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LogoFLUANXOL Tablets 0,25 mg FLUANXOL Tablets 0,5 mg FLUANXOL Tablets 1 mg SCHEDULING STATUS: S5 PROPRIETARY NAME (and dosage form): FLUANXOL Tablets 0,25 mg FLUANXOL Tablets 0,5 mg FLUANXOL Tablets 1 mg COMPOSITION: Each tablet contains flupenthixol dihydrochloride equivalent to flupenthixol 0,25 mg, 0,5 mg or 1 mg. PHARMACOLOGICAL CLASSIFICATION: A 2.6.5 Miscellaneous Structures PHARMACOLOGICAL ACTION: Fluanxol contains flupenthixol which is a low dose neuroleptic of the thioxanthene group. In low doses (up to 3 mg/day) Fluanxol has an anxiolytic, antidepressive and mood stabilising effect and certain activating properties. Fluanxol is mainly effective through a blockade of central monoamine receptors, especially in the dopaminergic system. Maximum serum concentration is reached about 4 hours after oral administration. The bioavailability of Fluanxol is about 40%. Protein binding is above 95%. The half-life is about 35 (19-39) hours. There are large individual variations in the therapeutic serum concentration. Fluanxol is metabolized mainly in the liver and is excreted mainly via the faeces and the urine. INDICATIONS: Short term symptomatic treatment of depression of mild to moderate severity (with or without anxiety). CONTRA-INDICATIONS: Fluanxol is not recommended for the treatment of severe depression requiring ECT and/or hospitalisation. In states of excitement or overactivity (including mania). Pre-existing CNS depression or coma, bone marrow suppression or phaechromocytoma. Severe alcohol, barbiturate and opiate intoxications. Safety in pregnancy and lactation has not been established. Not recommended for children. WARNINGS: Fluanxol should be used with caution in patients with Parkinson’s disease, severe arteriosclerosis, senile confusional state or severe hepatic, renal, cardiovascular, cerebrovascular or respiratory disease. DOSAGE AND DIRECTIONS FOR USE: Adults: Standard initial dosage is 1 mg as a single morning dose. After one week the dose may be increased to 2 mg if there is inadequate clinical response. Daily dosage of more than 2 mg should be in divided doses up to a maximum 3 mg. In view of the activating properties of Fluanxol it is advisable to give the last dose of the day no later than 4.00 p.m. Patients often respond to Fluanxol within two or three days. If no effect has been observed within one week at maximum dosage the drug should be withdrawn. Elderly: Standard initial dosage is 0,5 mg as a single morning dose. After one week, if response is inadequate, dosage may be increased to 1 mg once a day. Caution should be exercised in further increasing the dosage but occasional patients may require up to a maximum of 2 mg a day which should be given in divided doses (1 mg at breakfast time and 1 mg at about 4.00 p.m.). SIDE-EFFECTS AND SPECIAL PRECAUTIONS: Side-effects: Insomnia is the most frequent adverse event. However, as Fluanxol is a thioxanthene which is structurally related to the phenothiazines, side-effects may include: Central depression. Dry mouth, constipation, difficulty with micturition, blurred vision, mydriasis. Tachycardia, ECG changes, cardiac arrhythmias, hypotension. Delirium, agitation, catatonic-like states, insomnia, depression, miosis, EEG changes and convulsions, nasal congestion, minor abnormalities in liver function tests, inhibition of ejaculation, impotence, priapism. Hypersensitivity reactions include urticaria, exfoliative dermatitis, erythema multiforme, and contact sensitivity. A syndrome resembling systemic lupus erythematosus has been reported. Jaundice. Prolonged therapy may lead to deposition of pigment in the skin or eyes: corneal and lens opacities have been observed. Pigmented retinopathy, photosensitivity reactions. Haemolytic anaemia, aplastic anaemia, thrombocytopenic purpurea, potentially fatal agranulocytosis. Acute dystonia, a parkinsonism-like syndrome, akathisia, late effects include tardive dyskinesia and perioral tremor. Neuroleptic malignant syndrome. Amenorrhoea, galactorrhoea, gynaecomastia, weight gain, hyperglycaemia and altered glucose tolerance. Hypo- or hyperthermia. Fluanxol is less likely than the phenothiazines to cause sedation but initially it may cause drowsiness. Patients should be warned of this possibility if driving or operating machinery. Alcohol may potentiate this effect. There have been isolated reports of sudden death with phenothiazines. Phenothiazines have not been reported to cause dependence of the type encountered with barbiturates or benzodiazepines. However, mild symptoms resembling the withdrawal symptoms of dependence have been seen following the abrupt withdrawal of phenothiazines from patients receiving prolonged maintenance therapy. Special Precautions: Patients with closed-angle glaucoma, diabetes mellitus, hypothyroidism, myasthenia gravis, or prostatic hypertrophy. Epileptic patients as phenothiazines may lower the convulsive threshold. Elderly and debilitated patients may be more prone to the adverse effects of phenothiazines. Phenothiazine effects on the vomiting centre may mask the symptoms of overdosage of other agents and or disorders such as gastro-intestinal obstructions. Regular eye examinations are advisable for patients receiving long-term phenothiazine therapy and avoidance of undue exposure to sunlight is recommended. Haematological parameters should be monitored periodically. Interactions: When given with other drugs that product postural hypotension dosage adjustments may be necessary. Phenothiazines have been reported to reduce the antihypertensive action of guanethidine and other adrenergic neurone blockers. Phenothiazines may potentiate the adverse effects of other antimuscarinics. Concomitant administration of metoclopramide may increase the risk of neuroleptic-induced extrapyramidal effects and antiarrhythmics which prolong the QT interval may increase the likelihood of ventricular arrhythmias. KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT: See side-effects and special precautions. Treatment is supportive and symptomatic. IDENTIFICATION: 0,25 mg : Round, biconvex, ochre yellow, sugar-coated tablet 0,5 mg : Round, biconvex, ochre yellow, sugar-coated tablet 1 mg : Round, biconvex, ochre yellow, sugar-coated tablet PRESENTATION: Fluanxol Tablets 0,25 mg, 0,5 mg and 1 mg are blister packed in packs of 30. STORAGE INSTRUCTIONS: Store below 30ºC and protect from light. Keep out of reach of children. REGISTRATION NUMBERS: Fluanxol Tablets 0,25 mg : B/2.6.5/1371 Fluanxol Tablets 0,5 mg : B/2.6.5/1372 Fluanxol Tablets 1 mg : B/2.6.5/1380 NAME AND BUSINESS ADDRESS OF THE APPLICANT: H. Lundbeck (Pty) Ltd P O Box 2357 Randburg 2125 DATE OF PUBLICATION OF THIS PACKAGE INSERT: January 1994 Updated on this site: May 2000