Also known as Apo-Alpzar, Nu-Alpraz, Xanax

A triazolobenzodiazepine agent with anxiolytic, sedative-hypnotic and anticonvulsant activities. Alprazolam binds to a specific site distinct from the inhibitory neurotransmitter gamma-aminobutyric acid (GABA) binding site on the benzodiazepine-GABA-A-chloride ionophore receptor complex located in the limbic, thalamic and hypothalamic regions of the central nervous system (CNS). This binding causes an allosteric modification of the receptor and enhances the affinity of GABA to the receptor leading to an increase in the frequency of chloride-channel opening events. This leads to an increase in chloride ion conductance, neuronal hyperpolarization, inhibition of the action potential and leads to a decrease in neuronal excitability.

Originator: NCI Thesaurus | Source: The website of the National Cancer Institute (http://www.cancer.gov)

Can I take Alprazolam while breastfeeding?

Because of reports of effects in infants, including sedation, alprazolam is probably not the best benzodiazepine for repeated use during nursing, especially with a neonate or premature infant. A shorter-acting benzodiazepine without active metabolites is preferred. After a single dose of alprazolam, there is usually no need to wait to resume breastfeeding.

Drug levels

Maternal Levels. Eight lactating women who averaged 11.8 weeks postpartum (range 6 to 28 weeks) were given a single 0.5 mg dose of alprazolam orally. Eleven breastmilk samples were obtained over the 36 hours after the dose. A mean peak alprazolam milk level of 3.7 mcg/L occurred at an average of 1.1 hours (range 0.47 to 3.8 hours) after the dose. The half-life of alprazolam in milk averaged 14.5 hours. The metabolites 4-hydroxyalprazolam and alpha-hydroxyalprazolam were not detected (<0.5 to 1 mcg/L) in milk. The authors calculated that an exclusively breastfed infant whose mother was taking alprazolam in the normal dosage range would receive a dose of 0.5 to 5 mcg/kg/day or about 3% of the maternal weight-adjusted dosage.[1] Infant Levels. Relevant published information was not found as of the revision date.

Effects in breastfed infants

Maternal Levels. Eight lactating women who averaged 11.8 weeks postpartum (range 6 to 28 weeks) were given a single 0.5 mg dose of alprazolam orally. Eleven breastmilk samples were obtained over the 36 hours after the dose. A mean peak alprazolam milk level of 3.7 mcg/L occurred at an average of 1.1 hours (range 0.47 to 3.8 hours) after the dose. The half-life of alprazolam in milk averaged 14.5 hours. The metabolites 4-hydroxyalprazolam and alpha-hydroxyalprazolam were not detected (<0.5 to 1 mcg/L) in milk. The authors calculated that an exclusively breastfed infant whose mother was taking alprazolam in the normal dosage range would receive a dose of 0.5 to 5 mcg/kg/day or about 3% of the maternal weight-adjusted dosage.[1] Infant Levels. Relevant published information was not found as of the revision date.

Possible effects on lactation

Unlike other benzodiazepines, alprazolam can increase serum prolactin.[5][6] One woman developed galactorrhea, amenorrhea and elevated serum prolactin after taking 3 mg of sustained-release alprazolam and 5 to 6 mg of immediate-release alprazolam daily for several months for self-treatment of fear, poor sleep, palpitations and gastrointestinal discomfort. After slow discontinuation of alprazolam and institution of quetiapine and fluvoxamine, galactorrhea ceased after about one month, menses normalized after about 2 months, and serum prolactin decreased to a normal level.[7] The prolactin level in a mother with established lactation may not affect her ability to breastfeed.

Alternate drugs to consider

Lorazepam, Oxazepam

References

1. Oo CY, Kuhn RJ, Desai N et al. Pharmacokinetics in lactating women: prediction of alprazolam transfer into milk. Br J Clin Pharmacol. 1995;40:231-6. PMID: 8527284

2. Anderson PO, McGuire GG. Neonatal alprazolam withdrawal — possible effects of breast feeding. DICP. 1989;23:614. Letter. PMID: 2763587

3. Ito S, Blajchman A, Stephenson M et al. Prospective follow-up of adverse reactions in breast-fed infants exposed to maternal medication. Am J Obstet Gynecol. 1993;168:1393-9. PMID: 8498418

4. Kelly LE, Poon S, Madadi P, Koren G. Neonatal benzodiazepines exposure during breastfeeding. J Pediatr. 2012;161:448-51. PMID: 22504099

5. Zemishlany Z, McQueeney R, Gabriel SM, Davidson M. Neuroendocrine and monoaminergic responses to acute administration of alprazolam in normal subjects. Neuropsychobiology. 1990-1991;23:124-8. PMID: 2098668

6. Madhusoodanan S, Parida S, Jimenez C. Hyperprolactinemia associated with psychotropics–a review. Hum Psychopharmacol. 2010;25:281-97. PMID: 20521318

7. Petric D, Peitl MV, Peitl V. High doses alprazolam induced amenorrhoea and galactorrhoea. Psychiatr Danub. 2011;23:123-4. PMID: 21448116

Last Revision Date

20150310

Disclaimer:Information presented in this database is not meant as a substitute for professional judgment. You should consult your healthcare provider for breastfeeding advice related to your particular situation. The U.S. government does not warrant or assume any liability or responsibility for the accuracy or completeness of the information on this Site.

Source: LactMed – National Library of Medicine (NLM)

3D Model of the Alprazolam molecule

MolView – data visualization platform