Last update June 13, 2022

1-{1-[3-(4-Fluorobenzoyl)propyl]-1,2,3,6-tetrahydro-4-pyridyl}-benzimidazolin-2-one

Likely Compatibility

Fairly safe. Mild or unlikely adverse effects. Compatible under certain circumstances. Follow-up recommended. Read Commentary.

It is a neuroleptic butyrophenone (tranquilizer) with properties similar to haloperidol. Used as a pre-anesthetic and for the management of postoperative and chemotherapy-induced nausea and vomiting. Intravenous administration.

Since the last update we have not found any published data on its excretion in breast milk.

Its pharmacokinetic characteristics: high plasma protein binding, large volume of distribution and short half-life (AEMPS 2018), make it very unlikely its excretion into breast milk in significant amounts.

Neurodevelopmental and adaptive problems have been observed in one newborn and one infant of mothers treated with haloperidol, even though they were also taking other medications. (Gardiner 2003, Bonhomme 2002)

It can increase prolactin levels. (Foley 2006).

An isolated dose has a low risk during lactation (Spigset 1994). Due to its powerful sedative effect, continued use is not recommended. (AEMPS 2018) 

Until there is more published data on this drug in relation to breastfeeding, safer known alternatives may be preferable (Klinger 2013), especially during the neonatal period and in cases of prematurity.

Alternatives

  • Haloperidol (Fairly safe. Mild or unlikely adverse effects. Compatible under certain circumstances. Follow-up recommended. Read Commentary.)
  • Ondansetron (Safe substance and/or breastfeeding is the best option.)

Suggestions made at e-lactancia are done by APILAM team of health professionals, and are based on updated scientific publications. It is not intended to replace the relationship you have with your doctor but to compound it. The pharmaceutical industry contraindicates breastfeeding, mistakenly and without scientific reasons, in most of the drug data sheets.

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Other names

1-{1-[3-(4-Fluorobenzoyl)propyl]-1,2,3,6-tetrahydro-4-pyridyl}-benzimidazolin-2-one is Droperidol in Chemical name.

Is written in other languages:

Group

1-{1-[3-(4-Fluorobenzoyl)propyl]-1,2,3,6-tetrahydro-4-pyridyl}-benzimidazolin-2-one belongs to this group or family:

Tradenames

Main tradenames from several countries containing 1-{1-[3-(4-Fluorobenzoyl)propyl]-1,2,3,6-tetrahydro-4-pyridyl}-benzimidazolin-2-one in its composition:

List of 10 tradenames
  • Dehidrobenzperidol™
  • Dehydrobenzperidol™
  • Disifelit™. Contains other elements than 1-{1-[3-(4-Fluorobenzoyl)propyl]-1,2,3,6-tetrahydro-4-pyridyl}-benzimidazolin-2-one in its composition
  • Dridol™
  • Droleptan™
  • Droperdal™
  • Inapsine™
  • Nilperidol™. Contains other elements than 1-{1-[3-(4-Fluorobenzoyl)propyl]-1,2,3,6-tetrahydro-4-pyridyl}-benzimidazolin-2-one in its composition
  • Thalamonal™. Contains other elements than 1-{1-[3-(4-Fluorobenzoyl)propyl]-1,2,3,6-tetrahydro-4-pyridyl}-benzimidazolin-2-one in its composition
  • Xomolix™

Pharmacokinetics

Variable Value Unit
Molecular weight 379 daltons
Protein Binding 85 - 90 %
VD 1.5 l/Kg
pKa 12.7 -
Tmax 0.2 - 0.5 hours
T½ 2.2 ± 0.2 hours

References

  1. AEMPS. Droperidol. Ficha técnica. 2018 Full text (in our servers)
  2. Klinger G, Stahl B, Fusar-Poli P, Merlob P. Antipsychotic drugs and breastfeeding. Pediatr Endocrinol Rev. 2013 Mar-Apr;10(3):308-17. Review. Abstract
  3. Sandoz Canada. Droperidol. Drug Summary. 2010 Full text (in our servers)
  4. Foley KF, Kast RE. Review of evidence that posttransplantation psychiatric treatment commonly affects prolactin levels and thereby influences graft fate. Gen Hosp Psychiatry. 2006 May-Jun;28(3):230-3. Abstract
  5. Gardiner SJ, Kristensen JH, Begg EJ, Hackett LP, Wilson DA, Ilett KF, Kohan R, Rampono J. Transfer of olanzapine into breast milk, calculation of infant drug dose, and effect on breast-fed infants. Am J Psychiatry. 2003 Abstract
  6. Bonhomme V, Brichant JF, Wuilmart M, Dewandre PY, Hans P. Droperidol reduces nausea after caesarean section but alters the neurological status of the breastfed infants. Anesthesiology. 2002;96:Abstract 1044 Full text (link to original source) Full text (in our servers)
  7. Spigset O. Anaesthetic agents and excretion in breast milk. Acta Anaesthesiol Scand. 1994 Abstract

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