Tramadol Geksal of the capsule

General characteristics. Structure:

Active agent: tramadola hydrochloride of 50,0 mg.

Excipients: calcium hydrophosphate, sodium of starch glikolit, magnesium stearate, gelatin, E 132, E 171, E 172 dye.

Pharmacological properties:

Drug belongs to the list No. 1 of strong substances of Standing committee on control of MZ Russian Federation drugs.
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 specific opioid receptors (a mu - delta, a kappa-) on pre-and postsynaptic membranes of afferent fibers of nociceptive system in a brain and a GIT.

Pharmacokinetics. After intake quickly and almost it is completely absorbed from a GIT (about 90%). The maximum concentration in a blood plasma is defined in 2 hours after intake. Bioavailability at a single dose inside makes 68% and increases at repeated use. Gets through gemato-entsefallichesky and placental barriers.
0,1% are allocated with breast milk. Distribution volume – 306 l. Communication with proteins of plasma - 20%.
In a liver it is metabolized by N-and O - demethylation with the subsequent conjugation with glucuronic acid. 11 metabolites from which mono - About - desmetiltramadol (M1) has pharmacological activity are revealed. T ½ in the second phase are 6 h (трамадол), 7,9 h (mono - About - desmetiltramadol); at patients 75 years – 7,4 h are more senior (трамадол); at cirrhosis – 13,3 + 4,9 h (трамадол), 18,5 + 9,4 h (mono - About - desmetiltramadol), in hard cases – 22,3 h and 36 h, respectively; at HPN (KK less than 5 ml/min.) – 11 + 3,2 h (трамадол), 16,9 + 3 h (mono - About - desmetiltramadol), in hard cases – 19,5 h and 43,2 h, respectively.
The average cumulative value of renal removal – 94% is removed by kidneys (25-35% in not changed look). About 7% are removed by means of a hemodialysis.

Indications to use:

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

Route of administration and doses:

Tramadol is applied at appointment of the doctor, the mode of dosing is selected individually depending on expressiveness of a pain syndrome and sensitivity of the patient.
In the absence of other instructions Tramadol it is necessary to appoint in the following dosages:
For adults and teenagers 14 years - 1 capsule (50 mg) are aged more senior, in the absence of effect within 30-60 minutes it is possible to accept one more capsule (50 mg); at severe pains the single dose can be 100 mg (2 capsules). It is necessary to swallow of capsules without chewing, washing down with necessary amount of liquid, irrespective of meal.
The daily dose should not exceed 400 mg (8 capsules).
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 administration 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 introduction of single doses.
Tramadol should not be appointed longer, than it therapeutic is necessary.

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.
It is forbidden to take alcohol at treatment.
Do not apply to therapy of a syndrome of "cancellation" of narcotic substances.
In case of one-time reception there is no need to interrupt feeding with a breast.
At use of drug it is necessary to abstain from driving of the car and occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

- From cardiovascular system: tachycardia, orthostatic hypotension, syncope, collapse.
- From the alimentary system: dryness in a mouth, nausea, vomiting, a meteorism, abdominal pains, a lock, diarrhea, difficulty when swallowing.
- 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 maintaining in high doses or at co-administration of antipsychotic means), a depression, amnesia, disturbance of cognitive function, paresthesia, instability of gait.
- 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 – development of a syndrome of "cancellation" is not excluded.

Interaction with other medicines:

Strengthens effect of ethanol and the means exerting the oppressing impact on TsNS.
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, duration of anesthesia increases at a combination with barbiturates.
Naloxonum activates breath, eliminating an analgesia after use of opioid analgetics. MAO inhibitors, furasolidone, Procarbazinum, neuroleptics can cause risk of development of spasms (decrease in a convulsive threshold).
Quinidine increases concentration in a blood plasma 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).

- 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.
- 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 a craniocereberal injury, the increased intracranial pressure, to patients with epilepsy, 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").

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 25 °C 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:

On 10 capsules in a blister strip packaging from polypropylene / aluminum foil or PVC / aluminum foil.
On 1, either 2, or 3, or 5, or 10 blister strip packagings with the application instruction in a cardboard pack.