DT-Web

DB00771 - Clidinium


Identification
Name Clidinium
Accession Number DB00771 (APRD00737)
Type small molecule
Description Clidinium is a synthetic anticholinergic agent which has been shown in experimental and clinical studies to have a pronounced antispasmodic and antisecretory effect on the gastrointestinal tract. It inhibits muscarinic actions of acetylcholine at postganglionic parasympathetic neuroeffector sites. It is used for the treatment of peptic ulcer disease and also to help relieve abdominal or stomach spasms or cramps due to colicky abdominal pain, diverticulitis, and irritable bowel syndrome.
Structure
MOL SDF PDB SMILES InChI
Categories (*)
Molecular Weight 352.4467
Groups approved
Monoisotopic Weight 352.191268703
Pharmacology
Indication For the treatment of peptic ulcer disease and also to help relieve abdominal or stomach spasms or cramps due to colicky abdominal pain, diverticulitis, and irritable bowel syndrome.
Mechanism of action Inhibits muscarinic actions of acetylcholine at postganglionic parasympathetic neuroeffector sites primarily by inhibiting the M1 muscarinic receptors.
Absorption Not Available
Protein binding Not Available
Biotransformation Not Available
Route of elimination Not Available
Toxicity Signs of toxicity include confusion, paralytic ileus, urinary hesitancy/retention, and blurred vision.
Affected organisms
  • Humans and other mammals
Interactions
Drug Interactions
Drug Mechanism of interaction
Donepezil Possible antagonism of action
Galantamine Possible antagonism of action
Haloperidol The anticholinergic increases the risk of psychosis and tardive dyskinesia
Potassium Chloride Anticholinergic agents such as clidinium may enhance the ulcerogenic effect of potassium chloride. Solid oral dosage forms of potassium chloride are contraindicated in patients with impaired gastric emptying (e.g., due to the effects of drugs such as many anticholinergics). Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium chloride; liquid or effervescent potassium preparations are possible alternatives.
Pramlintide Pramlintide may enhance the anticholinergic effect of anticholinergics such as clidinium. These effects are specific to the GI tract. Use caution during concomitant therapy with pramlintide and anticholinergics. Additive effects on reduced GI motility may occur.
Secretin Anticholinergic agents such as secretin may diminish the stimulatory effect of secretin. Avoid using drugs with substantial anticholinergic effects in patients receiving secretin whenever possible. If such agents must be used in combination, monitor response to secretin closely.
Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor, Tacrine, and/or the anticholinergic, Clidinium, may be reduced due to antagonism. The interaction may be beneficial when the anticholinergic action is a side effect. Monitor for decreased efficacy of both agents.
Trimethobenzamide Trimethobenzamide and Clidinium, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Triprolidine Triprolidine and Clidinium, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Trospium Trospium and Clidinium, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Food Interactions Not Available

Targets


Muscarinic acetylcholine receptor M1
Name Muscarinic acetylcholine receptor M1
Gene Name CHRM1
Pharmacological action yes
Actions antagonist
References
  • Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. - Pubmed
  • Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. - Pubmed
  • Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. - Pubmed
DTHybrid score 0.3722

Predictions


Id Partner name Gene Name Score
617 Muscarinic acetylcholine receptor M2 CHRM2 0.128
51 Muscarinic acetylcholine receptor M3 CHRM3 0.1189
450 Muscarinic acetylcholine receptor M4 CHRM4 0.0681
274 Muscarinic acetylcholine receptor M5 CHRM5 0.0566
4119 Cytochrome P450 2D6 CYP2D6 0.0369
492 Histamine H1 receptor HRH1 0.0352
4512 Cytochrome P450 3A4 CYP3A4 0.022
831 D(2) dopamine receptor DRD2 0.0212
502 5-hydroxytryptamine 2A receptor HTR2A 0.021
3923 Cholinesterase BCHE 0.0188
556 Alpha-1A adrenergic receptor ADRA1A 0.0169
1588 Multidrug resistance protein 1 ABCB1 0.0164
23 D(1A) dopamine receptor DRD1 0.0146
824 Sodium-dependent serotonin transporter SLC6A4 0.012
590 5-hydroxytryptamine 2C receptor HTR2C 0.0118
540 Sodium-dependent noradrenaline transporter SLC6A2 0.0116
6016 Cytochrome P450 2C19 CYP2C19 0.0114
124 Histamine H2 receptor HRH2 0.0113
813 Neuronal acetylcholine receptor subunit alpha-2 CHRNA2 0.0094
1656 CYP2B protein CYP2B 0.0087
320 5-hydroxytryptamine 1A receptor HTR1A 0.0085
1181 Alpha-1-acid glycoprotein 1 ORM1 0.0083
4200 Cytochrome P450 1A2 CYP1A2 0.0083
713 Sodium-dependent dopamine transporter SLC6A3 0.0082
6013 Cytochrome P450 2E1 CYP2E1 0.0077
4757 Cytochrome P450 2C9 CYP2C9 0.0076
789 Alpha-1D adrenergic receptor ADRA1D 0.0073
436 5-hydroxytryptamine 2B receptor HTR2B 0.007
632 Alpha-1B adrenergic receptor ADRA1B 0.0068
833 Organic cation/carnitine transporter 1 SLC22A4 0.0063
432 D(4) dopamine receptor DRD4 0.0061
6030 Cytochrome P450 2B6 CYP2B6 0.006
318 Alpha-2A adrenergic receptor ADRA2A 0.0058
4924 Cytochrome P450 2C8 CYP2C8 0.0057
723 Cytosolic phospholipase A2 PLA2G4A 0.0057
4118 Cytochrome P450 3A5 CYP3A5 0.0054
6104 Dimethylaniline monooxygenase [N-oxide-forming] 1 FMO1 0.0053
6024 Cytochrome P450 1A1 CYP1A1 0.0051
118 Organic cation/carnitine transporter 2 SLC22A5 0.005
638 D(3) dopamine receptor DRD3 0.005
706 Glutamate [NMDA] receptor subunit 3A GRIN3A 0.0049
6098 Potassium voltage-gated channel subfamily D member 2 KCND2 0.0046
6099 Potassium voltage-gated channel subfamily D member 3 KCND3 0.0046
5878 Alpha-7 nicotinic cholinergic receptor subunit CHRFAM7A 0.0044
2129 Sucrase-isomaltase, intestinal SI 0.0043
378 Alpha-2C adrenergic receptor ADRA2C 0.0042
629 Alpha-2B adrenergic receptor ADRA2B 0.0042
458 Neuronal acetylcholine receptor subunit alpha-10 CHRNA10 0.004
528 5-hydroxytryptamine 1E receptor HTR1E 0.0038
6144 Solute carrier family 22 member 2 SLC22A2 0.0037
94 5-hydroxytryptamine 4 receptor HTR4 0.0036
1256 5-hydroxytryptamine 6 receptor HTR6 0.0035
163 D(1B) dopamine receptor DRD5 0.0034
5718 Cytochrome P450 2A6 CYP2A6 0.0034
6023 Cytochrome P450 11B2, mitochondrial CYP11B2 0.0033
3876 Aromatic-L-amino-acid decarboxylase DDC 0.0033
380 Cytochrome P450 17A1 CYP17A1 0.0032
716 5-hydroxytryptamine 7 receptor HTR7 0.0032
341 5-hydroxytryptamine 3 receptor HTR3A 0.003
220 Sodium channel protein type 5 subunit alpha SCN5A 0.003
805 Cytochrome P450 11B1, mitochondrial CYP11B1 0.0029
725 5-hydroxytryptamine 1D receptor HTR1D 0.0028
885 5-hydroxytryptamine 1B receptor HTR1B 0.0028
6176 UDP-glucuronosyltransferase 1-3 UGT1A3 0.0027
6107 Cytochrome P450 3A7 CYP3A7 0.0027
6145 Solute carrier family 22 member 1 SLC22A1 0.0025
465 Calmodulin CALM1 0.0022
215 Sodium channel protein type 11 subunit alpha SCN11A 0.0021
6432 Transporter snf 0.0018
3941 Amine oxidase [flavin-containing] A MAOA 0.0018
474 Acetylcholinesterase ACHE 0.0016
872 Gamma-aminobutyric-acid receptor subunit alpha-1 GABRA1 0.0015
587 Serum albumin ALB 0.0014
198 Sodium channel protein type 10 subunit alpha SCN10A 0.0014
6106 Cytochrome P450 2C18 CYP2C18 0.0013
6147 Solute carrier family 22 member 3 SLC22A3 0.0012
1360 Sphingomyelin phosphodiesterase SMPD1 0.0012
6101 Dimethylaniline monooxygenase [N-oxide-forming] 3 FMO3 0.0012
6047 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A PDE1A 0.0012
6100 BDNF/NT-3 growth factors receptor NTRK2 0.0011
5692 Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1B PDE1B 0.0011
762 Voltage-dependent calcium channel subunit alpha-2/delta-1 CACNA2D1 0.0009
4110 Voltage-dependent L-type calcium channel subunit beta-2 CACNB2 0.0009
4115 Voltage-dependent L-type calcium channel subunit alpha-1D CACNA1D 0.0009
1618 High affinity nerve growth factor receptor NTRK1 0.0009
478 Voltage-dependent L-type calcium channel subunit alpha-1C CACNA1C 0.0008
1086 Potassium voltage-gated channel subfamily KQT member 2 KCNQ2 0.0008
164 Histamine H4 receptor HRH4 0.0008
734 D1 dopamine receptor-interacting protein calcyon CALY 0.0007
858 Potassium voltage-gated channel subfamily A member 1 KCNA1 0.0007
20 Prostaglandin G/H synthase 1 PTGS1 0.0006
193 Beta-1 adrenergic receptor ADRB1 0.0006
766 Beta-2 adrenergic receptor ADRB2 0.0006
6025 UDP-glucuronosyltransferase 1-4 UGT1A4 0.0006
467 Delta-type opioid receptor OPRD1 0.0005
696 Kappa-type opioid receptor OPRK1 0.0005
1898 Cytochrome P450 1B1 CYP1B1 0.0004
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