Tiapridal
Tiapridal: 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. Drug interactions
- 11. Analogs
- 12. Terms and conditions of storage
- 13. Terms of dispensing from pharmacies
- 14. Reviews
- 15. Price in pharmacies
Latin name: Tiapridal
ATX code: N05AL03
Active ingredient: Tiapride (Tiapride)
Producer: Sanofi-Winthrop Industrie (France)
Description and photo update: 2019-12-08
Prices in pharmacies: from 999 rubles.
Buy
Tiapridal is a neuroleptic, antipsychotic drug.
Release form and composition
Dosage forms of Tiapridal:
- tablets: white with a cream shade or white, round flat shape, with beveled edges on each side, engraved "T100" on one side and a cross-shaped dividing line on the other, there may be a slight odor (10 pcs. in a blister, in cardboard box 2 blisters);
- solution for intravenous (intravenous) and intramuscular (intramuscular) administration: almost colorless or colorless transparent liquid [2 ml in glass ampoules (in the upper part with two marking rings and a break point) without color, in a blister strip plastic packaging 6 pcs., In a cardboard box 2 packages].
1 tablet contains:
- active substance: tiapride hydrochloride - 111.1 mg, which is equivalent to the content of 100 mg of tiapride;
- auxiliary components: colloidal aqueous silicon dioxide, microcrystalline cellulose, mannitol, povidone, magnesium stearate.
1 ml of solution contains:
- active substance: tiapride hydrochloride - 55.55 mg, which is equivalent to 50 mg of tiapride;
- auxiliary components: sodium chloride, water for injection.
Pharmacological properties
Tiapridal has a neuroleptic, analgesic and anxiolytic effect.
Pharmacodynamics
Tiapride is an antipsychotic agent - an atypical neuroleptic, in vitro selectively blocking the D2 and D3 dopamine receptor subtypes. At the same time, there is no significant affinity for the receptors of the main central neurotransmitters (including histamine, norepinephrine, serotonin). These properties of tiapride have been confirmed by in vivo behavioral and neurochemical studies. They proved the presence of antidopaminergic effects against the background of the absence of significant signs of catalepsy, sedation and impairment of cognitive abilities.
Tiapride is able to influence dopamine receptors, which are already hypersensitive to dopamine, when taking any other antipsychotic drugs. This is due to its antidyskinetic effects.
Several experimental stress models tested in animals (for example, alcohol withdrawal in primates and mice) have shown the anxiolytic activity of tiapride. This substance does not cause psychological or physical dependence.
This atypical pharmacodynamic profile explains the clinical efficacy of Tiapridal in the treatment of many disorders, including hyperdopaminergic states: dyskinesias and psychobehavioral disorders, which occur in patients with dementia or in alcohol abusers. At the same time, in comparison with typical antipsychotics, the number of side effects from the central nervous system is minimized.
Tiapride is characterized by pronounced hypothermic (due to blockade of dopamine receptors located in the hypothalamus), antiemetic (due to blockade of dopamine Og receptors located in the trigger zone of the vomiting center) and analgesic (both with exteroceptive and interoceptive pain) action.
Pharmacokinetics
After intramuscular administration of 200 mg of tiapride, its maximum plasma content - 2.5 μg / ml - is reached in 30 minutes. The substance is distributed in the body relatively quickly: this process takes less than 1 hour. It crosses the blood-brain barrier and into the placenta, but there is no cumulative effect. The volume of distribution is 1.43 l / kg. In animals, the penetration of tiapride into milk was observed, and the ratio of its concentrations in milk and blood was 1.2: 1.
Tiapride does not bind to plasma proteins, and the degree of its binding to erythrocytes is negligible. It is metabolized slightly (up to 15%) with the formation of predominantly inactive metabolites. Conjugated metabolites are not detected. 70% of the administered dose is excreted in the urine unchanged. After intramuscular administration of Tiapridal, the plasma half-life of its active substance is 3.6 hours in men and 2.9 hours in women. Tiapride is excreted mainly through the kidneys through tubular secretion and glomerular filtration. Renal clearance is 330 l / min. In patients with renal dysfunction, the rate of elimination of tiapride is determined by creatinine clearance, with a decrease in which the rate of excretion of the drug decreases. Tiapride is poorly removed from the bloodstream by hemodialysis (11 ± 7 mg) within 4 hours after intramuscular injection at a dose of 100 mg.
The absorption of tiapride, taken in tablet form, is very rapid. After oral administration of 200 mg of Tiapridal, the maximum concentration of its active component in plasma is reached in 1 hour and is 1.3 μg / ml. The bioavailability of the drug is 75%. When tablets are taken immediately before meals, bioavailability increases by 20%, and the maximum plasma concentration is increased by 40%. In elderly patients, absorption slows down.
Indications for use
- relief of aggressive states and psychomotor agitation, especially when treating patients in old age or with chronic alcoholism;
- chronic intense pain syndrome.
In addition, the use of Tiapridal is shown:
- adults and children over 6 years old: chorea of various etiology, Gilles de la Tourette's syndrome;
- children over 6 years of age: behavioral disorders with aggressiveness and agitation.
Contraindications
- pheochromocytoma (including if it is suspected);
- breast cancer, pituitary prolactinoma and other prolactin-dependent tumors, including if they are suspected;
- severe renal and / or liver failure;
- hypertensive crisis;
- I trimester of pregnancy;
- breast-feeding;
- simultaneous therapy with drugs that can cause arrhythmias: class IA antiarrhythmic drugs (hydroquinidine, disopyramide, quinidine) and class III (ibutilide, amiodarone, dofetilide, sotalol), certain antipsychotics (thioridazine, levomepromazine, trifluoperazine, droperidol, cyamloridemazine, pimozide, haloperidol, sulpiride), levodopa, cisapride, diphemanil, bepridil, mizolastine, erythromycin, vincamine (i.v.), moxifloxacin, sparfloxacin;
- combination with dopamine receptor agonists (apomorphine, entacapone, amantadine, bromocriptine, ropinirole, cabergoline, pergolide, lisuride, piribedil, quinagolide, pramipexole), except for patients with Parkinson's disease;
- simultaneous use of sultopride;
- individual intolerance to the components of the drug.
In addition, age-related contraindications for Tiapridal: tablets are not prescribed for children under 6 years of age, the solution is used only for the treatment of adult patients.
It is recommended to prescribe Tiapridal with caution to patients with chronic renal failure, epilepsy, cardiovascular diseases in the stage of decompensation, hypokalemia, Parkinson's disease, in combination with ethanol-containing drugs, with congenital prolongation of the QT interval, bradycardia with heart rate (heart rate below 55) per minute, concomitant therapy with drugs that can cause hypokalemia, severe bradycardia (heart rate less than 55 beats per minute), lengthening of the QT interval or slowing of cardiac conduction, in old age.
Instructions for the use of Tiapridal: method and dosage
Pills
Tiapridal tablets are taken orally.
Given the patient's condition, treatment should be started with a low dose, gradually increasing it, it should be brought to the minimum dose that provides a clinical effect.
Recommended dosage of Tiapridal:
- relief of aggressive states and psychomotor agitation: 200-300 mg per day, course duration - 30-60 days. The initial dose for elderly patients is 50 mg 2 times a day, if necessary, with an interval of 2-3 days, the dose can be increased by 50-100 mg to 300 mg - the maximum dose;
- chorea, Gilles de la Tourette's syndrome: the initial dose for adults is 25 mg per day, then it is gradually increased to the minimum effective dose, which can range from 300 to 800 mg per day. For children, the dose is determined at the rate of 3–6 mg per 1 kg of the child's weight per day;
- intense chronic pain syndrome: adults - 200-400 mg per day;
- behavioral disorders with aggressiveness and agitation in children over 6 years of age: 100–150 mg per day.
Injection
Tiapridal solution is intended for use only in adult patients by intramuscular or intravenous administration.
Taking into account the patient's condition, treatment begins with a low dose and gradually increases it; it is always necessary to use the minimum effective dose.
The recommended dosage regimen of Tiapridal:
- relief of aggressive states and psychomotor agitation: usually - 200-300 mg per day; pre-relirious state or delirious syndrome - 400–1200 mg per day every 4–6 hours. The maximum daily dose is 1800 mg. For elderly patients - up to 100 mg 2-3 times a day;
- chronic intense pain syndrome: 200-400 mg per day.
Side effects
- from the central and peripheral nervous system: asthenia, fatigue, drowsiness, insomnia, agitation, psychomotor agitation, apathy, dizziness, headache, increased blood pressure (BP), bradykinesia, hypersalivation; with parkinsonism - tremor; rarely - akathisia, dystonia and early dyskinesia (oculogyric crises, spasmodic torticollis, trismus) - all of these symptoms usually disappear when anticholinergic antiparkinsonian drugs are prescribed or after drug withdrawal; against the background of prolonged use - tardive dyskinesia (involuntary characteristic movements of the face, tongue, limbs); possibly - the development of neuroleptic malignant syndrome (MNS);
- on the part of the cardiovascular system: atrial fibrillation, prolongation of the QT interval, postural hypotension;
- from the endocrine system: hyperprolactinemia, amenorrhea, swelling of the mammary glands, galactorrhea, chest pain, ejaculation disorders, impotence, weight gain.
Overdose
Symptoms of an overdose of Tiapridal include signs of extrapyramidal disorder, excessive sedation, drowsiness, arterial hypotension, clouded consciousness up to a coma. In this case, the drug is immediately canceled, the stomach is washed (when taking pills in high doses) and detoxification and symptomatic therapy is prescribed.
It is also necessary to regularly monitor the vital functions of the body, especially the indicators of the cardiovascular system due to the risk of lengthening the QT interval, until the signs of intoxication completely disappear. With pronounced extrapyramidal symptoms, anticholinergic drugs are prescribed.
Because tiapride is poorly eliminated from the body by dialysis, hemodialysis is not recommended to remove it from the blood. The specific antidote is currently unknown. When tiapride is combined with other psychotropic drugs, a fatal outcome is possible in case of an overdose.
special instructions
The appointment of anticholinergic antiparkinsonian drugs for the correction of tardive dyskinesia may worsen the patient's condition.
Symptoms of NMS include: pallor, hyperthermia, muscle stiffness, dysfunction of the peripheral nervous system, impaired consciousness. Signs of dysfunction of the peripheral nervous system that precede the onset of hyperthermia - lability of blood pressure and increased sweating - are warning signals for the development of NNS. Predisposing factors of the disease may include organic brain damage and dehydration.
Patients with chronic renal insufficiency need a dose reduction of Tiapridal and regular monitoring.
The action of the drug promotes a dose-dependent lengthening of the QT interval and increases the risk of severe ventricular arrhythmias. Since the effect is enhanced with hypokalemia, bradycardia, congenital or acquired prolongation of the QT interval, the drug should be prescribed after correcting hypokalemia. Treatment should be accompanied by careful monitoring of electrolyte balance, electrocardiography (ECG) and clinical presentation.
Due to a possible decrease in the threshold of convulsive readiness, Tiapridal should be used with caution in epilepsy.
The extrapyramidal syndrome caused by neuroleptics should be stopped by anticholinergics.
According to the instructions, Tiapridal affects the patient's ability to drive vehicles and mechanisms, therefore, during the period of treatment, one should refrain from these types of activities.
Application during pregnancy and lactation
Tiapridal is prohibited to appoint in the first trimester of pregnancy during lactation. There is no information on the effect of the drug used during pregnancy on the fetal brain. Tiaprid is not recommended to be prescribed in the II and III trimesters of pregnancy. However, if there is no alternative to drug treatment, the dose and duration of therapy should be reduced if possible.
With a long course of treatment and / or taking Tiapridal in high doses and / or in late pregnancy, it is necessary to constantly monitor the neurological functions of the newborn. It is not known whether tiapride penetrates into breast milk, therefore, if it is necessary to use the drug during lactation, breastfeeding should be abandoned.
Drug interactions
With the simultaneous use of Tiapridal:
- ethanol - enhances the sedative effect of the neuroleptic;
- beta-blockers, digitalis drugs, slow calcium channel blockers (verapamil, diltiazem), guanfacine, clonidine, cholinesterase inhibitors (donepezil, galantamine, neostigmine, rivastigmine, pyridostigmine), laxatives, potassium-excreting diuretics, increase the risk of glucose-excreting diuretics development of atrial fibrillation and ventricular arrhythmia;
- antihypertensive drugs - cause an additive effect, increasing the risk of postural hypotension;
- antitussives, opioid analgesics, substitution therapy (morphine derivatives), centrally acting antihypertensive drugs, barbiturates, anxiolytics (including benzodiazepines), hypnotics, sedative antidepressants, baclofen, histamine H 1 receptor blockers with a sedative effect increased inhibitory effect on the central nervous system.
In Parkinson's disease, levodopa in combination with tiapride is recommended to be taken in the minimum effective doses, since dopamine receptor agonists can increase or cause psychotic disorders. In the course of treatment with neuroleptics in patients with Parkinson's disease, the dose of dopaminergic drugs is gradually reduced until it is completely canceled.
In case of an urgent need for the simultaneous use of the drug with moxifloxacin or sparfloxacin, it is necessary to preset the value of the QT interval and ensure its control on the ECG.
Analogs
Tiapridal is analogous to Tiaprid.
Terms and conditions of storage
Keep out of the reach of children.
Store in a place protected from moisture and light at temperatures up to 25 ° C.
Shelf life: tablets - 5 years, solution - 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Tiapridal
Numerous reviews of Tiapridal indicate that it is often used to treat alcoholic psychosis, accompanied by aggression and agitation. Patients are satisfied with the result of treatment after the first course of administration, and also note the affordable price of the drug and the convenience of its use.
The price of Tiapridal in pharmacies
The approximate price of Tiapridal in the form of tablets is 1393–1601 rubles (the package includes 20 pcs.). You can buy a solution for intravenous and intramuscular administration for 1060–1168 rubles (the package includes 12 ampoules).
Tiapridal: prices in online pharmacies
|
Drug name Price Pharmacy |
|
Tiapridal 50 mg / ml solution for intravenous and intramuscular administration 2 ml 12 pcs. 999 RUB Buy |
|
Tiapridal 100 mg tablets 20 pcs. 1039 RUB Buy |
|
Tiapridal solution for intravenous and intramuscular injection. 50mg / ml 2ml 12 pcs. 1137 RUB Buy |
|
Tiapridal tablets 100mg 20 pcs. 1272 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!
