Tramadol

General characteristics. Structure:

Active ingredient: 50 mg of a tramadol of a hydrochloride.

Has the expressed anesthetizing effect.

Pharmacological properties:

Pharmacodynamics. Has the expressed anesthetizing effect which is caused by agonistic influence on opioid receptors (weak morfinopodobny action) and disturbance of the return serotonin reuptake and noradrenaline in the central nervous system. At injection introduction the analgetic effect develops in 5-10 minutes and 4-6 hours proceed.

On the main pharmacological properties has a certain similarity to morphine, but differs from it considerably in smaller ability to oppress a respiratory center and to brake motility of digestive tract, and also lack of gistaminovysvobozhdayushchy action.

In therapeutic doses drug has no significant effect on hemodynamics indicators; at controlled use accustoming and medicinal dependence develop extremely seldom and carry the character which was less expressed in comparison with morphine. Activates opiate receptors (a mu - delta and a kappa-) on pre-and postsynaptic membranes.

Indications to use:

Pain syndrome of average intensity at malignant new growths, an acute myocardial infarction, injuries, diagnostic and therapeutic procedures; neuralgia.

Route of administration and doses:

Doses are selected individually (depending on expressiveness of a pain syndrome and sensitivity of the patient). Duration of a course of treatment is also defined individually, but it is not necessary to appoint drug over the term, justified from the therapeutic point of view.

To adults and teenagers 14 years a usual dose for single oral administration are more senior makes 0,05 g with a small amount of liquid. If necessary, in case of insufficient effect, in 30-60 min. it is possible to repeat reception in the same dose, frequency rate of reception – to 4 doses a day. The maximum daily dose makes 0,4 g (400 mg). In exceptional cases, for example at oncological patients, reduction of an interval to 6 h and increase in a daily dose is possible.

The effect remains on average 4-8 h depending on character and intensity of pain.

With the increased intervals of time apply трамадол at patients of advanced age.

Features of use:

To children 1 years the only indication for use of a tramadol are more senior the expressed pain syndrome caused by acute or chronic pain is. 

Use during pregnancy is allowed if the expected effect of therapy exceeds potential risk for a fruit. For the period of treatment it is necessary to stop breastfeeding.

Precautionary measures. With care appoint drug sick with an impaired renal function and a liver, at craniocereberal injuries, the increased intracranial pressure, the patient with epilepsy. Use of a tramadol can complicate diagnosis at an acute pain syndrome in abdominal area.

Under careful observation in the reduced doses it is necessary to apply трамадол against the background of effect of anesthetics, somnolent drugs, anxiolytics and antidepressants in order to avoid excessive oppression of the central nervous system and suppression of activity of a respiratory center.

Use of a tramadol complicates performance of the work demanding the high speed of mental and physical reactions and the increased concentration of attention (driving of motor transport, control of mechanisms, devices, etc.).

Side effects:

Tramadol is rather well had, in therapeutic doses does not cause the expressed respiratory depression and significantly does not influence the blood circulatory system and digestive tract. Can cause however dizziness, a dysphoria, euphoria, hallucinations, decrease in cognitive abilities, spasms, nausea, pain in epigastric area, vomiting, a lock, the complicated urination, tachycardia, heartbeat, block. In rare instances, as a rule at prolonged use of a tramadol, accustoming, dependence, a syndrome of "cancellation" are possible; the expressed respiratory depression, hypotension, a collapse. At use of a tramadol for patients with burdened allergoanamnezy allergic reactions are possible.

Frequency of development of side effects increases with increase in duration of administration of drug.

Interaction with other medicines:

Strengthens effects of tranquilizers, somnolent, sedative and narcotic means, anxiolytics, alcohol.

Activity is reduced by analeptics and psychostimulants, completely block — Naloxonum of N naltrexone (direct antagonists).

In combination with neuroleptics and MAO inhibitors the risk of development of epileptiform spasms increases.

At patients, it is long receiving carbamazepine, metabolism of a tramadol considerably amplifies that can demand increase in a dosage of an analgetic.

Drug should not be combined with narcotic analgetics from group full (Promedolum, fentanyl) or partial agonists (buprenorphine), and also agonists antagonists (налбуфин, буторфанол) opioid receptors.

Inductors of a microsomal oxidation (including carbamazepine, barbiturates) reduce duration of analgetic effect. Prolonged use of opioid analgetics and barbiturates stimulates development of cross tolerance. Quinidine increases plasma concentration of a tramadol.

Tramadol pharmaceutical is incompatible "in one syringe" with solutions of non-steroidal anti-inflammatory drugs. 

Contraindications:

Hypersensitivity, acute alcoholic poisoning and intoxication with the depriving of bonuses means and drugs oppressing TsNS, epilepsy, disturbance of functions of a liver and kidneys, feeding by a breast. Children's age till 1 year. Use of a tramadol is contraindicated at the patients accepting drugs-inhibitors MAO (селегилин, hydrozene sulfate, deprenil, когнитив, Iproniazidum, harmin, паргилин and т.п). 

Overdose:

Symptoms: miosis, spasms, collapse, coma, oppression of a respiratory center, apnoea.

Treatment: ensuring passability of respiratory tracts, maintenance of adequate lung ventilation, maintenance of activity of cardiovascular system, symptomatic therapy (opiate effects can be stopped by Naloxonum; spasms – benzodiazepines (diazepam)). At chronic poisoning tramadoly development of an abstinenty syndrome is possible.  

Issue conditions:

According to the recipe

Packaging:

Solution for injections of 5% in ampoules of 1 ml in a blister strip packaging No. 5х1, No. 5х2

Solution for injections of 5% in ampoules of 2 ml in a blister strip packaging No. 5х1, No. 5х2