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Antituberculous drug

Antituberculous drug. First-line agents: Isoniazid(INH) Rifampin Pyrazinamide Ethambutol Streptomycin. Second-line agents : Ofloxacin Ciprofloxacin Para-amino salicylic acid Amikacin. Isoniazid. 【Antibacterial action】. Isoniazid has narrow antibacterial spectrum

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Antituberculous drug

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  1. Antituberculous drug First-line agents: Isoniazid(INH) Rifampin Pyrazinamide Ethambutol Streptomycin

  2. Second-line agents : Ofloxacin Ciprofloxacin Para-amino salicylic acid Amikacin

  3. Isoniazid 【Antibacterial action】 • Isoniazid has narrow antibacterial spectrum • It is active against mycobacterium tuberculosis • It is bacteriostatic in the stationary phase • it is bactericidal in rapidly dividing organisms • 3. It is able to penetrate into phagocytic cells

  4. 【Mechanism of action】 It inhibits the enzyme responsible for assembly of mycolic acids into the outer layer of the mycobacteria,

  5. 【Clinical uses 】 It is used for treatment of latent tuberculosis. Usually it combined with other dugs was given to treat tuberculosis.

  6. 【adverse effect 】 • Peripheral neuritis: • hand-foot trembling, anesthesia • 2. Hepatitis and idiosyncratic hepatotoxicity: • fatal hepatitis • 3. Other adverse effects: • mental abnormalities, seizures , optic neuritis , Hypersensitivity reactions

  7. Rifampicin • Rifampin is bactericidal for both intracellular and extracellular mycobacteria • It is effective against many gram (+) and gram (-) organisms • Rifampin is the most active anti-leprosy drug at present. • It blocks transcription by interacting with bacterial DNA-dependent RNA polymerase, thus inhibiting RNA synthesis

  8. 【Clinical uses and Adverse effects 】 • Mycobacterial infections: • rifampin is administered together with isoniazid, ethambutol, or another antituberculous drug • 2. Serious staphylococcal infections: • Rifampin combination therapy is use for • treatment of serious staphylococcal infections • 3. Rifampin causes nausea, vomiting, rash, and fever

  9. Antiviral drug and antifungal agent Section I Antiviral drug

  10. 一、Treatment of viral respiratory infections Amantadine Rimantadine Ribavirin

  11. Amantadine and rimantadine 【 Antiviral actions】 1. Antiviral spectrum : They are effective against RNA virus influenza A virus 2. Mechanism: Block the viral membrane matrix protein, M2 Interfere with the release of new virions

  12. 【Clinical uses and adverse effect】 • It is used for treatment of influenza A infection • Amantadine: CNS reaction • insomnia, dizziness, ataxia, hallucinations, seizures • 3. Contraindications: • psychiatric problems, cerebral atherosclerosis, • epilepsy; pregnant and nursing mothers

  13. Ribavirin 【 Antiviral actions】 1. Antiviral spectrum: Ribavirin is effective against a broad spectrum of RNA and DNA viruses RSV, hepatitis A virus, influenza A and B 2. Mechanism: Inhibiting viral mRNA synthesis

  14. 【Clinical uses】 • Ribavirin is used in treating infants and young children infected with severe RSV. • It is also used to treat acute hepatitis A virus and influenza A and B infections . • Ribavirin may reduce the mortality and viremia of Lassa fever.

  15. 【Adverse effect】 Transient anemia, elevated bilirubin. Ribavirin is contraindicated in pregnancy

  16. 二、Treatment of herpesvirus infections Acyclovir Ganciclovir

  17. Acyclovir 【Antiviral actions and clinical uses】 1. Antiviral spectrum Acyclovir is effective against DNA virus herpesviruses: herpes simplex virus-1 (HSV-1), HSV-2, varicella-zoster virus and Epstein-Barr virus, but CMV is resistant 2. Acyclovir is the treatment of choice in herpes simplex encephalitis, genital herpes infections.

  18. 【Mechanism of action】 Acyclovir thymidine kinase monophosphate derivative host’s celluar enzymes Acyclovir triphosphate incorporate into the viral DNA Inhibit viral DNA polymerase inhibits viral DNA synthesis

  19. 【Adverse effect】 1. Topical application : local irritation 2. Oral administration: headache, diarrhea, nausea, and vomiting 3. Intravenous infusion: phlebitis, transient renal dysfunction

  20. 三、Treatment for AIDS Zidovudine Didanosine Zalcitabine Stavudine Lamivudine

  21. Zidovudine 【Features】 • Zidovudine is a antiretroviral agents • It act by competitive inhibition of HIV-1 reverse transcriptase and can also be incorporated into the growing viral DNA chain to cause termination. • It is used for treatment of patients infected with HIV • Adverse effect is myelosuppression, gastrointestinal intolerance, headaches, and insomnia

  22. 四、Interferon 【Features】 • Actions: antiviral, immunomodulatory, and antiproliferative activities • Uses: treatment of both HBV and HCV virus infections • Adverse effects: fever, lethargy, bone marrow depression, cardiovascular problems and acute hypersensitivity reactions

  23. Section II Antifungal Agent Systemic antifungal drugs for systemic infections Topical antifungal drugs for mucocutaneous infections

  24. 一、Systemic antifungal drugs for systemic infections Amphotericin B Flucytosine Ketoconazole

  25. Amphotericin B 【Antifungal actions 】 • Antifungal spectrum: • It is either fungistatic or fungicidal • It is effective against a wide range of fungi • candida albicans, Histoplasma capsulatum, • cryptococcus neoformans • 2. Mode of action: • bind to ergosterol in cell membranes to form pores or channels

  26. 【 Clinical uses 】 It is often used as the initial induction regimen for serious fungal infections and is then replaced by one of the newer azole drugs for chronic therapy or prevention of relapse.

  27. 【Adverse effect】 Fever and chills, Renal impairment, Hypotension, Anemia, Neurological effects, Thrombophlebitis

  28. Flucytosine 【Antifungal actions 】 • Antifungal spectrum: • Flucytosine is fungistatic and effective against • Candida monilia, and Cryptococcus. • 2. Mode of action: • 5-FC is converted to 5-FdUMP, inhibits • thymidylate synthetase, thus disrupt nucleic acid • and protein synthesis

  29. 【 Clinical uses 】 Flucytosine is used only in combination with amphotericin for the treatment of systemic mycoses and meningitis caused by Cryptococcus neoformans and Candida.

  30. 【Adverse effect】 Hematologic toxicity, Hepatic dysfunction, Gastrointestinal disturbances

  31. Ketoconazole 【Antifungal actions 】 • Antifungal spectrum: • Ketoconazole is either fungistatic or fungicidal • It is active against thesame fungi as amphotericinB • 2. Mode of action: • Ketoconazole blocks ergosterol synthesis, increases • permeability of cell membrane

  32. 【 Clinical uses 】 Ketoconazole is most useful in the treatment of histoplasmosis, blastomycosis, Candida, and various dermatophytic infections

  33. 【Adverse effect】 Gastrointestinal distress, Endocrine effects, Hepatic dysfunction Contraindications: Ketoconazole and amphotericin B should not be used together.

  34. 二、Drugs for superficial mycoses Griseofulvin 【Antifungal actions 】 • Antifungal spectrum: • griseofulvin is principally fungistatic • It is effective only against the dermatophytes--Trichophyton, Microsporum, and Epidermophyton • 2. Mode of action: • interact with the microtubules to disrupt the mitotic • spindle and inhibit mitosis.

  35. 【 Clinical uses 】 It is used in the treatment of severe tinea infections that do not respond to other antifungal agents. Therapy must be continued until normal tissue replaces infected tissue.

  36. 【Adverse effect】 Allergic reactions, headache, nausea, hepatotoxicity

  37. Summary of antibacterial drugs

  38. β –Lactam Macrolides Lincosamides Polypeptides Aminoglycosides Tetracyclines Chloramphenicol Classification of antibacterial drugs Antibiotics Synthesis antibacterial drugs Quinolones Sulfonamides

  39. β –Lactam antibacterial drugs Penicillins Penicillin G Penicillinase-resistant penicillin (Oxacillin) Extended spectrum penicillins (Ampicillin, Amoxicillin) Antipseudomonal penicillins(Carbenicillin, Piperacillin)

  40. Penicillin G Gram-positive coccus Gram-negative coccus Gram-positive bacilli Helicoids

  41. Penicillinase-resistant penicillin( Oxacillin ) (1) They kill penicillinase-producing staphylococci (2) They can’t kill Methicillin-resistant strains of Staphylococcus aureus (MRSA) Vancomycin

  42. Extended spectrum penicillins (Ampicillin, Amoxicillin) • They are more effective against gram-negative bacilli • They can not kill pseudomonas aeruginosa Antipseudomonal penicillins Carbenicillin Piperacillin

  43. Cephalosporins Feature ＋＋＋

  44. most G+ a few G- Mycoplasma Chlamydia Legionella Macrolides Bacteriostatic G+ infection Legionella mycoplasma Chlamydia pneumonia Antibacterial spectrum

  45. Aminoglycosides Bactericidal They are effective against aerobic gram-negative bacilli They are ineffective against anaerobic organisms Antibacterial spectrum

  46. Tetracycline and Chloramphenicol antibacterial drugs

  47. Synthesis antibacterial drugs Quinolones • First generation: some G- • Second generation: More G- • Third: G+, chlamydia, mycoplasma, Legionella and Bacillus tuberculosis • The fourth: anaerobic bacterium Bactericidal Antibacterial spectrum

  48. Sulfonamides antibacterial drugs Bacteriostatic • effective against G＋and G－ • effective against Chlamydia • ineffective against mycoplasma, Rickettsia and helicoid Antibacterial spectrum

  49. Mechanism of action DNA Cell wall THF A 50S 50S 50S 30S 30S 30S DHF A Plasma membrane TMP Sulfonamides PABA Polymyxin Polyenes Azoles -lactam Vancomycin Quinolones mRNA Rifampin Tetracyclines Aminoglycosides Macrolides Chloramphenicol Lincomycin

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