loratadine Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
histamine-H1 receptor antagonists, tricyclic compounds	1605	79794-75-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: loratadine claritin loracert loradex loratidine loratyne	A second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (HISTAMINE H1 ANTAGONISTS) it lacks central nervous system depressing effects such as drowsiness. Molecular weight: 382.89 Formula: C22H23ClN2O2 CLOGP: 5.05 LIPINSKI: 1 HAC: 4 HDO: 0 TPSA: 42.43 ALOGS: -4.46 ROTB: 2 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

loratadine
claritin
loracert
loradex
loratidine
loratyne

A second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (HISTAMINE H1 ANTAGONISTS) it lacks central nervous system depressing effects such as drowsiness.

Molecular weight: 382.89
Formula: C22H23ClN2O2
CLOGP: 5.05
LIPINSKI: 1
HAC: 4
HDO: 0
TPSA: 42.43
ALOGS: -4.46
ROTB: 2

Status: OFP

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

Drug dosage:

Dose	Unit	Route
10	mg	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	0.01 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	5 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.44 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	40 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

Date	Agency	Company	Orphan
April 12, 1993	FDA	BAYER HEALTHCARE LLC

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
Extra dose administered	363.22	9.83	169	75093	4538	46606262
Accidental exposure to product by child	187.69	9.83	70	75192	1053	46609747
Gastrooesophageal reflux disease	130.54	9.83	336	74926	74008	46536792
Failure of child resistant product closure	117.36	9.83	23	75239	9	46610791
Drug ineffective	103.28	9.83	656	74606	677182	45933618
Rheumatoid arthritis	102.19	9.83	143	75119	240072	46370728
Pneumonia aspiration	98.24	9.83	180	75082	31425	46579375
Urticaria	96.38	9.83	411	74851	117481	46493319
Contraindicated product administered	86.15	9.83	13	75249	79934	46530866
Toxicity to various agents	74.21	9.83	143	75119	211623	46399177
Acute kidney injury	69.71	9.83	175	75087	235680	46375120
Sinusitis	69.37	9.83	401	74861	129367	46481433
Drug intolerance	69.24	9.83	81	75181	146968	46463832
Asthma	65.63	9.83	307	74955	91235	46519565
Drug abuse	62.46	9.83	13	75249	63395	46547405
Treatment failure	58.59	9.83	39	75223	93048	46517752
Synovitis	57.20	9.83	14	75248	61061	46549739
Cholecystitis chronic	53.60	9.83	75	75187	10424	46600376
Pruritus	51.01	9.83	606	74656	241746	46369054
Somnolence	50.69	9.83	428	74834	156093	46454707
Maternal exposure during pregnancy	48.78	9.83	56	75206	102493	46508307
Off label use	48.56	9.83	386	74876	379455	46231345
Dizziness	45.90	9.83	787	74475	339627	46271173
Seasonal allergy	45.34	9.83	79	75183	13255	46597545
Infective pulmonary exacerbation of cystic fibrosis	40.69	9.83	67	75195	10740	46600060
Butterfly rash	40.31	9.83	23	75239	951	46609849
Anxiety	39.58	9.83	458	74804	181499	46429301
Pancytopenia	38.79	9.83	48	75214	85010	46525790
Swelling face	38.04	9.83	178	75084	52881	46557919
Insomnia	37.16	9.83	418	74844	164506	46446294
General physical health deterioration	36.45	9.83	83	75179	115686	46495114
Muscle spasms	35.36	9.83	328	74934	122785	46488015
Systemic lupus erythematosus	35.07	9.83	32	75230	65148	46545652
Coma	34.93	9.83	186	75076	58163	46552637
Glossodynia	34.72	9.83	14	75248	44359	46566441
Joint swelling	34.53	9.83	144	75118	165929	46444871
Angioedema	34.32	9.83	140	75122	39202	46571598
Dyspnoea	34.17	9.83	1079	74183	514469	46096331
Rhinitis allergic	33.27	9.83	48	75214	6860	46603940
Chest discomfort	33.08	9.83	254	75008	90015	46520785
Gallbladder disorder	32.67	9.83	81	75181	17417	46593383
C-reactive protein increased	32.44	9.83	28	75234	58562	46552238
Palpitations	31.61	9.83	262	75000	94997	46515803
Multiple organ dysfunction syndrome	30.77	9.83	23	75239	51687	46559113
Emotional distress	30.63	9.83	114	75148	30593	46580207
Hand deformity	30.34	9.83	9	75253	34565	46576235
Sinus disorder	29.18	9.83	75	75187	16488	46594312
Allergy test positive	28.93	9.83	13	75249	321	46610479
Rhabdomyolysis	28.53	9.83	16	75246	41893	46568907
Completed suicide	28.21	9.83	130	75132	145790	46465010
Multiple allergies	28.15	9.83	46	75216	7325	46603475
Cough	27.67	9.83	523	74739	229726	46381074
Injury	26.79	9.83	141	75121	43886	46566914
Drug interaction	26.53	9.83	205	75057	202889	46407911
Hyponatraemia	26.29	9.83	80	75182	101252	46509548
Tinnitus	26.16	9.83	101	75161	27572	46583228
Headache	26.08	9.83	979	74283	477373	46133427
Lactic acidosis	26.04	9.83	11	75251	33898	46576902
Feeling abnormal	25.93	9.83	312	74950	124748	46486052
Death	25.87	9.83	383	74879	335165	46275635
Hepatocellular injury	25.34	9.83	8	75254	29514	46581286
Nasal congestion	25.22	9.83	148	75114	47965	46562835
Depression	24.21	9.83	397	74865	169707	46441093
Rash	24.03	9.83	748	74514	355764	46255036
Therapeutic product effect decreased	23.80	9.83	62	75200	82539	46528261
Acquired haemophilia	23.37	9.83	16	75246	915	46609885
Hypersensitivity	23.34	9.83	356	74906	149965	46460835
Product dose omission issue	23.14	9.83	391	74871	168129	46442671
Wound	23.03	9.83	21	75241	42781	46568019
Throat irritation	22.99	9.83	100	75162	28801	46581999
Periorbital oedema	22.82	9.83	34	75228	5001	46605799
Expired product administered	22.72	9.83	36	75226	5586	46605214
Thrombocytopenia	22.59	9.83	116	75146	126465	46484335
Sopor	21.87	9.83	3	75259	19825	46590975
Bronchitis	21.79	9.83	264	74998	105715	46505085
Hyperkalaemia	21.69	9.83	30	75232	50679	46560121
Tinea pedis	21.49	9.83	18	75244	1395	46609405
Arthropathy	21.17	9.83	68	75194	84632	46526168
Malignant neoplasm progression	20.87	9.83	46	75216	64880	46545920
Upper respiratory tract infection	20.64	9.83	174	75088	63382	46547418
Hypersomnia	20.41	9.83	63	75199	15376	46595424
Septic shock	20.32	9.83	39	75223	57854	46552946
Lip swelling	20.30	9.83	88	75174	25307	46585493
C-reactive protein abnormal	19.67	9.83	5	75257	21265	46589535
Cardiac failure	19.42	9.83	65	75197	79883	46530917
Leukopenia	19.15	9.83	52	75210	68291	46542509
Biliary dyskinesia	19.15	9.83	23	75239	2750	46608050
Renal impairment	19.08	9.83	59	75203	74313	46536487
Wheezing	18.87	9.83	149	75113	53237	46557563
Sinus headache	18.86	9.83	30	75232	4670	46606130
Oropharyngeal pain	18.54	9.83	192	75070	73976	46536824
Fatigue	18.41	9.83	1176	74086	607521	46003279
Osteonecrosis of jaw	18.37	9.83	17	75245	34385	46576415
Drug resistance	18.30	9.83	3	75259	17365	46593435
Anaphylactic reaction	18.10	9.83	147	75115	52965	46557835
Essential hypertension	17.98	9.83	28	75234	4282	46606518
Premature baby	17.25	9.83	4	75258	18108	46592692
Lupus hepatitis	16.94	9.83	5	75257	34	46610766
Alopecia	16.78	9.83	174	75088	162240	46448560
Photosensitivity reaction	16.72	9.83	52	75210	12740	46598060
Therapeutic product effect incomplete	16.70	9.83	67	75195	78086	46532714
Allergic cystitis	16.30	9.83	3	75259	0	46610800
Hepatic failure	16.15	9.83	18	75244	33398	46577402
Gallbladder injury	15.91	9.83	15	75247	1359	46609441
Nervousness	15.84	9.83	89	75173	28386	46582414
Chest pain	15.52	9.83	383	74879	175941	46434859
Foetal exposure during pregnancy	15.48	9.83	16	75246	30731	46580069
Cholelithiasis	15.38	9.83	111	75151	38570	46572230
Neutropenia	15.38	9.83	152	75110	143052	46467748
Basophil count decreased	15.36	9.83	6	75256	103	46610697
Victim of chemical submission	15.27	9.83	8	75254	279	46610521
Cystitis noninfective	15.25	9.83	12	75250	851	46609949
Neuropathy peripheral	15.17	9.83	218	75044	90675	46520125
Posterior reversible encephalopathy syndrome	15.12	9.83	3	75259	15138	46595662
Circulatory collapse	15.09	9.83	8	75254	21616	46589184
Abdominal distension	14.76	9.83	182	75080	73169	46537631
Dyspepsia	14.70	9.83	172	75090	68300	46542500
Incorrect dose administered	14.42	9.83	124	75138	45426	46565374
Exposure to toxic agent	14.39	9.83	17	75245	1997	46608803
Status asthmaticus	14.39	9.83	12	75250	924	46609876
Agranulocytosis	14.35	9.83	9	75253	22176	46588624
Overdose	14.22	9.83	101	75161	101878	46508922
Migraine	14.20	9.83	174	75088	69852	46540948
Dry mouth	14.11	9.83	143	75119	54783	46556017
Throat tightness	13.89	9.83	68	75194	20571	46590229
Neurological examination abnormal	13.66	9.83	7	75255	233	46610567
Cardio-respiratory arrest	13.65	9.83	50	75212	59819	46550981
Diarrhoea	13.40	9.83	1061	74201	558541	46052259
Sinus congestion	13.35	9.83	49	75213	13060	46597740
Fracture	13.21	9.83	5	75257	16466	46594334
Infection	13.04	9.83	145	75117	133447	46477353
Mobility decreased	12.91	9.83	52	75210	60542	46550258
Renal failure	12.86	9.83	119	75143	113475	46497325
Suicidal ideation	12.71	9.83	143	75119	56239	46554561
Xanthogranuloma	12.70	9.83	3	75259	7	46610793
Hepatotoxicity	12.61	9.83	13	75249	24996	46585804
Metastases to liver	12.59	9.83	8	75254	19577	46591223
Pericarditis	12.57	9.83	12	75250	23915	46586885
Vision blurred	12.45	9.83	189	75073	79519	46531281
Feeling hot	12.40	9.83	104	75158	37824	46572976
Abdominal pain upper	12.30	9.83	314	74948	144991	46465809
Cytomegalovirus infection	12.24	9.83	7	75255	18137	46592663
Cyclic vomiting syndrome	11.94	9.83	4	75258	43	46610757
Burns first degree	11.69	9.83	3	75259	11	46610789
Acute sinusitis	11.66	9.83	22	75240	3925	46606875
Incorrect dosage administered	11.63	9.83	14	75248	1677	46609123
Pneumocystis jirovecii pneumonia	11.62	9.83	5	75257	15243	46595557
Hypotension	11.56	9.83	286	74976	232303	46378497
Cataract subcapsular	11.54	9.83	9	75253	630	46610170
Reflux gastritis	11.48	9.83	10	75252	817	46609983
Ear congestion	11.48	9.83	14	75248	1701	46609099
Sleep apnoea syndrome	11.44	9.83	68	75194	22133	46588667
Hepatic enzyme increased	11.40	9.83	81	75181	81706	46529094
Upper-airway cough syndrome	11.30	9.83	33	75229	7814	46602986
Deep vein thrombosis	11.26	9.83	186	75076	79587	46531213
Red blood cell sedimentation rate abnormal	11.19	9.83	4	75258	13645	46597155
Mitral valve prolapse	11.16	9.83	16	75246	2273	46608527
Interstitial lung disease	11.06	9.83	47	75215	53902	46556898
Hot flush	11.03	9.83	113	75149	43404	46567396
Nasal oedema	11.03	9.83	10	75252	862	46609938
Acute hepatic failure	10.95	9.83	5	75257	14716	46596084
Multiple lentigines syndrome	10.86	9.83	6	75256	233	46610567
Patellofemoral pain syndrome	10.83	9.83	8	75254	516	46610284
Head discomfort	10.80	9.83	39	75223	10312	46600488
Hypoaesthesia	10.69	9.83	259	75003	118610	46492190
Lower respiratory tract infection	10.68	9.83	49	75213	55040	46555760
Depressed level of consciousness	10.66	9.83	40	75222	47529	46563271
Eye swelling	10.64	9.83	62	75200	20041	46590759
Cluster headache	10.60	9.83	8	75254	533	46610267
Oesophageal adenocarcinoma recurrent	10.49	9.83	3	75259	18	46610782
Cholestasis	10.44	9.83	17	75245	26876	46583924
Bone marrow failure	10.40	9.83	20	75242	29649	46581151
Torsade de pointes	10.40	9.83	43	75219	12111	46598689
Contraindicated product prescribed	10.39	9.83	9	75253	730	46610070
Hypocalcaemia	10.34	9.83	17	75245	26768	46584032
Paraesthesia	10.30	9.83	255	75007	117182	46493618
Bezoar	10.18	9.83	12	75250	1407	46609393
Knee arthroplasty	10.12	9.83	14	75248	23651	46587149
Myxoedema coma	10.10	9.83	7	75255	408	46610392
Musculoskeletal stiffness	10.10	9.83	105	75157	97888	46512912
Eye pruritus	10.10	9.83	42	75220	11856	46598944
Broad ligament tear	10.09	9.83	3	75259	21	46610779
Tympanic membrane disorder	10.02	9.83	5	75257	157	46610643
Status epilepticus	10.01	9.83	5	75257	13974	46596826
Congenital cystic lung	9.97	9.83	3	75259	22	46610778
Presbyoesophagus	9.97	9.83	3	75259	22	46610778
Snoring	9.94	9.83	19	75243	3423	46607377
Rhinorrhoea	9.90	9.83	119	75143	47546	46563254

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
Accidental exposure to product by child	314.25	10.65	104	36328	1459	29914587
Extra dose administered	269.15	10.65	109	36323	2777	29913269
Failure of child resistant product closure	91.41	10.65	18	36414	16	29916030
Drug abuse	64.67	10.65	11	36421	82061	29833985
Urticaria	53.53	10.65	167	36265	54439	29861607
General physical health deterioration	44.35	10.65	34	36398	99910	29816136
Drug interaction	42.81	10.65	114	36318	199454	29716592
Infective pulmonary exacerbation of cystic fibrosis	42.01	10.65	52	36380	8520	29907526
Completed suicide	40.27	10.65	37	36395	99455	29816591
Sinusitis	39.38	10.65	109	36323	33236	29882810
Asthma	32.14	10.65	107	36325	36067	29879979
Toxicity to various agents	31.69	10.65	110	36322	177073	29738973
Rash	31.40	10.65	364	36068	191525	29724521
Fatigue	29.41	10.65	550	35882	320123	29595923
Throat irritation	28.46	10.65	43	36389	8505	29907541
Pruritus	28.44	10.65	243	36189	117961	29798085
Sinus disorder	27.71	10.65	36	36396	6189	29909857
Cough	26.00	10.65	250	36182	125392	29790654
Acute kidney injury	25.96	10.65	211	36221	273631	29642415
Expired product administered	25.77	10.65	24	36408	2845	29913201
PO2 increased	22.62	10.65	12	36420	573	29915473
Blood pH decreased	22.18	10.65	20	36412	2275	29913771
Gastrointestinal mucosal necrosis	21.64	10.65	8	36424	158	29915888
Chronic spontaneous urticaria	21.36	10.65	7	36425	95	29915951
Rheumatoid arthritis	20.98	10.65	12	36420	41185	29874861
Treatment failure	20.90	10.65	8	36424	34671	29881375
Drug ineffective	20.63	10.65	291	36141	340096	29575950
Seasonal allergy	20.40	10.65	27	36405	4726	29911320
Dizziness	19.82	10.65	340	36092	194569	29721477
Bronchitis	19.70	10.65	97	36335	39028	29877018
Renal impairment	19.63	10.65	46	36386	84138	29831908
Ultrasound skull abnormal	18.61	10.65	6	36426	77	29915969
CADASIL	18.61	10.65	6	36426	77	29915969
Magnetic resonance imaging spinal abnormal	18.33	10.65	6	36426	81	29915965
Oral pruritus	18.05	10.65	8	36424	256	29915790
Visual evoked potentials abnormal	18.00	10.65	6	36426	86	29915960
Hyperkalaemia	17.98	10.65	33	36399	65977	29850069
Eye pruritus	17.93	10.65	23	36409	3904	29912142
Physical examination abnormal	17.40	10.65	6	36426	96	29915950
Infusion related reaction	17.27	10.65	96	36336	40468	29875578
Wheezing	17.24	10.65	79	36353	30859	29885187
Tunnel vision	17.23	10.65	9	36423	416	29915630
Central nervous system inflammation	17.06	10.65	6	36426	102	29915944
Double stranded DNULL antibody positive	16.90	10.65	6	36426	105	29915941
Swelling face	16.47	10.65	60	36372	21144	29894902
Anxiety	16.25	10.65	174	36258	89697	29826349
Ejaculation delayed	16.21	10.65	7	36425	210	29915836
Tension headache	16.03	10.65	13	36419	1280	29914766
Glossodynia	15.85	10.65	20	36412	3341	29912705
Saccadic eye movement	15.67	10.65	6	36426	131	29915915
Off label use	15.47	10.65	212	36220	249078	29666968
Feeling abnormal	15.42	10.65	120	36312	56636	29859410
Chest pain	15.30	10.65	214	36218	117413	29798633
Drug resistance	15.20	10.65	3	36429	20130	29895916
Upper respiratory tract infection	15.19	10.65	70	36362	27406	29888640
Gastrooesophageal reflux disease	14.86	10.65	78	36354	32177	29883869
Interstitial lung disease	14.76	10.65	32	36400	60165	29855881
Metamorphopsia	14.66	10.65	9	36423	568	29915478
Rhabdomyolysis	14.61	10.65	35	36397	63545	29852501
Suicidal ideation	14.41	10.65	84	36348	36030	29880016
Sleep apnoea syndrome	14.20	10.65	49	36383	16808	29899238
Migraine	14.13	10.65	41	36391	12833	29903213
Vision blurred	14.01	10.65	93	36339	41723	29874323
Lacrimation increased	13.81	10.65	28	36404	6988	29909058
Leukopenia	13.64	10.65	30	36402	56129	29859917
Depression	13.62	10.65	169	36263	90268	29825778
Cerebral microangiopathy	13.48	10.65	6	36426	194	29915852
Lactic acidosis	13.35	10.65	11	36421	31202	29884844
Rhinitis allergic	13.29	10.65	17	36415	2877	29913169
Renal failure	13.29	10.65	97	36335	128869	29787177
Conduction disorder	13.22	10.65	14	36418	1937	29914109
Hyponatraemia	13.18	10.65	40	36392	67162	29848884
Intercepted medication error	13.16	10.65	8	36424	496	29915550
Heart rate increased	12.90	10.65	86	36346	38635	29877411
Chest discomfort	12.82	10.65	97	36335	45383	29870663
Thrombocytopenia	12.76	10.65	106	36326	136938	29779108
Body height decreased	12.74	10.65	19	36413	3715	29912331
PCO2 decreased	12.59	10.65	12	36420	1464	29914582
Septic shock	12.37	10.65	38	36394	63569	29852477
Burning sensation	12.27	10.65	46	36386	16428	29899618
Contraindicated product administered	12.13	10.65	3	36429	17228	29898818
Intentional self-injury	11.99	10.65	40	36392	13492	29902554
Spinal osteoarthritis	11.96	10.65	25	36407	6374	29909672
Lipid metabolism disorder	11.93	10.65	6	36426	256	29915790
Stress at work	11.64	10.65	5	36427	148	29915898
Convulsions local	11.62	10.65	3	36429	16	29916030
Lip swelling	11.58	10.65	38	36394	12706	29903340
Rhinorrhoea	11.57	10.65	53	36379	20701	29895345
Blood cholesterol increased	11.51	10.65	46	36386	16924	29899122
Muscle tightness	11.19	10.65	20	36412	4543	29911503
Upper-airway cough syndrome	11.03	10.65	15	36417	2695	29913351
Insomnia	11.02	10.65	167	36265	93169	29822877
Muscle spasms	11.01	10.65	124	36308	64714	29851332
Bone marrow failure	10.98	10.65	12	36420	29773	29886273
Melaena	10.96	10.65	14	36418	32423	29883623
Hepatocellular injury	10.86	10.65	9	36423	25462	29890584
Metabolic acidosis	10.86	10.65	18	36414	37443	29878603
Dyspnoea	10.82	10.65	502	35930	332793	29583253
Chills	10.81	10.65	135	36297	72203	29843843
Hyperprolactinaemia	10.71	10.65	10	36422	1190	29914856

Pharmacologic Action:

Source	Code	Description
ATC	R06AX13	RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Other antihistamines for systemic use
MeSH PA	D018926	Anti-Allergic Agents
MeSH PA	D000982	Antipruritics
MeSH PA	D003879	Dermatologic Agents
MeSH PA	D018494	Histamine Agents
MeSH PA	D006633	Histamine Antagonists
MeSH PA	D006634	Histamine H1 Antagonists
MeSH PA	D039563	Histamine H1 Antagonists, Non-Sedating
MeSH PA	D018377	Neurotransmitter Agents

Drug Use (View source of the data)

Disease	Relation	SNOMED_ID	DOID
Vasomotor rhinitis	indication	8229003	DOID:4730
Allergic rhinitis	indication	61582004
Nasal discharge	indication	64531003
Nasal congestion	indication	68235000
Sneezing	indication	76067001
Common cold	indication	82272006	DOID:10459
Chronic idiopathic urticaria	indication	302162004
Seasonal allergic rhinitis	indication	367498001
Allergic conjunctivitis	indication	473460002	DOID:11204
Bone pain after neupogen	off-label use	12584003
Urticaria	off-label use	126485001
Hyperthyroidism	contraindication	34486009	DOID:7998
Hypertensive disorder	contraindication	38341003	DOID:10763
Coronary arteriosclerosis	contraindication	53741008	DOID:3393
Hepatic failure	contraindication	59927004
Diabetes mellitus	contraindication	73211009	DOID:9351
Kidney disease	contraindication	90708001	DOID:557
Impaired renal function disorder	contraindication	197663003
Disease of liver	contraindication	235856003	DOID:409
Benign prostatic hyperplasia	contraindication	266569009
Retention of urine	contraindication	267064002
Angle-closure glaucoma	contraindication	392291006	DOID:13550
Hypertensive urgency	contraindication	443482000

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	4.43	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN	ANTAGONIST	Ki	6.97	WOMBAT-PK	CHEMBL
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	6.81	DRUG MATRIX
Cytochrome P450 2C19	Enzyme	P33261	CP2CJ_HUMAN		IC50	7.80	DRUG MATRIX
Multidrug resistance protein 1	Transporter	P08183	MDR1_HUMAN		Ki	4.94	WOMBAT-PK
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	6.77	WOMBAT-PK
Nuclear receptor subfamily 1 group I member 2	Nuclear hormone receptor	O75469	NR1I2_HUMAN		EC50	5.52	CHEMBL
Bile acid receptor	Nuclear hormone receptor	Q96RI1	NR1H4_HUMAN		IC50	5.51	CHEMBL
Sodium-dependent neutral amino acid transporter B(0)AT2	Transporter	Q9H2J7	S6A15_HUMAN		IC50	5.40	CHEMBL
Histamine H1 receptor	GPCR		HRH1_RAT		Ki	6.46	CHEMBL
Histamine H1 receptor	GPCR		HRH1_CAVPO		Kd	7.14	CHEMBL

External reference:

ID	Source
4020716	VUID
N0000148306	NUI
D00364	KEGG_DRUG
4020716	VANDF
C0701055	UMLSCUI
CHEBI:6538	CHEBI
CHEMBL998	ChEMBL_ID
D017336	MESH_DESCRIPTOR_UI
DB00455	DRUGBANK_ID
3957	PUBCHEM_CID
7216	IUPHAR_LIGAND_ID
5864	INN_ID
7AJO3BO7QN	UNII
203576	RXNORM
191	MMSL
45829	MMSL
4994	MMSL
d03050	MMSL
003909	NDDF
015760	NDDF
108652002	SNOMEDCT_US
386884002	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
allergy relief	HUMAN OTC DRUG LABEL	1	0067-6066	TABLET	10 mg	ORAL	NDA	15 sections
allergy relief	HUMAN OTC DRUG LABEL	1	0067-6122	TABLET	10 mg	ORAL	NDA	15 sections
good sense allergy relief	HUMAN OTC DRUG LABEL	1	0113-0612	TABLET	10 mg	ORAL	ANDA	15 sections
Good Sense childrens allergy relief	HUMAN OTC DRUG LABEL	1	0113-0671	SOLUTION	5 mg	ORAL	ANDA	14 sections
good sense childrens allergy relief	HUMAN OTC DRUG LABEL	1	0113-1019	TABLET, CHEWABLE	5 mg	ORAL	ANDA	15 sections
good sense allergy relief	HUMAN OTC DRUG LABEL	1	0113-1191	TABLET, ORALLY DISINTEGRATING	10 mg	ORAL	ANDA	15 sections
good sense allergy relief	HUMAN OTC DRUG LABEL	1	0113-1612	TABLET	10 mg	ORAL	ANDA	15 sections
good sense childrens allergy relief	HUMAN OTC DRUG LABEL	1	0113-1719	SOLUTION	5 mg	ORAL	ANDA	14 sections
Allergy and Congestion Relief	HUMAN OTC DRUG LABEL	2	0113-2007	TABLET, FILM COATED, EXTENDED RELEASE	5 mg	ORAL	ANDA	14 sections
basic care childrens allergy relief	HUMAN OTC DRUG LABEL	1	0113-7500	TABLET, CHEWABLE	5 mg	ORAL	ANDA	15 sections
Basic Care allergy relief	HUMAN OTC DRUG LABEL	1	0113-7612	TABLET	10 mg	ORAL	ANDA	15 sections
Basic Care Childrens Allergy Relief	HUMAN OTC DRUG LABEL	1	0113-7671	SOLUTION	5 mg	ORAL	ANDA	14 sections
good sense allergy relief	HUMAN OTC DRUG LABEL	1	0113-9755	TABLET, ORALLY DISINTEGRATING	10 mg	ORAL	ANDA	15 sections
Childrens Loratadine	HUMAN OTC DRUG LABEL	1	0121-0849	SOLUTION	5 mg	ORAL	ANDA	16 sections
Loratadine	HUMAN OTC DRUG LABEL	1	0363-0522	TABLET	10 mg	ORAL	ANDA	15 sections
Loratadine	HUMAN OTC DRUG LABEL	1	0363-0527	TABLET, ORALLY DISINTEGRATING	10 mg	ORAL	ANDA	15 sections
Wal itin	HUMAN OTC DRUG LABEL	1	0363-0699	TABLET	10 mg	ORAL	ANDA	15 sections
Loratadine and Pseudoephedrine	HUMAN OTC DRUG LABEL	2	0363-0725	TABLET, FILM COATED, EXTENDED RELEASE	10 mg	ORAL	ANDA	16 sections
Loratadine	HUMAN OTC DRUG LABEL	1	0363-0752	TABLET, CHEWABLE	5 mg	ORAL	ANDA	16 sections
Wal-itin	HUMAN OTC DRUG LABEL	1	0363-0754	TABLET, CHEWABLE	5 mg	ORAL	ANDA	16 sections
Indoor Outdoor Allergy Relief	HUMAN OTC DRUG LABEL	1	0363-0858	TABLET	10 mg	ORAL	ANDA	14 sections
12 hour allergy and congestion	HUMAN OTC DRUG LABEL	2	0363-1133	TABLET, FILM COATED, EXTENDED RELEASE	5 mg	ORAL	ANDA	14 sections
WAL-ITIN	HUMAN OTC DRUG LABEL	1	0363-1686	CAPSULE, LIQUID FILLED	10 mg	ORAL	ANDA	9 sections
Wal-itin Allergy Relief	HUMAN OTC DRUG LABEL	1	0363-2085	SOLUTION	5 mg	ORAL	ANDA	15 sections
Childrens Wal-itin	HUMAN OTC DRUG LABEL	1	0363-2092	SOLUTION	5 mg	ORAL	ANDA	16 sections
Childrens Walitin	HUMAN OTC DRUG LABEL	1	0363-2108	SOLUTION	5 mg	ORAL	ANDA	16 sections
Childrens Loratadine Sugar Free	HUMAN OTC DRUG LABEL	1	0363-2131	SOLUTION	5 mg	ORAL	ANDA	16 sections
Wal-itin D24 Hour	HUMAN OTC DRUG LABEL	2	0363-2390	TABLET, EXTENDED RELEASE	10 mg	ORAL	ANDA	16 sections
CHILDRENS LORATADINE ODT	Human OTC Drug Label	1	0363-4020	TABLET, ORALLY DISINTEGRATING	10 mg	ORAL	ANDA	15 sections
Wal-itin	HUMAN OTC DRUG LABEL	1	0363-9150	TABLET	10 mg	ORAL	ANDA	14 sections