This document provides information on the fixed-dose combination drug Instgra Tafero EM, which contains dolutegravir, tenofovir alafenamide, and emtricitabine. It is used to treat HIV-1 infection in adults and pediatric patients weighing at least 30kg. The drug works by inhibiting HIV enzymes through different mechanisms of action. Common side effects include hypersensitivity reactions, liver toxicity, and immune reconstitution syndrome. Special precautions are required regarding drug interactions and use in pregnancy.

1. MILLION
HEALTH
PHARMACEUTICALS
INSTGRA AND TAFERO
EM 12 MONTHS

2.  Instgra Tafero EM tablets are used for treatment involved in HIV-
1 infections.
 Instgra tablets are containing Dolutegravir as an active
component; whereas Tafero EM tablets are containing Tenofovir
Alafenamide & Emtricitabine as active ingredients.
 Instgra is pharmacologically classified as an integrase inhibitor.
 Tafero EM is pharmacologically classified as nucleoside reverse
transcriptase inhibitor.
 This Instgra Tafero EM combination is approved by FDA, which
may provide better activity against HIV-1 infections.
 Instgra Tafero EM should not have capability of curing the HIV
infection, but it can able to reduce the development of HIV-1
further to AIDS.
 This is a fixed dose combination of one Integrase inhibitor with
two nucleoside reverse transcriptase inhibitors.
DRUG PROFILE OF INSTGRA TAFERO EM
12 MONTHS TABLETS

3.  Brand name: Instgra Tafero EM 12 months tablets
 Active components: Dolutegravir + Tenofovir Alafenamide &
Emtricitabine
 Strength: 50mg + 25mg & 200mg respectively
 Pack: 30 tablets in a container of both products
 Mfg: Instgra – Emcure; Tafero EM - Hetero
 Category: Anti-retroviral drugs
PRODUCT DETAILS

4. INSTGRA TAFERO EM

5.  The prescribing information of Instgra Tafero EM is used for
treating the HIV 1 infection for both adults and pediatric
weighing of at least 30kg.
 Tafero EM should not be combined with protease inhibitors.
 Tafero EM indicated in pediatric patient with weight of at least
25kg & below 35kg.
 Drawback occurs in Tafero EM uses;
 Tafero EM should not be used in pre exposure prophylaxis
therapy to diminish the danger of sexually obtained HIV-1 in
grown-ups at high hazard.
PRESCRIBING INFORMATION OF INSTGRA
TAFERO EM

6.  Instgra- Dolutegravir is a competitive to virus associated to HIV
infection.
 Dolutegravir is an Integrase strand transferase inhibitor, which is
active against HIV type 1 infection. Dolutegravir binds to the active site
of integrase enzyme, HIV enzyme that helps to transmit viral genetic
material into human chromosomes.
 This binding inhibition prevents integrase binding to retro virus DNA
and causes blockade of strand transfer step which is required for cell
proliferation process.
 Instgra helps to prevent the HIV type 1 cell production.
 TAF is manufactured as prodrug, which is conversed into active form
inside the body known as tenofovir. TAF containing cell permeability
activities, through this effect it get penetrate into the infected cells
and changed over as tenofovir.
 Inside the cells, tenofovir is phosphorylated into tenofovir diphosphate
by hydrolysis.
 Tenofovir diphosphate shown anti-retroviral activity by intercedes into
viral DNA and causes inhibition of chain formation leads to stopping
the viral production.
MECHANISM OF INSTGRA TAFERO EM

7.  After administration, the maximum plasma concentration
of Tafero EM;
 TAF within 60 minutes; Emtricitabine occurs within 3 hours
 Dolutegravir reaches within 2 to 3 hours.
 The steady state level of Dolutegravir occurs within 5 days
 The blood plasma ratio of Tafero EM;
 TAF: 1.0; Emtricitabine: 0.6
ABSORPTION

8.  Binding property of TAF to human plasma protein by 80%;
Emtricitabine to <4%
 Dolutegravir is broadly binds to proteins by 98.9%.
DISTRIBUTION

9.  The metabolism of Dolutegravir is majorly occurs with the aid
of UTG1A1 with lesser range of CYP3A
 The metabolism of TAF is occurs through cathepsin A, carboxyl
esterase 1
 Emtricitabine undergoes biotransformation.
METABOLISM

10.  The major metabolism of Tafero EM is occurs through kidneys.
 70% of Emtricitabine dose occurs via urine; 13.7% via feces.
 <1% of TAF dose eliminated via urine; 31.7% eliminated via
feces.
 The elimination route of Dolutegravir is majorly occurs in
urine, feces.
 The half life period of Instgra is 14 hours
 The half life period of Tafero EM is;
 TAF: 0.51 hour; Emtricitabine 10 hours
EXCRETION

11.  Both Instgra Tafero EM tablets should be administered with or
without food.
 Before taking the Tafero EM tablet, patient must be examine
for hepatitis B infection.
 Renal function test should be followed.
WHEN TO TAKE THE INSTGRA TAFERO EM

12.  The prescribed dose of Tafero EM is one tablet should be
administered as a single dose.
 Tafero EM is applicable for adults, pediatric with body weight at
least 25 kg or below 35kg, or creatinine clearance higher or
equal to 30ml/min.
 Tafero EM should not be used in patient with CrCl below
30ml/min.
 The dosage of Instgra tablets;
 For adults;
 Therapy naïve or therapy experienced INSTI:
 The dose of Instgra is 50mg should be administered orally as
once a day.
 Therapy naïve or therapy experienced by combining with UGT1A
or CYP3A:
 The dose of Instgra is 50mg should be administered orally as two
ti
DOSAGE REGIMENS OF INSTGRA TAFERO
EM

13.  The dose of Instgra is 50mg should be administered orally as
two times a day.
 For pediatrics;
 The potency of Instgra is applicable only for patient with
weight of at least 30kg.
 30 to less than 40kg: 35mg of Instgra tablet should be given
as once a day
 (One 25 mg tablet + one 10 mg tablet).
 40kg or higher: 50mg Instgra is administered as once a day
INSTI EXPERIENCED WITH INSTI RELATED
RESISTANCE

14.  Instgra associated side effects;
 Hypersensitivity reactions
 Liver toxicity
 Immune reconstitution syndrome
 Insomnia
 Rash
 Fatigue
 Vertigo
 Elevation of;
 AST, ALT
 Bilirubin
 Creatine kinase
 Blood glucose
 Lipase
INSTGRA TAFERO EM CAUSED SIDE
EFFECTS

15.  Aggravation of hepatitis B
 Immune reconstitution syndrome
 Outbreak or severity of renal impairment
 Lactic acidosis or hepatic steatosis
 Loss of bone mineral density
 Laboratory abnormality
 Virological response alteration
TAFERO EM ASSOCIATED SIDE EFFECTS

16.  1. TAF is a component of Tafero EM which is considered as
substrate of P-gp, BCRP, OATP1B1, & OATP1B3.
 2. Tafero EM co administered with strong P-gp or BCRP inhibitors
leads to cause variation in TAF absorption.
 3. Tafero EM co administered with P-gp inducers leads to cause
depleting the absorption of TAF concludes as decreasing in
plasma concentration of TAF and loss of effectiveness of Tafero
EM.
 4. Co administration of Tafero EM with drugs that inhibits the P-
gp or BCRP leads to cause elevates the absorption & plasma
concentration of TAF.
 5. Tafero EM is majorly eliminated via kidneys. Tafero
EM combined with drugs which affect the kidney functions
causes increasing the concentration of component in Tafero
EM and causes increasing the risk effects of Tafero EM.
DRUG- DRUG INTERACTION

17.  Minor food drug interaction is occur
 Diet should be followed by the patients after getting advice
from the physician.
 Possible contraindications
 Hypersensitivity reactions produces, if patients are
contraindicate to the component present in
both Instgra & Tafero EM.
 Co administration of Instgra & dofetilide or metformin is
contraindicated because this combination leads to cause
increasing the concentration of dofetilide or metformin. This
may concludes as life threatening conditions.
FOOD DRUG INTERACTION

18.  1. An anaphylactic reaction occurs like rashes, sometimes organ
dysfunction also occurs.
 In this condition, patient may provide with general supportive measures
and monitoring the liver enzymes level periodically.
 In severe condition therapy should be discontinued.
 2. Liver toxicity: This condition occurs due to increased serum AST &
ALT levels.
 Hepatic function test should be performed regularly and maintained
the levels of hepatic enzymes.
 In severe condition, therapy should be stopped.
 3. Exposure of adverse reactions due to drug interactions; some drugs
may reduce the plasma concentration of both the products and leads to
loss the activity.
 Avoid this type of concomitant treatment.
 4. Immune reconstitution syndrome, this condition only occurred in the
patients who are receiving anti-retroviral therapy. In severe condition
patient should be discontinued with the treatment.
SAFETY MEASURES

19.  Pregnancy category of Tafero EM is B; Instgra is B
 Instgra Tafero EM uses in pregnancy condition as cautiously.
Counsel the patients about the risk benefits before starting
the treatment with Instgra Tafero EM.
 Breast feeding should not be allowed.
PREGNANCY AND LACTATION

20.  Instgra container should be stores at 25oC; Tafero EM should
be stored below 30oC.
 Protect from light
 Keep away from moisture & heat
STORAGE AND HANDLING

21.  In case of missed dose, patient must be consult with
physician and follow the regular dosing schedule.
 Over dosage
 In case of over dosage of Instgra Tafero EM, patient should be;
 Provide with general supportive management
 The manifestation of over dosage should be monitored.
MISSED DOSE

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