International name: Tramadol (Tramadol).
Mode of action of tramadol
The drug Tramadol - a synthetic analgesic,
refers to the group of opioids, it has an effect on the central nervous system and spinal cord, causing hyperpolarization of membranes and hinders pain impulses. It gives a powerful analgesic effect, lasting a long time. Activates the opiate receptors in the brain and the gastrointestinal tract. It slows down the destruction and to stabilize the concentration of catecholamines in the central nervous system.
The drug Tramadol - selective agonist of the mu-opioid receptors, selectively inhibiting the reverse neuronal uptake of serotonin and norepinephrine. Analgesic effect of tramadol at the same doses 5-10 times weaker than morphine.
Subject to the dosage indicated in the instructions, Tramadol does not have a significant effect on respiration and hemodynamics, does not change the parameters of pressure in the pulmonary artery, no significant moderating effect on intestinal motility.
It has sedative and easy antitussive effect. When long-term therapy is probably the development of tolerance. The analgesic effect occurs within 15-30 minutes after the internal use of the drug and continues to operate up to 6 hours.
After oral administration, the drug is approximately 90% absorbed gastro-intestinal tract. The maximum concentration of tramadol in plasma achieved two hours after administration. In single dose of the drug, the bioavailability is 68%, and increases as the application.
The drug binds to plasma proteins by 20%. Tramadol can penetrate through the placental barrier in a concentration similar to the concentration in plasma. It metabolized metabolites to 11, of which one is active. Output by 10% and intestine by 90% by the kidneys.
Indications for use Tramadol
Tramadol is used in severe to moderate inflammatory pain sensation, traumatic and vascular etiology. When conducting diagnostic or therapeutic procedures associated with painful sensations. And also in the postoperative period, and patients with cancer. With weak pain use of the drug is not recommended.
Contraindications for use Tramadol
Tramadol is not recommended for use in:
- hypersensitivity to tramadol;
- states with respiratory depression, or depression of the central nervous system due to alcohol or drug poisoning;
- breastfeeding (except for occasional receptions);
- receiving monoamine oxidase inhibitors;
- severe renal or hepatic insufficiency.
Instructions Tramadol is not recommended for children under 1 year (parenteral administration) and children up to 14 years (internal adoption).
It should be used with caution in patients with Tramadol: addiction, confusion, intracranial hypertension, brain injuries, epileptic syndromes (cerebral origin), abdominal pain of unknown origin.
Tramadol Side Effects
According to the feedback received Tramadol can cause side effects in the form of increased sweating, dizziness, headache,
weakness, lethargy, paradoxical stimulation of the central nervous system (hallucinations, nervousness, anxiety, agitation, muscle spasms, tremors, euphoria, emotional lability), sleepiness, sleep disturbances, confusion, incoordination, convulsions, depression, amnesia, cognitive impairment , unsteady gait.
Tramadol Side Effects of the digestive system may take the form of: dry mouth, nausea, flatulence, abdominal pain, constipation or diarrhea.
Cardio-vascular system in the form of tachycardia, orthostatic hypotension, syncope, collapse.
From the urinary system: difficulty urinating, dysuria, urinary retention.
It is also possible side effects such as: allergic reactions, visual disturbances, taste, menstrual disorders.
Long-term use of the drug is addictive. With a sharp lifting manifested syndrome "cancel".
These overdose tramadol reviews indicate the possible manifestations of the following symptoms: collapse, coma, miosis, apnea, vomiting, depression of the respiratory center, seizures.
Treatment of overdoses is carried by support airway and maintenance of the cardiovascular system. For relief of opiate effects using naloxone, in convulsions - benzodiazepine.
According to the instructions, Tramadol administered intravenously, intramuscularly, subcutaneously, orally, and rectally.
Orally: adults and children over 14 years old, a single application - one tablet or capsule 0, 05 g of liquid or 20 drops of the solution to the internal reception with a liquid or on sugar. Repeated reception is possible after 30-60 minutes, at the same dosage, no more than 8 times per day.
Rectal: 0, 1 gram to 4 times per day.
Intravenously (slowly), subcutaneously and intramuscularly: 0.05-0.1 g With little effect further infusion at 12 mg / h or additional intake. The total dose per day should not exceed 0.4 g
Children older than one year, only in the form of droplets or parenterally at a dosage of 1-2 mg / kg. The daily dosage of 8 mg / kg.
Elderly and patients with renal insufficiency, a prescription for Tramadol should be tailored to the individual dosage.
Tramadol should not be used to treat the syndrome of "cancellation" of drugs. Not available in conjunction with ethanol. When single application permitted not to interrupt breastfeeding. During therapy, you should be careful to persons engaged in potentially hazardous work, including driving motor vehicles.
Interaction with other drugs
Tramadol incompatible with solutions of diclofenac, indomethacin, diazepam, nitroglycerin, phenylbutazone, flunitrazepam. It enhances the effect of drugs which depress the central nervous system, and ethanol.
With prolonged use of barbiturates or opioids is the development of cross-tolerance. When combined with barbiturates receiving tramadol reviews show increased anesthetic effect.
In combination with monoamine oxidase inhibitors, furazolidone, procarbazine and antipsihotropnymi means a reduction in seizure threshold and there is risk of seizures.
Tramadol is stored on rules similar to the rules of storage of morphine and other narcotic drugs. Leave from pharmacies only upon presentation of a prescription for Tramadol.