Tramadol Geksal suppositories

General characteristics. Structure:

Active agent: a tramadola a hydrochloride - 100 mg;

Excipients: fat firm, глицерол (mono, di, three) алканоат.

Pharmacological properties:

Drug belongs to the list No. 1 of strong substances of Standing committee on control of MZ Russian Federation drugs.
Tramadol – the opioid synthetic analgetic possessing the central action and action on a spinal cord (promotes opening of K+ and Sa + channels, causes hyperpolarization of membranes and slows down carrying out painful impulses), strengthens effect of sedatives. Activates opioid receptors (a mu - delta, a kappa-) on pre-and postsynaptic membranes of afferent fibers of nociceptive system in a brain and digestive tract. The analgetic effect is caused by decrease of the activity nociceptive and increase anti-nociceptive systems of an organism.
In therapeutic doses does not influence significantly a hemodynamics and breath, does not change pulmonary pressure, slightly slows down an intestines peristaltics, without causing at the same time locks. Has some antibechic and sedative effect. The respiratory center oppresses, excites a starting zone of the emetic center, a kernel of the oculomotor center.
At long use tolerance development is possible.

Pharmacokinetics. At rectal use bioavailability of a tramadol makes 80%; communication with proteins of plasma – 20%. Tramadol and his metabolites are removed with urine, the elimination half-life makes about 6 hours. Gets through hematoencephalic and placental barriers, 0,1% are allocated with breast milk.
About 7% are removed by a hemodialysis.

Indications to use:

Pain syndrome of average and strong intensity of various etiology (the postoperative period, injuries, neuralgia, hurt oncological patients). Anesthesia when carrying out painful diagnostic or medical manipulations.

Route of administration and doses:

Tramadol is applied on doctor's orders, the mode of a drug dosing is selected individually depending on expressiveness of a pain syndrome and sensitivity of the patient. Duration of treatment is defined by the doctor individually, it is not necessary to appoint drug over the term, justified from the therapeutic point of view.

In the absence of other instructions Tramadol it is necessary to appoint in the following dosages.
Usual dose – 1 suppository (100 mg) 2 times a day, in the morning and in the evening. If the analgesic effect is insufficient, then in 1-2 hours the repeated dose – 100 mg can be appointed. The maximum daily dose of a tramadol – 400 mg.

For treatment of pain at oncological diseases and the expressed pain in the postoperative period higher doses can be used.
At elderly patients (at the age of 75 years and more) in connection with a possibility of the slowed-down removal the interval between administrations of drug can be increased according to specific features.

At patients with diseases of kidneys and a liver Tramadol can longer act. For similar patients the doctor can recommend increase in an interval between introductions of single doses.
Tramadol's suppositories enter into a rectum. Directly after introduction 30 minutes of rest in a prone position are recommended.

Features of use:

With the increased intervals of time apply трамадол at patients of advanced age. Under careful medical observation and in the reduced doses it is necessary to apply трамадол against the background of effect of anesthetics, hypnotic drugs and psychotropic drugs. Drug is not used for therapy of a syndrome of "cancellation" of drugs.
It is forbidden to take alcohol at treatment by Tramadol.
At Tramadol's use it is necessary to abstain from driving of motor transport and occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

- From a nervous system: perspiration, dizziness, a headache, weakness, increased fatigue, block, paradoxical stimulation of TsNS (nervousness, agitation, uneasiness, a tremor, spasms of muscles, euphoria, emotional lability, hallucinations), drowsiness, a sleep disorder, confusion of consciousness, an incoordination, spasms of the central genesis (at intravenous administration in high doses or at co-administration of antipsychotic means), a depression, amnesia, disturbance of cognitive function, paresthesia, instability of gait.
- From the alimentary system: dryness in a mouth, nausea, vomiting, a meteorism, abdominal pains, a lock, diarrhea, difficulty when swallowing.
- From cardiovascular system: tachycardia, orthostatic hypotension, syncope, collapse.
- Allergic reactions: urticaria, itch, dieback, violent rash.
- From an urinary system: difficulty of an urination, dysuria, ischuria.
- From sense bodys: vision disorder, taste.
- From respiratory system: диспноэ.
- Other: disturbance of a menstrual cycle.
- At prolonged use – development of medicinal dependence. At sharp cancellation – a syndrome of "cancellation".

Interaction with other medicines:

Strengthens action of the means exerting the oppressing impact on TsNS, ethanol.
Inductors of a microsomal oxidation (including carbamazepine, barbiturates) reduce expressiveness of analgetic effect and duration of action. Prolonged use of opioid analgetics or barbiturates stimulates development of cross tolerance.
Anxiolytics increase expressiveness of analgetic effect. Naloxonum activates breath, eliminating an analgesia after use of opioid analgetics. MAO inhibitors, furasolidone, Procarbazinum, neuroleptics - risk of development of spasms (decrease in a convulsive threshold).
Quinidine increases plasma concentration of a tramadol and reduces the maintenance of a metabolite of M1 at the expense of competitive inhibition of CYP2D6 isoenzyme.

Contraindications:

- Hypersensitivity to drug and other opioids.
- The states which are followed by respiratory depression or the expressed oppression of the central nervous system (an alcoholic poisoning, somnolent drugs, narcotic analgetics, psychotropic drugs).
- Heavy liver and/or renal failure (clearance of creatinine less than 10 ml/min.).
- Simultaneous use of MAO inhibitors (and two weeks after their cancellation).
- Children's age (up to 14 years).
- With care and under observation of the doctor patients should use drug with an impaired renal function and a liver, at craniocereberal injuries, the increased intracranial pressure, to patients with epilepsy, and also persons with medicinal dependence to opioids, at patients against the background of pains in an abdominal cavity of not clear genesis is ("acute abdomen").

Pregnancy and period of a lactation:
At pregnancy and in the period of a lactation use is possible only according to vital indications, use has to be limited only to one-time reception.

Overdose:

Symptoms: miosis, vomiting, collapse, coma, spasms, depression of a respiratory center, apnoea.
Treatment: ensuring passability of respiratory tracts, support of breath and activity of cardiovascular system. Opiatopodobny effects can be stopped by Naloxonum, spasms – benzodiazepine.

Storage conditions:

At a temperature not above 30 °C. STORE MEDICINES IN the PLACE, UNAVAILABLE TO CHILDREN! Drug belongs to the list No. 1 of strong substances of Standing committee on control of MZ Russian Federation drugs.

Issue conditions:

According to the recipe

Packaging:

Suppositories rectal on 100 mg. On 10 suppositories in the blister from polyvinylchloride / polyethylene. On 1 or on 2 blisters together with the application instruction in a pack.