The international name:
Tramadol
Group accessory:
Analgetic опиоидное an agent
The description of operating substance (МНН):
Tramadol
The medicinal form:
Drops for intake, capsules, capsules of the prolonged action, a solution for injections, a solution for intake, суппозитории rectal, tablets, tablets covered with a cover, tablets of the prolonged action, a tablet of the prolonged action
Pharmacological action:
The synthetic analgetic possessing the central action and action on a spinal cord (promotes opening K + and Ca2 +-channels, causes a hyperpolarization of membranes and carrying out of painful impulses brakes), strengthens action sedative ЛС. Activates опиатные receptors (a mu - delta - kappa-) on pre - and постсинаптических membranes of eisodic fibers ноцицептивной systems in a brain and GASTROINTESTINAL TRACT. Slows down destruction of catecholamins, stabilises their concentration in ЦНС. Represents рацемическую an admixture 2 энантиомеров - правовращающих (+) and левовращающих (-), each of which shows distinct from other receptor affinity. (+) Трамадол is a selective agonist of a mu-opioidnyh of receptors, and also return selectively brakes нейрональный serotonin capture. (-) Трамадол return brakes нейрональный Noradrenalinum capture. Mono-about-dezmetiltramadol (М1 the metabolite) also selectively stimulates a mu-opiatnye receptors. Affinity трамадола to опиоидным to receptors in 10 times is more weak, than at Codeinum, and in 6000 times is more weak, than at Morphinum. Expression анальгезирующего action at 5-10 time is more weak than Morphinum. The analgetic effect is caused by activity depression ноцицептивной and augmentation антиноцицептивной organism systems. In therapeutic doses does not influence in the significant image a hemodynamic and breath, does not change pressure in a pulmonary artery, slightly slows down an intestine peristalsis, not causing thus constipations. Some antibechic and sedative an effect has. Oppresses the respiratory centre, raises a starting zone of the vomitive centre, a third cranial nerve kernel. At long application tolerance development is possible. Анальгезирующее action develops through 15-30 mines after intake and proceeds to 6 ч.
Indications:
Painful syndrome (strong and average intensity, including an inflammatory, traumatic, vascular parentage). Anaesthesia at carrying out of painful diagnostic or therapeutic actions.
Contraindications:
Hypersensitivity, the conditions accompanied by a respiratory depression or expressed oppression ЦНС (an alcoholic poisoning, soporific ЛС, narcotic analgetics, etc. psychoactive ЛС), pregnancy, the lactemia period (in case of long application), children's age (till 1 year - for parenteral introduction; till 14 years - for intake), reception of inhibitors MAO, serious hepatic and-or renal insufficiency (КК less than 10 ml/mines).C care. A narcomania, confusion of consciousness, intracranial hypertensia ЧМТ, an epileptic syndrome (a cerebral genesis), at patients against pains in an abdominal cavity of an obscure genesis
Side effects:
From nervous system: the raised diaphoresis, giddiness, a headache, delicacy, undue fatigability, block, paradoxical stimulation ЦНС (nervousness, agitation, uneasiness, a tremor, spastic strictures of muscles, euphoria, emotional lability, hallucinations), drowsiness, dream disturbances, confusion of consciousness, disturbance of coordination of movements, cramps of the central genesis (at i.v. introduction in high doses or at simultaneous appointment antipsychotic ЛС (neuroleptics), depression, an amnesia, disturbance когнитивной functions, paresthesias, instability of a gait. From the alimentary system: dryness in a mouth, a nausea, vomiting, a meteorism, an abdominal pain, constipations or a diarrhoeia, difficulty at swallowing. From party SSS: implications вазодилатации - a tachycardia, an orthostatic hypotension, a syncope, a collapse. Allergic reactions: an urticaria, an itch, an exanthema, a violent eruption. From the party мочевыделительной systems: Difficulty of an emiction, dysuria, ischuria. From sense organs: disturbance of sight, taste. From respiratory system: диспноэ. Other: disturbance of a menstrual cycle. At long application - medicinal dependence. At sharp cancellation - a "cancellation" syndrome.Передозировка. Symptoms: a miosis, vomiting, a collapse, a coma, cramps, depression of the respiratory centre, апноэ. Treatment: maintenance of passableness of respiratory tracts, breath and activity ССС maintenance. Опиатоподобные effects can be stopped Naloxonum, cramps - benzodiazepine
Way of application and dose:
I.v., в/м, п/к, inside, it is rectal. Inside: for unitary application by the adult and to children is more senior 14 years - till 0.05 г (tablets, capsules) with a small amount of a liquid or 20 кап a solution (or a thaw) for intake with a small amount of a liquid or on Saccharum. Through 30-60 mines it is possible to repeat reception in the same dose, but no more than 8 doses a day. Tablets ретард - 100-200 mg everyone 12 ч. The Daily dose - 0.4 г (in unusual cases, for example at oncologic patients, it is possible reduction of an interval to 6 ч and daily dose augmentation). It is rectal - 0.1 Frequency rate of reception - to 4 times a day. I.v. slowly, п/к or в/м: 0 If the effect is insufficient, through 20-30 mines after i.v. introduction it is possible to continue infusion with rate of 12 mg/ch or in addition to prescribe inside. The total daily dose - to Children aged is more senior 0.4 1 year - inside, only a drop or парентерально (i.v., в/м, п/к), in a dose of 1-2 mg/kg. Daily dose - 4-8 mg/kg (1 кап - 2.5 mg). With renal insufficiency the individual dosage (probably elongation T1/2) is necessary for persons of advanced age and patients. At КК less than 30 ml/mines and at patients with hepatic insufficiency it is necessary 12 ч an interval between reception of the next doses of a preparation.
Special indicatings:
Do not apply to therapy of a syndrome of "cancellation" of narcotics. It is not necessary to use ethanol simultaneously. In case of single reception there is no necessity to interrupt feeding by a breast. In treatment it is necessary to be careful at driving of motor transport and employment by other potentially dangerous kinds of the activity demanding raised concentration of attention and speed of psychomotor reactions.
Interaction:
Tramadol it is incompatible with solutions of diclofenac, indometacin, Phenylbutazonum, Diazepamum, флунитразепама, Nitroglycerinum. Strengthens action ЛС, oppressing ЦНС, and ethanol. Inductors микросомального oxidations (including carbamazepine, barbiturates) reduce expression анальгезирующего effect and duration of action. Long application опиоидных analgetics or barbiturates stimulates development of two-dimensional tolerance. Анксиолитики raise expression анальгезирующего effect; duration of anaesthesia is enlarged at a combination with barbiturates. Naloxonum activates breath, eliminating an analgesia after application опиоидных analgetics. Inhibitors MAO, Furazolidonum, Procarbazinum, antipsychotic ЛС (neuroleptics) raise risk of development of cramps (depression of a convulsive threshold). Chinidinum raises plasma concentration трамадола and reduces М1 a metabolite at the expense of competitive inhibition of isoenzyme CYP2D6
