Isentress 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.
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.
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
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
Isentress side effects
Some of adverse effects may occur during the therapy. It may be alone or with combination of other ART’s:
abnormal dreams, insomnia, nightmare, abnormal behavior, depression
dizziness, headache, amnesia, peripheral neuropathy, tremor
Eye & ear:
visual impairment, vertigo, tinnitus
palpitations, sinus bradycardia, ventricular extra systoles, hot flush hypertension
dysphonia, Epistaxis, nasal decongestion
abdominal discomfort, dyspepsia, gastro esophageal reflux, ulcer
rashes, lesions, alopecia
hepatitis, hepatitis alcoholic, hepatic steatosis, hepatic failure
Blood related disorders:
anemia, lymph node pain, lymphadenopathy, neutropenia, and thrombocytopenia
Infection and infestation:
genital herpes, folliculitis, gastroenteritis, herpes simplex, herpes zoster, upper respiratory tract infection, Nasopharyngitis Skin papilloma
immune reconstitution syndrome, drug hypersensitivity
decreased appetite, diabetes, hyperlipidaemia, hyperphagia, polydipsia, fat redistribution
arthralgia, arthritis, back pain, rhabdomyolysis
renal failure, nocturia, renal cyst
erectile dysfunction, gynecomastia, menopausal symptoms
asthenia, fatigue, pyrexia, chest discomfort Elevation of Alanine aminotransferase, atypical lymphocytes, aspartate aminotransferase, blood triglycerides, lipase, blood pancreatic amylase
Isentress precautions and warning
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; Antacids, rifampin Myopathy and rhabdomyolysis, skin and hypersensitivity reactions, rashes
Isentress drug interaction
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