Description of Instgra
Trade name: Instgra
Active component: Dolutegravir
Company: Emcure pharmaceuticals
Strength of the component: 50MG
Category: Anti-retroviral agent
Package: 30 tablets in a container
Instgra contains an active substance like Dolutegravir; it is a FDA-approved product.
Instgra tablet is used to treat HIV type I infection.
Instgra tablet preferred for HIV infection, it is non-curable and non-preventable. But it can able to suppress the growth of HIV virus and leads to elevate immune cells (T cells)
Dolutegravir, it is an IInd generation HIV Integrase strand transfer inhibitor
Instgra is recent anti-retroviral drug, used in HIV infection associated to AIDS
Instgra is recommended to combine with other medicines containing anti-retroviral properties.
Pharmacology of Instgra
Mechanism of action:
Instgra (Dolutegravir) contains anti-viral property against HIV type I infection.
Instgra is an Integrase inhibitor, which can able to prohibit HIV cell growth by interfering with Integrase binding to the active site and blockade of strands transfer step occurred.
The viral DNA integration into host cells get stopped
This transfer process is responsible for HIV cell multiplication cycle.
This leads to inhibition of viral activity
In HIV infected adults patients, 50mg of Instgra tablets (Dolutegravir) is given orally; the peak plasma concentration of the drug occurs within 2 to 3 hours post-dose.
The steady state is attains within 5 days
The volume of distribution of Dolutegravir is 17.4 L
Instgra (Dolutegravir) is largely bound to the human plasma protein at the range of 98.9% of administered dose.
Instgra tablet is metabolized by three pathways
Glucuronidation by UGT1A1
Carbon oxidation by CYP3A4
Sequential oxidative defluorination and glutathione conjugation
The major metabolite of Dolutegravir is occur in blood plasma, it is in ether glucoronide form and the chemical property of the metabolite is disrupt its efficiency to bind with metal ion so it is in inactive stage
The drug is in unchanged form should be excreted through feces 53%; urine 31%
The terminal half life of Dolutegravir is 14 hours
The clearance rate of Dolutegravir is 1.0L/hr
Indication of Instgra
Instgra (Dolutegravir) is mainly indicated for HIV type I infections, used with other anti-retroviral drugs to treat the infection affected in both adults and pediatric patients
If patient those who are virologically suppressed, will take Rilpivirine; it is a complete regimen to treat HIV-1 infection in adults to replace the current anti-retroviral drugs.
Dose & Dosage's of Instgra
The recommended dosage of Instgra tablets for various conditions;
Treatment naïve or treatment-experienced INSTI-naïve or virologically suppressed adults turns to Dolutegravir plus rilpivirine: The prescribed dose of Dolutegravir is 50mg once daily
Treatment naïve or therapy-experienced naïve 50mg of Dolutegravir should be concomitant with certain UGT1A or CYP3A inducers as twice daily
INSTI-experienced with certain INSTI-associated resistance substitutions or INSTI resistance: 50mg of Dolutegravir should be administered as twice daily
Instgra should be taken with or without food
Rilpivirine dose is 25mg once daily
Depending upon the body surface area of the pediatric patients, the dosage of Instgra tablet should be calculated;
30kg to less than 40kg: 35mg of Dolutegravir should be recommended as a single dose (one 25mg + one 10mg)
40kg or greater: 50mg once daily
If Instgra concomitant with UGT1A or CYP3A inducers, then increase the weight based dose of Dolutegravir to twice daily
Instgra tablet should be administered 2 hours before or 6 hours after cation containing antacids or laxatives, sucralfate, oral supplements.
Dolutegravir with calcium or iron supplements should be taken together with food
If patient fail to take the dose, they must be administered within 4 hours of next dose.
Otherwise the missed dose should be skipped and follow the regular dosing schedule.
Side Effects of Instgra
Hyperglycemia, increased serum ALT, insomnia, fatigue, headache, suicidal ideation, depression, suicidal tendencies, Pruritus, increased serum lipase, diarrhea, abdominal distress, abdominal pain, flatulence, neutropenia, leucopenia, Hyperbilirubinaemia, hepatitis, hypersensitivity reactions, increased creatinine phosphokinase, myositis, renal insufficiency, acute hepatic failure, increase serum creatinine, Myalgia, rashes,
Contraindication of Instgra
Instgra tablets are contraindicated in patients;
Hypersensitivity reaction to Dolutegravir
Co administration of Instgra with dofetilide, leads to increased the plasma concentration of dofetilide cause serious life threatening conditions
Drug Interaction of Instgra
Dolutegravir with metformin or dofetilide, the plasma concentration of these drugs are elevated
Dolutegravir is metabolized by UGT1A1, drug that induce this enzymes may decrease the plasma concentration of Dolutegravir leads to reduce therapeutic effects of the drug
Co administration of Instgra tablet with etravirine leads to decrease the plasma concentration of Instgra
Avoid some drugs to concomitant with Dolutegravir like;
Nevirapine, fosamprenavir/ritonavir, tipranavir/ritonavir, carbamazepine, Phenobarbital, phenytoin, antacids, rifampin, oral calcium or iron supplements
Precaution of Instgra
Caution with use;
Immune reconstitution syndrome
Usage & Safety profile of Instgra Pregnancy & Lactation
Pregnancy category: B
Dolutegravir is largely transfer through placenta, no birth defects has observed at first trimester
Maternal anti-retroviral therapy increase the risk of preterm delivery
Dolutegravir, it is an initial regimen when the patient infected with HIV virus
Breastfeeding is not recommended
Storage of Instgra
The storage condition of Instgra tablet should be at room temperature (below 25oC)
Keep away from heat, moisture and light