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Brand Name :
Isentress, Isentress HD
Synonyms :
raltegravir
Class :
Integrase Inhibitor (Anti-HIV), Antiretroviral
Brand Name :
Isentress, Isentress HD
Synonyms :
raltegravir
Class :
Integrase Inhibitor (Anti-HIV), Antiretroviral
Dosage Forms & StrengthsÂ
TabletÂ
400mgÂ
600mg Â
Chewable tabletÂ
25mgÂ
100mgÂ
If a patient has HIV RNA >100,000 copies/mL and a CD4 count <200 cells/mm3, they should not take raltegravir with darunavir and ritonavir. They should also avoid using raltegravir when used with abacavir and lamivudine.
Patients new to treatment:
Administer 400mg of Isentress tablets orally twice a day.
Note: Patients who first took raltegravir 400 mg twice a day and were virologically suppressed may change to taking Isentress HD once daily
Administer 1.2g daily once or 600mg Isentress HD twice daily
Note: Once-daily dose is not advised during pregnancy.
Patients with a prior medical history
Administer 400mg of Isentress tablets orally twice a day.
Non-occupational post-exposure prevention for HIV-1
Administer 400 mg twice daily for 28 days along with other antiretroviral medications. Begin treatment within 72 hours after exposure.
Occupational HIV-1 postexposure prophylaxis
Dosage modification for concurrent therapy: Serious medication interactions exist, necessitating dose/frequency modification or avoidance.
Dosage Forms & StrengthsÂ
TabletÂ
400mgÂ
600mg Â
Chewable tabletÂ
25mgÂ
100mgÂ
Oral suspension (10 mg/mL):
Infants and Children weighing <20 kg:
Administer 6 mg/kg/dose orally twice a day. Do not exceed 100 mg/dose
Fixed dosing:
3 to <4 kg: Administer 25 mg orally twice a day.
4 to <6 kg: Administer 30 mg orally twice a day.
6 to <8 kg: Administer 40 mg orally twice a day.
8 to <11 kg: Administer 60 mg orally twice a day.
11 to <14 kg: Administer 80 mg orally twice a day.
14 to <20 kg: Administer 100 mg orally twice a day.
Chewable tablets
Children, Adolescents, and Infants weighing ≥3 kg:
Administer 6 mg/kg/dose orally twice a day. Do not exceed 300 mg/dose.
3 to <6 kg: Administer 25 mg orally twice a day.
6 to <10 kg: Administer 50 mg orally twice a day.
10 to <14 kg: Administer 75 mg orally twice a day.
14 to <20 kg: Administer 100 mg orally twice a day.
20 to <28 kg: Administer 150 mg orally twice a day.
28 to <40 kg: Administer 200 mg orally twice a day.
≥40 kg: Administer 300 mg orally twice a day.
Film-coated tablets
Isentress: Children and Adolescents ≥25 kg: Administer 400 mg orally twice daily.
Isentress HD: Children and Adolescents ≥40 kg:
Administer 1200 mg orally once a day.
Treatment-naive individuals should follow a different regimen than those who have been virologically suppressed by raltegravir 400 mg twice daily.
Non-occupational post-exposure prevention for HIV-1
Children <2 years and Infants:
Administer 6mg/kg/dose twice a day orally
Children >2 years:
11 to <14 kg: Administer 75 mg twice a day.
14 to <20 kg: Administer 100 mg twice a day.
20 to <28 kg: Administer 150 mg twice a day.
28 to <40 kg: Administer 200 mg twice a day.
≥40 kg: Administer 300 mg twice a day.
Film-coated tablets
Isentress: Children > 6 years weighing ≥25 kg: Administer 400 mg orally twice a day.
Refer to adult dosing
may diminishes the serum concentration of each other when combined
may diminish the serum concentration of each other when combined
may decrease the therapeutic effect when combined
may diminish the serum concentration when combined with raltegravir
may diminish the serum concentration when combined with raltegravir
may diminish the serum concentration when combined with raltegravir
may diminish the serum concentration when combined with raltegravir
may diminish the serum concentration when combined with raltegravir
may diminish the serum concentration of each other when combined
may decrease the therapeutic effect of Antiretroviral Agents
may diminish the serum concentration of each other when combined
may diminish the serum concentration of each other when combined
may diminish the serum concentration of each other when combined
may diminish the serum concentration of each other when combined
may diminish the serum concentration of each other when combined
may diminish the serum concentration of magnesium salts
may diminish the serum concentration of magnesium salts
aluminum hydroxide/magnesium hydroxideÂ
may decrease the serum concentration of aluminum hydroxide
may diminish the serum concentration of each other when combined
antiretroviral agents undergo intracellular phosphorylation that will reduce the efficacy of cladribine
may diminish the serum concentration of each other when combined
may increase the myopathic effect of Fibric Acid Derivatives
may increase the myopathic effect of Fibric Acid Derivatives
may increase the myopathic effect of Fibric Acid Derivatives
may increase the myopathic effect of Fibric Acid Derivatives
may increase the myopathic effect of Fibric Acid Derivatives
may increase the myopathic effect of HMG-CoA Reductase Inhibitors
may increase the myopathic effect of HMG-CoA Reductase Inhibitors
may increase the myopathic effect of HMG-CoA Reductase Inhibitors
may increase the myopathic effect of HMG-CoA Reductase Inhibitors
may increase the myopathic effect of HMG-CoA Reductase Inhibitors
may diminish the serum concentration of each other when combined
may diminish the serum concentration of each other when combined
may diminish the serum concentration of each other when combined
may diminish the serum concentration of each other when combined
may diminish the serum concentration of each other when combined
may increase the myopathic effect of each other when combined
may diminish the serum concentration of each other when combined
May decrease the serum concentration of raltegravir, avoid coadministration
may intensify the potentially negative effects of HMG-CoA Reductase Inhibitors
it decreases the concentration of antiretroviral agent in the serum
may increase the myopathic effect of HMG-CoA Reductase Inhibitors
Actions and Spectrum:Â
Frequency definedÂ
>10%Â
Increased serum alanine aminotransferaseÂ
1-10%Â
Increase in fasting plasma glucoseÂ
Decreased appetiteÂ
Genital herpes simplexÂ
HepatitisÂ
Herpes zoster infectionÂ
Abnormal dreamsÂ
Increased serum creatinineÂ
<1%Â
Abnormal behaviour Â
Frequency not definedÂ
Increased HDL cholesterolÂ
Malignant neoplasmÂ
Skin rashÂ
Black box warning:Â
NoneÂ
Contraindications/caution:Â
Contraindications:Â
NoneÂ
Caution:Â
Pregnancy consideration: It may be used during pregnancy if the potential benefits outweigh the risks.Â
Lactation: Excretion of the drug in human breast milk is knownÂ
Pregnancy category:Â
Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.Â
Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.Â
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.   Â
Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.   Â
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.   Â
Category N: There is no data available for the drug under this categoryÂ
Pharmacology:Â
It is an antiretroviral medication used for the treatment of HIV-1 infection. As an integrase strand transfer inhibitor (INSTI), it specifically targets the integrase enzyme of the human immunodeficiency virus (HIV), interfering with the viral replication process.Â
Pharmacodynamics:Â Â
The primary pharmacodynamic effect of raltegravir is its potent antiviral activity against HIV-1. By inhibiting integrase, the drug effectively reduces the viral load (the amount of HIV in the blood) and slows the progression of HIV infection. Suppression of viral replication is essential for improving immune function, reducing the risk of opportunistic infections, and ultimately improving the quality and length of life in people with HIV. Â
Pharmacokinetics:Â
AbsorptionÂ
raltegravir is administered orally, and it is well-absorbed from the gastrointestinal tract. However, its absorption is influenced by food intake. Taking raltegravir with food can increase its bioavailability, so taking it with a meal is generally recommended. Â
DistributionÂ
After absorption, raltegravir is distributed throughout the body, including tissues and organs. It reaches the site of action, HIV replication in immune cells (CD4+ T-lymphocytes), where it exerts its antiviral effects by inhibiting the integrase enzyme.Â
MetabolismÂ
raltegravir undergoes metabolism primarily in the liver. The main metabolic pathway involves glucuronidation, where raltegravir is conjugated with glucuronic acid to form an inactive glucuronide metabolite. The enzyme responsible for this glucuronidation process is UDP-glucuronosyltransferase 1A1 (UGT1A1).Â
Elimination and ExcretionÂ
The metabolites of raltegravir and any unmetabolized drug are primarily eliminated through the feces (51%) and urine (32%). Renal excretion is a significant route of elimination for raltegravir and its metabolites.Â
Administration:Â
Oral administrationÂ
Can be given without consideration to food.Â
Chewable tabletsÂ
The chewable 100 mg tablet can be cut into equal halves or chewed before being consumed whole.Â
Patient information leafletÂ
Generic Name: raltegravirÂ
Why do we use raltegravir?Â
raltegravir is primarily used to treat HIV-1 infection and other antiretroviral medications. It belongs to the class of drugs known as integrase strand transfer inhibitors (INSTIs), and its main use is as a potent antiretroviral agent to suppress HIV replication. Here are the main uses of raltegravir:Â
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