Levosulpiride

Therapeutic Indications

Levosulpiride is classified as an antipsychotic medicine, also known as tranquilizer or neuroleptic. The drug has a number of properties that include antiemetic as it prevents vomiting, antidepressant, antipsychotic and anti-dyspeptic as in anti-indigestion. The drug is used in:

• Irritable bowel syndrome
• Gastroesophageal reflux disease
• Vertigo
• Hallucinations
• Anxiety disorder
• Schizophrenia
• Premature ejaculation
• Depression
• Dyspepsia
• Emesis
• Psychosis
• Somatoform disorder
• Burning mouth syndrome
• Diabetic gastroparesis
• Indigestion
• Frequent persistent heartburn
• Acute unilateral labyrinthine dysfunction
• Cataplexy
• Heartburn
• Nausea
• Vomiting

Do I need a prescription?

Levosulpiride can be bought from pharmacies and online drug stores. But a doctor’s prescription is a must.

Dosage

The dosage for levosulpiride will depend on the condition being treated, the age and how you respond to the first dose. The first dosage is usually limited to a small amount that is effective so as to reduce on the side effects that may occur. For better results, dose increment is usually advised. If you are elderly, dose reduction is recommended. The dosage that is recommended for a number of conditions include:

• Dyspepsia and other GI problems: 25 mg three times a day.
• Schizophrenia: Up to 1200 mg taken twice a day in patients with positive symptoms
• Up to 800 mg taken twice a day in patients with negative symptoms

Chemical Composition

The tablets contain 25 mg of levosulpiride. The drug can be a single composite and also as combinations.

Mechanism of Action (MOA)

Levosulpiride works by inhibiting a number of neurotransmitters in the brain as well as in specific stomach and intestine regions. Levosulpiride blocks presynaptic dopaminergic receptors. This results in reduced synthesis of dopamine and its release and at higher doses, it causes receptor antagonism at postsynaptic D2. This makes it possible for the drug to treat positive and negative symptoms in schizophrenia.

It also increases the production of acetylcholine that improves the movement in the intestines and stomach and also prevents acid reflux.

Facts on Levosulpiride

• Levosulpiride is not approved for use in the USA by the U.S.Food and Drug Administration(FDA)
• Levosulpiride has been shown to be effective in the treatment of premature ejaculation.
• Levosulpiride hold not be used in pregnancy and by nursing mothers.
• Use of alcohol committed with Levosulpiride is discouraged.
• Levosulpiride is mainly used in the treatment of mental disorders.
• The effects or Levosulpiride can be observed after 1-2 hours after being administered orally and last for about 5-8 hours.

Contraindications

Levosulpiride use is not recommended in a number of conditions as it may worsen them or result in severe side effects. Inform your doctor if you have any of the following conditions as it may affect the prescription:

• Levosulpiride is not recommended if you have an allergic reaction to the active ingredient.
• Epilepsy
• Bipolar disorder
• Tumor in the adrenal glands(pheochromocytoma)
• Pituitary prolactinoma
• Gastrointestinal perforation (Ruptured bowel)
• Breast cancer
• Parkinson disease
• Severe renal or hepatic diseases
• Levosulpiride should not be used if you are pregnant or planning to be pregnant. It should only be used when the benefits outweigh the risks.
• Levosulpiride is secreted in breast milk and should not be used by nursing mothers as it may harm the baby thus breastfeeding should be stopped when using the drug.
• Alcohol intoxication may result in severe side effects.
• Porphyrias
• In the elderly
• Hypokalemia
• Prolactin imbalance
• Asthmatics
• Heart diseases
• In children less than 14 years
• Leukopenia
• Manic states

Side effects

Levosulpiride use may result in a number of side effects apart from the desired effects. The side effects may occur in some individuals while others may not experience them. The effects depend on the dosage and duration of use. Some may stop with the continued use of the drug. The side effects may be common and less serious while others are rare and very serious requiring medical attention. Inform your doctor of any side effects you experience while using the drug especially if they do not go away. Common side effects include:

• Increase in blood prolactin levels
• Sedation
• Galactorrhea
• Hypotension
• Overstimulation
• Tardive dyskinesia
• Gynecomastia
• Agitation
• Sleep disturbance
• A headache
• Unusual weakness and tiredness
• Irregular menstrual cycle
• Breast tenderness
• Constipation
• Weight gain
• Acute muscular dystonia
• Elevation in liver transaminases
• Akathisia
• Lightheadedness
• A heartbeat that is irregular or rapid
• Abdominal cramps and pain

Rare and very serious side effects include:

• Changes in libido (decrease)
• The neuroleptic malignant syndrome characterized by rigid muscles and a fever that is high.
• The absence of menstrual periods
• Galactorrhea
• Enlargement of a breast in men
• Milk secretion that’s spontaneous
• Uncontrolled sweating
• Fever
• Increase in salivation

In case you accidentally take an overdose of Levosulpiride, contact your doctor immediately or rush to the nearest emergency center of the nearest hospital and carry the drug package or label with you for identification. Symptoms of an overdose include the drop in blood pressure, excessive drowsiness, being agitated and coma.

Drug Interactions

Inform your doctor of any products and medicines you are using whether over the counter drugs, prescription drugs, vitamin supplements, and any herbal supplements. This information will help your doctor to limit or prevent drug interactions. When some products and drugs are taken together with Levosulpiride, they increase the chances of severe side effects occurring or interfere with the drug functioning lowering its effectiveness. Products and drugs that interact with Levosulpiride include:

• Antacids that contain magnesium and aluminum lower uptake of Levosulpiride form the intestines.
• Sucralfate also lower uptake of Levosulpiride form the intestines.
• Chloroquine
• Corticosteroids
• Furosemide
• Cisapride
• Levodopa
• Antihypertensive medications
• When taken with the drug can result in the central nervous system depression. Signs of CNS depression include increased drowsiness, confusion, anxiety and lack of focus.
• Smoking while using the drug increases the metabolism of the drug that may require the dosage to be increased to be effective.
• Anticholinergics
• Concurrent use opposes the antipsychotic effects of Levosulpiride.
• Quinine
• Terfenadine
• Atomoxetine
• Laxatives
• Antiarrhythmics
• Diltiazem
• Pregabalin
• Tramadol
• Ipratropium

What to do if you skip a dose?

If you skip a dose of Levosulpiride, take it immediately you notice. But if it close to the next dose, skip it and continue with the normal schedule. Do not take double the dose to compensate for the skipped dose. If you skip doses frequently, set a reminder or have a family member remind you. Skipping doses makes the drug not to be effective.

Precautions

When using Levosulpiride, a number of precautions should be considered. The precautions include:

• Allergic reactions to the active ingredient of Levosulpiride: Allergic reactions signs include rashes, swelling of the throat, face, lips, tongue, throat, difficulties in breathing and loss of consciousness.
• While you use Levosulpiride, ensure that you follow your doctor’s instructions for it to work effectively. Do not change the dosage.
• Levosulpiride should be taken at least 30 minutes before meals.
• The drug causes drowsiness thus it is not recommended to take part in activities that require high alertness like driving and operating heavy machinery.
• If you are elderly, using the drug should at close observation from your doctor because of the increased risk of adverse effects.
• Levosulpiride should be used in caution if you have a blood clotting disorder, any heart problems and have ever suffered from a stroke.
• Levosulpiride should not be used if you have low potassium levels in body fluids and low white blood cell count, which is characterized by being prone to infections, mouth ulcers, fever, and sore throat.
• Expecting or planning to expect as Levosulpiride may harm the growing fetus.
• Nursing mothers. Levosulpiride is secreted into breast milk and may harm the nursing baby.
• A history of seizures or epilepsy.
• Cancer or cancer-related disorders.
• Levosulpiride should not be used if you have gastrointestinal perforations.
• Do not take Levosulpiride that is expired as its effectiveness will have reduced thus affects its working. Always check the package for expiry date.
• Levosulpiride should be stored away from the sun and heat at room temperature.
• If you experience the following signs while on Levosulpiride, immediately contact your doctor: lack of menstruation, abnormal secretion of milk, the decrease in sexual desire, fever and stiffness of muscles.
• Renal impairment
• Avoid the use of alcohol while you are taking Levosulpiride.
• Taking of Levosulpiride interferes with the levels of prolactin hormone in the body, thus inform your doctor before undergoing a laboratory test of the same.
• Take plenty of water while using Levosulpiride.
• Inform your doctor if you have a surgery scheduled or have already had one before using the drug.

Different brands and manufacturing companies of the drug

Levosulpiride is manufactured by different companies at different strengths. It can be bought in a tablet form, capsule form or injectable. The strengths can be 25 mg, 50 mg, 75 mg or 100 mg.

Levosulpiride ca also be found in tablets as a single ingredient or in combinations such as:

• Leosulpiride and Esomeprazole
• Levosulpiride and Ilaprazole.
• Levosulpiride and Rabeprazole
• Levosulpiride and Pantoprazole

Levosulpiride is marketed under different brand names by different pharmaceuticals that include:

• Lesuride – Sun Pharmaceuticals Ltd
• Volapride – Mankind Pharmaceuticals Ltd
• Micropride – Micro Labs Ltd
• Neopride – Mankind Pharma Ltd
• Leovogastrol – Alembic Pharmaceuticals Ltd
• Levazeo – Torrent Pharmaceuticals Ltd
• Biomotil – Biotoscana
• Domatil – Daewoo
• Happi-L – Zydus
• Lorab-L – Lifecare
• Panlife –LS – Beulah
• Emlevo – Emcure Pharmaceutical Ltd
• Lesu – Vanran Healthcare Pvt Ltd
• Leviride – Intas Pharmaceutical Ltd
• Livogold – Lupin Lbaoratories Ltd
• Neopride – Intas Pharmaceutical Ltd
• Nexipride – Sun Pharmaceuticals Industries Ltd
• Psycolev – Invision Medi Sciences Pvt Ltd ( Marx Remedies)
• Sertive – Emcure Pharmaceuticals Ltd
• Zenpride – Eris (Enzo Biopharma)

The above list is not the complete list for Levosulpiride brand names.

Substitutes of the drug

Substitutes of Levosulpiride 25 mg tablet have the same composition and strength and include:

• Retune-Ls 25 mg tablet – Zunentus Healthcare Ltd
• Tilpride – Tablets India Ltd
• Lesuride 25 mg tablet/ Injection – Sun Pharma Laboratories Ltd
• Ulpride 25 mg tablet – Eris Life Sciences Pvt Ltd
• Nexipride 25 mg injection – Sun Pharma Laboratories Ltd
• Levazeo 25 mg tablet – Torrent Pharmaceuticals Ltd
• Skizolev 25 mg tablet – Alkem Laboratories Ltd
• Rithem 25 mg tablet – Cadila Pharmaceuticals Ltd
• Levipride 25 mg Tablet – Torrent Pharmaceuticals Ltd
• Levogastrol 25 mg tablet – Alembic Ltd
• Neopride 25 mg tablet – Intas Pharmaceutical Ltd

References

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