Istefral

Istefral Uses, Dosage, Side Effects, Food Interaction and all others data.

Istefral first appeared in published literature in 1967. Clinical studies show a greater effect on treating the negative symptoms of schizophrenia rather than positive symptoms at low doses, though the effects are more equal at higher doses.

Istefral is not approved by the FDA, Health Canada, or the EMA; though it is approved in individual European countries.

Istefral is a substituted benzamide derivative and a selective dopamine D2 antagonist indicated to treat acute and chronic schizophrenia. It has a short duration of action as it is given twice daily, and a wide therapeutic window as patients have survived single doses as high as 16g. Patients should be counselled regarding increased motor agitation, extrapyramidal reactions, and neuroleptic malignant syndrome.

Table Of contents

• Istefral
• Uses
• Dosage
• Side Effect
• Precautions
• Interactions
• Uses during Pregnancy
• Uses during Breastfeeding
• Accute Overdose
• Food Interaction
• Half Life
• Volume of Distribution
• Clearance
• Interaction With other Medicine
• Contradiction
• Storage

Trade Name	Istefral
Generic	Sulpiride
Sulpiride Other Names	Sulpirid, Sulpirida, Sulpiride, Sulpiridum, Sulpyrid
Type
Formula	C15H23N3O4S
Weight	Average: 341.426 Monoisotopic: 341.140926929
Protein binding	Sulpiride is approximately 40% protein bound in plasma, particularly to albumin.
Groups	Approved, Investigational
Therapeutic Class
Manufacturer
Available Country	Chile
Last Updated:	September 19, 2023 at 7:00 am

Uses

Istefral is a selective D2 dopamine receptor antagonist indicated to treat chronic and acute schizophrenia.

Istefral is indicated for the treatment of acute and chronic schizophrenia.

Istefral is also used to associated treatment for these conditions: Acute Schizophrenia, Chronic Schizophrenia, Constipation, Dyspepsia, Menière's Disease, Nausea, Psychosis, Schizophrenia, Vomiting

How Istefral works

Istefral is a selective dopamine D2 and D3 receptor antagonist. In silico studies show that sulpiride may interact with the Asp-119 and Phe-417 amino acid residues of these receptors. It is estimated that D2 receptors should be 65-80% occupied for optimal treatment and minimal adverse effects.

Toxicity

Patients experiencing an overdose of sulpiride may present with hypotension, sinus tachycardia, arrhythmia, dystonia, CNS depression, hallucinations, vomiting, agitation, dysarthria, salivation, as well as increased muscle tone, hyperreflexia, and extensor plantar reflex. Patients should be treated with symptomatic and supportive treatment.

Food Interaction

• Avoid alcohol. Alcohol enhances the sedative effects of sulpiride.

Volume of Distribution

The average volume of distribution of sulpiride is 2.72 ± 0.66 L/kg.

Elimination Route

Istefral has an oral bioavailability of 27 ± 9%. A 100-108 mg dose of sulpiride reaches a C_max of 232-403 ng/mL, with a T_max of 8.3 h. In another study, the AUC of a 100mg oral dose of sulpiride is 1156 ± 522 h*ng/mL and for an intravenous dose is 3981 ± 813 h*ng/mL.

Half Life

Reports of the half life of sulpiride have only been performed with small numbers of subjects. Therefore, the average half life may be 7.15 hours to 8.3 hours.

Clearance

The total systemic clearance of sulpiride if 415 ± 84 mL/min, while the mean renal clearance was 310 ± 91 mL/min.

Elimination Route

An intravenous dose of sulpiride is 70 ± 9% eliminated in the urine within 36 hours, while an oral dose is 27 ± 9% eliminated in urine. In both cases, the dose is recovered as the unchanged parent compound.

Innovators Monograph

You find simplified version here Istefral