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Tuberculosis Drugs, Antivirals, Antiretrovirals, Antifungal and Anti-Parasitics Felix Hernandez, M.D.

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Presentation on theme: "Tuberculosis Drugs, Antivirals, Antiretrovirals, Antifungal and Anti-Parasitics Felix Hernandez, M.D."— Presentation transcript:

1 Tuberculosis Drugs, Antivirals, Antiretrovirals, Antifungal and Anti-Parasitics Felix Hernandez, M.D.

2 Antituberculosis Drugs Isoniazid Isoniazid MOA: inhibits mycolic acid synthesis in the wall MOA: inhibits mycolic acid synthesis in the wall Side Effects: peripheral neuropathies (prevent with treatment with pyridoxine), hepatitis, hepatotoxicity Side Effects: peripheral neuropathies (prevent with treatment with pyridoxine), hepatitis, hepatotoxicity Rifampin Rifampin MOA: blocks the beta subunit of bacterial RNA polymerase thus stopping bacterial RNA synthesis MOA: blocks the beta subunit of bacterial RNA polymerase thus stopping bacterial RNA synthesis Side Effects: urine and sweat turn red, induces P450, hepatitis Side Effects: urine and sweat turn red, induces P450, hepatitis Pyrazinamide Pyrazinamide MOA: nicotinamide analog with unknown mechanism MOA: nicotinamide analog with unknown mechanism Side Effects: hepatitis, hyperuricemia with gouty arthritis. Side Effects: hepatitis, hyperuricemia with gouty arthritis. Is never used alone because of rapid resistance Is never used alone because of rapid resistance Ethambutol Ethambutol MOA: inhibits mycolic acid synthesis in bacterial cell wall MOA: inhibits mycolic acid synthesis in bacterial cell wall Side Effects: reversible retrobulbar neuritis, loss of central vision Side Effects: reversible retrobulbar neuritis, loss of central vision

3 Antiviral Drugs (DNA and RNA) Acyclovir Acyclovir MOA: inhibits DNA polymerase and incorporates itself into viral DNA MOA: inhibits DNA polymerase and incorporates itself into viral DNA Clinical Use: herpes simplex 1 and 2 and Varicella zoster Clinical Use: herpes simplex 1 and 2 and Varicella zoster Side Effects: skin irritation and burning, crystalline nephropathy with rapid infusion Side Effects: skin irritation and burning, crystalline nephropathy with rapid infusion Ganciclovir Ganciclovir MOA: same as Acyclovir MOA: same as Acyclovir Clinical Uses: CMV retinitis and severe systemic CMV infections in immunocompromised patients Clinical Uses: CMV retinitis and severe systemic CMV infections in immunocompromised patients Side Effects: granulocytopenia, anemia, thrombocytopenia, renal dysfunction Side Effects: granulocytopenia, anemia, thrombocytopenia, renal dysfunction

4 Antiviral Drugs (DNA and RNA) Foscarnet Foscarnet MOA: analog of pyrophosphate and competes with it in viral DNA polymerase and reverse transcriptase therefore inhibiting DNA synthesis MOA: analog of pyrophosphate and competes with it in viral DNA polymerase and reverse transcriptase therefore inhibiting DNA synthesis Clinical Uses: CMV retinitis in immunocompromised patients and acyclovir resistant HSV Clinical Uses: CMV retinitis in immunocompromised patients and acyclovir resistant HSV Side Effects: renal toxicity, seizures, hypocalcaemia, anemia Side Effects: renal toxicity, seizures, hypocalcaemia, anemia Is deposited in bone and teeth. Is deposited in bone and teeth. Hydrate patient to protect the kidneys Hydrate patient to protect the kidneys Amantadine Amantadine MOA: prevents virus from entering susceptible cells MOA: prevents virus from entering susceptible cells Clinical Uses: treatment/prophylaxis of Influenza A in the elderly Clinical Uses: treatment/prophylaxis of Influenza A in the elderly Side Effects: depression, CNS toxicity, CHF, orthostatic hypotension, urinary retention Side Effects: depression, CNS toxicity, CHF, orthostatic hypotension, urinary retention Rimantadine is used for prophylaxis in children Rimantadine is used for prophylaxis in children

5 Antiviral Drugs (DNA and RNA) Ribavirin Ribavirin MOA: unknown MOA: unknown Clinical Uses: RSV in children Clinical Uses: RSV in children Side Effects: decreased pulmonary function, teratogenic in animals Side Effects: decreased pulmonary function, teratogenic in animals Is given via aerosol but is absorbed systemically Is given via aerosol but is absorbed systemically Oseltamivir Oseltamivir MOA: analog of adenosine monophosphate MOA: analog of adenosine monophosphate Clinical Uses: chronic hepatitis B Clinical Uses: chronic hepatitis B Side Effects: HA, asthenia (weakness and loss of strength) Side Effects: HA, asthenia (weakness and loss of strength)

6 Antiretroviral Therapy Zidovudine, Didanosine, Lamivudine Zidovudine, Didanosine, Lamivudine MOA: nucleoside HIV reverse transcriptase inhibitor MOA: nucleoside HIV reverse transcriptase inhibitor Clinical Uses: HIV in combination therapy Clinical Uses: HIV in combination therapy Zidovudine is used in the prevention of maternal- fetal transmission Zidovudine is used in the prevention of maternal- fetal transmission Mom takes it prenatally then infant takes it for 6 weeks Mom takes it prenatally then infant takes it for 6 weeks Side Effects: peripheral neuropathy, pancreatitis, myelosuppression with Zidovudine Side Effects: peripheral neuropathy, pancreatitis, myelosuppression with Zidovudine

7 Antiretroviral Therapy Ritonavir, Indinavir Ritonavir, Indinavir MOA: protease inhibitor (cleaves gag-pol) that results in immature virus formation MOA: protease inhibitor (cleaves gag-pol) that results in immature virus formation Clinical Uses: HIV in combination therapy Clinical Uses: HIV in combination therapy Side Effects: weakness, anorexia, parasthesias, indinavir has an increased risk of kidney stones Side Effects: weakness, anorexia, parasthesias, indinavir has an increased risk of kidney stones

8 Antiretroviral Therapy Nevirapine, Efavirenz Nevirapine, Efavirenz MOA: non-nucleoside inhibitor of HIV reverse transcriptase MOA: non-nucleoside inhibitor of HIV reverse transcriptase Clinical Uses: HIV  never as monotherapy due to rapid resistance Clinical Uses: HIV  never as monotherapy due to rapid resistance Side Effects: severe skin rash Side Effects: severe skin rash Nevirapine crosses the placenta Nevirapine crosses the placenta

9 Pneumocystis carinii Agents Trimethoprim-Sulfamethoxazole (Bactrim) Trimethoprim-Sulfamethoxazole (Bactrim) MOA: inhibits folate synthesis pathway MOA: inhibits folate synthesis pathway Clinical Uses: Oral is DOC for PCP prophylaxis in immunocompromised patients. IV is DOC for PCP infection Clinical Uses: Oral is DOC for PCP prophylaxis in immunocompromised patients. IV is DOC for PCP infection Pentamidine (Pentam) Pentamidine (Pentam) MOA: unknown MOA: unknown Clinical Uses: nebulized form used as an alternative for prophylaxis, IV is alternative for treatment Clinical Uses: nebulized form used as an alternative for prophylaxis, IV is alternative for treatment Side Effects: Bronchospasm Side Effects: Bronchospasm Atovaquone (Mepron) Atovaquone (Mepron) MOA: unknown MOA: unknown Clinical Uses: treatment for TMP-SMZ resistant strains Clinical Uses: treatment for TMP-SMZ resistant strains

10 Antifungal Drugs Polyenes Polyenes Amphotericin B Amphotericin B MOA: disrupts the plasma membrane of fungal cells MOA: disrupts the plasma membrane of fungal cells Clinical Uses: DOC for systemic fungal infections, fungal meningitis and fungal UTI Clinical Uses: DOC for systemic fungal infections, fungal meningitis and fungal UTI Side Effects: is toxic at therapeutic doses, nephrotoxicity, hypokalemia, thrombophlebitis, anemia Side Effects: is toxic at therapeutic doses, nephrotoxicity, hypokalemia, thrombophlebitis, anemia Nystatin Nystatin MOA: same MOA: same Clinical Uses: DOC for intestinal Candida or thrush Clinical Uses: DOC for intestinal Candida or thrush Side Effects: few adverse effects Side Effects: few adverse effects

11 Antifungal Drugs Imidazoles Imidazoles Ketoconazole Ketoconazole MOA: impairs synthesis of ergosterol which is a principle component of the fungal plasma membrane MOA: impairs synthesis of ergosterol which is a principle component of the fungal plasma membrane Clinical Uses: DOC for thrush and chronic mucocutaneous candidiasis Clinical Uses: DOC for thrush and chronic mucocutaneous candidiasis Side Effects: fetal hepatic necrosis, gynecomastia and breast pain (due to inhibition of testosterone synthesis) Side Effects: fetal hepatic necrosis, gynecomastia and breast pain (due to inhibition of testosterone synthesis) Fluconazole (Diflucan) Fluconazole (Diflucan) MOA: inhibits fungal P450 and damages the plasma membrane by inhibiting sterol demethylation which is an integral step in plasma membrane synthesis MOA: inhibits fungal P450 and damages the plasma membrane by inhibiting sterol demethylation which is an integral step in plasma membrane synthesis Clinical Uses: systemic histoplasmosis, candidal vaginitis and esophagitis Clinical Uses: systemic histoplasmosis, candidal vaginitis and esophagitis Side Effects: rash, diarrhea Side Effects: rash, diarrhea Has no effects on testosterone synthesis Has no effects on testosterone synthesis

12 Antifungal Drugs Itraconazole Itraconazole MOA: same as fluconazole MOA: same as fluconazole Clinical Uses: aspergillosis, histoplasmosis, local tinea or candidal infections Clinical Uses: aspergillosis, histoplasmosis, local tinea or candidal infections Side Effects: edema, hepatitis Side Effects: edema, hepatitis No testosterone effects No testosterone effects Clotrimazole (Lotrimin) Clotrimazole (Lotrimin) MOA: mechanism unknown MOA: mechanism unknown Clinical Uses: DOC for candida and dermatophyte infections of the skin and vaginal candidiasis Clinical Uses: DOC for candida and dermatophyte infections of the skin and vaginal candidiasis Miconazole (Monistat) Miconazole (Monistat) MOA: unknown MOA: unknown Clinical Uses: vaginal candidiasis Clinical Uses: vaginal candidiasis Side Effects: phlebitis, pruritis, rash Side Effects: phlebitis, pruritis, rash

13 Antifungal Drugs Flucytosine Flucytosine MOA: converted to 5-fluoro-uracil by the fungus and is incorporated into the RNA where thymidilate synthetase is inhibited MOA: converted to 5-fluoro-uracil by the fungus and is incorporated into the RNA where thymidilate synthetase is inhibited Side Effects: leukopenia, increased LFT, bone marrow suppression Side Effects: leukopenia, increased LFT, bone marrow suppression Griseofulvin Griseofulvin MOA: interferes with the synthesis of nucleic acids MOA: interferes with the synthesis of nucleic acids Clinical Uses: dermatophytes of hair, skin and nail. May require up to 6mo treatment Clinical Uses: dermatophytes of hair, skin and nail. May require up to 6mo treatment Side Effects: decreased memory and judgment, leukopenia, photosensitivity, possible teratogen (CI in prego) Side Effects: decreased memory and judgment, leukopenia, photosensitivity, possible teratogen (CI in prego) Terbinafine (Lamisil) Terbinafine (Lamisil) MOA: inhibits squalene epoxidase a critical enzyme in ergosterol synthesis MOA: inhibits squalene epoxidase a critical enzyme in ergosterol synthesis Clinical Uses: toe nail infection due to Trichophyton Clinical Uses: toe nail infection due to Trichophyton Side Effects: neutropenia, skin reactions and ophthalmic toxicity Side Effects: neutropenia, skin reactions and ophthalmic toxicity

14 Antiparasitic Drugs Metronidazole (Flagyl) Metronidazole (Flagyl) MOA: binds DNA and inhibits synthesis in bacteria. In parasites it’s unknown MOA: binds DNA and inhibits synthesis in bacteria. In parasites it’s unknown Clinical Uses: E. histolytica, Trichomonas, Giardia Clinical Uses: E. histolytica, Trichomonas, Giardia Side Effects: seizures, ataxia, Disulfiram-like reaction Side Effects: seizures, ataxia, Disulfiram-like reaction Lindane Lindane MOA: induces seizures in ectoparasites MOA: induces seizures in ectoparasites Clinical Uses: Scabies and lice Clinical Uses: Scabies and lice Side Effects: seizures, CNS disturbance and risk of arrhythmias Side Effects: seizures, CNS disturbance and risk of arrhythmias

15 Antiparasitic Drugs Antihelminthic Drugs Antihelminthic Drugs Mebendazole Mebendazole MOA: disrupts microtubules in worms MOA: disrupts microtubules in worms Clinical Uses: DOC for pinworm and is also effective against roundworms Clinical Uses: DOC for pinworm and is also effective against roundworms Pinworms is highly contagious and the entire family should be treated Pinworms is highly contagious and the entire family should be treated Side Effects: GI pain Side Effects: GI pain Praziquantel Praziquantel MOA: increases cell membrane permeability causing a loss of calcium which results in paralysis of the worm and release from host tissue MOA: increases cell membrane permeability causing a loss of calcium which results in paralysis of the worm and release from host tissue Clinical Uses: Schistosomiasis (single dose) Clinical Uses: Schistosomiasis (single dose) Side Effects: minimal, flu-like symptoms Side Effects: minimal, flu-like symptoms Ivermectin Ivermectin MOA: Glutamate-gated channel antagonist that causes worm paralysis MOA: Glutamate-gated channel antagonist that causes worm paralysis Clinical Uses: strongyloides and Onchocerca Clinical Uses: strongyloides and Onchocerca Side Effects: pruritis Side Effects: pruritis

16 Antimalarial Drugs Chloroquine or Hydroxychloroquine Chloroquine or Hydroxychloroquine MOA: Mechanism unclear and has wide resistance (UK) MOA: Mechanism unclear and has wide resistance (UK) Clinical Uses: prophylaxis and acute attacks Clinical Uses: prophylaxis and acute attacks Side Effects: irreversible retinal damage, hemolysis in G6PD-deficient patients Side Effects: irreversible retinal damage, hemolysis in G6PD-deficient patients Quinine Quinine MOA: not clear MOA: not clear Clinical Uses: treat chloroquine resistant P. falciparum Clinical Uses: treat chloroquine resistant P. falciparum Side Effects: Cinchonism (flushed and sweaty skin, ringing of the ears (tinnitus), blurred vision, impaired hearing, confusion, reversible high-frequency hearing loss), Most toxic antimalarial and should only be used when all other fail, cardiac arrhythmias Side Effects: Cinchonism (flushed and sweaty skin, ringing of the ears (tinnitus), blurred vision, impaired hearing, confusion, reversible high-frequency hearing loss), Most toxic antimalarial and should only be used when all other fail, cardiac arrhythmiasflushedtinnitusflushedtinnitus

17 Antimalarial Drugs Mefloquine Mefloquine MOA: structural analog of quinine MOA: structural analog of quinine Clinical Uses: multidrug resistant malaria Clinical Uses: multidrug resistant malaria Side Effects: well tolerated, benign sinus bradycardia Side Effects: well tolerated, benign sinus bradycardia Pyrimethamine Pyrimethamine MOA: inhibits folate synthesis by inhibiting dihydrofolate reductase MOA: inhibits folate synthesis by inhibiting dihydrofolate reductase Clinical Uses: Malaria prophylaxis and used in combination for acute attacks Clinical Uses: Malaria prophylaxis and used in combination for acute attacks Side Effects: Few and are very mild Side Effects: Few and are very mild Primaquine Primaquine MOA: unclear but likely to involve crosslinking of glutathione MOA: unclear but likely to involve crosslinking of glutathione Clinical Uses: chloroquine resistant Vivax malarias Clinical Uses: chloroquine resistant Vivax malarias Side Effects: hemolysis in patients with G6PD deficiency Side Effects: hemolysis in patients with G6PD deficiency


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