Tox | Related Drugs | BioActivity |

Stem definition	Drug id	CAS RN
	4302	596-51-0

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: sialanar NVA237 Seebri Breezhaler glycopyrronium bromide copyrrolate gastrodyn glycopyrrolate robanul glycopyrronium glycopyrrolate bromide glycopyrronium tosilate glycopyrronium tosilate hydrate	Glycopyrrolate is a long-acting muscarinic antagonist, which is often referred to as an anticholinergic. It has similar affinity to the subtypes of muscarinic receptors M1 to M5. In the airways, it exhibits pharmacological effects through inhibition of M3 receptor at the smooth muscle leading to bronchodilation. The competitive and reversible nature of antagonism was shown with human and animal origin receptors and isolated organ preparations. In preclinical in vitro as well as in vivo studies, prevention of methacholine and acetylcholine induced bronchoconstrictive effects was dose-dependent and lasted longer than 24 hours. The clinical relevance of these findings is unknown. The bronchodilation following inhalation of glycopyrrolate is predominantly a site-specific effect. Molecular weight: 318.44 Formula: C19H28NO3 CLOGP: 0.12 LIPINSKI: 0 HAC: 4 HDO: 1 TPSA: 46.53 ALOGS: -5.57 ROTB: 5 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

sialanar
NVA237
Seebri Breezhaler
glycopyrronium bromide
copyrrolate
gastrodyn
glycopyrrolate
robanul
glycopyrronium
glycopyrrolate bromide
glycopyrronium tosilate
glycopyrronium tosilate hydrate

Glycopyrrolate is a long-acting muscarinic antagonist, which is often referred to as an anticholinergic. It has similar affinity to the subtypes of muscarinic receptors M1 to M5. In the airways, it exhibits pharmacological effects through inhibition of M3 receptor at the smooth muscle leading to bronchodilation. The competitive and reversible nature of antagonism was shown with human and animal origin receptors and isolated organ preparations. In preclinical in vitro as well as in vivo studies, prevention of methacholine and acetylcholine induced bronchoconstrictive effects was dose-dependent and lasted longer than 24 hours. The clinical relevance of these findings is unknown. The bronchodilation following inhalation of glycopyrrolate is predominantly a site-specific effect.

Molecular weight: 318.44
Formula: C19H28NO3
CLOGP: 0.12
LIPINSKI: 0
HAC: 4
HDO: 1
TPSA: 46.53
ALOGS: -5.57
ROTB: 5

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
3	mg	O
0.30	mg	P
3	mg	R
44	mcg	Inhal.powder

ADMET properties:

Property	Value	Reference
BA (Bioavailability)	17 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	0.37 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	16.80 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	0.65 hours	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.48 %	Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
azlogd74	LogD at pH 7.4	-0.904		High	1
caco2-efflux	Caco-2 efflux ratio (BA/AB)	1.766		High	1
caco2-intrinsic-papp	Caco-2 intrinsic apparent permeability	0.368	10^-6 cm/s	High	1
dh-clint	Dog hepatocyte intrinsic clearance	2.547	uL/min/10^6 cells	High	1
dppb	Dog plasma protein binding (% unbound)	76.230	%	High	1
fcs-ppb	Fetal calf serum protein binding (% unbound)	66.250	%	High	1
herg	hERG pIC50	4.298	pIC50	High	1
hh-clint	Human hepatocyte intrinsic clearance	1.091	uL/min/10^6 cells	High	1
hlm-clint	Human liver microsomal intrinsic clearance	3.311	uL/min/mg protein	High	1
hppb	Human plasma protein binding (% unbound)	76.310	%	High	1
kinase-safety-class	ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAPK7,NTRK2,PDK1,PDK2,PDK4,PIK3CG,PRKDC,TEK,TGFBR1	22
kinase-selectivity-class	AXL,GRK2,PDK4	3
mdck-mdr1-bcrp-efflux	MDCK-MDR1-BCRP efflux ratio	1.125		High	1
mdck-mdr1-efflux	MDCK-MDR1 efflux ratio	0.798		High	1
mh-clint	Mouse hepatocyte intrinsic clearance	19.543		High	1
mppb	Mouse plasma protein binding (% unbound)	63.580		High	1
nih-mdck-mdr1-efflux	NIH MDCK-MDR1 efflux ratio	1.169		High	1
pfas-class	PFAS structural alert (1 = True, 0 = False)	0
pppb	Pig plasma protein binding (% unbound)	73.500	%	High	1
rat-kpuu-brain	Rat brain Kpuu	0.015	%	High	1
rh-clint	Rat hepatocyte intrinsic clearance	23.605	uL/min/10^6 cells	High	1
rh-fuinc	Rat hepatocyte fraction unbound in incubation	89.130	%	High	1
rppb	Rat plasma protein binding (% unbound)	68.730	%	High	1
solubility-dd	Solubility at pH 7.4 in DMSO	928.966	uM	High	1

Approvals:

Date	Agency	Company
Aug. 11, 1961	FDA	SHIONOGI INC
June 18, 2019	PMDA	AstraZeneca K.K.
Sept. 28, 2012	EMA	Novartis Europharm Limited

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Total lung capacity increased	566.07	17.72	148	21546	4873	90601880
Asthma-chronic obstructive pulmonary disease overlap syndrome	469.52	17.72	127	21567	4772	90601981
Wheezing	468.91	17.72	415	21279	237665	90369088
Bronchiectasis	445.01	17.72	176	21518	22154	90584599
Asthma	439.18	17.72	403	21291	241757	90364996
Nasal polyps	420.86	17.72	140	21554	10740	90596013
Obstructive airways disorder	396.62	17.72	169	21525	25700	90581053
Sarcoidosis	360.30	17.72	124	21570	10549	90596204
Chronic obstructive pulmonary disease	325.82	17.72	209	21485	73620	90533133
Rhinitis allergic	312.50	17.72	126	21568	16659	90590094
Lung neoplasm malignant	302.18	17.72	137	21557	24136	90582617
Cardiac murmur	295.95	17.72	124	21570	18070	90588683
Cough	260.39	17.72	377	21317	368585	90238168
Dyspnoea	231.26	17.72	590	21104	880365	89726388
Forced expiratory volume decreased	225.61	17.72	75	21619	5733	90601020
Jaundice cholestatic	224.21	17.72	86	21608	9957	90596796
Hypomania	223.30	17.72	83	21611	8814	90597939
Nasal congestion	199.69	17.72	163	21531	83251	90523502
Schizophrenia	197.75	17.72	88	21606	14826	90591927
Blood immunoglobulin E increased	187.40	17.72	61	21633	4364	90602389
Sputum discoloured	180.27	17.72	91	21603	20300	90586453
Productive cough	168.66	17.72	143	21551	76920	90529833
Malignant mediastinal neoplasm	165.88	17.72	43	21651	1365	90605388
Stress cardiomyopathy	149.34	17.72	70	21624	13285	90593468
Psychotic disorder	149.09	17.72	93	21601	31137	90575616
Full blood count abnormal	142.77	17.72	96	21598	36501	90570252
Respiration abnormal	142.07	17.72	58	21636	7905	90598848
Bronchial neoplasm	139.61	17.72	31	21663	499	90606254
Bronchial haemorrhage	133.17	17.72	31	21663	622	90606131
Sleep apnoea syndrome	130.40	17.72	86	21608	31661	90575092
Blood bilirubin increased	130.12	17.72	97	21597	43373	90563380
Nasal turbinate hypertrophy	122.57	17.72	31	21663	890	90605863
Endometrial ablation	119.16	17.72	31	21663	998	90605755
Chest discomfort	117.67	17.72	155	21539	138210	90468543
Bronchial disorder	115.50	17.72	33	21661	1517	90605236
Gastrooesophageal reflux disease	112.62	17.72	167	21527	166170	90440583
Pneumonia	108.54	17.72	367	21327	637692	89969061
Hyper IgE syndrome	108.43	17.72	25	21669	480	90606273
Hepatotoxicity	108.41	17.72	89	21605	45753	90561000
Glaucoma	107.19	17.72	65	21629	20690	90586063
Rhonchi	102.02	17.72	35	21659	2943	90603810
Cholelithiasis	97.92	17.72	89	21605	52417	90554336
Rhinorrhoea	97.75	17.72	113	21581	88203	90518550
Heart sounds	97.25	17.72	27	21667	1117	90605636
Alopecia	94.90	17.72	6	21688	495065	90111688
Prolonged expiration	94.73	17.72	27	21667	1230	90605523
Frustration tolerance decreased	93.29	17.72	43	21651	7853	90598900
Pain	91.01	17.72	64	21630	996277	89610476
Infusion related reaction	86.47	17.72	3	21691	416777	90189976
Restrictive pulmonary disease	85.77	17.72	29	21665	2333	90604420
Sleep disorder due to a general medical condition	83.74	17.72	76	21618	44662	90562091
Humidity intolerance	80.70	17.72	19	21675	401	90606352
Rhinitis	79.21	17.72	46	21648	13526	90593227
Peak expiratory flow rate decreased	72.69	17.72	19	21675	623	90606130
Dyspnoea exertional	69.31	17.72	86	21608	72202	90534551
Rales	67.72	17.72	44	21650	15783	90590970
Secretion discharge	67.55	17.72	44	21650	15852	90590901
Joint swelling	66.62	17.72	19	21675	503281	90103472
Rash	65.18	17.72	57	21637	796043	89810710
Granuloma	64.79	17.72	31	21663	6154	90600599
Systemic lupus erythematosus	64.76	17.72	6	21688	361890	90244863
Breath sounds abnormal	63.94	17.72	42	21652	15344	90591409
Oedema peripheral	63.19	17.72	169	21525	257746	90349007
Breast cancer recurrent	62.00	17.72	29	21665	5474	90601279
Middle insomnia	60.70	17.72	42	21652	16709	90590044
Depressive symptom	60.00	17.72	28	21666	5257	90601496
Oxygen saturation decreased	58.91	17.72	98	21596	107385	90499368
Affective disorder	58.01	17.72	31	21663	7762	90598991
Synovitis	55.09	17.72	7	21687	329745	90277008
Influenza	54.79	17.72	110	21584	139154	90467599
Pulmonary function test decreased	54.74	17.72	25	21669	4469	90602284
Drug intolerance	52.09	17.72	21	21673	447570	90159183
Treatment failure	51.88	17.72	6	21688	303922	90302831
Rheumatoid arthritis	51.19	17.72	12	21682	362602	90244151
Appetite disorder	50.78	17.72	30	21664	9103	90597650
Pulmonary congestion	50.75	17.72	40	21654	19393	90587360
Therapeutic product effect incomplete	49.44	17.72	129	21565	193767	90412986
Polycystic ovaries	49.27	17.72	25	21669	5629	90601124
Therapeutic product effect decreased	48.60	17.72	5	21689	277566	90329187
Seizure	47.90	17.72	110	21584	152519	90454234
Pulmonary oedema	47.32	17.72	66	21628	62014	90544739
Increased bronchial secretion	46.48	17.72	18	21676	2135	90604618
Lung diffusion test decreased	45.76	17.72	14	21680	817	90605936
Swelling	45.07	17.72	22	21672	419036	90187717
Forced vital capacity decreased	44.90	17.72	15	21679	1163	90605590
Sinus tachycardia	44.85	17.72	44	21650	28469	90578284
Impaired healing	44.34	17.72	3	21691	234196	90372557
Arthralgia	41.58	17.72	77	21617	778445	89828308
Blister	41.19	17.72	6	21688	254992	90351761
Acute pulmonary oedema	39.44	17.72	26	21668	9554	90597199
Choking	38.58	17.72	28	21666	12005	90594748
Diarrhoea	37.95	17.72	108	21586	939082	89667671
Lower respiratory tract infection	37.92	17.72	139	21555	250520	90356233
Helicobacter infection	37.43	17.72	5	21689	226845	90379908
Pulmonary thrombosis	36.56	17.72	25	21669	9757	90596996
Bronchial obstruction	36.03	17.72	14	21680	1675	90605078
Dyslipidaemia	35.82	17.72	25	21669	10082	90596671
Nail dystrophy	35.66	17.72	13	21681	1305	90605448
Tachycardia	35.27	17.72	100	21594	157573	90449180
Lung neoplasm	34.53	17.72	21	21673	6714	90600039
Dystonia	34.29	17.72	30	21664	16789	90589964
Angioplasty	34.22	17.72	13	21681	1464	90605289
Restless legs syndrome	34.09	17.72	34	21660	22436	90584317
Coronary artery disease	33.83	17.72	41	21653	33582	90573171
Hypoventilation	33.71	17.72	19	21675	5277	90601476
Irritable bowel syndrome	33.23	17.72	5	21689	207443	90399310
Laryngitis fungal	33.04	17.72	8	21686	191	90606562
Blood pressure systolic increased	33.03	17.72	54	21640	58291	90548462
Bronchial wall thickening	32.89	17.72	14	21680	2117	90604636
Brain injury	31.85	17.72	21	21673	7717	90599036
Stomatitis	31.75	17.72	13	21681	274685	90332068
Ankle fracture	31.23	17.72	31	21663	20339	90586414
Nasal inflammation	31.03	17.72	10	21684	692	90606061
Bronchospasm paradoxical	30.84	17.72	7	21687	125	90606628
Blood test abnormal	30.50	17.72	31	21663	20921	90585832
Abdominal discomfort	30.35	17.72	42	21652	477286	90129467
Body temperature abnormal	30.14	17.72	14	21680	2601	90604152
Loss of personal independence in daily activities	30.12	17.72	86	21608	136019	90470734
Laryngospasm	29.81	17.72	15	21679	3318	90603435
Staphylococcal scalded skin syndrome	29.59	17.72	7	21687	151	90606602
Sneezing	29.36	17.72	36	21658	29833	90576920
Oropharyngitis fungal	29.13	17.72	6	21688	66	90606687
Staphylococcus test positive	28.78	17.72	16	21678	4329	90602424
Urinary retention	28.57	17.72	40	21654	37704	90569049
Axillary pain	28.54	17.72	13	21681	2308	90604445
Paranoia	28.30	17.72	24	21670	12884	90593869
Respiratory rate increased	27.64	17.72	26	21668	15975	90590778
Granulomatosis with polyangiitis	27.21	17.72	13	21681	2572	90604181
Discomfort	27.13	17.72	16	21678	274319	90332434
Dysphonia	26.20	17.72	51	21643	63033	90543720
Apnoea	25.93	17.72	20	21674	9394	90597359
Brachial plexopathy	25.91	17.72	7	21687	261	90606492
Abscess	25.78	17.72	27	21667	18864	90587889
C-reactive protein increased	25.58	17.72	6	21688	181383	90425370
Peripheral vascular disorder	25.38	17.72	17	21677	6414	90600339
Anaphylactic reaction	25.18	17.72	61	21633	87463	90519290
Maternal exposure during delivery	25.03	17.72	14	21680	3832	90602921
Vulvovaginal candidiasis	24.85	17.72	14	21680	3886	90602867
Musculoskeletal stiffness	24.46	17.72	21	21673	296511	90310242
Condition aggravated	24.22	17.72	233	21461	595312	90011441
General physical health deterioration	23.83	17.72	30	21664	355085	90251668
Diplegia	23.79	17.72	10	21684	1465	90605288
Respiratory symptom	23.72	17.72	14	21680	4238	90602515
Flank pain	23.64	17.72	26	21668	19196	90587557
Confusional state	23.53	17.72	35	21659	386170	90220583
Musculoskeletal pain	23.49	17.72	6	21688	171245	90435508
Sleep disorder	23.48	17.72	9	21685	198021	90408732
Opisthotonus	23.37	17.72	7	21687	380	90606373
Catheter site haemorrhage	22.92	17.72	13	21681	3655	90603098
Drug ineffective	22.81	17.72	217	21477	1384081	89222672
Crepitations	22.64	17.72	18	21676	8834	90597919
Depression	22.63	17.72	136	21558	300465	90306288
Pancreatic mass	22.21	17.72	9	21685	1202	90605551
Drug hypersensitivity	22.01	17.72	49	21645	463560	90143193
Cerebral thrombosis	21.86	17.72	10	21684	1793	90604960
Smoke sensitivity	21.52	17.72	7	21687	499	90606254
Bursitis	21.48	17.72	3	21691	131651	90475102
Osteoarthritis	21.44	17.72	10	21684	195720	90411033
Ill-defined disorder	20.95	17.72	9	21685	184882	90421871
Sleep disorder due to general medical condition, insomnia type	20.84	17.72	3	21691	128691	90478062
Blood cholesterol increased	20.75	17.72	12	21682	208000	90398753
Respiratory disorder	20.63	17.72	47	21647	64769	90541984
Muscle disorder	20.47	17.72	14	21680	5465	90601288
Infective exacerbation of chronic obstructive airways disease	20.44	17.72	9	21685	1477	90605276
Appendicitis	20.36	17.72	18	21676	10213	90596540
Blood disorder	20.26	17.72	16	21678	7774	90598979
Seasonal allergy	19.89	17.72	26	21668	22957	90583796
Neutropenia	19.70	17.72	15	21679	224889	90381864
Abdominal pain	19.46	17.72	41	21653	395680	90211073
Respiratory rate decreased	19.35	17.72	12	21682	3971	90602782
Respiratory failure	19.01	17.72	67	21627	118351	90488402
Wound	18.89	17.72	27	21667	302953	90303800
Weight decreased	18.69	17.72	155	21539	379755	90226998
Stress	18.56	17.72	52	21642	81343	90525410
Adverse event	18.41	17.72	3	21691	117415	90489338
Conjunctivitis	18.30	17.72	27	21667	26679	90580074
Heart rate increased	18.23	17.72	64	21630	112838	90493915
Mite allergy	18.05	17.72	7	21687	833	90605920
Peripheral swelling	17.75	17.72	46	21648	413060	90193693

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Asthma	252.37	17.53	183	12748	62131	42546273
Wheezing	208.45	17.53	155	12776	54626	42553778
Productive cough	174.31	17.53	136	12795	51431	42556973
Dyspnoea	156.19	17.53	384	12547	442237	42166167
Obstructive airways disorder	128.97	17.53	85	12846	24674	42583730
Full blood count abnormal	125.91	17.53	90	12841	29786	42578618
Sputum discoloured	118.52	17.53	59	12872	10073	42598331
Chronic obstructive pulmonary disease	107.09	17.53	113	12818	63001	42545403
Cough	103.66	17.53	190	12741	177913	42430491
Asthma-chronic obstructive pulmonary disease overlap syndrome	103.37	17.53	32	12899	1527	42606877
Pulmonary function test abnormal	89.90	17.53	33	12898	2661	42605743
Gastrooesophageal reflux disease	86.09	17.53	86	12845	44937	42563467
Chest discomfort	84.06	17.53	100	12831	63516	42544888
Therapeutic product effect incomplete	83.20	17.53	105	12826	70834	42537570
Adjustment disorder	82.51	17.53	26	12905	1316	42607088
Eosinophil count increased	76.38	17.53	45	12886	10718	42597686
Sleep disorder due to a general medical condition	72.17	17.53	52	12879	17401	42591003
Rhinitis perennial	67.50	17.53	15	12916	188	42608216
Dyspnoea exertional	64.86	17.53	78	12853	50070	42558334
Tachycardia	62.70	17.53	111	12820	100976	42507428
Bronchial hyperreactivity	62.04	17.53	23	12908	1906	42606498
Eosinophilic granulomatosis with polyangiitis	60.99	17.53	36	12895	8602	42599802
Forced expiratory volume decreased	59.71	17.53	34	12897	7596	42600808
Blood immunoglobulin E increased	57.36	17.53	26	12905	3599	42604805
Respiratory disorder	47.46	17.53	45	12886	22040	42586364
Loss of personal independence in daily activities	46.50	17.53	66	12865	49750	42558654
Prolonged expiration	46.02	17.53	12	12919	305	42608099
Serotonin syndrome	45.07	17.53	47	12884	25798	42582606
Angle closure glaucoma	42.13	17.53	15	12916	1107	42607297
Dehiscence	41.73	17.53	13	12918	633	42607771
Upper respiratory tract infection	41.03	17.53	57	12874	42116	42566288
Rhinitis allergic	40.90	17.53	21	12910	3821	42604583
Smoke sensitivity	40.53	17.53	10	12921	202	42608202
Drug dependence	40.48	17.53	47	12884	29047	42579357
Ischaemic cardiomyopathy	40.41	17.53	25	12906	6497	42601907
Heat stroke	38.55	17.53	14	12917	1094	42607310
Perfume sensitivity	37.73	17.53	9	12922	157	42608247
Emphysema	37.30	17.53	30	12901	11805	42596599
Salivary hypersecretion	37.20	17.53	29	12902	10914	42597490
Breath sounds abnormal	36.74	17.53	30	12901	12063	42596341
Vasculitis	36.73	17.53	36	12895	18358	42590046
Sputum purulent	36.43	17.53	12	12919	700	42607704
Dyspnoea at rest	36.14	17.53	20	12911	4229	42604175
Precancerous condition	34.79	17.53	8	12923	118	42608286
Haemoptysis	34.30	17.53	55	12876	46112	42562292
Orthostatic hypertension	32.40	17.53	10	12921	472	42607932
Discomfort	32.21	17.53	39	12892	25180	42583224
Cardiomyopathy	31.82	17.53	34	12897	19176	42589228
Middle insomnia	31.60	17.53	23	12908	7810	42600594
Hypercholesterolaemia	31.13	17.53	28	12903	12821	42595583
Drug intolerance	30.40	17.53	72	12859	80352	42528052
Saliva altered	30.32	17.53	8	12923	213	42608191
Dyspnoea paroxysmal nocturnal	30.08	17.53	13	12918	1607	42606797
Bradycardia	29.61	17.53	74	12857	85410	42522994
Umbilical hernia	29.06	17.53	19	12912	5428	42602976
Obesity	28.81	17.53	30	12901	16429	42591975
Disease recurrence	28.69	17.53	40	12891	29638	42578766
Off label use	26.60	17.53	102	12829	638233	41970171
Accelerated idioventricular rhythm	26.48	17.53	7	12924	188	42608216
Cardiorenal syndrome	26.36	17.53	10	12921	883	42607521
Paraesthesia	24.82	17.53	63	12868	73396	42535008
Carboxyhaemoglobin increased	23.18	17.53	5	12926	54	42608350
Pseudomonal sepsis	23.11	17.53	15	12916	4234	42604170
Parkinsonian rest tremor	22.81	17.53	7	12924	324	42608080
Occupational exposure to air contaminants	22.52	17.53	6	12925	166	42608238
Forced vital capacity decreased	22.36	17.53	9	12922	931	42607473
Physical deconditioning	22.34	17.53	12	12919	2393	42606011
Hypoxia	21.67	17.53	58	12873	69728	42538676
Infective exacerbation of chronic obstructive airways disease	21.31	17.53	11	12920	2022	42606382
Mydriasis	21.02	17.53	19	12912	8751	42599653
Volume blood decreased	20.47	17.53	6	12925	237	42608167
Expiratory reserve volume decreased	19.61	17.53	5	12926	116	42608288
Lung diffusion test decreased	19.48	17.53	8	12923	871	42607533
Pulmonary mass	18.91	17.53	24	12907	16241	42592163
Laryngospasm	18.69	17.53	10	12921	1978	42606426
Proctitis bacterial	18.61	17.53	5	12926	143	42608261
Bronchiectasis	18.49	17.53	25	12906	17994	42590410
Appendicitis perforated	18.15	17.53	10	12921	2096	42606308
Nasal congestion	17.74	17.53	32	12899	29469	42578935
Orthopnoea	17.64	17.53	14	12917	5403	42603001

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Asthma	600.94	15.70	531	31584	249760	110307424
Wheezing	562.45	15.70	516	31599	254714	110302470
Total lung capacity increased	539.54	15.70	149	31966	4963	110552221
Asthma-chronic obstructive pulmonary disease overlap syndrome	520.95	15.70	152	31963	6192	110550992
Obstructive airways disorder	458.01	15.70	237	31878	45912	110511272
Chronic obstructive pulmonary disease	393.60	15.70	294	31821	108864	110448320
Bronchiectasis	375.31	15.70	192	31923	36301	110520883
Nasal polyps	353.48	15.70	136	31979	13064	110544120
Rhinitis allergic	346.29	15.70	146	31969	17776	110539408
Sarcoidosis	327.57	15.70	127	31988	12452	110544732
Cough	326.77	15.70	524	31591	461117	110096067
Dyspnoea	318.41	15.70	866	31249	1106006	109451178
Productive cough	307.10	15.70	259	31856	114046	110443138
Sputum discoloured	281.44	15.70	145	31970	27800	110529384
Forced expiratory volume decreased	243.44	15.70	104	32011	13072	110544112
Lung neoplasm malignant	241.99	15.70	140	31975	33702	110523482
Cardiac murmur	239.99	15.70	125	31990	24503	110532681
Full blood count abnormal	224.56	15.70	161	31954	55891	110501293
Blood immunoglobulin E increased	210.75	15.70	80	32035	7402	110549782
Hypomania	203.31	15.70	85	32030	10125	110547059
Nasal congestion	197.23	15.70	189	31926	98093	110459091
Gastrooesophageal reflux disease	194.16	15.70	250	31865	179726	110377458
Jaundice cholestatic	189.28	15.70	90	32025	14518	110542666
Chest discomfort	154.76	15.70	220	31895	173628	110383556
Malignant mediastinal neoplasm	153.88	15.70	42	32073	1336	110555848
Schizophrenia	152.59	15.70	89	32026	21737	110535447
Bronchial neoplasm	133.29	15.70	31	32084	505	110556679
Prolonged expiration	130.99	15.70	38	32077	1514	110555670
Respiration abnormal	125.75	15.70	60	32055	9749	110547435
Stress cardiomyopathy	122.66	15.70	69	32046	15737	110541447
Nasal turbinate hypertrophy	119.30	15.70	31	32084	813	110556371
Sleep apnoea syndrome	117.54	15.70	96	32019	40351	110516833
Dyspnoea exertional	115.98	15.70	147	31968	103913	110453271
Endometrial ablation	115.73	15.70	31	32084	917	110556267
Bronchial haemorrhage	104.06	15.70	31	32084	1356	110555828
Sleep disorder due to a general medical condition	102.19	15.70	99	32016	52013	110505171
Rhinorrhoea	101.92	15.70	137	31978	102529	110454655
Glaucoma	100.19	15.70	69	32046	22448	110534736
Psychotic disorder	98.44	15.70	96	32019	50841	110506343
Breath sounds abnormal	97.20	15.70	71	32044	25333	110531851
Hyper IgE syndrome	96.20	15.70	25	32090	656	110556528
Bronchial disorder	94.05	15.70	34	32081	2742	110554442
Pneumonia	93.69	15.70	501	31614	876213	109680971
Heart sounds	92.11	15.70	27	32088	1116	110556068
Tachycardia	89.50	15.70	201	31914	226444	110330740
Rhonchi	87.89	15.70	37	32078	4481	110552703
Blood bilirubin increased	87.31	15.70	109	32006	75863	110481321
Pain	86.59	15.70	90	32025	954865	109602319
Restrictive pulmonary disease	85.17	15.70	33	32082	3226	110553958
Middle insomnia	84.62	15.70	60	32055	20442	110536742
Cholelithiasis	84.34	15.70	98	32017	63324	110493860
Frustration tolerance decreased	81.29	15.70	43	32072	8688	110548496
Therapeutic product effect incomplete	81.22	15.70	192	31923	223613	110333571
Pulmonary function test abnormal	77.85	15.70	35	32080	4965	110552219
Alopecia	77.41	15.70	8	32107	364745	110192439
Infusion related reaction	76.81	15.70	10	32105	381152	110176032
Hepatotoxicity	76.12	15.70	93	32022	63307	110493877
Humidity intolerance	73.76	15.70	19	32096	481	110556703
Joint swelling	69.73	15.70	21	32094	442824	110114360
Rash	68.21	15.70	83	32032	820881	109736303
Eosinophilic granulomatosis with polyangiitis	67.95	15.70	41	32074	10645	110546539
Peak expiratory flow rate decreased	67.42	15.70	19	32096	681	110556503
Forced vital capacity decreased	66.26	15.70	24	32091	1946	110555238
Rhinitis perennial	66.03	15.70	15	32100	219	110556965
Oedema peripheral	65.39	15.70	227	31888	328433	110228751
Eosinophil count increased	61.21	15.70	50	32065	21008	110536176
Lung diffusion test decreased	58.69	15.70	21	32094	1644	110555540
Contraindicated product administered	56.60	15.70	4	32111	248263	110308921
Bronchial hyperreactivity	55.79	15.70	25	32090	3519	110553665
Synovitis	55.66	15.70	7	32108	274085	110283099
Secretion discharge	54.54	15.70	46	32069	20198	110536986
Arthropathy	54.53	15.70	9	32106	287513	110269671
Pulmonary function test decreased	54.34	15.70	33	32082	8667	110548517
Treatment failure	54.12	15.70	8	32107	277226	110279958
Smoke sensitivity	53.68	15.70	16	32099	701	110556483
Systemic lupus erythematosus	52.87	15.70	6	32109	254332	110302852
Pericarditis	51.52	15.70	3	32112	219111	110338073
Hypoventilation	51.37	15.70	31	32084	8050	110549134
Rhinitis	50.25	15.70	46	32069	22499	110534685
Polycystic ovaries	48.59	15.70	25	32090	4771	110552413
Rales	48.49	15.70	47	32068	24692	110532492
Rheumatoid arthritis	47.51	15.70	14	32101	299599	110257585
Loss of personal independence in daily activities	47.29	15.70	122	31993	149898	110407286
Granuloma	46.80	15.70	31	32084	9459	110547725
Respiratory disorder	46.14	15.70	78	32037	71304	110485880
Swelling	44.79	15.70	23	32092	351018	110206166
Salivary hypersecretion	43.70	15.70	38	32077	17383	110539801
Appetite disorder	43.60	15.70	30	32085	9739	110547445
Laryngospasm	43.48	15.70	23	32092	4645	110552539
Depressive symptom	42.74	15.70	28	32087	8386	110548798
Impaired healing	42.53	15.70	4	32111	196713	110360471
Affective disorder	42.06	15.70	31	32084	11210	110545974
Oxygen saturation decreased	41.82	15.70	120	31995	156862	110400322
Therapeutic product effect decreased	41.41	15.70	10	32105	244306	110312878
Lower respiratory tract infection	40.81	15.70	159	31956	242947	110314237
Pulmonary oedema	40.50	15.70	90	32025	100569	110456615
Orthostatic hypertension	40.08	15.70	14	32101	1021	110556163
Influenza	40.05	15.70	124	31991	168977	110388207
Choking	40.02	15.70	34	32081	15076	110542108
Perfume sensitivity	39.36	15.70	14	32101	1077	110556107
Ischaemic cardiomyopathy	39.09	15.70	26	32089	7985	110549199
Angle closure glaucoma	37.66	15.70	19	32096	3480	110553704
Upper respiratory tract infection	37.54	15.70	103	32012	131225	110425959
Seizure	37.40	15.70	145	31970	221040	110336144
Diarrhoea	36.94	15.70	188	31927	1139317	109417867
Sneezing	36.91	15.70	46	32069	31938	110525246
Pulmonary congestion	36.48	15.70	45	32070	30921	110526263
Toxicity to various agents	36.34	15.70	52	32063	480503	110076681
Dehiscence	36.20	15.70	12	32103	746	110556438
Sinus tachycardia	36.18	15.70	54	32061	44439	110512745
Depressed mood	36.10	15.70	64	32051	60745	110496439
Seasonal allergy	35.92	15.70	36	32079	19686	110537498
Arthralgia	35.08	15.70	113	32002	779519	109777665
Heat stroke	34.83	15.70	15	32100	1920	110555264
Apnoea	34.71	15.70	30	32085	13609	110543575
Nail dystrophy	34.11	15.70	13	32102	1215	110555969
Irritable bowel syndrome	33.80	15.70	4	32111	164211	110392973
Helicobacter infection	33.80	15.70	6	32109	181871	110375313
Respiratory rate increased	33.74	15.70	39	32076	25044	110532140
Blood pressure systolic increased	33.16	15.70	74	32041	82917	110474267
C-reactive protein increased	33.08	15.70	11	32104	217908	110339276
Adjustment disorder	32.15	15.70	26	32089	10769	110546415
Lung neoplasm	31.86	15.70	23	32092	8053	110549131
Angioplasty	31.33	15.70	14	32101	1957	110555227
Dyspnoea paroxysmal nocturnal	31.14	15.70	15	32100	2487	110554697
Blister	30.36	15.70	14	32101	227362	110329822
Drug dependence	30.15	15.70	53	32062	49967	110507217
Umbilical hernia	30.02	15.70	21	32094	7001	110550183
Increased bronchial secretion	29.99	15.70	17	32098	3931	110553253
Pancytopenia	29.42	15.70	12	32103	209601	110347583
Nasal inflammation	29.13	15.70	11	32104	1002	110556182
Bronchitis	29.07	15.70	106	32009	156926	110400258
Ankle fracture	28.67	15.70	32	32083	19787	110537397
Abdominal discomfort	28.42	15.70	44	32071	393814	110163370
Bradycardia	27.97	15.70	104	32011	155413	110401771
Intentional product misuse	27.95	15.70	3	32112	132901	110424283
Abscess	27.76	15.70	37	32078	27432	110529752
Axillary pain	27.71	15.70	14	32101	2572	110554612
Stomatitis	27.30	15.70	23	32092	270219	110286965
Acute pulmonary oedema	27.30	15.70	29	32086	16967	110540217
Drug hypersensitivity	27.15	15.70	57	32058	454033	110103151
Musculoskeletal stiffness	26.84	15.70	25	32090	279797	110277387
Pulmonary thrombosis	26.53	15.70	26	32089	13837	110543347
Aphonia	26.27	15.70	25	32090	12835	110544349
Restless legs syndrome	26.17	15.70	34	32081	24592	110532592
Neutropenia	25.94	15.70	43	32072	374577	110182607
Bronchospasm paradoxical	25.91	15.70	7	32108	214	110556970
Off label use	25.56	15.70	296	31819	1499889	109057295
Sputum purulent	25.52	15.70	12	32103	1886	110555298
Body temperature abnormal	25.28	15.70	14	32101	3095	110554089
Osteoarthritis	24.76	15.70	11	32104	182612	110374572
Dyspnoea at rest	24.64	15.70	20	32095	8326	110548858
Vulvovaginal candidiasis	24.56	15.70	14	32101	3271	110553913
Mydriasis	24.19	15.70	31	32084	22126	110535058
Dysphonia	24.17	15.70	62	32053	75867	110481317
Inflammation	24.13	15.70	13	32102	193225	110363959
Accelerated idioventricular rhythm	23.98	15.70	7	32108	285	110556899
Brachial plexopathy	23.66	15.70	7	32108	299	110556885
Dyslipidaemia	23.47	15.70	26	32089	15939	110541245
Dystonia	23.42	15.70	33	32082	25772	110531412
Saliva altered	23.36	15.70	8	32107	550	110556634
Flank pain	23.14	15.70	31	32084	23099	110534085
Precancerous condition	23.01	15.70	8	32107	575	110556609
Disease recurrence	22.94	15.70	53	32062	60731	110496453
Serotonin syndrome	22.79	15.70	52	32063	59101	110498083
Occupational exposure to air contaminants	22.78	15.70	6	32109	166	110557018
Hypoxia	22.77	15.70	86	32029	129429	110427755
Anaphylactic reaction	22.73	15.70	79	32036	114221	110442963
Bronchial obstruction	22.70	15.70	13	32102	3066	110554118
White blood cell count decreased	22.59	15.70	20	32095	229370	110327814
Haemoptysis	22.44	15.70	58	32057	71296	110485888
Infective exacerbation of chronic obstructive airways disease	22.27	15.70	13	32102	3177	110554007
Laryngitis fungal	22.19	15.70	6	32109	184	110557000
Cardiomyopathy	22.15	15.70	37	32078	33488	110523696
Liver injury	22.12	15.70	8	32107	150405	110406779
Ill-defined disorder	21.98	15.70	9	32106	156844	110400340
Liver disorder	21.90	15.70	7	32108	142236	110414948
Platelet count decreased	21.62	15.70	21	32094	230422	110326762
Adverse event	21.55	15.70	3	32112	108806	110448378
Maternal exposure during delivery	20.93	15.70	13	32102	3552	110553632
Blood test abnormal	20.88	15.70	33	32082	28521	110528663
Peripheral swelling	20.72	15.70	55	32060	403979	110153205
Choking sensation	20.69	15.70	14	32101	4422	110552762
Opisthotonus	20.68	15.70	8	32107	778	110556406
Decreased appetite	20.65	15.70	70	32045	475776	110081408
Sinus operation	20.38	15.70	12	32103	2979	110554205
Vasculitis	20.32	15.70	37	32078	35836	110521348
Urinary retention	20.25	15.70	55	32060	69628	110487556
Respiratory failure	20.15	15.70	119	31996	215213	110341971
Crepitations	20.14	15.70	20	32095	10815	110546369
Cerebral thrombosis	19.84	15.70	11	32104	2437	110554747
Pancreatic mass	19.75	15.70	10	32105	1845	110555339
Staphylococcal scalded skin syndrome	19.69	15.70	7	32108	538	110556646
Intentional overdose	19.56	15.70	7	32108	132494	110424690
Respiratory acidosis	19.44	15.70	22	32093	13804	110543380
Cardiorenal syndrome	19.44	15.70	10	32105	1908	110555276
Acute kidney injury	19.31	15.70	107	32008	635323	109921861
Drug abuse	19.30	15.70	14	32101	177397	110379787
Cerebrovascular accident	18.83	15.70	15	32100	181269	110375915
Proctitis bacterial	18.83	15.70	5	32110	143	110557041
Joint range of motion decreased	18.75	15.70	6	32109	121826	110435358
Hypotonia	18.73	15.70	23	32092	15722	110541462
Vital capacity decreased	18.70	15.70	10	32105	2063	110555121
Anaesthetic complication neurological	18.57	15.70	8	32107	1025	110556159
Physical deconditioning	18.53	15.70	12	32103	3525	110553659
Fatigue	18.38	15.70	246	31869	1215712	109341472
Staphylococcus test positive	18.33	15.70	16	32099	7354	110549830
Drug-induced liver injury	18.32	15.70	6	32109	120061	110437123
Peripheral vascular disorder	18.15	15.70	17	32098	8559	110548625
Fibromyalgia	17.93	15.70	14	32101	170895	110386289
Extrapyramidal disorder	17.93	15.70	31	32084	28836	110528348
Diplegia	17.81	15.70	10	32105	2271	110554913
Muscle disorder	17.64	15.70	15	32100	6657	110550527
Sleep disorder	17.61	15.70	19	32096	198625	110358559
Carboxyhaemoglobin increased	17.38	15.70	4	32111	62	110557122
Catheter site haemorrhage	17.17	15.70	14	32101	5866	110551318
Upper airway obstruction	17.13	15.70	9	32106	1793	110555391
Drug ineffective	16.55	15.70	327	31788	1520213	109036971
Brain injury	16.54	15.70	20	32095	13456	110543728
Respiratory symptom	16.45	15.70	21	32094	14924	110542260
Anticholinergic syndrome	16.45	15.70	12	32103	4268	110552916
Cellulitis	16.44	15.70	8	32107	126008	110431176
Granulomatosis with polyangiitis	16.24	15.70	11	32104	3479	110553705
Emphysema	16.09	15.70	24	32091	19732	110537452
Suicide attempt	16.07	15.70	5	32110	103389	110453795
Blood cholesterol increased	16.02	15.70	18	32097	184767	110372417
Pain in extremity	15.92	15.70	80	32035	487038	110070146
Abdominal pain	15.78	15.70	86	32029	512903	110044281
Pulmonary mass	15.73	15.70	34	32081	37267	110519917

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	A03AB02	ALIMENTARY TRACT AND METABOLISM DRUGS FOR FUNCTIONAL GASTROINTESTINAL DISORDERS DRUGS FOR FUNCTIONAL GASTROINTESTINAL DISORDERS Synthetic anticholinergics, quaternary ammonium compounds
ATC	A03CA05	ALIMENTARY TRACT AND METABOLISM DRUGS FOR FUNCTIONAL GASTROINTESTINAL DISORDERS ANTISPASMODICS IN COMBINATION WITH PSYCHOLEPTICS Synthetic anticholinergic agents in combination with psycholeptics
ATC	D11AA01	DERMATOLOGICALS OTHER DERMATOLOGICAL PREPARATIONS OTHER DERMATOLOGICAL PREPARATIONS Antihidrotics
ATC	R03AL04	RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES ADRENERGICS, INHALANTS Adrenergics in combination with anticholinergics incl. triple combinations with corticosteroids
ATC	R03AL07	RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES ADRENERGICS, INHALANTS Adrenergics in combination with anticholinergics incl. triple combinations with corticosteroids
ATC	R03AL09	RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES ADRENERGICS, INHALANTS Adrenergics in combination with anticholinergics incl. triple combinations with corticosteroids
ATC	R03AL11	RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES ADRENERGICS, INHALANTS Adrenergics in combination with anticholinergics incl. triple combinations with corticosteroids
ATC	R03AL12	RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES ADRENERGICS, INHALANTS Adrenergics in combination with anticholinergics incl. triple combinations with corticosteroids
ATC	R03BB06	RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES OTHER DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES, INHALANTS Anticholinergics
FDA MoA	N0000000125	Cholinergic Muscarinic Antagonists
FDA MoA	N0000175370	Cholinergic Antagonists
FDA EPC	N0000175574	Anticholinergic
MeSH PA	D000759	Adjuvants, Anesthesia
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018678	Cholinergic Agents
MeSH PA	D018680	Cholinergic Antagonists
MeSH PA	D018727	Muscarinic Antagonists
FDA EPC	N0000175700	Cholinergic Muscarinic Antagonist
CHEBI has role	CHEBI:35469	antidepressant
CHEBI has role	CHEBI:65023	anti-asthmatic agent
CHEBI has role	CHEBI:231911	renoprotective agent
CHEBI has role	CHEBI:22587	antiviral agent

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A03AB Synthetic anticholinergics, quaternary ammonium compounds 19 drugs

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Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Peptic ulcer	indication	13200003	DOID:750
Chronic obstructive lung disease	indication	13645005	DOID:3083
General anesthesia	indication	50697003
Excessive salivation	indication	53827007
Hyperhidrosis of axilla	indication	303089000
Vagal Reflex Bradycardia	indication
Irritable bowel syndrome	off-label use	10743008	DOID:9778
Diarrhea	off-label use	62315008
Brain damage	contraindication	2470005
Tachyarrhythmia	contraindication	6285003
Suicidal thoughts	contraindication	6471006
Urinary tract obstruction	contraindication	7163005	DOID:5200
Alcoholism	contraindication	7200002
Hyperammonemia	contraindication	9360008
Hepatic encephalopathy	contraindication	13920009	DOID:13413
Severe chronic ulcerative colitis	contraindication	14311001
Toxic megacolon	contraindication	28536002	DOID:1770
Atony of colon	contraindication	29479008
Hyperthyroidism	contraindication	34486009	DOID:7998
Depressive disorder	contraindication	35489007
Hypertensive disorder	contraindication	38341003	DOID:10763
Complete trisomy 21 syndrome	contraindication	41040004	DOID:14250
Achalasia of esophagus	contraindication	45564002	DOID:9164
Chronic heart failure	contraindication	48447003
Paralytic ileus	contraindication	55525008	DOID:8442
Peptic reflux disease	contraindication	57643001
Hepatic failure	contraindication	59927004
Ulcerative colitis	contraindication	64766004	DOID:8577
Poisoning by phenobarbital	contraindication	64921004
Drug AND/OR toxin-induced diarrhea	contraindication	65979008
Substance abuse	contraindication	66214007
Hepatic coma	contraindication	72836002	DOID:12550
Sleep apnea	contraindication	73430006	DOID:0050847
Spastic paralysis	contraindication	78403003
Disturbance of salivary secretion	contraindication	78948009
Hiatal hernia	contraindication	84089009	DOID:12642
Kidney disease	contraindication	90708001	DOID:557
Myasthenia gravis	contraindication	91637004	DOID:437
Gastrointestinal obstruction	contraindication	126765001
Autonomic dysreflexia	contraindication	129618003
Bleeding	contraindication	131148009
Myocardial dysfunction	contraindication	233928007
Disease of liver	contraindication	235856003	DOID:409
Bladder outflow obstruction	contraindication	236645006
Pyloric obstruction	contraindication	244815007
Benign prostatic hyperplasia	contraindication	266569009
Dyspnea	contraindication	267036007
Retention of urine	contraindication	267064002
Anemia	contraindication	271737000	DOID:2355
Drowsy	contraindication	271782001
Pregnancy, function	contraindication	289908002
Thrombocytopenic disorder	contraindication	302215000	DOID:1588
Neutropenic disorder	contraindication	303011007	DOID:1227
Angle-closure glaucoma	contraindication	392291006	DOID:13550
Gastric ulcer	contraindication	397825006	DOID:10808
Breastfeeding (mother)	contraindication	413712001
Chronic lung disease	contraindication	413839001
Disorder of coronary artery	contraindication	414024009
Porphyria	contraindication	418470004

🐶 Veterinary Drug Use

Species	Use	Relation
Cats	Preanesthesia	Indication
Dogs	Preanesthesia	Indication

🐶 Veterinary products

Product	Applicant	Ingredients
Robinul-V Injectable	Zoetis Inc.	1
Glycopyrrolate Injectable, Robinul-V	Cronus Pharma Specialities India Private Limited	1

Acid dissociation constants calculated using MoKa v3.0.0