Also known as Haldol, Haloperidolum, R 1625, R-1625

A phenylbutylpiperadine derivative with antipsychotic, neuroleptic, and antiemetic activities. Haloperidol competitively blocks postsynaptic dopamine (D2) receptors in the mesolimbic system of the brain, thereby eliminating dopamine neurotransmission and leading to antidelusionary and antihallucinagenic effects. Antagonistic activity mediated through D2 dopamine receptors in the chemoreceptive trigger zone (CTZ) accounts for its antiemetic activity.

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Can I take Haloperidol while breastfeeding?

Limited information indicates that maternal doses of haloperidol up to 10 mg daily produce low levels in milk and do not affect the breastfed infant. Very limited long-term follow-up data indicate no adverse developmental effects when haloperidol is used alone. However, use with chlorpromazine occasionally might negatively affect development. Monitor the infant for developmental milestones, especially if other antipsychotics are used concurrently.

Drug levels

Maternal Levels. In one woman, a milk level of 5 mcg/L was detected 11 hours after a dose during therapy with an average dose of 29.2 mg daily. Another level of 2 mcg/L was measured 9 hours after a 12 mg oral dose. Haloperidol was not detectable in milk 3 days after the last 7 mg dose.[1]

During a regimen of haloperidol 5 mg orally twice daily in one woman, random milk levels were 18 and 23.5 mcg/L. On day 21 of therapy, the mother’s milk level was 4 mcg/L.[2]

A woman had been taking haloperidol for 29 days before and after delivery. Although she was not breastfeeding, a breastmilk sample was obtained 12 days postpartum when the dose had been 6 mg orally for 7 days. The milk haloperidol level 3 hours after the last dose was 1.7 mcg/L.[3]

Three patients taking haloperidol 3, 4 and 6 mg daily had random milk levels of 32, 17 and 4.7 mcg/L at unspecified times after a dose, although the latter patient was reportedly nonadherent to the drug regimen.[4][5]

Nine patients who were taking haloperidol had foremilk and/or hindmilk samples collected on 1 to 3 occasions 12 to 15 hours after the previous dose of haloperidol. HPLC assay found that foremilk haloperidol levels ranged from undetectable (<1 mcg/L) to 24.9 mcg/L, with no correlation to the maternal doses of 1 to 40 mg daily. Foremilk haloperidol concentrations correlated better with maternal plasma levels. Hindmilk concentrations were slightly higher than foremilk concentrations when both samples were collected. Measurement of the same samples with an enzyme immunoassay found higher levels, ranging from undetectable (<10 mcg/L) to 988 mcg/L, again correlated better with maternal serum concentrations than maternal dosage. The authors considered the higher values to represent the contribution of undetermined metabolites that were unmeasured by HPLC.[6] Infant Levels. A nursing mother took haloperidol 5 mg orally twice daily. On day 21 of therapy, the infant’s urine contained 1.5 mcg/L of haloperidol.[2]

Four breastfed infants whose mothers were taking haloperidol is doses of 5 to 20 mg daily had serum concentrations measured by enzyme immunoassay. Serum concentrations ranged from 0.8 to 2.1 mcg/L. Neither the extent of nursing, the exact age at the time of sample collection, nor the time of sampling were stated.[6]

Effects in breastfed infants

Maternal Levels. In one woman, a milk level of 5 mcg/L was detected 11 hours after a dose during therapy with an average dose of 29.2 mg daily. Another level of 2 mcg/L was measured 9 hours after a 12 mg oral dose. Haloperidol was not detectable in milk 3 days after the last 7 mg dose.[1]

During a regimen of haloperidol 5 mg orally twice daily in one woman, random milk levels were 18 and 23.5 mcg/L. On day 21 of therapy, the mother’s milk level was 4 mcg/L.[2]

A woman had been taking haloperidol for 29 days before and after delivery. Although she was not breastfeeding, a breastmilk sample was obtained 12 days postpartum when the dose had been 6 mg orally for 7 days. The milk haloperidol level 3 hours after the last dose was 1.7 mcg/L.[3]

Three patients taking haloperidol 3, 4 and 6 mg daily had random milk levels of 32, 17 and 4.7 mcg/L at unspecified times after a dose, although the latter patient was reportedly nonadherent to the drug regimen.[4][5]

Nine patients who were taking haloperidol had foremilk and/or hindmilk samples collected on 1 to 3 occasions 12 to 15 hours after the previous dose of haloperidol. HPLC assay found that foremilk haloperidol levels ranged from undetectable (<1 mcg/L) to 24.9 mcg/L, with no correlation to the maternal doses of 1 to 40 mg daily. Foremilk haloperidol concentrations correlated better with maternal plasma levels. Hindmilk concentrations were slightly higher than foremilk concentrations when both samples were collected. Measurement of the same samples with an enzyme immunoassay found higher levels, ranging from undetectable (<10 mcg/L) to 988 mcg/L, again correlated better with maternal serum concentrations than maternal dosage. The authors considered the higher values to represent the contribution of undetermined metabolites that were unmeasured by HPLC.[6] Infant Levels. A nursing mother took haloperidol 5 mg orally twice daily. On day 21 of therapy, the infant’s urine contained 1.5 mcg/L of haloperidol.[2]

Four breastfed infants whose mothers were taking haloperidol is doses of 5 to 20 mg daily had serum concentrations measured by enzyme immunoassay. Serum concentrations ranged from 0.8 to 2.1 mcg/L. Neither the extent of nursing, the exact age at the time of sample collection, nor the time of sampling were stated.[6]

Possible effects on lactation

Galactorrhea has been reported with haloperidol.[10] Hyperprolactinemia appears to be the cause of the galactorrhea.[10][11][12][13][14][15] The hyperprolactinemia is caused by the drug’s dopamine-blocking action in the tuberoinfundibular pathway.[16] The maternal prolactin level in a mother with established lactation may not affect her ability to breastfeed.

Alternate drugs to consider

Olanzapine, Risperidone

References

1. Stewart RB, Karas B, Springer PK. Haloperidol excretion in human milk. Am J Psychiatry. 1980;137:849-50. PMID: 7386670

2. Whalley LJ, Blain PG, Prime JK. Haloperidol secreted in breast milk. Br Med J. 1981;282:1746-7. PMID: 6786603

3. Kuniyoshi M, Inanaga K. Haloperidol and biperiden plasma levels in a pregnant atypical psychotic woman and a neonate–a case report. Kurume Med J. 1985;32:199-202. PMID: 3835398

4. Ohkubo T, Shimoyama R, Sugawara K. Measurement of haloperidol in human breast milk by high-performance liquid chromatography. J Pharm Sci. 1992;81:947-9. PMID: 1432646

5. Sugawara K, Shimoyama R, Ohkubo T. Determinations of psychotropic drugs and antiepileptic drugs by high-performance liquid chromatography and its monitoring in human breast milk. Hirosaki Med J. 1999;51(Suppl):S81-6.

6. Yoshida K, Smith B, Craggs M et al. Neuroleptic drugs in breast-milk: a study of pharmacokinetics and of possible adverse effects in breast-fed infants. Psychol Med. 1998;28:81-91. PMID: 9483685

7. Yoshida K, Smith B, Craggs M et al. Investigation of pharmacokinetics and possible adverse effects in infants exposed to tricyclic antidepressants in breast-milk. J Affective Disord. 1997;43:225-37. PMID: 9186793

8. Mendhekar DN, Andrade C. Uneventful use of haloperidol and trihehexyphenidyl during three consecutive pregnancies. Arch Womens Ment Health. 2011;14:83-4. PMID: 21116668

9. Uguz F. Breastfed infants exposed to combined antipsychotics: Two case reports. Am J Ther. 2015. PMID: 26539905

10. Atmaca M, Kuloglu M, Tezcan E et al. Quetiapine is not associated with increase in prolactin secretion in contrast to haloperidol. Arch Med Res. 2002;33(6):562-5. PMID: 12505103

11. Turkington RW. Prolactin secretion in patients treated with various drugs: phenothiazines, tricyclic antidepressants, reserpine, and methyldopa. Arch Intern Med. 1972;130:349-54. PMID: 4560178

12. Turkington RW. Serum prolactin levels in patients with gynecomastia. J Clin Endocrinol Metab. 1972;34:62-6. PMID: 5061776

13. Fiore L, Scapagnini U, Canonico PL. Effect of dihydroergocryptine and dihydroergocristine on cyclic AMP accumulation and prolactin release in vitro: evidence for a dopaminomimetic action. Horm Res. 1987;25:171-7. PMID: 3032757

14. Crawford AM, Beasley CM Jr, Tollefson GD. The acute and long-term effect of olanzapine compared with placebo and haloperidol on serum prolactin concentrations. Schizophr Res. 1997;26 (1):41-54. PMID: 9376336

15. Langer G, Puhringer W. Haloperidol and droperidol treatment in schizophrenics. Clinical application of the “prolactin-model”. Acta Psychiatr Belg. 1980;80:574-83. PMID: 7234451

16. Maguire GA. Prolactin elevation with antipsychotic medications: mechanisms of action and clinical consequences. J Clin Psychiatry. 2002;63(suppl 4):56-62. PMID: 11913677

Last Revision Date

20151210

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Source: LactMed – National Library of Medicine (NLM)

3D Model of the Haloperidol molecule

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