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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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