preloder

Abacavir Sulfate-Lamivudine


Abacavir

and

lamivudine

are

antiviral

medicines

that prevent

human immunodeficiency virus

(

HIV

) from multiplying in your body.

Abacavir

and

lamivudine

is a combination

medicine

used to treat

HIV

, which can cause the

acquired immunodeficiency syndrome

(

AIDS

). This

medicines

is not a cure for

HIV

or AIDS.
Dosing
Adult dosing:
General Dosage:
Safety and efficacy of

lamivudine

have not been established in patients with

HIV

-1 and comorbid chronic

hepatitis B

virus

infection

.

HIV infection:
1
tablet
(

Abacavir

Sulfate 600 mg/

lamivudine

300 mg)
orally
once a day.

Pediatric dosing:
General Dosage:
Safety and efficacy of

lamivudine

have not been established in patients with

HIV

-1 and comorbid chronic

hepatitis B

virus

infection

.

HIV infection:
25 kg or greater:
1
tablet
(

Abacavir

Sulfate 600 mg/

lamivudine

300 mg)
orally
once a day

Indications
FDA-Labeled Indications:

HIV

infection



Mechanism of Action

Abacavir

Sulfate is a carboxylic synthetic nucleoside analogue that transforms
intracellular
to carbovir triphosphate to inhibit the activity of

HIV

-1 reverse transcriptase (RT) in

viral

DNA
synthesis by contending with the natural substrate deoxyguanosine-5′-triphosphate (dGTP) and by incorporating into

viral

DNA
resulting in chain termination.

Lamivudine

is a synthetic nucleoside analogue that is phosphorylated
intracellular
to

lamivudine

triphosphate to inhibit

HIV

-1
reverse transcriptase
(RT) via

viral

DNA
chain termination.
Adverse Effect
Common:
Gastrointestinal:

Diarrhea

(5%)

Nausea

(5%)

Neurologic:

Dizziness


Headache

(7%)

Insomnia

(7%)

Vertigo


Psychiatric:

Depression (7%)

Other:

Fatigue

Malaise

Serious:
Cardiovascular:

Myocardial infarction



Dermatologic:

Stevens-Johnson syndrome


Toxic epidermal necrolysis



Endocrine metabolic:

Lactic acidosis



Gastrointestinal:

Pancreatitis

Hematologic:

Anemia


Thrombocytopenia



Hepatic:

Hepatomegaly

(Severe)

Hepatotoxicity


Reactivation

of

hepatitis B

viral

hepatitis


Steatosis of liver



Immunologic:

Hypersensitivity reaction

(9%)

Contraindication
Moderate or severe (i.e., Child-Pugh class B or C) hepatic impairment
Patients with the HLA-B*5701 al≤
Prior hypersensitivity reaction to

Abacavir

or

lamivudine


Interaction
Major:
Dasabuvir (theoretical)
Orlistat (theoretical)
Ribavirin (probable)
Sorbitol (probable)

Moderate:
Methadone (established)
Tipranavir (established)
Phamacokinetics
Absorption:

Abacavir

Sulfate:
Oral: rapidly absorbed

Lamivudine

:
Oral: rapidly absorbed

Abacavir Sulfate

:
Bioavailability: 86% +/- 25%

Lamivudine

:
Bioavailability: 86% +/- 16%.

Distribution:

Abacavir Sulfate

:
Volume of Distributor (Vd): 0.86 L/kg +/- 0.15 L/kg

Lamivudine

:
Volume of Distribution (Vd): 1.3 L/kg +/- 0.4 L/kg

Abacavir Sulfate

:
Protein binding: approximately 50%

Lamivudine

:
Protein binding: low

Metabolism:

Abacavir Sulfate

:
Alcohol dehydrogenase and glucuronyltransferase
Metabolites:5′-carboxylic acid, 5′-glucuronide, and carbovir triphosphate

Lamivudine

:
Metabolite: trans-sulfoxide metabolite and lamivudine triphosphate

Excretion:

Lamivudine

:
Renal: (intravenous) approximately 70% unchanged

Elimination:

Abacavir Sulfate

: 1.45 hour+/- 0.32 hour

Lamivudine

: approximately 5 hour to 7 hour

Precaution
Concomitant use:
Hepatic decompensation may occur.

Immunologic:
Sometimes fatal hypersensitivity reactions have occurred.
Immune reconstitution syndrome has been reported.

Renal:
Use not recommended in patients with impaired
renal function
.

Pregnancy Category
Fetal risk cannot be ruled out.
Breast Feeding
Infant risk cannot be ruled out.
Monitoring
(Adult):CD4
cell
counts, ALT, AST, and total
bilirubin
,

hepatitis B

screening,

viral

load, fasting lipid profile, urinalysis
How to Take or Administration
General Information:
The National Institute for Occupational Safety and Health (NIOSH) recommends the use of single gloves by anyone handling intact
tablets
or
capsules
or administering from a unit-dose package.

In the preparation of
tablets
or
capsules
, including cutting, crushing, or manipulating, or the handling of uncoated
tablets
, NIOSH recommends the use of double gloves and a protective gown. Prepare in a ventilated control device, if possible. Use respiratory protection if not prepared in a control device. During administration, wear single gloves, and wear eye/face protection if the formulation is hard to swallow or if the patient may resist, vomit, or spit up.

NIOSH recommends the use of double gloves and a protective gown by anyone handling a hazardous oral liquid or any hazardous drug via a feeding tube. Prepare in a control device, if possible. Use respiratory, eye, and face protection if not done in a control device. During administration, eye/face protection is needed if the patient may resist, or if there is potential to vomit or spit up.

Oral:
Take with or without food.

Dosage Form
Oral Tablet:
(

Abacavir

Sulfate –

Lamivudine

) 600 MG-300 MG
Patient Counselling or Clinical Teaching
Instruct patient to immediately report symptoms of an

infection

.
Warn patient to immediately report symptoms of

lactic acidosis

or

hepatotoxicity

.
Advice patient to consult physician before resuming therapy if there is an interruption in therapy.
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