Isentress

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.

Raltegravir

Isentress

400mg

MSD




Isentress indication

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.



Pharmacokinetic

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




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Isentress
Brand Isentress
Ingredients Raltegravir
Strength 400mg
Manufactured MSD
Rating

In adults

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

In pediatrics

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:

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

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 disorders:
immune reconstitution syndrome, drug hypersensitivity

Metabolism:
decreased appetite, diabetes, hyperlipidaemia, hyperphagia, polydipsia, fat redistribution

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

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



Contraindicated to the patients having Hypersensitivity reactions to the active substance of the Isentress

Isentress is not recommended in pregnancy period. Pregnancy category: C The metabolites of Isentress are present in human milk, breast feeding is not recommended

Isentress tablet containers should be stored at room temperature between 20°C to 25°C (68°F to 77°F) It should be keep away from heat, moisture and light

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.

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