Anastrozole for men administration of 200 mg tiapride maximum drug concentration in plasma – 1.3 ug / ml – achieved 1 hour. After intramuscular injection of 200 mg tiapride maximum drug concentration in plasma – 2.5 mcg / ml – 30 minutes is achieved. The bioavailability of the tablets is 75%. When receiving them directly before ingestion bioavailability is increased by 20% and the maximum plasma concentration – 40%.
Absorption is slowed in the elderly. The distribution in the body is rapid (less than 1 h). Penetrates through the blood-brain barrier and the placenta, accumulation does not occur. Animals in drug penetration mentioned milk with a ratio of concentrations in milk and blood of 1.2. Contact with plasma proteins and erythrocytes weak. Metabolism tiapride is very low: 70% of the dose found in the urine in unchanged form. Women and in men 3.6 hours. Selection takes place mainly in the urine, and renal clearance of up to 330 ml / min. In patients with renal function impaired excretion correlates with creatinine clearance. If creatinine clearance below 20 ml / min, the daily dose should be installed depending on the severity of renal failure: use half the dose when creatinine clearance 11-20 ml / min, and a quarter of the dose when creatinine clearance 10 mL / min.
Indications Tablets Adults:
- Relief of psychomotor agitation and aggressive states, especially in chronic alcoholism or in old age.
- Intense chronic pain syndrome.
In adults and children older than 6 years:
- Different types of chorea, Gilles de la Tourette syndrome
In children older than 6 years:
- Conduct disorder with agitation and aggressiveness.
- Relief of psychomotor agitation and aggressive states, especially in chronic alcoholism or in old age. Intense chronic pain syndrome.
: Hypersensitivity to tiaprid or to other components of the preparation.
- Diagnosed or suspected prolactin-dependent tumors, such as pituitary gland prolactinoma and breast cancer.
- Confirmed or suspected pheochromocytoma.
- In combination with sultopride;
- Pregnancy (I term)
- Children’s age (up to 6 years)
- Hypertensive crisis anastrozole for men
- Severe renal and / or hepatic impairment
- In combination with dopaminergic agonists (amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lisuride, pergolide, piribedil, pramipexole, quinagolide, ropinirole), except in patients suffering from Parkinson’s disease.
In combination with medicines that can cause heart rhythm disturbance: antiarrhythmics Ia class (quinidine, gidrohinidin, disopyramide) and class III (amiodarone, sotalol, dofetilide, Ibutilide), some antipsychotics (thioridazine, chlorpromazine, Levomepromazine, trifluoperazine, tsiamemazin, amisulpride, sulpiride, pimozide, haloperidol, droperidol), and with the following medications: levodopa, bepridil, cisapride, difemanil, erythromycin, mizolastine, intravenous vincamine, sparfloxacin, moxifloxacin. (see. section “Interaction with other medicinal products” ).
- Epilepsy, in connection with the possibility of lowering the seizure threshold;
- Cardiovascular diseases in the stage of decompensation;
- Parkinson’s disease;
- Combined use of drugs containing alcohol;
- In old age, bradycardia , hypokalaemia, congenital prolongation, and in the combined use of drugs that can cause severe bradycardia, hypokalaemia, decreased cardiac conduction, or prolongation of the interval QT.
Pregnancy and lactation The drug is contraindicated in the I trimester of pregnancy and lactation. Regarding the effect of neuroleptics used during pregnancy, fetal brain, the data are not available (preferably not be used during pregnancy tiaprid). However, if the drug is still applied during pregnancy, it is recommended whenever possible to limit the dose and duration of treatment. Prolonged treatment and / or use of high doses and / or late pregnancy justified control neurological neonate functions.
Breastfeeding known whether tiapride penetrates breast milk, so breast-feeding is forbidden.
Dosing and Administration The tablets only for adults and children over 6 years. It is always necessary to select the minimum effective dose. If the patient’s condition allows, treatment should be started at a low dose and then gradually increasing it.
- Relief of psychomotor anastrozole for men agitation and aggressive states, especially in chronic alcoholism or in old age:
- In adults: 200 – 300 mg / day course of treatment 1 – 2 months.
- In old age: 50 mg twice a day. The dose can be gradually increased to 50 to 100 mg every 2-3 days to a maximum daily dose of 300 mg.
- Chorea, Gilles de la Tourette syndrome
- In adults: 300 – 800 mg / day
- Treatment should start with a dose – 25 mg a day, and then slowly raise it until the minimum effective dose.
- In children older than 6 years: 3-6 mg / kg / day
- Intense chronic pain syndrome.
- The usual dose for adults is 200 – 400 mg / day.
- Conduct disorder with agitation and aggression in children older than 6 years -Dose is 100 – 150 mg / day.
Solution for injection Intramuscular or intravenous
should always choose the minimum effective dose. If the patient’s condition allows, treatment should be started at a low dose and then gradually increasing it.
Relief of psychomotor agitation and aggressive states, especially in chronic alcoholism or in old age:
- In adults:
The usual dose is 200 – 300 mg / day.
When delirious predelirioznom syndrome or condition. 400 – 1200 mg / day (up to 1800 mg / day)
Injection be administered every 4-6 hours.
- In old age:
200 – 300 mg / day, 2-3 injections i.e. to 6-hour intervals.
Not more than a single dose of 100 mg.
- Intense chronic pain syndrome.
The usual dose is 200 – 400 mg / day, ie, 2-4 capsules a day.
- Asthenia, fatigue (9.4%)
- Drowsiness (6.6%)
- Insomnia (4.4%)
- Agitation, agitation (3.7%)
- Apathetic state (2.8%)
- Dizziness (2.6%)
- Headache (2%)
- Parkinson’s syndrome: tremor (2.3%), increased blood pressure, bradykinesia (1.2%), hypersalivation (1.2%).
- Much less:
- Early dyskinesia and dystonia (spasmodic torticollis, oculogyric crises, lockjaw), akathisia (0.9%).
- These symptoms are usually reversible upon discontinuation of the drug or destination protivoparkinsonnyh anticholinergic agents.
- Tardive dyskinesia (involuntary stereotypic movements of the tongue, face and limbs) occurring with prolonged use (anticholinergic antiparkinsonian agents appointed as correctors may worsen the patient’s condition).
- Hyperprolactinemia and mating with her disorder (<0.2%): amenorrhea, galactorrhea, breast swelling, chest pain, impotence and ejaculation disorders,
- Weight gain
- QT prolongation
- atrial fibrillation
- postural hypotension
- Neuroleptic malignant syndrome.
Overdose Symptoms: excessive sedation, drowsiness, depression of consciousness up to coma, hypotension, extrapyramidal symptoms. Treatment: removal of the drug, gastric lavage (in case of poisoning pills), symptomatic and detoxification therapy, monitoring of vital functions of the body (especially of cardiac function up to the complete disappearance of symptoms of intoxication In case of severe extrapyramidal symptoms -.. anticholinergic treatment As tiaprid weakly dialyzed to remove the substance is not recommended dialysis Antidote tiapride unknown..
- When used in conjunction with anti-arrhythmic drugs 1a class (quinidine, gidrohinidin, disopyramide) and III-class (amiodarone, sotalol, dofetilide, Ibutilide), antiarrhythmic drugs, some antipsychotics (thioridazine, chlorpromazine, levomepromazine, trifluoperazine, tsiamemazin, sulpiride, amisulpride, pimozide, haloperidol, droperidol), and other drugs such as bepridil, cisapride, difemanil, erythromycin, mizolastine, vincamine, an increased risk of ventricular arrhythmias, and atrial fibrillation.
Alcohol increases the sedative effect of neuroleptics.
There is a joint action antagonism 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 may cause or exacerbate psychotic disorders. If you need neuroleptic treatment to a patient suffering from Parkinson’s disease receiving dopaminergic drug, the dose should be gradually reduce the latter to cancel (abrupt withdrawal may lead to the development of neuroleptic malignant syndrome).
- Sparfloxacin, moxifloxacin:
There is a growing risk of ventricular arrhythmias, and atrial fibrillation. If the combination can not be avoided, you should first check the QT interval and provide ECG monitoring.
Combinations requiring caution
- Drugs associated with bradycardia (blockers “slow” calcium channel blockers: diltiazem, verapamil, beta-blockers, clonidine, guanfacine; digitalis drugs that are inhibitors of cholinesterase: donezepil, rivastigmine, galantamine, pyridostigmine, neostigmine).
- Drugs that can cause hypokalaemia: potassium carve diuretics, laxatives, amphotericin B, glucocorticoids, tetrakozaktid. There is a growing risk of ventricular arrhythmias, and atrial fibrillation.
Combinations to be taken into account
- Antihypertensive drugs (all):
An additive effect, increasing the risk of postural hypotension.
- Preparations depressing central nervous system function:
Morphine derivatives (analgesics, cold preparations and means of substitutional therapy); barbiturates; benzodiazepines and other anxiolytics; sleeping pills; antidepressants with sedative effect; HI antihistamines with sedative effect; antihypertensive medications central action; baclofen; Thalidomide contributed to increasing oppression of the central nervous system.
Cautions Neuroleptic malignant syndrome: Neuroleptic malignant syndrome, characterized by paleness, hyperthermia, muscle rigidity, dysfunction of the peripheral nervous system, impaired consciousness.Signs of peripheral nervous system dysfunction, such as increased perspiration, and blood pressure lability may precede onset of hyperthermia, and thus, be an early warning signals. Some risk factors, such as dehydration or organic brain damage, despite the fact that such action can be attributed to antipsychotics idiosyncrasy probably are predisposing. Lengthening the interval: tiaprid causes dose-dependent lengthening of the interval. It is known that this effect increases the risk of serious ventricular arrhythmia, it is enhanced by bradycardia, with hypokalemia as well as in the case of congenital or acquired long interval QT (combination with drugs that prolong the anastrozole for men interval). Hypokalemia should be adjusted prior to use of the drug, except it should ensure that control of clinical, and electrolyte balance. When extrapyramidal syndrome induced by neuroleptics, instead of using dopamine agonists should be prescribed anticholinergic drugs. In the period of treatment should refrain from activities potentially hazardous activities that require high concentration and psychomotor speed reactions.