Fluphenazine

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Substrate of
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Bulgaria: Moditen; Czech Republic: Moditen; Denmark: Siqualone; Finland: Siqualone; France: Modecate, Moditen; Germany: Dapatum, Fluphenazin, Lyogen; Hungary: Moditen; Ireland: Modecate; Italy: Moditen; Lithuania: Moditen; Malta: Fluphenazine, Modecate; Netherlands: Anatensol, Flufenazine; Poland: Mirenil; Portugal: Anatensol; Slovakia: Moditen; Spain: Modecate; Sweden: Siqualone; UK: Fluphenazine, Modecate.

North America

Canada: Fluphenazine, Modecate; USA: Fluphenazine.

Latin America

Brazil: Flufenan; Mexico: Siqualine.

Asia

Japan: Fludecasin, Flumezin.

Drug combinations

Chemistry

Fluphenazine Hydrochloride: C~22~H~26~F~3~N~3~OS 2HCl. Mw: 510.44. (1) 1-Piperazineethanol, 4-[3-[2-(trifluoromethyl)-10H-phenothiazin-10-yl]propyl]-, dihydrochloride; (2) 4-[3-[2-(Trifluoromethyl)phenothiazin-10-yl]propyl]-1-piperazineethanol dihydrochloride. CAS-146-56-5; CAS-69-23-8 (fluphenazine).

Pharmacologic Category

Antipsychotics; Phenothiazines. Typical Antipsychotic Agent. (ATC-Code: N05AB02).

Mechanism of action

Fluphenazine is a piperazine phenothiazine antipsychotic which blocks postsynaptic mesolimbic dopaminergic D~1~ and D~2~ receptors in the brain. Depresses release of hypothalamic and hypophyseal hormones. Believed to depress reticular activating system, thus affecting basal metabolism, body temperature, wakefulness, vasomotor tone, and emesis.

Therapeutic use

Management of manifestations of psychotic disorders and schizophrenia.

Pregnancy and lactiation implications

Unlabeled use

Pervasive developmental disorder. Nonpsychotic patient, dementia behavior in the elderly. Psychosis/agitation related to Alzheimer’s dementia.

Contraindications

Hypersensitivity to fluphenazine or any component of the formulation (cross-reactivity between phenothiazines may occur). Severe CNS depression. Coma. Subcortical brain damage. Blood dyscrasias. Hepatic disease.

Warnings and precautions

May alter cardiac conduction (life-threatening arrhythmias have occurred). May cause anticholinergic effects (use with caution in decreased GI motility, paralytic ileus, urinary retention, BPH, xerostomia, or visual problems). Blood dyscrasias might occur (use contraindicated in bone marrow suppression). Esophageal dysmotility or aspiration possible (use with caution in risk of pneumonia). May cause extrapyramidal symptoms, including pseudoparkinsonism, acute dystonic reactions, akathisia, and tardive dyskinesia. Hypotension might occur, particularly with I.M. administration. Neuroleptic malignant syndrome might occur (risk may be increased in Parkinson’s disease or Lewy body dementia). May cause orthostatic hypotension (use with caution in risk of this effect or in patients who would not tolerate transient hypotensive episodes). May be associated with pigmentary retinopathy. May cause sedation. Impaired core body temperature regulation might occur. Use with caution in severe cardiovascular disease, narrow-angle glaucoma, hepatic impairment, myasthenia gravis, Parkinson’s disease, breast cancer or other prolactin-dependent tumors, renal impairment, or respiratory disease. Use with caution in risk of seizures. May mask toxicity of other drugs or conditions (e.g. intestinal obstruction, Reye’s syndrome, brain tumor) due to antiemetic effects. Effects may be potentiated when used with other sedative drugs or ethanol. Use with caution in the elderly (increased risk for developing tardive dyskinesia). Adverse effects of depot injections may be prolonged.

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