Dogmakern

Sulpiride.

Each capsule contains: Sulpiride 50 mg.
Excipients/Inactive Ingredients: Lactose monohydrate, colloidal anhydrous silica, methylcellulose, magnesium stearate, talc, hard follicle No. 4.

Pharmacology: Pharmacodynamics: Sulpirides belong to the benzamide group, which has antipsychotic effects through selective blockade of dopamine D receptors in the brain. Sulpirides can be thought of as an intermediate between neuroleptics and antidepressants, as sulpirides have both. Sulpirides are mainly used to treat psychotic diseases such as schizophrenia. The mood increases after a few days of treatment, accompanied by the loss of all the symptoms of the disease. Sulpirides do not cause drowsiness and loss of feeling like classic sedatives such as phenothiazine or butyrophenone. High-dose sulpirides control the rampant positive symptoms of schizophrenia, but low doses have the effect of making people with schizophrenia apathetic, withdrawn and out of contact with society. Although there are some properties of classical neuroleptics, sulpirides differ from them in chemical structure and do not cause postural retention, do not affect the dopamine-sensitive adenylcyclase system, do not affect the circulation of noradrenaline and 5-HT, have almost no anticholinesterase effect, and do not affect muscarinic receptors or GABA.
Pharmacokinetics: Taken orally, sulpiride is absorbed in 4.5 hours; The peak plasma sulpiride concentration was 0.25 mg/L after taking 50 mg capsules. The bioavailability of the oral form is between 25 and 35%, there can be significant differences between one person and another; The concentration of sulpiride in plasma is linearly related to the dosage. Sulpiride is rapidly diffused to tissues, especially to the liver and kidneys; diffusion to the brain is poor, mainly to the pituitary gland.
The rate of adhesion to plasma protein is less than 40%; the distribution coefficient to red blood cells and plasma is 1. Excretion through breast milk is estimated to be 1/1000 of the daily dose. Figures made on animals with marked sulpiride (C14) demonstrate that excretion through the placental barrier is very poor. Contrary to animal records, sulpiride is very rarely metabolized in humans; 92% of intramuscular doses of sulpiride are found in the urine as unchanged.
The pharmacokinetics of sulpiride include the absorption phase, followed by the distribution phase, followed by the elimination phase. The half-life of elimination in plasma is 7 hours; the volume of distribution is 0.94 L/kg. Total purge is 126 mL/min.
Sulpiride is excreted mainly through the kidneys, thanks to filtration in the glomeruli. Clearance in the kidneys is usually close to total clearance.

Acute and chronic schizophrenia (prescribed by a specialist physician).
Acute psychotic state.
Treatment of short-term symptoms of anxiety in adults in case of failure with conventional treatments.
Severe behavioral disorders in children (struggle, self-mutilation of a body part, shaping movements), especially in autism syndrome.
Brief treatment of agitated, aggressive states that cause quarrels in acute and chronic psychotic states.

Adult: Negative symptoms of schizophrenia: Start by taking 200-400 mg/time, twice daily, if necessary, the maximum dose can be increased to 800 mg/day.
Positive symptoms of schizophrenia: 400 mg/time, twice daily. Gradually increase the dose to a maximum of 1200 mg/time, twice daily.
Combined negative and positive symptoms: 400-600 mg/time, twice daily.
Children: Children over 14 years old: Take 3-5 mg/kg/day.
Children under 14 years old: No indication.
Elderly: The dose for the elderly is the same as for adults, but the initial dose is always low and then gradually increased.
Start 50-100 mg/time, twice daily, then gradually increase to an effective dose.
Renal impairment: The dose must be reduced or the interval between doses must be increased depending on creatinine clearance.
Creatinine clearance 30-60 mL/min: The dose is 2/3 of the normal dose.
Creatinine clearance 10-30 mL/min: Take a dose equal to 1/2 of the normal dose.
Clearance less than 10 mL/min: Take a dose equal to 1/3 of the normal dose.
Or it is possible to increase the gap between doses by 1.5; 2 and 3 times more than normal.
However, in cases of moderate to severe renal impairment, sulpiride should not be used, if possible.

Overdose can be manifested by signs of spasmodic dyskinesia that cause a crooked neck, protruding tongue, and stiff jaw. In some cases: very severe tremor syndrome, coma.
Treatment is limited to treating symptoms.

Hypersensitivity to sulpirides or any of its ingredients.
Adrenal myeloma.
Acute porphyrin metabolism disorders.
Suppressed central nervous system state, coma, alcohol poisoning, and neurodepressants.
Prolactin-dependent tumors (such as prolactin pituitary adenoma and breast cancer).

If there is a high fever, treatment must be discontinued, as this sign may be one of the factors of "neurotic drug malignancy syndrome".
Special Warnings and Precautions for Use: Caution must be exercised when taking sulpiride, as the drug can cause neuroleptic malignancy. During treatment, if the patient sees an unexplained high fever, the drug must be stopped immediately because high fever can be a manifestation of neuroleptic malignancy.
Sulpirides prolong the QT interval, depending on the dose. This effect increases the risk of severe arrhythmias, especially torsion, especially when there is a slow heart rate < 55 beats/minute, hypokalemia, congenital or acquired long QT interval (due to combination with another drug increases the QT interval). Before taking sulpiride, if possible, the previously mentioned factors must be excluded, an additional ECG should be done.
Caution must be exercised when using sulpirides for the elderly, especially when suffering from dementia, when there are risk factors for cerebrovascular accidents because of susceptibility to orthostatic hypotension, easy falls, drowsiness, and extrapyramidal effects. The risk of death is usually increased with the use of antipsychotics at this age.
Blood glucose monitoring for people with diabetes or at risk of diabetes must be monitored at the start of sulpride therapy.
In cases of renal failure, the dose of sulpiride should be reduced and monitoring should be increased. If kidney failure is severe, intermittent treatment should be given.
It is necessary to strengthen the monitoring of the following subjects: People with epilepsy because they are likely to have a lowered seizure threshold.
People who drink alcohol or take alcohol-containing drugs do so because it increases drowsiness.
People with mild mania, low-dose sulpirides can cause severe symptoms.
Effects on Ability to Drive and Use Machines: The drug can cause drowsiness, so caution should be exercised for drivers or machinery operators.

Pregnancy: Limit use during pregnancy and dosage should be reduced at the end of pregnancy.
Infants: neurological (and gastrointestinal) functions should be monitored in case of combination with anti-vibration drugs.
Lactation: Excretion through breast milk is estimated to be 1/1000 of the daily dose.

Sulpiride is well tolerated. At therapeutic doses, ADRs are usually milder than other antipsychotics.
Common, ADR >1/100: Nervous: Insomnia or drowsiness.
Endocrinology: Hyperprolactinemia, hyperlactation, menstrual disorders or amenorrhea.
Rare, 1/1,000 < ADR <1/100: Neurological: Hyperstimulation, extrapyramidal syndrome (restlessness, crooked neck, eye rotation), Parkinson's syndrome.
Cardiovascular: Prolonged QT interval (causing arrhythmias, apical torsion).
Rare, ADR <1/1,000: Endocrinology: Enlarged breasts in men.
Neurological: Late dyskinesia, malignant high fever syndrome due to neuroleptics.
Blood pressure: Orthostatic hypotension, bradycardia or arrhythmia.
Other: Hypothermia, sensitivity to light, jaundice due to cholestasis.
Inform a doctor of any unwanted side effects experienced when taking the drug.

Contraindications to coordination: Levodopa: there is a competitive antagonism between levodopa and neuroleptics. In the case of extrapyramidal syndrome caused by neuroleptics, levodopa (because dopaminergic receptors have been blocked by neuroleptics) should not be used, but anticholinergic drugs should be used.
In patients with palsy (parkinson) treated with levodopa, in cases where neuroleptic treatment is required, levodopa should not be continued because it may aggravate psychiatric disorders and may have an effect on receptors that have been blocked by neuroleptics.
Caution when coordinating: Alcohol: alcohol can increase the sedative effect of sedatives.
Avoid alcohol and alcohol-containing drugs or drinks.
Notes when coordinating: Hypertension drugs: increase the effect of lowering blood pressure and can cause postural hypotension (due to synergistic effects).
Other central nervous system depressants: antidepressants with sedative effects, H1 antihistamines with sedative effects, barbiturates, anxiolytic sedatives, clonidine and similar drugs, sleeping pills, methadone: increase central nervous system inhibition, can have bad consequences, especially in people who have to drive or operate machines.

Store at a temperature below 30°C, protect from light and moisture.
Shelf Life: 3 years from the date of manufacture.

Antipsychotics / Anxiolytics

N05AL01 - sulpiride ; Belongs to the class of benzamides antipsychotics.