This document discusses first-line drugs used to treat tuberculosis (TB), including isoniazid, rifampin, pyrazinamide, and ethambutol. It provides details on the mechanisms of action, mechanisms of resistance, pharmacokinetics, clinical uses, and adverse reactions of each drug. It emphasizes that combinations of two or more drugs are required to prevent the emergence of drug resistance during TB treatment, which typically lasts for months to years depending on the drug regimen used.
This document discusses drugs used to treat protozoal infections, focusing on those that treat amoebiasis caused by Entamoeba histolytica. It describes first-line treatments like metronidazole, ornidazole, and secnidazole, which are nitroimidazoles active against both intestinal and extraintestinal amoebiasis. For intestinal amoebiasis only, it mentions luminal amoebicides like diloxanide furoate and nitazoxanide. Rarely used reserve drugs for severe cases include emetine, dehydroemetine, and chloroquine. Other drugs mentioned are paromomycin, tetracyclines,
1) The document discusses drugs used in the treatment of constipation, including laxatives, which are classified based on their mechanism and intensity of action.
2) Bulk forming agents like fiber, psyllium, and methylcellulose work by absorbing water in the intestines and forming a gel, which softens stool and increases stool mass. Stool softeners like docusates and liquid paraffin work by a detergent action that softens stool.
3) Stimulant purgatives like bisacodyl and senna irritate the intestinal mucosa, increasing motility and fluid accumulation in the intestines. They have more potent effects than bulk formers or softeners.
Rheumatoid arthritis and osteoarthritis are common forms of arthritis. Rheumatoid arthritis is a systemic inflammatory disease that affects the joints and other organs, causing progressive joint deformity if not treated early. It can be a potentially fatal illness with increased risks of infections, renal impairment and cardiovascular disease. Osteoarthritis is the most common joint disorder and affects older individuals, particularly the weight-bearing joints like the hips and knees. It involves the breakdown of cartilage and bone within a joint. Management of both conditions involves conservative measures as well as medications aimed at reducing pain and inflammation.
This document discusses various antiamoebic drugs used to treat protozoal infections caused by Entamoeba histolytica, the parasite that causes amebiasis. It describes the life cycle of E. histolytica and clinical manifestations of amebiasis. Several classes of antiamoebic drugs are outlined, including their mechanisms of action, pharmacokinetics, clinical uses, and adverse effects. The main drugs discussed are metronidazole, tinidazole, diloxanide furoate, iodoquinol, emetine/dehydroemetine, paromomycin, and tetracyclines. Metronidazole is highlighted as the drug of choice for
This document provides information on various antihelmintic drugs used to treat helminth infections. It discusses the epidemiology of soil-transmitted helminth infections and mechanisms of action of different classes of antihelmintics. Key drugs discussed include mebendazole, albendazole, ivermectin, praziquantel, diethylcarbamazine, and piperazine. Each drug's indications, mechanisms of action, pharmacokinetics, clinical uses, and adverse effects are summarized.
Lecture slides for undergraduate MBBS class in Pharmacology on " Drugs for Diarrhoea" . It includes various treatment modalities which are used in the management of Diarrhoea. Basic source of information for preparing this slides is" Essentials of Pharmacology by KD tripathi, 7th Edition". Images are searched with the help of google images.
The document discusses drugs used to treat sexually transmitted infections. It begins by defining key terms like venereal disease, sexually transmitted disease, and sexually transmitted infection. It then covers the etiological classification of STIs, listing the causative organisms for various conditions. The majority of the document discusses treatment for specific STIs, including drugs, doses, and regimens used to treat infections like syphilis, gonorrhea, chlamydia, herpes, and HIV/AIDS. It also covers the syndromic approach for STI treatment, which classifies infections according to clinical manifestations and recommends therapy using clinical algorithms.
Non-steroidal anti-inflammatory drugs (NSAIDs) are used to treat pain and inflammation. They work by inhibiting the enzyme cyclooxygenase (Cox) and subsequent prostaglandin production. NSAIDs can be non-selective Cox inhibitors or selective Cox-2 inhibitors. Common side effects include gastrointestinal upset, which can be reduced by selective Cox-2 inhibitors or gastroprotectants. Ibuprofen is often preferred due to its relatively mild side effect profile. Proper patient selection and risk minimization strategies are important due to the side effect risks of long-term NSAID use.
This document discusses drugs used to treat protozoal infections, focusing on those that treat amoebiasis caused by Entamoeba histolytica. It describes first-line treatments like metronidazole, ornidazole, and secnidazole, which are nitroimidazoles active against both intestinal and extraintestinal amoebiasis. For intestinal amoebiasis only, it mentions luminal amoebicides like diloxanide furoate and nitazoxanide. Rarely used reserve drugs for severe cases include emetine, dehydroemetine, and chloroquine. Other drugs mentioned are paromomycin, tetracyclines,
1) The document discusses drugs used in the treatment of constipation, including laxatives, which are classified based on their mechanism and intensity of action.
2) Bulk forming agents like fiber, psyllium, and methylcellulose work by absorbing water in the intestines and forming a gel, which softens stool and increases stool mass. Stool softeners like docusates and liquid paraffin work by a detergent action that softens stool.
3) Stimulant purgatives like bisacodyl and senna irritate the intestinal mucosa, increasing motility and fluid accumulation in the intestines. They have more potent effects than bulk formers or softeners.
Rheumatoid arthritis and osteoarthritis are common forms of arthritis. Rheumatoid arthritis is a systemic inflammatory disease that affects the joints and other organs, causing progressive joint deformity if not treated early. It can be a potentially fatal illness with increased risks of infections, renal impairment and cardiovascular disease. Osteoarthritis is the most common joint disorder and affects older individuals, particularly the weight-bearing joints like the hips and knees. It involves the breakdown of cartilage and bone within a joint. Management of both conditions involves conservative measures as well as medications aimed at reducing pain and inflammation.
This document discusses various antiamoebic drugs used to treat protozoal infections caused by Entamoeba histolytica, the parasite that causes amebiasis. It describes the life cycle of E. histolytica and clinical manifestations of amebiasis. Several classes of antiamoebic drugs are outlined, including their mechanisms of action, pharmacokinetics, clinical uses, and adverse effects. The main drugs discussed are metronidazole, tinidazole, diloxanide furoate, iodoquinol, emetine/dehydroemetine, paromomycin, and tetracyclines. Metronidazole is highlighted as the drug of choice for
This document provides information on various antihelmintic drugs used to treat helminth infections. It discusses the epidemiology of soil-transmitted helminth infections and mechanisms of action of different classes of antihelmintics. Key drugs discussed include mebendazole, albendazole, ivermectin, praziquantel, diethylcarbamazine, and piperazine. Each drug's indications, mechanisms of action, pharmacokinetics, clinical uses, and adverse effects are summarized.
Lecture slides for undergraduate MBBS class in Pharmacology on " Drugs for Diarrhoea" . It includes various treatment modalities which are used in the management of Diarrhoea. Basic source of information for preparing this slides is" Essentials of Pharmacology by KD tripathi, 7th Edition". Images are searched with the help of google images.
The document discusses drugs used to treat sexually transmitted infections. It begins by defining key terms like venereal disease, sexually transmitted disease, and sexually transmitted infection. It then covers the etiological classification of STIs, listing the causative organisms for various conditions. The majority of the document discusses treatment for specific STIs, including drugs, doses, and regimens used to treat infections like syphilis, gonorrhea, chlamydia, herpes, and HIV/AIDS. It also covers the syndromic approach for STI treatment, which classifies infections according to clinical manifestations and recommends therapy using clinical algorithms.
Non-steroidal anti-inflammatory drugs (NSAIDs) are used to treat pain and inflammation. They work by inhibiting the enzyme cyclooxygenase (Cox) and subsequent prostaglandin production. NSAIDs can be non-selective Cox inhibitors or selective Cox-2 inhibitors. Common side effects include gastrointestinal upset, which can be reduced by selective Cox-2 inhibitors or gastroprotectants. Ibuprofen is often preferred due to its relatively mild side effect profile. Proper patient selection and risk minimization strategies are important due to the side effect risks of long-term NSAID use.
The document categorizes and describes various classes of drugs used in cancer chemotherapy, including their mechanisms of action, pharmacokinetics, adverse effects, and clinical uses. It discusses cytotoxic drugs that act directly on cells like alkylating agents, antimetabolites, vinca alkaloids, taxanes, and antibiotics. It also covers drugs that alter the hormonal milieu and miscellaneous drugs like hydroxyurea. For each class, it provides one or more examples and describes in detail the example drug's mechanism, pharmacokinetics, adverse effects and clinical applications.
Rheumatoid arthritis is a chronic inflammatory disease characterized by joint swelling and pain. It results from an immune system dysfunction causing inflammation. Symptoms include joint issues like stiffness and pain as well as general symptoms like fatigue. Tests can detect rheumatoid factors and inflammation markers. Treatment aims to reduce symptoms and inflammation through medications like DMARDs and biologics which suppress the immune system. DMARDs include methotrexate and sulfasalazine, while biologics target cytokines like TNF and IL-6. Care must be taken due to potential side effects of immunosuppression.
This document discusses anti-tuberculosis drugs and their use in treating tuberculosis (TB) and leprosy. It outlines the first-line drugs used to treat TB, including isoniazid, rifampin, ethambutol, pyrazinamide, and streptomycin. It describes their mechanisms of action, therapeutic uses, and potential adverse effects. The document also discusses second-line drugs and treatment regimens for both active and latent TB. Finally, it covers the drugs used to treat leprosy, including dapsone, clofazimine, and rifampin.
This document discusses anti-diarrheal treatments. It introduces that diarrhoea and constipation negatively impact quality of life and health care costs. About 8-9% of people suffer from chronic constipation and 4-5% from chronic diarrhoea. Common causes of diarrhoea include infection, diet, medication, and intestinal disease. Treatment involves rehydration, antimotility agents like loperamide to reduce motility, and antimicrobials for infectious causes. Prevention emphasizes good hygiene and handwashing to avoid spread of infectious diarrhoea.
This document provides an overview of the treatment of rheumatoid arthritis (RA). It discusses the epidemiology and etiology of RA and outlines past, present, and future treatment paradigms. The importance of early diagnosis and treatment is emphasized. Diagnostic criteria and methods for assessing disease severity are presented. Guidelines are provided for using nonsteroidal anti-inflammatory drugs, corticosteroids, disease-modifying antirheumatic drugs (DMARDs), and biological response modifiers (BRMs) to treat RA. Specific DMARDs and BRMs discussed include methotrexate, hydroxychloroquine, sulfasalazine, leflunomide, etanercept, infliximab, and
This document discusses anti-leprotic drugs used to treat leprosy, which is caused by Mycobacterium leprae. It outlines the classification, mechanisms of action, adverse effects, and resistance issues of main drugs used including dapsone, clofazimine, rifampin, ofloxacin and minocycline. It also describes multidrug therapy regimens introduced by WHO using combinations of these drugs to shorten treatment duration and prevent resistance. Alternative regimens are discussed for cases of rifampin resistance. Reactions during leprosy treatment like lepra reaction are also summarized.
Entamoeba histolytica is a protozoan parasite that causes amoebiasis. It is transmitted through the oral-fecal route by ingesting cysts from contaminated food or water. In the intestines, cysts excyst into trophozoites which multiply and may invade the intestinal wall, causing dysentery. Trophozoites can spread to other organs through the bloodstream. Metronidazole is effective against both intestinal and tissue infections, as it is activated by anaerobic metabolism and kills the trophozoites. Other nitroimidazole derivatives like tinidazole and ornidazole are also used to treat amoebiasis.
The document discusses drug therapy for diabetes, including types of insulin, oral medications to treat type 2 diabetes, and guidelines for treatment. It provides details on short acting, intermediate acting, and long acting insulins. It also describes classes of oral medications like thiazolidinediones, biguanides, sulfonylureas, meglitinides, and alpha-glucosidase inhibitors. The document outlines targets for managing diabetes and discusses combination therapy options.
This document discusses doxycycline, a broad-spectrum antibiotic derived from tetracycline. It inhibits protein synthesis by reversibly binding to the 30S subunit of bacteria to block aminoacyl-tRNA binding. It has activity against many gram-positive and gram-negative bacteria. Doxycycline is used to treat infections caused by Mycoplasma pneumoniae, Rickettsiae, Chlamydia, Vibrio cholerae, Bacillus anthracis, and spirochetes. Adverse effects include gastrointestinal issues, tooth discoloration in children, and liver and photosensitization. It is contraindicated in pregnancy, infants, and those with hypersensitivity.
The document discusses drugs used for treating tuberculosis and related mycobacterial infections. It provides learning outcomes on first-line and second-line antitubercular drugs, their mechanisms of action, mechanisms of resistance, pharmacokinetics, and management of tuberculosis. The first section introduces commonly used first-line drugs like isoniazid, rifampin, pyrazinamide, ethambutol, and streptomycin. The second section covers second-line drugs and new drugs like bedaquiline used for multidrug-resistant tuberculosis. The last section discusses principles of antituberculosis chemotherapy and types of treatment including prophylaxis and therapy for drug-susceptible and drug-resistant tuberculosis.
The document summarizes the key aspects of thyroid hormone synthesis and regulation. It discusses:
1) The thyroid gland secretes the hormones triiodothyronine (T3), tetraiodothyronine (T4), and calcitonin. T3 and T4 are synthesized from tyrosine residues within the thyroglobulin molecule through iodination and coupling reactions.
2) Thyroid stimulating hormone (TSH) from the pituitary stimulates thyroid hormone production and release, forming a negative feedback loop with T3 and T4.
3) Thyroid hormones regulate growth, development, metabolism and have wide-ranging effects in the body through nuclear receptors that control gene expression.
This document discusses drugs used to treat constipation and diarrhea. For constipation, it describes laxatives that promote bowel evacuation, including bulk formers, stool softeners, and stimulant purgatives. For diarrhea, it outlines rehydration therapy and maintaining nutrition. Drug treatment includes specific antimicrobials, probiotics, drugs for inflammatory bowel disease, and nonspecific antidiarrheal drugs that are absorbents, antisecretory, or antimotility agents.
The document discusses various anthelmintic drugs, including their mechanisms of action, pharmacokinetics, therapeutic uses, and adverse effects. It focuses on commonly used drugs like albendazole, mebendazole, piperazine, diethylcarbamazine, ivermectin, praziquantel, and niclosamide which are used to treat infections caused by different types of intestinal worms and parasites. The document also provides an overview of the epidemiology and control of helminth infections.
Helminth infections affect over two billion people worldwide. Anthelmintic drugs are used to kill or expel parasitic helminths. Major anthelmintic drug classes include piperazines, benzimidazoles, heterocyclics, and natural products. Mebendazole is a commonly used benzimidazole with broad-spectrum activity against intestinal worms and low incidence of side effects. Albendazole is similarly broad-spectrum but also treats cystic diseases. Diethyl carbamazine selectively kills microfilariae and is used to treat filariasis. Ivermectin is the treatment of choice for onchocerciasis and strongyloidiasis by enhancing chloride
This document discusses drugs used to treat gout, including colchicine, NSAIDs, corticosteroids, uricosuric agents like probenecid and sulfinpyrazone, and the uric acid synthesis inhibitor allopurinol. It provides details on the pathophysiology of gout, mechanisms of action, pharmacokinetics, indications, dosages and adverse effects of these drugs for both acute gout attacks and long-term treatment of chronic gout and hyperuricemia.
This document discusses mycobacterial infections, focusing on tuberculosis and leprosy. It provides details on the causative organisms, epidemiology, pathogenesis, classification of anti-tubercular drugs, mechanisms of action, resistance, treatment approaches, and drug-resistant tuberculosis. The main points covered are that tuberculosis is caused by Mycobacterium tuberculosis and is the leading infectious disease worldwide. Treatment involves a combination of first-line and second-line drugs administered for extended periods to prevent resistance and achieve cure. Drug-resistant tuberculosis including multi-drug resistant TB requires complex second-line drug regimens.
Clinical situations when to use 2nd line agents
In case of resistance to first-line agents
In case of failure of clinical response to conventional therapy
In case of serious Rx-limiting adverse drug reactions
When expert guidance is available to deal with the toxic effects
Many of 2nd -line drugs , their dosage, emergence of resistance & long-term toxicity have not been fully established.
Ethionamide
Chemically related to isoniazid
Mechanism of action
Blocks synthesis of mycolic acids.
Anti-mycobacterial activity
M. tuberculosis & some other Spp of mycobacteria
This document discusses antimycobacterial drugs used to treat tuberculosis and other mycobacterial infections. It provides information on various first-line drugs including isoniazid, rifampin, pyrazinamide, ethambutol, and streptomycin. It notes that combinations of two or more drugs are required to treat mycobacterial infections due to slow growth and potential drug resistance. Treatment must be prolonged, typically for months to years, to eliminate both actively dividing and dormant bacteria. Second-line drugs are discussed for treatment of multi-drug resistant infections. Worldwide tuberculosis statistics and drug regimens are also summarized.
The document categorizes and describes various classes of drugs used in cancer chemotherapy, including their mechanisms of action, pharmacokinetics, adverse effects, and clinical uses. It discusses cytotoxic drugs that act directly on cells like alkylating agents, antimetabolites, vinca alkaloids, taxanes, and antibiotics. It also covers drugs that alter the hormonal milieu and miscellaneous drugs like hydroxyurea. For each class, it provides one or more examples and describes in detail the example drug's mechanism, pharmacokinetics, adverse effects and clinical applications.
Rheumatoid arthritis is a chronic inflammatory disease characterized by joint swelling and pain. It results from an immune system dysfunction causing inflammation. Symptoms include joint issues like stiffness and pain as well as general symptoms like fatigue. Tests can detect rheumatoid factors and inflammation markers. Treatment aims to reduce symptoms and inflammation through medications like DMARDs and biologics which suppress the immune system. DMARDs include methotrexate and sulfasalazine, while biologics target cytokines like TNF and IL-6. Care must be taken due to potential side effects of immunosuppression.
This document discusses anti-tuberculosis drugs and their use in treating tuberculosis (TB) and leprosy. It outlines the first-line drugs used to treat TB, including isoniazid, rifampin, ethambutol, pyrazinamide, and streptomycin. It describes their mechanisms of action, therapeutic uses, and potential adverse effects. The document also discusses second-line drugs and treatment regimens for both active and latent TB. Finally, it covers the drugs used to treat leprosy, including dapsone, clofazimine, and rifampin.
This document discusses anti-diarrheal treatments. It introduces that diarrhoea and constipation negatively impact quality of life and health care costs. About 8-9% of people suffer from chronic constipation and 4-5% from chronic diarrhoea. Common causes of diarrhoea include infection, diet, medication, and intestinal disease. Treatment involves rehydration, antimotility agents like loperamide to reduce motility, and antimicrobials for infectious causes. Prevention emphasizes good hygiene and handwashing to avoid spread of infectious diarrhoea.
This document provides an overview of the treatment of rheumatoid arthritis (RA). It discusses the epidemiology and etiology of RA and outlines past, present, and future treatment paradigms. The importance of early diagnosis and treatment is emphasized. Diagnostic criteria and methods for assessing disease severity are presented. Guidelines are provided for using nonsteroidal anti-inflammatory drugs, corticosteroids, disease-modifying antirheumatic drugs (DMARDs), and biological response modifiers (BRMs) to treat RA. Specific DMARDs and BRMs discussed include methotrexate, hydroxychloroquine, sulfasalazine, leflunomide, etanercept, infliximab, and
This document discusses anti-leprotic drugs used to treat leprosy, which is caused by Mycobacterium leprae. It outlines the classification, mechanisms of action, adverse effects, and resistance issues of main drugs used including dapsone, clofazimine, rifampin, ofloxacin and minocycline. It also describes multidrug therapy regimens introduced by WHO using combinations of these drugs to shorten treatment duration and prevent resistance. Alternative regimens are discussed for cases of rifampin resistance. Reactions during leprosy treatment like lepra reaction are also summarized.
Entamoeba histolytica is a protozoan parasite that causes amoebiasis. It is transmitted through the oral-fecal route by ingesting cysts from contaminated food or water. In the intestines, cysts excyst into trophozoites which multiply and may invade the intestinal wall, causing dysentery. Trophozoites can spread to other organs through the bloodstream. Metronidazole is effective against both intestinal and tissue infections, as it is activated by anaerobic metabolism and kills the trophozoites. Other nitroimidazole derivatives like tinidazole and ornidazole are also used to treat amoebiasis.
The document discusses drug therapy for diabetes, including types of insulin, oral medications to treat type 2 diabetes, and guidelines for treatment. It provides details on short acting, intermediate acting, and long acting insulins. It also describes classes of oral medications like thiazolidinediones, biguanides, sulfonylureas, meglitinides, and alpha-glucosidase inhibitors. The document outlines targets for managing diabetes and discusses combination therapy options.
This document discusses doxycycline, a broad-spectrum antibiotic derived from tetracycline. It inhibits protein synthesis by reversibly binding to the 30S subunit of bacteria to block aminoacyl-tRNA binding. It has activity against many gram-positive and gram-negative bacteria. Doxycycline is used to treat infections caused by Mycoplasma pneumoniae, Rickettsiae, Chlamydia, Vibrio cholerae, Bacillus anthracis, and spirochetes. Adverse effects include gastrointestinal issues, tooth discoloration in children, and liver and photosensitization. It is contraindicated in pregnancy, infants, and those with hypersensitivity.
The document discusses drugs used for treating tuberculosis and related mycobacterial infections. It provides learning outcomes on first-line and second-line antitubercular drugs, their mechanisms of action, mechanisms of resistance, pharmacokinetics, and management of tuberculosis. The first section introduces commonly used first-line drugs like isoniazid, rifampin, pyrazinamide, ethambutol, and streptomycin. The second section covers second-line drugs and new drugs like bedaquiline used for multidrug-resistant tuberculosis. The last section discusses principles of antituberculosis chemotherapy and types of treatment including prophylaxis and therapy for drug-susceptible and drug-resistant tuberculosis.
The document summarizes the key aspects of thyroid hormone synthesis and regulation. It discusses:
1) The thyroid gland secretes the hormones triiodothyronine (T3), tetraiodothyronine (T4), and calcitonin. T3 and T4 are synthesized from tyrosine residues within the thyroglobulin molecule through iodination and coupling reactions.
2) Thyroid stimulating hormone (TSH) from the pituitary stimulates thyroid hormone production and release, forming a negative feedback loop with T3 and T4.
3) Thyroid hormones regulate growth, development, metabolism and have wide-ranging effects in the body through nuclear receptors that control gene expression.
This document discusses drugs used to treat constipation and diarrhea. For constipation, it describes laxatives that promote bowel evacuation, including bulk formers, stool softeners, and stimulant purgatives. For diarrhea, it outlines rehydration therapy and maintaining nutrition. Drug treatment includes specific antimicrobials, probiotics, drugs for inflammatory bowel disease, and nonspecific antidiarrheal drugs that are absorbents, antisecretory, or antimotility agents.
The document discusses various anthelmintic drugs, including their mechanisms of action, pharmacokinetics, therapeutic uses, and adverse effects. It focuses on commonly used drugs like albendazole, mebendazole, piperazine, diethylcarbamazine, ivermectin, praziquantel, and niclosamide which are used to treat infections caused by different types of intestinal worms and parasites. The document also provides an overview of the epidemiology and control of helminth infections.
Helminth infections affect over two billion people worldwide. Anthelmintic drugs are used to kill or expel parasitic helminths. Major anthelmintic drug classes include piperazines, benzimidazoles, heterocyclics, and natural products. Mebendazole is a commonly used benzimidazole with broad-spectrum activity against intestinal worms and low incidence of side effects. Albendazole is similarly broad-spectrum but also treats cystic diseases. Diethyl carbamazine selectively kills microfilariae and is used to treat filariasis. Ivermectin is the treatment of choice for onchocerciasis and strongyloidiasis by enhancing chloride
This document discusses drugs used to treat gout, including colchicine, NSAIDs, corticosteroids, uricosuric agents like probenecid and sulfinpyrazone, and the uric acid synthesis inhibitor allopurinol. It provides details on the pathophysiology of gout, mechanisms of action, pharmacokinetics, indications, dosages and adverse effects of these drugs for both acute gout attacks and long-term treatment of chronic gout and hyperuricemia.
This document discusses mycobacterial infections, focusing on tuberculosis and leprosy. It provides details on the causative organisms, epidemiology, pathogenesis, classification of anti-tubercular drugs, mechanisms of action, resistance, treatment approaches, and drug-resistant tuberculosis. The main points covered are that tuberculosis is caused by Mycobacterium tuberculosis and is the leading infectious disease worldwide. Treatment involves a combination of first-line and second-line drugs administered for extended periods to prevent resistance and achieve cure. Drug-resistant tuberculosis including multi-drug resistant TB requires complex second-line drug regimens.
Clinical situations when to use 2nd line agents
In case of resistance to first-line agents
In case of failure of clinical response to conventional therapy
In case of serious Rx-limiting adverse drug reactions
When expert guidance is available to deal with the toxic effects
Many of 2nd -line drugs , their dosage, emergence of resistance & long-term toxicity have not been fully established.
Ethionamide
Chemically related to isoniazid
Mechanism of action
Blocks synthesis of mycolic acids.
Anti-mycobacterial activity
M. tuberculosis & some other Spp of mycobacteria
This document discusses antimycobacterial drugs used to treat tuberculosis and other mycobacterial infections. It provides information on various first-line drugs including isoniazid, rifampin, pyrazinamide, ethambutol, and streptomycin. It notes that combinations of two or more drugs are required to treat mycobacterial infections due to slow growth and potential drug resistance. Treatment must be prolonged, typically for months to years, to eliminate both actively dividing and dormant bacteria. Second-line drugs are discussed for treatment of multi-drug resistant infections. Worldwide tuberculosis statistics and drug regimens are also summarized.
Tuberculosis is caused by infection with Mycobacterium tuberculosis. It infects over a billion people worldwide and kills millions each year. A combination of drugs, including isoniazid, rifampin, pyrazinamide, and ethambutol or streptomycin, are used to treat tuberculosis. Isoniazid and rifampin are the most effective drugs but multi-drug therapy is required to prevent resistance. Both drugs have bactericidal effects and penetrate tissues well but can cause adverse reactions like hepatitis which requires monitoring during treatment.
This PPT covers drug therapy for tuberculosis. It includes classification of antitubercular drugs, chemotherapy for tuberculosis, strategies for addressing resistance and pharmacotherapy of antitubercular drugs
CHEMOTHERAPY OF TUBERCULOSIS AND LEPROSY.POWERPOINT.pptxSamuelAgboola11
This document provides information on the chemotherapy of tuberculosis and leprosy. It defines tuberculosis and leprosy, and describes their causative organisms. It discusses first and second line drugs used to treat tuberculosis, including isoniazid, rifampicin, ethambutol, pyrazinamide, and streptomycin. It describes the dosages and unwanted effects of these drugs. It also discusses multidrug-resistant tuberculosis. For leprosy, it discusses the drugs used, including dapsone, rifampin, and clofazimine, and the WHO recommendations for treatment of multibacillary and paucibacillary leprosy.
Leprosy
Tuberculosis
TYB pharmacy
Pharmacology semester VI notes
Pharmacology VI semester
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Third year B pharmacy pharmacology notes
Pharmacology unit 3 notes
Pharmacology VI semester notes
- Mycobacterium infections like tuberculosis are difficult to treat due to their lipid-rich cell walls and ability to reside intracellularly. Combination drug therapy is required to prevent resistance.
- Common first-line drugs include isoniazid, rifampin, pyrazinamide, and ethambutol. Second-line alternatives include ethionamide, capreomycin, cycloserine, aminoglycosides, and fluoroquinolones.
- Each drug has a unique mechanism of action and potential adverse effects that require monitoring like hepatitis, neuropathy, and optic neuritis. Combination therapy and treatment duration aims to kill both actively growing and dormant bacilli.
The document discusses antimycobacterial drugs used to treat tuberculosis and leprosy. It begins by outlining the challenges of treating infections caused by slow-growing mycobacteria, including their intrinsic resistance. It then describes the goals and principles of TB therapy, including using multi-drug regimens to prevent resistance. The first-line drugs for TB, including isoniazid, rifampin, pyrazinamide, and ethambutol are discussed in detail. Treatment regimens for both adults and children are provided. The document also covers definitions and treatment approaches for drug-resistant TB. Finally, it concludes with an overview of drugs used to treat leprosy such as dapsone, rifamp
This document provides information on Mycobacterium tuberculosis, the bacteria that causes tuberculosis (TB). It discusses the physiology and structure of M. tuberculosis, how it is transmitted, diagnosed, and its typical appearance under microscopy. The document also categorizes and describes the mechanisms and uses of both first- and second-line anti-tuberculosis drugs, including isoniazid, rifampin, pyrazinamide, ethambutol, and streptomycin from the first line and ethionamide, cycloserine, and thiacetazone from the second line. It addresses drug-resistant TB and the different groupings of alternative drugs used to treat multi- and extensively drug-resistant strains.
Clinical Pharmacology of the Anthelmintic Drugs.pptNorhanKhaled15
This document summarizes several anthelmintic drugs including albendazole, bithionol, diethylcarbamazine, and ivermectin. It provides information on the chemistry, pharmacokinetics, anthelmintic actions, clinical uses, adverse reactions, and contraindications for each drug. Albendazole is the drug of choice for many intestinal helminth infections. Bithionol is used for fascioliasis and paragonimiasis. Diethylcarbamazine treats filariasis and loiasis. Ivermectin is primarily used for strongyloidiasis and onchocerciasis. Each drug requires careful administration and monitoring for
This document discusses anti-tubercular drugs. It begins by describing tuberculosis and its transmission. It then discusses the classification of anti-TB drugs into 1st line essential, 1st line supplemental, and 2nd line drugs. The individual drugs discussed in detail include isoniazid, rifampicin, ethambutol, pyrazinamide, and streptomycin. It covers their mechanisms of action, mechanisms of resistance, pharmacokinetics, dosages, adverse effects, and interactions. Treatment categories and regimens are also summarized.
This document discusses anti-tuberculosis drugs used to treat bone tuberculosis. It describes the standard Category I treatment regimen of 2 months of isoniazid, rifampin, pyrazinamide, and ethambutol, followed by 4 months of isoniazid and rifampin. While treatment duration was historically long, modern drugs achieve high bone concentrations and shorter regimens are effective. The document also details first-line drugs like isoniazid and rifampin and second-line drugs used to treat multidrug-resistant tuberculosis. Adverse effects and mechanisms of action are provided for each major anti-tuberculosis medication.
Viruses rely on host cell processes for replication, so antiviral agents target specific steps in the viral life cycle. Acyclovir inhibits herpes virus DNA synthesis and is used to treat herpes infections. Antiretrovirals target HIV replication through four classes: nucleoside/nucleotide reverse transcriptase inhibitors, protease inhibitors, non-nucleoside reverse transcriptase inhibitors, and fusion inhibitors. Antifungals include polyenes like amphotericin B, which forms pores in fungal cell membranes, and azoles like fluconazole and itraconazole, which inhibit fungal enzyme synthesis. Each drug has characteristic mechanisms, spectrums of activity, and side effect profiles for treating
Viruses rely on host cell processes for replication, so antiviral agents target specific steps in the viral life cycle. Acyclovir inhibits herpes virus DNA synthesis and is used to treat herpes infections. Antiretrovirals target HIV replication through four classes: nucleoside/nucleotide reverse transcriptase inhibitors, protease inhibitors, non-nucleoside reverse transcriptase inhibitors, and fusion inhibitors. Amphotericin B and azoles such as fluconazole and itraconazole are broad-spectrum antifungals used to treat serious fungal infections. They work by binding to ergosterol in fungal cell membranes or inhibiting fungal enzyme production.
Viruses rely on host cell processes for replication, so antiviral agents target specific steps in the viral life cycle. Acyclovir inhibits herpes virus DNA synthesis and is used to treat herpes infections. Antiretrovirals for HIV include nucleoside/nonnucleoside reverse transcriptase inhibitors and protease inhibitors. Antifungals include polyenes like amphotericin B, which forms pores in fungal membranes, and azoles like fluconazole and itraconazole, which inhibit fungal enzyme synthesis. These drugs have different mechanisms and are used to treat various fungal infections.
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.
This document provides an overview and update on anti-tuberculosis therapy. It begins by outlining the objectives of becoming familiar with first and second line anti-tuberculosis drugs, their treatment regimens, adverse effects and drug interactions. It then reviews the standard first line treatment regimen of 2HRZE/4HR, describes the common first line drugs isoniazid, rifampin and ethambutol and their adverse effects. It also briefly discusses second line drugs and treatment in special populations before concluding with a review of multi-drug resistant tuberculosis and second line treatment options.
This document discusses chemotherapy for tuberculosis, including first-line and second-line antitubercular drugs. It describes the classification, mechanisms of action, pharmacokinetics, and adverse effects of isoniazid, rifampin, pyrazinamide, ethambutol, and streptomycin as first-line drugs. It also mentions that the goals of antitubercular chemotherapy are to kill dividing bacilli, kill persisting bacilli, and prevent emergence of drug resistance. The document assigns discussing the mechanisms, adverse effects, and uses of second-line drugs including kanamycin, amikacin, capreomycin, fluoroquinolones, and ethionamide.
This document discusses chemotherapy for tuberculosis, including first-line and second-line antitubercular drugs. It describes the classification, mechanisms of action, pharmacokinetics, and adverse effects of isoniazid, rifampin, pyrazinamide, ethambutol, and streptomycin as first-line drugs. It also mentions that the goals of antitubercular chemotherapy are to kill dividing bacilli, kill persisting bacilli, and prevent emergence of drug resistance. The document assigns discussing the mechanisms, adverse effects, and uses of second-line drugs including kanamycin, amikacin, capreomycin, fluoroquinolones, and ethionamide.
This document discusses anti-protozoal agents used to treat various protozoal infections. It begins by listing important protozoal infections and their causative organisms. It then describes the drugs used to treat each infection, including nitroimidazoles, amphotericin B, eflornithine, iodoquinol, melarsoprol, miltefosine, nifurtimox, benznidazole, and nitazoxanide. It provides details on the mechanisms of action, pharmacokinetics, therapeutic uses and dosages, toxicities, and side effects of these individual agents.
Pyramidal, bony cavity facial skeleton
Base anterior, apex posterior
Contains and protects eyeball, muscles, nerves, vessels & most of the lacrimal apparatus
Bones forming orbit lined with periorbita
Forms Fascial sheath of the eyeball
By the end of the lecture, students should be able to:
Describe briefly development of the thyroid & parathyroid glands.
Describe the shape, position, relations and structure of the thyroid gland.
Describe the shape, position, blood supply & lymphatic drainage of the parathyroid glands.
List the blood supply & lymphatic drainage of the thyroid gland.
Describe the most common congenital anomalies of the thyroid gland.
List the nerves endanger with thyroidectomy operation.
Is a multilayered structure with the layers that can be defined by the word itself.
Extends from;
The supraorbital margins anteriorly
To the highest nuchal line posteriorly
Down to the ears & zygomatic arches laterally.
The forehead is common to both the scalp & face.
1. The document discusses the meninges, cerebral spinal fluid, and dural venous sinuses. It describes the three meningeal layers - dura mater, arachnoid mater, and pia mater.
2. It then provides details on the various dural venous sinuses, including their locations, tributaries, and drainage. Key sinuses discussed include the superior sagittal sinus, straight sinus, transverse sinus, sigmoid sinus, and cavernous sinus.
3. The document also covers cerebral spinal fluid, including its composition and functions. The choroid plexus is described as actively secreting CSF in the ventricles.
The document discusses the temporomandibular joint (TMJ) and types of dislocations that can occur. It notes that the masticatory system includes the TMJ and masticatory muscles. There are four types of TMJ dislocations: anterior from contraction of lateral pterygoid muscles, lateral from blows to the jaw when open, posterior which are uncommon, and those caused by fractures involving the mandible neck. Treatment involves reduction maneuvers. The document also lists clinical correlates of TMJ issues like arthritis, developmental disorders, metabolic/neoplastic disorders, and inflammatory/pain dysfunction syndromes.
The region on the lateral surface of the face that comprises the parotid gland & the structures immediately related to it
Largest of the salivary glands
Located subcutaneously, below and in front of the external auditory meatus
Occupies the deep hollow behind the ramus of the mandible
Wedge-shaped when viewed externally, with the base above & the apex behind the angle of the mandible
Part of the body between the head and the thorax
Contains a number of vessels, nerves and structures connecting the head to the trunk and upper limbs
These include the esophagus, trachea, brachial plexus, carotid arteries, jugular veins, vagus and accessory nerves, lymphatics among others
A layer of pseudostratified ciliated columnar epithelial cells that secrete mucus
Found in nose, sinuses, pharynx, larynx and trachea
Mucus can trap contaminants
Cilia move mucus up towards mouth
Has a free tip and attached to forehead by the bridge.
External orifices (nares) bounded laterally by the ala & medially by nasal septum.
Framework above made up of: nasal bones, frontal process of maxilla, nasal part of frontal bone.
Framework below : by plates of hyaline cartilage; upper and lower nasal cartilages, and septal cartilage
The head and neck region of four week human embryo somewhat resemble these regions of a fish embryo of comparable stage
This explains the former use of designation branchial apparatus
Branchial is derived from the Greek word branchia or gill
Located on the side of the head
Extends from the superior temporal lines to the zygomatic arch.
Communicates with the infratemporal fossa deep to the zygomatic arch.
Contains a numbers of structures that include a muscle, nerves, blood vessels
The larynx is a respiratory organ located located within the anterior aspect of the neck.
Anterior to the inferior portion of the pharynx but superior to the trachea, lies below the hyoid bone in the midline at C3-6 vertebra level.
Its primary function is to provide a protective sphincter for air passages.
This document provides an overview of the anatomy of the upper and lower urinary tract. It describes the kidneys, including their location, internal structure consisting of the cortex, medulla and renal sinus. It discusses the vascular segments and blood supply to the kidneys. It also describes the ureters that carry urine from the kidneys to the urinary bladder, and provides details on the anatomy of the urinary bladder in both males and females.
The esophagus is a muscular tube connecting the throat (pharynx) with the stomach. The esophagus is about 8 inches long, and is lined by moist pink tissue called mucosa. The esophagus runs behind the windpipe (trachea) and heart, and in front of the spine. Just before entering the stomach, the esophagus passes through the diaphragm.
This document summarizes the internal female genitalia, including the ovaries, fallopian tubes, uterus, cervix, and upper part of the vagina. It describes the location, structure, blood supply, functions, and common disorders of each organ. The ovaries produce eggs and sex hormones. The fallopian tubes receive eggs from the ovaries, provide a site for fertilization, and transport fertilized eggs to the uterus. The uterus receives and nourishes a fertilized egg. The cervix connects the uterus to the vagina, which acts as a birth canal. Common disorders like ovarian cysts, ovarian cancer, and ectopic pregnancies are also discussed.
At the end of the presentation ,we should be able to describe the:
Location, shape and relations of the right and left adrenal glands.
Blood supply, lymphatic drainage and nerve supply of right and left adrenal glands
Parts of adrenal glands and function of each part.
Development of adrenal gland and common anomalies.
The pericardium is the sac that encloses the heart. It consists of an outer fibrous part known as the fibrous pericardium, and a double layered serous sac known as the serous pericardium.
The pericardium prevents
sudden dilatation of the heart, especially the right chamber, and displacement of the heart and great vessels,
minimizes friction between the heart and surrounding structures, and
prevents the spread of infection or cancer from the lung or pleura.
Major Function:
Makes sperm cells (gametes) and transfer the sperm into the female reproductive system in order to fertilize the female gametes to produce a zygote.
Include:
the testes, the epididymis, the vas deferens, the seminal vesicles, the prostate gland, and the Cowper’s glands.
The testes, (To Testify) the paired, oval-shaped organs that produce sperm and male sex hormones, are located in the scrotum.
They are highly innervated and sensitive to touch and pressure.
The testes produce testosterone, which is responsible for the development of male sexual characteristics and sex drive (libido).
The azygos vein connects the inferior vena cava and the superior vena cava
The thoracic duct is the largest lymph vessel that ultimately drains lymph from all parts of the body into the blood circulation
We shall look at them one at a time
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Histololgy of Female Reproductive System.pptxAyeshaZaid1
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Overall life span (LS) was 1671.7±1721.6 days and cumulative 5YS reached 62.4%, 10 years – 50.4%, 20 years – 44.6%. 94 LCP lived more than 5 years without cancer (LS=2958.6±1723.6 days), 22 – more than 10 years (LS=5571±1841.8 days). 67 LCP died because of LC (LS=471.9±344 days). AT significantly improved 5YS (68% vs. 53.7%) (P=0.028 by log-rank test). Cox modeling displayed that 5YS of LCP significantly depended on: N0-N12, T3-4, blood cell circuit, cell ratio factors (ratio between cancer cells-CC and blood cells subpopulations), LC cell dynamics, recalcification time, heparin tolerance, prothrombin index, protein, AT, procedure type (P=0.000-0.031). Neural networks, genetic algorithm selection and bootstrap simulation revealed relationships between 5YS and N0-12 (rank=1), thrombocytes/CC (rank=2), segmented neutrophils/CC (3), eosinophils/CC (4), erythrocytes/CC (5), healthy cells/CC (6), lymphocytes/CC (7), stick neutrophils/CC (8), leucocytes/CC (9), monocytes/CC (10). Correct prediction of 5YS was 100% by neural networks computing (error=0.000; area under ROC curve=1.0).
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Cell Therapy Expansion and Challenges in Autoimmune DiseaseHealth Advances
There is increasing confidence that cell therapies will soon play a role in the treatment of autoimmune disorders, but the extent of this impact remains to be seen. Early readouts on autologous CAR-Ts in lupus are encouraging, but manufacturing and cost limitations are likely to restrict access to highly refractory patients. Allogeneic CAR-Ts have the potential to broaden access to earlier lines of treatment due to their inherent cost benefits, however they will need to demonstrate comparable or improved efficacy to established modalities.
In addition to infrastructure and capacity constraints, CAR-Ts face a very different risk-benefit dynamic in autoimmune compared to oncology, highlighting the need for tolerable therapies with low adverse event risk. CAR-NK and Treg-based therapies are also being developed in certain autoimmune disorders and may demonstrate favorable safety profiles. Several novel non-cell therapies such as bispecific antibodies, nanobodies, and RNAi drugs, may also offer future alternative competitive solutions with variable value propositions.
Widespread adoption of cell therapies will not only require strong efficacy and safety data, but also adapted pricing and access strategies. At oncology-based price points, CAR-Ts are unlikely to achieve broad market access in autoimmune disorders, with eligible patient populations that are potentially orders of magnitude greater than the number of currently addressable cancer patients. Developers have made strides towards reducing cell therapy COGS while improving manufacturing efficiency, but payors will inevitably restrict access until more sustainable pricing is achieved.
Despite these headwinds, industry leaders and investors remain confident that cell therapies are poised to address significant unmet need in patients suffering from autoimmune disorders. However, the extent of this impact on the treatment landscape remains to be seen, as the industry rapidly approaches an inflection point.
2. Antituberculosis
First line anti-TB
agents
Isoniazid
Rifampicin
Ethambutol
Pyrazinamide
Second line agents
Cycloserine
Streptomycin
Rifabutin
Ethionamide
Prothionamide
Capreomycin
Dr Ndayisaba Corneille
3. Introduction
Mycobacteria are intrinsically resistant to
most antibiotics & they grow slowly
compared with other bacteria.
Thus antibiotics that are most active
against growing cells are relatively
ineffective.
Mycobacterial cells can also be dormant &
thus completely resistant to many drugs or
killed only very slowly.
Dr Ndayisaba Corneille
4. The lipid-rich mycobacterial cell wall is
impermeable to many agents.
Mycobacterial species are intracellular
pathogens & organisms residing within
macrophages are inaccessible to drugs that
penetrate these cells poorly.
Dr Ndayisaba Corneille
5. Mycobacteria have ability to develop
resistance.
Combinations of 2 or more drugs is
required to overcome emergence of
resistance during course of therapy.
The response to chemotherapy is slow &
Rx must be administered for months to
years, depending on which drugs are used.
Dr Ndayisaba Corneille
6. FIRST LINE DRUGS USED IN TB RX
1st line agents
Isoniazid (H)
Rifampin (R)
Pyrazinamide(P)
Ethambutol (E)
Streptomycin (S)
Thiacetazone (T)
Dr Ndayisaba Corneille
7. Isoniazid & rifampin are the most active
drugs.
In practice, therapy is initiated with a four-
drug regimen of 2HERZ/6EH OR
2HERZ/4RH after pts are diagnosed of TB.
Prevalence of isoniazid resistance among
US clinical isolates is approx 10%.
Prevalence of resistance to both H&R
(multiple drug resistance) is about 3%.
Dr Ndayisaba Corneille
8. Isoniazid (H) or (INH)
Most active drug for Rx of TB cozed by susceptible
strains.
Has structural similarity to pyridoxine
Its bactericidal for actively growing tubercle bacilli.
It is less effective against atypical mycobacterial
species.
It penetrates into macrophages & is active against
both extracellular & intracellular organisms.
Dr Ndayisaba Corneille
9. Mechanism of Action
Inhibits synthesis of mycolic acids, which are
essential components of mycobacterial cell walls.
Blocks mycolic acid synthesis & kills the cell.
Basis of Resistance
Mutations in certain genes controlling synthesis of
mycolic acids
Dr Ndayisaba Corneille
10. Mutants are readily selected out if isoniazid or any
other drug is given as a single agent.
The use of two or more independently acting
drugs in combination is much more effective.
Probability that a bacillus is resistant to both drugs
is usually less
Dr Ndayisaba Corneille
11. Thus, at least two or more active agents
shld always be used to Rx active TB to
prevent emergence of resistance during
therapy.
Pharmacokinetics
Typical adult dose is 300 mg o.d. (5
mg/kg/d)
Up to 10 mg/kg/d may be used for serious
infections or if malabsorption is a problem.
Dr Ndayisaba Corneille
12. 5 mg/kg/d, or 900 mg, may be used in some
situations
Given IV or PO & is readily absorbed frm
GIT.
It diffuses readily into all body fluids &
tissues.
The [CNS & CSF]s ranges btn 20% & 100%
of simultaneous [serum]s.
Metabolism is esp by acetylation by liver N-
acetyltransferase & this is genetically
determined.
Dr Ndayisaba Corneille
13. Rapid clearance of drug occurs in rapid
acetylators but its usually of no
therapeutic consequence whn appropriate
doses are administered daily.
[subtherapeutic]s may occur if drug is
administered as a once-weekly dose or if
there is malabsorption.
Drug metabolites & a small amount of
unchanged drug are excreted mainly in
Dr Ndayisaba Corneille
14. The dose need not be adjusted in renal failure.
Is contraindicated if it is the coz of hepatitis
Clinical Uses
Rx of active TB in combination with other agents
Rx of Latent tuberculosis with 300 mg/d
Dr Ndayisaba Corneille
15. Adverse Reactions
The incidence & severity of unwanted effects to
isoniazid are related to dosage & duration of
administration.
Immunologic reactions
Fever
skin rashes.
Drug-induced systemic lupus erythematosus has
been reported. Dr Ndayisaba Corneille
16. Direct toxicity
Isoniazid-induced hepatitis
Most common major toxic effect.
Liver aminotransferases increase 3- 4 times
normal.
This does not require cessation of drug if pt is
asymptomatic
This is seen in 10–20% of pts.
Dr Ndayisaba Corneille
17. Clinical hepatitis with;loss of appetite, nausea,
vomiting, jaundice & right upper quadrant pain
occurs in 1% of (H) recipients & can be fatal,
particularly if drug is not discontinued promptly.
There is histologic evidence of hepatocellular
damage & necrosis is present
Dr Ndayisaba Corneille
18. Pts at high risk of Isoniazid hepatitis;
Age >50 years
Alcoholics
Pregnant women
Postpartum mothers
Dev’t of (H) hepatitis contraindicates its further
use.
Dr Ndayisaba Corneille
19. Peripheral neuropathy
Observed in 10–20% of pts given dosages >5
mg/kg/d
Infrequently seen with standard 300 mg adult
dose.
Patients at risk of neuropathy
Slow acetylators
Those with predisposing conditions like AIDS,
malnutrition, alcoholism, DM, & uremia.
Dr Ndayisaba Corneille
20. Pyridoxine, 25–50 mg/d, is recommended
for those with conditions predisposing to
neuropathy
Neuropathy is due to a relative pyridoxine
deficiency as (H) promotes excretion of
pyridoxine
Dr Ndayisaba Corneille
21. CNS toxicity;
less common
Memory loss,
Psychosis &
Seizures.
These may also respond to pyridoxine.
Dr Ndayisaba Corneille
22. Miscellaneous adverse effects
Hematologic abnormalities
Provocation of pyridoxine deficiency anemia.
Tinnitus
GI discomfort
Reduced metabolism of phenytoin, increasing its
blood level & toxicity
Dr Ndayisaba Corneille
23. Rifampin
A semisynthetic derivative of rifamycin, an
antibiotic produced by Streptomyces mediterranei.
Antibacterial activity . Active against;
Gram-positive & gram-negative cocci,
Some enteric bacteria,
Mycobacteria,
Chlamydia. Dr Ndayisaba Corneille
24. Resistant mutants are present in all microbial
popns at approx 1 in 106 & are rapidly
selected out if rifampin is used as a single
drug during active infection.
No cross-resistance to other classes of
antimicrobial drugs but cross-resistance
occur to other rifamycin derivatives, eg,
rifabutin & rifapentine.
Dr Ndayisaba Corneille
25. Mechanism of action
Thus inhibits DNA synthesis
Bactericidal
Binds to the subunit of bacterial DNA-dependent
RNA polymerase & thereby inhibits RNA synthesis.
Dr Ndayisaba Corneille
26. Pharmacokinetics
Dosage is usually 600 mg/d (10 mg/kg/d)
Given PO & well absorbed frm GIT with wide
distribution in body fluids & tissues.
Relatively highly protein-bound & adequate [CSF]s
are achieved only in presence of meningeal
inflammation.
Dr Ndayisaba Corneille
27. Readily penetrates most tissues &
phagocytic cells.
Kills organisms that are inaccessible to
many drugs, such as intracellular organisms
& those sequestered in abscesses + lung
cavities.
Excreted mainly thru liver into bile. Then
undergoes enterohepatic recirculation, with
the bulk excreted as a deacylated metabolite
in feces & a small amount in urine.
Dr Ndayisaba Corneille
28. Dose reduction in liver & renal insufficiency are not
required
Resistance
Results frm any one of several possible point
mutations in rpoB, the gene for the subunit of RNA
polymerase.
This result in reduced binding of rifampin to RNA
polymerase.
Dr Ndayisaba Corneille
29. Clinical uses
1) Mycobacterial infections like
TB
Atypical mycobacterial infections
Leprosy.
Alternative to (H) prophylaxis for pts with latent
TB only who are unable to take isoniazid.
Dr Ndayisaba Corneille
30. 2) Other indications
Elimination of meningococcal carriage
Prophylaxis for haemophilus influenzae type b
disease in contacts of children.
Eradication of staphylococcal carriage whn
combined with a 2nd agent .
Rx of serious staphylococcal infections such as
osteomyelitis & prosthetic valve endocarditis whn
used in combination therapy
Dr Ndayisaba Corneille
31. Adverse Reactions
Imparts a harmless orange color to urine, sweat,
tears & contact lenses (soft lenses may be
permanently stained).
Occasional adverse effects
Rashes
Thrombocytopenia
Nephritis or ATN
Dr Ndayisaba Corneille
32. Cholestatic jaundice
Hepatitis.
Light-chain proteinuria.
If administered less often than twice weekly it
cozes a flu-like syndrome with;
Fever
Chills,
Myalgias,
Anemia, & thrombocytopenia
Dr Ndayisaba Corneille
33. Drug interactions
Strongly induces most P450 enzymes thus
increased elimination of drugs including
methadone, anticoagulants, cyclosporine, some
anticonvulsants, PIs, NNRTIs esp neverapine, oral
contraceptives & a host of others.
Dr Ndayisaba Corneille
34. ETHAMBUTOL
Synthetic, water-soluble, heat-stable compound
Mechanism of action
Inhibit mycobacterial cell wall synthesis
Inhibits mycobacterial arabinosyl transferases,
which are encoded by embCAB operon.
Dr Ndayisaba Corneille
35. Arabinosyl transferases are involved in
polymerization reaction of arabinoglycan, an
essential component of mycobacterial cell wall.
Resistance
Resistance to ethambutol is due to mutations
resulting in overexpression of emb gene pdts or
within the embB structural gene.
Dr Ndayisaba Corneille
36. As with all other anticocks, resistance to emerges
rapidly whn drug is used alone.
Pharmacokinetics
Given PO & well absorbed frm the gut
Dosage is 15–25 mg/kg/d ,usually given as a
single daily dose in combination with other drugs.
Dr Ndayisaba Corneille
37. It crosses BBB only if meninges are
inflamed with highly variable [CSF]s of drug,
(4% to 64%) of serum levels in the setting of
meningeal inflammation.
About 20% of drug is excreted in feces &
50% in urine in unchanged form.
It accumulates in renal failure.
Dose shld be reduced by half if creatinine
clearance is < 10 mL/min.
Dr Ndayisaba Corneille
38. Clinical Use
Rx of active TB
*A higher dose is recommended for Rx of TBM
Dr Ndayisaba Corneille
39. Adverse Reactions
Hypersensitivity; Is rare.
Retrobulbar neuritis, resulting in loss of visual
acuity & red-green color blindness.
Most common serious adverse event
This dose-related S/E, more likely to occur at
doses of 25 mg/kg/d continued for several months.
Dr Ndayisaba Corneille
40. At 15 mg/kg/d or less, visual disturbances are very
rare.
Periodic visual acuity testing is desirable if 25
mg/kg/d dosage is used.
Contraindications
Relatively contraindicated in children too young to
permit assessment of visual acuity & red-green
color discrimination.
Dr Ndayisaba Corneille
41. PYRAZINAMIDE
A relative of nicotinamide.
Stable & slightly soluble in water.
An important front-line drug used in conjunction
with H&R in short-course (ie, 6-month) regimens
as a "sterilizing" agent active against residual
intracellular organisms that may cause relapse.
Dr Ndayisaba Corneille
42. Mechanism of action
The drug target & mechanism of action are
unknown.
Pyrazinamide is converted to pyrazinoic acid the
active form of the drug—by mycobacterial
pyrazinamidase, which is encoded by pncA.
The drug is taken up by macrophages & exerts its
activity against mycobacteria residing within acidic
environ’t of lysosomes.
Dr Ndayisaba Corneille
43. Resistance
Resistance may be due to impaired uptake of drug
Mutations in pncA that impair conversion of
pyrazinamide to its active form.
Tubercle bacilli develop resistance to it fairly
readily.
No cross-resistance with other anti-cocks.
Dr Ndayisaba Corneille
44. Pharmacokinetics
Given PO
Dose of 25 mg/kg/d.
Half-life is 8–11 hours.
Well absorbed frm GIT & widely distributed in body
tissues, including inflamed meninges.
It is inactive at neutral pH, but at pH 5.5 it inhibits
tubercle bacilli & some other mycobacteria
Dr Ndayisaba Corneille
45. Parent compound is metabolized by liver, but
metabolites are renally cleared.
Thus doses shld be lowered in renal insufficiency.
In pts with normal renal function, a dose of 40–50
mg/kg is used for thrice-wkly or twice-wkly Rx
regimens.
Dr Ndayisaba Corneille
46. Adverse Reactions ;
Major adverse effects include
Hepatotoxicity (1–5% of pts),
Nausea
Vomiting
Drug fever occurs uniformly & is not a reason to
halt therapy.
Hyperuricemia. May provoke acute gouty
arthritis.
Dr Ndayisaba Corneille
47. Streptomycin
o Isolated frm a strain of Streptomyces griseus.
o The antimicrobial activity is typical of that of other
aminoglycosides, as are the mechanisms of
resistance.
Dr Ndayisaba Corneille
48. Spectrum of activity against in mycobacteria
M.tuberculosis spp
Mycobacterium avium complex (MAC)
Mycobacterium kansasii
Rest of the Spp of mycobacterium are resistant .
Resistance
All large popns of tubercle bacilli contain some
streptomycin-resistant mutants.
Dr Ndayisaba Corneille
49. Resistance is due to a point mutation in either the
rpsL gene encoding the S12 ribosomal protein
gene or the rrs gene encoding 16S ribosomal
rRNA, which alters the ribosomal binding site.
Ribosomal resistance develops readily, limiting its
role as a single agent.
Dr Ndayisaba Corneille
50. Pharmacokinetics
Given IM or IV
Typical adult dosage is 1g/day (15 mg/kg/d )daily
for adults & 7.5–15 mg/kg/d for children
It penetrates into cells poorly & is active mainly
against extracellular tubercle bacilli.
It crosses BBB & achieves [therapeutic]s with
inflamed meninges.
Dr Ndayisaba Corneille
51. Clinical Uses
1. Mycobacterial infections
Used when an injectable drug is needed or
desirable
2nd -line agent for Rx of MDR-TB with other
agents.
Severe & possibly life-threatening forms of TB eg,
TBM & disseminated disease
Dr Ndayisaba Corneille
52. Adverse Reactions
Hypersensitivity
Fever
skin rashes & other allergic
manifestations.
Occurs most frequently with prolonged
contact with drug either in pts who
receive a prolonged course of Rx or in
medical personnel who handle the drug.
Dr Ndayisaba Corneille
53. Pain at the injection site
o Common but usually not severe
Disturbance of vestibular function.
o Most serious toxic effect & manifest by
Vertigo &
Loss of balance.
o Toxicity tends to be irreversible.
Dr Ndayisaba Corneille
55. Thiacetazone
Is bacteriostatic
With a low potency
Dosage is 2.5mg/day
Is the only essential anti-TB drug that can not be
given intermittently e.g. 2 timely weekly
Dr Ndayisaba Corneille
56. Has a narrow therapeutic range thus margin btn
therapeutic & toxic dose is very small
Some countries still use it in combination with
Isoniazid during continuation phase of Rx
Known ISS pts shld not be put on this drug bcoz of
its severe skin reactions thus Ethambutol shld
replace this drug in areas where HIV is common
Dr Ndayisaba Corneille
57. Side effects
Common
Skin rash often involving mucous membrane &
some times blistering
Others
Agranulocytosis
Hepatitis
Dr Ndayisaba Corneille