Levosulpiride 25 mg
Reg. No.: VD-24418-16
Each tablet contains:
Levosulpiride……………………………………………………………………………………………………. 25 mg
Excipients: Lactose DC, Microcrystalline Cellulose 102, Sodium starch glycolate, Collodidal Silicon dioxide, Magnesium stearate.
The mechanism of action of Levosulpiride is selective inhibition on dopamine D2 receptor, mainly in the presynapse membrane during transmitter dopamine.
The drug increases the motility of the gastrointestinal tract (stomach, intestine and gallbladder), thus accelerating the process of empty stomach, shorter the delay of food in the intestine and increased the excretion of bile that results in reducing the symptoms of functional gastrointestinal disorders.
Levosulpiride is absorbed slowly from the gastrointestinal tract, peak plasma concentration after about 3 hours. Oral bioavailability is about 30% with marked interindividual differences. The drug is rapidly distributed to tissues but difficult to cross blood-brain barrier. Levosulpiride is bound 40% to plasma protein and the half-time is about 6-9 hours. Levosulpiride are excreted mainly in urine as unchanged. Levosulpiride cross to breast milk.
It is mainly used in the treatment of psychoses such as schizophrenia. It has also been given in the management of Tourette’s syndrome and benign peptic ulceration (including irritable bowel disease, decreased gastrointestinal motility, and nausea and vomiting).
DOSAGE AND ADMINISTRATIONS
In the treatment of schizophrenia:
Adults and children aged 14 years and over: Initial oral doses of 200 to 400 mg are given twice daily, increased if necessary up to a maximum of 1200 mg twice daily in patients with mainly positive symptoms or up to a total of 800 mg daily in patients with mainly negative symptoms. Patients with mixed positive and negative symptoms, with neither predominating, are given usual doses of 400 to 600 mg twice daily.
Elderly patients: Lower initial doses have been recommended in elderly patients, subsequently adjusted as required.
Children under 14 years of age: No indications.
Renal impairment: It has been recommended that the oral dose be reduced according to CC as follows:
+ CC 30 to 60 mL/minute: Two-thirds of the usual dose, or pro-long dosage interval by a factor of 1.5.
+ •CC 10 to 30 mL/minute: Half the usual dose, or double dosage interval.
+ CC less than 10mL/minute: One-third of the usual dose, or triple dosage interval However, drug should be avoided if CC is less than 10mL/minute.
From 2 to 12 years: 50 to 400 mg twice daily may be given to those aged from 2 to 12 years.
From 12 to 18 years: 100 to 400mg twice daily to adolescents aged from 12 to 18 years.
Benign peptic ulceration:
Adult: 25 mg, three times daily before meals.
Elderly: Dose reductions may be necessary.
Pregnant women or women of childbearing potential who might become pregnant.
Patients with gastro-intestinal tract bleeding, mechanical disorder or perforation.
Patients with pheochromocytoma; hypertension due to release of cathecolamine may be induced.
Patients with a hypersensitivity to Levosulpiride or intolerability.
Patients with epilepsy, mania, or patients in manic step of manic-depressive psychosis.
It is thought that there’s an interaction between hypomazia and hyperprolacinemia, which most psychotropic drugs have. Therefore, the drug should not be administered in patients with malignant mastopathy.
The following patients should be carefully administered.
- Patients with hypertension.
- Children: Since extrapyramidal symptoms may develop, overdose should be warned.
- The elderly: Particular care, including the dosage or the administration interval, should be taken in the elderly where renal function may be reduced thus leading to high concentration of the drug in blood plasma with the consequent prolongation of action.
Levosulpiride must not be used when stimulation of GI motility can be hazardous, for example, in presence of GI hemorrhages, mechanical obstruction or perforations.
It is recommended to be cautions when administering Levosulpiride altogether with alcohol intake, since it can produce an increase in the sedative effects of alcohol.
Levosulpiride can cause somnolence or sedation and dyskinesia in some patients; if some of these symptoms appear, avoid driving a vehicle or machinery.
Special caution is recommended in case of administering Levosulpiride together with psychopharmaceutical drugs, since an increase of undesired effects may occur.
Prior to prescribing the drug, a patient should be advised that there’ll be such side effects as lactation, increase in secretion of prolactin due to pathocrine regulation of diencephalon.
Since pathocrine regulation of diencephalons or extrapyramidal symptom may occur, the safety and effectiveness in use should be carefully considered.
Endocrine system: Occasionally, amenorrhea suspected to result from diencephalic pathocrine (disorders in secretion of gonadotropin or prolactin), continuous lactation, gynecomastia may occur. The patients should be carefully observed, and if they occur, the administration should be discontinued.
Extrapyramidal system: Rare cases of tremor, numbness of tongue, anxiety may occur may require the discontinuance of the administration. Rarely, also, involuntary motion surrounding lips and so on due to the long-term therapy may be developed, and it can be prolonged even after the discontinuance of the use.
Gastro-intestinal system: Occasionally, dipsia, heartburn, nausea, vomiting, diarrhea, and constipation may occur.
Circulatory system: Hypertension.
Others: If eruption or edema occurs infrequently, the administration should be discontinued. And occasionally heat, malaise, insomnia, drowsiness, dizziness, and titubation may occur, and rarely impotence may occur.
In the long-term use, such side effects as amenorrhea, gynecomastia, galactorrhea, and increase or decrease of sexual desire may occur. They are the effect on the 2nd cervical verterbrae of hypothalamic hypophysis gonad, which is reversible.
* Inform your doctor in case of any adverse reactions related to drug use.
Since the prokinetic activity of the drug may be antagonized by anticholinergic agents (e.g., Atropin, Methyl scopolamine etc.) or analgesic agents, the concomitant use with those agents is not recommended.
Nausea, vomiting, anorexia, as index in saturation of digitalis drugs, may be masked. Therefore, the patients receiving digitalis drugs should be carefully observed, and also the administration should be cautioned.
-Since the concomitant use of the drug with other benzamide drugs (e.g., Methochlopramide, etc.) may cause disorder of endocrinal function or extrapyramidal symptoms, the administration should be cautioned.
The concomitant use of the drug with psychotropic drugs should be warned to avoid unexpected reactions due to the drug interactions. And alcohol should not be taken concomitantly.
Antacid and sucralfat reduced the bioavailability of drug, it is recommended that KUPLEVOTIN be taken at before 2 hours.
Levodopa may oppose the antipsychotic action of Levosulpiride, conversely Levosulpiride can cause decrease the efficacy of Levodopa in the management of Parkinsonism.
Arrhythmia especially prolonged QT interval with the concurrent use of Atomoxetine, Antiarrhythmics, Terfenadine, Chloroquine, Quinine, Cisapride, drugs causing hypokalemia (corticosteroids, laxatives, diuretics like Furosemide).
USE IN PREGNANCY
Animal studies have demonstrated teratogenic effects on fetus and the safety use in pregnancy has not been established. Therefore, the drug should not be administered to pregnant women or women of childbearing potential who might become pregnant.
USE IN LACTATION
Since safety use in lactation has not been established, the drug should be used only when the expected benefits clearly outweigh the potential risks to the fetus.
Since the drug has an antiemetic activity, which may mask vomiting associated with encephalophyma, ileus, or intoxication due to the other drugs, the patients should be carefully observed and the administration cautioned.
Contraction of testis and fertility study in animal studies on chronic toxicity has demonstrated that the drug caused the reduced fertility.
In the long-term therapy with a large dose to rats and mice, tumor generation on p. gland, mammary etc. line was higher than the control group.
10 Tabs./ Blister x 3 Blisters/ Box.
36 months from manufacturing date.
Do not exceed the expired date for use printed on the box.
Preserve in tight containers. Store at room temperature not exceeding 300C.
Keep out of reach of children.
Read Dosage & Administration carefully before using.
For any more information, please consult your doctor.
KOREA UNITED PHARM. INT’L JSC
No. 2A, Tu Do Boulevard, Vietnam – Singapore Industrial Park, Thuan An Town,
Binh Duong Province, Vietnam.