Eptifibatide

Gross

C35-H49-N11-O9-S2

Characteristics

Synthetic cyclical geptapeptid containing six amino acids and меркаптопропиониловы й balance dezaminotisteinil.

Of drugs

The drugs-antiagregatine. Warn tying fibrinoguena factor Villebranda etc. adgeziveh ligands with glikoproteinovmi IIb / IIIa receptor platelets, reversible suppresses agregatia Trombozitov.v studies ex vivo with the use of the ADF and other inducers aggregation of platelets has been shown that the in / in bolusni introduction dose of 180 µ g / kg of there immediately. Moreover, infusions in the dose of 2 µ g / kg / min is the suppression of more than 80% Adf-inducyrovanna aggregation of platelets, no less than 80% of patients (with the calcium content of the physiological level). After 4 h after infusions functional activity of platelets is a 50% base. No significant impact on the protrombinovoe time, activated partial tromboplastinovoe Wrema.v conditions bolusni doses of 90-250 µ g / kg and Infusion Quick 0.5-3.0 µ g / kg / min farmakokinetika is linear and dozozawisimy nature. In imposing the recommended scheme (bolus, and then cefuroxim) quickly achieved C_max, then concentration decreases slightly and reaches equilibrium level for a period of 4-6 hours Linking blood plasma is about 25%. T_1/2 of plasma-2.5 hour klirens - 55-58 ml / kg / h, the volume of distribution 185-260 ml / kg In healthy people klirens kidney is 50% of the total clearance. Report mostly in the urine, unedited, and in the form of metabolites.

Indications

The acute coronary syndrome : unstable stenocardia, myocardial infarction without zubza Q (prevention of deaths and re-myocardial infarction); The transluminalna percutaneous coronary angioplastiki - CTKA (prevention tromboticescoy occluzii artery diseases and acute ischaemic complications, death, myocardial infarction).

Restrictions on the use of

Pregnancy, breast feeding, age and 18 years of age (the safety and effectiveness of the variables).

Pregnancy and lactation

Perhaps if the effect of therapy outweighs the potential risk to the fetus (research on the application during pregnancy did not). At the time of treatment should stop breast-feeding (is not known whether the move eptifibatid in breast milk).

Contraindications

Hypersensitivity, bloody diates in history expressed or pathological bleeding in the past 30 days, expressed arterial hypertension (Sad greater than 200 mm Hg or Dad more than 110 mm Hg), while hypertensive therapy; "Major" surgery in the previous six weeks, stroke in the past 30 days or haemorrhagic stroke in history, ongoing or planned use another receptor inhibitor IIb / IIIa for injecting, dependence on dialysis due to renal failure.

Side-Effects

Small haemorrhage (accompanied by declining levels of hemoglobin of more than 40 g / l), incl. macrogematuria, gematemezis 13.1% (7.6% placebo); great haemorrhage (accompanied by low haemoglobin levels by more than 50 g / l) 10.8% (9.3% placebo), including life-threatening (and gastrointestinal bleeding lung) 1.9% (1.1% placebo); thrombocytopenia (100h10 ^ 9 / l or decrease the number of platelets by 50% or more from baseline) 1.2% (0.6% placebo).

Patient interaction

Be wary combined with other drugs that affect hemostasis system. Simultaneous use of streptokinazoy increases the risk Krovotechenia.ne encourages the use of the molecular geparinom (not available from the combination). Farmatsevticeski incompatible with furosemidom (it is not possible to impose on the same system).

Overdosing

Symptoms : Krovotechenia.lechenie : an introduction. Effective dialysis.

Precautions

Use only in a hospital environment. All patients should be carefully screened for possible bleeding, particularly patients with increased risk of bleeding : women, the elderly, patients with low birth weight. Prior to the application for the detection of possible violations that coagulates the protrombinovogo time, activated partial tromboplastinovogo time whey creatinine, the number of platelets, the level of hemoglobin, gematokrita. There is a need to continually monitor the number of platelets, the level of hemoglobin and gematokrit for 6 h after the start of treatment and then once a day throughout therapy (in the case of reducing more often). Continuous monitoring of sites of possible bleeding, including place a catheter, the arterial, venous or Puncture (risk of bleeding highest in the field of arterial access in CTKA). When it is necessary to carry out emergency or routine surgery infuziu eptifibatida Prekrashchaut.s caution applied to the taking of human liver (koagulopatii probability).

Dosing and Administration

The acute coronary syndrome. B / bolusno to 180 µ g / kg, followed by a continuous infusions to 2 µ g / kg / min (in the level of serum creatinine below 1.912 mmol / l), or 1 µ g / kg / min (in the level of serum creatinine 1,912-3,824 mmol / l) for a duration of not more than 72 h (or before discharge from the hospital if it is sooner). In the case of a patient CTKA on urgent testimony infuziu should continue for the next 18 to 24 hours after the intervention (maximum total duration of therapy, 96 h). CTKA. Before manipulation give / in bolusno 180 µ g / kg, followed by a continuous infusions to 2 µ g / kg / min (in the level of serum creatinine below 1.912 mmol / l), or 1 µ g / kg / min (in the level of serum creatinine 1,912-3,824 mmol / l). Ten minutes after the start of infusions again impose 180 µ g / kg in the form of bolusa. Infuziu continue for 18-24 hours, or until the patient discharge from the hospital if it is sooner, but at least 12 C.primenaetsa usually with acetylsalicylic acid and nefrackzionirovannam geparinom.

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