ANTICHOLINERGICS: Reference List of Drugs with Potential Anticholinergic Effects 1, 2, 3, 4, 5 J Bareham BSP © www.RxFiles.ca Aug 2021 WHENEVER POSSIBLE, AVOID DRUGS WITH MODERATE TO HIGH ANTICHOLINERGIC ACTIVITY IN OLDER ADULTS (>65 YEARS OF AGE) Low Anticholinergic Activity; Moderate/High Anticholinergic Activity -B in combo Beers Antibiotics Antiparkinsonian Cardiovascular Agents Immunosuppressants ampicillin *ALL AVAILABLE AS amantadine SYMMETREL atenolol TENORMIN azaTHIOprine IMURAN cefOXitin GENERIC benztropine mesylate COGENTIN captopril CAPOTEN cyclosporine NEORAL clindamycin bromocriptine PARLODEL chlorthalidone GENERIC ONLY hydrocortisone CORTEF gentamicin (Oint & Sol’n NIHB covered) carbidopa/levodopa SINEMET digoxin LANOXIN, TOLOXIN methylprednisolone MEDROL piperacillin entacapone COMTAN dilTIAZem CARDIZEM, TIAZAC prednisone WINPRED dipyridamole PERSANTINE, ethopropazine PARSITAN vancomycin phenelzine NARDIL AGGRENOX disopyramide RYTHMODAN Muscle Relaxants pramipexole MIRAPEX Antidepressants baclofen LIORESAL ( on intrathecal only) procyclidine KEMADRIN furosemide LASIX amitriptyline ELAVIL cyclobenzaprine FLEXERIL selegiline ELDEPRYL hydrALAZINE APRESOLINE clomiPRAMINE ANAFRANIL isosorbide ISORDIL methocarbamol ROBAXIN OTC trihexyphenidyl ARTANE desipramine NORPRAMIN metoprolol LOPRESOR orphenadrine NORFLEX OTC doxepin >6mg SINEQUAN Antipsychotics NIFEdipine ADALAT tiZANidine ZANAFLEX A imipramine TOFRANIL quiNIDine GENERIC ONLY C ARIPiprazole ABILIFY & MAINTENA T Baclofen is the preferred agent of the above listed muscle nortriptyline AVENTYL asenapine SAPHRIS (-BPAD) triamterene DYRENIUM -less anticholinergic effects than amitriptyline & imipramine warfarin COUMADIN relaxants however, it does display moderate to high chlorproMAZINE LARGACTIL anticholinergic activity. trimipramine SURMONTIL cloZAPine CLOZARIL Gastrointestinal Agents ----------------------------------------------------------------------------------------------- flupentixol FLUANXOL ⌂ citalopram CELEXA atropine LOMOTIL on SPDP, Opioids fluPHENAZine MODITEN CIPRALEX belladonna GENERIC ONLY meperidine DEMEROL*Not for chronic use I escitalopram haloperidol HALDOL OTC R bisacodyl BISACODYL codeine ( on controlled release only, , inj & liquid) FLUoxetine PROZAC loxapine LOXAPAC S LUVOX chlordiazepoxide/clidinium LIBRAX fentaNYL DURAGESIC ⌂ S fluvoxaMINE lurasidone ◊ LATUDA cimetidine TAGAMET HYDROmorphone DILAUDID, PARoxetine PAXIL methotrimeprazine NOZINAN sertraline ZOLOFT dicyclomine BENTYLOL HYDROMORPH CONTIN on CR only ----------------------------------------------------------------------------------------------- OLANZapine ZYPREXA OTC dimenhyDRINATE GRAVOL morphine STATEX, M.O.S., KADIAN , paliperidone INVEGA ( on injection only) ⌂ buPROPion WELLBUTRIN ZYBAN diphenoxylate/atropine LOMOTIL on SPDP, oxyCODONE SUPEDOL, OXY IR PRISTIQ pericyazine NEULEPTIL desvenlafaxine domperidone MOTILIUM OXYNEO DULoxetine CYMBALTA perphenazine TRILAFON OTC & Rx famotidine PEPCID traMADol ULTRAM, RALIVIA, TRIDURAL, r mirtazapine REMERON pimozide ORAP OTC e loperamide IMODIUM ZYTRAM XL h SEROQUEL moclobemide MANERIX QUEtiapine t if used short term Preferred Alternatives: risperiDONE RISPERDAL ( on injection) O NARDIL phenelzine meclizine BONAMINE acetaminophen , NSAIDs (e.g. ibuprofen, naproxen) STELAZINE traZODone TRAZOREL trifluoperazine metoclopramide MAXERAN venlafaxine EFFEXOR ziprasidone ZELDOX nizatidine AXID Miscellaneous CELEXA ZOLOFT zuclopenthixol ◊ CLOPIXOL In the elderly, citalopram & sertraline prochlorperazine STEMETIL busPIRone ◊ BUSPAR are the usually preferred SSRIs. Antiseizure Drugs if used short term celecoxib CELEBREX carBAMazepine TEGRETOL promethazine PHENERGAN OTC colchicine GENERIC ONLY Antihistamines/Antipruritics divalproex EPIVAL raNITIdine ZANTAC OTC & Rx ketotifen ophthalmic ZADITOR brompheniramine COUGH&COLD PRODUCTS OTC OXcarbazepine TRILEPTAL -low anticholinergic activity if adjusted for renal function lithium CARBOLITH, chlorpheniramine CHLOR-TRIPOLON OTC DEPAKENE scopolamine TRANSDERM V OTC on SPDP, ⌂ DURALITH valproic acid OTC cyproheptadine PERIACTIN Preferred Alternatives: divalproex EPIVAL, Preferred Alternatives: bisacodyl , PPIs, metformin GLUCOPHAGE, GLYCON, g OTC diphenhydrAMINE BENADRYL NEURONTIN LAMICTAL KEPPRA domperidone; famotidine, or ranitidine if ≤150mg/day methotrexate GENERIC ONLY gabapentin , lamotrigine , levetiracetam . doxylamine UNISOM naratriptan AMERGE hydrOXYzine ATARAX Respiratory Meds Antispasmotics pancuronium GENERIC ONLY , OTC aclidinium bromide TUDORZA GENUAIR pyrilamine MIDOL PAMPRIN , SUMAtriptan IMITREX dicyclomine FORMULEX BENTYLOL aclidinium/formoterol DUAKLIR GENUAIR trimeprazine ◊ PANECTYL ⌂ ZOLMitriptan ZOMIG glycopyrrolate ROBINUL fluticasone/salmeterol ADVAIR COTRIDIN OMBIVENT triprolidine /salbutamol ATROVENT/C REACTINE hyoscine butylbromide BUSCOPAN ipratropium _______ = Possible preferred alternatives Preferred Alternatives: cetirizine & glycopyrronium SEEBRI BREEZHALER = Denotes agents with anticholinergic activity that fexofenadine ALLEGRA (controversial rating as medium/ Benzodiazepines glycopyrronium/Indacaterol may be better tolerated than others. Whenever high activity) , desloratadine AERIUS , ALPRAZolam XANAX half-life: ~12 hr ULTIBRO BREEZHALER possible, anticholinergic drugs should be avoided, & loratadine CLARITIN . chlordiazePOXIDE LIBRIUM half-life: ~100 hr pseudoephedrine COUGH & COLD PRODUCTS OTC the preferred agents used. ◊ = Unable to confirm anticholinergic activity (black font) clonazePAM RIVOTRIL half-life: ~34 hr THEOLAIR, UNIPHYL theophylline AChEI = Acetylcholinesterase Inhibitor (e.g. donepezil clorazepate TRANXENE half-life:~100 hr Antimuscarinics/Incontinence Meds tiotropium SPIRIVA ARICEPT, galantamine REMINYL, rivastigmine EXELON) darifenacin ENABLEX diazePAM VALIUM half-life: ~100 hr tiotropium/olodaterol INSPIOLTO CR = Controlled Release Formulation TOVIAZ flurazepam DALMANE half-life:~100 hr fesoterodine PPI = Proton Pump Inhibitor (e.g. rabeprazole) flavoxate URISPAS LORazepam ATIVAN half-life: ~15 hr umeclidinium INCRUSE ELLIPTA OTC = Over-the-counter mirabegron ◊ MYRBETRIQ midazolam VERSED half-life: ~3 hr umeclidinium/vilanterol ANORO ELLIPTA oxybutynin DITROPAN ( on XL only) oxazepam SERAX half-life: ~8 hr umeclidinium/vilanterol/fluticasone = Saskatchewan Health finds co-administration PEDIATRIC temazepam RESTORIL half-life: ~11 hr of this agent with a AChEI acceptable propiverine MICTORYL TRELEGY ELLIPTA on SPDP triazolam HALCION half-life: ~2 hr solifenacin VESICARE TO MINIMIZE SYSTEMIC EFFECTS OF INHALATIONAL MEDS: AVOID on SPDP = If patient is currently on this medication, tolterodine l-tartrate DETROL LA Avoid long- & ultra-short acting agents in the elderly. OVERUSE, USE AEROCHAMBER FOR IPRATROPIUM INHALER. Saskatchewan Health will NOT cover AChEI trospium TROSEC (Clonazepam ok, if long-acting required e.g. chronic anxiety) 154 Drugs with Anticholinergic Effects 5,6,7,8 Diseases associated with an essential cholinergic deficit include Alzheimer’s dementia, Lewy body dementia & to some extent other dementias (not frontal). Anticholinergic drugs worsen the deficit & are therefore highly problematic. Donepezil ARICEPT, rivastigmine EXELON, and galantamine REMINYL are reversible inhibitors of the enzyme acetylcholinesterase. Because of the mechanism of action, medications with anticholinergic effects can interfere with the activity of donepezil, rivastigmine and galantamine. The reverse page of this document contains a list of drugs with anticholinergic effects, with an emphasis on those with moderate to high activity. Drug coverage (in Sask.) may be affected if a patient is using a drug on this list concurrently with donepezil, rivastigmine or galantamine. Not only is drug coverage of concern, the use of drugs with anticholinergic activity can increase the risk of adverse effects (e.g., cognitive dysfunction, delirium) in the elderly. Drugs with low anticholinergic activity may be good alternatives to drugs with more anticholinergic activity. For example, SSRIs with lower anticholinergic activity are preferred over tricyclics for treatment of depression in the elderly. However, it’s not just the use of single drugs with significant anticholinergic activity that can cause trouble. Individuals who take multiple medications with low anticholinergic activity may also have increased risk of adverse effects. In fact, even small increases in so-called anticholinergic burden or load increases the risk of morbidity & mortality in older individuals.9 Total Anticholinergic Load: both highly anticholinergic drugs plus others (e.g. digoxin, paroxetine, ranitidine) contribute to the anticholinergic load & cognitive impairment. Review each medication the patient is taking. Tips to Deal with Anticholinergic Side-Effects Spectrum of Anticholinergic Side-Effects Mild Moderate Severe General approach: Dryness of mouth Moderately disturbing Difficulty chewing, swallowing, Mucosal damage Identify the cause Discontinue unnecessary offending medications (modest) dry mouth/thirst speaking Malnutrition Reduce the dose Speech problems Impaired perception of taste Respiratory Reduced appetite & texture of food infection Look for effective alternatives that are less likely to cause the side