Tramadol Hydrochloride: Tramadol Description, instructions, price Pharmacy reference Your Medicine

Tramadol Hydrochloride: Tramadol Description, instructions, price Pharmacy reference Your Medicine

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Tramadol Hydrochloride: Tramadol Description, instructions, price Pharmacy reference Your Medicine

Tramadol: description, instruction, price | Pharmacy reference Your medicine

Tramadol: prices and availability in pharmacies of the city, indications for use and contraindications, packaging, dosage, side effects, pharmacokinetics.

Chemical name

trans – (±) – 2 – [(dimethylamino) methyl] – 1 – (3 – methoxyphenyl) cyclohexanol (as hydrochloride)

Description

White crystalline powder, odorless, bitter taste, highly soluble in water and ethanol.

pharmachologic effect

An opioid synthetic analgesic with a central action and action on the spinal cord (facilitates the discovery of K + and Ca2 + channels, causes hyperpolarization of the membranes and inhibits the conduction of pain impulses), enhances the effect of sedative drugs. Activates opiate receptors (mu, delta, kappa) on the pre- and postsynaptic membranes of the afferent fibers of the nociceptive system in the brain and gastrointestinal tract.

Slows the destruction of catecholamines, stabilizes their concentration in the central nervous system.

It is a racemic mixture of 2 enantiomers – dextrorotatory (+) and levorotatory (-), each of which exhibits a different receptor affinity from others.

(+) Tramadol is a selective mu-opioid receptor agonist, and also selectively inhibits the inverse neuronal serotonin uptake.

(-) Tramadol inhibits the reverse neuronal capture of norepinephrine. Mono-O-desmethyltramadol (M1 metabolite) also selectively stimulates mu-opioid receptors.

The affinity of tramadol to opioid receptors is 10 times weaker than that of codeine, and 6000 times weaker than that of morphine. The severity of analgesic action is 5-10 times weaker than morphine.

Analgesic effect due to a decrease in the activity of nociceptive and an increase in the antinociceptive systems of the body.

In therapeutic doses, it does not significantly affect hemodynamics and respiration, does not alter the pressure in the pulmonary artery, and slightly slows down intestinal motility, without causing constipation. It has some antitussive and sedative effects. Inhibits the respiratory center, stimulates the starting area of ​​the vomiting center, the nucleus of the oculomotor nerve.

With prolonged use may develop tolerance.

Analgesic effect develops 15-30 minutes after ingestion and lasts up to 6 hours.

Pharmacokinetics

Absorption – 90%; bioavailability – 68% when administered orally (increased with repeated use), 70% – with rectal intake, with i / m administration of tramadol hydrochloride: – 100%.

TCmax after ingestion of tablets – 2 hours, when taking drops – 1 hour, with i / m administration – 45 minutes, M1 metabolite – 3 hours.

It penetrates the BBB and the placenta, 0.1% is excreted in breast milk.

The volume of distribution is 203 l with intravenous administration and 306 l with oral administration.

Communication with plasma proteins – 20%.

Is Tramadol A Blood Thinner – how to take, effectiveness and feedback

In the liver, it is metabolized by N- and O-demethylation with subsequent conjugation with glucuronic acid. 11 metabolites were detected, of which mono-O-desmethyltramadol (M1) has pharmacological activity. CYP2D6 isoenzyme is involved in the metabolism of the drug.

T1 / 2 in the second phase – 6 h (tramadol), 7.9 h (mono-O-dezmetiltramadol); in patients older than 75 years – 7.4 h (tramadol); in liver cirrhosis – 13.3 ± 4.9 h (tramadol), 18.5 ± 9.4 h (mono-O-dezmetiltramadol), in severe cases – 22.3 h and 36 h, respectively. T1 / 2 with CRF (CC less than 5 ml / min) – 11 ± 3.2 h (tramadol), 16.9 ± 3 h (mono-O-dezmetiltramadol), in severe cases – 19.5 h and 43.2 h, respectively.

Excreted by the kidneys (25-35% unchanged), the average cumulative rate of renal excretion – 94%.

About 7% is excreted through hemodialysis.

Indications for use

Tramadol Hydrochloride for 10 days, recipes

Pain syndrome (strong and moderate intensity, including inflammatory, traumatic, vascular origin).

Pain relief during painful diagnostic or therapeutic interventions.

Contraindications

Hypersensitivity, alcohol poisoning, hypnotic drugs, narcotic analgesics and other psychoactive drugs, taking MAO inhibitors, risk of suicide, susceptibility to substance abuse, pregnancy, lactation (in case of long-term use), children (up to 1 year for parenteral administration) up to 14 years – for oral administration).

Carefully

Opioid addiction, impaired consciousness of various origins, intracranial hypertension, TBI, epileptic syndrome (cerebral genesis), conditions accompanied by respiratory depression or marked depression of the central nervous system; co-administration with selective serotonin reuptake inhibitors (some antidepressants and appetite-reducing drugs), tricyclic antidepressants, other tricyclic compounds (for example, promethazine), anti-migraine drugs (triptans), narcotic analgesics, MAO inhibitors, neuroleptics, etc. convulsive readiness.

Dosing regimen

In / in, in / m, p / to, inside, rectally.

Dosing: For single use for adults and children over 14 years old – at 0.05 g (tablets, capsules) with a small amount of liquid or 20 drops of the solution (or drops) for ingestion with a small amount of liquid or on sugar. After 30-60 minutes, you can repeat the reception in the same dose, but not more than 8 doses per day.

Retard tablets – 100-200 mg every 12 hours. Daily dose – 0.4 g (in exceptional cases, for example in cancer patients, a reduction in the interval to 6 hours and an increase in the daily dose is possible).

Rectal – 0.1 g. Reception frequency – up to 4 times per day.

In / in slowly, p / k or v / m: 0.05-0.1 g. If the effect is not sufficient, then 20-30 minutes after the intravenous route, infusion can be continued at a rate of 12 mg / h or additionally administered orally. Total daily dose – 0.4 g.

Children over the age of 1 year – inside, only drops or parenteral (IV, IM, P / C), at a dose of 1-2 mg / kg. The daily dose is 4-8 mg / kg (1 cap – 2.5 mg).

The elderly and patients with renal insufficiency require an individual dosage (T1 / 2 lengthening is possible). When QA is less than 30 ml / min and in patients with liver failure, a 12-hour interval is necessary between taking the next dose of the drug.

Side effect

Nervous system disorders: hyperhidrosis, dizziness, headache, weakness, fatigue, lethargy, paradoxical stimulation of the CNS (nervousness, agitation, anxiety, tremor, muscle spasms, euphoria, emotional lability, hallucinations), drowsiness, sleep disorders, confusion , impaired motor coordination, convulsions of central genesis (with intravenous administration in high doses or with simultaneous administration of tramadol hydrochloride: antipsychotic drugs (neuroleptics), depression, amnesia, cognitive impairment valued function, paresthesia, 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 cardiovascular system: manifestations of vasodilation – tachycardia, orthostatic hypotension, syncope, collapse.

Allergic reactions: urticaria, pruritus, rash, bullous rash.

On the part of the urinary system: difficulty urinating, dysuria, urinary retention.

From the senses: visual impairment, taste.

On the part of the respiratory system: dyspnea.

Other: irregular menstruation.

With prolonged use – drug dependence. When abruptly canceled – ‘cancellation’ syndrome.

Overdose

Symptoms: miosis, vomiting, collapse, coma, convulsions, depression of the respiratory center, apnea.

5 tips from Tramadol Hydrochloride

Treatment: ensuring the airway, maintaining breathing and the activity of the cardiovascular system. Opiate-like effects can be stopped by naloxone, seizures by benzodiazepine.

Interaction

Pharmaceutically incompatible with solutions of diclofenac, indomethacin, phenylbutazone, diazepam, flunitrazepam, nitroglycerin.

Enhances the effect of drugs that inhibit the central nervous system, and ethanol.

Inductors of microsomal oxidation (including carbamazepine, barbiturates) reduce the severity of the analgesic effect and the duration of action. Because of the increased risk of seizures, the simultaneous use of carbamazepine and tramadol is not recommended.

Prolonged tramadol hydrochloride: the use of opioid analgesics or barbiturates stimulates the development of cross-tolerance.

Anxiolytics increase the severity of the analgesic effect; the duration of anesthesia is increased when combined with barbiturates.

Naloxone activates respiration, eliminating analgesia after the use of opioid analgesics.

MAO inhibitors, furazolidone, procarbazine, antipsychotic drugs (neuroleptics) increase the risk of seizures (decrease in convulsive tramadol hydrochloride: threshold).

Quinidine increases the plasma concentration of tramadol and reduces the metabolite M1 due to competitive inhibition of the CYP2D6 isoenzyme.

Inhibitors of the isoenzyme CYP2D6 (such as fluoxetine, paroxetine and amitriptyline) reduce the metabolism of tramadol.

Selective serotonin reuptake inhibitors (some antidepressants and appetite-reducing drugs), tricyclic antidepressants, other tricyclic compounds (for example, promethazine), anti-migraine drugs (triptans), narcotic analgesics, MAO inhibitors, neuroleptics, etc. Medicines, anti-inflammatory drugs, triggered anti-depressants, anti-depressants increase the risk of seizures.

Selective serotonin reuptake inhibitors, serotonin and norepinephrine reuptake inhibitors, tricyclic antidepressants, MAO inhibitors, anti-migraine drugs (triptans) and drugs that disrupt tramadol metabolism (CYP2D6 and CYP3A4 isoenzymes inhibitors), I can use a default, and I will be able to use this time to use it.

special instructions

Do not use for the treatment of drug withdrawal syndrome.

Do not use ethanol at the same time.

In the case of a single dose there is no need to interrupt breastfeeding.

During the period of treatment, care must be taken when driving and engaging in other potentially hazardous activities that require increased concentration and psychomotor reactions.

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