Indinavir
IndinavirPharmacological action
Indinavir preparation. (HIV-1) is active concerning a human immunodeficiency virus. Is a specific inhibitor of a protease of a HIV-1.
Indications
- The diseases caused by a HIV-1 at adult patients, before receiving or not receiving therapy antirethroviruse agents
Dosage regimen
Recommended Indinavir dose makes 800 mg inside everyone 8 h. It is necessary to begin treatment with a dose 2.4/days
For maintenance of optimum Indinavir absorption is necessary to accept for 1 h to or through 2 h after food intake, washing down with water. Indinavir is possible to accept also together with other drinks (the taken out milk, juice, coffee, tea) or with easy nutrition (a dry toast with jelly and apple juice or coffee with the taken out milk; the corn-flakes, the taken out milk and Saccharum).
For maintenance of adequate hydration the patient is recommended to drink for 24 h not less than 1.5 l of a liquid.
At weak and moderate hepatic insufficiency owing to a cirrhosis Indinavir dose should be lowered to 600 mg, the interval between receptions makes 8 h.
At a nephrolithiasis along with adequate hydration recommend during an attack time (1-3 days) or full cancellation of a preparation.
Side effect
The clinical expressed collateral reactions, becoming perceptible researchers as it is possible, possibly or definitely bound to a preparation at 5 % of the patients accepting only Indinavir, regardless to gravity of their implications included:
From the alimentary system: abdominal pains, a heartburn, a diarrhoeia, dryness in a mouth, a dyspepsia, a meteorism, a nausea, vomiting, taste disturbance, nuclear heating plant, an indirect bilirubin in blood serum, a hepatitis; seldom - development of hepatic insufficiency. The isolated asymptomatic hyperbilirubinemia (the general bilirubin of 2.5 mg/dl and more), basically at the expense of indirect bilirubin rising, nuclear heating plant.
From party TSNS and peripheric nervous system: an asthenia, undue fatigability, giddiness, a headache, dream disturbances.
From kidneys: development of a nephrolithiasis is possible, which is shown by pains in a side with or without a hematuria (including a microhematuria), in 5 % of cases - fiber occurrence in urine. During clinical tests approximately in 4 % of cases (79/2205) the nephrolithiasis became perceptible. These conditions have been estimated as the functions of kidneys bound to disturbances and stopped at the expense of time cancellation of a preparation and introduction of enough of a liquid. Because of occurrence of acute attacks therapy has been stopped at 9.2 % (7/79) patients.
Dermatological reactions: a xeroderma, an itch.
The other: a lymphadenopathy. During clinical researches cases of an acute hemolitic anaemia which sometimes were serious became perceptible and quickly progressed. In such cases it is necessary to cancel a preparation and to spend corresponding treatment. It was informed on cases of spontaneous bleedings at patients with hemophilia A and B which received protease inhibitors. To some patients the additional factor VIII was required. Cases of redistribution/accumulation of Adeps on a nape, on a stomach, in retroperitoneal area became perceptible. In the majority of noted cases therapy by protease inhibitors has been continued or started over again.
Contraindications
- A hypersensibility to preparation components.
Pregnancy and lactemia
Adequate and strictly controllable Indinavir researches at pregnant women it was not spent. At pregnancy Indinavir it is possible to apply only when the potential advantage of a preparation for mother justifies possible risk for a foetus.
Now definitively it is not established, whether causes Indinavir an exacerbation of a physiological icterus of newborns. However in view of theoretical possibility of a preparation to aggravate a physiological icterus at newborn children, application of a preparation in the end of III trimester of pregnancy is justified only in the presence of vital indications.
In need of Indinavir application in a lactemia it is necessary to interrupt thoracal feeding, as it is not known, whether the active substance of a preparation with thoracal milk is allocated.
Special indicatings
Signs and the symptoms of a nephrolithiasis including a painful syndrome with or without a hematuria (including a microscopical hematuria), at the patients receiving recommended Indinavir dose, were observed rather seldom. In Indinavir treatment the adequate water load is recommended. At occurrence of symptoms of a nephrolithiasis dose change can be demanded.
At patients with hepatic insufficiency owing to a cirrhosis Indinavir metabolism decreases, therefore the preparation dose should be reduced.
Overdosage
There are reports on cases of Indinavir overdosage for the person. Symptoms from the party GASTROINTESTINAL TRACT (a nausea, vomiting, a diarrhoeia) and kidneys (a nephrolithiasis, a hematuria) most often became perceptible.
It is not known, whether is exposed Indinavir to a peritoneal dialysis or a hemodialysis.
Conditions and periods of storage
The preparation should be stored in a dry place, in densely closed vial at temperature from 15 to 30 C. The preparation should be stored only in an original vial.
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