Stelazine

Before taking trifluoperazine,

• tell your doctor and pharmacist if you are allergic to trifluoperazine; other phenothiazines such as chlorpromazine, fluphenazine, perphenazine, prochlorperazine (Compazine), promethazine (Phenergan), or thioridazine; or any other medications.
• tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention any of the following: anticoagulants (blood thinners) such as warfarin (Coumadin); antidepressants; antihistamines; atropine (in Motofen, in Lomotil, in Lonox); barbiturates such as pentobarbital (Nembutal), phenobarbital (Luminal), and secobarbital (Seconal); diuretics ('water pills'); epinephrine (Epipen); guanethidine (not available in the US); ipratropium (Atrovent); lithium (Eskalith, Lithobid); medications for anxiety, irritable bowel disease, mental illness, motion sickness, Parkinson's disease, ulcers, or urinary problems; medications for seizures such as phenytoin (Dilantin); narcotic medications for pain; propranolol (Inderal); sedatives; sleeping pills; and tranquilizers. Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
• tell your doctor if you have or have ever had liver disease or any condition that affects your blood cells, including conditions that affect the production of blood cells by your bone marrow. Your doctor may tell you not to take trifluoperazine.
• tell your doctor if you have or have ever had pheochromocytoma (tumor on a small gland near the kidneys), breast cancer, glaucoma (condition in which increased pressure in the eyes can lead to gradual loss of vision), trouble keeping your balance, seizures, chest pain, or heart disease. Also tell your doctor if you plan to work with organophosphorus insecticides (a type of chemical used to kill insects) or if you have ever had to stop taking a medication for mental illness due to severe side effects.
• tell your doctor if you are pregnant, especially if you are in the last few months of your pregnancy, or if you plan to become pregnant or are breast-feeding. If you become pregnant while taking trifluoperazine, call your doctor. Trifluoperazine may cause problems in newborns following delivery if it is taken during the last months of pregnancy.
• if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking trifluoperazine.
• if you are having a myelogram (x-ray examination of the spine), tell your doctor and the radiographer that you are taking trifluoperazine. Your doctor will probably tell you not to take trifluoperazine for 2 days before the myelogram and for one day after the myelogram.
• you should know that this medication may make you drowsy and may affect your thinking and movements, especially at the beginning of your treatment. Do not drive a car or operate machinery until you know how this medication affects you.
• you should know that trifluoperazine may cause dizziness, lightheadedness, and fainting when you get up too quickly from a lying position. To avoid this problem, get out of bed slowly, resting your feet on the floor for a few minutes before standing up.
• ask your doctor about the safe use of alcohol during your treatment with trifluoperazine. Alcohol can make the side effects of trifluoperazine worse.
• plan to avoid unnecessary or prolonged exposure to sunlight and to wear protective clothing, sunglasses, and sunscreen. Trifluoperazine may make your skin sensitive to sunlight.
• you should know that trifluoperazine may make it harder for your body to cool down when it gets very hot. Tell your doctor if you plan to do vigorous exercise or be exposed to extreme heat.
• you should know that there is a small chance that people who handle trifluoperazine tablets will develop a skin rash. Anyone who helps you take your medication should avoid touching the tablets directly.

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have:

• uncontrolled muscle movements in your face (chewing, lip smacking, frowning, tongue movement, blinking or eye movement);
• stiffness in your neck, tightness in your throat, trouble breathing or swallowing;
• feeling restless, jittery, or agitated;
• sudden weakness or ill feeling, fever, chills, sore throat, swollen gums, painful mouth sores, pain when swallowing, skin sores, cold or flu symptoms, cough;
• pale skin, easy bruising or bleeding;
• decreased night vision, tunnel vision, watery eyes, increased sensitivity to light;
• seizure (black-out or convulsions);
• liver problems--nausea, upper stomach pain, itching, tired feeling, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes); or
• severe nervous system reaction--very stiff (rigid) muscles, high fever, sweating, confusion, fast or uneven heartbeats, tremors, feeling like you might pass out.

Common side effects may include:

• dizziness, drowsiness, tired feeling;
• blurred vision;
• dry mouth, loss of appetite;
• sleep problems (insomnia);
• muscle weakness;
• itching or rash;
• missed menstrual periods; or
• breast swelling or discharge.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Schizophrenia

Treatment of schizophrenia.a b c e

American Psychiatric Association (APA) considers most atypical antipsychotic agents first-line drugs for management of the acute phase of schizophrenia (including first psychotic episodes).e APA considers conventional antipsychotic agents first-line in patients with acute psychotic episodes who have been treated successfully in the past with, or who prefer, conventional agents.e

Patients who do not respond to or tolerate one drug may be successfully treated with an agent from a different class or with a different adverse effect profile.e i p q

Nonpsychotic Anxiety

Short-term management of nonpsychotic anxiety in patients with generalized anxiety disorder.a b c

Not established whether trifluoperazine is useful for the management of other nonpsychotic conditions in which anxiety or manifestations that mimic anxiety are evident (e.g., physical illness, organic mental conditions, agitated depression, character pathologies).a b

Because of the risks of toxicity, use only as an alternative to other less toxic anxiolytic agents (e.g., benzodiazepines) in most patients.a b

Mental Retardation

Efficacy not established for the management of behavioral complications in patients with mental retardation.a b

Storage

Oral

Tight, light-resistant containers at 20–25°C; protect from moisture.a

• Precise mechanism(s) of antipsychotic action not determined, but may be principally related to antidopaminergic effects.b c

• Exhibits weak anticholinergic and sedative effects and strong extrapyramidal effects and antiemetic activity.b c

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Recommended dose: 1 to 2 mg orally 2 times a day
Maximum dose: 6 mg/day
Duration of therapy: Up to 12 weeks

Comment:
-The lowest effective dosage should be used for the shortest duration of time.

Use: Treatment of non-psychotic anxiety

Initial dose: 2 mg orally 2 times a day
Maintenance dose: 15 to 20 mg/day
Maximum dose: 40 mg/day

Comment:
-Most patients should reach therapeutic levels in 2 to 3 weeks

Use: Management of schizophrenia

Initial dose: 1 mg orally 2 times a day
Maximum dose: 6 mg/day
Duration of therapy: Up to 12 weeks

Comments:
-Due to the long half-life of this drug, this drug may be given as a once a day dose.
-The lowest effective dosage should be used for the shortest duration of time.

Use: Treatment of non-psychotic anxiety

Summary of Use during Lactation

Limited information indicates that maternal doses of trifluoperazine up to 10 mg daily do not affect the breastfed infant. Very limited long-term follow-up data indicate no adverse developmental effects when other phenothiazines are used alone. Because there is little published experience with trifluoperazine during breastfeeding, other antipsychotic agents may be preferred, especially wile nursing an newborn or preterm infant.

Drug Levels

Maternal Levels. Two mothers taking trifluoperazine 5 and 10 mg per day orally had undetectable milk levels (<1 mcg/L) of trifluoperazine.[1]

Infant Levels. Trifluoperazine was undetectable (<2 mcg/L) in urine at 86 days of age in an infant whose mother was taking trifluoperazine 10 mg daily.[1]

The infant of one mother who was taking trifluoperazine 10 mg per day orally while breastfeeding had a serum trifluoperazine level of 1 mcg/L. The infant was 1.9 weeks old when tested and the mother had been taking trifluoperazine during pregnancy which might have contributed to the infant's serum level.[2]

Effects in Breastfed Infants

One infant was breastfed from birth during maternal trifluoperazine 10 mg daily in addition to clonazepam 0.25 mg daily and valproic acid 500 mg daily. No adverse effects in the infant were reported by the mother (follow-up time unspecified).[2]

One mother began taking trifluoperazine (dosage unspecified) 2 months postpartum while breastfeeding her infant. She also started olanzapine 10 mg daily, paroxetine and procyclidine (dosages unspecified). The infant experiences no adverse reactions.[3]

Two mothers taking trifluoperazine 5 and 10 mg per day orally breastfed their infants from 1 week and 8 weeks of age, respectively. Mental and psychomotor development were measured at various time up to 30 months of age and were found to be normal.[1]

Effects on Lactation and Breastmilk

Phenothiazines cause galactorrhea in 26 to 40% of female patients.[4][5] Hyperprolactinemia appears to be the cause of the galactorrhea.[6][7][8] The hyperprolactinemia is caused by the drug's dopamine-blocking action in the tuberoinfundibular pathway.[9]

Alternate Drugs to Consider

Haloperidol, Olanzapine

References

1. Yoshida K, Smith B, Craggs M et al. Neuroleptic drugs in breast-milk: a study of pharmacokinetics and of possible adverse effects in breast-fed infants. Psychol Med. 1998;28:81-91. PMID: 9483685

2. Birnbaum CS, Cohen LS, Bailey JW et al. Serum concentrations of antidepressants and benzodiazepines in nursing infants: a case series. Pediatrics. 1999;104:e11. PMID: 10390297

3. Goldstein DJ, Corbin LA, Fung MC. Olanzapine-exposed pregnancies and lactation: early experience. J Clin Psychopharmacol. 2000;20:399-403. PMID: 10917399

4. Polishuk WZ, Kulcsar S. Effects of chlorpromazine on pituitary function. J Clin Endocrinol Metab. 1956;16:292-3. PMID: 13286329

5. Hooper JH Jr, Welch VC, Shackelford RT. Abnormal lactation associated with tranquilizing drug therapy. JAMA. 1961;178:506-7. PMID: 14448766

6. Turkington RW. Prolactin secretion in patients treated with various drugs: phenothiazines, tricyclic antidepressants, reserpine, and methyldopa. Arch Intern Med. 1972;130:349-54. PMID: 4560178

7. Turkington RW. Serum prolactin levels in patients with gynecomastia. J Clin Endocrinol Metab. 1972;34:62-6. PMID: 5061776

8. Meltzer HY, Fang VS. The effect of neuroleptics on serum prolactin in schizophrenic patients. Arch Gen Psychiatry. 1976;33:279-86. PMID: 1259521

9. Maguire GA. Prolactin elevation with antipsychotic medications: mechanisms of action and clinical consequences. J Clin Psychiatry. 2002;63(suppl 4):56-62. PMID: 11913677