Raltegravir

BRAND NAMES:

Isentress -  It contains the active ingredients of raltegravir. It is available in the form of tablets and oral suspension used to treat HIV infections.

MECHANISM OF ACTION:

Raltegravir is primarily metabolized by glucuronidation. Raltegravir inhibits HIV integrase to prevent the viral genome from being incorporated into the human genome.

PHARMACOKINETICS:

Absorption: Raltegravir is absorbed quickly from the gastrointestinal tract.

Distribution: It is distributed into red blood cells. 83% bound to human plasma protein. 

Metabolism: Raltegravir is primarily metabolized by glucuronidation in the liver.

Excretion: Raltegravir is excreted through urine and feces.

PHARMACODYNAMICS:

It inhibits HIV integrase by binding to the active site and blocking the strand transfer step of retroviral DNA integration in the host cell. The strand transfer step is essential in the HIV replication cycle and results in the inhibition of viral activity. 

DOSAGE AND ADMINISTRATION:

Raltegravir is available in three forms: tablet, chewable tablet, and granules for oral suspension. Raltegravir (Isentress) tablets and oral suspensions are typically taken twice daily, with or without food. Raltegravir (Isentress HD) pills are typically used once a day, with or without food.     

• Raltegravir is available in film-coated tablets with the strengths of 400 mg and 600 mg.
• It is also available in chewable tablets with strengths of 25 mg and 100 mg.
• It is also available as granules for oral suspension with the strength of 100 mg per raltegravir packets.

DRUG INTERACTIONS:

Drug interactions with raltegravir may include 

• Anti-HIV drugs – atazanavir, ritonavir and tipranavir
• Anti-tuberculosis drugs – rifampicin
• Anti-depressants – fluoxetine, sertraline
• Iron supplements 
• Antacids 
• Anti-obesity

 CONTRAINDICATIONS:

Hypersensitivity to raltegravir or any other ingredient in the formulations.

SIDE EFFECTS:

When the drug is administered it causes some unwanted effects while it needs effects.

Side effects of raltegravir may include

• Stomach pain
• Diarrhea
• Insomnia
• Heartburn
• Abnormal dreams
• Headache
• Depression
• Muscle pain
• Rash
• Muscle weakness
• Chest pain
• Hives
• Fever
• Itching
• Peeling of skin
• Chest pain
• Vomiting
• Fast heartbeat
• Pale stools
• Nausea
• Lack of energy
• Drowsiness

OVERDOSE:

Taking excessive drugs more than prescribed drugs leads to overdose. 

There is no antidote for overdose of the raltegravir. Symptomatical treatment should be given for overdose.

Symptoms of overdose may include

• Drowsiness
• Nausea
• Vomiting
• Fever

TOXICITY:

Overdose of the drug leads to toxicity. Raltegravir has no serious adverse events despite excessively high serum concentrations. It may therefore be well-indicated for HIV patients at risk of overdosing.