Tramal Retard - Instructions For Use, 100 And 200 Mg, Price Of Tablets

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Tramal retard

Tramal retard: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. For violations of liver function
13. 13. Drug interactions
14. 14. Analogs
15. 15. Terms and conditions of storage
16. 16. Terms of dispensing from pharmacies
17. 17. Reviews
18. 18. Price in pharmacies

Latin name: Tramal retard

ATX code: N02AX02

Active ingredient: tramadol (Tramadol)

Manufacturer: Pharmaceutichi Formenty S.p. A. (Farmaceutici Formenti, SpA) (Italy); Grunenthal GmbH (Germany)

Description and photo update: 2020-20-02

Tramal retard is an analgesic opioid drug with a mixed mechanism of action.

Release form and composition

Tramal retard is available in the form of prolonged-release film-coated tablets:

• dosage of 100 mg: biconvex, round, white, engraved with "T1" on one side and the "~" sign on the other;
• dosage 150 mg: biconvex, round, light orange, engraved with "T2" on one side and the sign "~" on the other;
• dosage 200 mg: biconvex, round, light orange in color with a brownish tint, engraved with "T3" on one side and a "~" sign on the other.

All tablets, regardless of dosage, are packed in blisters of 10 pcs., In a cardboard box 1 blister and instructions for the use of Tramal retard.

Composition for 1 tablet of prolonged action, film-coated:

• active substance: tramadol hydrochloride - 100, 150 or 200 mg;
• auxiliary components: hypromellose 100,000 mPa × s, magnesium stearate, microcrystalline cellulose, colloidal silicon dioxide;
• film shell: macrogol 6000, talc, hypromellose 6 mPa × s, titanium dioxide, lactose monohydrate, propylene glycol; additionally for tablets with a dosage of 150 mg - dye iron oxide red and quinoline yellow dye; additionally for tablets with a dosage of 200 mg - dye iron oxide red, dye quinoline yellow and dye iron oxide brown.

Pharmacological properties

Pharmacodynamics

Tramadol is an opioid analgesic with a central mechanism of action. It is a non-selective full agonist of µ-opioid, δ-opioid and κ-opioid receptors, and also has a high affinity for µ-receptors. The analgesic effect of tramadol is enhanced by the second mechanism of action - suppression of the reuptake of norepinephrine by nerve cells and an increase in the release of the neurotransmitter serotonin.

Tramal retard also has antitussive properties. In therapeutic doses, tramadol, unlike morphine, does not depress respiration, has only a slight effect on intestinal motility and has almost no effect on the cardiovascular system. The analgesic potential of tramadol is 1/10 to 1/6 of the effect of morphine.

Pharmacokinetics

The absorption of the drug is quite high (more than 90% of the substance is absorbed in the gastrointestinal tract). The absolute bioavailability is on average 70%, it does not depend on food intake. Tramadol undergoes the effect of primary passage through the liver, which causes a decrease in bioavailability. After taking a tablet with a dosage of 100 mg, the maximum plasma concentration of tramadol is 141 ± 40 ng / ml and is reached after about 4.9 hours; after taking the Tramal retard 200 mg tablet, the plasma concentration is 260 ± 62 ng / ml and is achieved after 4.8 hours.

The volume of distribution is quite large (203 ± 40 l), the affinity for tissues is high. About 20% of tramadol binds to plasma proteins. The drug passes through the blood-brain barrier and crosses the placenta to the fetus. A small amount of tramadol is secreted with breast milk.

Metabolism occurs with the participation of isoenzymes CYP2D6 and CYP3A4, therefore, when they are suppressed by other pharmacologically active substances, a significant change in the concentration of tramadol and its active metabolite is possible. Tramadol is metabolized in the liver by N- and O-demethylation, and then conjugated with glucuronic acid. Only O-demethyltramadol is pharmacologically active. A total of 11 metabolites were found.

The drug and its metabolites are excreted mainly in the urine. The half-life is 6 hours. In elderly patients (over 75 years old), it can increase by 1.4 times; in patients with liver cirrhosis, the elimination half-life is extended to 13.3 ± 4.9 h (for tramadol) and up to 18.5 ± 9.4 h (for O-demethyltramadol), and in severe cases even more (up to 22.3 h and 36 h). In patients with renal insufficiency (with creatinine clearance less than 5 ml / min), the half-life of tramadol is 11 ± 3.2 hours, O-demethyltramadol is 16.9 ± 3 hours (in severe cases - 19.5 hours and 43.2 hours).

The analgesic effect of tramadol depends on its serum concentration, that is, it is dose-dependent. This ratio varies from individual to individual.

Indications for use

Tramal retard is used for pain syndrome of medium and high intensity of various origins, in particular in patients with oncology, in the postoperative period and in trauma.

Contraindications

Absolute:

• epilepsy that does not respond to adequate drug therapy;
• acute intoxication with analgesics, alcohol, opioids, hypnotics and other psychotropic substances;
• drug withdrawal syndrome (tramadol should not be used to treat this syndrome);
• joint administration with MAO (monoamine oxidase) inhibitors, as well as a period up to 14 days after their cancellation;
• lactose intolerance, lactase enzyme deficiency, glucose-galactose malabsorption syndrome (since the tablets contain lactose);
• period of pregnancy;
• children and adolescents up to 14 years old;
• hypersensitivity to the main or auxiliary components of the drug.

Relative (Tramal retard tablets are used with caution):

• convulsions and epilepsy, amenable to adequate drug therapy (use is possible only for health reasons);
• craniocerebral trauma, impaired consciousness of unclear etiology, respiratory disorders and respiratory disorders, a state of shock, increased intracranial pressure;
• opioid dependence;
• tendency to abuse drugs or drug addiction (therapy should be carried out under the supervision of a doctor and in as short a course as possible);
• established severe intolerance to opioids of non-allergic and allergic origin;
• period of breastfeeding (use is possible, but only one-time and for health reasons).

Tramal retard, instructions for use: method and dosage

Tramal retard tablets are taken orally with a sufficient amount of water or other liquid. They should not be chewed or broken, but should be swallowed whole. Taking the drug does not depend on the time of the meal.

The dose of Tramal retard is selected individually, taking into account the severity of the pain syndrome and the patient's sensitivity to the drug. The doses given below are indicative. It is recommended to select the lowest effective dose of tramadol. With long-term therapy, you should adhere to the established schedule for taking the pills.

Adults and adolescents over 14 years of age are usually prescribed one tablet of Tramal retard 100 mg 2 times a day (morning and evening). In case of insufficient effectiveness, you can increase the dose by increasing the dosage of tablets (for example, take Tramal retard 150 mg or 200 mg). The interval between doses should not be less than 6 hours, and the maximum daily dose should not be more than 400 mg.

In the elderly up to 75 years of age, if there is no clinically expressed renal or hepatic failure, the dose of the drug is usually not adjusted. In patients 75 years of age and older, as well as in patients with impaired liver and / or kidney function, tramadol excretion may be slowed down, which should be taken into account when prescribing it (for example, it is recommended to lengthen the interval between pills). Tramal retard should not be used in patients with severe hepatic or renal impairment.

Side effects

Negative side reactions from systems and organs when taking Tramal retard:

• digestive system: very often - nausea; often - vomiting, dry mouth, constipation; infrequently - bloating, abdominal pain, vomiting, diarrhea;
• hepatobiliary system: isolated cases - increased activity of liver enzymes;
• metabolism and nutrition: rarely - a change in appetite;
• cardiovascular system: infrequently - tachycardia, palpitations, orthostatic hypotension, collapse; rarely - bradycardia, increased blood pressure;
• respiratory system: rarely - shortness of breath, respiratory depression;
• nervous system and psyche: very often - dizziness; often - drowsiness, headache; rarely - coordination disorders, anxiety, sleep disturbances, nightmares, tremors, speech disorders, fainting, involuntary muscle contractions, confusion, epileptiform seizures, paresthesias, hallucinations, delirium, mood lability, changes in activity, impaired perception and cognitive functions, drug dependence;
• organ of vision: rarely - blurred vision, dilated or narrowed pupils;
• urinary system: rarely - urinary retention, dysuria;
• musculoskeletal system: rarely - muscle weakness;
• skin and subcutaneous fat: often - increased sweating; infrequently - urticaria, flushing of the skin, pruritus;
• immune system: rarely - bronchospasm, Quincke's edema, shortness of breath, wheezing, anaphylaxis;
• other reactions: often - fatigue; frequency unknown - hypoglycemia.

When Tramal retard therapy is discontinued, withdrawal symptoms may occur, which are similar to the withdrawal symptoms of other opioids: nervousness, tremors, anxiety, sleep disturbances, agitation, hyperkinesia, and disorders of the digestive system. Also, when tramadol is discontinued, in very rare cases, symptoms such as severe anxiety, panic attacks, ringing in the ears, paranoia, paresthesia, confusion, depersonalization and hallucinations occur.

Overdose

In case of an overdose of tramadol, symptoms may appear that are characteristic of narcotic analgesics (vomiting, constriction of the pupil, depression of the respiratory center up to apnea, collapse, convulsions, disturbances of consciousness and even coma).

In the first 2 hours after an overdose, the patient is washed with a stomach and given activated charcoal. The patient should be provided with airway patency. Measures are being taken to maintain the activity of the respiratory and cardiovascular systems. For seizures, intravenous diazepam is recommended. Hemofiltration and hemodialysis are ineffective.

special instructions

The maximum recommended daily dose of Tramal retard (400 mg) should not be exceeded, as this increases the risk of seizures. The likelihood of seizures increases with simultaneous use with drugs that lower the seizure threshold. For patients with epilepsy and a predisposition to seizures, the drug is prescribed exclusively for health reasons.

Tramadol has a rather low potential for drug dependence. But despite this, with long-term therapy, mental and physical dependence, as well as addiction, are possible. Tramal retard should not be used as a substitution therapy in opioid-dependent patients, since tramadol cannot suppress morphine withdrawal symptoms, even though it is an opioid receptor agonist.

Influence on the ability to drive vehicles and complex mechanisms

Tramal retard can cause dizziness and drowsiness, therefore, when taking the drug, you must refrain from driving and other vehicles, as well as performing potentially dangerous and difficult work.

Application during pregnancy and lactation

Tramal retard is contraindicated during pregnancy, since reliable evidence of its safety for the growth and development of the fetus has not been obtained. With long-term use of tramadol during pregnancy, the newborn may experience withdrawal symptoms. Also, the drug can cause a clinically insignificant change in respiratory rate in newborns.

The amount of tramadol entering the breast milk of a lactating woman is insignificant and amounts to about 0.1% of the dose taken, therefore, after a single dose of Tramal retard during lactation, there is no need to stop breastfeeding.

Pediatric use

Tramal retard should not be prescribed to children under 14 years of age.

With impaired renal function

The drug is not recommended for use in patients with severe renal impairment. For mild to moderate renal impairment, an individual selection of the interval between pills is required.

For violations of liver function

Tramadol is undesirable for patients with severe hepatic impairment. With mild and moderate impairment of liver function, the interval between doses of Tramal retard should be increased.

Drug interactions

Tramal retard is contraindicated to be used in conjunction with MAO inhibitors or within 14 days after their cancellation (life-threatening drug interactions from the respiratory, cardiovascular and nervous systems may occur).

Alcohol and substances that suppress the activity of the central nervous system can increase the unwanted side effects of tramadol on the nervous system.

Inducers of microsomal liver enzymes can reduce the analgesic properties of Tramal retard and shorten its duration of action.

Tramadol can induce seizures and enhance the effects of tricyclic antidepressants, selective serotonin reuptake inhibitors, antipsychotics, serotonin-norepinephrine reuptake inhibitors and other drugs that lower the seizure threshold.

Serotonergic drugs when used together with tramadol can lead to the development of serotonin syndrome, especially if one of the following syndromes / symptoms is present:

• hyperreflexia and tremor;
• spontaneous muscle clonus;
• increased body temperature over 38 ° C, hypertension, ocular or induced myoclonus;
• increased sweating or agitation in conjunction with ocular or induced myoclonus.

Some inhibitors of the isoenzyme CYP3A4 (erythromycin, ketoconazole) can slow down the metabolism of tramadol and its active metabolite.

The use of ondansetron (a 5-HT3 receptor blocker) before or after surgery increased the need for tramadol in people with postoperative pain.

Analogs

Tramal retard analogues are: Tramadol, Tramadol Kalceks, Tramadol-Acri, Tramadol Avexima, Tramadol retard, Tramadol-GR, Tramadol Stada, Tramadol-Pletchiko, Tramal, Tramaclosidol, Tramolin.

Terms and conditions of storage

Keep out of the reach of children. Store at a temperature not exceeding 25 ° C.

The shelf life of the drug is 5 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Tramal retard

According to reviews, Tramal retard is a fairly strong pain reliever that acts very quickly and helps with pain of any intensity and of various origins. Some patients compare the effect of the drug with that of morphine. At the same time, users note that with prolonged use, it is possible to develop strong mental and physical dependence, as well as the appearance of other unwanted side effects.

The price of Tramal retard in pharmacies

The price of Tramal retard 100 mg is 100-155 rubles. for a pack of 10 tablets of prolonged action, film-coated. The actual cost of Tramal retard tablets 200 mg and 150 mg is unknown.

Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!