Heptavir tablets are anti-retroviral medication, which containing an active substance like lamivudine. Heptavir is involved in HIV-1infection treatment. Lamivudine is a prohibitor of reverse transcriptase enzyme, analogue of Zalcitabine. Lamivudine is chemically classified as nucleoside analogue, active in both HIV-1 infections & hepatitis B infection conditions. Lamivudine are none curing the infection, but it able to reduce the progression of HIV infection to AIDS.
Indication of Heptavir
The common prescribing information of Heptavir is indicated for theHIV-1 infections.
Mechanism of Heptavir
Lamivudine is one of the active moieties present in Heptavir tablets. Lamivudine is chemically structured as nucleoside analogue. Lamivudine is phosphorylated into dynamic 5' triphosphate metabolite intracellularly (lamivudine triphosphate 3TC-TP. This dynamic metabolite includes in hindrance of switch transcriptase through chain end after addition of nucleotide simple.
Both the component has better absorption capacity, which is highly absorbed after administration. The oral mean bioavailability of both lamivudine is occurring by 87% &
The human plasma protein binding nature of lamivudine is very low. The apparent volume of distribution of lamivudine is 1.3 plus or minus 0.4L/kg.
The metabolism of lamivudine is highly metabolized to trans-sulfoxide and sulfotransferases is essential for biotransformation of lamivudine.
The systemic clearance value of lamivudine is 0.33 plus or minus of 0.06L/hr./kg. The renal clearance of lamivudine is 0.22 plus or minus to 0.06L/h/kg. The mean terminal half-life period of Heptavir tablets are; Lamivudine: 5 to 7 hours
Dosage and administration of Heptavir
The prescribed dose of Heptavir 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 Heptavir 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 patient’s 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
Heptavir tablets should be administered with or without food. Heptavir should not be chew, crush or broke. It should be administering with whole of water. Heptavir tablets should be administered with or without food. Heptavir should not be chew, crush or broke. It should be administering with whole of water.
The over dosage of Heptavir is treated by; Providing supportive treatment for the patients Monitor the manifestation associated with over dosage of Heptavir tablets Lamivudine is removed by using hemodialysis process, because it has low protein binding effect.
Heptavir caused side effects
Insomnia, Depression, Headache or migraine, Fatigue, Malaise, Dizziness, Vertigo, Nausea, Diarrhea, Rash, Pyrexia, Abdominal pain, Abnormal dreams, Anxiety
Pancreatitis, Myocardial infarction, Stevens Johnson’s syndrome, Toxic epidermal necrolysis, Fat redistribution, Stomatitis, Weakness, Aplastic anemia, Lymphadenopathy, Splenomegaly, Lactic acidosis, hepatic steatosis, Rhabdomyolysis, Seizures, Wheezing, Alopecia, Erythema multiforme
The most serious adverse reactions occur during Heptavir therapy is
Immune reconstitution syndrome
If this fatal case occurs, discontinue the treatment.
This may lead to obesity majorly occurred in women. To overcome the problem patient should be treated with alternative measures and in severe condition stop the treatment. To avoid this condition, patient must be screened for HLA-B*5701 allele before initiating the treatment with Heptavir .
Lactic acidosis, hepatic steatosis
These fatal cases are majorly occurred in patients receiving anti-retroviral treatment as monotherapy or in combinations. Discontinue the treatment for reducing this kind of adverse.
Aggravation of hepatitis B
This is occurred in patients who are affected by HIV/HBV co infection. Monitor the patient’s hepatic functions very closely for preventing this fatal case. In severe condition, continue the anti-hepatitis drugs.
Occurrence of lamivudine resistance may happen
The potency of lamivudine for HIV/HBV co infected patients has not been evaluated. Rise of hepatitis B infection variations related with protection from lamivudine has additionally been accounted for in HIV-1-contaminated subjects who have gotten lamivudine-containing antiretroviral regimens within the sight of simultaneous disease with hepatitis B infection.
Patient has any risk of CVS disorders should be examine before starting the treatment. In severe condition, stop the therapy.
Renal & liver damage
Patient with creatinine clearance <50ml/min, Heptavir should not be used. For severe liver damage, this medication should not be used.
Drug- drug interaction
This adjustment won't bring about a methadone measurement alteration in the larger part of patients; be that as it may, an expanded methadone dosage might be required in few patients.
Drug that varies the blood concentration of lamivudine is:
Lamivudine 150mg with Nelfinavir 750mg for three times a day leads to causes increasing AUC of lamivudine by 10%. Lamivudine 300mg with trimethoprim 160mg & Sulfamethoxazole 800mg causes increasing AUC of lamivudine by 43%. Ribavirin causes reduction of phosphorylation of lamivudine.