Heptavir is a prominent nucleoside analogues which exhibiting anti-retroviral activity and combined with other anti-retroviral drugs for better action to prevent HIV-1infection in patients.
Heptavir tablets are combination tablets which containing an active constituents known as lamivudine as an anti-retroviral medications. This therapy is used with other anti-retroviral drugs for better activity. Heptavir is pharmacologically categorized as nucleoside reverse transcriptase inhibitor. Reverse transcriptase enzyme is essential for viral production.
Heptavir containing 150mg of lamivudine Patients who are getting Heptavir tablets treatment should have better able to attach to complex drug therapy regimen, thereby improving the compliance.
Basically Heptavir is a prominent nucleoside analogues which exhibiting anti-retroviral activity and combined with other anti-retroviral drugs for better action to prevent HIV-1infection in patients.
MECHANISM OF ACTION
Lamivudine: Lamivudine go through phosphorylation intracellularly, to form active molecule known as 5’ triphosphate metabolite, lamivudine triphosphate which show anti-retro viral action. The most important action of this metabolite is prevention of reverse transcriptse via DNA chain elimination which is occurring after infusion of nucleoside analogues.
The absorption of lamivudine is occurs very quickly. The oral bioavailability of Heptavir ; Lamivudine: 86 ± 16%;
The Heptavir is highly distributed in body. The component of Heptavir tablets are binding to human plasma protein with the range of <36% for lamivudine.
The known metabolite of lamivudine is trans-sulfoxide metabolite. Biotransformation is occurred by using sulfotransferases.
Heptavir is undergoes hepatic metabolism elimination. The major route of elimination of lamivudine occurs via urine as an unchanged form. It also excreted in human milk. The terminal half life period of lamivudine is 5 to 7 hours. The renal creatinine clearance of lamivudine is 0.22 plus or minus 0.06 L/hr/kg;
DOSAGE REGIMENS OF LAMIVIR
The prescribed dose of Lamivudine for adult in HIV-1 infection is 150mg given orally for twice a day or 300mg given orally for once a day in combination with other antiretroviral agents. The prescribed dose of Lamivudine for adult in chronic Hepatitis B is 100mg given orally for once a day for the treatment of chronic HBV infection along with evidence of hepatitis B viral replication and active liver inflammation. In pediatric patients usual dose for HIV-1 infections administered as The patient weighing of 14 to < 20 given one tablet of 150mg as morning 75mg and evening 75mg. The patient weighing of ≥ 20 kg to 25 kg given 1 1/2 tablet of 225mg as administer morning 75mg and evening 150mg The patients weighing of ≥ 25kg given 2 tablets of 300mg as morning 150mg and evening 150mg. For chronic hepatitis B: max dose is 100mg/day 2 years or older administrate 3mg/kg orally once a day When to take the Heptavir : Heptavir tablet should be administered with or without food.
HEPTAVIR CAUSED SIDE EFFECTS
The most serious adverse effects are; Hematological toxicity Symptomatic myopathy Lactic acidosis or hepatomegaly with steatosis Aggravation of hepatitis B Hepatic decompensated cirrhosis in patient with HCV/HIV co infection. Aggravation of anemia due to patients who are co infected with HIV-1/HCV getting ribavirin & zidovudine. Pancreatitis Immune reconstitution syndrome Lipoatrophy The most common side effects; Headache Malaise Fatigue Fever, chills Nausea Diarrhea Vomiting Anorexia Loss of appetite Abdominal pain Dyspepsia Abdominal cramps Neuropathy Insomnia Dizziness Depression Nasal signs Cough Rashes Musculoskeletal pain Myalgia Arthralgia
Hematological toxicity, lactic acidosis or hepatomegaly with steatosis & aggravation of hepatitis B infection; these are all possible adverse occurred during or after completion of therapy with Heptavir .
Periodic blood cells count should be taken. In case of neutropenia or thrombocytopenia, Heptavir treatment should be postponed.
LACTIC ACIDOSIS OR HEPATOMEGALY WITH STEATOSIS
This condition may leads to produce fatal cases, majorly in women. The most common adverse effect is obesity In severe condition treatment should be discontinued.
HEPATITIS B CO INFECTION
To overcome the post treatment aggravation of hepatitis infection, patient should be monitored with hepatic function frequently after completion of treatment. The incidence of lamivudine resistance caused hepatitis infection; the potency of lamivudine in patient with HIV-1 HCV co infection has not been evaluated. The concurrent use of lamivudine may leads to cause this type of infection.
In HIV-1 infected patients who are receiving Heptavir having a chance of getting myopathy.
RIBAVIRIN BASED THERAPY
Heptavir combined with ribavirin causes hematological problems in severe condition. Avoid the concomitant use Check the blood cell count during the therapy if necessary. In Immune reconstitution syndrome, Heptavir tablets should be discontinued
Drugs which are opposing the activity of zidovudine; The combination of zidovudine with some drugs produces antagonist effects, like Stavudine Doxorubicin Nucleoside analogues like ribavirin
Heptavir tablets are concurrent use with ribavirin, Ganciclovir, interferon alfa or other drugs may elevate the hematological toxicity effect of zidovudine. Avoid this concomitant treatment. Co administration of lamivudine with sorbitol leads to produce sorbitol dose dependent depletion of lamivudine exposure; this may cause loss of effect. Avoid this combination therapy. Heptavir should not be combined with Zalcitabine which may alters t or inhibits the intracellular phosphorylation of one another.
Anaphylactic reaction may occur in the patient are contraindicated to the component present in Heptavir tablets.
PREGNANCY & LACTATION
The pregnancy category of Heptavir is C Heptavir should not be used in pregnancy & lactating women Generally HIV infected patients should not feed the baby. Heptavir metabolites are eliminated via human breast milk.
Heptavir tablet Store at 20° to 25°C Protect away from moisture, heat & light.
The over dosage of Heptavir should be treated by undergoing hemodialysis. The acute over dosage condition, causes adverse effects like fatigue, headache, vomiting & hematological disturbance. Provide supportive measures. Hemodialysis helps to remove the content of lamivudine from the body.
If missed dose taken without knowledge of medical adviser may causes over dosage. In case missed dose occurs patient must be consult with physician and follow the instructions. Correct dosing schedule should be followed for avoiding over dosage.
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