Buy Tiapride ampoules 5%, 2 ml, 10 pcs
  • Buy Tiapride ampoules 5%, 2 ml, 10 pcs

Tiapride

Organica
1099 Items
2019-09-19
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Clinical Pharmacology

Tiapride has a neuroleptic effect.

Pharmacodynamics
The antipsychotic agent is an atypical neuroleptic that in vitro selectively blocks D2 and D3 subtypes of dopamine receptors without any significant affinity for the receptors of the main central neurotransmitters (including serotonin, norepinephrine, histamine). Studies of neurochemical and behavioral reactions conducted in vivo, confirmed these properties of Tiapride, showing the presence of anti-dopaminergic effects in the absence of significant sedation, catalepsy and a decrease in cognitive abilities.

Tiapride can affect dopamine receptors, which have already been previously sensitized to dopamine when using any other antipsychotic drugs, and its anti-diskinetic effects are associated with this.

In some experimental animal stress models, including alcohol withdrawal in mice and primates, the anxiolytic activity of Tiapride was confirmed.

Tiapride showed no formation of physical or psychological dependence.

This atypical pharmacodynamic profile explains the clinical efficacy of Tiapride in many disorders, including hyperdopaminergic conditions, such as dyskinesias and psycho-behavioral disorders, seen in patients with dementia or in alcohol abusers with fewer neurological side effects than typical neuroleptics.

Tiapride has a pronounced analgesic (both in interoceptive and exteroceptive pain), antiemetic due to the blockade of dopamine D2-receptors of the trigger zone of the vomiting center, hypothermic effect due to the blockade of hypothalamic dopamine receptors.

Pharmacokinetics
After intramuscular injection of 200 mg Tiapride, the maximum concentration of the drug in plasma — 2.5 mcg / ml — is reached in 30 minutes.

Distribution in the body occurs quickly (less than 1 hour). Penetrates through the blood-brain barrier and through the placenta without accumulation. The volume of distribution is 1.43 l / kg. The animals noted the penetration of the drug into milk, with a ratio of concentrations in milk and blood 1,2.

Does not bind to plasma proteins, weakly binds to erythrocytes. Tiapride is metabolized slightly (up to 15%), the metabolites are mostly inactive. No conjugated metabolites detected. 70% of the administered dose is found unchanged in the urine. The half-life of plasma after intramuscular administration of the drug is 2.9 hours in women and 3.6 hours in men. Isolation occurs predominantly by the kidneys by glomerular filtration and tubular secretion, the renal clearance is 330 ml / minute.

In patients with impaired renal function, the release of Tiapride depends on creatinine clearance, at a decrease in which the excretion of the drug slows down.

Tiapride is weakly removed from the blood by hemodialysis (11 ± 7 mg) within 4 hours after intramuscular administration at a dose of 100 mg.

Indications

  • Hyperkinetic and dyskinetic syndrome (including when using antipsychotic drugs (neuroleptics), parkinsonism, vascular origin, late dyskinesias):
  • acute and chronic chorea;
  • nervous tic;
  • senile motor imbalance;
  • tremor;
  • headache (neurogenic origin);
  • behavior disorder (alcoholism);
  • psychomotor agitation;
  • behavior disorders in old age;
  • alcoholic psychosis;
  • abstinence syndrome (alcoholism, drug addiction);
  • chronic pain syndrome (including arthralgia, spastic pain in the limbs, pain in cancer patients, pain of neurotic origin).

Composition

1 ml solution for intravenous and intramuscular administration contains:
active ingredient: Tiapride 50 mg;
Excipients: sodium chloride; water for injections

Tiapride is marketed under different brands and generic names, and comes in different dosage forms:

Brand nameManufacturerCountryDosage form
Tiapride Organica Russia ampoules
Tiapridal Sanofi-aventis France pills
Tiapridal Sanofi-aventis France solution

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Tiapride

Dosage and Administration

For intramuscular or intravenous administration. The drug is used only for adults. It is always necessary to select the minimum effective dose. If the condition of the patient allows, treatment should begin with a low dose, then gradually increasing it.
Relief of psychomotor agitation and aggressive states, especially in chronic alcoholism or in old age: The usual dose is 200 - 300 mg / day.
In delirious syndrome or precalibar state: adults - 400-1200 mg / day (up to a maximum of 1800 mg / day). Injections should be given every 4–6 hours; in old age - 200 - 300 mg / day, that is, 2-3 injections with 6-hour intervals. Do not exceed a single dose of 100 mg.
Intense chronic pain syndrome: adults - 200-400 mg / day, that is, 2-4 ampoules per day.

Adverse reactions

With prolonged use Tiaprideal high dose sometimes possible sleepiness, muscular hypotonia, dyskinesia (early - spastic, torticollis, trismus, oculomotor disorders, and later), extrapyramidal symptoms, muscle relaxation, reduction of blood pressure, amenorrhea, galactorrhea, hyperprolactinemia, gynecomastia, impotence, frigidity , weight gain, neuroleptic malignant syndrome (unexplained hyperthermia - requires discontinuation of the drug).

Contraindications

- Hypersensitivity to Tiapride or to other components of the drug.
- Diagnosed or suspected prolactin-dependent tumors, such as pituitary prolactinoma and breast cancer.
- Diagnosed or suspected pheochromocytoma.
- In combination with sultoprid.
- Pregnancy (I trimester).
- Lactation period.
- Children's age (up to 6 years).
- Hypertensive crisis.
- Severe renal and / or liver failure.
- In combination with dopaminergic agonists (amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lizurid, pergolid, piribedil, pramipexol, quinagolid, ropinirole), with the exception of patients suffering from Parkinson's disease.
- In combination with drugs that can cause heart rhythm disturbances: class 1a antiarrhythmic drugs (quinidine, hydroquinidine, disopyramide) and class III (amiodarone, sotalol, dofetilide, ibutilid).
- In combination with some neuroleptics (thioridazine, chlorpromazine, levomepromazine, trifluoperazin, cyamemazine, amisulpride, sulpiride, pimozide, haloperidol, droperidol).
- In combination with the following drugs: levodopa, bepridil, cisapride, difemanil, erythromycin, mizolastin, intravenous vincamine, sparfloxacin, moxifloxacin.
Carefully:
- Chronic renal failure. When using, it is necessary to reduce the dose and strengthen the observation.
- Epilepsy, due to the possibility of lowering the seizure threshold.
- Cardiovascular diseases in the stage of decompensation.
- Parkinson's disease.
- The combined use of drugs containing alcohol.
- In old age, with bradycardia (rarely 55 beats / min), hypokalemia, congenital lengthening of the QT interval, as well as with the joint use of drugs that can cause pronounced bradycardia.

Drug interactions

Not recommended combinations

  • When used in conjunction with class 1a antiarrhythmic drugs (quinidine, hydroquinidine, disopyramide), and those of the third-rounds (aymear oem, sotalol, dofetilide, ibutilid), antiarrhythmic drugs, some neuroleptics (thioridazine, chlorpromazine, levomepromazine, triflurozopine, cyamemezine, cyphermezine, chloropromazine, levomepromazine, trifluoperazine, ciamesemazine, cymemezine, cytomezine, chloropromazine, levomepromazine, trifluoperazine, cyammezine, cymemezine, cytomezine, cytomezine, cytomezine, cytomezine, cytomezine, cytomezine, cytomezine, cytomezine, cytomethazine haloperidol, droperidol) and other drugs such as bepridil, cisapride, difemanil, erythromycin, mizolastine, vincamine, increases the risk of ventricular arrhythmias, as well as atrial fibrillation.
  • Alcohol
    Alcohol enhances the sedative effect of neuroleptics.
  • Levodopa
    There is a joint antagonism of the action of levodopa and neuroleptics.In patients with Parkinson's disease, it is recommended to use the minimum effective dose of levodopa and Tiapride.
  • Dopaminergic agonists can cause or exacerbate psychotic disorders. If treatment with neuroleptics is necessary for a patient suffering from Parkinson's disease, who is receiving a dopaminergic drug, the dose of the latter should be gradually reduced to cancellation (abrupt cancellation may lead to the development of a neuroleptic malignant syndrome).
  • Sparfloxacin, moxifloxacin:
    Increased risk of ventricular arrhythmias, as well as atrial fibrillation. If the combination cannot be avoided, first check the QT interval and ensure ECG monitoring.

Combinations that require caution

  • Drugs that cause bradycardia (blockers of "slow" calcium channels: diltiazem, verapamil; beta-blockers; clonidine, guanfacine; digitalis preparations, cholinesterase inhibitors: nedezepil, rivastigmine, galantamine, pyridostigmine, neostigmine).
  • Drugs that can cause hypokalemia: potassium-withdrawing diuretics, laxatives, amphotericin B, glucocorticoids, tetracosactide. Increased risk of ventricular arrhythmias, as well as atrial fibrillation.

Combinations to be taken into account

  • Antihypertensive drugs (all):
    Additive effect, increased risk of postural hypotension.
  • Medications that inhibit the function of the central nervous system:
    Morphine derivatives (analgesics, antitussive drugs and substitutional therapy agents); barbiturates; benzodiazepines and other anxiolytics; sleeping pills; antidepressants with a sedative effect; HI antihistamines with a sedative effect; antihypertensive agents of central action; baclofen; thalidomide promotes increased inhibition of the function of the central nervous system.

Pregnancy and Lactation

The drug is contraindicated in the first trimester of pregnancy and lactation.
Regarding the effect of neuroleptics used during pregnancy on the fetal brain, there is no data (it is preferable not to use Tiapride during pregnancy). However, if the drug is still used during pregnancy, it is recommended, if possible, to limit the dose and duration of treatment.
With prolonged treatment and / or use of high doses and / or with late pregnancy, control of the neurological functions of the newborn is justified.
Lactation
It is not known whether Tiapride penetrates breast milk, so breastfeeding is prohibited.

Special instructions

Malignant neuroleptic syndrome is characterized by pallor, hyperthermia, muscle rigidity, dysfunction of the peripheral nervous system, impaired consciousness. Signs of peripheral nervous system dysfunction, such as increased sweating and blood pressure lability, may precede the onset of hyperthermia and, therefore, represent early warning signs. Some risk factors, such as dehydration or organic brain damage, although the effect of antipsychotics may be due to idiosyncrasy, are apparently predisposing. Tiapride causes a dose-dependent prolongation of the QT interval. It is known that this effect increases the risk of serious ventricular arrhythmias, it is enhanced against the background of bradycardia, with hypokalemia, as well as in the case of congenital or acquired long QT interval (combination with drugs that extend the QT interval). Hypokalemia should be adjusted prior to the use of the drug, in addition, the clinical picture, electrolyte balance and ECG should be monitored. When extrapyramidal syndrome caused by neuroleptics, instead of using dopaminergic agonists, anticholinergic drugs should be prescribed.
Influence on ability to drive motor transport and control mechanisms: during the period of treatment, it is necessary to refrain from engaging in potentially hazardous activities that require increased concentration of attention and quickness of psychomotor reactions.

Overdosage

Symptoms: excessive sedation, drowsiness, depression of consciousness up to coma, arterial hypotension, extrapyramidal symptoms.
Treatment: drug withdrawal, symptomatic and detoxification therapy, monitoring of vital body functions (especially cardiac activity - the risk of prolonged QT interval) until the symptoms of intoxication disappear completely. When severe extrapyramidal symptoms appear, anticholinergic treatment. Since Tiapride is poorly dialyzed, hemodialysis is not recommended for removal. Antidote Tiapride unknown.

  • Brand name: Tiapride
  • Active ingredient: Tiapride
  • Dosage form: Solution for intravenous and intramuscular administration
  • Manufacturer: Organics
  • Country of Origin: Russia

Studies and clinical trials of Tiapride (Click to expand)

  1. Evaluation of tiapride in agitated elderly outpatients: an open study
  2. Tourette syndrome: Efficient treatment with ziprasidone and normalization of body weight in a patient with excessive weight gain under tiapride
  3. Determination of sultopride and tiapride in serum by gas chromatography using a surface ionisation detector
  4. Etude comparée des spectres de vibration du tiapride. Base et chlorhydrate
  5. Simultaneous electrochemiluminescence determination of sulpiride and tiapride by capillary electrophoresis with cyclodextrin additives
  6. Determination of tiapride in plasma by high-performance liquid chromatography
  7. Effects of tiapride in tardive dyskinesia
  8. Acute dyskinesias in monkeys elicited by halopemide, mezilamine and the “antidyskinetic” drugs, oxiperomide and tiapride
  9. Effects of tiapride on homovanillic acid levels in human cerebrospinal fluid drawn at pneumoencephalography
  10. Clinical and neurobiological findings in children suffering from tic disease following treatment with tiapride
  11. Pharmacokinetics of tiapride in patients with tardive dyskinesia and Huntington's disease
  12. Release hallucinations and tiapride
  13. Single oral dose pharmacokinetics of tiapride in patients with Huntington's disease
  14. Determination of tiapride in human plasma using hydrophilic interaction liquid chromatography-tandem mass spectrometry
  15. Double blind study of tiapride versus haloperidol and placebo in agitation and aggressiveness in elderly patients with cognitive impairment
  16. A combination of carbamazepine/tiapride in outpatient alcohol detoxification
  17. Treatment of alcohol withdrawal syndrome with a combination of tiapride/carbamazepine
  18. Treatment of alcohol withdrawal: tiapride and carbamazepine versus clomethiazole.
  19. Tiapride pre-treatment in acute exposure to paraoxon: Comparison of effects of administration at different points-in-time in rats
  20. Pregabalin, tiapride and lorazepam in alcohol withdrawal syndrome: a multi-centre, randomized, single-blind comparison trial
  21. Tiapride for pathological jealousy (Othello syndrome) in elderly patients
  22. Efficacy of combination treatment of fluvoxamine and tiapride for repetitive behaviors in frontotemporal lobar degeneration
  23. Tiapride for monosymptomatic hypochondriacal psychosis (dysmorphic delusion subtype) in presenile patients
  24. TIAPRIDE MAY ACCELERATE LUNG CANCER IN OLDER PEOPLE: A CASE REPORT

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