Zaldiar
Zaldiar: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Zaldiar
ATX code: N02AX52
Active ingredient: paracetamol (paracetamol) + tramadol (tramadol)
Producer: Farmaceutici Formenti (Italy), Grunenthal (Germany)
Description and photo update: 2019-18-09
Prices in pharmacies: from 904 rubles.
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Zaldiar is a combined drug with an analgesic effect.
Release form and composition
Zaldiar is produced in the form of film-coated tablets: oblong, biconvex, light yellow, at the break - almost white: on one side - engraving "T5", on the other - the logo of the company "Grunental" (10 pcs. In blisters, 1-3 or 5 blisters in a cardboard box).
The composition of 1 tablet contains active substances:
- Tramadol - 37.5 mg (in the form of hydrochloride);
- Paracetamol - 325 mg.
Auxiliary components: microcrystalline cellulose, pregelatinized starch, sodium starch glycolate, corn starch, purified water, magnesium stearate.
Shell composition: Opadry light yellow YS-1-6382-G (hypromellose, polysorbate, titanium dioxide, macrogol (polyethylene glycol 400), iron oxide yellow dye), carnauba wax.
Pharmacological properties
Pharmacodynamics
Zaldiar is a combined drug with an analgesic effect, due to the properties of its active components:
- tramadol: is a synthetic opioid analgesic, opioid receptor agonist. The mechanism of action is based on the activation of opioid receptors (mu-, delta-, kappa-) in the brain and gastrointestinal tract on the pre- and postsynaptic membranes of the afferent fibers of the nociceptive system. It affects the brain and spinal cord, promotes the opening of K + - and Ca 2+ -channels, causes hyperpolarization of membranes and inhibition of pain impulses. Enhances the effects of sedative drugs;
- paracetamol: is an antipyretic analgesic. It blocks cyclooxygenase in the central nervous system, affecting the centers of thermoregulation and pain. Irritation of the intestinal and stomach mucosa does not cause, does not affect water-salt metabolism (due to the fact that it does not affect the synthesis of prostaglandins in peripheral tissues).
Paracetamol provides a rapid onset of analgesic action, and tramadol is required to prolong analgesia. Due to the synergism of the analgesic effect of the two active components, the likelihood of adverse reactions is reduced.
Pharmacokinetics
The active components of Zaldiar after oral administration are rapidly and almost completely absorbed in the gastrointestinal tract. Paracetamol is absorbed faster than tramadol.
C max (maximum concentration of the substance) of paracetamol in blood plasma is achieved in 1 hour, while in combination with tramadol this indicator does not change. The bioavailability of tramadol is about 75%, with repeated use it increases to 90%.
The connection of paracetamol with plasma proteins is insignificant (up to 20%). Tramadol binds to plasma proteins by about 20%, Vd (volume of distribution) is about 0.9 l / kg.
The process of metabolism of tramadol occurs in the liver by O- and N-demethylation, followed by conjugation with glucuronic acid. One of the 11 identified metabolites, mono-O-desmethyltramadol (M 1), has pharmacological activity. The metabolism of paracetamol occurs mainly in the liver.
The average T 1/2 (half-life) of the metabolite of tramadol is in the range from 4.7 to 5.1 hours, T 1/2 of paracetamol is 2-3 hours.
Excretion of tramadol and its metabolites (about 30% and 60%, respectively) is carried out mainly in the urine. In the same way, paracetamol with its conjugates is excreted.
Indications for use
- Pain syndrome of various etiologies, including vascular, traumatic, inflammatory origin (moderate and severe intensity);
- Pain relief during painful therapeutic or diagnostic procedures.
Contraindications
- Acute intoxication with alcohol or drugs that depress the central nervous system (psychotropic and hypnotic drugs, opioid analgesics);
- Severe hepatic and / or renal failure (with creatinine clearance less than 10 ml per minute);
- Drug withdrawal syndrome;
- Treatment-uncontrolled epilepsy;
- Simultaneous use with monoamine oxidase inhibitors and for 14 days after their withdrawal;
- Age under 14;
- Pregnancy and lactation;
- Hypersensitivity to drug components.
According to the instructions, Zaldiar should be used with caution in patients over 75 years old, as well as in the following diseases / conditions:
- Confusion of consciousness of unknown etiology;
- Symptom complex "acute" abdomen of unknown origin;
- States of shock;
- Intracranial hypertension;
- Traumatic brain injury;
- Tendency to convulsive syndrome (with therapeutically controlled epilepsy, Zaldiar can be used only for health reasons);
- Respiratory dysfunction;
- Benign hyperbilirubinemia;
- Diseases of the biliary tract;
- Deficiency of glucose-6-phosphate dehydrogenase;
- Viral hepatitis;
- Alcoholism, drug addiction;
- Alcoholic liver damage;
- Simultaneous use with psychotropic drugs, local anesthetics and other central analgesics.
Instructions for use of Zaldiar: method and dosage
Zaldiar is taken orally, swallowing whole, without chewing, without breaking and washing it down with liquid. The tablets can be taken with or without food. If the patient has forgotten to take a pill, do not double the next dose.
The doctor sets the duration of therapy and the dosage regimen individually, depending on the severity of the pain syndrome and sensitivity to the action of the drug. It is not recommended to prescribe Zaldiar beyond the period justified from a therapeutic point of view.
For adults and children over 14 years old, Zaldiar is prescribed in an initial single dose of 1-2 tablets. Between the receptions of single doses, an interval of at least 6 hours must be observed. The maximum dose is 8 tablets per day.
Elderly patients (over the age of 75) do not need to adjust a single dose. However, due to the possibility of delayed elimination of active substances of Zaldiar, the interval between single doses should be increased.
For patients with functional impairment of the kidneys (with creatinine clearance of 30-10 ml per minute), the interval between single doses should be at least 12 hours. Since tramadol is excreted very slowly during hemodialysis or hemofiltration, post-dialysis use of Zaldiar to maintain the analgesic effect is usually not required.
In case of moderate violations of liver function, the interval between taking single doses of the drug should be increased. In case of severe liver dysfunction, Zaldiar is contraindicated.
Side effects
During the reception of Zaldiar, disorders may develop from some body systems, which manifest themselves with different frequencies:
- Digestive system: diarrhea, dry mouth, abdominal pain, nausea, difficulty swallowing, flatulence, vomiting, constipation, increased activity of liver enzymes (usually without the development of jaundice);
- Central and peripheral nervous system: headache, dizziness, weakness, lethargy, increased fatigue, paradoxical stimulation of the central nervous system (agitation, nervousness, tremor, anxiety, muscle spasms, emotional lability, euphoria, hallucinations), sleep disturbance, drowsiness, impaired coordination movements, confusion, seizures of central origin (when administered simultaneously with antipsychotic drugs), gait instability, amnesia, depression, paresthesia, impaired cognitive function, impaired taste and vision;
- Urinary system: dysuria, difficulty urinating, urinary retention. With prolonged use in doses significantly higher than recommended, - nephrotoxicity (papillary necrosis, interstitial nephritis);
- Respiratory system: dyspnea;
- Endocrine system: hypoglycemia up to hypoglycemic coma;
- Cardiovascular system: collapse, orthostatic hypotension, tachycardia, fainting;
- Hematopoietic organs: sulfhemoglobinemia. With prolonged use in doses significantly exceeding the recommended ones - pancytopenia, aplastic anemia, agranulocytosis;
- Dermatological reactions: toxic epidermal necrolysis (Lyell's syndrome), bullous rash, exanthema, erythema multiforme (including Stevens-Johnson syndrome);
- Allergic reactions: itching, urticaria, Quincke's edema;
- Others: violation of the menstrual cycle, increased sweating.
Overdose
Acute overdose of Zaldiar can manifest itself with symptoms characteristic of an overdose of tramadol and / or paracetamol:
- tramadol: apnea, depression of the respiratory center, convulsions, miosis, vomiting, collapse, coma;
- paracetamol: acute course (symptoms appear 6-14 hours after ingestion) - decreased appetite, diarrhea; chronic course (after 2-4 days) - metabolic acidosis, hypoglycemia, hypocoagulation, cerebral edema, development of disseminated intravascular coagulation syndrome, arrhythmia, collapse. In rare cases, there is a violation of hepatic function, which can be complicated by renal failure (in the form of renal tubular necrosis).
Therapy: gastric lavage, the use of enterosorbents (polyphepan, activated carbon), ensuring airway patency, maintaining the function of the cardiovascular system.
If respiratory depression develops (such as tramadol overdose syndrome), naloxone is given; seizures can be treated with diazepam. By hemofiltration or hemodialysis, a minimal amount of tramadol is removed from the blood serum, therefore, carrying out these measures exclusively is ineffective.
In case of symptoms of paracetamol overdose, donors of SH-groups and precursors of glutathione synthesis are administered (8-9 hours after the overdose - methionine, after 12 hours - N-acetylcysteine). The duration of therapy with these drugs depends on the concentration of paracetamol in the blood, as well as on the time that has passed since the application of Zaldiar.
special instructions
Do not exceed the recommended dosage regimen. While taking Zaldiar without a doctor's prescription, you cannot use other medicines containing tramadol or paracetamol.
With prolonged uncontrolled intake of Zaldiar, symptoms of drug dependence may develop, manifested in the form of phobias, irritability, nervousness, sleep disturbances, tremors, psychomotor activity and discomfort from the gastrointestinal tract. With a sudden withdrawal of the drug, signs of withdrawal may appear.
In patients with a tendency to addiction or abuse, therapy should be carried out for a short period of time under close medical supervision.
Drinking alcohol while using the drug is prohibited. The risk of developing functional liver disorders increases in patients with alcoholic hepatosis.
With prolonged use of Zaldiar, it is necessary to monitor the picture of the functional state of the liver and peripheral blood.
Influence on the ability to drive vehicles and complex mechanisms
During therapy, it is recommended to refrain from driving vehicles and performing potentially hazardous types of work that require an increased concentration of attention and rapid psychomotor reactions.
Application during pregnancy and lactation
Zaldiar is not prescribed during pregnancy / lactation.
Pediatric use
Zaldiar therapy is contraindicated in patients under 14 years of age.
With impaired renal function
Zaldiar tablets for severe renal failure (in patients with creatinine clearance of 10-30 ml / min) are contraindicated.
For violations of liver function
Zaldiar tablets are contraindicated in severe hepatic insufficiency.
Use in the elderly
For patients over 75 years old, Zaldiar can be prescribed under medical supervision.
Drug interactions
With the simultaneous use of Zaldiar with certain drugs, undesirable effects may occur:
- Opioid agonists-antagonists (buprenorphine, nalbuphine, pentazocine): decreased analgesic effect, risk of withdrawal syndrome (such a combination of drugs is undesirable);
- Barbiturates (with long-term use): decrease in the effectiveness of paracetamol;
- Naloxone: decreased analgesic effect;
- Drugs that have a depressing effect on the central nervous system (tranquilizers or hypnotics), ethanol: increased severity of side effects characteristic of tramadol;
- Microsomal oxidation inducers (barbiturates, carbamazepine, ethanol, phenytoin, rifampicin, tricyclic antidepressants, phenylbutazone): decrease in the severity and duration of the analgesic effect;
- Inhibitors of microsomal oxidation (cimetidine): reducing the risk of developing hepatotoxic effects of Zaldiar;
- Non-steroidal anti-inflammatory drugs (with long-term use): increased risk of developing renal papillary necrosis and nephropathy, the onset of end-stage renal failure;
- Salicylates (with long-term use): increased risk of bladder or kidney cancer;
- Quinidine: increasing the concentration of tramadol in the blood plasma, decreasing the concentration of the M 1 metabolite;
- Drugs that lower the seizure threshold (tricyclic antidepressants, selective serotonin reuptake inhibitors, antipsychotics): increased risk of seizures;
- Indirect anticoagulants, including warfarin and other coumarins (with prolonged use): an increase in their effect, which increases the risk of bleeding;
- Metoclopramide, domperidone: increase in the rate of absorption of paracetamol;
- Drugs that inhibit the CYP3A4 isoenzyme (erythromycin, ketoconazole): slowing down the metabolism of tramadol and the active O-demethylated metabolite;
- Diflunisal: increased concentration of paracetamol in blood plasma, increased risk of hepatoxicity;
- Cholestyramine: a decrease in the rate of absorption of paracetamol.
Analogs
Zaldiar's analogues are: Para-Thral, Ramlepsa, Tramacet, Forsodol.
Terms and conditions of storage
Keep out of reach of children at temperatures up to 25 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Zaldiar
According to reviews, Zaldiar is an effective pain reliever used for various types of pain syndrome. It is noted that it is important to comply with the doctor's recommended periods for using the drug, since addiction may develop.
Price for Zaldiar in pharmacies
The approximate price for Zaldiar is 569-799 rubles. (20 tablets) or 1389-1500 rubles. (50 tablets).
Zaldiar: prices in online pharmacies
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Drug name Price Pharmacy |
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Zaldiar coated tablets 20 pcs. 904 RUB Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, 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!
