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droperidol (Inapsine)
Tradename: Inapsine.
Indications:
1) symptomatic treatment of nausea & vomiting
2) adjunct to analgesia
Dosage:
1) tranquilization & reduction of operative nausea
- 2.5 to 10 mg IV/IM
2) adjunct to analgesia with fentanyl
- 1.25 to 5.0 mg IV/IM
3) chemotherapy-induced nausea/vomiting
a) haloperidol is 1st line agent
b) 2.5 mg IV/IM every 3-6 hours PRN.
4) treatment of vomiting in the emergency department [5]
Contraindications:
1) NOT to be used for sedation/anxiolysis in intensive care patients
2) avoid in elderly patients
Pharmacokinetics:
1) onset of action is 3-10 minutes, sometimes longer
- when given IM, droperidol has a more rapid onset of action & a shorter 1/2life than haloperidol
2) tranquility effect lasts 2-4 hours
3) drowsiness & altered consciousness may last 12 hours
4) readily crosses blood-brain barrier
5) metabolized by liver
6) excreted in urine & feces
Monitor: blood pressure, EKG [4]
Adverse effects:
1) common (> 10%)
- drowsiness, hypotension (mild to moderate), tachycardia
2) less common (1-10%)
- extrapyramidal (dystonic) reactions, respiratory depression, hypertension
3) uncommon (< 1%)
- dizziness, chills, shivering, laryngospasm, bronchospasm, hallucinations
4) other [2]
- restlessness
- facial sweating
- may cause delirium in elderly patients
- prolongation of QT interval -> torsades de pointes [4]
Drug interactions:
1) lowers seizure threshold when used concurrently with analeptics
2) increased CNS depression when used concurrently with CNS depressants
3) antagonizes dopaminergic activity of anti-Parkinson agents
4) in combination with alpha-methyldopa may cause dementia
5) reverses pressor effects of epinephrine
6) fentanyl or other analgesics in combination may exacerbate hypertension
7) avoid use with other agents that prolong the QT interval
Mechanism of action:
1) butyrophenone, similar to haloperidol
2) strong central dopamineric (D2-selective) antagonism
a) mesolimbic system
b) frontal cortex
c) chemoreceptor trigger zone (CTZ)
3) inhibits sympathetic postganglionic alpha-receptors, causing vasodilation
Interactions
drug interactions
drug adverse effects (more general classes)
General
anti-emetic
butyrophenone
dopaminergic receptor antagonist
Properties
MISC-INFO: elimination route LIVER
pregnancy-category C
safety in lactation ?
Database Correlations
PUBCHEM cid=3168
References
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- 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
- Prescriber's Letter 9(1):5 2002
- 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
Component-of
droperidol/fentanyl
intravenous anti-emetic combination