INSTGRA AND TAFERO
EM 12 MONTHS
Drug profile of
Instgra Tafero EM 12 months tablets
Instgra
Tafero EM tabletare 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.
PRODUCT DETAILS
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
Prescribing information
of Instgra Tafero EM
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.
Instgra Tafero EM tablet 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;
Instgra Tafero EM tablet should not be used in pre exposure prophylaxis therapy to
diminish the danger of sexually obtained HIV-1 in grown-ups at high hazard.
Mechanism of Instgra Tafero EM
Instgra Tafero EM - 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.
Emtricitabine into Emtricitabine 5’ triphosphate, this conversion occurs
inside the body and causes chain eliminator effect by struggling with
deoxycytidine 5’triphosphate.
Absorption
After administration, the maximum plasma
concentration of Instgra Tafero EM tablet ;
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 Instgra Tafero EM tablet ;
TAF: 1.0; Emtricitabine: 0.6
Distribution
Binding property of TAF to human plasma protein by
80%; Emtricitabine to <4%
Dolutegravir is broadly binds to proteins by 98.9%.
Metabolism
Instgra Tafero EM 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.
Excretion
The major metabolism of Instgra Tafero EM tablet 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.
 |
| INSTGRA TAFERO EM |
The elimination route of Dolutegravir is majorly
occurs in urine, feces.
The half life period ofInstgra Tafero EM tablet is
14 hours
The half life period of Instgra Tafero EM is;
TAF: 0.51 hour; Emtricitabine 10 hours
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.
The prescribed dose of Instgra Tafero EM tablet 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 Tafero EM tablet ;
For adults;
Therapy naïve or therapy experienced INSTI:
The dose of Instgra Tafero EM 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 times a day.
INSTI experienced with INSTI related resistance:
The dose of Instgra is 50mg should be administered
orally as two times a day.
For pediatrics;
The potency ofInstgra Tafero EM tablet 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
Instgra Tafero EM caused side effects
Instgra associated side effects;
Hypersensitivity reactions
Liver toxicity
Immune reconstitution syndrome
Insomnia
Depression
Abnormal dreams
Dizziness
Headache
Diarrhea
Nausea
Rash
Fatigue
Vertigo
Elevation of;
AST, ALT
Bilirubin
Creatine kinase
Blood glucose
Lipase
Post marketing effects;
Acute liver damage, liver toxicity
Arthralgia
Myalgia
Anxiety
Tafero EM associated side effects;
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
Drug- drug interaction
1. TAF is a component of Tafero EM which
is considered as substrate of P-gp, BCRP, OATP1B1, & OATP1B3.
2. Instgra Tafero EM tablet 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 Instgra 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. Instgra Tafero EM tablet 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.
6. Tafero EM with protease inhibitors
causes decreasing the effect of concentration of TAF.
Tafero EM combines with anti-convulsants agent, anti-mycobacterials,
or st Johns wort leads to produce decreasing effect of concentration of TAF.
7. Instgra elevates the plasma concentration of
drugs which excreted through OCT2 or MATE1.
8. Etravirine diminishes the plasma concentration of
Dolutegravir.
9. Instgra combined with efavirenz causes
decrease the effect of concentration of Dolutegravir.
10. Instgra combined with protease enzymes leads
to cause decreasing the effect of concentration of Dolutegravir.
11. Co administration of Instgra Tafero EM tablet with
dofetilide causes increasing concentration of dofetilide.
Instgra combined with anti-convulsants causing depletion of effect
of concentration of Dolutegravir.
11. Instgra Tafero EM combined with calcium or iron
containing supplements causes decreasing the effect of concentration of
Dolutegravir.
12. Instgra combined with metformin, causes
elevation of metformin concentration.
13. Instgra Tafero EM tablet with rifampin produces depletion of
Dolutegravir concentration.
Food drug interaction
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.
Safety measures
During the treatment with Instgra Tafero EM some
life threatening conditions may produce. Some safety precautions should be
taken during or after completion of treatment.
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.
5. Severe aggravation of hepatitis B infection
occurred in the patient receiving Tafero EM. The potency of Tafero EM in
chronic hepatitis B infection has not been evaluated.
To overcome the problem patient should be treated
with anti-hepatitis B drugs.
6. Renal impairment should be in severe condition in
case of combining Tafero EM with drugs affecting the kidney
functions. To avoid the problem kidney function test should be performed.
Patients, who are having creatinine clearance level
below 30ml/min, should not be taking anti-retroviral medicines.
7. Lactic acidosis or hepatic steatosis; the major
risk factor occurs during this condition is obesity. In severe condition stop
the treatment.
Pregnancy and lactation
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.
Storage and handling
Instgra container should be stores at 25oC; Tafero EM should
be stored below 30oC.
Protect from light
Keep away from moisture & heat
Missed dose
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.
Instgra is crucial to remove through dialysis, because it is
largely bound to human plasma protein.
Tafero EM should be removed by undergoing hemodialysis.
30% of Emtricitabine dose should be eliminated after
3 hours of hemodialysis.
54% of tenofovir content should be removed over the
period of 4 hours of dialysis session.
CONTACT US :
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KEYWORDS : instgra tafero em, instgra tafero em price in India, instgra tafero em tablet
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