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Tox | Related Drugs | BioActivity |

Stem definition	Drug id	CAS RN
antihypertensive substances, prazosin derivatives	4209	19216-56-9

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: prazosin prazosin hydrochloride furazosin prazosin HCl	A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION. Molecular weight: 383.41 Formula: C19H21N5O4 CLOGP: 2.08 LIPINSKI: 0 HAC: 9 HDO: 1 TPSA: 106.95 ALOGS: -2.74 ROTB: 4 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

prazosin
prazosin hydrochloride
furazosin
prazosin HCl

A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.

Molecular weight: 383.41
Formula: C19H21N5O4
CLOGP: 2.08
LIPINSKI: 0
HAC: 9
HDO: 1
TPSA: 106.95
ALOGS: -2.74
ROTB: 4

Status: OFP

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

Drug dosage:

Dose	Unit	Route
5	mg	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	1.40 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0.50 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	1.49 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	68 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	0.73 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	4.70 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.06 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	2 hours	Lombardo F, Berellini G, Obach RS

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
kinase-safety-class	ACVR2B,AXL,BRAF,CAMK2D,CDK5,CDK9,DDR1,EIF2AK3,ERBB2,GRK2,MAP3K21,MAPK7,MET,PDK2,PDK4,PIK3CD,PRKDC,TTK	18
kinase-selectivity-class	AXL,DDR1,ERBB2,MARK4,PRKDC,SIK2,STK33,TTK	8
mdck-mdr1-bcrp-efflux	MDCK-MDR1-BCRP efflux ratio	10.399		High	1
pfas-class	PFAS structural alert (1 = True, 0 = False)	0
rat-kpuu-brain	Rat brain Kpuu	0.021	%	High	1

Approvals:

Date	Agency	Company	Orphan
June 23, 1976	FDA	PFIZER

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
Completed suicide	132.82	17.06	118	10024	144940	90473365
Body mass index abnormal	117.90	17.06	25	10117	714	90617591
Serositis	103.52	17.06	25	10117	1292	90617013
Central nervous system lupus	102.67	17.06	25	10117	1338	90616967
Atrioventricular block first degree	99.42	17.06	37	10105	8474	90609831
Dissociation	96.42	17.06	34	10108	6681	90611624
Post-traumatic stress disorder	95.86	17.06	34	10108	6794	90611511
Suicidal ideation	92.32	17.06	72	10070	73783	90544522
Bezoar	76.69	17.06	23	10119	2711	90615594
Corneal reflex decreased	75.56	17.06	15	10127	306	90617999
Lupus nephritis	75.27	17.06	26	10116	4806	90613499
Toxicity to various agents	74.42	17.06	123	10019	287723	90330582
Post cholecystectomy syndrome	65.54	17.06	16	10126	865	90617440
Cardiogenic shock	64.75	17.06	38	10104	24430	90593875
Areflexia	58.23	17.06	20	10122	3633	90614672
Glomerular filtration rate increased	56.35	17.06	17	10125	2043	90616262
Electric shock	54.91	17.06	16	10126	1706	90616599
Blood immunoglobulin A increased	54.89	17.06	15	10127	1268	90617037
Haematuria	54.67	17.06	39	10103	34898	90583407
Vitamin B12 increased	53.99	17.06	16	10126	1810	90616495
Intentional overdose	53.46	17.06	59	10083	93775	90524530
Granulocyte count increased	52.24	17.06	15	10127	1519	90616786
Hypotension	48.29	17.06	110	10032	325287	90293018
Depression	47.27	17.06	104	10038	300497	90317808
Rheumatoid factor increased	45.55	17.06	15	10127	2396	90615909
Pupillary reflex impaired	44.76	17.06	15	10127	2530	90615775
Gout	44.12	17.06	26	10116	16833	90601472
Unmasking of previously unidentified disease	43.93	17.06	13	10129	1463	90616842
Intervertebral discitis	43.27	17.06	17	10125	4503	90613802
Dactylitis	42.18	17.06	16	10126	3857	90614448
Cardio-respiratory arrest	41.79	17.06	43	10099	63097	90555208
Electrocardiogram ST segment elevation	41.62	17.06	16	10126	4000	90614305
Norepinephrine increased	40.68	17.06	7	10135	62	90618243
Electrocardiogram repolarisation abnormality	40.43	17.06	12	10130	1364	90616941
Renal impairment	40.03	17.06	54	10088	105367	90512938
Throat clearing	38.70	17.06	15	10127	3832	90614473
Electrocardiogram QRS complex prolonged	38.39	17.06	18	10124	7330	90610975
Sinus tachycardia	38.23	17.06	29	10113	28484	90589821
Drug withdrawal syndrome	38.04	17.06	29	10113	28694	90589611
Aspartate aminotransferase	37.96	17.06	10	10132	735	90617570
Systolic dysfunction	36.59	17.06	12	10130	1892	90616413
Sinus bradycardia	36.31	17.06	23	10119	16929	90601376
Blood alkaline phosphatase increased	35.96	17.06	35	10107	48044	90570261
Vitamin B12 deficiency	35.03	17.06	17	10125	7469	90610836
Circulatory collapse	34.88	17.06	26	10116	24878	90593427
Monocyte count increased	34.74	17.06	18	10124	9079	90609226
Blood uric acid increased	34.56	17.06	17	10125	7687	90610618
Blood pressure systolic decreased	34.42	17.06	18	10124	9252	90609053
Tardive dyskinesia	34.36	17.06	19	10123	10911	90607394
White blood cells urine positive	34.20	17.06	16	10126	6482	90611823
Joint noise	34.09	17.06	15	10127	5275	90613030
Status epilepticus	34.05	17.06	23	10119	18851	90599454
Metabolic acidosis	33.42	17.06	36	10106	55640	90562665
Cardiac arrest	32.81	17.06	49	10093	104886	90513419
Aspartate aminotransferase abnormal	32.71	17.06	12	10130	2637	90615668
Temperature intolerance	32.66	17.06	19	10123	12011	90606294
Miosis	31.23	17.06	17	10125	9467	90608838
Suspected suicide	31.09	17.06	17	10125	9551	90608754
Demyelination	30.78	17.06	16	10126	8124	90610181
Vitamin D deficiency	30.74	17.06	21	10121	17535	90600770
Posterior reversible encephalopathy syndrome	30.56	17.06	23	10119	22316	90595989
Phaeochromocytoma	30.09	17.06	8	10134	609	90617696
Systemic lupus erythematosus	29.76	17.06	3	10139	361893	90256412
Piloerection	29.73	17.06	8	10134	638	90617667
Drug intolerance	29.41	17.06	7	10135	447584	90170721
Seizure	28.85	17.06	57	10085	152572	90465733
Electrocardiogram QT prolonged	28.85	17.06	38	10104	72418	90545887
Swelling	28.64	17.06	6	10136	419052	90199253
Cholecystitis acute	28.61	17.06	16	10126	9388	90608917
Abdominal discomfort	28.49	17.06	9	10133	477319	90140986
Ventricular hypokinesia	27.64	17.06	13	10129	5328	90612977
Cardiac failure	27.16	17.06	46	10096	109450	90508855
Alopecia	26.72	17.06	11	10131	495060	90123245
Blood pressure fluctuation	26.51	17.06	31	10111	52382	90565923
Joint swelling	25.87	17.06	12	10130	503288	90115017
Spinal disorder	25.40	17.06	16	10126	11663	90606642
Cardiac hypertrophy	24.98	17.06	8	10134	1170	90617135
Metabolic myopathy	24.29	17.06	5	10137	123	90618182
Depressed mood	24.23	17.06	29	10113	50193	90568112
Premature baby	24.09	17.06	21	10121	25056	90593249
Withdrawal syndrome	23.96	17.06	20	10122	22504	90595801
Glycosylated haemoglobin increased	23.49	17.06	17	10125	15545	90602760
Hypertrichosis	23.19	17.06	8	10134	1471	90616834
Contraindicated product administered	23.11	17.06	4	10138	320135	90298170
Hepatic enzyme increased	22.99	17.06	6	10136	360730	90257575
Hyperkalaemia	22.72	17.06	32	10110	64932	90553373
Blood prolactin increased	22.43	17.06	10	10132	3627	90614678
Generalised tonic-clonic seizure	21.70	17.06	23	10119	34880	90583425
Hypertensive crisis	21.47	17.06	17	10125	17767	90600538
Wound	21.40	17.06	4	10138	302976	90315329
BRASH syndrome	21.32	17.06	8	10134	1871	90616434
Progressive multifocal leukoencephalopathy	21.15	17.06	16	10126	15639	90602666
Cardiotoxicity	20.83	17.06	14	10128	11375	90606930
Coordination abnormal	20.75	17.06	18	10124	21338	90596967
Suicide attempt	20.47	17.06	33	10109	75366	90542939
Renal papillary necrosis	20.33	17.06	5	10137	279	90618026
Neutrophil count increased	20.18	17.06	17	10125	19373	90598932
Dissociative identity disorder	19.99	17.06	4	10138	85	90618220
Occipital neuralgia	19.94	17.06	6	10136	714	90617591
Blood glucose decreased	19.31	17.06	18	10124	23411	90594894
Gastrointestinal disorder	18.98	17.06	3	10139	256684	90361621
Ventricular extrasystoles	18.92	17.06	14	10128	13236	90605069
Sedation	18.77	17.06	25	10117	48146	90570159
Overdose	18.73	17.06	49	10093	157660	90460645
Myasthenic syndrome	18.73	17.06	5	10137	387	90617918
Hyperprolactinaemia	18.61	17.06	10	10132	5423	90612882
Multiple sclerosis	18.48	17.06	19	10123	27821	90590484
Product dose omission issue	18.48	17.06	73	10069	291614	90326691
Antipsychotic drug level decreased	18.47	17.06	5	10137	408	90617897
Alcoholism	18.04	17.06	7	10135	1793	90616512
Feeling abnormal	17.90	17.06	50	10092	167185	90451120
Mental disorder	17.83	17.06	20	10122	32298	90586007
Anxiety	17.63	17.06	75	10067	309697	90308608
General physical health deterioration	17.42	17.06	9	10133	355106	90263199
Depressed level of consciousness	17.28	17.06	30	10112	72754	90545551
Blood test abnormal	17.08	17.06	16	10126	20936	90597369

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
Serotonin syndrome	109.14	17.03	59	5955	25786	42589535
Antidepressant drug level above therapeutic	105.04	17.03	20	5994	254	42615067
Analgesic drug level above therapeutic	101.27	17.03	20	5994	311	42615010
Completed suicide	94.10	17.03	90	5924	96375	42518946
Priapism	93.97	17.03	35	5979	6372	42608949
Parasomnia	77.42	17.03	17	5997	452	42614869
Drug interaction	54.94	17.03	118	5896	266881	42348440
Sudden cardiac death	52.32	17.03	20	5994	3904	42611417
Abnormal sleep-related event	49.96	17.03	12	6002	478	42614843
Suicidal behaviour	48.70	17.03	15	5999	1531	42613790
Vasoplegia syndrome	40.74	17.03	15	5999	2640	42612681
Suicidal ideation	39.58	17.03	41	5973	48120	42567201
Cardiac autonomic neuropathy	38.29	17.03	7	6007	70	42615251
Blood pressure ambulatory increased	38.20	17.03	7	6007	71	42615250
Somnambulism	33.67	17.03	14	6000	3401	42611920
Supine hypertension	32.00	17.03	8	6006	377	42614944
Lactic acidosis	31.00	17.03	35	5979	45226	42570095
Pulmonary congestion	30.71	17.03	22	5992	15708	42599613
Syncope	28.98	17.03	51	5963	99355	42515966
Tri-iodothyronine decreased	28.32	17.03	6	6008	134	42615187
Hypotension	27.27	17.03	89	5925	257542	42357779
Paradoxical drug reaction	26.26	17.03	13	6001	4725	42610596
Globulins increased	26.22	17.03	7	6007	428	42614893
Non-high-density lipoprotein cholesterol increased	26.01	17.03	6	6008	200	42615121
Overdose	25.65	17.03	50	5964	105214	42510107
Thyroxine decreased	25.51	17.03	6	6008	218	42615103
Sinus bradycardia	25.01	17.03	19	5995	14834	42600487
Compartment syndrome	24.30	17.03	11	6003	3278	42612043
Spleen tuberculosis	22.57	17.03	4	6010	33	42615288
Electrocardiogram QT prolonged	21.49	17.03	30	5984	47915	42567406
Rhabdomyolysis	21.40	17.03	39	5975	77980	42537341
Autonomic neuropathy	20.19	17.03	7	6007	1036	42614285
Toxicity to various agents	18.92	17.03	73	5941	229063	42386258
Sleep disorder	18.51	17.03	28	5986	48067	42567254
Suspected suicide	17.73	17.03	11	6003	6188	42609133
Left atrial dilatation	17.64	17.03	8	6006	2394	42612927

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
Completed suicide	211.21	15.00	205	14193	242176	110332725
Body mass index abnormal	108.45	15.00	25	14373	903	110573998
Priapism	99.71	15.00	35	14363	5826	110569075
Central nervous system lupus	99.08	15.00	25	14373	1328	110573573
Dissociation	95.54	15.00	39	14359	9803	110565098
Serositis	95.41	15.00	25	14373	1544	110573357
Analgesic drug level above therapeutic	94.28	15.00	20	14378	489	110574412
Atrioventricular block first degree	87.90	15.00	41	14357	14184	110560717
Antidepressant drug level above therapeutic	86.37	15.00	20	14378	737	110574164
Toxicity to various agents	85.31	15.00	191	14207	480364	110094537
Suicidal ideation	82.64	15.00	80	14318	93857	110481044
Parasomnia	80.73	15.00	19	14379	752	110574149
Hypotension	76.51	15.00	193	14205	523656	110051245
Serotonin syndrome	75.12	15.00	62	14336	59091	110515810
Post-traumatic stress disorder	73.95	15.00	29	14369	6567	110568334
Lupus nephritis	72.41	15.00	26	14372	4619	110570282
Corneal reflex decreased	65.17	15.00	15	14383	538	110574363
Bezoar	64.36	15.00	23	14375	4031	110570870
Sinus bradycardia	62.38	15.00	42	14356	29441	110545460
Post cholecystectomy syndrome	58.72	15.00	15	14383	837	110574064
Vitamin B12 increased	58.04	15.00	18	14380	2037	110572864
Drug interaction	55.76	15.00	167	14231	500016	110074885
Cardiogenic shock	54.53	15.00	51	14347	57287	110517614
Electrocardiogram QT prolonged	51.30	15.00	67	14331	108893	110466008
Glomerular filtration rate increased	50.60	15.00	16	14382	1929	110572972
Tardive dyskinesia	48.39	15.00	27	14371	13552	110561349
Suspected suicide	48.19	15.00	28	14370	15171	110559730
Electric shock	47.40	15.00	15	14383	1813	110573088
Sudden cardiac death	46.85	15.00	20	14378	5617	110569284
Blood immunoglobulin A increased	45.40	15.00	14	14384	1554	110573347
Systolic dysfunction	44.58	15.00	18	14380	4397	110570504
Cardio-respiratory arrest	43.67	15.00	64	14334	115772	110459129
Abnormal sleep-related event	43.59	15.00	12	14386	894	110574007
Areflexia	43.34	15.00	20	14378	6749	110568152
Rheumatoid factor increased	42.76	15.00	15	14383	2490	110572411
Granulocyte count increased	42.17	15.00	14	14384	1969	110572932
Syncope	40.98	15.00	85	14313	202451	110372450
Overdose	40.33	15.00	92	14306	233702	110341199
Posterior reversible encephalopathy syndrome	39.90	15.00	34	14364	33827	110541074
Cardiac autonomic neuropathy	38.76	15.00	7	14391	71	110574830
Blood pressure ambulatory increased	38.41	15.00	7	14391	75	110574826
Suicidal behaviour	37.89	15.00	15	14383	3482	110571419
Norepinephrine increased	37.61	15.00	7	14391	85	110574816
Electrocardiogram ST segment elevation	37.60	15.00	20	14378	9140	110565761
Pupillary reflex impaired	35.88	15.00	15	14383	4000	110570901
Dactylitis	35.46	15.00	15	14383	4118	110570783
Aspartate aminotransferase	33.86	15.00	10	14388	959	110573942
Unmasking of previously unidentified disease	33.53	15.00	13	14385	2855	110572046
Intentional overdose	33.36	15.00	61	14337	132440	110442461
Electrocardiogram repolarisation abnormality	32.42	15.00	12	14386	2323	110572578
Blood alkaline phosphatase increased	32.42	15.00	43	14355	70892	110504009
Somnambulism	32.11	15.00	16	14382	6389	110568512
Joint swelling	32.02	15.00	9	14389	442836	110132065
Gross motor delay	32.01	15.00	7	14391	198	110574703
Throat clearing	31.53	15.00	14	14384	4319	110570582
Vasoplegia syndrome	31.51	15.00	15	14383	5424	110569477
Supine hypertension	31.38	15.00	8	14390	443	110574458
Hyperkalaemia	31.06	15.00	60	14338	135736	110439165
Intervertebral discitis	30.79	15.00	16	14382	6974	110567927
Lactic acidosis	30.34	15.00	48	14350	92763	110482138
Sinus tachycardia	30.24	15.00	33	14365	44460	110530441
White blood cells urine positive	29.68	15.00	16	14382	7508	110567393
Joint noise	29.24	15.00	14	14384	5129	110569772
Ventricular hypokinesia	28.68	15.00	18	14380	11196	110563705
Aspartate aminotransferase abnormal	28.30	15.00	12	14386	3313	110571588
Blood pressure systolic decreased	28.07	15.00	19	14379	13422	110561479
Drug withdrawal syndrome	27.22	15.00	29	14369	38025	110536876
Alopecia	27.14	15.00	7	14391	364746	110210155
Electrocardiogram QRS complex prolonged	26.23	15.00	18	14380	13003	110561898
Piloerection	26.18	15.00	8	14390	861	110574040
Neutrophil count increased	25.84	15.00	27	14371	34625	110540276
Swelling	25.62	15.00	7	14391	351034	110223867
Sedation	25.53	15.00	38	14360	69645	110505256
Temperature intolerance	25.11	15.00	18	14380	13932	110560969
Stomatitis	24.83	15.00	3	14395	270239	110304662
Drug intolerance	24.71	15.00	11	14387	406501	110168400
Gout	24.64	15.00	27	14371	36539	110538362
Withdrawal syndrome	24.39	15.00	25	14373	31355	110543546
Akathisia	23.96	15.00	19	14379	17094	110557807
Alcoholism	23.88	15.00	11	14387	3696	110571205
Depression	23.87	15.00	93	14305	317242	110257659
Hypertensive crisis	23.79	15.00	22	14376	24350	110550551
Demyelination	23.78	15.00	15	14383	9414	110565487
Monocyte count increased	23.58	15.00	17	14381	13276	110561625
Cardiac hypertrophy	23.38	15.00	9	14389	1938	110572963
Blood urea increased	23.11	15.00	32	14366	54925	110519976
Metabolic myopathy	22.99	15.00	5	14393	138	110574763
Vitamin B12 deficiency	22.90	15.00	15	14383	10040	110564861
Vitamin D deficiency	22.61	15.00	19	14379	18533	110556368
Status epilepticus	22.47	15.00	24	14374	31547	110543354
Antipsychotic drug level decreased	22.37	15.00	8	14390	1404	110573497
Phaeochromocytoma	22.18	15.00	7	14391	838	110574063
Seizure	21.93	15.00	71	14327	221114	110353787
Abdominal discomfort	21.90	15.00	12	14386	393846	110181055
Spleen tuberculosis	21.85	15.00	4	14394	44	110574857
Compartment syndrome	21.74	15.00	12	14386	5898	110569003
Lower respiratory tract infection	21.61	15.00	3	14395	243103	110331798
Blood prolactin increased	21.52	15.00	11	14387	4631	110570270
Bradycardia	21.26	15.00	56	14342	155461	110419440
Cardiac arrest	21.20	15.00	65	14333	196688	110378213
Pulmonary congestion	21.10	15.00	23	14375	30943	110543958
General physical health deterioration	20.84	15.00	15	14383	425280	110149621
Spinal disorder	20.81	15.00	15	14383	11713	110563188
Hypertrichosis	20.58	15.00	8	14390	1770	110573131
Renal impairment	20.06	15.00	62	14336	188383	110386518
Rash	19.79	15.00	49	14349	820915	109753986
Circulatory collapse	19.54	15.00	26	14372	42967	110531934
Occipital neuralgia	19.18	15.00	6	14392	698	110574203
Anxiety	18.95	15.00	92	14306	344986	110229915
Arthropathy	18.73	15.00	7	14391	287515	110287386
Autonomic neuropathy	18.58	15.00	8	14390	2292	110572609
Paradoxical drug reaction	18.44	15.00	13	14385	9804	110565097
Haematuria	18.15	15.00	36	14362	82969	110491932
Metabolic acidosis	18.01	15.00	40	14358	99704	110475197
Tri-iodothyronine decreased	17.95	15.00	5	14393	389	110574512
Hyperprolactinaemia	17.95	15.00	11	14387	6564	110568337
Feeling abnormal	17.90	15.00	58	14340	180653	110394248
Non-high-density lipoprotein cholesterol increased	17.78	15.00	5	14393	403	110574498
Coordination abnormal	17.64	15.00	19	14379	25209	110549692
Speech disorder developmental	17.61	15.00	6	14392	913	110573988
Respiratory arrest	17.48	15.00	29	14369	58270	110516631
Renal papillary necrosis	17.30	15.00	5	14393	444	110574457
Febrile neutropenia	17.11	15.00	10	14388	316757	110258144
Blood pressure fluctuation	17.02	15.00	33	14365	74791	110500110
Nightmare	16.90	15.00	23	14375	38840	110536061
Cholecystitis acute	16.88	15.00	15	14383	15767	110559134
Mobility decreased	16.83	15.00	5	14393	237417	110337484
Pericarditis	16.69	15.00	4	14394	219110	110355791
Blood uric acid increased	16.45	15.00	17	14381	21512	110553389
Impaired healing	16.20	15.00	3	14395	196714	110378187
Hepatic enzyme increased	16.13	15.00	11	14387	320881	110254020
Rhabdomyolysis	16.09	15.00	43	14355	120358	110454543
Asthenia	15.91	15.00	42	14356	688957	109885944
Myasthenic syndrome	15.69	15.00	6	14392	1270	110573631
Gastrointestinal disorder	15.57	15.00	6	14392	241946	110332955
Mental disorder	15.44	15.00	22	14376	38769	110536132
Hypersensitivity	15.34	15.00	18	14380	403980	110170921
Muscular dystrophy	15.31	15.00	4	14394	244	110574657
Needle issue	15.31	15.00	15	14383	17825	110557076
Glycosylated haemoglobin increased	15.15	15.00	17	14381	23602	110551299

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	C02CA01	CARDIOVASCULAR SYSTEM ANTIHYPERTENSIVES ANTIADRENERGIC AGENTS, PERIPHERALLY ACTING Alpha-adrenoreceptor antagonists
ATC	C02LE01	CARDIOVASCULAR SYSTEM ANTIHYPERTENSIVES ANTIHYPERTENSIVES AND DIURETICS IN COMBINATION Alpha-adrenoreceptor antagonists and diuretics
FDA MoA	N0000000099	Adrenergic alpha-Antagonists
FDA EPC	N0000175553	alpha-Adrenergic Blocker
MeSH PA	D000317	Adrenergic alpha-Antagonists
MeSH PA	D000959	Antihypertensive Agents
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018663	Adrenergic Agents
MeSH PA	D018674	Adrenergic Antagonists
MeSH PA	D058668	Adrenergic alpha-1 Receptor Antagonists
CHEBI has role	CHEBI:22587	antiviral agent
CHEBI has role	CHEBI:35469	antidepressant
CHEBI has role	CHEBI:35474	anxiolytic drug
CHEBI has role	CHEBI:35674	antihypertensive agent
CHEBI has role	CHEBI:37890	α-adrenergic antagonist
CHEBI has role	CHEBI:76779	EC 3.4.21.26 (prolyl oligopeptidase) inhibitor

Related Drugs by ATC class:

C02CA Alpha-adrenoreceptor antagonists 4 drugs

doxazosin indoramin trimazosin urapidil

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

Disease	Relation	SNOMED_ID	DOID
Hypertensive disorder	indication	38341003	DOID:10763
Benign prostatic hyperplasia	off-label use	266569009
PTSD related nightmares	off-label use	428687006
Chronic Post Traumatic Stress Disorder with Trauma-related Nightmares	off-label use
End stage renal disease	contraindication	46177005	DOID:784
Narcolepsy	contraindication	60380001	DOID:8986
Cataract surgery	contraindication	110473004
Micturition syncope	contraindication	234168001
Syncope	contraindication	271594007
Intraoperative floppy iris syndrome	contraindication	418801006

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	7.22	Basic
pKa2	0.72	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
Alpha-1B adrenergic receptor	GPCR	P35368	ADA1B_HUMAN	INVERSE AGONIST	Ki	9.68	CHEMBL	IUPHAR
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN	INVERSE AGONIST	Ki	10.40	CHEMBL	IUPHAR
Alpha-1D adrenergic receptor	GPCR	P25100	ADA1D_HUMAN	INVERSE AGONIST	Ki	9.70	CHEMBL	IUPHAR
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	5.80	CHEMBL
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		Ki	7.73	WOMBAT-PK
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	5.58	DRUG MATRIX
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		Ki	7.89	CHEMBL
5-hydroxytryptamine receptor 1D	GPCR	P28221	5HT1D_HUMAN		Ki	9.48	CHEMBL
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN		Ki	7.62	CHEMBL
Adenosine receptor A3	GPCR	P0DMS8	AA3R_HUMAN		IC50	9.07	CHEMBL
D(4) dopamine receptor	GPCR	P21917	DRD4_HUMAN		Ki	5.08	CHEMBL
5-hydroxytryptamine receptor 5A	GPCR	P47898	5HT5A_HUMAN		Ki	6.10	CHEMBL
Ribosyldihydronicotinamide dehydrogenase [quinone]	Enzyme	P16083	NQO2_HUMAN		IC50	8.11	CHEMBL
Matrix metalloproteinase-9	Enzyme	P14780	MMP9_HUMAN		IC50	5.16	DRUG MATRIX
Interstitial collagenase	Enzyme	P03956	MMP1_HUMAN		IC50	5.39	DRUG MATRIX
Solute carrier family 22 member 1	Transporter	O15245	S22A1_HUMAN		IC50	5	CHEMBL
Solute carrier family 22 member 2	Transporter	O15244	S22A2_HUMAN		IC50	4.87	CHEMBL
Multidrug and toxin extrusion protein 1	Transporter	Q96FL8	S47A1_HUMAN		IC50	5.80	CHEMBL
Multidrug and toxin extrusion protein 2	Transporter	Q86VL8	S47A2_HUMAN		IC50	4.42	CHEMBL
Sodium channel alpha subunits; brain (Types I, II, III)	Ion channel	P35498 Q99250 Q9NY46	SCN1A_HUMAN SCN2A_HUMAN SCN3A_HUMAN		IC50	5	CHEMBL
Mu-type opioid receptor	GPCR	P35372	OPRM_HUMAN		Ki	5.75	CHEMBL
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	6.68	CHEMBL
Sigma non-opioid intracellular receptor 1	Membrane receptor	Q99720	SGMR1_HUMAN		Ki	5.53	CHEMBL
Alpha-1B adrenergic receptor	GPCR		ADA1B_RAT		Ki	10	CHEMBL
Alpha-1A adrenergic receptor	GPCR		ADA1A_RAT		Ki	10.15	CHEMBL
Alpha-1D adrenergic receptor	GPCR		ADA1D_RAT		Ki	9.70	CHEMBL
Mu-type opioid receptor	GPCR		OPRM_RAT		Ki	9.70	CHEMBL
D(2) dopamine receptor	GPCR		DRD2_RAT		IC50	4.96	CHEMBL
5-hydroxytryptamine receptor 1A	GPCR		5HT1A_RAT		Ki	5.63	CHEMBL
5-hydroxytryptamine receptor 2A	GPCR		5HT2A_RAT		Ki	5.82	CHEMBL
Alpha-2A adrenergic receptor	GPCR		ADA2A_RAT		Ki	5.78	CHEMBL
Alpha-1A adrenergic receptor	GPCR		ADA1A_BOVIN		Ki	9.77	CHEMBL
Alpha-2A adrenergic receptor	GPCR		ADA2A_PIG		Ki	5.39	CHEMBL
Alpha-2A adrenergic receptor	GPCR		ADA2A_BOVIN		Ki	6.97	CHEMBL
Alpha-1B adrenergic receptor	GPCR		ADA1B_MESAU		Ki	9.08	CHEMBL
Adrenergic receptor alpha-2	GPCR		ADA2B_RAT ADA2C_RAT ADA2A_RAT		Ki	9.40	CHEMBL
Adrenergic receptor alpha-1	GPCR		ADA1B_RAT ADA1D_RAT ADA1A_RAT		Kd	10.99	CHEMBL
Serotonin 2 (5-HT2) receptor	GPCR		5HT2C_RAT 5HT2A_RAT 5HT2B_RAT		IC50	4.38	CHEMBL
Alpha-2 adrenergic receptor	GPCR		ADA2B_MOUSE ADA2C_MOUSE ADA2A_MOUSE		Ki	7.89	CHEMBL
Beta-casein	Secreted		CASB_RAT		Ki	9.44	CHEMBL

External reference:

ID	Source
4019901	VUID
N0000147986	NUI
D00609	KEGG_DRUG
19237-84-4	SECONDARY_CAS_RN
4018850	VANDF
4019901	VANDF
C0032912	UMLSCUI
CHEBI:8364	CHEBI
XRA	PDB_CHEM_ID
CHEMBL2	ChEMBL_ID
CHEMBL1558	ChEMBL_ID
D011224	MESH_DESCRIPTOR_UI
DB00457	DRUGBANK_ID
503	IUPHAR_LIGAND_ID
2593	INN_ID
XM03YJ541D	UNII
4893	PUBCHEM_CID
203210	RXNORM
2426	MMSL
5345	MMSL
d00138	MMSL
000635	NDDF
004491	NDDF
387283005	SNOMEDCT_US
387433003	SNOMEDCT_US
76058001	SNOMEDCT_US
XM03YJ541D	INXIGHT DRUGS

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Prazosin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0093-4067	CAPSULE	1 mg	ORAL	ANDA	21 sections
Prazosin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0093-4068	CAPSULE	2 mg	ORAL	ANDA	21 sections
Prazosin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0093-4069	CAPSULE	5 mg	ORAL	ANDA	21 sections
Prazosin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0378-1101	CAPSULE	1 mg	ORAL	ANDA	21 sections
Prazosin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0378-2302	CAPSULE	2 mg	ORAL	ANDA	21 sections
Prazosin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0378-3205	CAPSULE	5 mg	ORAL	ANDA	21 sections
Prazosin	HUMAN PRESCRIPTION DRUG LABEL	1	0527-4180	CAPSULE	1 mg	ORAL	ANDA	22 sections
Prazosin	HUMAN PRESCRIPTION DRUG LABEL	1	0527-4181	CAPSULE	2 mg	ORAL	ANDA	22 sections
Prazosin	HUMAN PRESCRIPTION DRUG LABEL	1	0527-4182	CAPSULE	5 mg	ORAL	ANDA	22 sections
Prazosin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8519	CAPSULE	1 mg	ORAL	ANDA	20 sections
Prazosin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8520	CAPSULE	2 mg	ORAL	ANDA	20 sections
Prazosin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0904-7020	CAPSULE	1 mg	ORAL	ANDA	20 sections
Prazosin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0904-7021	CAPSULE	2 mg	ORAL	ANDA	20 sections
Prazosin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0904-7022	CAPSULE	5 mg	ORAL	ANDA	20 sections
Prazosin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	10135-666	CAPSULE	1 mg	ORAL	ANDA	20 sections
Prazosin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	10135-667	CAPSULE	2 mg	ORAL	ANDA	20 sections
Prazosin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	10135-668	CAPSULE	5 mg	ORAL	ANDA	20 sections
Prazosin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	33261-860	CAPSULE	1 mg	ORAL	ANDA	21 sections
Prazosin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	33261-861	CAPSULE	2 mg	ORAL	ANDA	21 sections
Prazosin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	43063-248	CAPSULE	5 mg	ORAL	ANDA	21 sections
Prazosin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	43063-248	CAPSULE	5 mg	ORAL	ANDA	21 sections
Prazosin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	43063-260	CAPSULE	2 mg	ORAL	ANDA	21 sections
Prazosin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	43063-260	CAPSULE	2 mg	ORAL	ANDA	21 sections
Prazosin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	43353-035	CAPSULE	2 mg	ORAL	ANDA	21 sections
Prazosin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	43353-868	CAPSULE	2 mg	ORAL	ANDA	22 sections
PRAZOSIN HYDROCHLORIDE	Human Prescription Drug Label	1	46708-691	CAPSULE	1 mg	ORAL	ANDA	18 sections
PRAZOSIN HYDROCHLORIDE	Human Prescription Drug Label	1	46708-692	CAPSULE	2 mg	ORAL	ANDA	18 sections
PRAZOSIN HYDROCHLORIDE	Human Prescription Drug Label	1	46708-693	CAPSULE	5 mg	ORAL	ANDA	18 sections
Prazosin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	48433-084	CAPSULE	1 mg	ORAL	ANDA	21 sections
Prazosin Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	48433-085	CAPSULE	2 mg	ORAL	ANDA	21 sections

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prazosin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Description:

Drug dosage:

ADMET properties:

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Approvals:

FDA Adverse Event Reporting System (Female)

FDA Adverse Event Reporting System (Male)

FDA Adverse Event Reporting System (Geriatric)

FDA Adverse Event Reporting System (Pediatric)

Pharmacologic Action:

Related Drugs by ATC class:

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

🐶 Veterinary Drug Use

🐶 Veterinary products

Acid dissociation constants calculated using MoKa v3.0.0

Orange Book patent data (new drug applications)

Orange Book exclusivity data (new drug applications)

Bioactivity Summary:

External reference:

Pharmaceutical products: