Maraviroc
Indications
Maraviroc is used for:
HIV infection, Allogeneic bone marrow transplantation
Adult Dose
HIV-1 Infection
Indicated for combination antiretroviral treatment of CCR5-tropic HIV-1 in patients who have viral replication and HIV-1 strains resistant to multiple antiretroviral agents
With NRTIs, tipranavir/ritonavir, nevirapine, raltegravir, and other drugs that are not potent CYP3A inhibitors or CYP3A4 inducers: 300 mg PO q12hr
Coadministration with strong CYP3A4 inhibitors (with or without potent CYP3A4 inducers): 150 mg PO q12hr
Coadministration with CYP3A inducers including efavirenz (without a strong CYP3A inhibitor): 600 mg PO q12hr
Hepatic Impairment
Mild to moderate impairment: Maraviroc concentrations increased but dose adjustment not recommended; monitor
Moderate impairment and strong CYP 3A4 inhibitor: Use caution; monitor closely for adverse reactions
Severe impairment: Not studied
Child Dose
HIV-1 Infection
<16 years: Safety and efficacy not established
>16 years: As in adults; indicated for combination antiretroviral treatment of CCR5-tropic HIV-1 in patients who have viral replication and HIV-1 strains resistant to multiple antiretroviral agents
With NRTIs, tipranavir/ritonavir, nevirapine, raltegravir, and other drugs that are not potent CYP3A4 inhibitors or CYP3A4 inducers: 300 mg PO q12hr
Coadministration with strong CYP3A4 inhibitors (with or without potent CYP3A4 inducers): 150 mg PO q12hr
Coadministration with CYP3A4 inducers including efavirenz (without a strong CYP3A4 inhibitor): 600 mg PO q12hr
Renal Dose
Renal Impairment
CrCl <30 mL/min or hemodialysis
Experiencing postural hypotension: 150 mg PO q12hr
Concomitantly administraiton with NRTIs and other medications but without concomitant CYP3A inducers or inhibitors: 300 mg PO q12hr; if postural hypotension occurs, reduce dose to 150 mg q12hr
With potent CYP3A inducers or inhibitors: Not recommended
CrCl>30 mL/min
Concomitant administration with potent CYP 3A4 inhibitors with or without a CYP3A4 inducer: 150 mg PO q12hr
With potent CYP3A4 inducer without CYP3A4 inhibitor: 600 mg PO q12hr
With NRTIs and other medications but without concomitant CYP3A inducers or inhibitors: 300 mg PO q12hr
Administration
May be taken with or without food.
Contra Indications
Patients with severe renal impairment or end-stage renal disease (ESRD) (CrCl < 30 mL/min) who are taking potent CYP3A inhibitors or inducers.
Precautions
Hepatotoxicity
Cardiovascular Events
Immune Reconstitution Syndrome
Potential Risk of Infection
Potential Risk of Malignancy
Lactation: breastfeeding not recommended in HIV+ mothers
Pregnancy-Lactation
Interactions
Increased or decreased conc w/ CYP3A inhibitors &/or inducers, respectively. Increased metabolic ratio of debrisoquine. Increased conc w/ elvitegravir/ritonavir, delavirdine, boceprevir, telaprevir, HIV PIs (except tipranavir/ritonavir), NNRTI + PI, rifabutin + PI, clarithromycin, telithromycin, ketoconazole, itraconazole. Decreased conc w/ efavirenz, etravirine, rifampicin, St. John's wort.
Adverse Effects
Side effects of Maraviroc :
>10%
Upper respiratory infections (20%),Arthritis and musculoskeletal S/S (15%),Cough (13%),Pyrexia (12%),Rash (11%),Fever (13%)
2-10%
Dizziness (9%),Appetite disorder (8%),Herpes infection (8%),Bronchitis (7%),Sinusitis (7%),Constipation (6%),Apocrine and eccrine gland disorder (5%),Paresthesia/dysesthesia (5%),Renal/urinary disorder (3-5%),Depression (4%),Disturbed consciousness (4%),Periph neuropathies (4%),Pruritus (4%),Sensory abnormalities (4%),Folliculitis (3%),Hypertension (3%),Lipodystrophy (3%),Muscle pain (3%),Influenza (2%),Pneumonia (2%),Condyloma acuminata,Dermatitis/eczema,Dyspepsia,GI pain,Stomatitis/ulceration
Mechanism of Action
Selective antagonist of the interaction between human CCR5 and HIV-1 gp120; blocking this interaction prevents CCR5-tropic HIV-1 entry into cells.