2010/06/05

Tramadol

Group Affiliation:
Analgetic opioid tool

Description of the active substance (INN):
Tramadol

Dosage form:
drops for oral administration, capsules, capsule-acting, injectable solution, a solution for oral, rectal suppositories, tablets, coated tablets, prolonged action tablets, tablets with prolonged action of

Mode of action:
Synthetic opioid analgesic with a central action and action on the spinal cord (promotes opening of K + and Ca2 +-channels, causing membrane hyperpolarization and inhibits the conduct pain impulses) increases the effects of sedative drugs. Activates opioid receptors (mu, delta, kappa) on the pre-and post-synaptic membranes of afferent nociceptive fibers of the brain and gastrointestinal tract. Slows destruction of catecholamines stabilize their concentrations in the CNS. It is a racemic mixture of two enantiomers - dextrorotatory (+) and levogyrate (-), each of which displays different from the other receptor affinity. (+) Tramadol is a selective agonist of mu-type opioid receptors and selectively inhibits the reverse neuronal serotonin. (-) Tramadol inhibits reverse neuronal capture noradrenaline. Mono-O-dezmetiltramadol (metabolite M1) also selectively stimulates the mu-opiate receptors. The affinity of tramadol to the opioid receptors is 10 times weaker than codeine and 6000 times weaker than morphine. Severity of analgesic effect is 5-10 times weaker than morphine. The analgesic effect is due to decreased activity of nociceptive and antinociceptive systems of the body increases. In therapeutic doses does not affect in a meaningful way on hemodynamics and respiration does not alter the pressure in the pulmonary artery, slightly slowing peristalsis, without causing This constipation. Has some antitussive and sedative effect. Inhibits the respiratory center, excites the launcher zone of the vomiting center, the nucleus of the oculomotor nerve. Prolonged use may develop tolerance. Analgesic effect develops within 15-30 minutes after ingestion and lasts till 6 pm

Indications:
Pain (strong and medium intensity, including inflammation, trauma, vascular disease). Analgesia during painful diagnostic or therapeutic interventions.

Contraindications:
Hypersensitivity, state, accompanied by respiratory depression or marked depression of the central nervous system (alcohol poisoning, sleeping drugs, narcotic analgesics and other psychoactive drugs), pregnancy, lactation period (in case of prolonged use), children's age (under 1 year - for parenteral administration; to 14 - Oral), receiving MAO inhibitors, severe hepatic and / or renal failure (CC <10 ml / min). C care. Drug addiction, mental confusion, intracranial hypertension TBI, epileptic syndrome (cerebral dysfunction), patients on a background of pain in the abdominal cavity of unknown origin.

Side effects:
On the part of the nervous system: increased sweating, dizziness, headache, weakness, fatigue, lethargy, paradoxical CNS stimulation (nervousness, agitation, anxiety, tremors, muscle spasms, euphoria, emotional lability, hallucinations), sleepiness, sleep disturbance, confusion , violation of motor coordination, seizures of central origin (with a / in the introduction of high-dose or while the appointment of antipsychotic drugs (neuroleptics), depression, amnesia, violation of cognitive function, paresthesias, unsteady gait. On the part of the digestive system: Dry mouth, nausea , vomiting, flatulence, abdominal pain, constipation or diarrhea, difficulty in swallowing. On the part of the SSA: manifestations of vasodilation - tachycardia, orthostatic hypotension, syncope, collapse. Allergic reactions: rash, itching, rash, bullous eruption. On the part of the urinary system: difficulty in urination, dysuria, urinary retention. On the part of the senses: blurred vision, taste. the respiratory system: dyspnea. Other: menstrual irregularities. With prolonged use - drug addiction. With a sharp lifting - syndrome "cancel." Overdose. Symptoms : miosis, vomiting, collapse, coma, convulsions, depression of the respiratory center, sleep apnea. Treatment: the provision of airway, breathing and maintenance of the SSA. opiate effects may be cropped naloxone, cramps - benzodiazepines.

Dosage and administration:
B / B, / m, n / a, mouth, rectum. Inside: For single use only in adults and children over 14 years - to 0.05 grams (tablets, capsules) with a small amount of liquid or 20 cap solution (or drops) for admission inside with a small number of liquid or on sugar. After 30-60 minutes you can repeat the method with the same dose, but no more than 8 doses per day. Retard Tablets - 100-200 mg every 12 hours daily dose - 0.4 grams (in exceptional cases, such as cancer patients, possibly reducing the interval Up to 6 h and an increase in daily dose). Rectal - 0.1, the multiplicity of reception - up to 4 times per day. / in slowly, s / c or i / m: 0.05-0.1 g. If the effect is insufficient, 20-30 minutes after i / v administration can continue infusion at 12 mg / h or additionally appoint inside. The total daily dose - 0.4, the kids over the age of 1 year - inside, only a drop or parenteral (IV, V / m, n / k), a dose of 1-2 mg / kg. Daily dose - 4-8 mg / kg (1 cap - 2.5 mg). Elderly and patients with renal insufficiency require individual dosage (possibly lengthening T1 / 2). When spacecraft less than 30 ml / min and in patients with liver failure required 12 h interval between doses of regular doses of the drug.

Cautions:
Do not use for the treatment of the syndrome of "cancellation" of drugs. It should not be used simultaneously to ethanol. In the case of single dose is not necessary to interrupt breast-feeding. In the period of treatment must be careful when driving and occupation of other potentially hazardous activities that require high concentration and the rapidity psychomotor reactions.

Interaction:
Pharmaceutical incompatible with solutions of diclofenac, indomethacin, fenilbutazona, diazepam, flunitrazepam, nitroglycerin. Enhances the action of drugs which depress the central nervous system, and ethanol. Inductors microsomal oxidation (including carbamazepine, barbiturates) reduce the severity of analgesic effect and duration of action. Prolonged use of opioid analgesics, or barbiturates stimulate the development of cross-tolerance. generalized anxiety increases the expression of analgesic effect, duration of anesthesia increases in combination with barbiturates. naloxone activates respiration, analgesia after eliminating the use of opioid analgesics. MAO inhibitors, furazolidone, procarbazine, antipsychotic drugs (neuroleptics) increase the risk of convulsions ( decrease the convulsive threshold). Quinidine increases the plasma concentration of tramadol and metabolite M1 reduces the expense of competitive inhibition of isoenzyme CYP2D6.