Description of Trustiva
* Brand Name : TRUSTIVA
* Active ingredient: Tenofovir Disoproxil Fumarate + * Emtricitabine+ Efavirenz
* Manufactured by : Hetero Drugs Ltd.
* Strength : 300 mg + 200mg +600mg
* Dosage Form : Tablets
* Packing : Pack of 30 Tablets
Trustiva is a combination of three active ingredients (Efavirenz + Emtricitabine + Tenofovir) is used alone or with other antiviral drug for the treatment of HIV infection. It will not cure or prevent HIV/AIDS. Trustiva suppress the HIV replication of virus cell and despite the destruction of the immune system. Trustiva may help to delay the problems arises from AIDS/HIV diseases. The medicine allowed to purchase only with doctors prescription.
Pharmacology of Trustiva
MECHANISM OF ACTION:
An acyclic nucleoside phosphonate di ester associate of adenosine monophosphate is Tenofovir Disoproxil Fumarate (trustiva), that hydrolysed to Tenofovir, finally cellular enzymes phosphorylated to form Tenofovir diphosphate, an restrict chain terminator. Tenofovir involves with DNA synthesis of HIV through aggressive inhibition of reverse transcriptase and fusion into viral DNA. Tenofovir also prevents hepatitis B virus polymerase, resulting in blockage of viral replication.
Emtricitabine is a synthetic nucleoside coordinate of cytidine, which go through phosphorylation occurring inside a cell to emtricitabine 5'-triphosphate, then take part with deoxycytidine 5'-triphosphate and is incorporated into viral DNA which leads to chain termination. Emtricitabine activity against HIV-1, HIV-2 viruses and hepatitis B virus (HBV) while Efavirenz is an non nucleoside reverse transcriptase inhibitor that fight against HIV-1 and stops HIV-1 replication and RNA & DNA dependent polymerase activities.
ABSORPTION: Tenofovir (Trustiva) absorbed immediately from the GI tract, bioavailability with high fat meal is approx 25% and duration of peak plasma concentration (PPC) is 1-2hr. In Emtricitabine (Trustiva) , bioavailability is 93%(capsulel) and solution 75%, PPC is 1-2 hrs. finally Efavirenz (Trustiva) , bioavailabilty is 42% and PPC is 3-5hr.
DISTRIBUTION: Tenofovir(Trustiva) volume of distribution is 1.2-1.3 L/kg and plasma protein binding is <1%, In Emtricitabine (Trustiva) independent of concentration and protein binding is <4%. Efavirenz (Trustiva) is distributed in CSF, enter into breast milk and protein bound is 99%
METABOLISM: Tenofovir Disoproxil Fumarate (trustiva), that hydrolysed to Tenofovir, finally cellular enzymes phosphorylated to form Tenofovir diphosphate, an restrict chain terminator. In Emtricitabine (Trustiva) is limited metabolism. while in Efavirenz (Trustiva) mainly metabolized inCYP3A4 and CYP2B and isoenzyme to inactive hydroxyl metabolite.
ELIMINATION: Tenofovir (Trustiva) excreted through urine by active glomerular filtration and tubular secretion and half life is 18hr. Emtricitabine (Trustiva) eliminated highly unchanged in urine and low limit in faeces, half life is 10hr. In Efavirenz (Trustiva) excreted via urine(14-34%) and faeces is 16-61% while terminal half life is 52-76hr(single dose) and 40-55hr (multiple dose).
Indication of Trustiva
Trustiva is used with combination of antiretroviral drug or alone medicine in adult and children 12yrs / >12yrs for the treatment of HIV-1 infection.
Dose & Dosage's of Trustiva
In adult Trustiva medicine should administrated at bedtime, one tablet orally in an empty stomach.
In children, safety and efficacy of drug is not recommended at age <18yrs.
Side Effects of Trustiva
Major effects: Lactic acidosis, severe hepatomegaly with steatosis
Renal effects: Nephritis, Nephrogenic, diabetes insipidus, renal failure
GI events: Anorexia, abdominal distention, diarrhea, dyspepsia, flatulence
Common effects: vertigo, fatigue, raised liver enzyme, athralgia,rhabdomyolysis, osteomalacia.
Contraindication of Trustiva
Trustiva contraindicated in patient with hypersensitivity to Efavirenz. When coadministration with voriconazole, Trustiva is contraindicated and lactation patient is also contraindicated with Trustiva.
Drug Interaction of Trustiva
• Hormonal Contraceptives; Trustiva interaction with Antibacterial E.G. (Rifampicin, Rifabutin, Clarithromycin) causes enzyme Inducers may Decrease Serum Level and With Ethanol (Hepatic And CNS Adverse Effects).
• Life-Threatening Adverse Effects will cause by Trustiva Used With Cisapride , Midazolam, Terfenadine, Astemizole, Triazolam And Ergot Alkaloids.
Precaution of Trustiva
Monitor the patients with these problems and inform the healthcare providers:
* Cholesterol and triglycerides.
* LFTs in patients with history of hepatitis B and/or C.Hepatic Function Use.
* Convulsions Use with caution in patients with history of seizures..
* CNS symptoms
* Redistribution/accumulation of body fat, including central obesity, dorsocervical fat enlargement, peripheral wasting, facial wasting, breast enlargement..
* Liver enzymes in patients with suspected past of hepatitis B or C infection and liver toxicity.
* Immune reconstitution syndrome . Lipids Increases in total cholesterol and triglycerides have been checked, Monotherapy Resistant virus may emerge rapidly.
* Psychiatric symptoms psychiatric disorders may be at greater risk. There have been occasional reports of death by suicide, delusions, and psychosis-like behavior.
* Skin rash Reported in 26% of adults and 46% of children.
* Overdosage Symptoms Increased CNS symptoms, involuntary muscle contractions.
Usage & Safety profile of Trustiva Pregnancy & Lactation
Tenofovir and Emtricitabine ( Trustiva) has category B: Animal studies have been developed adverse effect, but sufficient and well-tolerated studies in pregnant women which have failed to develop arisk to the fetus in all trimester in pregnancy. While Efavirenz has category D:Based on adverse effects by investigation and experience studies in humans a positive identification of human fetal risk is reported.
Storage of Trustiva
* Trustiva store at temperature of 15-300C.
* Trustiva store with caution and proper label.
* Trustiva store in a cool and dry place.
* Trustiva should kept in children resistance place.
* Trustiva should used before expiry date.