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 ยตM/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 | 126.72 | 26.41 | 39 | 2014 | 14018 | 50589053 |
Aggression | 81.33 | 26.41 | 31 | 2022 | 21085 | 50581986 |
Somnolence | 62.54 | 26.41 | 51 | 2002 | 154934 | 50448137 |
Abnormal behaviour | 51.89 | 26.41 | 22 | 2031 | 19636 | 50583435 |
Impulsive behaviour | 51.85 | 26.41 | 12 | 2041 | 1446 | 50601625 |
Intentional overdose | 49.34 | 26.41 | 31 | 2022 | 62473 | 50540598 |
Psychomotor hyperactivity | 44.39 | 26.41 | 16 | 2037 | 9285 | 50593786 |
Suicidal ideation | 42.53 | 26.41 | 27 | 2026 | 55358 | 50547713 |
Product administered to patient of inappropriate age | 40.13 | 26.41 | 11 | 2042 | 2619 | 50600452 |
Bradycardia | 36.48 | 26.41 | 26 | 2027 | 64400 | 50538671 |
Atrioventricular dissociation | 32.92 | 26.41 | 6 | 2047 | 220 | 50602851 |
Irritability | 32.68 | 26.41 | 18 | 2035 | 28408 | 50574663 |
Educational problem | 29.82 | 26.41 | 6 | 2047 | 373 | 50602698 |
Sinus arrhythmia | 26.92 | 26.41 | 7 | 2046 | 1362 | 50601709 |
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 | 354.58 | 31.33 | 105 | 4255 | 9067 | 29561100 |
Aggression | 246.83 | 31.33 | 115 | 4245 | 35426 | 29534741 |
Agitation | 121.64 | 31.33 | 82 | 4278 | 51222 | 29518945 |
Psychomotor hyperactivity | 115.51 | 31.33 | 44 | 4316 | 8169 | 29561998 |
Abnormal behaviour | 112.97 | 31.33 | 59 | 4301 | 23068 | 29547099 |
Irritability | 101.06 | 31.33 | 54 | 4306 | 22098 | 29548069 |
Tic | 93.05 | 31.33 | 26 | 4334 | 1809 | 29568358 |
Impulsive behaviour | 87.08 | 31.33 | 25 | 4335 | 1918 | 29568249 |
Somnolence | 80.01 | 31.33 | 83 | 4277 | 93872 | 29476295 |
Drug ineffective | 79.19 | 31.33 | 168 | 4192 | 363002 | 29207165 |
Bradycardia | 68.84 | 31.33 | 65 | 4295 | 65564 | 29504603 |
Anger | 56.62 | 31.33 | 29 | 4331 | 10861 | 29559306 |
Educational problem | 53.66 | 31.33 | 13 | 4347 | 514 | 29569653 |
Dystonia | 50.79 | 31.33 | 26 | 4334 | 9723 | 29560444 |
Disturbance in attention | 50.06 | 31.33 | 34 | 4326 | 21390 | 29548777 |
Brugada syndrome | 49.97 | 31.33 | 13 | 4347 | 688 | 29569479 |
Insomnia | 44.71 | 31.33 | 60 | 4300 | 88701 | 29481466 |
Negativism | 42.05 | 31.33 | 10 | 4350 | 365 | 29569802 |
Product quality issue | 41.41 | 31.33 | 27 | 4333 | 15868 | 29554299 |
Sinus bradycardia | 41.16 | 31.33 | 24 | 4336 | 11579 | 29558588 |
Emotional disorder | 40.53 | 31.33 | 18 | 4342 | 4913 | 29565254 |
Suicidal ideation | 39.46 | 31.33 | 36 | 4324 | 34680 | 29535487 |
Attention deficit hyperactivity disorder | 38.95 | 31.33 | 14 | 4346 | 2203 | 29567964 |
Affective disorder | 37.73 | 31.33 | 15 | 4345 | 3111 | 29567056 |
Sinus arrest | 36.59 | 31.33 | 12 | 4348 | 1435 | 29568732 |
Product administered to patient of inappropriate age | 36.49 | 31.33 | 14 | 4346 | 2641 | 29567526 |
Defiant behaviour | 36.18 | 31.33 | 5 | 4355 | 4 | 29570163 |
Anxiety | 35.98 | 31.33 | 53 | 4307 | 85312 | 29484855 |
Hallucination | 35.27 | 31.33 | 38 | 4322 | 44674 | 29525493 |
Disturbance in social behaviour | 34.68 | 31.33 | 12 | 4348 | 1690 | 29568477 |
Drug dose titration not performed | 34.65 | 31.33 | 8 | 4352 | 256 | 29569911 |
Autism spectrum disorder | 32.60 | 31.33 | 12 | 4348 | 2020 | 29568147 |
Priapism | 32.50 | 31.33 | 15 | 4345 | 4473 | 29565694 |
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 | 389.67 | 24.47 | 116 | 5368 | 17745 | 64475503 |
Aggression | 305.76 | 24.47 | 123 | 5361 | 46109 | 64447139 |
Psychomotor hyperactivity | 140.48 | 24.47 | 51 | 5433 | 14400 | 64478848 |
Impulsive behaviour | 131.73 | 24.47 | 33 | 5451 | 2630 | 64490618 |
Abnormal behaviour | 122.75 | 24.47 | 59 | 5425 | 33563 | 64459685 |
Agitation | 114.85 | 24.47 | 79 | 5405 | 88288 | 64404960 |
Irritability | 111.91 | 24.47 | 57 | 5427 | 36689 | 64456559 |
Bradycardia | 98.54 | 24.47 | 81 | 5403 | 118138 | 64375110 |
Tic | 98.05 | 24.47 | 26 | 5458 | 2593 | 64490655 |
Somnolence | 86.31 | 24.47 | 96 | 5388 | 203549 | 64289699 |
Educational problem | 76.24 | 24.47 | 15 | 5469 | 389 | 64492859 |
Suicidal ideation | 60.45 | 24.47 | 48 | 5436 | 66494 | 64426754 |
Anger | 58.54 | 24.47 | 28 | 5456 | 15713 | 64477535 |
Intentional overdose | 55.51 | 24.47 | 52 | 5432 | 89892 | 64403356 |
Brugada syndrome | 51.52 | 24.47 | 13 | 5471 | 1065 | 64492183 |
Disturbance in attention | 46.95 | 24.47 | 34 | 5450 | 41040 | 64452208 |
Sinus bradycardia | 46.01 | 24.47 | 27 | 5457 | 22866 | 64470382 |
Electrocardiogram QT prolonged | 45.33 | 24.47 | 44 | 5440 | 79404 | 64413844 |
Hypotension | 44.40 | 24.47 | 99 | 5385 | 380875 | 64112373 |
Priapism | 42.27 | 24.47 | 15 | 5469 | 3955 | 64489293 |
Dystonia | 39.90 | 24.47 | 23 | 5461 | 18842 | 64474406 |
Mood swings | 38.82 | 24.47 | 22 | 5462 | 17446 | 64475802 |
Autism spectrum disorder | 38.37 | 24.47 | 10 | 5474 | 931 | 64492317 |
Defiant behaviour | 37.09 | 24.47 | 5 | 5479 | 8 | 64493240 |
Product administered to patient of inappropriate age | 36.49 | 24.47 | 14 | 5470 | 4587 | 64488661 |
Drug ineffective | 36.36 | 24.47 | 154 | 5330 | 840093 | 63653155 |
Sedation | 35.70 | 24.47 | 29 | 5455 | 41433 | 64451815 |
Attention deficit hyperactivity disorder | 35.42 | 24.47 | 12 | 5472 | 2758 | 64490490 |
Disturbance in social behaviour | 35.08 | 24.47 | 13 | 5471 | 3874 | 64489374 |
Affective disorder | 34.91 | 24.47 | 15 | 5469 | 6565 | 64486683 |
Product quality issue | 34.81 | 24.47 | 25 | 5459 | 29774 | 64463474 |
Sinus arrest | 34.13 | 24.47 | 12 | 5472 | 3078 | 64490170 |
Overdose | 32.93 | 24.47 | 53 | 5431 | 159513 | 64333735 |
Insomnia | 32.02 | 24.47 | 59 | 5425 | 197777 | 64295471 |
Drug dose titration not performed | 31.47 | 24.47 | 8 | 5476 | 675 | 64492573 |
Emotional disorder | 31.08 | 24.47 | 17 | 5467 | 12590 | 64480658 |
Hallucination | 30.18 | 24.47 | 34 | 5450 | 72754 | 64420494 |
Homicidal ideation | 29.79 | 24.47 | 11 | 5473 | 3246 | 64490002 |
Hyperammonaemia | 29.06 | 24.47 | 15 | 5469 | 9889 | 64483359 |
Tachycardia | 28.59 | 24.47 | 48 | 5436 | 149531 | 64343717 |
Lethargy | 26.90 | 24.47 | 32 | 5452 | 72562 | 64420686 |
Atrioventricular dissociation | 26.31 | 24.47 | 6 | 5478 | 319 | 64492929 |
None
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 |
CHEBI has role | CHEBI:176497 | geroprotectors |
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 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 11.71 | acidic |
pKa2 | 8.15 | Basic |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
---|---|---|---|---|---|---|---|---|---|---|
EQ 1MG BASE | INTUNIV | TAKEDA PHARMS USA | N022037 | Sept. 2, 2009 | RX | TABLET, EXTENDED RELEASE | ORAL | 6811794 | July 4, 2022 | TREATMENT OF ATTENTION-DEFICIT HYPERACTIVITY DISORDER |
EQ 2MG BASE | INTUNIV | TAKEDA PHARMS USA | N022037 | Sept. 2, 2009 | RX | TABLET, EXTENDED RELEASE | ORAL | 6811794 | July 4, 2022 | TREATMENT OF ATTENTION-DEFICIT HYPERACTIVITY DISORDER |
EQ 3MG BASE | INTUNIV | TAKEDA PHARMS USA | N022037 | Sept. 2, 2009 | RX | TABLET, EXTENDED RELEASE | ORAL | 6811794 | July 4, 2022 | TREATMENT OF ATTENTION-DEFICIT HYPERACTIVITY DISORDER |
EQ 4MG BASE | INTUNIV | TAKEDA PHARMS USA | N022037 | Sept. 2, 2009 | RX | TABLET, EXTENDED RELEASE | ORAL | 6811794 | July 4, 2022 | TREATMENT OF ATTENTION-DEFICIT HYPERACTIVITY DISORDER |
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 2B | GPCR | Ki | 5.88 | DRUG MATRIX | |||||
5-hydroxytryptamine receptor 2C | GPCR | Ki | 6.12 | DRUG MATRIX | |||||
Alpha-2B adrenergic receptor | GPCR | AGONIST | EC50 | 5.93 | WOMBAT-PK | ||||
5-hydroxytryptamine receptor 2A | GPCR | Ki | 6.07 | DRUG MATRIX | |||||
Alpha-1D adrenergic receptor | GPCR | Ki | 6.26 | DRUG MATRIX | |||||
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 |
DB01018 | DRUGBANK_ID |
CHEMBL1200494 | ChEMBL_ID |
D016316 | MESH_DESCRIPTOR_UI |
3519 | PUBCHEM_CID |
522 | IUPHAR_LIGAND_ID |
3999 | INN_ID |
30OMY4G3MK | UNII |
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 | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0904-7140 | TABLET | 1 mg | ORAL | ANDA | 24 sections |
Guanfacine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16714-190 | TABLET, EXTENDED RELEASE | 1 mg | ORAL | ANDA | 28 sections |
Guanfacine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16714-191 | TABLET, EXTENDED RELEASE | 2 mg | ORAL | ANDA | 28 sections |
Guanfacine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16714-192 | TABLET, EXTENDED RELEASE | 3 mg | ORAL | ANDA | 28 sections |
Guanfacine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16714-193 | TABLET, EXTENDED RELEASE | 4 mg | ORAL | ANDA | 28 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 | 42291-310 | 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 |