Maraviroc

Trade Names:
Selzentry
- Tablets 150 mg, 300 mg

Pharmacology

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Selectively binds to CCR5 present on the cell membrane, preventing CCR5-tropic HIV-1 to enter cells.

Pharmacokinetics

Absorption

After oral dosing, C _max attained in 0.5 to 4 h. Bioavailability is 23% at a 100 mg dose and 33% at a 300 mg dose. Maraviroc is a substrate for the efflux transporter P-glycoprotein.

Distribution

Approximately 76% bound to human plasma protein and shows moderate affinity for albumin and alpha-1 acid glycoprotein. Vd is approximately 194 L.

Metabolism

Primarily metabolized by CYP3A to inactive metabolites.

Elimination

Terminal t _½ is 14 to 18 h. Elimination is approximately 76% and 20% in the feces and urine, respectively, over 168 h. Maraviroc is the major component excreted and the remainder are metabolites.

Special Populations

Not sufficiently studied; however, renal Cl accounts for approximately 25% of total Cl.

Not sufficiently studied; however, maraviroc is metabolized by the liver.

Does not affect concentrations.

Dosage adjustment based on race is not needed.

Indications and Usage

In combination with other antiretroviral agents for treatment-experienced patients infected with only CCR5-tropic HIV-1 detectable, who have evidence of HIV-1 replication despite ongoing antiretroviral therapy.

Contraindications

None.

Dosage and Administration

PO 150 mg twice daily.

PO 300 mg twice daily.

PO 600 mg twice daily.

General Advice

• May be taken without regard to food.
• Must be taken in combination with other antiretroviral agents.

Storage/Stability

Store at 59° to 86°F.

Drug Interactions

Maraviroc concentrations may be reduced. Determine dosage selection based on concurrent medications.

Maraviroc concentrations may be elevated. Determine dosage selection based on concurrent medications.

Maraviroc concentrations may be altered. Determine dosage selection based on concurrent medications.

Coadministration is not recommended. Maraviroc concentrations may be reduced, which may result in suboptimal levels of maraviroc and lead to loss of virologic response and possible resistance.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Vascular hypotension disorders (3%); acute cardiac failure, coronary artery disease and occlusion, MI, myocardial ischemia, unstable angina (less than 2%).

CNS

Dizziness/postural dizziness (8%); disturbances in initiating and maintaining sleep (7%); paresthesias and dysesthesias (5%); depressive disorders, disturbances in consciousness, sensory abnormalities (4%); peripheral nephropathies (3%); cerebrovascular accident (less than 2%).

Dermatologic

Rash (10%); apocrine and eccrine gland disorders (5%); pruritus (4%); benign skin neoplasms, dermatitis and eczema, lipodystrophies (3%); squamous cell carcinoma of skin (less than 2%).

GI

GI and abdominal pain (8%); constipation (5%); dyspeptic signs and symptoms, stomatitis, ulceration (3%); anal cancer, esophageal carcinoma, tongue neoplasm (less than 2%).

Genitourinary

Bladder and urethral symptoms (5%); urinary tract signs and symptoms (3%).

Hepatic

Cholestatic jaundice, hepatic cirrhosis or failure, metastases to liver (less than 2%).

Hematologic-Lymphatic

Increased blood CK (less than 2%).

Lab Tests

Elevated amylase or total bilirubin (6%); elevated AST or lipase (5%); decreased absolute neutrophil count (4%); elevated ALT (2%).

Metabolic-Nutritional

Appetite disorders (7%).

Musculoskeletal

Musculoskeletal and connective tissue signs and symptoms (9%); joint-related signs and symptoms (6%); muscle pains (3%); myositis, osteonecrosis, rhabdomyolysis (less than 2%).

Respiratory

Upper respiratory tract infection (20%); coughing and associated symptoms (13%); bronchitis, sinusitis (6%); breathing abnormalities (3%); bronchospasm and obstruction, paranasal sinus disorders, pneumonia, respiratory tract disorders (2%).

Miscellaneous

Pyrexia (12%); herpes infection (7%); pain and discomfort (4%); folliculitis (3%); condyloma acuminatum, influenza (2%); abdominal neoplasm, basal cell carcinoma, Bowen disease, cholangiocarcinoma, Clostridium difficile colitis, lymphoma, septic shock, viral meningitis (less than 2%).

Precautions

Pregnancy

Category B .

Lactation

Undetermined; however, HIV-infected mothers should not breast-feed in order to avoid risking potential transmission of HIV to infant.

Children

Safety and efficacy not established in patients younger than 16 years of age.

Elderly

Use with caution because of the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant diseases or other drug therapy.

Renal Function

Use with caution; patients with a CrCl of less than 50 mL/min should receive maraviroc and a CYP3A inhibitor only if the potential benefit outweighs the risk.

Cardiovascular

Use with caution in patients at increased risk of CV event and in patients with history of postural hypotension or receiving medication known to lower BP.

Immune reconstitution syndrome

Has been reported; during initial phase of combination antiretroviral treatment, patients whose immune system responds may develop an inflammatory response to indolent or residual opportunistic infections (eg, Mycobacterium avium , cytomegalovirus, Mycobacterium tuberculosis ) and may require additional evaluation and treatment.

Infection

Because the CCR5 coreceptor located on some immune cells is antagonized, there can be an increased risk of developing infections.

Malignancy

May increase risk of malignancy.

Overdosage

Symptoms

Postural hypotension.

Patient Information

• Advise patient to read the Medication Guide before using product the first time and with each refill.
• Advise patients to stop treatment and seek immediate medical attention if they develop signs or symptoms of hepatitis or allergic reaction.
• Inform patients that treatment is not a cure for HIV infection and that they may still develop illnesses associated with HIV infection, including opportunistic infections.
• Inform patient that treatment does not reduce risk of transmission of HIV to others through sexual contact, sharing needles, or blood contamination.
• Advise patient that it is important to remain under the care of a health care provider.
• Advise patient to take the medication every day as prescribed and in combination with other antiretroviral drugs.
• Instruct patient to take exactly as prescribed and not to change the dose or discontinue therapy unless advised by health care provider.
• Advise patient that if a dose is missed to take the next dose as soon as possible and then take the next scheduled dose at its regular time. If it is less than 6 hours before the next schedule dose, they should not take the missed dose and should instead wait and take the next dose at the regular time.
• Advise patients that if they experience dizziness while taking the medication, they should avoid driving or operating machinery.

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