Measurement of Anticholinergic Effects of Psychotropic Drugs in Humans

Abstract

Psychotropic drugs are often liable to unwanted anticholinergic effects that reduce tolerance and compliance. Especially, in certain patient groups, such as elderly patients, anticholinergic adverse effects may be hazardous. There are also occasions in therapy when antimuscarinic activity is desired, e. g. in the treatment of neuroleptic-induced extrapyramidal symptoms with biperiden and other potent anticholinergic drugs. In this review, we describe various techniques to evaluate the anticholinergic influences of psychotropic drugs in vivo and also provide examples of previous human studies where these methods have been applied. By combining subjective ratings of anticholinergic effects to in vitro measurements of antimuscarinic activity in blood, as well as the functional state of salivary glands, sweat glands, heart and eye, a researcher can obtain a detailed anticholinergic profile of the drug in question, or a clinician can estimate the anticholinergic burden of his/her psychiatric patient who often uses multiple medications.

Challenges in pharmacologic management of the hospitalized patient with psychiatric comorbidity

“…Anticholinergic effects have also been reported with the low potency first generation neuroleptics and with the atypical antipsychotics olanzapine and clozapine. Additionally, medications used to treat the extrapyramidal symptoms associated with antipsychotics (such as benztropine and diphenhydramine) are strongly anticholinergic . Patients without previous overt anticholinergic symptoms from these medications may experience adverse effects when hospitalized.…”

Acute and subchronic effects of bilastine (20 and 40 mg) and hydroxyzine (50 mg) on actual driving performance in healthy volunteers

“…Besides antihistaminergic effects, hydroxyzine is also known for its anticholinergic effects in the CNS. Anticholinergic effects may include memory impairment and impaired concentration as well as drowsiness and fatigue (Lieberman, 2004; Penttila et al, 2005). Partial tolerance to the behavioural effects of anticholinergic drugs has been reported (Gillin et al, 1991), which may explain why hydroxyzine’s detrimental effect on driving only partially subsides.…”

A Report of Rabbit Syndrome Who Benefited from Sigma 1 Agonist Fluvoxamine

“…Anticholinergic agents such as, benzatropine, biperiden, trihexyphenidyl are accepted to be the most effective agents for the treatment of Rabbit syndrome12); however, besides treatment, these agents can affect various systems of the body regarding cholinergic distribution of cholinergic receptors 35). Although fluvoxamine has anticholinergic activities on the living body, it has been considered to lack specific and significant affinity on muscarinic receptors.…”

“…Although fluvoxamine has anticholinergic activities on the living body, it has been considered to lack specific and significant affinity on muscarinic receptors. Among antidepressants, fluvoxamine has been placed in the low anticholinergic effect class with antidepressants, such as bupropion, fluoxetine, mirtazapine, sertraline, and trazodone 35–37). Since the most acceptable approach in the treatment of Rabbit syndrome is the use of anticholinergics, in this case a question arises that the action of mechanism of fluvoxamine might be due to its low anticholinergic effects.…”