Classification of Antiretroviral Agents

Antiretroviral agents are synthetic antiviral agents that have antiviral activity against human immunodeficiency virus (HIV) and are used in the management of HIV infection. There currently are 5 different classes of antiretroviral agents commercially available: nucleoside reverse transcriptase inhibitors (NRTIs), HIV protease inhibitors, nonnucleoside reverse transcriptase inhibitors (NNRTIs), nucleotide reverse transcriptase inhibitors, and HIV fusion inhibitors.

Rimantadine Hydrochloride

While the optimum dose and duration of therapy have not been established, rimantadine also has been used for the treatment of influenza A virus infection in children. While chemoprophylaxis with the drug should not be considered a substitute for annual vaccination with influenza virus vaccine, antiviral agents are an important adjunct to influenza vaccine for the control and prevention of influenza.

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The most frequently reported adverse effects with amantadine are similar to those observed with rimantadine and include adverse CNS and GI effects; however, amantadine is associated with more frequent and/or severe nervous system effects than rimantadine, including in geriatric adults. Adverse effects associated with amantadine usually are mild and are reversible upon discontinuance of the drug.

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Amantadine hydrochloride is used for symptomatic treatment and for prophylaxis of signs and symptoms of infection caused by various human and animal or avian strains of influenza A virus. While chemoprophylaxis with the drug should not be considered a substitute for annual vaccination with influenza virus vaccine, antiviral agents are critical adjuncts to influenza vaccine for the control and prevention of influenza.

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Administration of amantadine in patients receiving drugs with anticholinergic activity may result in increased adverse anticholinergic and CNS effects. When amantadine is administered to patients already near the limit of tolerance for anticholinergic agents, atropinism with nocturnal confusion and hallucinations may gradually develop. It has been suggested that the dosage of the anticholinergic agent be reduced prior to the initiation of amantadine therapy or that the dose of either drug be reduced if atropine-like adverse effects appear.

Dapsone (Aczone)

The most frequent adverse effects of dapsone are dose-related hemolytic anemia and methemoglobinemia. Hemolysis occurs in most patients receiving 200 mg or more of dapsone daily; however, symptomatic anemia occurs only occasionally. The manufacturer states that the hemoglobin level is generally decreased by 1-2 g/dL, the reticulocyte count is increased 2-12%, erythrocyte life span is shortened, and methemoglobinemia occurs in most patients receiving dapsone. Heinz body formation also occurs frequently.

Dapsone (Aczone): Dosage and Administration

Dapsone is administered orally. For administration to children, commercially available tablets of dapsone have been crushed and dissolved in strawberry syrup; however, studies evaluating bioavailability of the drug following administration of this preparation have not been published to date.

Dapsone (Aczone): Uses

Dapsone is used in rifampin-based multiple-drug regimens for the treatment of multibacillary and paucibacillary leprosy. Although dapsone was used alone in the past for the treatment of leprosy, the World Health Organization (WHO) and most clinicians currently recommend that rifampin-based multiple-drug regimens be used for the treatment of all forms of leprosy. Multiple-drug regimens may reduce infectiousness of the patient more rapidly as well as delay or prevent the emergence of resistant organisms. Rifampin-based regimens are necessary because of the increasing incidence of dapsone-resistant Mycobacterium leprae, and these regimens are designed to be effective against all strains of M. leprae, regardless of their susceptibility to dapsone.

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Clofazimine is administered orally. Clofazimine should be taken with a meal to maximize absorption of the drug. The usual adult dosage of clofazimine for the treatment of leprosy is 50-100 mg once daily. Clofazimine also is given in a dosage regimen that includes 50 mg once daily plus an additional 300-mg dose given once monthly.