Anticholinergic activity of 107 medications commonly used by older adults

Marci L. Chew, Benoit H. Mulsant, Bruce G. Pollock, Mark E. Lehman, Andrew Greenspan, Ramy A. Mahmoud, Margaret A. Kirshner, Denise A. Sorisio, Robert Bies, Georges Gharabawi

Research output: Contribution to journalArticle

259 Citations (Scopus)

Abstract

The objective of this study was to measure the anticholinergic activity (AA) of medications commonly used by older adults. A radioreceptor assay was used to investigate the AA of 107 medications. Six clinically relevant concentrations were assessed for each medication. Rodent forebrain and striatum homogenate was used with tritiated quinuclidinyl benzilate. Drug-free serum was added to medication and atropine standard-curve samples. For medications that showed detectable AA, average steady-state peak plasma and serum concentrations (Cmax) in older adults were used to estimate relationships between in vitro dose and AA. All results are reported in pmol/mL of atropine equivalents. At typical doses administered to older adults, amitriptyline, atropine, clozapine, dicyclomine, doxepin, L-hyoscyamine, thioridazine, and tolterodine demonstrated AA exceeding 15 pmol/mL. Chlorpromazine, diphenhydramine, nortriptyline, olanzapine, oxybutynin, and paroxetine had AA values of 5 to 15 pmol/mL. Citalopram, escitalopram, fluoxetine, lithium, mirtazapine, quetiapine, ranitidine, and temazepam had values less than 5 pmol/mL. Amoxicillin, celecoxib, cephalexin, diazepam, digoxin, diphenoxylate, donepezil, duloxetine, fentanyl, furosemide, hydrocodone, lansoprazole, levofloxacin, metformin, phenytoin, propoxyphene, and topiramate demonstrated AA only at the highest concentrations tested (patients with above-average Cmax values, who receive higher doses, or are frail may show AA). The remainder of the medications investigated did not demonstrate any AA at the concentrations examined. Psychotropic medications were particularly likely to demonstrate AA. Each of the drug classifications investigated (e.g., antipsychotic, cardiovascular) had at least one medication that demonstrated AA at therapeutic doses. Clinicians can use this information when choosing between equally efficacious medications, as well as in assessing overall anticholinergic burden.

Original languageEnglish (US)
Pages (from-to)1333-1341
Number of pages9
JournalJournal of the American Geriatrics Society
Volume56
Issue number7
DOIs
StatePublished - Jul 2008
Externally publishedYes

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Cholinergic Antagonists
Atropine
Citalopram
Celecoxib
olanzapine
Dicyclomine
Diphenoxylate
Hyoscyamine
Hydrocodone
Doxepin
Quinuclidinyl Benzilate
Dextropropoxyphene
Nortriptyline
Lansoprazole
Thioridazine
Cephalexin
Diphenhydramine
Paroxetine
Radioligand Assay
Levofloxacin

Keywords

  • Anticholinergic activity
  • Elderly
  • Medications

ASJC Scopus subject areas

  • Geriatrics and Gerontology

Cite this

Chew, M. L., Mulsant, B. H., Pollock, B. G., Lehman, M. E., Greenspan, A., Mahmoud, R. A., ... Gharabawi, G. (2008). Anticholinergic activity of 107 medications commonly used by older adults. Journal of the American Geriatrics Society, 56(7), 1333-1341. https://doi.org/10.1111/j.1532-5415.2008.01737.x

Anticholinergic activity of 107 medications commonly used by older adults. / Chew, Marci L.; Mulsant, Benoit H.; Pollock, Bruce G.; Lehman, Mark E.; Greenspan, Andrew; Mahmoud, Ramy A.; Kirshner, Margaret A.; Sorisio, Denise A.; Bies, Robert; Gharabawi, Georges.

In: Journal of the American Geriatrics Society, Vol. 56, No. 7, 07.2008, p. 1333-1341.

Research output: Contribution to journalArticle

Chew, ML, Mulsant, BH, Pollock, BG, Lehman, ME, Greenspan, A, Mahmoud, RA, Kirshner, MA, Sorisio, DA, Bies, R & Gharabawi, G 2008, 'Anticholinergic activity of 107 medications commonly used by older adults', Journal of the American Geriatrics Society, vol. 56, no. 7, pp. 1333-1341. https://doi.org/10.1111/j.1532-5415.2008.01737.x
Chew, Marci L. ; Mulsant, Benoit H. ; Pollock, Bruce G. ; Lehman, Mark E. ; Greenspan, Andrew ; Mahmoud, Ramy A. ; Kirshner, Margaret A. ; Sorisio, Denise A. ; Bies, Robert ; Gharabawi, Georges. / Anticholinergic activity of 107 medications commonly used by older adults. In: Journal of the American Geriatrics Society. 2008 ; Vol. 56, No. 7. pp. 1333-1341.
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