Apo-Trifluoperazine

Apo-Trifluoperazine

trifluoperazine

Manufacturer:

Apotex

Distributor:

Pharmaforte
Full Prescribing Info
Contents
Trifluoperazine.
Description
Each film-coated tablet contains trifluoperazine 1 mg or 5 mg, respectively.
Action
Pharmacotherapeutic Group: Antipsychotic/antiemetic.
Indications/Uses
Trifluoperazine, a piperazine phenothiazine derivative, is indicated in the treatment of psychotic disorders particularly to produce a quieting effect in hyperactive or excited psychotic patients. Used in the treatment of behavioral disorders in adults, in the aged and in children, and to prevent or relieve nausea and vomiting due to stimulation of chemoreceptor trigger zone.
Dosage/Direction for Use
Adjust the dosage to the individual and severity of condition. When maximum therapeutic dose is obtained, dosage is gradually reduced to maintenance level.
To control anxiety, for adults, treatment normally starts with 1 mg twice daily. Dosage exceeding 4 mg daily are rarely needed.
Psychotic patients: for adequately supervised adults, the usual starting dose ranges between 2 to 5 mg twice daily with optimum response occurring in most patients on 15 to 20 mg daily, but some patients may require as much as 40 mg daily. Ordinarily 2 to 3 weeks are required to obtain optimum response and improvement. Maintenance dosage should not be instituted prematurely. In hospitalized psychotic children: 6 to 12 years old, 1 mg may be given once or twice daily. This dose may be increased if necessary but extra caution must be exercised at higher doses. As an antiemetic: for adults, 1 or 2 mg twice daily, or as required.
Overdosage
Symptoms: Symptoms of minor overdosage include drowsiness, dizziness or muscular twitching. Gross overdosage may produce CNS depression, dystonia, torticollis, tremor, salivation, difficulty in swallowing and disturbances of gait.
Treatment: Treatment is essentially symptomatic and supportive. In adults, perform gastric lavage or, in children, induce emesis and if there is no immediate response, use gastric lavage. Centrally acting emetic to induce emesis are ineffective due to the antiemetic effect of trifluoperazine. Stimulants that may cause convulsions (e.g., picrotoxin or pentylenetetrazol) should be avoided. Hypotension should be treated with levarterenol or phenylephrine. Epinephrine should not be used because it may cause futher hypotension. Extrapyramidal symptoms may be treated with diphenhydramine or benztropine mesylate.
Contraindications
Comatose or depressed states due to CNS depressants; blood dyscrasias; bone marrow depression; liver damage. Hypersensitivity to trifluoperazine; cross-sensitivity to other phenothiazines may occur.
Special Precautions
Animal reproductive studies and clinical experience to date have not demonstrated any teratogenic effect from trifluoperazine. However, the drug should used in pregnant women only when deemed necessary for the patient's welfare. Use of the drug should also be avoided during lactation.
Phenothiazines may increase the effects of general anesthetics, opiates, barbiturates, alcohol and other CNS depressants as well as atropine and phosphorous insecticides.
Avoid epinephrine in the treatment of phenothiazine induced hypotension because phenothiazines may reverse epinephrine's action and thereby cause a further fall in blood pressure.
Hypotension, which is typically orthostatic, may occur especially in elderly and in alcoholic patients. This effect may be additive with other agents that cause a lowering of blood pressure. Exercise special care in those patients in whom a hypotensive crisis would be undesirable such as those with arteriosclerosis or other cardiovascular disease.
Prolongation of the QT interval, flattening and inversion of the T wave and appearance of a wave tentatively identified as a bifid T or a U wave have been observed in some patients receiving phenothiazines. These changes appear to be reversible and related to a disturbance in repolarization. Give phenothiazines cautiously to patients with heart disease. Most reported cases of agranulocytosis associated with the administration of phenothiazines derivatives have occurred between the fourth and tenth week of treatment. Therefore, observe patients on prolonged therapy with particular care during that time for the appearance of such signs as sore throat, fever and weakness. If these symptoms appear, discontinue the drug and perform WBC and differential counts. Routine periodic WBC and differential counts are also advisable during prolonged but uncomplicated therapy.
If bilirubinemia, bilibinuria or icterus occurs, discontinue the drug and perform liver function tests. Routine periodic liver function test are advisable during prolonged therapy. Phenothiazines have been associated with retinopathy. Discontinue trifluoperazine if retinal changes are observed.
Use trifluoperazine cautiously in patients with a history of seizures.
The occasional increase in physical activity resulting from trifluoperazine administration may augment the severity of pain in angina pectoris patients. Observe such patients carefully and withdraw the drug if necessary.
Where patients are participating in activities requiring complete mental alertness such as driving an automobile or operating machinery, administer the phenothiazine cautiously, forewarn the patient and increase the dosage gradually.
Trifluoperazine's antiemetic effect may mask signs of overdosage of toxic drugs or obscure the diagnosis of conditions such as intestinal obstruction and brain tumor.
Use In Pregnancy & Lactation
Pregnancy: Teratogenic effects have not been demostrated. However, the drug should be used in pregnant women only when essential. Use of the drug should be avoided during lactation.
Adverse Reactions
Adverse effects with different phenothiazines vary in type, frequency and mechanism of occurrence, i.e., some are dose-related, while others involve individual patient sensitivity. Some adverse effects may be more likely to occur; or occur with greater intensity, in patients with special medical problems, e.g., patients with mitral insufficien­cy or pheochromocytoma have experienced severe hypotension following recommended doses of certain phenothiazines.
In general, members of the piperazine group of phenothiazines have more marked stimulating effects, are more likely to cause motor disorders associated with ex­trapyramidal reactions, particularly in children, but are less likely to cause blood dyscrasias, hypotension, tachycardia, and drowsiness than the members of the other phenothiazine groups. Not all of the following adverse reactions have been observed with every phenothiazine derivative, but they have been reported with one or more and should be borne in mind when drugs of this class are administered.
Behavioral reactions: oversedation; impaired psychomotor function; paradoxical effects, such as agitation, excitement, insomnia, bizarre dreams, aggravation of psychotic symptoms, and toxic confusional states.
CNS: extrapyrimidal reactions, including Parkinsonism (with motor retardation, rigidity, masklike facies, tremor, salivation, etc); dystonic reactions (including facial grimacing, tics, torticollis, oculogyric crises, etc); and akathisia. Persistent dyskinesias resistant to treatment have also been reported. In addition, slowing of EEG, disturbed body temperature, and lowering of the convulsive threshold have occured.
Tardive Dyskinesias: Tardive dyskinesia may appear in some patients on long-term antipsychotic therapy or may appear after the drug therapy has been discontinued. The risk appears to be greater in elderly patients on high dose therapy, especially females. The symptoms are persistent and in some patients appear to be irreversible. The syndrome is characterized by rhythmical involuntary movements of the tongue, face, mouth or jaw (e.g. protrusion of tongue, puffing of cheeks, puckering of mouth, chewing movements). Sometimes these may be accompanied by involuntary movements of extremities.
There is known effective treatment for tardive dyskinesia; anti-parkinsonian agents usually do not alleviate the symptoms of this syndrome. All antipsychotic agents should be discontinued if these symptoms appear. Should it be necessary to reinstitute treatment or increase the dosage of the agent, or switch to a different anti-psychotic agent, the syndrome may be masked. The physician may be able to reduce the risk of this syndrome by minimizing the unnecessary use of neuroleptics and reducing the dose or discontinuing the drug, if possible, when manifestations of this syndrome are recognized, particularly in patients over the age of 50. Fine vermicular movement of the tongue maybe a early sign of the syndrome. If the medication is stopped at that time, the syndrome may not develop.
Autonomic nervous system: dry mouth, fainting, stuffy nose, photophobia, blurred vision, miosis.
Gastrointestinal: anorexia, increased appetite, gastric irritation, nausea, vomiting, constipation, paralytic ileus.
Endocrine system: altered libido, menstrual irregularities, lactation, false positive pregnancy tests, inhibition of ejaculation, gynecomastia, weight gain.
Skin: itching, rash, hypertrophic papillae of the tongue, angioneurotic edema, erythema, allergic purpura, exfoliative dermatitis, contact dermatitis.
Cardiovascular effects: hypotension, tachycardia, ECG changes (see Precautions).
Blood dyscrasias: agranulocytosis, leukopenia, granulocytopenia, eosinophilia, thrombocytopenia, anemia, aplastic anemia, pancytopenia.
Allergic Reactions: fever, laryngeal edema, angioneurotic edema, asthma.
Hepatotoxicity: jaundice, biliary stasis.
Urinary disturbances: retention, incontinence.
Abnormal pigmentation: more recently a peculiar skin-eye syndrome has been recognized as an adverse effect following long-term with phenothiazines. This reaction is marked by progressive pigmentation of areas of skin or conjunctiva and/or discoloration of the exposed sclera and cornea. Opacities of the anterior lens and cornea described as irregular or stellate in shape have also been reported. Patients receiving higher doses of phenothiazines for prolonged periods should have periodic complete eye examinations.
Miscellaneous: Unexpected and sudden deaths have been reported in hospitalized psychotic patients receiving phenothiazines. In some unexpected deaths, myocardial le­sions have been observed. Previous brain damage or seizures may also be predisposing factors; high doses should be avoided in known seizure patients. Several patients have shown sudden exacerbations of psychotic behavior patterns shortly before death. Autopsy findings have also revealed acute fulminating pneumonia or pneumonitis and aspiration of gastric contents. The physician should therefore be alerted to the possible development of silent pneumonias.
Drug Interactions
Phenothiazines may increase the effects of general anesthetics, opiates, barbiturates, alcohol and other CNS depressants as well as atropine and phosphorus insecticides.
Avoid epinephrine in the treatment of phenothiazines induced hypotension because phenothiazines may reverse epinephrine's action and thereby cause a further fall in blood pressure.
Storage
Store at room temperature in tight light resistant containers. Protect from moisture, freezing and excessive heat.
MIMS Class
ATC Classification
N05AB06 - trifluoperazine ; Belongs to the class of phenothiazine antipsychotics with piperazine structure.
Presentation/Packing
Tab (blue, biconvex film-coated) 1 mg x 100's. 5 mg x 1,000's.
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