Anticholinergic Accumulation: A Slumbering Interaction between Drugs and Food Supplements

Research output: Contribution to journalArticleAcademicpeer-review

Abstract

Many compounds display anticholinergic effects which might give rise to cognitive impairment and even delirium. These side effects are caused by their ability to bind to muscarinic receptors in our brain. Especially with combination of compounds, these serious effects are seen. This phenomenon, known as anticholinergic accumulation, is especially seen in the elderly. A classification of drugs for anticholinergic side effects has been made based on clinical observations, the ACB score. Here, we aimed to substantiate this classification by comparing the affinity of numerous drugs for the muscarinic receptors to the ACB score. Additionally, a number of supplements were screened. The affinity of the compounds was determined by their ability to displace the radioligand [(3) H]pirenzepine of the muscarinic receptor induced by these compounds. Our results show that the affinity of a compound for the muscarinic receptors correlated with its ACB score. Also food supplements appeared to bind to these muscarinic receptors. Moreover, several drug-drug, supplement-supplement and supplement-drug combinations had an affinity that is higher than the affinity of single compounds. This explains the phenomenon of anticholinergic accumulation. In conclusion, care should be taken to drug-drug and supplement-drug combinations with respect to anticholinergic accumulation.
Original languageEnglish
Pages (from-to)427-432
Number of pages6
JournalBasic & Clinical Pharmacology & Toxicology
Volume117
Issue number6
DOIs
Publication statusPublished - Dec 2015

Keywords

  • BLOOD-BRAIN-BARRIER
  • COGNITIVE IMPAIRMENT
  • DELIRIUM
  • POPULATION
  • DEMENTIA
  • IMPACT
  • MEDICATIONS
  • BURDEN
  • RISK
  • ASSOCIATION

Cite this

@article{a750e51a486d46e2972c8b838b2c116d,
title = "Anticholinergic Accumulation: A Slumbering Interaction between Drugs and Food Supplements",
abstract = "Many compounds display anticholinergic effects which might give rise to cognitive impairment and even delirium. These side effects are caused by their ability to bind to muscarinic receptors in our brain. Especially with combination of compounds, these serious effects are seen. This phenomenon, known as anticholinergic accumulation, is especially seen in the elderly. A classification of drugs for anticholinergic side effects has been made based on clinical observations, the ACB score. Here, we aimed to substantiate this classification by comparing the affinity of numerous drugs for the muscarinic receptors to the ACB score. Additionally, a number of supplements were screened. The affinity of the compounds was determined by their ability to displace the radioligand [(3) H]pirenzepine of the muscarinic receptor induced by these compounds. Our results show that the affinity of a compound for the muscarinic receptors correlated with its ACB score. Also food supplements appeared to bind to these muscarinic receptors. Moreover, several drug-drug, supplement-supplement and supplement-drug combinations had an affinity that is higher than the affinity of single compounds. This explains the phenomenon of anticholinergic accumulation. In conclusion, care should be taken to drug-drug and supplement-drug combinations with respect to anticholinergic accumulation.",
keywords = "BLOOD-BRAIN-BARRIER, COGNITIVE IMPAIRMENT, DELIRIUM, POPULATION, DEMENTIA, IMPACT, MEDICATIONS, BURDEN, RISK, ASSOCIATION",
author = "M.F. Vrolijk and A. Opperhuizen and E.H. Jansen and A. Bast and G.R. Haenen",
year = "2015",
month = "12",
doi = "10.1111/bcpt.12437",
language = "English",
volume = "117",
pages = "427--432",
journal = "Basic & Clinical Pharmacology & Toxicology",
issn = "1742-7835",
publisher = "Wiley",
number = "6",

}

Anticholinergic Accumulation: A Slumbering Interaction between Drugs and Food Supplements. / Vrolijk, M.F.; Opperhuizen, A.; Jansen, E.H.; Bast, A.; Haenen, G.R.

In: Basic & Clinical Pharmacology & Toxicology, Vol. 117, No. 6, 12.2015, p. 427-432.

Research output: Contribution to journalArticleAcademicpeer-review

TY - JOUR

T1 - Anticholinergic Accumulation: A Slumbering Interaction between Drugs and Food Supplements

AU - Vrolijk, M.F.

AU - Opperhuizen, A.

AU - Jansen, E.H.

AU - Bast, A.

AU - Haenen, G.R.

PY - 2015/12

Y1 - 2015/12

N2 - Many compounds display anticholinergic effects which might give rise to cognitive impairment and even delirium. These side effects are caused by their ability to bind to muscarinic receptors in our brain. Especially with combination of compounds, these serious effects are seen. This phenomenon, known as anticholinergic accumulation, is especially seen in the elderly. A classification of drugs for anticholinergic side effects has been made based on clinical observations, the ACB score. Here, we aimed to substantiate this classification by comparing the affinity of numerous drugs for the muscarinic receptors to the ACB score. Additionally, a number of supplements were screened. The affinity of the compounds was determined by their ability to displace the radioligand [(3) H]pirenzepine of the muscarinic receptor induced by these compounds. Our results show that the affinity of a compound for the muscarinic receptors correlated with its ACB score. Also food supplements appeared to bind to these muscarinic receptors. Moreover, several drug-drug, supplement-supplement and supplement-drug combinations had an affinity that is higher than the affinity of single compounds. This explains the phenomenon of anticholinergic accumulation. In conclusion, care should be taken to drug-drug and supplement-drug combinations with respect to anticholinergic accumulation.

AB - Many compounds display anticholinergic effects which might give rise to cognitive impairment and even delirium. These side effects are caused by their ability to bind to muscarinic receptors in our brain. Especially with combination of compounds, these serious effects are seen. This phenomenon, known as anticholinergic accumulation, is especially seen in the elderly. A classification of drugs for anticholinergic side effects has been made based on clinical observations, the ACB score. Here, we aimed to substantiate this classification by comparing the affinity of numerous drugs for the muscarinic receptors to the ACB score. Additionally, a number of supplements were screened. The affinity of the compounds was determined by their ability to displace the radioligand [(3) H]pirenzepine of the muscarinic receptor induced by these compounds. Our results show that the affinity of a compound for the muscarinic receptors correlated with its ACB score. Also food supplements appeared to bind to these muscarinic receptors. Moreover, several drug-drug, supplement-supplement and supplement-drug combinations had an affinity that is higher than the affinity of single compounds. This explains the phenomenon of anticholinergic accumulation. In conclusion, care should be taken to drug-drug and supplement-drug combinations with respect to anticholinergic accumulation.

KW - BLOOD-BRAIN-BARRIER

KW - COGNITIVE IMPAIRMENT

KW - DELIRIUM

KW - POPULATION

KW - DEMENTIA

KW - IMPACT

KW - MEDICATIONS

KW - BURDEN

KW - RISK

KW - ASSOCIATION

U2 - 10.1111/bcpt.12437

DO - 10.1111/bcpt.12437

M3 - Article

VL - 117

SP - 427

EP - 432

JO - Basic & Clinical Pharmacology & Toxicology

JF - Basic & Clinical Pharmacology & Toxicology

SN - 1742-7835

IS - 6

ER -