Isentress 400mg (Raltegravir)

DESCRIPTION

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

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.

INDICATION

Isentress tablets are indicated for treatment of HIV-1 infection by combining with other anti-retroviral medicines. Thus the evidence is based on examining the plasma HIV-1 RNA levels. The indication of Isentress is based on assessment of safety, tolerability, pharmacokinetic parameters & efficacy of Raltegravir.

MECHANISM OF ACTION

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.

PHARMACOKINETIC

ABSORPTION

Maximum plasma concentration time is almost 3 hours.

DISTRIBUTION

Raltegravir is largely bound to human serum protein by 83%. It is distributed in red blood cells at minor range.

METABOLISM

Majorly in liver metabolism of Isentress is occurs

EXCRETION

The elimination route of Raltegravir is occurs through feces & urine. The terminal half life period of Raltegravir is 9 hours.

DOSAGE MANAGEMENT

DOSAGE AND ADMINISTRATION

Isentress tablet should be administered with or without food. 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

OVERDOSAGE

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 and Eliminate the unabsorbed dose from GI tract Monitor the manifestation occurs due to over dosage

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.

PHENYLKETONURICS

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

SIDE EFFECTS

SIDE EFFECTS IN ISENTRESS

Insomnia Abnormal dreams Fatigue Neutropenia Anemia Decreased in platelets count Elevation of blood glucose level Increased bilirubin Increased serum AST, ALT Increased alkaline phosphatase Headache Nausea Asthenia Abdominal pain Gastritis Hepatitis Hypersensitivity Herpes zoster Dizziness Renal failure Suicidal ideation Rash Stevens Johnson syndrome

DRUG INTERACTION

Isentress combined with atazanavir causes increasing the concentration of Raltegravir. Raltegravir is not inhibits the CYP1A2, 2B6, 2C8, 2C9, 2C19, 2D6 or 3A. 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. Isentress interaction 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.

PREGNANCY & LACTATION

The pregnancy category of Isentress is C.   Isentress should not be used in pregnancy and lactating period.

STORAGE 

The storage of Isentress container should be kept at 20°C to 25°C 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.