2010/09/17

Actastav

Composition, structure and packing

Composition, structure and packing

Capsules

1 capsule. Stavudine 30 mg /

Excipients: lactose anhydrous, sodium karboksimetilkrahmal (sodium starch glycolate), sodium lauryl sulfate, magnesium stearate.

The composition of the shell: titanium dioxide, water, sodium lauryl sulfate, gelatin, metilparagidroksibenzoat (methylparaben), propilparagidroksibenzoat (propylparaben).

Hard gelatin capsules, size number 2, white or nearly white, the contents of capsules - white powder.

1 capsule. Stavudine 40 mg

Excipients: lactose anhydrous, sodium starch glycolate, sodium lauryl sulfate, magnesium stearate, dye Ponceau-4R, titanium dioxide, water, gelatin, methylparaben, propylparaben.

Pharmacological action

Antiviral agent, a synthetic analogue of thymidine. It is active against HIV. Metabolised in the cells to stavudine triphosphate, which is due to inhibition of reverse transcriptase of HIV interferes with the elongation of viral DNA. In addition, stavudine triphosphate inhibits cellular DNA polymerase, significantly inhibiting the synthesis of mitochondrial DNA.

Pharmacokinetics

Rapidly absorbed from the gastrointestinal tract. Bioavailability is 78-86%. Cmax is achieved through 0.5-1.5 hours penetrates through the BBB. Vd is 0.8-1.1 L / kg. Metabolised by phosphorylation with the formation of an active metabolite - stavudine triphosphate. 40% of stavudine is excreted in the urine in unchanged form. T1 / 2 - 1-1.6 hours

Statement
treatment of infections caused by HIV, with pronounced clinical manifestations and the ineffectiveness or intolerance to zidovudine and other antiretroviral drugs.

Dosage regimen

When administered a single dose for patients weighing 60 kg and over is 40 mg, less than 60 kg - 30 mg, the frequency of reception - 2 times per day with an interval of 12 h. In marked violation of renal function reduce the dose of stavudine in accordance with the values of QA .

Side effect

From the side of the central nervous system and peripheral nervous system:

peripheral neuropathy, headache, asthenia, insomnia.

The part of the digestive system:

dyspepsia, anorexia, increased hepatic transaminases, pancreatitis.

On the part of the musculoskeletal system:

arthralgia, myalgia.

The part of the hemopoietic system:

anemia.

Allergic reactions: skin rash.

Contraindications

Peripheral neuropathy, renal failure, increased sensitivity to stavudine.

Pregnancy and lactation

There are no adequate and strictly controlled clinical trials the safety of stavudine in pregnancy was conducted. Application of pregnancy is only possible after an assessment of anticipated benefits to the mother and the potential risk to the fetus.

If necessary, use during lactation breastfeeding should be discontinued.

Cautions

With caution used in patients with impaired liver function.

In the treatment of stavudine is necessary to monitor the activity of liver enzymes (ALT, AST, alkaline phosphatase), amylase and lipase in blood plasma.

Drug Interactions

At simultaneous application with chloramphenicol, cisplatin, didanosine, ethambutol, Ethionamide, hydralazine, isoniazid, metronidazole, vincristine, zalcitabine increased risk of developing peripheral neuropathy.

When applied simultaneously with zidovudine installed antagonism in the manifestation of antiviral action.