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prochlorperazine (Compazine, Stemetil, Novamin, Buccastem)
Tradename: Compazine.
Indications:
- severe nausea & vomiting (no better than placebo [5])
- NOT effective in preventing vertigo or motion sickness or management of emesis caused by action of drugs on the nodose ganglion
- anxiety [6]
- schizophrenia [6]
Contraindications:
- children < 2 years of age
Dosage:
1) 5-10 mg IV over at least 2 min
2) 5-10 mg PO/IM TID/QID
3) 25 mg PR every 12 hours
4) pediatrics:
a) 0.4 mg/kg/day PO/PR divided TID-QID
b) 0.13 mg/kg/dose IM (IV not recommended)
Tabs: 5, 10, 25 mg.
Elixir: 5 mg/5 mL.
Suppositories: 2.5, 5, 25 mg.
Injection: 5 mg/mL (2 mL, 10 mL).
Sustained-release: (Compazine spansules)
- 10 mg PO every 12 hours.
- Tabs: 10, 15, 30 mg.
Pharmacokinetics:
1) onset of action:
a) 30-40 minutes oral
b) 60 minutes rectal
c) 10-20 minutes IM
2) duration of action: 3-4 hours
3) eliminated primarily by hepatic metabolism & biliary secretion
Adverse effects:
1) common (> 10%)
- pseudoparkinsonism, akathisia, dystonias, hypotension, pigmentary retinopathy, persistent tardive dyskinesia, constipation, decreased sweating, dizziness, orthostatic hypotension, nasal congestion
2) less common (1-10%)
- difficulty urinating, photosensitivity, rash, changes in menstrual cycle, sexual dysfunction, breast pain, weight gain, dizziness, nausea/vomiting, epigastric pain, trembling of fingers
3) uncommon (< 1%)
- leukopenia, agranulocytosis, hepatotoxicity, cholestatic jaundice, neuroleptic malignant syndrome, priapism, blue-gray discoloration of skin, impaired temperature regulation, galactorrhea, changes in cornea & lens
4) other
- shares toxic potential of other phenothiazines, extrapyramidal reactions common
- lowering of seizure threshold
- hypersensitivity
- anticholinergic effects
- dry mouth
- mydriasis
- decreased GI motility
Mechanism of action:
-> directly effects the medullary chemoreceptor trigger zone (CTZ) in the area postrema
Interactions
drug interactions
drug adverse effects (more general classes)
Related
chemoreceptor trigger zone (CTZ)
General
anti-emetic
dopaminergic receptor antagonist
phenothiazine
Properties
MISC-INFO: elimination route LIVER
KIDNEY
pregnancy-category C
safety in lactation ?
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- AHFS 96 Drug Information, GK McEnvoy et al (ed), American
Society of Health-System Pharmacists, Bethesda, MD 1996,
pg 2135
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998
- Braude D, Soliz T, Crandall C, Hendey G, Andrews J,
Weichenthal L.
Antiemetics in the ED: a randomized controlled trial comparing
3 common agents.
Am J Emerg Med. 2006 Mar;24(2):177-82.
PMID: 16490647
- Deprecated Reference
Component-of
intravenous anti-emetic combination