II. Indications
- HIV Infection in either Antiretroviral naive or experienced patients (combination therapy)
III. Contraindications
- Creatinine Clearance <30 ml/min and use of a strong CYP3A4 inhibitor or inducer
IV. Mechanism
V. Medications: Maraviroc
- Tabs: 25, 75, 150 and 300 mg
- Solution: 20 mg/ml
VI. Dosing: Adult
- Strong CYP3A4 Inhibitors (e.g. Clarithromycin, Itraconazole, most HIV Protease Inhibitors except Tipranavir/r)
- Take 150 mg orally twice daily
- Avoid if Creatinine Clearance <30 ml/min
- Insignificant CYP3A4 Effects (e.g. nRTIs, Nevirapine, Raltegravir, Tipranavir/r)
- Take 300 mg orally twice daily
- Strong CYP3A4 Inducers (e.g. Carbamazepine, Efavirenz, Etravirine, Phenobarbital, Phenytoin, Rifampin)
- Take 600 mg orally twice daily
- Avoid if Creatinine Clearance <30 ml/min
VII. Dosing: Child (age >2 years, weight >=10 kg)
- Strong CYP3A4 Inhibitors (e.g. Clarithromycin, Itraconazole, most HIV Protease Inhibitors except Tipranavir/r)
- Weight 10 to 20 kg: Give 50 mg orally twice daily
- Weight 20 to 30 kg: Give 75 mg orally twice daily
- Weight 30 to 40 kg: Give 100 mg orally twice daily
- Weight >40 kg: Give 150 mg orally twice daily (adult dose)
- Avoid if Creatinine Clearance <30 ml/min
- Insignificant CYP3A4 Effects (e.g. nRTIs, Nevirapine, Raltegravir, Tipranavir/r)
- Weight >=30 kg: Give 300 mg orally twice daily (adult dose)
- Strong CYP3A4 Inducers (e.g. Carbamazepine, Efavirenz, Etravirine, Phenobarbital, Phenytoin, Rifampin)
- Avoid Maraviroc in children with concurrent use of strong CYP3A4 inducers
VIII. Adverse Effects
- Well tolerated overall
- Fever
- Upper respiratory symptoms (e.g. cough, Bronchitis)
- Abdominal Pain
-
Orthostatic Hypotension
- More common with Renal Insufficiency
- Myalgia
- Increased Myocardial Infarction risk
-
Hypersensitivity Rash
- DRESS Syndrome risk (rash and Eosinophilia)
- May be associated with hepatoxicity
- Stop Maraviroc immediately for signs of Hypersensitivity
- Hepatotoxicity
- Higher risk if comorbid Hepatitis B or Hepatitis CVirus infection
- Comorbid hepatic Impairment (esp. with strong CYP3A4 Inhibitor use) also increases other adverse effects
- May be associated with DRESS Syndrome
- Liver Function Tests baseline and periodically
- Stop Maraviroc immediately for signs of hepatotoxicity
IX. Drug Interactions
- Maraviroc is a substrate of CYP3A4 and very sensitive to the enzyme's activity (see dosing above)
- Contraindicated agents with Maraviroc
- Unboosted Fosamprenavir
- St Johns Wort
X. Resources
XI. References
- (2007) Presc Lett, New Drug: Maraviroc, Resource #230904
- (2009) Treat Guidel Med Lett 7(78): 11-22 [PubMed]
- Reust (2011) Am Fam Physician 83(12): 1443-51 [PubMed]
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Related Studies
selzentry (on 1/1/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
SELZENTRY 150 MG TABLET | $26.39 each | |
SELZENTRY 300 MG TABLET | $26.46 each |
Ontology: HIV Entry Inhibitors (C1449715)
Concepts | Pharmacologic Substance (T121) |
MSH | D023581 |
English | HIV ENTRY INHIB, Entry Inhibitors, HIV, HIV Entry Inhibitors |
Portuguese | Inibidores da Entrada do HIV |
Spanish | Inhibidores de Entrada del VIH |
French | Inhibiteurs d'entrée du VIH |
German | HIV-Eintrittsinhibitoren |
Ontology: maraviroc (C1667052)
Definition (NCI) | A C-C Chemokine Receptor Type 5 (CCR5) antagonist with activity against human immunodeficiency virus (HIV). Maraviroc inhibits HIV-1 entry via CCR5 coreceptor interaction. |
Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
MSH | C502411 |
SnomedCT | 429603001, 427805000 |
English | Maraviroc, Maraviroc (substance), Maraviroc (product), maraviroc, maraviroc (medication), maraviroc [Chemical/Ingredient], MARAVIROC, 4,4-difluoro-N-((1S)-3-(exo-3-(3-isopropyl-5-methyl-4H-1,2,4-triazol-4-yl)-8-azabicyclo(3.2.1)oct-8-yl)-1-phenylpropyl)cyclohexanecarboxamide |
Spanish | maraviroc, maraviroc (sustancia), maraviroc (producto) |
Ontology: Selzentry (C1964465)
Concepts | Pharmacologic Substance (T121) , Organic Chemical (T109) |
MSH | C502411 |
English | Selzentry, Pfizer Brand of maraviroc |
Ontology: CCR5 Receptor Antagonists (C3850102)
Definition (MSH) | Compounds and drugs that inhibit or block the activity of CCR5 RECEPTORS. |
Concepts | Pharmacologic Substance (T121) |
MSH | D065100 |
English | CCR5 Receptor Antagonists, Chemokine Co-receptor 5 Antagonists, CCR5 Receptor Blockers, Antagonists, CCR5 Receptor, CC Chemokine Receptor 5 Blockers, HIV-1 Fusion Coreceptor Antagonists, HIV 1 Fusion Coreceptor Antagonists, Receptor Blockers, CCR5, Chemokine Co receptor 5 Antagonists, Receptor Antagonists, CCR5, CC Chemokine Receptor 5 Antagonists, Blockers, CCR5 Receptor |