Gastroenterology Book

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Droperidol

Aka: Droperidol, Inapsine
  1. Background
    1. Developed in the 1960s and available in U.S. until 2012, when U.S. manufacturing ceased
      1. Followed 2001 reports of QTc Prolongation
      2. Mayo Clinic continued to use Droperidol between 2001 and 2020 without significant adverse events
    2. Multiple studies demonstrated safety of Droperidol and as of 2015 was cleared to return to market in U.S. (available as of 2019)
  2. Indications: Not a first line drug due to QT Prolongation
    1. Antiemetic in refractory Vomiting
    2. Surgical or Diagnostic procedure
      1. Procedure related Nausea or Vomiting
      2. Conscious Sedation
    3. Migraine Headache
    4. Chemical Restraint (e.g. Sedation of the Violent Patient)
    5. Cannabinoid Hyperemesis
    6. First generation Antipsychotic (Neuroleptic)
  3. Contraindications
    1. Absolute contraindications
      1. QT Prolongation prior to use (>440 ms)
    2. Relative contraindications: Risk of QT Prolongation
      1. Congestive Heart Failure
      2. Bradycardia (Heart Rate <50 beats per minute)
      3. Concurrent Diuretic use
      4. Cardiac hypertrophy
      5. Hypokalemia
      6. Hypomagnesemia
      7. Other medication use associated with QT Prolongation
        1. Class I Antiarrhythmics
        2. Class III Antiarrhythmics
        3. Monoamine Oxidase Inhibitors
  4. Mechanism
    1. Butyrophenone Neuroleptic (first generation Antipsychotic) similar to Haloperidol
    2. Potent Dopamine receptor antagonist at D2
    3. Serotonin Antagonist activity
    4. Antiemetic activity via Dopamine antagonist
  5. Pharmacokinetics
    1. Rapid onset (esp. Droperidol IM compared with Haloperidol IM)
  6. Adverse Effects
    1. QT Prolongation
      1. Avoid use with other agents causing Prolonged QT Interval due to Medication
      2. May consider EKG before use (but not required)
      3. FDA Black box warning due to observed QT Prolongation at therepeutic doses
        1. First reported in 2001, but rare in clinical use
        2. Report coincided with release of new, on patent Antiemetic (Ondansetron)
          1. Curiously, 12 years later Ondansetron was reported to have the potential for QTc Prolongation
      4. Studies have since demonstrated its safety when used at moderate dose
        1. Calver (2015) Ann Emerg Med 66(3): 230-8 +PMID:25890395 [PubMed]
        2. Gaw (2020) Am J Emerg Med 38(7): 1310-14 [PubMed]
        3. Jackson (2007) Am J Syst Pharm 64(11): 1174-86 [PubMed]
    2. Sedation
      1. Usually resolves within 4 hours of dose
      2. Alertness may be decreased for 12 hours after dose
    3. Neurologic effects (treat with benztropine, Diphenhydramine)
      1. Extrapyramidal Side Effects
      2. Akasthisia
      3. Dystonia
    4. Neuroleptic Malignant Syndrome
  7. Drug Interactions
    1. Other agents that prolong QT Interval (see above)
  8. Dosing: Antiemetic
    1. Adults: 1.25 to 2.5 mg IM or IV slowly (may give up to 5 mg IV or IM)
    2. Children: 0.1 mg/kg IM or IV slowly
  9. Dosing: Headache
    1. Adults: 5 mg IM or slow IV
  10. Dosing: Agitation
    1. Adults: 5 mg IM (range 2.5 to 7.5 mg IM) or slow IV
    2. May combine with Midazolam 2 mg (up to 5 mg if needed)
  11. Monitoring
    1. Baseline EKG
    2. Continuous cardiac monitoring for 3 hours after dose
  12. References
    1. (2002) Mosby's Drug Consult, p. 001117
    2. Hill (2000) Emerg Med Clin North Am 18(2):301-15 [PubMed]
    3. Richman (2002) Am J Emerg Med 20(1):39-42 [PubMed]
    4. Strayer (2020) EM:Rap 20(9): 7-9 [PubMed]

Droperidol (C0013136)

Definition (NCI) A butyrophenone with anti-emetic, sedative and anti-anxiety properties. Although the exact mechanism through which droperidol exerts its effects is unknown, droperidol may block dopamine receptors in the chemoreceptor trigger zone (CTZ), which may lead to its anti-emetic effect. This agent may also bind to postsynaptic gamma-aminobutyric acid (GABA) receptors in the central nervous system (CNS), which increases the inhibitory effect of GABA and leads to sedative and anti-anxiety activities.
Definition (NCI_NCI-GLOSS) A drug used to prevent nausea and vomiting in patients who receive anesthesia before surgery. It is also used to treat anxiety. Droperidol is a type of antiemetic, adjunct anesthesia, and antipsychotic.
Definition (MSH) A butyrophenone with general properties similar to those of HALOPERIDOL. It is used in conjunction with an opioid analgesic such as FENTANYL to maintain the patient in a calm state of neuroleptanalgesia with indifference to surroundings but still able to cooperate with the surgeon. It is also used as a premedicant, as an antiemetic, and for the control of agitation in acute psychoses. (From Martindale, The Extra Pharmacopoeia, 29th ed, p593)
Definition (PDQ) A butyrophenone with anti-emetic, sedative and anti-anxiety properties. Although the exact mechanism through which droperidol exerts its effects is unknown, droperidol may block dopamine receptors in the chemoreceptor trigger zone (CTZ), which may lead to its anti-emetic effect. This agent may also bind to postsynaptic gamma-aminobutyric acid (GABA) receptors in the central nervous system (CNS), which increases the inhibitory effect of GABA and leads to sedative and anti-anxiety activities. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=39227&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=39227&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C458" NCI Thesaurus)
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D004329
SnomedCT 321398008, 334009009, 26574002, 387146001
LNC LP18863-8, MTHU006087
English 2H-Benzimidazol-2-one, 1-(1-(4-(4-fluorophenyl)-4-oxobutyl)-1,2,3,6-tetrahydro-4-pyridinyl)-1,3-dihydro-, Droperidol [CNS], droperidol, Droperidol [anaesthesia], Droperidol [anesthesia], Droperidol [central nervous system use], droperidol (medication), Droperidol [Chemical/Ingredient], dehydrobenzperidol, DROPERIDOL, Droperidol, Droperidol [central nervous system use] (product), Droperidol [anesthesia] (product), Droperidol (product), Droperidol (substance), Droperidol [anesthesia] (substance), Droperidol [central nervous system use] (substance)
Swedish Droperidol
Czech droperidol
Finnish Droperidoli
Russian DEGIDROBENZPERIDOL, DROPERIDOL, ДЕГИДРОБЕНЗПЕРИДОЛ, ДРОПЕРИДОЛ
Croatian DROPERIDOL
Polish Dehydrobenzoperidol, Properidol, Inapsin, Droperidol
Japanese デヒドロベンツペリドール, ドロペリドール
Spanish droperidol [con indicación para el sistema nervioso central] (producto), droperidol [con indicación para el sistema nervioso central], droperidol [anestésico], droperidol [anestésico] (producto), droperidol (producto), droperidol (sustancia), droperidol, Droperidol
French Dropéridol
German Droperidol
Italian Droperidolo
Portuguese Droperidol
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Inapsine (C0699335)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D004329
German Inapsin
English inapsine, Inapsine, Taylor Brand of Droperidol
Sources
Derived from the NIH UMLS (Unified Medical Language System)


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