Table 5.

Universal list of drugs with documented anticholinergic activity, based on objective pharmacological data, according to ATC classification, and considering the five muscarinic receptor subtypes.

ATC CLASSIFICATION	Drug	M1	M2	M3	M4	M5	Mu	BBB
A03A. DRUGS FOR FUNCTIONAL GASTROINTESTINAL DISORDERS
A03AA. Synthetic anticholinergics, esters with tertiary amino group
A03AA04	Mebeverine	✓	✓	✓	✓	✓		?
A03AA05	Trimebutine	✓	✓	✓	✓	✓		+
A03AA07	Dicyclomine	+++	++	+++	+++	0		+
A03AA09	Difemerine	✓	✓	✓	✓	✓		?
A03AB. Synthetic anticholinergics, quaternary ammonium compounds
A03AB05	Propantheline	+++	+++	+++	+++	0		-
A03AB06	Octylonium bromide	+++	++	++	++	0		-
A03AB17	Tiemonium	✓	✓	✓	✓	✓		?
A03AB19	Timepidium	+++	+++	+++	+++	+++		-
A03AX. Other drugs for functional gastrointestinal disorders
A03AX14	Valethamate bromide	✓	✓	✓	✓	✓		?
A03B. BELLADONNA AND DERIVATIVES, PLAIN
A03BA. Belladonna alkaloids, tertiary amines
A03BA01	Atropine	+++	+++	+++	+++	+++		+
A03BA03	Hyoscyamine	+++	+++	+++	+++	+++		+
A03BA04	Belladona	✓	✓	✓	✓	✓		+
A03BB. Belladonna alkaloids, semisynthetic, and quaternary ammonium compounds
A03BB01	Butylscopolamine	0	++	++	0	0		-
A03BB05	Cimetropium	✓	✓	✓	✓	✓		?
A03BB06	Homatropine	+++	++	+++	+++	+++		-
A03C. ANTISPASMODICS IN COMBINATION WITH PSYCHOLEPTICS
A03CA. Synthetic anticholinergic agents in combination with psycholeptics
A03CA02	Clidinium	0	0	+++	0	0		+
A04A. ANTIEMETICS AND ANTINAUSEANTS
A04AD. Other antiemetics
A04AD01	Scopolamine	+++	+++	+++	+++	+++		+
C01B. ANTIARRHYTHMICS, CLASS I AND III
C01BA. Antiarrhythmics, class Ia
C01BA01	Quinidine	0	+++	0	0	0		+
C01BA02	Procainamide	0	+++	0	0	0		+
C01BA03	Disopyramide	+	+	0	0	0	+	+
C01BD. Antiarrhythmics, class III
C01BD01	Amiodarone						+	+
G04B. UROLOGICALS
G04BD. Drugs for urinary frequency and incontinence
G04BD01	Emepronium	✓	✓	✓	✓	✓		?
G04BD02	Flavoxate	✓	✓	✓	✓	✓		+
G04BD04	Oxybutynin chloride	+++	+++	+++	+++	+++		+
G04BD06	Propiverine	++	+	++	++	0		?
G04BD07	Tolterodine tartrate	+++	+++	+++	+++	+++		+
G04BD08	Solifenacin	+++	++	+++	+++	+++		+
G04BD09	Trospium chloride	+++	+++	+++	+++	+++		-
G04BD10	Darifenacin	+++	+++	+++	+++	+++		+
G04BD11	Fesoterodine	+++	++	+++	+++	+++		+
-	Imidafenacin	+++	+++	+++	+++	+++		+
M01A. ANTIINFLAMMATORY AND ANTIRHEUMATIC PRODUCTS, NON-STEROIDS
M01AH. Coxibs
M01AH05	Etoricoxib	+	0	0	0	0		+
M03A. MUSCLE RELAXANTS, PERIPHERALLY ACTING AGENTS
M03AC. Other quaternary ammonium compounds
M03AC01	Pancuronium	++	+++	++	++	+		-
M03B. MUSCLE RELAXANTS, CENTRALLY ACTING AGENTS
M03BX. Other centrally acting agents
M03BX03	Pridinol							+
M03BX08	Cyclobenzaprine	+++	+++	+++	0	0		+
N02A. OPIOIDS
N02AB. Phenylpiperidine derivatives
N02AB02	Pethidine						++	+
N02AB03	Fentanyl						+	+
N02AX. Other opioids
N02AX02	Tramadol	0	0	++	0	0		+
N04A. ANTICHOLINERGIC AGENTS
N04AA. Tertiary amines
N04AA01	Trihexyphenidyl	+++	+++	+++	+++	+++		+
N04AA02	Biperiden	+++	+++	+++	+++	0		+
N04AA04	Procyclidine	+++	+++	+++	+++	+++		+
N04AA12	Tropatepine	✓	✓	✓	✓	✓		?
N04AB. Ethers chemically close to antihistamines
N04AB02	Orphenadrine	+++	++	++	++	++		+
N04AC. Ethers of tropine or tropine derivatives
N04AC01	Benzatropine	+++	+++	+++	+++	+++		+
N05A. ANTIPSYCHOTICS
N05AA. Phenothiazines with aliphatic side-chain
N05AA01	Chlorpromazine	+++	++	+++	+++	+++		+
N05AA02	Levomepromazine						++	+
N05AA03	Promazine	+++	++	0	0	0		+
N05AA04	Acepromazine							+
N05AA06	Cyamemazine	+++	+++	+++	+++	+++		+
N05AB. Phenothiazines with piperazine structure
N05AB02	Fluphenazine	+	+	+	+	++		+
N05AB03	Perphenazine	+	+	+	0	0		+
N05AB04	Prochlorperazine	++	+	0	0	0		+
N05AB06	Trifluoperazine	+	+	++	0	0		+
N05AC. Phenothiazines with piperidine structure
N05AC01	Periciazine	✓	✓	✓	✓	✓		+
N05AC02	Thioridazine	+++	++	+++	++	+++	++	+
N05AC03	Mesoridazine	+++	+++	+++	+++	+++	+++	+
N05AC04	Pipotiazine	✓	✓	✓	✓	✓		+
N05AD. Butyrophenone derivatives
N05AD01	Haloperidol	+	+	0	+	+		+
N05AD06	Bromperidol	+	+	+	+	+		?
N05AE. Indole derivatives
N05AE03	Sertindole	++	0	+	0	0		+
N05AE04	Ziprasidone	+	+	+	+	+		+
N05AF. Thioxanthene derivatives
N05AF01	Flupentixol	✓	✓	✓	✓	✓		+
N05AF03	Chlorprothixene	+++	+++	+++	+++	+++		+
N05AF04	Tiotixene	+	+	+	0	0		+
N05AG. Diphenylbutylpiperidine derivatives
N05AG02	Pimozide			+			+	+
N05AH. Diazepines, oxazepines, thiazepines, and oxepines
N05AH01	Loxapine	++	++	++	++	++		+
N05AH02	Clozapine	+++	+++	+++	+++	+++		+
N05AH03	Olanzapine	+++	++	+++	++	+++		+
N05AH04	Quetiapine	++	++	+	++	+		+
N05AH05	Asenapine	+	0	0	+	0		+
N05AX. Other antipsychotics
N05AX08	Risperidone	0	0	0	+	0		+
N05AX11	Zotepine	+++	++	+++	+++	++	++	+
N05AX12	Aripiprazol	+	+	+	+	+		+
N05AX14	Iloperidone	+	+	+	+	+		+
N05	Blonanserin						++	+
N05B. ANXIOLYTICS
N05BB. Diphenylmethane derivatives
N05BB01	Hydroxyzine						+	+
N06A. ANTIDEPRESSANTS
N06AA. Non-selective monoamine reuptake inhibitors
N06AA01	Desipramine	++	++	++	++	++		+
N06AA02	Imipramine	+++	+++	+++	++	+++		+
N06AA04	Clomipramine						+++	+
N06AA05	Opipramol	✓	✓	✓	✓	✓		?
N06AA06	Trimipramine						+++	+
N06AA07	Lofepramine	+++	++	++	++	++		+
N06AA09	Amitriptyline	+++	+++	+++	+++	+++		+
N06AA10	Nortriptyline	+++	++	+++	+++	+++		+
N06AA11	Protriptyline						+++	+
N06AA12	Doxepin	+++	++	+++	+++	+++		+
N06AA16	Dosulepin	+++	++	+++	+++	+++		+
N06AA17	Amoxapine						++	+
N06AA21	Maprotiline	✓	✓	✓	✓	✓		+
N06AB. Selective serotonin reuptake inhibitors
N06AB03	Fluoxetine	++	+	++	+	+		+
N06AB04	Citalopram	+	0	+	0	0		+
N06AB05	Paroxetine	++	++	+++	++	++		+
N06AB06	Sertraline	++	+	+	+	+		+
N06AB10	Escitalopram	+	0	+	0	0		+
N06AG. Monoamine oxidase A inhibitors
N06AG02	Moclobemide	✓	✓	✓	✓	✓		+
N06AX. Other antidepressants
N06AX06	Nefazodone						+	+
N06AX11	Mirtazapine			++			+	+
N06AX21	Duloxetine	++	++	+	0	0		+
N07C. ANTIVERTIGO PREPARATIONS
N07CA. Antivertigo preparations
N07C	Difenidol	++	+	++	++	+		+
N07CA02	Cinnarizine						++	+
R03B. OTHER DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES, INHALANTS
R03BB. Anticholinergics
R03BB01	Ipratropium	+++	+++	+++	+++	+++		+
R03BB02	Oxitropium bromide	+++	+++	+++	0	0		?
R03BB04	Tiotropium	+++	+++	+++	+++	+++		-
R03BB05	Aclidinium	+++	+++	+++	+++	+++		-
R03BB06/A03AB02	Glycopyrronium/Glycopyrrolate	+++	+++	+++	+++	+++		-
R05D. COUGH SUPPRESSANTS, EXCL. COMBINATIONS WITH EXPECTORANTS
R05DB. Other cough suppressants
R05DB21	Cloperastine	✓	✓	✓	✓	✓		-
R06A. ANTIHISTAMINES FOR SYSTEMIC USE
R06AA. Aminoalkyl ethers
R06AA02	Diphenhydramine	++	++	++	++	++	++	+
R06AA04	Clemastine						+++	+
R06AA07	Piprinhydrinate						+++	+
R06AA08	Carbinoxamine						++	+
R06AA09	Doxylamine	✓	✓	✓	✓	✓		+
R06AA11	Dimenhydrinate						++	+
R06AB. Substituted alkylamines
R06AB01	Brompheniramine	✓	✓	✓	✓	✓		+
R06AB02	Dexchlorpheniramine						++	+
R06AB03	Dimetindene	++	++	++	++	+		-
R06AB06	Dexbrompheniramine	✓	✓	✓	✓	✓		+
R06AD. Phenothiazine derivatives
R06AD01	Alimemazine						+++	-
R06AD02	Promethazine						+++	+
R06AD07	Mequitazine	+++	+++	+++	+++	+++		+
R06AE. Piperazine derivatives
R06AE01	Buclizine	✓	✓	✓	✓	✓		+
R06AE05	Meclizine						+	+
R06AX. Other antihistamines for systemic use
R06AX02	Cyproheptadine	+++	+++	+++	+++	+++		+
R06AX07	Triprolidine						++	+
R06AX11	Astemizole						+	-
R06AX13	Loratadine	✓	✓	✓	✓	✓		-
R06AX17	Ketotifen	++	++	++	0	0		+
S01F. MYDRIATICS AND CYCLOPLEGICS
S01FA. Anticholinergics
S01FA01	Atropine Sulfate ophthalmic	+++	+++	+++	+++	+++		+
S01FA04	Cyclopentolate ophthalmic	+++	+++	+++	+++	0		+
S01FA06	Tropicamide ophthalmic	+++	+++	+++	+++	++		+
S01G. DECONGESTANTS AND ANTIALLERGICS
S01GX. Other antiallergics
S01GX08	Ketotifen ophthalmic	++	++	++	0	0		+
DRUGS WITHOUT ATC
-	Homochlorcyclizine						+++	?
-	Oxapium iodide	✓	✓	✓	✓	✓		?
-	Tiquizium	+++	+++	+++	+++	+++		?

M1—muscarinic receptor M1; M2—muscarinic receptor M2; M3—muscarinic receptor M3; M4—muscarinic receptor M4; and M5—muscarinic receptor M5. Mu: muscarinic acetylcholine receptor (no specific subtype) Classification +: 5.00 ≤ pK_i ≤ 5.99; 5.00 ≤ pK_d ≤ 5.99; 5.00 ≤ pIC₅₀ ≤ 5.99; 5.00 ≤ pA₂ ≤ 5.99. Classification ++: 6.00 ≤ pK_i ≤ 7.00; 6.00 ≤ pK_d≤ 7.00; 6.00 ≤ pIC₅₀ ≤ 7.00; 6.00 ≤ pA₂ ≤ 7.00. Classification +++: pK_i > 7; pK_d > 7; pIC₅₀ > 7; pA₂ > 7. ✓: reported affinity, but no experimental measure of ligand action identified. 0: no specific affinity was found for a particular receptor subtype. BBB: blood-brain barrier. +: drug crosses BBB. -: drug does not cross BBB. ?: information not available in databases.