Stem definition | Drug id | CAS RN |
---|---|---|
antihypertensives, guanidine derivatives | 1343 | 29110-47-2 |
Dose | Unit | Route |
---|---|---|
3 | mg | O |
Property | Value | Reference |
---|---|---|
BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Benet LZ, Broccatelli F, Oprea TI |
S (Water solubility) | 1 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
EoM (Fraction excreted unchanged in urine) | 50 % | Benet LZ, Broccatelli F, Oprea TI |
MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.35 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
BA (Bioavailability) | 81 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Vd (Volume of distribution) | 5.60 L/kg | Lombardo F, Berellini G, Obach RS |
CL (Clearance) | 4.50 mL/min/kg | Lombardo F, Berellini G, Obach RS |
fu (Fraction unbound in plasma) | 0.28 % | Lombardo F, Berellini G, Obach RS |
t_half (Half-life) | 15 hours | Lombardo F, Berellini G, Obach RS |
Date | Agency | Company | Orphan |
---|---|---|---|
Oct. 27, 1986 | FDA | PROMIUS PHARMA | |
March 30, 2017 | PMDA | Shionogi & Co., Ltd. |
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 |
---|---|---|---|---|---|---|
Product substitution issue | 121.12 | 26.60 | 38 | 1801 | 14993 | 46669230 |
Aggression | 90.83 | 26.60 | 34 | 1805 | 22710 | 46661513 |
Somnolence | 55.09 | 26.60 | 47 | 1792 | 156474 | 46527749 |
Impulsive behaviour | 51.74 | 26.60 | 12 | 1827 | 1503 | 46682720 |
Psychomotor hyperactivity | 40.62 | 26.60 | 15 | 1824 | 9598 | 46674625 |
Suicidal ideation | 37.89 | 26.60 | 25 | 1814 | 56357 | 46627866 |
Intentional overdose | 37.00 | 26.60 | 26 | 1813 | 64918 | 46619305 |
Bradycardia | 36.51 | 26.60 | 26 | 1813 | 66272 | 46617951 |
Product administered to patient of inappropriate age | 35.58 | 26.60 | 10 | 1829 | 2686 | 46681537 |
Atrioventricular dissociation | 33.12 | 26.60 | 6 | 1833 | 219 | 46684004 |
Abnormal behaviour | 32.25 | 26.60 | 16 | 1823 | 21042 | 46663181 |
Educational problem | 31.75 | 26.60 | 6 | 1833 | 277 | 46683946 |
Irritability | 30.14 | 26.60 | 17 | 1822 | 28929 | 46655294 |
Sinus arrhythmia | 27.18 | 26.60 | 7 | 1832 | 1353 | 46682870 |
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 |
---|---|---|---|---|---|---|
Product substitution issue | 323.64 | 32.41 | 97 | 3789 | 9938 | 29938654 |
Aggression | 247.34 | 32.41 | 112 | 3774 | 36795 | 29911797 |
Agitation | 127.35 | 32.41 | 82 | 3804 | 53991 | 29894601 |
Abnormal behaviour | 120.24 | 32.41 | 61 | 3825 | 25562 | 29923030 |
Psychomotor hyperactivity | 106.23 | 32.41 | 40 | 3846 | 8184 | 29940408 |
Irritability | 99.80 | 32.41 | 52 | 3834 | 22998 | 29925594 |
Tic | 98.34 | 32.41 | 27 | 3859 | 2005 | 29946587 |
Drug ineffective | 81.57 | 32.41 | 152 | 3734 | 340235 | 29608357 |
Somnolence | 66.77 | 32.41 | 72 | 3814 | 96691 | 29851901 |
Impulsive behaviour | 63.21 | 32.41 | 19 | 3867 | 1946 | 29946646 |
Educational problem | 61.81 | 32.41 | 13 | 3873 | 306 | 29948286 |
Anger | 53.62 | 32.41 | 27 | 3859 | 11093 | 29937499 |
Brugada syndrome | 53.46 | 32.41 | 13 | 3873 | 595 | 29947997 |
Disturbance in attention | 53.03 | 32.41 | 34 | 3852 | 22095 | 29926497 |
Bradycardia | 45.54 | 32.41 | 49 | 3837 | 65477 | 29883115 |
Negativism | 42.93 | 32.41 | 10 | 3876 | 380 | 29948212 |
Emotional disorder | 42.18 | 32.41 | 18 | 3868 | 5076 | 29943516 |
Insomnia | 42.12 | 32.41 | 56 | 3830 | 93280 | 29855312 |
Disturbance in social behaviour | 42.09 | 32.41 | 13 | 3873 | 1458 | 29947134 |
Sinus bradycardia | 41.10 | 32.41 | 23 | 3863 | 11672 | 29936920 |
Product quality issue | 38.07 | 32.41 | 26 | 3860 | 18748 | 29929844 |
Anxiety | 37.62 | 32.41 | 52 | 3834 | 89819 | 29858773 |
Sinus arrest | 37.52 | 32.41 | 12 | 3874 | 1508 | 29947084 |
Drug dose titration not performed | 36.20 | 32.41 | 8 | 3878 | 239 | 29948353 |
Affective disorder | 36.09 | 32.41 | 14 | 3872 | 3094 | 29945498 |
Attention deficit hyperactivity disorder | 35.37 | 32.41 | 12 | 3874 | 1812 | 29946780 |
Product administered to patient of inappropriate age | 35.11 | 32.41 | 13 | 3873 | 2530 | 29946062 |
Defiant behaviour | 33.64 | 32.41 | 5 | 3881 | 12 | 29948580 |
Priapism | 33.55 | 32.41 | 15 | 3871 | 4728 | 29943864 |
Source | Code | Description |
---|---|---|
ATC | C02AC02 | CARDIOVASCULAR SYSTEM ANTIHYPERTENSIVES ANTIADRENERGIC AGENTS, CENTRALLY ACTING Imidazoline receptor agonists |
FDA MoA | N0000009918 | Adrenergic alpha2-Agonists |
FDA EPC | N0000175554 | Central alpha-2 Adrenergic Agonist |
MeSH PA | D018663 | Adrenergic Agents |
MeSH PA | D000322 | Adrenergic Agonists |
MeSH PA | D058647 | Adrenergic alpha-2 Receptor Agonists |
MeSH PA | D000316 | Adrenergic alpha-Agonists |
MeSH PA | D000959 | Antihypertensive Agents |
MeSH PA | D002317 | Cardiovascular Agents |
MeSH PA | D018377 | Neurotransmitter Agents |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Hypertensive disorder | indication | 38341003 | DOID:10763 |
Attention deficit hyperactivity disorder | indication | 406506008 | |
Constipation | contraindication | 14760008 | DOID:2089 |
Myocardial infarction | contraindication | 22298006 | DOID:5844 |
Alcohol intoxication | contraindication | 25702006 | |
Orthostatic hypotension | contraindication | 28651003 | |
Dehydration | contraindication | 34095006 | |
Depressive disorder | contraindication | 35489007 | |
Low blood pressure | contraindication | 45007003 | |
End stage renal disease | contraindication | 46177005 | DOID:784 |
Bradycardia | contraindication | 48867003 | |
Cerebrovascular disease | contraindication | 62914000 | DOID:6713 |
Heart block | contraindication | 233916004 | |
Disease of liver | contraindication | 235856003 | DOID:409 |
Syncope | contraindication | 271594007 | |
Drowsy | contraindication | 271782001 | |
Chronic myocardial ischemia | contraindication | 413844008 | DOID:3393 |
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 11.71 | acidic |
pKa2 | 8.15 | Basic |
None
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Alpha-2A adrenergic receptor | GPCR | AGONIST | EC50 | 7.16 | WOMBAT-PK | DRUG LABEL | |||
5-hydroxytryptamine receptor 2A | GPCR | Ki | 6.06 | DRUG MATRIX | |||||
5-hydroxytryptamine receptor 2B | GPCR | Ki | 5.87 | DRUG MATRIX | |||||
5-hydroxytryptamine receptor 2C | GPCR | Ki | 6.12 | DRUG MATRIX | |||||
Alpha-1D adrenergic receptor | GPCR | Ki | 6.26 | DRUG MATRIX | |||||
Alpha-2B adrenergic receptor | GPCR | AGONIST | EC50 | 5.93 | WOMBAT-PK | ||||
Nischarin | Membrane receptor | Ki | 7.72 | CHEMBL | |||||
Alpha-2C adrenergic receptor | GPCR | AGONIST | EC50 | 5.68 | WOMBAT-PK | ||||
Alpha-1A adrenergic receptor | GPCR | IC50 | 5.87 | CHEMBL |
ID | Source |
---|---|
4019771 | VUID |
N0000147862 | NUI |
D00606 | KEGG_DRUG |
29110-48-3 | SECONDARY_CAS_RN |
4019438 | VANDF |
4019771 | VANDF |
C0079466 | UMLSCUI |
CHEBI:5558 | CHEBI |
CHEMBL862 | ChEMBL_ID |
CHEMBL1200494 | ChEMBL_ID |
DB01018 | DRUGBANK_ID |
D016316 | MESH_DESCRIPTOR_UI |
522 | IUPHAR_LIGAND_ID |
3999 | INN_ID |
30OMY4G3MK | UNII |
3519 | PUBCHEM_CID |
203142 | RXNORM |
4809 | MMSL |
521 | MMSL |
6549 | MMSL |
d00717 | MMSL |
000650 | NDDF |
004497 | NDDF |
108553003 | SNOMEDCT_US |
108554009 | SNOMEDCT_US |
372507007 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Guanfacine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0093-5960 | TABLET, EXTENDED RELEASE | 1 mg | ORAL | ANDA | 28 sections |
Guanfacine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0093-5961 | TABLET, EXTENDED RELEASE | 2 mg | ORAL | ANDA | 28 sections |
Guanfacine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0093-5963 | TABLET, EXTENDED RELEASE | 3 mg | ORAL | ANDA | 28 sections |
Guanfacine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0093-5964 | TABLET, EXTENDED RELEASE | 4 mg | ORAL | ANDA | 28 sections |
guanfacine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0228-2850 | TABLET, EXTENDED RELEASE | 1 mg | ORAL | ANDA | 28 sections |
guanfacine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0228-2851 | TABLET, EXTENDED RELEASE | 2 mg | ORAL | ANDA | 28 sections |
guanfacine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0228-2853 | TABLET, EXTENDED RELEASE | 3 mg | ORAL | ANDA | 28 sections |
guanfacine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0228-2855 | TABLET, EXTENDED RELEASE | 4 mg | ORAL | ANDA | 28 sections |
Guanfacine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-0444 | TABLET | 1 mg | ORAL | ANDA | 24 sections |
Guanfacine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-0453 | TABLET | 2 mg | ORAL | ANDA | 24 sections |
Guanfacine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 17856-0711 | TABLET | 1 mg | ORAL | ANDA | 13 sections |
Guanfacine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24658-730 | TABLET | 1 mg | ORAL | ANDA | 24 sections |
Guanfacine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24658-731 | TABLET | 2 mg | ORAL | ANDA | 24 sections |
Guanfacine Extended-Release | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24979-533 | TABLET, EXTENDED RELEASE | 1 mg | ORAL | ANDA | 27 sections |
Guanfacine Extended-Release | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24979-534 | TABLET, EXTENDED RELEASE | 2 mg | ORAL | ANDA | 27 sections |
Guanfacine Extended-Release | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24979-536 | TABLET, EXTENDED RELEASE | 3 mg | ORAL | ANDA | 27 sections |
Guanfacine Extended-Release | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24979-538 | TABLET, EXTENDED RELEASE | 4 mg | ORAL | ANDA | 27 sections |
Guanfacine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 29300-458 | TABLET | 1 mg | ORAL | ANDA | 21 sections |
Guanfacine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 29300-459 | TABLET | 2 mg | ORAL | ANDA | 21 sections |
Guanfacine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42291-310 | TABLET | 1 mg | ORAL | ANDA | 20 sections |
Guanfacine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42291-311 | TABLET | 2 mg | ORAL | ANDA | 20 sections |
guanfacine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42291-324 | TABLET, EXTENDED RELEASE | 1 mg | ORAL | ANDA | 29 sections |
guanfacine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42291-325 | TABLET, EXTENDED RELEASE | 2 mg | ORAL | ANDA | 29 sections |
guanfacine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42291-326 | TABLET, EXTENDED RELEASE | 3 mg | ORAL | ANDA | 29 sections |
guanfacine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42291-327 | TABLET, EXTENDED RELEASE | 4 mg | ORAL | ANDA | 29 sections |
Guanfacine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42806-048 | TABLET | 1 mg | ORAL | ANDA | 24 sections |
Guanfacine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42806-296 | TABLET | 2 mg | ORAL | ANDA | 24 sections |
Guanfacine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50090-4119 | TABLET | 1 mg | ORAL | ANDA | 14 sections |
Guanfacine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50268-373 | TABLET | 1 mg | ORAL | ANDA | 13 sections |
Guanfacine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50268-374 | TABLET | 2 mg | ORAL | ANDA | 13 sections |