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Pronunciation |
|
(a
set oh FEN a
zeen) |
|
|
Generic
Available |
|
No |
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Synonyms |
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Acetophenazine Maleate |
|
|
Pharmacological Index |
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Antipsychotic Agent, Phenothazine, Piperazine |
|
|
Use |
|
Management of manifestations of psychotic disorders |
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Pregnancy Risk
Factor |
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C |
|
|
Contraindications |
|
Blood dyscrasias and bone marrow suppression, patients in coma or brain
damage, known hypersensitivity to acetophenazine |
|
|
Adverse
Reactions |
|
>10%:
Cardiovascular: Hypotension, orthostatic hypotension
Central nervous system: Pseudoparkinsonism, akathisia, dystonias, tardive
dyskinesia, dizziness
Gastrointestinal: Constipation
Ocular: Pigmentary retinopathy
Respiratory: Nasal congestion
Miscellaneous: Diaphoresis (decreased)
1% to 10%:
Dermatologic: Increased sensitivity to sun, rash
Endocrine & metabolic: Changes in menstrual cycle, breast pain, changes
in libido
Gastrointestinal: Weight gain, nausea, vomiting, stomach pain
Genitourinary: Difficulty in urination, ejaculatory disturbances
Neuromuscular & skeletal: Trembling fingers
<1%:
Central nervous system: Neuroleptic malignant syndrome (NMS), impairment of
temperature regulation, lowering of seizures threshold
Dermatologic: Discoloration of skin (blue-gray)
Endocrine & metabolic: Galactorrhea
Genitourinary: Priapism
Hematologic: Agranulocytosis, leukopenia
Hepatic: Cholestatic jaundice, hepatotoxicity
Ocular: Cornea and lens changes, pigmentary retinopathy |
|
|
Drug
Interactions |
|
Methyldopa, propranolol, CNS depressants (including tricyclic
antidepressants) can
effect; lithium and fluoxetine
can toxicities; antacids,
carbamazepine, barbiturates,
and anticholinergics can
effect; phenothiazines
effect of bromocriptine
and valproic
acid |
|
|
Stability |
|
Protect from light; dispense in amber or opaque vials |
|
|
Mechanism of
Action |
|
Antagonizes the effects of dopamine in the basal ganglia and limbic areas of
the forebrain; this activity appears responsible for the antipsychotic efficacy,
as well as the production of extrapyramidal symptoms; increases the secretion of
prolactin and has a marked suppressive effect on the chemoreceptor trigger zone;
also produces peripheral blockade of cholinergic neurons |
|
|
Pharmacodynamics/Kinetics |
|
Onset: 2-4 hours
Duration: ~24 hours, permitting daily dosing
Absorption: Tissue saturation, particularly in high lipid tissues such as the
central nervous system
Serum half-life: Range: 20-40 hours |
|
|
Usual Dosage |
|
Adults: Oral: 20 mg 3 times/day up to 60-120 mg/day
Hemodialysis: Not dialyzable (0% to 5%) |
|
|
Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
|
No information available to require special precautions |
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|
Dental Health:
Effects on Dental Treatment |
|
Orthostatic hypotension and nasal congestion possible in dental patients.
Since the drug is a dopamine antagonist, extrapyramidal symptoms of the TMJ is a
possibility; increased motor activity of head, face, and neck may occur. This
drug is also an anticholinergic causing xerostomia. |
|
|
Patient
Information |
|
Do not take antacid within 1 hour of taking drug; may cause drowsiness, avoid
alcohol; avoid excess sun exposure (use sun block); rise slowly from recumbent
position; use of supportive stockings may help prevent orthostatic
hypotension |
|
|
Nursing
Implications |
|
Observe for tremor and abnormal movement or posturing (extrapyramidal
symptoms), increased confusion or psychotic behavior, constipation, urinary
retention, abnormal gait |
|
|
Dosage Forms |
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Tablet, as maleate: 20 mg |
|
|
References |
|
Peabody CA, Warner MD, Whiteford HA, et al,
"Neuroleptics and the Elderly," J Am Geriatr Soc, 1987, 35(3):233-8.
Risse SC and Barnes R,
"Pharmacologic Treatment of Agitation Associated With Dementia," J Am Geriatr
Soc, 1986, 34(5):368-76.
Saltz BL, Woerner MG, Kane JM, et al,
"Prospective Study of Tardive Dyskinesia Incidence in the Elderly," JAMA,
1991, 266(17):2402-6.
Seifert RD, "Therapeutic Drug Monitoring: Psychotropic Drugs," J Pharm
Pract, 1984, 6:403-16. |
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