Description of ISENTRESS
Brand name: Isentress
Active ingredients: Raltegravir
Strength of the ingredient: 400mg
Company: Merck & company
Pack: 30 tablets in a container
Classified as: Integrase inhibitor or anti retroviral agent
Isentress (Raltegravir) is a prescription HIV medicine which is used under the supervision of medical practitioner
Raltegravir is a FDA approved product, used in combination with other anti-retroviral medicines.
Pharmacology of ISENTRESS
Mechanism of action:
Isentress is an Integrase strand transfer inhibitor effective against human immunodeficiency virus type I infection.
Raltegravir prohibit the catalytic activity of Integrase, an HIV-encoded enzyme, responsible for viral replication.
Incorporation of HIV chromosomes into the host cell genomes will be inhibited
This leads to depletion in the production of new infectious viral particles.
The absorption of Raltegravir is occurs at the range with the Tmax of approximately 3 hours post dose. The steady state of the drug is achieved rapidly within 2 days
Raltegravir is largely bound to the human plasma protein with 83%
The metabolism of the Raltegravir occurs majorly in liver with the help of UGT1A1. The drug is metabolized away through Glucuronidation
The metabolites are excreted through feces and urine. The terminal half life of the drug is 9 hours
Indication of ISENTRESS
Isentress is primarily indicated for the treatment of HIV type I infection, active against Integrase enzyme which is responsible for the growth of HIV infectious cells.
Isentress is not cure the disease but it can control the progression.
Dose & Dosage's of ISENTRESS
Treatment naïve patients or patients who are virologically suppressed on an initial regimen are 400mg should be recommended as twice daily.
Therapy experienced: 400mg twice daily
Therapy naïve or therapy experienced when concomitant with rifampin: 800mg (2×400mg) twice daily
The dosage of Raltegravir should be based on body surface area
At least 40kg:
Treatment naïve or virologically suppressed on an initial regimen: 400mg twice daily
At least 25kg: 400mg PO twice daily
At least 4 weeks of age and weighing 3kg to less than 25kg: not applicable
Birth to 4 weeks or weighing at least 2kg: not applicable
Isentress tablet should be taken with or without food.
If patient fail to take the dose of Isentress tablet, it should be administered within 4 hours to next dose.
Otherwise the missed dose should be skipped and follow the regular schedule
Do not double the dose.
Side Effects of ISENTRESS
Some of adverse effects may occur during the therapy. It may be alone or with combination of other ART’s;
Infection and infestation: genital herpes, folliculitis, gastroenteritis, herpes simplex, herpes zoster, upper respiratory tract infection, Nasopharyngitis
Blood related disorders: anemia, lymph node pain, lymphadenopathy, neutropenia, and thrombocytopenia
Immune disorders: immune reconstitution syndrome, drug hypersensitivity
Metabolism: decreased appetite, diabetes, hyperlipidaemia, hyperphagia, polydipsia, fat redistribution
Psychiatric: abnormal dreams, insomnia, nightmare, abnormal behavior, depression
Nerve disorders: dizziness, headache, amnesia, peripheral neuropathy, tremor,
Eye & ear: visual impairment, vertigo, tinnitus
CVS: palpitations, sinus bradycardia, ventricular extra systoles, hot flush hypertension
Pulmonary: dysphonia, Epistaxis, nasal decongestion
GIT: abdominal discomfort, dyspepsia, gastro esophageal reflux, ulcer
Skin: rashes, lesions, alopecia
Liver: hepatitis, hepatitis alcoholic, hepatic steatosis, hepatic failure
Musculoskeletal: arthralgia, arthritis, back pain, rhabdomyolysis
Renal: renal failure, nocturia, renal cyst
Reproduction: erectile dysfunction, gynecomastia, menopausal symptoms
General: asthenia, fatigue, pyrexia, chest discomfort
Elevation of Alanine aminotransferase, atypical lymphocytes, aspartate aminotransferase, blood triglycerides, lipase, blood pancreatic amylase
Contraindication of ISENTRESS
Contraindicated to the patients having
Hypersensitivity reactions to the active substance of the Isentress
Drug Interaction of ISENTRESS
While taking Isentress with some drugs may cause some interactions; list of medicines
Aluminium or magnesium containing antacids
Calcium carbonate antacids
Rifampin: while concomitant with Isentress, rifampin reduce the concentration of Isentress, the recommended dose of Isentress is 800mg twice daily with rifampin
Carbamazepine, Phenobarbital, phenytoin
Precaution of ISENTRESS
Caution should be taken while using Isentress tablets in the conditions like;
Depression, hepatic impairment, osteonecrosis
Patients must be advised while taking some list of medicines with Isentress causes adverse effects like;
Myopathy and rhabdomyolysis, skin and hypersensitivity reactions, rashes
Usage & Safety profile of ISENTRESS Pregnancy & Lactation
Isentress is not recommended in pregnancy period. Pregnancy category: C
The metabolites of Isentress are present in human milk, breast feeding is not recommended
Storage of ISENTRESS
Isentress tablet containers should be stored at room temperature between 20oC to 25oC (68oF to 77oF)
It should be keep away from heat, moisture and light