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Anticholinergic Activity of 107 Medications Commonly Used by Older Adults

Authors

  • Marci L. Chew PhD,

    1. From the *Department of Pharmaceutical Sciences, School of PharmacyGeriatric Psychopharmacology Laboratory, Department of Psychiatry, School of Medicine, University of Pittsburgh, Pittsburgh, PennsylvaniaGeriatric Mental Health Program, Centre for Addiction and Mental Health, Toronto, Ontario, Canada§Rotman Research Institute, Toronto, Ontario, CanadaDepartment of Psychiatry, University of Toronto, Toronto, Ontario, Canada#Johnson & Johnson Health Care Systems Inc., Piscataway, New Jersey**Johnson & Johnson Pharmaceutical Research and Development, Raritan, New Jersey††ETHICON, Inc., Somerville, New Jersey‡‡F. Hoffman-La Roche Inc., Nutley, New Jersey.
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  • Benoit H. Mulsant MD,

    1. From the *Department of Pharmaceutical Sciences, School of PharmacyGeriatric Psychopharmacology Laboratory, Department of Psychiatry, School of Medicine, University of Pittsburgh, Pittsburgh, PennsylvaniaGeriatric Mental Health Program, Centre for Addiction and Mental Health, Toronto, Ontario, Canada§Rotman Research Institute, Toronto, Ontario, CanadaDepartment of Psychiatry, University of Toronto, Toronto, Ontario, Canada#Johnson & Johnson Health Care Systems Inc., Piscataway, New Jersey**Johnson & Johnson Pharmaceutical Research and Development, Raritan, New Jersey††ETHICON, Inc., Somerville, New Jersey‡‡F. Hoffman-La Roche Inc., Nutley, New Jersey.
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  • Bruce G. Pollock MD, PhD,

    1. From the *Department of Pharmaceutical Sciences, School of PharmacyGeriatric Psychopharmacology Laboratory, Department of Psychiatry, School of Medicine, University of Pittsburgh, Pittsburgh, PennsylvaniaGeriatric Mental Health Program, Centre for Addiction and Mental Health, Toronto, Ontario, Canada§Rotman Research Institute, Toronto, Ontario, CanadaDepartment of Psychiatry, University of Toronto, Toronto, Ontario, Canada#Johnson & Johnson Health Care Systems Inc., Piscataway, New Jersey**Johnson & Johnson Pharmaceutical Research and Development, Raritan, New Jersey††ETHICON, Inc., Somerville, New Jersey‡‡F. Hoffman-La Roche Inc., Nutley, New Jersey.
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  • Mark E. Lehman PharmD,

    1. From the *Department of Pharmaceutical Sciences, School of PharmacyGeriatric Psychopharmacology Laboratory, Department of Psychiatry, School of Medicine, University of Pittsburgh, Pittsburgh, PennsylvaniaGeriatric Mental Health Program, Centre for Addiction and Mental Health, Toronto, Ontario, Canada§Rotman Research Institute, Toronto, Ontario, CanadaDepartment of Psychiatry, University of Toronto, Toronto, Ontario, Canada#Johnson & Johnson Health Care Systems Inc., Piscataway, New Jersey**Johnson & Johnson Pharmaceutical Research and Development, Raritan, New Jersey††ETHICON, Inc., Somerville, New Jersey‡‡F. Hoffman-La Roche Inc., Nutley, New Jersey.
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  • Andrew Greenspan MD,

    1. From the *Department of Pharmaceutical Sciences, School of PharmacyGeriatric Psychopharmacology Laboratory, Department of Psychiatry, School of Medicine, University of Pittsburgh, Pittsburgh, PennsylvaniaGeriatric Mental Health Program, Centre for Addiction and Mental Health, Toronto, Ontario, Canada§Rotman Research Institute, Toronto, Ontario, CanadaDepartment of Psychiatry, University of Toronto, Toronto, Ontario, Canada#Johnson & Johnson Health Care Systems Inc., Piscataway, New Jersey**Johnson & Johnson Pharmaceutical Research and Development, Raritan, New Jersey††ETHICON, Inc., Somerville, New Jersey‡‡F. Hoffman-La Roche Inc., Nutley, New Jersey.
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  • Ramy A. Mahmoud MD,

    1. From the *Department of Pharmaceutical Sciences, School of PharmacyGeriatric Psychopharmacology Laboratory, Department of Psychiatry, School of Medicine, University of Pittsburgh, Pittsburgh, PennsylvaniaGeriatric Mental Health Program, Centre for Addiction and Mental Health, Toronto, Ontario, Canada§Rotman Research Institute, Toronto, Ontario, CanadaDepartment of Psychiatry, University of Toronto, Toronto, Ontario, Canada#Johnson & Johnson Health Care Systems Inc., Piscataway, New Jersey**Johnson & Johnson Pharmaceutical Research and Development, Raritan, New Jersey††ETHICON, Inc., Somerville, New Jersey‡‡F. Hoffman-La Roche Inc., Nutley, New Jersey.
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  • Margaret A. Kirshner BA,

    1. From the *Department of Pharmaceutical Sciences, School of PharmacyGeriatric Psychopharmacology Laboratory, Department of Psychiatry, School of Medicine, University of Pittsburgh, Pittsburgh, PennsylvaniaGeriatric Mental Health Program, Centre for Addiction and Mental Health, Toronto, Ontario, Canada§Rotman Research Institute, Toronto, Ontario, CanadaDepartment of Psychiatry, University of Toronto, Toronto, Ontario, Canada#Johnson & Johnson Health Care Systems Inc., Piscataway, New Jersey**Johnson & Johnson Pharmaceutical Research and Development, Raritan, New Jersey††ETHICON, Inc., Somerville, New Jersey‡‡F. Hoffman-La Roche Inc., Nutley, New Jersey.
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  • Denise A. Sorisio BS,

    1. From the *Department of Pharmaceutical Sciences, School of PharmacyGeriatric Psychopharmacology Laboratory, Department of Psychiatry, School of Medicine, University of Pittsburgh, Pittsburgh, PennsylvaniaGeriatric Mental Health Program, Centre for Addiction and Mental Health, Toronto, Ontario, Canada§Rotman Research Institute, Toronto, Ontario, CanadaDepartment of Psychiatry, University of Toronto, Toronto, Ontario, Canada#Johnson & Johnson Health Care Systems Inc., Piscataway, New Jersey**Johnson & Johnson Pharmaceutical Research and Development, Raritan, New Jersey††ETHICON, Inc., Somerville, New Jersey‡‡F. Hoffman-La Roche Inc., Nutley, New Jersey.
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  • Robert R. Bies PharmD, PhD,

    1. From the *Department of Pharmaceutical Sciences, School of PharmacyGeriatric Psychopharmacology Laboratory, Department of Psychiatry, School of Medicine, University of Pittsburgh, Pittsburgh, PennsylvaniaGeriatric Mental Health Program, Centre for Addiction and Mental Health, Toronto, Ontario, Canada§Rotman Research Institute, Toronto, Ontario, CanadaDepartment of Psychiatry, University of Toronto, Toronto, Ontario, Canada#Johnson & Johnson Health Care Systems Inc., Piscataway, New Jersey**Johnson & Johnson Pharmaceutical Research and Development, Raritan, New Jersey††ETHICON, Inc., Somerville, New Jersey‡‡F. Hoffman-La Roche Inc., Nutley, New Jersey.
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  • Georges Gharabawi MD

    1. From the *Department of Pharmaceutical Sciences, School of PharmacyGeriatric Psychopharmacology Laboratory, Department of Psychiatry, School of Medicine, University of Pittsburgh, Pittsburgh, PennsylvaniaGeriatric Mental Health Program, Centre for Addiction and Mental Health, Toronto, Ontario, Canada§Rotman Research Institute, Toronto, Ontario, CanadaDepartment of Psychiatry, University of Toronto, Toronto, Ontario, Canada#Johnson & Johnson Health Care Systems Inc., Piscataway, New Jersey**Johnson & Johnson Pharmaceutical Research and Development, Raritan, New Jersey††ETHICON, Inc., Somerville, New Jersey‡‡F. Hoffman-La Roche Inc., Nutley, New Jersey.
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  • Data from this study were presented at the 2006 meeting of the American Association of Pharmaceutical Sciences, October 29 to November 2, 2006, San Antonio, Texas.

Address correspondence to Benoit H. Mulsant, MD, CAMH, #3011, 1001 Queen Street West, Toronto, Ontario, Canada, M6J 1H4. E-mail: benoit_mulsant@camh.net

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.

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