Tramadol treatment. Tramadol instructions for use, contraindications, side effects, reviews
Registration number: P No. 014048/03-2002
Trade name of the drug: Tramadol Lannacher
International non-proprietary name:
Tramadol hydrochlorideChemical rational name: (±)trans-2-[(dimethylamino)methyl]-1-(3-methoxy-phenyl)-cyclohexanol hydrochloride
Dosage form: Solution for injection in ampoules 50 mg / ml and 100 mg / 2 ml.
Composition:
1 ml of solution contains 50 mg of tramadol hydrochloride.
Excipients: sodium acetate, water for injection.
Description: Colorless, transparent liquid.
Pharmacotherapeutic group: Analgesic opioid. ATC code: .
Pharmacological properties
Tramadol hydrochloride is a centrally acting analgesic. It has a pronounced analgesic effect.
Indications for use
Pain syndrome of moderate and severe intensity of various etiologies:
Opioid analgesic, a derivative of cyclohexanol.
Drug: TRAMADOL
The active substance of the drug:
tramadol
ATX encoding: N02AX02
CFG: Opioid analgesic with a mixed mechanism of action
Registration number: P No. 011409/01
Date of registration: 20.09.04
The owner of the reg. credit: ZENTIVA a.s. (The Slovak Republic)
Tramadol release form, drug packaging and composition.
Capsules white, opaque; the contents of the capsules are white powder. 1 caps. tramadol hydrochloride 50 mg
Excipients: anhydrous calcium hydrogen phosphate, magnesium stearate, colloidal silicon dioxide.
The composition of the capsule shell: gelatin, titanium dioxide.
10 pieces. - blisters (1) - packs of cardboard.
10 pieces. - blisters (2) - packs of cardboard.
The solution for injection is clear, colorless, odorless. 1 ml tramadol hydrochloride 50 mg
1 ml - ampoules (5) - plastic containers (1) - cardboard packs.
1 ml - ampoules (5) - plastic containers (2) - cardboard packs.
1 ml - ampoules (5) - plastic containers (20) - cardboard packs.
The solution for injection is clear, colorless, odorless. 1 ml 1 amp. tramadol hydrochloride 50 mg 100 mg
Excipients: sodium acetate, water for injection.
2 ml - ampoules (5) - plastic containers (1) - cardboard packs.
2 ml - ampoules (5) - plastic containers (2) - cardboard packs.
2 ml - ampoules (5) - plastic containers (20) - cardboard packs.
DESCRIPTION OF THE ACTIVE SUBSTANCE.
All the information provided is provided only for familiarization with the drug, you should consult a doctor about the possibility of using it.
Pharmacological action Tramadol
Opioid analgesic, a derivative of cyclohexanol. Non-selective agonist of mu-, delta- and kappa receptors in the CNS. It is a racemate of (+) and (-) isomers (50% each), which are involved in analgesic effects in various ways. Isomer(+) is a pure opioid receptor agonist, has a low tropism and does not have a pronounced selectivity for various receptor subtypes. Isomer (-), inhibiting the neuronal uptake of norepinephrine, activates descending noradrenergic influences. Due to this, the transmission of pain impulses to the gelatinous substance of the spinal cord is disrupted.
Causes a sedative effect. In therapeutic doses, it practically does not depress breathing. It has an antitussive effect.
Pharmacokinetics of the drug.
After oral administration, it is rapidly and almost completely absorbed from the gastrointestinal tract (about 90%). Cmax in plasma is achieved 2 hours after ingestion. Bioavailability at a single dose is 68% and increases with repeated use.
Plasma protein binding - 20%. Tramadol is widely distributed in tissues. Vd after oral administration and intravenous administration is 306 liters and 203 liters, respectively. Penetrates through the placental barrier at a concentration equal to the concentration of the active substance in plasma. 0.1% is excreted in breast milk.
It is metabolized by demethylation and conjugation to 11 metabolites, of which only 1 is active.
Excreted by the kidneys - 90% and through the intestines - 10%.
Indications for use:
Moderate and severe pain syndrome of various origins (including with malignant tumors, acute infarction myocardium, neuralgia, trauma). Conducting painful diagnostic or therapeutic procedures.
Dosage and method of application of the drug.
For adults and children over 14 years of age, a single dose when taken orally - 50 mg, rectally - 100 mg, intravenously slowly or intramuscularly - 50-100 mg. If the effectiveness of parenteral administration is insufficient, then after 20-30 minutes, oral administration at a dose of 50 mg is possible.
For children aged 1 to 14 years, the dose is set at the rate of 1-2 mg / kg.
The duration of treatment is determined individually.
Maximum dose: adults and children over 14 years of age, regardless of the route of administration - 400 mg / day.
Side effects of Tramadol:
From the side of the central nervous system: dizziness, weakness, drowsiness, confusion; in some cases, seizures of cerebral genesis (with intravenous administration in high doses or with the simultaneous appointment of antipsychotics).
From the side cardiovascular systems s: tachycardia, orthostatic hypotension, collapse.
From the side digestive system: dry mouth, nausea, vomiting.
On the part of metabolism: increased sweating.
From the musculoskeletal system: miosis.
Contraindications to the drug:
Acute intoxication with alcohol and drugs that have a depressant effect on the central nervous system, children under 1 year of age, hypersensitivity to tramadol.
Use during pregnancy and lactation.
During pregnancy, prolonged use of tramadol should be avoided due to the risk of developing addiction in the fetus and the occurrence of withdrawal syndrome in the neonatal period.
If necessary, use during lactation ( breastfeeding) it must be borne in mind that tramadol is excreted in breast milk in small quantities.
Special instructions for the use of Tramadol.
Caution should be used in convulsions of central origin, drug dependence, confusion, in patients with impaired renal and hepatic function, as well as in hypersensitivity to other opioid receptor agonists.
Tramadol should not be used longer than is therapeutically justified. In the case of long-term treatment, the possibility of developing drug dependence cannot be ruled out.
Not recommended for the treatment of drug withdrawal syndrome.
Combination with MAO inhibitors should be avoided.
Avoid drinking alcohol during treatment.
Tramadol extended-release formulations should not be used in children under 14 years of age.
Influence on the ability to drive vehicles and control mechanisms
During the period of tramadol use, it is not recommended to engage in activities that require increased attention, a high speed of psychomotor reactions.
Interaction of Tramadol with other drugs.
With simultaneous use with drugs that have a depressant effect on the central nervous system, with ethanol, an increase in the inhibitory effect on the central nervous system is possible.
With simultaneous use with MAO inhibitors, there is a possibility of developing serotonin syndrome.
When used simultaneously with serotonin reuptake inhibitors, tricyclic antidepressants, antipsychotics, other means that reduce the threshold of convulsive readiness, the risk of developing seizures increases.
With simultaneous use, the anticoagulant effect of warfarin and phenprocoumon is enhanced.
With simultaneous use with carbamazepine, the concentration of tramadol in the blood plasma and its analgesic effect decrease.
With simultaneous use with paroxetine, cases of the development of serotonin syndrome, seizures are described.
With simultaneous use with sertraline, fluoxetine, cases of the development of serotonin syndrome are described.
With simultaneous use, there is a possibility of a decrease in the analgesic effect of opioid analgesics. Long-term use of opioid analgesics or barbiturates stimulates the development of cross-tolerance.
Naloxone activates respiration, eliminating analgesia after the use of opioid analgesics.
Tramadol
International non-proprietary name
Tramadol
Dosage form
Capsules 50 mg
Composition
1 capsule contains
active substance- tramadol hydrochloride in terms of 100% substance 50 mg
Excipients: lactose monohydrate, magnesium stearate
composition of the capsule shell: brilliant black PN (E 151), patent blue (E 131), quinoline yellow (E 104), erythrosine (E 127), titanium dioxide
(E 171), gelatin.
Description
Hard gelatin capsules with a green body and cap, cylindrical shape, size No. 2. The contents of the capsule are white powder.
Pharmacotherapeutic group
Analgesics. Opioids. Opioids are different. Tramadol
ATX code N02A X02
Pharmacological properties
Pharmacokinetics
When taken orally, more than 90% of tramadol is absorbed in the gastrointestinal tract. The maximum plasma concentration is reached after 4.8 hours. Absolute bioavailability - 68%. Binding to plasma proteins - 20%. Penetrates through the blood-brain and placental barriers. 0.1% of the drug penetrates into breast milk. Metabolized in the liver. The half-life is 6 hours. Tramadol hydrochloride and its metabolites are excreted by the kidneys (25-35%) unchanged. Approximately 7% is excreted by hemodialysis.
There was an increase in the half-life in patients older than 75 years.
Pharmacodynamics
Tramadol is a centrally acting analgesic. It has a mixed mechanism of action. It is a non-selective mu-, delta- and kappa-receptor opioid agonist. Other mechanisms that are involved in providing the analgesic effect of tramadol hydrochloride are the inhibition of the reuptake of noradrenaline in neurons and the enhancement of the serotonergic response.
It opens K + and Ca ++ channels, causes membrane hyperpolarization and inhibits the conduction of pain impulses. The analgesic effect is due to a decrease in the activity of the nociceptive and an increase in the antinociceptive system of the body. Tramadol hydrochloride has an antitussive effect. At therapeutic doses, tramadol hydrochloride does not depress respiration and does not affect intestinal motility.
Indications for use
Acute and chronic pain syndrome of moderate and significant severity (pre- and postoperative periods, malignant tumors, injuries, neuralgia)
Dosage and administration
The doctor determines the dose and duration of treatment individually, based on the intensity of the pain syndrome.
Adults appoint inside (with a small amount of liquid, regardless of food intake) 1 capsule (50 mg). At severe pain a single dose may be 2 capsules (100 mg).
The daily dose should not exceed 5-6 capsules. Dosing frequency should not be more than every 4 hours.
The drug should not be used longer than the period justified from a therapeutic point of view. Patients with moderate hepatic / renal dysfunction, as well as the elderly, doses are selected individually.
In moderate hepatic insufficiency, it is recommended to reduce the dose or increase the interval between doses.
With moderate kidney failure it is advisable to increase the interval between doses. For patients with creatinine clearance less than 30 ml / min, the interval should be increased to 12 hours. In such cases, the maximum recommended daily dose is 200 mg. In connection with possible development Tramadol addiction treatment should be short-term and intermittent. The potential benefit of long-term therapy should be carefully reviewed to ensure that it outweighs the risk of dependence.
Side effects
-
Dry mouth
Change in appetite
-
Flatulence
Pain in the epigastrium
-
Infrequently:
Tachycardia
Feeling the heartbeat
Decreased blood pressure to the point of collapse (orthostatic collapse)
Seldom:
Weakness
lethargy
Reducing the rate of reactions
Sleep disturbance
Nightmares
Euphoria
hallucinations
Anxiety
Emotional lability
Depression
Amnesia
Paresthesia
Drowsiness
epileptiform seizures
-
Respiratory depression
Impaired coordination and speech
Syncope
Confusion
Anxiety
Visual impairment, taste
midriaz
Bradycardia
Increase in blood pressure
Muscle spasm
Involuntary muscle contraction
muscle weakness
Frequency unknown:
Increased levels of liver enzymes
- hives
- itching
- exanthema
- bullous rash
- angioedema
- anaphylactic reactions
- difficulty urinating
- dysuria
- urinary retention
- dyspnea
- worsening of bronchial asthma
- bronchospasm
- violation menstrual cycle
- fatigue
- drug dependence in patients prone to drug abuse, as well as with prolonged use of large doses of the drug.
Abrupt withdrawal after prolonged use of the drug can cause withdrawal syndrome (manifestations similar to withdrawal symptoms narcotic drugs: psychomotor agitation, anxiety, irritability, insomnia, tremor, paresthesia, phobia attacks, hallucinations, confusion, depersonalization, paranoia, tinnitus, side effects gastrointestinal tract).
Often:
- increased sweating
- headache
- dizziness
Nausea
Contraindications
Hypersensitivity to active substance or to other components of the drug
Acute alcohol intoxication
Acute poisoning with sleeping pills, analgesics or psychotropic drugs
severe liver failure
Severe renal failure (creatinine clearance less than 10 ml/min)
Epilepsy with frequent seizures
The period of treatment with MAO inhibitors and the next 14 days after their cancellation
Not used to treat opioid dependence
Pregnancy or lactation
Children's age up to 18 years
Drug Interactions
With the simultaneous appointment of Tramadol with drugs that depress the central nervous system, mutual enhancement of central effects, including respiratory depression, is possible.
Inducers of microsomal oxidation (carbamazepine, barbiturates) reduce the severity of the analgesic effect and the duration of action. Long-term use of opioid analgesics or barbiturates stimulates the development of cross-tolerance.
Anxiolytics increase the severity of the analgesic effect, the duration of anesthesia increases when combined with barbiturates. Naloxone activates respiration, stopping analgesia after the use of opioid analgesics. When used together with MAO inhibitors and within 14 days after their withdrawal, furazolidone, procarbazine and antipsychotics, there is a risk of convulsions.
Quinidine increases the plasma concentration of tramadol and reduces the content of the M1 metabolite due to competitive inhibition of the CYP2D6 isoenzyme.
With the simultaneous use of Tramadol and warfarin, the risk of side effects from the blood coagulation system increases. Tramadol can cause seizures and/or the development of potentially life-threatening serotonin syndrome when used in conjunction with serotonergic drugs.
Ketoconazole and erythromycin may interfere with the metabolism of tramadol. The clinical significance of this interaction has not been studied.
Ondansetron increases the need for tramadol in patients with postoperative pain.
special instructions
During treatment with Tramadol, alcohol should not be consumed.
With prolonged use of Tramadol, addiction and drug dependence may develop.
Tramadol should not be used to treat drug withdrawal syndrome.
Special care should be taken when prescribing the drug to patients with head injuries, increased intracranial pressure, moderate renal or hepatic impairment, patients with a tendency to convulsions, as well as patients with hypersensitivity to opiates. The risk of seizures may be higher in patients who use concurrent anticonvulsants with Tramadol. Patients with a history of epilepsy and a tendency to epileptic seizures can be prescribed the drug only if absolutely necessary. Use with caution in the treatment of patients with impaired respiratory function or in the case of simultaneous use of agents that depress the activity of the central nervous system, due to the risk of further respiratory depression.
The drug contains lactose, so patients with rare hereditary forms of galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome should not use the drug.
Application in pediatrics
The drug is not used to treat children under 18 years of age.
Use during pregnancy or lactation
Tramadol crosses the placental barrier, so it is not recommended to use the drug during pregnancy. If there is an indication for opioid analgesic therapy during pregnancy, single use should be limited.
A small amount of Tramadol passes into breast milk, so the drug should not be used during the period of breastfeeding. With a single use, breastfeeding can not be interrupted.
Features of the effect of the drug on the ability to drive vehicles and potentially dangerous mechanisms
When using the drug, you should refrain from driving vehicles and working with other mechanisms, which require increased attention and rapid mental and motor reactions.
Overdose
Symptoms: vomiting, miosis, circulatory disturbances, depression of consciousness (up to coma), convulsions, depression of the respiratory center until complete cessation of breathing.
Treatment aimed at ensuring patency respiratory tract, maintenance of respiration and the function of the cardiovascular system.
The antidote for depression of the respiratory center is naloxone, for convulsions - benzodiazepine. Tramadol is poorly excreted by dialysis, so the separate use of hemodialysis or hemofiltration is not enough.
Release form and packaging
Tramadol is a drug from the group of opioid analgesics with a central mechanism of action, also related to antitussive drugs.
Release form and composition
Tramadol is produced in the form of the following dosage forms:
- capsules: hard gelatin No. 2 with a yellow body and cap, inside the capsules contains white or white with a yellowish tint powder (5, 6, 7, 8 or 10 capsules in a blister pack made of PVC film and aluminum printed lacquered foil, in carton pack 1, 2, 3, 4, 5, 6, 8 or 10 packs; 5, 6, 7, 8, 10, 20, 30, 40, 50 or 10 capsules in a polymer container, in a carton pack 1 container) ;
- tablets: white or white with a slightly yellowish tint (10 or 20 tablets in a blister pack, 1 or 2 packs in a carton box);
- solution for injection: colorless transparent, without noticeable mechanical impurities [1 or 2 ml in a transparent neutral glass ampoule (the ampoule has a color coding ring and a colored dot), in a blister of aluminum foil and PVC films 5 ampoules, 1 blister in a cardboard bundle];
- rectal suppositories: torpedo-shaped with a smooth surface, white, with a subtle odor (5 suppositories in a PVC and polyethylene blister, in a cardboard box 1 or 2 blisters);
- drops: a clear, colorless or slightly brownish solution with a distinct smell of anise and mint (10 ml each in an amber glass bottle, complete with a built-in polyethylene dropper and a polypropylene screw cap with first opening control, 1 bottle in a carton box).
1 capsule of Tramadol contains:
- active ingredient: tramadol - 50 mg;
- auxiliary components: magnesium stearate - 1.5 mg, microcrystalline cellulose - 37.14 mg, milk sugar (lactose monohydrate) - 66.36 mg.
The capsule shell (body and cap) contains: gelatin - up to 100%, titanium dioxide - 2%, sunset yellow dye - 0.0059%, quinoline yellow dye - 0.75%.
1 Tramadol tablet contains:
- active ingredient: tramadol hydrochloride - 50 or 100 mg;
- auxiliary components: potato starch, magnesium stearate, lactose (milk sugar).
1 ml solution for injection Tramadol contains:
- active substance: tramadol hydrochloride - 50 mg;
- auxiliary components: water for injection - up to 1 ml, anhydrous sodium acetate - 2.5 mg.
1 suppository Tramadol contains:
- auxiliary components: witepsol E75 (fat W solid) - 145 mg, witepsol W35 (fat solid) - 900 mg.
1 ml Tramadol drops contains:
- active ingredient: tramadol hydrochloride - 100 mg;
- auxiliary components: sucrose - 200 mg, anise flavor - 0.1 mg, peppermint flavor - 0.1 mg, glycerol - 180 mg, sodium saccharinate dihydrate - 5 mg, propylene glycol - 160 mg, potassium sorbate - 1.64 mg, polysorbate - 201 mg, purified water - up to 1 ml.
Indications for use
- diagnostic and therapeutic manipulations, accompanied by painful sensations;
- pain syndrome of moderate and severe degree of various origin (in the postoperative period, with injuries, pain in patients with oncological diagnoses, myocardial infarction, neuralgia and other conditions).
Contraindications
Capsules and tablets
- epilepsy, not amenable to full medical treatment;
- opioid withdrawal syndrome;
- intoxication with sleeping pills, analgesics, alcohol, opioids or other psychotropic drugs;
- glucose-galactose malabsorption, lactose intolerance, lactase deficiency;
- combination with MAO inhibitors (monoamine oxidase), as well as for 2 weeks after the end of their intake;
- age up to 14 years;
- hypersensitivity to the active substance or auxiliary components of the drug.
Solution for injection, rectal suppositories, drops
- suicidal moods, addiction to the abuse of substances that increase mental activity;
- conditions accompanied by depression of the respiratory center or central nervous system (including poisoning with narcotic analgesics and other psychoactive drugs, sleeping pills, alcohol);
- combination with MAO inhibitors (including linezolid), including a period of 2 weeks after their cancellation;
- epilepsy resistant to drug therapy;
- complex therapy of drug withdrawal syndrome;
- severe renal and / or hepatic insufficiency (creatinine clearance (CC) is less than 10 ml / min);
- glucose-galactose malabsorption, fructose intolerance, sucrase / isomaltase deficiency (for Tramadol drops);
- pregnancy and the period of breastfeeding (use is possible only in case of a threat to life and health);
- age up to 1 year;
- hypersensitivity to tramadol and other analgesics.
Relative contraindications for all dosage forms
With extreme caution, Tramadol should be prescribed for pronounced drug dependence on opioid substances, increased intracranial pressure and traumatic brain injury, as well as for patients with disorders of consciousness of unknown origin.
Relative contraindications for solution for injection, drops and rectal suppositories
- dysfunction of the liver and / or kidneys (CC is 10-30 ml / min);
- combined use with antipsychotics, selective serotonin reuptake inhibitors (some antidepressants and drugs that reduce appetite), narcotic analgesics, tricyclic antidepressants and other tricyclic substances (for example, promethazine), anti-migraine drugs (triptans);
- epilepsy;
- convulsions;
- acute abdominal pain of unknown origin ("acute" abdomen).
Relative contraindications for capsules and tablets
- diagnosed severe intolerance to opioids of non-allergic and allergic genesis;
- state of shock;
- epilepsy and tendency to convulsive seizures (for tablets);
- violations of the functioning of the respiratory center and breathing problems.
Method of application and dosage
Tramadol is taken orally with or without food. The dose depends on the severity of the pain syndrome.
Tramadol should not be used after it is no longer needed. With prolonged therapy with the drug, periodic monitoring of the patient's condition is required to determine the appropriateness of further use of the drug and dose adjustment.
In patients over 75 years of age without a history of hepatic or renal insufficiency, dose adjustment is usually not required. However, in patients of this age group, Tramadol may be excreted from the body more slowly. Therefore, subject to constant monitoring of the patient's condition, an increase in the interval between doses of the drug is allowed. The same is done in case of kidney and / or liver dysfunction: the standard scheme involves taking 50-100 mg of the drug 2 times a day.
The maximum daily dose is 400 mg (for tablets - 300 mg), excluding severe pain in the postoperative period or pain of oncological origin. In the case of the use of Tramadol injection solution, it can be increased to 1600 mg.
Capsules and tablets
Tramadol capsules are swallowed whole, without extracting the contents, without chewing and drinking plenty of liquid. The recommended doses are approximate, it is always necessary to select the minimum dose of the drug, which will give a tangible effect when taken regularly. The duration of treatment varies depending on the condition of the patient. In the treatment of chronic pain syndrome, it is necessary to take the drug strictly according to the scheme prescribed by the specialist.
For adults and adolescents over the age of 14, a single dose of Tramadol should not exceed 50 mg. If the analgesic effect is weak, after 30-60 minutes, 50 mg of the drug is taken again. With severe pain, it is recommended to increase the single dose to 100 mg.
Depending on the intensity of the pain syndrome, the analgesic effect of the drug lasts for 4-6 hours (in the case of tablets - up to 8 hours). In the postoperative period, short-term use of higher doses of Tramadol is allowed.
Injection
Solution for injection Tramadol is administered by infusion, subcutaneously, intramuscularly, intravenously. The dose of the drug is determined individually and changed in accordance with the intensity of pain. The standard reception scheme is as follows:
- adults and children over 14 years old: single dose - 50-100 mg (1-2 ampoules);
- children from 1 to 14 years of age: a single dose - 1-2 mg / kg of body weight, the maximum daily dose should not exceed 4-8 mg / kg of body weight.
Re-introduction of the drug is allowed after 4-6 hours. Intravenously, the drug is administered slowly, at a rate of not more than 1 ml per minute (corresponding to 50 mg of the active substance) or used diluted, mixed with an infusion solution. If the desired therapeutic effect could not be achieved, 20-30 minutes after intravenous administration, you can continue to inject Tramadol at a rate of 12 mg / h or take it orally in the form of tablets or capsules.
Suppositories rectal
Tramadol suppositories are injected directly into the rectum. Immediately after administration, it is recommended to remain in the supine position for 30 minutes.
Adults and adolescents over 14 years of age are prescribed 1 suppository 2 times a day: in the morning and in the evening, preferably after a bowel movement. Before use, the candle must be warmed by holding it in your hand a little. If necessary, the introduction of the suppository is repeated after 1-2 hours. It is unacceptable to exceed the maximum daily dose (4 suppositories).
In patients on hemodialysis, the drug is not canceled even on the day of dialysis. In patients with cirrhosis of the liver, the recommended maximum daily dose of 100 mg (1 suppository) should not be exceeded.
Drops
For adults and adolescents over 12 years of age, the standard single dose is 20-40 drops (corresponding to 50 mg of tramadol). If the analgesic effect is not sufficiently pronounced, after 30-60 minutes, 50 mg of Tramadol is taken again.
With a clearly expressed pain syndrome the initial dose of the drug can be increased to 100 mg (no more than 1 time). The maximum daily dose is 160 drops.
A single dose for children from 1 to 12 years of age should not exceed 1–2 mg/kg, and the maximum daily dose should not exceed 4–8 mg/kg. A typical treatment regimen for patients of this age is as follows (in 1 drop - 2.5 mg of tramadol):
- up to 10 kg: 4-8 drops;
- 11-15 kg: 6-12 drops;
- 16-20 kg: 8-16 drops;
- 21-30 kg: 12-24 drops;
- 31-45 kg: 18-36 drops.
Side effects
- general plan: often - increased fatigue;
- cardiovascular system: infrequently - palpitations, orthostatic hypotension, tachycardia, collapse (mainly during physical exertion or intravenous administration); rarely - increased blood pressure, bradycardia;
- immune system: rarely - anaphylactic shock and other allergic reactions (wheezing, shortness of breath, angioedema, bronchospasm);
- digestive system: very often - nausea; often - dryness of the oral mucosa, vomiting, constipation; infrequently - diarrhea, flatulence, a feeling of heaviness in the epigastric region, difficulty swallowing, vomiting, increased activity of liver enzymes; rarely - a change in appetite;
- kidneys and urinary system: rarely - urination disorders (urinary retention, dysuria, difficulty urinating);
- respiratory system: rarely - shortness of breath, respiratory depression (with a significant excess of the recommended doses and the simultaneous use of other drugs that depress the activity of the central nervous system);
- musculoskeletal system: rarely - muscle weakness;
- nervous system: very often - dizziness; often - drowsiness, headaches; rarely - fainting, paresthesia, impaired coordination, involuntary muscle contractions, convulsions (when taking high doses of the drug in combination with drugs that lower the threshold of convulsive activity), tremor; occasionally - speech disorders;
- mental state: rarely - nightmares, sleep disturbances, clouded consciousness, anxiety, hallucinations, impaired perception of reality and cognitive functions, mood changes (dysphoria and euphoria), increased or decreased motor activity; very rarely - paranoia, impaired orientation in time and space, derealization, depersonalization, tinnitus, paresthesia, panic attacks;
- sense organs: rarely - blurred vision; sometimes - mydriasis, taste disorders;
- skin: often - increased sweating; infrequently - urticaria, rash, itching.
Additionally for solution for injection: infrequently - menstrual irregularities, signs of menopause, anorexia; rarely - pulmonary edema; with long-term therapy - drug dependence, after discontinuation - withdrawal syndrome.
When using suppositories, manifestations of diaphoresis are frequent.
special instructions
With prolonged use of Tramadol, addiction and the development of physical and mental dependence are likely. In patients with a tendency to drug abuse or to the development of pharmacological dependence, it is necessary to carry out drug therapy with extremely short courses under medical supervision.
Tramadol should not be used as replacement therapy in patients diagnosed with opioid dependence and is not able to get rid of the opioid withdrawal syndrome.
During the period of taking the drug, administration should be avoided. vehicles and engaging in activities that require concentration and rapid psychomotor reactions, especially while taking Tramadol with other psychotropic drugs.
The active substance of the drug crosses the placenta. Wherein clinical researches do not confirm the safety of tramadol during pregnancy, so its use is not recommended. Long-term drug therapy during pregnancy can cause withdrawal syndrome in the newborn.
During lactation, you should also refuse to use Tramadol or stop breastfeeding, with the exception of a single dose - in this case, breastfeeding is not required.
The use of alcohol during therapy should be excluded.
drug interaction
Tramadol in any dosage form can interact with other drugs or substances, which causes the following effects:
- MAO inhibitors: when tramadol is combined with them or taken for 14 days after the abolition of MAO inhibitors, life-threatening symptoms from the cardiovascular, respiratory and central nervous system;
- drugs that depress the activity of the central nervous system, and alcohol: increased adverse reactions from the central nervous system;
- pre- or postoperative use of antiemetics belonging to the group of 5-HT 3 -serotonin receptor blockers (ondansetron, etc.): an increase in the need for tramadol in patients with a clear postoperative pain syndrome;
- carbamazepine: reducing the analgesic effect of tramadol and reducing its time of action;
- inhibitors of the CYP3A4 isoenzyme (for example, erythromycin, ketoconazole): inhibition of the metabolism of tramadol in the body;
- agonists-antagonists of opioid receptors (pentazocine, nalbuphine, buprenorphine, etc.): decrease in the analgesic effect of tramadol;
- indirect anticoagulants - coumarin derivatives (warfarin, etc.): the risk of bleeding and ecchymosis;
- antipsychotics, selective serotonin reuptake inhibitors, tricyclic antidepressants and other drugs that reduce the threshold for convulsive readiness: increased their action and the possible occurrence of seizures;
- serotonergic drugs: the development of serotonin syndrome (sweating, diarrhea, myoclonus, hyperreflexia, ataxia, hyperthermia, agitation, clouding of consciousness).
Analogues
Analogues of Tramadol tablets are: Tramadol-ratiopharm, Tramaclosidol.
Analogues of Tramadol capsules are: Tramadol GR, Tramadol Retard, Tramadol Stada, Tramadol Akri, Tramadol-ratiopharm, Tramal.
An analogue of rectal suppositories Tramadol is Tramal.
Analogues of Tramadol drops are: Tramadol Shtada, Tramadol-ratiopharm, Tramal.
Analogues of the solution for injection Tramadol are: Tramadol GR, Tramadol Shtada, Tramadol Plethiko, Tramadol-ratiopharm, Tramaclosidol, Tramal, Tramolin.
Tramadol analogues according to the mechanism of action: Palexia, Zaldiar, Tramacet, Omnopon, Ramleps, Forsodol, Prosidol.
Terms and conditions of storage
Store Tramadol capsules, tablets and solution for injection in a dry and dark place at a temperature not exceeding 25 ° C, keep out of the reach of children.
Tramadol rectal drops and suppositories should be stored at a temperature not exceeding 30 ° C in the original packaging, keep out of the reach of children.
The shelf life of Tramadol capsules and tablets is 3 years.
The shelf life of drops, solution for injection and rectal suppositories is 5 years.
Terms of dispensing from pharmacies
Released by prescription.
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Description
Clear, colorless or slightly yellowish solution.
Composition per ampoule
BUTactive substance- tramadol hydrochloride - 50.0 mg / 100.0 mg;
Excipients: sodium acetate trihydrate - 4.98 mg / 9.96 mg, water for injection - up to 1 ml / 2 ml.
Pharmacotherapeutic group
Analgesics, other opioids.
ATC code: N02AX02.
pharmachologic effect
Tramadol is an opioid analgesic with a central mechanism of action. It is a non-selective full agonist of mu-, delta-, kappa-opioid receptors with high affinity for mu-opioid receptors. The second mechanism of action of tramadol, which enhances its analgesic effect, is the suppression of norepinephrine reuptake and increased release of serotonin.
Tramadol has an antitussive effect. In therapeutic doses, it does not depress breathing and practically does not affect intestinal motility. The effect on the cardiovascular system is weakly expressed. The analgesic potential of tramadol is 1/10-1/6 of the activity of morphine.
Indications for use
Pain syndrome of moderate intensity in malignant neoplasms, acute myocardial infarction, trauma, diagnostic and therapeutic procedures, neuralgia.
Dosage and administration
Designed for intravenous, intramuscular, subcutaneous administration. In / in the introduction is carried out by slow injection, preferably into the superficial brachial vein, at a rate of 1 ml / min.
The dose of the drug should be adjusted depending on the intensity of the pain syndrome and the sensitivity of the patient. For pain relief, the lowest effective therapeutic dose should be selected. The duration of the course of treatment is also determined individually, but the drug should not be prescribed beyond the period justified from a therapeutic point of view.
For adults and adolescents over 14 years of age, the usual single dose for intravenous administration is 0.05-0.1 g (50-100 mg). If necessary, in case of insufficient effect, further
injections are possible after 30-60 minutes, up to the maximum possible daily dose. When conducting an intravenous drip infusion, the initial dose of 0.05-0.1 g (50-100 mg) is administered intravenously slowly (over 20 minutes), then a maintenance drip infusion is started at a rate of 12 mg / h up to the maximum possible daily dose, which is 0.4 g (400 mg). The effect lasts an average of 4-8 hours, depending on the nature and intensity of pain.
With intramuscular and s / c administration, the initial dose for adults and children over 14 years of age is usually 0.05-0.1 g (50-100 mg), further injections are possible, if necessary, at a dose of 0.03 g (30 mg) up to the maximum possible daily dose.
The maximum daily dose of the drug should not exceed 0.4 g (400 mg).
Children aged 1 to 14 years are recommended to prescribe tramadol in a single dose at the rate of 1-2 mg / kg, the maximum daily dose should not exceed 4-8 mg / kg. The drug should be diluted with water for injection, while it is necessary to take into account what concentrations of the drug can be obtained in this case (1 ml of the drug contains 0.05 g (50 mg), 2 ml - 100 mg of tramadol). To dilute the drug, you can use water for injection, saline and 5% glucose solution. It is recommended to use freshly prepared solutions. Tramadol solutions can be used within 24 hours of preparation if stored in a refrigerator at 1 to 5 °C.
Calculation of the volume of solution for injection
1. To calculate the total dose of tramadol (mg), you need: body weight (kg) × dose (mg/kg).
2. The volume (ml) of the diluted solution for administration is calculated as follows: divide the total dose (mg) by the corresponding concentration of the diluted solution (mg/ml) (see table below).
In accordance with the calculation, dilute the contents of the ampoule by adding a solvent, mix and inject the calculated volume of the finished solution.
With prolonged use, periodic monitoring is necessary to determine the need for further therapy and optimize the dosing regimen.
Elderly patients
There is usually no need to adjust the dose in patients under 75 years of age without clinical manifestations hepatic/renal failure. In patients older than 75 years, elimination of tramadol may be prolonged. Therefore, if necessary, the interval between doses of the drug should be extended in accordance with the need for pain relief of the patient.
Patients with impaired renal/liver function
In patients with renal / hepatic insufficiency, the excretion of the drug is slowed down. Therefore, the lengthening of the interval between doses of the drug must be carefully monitored in accordance with the need for patient pain relief.
Side effect
The incidence of side effects is given in the following gradation: very often (≥1 / 10); often (≥1/100,
Violations bycardiovascularsystems
Uncommon: Cardiovascular dysregulation (palpitations, tachycardia, postural hypotension or cardiovascular failure). These side effects are observed mainly with intravenous administration of the drug and with significant physical exertion.
Rarely: bradycardia, increased blood pressure.
Metabolic and nutritional disorders
Rarely: change in appetite.
Frequency unknown: hypoglycemia.
ViolationsIfrom the side respiratory system, organs chest and mediastinum Rarely: respiratory depression, shortness of breath.
There was a deterioration in the condition bronchial asthma, however, a causal relationship with the use of the drug has not been established.
Nervous System Disorders
Very common: dizziness.
Often: headache, drowsiness.
Rare: speech disorder, paresthesia, tremor, respiratory depression, epileptiform convulsions, involuntary muscle contractions, impaired coordination, syncope.
Convulsions are possible with the simultaneous use of high doses of tramadol and medicines lowering the seizure threshold.
Mental disorders
Rare: hallucinations, confusion, sleep disturbance, anxiety, delirium, restlessness and nightmares.
After the use of tramadol, various rarely observed adverse reactions from the psyche are possible (depending on the personality characteristics of the patient and the duration of treatment). These adverse drug reactions include mood changes (usually euphoria, sometimes dysphoria), changes in motor activity (usually decreased, sometimes increased), cognitive and perceptual impairment (eg, decision-making, perceptual disturbance). Perhaps the development of drug dependence. Possible withdrawal symptoms are similar to those of opioid withdrawal: agitation, anxiety, nervousness, sleep disturbances, hyperkinesia, tremors, and gastrointestinal symptoms. Other symptoms that are very rare with tramadol withdrawal include: panic attacks, severe anxiety, hallucinations, paresthesias, tinnitus and other very rare CNS symptoms (disorientation in time and space, hallucinations, depersonalization, derealization, paranoia).
From the organ of vision
Rare: blurred vision, miosis, mydriasis.
From the gastrointestinal tract
Very common: nausea.
Often: vomiting, constipation, dry mouth.
Infrequently: vomiting, feeling of heaviness in the epigastrium, flatulence, diarrhea.
ViolationsIfrom the skin and subcutaneous tissues
Often: increased sweating.
Uncommon: skin reactions (eg, pruritus, erythema, urticaria).
Musculoskeletal and connective tissue disorders
Rare: muscle weakness.
ViolationsIfrom the liver and biliary tract
In some cases, an increase in the activity of liver enzymes was observed, which coincided in time with tramadol therapy.
ViolationsIfrom the kidneys and urinary tract
Rarely: violation of urination (dysuria and urinary retention).
ViolationsIfrom the immune system
Rare: allergic reactions (shortness of breath, bronchospasm, wheezing, angioedema) and anaphylaxis.
From the reproductive system
Not known: decreased libido, impotence, erectile dysfunction, lack of menstruation, infertility. In the event of the development of these adverse reactions, it is necessary to evaluate the level of sex hormones.
When tramadol is used concomitantly with serotonergic medicinal products, patients should be closely monitored if the following symptoms develop: agitation, hallucinations, palpitations, fever, increased sweating, chills or tremors, muscle twitching (muscle cramps) or rigidity (stiffness), impaired coordination, nausea, vomiting, or diarrhea (see Precautions section - Serotoninsyndrome).
General disorders and disorders at the injection site
Often: fatigue.
If any of the above adverse reactions or adverse reactions not listed in this leaflet occur, medical use medication, you should consult a doctor.
Contraindications
hypersensitivity to tramadol or any of the excipients; acute intoxication with alcohol, sleeping pills, analgesics, opioid or psychotropic drugs; epilepsy; dysfunction of the liver and kidneys; pregnancy, breastfeeding period; children's age up to 1 year; simultaneous use of monoamine oxidase inhibitors (MAO) and within 14 days after their cancellation; the use of tramadol as a drug for the treatment of drug withdrawal syndrome.
FROM caution. Use with caution in patients prone to substance abuse.
Overdose
With an overdose of tramadol, symptoms characteristic of narcotic analgesics should be expected.
Symptoms: miosis, convulsions, collapse, coma, depression of the respiratory center, apnea.
Treatment: ensuring the patency of the respiratory tract, maintaining adequate pulmonary ventilation, maintaining the activity of the cardiovascular system, symptomatic therapy (opiate effects can be stopped with naloxone; convulsions - benzodiazepines [diazepam]). With chronic tramadol poisoning, withdrawal symptoms may develop. Hemodialysis and hemofiltration are ineffective in case of overdose.
Precautionary measures
Do not use for the treatment of drug withdrawal syndrome. Ethanol should not be consumed at the same time.
Use during pregnancy and lactation
Tramadol crosses the placental barrier. There is no convincing evidence for the safety of tramadol during pregnancy in humans, so tramadol should not be used during pregnancy. Prolonged use of tramadol during pregnancy may lead to withdrawal symptoms in the newborn. About 0.1% of the dose of tramadol administered to the mother is excreted in milk during breastfeeding. Tramadol should not be used during breastfeeding. After a single dose of tramadol, there is no need to interrupt breastfeeding.
With caution, the drug is prescribed to patients with impaired kidney and liver function, with craniocerebral injuries, increased intracranial pressure, patients with epilepsy, with loss of consciousness of unknown origin, impaired function of the respiratory center. The use of tramadol can complicate the diagnosis of acute pain in the abdominal region.
Under close supervision in reduced doses, tramadol should be used against the background of the action of anesthetics, hypnotics, anxiolytics and antidepressants in order to avoid excessive depression of the central nervous system and suppression of the activity of the respiratory center.
With extreme caution, tramadol is used in patients sensitive to opiates. Seizures have been reported in patients receiving tramadol at the recommended dosage. The risk may increase when using a dose higher than the recommended maximum daily dose (400 mg). Tramadol may increase the risk of epileptic seizures when co-administered with drugs that lower the seizure threshold. In patients with epilepsy or who are prone to epileptic seizures, tramadol is used only for health reasons.
Tramadol has a low addiction potential. With prolonged use, tolerance, mental and physical dependence may develop. In patients prone to drug abuse or addiction, treatment with tramadol should be carried out only for a short period and under the strict supervision of a physician.
The use of tramadol makes it difficult to perform work that requires a high rate of mental and physical reactions and increased concentration of attention (driving vehicles, operating mechanisms, devices, etc.).
Influence on the ability to drive vehicles and other potentially dangerous mechanisms
Even at recommended doses, tramadol can cause effects such as drowsiness, dizziness and therefore may impair the response of car drivers and machine operators. When using the drug Tramadol, it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions, especially when used together with other psychomotor drugs or alcohol.
Serotoninsyndrome: when using tramadol with serotonergic drugs, patients should be carefully monitored if the following symptoms develop: agitation, hallucinations, heart palpitations, fever, increased sweating, chills or tremors, muscle twitches (muscle cramps) or rigidity (stiffness), impaired coordination, nausea, vomiting or diarrhea. Symptoms usually develop within hours to days of starting concomitant opioid therapy with other drugs. However, symptoms may develop later, especially after increasing the dose of drugs. If serotonin syndrome is suspected, the use of opioids and/or other concomitant medications should be discontinued.
Adrenal insufficiency: Patients should be closely monitored if symptoms of adrenal insufficiency such as nausea, vomiting, loss of appetite, fatigue, weakness, dizziness, or low blood pressure. If adrenal insufficiency is suspected, diagnostic testing should be performed. If necessary, with a positive result of the study, it is necessary to start treatment with corticosteroids and stop opioids. If opioids are discontinued, a follow-up evaluation of adrenal function should be performed to determine the need to continue or stop corticosteroid therapy.
Androgenicfailure: chronic use of opioids can affect the hypothalamic-pituitary-gonadal system, which can lead to androgen deficiency, which manifests itself in the form of low libido, impotence, erectile dysfunction, amenorrhea and infertility. If symptoms or signs of androgen deficiency appear, laboratory diagnostics should be performed.
Interaction with other drugs
Tramadol in the form of injection solutions is pharmaceutically incompatible with injection solutionsdiclofenac, indomethacin, phenylbutazone, diazepam, flunitrazepam, midazolam, nitroglycerin.
Tramadol should not be used simultaneously or within 14 days after the abolition of MAO inhibitors. In patients treated with MAO inhibitors within 14 days prior to the start of the use of the opioid analgesic pethidine, life-threatening drug interactions, manifested by symptoms from the central nervous system, respiratory and cardiovascular systems. Similar interactions with MAO inhibitors are possible with the use of tramadol.
Simultaneous use of tramadol and substances that suppress the activity of the central nervous system, including alcohol, may increase adverse reactions from the central nervous system.
It is noted that with simultaneous or previous use cimetidine(inhibitormicrosomalliver enzymes) clinically significant interactions are unlikely. Simultaneous or previous use carbamazepine(inductormicrosomalliver enzymes) may reduce the analgesic effect of tramadol and shorten its duration of action.
Tramadol may cause convulsions and increase the effect selective reuptake inhibitorsserotonin(SSRIs), reuptake inhibitorsserotoninand norepinephrine (ISOSN),tricyclicantidepressants, antipsychotics, and other drugs that lower the seizure threshold (eg,bupropion, mirtazapine) thus leading to the development of seizures.
Simultaneous use of tramadol with other serotonergic drugs, such as SSRIs, SNRIs, MAO inhibitors, tricyclic antidepressants and mirtazapine, can lead to the development of serotonin syndrome, even when using drugs at recommended doses. The likelihood of developing serotonin syndrome exists when one of the following symptoms/syndromes is observed:
Spontaneous muscle clonus; induced or ocular myoclonus with agitation or increased sweating; tremor and hyperreflexia; hypertension, fever > 38 °C, and induced or ocular myoclonus.
If concomitant use of opioids and serotonergic drugs is indicated,
it is necessary to carefully monitor patients, especially at the beginning of therapy and when increasing the dose (see section "Precautions" - Serotoninsyndrome).
If serotonin syndrome is suspected, the use of opioids and / or other concomitant drugs should be discontinued.
Withdrawal of serotonergic drugs causes rapid resolution of symptoms. Necessary therapy is determined clinical picture and severity of symptoms. With the simultaneous use of tramadol and coumarin derivatives (for example,warfarin) it is necessary to carefully monitor patients, as some of them showed an increase in the international normalized ratio (INR) with the development of bleeding and ecchymosis.
Do not use after the expiry date stated on the package.
Package
1 ml or 2 ml in ampoules. 5 ampoules are placed in a blister pack, 1 or 2 blister packs, together with instructions for use, are placed in a pack.
Holiday conditions
On prescription.
Manufacturer
RUE "Belmedpreparaty",
Republic of Belarus, 220007, Minsk,
st. Fabriciusa, 30, t./fa.: (+375 17) 220 37 16,
e-mail: [email protected]