Drug information of Maraviroc

Maraviroc

Drug group:

Maraviroc  is a chemokine receptor antagonist drug that is designed to act against HIV by interfering with the interaction between HIV and CCR5.

Mechanism of effect

Maraviroc is an entry inhibitor and works by blocking HIV from entering human cells. Specifically maraviroc is a selective, slowly reversible, small molecule antagonist of the interaction between human CCR5 and HIV-1 gp120. Maraviroc selectively binds to the human chemokine receptor CCR5 present on the membrane of CD4 cells (T-cells), preventing the interaction of HIV-1 gp120 and CCR5 necessary for CCR5-tropic HIV-1 to enter cells.

Pharmacodynamic

Maraviroc act against HIV by interfering with the interaction between HIV and CCR5.

Pharmacokinetics

Bioavailability: 23-33%

Peak plasma time: 0.5-4 hr

Peak plasma concentration: 333 ng/mL (330 mg BID)

Protein bound: 76%

Vd: 194 L

Metabolism: Metabolized by cytochrome P450 system, with CYP3A as major enzyme of metabolism

Half-life: 14-18 hr        

Excretion: 76% (feces); 20% (urine)

Dosage

Adult

HIV-1 Infection

Noninteracting concomitant medications

  • 300 mg PO BID
  • Noninteracting drugs include: tipranavir/ritonavir, nevirapine, raltegravir, all NRTIs, and enfuvirtide
  • Also, all other medications that are not potent CYP3A inhibitors or inducers

Potent CYP3A inhibitors (with or without a potent CYP3A inducer)

  • 150 mg PO BID
  • Potent CYP3A inhibitors include: protease inhibitors (except tipranavir/ritonavir), delavirdine, elvitegravir/ritonavir, ketoconazole, itraconazole, clarithromycin, and other potent CYP3A inhibitors (eg, nefazodone, telithromycin)

Potent CYP3A inducers (without a potent CYP3A inhibitor)

  • 600 mg PO BID
  • Potent CYP3A inducers include: efavirenz, rifampin, etravirine, carbamazepine, phenobarbital, and phenytoin

Pediatric

HIV-1 Infection

<2 years: Safety and efficacy not established

≥16 years: As in adults

Noninteracting concomitant medications

  • <30 kg: Not recommended
  • ≥30 kg: 300 mg PO BID
  • Noninteracting drugs include: tipranavir/ritonavir, nevirapine, raltegravir, all NRTIs, and enfuvirtide
  • Also, all other medications that are not potent CYP3A inhibitors or inducers

Potent CYP3A inhibitors (with or without a potent CYP3A inducer)

  • 10 kg to <20 kg: 50 mg PO BID
  • 20 kg to <30 kg: 75 mg (tablet) or 80 mg (oral solution) PO BID
  • 30 kg to <40 kg: 100 mg PO BID
  • ≥40 kg: 150 mg PO BID
  • Potent CYP3A inhibitors include: protease inhibitors (except tipranavir/ritonavir), delavirdine, elvitegravir/ritonavir, ketoconazole, itraconazole, clarithromycin, and other potent CYP3A inhibitors (eg, nefazodone, telithromycin)

Potent CYP3A inducers (without a potent CYP3A inhibitor)

  • Maraviroc is NOT recommended for children taking potent CYP3A inducers
  • Potent CYP3A inducers include: efavirenz, rifampin, etravirine, carbamazepine, phenobarbital, and phenytoin

Drug contraindications

Severe Renal Impairment , Hypersensitivity

Alerts

Risk of immune reconstitution syndrome if used in combination with other antiretroviral drugs

Autoimmune disorders (eg, Graves’ disease, polymyositis, Guillain-Barré syndrome) reported in the setting of immune reconstitution, however, the time to onset is more variable, and can occur many months after initiation of treatment

Do not use in treatment-naïve patients; more likely to experienced virologic failure and developed lamivudine resistance compared to efavirenz

Tropism testing with a highly sensitive tropism assay is required for the appropriate use

Evaluate if signs/symptoms of hepatitis, increase LFTs, or rash develop

Patient history of increased risk for cardiovascular events

History of postural hypotension or concomitant use of blood pressure lowering medication

Caution in renal and hepatic impairment; postural hypotension reported in patients with renal impairment

Monitor for developing infections

When administering to patients with pre-existing liver dysfunction or who are co-infected with hepatitis B and/or C virus, additional monitoring may be warranted

Cardiovascular adverse events triggered by postural hypotension’ additional monitoring may be warranted

Drug interaction overview

  • Drug is metabolized by CYP3A, and is also a substrate for P-glycoprotein (P-gp), organic anion-transporting polypeptide (OATP)1B1, and multidrug resistance-associated protein (MRP)2; pharmacokinetics of maraviroc are likely to be modulated by inhibitors and inducers of CYP3A and P-gp, and may be modulated by inhibitors of OATP1B1 and MRP2; therefore, dosage adjustment may be required when maraviroc is coadministered with those drugs

Black Box Warnings

Hepatotoxicity reported; may be preceded by systemic allergic reaction (eg, pruritic rash, eosinophilia, elevated IgE)

Immediately evaluate if signs or symptoms of hepatitis or allergic reaction occur

Points of recommendation

  • Tell all of your health care providers that you take this medicine (maraviroc tablets). This includes your doctors, nurses, pharmacists, and dentists.
  • Avoid driving and doing other tasks or actions that call for you to be alert until you see how this medicine (maraviroc tablets) affects you.
  • To lower the chance of feeling dizzy or passing out, rise slowly if you have been sitting or lying down. Be careful going up and down stairs.
  • Do not run out of this medicine (maraviroc tablets).
  • Have blood work checked as you have been told by the doctor. Talk with the doctor.
  • This medicine interacts with many other drugs. The chance of side effects may be raised or how well this medicine (maraviroc tablets) works may be lowered. Check with your doctor and pharmacist to make sure that it is safe for you to take this medicine (maraviroc tablets) with all of your other drugs (prescription or OTC, natural products, vitamins).
  • This medicine is not a cure for HIV. Stay under the care of your doctor.
  • This medicine does not stop the spread of diseases like HIV or hepatitis that are passed through blood or having sex. Do not have any kind of sex without using a latex or polyurethane condom. Do not share needles or other things like toothbrushes or razors. Talk with your doctor.
  • A very bad and sometimes deadly reaction has happened with this medicine (maraviroc tablets). Most of the time, this reaction has signs like fever, rash, or swollen glands with problems in body organs like the liver, kidney, blood, heart, muscles and joints, or lungs. Talk with the doctor.
  • Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using this medicine (maraviroc tablets) while you are pregnant.

Children:

  • If giving to your child, the dose of this medicine (maraviroc tablets) may need to be changed as your child's weight changes. Have your child's weight checked often. Talk with the doctor before changing your child's dose.
  • Take with or without food.
  • It is important that you do not miss or skip a dose of this medicine (maraviroc tablets) during treatment.
  • Keep taking this medicine (maraviroc tablets) as you have been told by your doctor or other health care provider, even if you feel well.
  • Swallow whole. Do not chew, break, or crush.
  • Take a missed dose as soon as you think about it.
  • If it is close to the time for your next dose, skip the missed dose and go back to your normal time.
  • Do not take 2 doses at the same time or extra doses.
  • If you are not sure what to do if you miss a dose, call your doctor.

Pregnancy level

B


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