TRUSTIVA
Drug profile of Trustiva
Trustiva tablet are containing active constituents which are having
anti-retroviral activity drugs known as Tenofovir disoproxil fumarate,
Efavirenz, Emtricitabine.
Trustiva is a FDA approved product, which is active against HIV 1
infection condition.
Trustiva tablet containing components are;
Efavirenz: Non nucleoside reverse transcriptase
inhibitor
Emtricitabine: Nucleoside reverse transcriptase
inhibitors
Tenofovir DF: Nucleoside reverse transcriptase
inhibitors.
All these drugs are involved in inhibiting reverse
transcriptase enzyme which is essential for viral multiplication.
Trustiva tablet are not considered as curable medicine, but it will diminish
the amount of HIV in the body and prevent the further progression into AIDS.
PRODUCT DETAILS
Brand name: Trustiva
Active substances: Efavirenz + Emtricitabine +
Tenofovir disoproxil fumarate
Strength: 600mg + 200mg + 300mg respectively
Mfg: Hetero
Pack: 30 tablets in a container
Category: Anti-retroviral drug
Prescribing
information of Trustiva
The common prescribing information of Trustiva tablet is used to treat HIV-1 infection by used alone or by combining with other
anti-retroviral drugs.
A Trustiva use is
applicable for adults & pediatric patients about 12 years of age and older.
Mechanism of Trustiva
Efavirenz:
Efavirenz exhibits anti-retroviral activity by
inhibiting the reverse transcriptase enzyme which is essential viral RNA directed
DNA polymerase enzyme.
The formation of active triphosphorylated form is
necessary for the effect of efavirenz, variation occurs intracellularly.
Based on the cell type present in the body is
required for phosphorylation.
The interfering of generation of DNA copies of viral
RNA is occurred by inhibiting the enzyme RT.
This new DNA copies is required for new viral
production.
This is concluded as inhibition of cell division.
Emtricitabine:
Emtricitabine is converted into active form known as
Emtricitabine 5’ triphosphate which is essential for inhibition of viral
proliferation. This metabolite fights with deoxycytidine 5’ triphosphate, is a
natural substrate and get merged into viral DNA which leads to chain
elimination.
Tenofovir DF:
This is similar to Emtricitabine, tenofovir is
struggling with substrate called deoxyadenosine 5’ triphosphate and merged into
DNA of virus which may concluded as prohibition of RT activity.
Finally viral multiplication gets affected.
NRT is an enzyme required for virion assembly,
tenofovir DF causes inhibition of viral chain elongation and to produce
immature destruction of DNA transcription, leads to obstruct the viral
multiplication.
Tenofovir DF is a chain eliminator.
Absorption
Efavirenz plasma concentration time is 3 to 5 hours
Steady state of efavirenz is reached between 6 to
10days.
Emtricitabine plasma concentration time reaches
within one hour.
Tenofovir bioavailability occurs by 25%
Maximum plasma concentration is 1.0 ± 0.4 hours.
Distribution
Volume of distribution of tenofovir is 1.3 ±
0.6L/kg.
Tenofovir has low plasma protein binding capacity
with the range of 0.7 to 7.2%
Emtricitabine is highly bound to plasma protein by
80%.
Blood plasma ratio of Emtricitabine is 1.0
Human plasma protein binding capacity of efavirenz
is by 99.5 to 99.7%.
Metabolism
The metabolism of efavirenz is involved by CYP3A
& CYP2B6 isoenzymes.
The efavirenz metabolite is induced majorly by
cytochrome isoenzymes to hydrolyzed metabolites.
The metabolism of tenofovir is not mediated by
cytochrome enzymes.
The metabolism process of Emtricitabine is not so
clear.
Excretion
Nearly 70% of Emtricitabine is occurred in urine,
13.7% in feces.
The terminal half life period of Emtricitabine is 10
hours.
The dose of tenofovir nearly 32% should be recovered
in urine which is in unchanged form.
The terminal half life period of tenofovir is 17
hours.
The elimination of tenofovir is majorly occurs
through glomerular filteration & tubular secretion.
The mean half life period of efavirenz is 52 to 76
hours
Elimination occurs via urine at 14 to 34%; feces at
16 to 61%.
When to take the Trustiva
Trustiva tablet should be taken on an empty stomach at bed time.
Dosage regimens of
Trustiva
The recommended dose of Trustiva for
both adults & pediatric patients with 12 years of age or older, one tablet
should be taken as a single dose.
In renal impairment:
Trustiva tablet is a fixed dose combination tablet, if patient may require
dosage adjustment should not recommended in moderate or severe conditions with
the creatinine clearance below 50ml/min.
Rifampin concomitant use:
Patients with weigh of 50kg or more, Trustiva should
be combined with rifampin, by increasing dose of efavirenz 200mg/day.
Trustiva caused side effects
The most common adverse effects;
Severe acute aggravation of hepatitis B
Lactic acidosis & hepatomegaly with steatosis
Nervous disorders
Newly commenced or worsening of renal impairment
Rash
Liver injury
Bone defects
Immune reconstitution syndrome
Redistribution of fat
Common side effects;
Diarrhea
Nausea
Vomiting
Fatigue
Infections & infestations
Sinusitis
Respiratory tract infections
Nasopharyngitis
Headache
Dizziness
Anxiety
Depression
Insomnia
Rash
Lab abnormality;
Increased levels of;
Cholesterol
Creatine kinase
Serum amylase
Alkaline phosphatase
AST, ALT
Blood glucose
Glycosuria
Neutropenia
Triglycerides
Post marketing reports:
Palpitations
Tinnitus
Vertigo
Gynecomastia
Abnormal vision
Constipation
Malabsorption
Asthenia
Hepatobiliary disorders
Allergy
Pancreatitis
Drug- drug interaction
The substrate of CYP3A or CYP2B6 combined with Trustiva,
causes decreasing plasma concentration of these substrates.
Trustiva tablet with CYP3A inducers causes increasing clearance of efavirenz
leads to decreasing the plasma concentrations.
Co administration of Trustiva with drugs which reduce the renal functions may leads to
increase the plasma concentration of Emtricitabine & tenofovir DF leads to
increase the adverse effects.
Trustiva tablet combined with atazanavir & other protease inhibitors,
causes decreasing the effect of concentration of atazanavir and increasing the
tenofovir concentration.
Trustiva with Didanosine causes increasing effect of concentration of
Didanosine
Trustiva tablet with other NNRTI leads to cause increasing or decreasing the
effect of concentration of efavirenz.
Trustiva with anti-coagulant, anti-convulsants, anti-depressants, or
anti-fungals leads to cause decreasing the effect of concentration of these
following drugs.
Trustiva tablet combined with any anti-infective, anti-mycobacterials,
anti-malarial or calcium channel blocker causes decreasing the effect of
concentration of these drugs.
Trustiva with lipid lowering drugs, hormonal contraceptives or immuno
suppressants, causes decreasing effect of concentration of these drugs.
Food drug
interaction
Trustiva tablet are administered on an empty stomach, at bedtime because of
decreasing neurological problems.
Possible contraindications
Anaphylactic reactions may produce due to patients
may contraindicate to the component present in the Trustiva tablet.
Trustiva is contraindicated to some drugs like;
Voriconazole
The co administration of Trustiva with
voriconazole, efavirenz one of the active component present in Trustiva tablet causes depletion of plasma concentration of voriconazole which may leads to
loss of therapeutic effects.
Safety measures
Safety precautions should be taken in the patients
who are suspected with;
Patients co infected with HIV-1 HBV
Drug interactions
Lactic acidosis or hepatomegaly with steatosis: Stop
the treatment
Co administration of some drugs: Some concomitant
use of drugs should be cause adverse effects.
QT prolongation: monitor ECG periodically and
patients may treat with alternative medications.
Psychiatric symptoms: risk factors should be
frequently and provided with supportive measures
Nervous symptoms: To reduce the symptoms, Trustiva should
be taken at bed time
Renal impairment: In severe condition, discontinue
the treatment.
Reproductive risk: Trustiva tablet is contraindicated to pregnancy condition. Avoid becoming pregnant
Rash: Alternative treatment should be provided
Liver toxicity: Liver function test should be taken
periodically
Bone defects: Vitamin D supplements should be given
to the patients, monitor the bone mineral density.
Convulsions: Provide with anti-convulsants
medication and monitor the risk of seizures.
Immune reconstitution syndrome: Discontinue the
therapy
Redistribution of fat: Discontinue the treatment.
The major risk of fat redistribution is obesity
Pregnancy and
lactation
Pregnancy category D
Trustiva should not be used in pregnancy and lactating period.
Storage and handling
Trustiva tablet container should be stored at 25oC (77oF)
Protect the container from moisture, heat &
light
Missed dose
Missed dose of Trustiva should
be avoided.
In case of missed dose of Trustiva,
must be consult with medical practitioner and follow the instructions.
Regular dosing schedule of Trustiva tablet
should be maintained.
Over dosage
The over dosage of Trustiva tablet are occurred due to missed dose.
The over dosage of efavirenz is caused nervous
system symptoms.
Nearly 3 hours of dialysis process, eliminates 30%
of Emtricitabine dose from the body within 1.5 hours of dosing time.
Tenofovir is easily removed with the range of 54% by
undergoing dialysis.
On 4 hours dialysis process, nearly 10% of dose should be
removed from the body.
Contacteaza-ne
EMAIL ID :
info@dailygenerics.com
Telefonul nr :
+91(994)047-29-02
+40(746)768 867
Website URL :
Keywords : trustiva,trustiva tablet,trustiva price in India
Keywords : trustiva,trustiva tablet,trustiva price in India
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