Drug information of raltegravir

raltegravir

Drug group:

Raltegravir is an antiviral medicine that prevents human immunodeficiency virus (HIV) from multiplying in your body.

Raltegravir is used to treat HIV, the virus that can cause acquired immunodeficiency syndrome (AIDS). Raltegravir is not a cure for HIV or AIDS.

Raltegravir is for use in adults and children who weigh at least 4.4 pounds (2 kilograms).

Mechanism of effect

Incorporation of viral DNA into the host cell’s genome is required to produce a self-replicating provirus and propagation of infectious virion particles. The viral cDNA strand produced by reverse transcriptase is subsequently processed and inserted into the human genome by the enzyme HIV-1 integrase (encoded by the pol gene of HIV). Raltegravir inhibits the catalytic activity of integrase, thus preventing integration of the proviral gene into human DNA.

Pharmacokinetics

Metabolism

Primarily hepatic glucuronidation mediated by UGT1A1

Absorption

Film-coated tablet (400 mg formulation): AUC increased twofold with high-fat meal; Chewable tablet: AUC decreased by ~6% with high-fat meal (not clinically significant); Oral suspension: The effect of food was not studied

Time to reach the peak

Film-coated tablet (400 mg formulation): ~3 hours; film-coated tablet (600 mg formulation): ~1.5 to 2 hours

Half life

~9 hours

Excretion

Feces (~51%, as unchanged drug); urine (~32%; 9% as unchanged drug)

Drug indications

HIV-1 infection, treatment: Treatment of HIV-1 infection in combination with other antiretroviral agents.

Dosage

Usual Adult Dose for HIV Infection

Therapy-naive patients or patients virologically-suppressed on an initial regimen of film-coated tablets 400 mg twice a day:

-Film-Coated Tablets 600 mg: 1200 mg orally once a day

-Film-Coated Tablets 400 mg: 400 mg orally twice a day

Therapy-experienced patients:

-Film-Coated Tablets 400 mg: 400 mg orally twice a day

Usual Pediatric Dose for HIV Infection

ORAL SUSPENSION:

Full-term neonates (birth to 4 weeks [28 days] of age):

Birth to 1 week:

-Weight 2 to less than 3 kg: 4 mg orally once a day

-Weight 3 to less than 4 kg: 5 mg orally once a day

-Weight 4 to less than 5 kg: 7 mg orally once a day

1 to 4 weeks:

-Weight 2 to less than 3 kg: 8 mg orally twice a day

-Weight 3 to less than 4 kg: 10 mg orally twice a day

-Weight 4 to less than 5 kg: 15 mg orally twice a day

Pediatric patients at least 4 weeks of age:

-Weight 3 to less than 4 kg: 25 mg orally twice a day

-Weight 4 to less than 6 kg: 30 mg orally twice a day

-Weight 6 to less than 8 kg: 40 mg orally twice a day

-Weight 8 to less than 11 kg: 60 mg orally twice a day

-Weight 11 to less than 14 kg: 80 mg orally twice a day

-Weight 14 to less than 20 kg: 100 mg orally twice a day

CHEWABLE TABLETS:

-Weight 11 to less than 14 kg: 75 mg orally twice a day

-Weight 14 to less than 20 kg: 100 mg orally twice a day

-Weight 20 to less than 28 kg: 150 mg orally twice a day

-Weight 28 to less than 40 kg: 200 mg orally twice a day

-Weight at least 40 kg: 300 mg orally twice a day

FILM-COATED TABLETS 400 MG:

-Weight at least 25 kg: 400 mg orally twice a day

FILM-COATED TABLETS 600 MG:

-Weight at least 40 kg and either therapy-naive or virologically-suppressed on an initial regimen of film-coated tablets 400 mg twice a day: 1200 mg orally once a day

Maximum dose:

-Oral suspension: 100 mg twice a day

-Chewable tablets: 300 mg twice a day

Drug contraindications

This drug is not recommended for use in preterm neonates or pediatric patients weighing less than 2 kg.

Side effects

Hepatic: Increased serum ALT (1% to 11%; incidence higher with hepatitis B and/or C coinfection)

Central nervous system: Headache, insomnia, abnormal dreams, nightmares, dizziness, fatigue, depression, suicidal ideation, suicidal tendencies, psychomotor agitation (children and adolescents), abnormal behavior (children and adolescents)

Dermatologic: Allergic rash (children and adolescents: 1%)

Endocrine & metabolic: Increased serum glucose

Gastrointestinal: Increased serum lipase, increased serum amylase, nausea, decreased appetite, diarrhea, flatulence, abdominal pain, dyspepsia, gastritis, vomiting

Genitourinary: Herpes genitalis

Hematologic & oncologic: Decrease in absolute neutrophil count, thrombocytopenia , decreased hemoglobin

Hepatic: Increased serum AST, hyperbilirubinemia, increased serum alkaline phosphatase, hepatitis

Hypersensitivity: Hypersensitivity reaction

Infection: Herpes zoster

Neuromuscular & skeletal: Increased creatine phosphokinase, weakness

Renal: Nephrolithiasis, renal failure, increased serum creatinine

Aluminum Hydroxide, Calcium Carbonate, Etravirine, Fibric Acid Derivatives, Fosamprenavir, HMG-CoA Reductase Inhibitors (Statins), Magnesium Salts, Orlistat, Polyvalent Cation Containing Products, Proton Pump Inhibitors, Rifabutin, RifAMPin, Rifapentine, Tipranavir, Zidovudine

Alerts

1-Raltegravir may cause a severe skin reaction that can be fatal. Stop taking raltegravir and get emergency medical help if you have skin redness or a rash that spreads and causes blistering and peeling.

2-Raltegravir chewable tablets contain phenylalanine. Talk to your doctor before using this form of raltegravir if you have phenylketonuria (PKU).

3-Avoid taking an antacid that contains aluminum or magnesium within 2 hours before or 2 hours after you take raltegravir.

Points of recommendation

1-To make sure raltegravir is safe for you, tell your doctor if you have ever had:

-a muscle disorder

-kidney disease (or if you are on dialysis)

-liver disease

-mental illness or depression

2-You may take raltegravir with or without food.

3-The raltegravir chewable tablet may be chewed or swallowed whole.

Do not crush, chew, or break a regular tablet. Swallow it whole.

4-Raltegravir oral suspension is a powder that must be mixed with water before you take it. Mix 1 packet of this powder with 1 teaspoon (5 milliliters) of water. Measure this mixture with the dosing syringe provided, and give the medicine by mouth within 30 minutes after mixing. Do not save any of the mixed medicine for later use.

5-If a child is using this medicine, tell your doctor if the child has any changes in weight. Raltegravir doses are based on weight in children, and any changes may affect your child's dose.

6-Use raltegravir regularly to get the most benefit. Get your prescription refilled before you run out of medicine completely.

7-This drug plus emtricitabine-tenofovir disoproxil fumarate is recommended as the preferred regimen for HIV postexposure prophylaxis; this drug is also recommended as a component in various alternative regimens.

Storage

-Store at 20C to 25C (68F to 77F); excursions permitted to 15C to 30C (59F to 86F).

-Film-coated and chewable tablets: Store in original package with bottle closed tightly; keep desiccant in bottle to protect from moisture.

-Oral suspension: Store in original container; do not open foil packet until ready for use.

Breast feeding warning

No data are available on presence of raltegravir in human milk, effects on breastfed infant, or on milk production; when administered to lactating rats, raltegravir was present in milk.

Related drugs

Dolutegravir

Drug forms

Isentress, Isentress HD

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