Drug profile of Abamune L
Abamune L tablets are anti-retroviral medication, which containing an active substances like abacavir & lamivudine.
Abamune L 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.
Abacavir is a nucleoside analogue of HIV reverse transcriptase inhibitor, analogue of guanosine.
Due to presence of this analogue, the HIV viral load should be reduced and postpones or prevents the destruction of immune system.
Both abacavir & lamivudine are none curing the infection, but it able to reduce the progression of HIV infection to AIDS.
Abacavir is mostly used by combination with other anti-retroviral medications
Brand name: Abamune L
Active substances: Lamivudine & Abacavir sulphate
Strength: 300mg & 600mg equivalent to abacavir
Pack: 30 tablets in a container
Classified as: Anti-retroviral drugs
Prescribing information of Abamune L
The common prescribing information of Abamune L is used to treat HIV-1 infections.
Mechanism of Abamune L
Abacavir is characterized as carboxylic synthetic nucleoside reverse transcriptase inhibitor, which is active against HIV infection.
Abacavir is phosphorylated into a functioning metabolite known as carbovir triphosphate (deoxyguanosine 5'triphosphate) dGTP
This dynamic metabolite forbids the activity of reverse transcriptase by contending with dGTP and embedded into viral DNA
The development of viral DNA gets influenced by inclusion of nucleotide which causes absence of OH particle.
For the development of 5' to 3' phosphodiester linkage, an OH atom is necessary. The formation of 3’ phosphodiester linkage is in charge of chain stretching which get inhibited.
Lamivudine is one of the active moieties present in Abamune L 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 & abacavir is occurs by 87% & 83% respectively.
The human plasma protein binding nature of lamivudine is very low.
Abacavir is bounds to human plasma protein by almost 50%.
The apparent volume of distribution of abacavir is 0.86 plus or minus 0.15L/kg; lamivudine is 1.3 plus or minus 0.4L/kg.
The metabolism of abacavir is held by using alcohol dehydrogenase & glucuronyl transferase enzymes.
The metabolism of lamivudine is highly metabolized to trans-sulfoxide and sulfotransferases is essential for biotransformation of lamivudine.
The systemic clearance value of abacavir 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.
The mean terminal half life period of Abamune L tablets are;
Abacavir: 1.45 plus or minus to 0.32 hours.
Lamivudine: 5 to 7 hours
When to take the Abamune L
Abamune L tablets should be administered with or without food.
Abamune L should not be chew, crush or broke. It should be administer with whole of water.
Dosage regimens of Abamune L
Before starting the treatment with Abamune L tablets, patient should be concealing for HLA-B*5701 allele.
The prescribed dose of Abamune L tablets is one tablet should be administered as a single dose.
Abamune L tablets should be combined with other anti-retroviral drugs.
The dosage adjustment should not be recommended;
Abamune L is a fixed dose combination, dosage adjustment should not be suggested in case of;
Patients having creatinine clearance <50ml/min
Patient with mild hepatic impairment condition
Abamune L is contraindicated to the patients suffered with moderate or severe hepatic impairment.
Abamune L caused side effects
Severe hypersensitivity or sometimes causes fatal related to abacavir
Headache or migraine
Hepatic function test abnormalities
Increased blood glucose
Increased level of bilirubin
Increased level of amylase, lipase
Stevens Johnson’s syndrome
Toxic epidermal necrolysis
Lactic acidosis, hepatic steatosis
Drug- drug interaction
The HIV infected patients who are receiving methadone continuance treatment, combined with 600mg of abacavir as two times a day, this concludes as increasing the oral clearance of methadone.
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 abacavir is;
Ethanol 0.7g/kg with 600mg of abacavir causes increasing AUC of abacavir by 41%.
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 trimethaprim 160mg & Sulfamethoxazole 800mg causes increasing AUC of lamivudine by 43%.
Ribavirin causes reduction of phosphorylation of lamivudine.
Food drug interaction
There is some minor food drug interaction may occur, alcohol containing food items should not consume during Abamune L treatment.
Severe hazard occurring during Abamune L treatment is increasing lipid levels.
Common food which produce interactions;
- Grape fruit & juice
- Seville orange
- Vitamin E containing foods
- St John’s wort (an herbal product)
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
The most serious adverse reactions occur during Abamune L therapy is hypersensitivity reactions.
This severe effect is occurs due to presence of two nucleoside analogues in Abamune L.
Major symptoms are;
Patient who are having a gene called HLA-B*5701 allele should have greater extent for hypersensitivity effects due to abacavir.
To avoid this condition, patient must be screened for HLA-B*5701 allele before initiating the treatment with Abamune L.
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.
Immune reconstitution syndrome: If this fatal case occurs, discontinue the treatment.
Fat redistribution: This may leads to obesity majorly occurred in women. To overcome the problem patient should be treated with alternative measures and in severe condition stop the treatment.
Myocardial infarction: 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, Abamune L should not be used.
For severe liver damage, this medication should not be used.
Pregnancy and lactation
Pregnancy category C
Abamune L should not be used in both pregnant & lactating women.
Exposure of postnatal transmission occurs
The potency of Abamune L has not been evaluated in pediatric patients.
Caution should be taken while using Abamune L in geriatric patients.
Storage and handling
Abamune L tablet container should be stored at 25oC (77oF).
Keep the container away from moisture, heat & light
In case of missed dose, patient should be consult with medical practitioner and follow the instruction given by physician.
The regular dosing schedule should be retained. The missed dose leads to over dosage condition.
The over dosage of Abamune L is treated by;
Providing supportive treatment for the patients
Monitor the manifestation associated with over dosage of Abamune L tablets
Lamivudine is removed by using hemodialysis process, because it has low protein binding effect.
The removal of abacavir content from the body by hemodialysis is not known because it has 5% protein binding effects.