Stem definition | Drug id | CAS RN |
---|---|---|
antihypertensive substances, prazosin derivatives | 4209 | 19216-56-9 |
Dose | Unit | Route |
---|---|---|
5 | mg | O |
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 |
Date | Agency | Company | Orphan |
---|---|---|---|
June 23, 1976 | FDA | PFIZER |
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 |
---|---|---|---|---|---|---|
Atrioventricular block first degree | 113.91 | 16.68 | 37 | 4791 | 6149 | 46675085 |
Unmasking of previously unidentified disease | 48.90 | 16.68 | 12 | 4816 | 719 | 46680515 |
Sinus bradycardia | 45.25 | 16.68 | 24 | 4804 | 13758 | 46667476 |
Circulatory collapse | 45.07 | 16.68 | 28 | 4800 | 21596 | 46659638 |
Electrocardiogram ST segment elevation | 40.46 | 16.68 | 15 | 4813 | 3680 | 46677554 |
Posterior reversible encephalopathy syndrome | 40.42 | 16.68 | 23 | 4805 | 15118 | 46666116 |
Norepinephrine increased | 40.20 | 16.68 | 7 | 4821 | 73 | 46681161 |
Electrocardiogram repolarisation abnormality | 37.89 | 16.68 | 11 | 4817 | 1254 | 46679980 |
Systolic dysfunction | 37.48 | 16.68 | 11 | 4817 | 1303 | 46679931 |
Ventricular hypokinesia | 32.01 | 16.68 | 13 | 4815 | 4065 | 46677169 |
Electrocardiogram QRS complex prolonged | 31.56 | 16.68 | 14 | 4814 | 5435 | 46675799 |
Toxicity to various agents | 31.17 | 16.68 | 68 | 4760 | 211698 | 46469536 |
Hypotension | 27.98 | 16.68 | 69 | 4759 | 232520 | 46448714 |
Cardiac arrest | 27.59 | 16.68 | 40 | 4788 | 90359 | 46590875 |
Hypertrichosis | 27.39 | 16.68 | 8 | 4820 | 932 | 46680302 |
Cardiac hypertrophy | 26.46 | 16.68 | 8 | 4820 | 1049 | 46680185 |
Cardiotoxicity | 25.78 | 16.68 | 13 | 4815 | 6709 | 46674525 |
Overdose | 25.31 | 16.68 | 41 | 4787 | 101938 | 46579296 |
Drug withdrawal syndrome | 23.94 | 16.68 | 21 | 4807 | 27363 | 46653871 |
Metabolic acidosis | 22.99 | 16.68 | 24 | 4804 | 38756 | 46642478 |
Bradycardia | 22.69 | 16.68 | 31 | 4797 | 66267 | 46614967 |
Ventricular extrasystoles | 22.22 | 16.68 | 14 | 4814 | 11049 | 46670185 |
Suicidal ideation | 21.82 | 16.68 | 28 | 4800 | 56354 | 46624880 |
Cardio-respiratory arrest | 20.49 | 16.68 | 28 | 4800 | 59841 | 46621393 |
Dissociative identity disorder | 20.49 | 16.68 | 4 | 4824 | 81 | 46681153 |
Haemophagocytic lymphohistiocytosis | 20.47 | 16.68 | 12 | 4816 | 8330 | 46672904 |
Hypertensive crisis | 19.58 | 16.68 | 14 | 4814 | 13601 | 46667633 |
Status epilepticus | 19.25 | 16.68 | 14 | 4814 | 13965 | 46667269 |
Electrocardiogram QRS complex shortened | 19.25 | 16.68 | 5 | 4823 | 377 | 46680857 |
Electrocardiogram QT prolonged | 19.09 | 16.68 | 25 | 4803 | 51300 | 46629934 |
Stress cardiomyopathy | 18.58 | 16.68 | 11 | 4817 | 7773 | 46673461 |
Withdrawal syndrome | 18.08 | 16.68 | 15 | 4813 | 18119 | 46663115 |
Acute kidney injury | 17.63 | 16.68 | 59 | 4769 | 235796 | 46445438 |
Coma scale abnormal | 17.23 | 16.68 | 9 | 4819 | 4997 | 46676237 |
Hypovolaemic shock | 16.93 | 16.68 | 9 | 4819 | 5174 | 46676060 |
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 |
---|---|---|---|---|---|---|
Priapism | 83.85 | 15.64 | 31 | 4924 | 4712 | 29942811 |
Parasomnia | 76.81 | 15.64 | 16 | 4939 | 278 | 29947245 |
Antidepressant drug level above therapeutic | 67.12 | 15.64 | 13 | 4942 | 153 | 29947370 |
Analgesic drug level above therapeutic | 62.08 | 15.64 | 13 | 4942 | 232 | 29947291 |
Abnormal sleep-related event | 47.50 | 15.64 | 12 | 4943 | 502 | 29947021 |
Serotonin syndrome | 44.86 | 15.64 | 31 | 4924 | 17860 | 29929663 |
Suicidal behaviour | 44.06 | 15.64 | 14 | 4941 | 1348 | 29946175 |
Vasoplegia syndrome | 32.75 | 15.64 | 11 | 4944 | 1260 | 29946263 |
Drug interaction | 31.60 | 15.64 | 88 | 4867 | 199480 | 29748043 |
Sudden cardiac death | 30.26 | 15.64 | 14 | 4941 | 3738 | 29943785 |
Orthostatic hypotension | 26.90 | 15.64 | 26 | 4929 | 23953 | 29923570 |
Somnambulism | 25.94 | 15.64 | 12 | 4943 | 3202 | 29944321 |
Compartment syndrome | 25.40 | 15.64 | 11 | 4944 | 2516 | 29945007 |
Sinus bradycardia | 24.11 | 15.64 | 18 | 4937 | 11677 | 29935846 |
Spleen tuberculosis | 24.01 | 15.64 | 4 | 4951 | 18 | 29947505 |
Syncope | 20.38 | 15.64 | 44 | 4911 | 84859 | 29862664 |
Hyperlactacidaemia | 18.79 | 15.64 | 9 | 4946 | 2597 | 29944926 |
Pulmonary congestion | 17.03 | 15.64 | 15 | 4940 | 12272 | 29935251 |
Electrocardiogram QT prolonged | 16.94 | 15.64 | 25 | 4930 | 35810 | 29911713 |
Aspiration | 16.91 | 15.64 | 14 | 4941 | 10537 | 29936986 |
Suicidal ideation | 16.80 | 15.64 | 25 | 4930 | 36089 | 29911434 |
Food interaction | 16.50 | 15.64 | 6 | 4949 | 869 | 29946654 |
Overdose | 16.15 | 15.64 | 40 | 4915 | 84297 | 29863226 |
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 | D018663 | Adrenergic Agents |
MeSH PA | D058668 | Adrenergic alpha-1 Receptor Antagonists |
MeSH PA | D000317 | Adrenergic alpha-Antagonists |
MeSH PA | D018674 | Adrenergic Antagonists |
MeSH PA | D000959 | Antihypertensive Agents |
MeSH PA | D002317 | Cardiovascular Agents |
MeSH PA | D018377 | Neurotransmitter Agents |
CHEBI has role | CHEBI:35674 | antihypertensive |
CHEBI has role | CHEBI:37890 | alpha-adrenoceptor antagonists |
CHEBI has role | CHEBI:76779 | prolyl oligopeptidase (ec 3.4.21.26) inhibitor |
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 |
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 7.22 | Basic |
pKa2 | 0.72 | Basic |
None
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Alpha-1A adrenergic receptor | GPCR | INVERSE AGONIST | Ki | 10.40 | CHEMBL | IUPHAR | |||
Alpha-1B adrenergic receptor | GPCR | INVERSE AGONIST | Ki | 9.68 | CHEMBL | IUPHAR | |||
Alpha-1D adrenergic receptor | GPCR | INVERSE AGONIST | Ki | 9.70 | CHEMBL | IUPHAR | |||
5-hydroxytryptamine receptor 2A | GPCR | Ki | 7.73 | WOMBAT-PK | |||||
Solute carrier family 22 member 1 | Transporter | IC50 | 5 | CHEMBL | |||||
Solute carrier family 22 member 2 | Transporter | IC50 | 4.87 | CHEMBL | |||||
Alpha-2A adrenergic receptor | GPCR | Ki | 6.68 | CHEMBL | |||||
D(4) dopamine receptor | GPCR | Ki | 5.08 | CHEMBL | |||||
5-hydroxytryptamine receptor 1D | GPCR | Ki | 9.48 | CHEMBL | |||||
Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 5.80 | CHEMBL | |||||
Alpha-2B adrenergic receptor | GPCR | Ki | 7.89 | CHEMBL | |||||
Alpha-2C adrenergic receptor | GPCR | Ki | 7.62 | CHEMBL | |||||
Multidrug and toxin extrusion protein 2 | Transporter | IC50 | 4.42 | CHEMBL | |||||
Multidrug and toxin extrusion protein 1 | Transporter | IC50 | 5.80 | CHEMBL | |||||
Adenosine receptor A3 | GPCR | IC50 | 9.07 | CHEMBL | |||||
Sodium channel alpha subunits; brain (Types I, II, III) | Ion channel | IC50 | 5 | CHEMBL | |||||
Ribosyldihydronicotinamide dehydrogenase [quinone] | Enzyme | IC50 | 8.11 | CHEMBL | |||||
5-hydroxytryptamine receptor 2B | GPCR | Ki | 5.58 | DRUG MATRIX | |||||
Matrix metalloproteinase-9 | Enzyme | IC50 | 5.16 | DRUG MATRIX | |||||
Interstitial collagenase | Enzyme | IC50 | 5.39 | DRUG MATRIX | |||||
Alpha-1B adrenergic receptor | GPCR | Ki | 9.08 | CHEMBL | |||||
Serotonin 2 (5-HT2) receptor | GPCR | IC50 | 4.38 | CHEMBL | |||||
Adrenergic receptor alpha-2 | GPCR | Ki | 9.40 | CHEMBL | |||||
Alpha-2A adrenergic receptor | GPCR | Ki | 5.78 | CHEMBL | |||||
Alpha-1D adrenergic receptor | GPCR | Ki | 9.70 | CHEMBL | |||||
Alpha-2A adrenergic receptor | GPCR | Ki | 5.39 | CHEMBL | |||||
Alpha-2 adrenergic receptor | GPCR | Ki | 7.89 | CHEMBL | |||||
5-hydroxytryptamine receptor 2A | GPCR | Ki | 5.82 | CHEMBL | |||||
Adrenergic receptor alpha-1 | GPCR | Kd | 10.99 | CHEMBL | |||||
Alpha-1A adrenergic receptor | GPCR | Ki | 9.77 | CHEMBL | |||||
Alpha-2A adrenergic receptor | GPCR | Ki | 6.97 | CHEMBL | |||||
Alpha-1A adrenergic receptor | GPCR | Ki | 10.15 | CHEMBL | |||||
5-hydroxytryptamine receptor 1A | GPCR | Ki | 5.63 | CHEMBL | |||||
Alpha-1B adrenergic receptor | GPCR | Ki | 10 | CHEMBL | |||||
D(2) dopamine receptor | GPCR | IC50 | 4.96 | CHEMBL | |||||
Mu-type opioid receptor | GPCR | Ki | 9.70 | CHEMBL | |||||
Beta-casein | Unclassified | Ki | 9.44 | CHEMBL |
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 |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Minipress | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0069-4310 | CAPSULE | 1 mg | ORAL | NDA | 22 sections |
Minipress | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0069-4370 | CAPSULE | 2 mg | ORAL | NDA | 22 sections |
Minipress | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0069-4380 | CAPSULE | 5 mg | ORAL | NDA | 22 sections |
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 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 | 21 sections |
Prazosin Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10135-667 | CAPSULE | 2 mg | ORAL | ANDA | 21 sections |
Prazosin Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10135-668 | CAPSULE | 5 mg | ORAL | ANDA | 21 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 | 43063-260 | 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 | 50090-0379 | CAPSULE | 1 mg | ORAL | ANDA | 21 sections |
Prazosin Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50090-1948 | CAPSULE | 1 mg | ORAL | ANDA | 21 sections |
Prazosin Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50090-1948 | CAPSULE | 1 mg | ORAL | ANDA | 21 sections |
Prazosin Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50090-2845 | CAPSULE | 1 mg | ORAL | ANDA | 21 sections |
Prazosin Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50090-5512 | CAPSULE | 2 mg | ORAL | ANDA | 21 sections |
Prazosin Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51079-630 | CAPSULE | 1 mg | ORAL | ANDA | 21 sections |
Prazosin Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51079-631 | CAPSULE | 2 mg | ORAL | ANDA | 21 sections |
Prazosin Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51079-632 | CAPSULE | 5 mg | ORAL | ANDA | 21 sections |
Prazosin Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 53808-1075 | CAPSULE | 2 mg | ORAL | ANDA | 21 sections |