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Drug profile of Isentress

Isentress tablets are therapeutically classified as anti-retroviral medicine by containing an active ingredient known as Raltegravir which is effective against HIV infection.

Raltegravir is chemically categorized as derivative of pyrrolidinone.

Isentress tablets are pharmacologically classified as an integrase inhibitor.

Isentress may used in combination with other anti-retroviral drugs for producing beneficial activity.

Isentress tablets are prescription medicine, which is used only under supervision of medical practitioner.

Raltegravir is a small molecule, containing anti-HIV activity.

Raltegravir is involved in major step in viral production like,

Integration process interfered by Raltegravir, by obstructing the integration of viral genome into host DNA, which is a critical step in HIV pathogenesis.

Brand name: Isentress

Active substance: Raltegravir         

Strength: 400mg

Pack: 60 tablets in a container

Mfg: MSD

Category: Anti-retroviral drug


Prescribing information of Isentress

Isentress tablets are used for treating HIV-1 infection by combining with other anti-retroviral medicines.

Thus the evidence is based on examining the plasma HIV-1 RNA levels.

In pediatric patients with the age of 2 years or older and weight of at least 10kg, the Isentress tablets should be used.

The potency of Isentress in pediatric patients with less than 2 years of age has not been evaluated.

The indication of Isentress is based on assessment of safety, tolerability, pharmacokinetic parameters & efficacy of Raltegravir.

Mechanism of Isentress

Isentress containing Raltegravir aimed the integrase which is an enzyme that incorporates the viral genetic material into human chromosome, a critical step in HIV pathogenesis.


The absorption of Raltegravir is occurs in gastrointestinal tract.

Maximum plasma concentration time is almost 3 hours.


Raltegravir is largely bound to human plasma protein by 83%.

It is distributed in red blood cells at minor range.


The metabolism of Isentress is occurs majorly in liver


The elimination route of Raltegravir is occurs through feces & urine.

The terminal half life period of Raltegravir is 9 hours.

When to take the Isentress

Isentress tablet should be administered with or without food.

Dosage regimens of Isentress

In adult, the prescribed dose of Isentress is 400mg should be administered as a two times a day.

In pediatrics;

12 years or older:

The prescribed dose is 400mg of Isentress should be administered as two times aaday.

6 to less than 12 years of age:

At least 25kg: One tablet of Isentress should be taken orally as two times a day

≥ 40kg: 400mg of Isentress should be administered two times a day

Isentress caused side effects


Abnormal dreams




Decreased in platelets count

Elevation of blood glucose level

Increased bilirubin

Increased serum AST, ALT

Increased alkaline phosphatase




Abdominal pain




Herpes zoster


Renal failure

Suicidal ideation


Stevens Johnson syndrome

Drug- drug interaction

Raltegravir is not inhibits the CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6 or 3A.

Raltegravir does not induce CYP1A2, 2B6, or 3A4.

Midazolam with Isentress causes low susceptibility of Raltegravir to vary the pharmacokinetic of agents metabolized by CYP3A4, an inadequacy of effect of Raltegravir on pharmacokinetic of Midazolam, sensitive CYP3A4 substrate.

 Raltegravir not prohibits the P-gp mediated transport.

Isentress tablets are combined with rifampin causes depletion of plasma concentration of Raltegravir. In case of this combination, the dose of Isentress should be increased for reducing this adverse.

Concurrent use of Isentress with drugs inhibits UGT1A1 leads to elevate the plasma levels of Raltegravir.

Isentress combined with atazanavir causes increasing the concentration of Raltegravir.

Isentress co administered with atazanavir/ritonavir, causes increasing concentration of Raltegravir

Isentress tablets are concurrently used with efavirenz leads to cause decreasing the concentration of Raltegravir.

Isentress with efavirine causes decreasing concentration of Raltegravir

Isentress tablets combined with tipranavir/ritonavir, causes depleting the effect of concentration of Raltegravir.

Co administration of Isentress with gastric regulators should be avoided, because this combination leads to increase the effect of concentration of Raltegravir.

Food drug interaction

Minor food drug interaction is occur

Diet should be discussed with medical practitioner and follow the diet chart.

Possible contraindications

There is no possible contraindication occurs.

Some hypersensitivity reactions may produces, if patients are contraindicated to the component present in the Isentress tablets.

Safety measures

Severe skin reactions & anaphylactic reactions:

Skin reactions like Stevens Johnson syndrome & toxic epidermal necrolysis are some of fatal cases occur. In case of life threatening condition, therapy should be discontinue and provide the general supportive therapy. Clinical status should be appropriately monitored for reducing the manifestations.

Immune reconstitution syndrome:

This fatal condition is commonly occurred in patients who are receiving anti-retroviral treatment.

Provide safety measures

In severe condition, stop the treatment.


Raltegravir chewable tablets are containing a component like phenylalanine (aspartame component) which is responsible for this fatal case.

Pregnancy and lactation

The pregnancy category of Isentress is C

Isentress should not be used in pregnancy and lactating period.

Storage and handling

The storage of Isentress container should be kept at 20oC to 25oC

Protect from light

Keep in dry & cool place

Missed dose

Isentress is an anti-retroviral medicine, in case of missed dose condition patient should be consult with medical practitioner and follow the guidance

Maintain the regular dosing schedule.

Over dosage

The maximum dose of Isentress is 1600mg as a single dose

The maximum dose of Isentress is 800mg as two times a day.

In case of over dosage of Isentress patient must be;

Initiate with supportive measures

Eliminate the unabsorbed dose from GI tract

Monitor the manifestation occurs due to over dosage


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