Maraviroc

Maraviroc is a prescription medication indicated in combination with other antiretroviral agents for the treatment of only CCR5-tropic human immunodeficiency virus type 1 (HIV-1) infection.

• Maraviroc is available under the following different brand names: Selzentry

Common side effects of Maraviroc include:

• stomach pain
• diarrhea
• constipation
• tiredness
• light-headedness or dizziness while standing
• cold symptoms (stuffy nose, sneezing, cough, sore throat)
• sleep problems (insomnia)
• swelling
• urinary problems
• muscle/joint pain or skin rash

Serious side effects of Maraviroc include:

• chest pain
• fever or chills
• swelling in the neck or throat
• numbness or tingling in hands and feet
• fast or irregular heartbeats
• signs of liver damage (such as yellowing of the eye or skin, dark urine, or unusual tiredness)
• loss of movement (anywhere in the body)
• muscle weakness
• pale or blue skin, lips, or fingernails
• shortness of breath
• red, peeling, or blistering skin
• light-colored stool
• unsteadiness while walking
• severe or persistent vomiting

Rare side effects of Maraviroc include:

• none

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, coordination loss, unsteady, very stiff muscles, high fever, profuse sweating, or tremors.
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights.
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out.

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult and pediatric dosage

Tablet

• 25 mg
• 75 mg
• 150 mg (Selzentry, generic)
• 300 mg (Selzentry, generic)

Oral solution

• 20 mg/mL

HIV-1 Infection

Adult dosage

• General dosage recommendations
• Administer orally two times a day
• Must be given in combination with other antiretroviral medications
• Recommended dose differs based on concomitant medications owing to drug interactions
• Noninteracting concomitant medications
  • 300 mg orally two times a day
• Noninteracting drugs include tipranavir/ritonavir, dolutegravir, 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 orally two times a day
• Potent CYP3A inhibitors include protease inhibitors (except tipranavir/ritonavir), elvitegravir/ritonavir, ketoconazole, itraconazole, clarithromycin, cobicistat, nefazodone, and telithromycin
• Potent and moderate CYP3A inducers (without a potent CYP3A inhibitor)
  • 600 mg orally two times a day
• Potent and moderate CYP3A inducers include efavirenz, rifampin, etravirine, carbamazepine, phenobarbital, and phenytoin

Pediatric dosage

• General dosing recommendations
  • Administer orally two times a day
  • Must be given in combination with other antiretroviral medications
  • Recommended dose differs based on concomitant medications owing to drug interactions
• Aged 2 years and older weighing at least 10 kg (tablets)
• Noninteracting concomitant medications
  • 10 kg to less than 14 kg: 150 mg orally two times a day
  • 14 kg to less than 30 kg: 200 mg orally two times a day
  • 30 kg and above: 300 mg orally two times a day
• Noninteracting drugs include: dolutegrative, 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 less than 20 kg: 50 mg orally two times a day
  • 20 kg to less than 30 kg: 75 mg orally two times a day
  • 30 kg to less than 40 kg: 100 mg orally two times a day
  • 40 kg and more: 150 mg orally two times a day
• Potent CYP3A inhibitors include protease inhibitors (except tipranavir/ritonavir), elvitegravir/ritonavir, ketoconazole, itraconazole, clarithromycin, nefazodone, and telithromycin.
• Potent and moderate CYP3A inducers (without a potent CYP3A inhibitor)
• Not recommended for children taking potent CYP3A inducers
• Potent and moderate CYP3A inducers include: efavirenz, rifampin, etravirine, carbamazepine, phenobarbital, and phenytoin
• Pediatric patients weighing at least 2 kg (oral solution)
• Noninteracting concomitant medications
  • 2 kg to less than 3 kg: 30 mg (1.5 mL) orally two times a day
  • 4 kg to less than 6 kg: 40 mg (2 mL) orally two times a day
  • 6 kg to less than 10 kg: 100 mg (5 mL) orally two times a day
  • 10 kg to less than 14 kg: 150 mg (7.5 mL) orally two times a day
  • 14 kg to less than 30 kg: 200 mg (10 mL) orally two times a day
  • 30 kg and more: 300 mg (15 mL) orally two times a day
• Potent CYP3A inhibitors (with or without a potent CYP3A inducer)
  • 2 kg to less than 10 kg: Not recommended
  • 10 kg to less than 20 kg: 50 mg (2.5 mL) orally two times a day
  • 20 kg to less than 30 kg: 80 mg (4 mL) orally two times a day
  • 30 kg to less than 40 kg: 100 mg (5 mL) orally two times a day
  • 40 kg and more: 150 mg (7.5 mL) orally two times a day
• Potent CYP3A inducers (without a potent CYP3A inhibitor)
  • NOT recommended for children taking potent CYP3A inducers
  • Potent and moderate CYP3A inducers include efavirenz, rifampin, etravirine, carbamazepine, phenobarbital, and phenytoin

Dosage Considerations – Should be Given as Follows:

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, healthcare provider, or pharmacist first.

• Maraviroc has severe interactions with the following drugs:
  • elvitegravir/cobicistat/emtricitabine/tenofovir DF
  • St. John's wort
• Maraviroc has serious interactions with at least 24 other drugs.
• Maraviroc has moderate interactions with at least 253 other drugs.
• Maraviroc has minor interactions with at least 29 other drugs.

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all the products you use. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, health questions, or concerns.

Contraindications

• Hypersensitivity
• Severe renal impairment or end-stage renal disease (CrCl below 30 mL/min) in patients taking potent CYP3A4 inhibitors or inducers

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Maraviroc?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Maraviroc?”

Cautions

• Risk for hepatotoxicity
• Risk for immune reconstitution syndrome if used in combination with other antiretroviral drugs
• Autoimmune disorders (eg, Graves’ disease, polymyositis, Guillain-Barré syndrome) are 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-naive patients; compared with efavirenz, maraviroc is more likely to cause virologic failure and lamivudine resistance in treatment-naïve patients
• Tropism testing with a highly sensitive tropism assay is required for appropriate use
• Evaluate if signs/symptoms of hepatitis, increased LFTs, or rash develop
• Preexisting liver dysfunction or viral hepatitis B or C coinfection
• Patient history of increased risk for cardiovascular events
• History of postural hypotension or concomitant use of blood pressure-lowering medications
• Use caution in patients with renal and hepatic impairment; postural hypotension reported in patients with renal impairment
• Monitor for developing infections
  • When administering to patients with preexisting liver dysfunction or viral hepatitis B or C coinfection, additional monitoring may be warranted
  • In case of cardiovascular adverse events triggered by postural hypotension, additional monitoring may be warranted
  • The Antiretroviral Pregnancy Registry (APR) has been established.to monitor maternal-fetal outcomes of pregnant women; register patients by calling 1-800-258-4263
• Drug interaction overview
  • Maraviroc is metabolized by CYP3A and is also a substrate of 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 as well as by inhibitors of OATP1B1 and MRP2; therefore, dosage adjustment may be required when Maraviroc is coadministered with those drugs

Pregnancy and Lactation

• Data on the use of maraviroc during pregnancy from the APR and case reports are not sufficient to inform a drug-associated risk for birth defects and miscarriage; in animal reproduction studies, no evidence of adverse developmental outcomes was observed with Maraviroc
• Lactation 
  • The CDC recommends that HIV-1-infected mothers in the US should not breastfeed their infants to avoid risking postnatal transmission of HIV-1 infection
  • There are no data on the presence of Maraviroc in human milk and its effects on breastfed infants or milk production; when administered to lactating rats, maraviroc was found to be present in milk; because of the potential for HIV transmission (in HIV-negative infants), development of viral resistance (in HIV-positive infants), and serious adverse reactions in a breastfed infant similar to those seen in adults, instruct mothers not to breastfeed if they are receiving therapy