Antivirals, Antimalarials, and Antihelminthic Drugs

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Dr Chand's PA lecture at UDM
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Flashcards by jmburk07, updated more than 1 year ago
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Created by jmburk07 over 9 years ago
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Question Answer
Antiviral Drugs Examples Acyclovir Famciclovir Ganciclovir
Acyclovir [Properties, MOA] Guanosine derivative active against herpes Simplex Virus (HSV-1 and HSV-2) Phosphorylated and inhibits viral DNA synthesis thus preventing formation of DNA chain Decreases duration of Herpes sx, time for healing, and duration of viral shedding
Acyclovir [Adverse effects] N/V/D Nephrotoxicity
Ganciclovir [MOA, Application, Adverse Effects] Inhibits viral DNA polymerase Used for CMV cytomegalovirus infections (sore throat, fever, retinal damage, intestinal sx and hepatitis) Causes myelosuppression
Antimycobacterial Drugs Application Most often used against Myobacterium Tuberculosis which is inherently resistant to most abx
Mycobacterium Tuberculosis [General Info] Slow growing organisms that can become dormant Intracellular pathogens w/ lipid rich cell walls imperbeable to abx Rapidly develop resistance Multiple drug therapy has to be given
Mycobacterium Tuberculosis [Drug Therapy] 6-24 Months of: Rifampin Isoniazid Ethambutol Pyrazinamide Streptomycin
Isoniazid Most active drug against susceptible strains of TB Structurally similar to Pyridoxine and inhibits synthesis of Mycolic acid, a component of bacterial cell wall
Isoniazid [MOA, Metabolism] Readily absorbed by GI Tract and enters all body tissues and fluids including CSF (80-100%) of plasma concentration Metabolized by acetylation by enzyme N-Acetyl transferase (genetically determined Rapid/Slow)
Isoniazid [Dosage, Adverse Effects] Oral 150-300 mg once daily for 6-24 months Direct toxicity: Hepatitis is the most common toxicity w/ loss of appetite, N/V, jaundice Peripheral neuropathy may occur d/t Pyridoxine deficiency
Abx produced by Streptomyces mediterranei Rifampin
Rifampin [MOA] Binds to Bacterial RNA polymerase enzyme and inhibits RNA synthesis, thus its Bactericidal effect Penetrates into all tissues, cell membranes and fluids
Rifampin [Administration Guidelines] Administration with Isoniazid and other drugs for 6-18 months
Rifampin [Adverse Effects] Harmless orange color to all bodily secretions including tears, sweat, urine, etc. Rash, nephritis, and cholestatic jaundice may occur
Ethambutol [General Info.] Synthetic abx which inhibits bacterial cell wall Well absorbed and excreted by kidneys Combined with isoniazid and Rifampin
Ethambutol [Adverse Effects] Retrobulbar neuritis with loss of red-green color discrimination and loss of visual acuity
Streptomycin [MOA] Aminoglycoside inhibits 30S Ribosomes (protein synthesis) Penetrates into tissues poorly, extracellular TB bacilli killed
Streptomycin [Administration] Given as IV or IM inj daily for several months
Streptomycin [Adverse effects & Guidelines] Ototoxic and Nephrotoxic Dose adjustment required and dose limited to 6 months
Malaria [General Info.] Plasmodium falciparum, P viva, P malariae, P ovale P falciparum Male or Female Anopheles Mosquio Only RBC parasites cause clinical illness Eradication of both erythrocytic and hepatic parasites Morbidity and Death
Antimalarial Drugs [Examples] Chloroquine Amodiaquine Quinine Primaquine Abx [Tetracycline, Doxycycline] Artemisinin
Chloroquine Drug of choice for prophylaxis and cure (1940) Synthetic 4 aminoquinolines Rapidly and completely absorbed by GIT and distributed Large Vd and then slowly released
Chloroquine [MOA, SE] Acts by concentrating in parasitic food vacuoles, preventing conversion of heme into hemozoin. Heme toxicity results. Rapidly terminates fever and clears parasitemia in 24-72 hrs SE: Pruritus, N/V, abd pain, HA; Hemolysis in G6PD deficient individuals Long term drug use: Retinopathy, ototoxicity, neuropathy which is irreversible
Amodiaquine Similar Chloroquine but used effectively in combination therapy with Artesunate or Sulfonamides in tx of Falciparum malaria
Quinine Severe malarial disease Derived from Cinchona tree bark; used for 2 centuries Highly effective against all stages of Malarial parasite
Primaquine Drug of choice for P vivax and P ovale Main drug for chemophylaxis Malaria
Antimalarial Abx Tetracycline and Doxycycline is effective against the schizonts. Clindamycin is used after Chloroquine therapy
Artemisinin Qinghaosu is an herbal, Chinese antipyretic used for 2000 yrs. Produces free radicals which kill the parasite.
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