
PRODUCT DETAILS
Trade name : Abamune L
Active ingredient : Abacavir & Lamivudine
Strength availability : 300mg & 600mg
Manufactured by : Cipla
Package : 30 tablets in a container
Abamune L is associated with HIV-1infection treatment. Abamune L tablets are Contrary to retroviral pharmaceutical, which consisting a functioning substances like abacavir and lamivudine. Abacavir is a nucleoside analogue of HIV reverse transcriptase inhibitor, also an analogue of guanosine. Lamivudine is a prohibitor of reverse transcriptase enzyme, analogue of Zalcitabine. Both abacavir and lamivudine are none relieving the contamination; however it ready to lessen the movement of HIV disease to AIDS.
INDICATION
The major recommended the drug Abamune L for the indication in patients for the treatment of HIV-1 infections.
DOSAGE
Prior to start the treatment with Abamune L tablets, patient should be disguise for HLA-B*5701 allele.
The usual dose of Abamune L tablets is one tablet should be administered as a single dose.
The drug will be combined with other anti-retroviral drugs.
The dosage adjustment should not be recommended;
Abamune L is a type of fixed dose combination, dosage adjustment should not be suggested in case of;
Patients having creatinine clearance <50ml/min
Patient with mild liver impairment condition
Administered Abamune L tablets with or without food.
It should be administer with whole of water. Abamune L should not be chew, crush or broke.
Over dosage :
The over dosage of Abamune L is treated by;
Monitor the manifestation associated with over dosage of Abamune L tablets
Providing supportive treatment for the patients
Lamivudine :
Lamivudine is one of the active moieties present in Abamune L tablets. Lamivudine is chemically structured as nucleoside analogue. Lamivudine is changes into dynamic 5' triphosphate metabolite intracellularly by phosphorylation (lamivudine triphosphate 3TC-TP. This effective metabolite involves in barrier of switch transcriptase via chain end after addition of nucleotide simple.
Abacavir :
Abacavir is describes as carboxylic synthetic nucleoside reverse transcriptase inhibitor, which is active opposite to HIV infection. Abacavir is phosphorylated into carbovir triphosphate (deoxyguanosine 5'triphosphate) dGTP a functioning metabolite This Aggressive metabolite stops the activity of reverse transcriptase by oppose with dGTP and fixed into viral DNA. The growth of viral DNA gets altered by inclusion of nucleotide which leads absence of OH particle. For the growth of 5' to 3' phosphodiester linkage, an OH atom is necessary. The 3’ phosphodiester linkage formation is in charge of chain stretching which get prohibited.
PHARMACOKINETIC
Absorption: The drug Abamune L highly absorbed after administration.
Bioavailability of both Lamivudine 87% & abacavir 83% respectively.
Distribution: The human plasma protein binding nature of lamivudine is very low.
Bounds to human plasma protein of Abacavir is almost 50%.
Metabolism :
Abacavir metabolized by using alcohol dehydrogenase & glucuronyl transferees’ enzymes.
The metabolism of Lamivudine is highly metabolized to trans-sulfoxide and sulfotransferases is essential for biotransformation of lamivudine.
Excretion :
The abacavir systemic clearance value is 0.80L/hr/kg plus or minus 0.24L/hr/kg & lamivudine is 0.33 plus or minus of 0.06L/hr/kg.
The renal clearance of abacavir is 0.007 plus or minus to 0.0008L/h/kg; lamivudine is 0.22 plus or minus to 0.06L/h/kg.
Half life period of Abamune L tablets are;
Abacavir: 1.45 plus or minus to 0.32 hours.
Lamivudine: 5 to 7 hours
PRECAUTION
Lactic acidosis, hepatic steatosis : These fatal cases are mainly occurred in patients getting anti-retroviral treatment as single therapy or in combinations.
Dropping the treatment for reducing this kind of adverse.
Aggravation of hepatitis B : This patients who are affected by HIV/HBV co infection will occur this condition.
Check the patient’s liver functions very closely for inhibition this fatal case.
In serious condition, continue the anti-hepatitis drugs.
Myocardial infarction : Patient has any risk of CVS disorders should be investigate prior to starting the treatment.
In severe condition, stop the therapy.
Immune reconstitution syndrome :, discontinue the treatment, If this fatal case occurs.
Occurrence of lamivudine resistance may happen;
The efficacy of lamivudine for HIV/HBV co infected patients has not been investigated.
hepatitis B infection risk 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.
Fat redistribution : This may cause to obesity mostly occurred in women. To overcome the problem patient should be treated with alternative measures and in serious condition discontinue the treatment.
DRUG INTERACTION
The patients infected by HIV who are receiving methadone concomitant treatment, combined with 600mg of abacavir as twice daily, this concludes as increasing the oral clearance of methadone. Drug that varies the blood concentration of abacavir is; Interaction of 600mg of abacavir with Ethanol 0.7g/kg will causes increasing AUC of abacavir by 41%. The blood concentration of lamivudine is varies by; Lamivudine 150mg interaction with Nelfinavir 750mg for thrice daily leads to causes increasing AUC of lamivudine by 10%. Interaction of Lamivudine 300mg with trimethaprim 160mg & Sulfamethoxazole 800mg causes increasing AUC of lamivudine by 43%. Ribavirin causes reduction of phosphorylation of lamivudine.
CONTRAINDICATION
Abamune L tablets are contraindicated to; Patients who are having HLA-B*5701 Patients are having any hypersensitivity reactions to abacavir Patients with moderate or severe liver damage
MISSED DOSE
Incase patients missed a dose, then consult with medical practitioner and follow the instruction given by physician. The normal dosing schedule should be retained. The missed dose leads to over dosage condition.
SIDE EFFECTS
Severe hypersensitivity or sometimes causes fatal related to abacavir :
Fatigue,
Malaise,
Dizziness,
Vertigo,
Nausea,
Diarrhea,
Rash,
Pyrexia,
Insomnia,
Depression,
Headache or migraine,
Abdominal pain,
Abnormal dreams,
Anxiety.
Other effects :
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.