Levosulpiride
Also known as: Benzamide
Levosulpiride is a substituted benzamide antipsychotic which is reported to be a selective antagonist of central dopamine (D-2, D-3 and D-4) receptors. Levosulpiride is also calimed to have mood elevating properties. Levosulpiride is used in the treatment of psychoses such as schizophrenia, anxiety disorders, vertigo and also in peptic ulceration.
Primary Characteristics
Levosulpiride is also known as Benzamide.
It belongs to Sulphamoylbenzamide.
It belongs to D2 antagonist pharmacological group on the basis of mechanism of action and also classified in Antidepressant pharmacological group. It is also classified under Psychotherapeutic Drugs .
Molecular Weight: 341.4 · Solubility in Water: insoluble · Solubility in Alcohol: slightly soluble · Non-proprietary name: Levosulpiride · pH: 8.
Pharmacokinetics
Absorption: Levosulpiride has an oral bioavailability is 35% (±5%).
Distribution: Levosulpiride has a plasma protein binding is >40 %.
Elimination: it is metabolised via hepatic, plasma half-life is 8-9 hr, renal excretion is Unchanged 25%.
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Indications
Levosulpiride is primarily indicated in conditions like Anxiety, Depression, Gastro-esophageal reflux disease, Irritable bowel syndrome, Schizophrenia, Tourette's syndrome.
Levosulpiride is also indicated for secondary conditions like Peptic ulcer, Vertigo.
Contraindications
Levosulpiride is contraindicated in conditions like Epilepsy, Hyperprolactinaemia, Mania, Breast feeding, Hypersensitivity to any component of product, Gastrointestinal hemorrhage, pheochromocytoma.
Dosage
Levosulpiride's dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 500 mg | 500 mg | Every 24h | IM | |
| 200 – 400 mg | — | Every 12h | PO | For the treatment of schizophrenia: upto 1200mg twice daily may be given in patients with positive symptoms or upto 800 mg in patients with mainly negative symptoms. |
| 25 mg | 25 mg | Every 8h | PO | For GERD, irritable bowel disease (IBS), dyspeptic syndrome, essential cephalgia. |
| Paediatric Dosage (20kg) | ||||
| 4 mg/kg | 4 mg/kg | — | PO | This is the dose for children above 14 years of age. (i.e. 3-5mg/Kg daily) |
| Neonatal Dosage (3kg) | ||||
| 0 – 0 | — | — | Not recommended in this age group | |
Drug Interactions
Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Side Effects
Levosulpiride in overdosage may give rise to further complications which include Amenorrhea, Gynacomastia , Galactorrhea, Changes in libido.
Levosulpiride produces potentially life-threatening effects which include Neuroleptic Malignant Syndrome , Neuroleptic malignant syndrome. Careful monitoring is needed with proper medical management.
Levosulpiride is known to cause more or less tolerable side effects which are usually transient. These include Agitation , Dyskinesia , Galactorrhea, Gynecomastia, Hyperprolactinemia, Hypotension , Overstimulation , Sedation , Sleep disturbance, Tardive dyskinesia.
Warnings / Precautions
Available Brands
Storage Conditions
Drug Classification
- 1.24.1 — Drugs used in psychotic disorders
Manufacturers
Manufacturers of Levosulpiride in Pakistan: