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Pronunciation |
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(thye
eth il PER a
zeen) |
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U.S. Brand
Names |
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Norzine®;
Torecan® |
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Generic
Available |
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No |
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Synonyms |
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Thiethylperazine Maleate |
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Pharmacological Index |
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Antiemetic |
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Use |
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Relief of nausea and vomiting |
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Pregnancy Risk
Factor |
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X |
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Contraindications |
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Comatose states, hypersensitivity to thiethylperazine or any component;
pregnancy, cross-sensitivity to other phenothiazines may
exist |
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Warnings/Precautions |
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Reduce or discontinue if extrapyramidal effects occur; safety and efficacy in
children <12 years of age have not been established; postural hypotension may
occur after I.M. injection; the injectable form contains sulfite which may cause
allergic reactions in some patients; use caution in patients with narrow-angle
glaucoma |
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Adverse
Reactions |
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>10%:
Central nervous system: Drowsiness, dizziness
Gastrointestinal: Xerostomia
Respiratory: Dry nose
1% to 10%:
Cardiovascular: Tachycardia, orthostatic hypotension
Central nervous system: Confusion, convulsions, extrapyramidal effects,
tardive dyskinesia, fever, headache
Hematologic: Agranulocytosis
Hepatic: Cholestatic jaundice
Otic: Tinnitus |
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Overdosage/Toxicology |
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Symptoms of overdose include deep sleep, coma, extrapyramidal symptoms,
abnormal involuntary muscle movements, hypotension
Following initiation of essential overdose management, toxic symptom
treatment and supportive treatment should be initiated. Hypotension usually
responds to I.V. fluids or Trendelenburg positioning. If unresponsive to these
measures, use of a parenteral inotrope may be required (eg, norepinephrine
0.1-0.2 mcg/kg/minute titrated to response); avoid epinephrine for
thiethylperazine-induced hypotension. Seizures commonly respond to diazepam
(I.V. 5-10 mg bolus in adults every 15 minutes if needed up to a total of 30 mg;
I.V. 0.25-0.4 mg/kg/dose up to a total of 10 mg in children) or to phenytoin or
phenobarbital. Critical cardiac arrhythmias often respond to I.V. phenytoin (15
mg/kg up to 1 g), while other antiarrhythmics can be used. Neuroleptics often
cause extrapyramidal symptoms (eg, dystonic reactions) requiring management with
diphenhydramine 1-2 mg/kg (adults) up to a maximum of 50 mg I.M. or I.V. slow
push followed by a maintenance dose for 48-72 hours. When these reactions are
unresponsive to diphenhydramine, benztropine mesylate I.V. 1-2 mg (adults) may
be effective. These agents are generally effective within 2-5 minutes.
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Drug
Interactions |
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Increased effect/toxicity with CNS depressants (eg, anesthetics, opiates,
tranquilizers, alcohol), lithium, atropine, epinephrine, MAO inhibitors,
TCAs |
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Stability |
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Store suppositories below 25°C
(77°F) in foil |
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Mechanism of
Action |
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Blocks postsynaptic mesolimbic dopaminergic receptors in the brain; exhibits
a strong alpha-adrenergic blocking effect and depresses the release of
hypothalamic and hypophyseal hormones; acts directly on chemoreceptor trigger
zone and vomiting center |
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Pharmacodynamics/Kinetics |
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Onset of antiemetic effect: Within 30 minutes
Duration of action: ~4 hours |
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Usual Dosage |
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Children >12 years and Adults:
I.V. and S.C. routes of administration are not recommended
Hemodialysis: Not dialyzable (0% to 5%)
Dosing comments in hepatic impairment: Use with caution
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Mental Health: Effects
on Mental Status |
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Drowsiness and dizziness are common; may cause confusion and extrapyramidal
symptoms |
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Mental Health:
Effects on Psychiatric
Treatment |
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May rarely cause agranulocytosis, caution with clozapine and carbamazepine.
Adverse effects may be increased with concurrent use of CNS depressants
(ethanol), lithium, TCAs, and MAO inhibitors |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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>10% of patients will experience dry mouth |
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Patient
Information |
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Take as directed; do not use more than recommended. Do not use alcohol and
prescription or OTC depressant without consulting prescriber. May cause
drowsiness, dizziness, stupor (use caution when driving or engaging in tasks
requiring alertness until response to drug is known); dry mouth (frequent oral
care and sucking on lozenges may help); photosensitivity (use sunscreen, wear
protective clothing and eyewear, and avoid direct sunlight); postural
hypotension (rise slowly from sitting or lying position and use caution when
climbing stairs). Report abnormal or involuntary muscle movements or twitching
or facial tics, acute drowsiness or restlessness, excessive fatigue or
dizziness. Pregnancy/breast-feeding precautions: Inform prescriber if
you are pregnant. Do not get pregnant during or for 1 month following therapy.
Consult prescriber for instruction on appropriate contraceptive measures. This
drug may cause severe fetal defects. Consult prescriber if
breast-feeding. |
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Nursing
Implications |
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Assist with ambulation, observe for extrapyramidal
symptoms |
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Dosage Forms |
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Injection, as maleate: 5 mg/mL (2 mL)
Suppository, rectal, as maleate: 10 mg
Tablet, as maleate: 10 mg |
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References |
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Diaz-Rubio E, Martin M, Rosell R, et al,
"The Antiemetic Efficacy of Thiethylperazine and Methylprednisolone Versus Thiethylperazine and Placebo in Breast Cancer Patients Treated With Adjuvant Chemotherapy (Fluorouracil, Doxorubicin, and Cyclophosphamide). A Randomized, Double-Blind, Cross-Over Trial,"
Acta Oncol, 1991, 30(3):339-42.
Fortner CL, Finley RS, and Grove WR,
"Combination Antiemetic Therapy in Control of Chemotherapy-Induced Emesis,"
Drug Intell Clin Pharm, 1985, 19:21-4.
Khanderia U, "Recurrent Dystonic Reactions Induced by Thiethylperazine,"
Drug Intell Clin Pharm, 1985, 19(7-8):550-1.
Plezia PM, Alberts DS, Kessler JF, et al,
"Randomized Crossover Comparison of High-Dose Intravenous Metoclopramide Versus a Five-Drug Antiemetic Regimen,"
J Pain Symptom Manage, 19909, 5(2):101-8.
Sulkava R, "Thiethylperazine and Tardive Dyskinesia," Acta Neurol
Scand, 1984, 70(5):364-72. |
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