Stavir 30mg (Stavudine)

DESCRIPTION

Stavir is a synthetic thymidine nucleoside analogue, and belongs to antiretroviral agents. Stavir is active against the human immunodeficiency virus type 1 (HIV-1) and AIDS. Its not a first line treatment.

Stavir an dideoxynucleoside analog which inhibits reverse transcriptase and has in vitro activity against HIV. Stavir is not a cure for HIV or AIDS.

INDICATION

Stavir capsules in combination with other antiretroviral drugs which are indicated for the treatment of human immunodeficiency virus (HIV)-1 infection. Stavir is may indicated for prevention after a needlestick injury or other potential exposure.

MECHANISM OF ACTION

Stavudine, is belongs to nucleoside analogue of thymidine, and by cellular kinases to the active metabolite is phosphorylated to Stavudine triphosphate. Stavudine triphosphate prohibits the activity of HIV-1 reverse transcriptase (RT) by battle with the natural substrate thymidine triphosphate (Ki=0.0083 to 0.032 μM) and by resulting DNA chain termination following its fusion into viral DNA. Stavudine triphosphate prohibits cellular DNA polymerases β and γ and markedly decreases the coalescence of mitochondrial DNA.

ADME PROPERTIES

ABSORPTION

Rapidly absorped with maximum plasma concentrations occurring within 1 hour after dosing.

DISTRIBUTION

Human plasma protein bounding is negligible

METABOLISM

The active substrate for HIV- reverse transcriptase is phosphorylated intracellularly to Stavudine triphosphate.

EXCRETION

Stavudine administrating to healthy subjects following 80mg dose then the total radioactivity was eliminated in urine 95% and feces 3% respectively.

DOSAGE MANAGEMENT

DOSAGE AND ADMINISTRATION

The prescribed dose of the adult for the treatment of HIV infection
The dosage is mainly based on body weight as follows: The patients weighing < 60kg administer 30mg every 12 hours The patients weighing at least 60kg administered 40mg every 12 hours

Prescribed dose for pediatrics
0.5mg/kg given 12 hours for newborns from birth to 13 days old. 1mg/kg given every 12 hours for pediatric patients at least 14 days old And weighing < 30 kg. Use same adult dose for pediatric patients weighing at least 30kg

Over dosage
The recommended daily dosage exposes no acute toxicity. The chronic dosage complication involves peripheral neuropathy and hepatic toxicity by hemodialysis Stavudine can be removed.

PRECAUTION

Lactic acidosis

Severe hepatomegaly with steatosis and lactic acidosis with the use in combination or nucleoside analogues involves stavudine and other antiretrovirals.

Hepatic toxicity

HIV patients with significant underlying liver disease, the safety and efficacy of stavudine have not been established. If combination with antiretroviral therapy, some serious problem arises and potentially fatal hepatic adverse events and should be checked according to standard practice.

Fat redistribution

Redistribution/aggregation of body fat involving central obesity, dorsocervical fat augmentation (buffalo hump), peripheral wasting, facial wasting, breast enlargement, and “cushingoid appearance” have been observed in patients getting antiretroviral therapy.

Neurologic symptoms

Motor weakness has been resulted rarely in patients getting combination with antiretroviral treatment involving Stavudine and patients should be monitored for the growth of peripheral neuropathy.

DRUG INTERACTION

Combination with zidovudine will competitively prohibits the intracellular phosphorylation of Stavudine . Stavir concomitant use with doxorubicin should be taken with caution, it will leads to the phosphorylation of Stavudine is inhibited at relevant concentrations by doxorubicin. While Stavir interaction with ribavirin will reduces phosphorylation of Lamivudine, Stavudine and zidovudine.

CONTRAINDICATION
In patients Stavir capsules is contraindicated with hypersensitivity to Stavudine or to any of the components.

PREGNANCY 

Pregnancy category C The pregnant women using the drug has no adequate amd well controlled studies of Stavudine only if can use the potential benefit justifies the potential risks.

LACTATION

The drug Stavir is excreted into milk even though not known stavir is excreted in human milk there are possibility of adverse effects. Hence mothers should be instructed not be breast feed if they getting stavudine.

STORAGE

Store at 20°C to 25°C

MISSED DOSE

If a dose is missed by patient then have the dose you remember before next dose or leave the missed dose then follow the regular schedule. Please consult with the doctor.