INSTGRA AND TAFERO

MILLION

EM 12 MONTHS HEALTH
PHARMACEUTICALS
 DRUG PROFILE OF INSTGRA TAFERO
EM 12 MONTHS TABLETS
 Instgra Tafero EM tablets are used for treatment involved in HIV-1
infections.
 I n s t g r a   t a b l e t s  are containing Dolutegravir as an active component;
whereas Tafero EM tablets are containing Tenofovir Alafenamide &
Emtricitabine as active ingredients.
 I n s t g r a  is pharmacologically classified as an integrase inhibitor.
 T a f e r o E M  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

 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
INSTGRA TAFERO EM
 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.
 T a f e r o E M  should not be combined with protease inhibitors.
 T a f e r o E M  indicated in pediatric patient with weight of at
least 25kg & below 35kg.
 Drawback occurs in T a f e r o E M  uses;
 T a f e r o E M  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

 I n s t g r a - D o lu t e gra v ir is a c o m p e t i ti v e t o v i r u s a sso c i a te d t o H IV i n f e c t i o n .
 D o l u t e g r a v ir is a n I nt e g ra se st r a n d t r a n sf e r a se i n h i b i t o r , w h i c h i s a c t i v e a ga i n st
H IV t y p e 1 in f e c t io n. D o lu t e g r a v i r b i n d s t o t h e a c t i v e s i t e o f i n t e g r a se e n z y m e ,
H IV e n z y m e t ha t he lp s t o t r a n sm i t v i r a l g e n e t i c m a t e r i a l i n t o h u m a n
c h r o m o so m e s.
 T h i s b i n d ing in hib it io n p re v e n ts i n t e gr a se b i n d i n g t o r e t r o v i r u s D N A a n d c a u s e s
b l o c k a d e o f st ra n d t ra n sf e r st e p w h i c h i s r e q u i r e d f o r c e l l p r o l i fe r a t i o n p r o c e s s.
 I n s t g r a h e lp s t o p re v e nt t h e H I V t y p e 1 c e l l p r o d u c ti o n .
 T A F   i s m a nu f a c t u re d a s p r o d r u g , w h i c h i s c o n v e r se d i n t o a c t i v e f o r m i n si d e t h e
b o d y k n o wn a s t e no f o v ir. T A F c o n t a i n i n g c e l l p e r m e a b i l i t y a c t i v i t i e s, t h r o u gh
t h i s e f f e c t it g e t p e ne t r a t e i n t o t h e i n f e c t e d c e l l s a n d c h a ng e d o v e r a s t e n o f o v i r .
 I n s i d e t h e c e lls, t e n o f o v ir i s p h o sp h o r y l a t e d i n t o t e n o f o v i r d i p h o s p h a t e b y
h y d r o l y si s.
 T en o f o v i r d ip ho s p ha t e sh o w n a n t i - r e t r o v i r a l a c t i v i t y b y i n t e r c e d e s i n t o v i r a l D N A
a n d c a u s e s in hib it io n o f c h a i n f o r m a t i o n l e a d s to st o p p i n g t h e v i r a l p r o d u c t i o n .
 ABSORPTION

 After administration, the maximum plasma concentration

of T a f e r o E M ;
 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 T a f e r o E M ;
 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

 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  T a f e r o E M  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  I n s t g r a  is 14 hours
 The half life period of  T a f e r o E M  is;
 TAF: 0.51 hour; Emtricitabine 10 hours
WHEN TO TAKE THE INSTGRA TAFERO
EM
 Both Instgra Tafero EM tablets should be administered with or
without food.
 Before taking the T a f e r o E M  tablet, patient must be examine
for hepatitis B infection.
 Renal function test should be followed.
 DOSAGE REGIMENS OF INSTGRA
TAFERO EM
 The prescribed dose of  T a f e r o E M  is one tablet should be
administered as a single dose.
 T a f e r o E M  is applicable for adults, pediatric with body weight at
least 25 kg or below 35kg, or creatinine clearance higher or equal
to 30ml/min.
 T a f e r o E M  should not be used in patient with CrCl below 30ml/min.
 The dosage of  I n s t g r a  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
 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 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
 INSTGRA TAFERO EM CAUSED SIDE
EFFECTS
 I n s t g r a  associated side effects;
 Hypersensitivity reactions
 Liver toxicity
 Immune reconstitution syndrome
 Insomnia
 Rash
 Fatigue
 Vertigo
 Elevation of;
 AST, ALT
 Bilirubin
 Creatine kinase
 Blood glucose
 Lipase
 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  T a f e r o E M  which is considered as

substrate of P-gp, BCRP, OATP1B1, & OATP1B3.
 2. T a f e r o E M  co administered with strong P-gp or BCRP inhibitors
leads to cause variation in TAF absorption.
 3.  T a f e r o E M  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   T a f e r o E M .
 4. Co administration of  T a f e r o E M  with drugs that inhibits the P-gp
or BCRP leads to cause elevates the absorption & plasma
concentration of TAF.
 5. T a f e r o E M  is majorly eliminated via kidneys.  T a f e r o
E M  combined with drugs which affect the kidney functions causes
increasing the concentration of component in  T a f e r o E M  and
causes increasing the risk effects of  T a f e r o E M .
 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 I n s t g r a  & 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.
 S A F E TY M E A S U R E S

 1 . An a n a p hy la c ti c re a c tio n o c c ur s lik e ra s h es , s o m etim es o rg an dy sf un c ti o n

a ls o o c c u r s.
 I n th is c o n d iti o n , p a ti e n t m a y p r o v id e w i th ge ne ra l su p p o r tiv e m ea s u res an d
m o n ito ri ng th e liv e r e n z y m es le v e l p er io di c a lly .
 I n s ev ere c o n d itio n th e r a p y s h o ul d b e di sc o n tin u ed .
 2 . Li v e r to x ic ity : T h is c o nd it io n o c c ur s d u e to in c rea s ed se ru m AS T & A LT
le v e ls.
 H e p a tic f un c ti o n t e s t s h o u l d be p e rfo rm e d r egu la rl y a n d m ai nt a ine d th e le v e ls
o f h ep a tic e n z y me s .
 I n s ev ere c o n d itio n , t he ra p y sh o u ld b e st o p p ed .
 3 . E x p o su re o f a d v e rs e r ea c ti o n s d u e to d ru g in ter a c tio n s; s o m e d ru gs m a y
r ed u c e t he p la s m a c o n c e n tr at io n o f b o t h th e p ro du c ts a n d le a d s to lo s s the
a c tiv ity .
 A v o i d th is ty p e o f c o n c o m ita n t tre a tm e nt .
 4 . Im m u n e r e c o n st itu tio n s y n d ro m e , th i s c o n d iti o n o n ly o c c ur re d in t he
p a tie nt s wh o a re re c e iv i ng a n ti- ret ro v ir a l th e ra p y . I n se v e re c o nd it io n p ati en t
s h o u ld b e d is c o n ti nu e d w ith the tre atm en t.
 PREGNANCY AND LACTATION

 Pregnancy category of T a f e r o E M  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 25 o C; T a f e r o E M  should

be stored below 30 o C.
 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.
 CONTACT US

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