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

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

4 Antiviral Drugs (DNA and RNA)
Foscarnet 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 Side Effects: renal toxicity, seizures, hypocalcaemia, anemia Is deposited in bone and teeth. Hydrate patient to protect the kidneys Amantadine MOA: prevents virus from entering susceptible cells Clinical Uses: treatment/prophylaxis of Influenza A in the elderly Side Effects: depression, CNS toxicity, CHF, orthostatic hypotension, urinary retention Rimantadine is used for prophylaxis in children

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

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

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

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

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

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

11 Antifungal Drugs Imidazoles Ketoconazole Fluconazole (Diflucan)
MOA: impairs synthesis of ergosterol which is a principle component of the fungal plasma membrane Clinical Uses: DOC for thrush and chronic mucocutaneous candidiasis Side Effects: fetal hepatic necrosis, gynecomastia and breast pain (due to inhibition of testosterone synthesis) Fluconazole (Diflucan) 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 Side Effects: rash, diarrhea Has no effects on testosterone synthesis

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

13 Antifungal Drugs Flucytosine Griseofulvin Terbinafine (Lamisil)
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 Griseofulvin MOA: interferes with the synthesis of nucleic acids 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) Terbinafine (Lamisil) MOA: inhibits squalene epoxidase a critical enzyme in ergosterol synthesis Clinical Uses: toe nail infection due to Trichophyton Side Effects: neutropenia, skin reactions and ophthalmic toxicity

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

15 Antiparasitic Drugs Antihelminthic Drugs Mebendazole Praziquantel
MOA: disrupts microtubules in worms Clinical Uses: DOC for pinworm and is also effective against roundworms Pinworms is highly contagious and the entire family should be treated Side Effects: GI pain Praziquantel 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) Side Effects: minimal, flu-like symptoms Ivermectin MOA: Glutamate-gated channel antagonist that causes worm paralysis Clinical Uses: strongyloides and Onchocerca Side Effects: pruritis

16 Antimalarial Drugs Chloroquine or Hydroxychloroquine Quinine
MOA: Mechanism unclear and has wide resistance (UK) Clinical Uses: prophylaxis and acute attacks Side Effects: irreversible retinal damage, hemolysis in G6PD-deficient patients Quinine MOA: not clear 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

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


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