Apexidone F.C. Tablets and Syrup – Risperidone

COMPOSITION

  • Each Apexidone 0.5 mg tablet contains: Risperidone 0.5 mg.
  • Each Apexidone 1 mg tablet contains: Risperidone 1 mg.
  • Each Apexidone 2 mg tablet contains: Risperidone 2 mg.
  • Each Apexidone 3 mg tablet contains: Risperidone 3 mg.
  • Each Apexidone 4 mg tablet contains: Risperidone 4 mg.
  • Each 1 ml Apexidone syrup contains: Risperidone 1 mg.

CLINICAL PHARMACOLOGY

Risperidone, a benzisoxazole derivative, has a high affinity to the serotonin type 2 (5-HT2), dopamine D2, and alpha-1 adrenergic receptors.

Risperidone binds with a lower affinity to the alpha-2 adrenergic and histamine H1 receptors.

Risperidone does not bind to dopamine D1 or muscarinic cholinergic receptors. Risperidone causes less depression of motor activity and induction of catalepsy than traditional antipsychotics.

Extrapyramidal effects are reported to be significantly less than classical neuroleptics.

Pharmacokinetics

Absorption: Is rapid nearly complete and is not affected by food. Peak plasma concentration is reached within 1-2 hours.

Distribution: Is rapid. Risperidone is bound to albumin and alpha-1 acid glycoprotein.

Elimination: Renal 70%, fecal 14% (one week after administration). The elimination half-life of risperidone is 3 hours and 24 hours for the metabolite and the active fraction.

Risperidone might increase serum prolactin level.

INDICATIONS

  • Apexidone is used for the treatment of acute and chronic psychosis.
  • In controlled clinical trials, Apexidone improves both positive and negative symptoms.

DOSAGE AND ADMINISTRATION

Adults

The dose of Apexidone must be titrated gradually.

Adult patients should start with 1 mg b.i.d. The dosage should be increased to 2 mg b.i.d. on second day and to 3 mg b.i.d. on the third day.

Acute or chronic patients should start with 2 mg/day.

The maintenance dose can be kept at 3 mg b.i.d. or increased or decreased if needed.

The usual optimal dosage is 4 to 8 my daily. Maximum dose is 16 mg daily.

Pediatrics and Adolescents

The dosage of Apexidone should be initiated at 0.5 mg once daily administered as a single daily dose in either the morning or evening.

Dosage adjustment, if indicated, should be at intervals not less than 24 hours, in increments of 0.5 mg or 1 mg/day as tolerated to a recommended dose of 3 mg/day.

WARNINGS & PRECAUTIONS

Special warnings and precautions for use

Intraoperative Floppy Iris Syndrome (IFIS) has been observed during cataract surgery in patients treated with medicines with alpha-1a adrenergic antagonist effect, including risperidone and paliperidone. IFIS may increase the risk of eye complications during and after the operation. Current or past use of medicines with alpha-1a adrenergic antagonist effect should be made known to the ophthalmic surgeon in
advance of surgery.

The potential benefit of stopping alpha-1a blocking therapy prior to cataract surgery has not been established and must be weighed against the risk of stopping the antipsychotic therapy.

During the initial dose titration period, risperidone can cause orthostatic hypotension and tachycardia.Therefore, risperidone should be used with caution in patients with cardiovascular diseases and in patients taking medications to lower blood pressure.

Neuroleptic malignant syndrome has been reported in association with neuroleptic medications, in such case all antipsychotic drugs including
risperidone should be stopped.

All antipsychotic drugs should be discontinued if symptoms and signs of tardive dyskinesia appear.

Increase chance of death in elderly patient with dementia-related psychosis.

“Use in specific population/Pregnancy (Non-teratogenic effects):

Neonates exposed to antipsychotic drugs during the third trimester of pregnancy are at risk for extrapyramidal and/or withdrawal symptoms
following delivery. There have been reports of agitation, hypertonia, hypotonia, tremor, somnolence, respiratory distress and feeding disorder in these neonates.

These complications have varied in severity; while in some cases symptoms have been self-limited, in other cases neonates have required intensive care unit support and prolonged hospitalization.

These products should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

SIDE EFFECTS

In general, the side effects are comparable to placebo. In many cases, it has been difficult to differentiate side effects from symptoms of underlying psychosis; the most frequent side effects are insomnia, agitation, anxiety and headache.

Less frequent: somnolence, impaired concentration, dizziness, constipation, anorexia, abdominal pain, abnormal vision, tachycardia and fatigue.

Extrapyramidal symptoms are usually mild and reversible upon dose reduction or administration of antiparkinsonian drugs.

Risperidone may elevate plasma prolactin level leading to amenorrhea, galactorrhea or menorrhagia.

Weight gain, erectile dysfunction, orgastic dysfunction and ejaculatory dysfunction have been observed.

DRUG INTERACTIONS

Centrally acting drugs, alcohol: levodopa & other dopamine agonists, antihypertensives, carbamazepine, phenothiazines, tricyclic anti-depressants selective serotonin reuptake inhibitors and some beta blockers.

CONTRAINDICATIONS

Hypersensitivity to the drug.

PACKAGE AND STORAGE

  • Apexidone 0.5 mg: Pack of 30 film coated tablets.
  • Apexidone 1 mg: Pack of 20 film coated tablets.
  • Apexidone 2 mg: Pack of 20 film coated tablets.
  • Apexidone 3 mg: Pack of 30 film coated tablets.
  • Apexidone 4 mg: Pack of 30 film coated tablets.
  • Apexidone Syrup: Pack of 100 ml syrup.
Apexidone F.C. Tablets and Syrup - Risperidone
Apexidone F.C. Tablets and Syrup – Risperidone
  • Store in a dry place at temperature not exceeding 30 °C.
  • Keep All Medicines Out of Reach of Children
  • Manufactured by: Apex Pharma – S.A.E-Badr City- Egypt.

Product Ref: N05AX08