Stelazine

Stelazine,

trademark for a phenothiazine antipsychotic agent (trifluoperazine).

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Stelazine [stel´ah-zēn]

trademark for preparations of trifluoperazine hydrochloride, an antipsychotic agent.

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trifluoperazine hydrochloride

Apo-Trifluoperazine (CA), Novo-Flurazine (CA), PMS-Trifluoperazine (CA), Solazine (CA), Stelazine (UK), Terfluzine (CA)

Pharmacologic class: Piperazine phenothiazine

Therapeutic class: Antipsychotic

Pregnancy risk category C

Action

Unknown. Thought to act on subcortical levels of hypothalamic and limbic systems by producing antidopaminergic effects. Also lowers seizure threshold and exhibits some adrenergic, muscarinic, and anticholinergic activity.

Availability

Injection: 2 mg/ml in 10-ml vials

Oral solution: 10 mg/ml in 60-ml bottles

Tablets: 1 mg, 2 mg, 5 mg, 10 mg, 20 mg

⊘Indications and dosages

➣ Schizophrenia

Adults: 2 to 5 mg P.O. b.i.d.; may increase gradually to obtain adequate response. Usual maintenance dosage is 15 to 20 mg/day. For prompt control of severe symptoms, 1 to 2 mg I.M. q 4 to 6 hours; some patients may need more than 6 mg/day.

Children ages 6 to 12: Initially, 1 mg P.O. once or twice daily in hospitalized patients or those under close supervision; may increase gradually up to 15 mg/day P.O. until symptoms are controlled or adverse reactions are intolerable. For prompt control of severe symptoms, 1 mg I.M. once or twice daily.

➣ Nonpsychotic anxiety

Adults: 1 to 2 mg P.O. b.i.d. Do not exceed 6 mg/day or 12 weeks' duration.

Dosage adjustment

• Hepatic disease
• Elderly or debilitated patients

Contraindications

• Hypersensitivity to drug, other phenothiazines, or bisulfites
• Severe hepatic disease
• Bone marrow depression
• Blood dyscrasias
• Coma
• Concomitant use of other CNS depressants in high doses

Precautions

Use cautiously in:
• seizure disorders, cardiovascular dis-orders, GI obstruction, glaucoma, retinopathy
• elderly or debilitated patients
• pregnant or breastfeeding patients.

Administration

• Mix oral solution in at least 60 ml of liquid or semisolid food just before giving.
• Administer I.M. injection deep into muscle.
• Know that parenteral solution should be colorless to pale yellow; discard if it's markedly discolored.

Route	Onset	Peak	Duration
P.O.	Unknown	2-4 hr	12-24 hr
I.M.	Unknown	Unknown	4-6 hr

Adverse reactions

CNS: sedation, dizziness, drowsiness, insomnia, fatigue, extrapyramidal effects, neuroleptic malignant syndrome

CV: tachycardia, hypotension, orthostatic hypotension, peripheral edema, prolonged QT interval, torsades de pointes

EENT: dry eyes, blurred vision, miosis, mydriasis, epithelial keratopathy, pigmentary retinopathy

GI: constipation, biliary stasis, dry mouth, anorexia, adynamic ileus

GU: urinary retention, glycosuria, amenorrhea, ejaculatory disorders, galactorrhea, gynecomastia

Hematologic: leukopenia, agranulocytosis

Hepatic: cholestatic jaundice

Musculoskeletal: muscle weakness

Skin: photosensitivity, altered pigmentation, erythema, rash

Other: mild fever, weight gain, allergic reaction

Interactions

Drug-drug. Alpha-adrenergic blockers: additive effect

Antacids containing aluminum: decreased trifluoperazine absorption

Anticholinergics, anticholinergic-like drugs (including antidepressants, antihistamines, disopyramide, other phenothiazines, quinidine): additive anticholinergic effects

Anticonvulsants: decreased seizure threshold

Antihistamines, CNS depressants, general anesthetics, opioids, sedative-hypnotics: additive CNS depression

Barbiturates: decreased blood levels of both drugs

Guanethidine: decreased antihypertensive effect

Lithium: increased risk of extrapyramidal reactions, disorientation, and unconsciousness

Oral anticoagulants: decreased anticoagulant effect

Phenytoin: interference with phenytoin metabolism, causing phenytoin toxicity

Propranolol: increased blood levels of both drugs

Thiazide diuretics: additive orthostatic hypotension

Drug-diagnostic tests. Hepatic enzymes: increased levels

Phenylketonuria test: false-positive result

Prolactin: increased level, causing interference with gonadotropin tests

Urine bilirubin: false-positive result

Drug-herbs. St. John's wort: increased risk of photosensitivity

Drug-behaviors. Alcohol use: additive CNS depression and hypotension

Sun exposure: increased risk of photosensitivity

Patient monitoring

• Monitor ECG and blood pressure. Watch closely for hypotension.
• Assess CBC (including platelet count) and liver function tests. Stay alert for signs and symptoms of hepatic damage and blood dyscrasias.
☞ Monitor neurologic status, especially for indications of neuroleptic malignant syndrome (unstable blood pressure, high fever, sweating, stupor, muscle rigidity, and autonomic dysfunction).

Patient teaching

• Instruct patient taking oral solution to add solution to 60 ml or more of liquid (tomato or fruit juice, milk, carbonated beverage, coffee, tea, or water) or semisolid food (such as soup or pudding) just before taking.
• Tell patient that drug's full effect usually occurs in 1 to 2 weeks.
• Instruct patient to move slowly when sitting up or standing, to avoid dizziness from sudden blood pressure drop.
☞ Teach patient to recognize and immediately report signs and symptoms of neuroleptic malignant syndrome.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects him.
• Tell patient to avoid alcohol and certain herbs.
• Advise patient to avoid sun exposure and to wear sunscreen and protective clothing when going outdoors.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, herbs, and behaviors mentioned above.

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Stelazine®

Trifluoperazine, see there