Anticholinergic Activity of 107 Medications Commonly Used by Older Adults
Marci L. Chew PhD
From the *Department of Pharmaceutical Sciences, School of Pharmacy†Geriatric Psychopharmacology Laboratory, Department of Psychiatry, School of Medicine, University of Pittsburgh, Pittsburgh, Pennsylvania‡Geriatric Mental Health Program, Centre for Addiction and Mental Health, Toronto, Ontario, Canada§Rotman Research Institute, Toronto, Ontario, Canada∥Department 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.
Search for more papers by this authorBenoit H. Mulsant MD
From the *Department of Pharmaceutical Sciences, School of Pharmacy†Geriatric Psychopharmacology Laboratory, Department of Psychiatry, School of Medicine, University of Pittsburgh, Pittsburgh, Pennsylvania‡Geriatric Mental Health Program, Centre for Addiction and Mental Health, Toronto, Ontario, Canada§Rotman Research Institute, Toronto, Ontario, Canada∥Department 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.
Search for more papers by this authorBruce G. Pollock MD, PhD
From the *Department of Pharmaceutical Sciences, School of Pharmacy†Geriatric Psychopharmacology Laboratory, Department of Psychiatry, School of Medicine, University of Pittsburgh, Pittsburgh, Pennsylvania‡Geriatric Mental Health Program, Centre for Addiction and Mental Health, Toronto, Ontario, Canada§Rotman Research Institute, Toronto, Ontario, Canada∥Department 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.
Search for more papers by this authorMark E. Lehman PharmD
From the *Department of Pharmaceutical Sciences, School of Pharmacy†Geriatric Psychopharmacology Laboratory, Department of Psychiatry, School of Medicine, University of Pittsburgh, Pittsburgh, Pennsylvania‡Geriatric Mental Health Program, Centre for Addiction and Mental Health, Toronto, Ontario, Canada§Rotman Research Institute, Toronto, Ontario, Canada∥Department 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.
Search for more papers by this authorAndrew Greenspan MD
From the *Department of Pharmaceutical Sciences, School of Pharmacy†Geriatric Psychopharmacology Laboratory, Department of Psychiatry, School of Medicine, University of Pittsburgh, Pittsburgh, Pennsylvania‡Geriatric Mental Health Program, Centre for Addiction and Mental Health, Toronto, Ontario, Canada§Rotman Research Institute, Toronto, Ontario, Canada∥Department 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.
Search for more papers by this authorRamy A. Mahmoud MD
From the *Department of Pharmaceutical Sciences, School of Pharmacy†Geriatric Psychopharmacology Laboratory, Department of Psychiatry, School of Medicine, University of Pittsburgh, Pittsburgh, Pennsylvania‡Geriatric Mental Health Program, Centre for Addiction and Mental Health, Toronto, Ontario, Canada§Rotman Research Institute, Toronto, Ontario, Canada∥Department 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.
Search for more papers by this authorMargaret A. Kirshner BA
From the *Department of Pharmaceutical Sciences, School of Pharmacy†Geriatric Psychopharmacology Laboratory, Department of Psychiatry, School of Medicine, University of Pittsburgh, Pittsburgh, Pennsylvania‡Geriatric Mental Health Program, Centre for Addiction and Mental Health, Toronto, Ontario, Canada§Rotman Research Institute, Toronto, Ontario, Canada∥Department 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.
Search for more papers by this authorDenise A. Sorisio BS
From the *Department of Pharmaceutical Sciences, School of Pharmacy†Geriatric Psychopharmacology Laboratory, Department of Psychiatry, School of Medicine, University of Pittsburgh, Pittsburgh, Pennsylvania‡Geriatric Mental Health Program, Centre for Addiction and Mental Health, Toronto, Ontario, Canada§Rotman Research Institute, Toronto, Ontario, Canada∥Department 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.
Search for more papers by this authorRobert R. Bies PharmD, PhD
From the *Department of Pharmaceutical Sciences, School of Pharmacy†Geriatric Psychopharmacology Laboratory, Department of Psychiatry, School of Medicine, University of Pittsburgh, Pittsburgh, Pennsylvania‡Geriatric Mental Health Program, Centre for Addiction and Mental Health, Toronto, Ontario, Canada§Rotman Research Institute, Toronto, Ontario, Canada∥Department 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.
Search for more papers by this authorGeorges Gharabawi MD
From the *Department of Pharmaceutical Sciences, School of Pharmacy†Geriatric Psychopharmacology Laboratory, Department of Psychiatry, School of Medicine, University of Pittsburgh, Pittsburgh, Pennsylvania‡Geriatric Mental Health Program, Centre for Addiction and Mental Health, Toronto, Ontario, Canada§Rotman Research Institute, Toronto, Ontario, Canada∥Department 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.
Search for more papers by this authorMarci L. Chew PhD
From the *Department of Pharmaceutical Sciences, School of Pharmacy†Geriatric Psychopharmacology Laboratory, Department of Psychiatry, School of Medicine, University of Pittsburgh, Pittsburgh, Pennsylvania‡Geriatric Mental Health Program, Centre for Addiction and Mental Health, Toronto, Ontario, Canada§Rotman Research Institute, Toronto, Ontario, Canada∥Department 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.
Search for more papers by this authorBenoit H. Mulsant MD
From the *Department of Pharmaceutical Sciences, School of Pharmacy†Geriatric Psychopharmacology Laboratory, Department of Psychiatry, School of Medicine, University of Pittsburgh, Pittsburgh, Pennsylvania‡Geriatric Mental Health Program, Centre for Addiction and Mental Health, Toronto, Ontario, Canada§Rotman Research Institute, Toronto, Ontario, Canada∥Department 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.
Search for more papers by this authorBruce G. Pollock MD, PhD
From the *Department of Pharmaceutical Sciences, School of Pharmacy†Geriatric Psychopharmacology Laboratory, Department of Psychiatry, School of Medicine, University of Pittsburgh, Pittsburgh, Pennsylvania‡Geriatric Mental Health Program, Centre for Addiction and Mental Health, Toronto, Ontario, Canada§Rotman Research Institute, Toronto, Ontario, Canada∥Department 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.
Search for more papers by this authorMark E. Lehman PharmD
From the *Department of Pharmaceutical Sciences, School of Pharmacy†Geriatric Psychopharmacology Laboratory, Department of Psychiatry, School of Medicine, University of Pittsburgh, Pittsburgh, Pennsylvania‡Geriatric Mental Health Program, Centre for Addiction and Mental Health, Toronto, Ontario, Canada§Rotman Research Institute, Toronto, Ontario, Canada∥Department 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.
Search for more papers by this authorAndrew Greenspan MD
From the *Department of Pharmaceutical Sciences, School of Pharmacy†Geriatric Psychopharmacology Laboratory, Department of Psychiatry, School of Medicine, University of Pittsburgh, Pittsburgh, Pennsylvania‡Geriatric Mental Health Program, Centre for Addiction and Mental Health, Toronto, Ontario, Canada§Rotman Research Institute, Toronto, Ontario, Canada∥Department 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.
Search for more papers by this authorRamy A. Mahmoud MD
From the *Department of Pharmaceutical Sciences, School of Pharmacy†Geriatric Psychopharmacology Laboratory, Department of Psychiatry, School of Medicine, University of Pittsburgh, Pittsburgh, Pennsylvania‡Geriatric Mental Health Program, Centre for Addiction and Mental Health, Toronto, Ontario, Canada§Rotman Research Institute, Toronto, Ontario, Canada∥Department 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.
Search for more papers by this authorMargaret A. Kirshner BA
From the *Department of Pharmaceutical Sciences, School of Pharmacy†Geriatric Psychopharmacology Laboratory, Department of Psychiatry, School of Medicine, University of Pittsburgh, Pittsburgh, Pennsylvania‡Geriatric Mental Health Program, Centre for Addiction and Mental Health, Toronto, Ontario, Canada§Rotman Research Institute, Toronto, Ontario, Canada∥Department 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.
Search for more papers by this authorDenise A. Sorisio BS
From the *Department of Pharmaceutical Sciences, School of Pharmacy†Geriatric Psychopharmacology Laboratory, Department of Psychiatry, School of Medicine, University of Pittsburgh, Pittsburgh, Pennsylvania‡Geriatric Mental Health Program, Centre for Addiction and Mental Health, Toronto, Ontario, Canada§Rotman Research Institute, Toronto, Ontario, Canada∥Department 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.
Search for more papers by this authorRobert R. Bies PharmD, PhD
From the *Department of Pharmaceutical Sciences, School of Pharmacy†Geriatric Psychopharmacology Laboratory, Department of Psychiatry, School of Medicine, University of Pittsburgh, Pittsburgh, Pennsylvania‡Geriatric Mental Health Program, Centre for Addiction and Mental Health, Toronto, Ontario, Canada§Rotman Research Institute, Toronto, Ontario, Canada∥Department 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.
Search for more papers by this authorGeorges Gharabawi MD
From the *Department of Pharmaceutical Sciences, School of Pharmacy†Geriatric Psychopharmacology Laboratory, Department of Psychiatry, School of Medicine, University of Pittsburgh, Pittsburgh, Pennsylvania‡Geriatric Mental Health Program, Centre for Addiction and Mental Health, Toronto, Ontario, Canada§Rotman Research Institute, Toronto, Ontario, Canada∥Department 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.
Search for more papers by this authorData 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.
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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