Nalbufin

General characteristics. Structure:

Active ingredient: 10 mg or 20 mg of a nalbufin of a hydrochloride (in terms of anhydrous) in 1 ml of solution.

Excipients: sodium chloride, sodium disulphite (sodium metabisulphite), sodium citrate 5,5 hydrate (sodium citrate 5,5-water), citric acid or citric acid monohydrate and anhydrous (in terms of monohydrate), water for injections.

Pharmacological properties:

Pharmacodynamics. Nalbufin has properties of an agonist antagonist of opioid receptors (an agonist a kappa - and the antagonist of a mu - opioid receptors). Activates endogenous anti-nociceptive system through a kappa - opiate receptors, breaks interneural transfer of painful impulses at various levels of the central nervous system. Influencing the highest departments of a brain, changes emotional coloring of pain. Brakes conditioned reflexes, has sedative effect, causes a dysphoria, a miosis, excites the emetic center. To a lesser extent, than morphine oppresses a respiratory center and influences motility of digestive tract. Does not influence hemodynamic indicators.

The risk of development of accustoming and opioid dependence at controlled use is small. Begins to work in 2-3 min. after intravenous administration and in 10-15 minutes after intramuscular introduction.

Pharmacokinetics. The maximum concentration in a blood plasma after intramuscular introduction is observed in 30-60 min. Action duration — 3-6 h, an elimination half-life makes 2,5-3 h TCmax at intramuscular introduction — 1 h, at intravenous administration — 30 min.

It is metabolized in a liver. It is removed in the form of metabolites, mainly, with bile and in small amounts with urine. Gets through a placental barrier, it is allocated with maternal milk (less than 1% of the entered dose).

Indications to use:

• the expressed pain syndrome of various origin (the postoperative period, a myocardial infarction, gynecologic interventions, injuries, malignant new growths);
• as an additional tool at the general anesthesia.

Route of administration and doses:

Intravenously, intramusculary or subcutaneously. At intravenous administration drug is dissolved by 10-15 ml of isotonic solution of sodium of chloride.

Pain syndrome: 0,15-0,3 mg/kg of body weight. If necessary it is possible to enter repeatedly in each 4-6 h. The maximum daily dose — 2,4 mg/kg. Duration of treatment is no more than 3 days. At suspicion of a myocardial infarction — 10-20 mg intravenously slowly. If necessary it is possible to increase a dose to 30 mg. In the absence of clear positive dynamics of a pain syndrome 20 mg of drug repeatedly in 30 min. are entered.

For premedication — 100-200 mkg/kg, for introduction anesthesia — 0,3-1 mg/kg in 10-15 min., for anesthesia maintenance — to 250-500 mkg/kg are each 30 min.

Features of use:

It is not necessary to apply more than 3 days and to exceed a dosage because of a possibility of development of physical dependence.

Ambulatories during treatment need to abstain from occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

From a nervous system and sense bodys: less often — fatigue, the general weakness; seldom (less than 1%) — nervousness, discomfort, an illegibility of visual perception, a diplopia, an uneasy dream, nightmares, unusual dreams, at children is paradoxical excitement; frequency is unknown — a ring in ears, spasms, muscle tension (especially respiratory), a tremor, involuntary muscular twitchings. Slackness, drowsiness, confusion of consciousness, dizziness, headache, excitement, euphoria or depression, hallucinations.

From cardiovascular system: decrease or increase in arterial pressure, takhi-or bradycardia.

From the alimentary system: anorexia, (6%); seldom — irritation of digestive tract, a spasm of a bile-excreting path, at inflammatory diseases of intestines — paralytic intestinal impassability and toxic megacolon (a lock, a meteorism, nausea, a gastralgia, vomiting); frequency is unknown — a lock, a hepatotoxic (dark urine, a pale chair, an ikterichnost of scleras and integuments). Dryness in a mouth, dyspepsia, spastic pains.

From an urinary system: seldom (less than 1%) — decrease in a diuresis, a spasm of ureters (difficulty and an urodynia, frequent desires to an urination).

Allergic reactions: less often — a face edema; seldom (less than 1%) Quincke's disease; local reactions: a hyperemia, hypostasis, burning in the place of an injection. Small tortoiseshell, acute anaphylaxis, bronchospasm, throat hypostasis, itch, sneezing.

From respiratory system: fluid lungs; decrease in minute volume of breath.

Others: sweating strengthening, morbidity in an injection site, medicinal dependence, a syndrome of "cancellation" (spastic abdominal pains, nausea, vomiting, a rhinorrhea, dacryagogue, weakness, feeling of alarm, fervescence).

Interaction with other medicines:

Strengthens the oppressing action on the central nervous system of means for the general anesthesia, hypnotic drugs, antihistamines, anxiolytic, antipsychotic, antidepressive means. Ethanol strengthens the oppressing action of a nalbufin on the central nervous system. It is not necessary to combine with other narcotic analgetics because of danger of weakening of an analgesia and a possibility of provoking of a syndrome of "cancellation" at patients with drug addiction. In a combination with derivatives of a fenotiazin and penicillin can strengthen nausea and vomiting. Pharmaceutical we will combine from 0,9% solution of sodium of chloride, 5% solution of a dextrose and Hartmann's solution in glass, polyvinyl chloride, polyethylene containers.

Strengthens the oppressing action on the central nervous system and breath of muscle relaxants.

Medicines with anticholinergic activity, antidiarrheal medicines (including loperamide) increase risk of emergence of a lock up to intestinal impassability, an ischuria and oppression of the central nervous system.

Strengthens: hypotensive effect of the medicines reducing arterial pressure (including ganglioblokator, diuretics).

Buprenorphine (including the previous therapy) reduces effect of other opioid analgetics; against the background of use of low doses of agonists of a mu - or the kappa - opioid receptors can strengthen respiratory depression.

Reduces effect of Metoclopramidum.

With care it is necessary to apply along with monoaminooxidase inhibitors because of possible overexcitation or braking with emergence hyper - or hypotensive crises (in the beginning for assessment of effect of interaction the dose should be lowered to 1/4 from recommended).

Naloxonum reduces effect of opioid analgetics, and also caused by them respiratory depression and the central nervous system; high doses for leveling of effects of a butorfanol, a nalbufin and pentazocine which were appointed for elimination of undesirable effects of other opioids can be required; can accelerate emergence of symptoms of a syndrome of "cancellation" against the background of drug addiction.

Naltrexone accelerates emergence of symptoms of a syndrome of "cancellation" against the background of drug addiction (symptoms can appear in 5 min. after administration of drug, proceed during 48 h, are characterized by firmness and difficulty of their elimination); reduces effect of opioid analgetics (analgetic, antidiarrheal, antibechic); does not influence the symptoms caused by histamine reaction.

Does not prevent and does not facilitate symptoms of a syndrome of "cancellation" at drug addiction (including against the background of fentanyl).

Contraindications:

Hypersensitivity; the expressed respiratory depression and the central nervous system; epileptic syndrome, intracranial hypertensia; head injuries, acute alcoholic poisoning, alcoholic psychosis; acute surgical diseases of abdominal organs (before establishment of the diagnosis); operative measures on gepatobiliarny system (the spasm of a sphincter of Oddi is possible); medicinal dependence to morfinopodobny drugs (morphine, Promedolum, fentanyl) — a possibility of development of a withdrawal; diarrhea against the background of the pseudomembranous colitis caused by cephalosporins, linkozamida, penicillin, toxic dyspepsia (delay of removal of toxins and the aggravation connected with it and prolongation of diarrhea).

With care - advanced age, a cachexia, a liver and/or renal failure, respiratory insufficiency (including at chronic obstructive pulmonary diseases, uraemia), premature births and estimated immaturity of a fruit, the lactation period, pregnancy, children's and youthful age (up to 18 years). The Zhelchekamenny disease, a serious inflammatory illness of intestines, bronchial asthma, arrhythmia, arterial hypertension, a hypothyroidism, a prostate hyperplasia, an urethra stenosis, suicide bent, emotional lability, the seriously ill patients weakened patients.

Overdose:

Symptoms: hypoventilation of lungs, consciousness change (up to a coma), periodic breathing of Cheyn-Stokes, pallor of integuments, a hypothermia, a miosis, a lowering of arterial pressure, cardiovascular insufficiency, paralysis of a respiratory center.

Treatment: at respiratory depression — intravenously Naloxonum or Nalorfinum. Maintenance of adequate lung ventilation and indicators of the central hemodynamics.

Storage conditions:

According to rules of storage of the psychotropic substances entered in the list III of "The list of the drugs, psychotropic substances and their precursors which are subject to control in the Russian Federation". In the place protected from light at a temperature not above 25 °C. To store in the places unavailable to children. A period of validity - 3 years. Not to use after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Solution for injections of 10 mg/ml or 20 mg/ml in ampoules on 1 ml. 5 ampoules in a blister strip packaging. 1 or 2 blister strip packagings with the application instruction and the scarificator or a knife ampoule in a pack from a cardboard. On 20, 50 or 100 blister strip packagings together with the equal number of application instructions, respectively, in a box from a cardboard or a box from corrugated fibreboard (for a hospital). When packaging ampoules with rings or points of a break scarificators or knives ampoule do not put.