CCR5 Antagonist

Question 1

CCR5 Antagonist prototype

Answer 1

Maraviroc (Decreases viral load, increases active CD4 cells).

Question 2

Maraviroc indications

Answer 2

Combination antiretroviral treatment of adults infected with CCR5-tropic HIV-1 who have evidence of viral replication and HIV-1 strains resistant to multiple antiretroviral agents.

Question 3

Maraviroc actions

Answer 3

Selectively binds to the human chemokine receptor CCR5 on the cell membrane, preventing interaction of HIV-1 and CCR5, which is necessary for the HIV to enter the cell; HIV cannot enter the cell and cannot multiply.

Question 4

Maraviroc route, onset, peak

Answer 4

Oral, slow, 0.5-4 h

Question 5

Maraviroc adverse effects

Answer 5

Dizziness, parasthesia, nausea, vomiting, diarrhea, cough, upper respiratory infection (URI), fever, musculoskeletal symptoms, hepatotoxicity.

Question 6

Maraviroc

Answer 6

• Has a Black Box Warning regarding the risk for hepatotoxicity.
• Patients at increased risk of infections because of the way the drug affects the cell membrane.
• Do not take with St. John’s wort. It lowers antiviral effects.