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3 Cards in this Set
- Front
- Back
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Maraviroc |
Maraviroc—HIV-1 infection begins with attachment of an HIV envelope protein called gp120 to CD4 molecules on surfaces of helper T cells and other antigen-presenting cells such as macrophages and dendritic cells. The attachment of many HIV strains involves a transmembrane chemokine receptor CCR5. This receptor, a human protein, is the target for maraviroc, which blocks viral attachment. Although resistance has occurred, there is minimal cross-resistance with other antiretroviral drugs. Maraviroc is used orally and has good tissue penetration. It is a substrate for CYP3A4, and dosage adjustments may be needed in the presence of drugs that induce or inhibit this enzyme. Adverse effects of maraviroc include cough, diarrhea, muscle and joint pain, and increases in hepatic transaminases. |
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Enfuvirtide |
Enfuvirtide—Enfuvirtide is a synthetic 36-amino-acid peptide. The drug binds to the gp41 subunit of the viral envelope glycoprotein, preventing the conformational changes required for the fusion of the viral and cellular membranes. There is no cross-resistance with other anti-HIV drugs, but resistance may occur via mutations in the env gene. Enfuvirtide is administered subcutaneously in combination with other anti-HIV agents in previously drug-treated patients with persistent HIV-1 replication despite ongoing therapy. Its metabolism via hydrolysis does notinvolve the cytochrome P450 system. Injection site reactions and hypersensitivity may occur. An increased incidence of bacterial pneumonia has been reported. |
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Integrase Strand Transfer Inhibitors (INSTs) Raltegravir |
Integrase Strand Transfer Inhibitors (INSTs) Raltegravir is a pyrimidine derivative that binds integrase, an enzyme essential to replication of both HIV-1 and HIV-2, inhibiting strand transfer. As a result, integration of reverse-transcribed HIV DNA into host cell chromosomes is inhibited. The drug has been used mainly in treatment-naïve HIV patients, usually in combination regimens. The drug is metabolized by glucuronidation and is not affected by agents that induce or inhibit hepatic cytochromes P450. However, if used with rifampin, which induces UDP-glucuronosyltransferase, the dose of raltegravir should be doubled. Adverse effects include nausea, dizziness, and fatigue. An increase in creatinine kinase has been reported, with potential for myopathy or rhabdomyolysis. Dolutegravir and elvitegravir are similar. |
