A strong analgesic, belonging to the group of exogenous opioids, with a very strong antagonistic component. It acts agonistically at the receptor and antagonist at the kappa receptor. It has a strong and long-lasting analgesic effect. In comparison with morphine, it has a weaker effect that contracted on smooth muscles and a lower tendency to induce dependence. May cause constriction of the pupils. In myocardial infarction has a smaller impact on cardiovascular parameters: does not change or slightly decreases the late diastolic pressure in the right ventricle, does not change peripheral resistance, slightly and only in high doses lowers arterial pressure, cardiac index and pulmonary artery pressure. After 10 minutes after intramuscular administration, the blood concentration does not differ significantly from the concentrations found after intravenous administration of the same doses of the drug. Buprenorphine is metabolised in the liver to norbuprenorphine, which is a mu receptor agonist characterized by poor intrinsic activity. T0,5 in the phase of elimination is 20-25 h. It is excreted in the faeces (80%), the remaining amounts are excreted in the urine.
Contraindications:
Hypersensitivity to buprenorphine, other opioid analgesics or other ingredients of the preparation.
Precautions:
Particularly cautiously use in patients taking drugs with an inhibitory activity o.u.n. (drugs used under general anesthetic, antihistamines, phenothiazine derivatives, sedatives, hypnotics) - in the case of such a combination therapy it is recommended to reduce the dose of one or both drugs. Caution in patients with: respiratory disorders (eg asthma, respiratory failure, right ventricular hypertrophy, reduced respiratory reserve, organ hypoxia, hypercapnia, previous respiratory suppression); with head injuries, intracranial changes and other changes at the risk of increased cerebrospinal fluid pressure; with diseases that hinder the outflow of bile; with hypothyroidism, adrenocortical insufficiency (eg Addison's disease), myasthenia gravis, hyperactivity o.u.n, psychosis, coma, hypertrophy of the prostate gland or urethral stenosis, alcoholism,delirium tremens or kyphoscoliosis; with impaired renal, liver or lung function; in old age, weakened; addicts or those suspected of opioid addiction. Use with caution in children. The safety of buprenorphine in children <6 months has not been studied.
Pregnancy and lactation:
Pregnancy is not recommended. Buprenorphine is excreted in human milk in small amounts and may reduce milk production. This should be borne in mind when prescribing this medicine to breastfeeding patients.
Side effects:
The following may occur: dizziness, headache, drowsiness, hypotension leading to syncope, nausea, vomiting, hallucinations and other psychomimetic side effects. Occasional: visual disturbances, breathing suppression, urination disorders, rash. Rare: severe allergic reactions. Cases of bronchoconstriction, angioneurotic edema and anaphylactic shock have been reported. Buprenorphine may cause pupil constriction and disturbances of consciousness that may make it difficult to assess the patient's condition.
Dosage:
Intramuscularly or by slow intravenous injection. In pains of various origins - adults and children> 12 years: usually 0.3-0.6 mg every 6-8 h; children <12 years: 3-6 μg / kg every 6-8 h (do not exceed the dose of 9 μg / kg). In premedication in adults: 0.3 mg intramuscularly administered 1 hour before the procedure. As a complementary analgesic in adults: 0.3-0.45 mg intravenously.
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