
Antitubercular drugs
The document discusses various aspects of anti-tubercular drugs including their classification, mechanisms of action, indications, adverse effects, contraindications and dosages. It describes key first-line drugs like Isoniazid, Rifampicin, Pyrazinamide, Ethambutol and their properties. Second-line drugs discussed include Para-Amino Salicylic Acid and Cycloserine. The goals of tuberculosis treatment are also mentioned which aim to kill dividing and persisting bacteria and prevent resistance.
TUBERCULOSIS AND ANTI-TUBERCULAR AGENTS
This presentation include every data related to TB and anti-TB drugs with neat and understandable picturization and tables..... pharma students are beneficial mostly
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This document summarizes anti-tubercular drugs used to treat tuberculosis and other mycobacterial diseases. It discusses first-line drugs like isoniazid, rifampicin, pyrazinamide, ethambutol, and streptomycin which are effective, less toxic options routinely used to treat tuberculosis. Second-line drugs discussed include fluoroquinolones, macrolides, rifapentine, and rifabutin which are used for multidrug-resistant tuberculosis or atypical mycobacterial infections. World Health Organization recommended treatment regimens including the directly observed treatment short course protocol are mentioned. Mechanisms of action, pharmacokinetics, uses, and side effects of various anti
Antitubercular drugs
This document provides information on antitubercular drugs used to treat tuberculosis. It discusses first-line drugs like isoniazid, rifampin, pyrazinamide, ethambutol and streptomycin that are routinely used. It also discusses second-line drugs used when first-line drugs are ineffective or cannot be tolerated. The document describes the mechanisms of action, pharmacokinetics, resistance mechanisms and adverse effects of various antitubercular drugs. It also discusses treatment considerations for special populations like pregnant women, HIV patients and for chemoprophylaxis.
antituberculardrugs-150922084323-lva1-app6892.pdf
This document provides information on antitubercular drugs used to treat tuberculosis. It discusses first-line drugs like isoniazid, rifampin, pyrazinamide, ethambutol and streptomycin that are routinely used. It also discusses second-line drugs used when first-line drugs are ineffective or cannot be tolerated. The document describes the mechanisms of action, pharmacokinetics, resistance mechanisms and adverse effects of various antitubercular drugs. It also discusses treatment considerations for special populations like pregnant women, HIV patients and for chemoprophylaxis.
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Praveen ATT.pptx
This document discusses antitubercular agents used to treat tuberculosis. It begins by describing the peculiar features of M. tuberculosis bacteria and the goals of anti-tuberculosis chemotherapy. The first-line drugs discussed are isoniazid, rifampin, pyrazinamide, ethambutol, and streptomycin. Their mechanisms of action, pharmacokinetics, adverse drug reactions, and dosing are summarized. The document also discusses second-line drugs and newer agents used to treat drug-resistant tuberculosis. It emphasizes the importance of multi-drug therapy to prevent the emergence of drug resistance.
ATT
This document provides information on tuberculosis (TB) and its management. It discusses how India has a high burden of TB cases, accounting for 27% of global cases. It also notes that multidrug-resistant TB (MDR-TB) has been reported in over 120 countries. Diagnosis involves bacteriological tests and radiography. Treatment involves a combination of first-line drugs like isoniazid and rifampin, as well as preventive measures and vaccination with BCG. Drug resistance is a major challenge, with estimates of MDR-TB and extensively drug-resistant TB cases on the rise in India.
Anti Tubercular and anti leprotic agents.pdf
This document provides information on antitubercular agents used to treat tuberculosis. It begins by describing tuberculosis as a chronic infection caused by Mycobacterium tuberculosis that primarily affects the lungs. It is a major global health problem, with over 2 million new cases annually in India alone. The document then discusses the characteristics of M. tuberculosis and the sites it commonly infects in the body. It provides details on first-line and second-line antitubercular drugs, including isoniazid, rifampin, pyrazinamide, ethambutol, and streptomycin. It focuses on the mechanisms of action, pharmacokinetics, adverse effects, drug interactions and other important aspects of isoniazid and
Antifungal drugs-Antibiotics
This document discusses various antifungal drugs including polyenes like amphotericin B and nystatin, echinocandins like caspofungin, and the heterocyclic benzofuran griseofulvin. It describes their mechanisms of action, spectra of activity, pharmacokinetics, therapeutic uses, and adverse effects. Amphotericin B is a broad-spectrum antifungal that is fungicidal but highly nephrotoxic. Caspofungin inhibits glucan synthase in fungal cell walls. Griseofulvin binds microtubules to treat dermatophytosis.
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Antituberculous 1
- 1. ANTI TUBERCULOUS DRUGS M.PRADEEPA B.PHARM FINAL YEAR
- 2. Mycobacteria • Slow-growing bacillus • Dormant forms in macrophages
- 3. • Kill 2 million people each year • Increase incidence due to HIV associated Mycobateria • Prevalence of TB in Sri Lanka is 79 per 100 000 population
- 4. • 40 years ago drugs were developed • Now multi- drug resistance strains are emerging
- 5. Anti-tuberculous drugs First-line – Isoniazid – Rifampicin – Ethambutol – Pyrazinamide Second-line – Clarithromycin – Ciprofloxacin – Capreomycin – Cycloserine – Kanamycin – Amikasin – streptomycin
- 6. Isoniazid (INAH) • Acts only on mycobacteria • Interferes with mycolic acid synthesis (unique to mycobacterial cell wall)
- 7. Isoniazid cont: • Passes freely to mammalian cell wall • Effective for intracellular organism • Bacteriostatic – to resting organism • Bactericidal – to multiplying organism
- 8. Isoniazid cont: Pharmacokinetics • Well absorbed from GIT • Fatty food & aluminum-containing antacids may reduce absorption • CSF penetration: 20% of plasma concentration with non-inflamed meninges • Penetrate well into caseous material • Excretion - urine
- 10. Isoniazid cont: Metabolism • By acetylation – genetically determined • Slow acetylation – better response t ½ - 3h • Fast acetylation – t ½ - 1h
- 11. Isoniazid cont: Adverse effect • Hepatotoxicity – Elderly, slow acetylators more prone • Polyneuropathy – Prevented by concurrent pyridoxine • Rashes, acne • Heamatological – haemolytic anaemia in G6PD deficiency
- 12. Rifampicin • Inhibits bacterial DNA-dependent RNA polymerase • bactericidal • Gram positive and negative • kill intracellular organism
- 13. Rifampicin cont: Pharmacokinetics • Well absorbed from GIT • CSF penetration: 10-40% of plasma concentration with non-inflamed meninges • Elimination hepatic, renal
- 14. Rifampicin cont: Adverse effects – Rashes, hepatotoxicity, thrombocytopenia – Mild elevation of liver enzymes - common
- 15. Rifampicin cont: • Orange discoloration of urine, sweat, tears • Potent CYP-P450 inducer- reduce the serum level of drugs • warfarin, oestrogen
- 16. Ethambutol • Inhibits arabinosyl transferases involved in cell wall biosynthesis • Bacteriostatic to M.tuberculosis • Resistance develops rapidly if used alone
- 17. Ethambutol cont: Pharmacokinetics • Well absorbed from GIT • bioavailability 80% • CSF penetration poor • Elimination renal
- 18. Ethambutol cont: Adverse effects • Optic retro-bulbar neuritis – Red-green colour blindness → reduced visual acuity – Dose-related – Reversible – May be unilateral
- 19. Pyrazinamide • Interferes with mycobacterial fatty acid synthesis • Inactivate mycobateria at acidic PH • Effective against intracellular organism in machrophages – PH is low
- 20. Pyrazinamide cont: • Well absorbed from GIT • CSF penetration: equal to plasma concentration • Hepatic metabolism • Excreation - kidney
- 21. Pyrazinamide cont: Adverse effect • GI disturbances • Hepatotoxicity • Hyperuricaemia – gout • Arthralgia
- 22. Anti-TB therapy • Multiple drugs are used to reduce the emergence of resistance • Given as combination tablets • Taken 30 min before the breakfast as absorption of rifampicin is influenced by food
- 23. Anti-TB therapy cont: • A fixed dose combination (FDC) - formulation of two or more active ingredients combined in a single dosage • Improve medication compliance • To target a single disease like AIDS, TB and malaria.
- 24. Anti-TB therapy cont: • For pulmonary TB – 6 months treatment • For renal, bone and CNS infection – longer treatment
- 25. Drug resistance • Multidrug resistance (MDR) – Resistant to at least isoniazid & rifampicin – MDR-TB rate - 1.4% among newly diagnosed cases in Sri Lanka • Extensive drug resistance (XDR) – MDR strains also resistant to any fluoroquinolone & at least one injectable second-line drugs (amikacin, capreomycin, kanamycin)
- 26. Drug resistance cont: Primary drug resistance • Those exposed to resistance organism Secondary drug resistance • After initial drug sensitivity • Due to non compliance
- 27. Drug resistance cont: • Treatment for 2 years • HIV positive patients 12 months after negative culture
- 28. Drug resistance cont: • Directly observed therapy (DOT) -To improve the compliance • Hospital stay for uncooperative people
- 30. Summary : • Isoniazid – bactericidal to rapidly dividing bacteria • Rifampicin - kill intracellular bacteria • Ethambutol – bacteriostatic against multiplying bacteria • Pyrazinamide - kill dormant mycobacteria
- 31. Thank you