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| 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 |
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 1.367 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 1.021 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 21.827 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 2.051 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 25.350 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 47.930 | % | High | 1 |
| herg | hERG pIC50 | 4.941 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 1.542 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 5.176 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 24.790 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT1,AKT2,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK1,CDK4,CDK5,CDK9,CHEK1,CSF1R,DDR1,DYRK1B,EGFR,EIF2AK3,EPHA2,EPHB4,ERBB2,FLT3,GRK2,GSK3B,IGF1R,IKBKB,ITK,JAK1,JAK2,JAK3,KIT,MAP2K6,MAP3K21,MAP3K7,MAP4K1,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MELK,MET,MTOR,NTRK2,PAK4,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIM2,PLK1,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ULK1,ULK2,ZAP70 | 70 | |||
| kinase-selectivity-class | AXL,BRAF,CSF1R,DDR1,EIF2AK3,EPHB4,GRK2,LYN,MAPK7,PDK4,SIK2 | 11 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 2.333 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 16.904 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 26.140 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 6.166 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 29.090 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 18.535 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 76.020 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 27.920 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 659.174 | uM | High | 1 |
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 30, 2017 | PMDA | Shionogi & Co., Ltd. | |
| Oct. 27, 1986 | FDA | PROMIUS PHARMA | |
| Sept. 17, 2015 | EMA | Takeda Pharmaceuticals International AG Ireland Branch |
| 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 |
|---|---|---|---|---|---|---|
| Intentional overdose | 208.91 | 23.74 | 97 | 4132 | 93737 | 90530481 |
| Bradycardia | 145.10 | 23.74 | 73 | 4156 | 83774 | 90540444 |
| Electrocardiogram QT prolonged | 116.33 | 23.74 | 60 | 4169 | 72396 | 90551822 |
| Product substitution issue | 111.68 | 23.74 | 39 | 4190 | 17969 | 90606249 |
| Somnolence | 107.26 | 23.74 | 84 | 4145 | 209000 | 90415218 |
| Aggression | 100.23 | 23.74 | 40 | 4189 | 26628 | 90597590 |
| Suicidal ideation | 74.27 | 23.74 | 45 | 4184 | 73810 | 90550408 |
| Overdose | 73.59 | 23.74 | 60 | 4169 | 157649 | 90466569 |
| Toxicity to various agents | 67.87 | 23.74 | 75 | 4154 | 287771 | 90336447 |
| Intentional self-injury | 67.19 | 23.74 | 31 | 4198 | 29303 | 90594915 |
| Hypotension | 65.30 | 23.74 | 78 | 4151 | 325319 | 90298899 |
| Impulsive behaviour | 63.48 | 23.74 | 15 | 4214 | 1715 | 90622503 |
| Distributive shock | 62.54 | 23.74 | 17 | 4212 | 3407 | 90620811 |
| Abnormal behaviour | 61.66 | 23.74 | 27 | 4202 | 22601 | 90601617 |
| Sinus bradycardia | 55.36 | 23.74 | 23 | 4206 | 16929 | 90607289 |
| Product administered to patient of inappropriate age | 53.05 | 23.74 | 16 | 4213 | 4637 | 90619581 |
| Bradypnoea | 53.03 | 23.74 | 16 | 4213 | 4642 | 90619576 |
| Psychomotor hyperactivity | 47.36 | 23.74 | 19 | 4210 | 12794 | 90611424 |
| Blood pressure decreased | 44.69 | 23.74 | 33 | 4196 | 74862 | 90549356 |
| Suicide attempt | 42.26 | 23.74 | 32 | 4197 | 75367 | 90548851 |
| Self-destructive behaviour | 38.88 | 23.74 | 8 | 4221 | 483 | 90623735 |
| Cerebral disorder | 37.86 | 23.74 | 13 | 4216 | 5681 | 90618537 |
| Off label use | 37.19 | 23.74 | 124 | 4105 | 1102128 | 89522090 |
| Coma | 34.59 | 23.74 | 28 | 4201 | 72604 | 90551614 |
| Irritability | 33.95 | 23.74 | 21 | 4208 | 35641 | 90588577 |
| Atrioventricular dissociation | 31.84 | 23.74 | 6 | 4223 | 229 | 90623989 |
| Sinus arrhythmia | 30.26 | 23.74 | 8 | 4221 | 1441 | 90622777 |
| Syncope | 30.20 | 23.74 | 34 | 4195 | 132629 | 90491589 |
| Attention deficit hyperactivity disorder | 29.57 | 23.74 | 10 | 4219 | 4174 | 90620044 |
| Sedation | 28.22 | 23.74 | 21 | 4208 | 48150 | 90576068 |
| Upper airway obstruction | 27.91 | 23.74 | 7 | 4222 | 1025 | 90623193 |
| Educational problem | 26.51 | 23.74 | 6 | 4223 | 567 | 90623651 |
| Orthostatic hypotension | 23.97 | 23.74 | 18 | 4211 | 41809 | 90582409 |
| Anger | 23.83 | 23.74 | 12 | 4217 | 13708 | 90610510 |
| 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 |
|---|---|---|---|---|---|---|
| Aggression | 335.69 | 29.14 | 159 | 7079 | 44004 | 42570093 |
| Product substitution issue | 326.03 | 29.14 | 107 | 7131 | 11183 | 42602914 |
| Agitation | 151.04 | 29.14 | 108 | 7130 | 64206 | 42549891 |
| Psychomotor hyperactivity | 140.13 | 29.14 | 57 | 7181 | 10901 | 42603196 |
| Abnormal behaviour | 129.79 | 29.14 | 71 | 7167 | 26380 | 42587717 |
| Bradycardia | 119.84 | 29.14 | 106 | 7132 | 85378 | 42528719 |
| Tic | 117.14 | 29.14 | 34 | 7204 | 2349 | 42611748 |
| Irritability | 112.35 | 29.14 | 66 | 7172 | 28062 | 42586035 |
| Somnolence | 104.49 | 29.14 | 124 | 7114 | 140981 | 42473116 |
| Impulsive behaviour | 103.43 | 29.14 | 31 | 7207 | 2394 | 42611703 |
| Electrocardiogram QT prolonged | 102.22 | 29.14 | 76 | 7162 | 47869 | 42566228 |
| Autism spectrum disorder | 88.89 | 29.14 | 29 | 7209 | 2959 | 42611138 |
| Dystonia | 78.80 | 29.14 | 40 | 7198 | 12750 | 42601347 |
| Intentional overdose | 72.39 | 29.14 | 64 | 7174 | 51392 | 42562705 |
| Drug ineffective | 72.32 | 29.14 | 252 | 6986 | 629945 | 41984152 |
| Anger | 66.74 | 29.14 | 36 | 7202 | 12982 | 42601115 |
| Sinus bradycardia | 59.65 | 29.14 | 35 | 7203 | 14818 | 42599279 |
| Insomnia | 59.47 | 29.14 | 86 | 7152 | 118167 | 42495930 |
| Suicidal ideation | 56.25 | 29.14 | 54 | 7184 | 48107 | 42565990 |
| Educational problem | 55.56 | 29.14 | 14 | 7224 | 564 | 42613533 |
| Attention deficit hyperactivity disorder | 49.64 | 29.14 | 19 | 7219 | 3089 | 42611008 |
| Product use issue | 49.47 | 29.14 | 63 | 7175 | 76688 | 42537409 |
| Disturbance in attention | 45.71 | 29.14 | 39 | 7199 | 29827 | 42584270 |
| Emotional disorder | 45.57 | 29.14 | 22 | 7216 | 6292 | 42607805 |
| Product administered to patient of inappropriate age | 45 | 29.14 | 20 | 7218 | 4741 | 42609356 |
| Brugada syndrome | 42.91 | 29.14 | 13 | 7225 | 1040 | 42613057 |
| Sedation | 41.03 | 29.14 | 37 | 7201 | 30438 | 42583659 |
| Oromandibular dystonia | 40.32 | 29.14 | 11 | 7227 | 605 | 42613492 |
| Product availability issue | 40.31 | 29.14 | 17 | 7221 | 3550 | 42610547 |
| Negativism | 39.25 | 29.14 | 10 | 7228 | 421 | 42613676 |
| Distractibility | 38.56 | 29.14 | 10 | 7228 | 452 | 42613645 |
| Hypertensive urgency | 38.16 | 29.14 | 10 | 7228 | 471 | 42613626 |
| Acute kidney injury | 38.16 | 29.14 | 8 | 7230 | 367329 | 42246768 |
| Accidental exposure to product by child | 37.83 | 29.14 | 13 | 7225 | 1554 | 42612543 |
| Nephrogenic diabetes insipidus | 37.78 | 29.14 | 13 | 7225 | 1561 | 42612536 |
| Behaviour disorder | 37.53 | 29.14 | 20 | 7218 | 7034 | 42607063 |
| Product quality issue | 37.28 | 29.14 | 28 | 7210 | 17854 | 42596243 |
| Intentional self-injury | 36.67 | 29.14 | 26 | 7212 | 15176 | 42598921 |
| Self-destructive behaviour | 35.39 | 29.14 | 9 | 7229 | 376 | 42613721 |
| Affect lability | 35.08 | 29.14 | 16 | 7222 | 4028 | 42610069 |
| Anxiety | 35.06 | 29.14 | 68 | 7170 | 118492 | 42495605 |
| Sinus arrest | 33.78 | 29.14 | 13 | 7225 | 2143 | 42611954 |
| Product dose omission issue | 33.45 | 29.14 | 78 | 7160 | 154287 | 42459810 |
| No adverse event | 33.32 | 29.14 | 37 | 7201 | 38984 | 42575113 |
| Withdrawal syndrome | 32.74 | 29.14 | 24 | 7214 | 14751 | 42599346 |
| Electrocardiogram QRS complex prolonged | 32.36 | 29.14 | 17 | 7221 | 5806 | 42608291 |
| Disturbance in social behaviour | 32.34 | 29.14 | 12 | 7226 | 1791 | 42612306 |
| Affective disorder | 31.99 | 29.14 | 17 | 7221 | 5943 | 42608154 |
| Death | 31.17 | 29.14 | 21 | 7217 | 471164 | 42142933 |
| Defiant behaviour | 30.36 | 29.14 | 5 | 7233 | 20 | 42614077 |
| Drug dose titration not performed | 29.93 | 29.14 | 8 | 7230 | 407 | 42613690 |
| 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 |
|---|---|---|---|---|---|---|
| Aggression | 415.65 | 23.40 | 167 | 9743 | 59043 | 110520346 |
| Product substitution issue | 362.04 | 23.40 | 118 | 9792 | 22943 | 110556446 |
| Bradycardia | 265.38 | 23.40 | 168 | 9742 | 155349 | 110424040 |
| Intentional overdose | 261.31 | 23.40 | 157 | 9753 | 132344 | 110447045 |
| Electrocardiogram QT prolonged | 235.44 | 23.40 | 137 | 9773 | 108823 | 110470566 |
| Psychomotor hyperactivity | 165.96 | 23.40 | 64 | 9846 | 20213 | 110559176 |
| Somnolence | 163.42 | 23.40 | 165 | 9745 | 297284 | 110282105 |
| Agitation | 158.21 | 23.40 | 108 | 9802 | 112943 | 110466446 |
| Impulsive behaviour | 156.49 | 23.40 | 40 | 9870 | 3275 | 110576114 |
| Abnormal behaviour | 143.46 | 23.40 | 70 | 9840 | 38969 | 110540420 |
| Irritability | 141.37 | 23.40 | 74 | 9836 | 47735 | 110531654 |
| Tic | 125.76 | 23.40 | 34 | 9876 | 3459 | 110575930 |
| Sinus bradycardia | 111.72 | 23.40 | 54 | 9856 | 29429 | 110549960 |
| Suicidal ideation | 111.08 | 23.40 | 81 | 9829 | 93856 | 110485533 |
| Autism spectrum disorder | 99.31 | 23.40 | 25 | 9885 | 1923 | 110577466 |
| Overdose | 98.81 | 23.40 | 113 | 9797 | 233681 | 110345708 |
| Intentional self-injury | 85.86 | 23.40 | 49 | 9861 | 37380 | 110542009 |
| Hypotension | 85.03 | 23.40 | 161 | 9749 | 523688 | 110055701 |
| Toxicity to various agents | 84.65 | 23.40 | 153 | 9757 | 480402 | 110098987 |
| Educational problem | 76.64 | 23.40 | 16 | 9894 | 532 | 110578857 |
| Anger | 75.60 | 23.40 | 36 | 9874 | 18971 | 110560418 |
| Product administered to patient of inappropriate age | 71.61 | 23.40 | 27 | 9883 | 8009 | 110571380 |
| Dystonia | 65.20 | 23.40 | 36 | 9874 | 25769 | 110553620 |
| Sedation | 58.28 | 23.40 | 49 | 9861 | 69634 | 110509755 |
| Attention deficit hyperactivity disorder | 54.66 | 23.40 | 19 | 9891 | 4472 | 110574917 |
| Blood pressure decreased | 52.59 | 23.40 | 58 | 9852 | 115033 | 110464356 |
| Bradypnoea | 52.41 | 23.40 | 22 | 9888 | 8627 | 110570762 |
| Drug ineffective | 51.13 | 23.40 | 269 | 9641 | 1520271 | 109059118 |
| Drug interaction | 50.44 | 23.40 | 127 | 9783 | 500056 | 110079333 |
| Lethargy | 49.55 | 23.40 | 51 | 9859 | 93525 | 110485864 |
| Self-destructive behaviour | 48.73 | 23.40 | 12 | 9898 | 843 | 110578546 |
| Accidental exposure to product by child | 48.66 | 23.40 | 16 | 9894 | 3182 | 110576207 |
| Brugada syndrome | 45.84 | 23.40 | 13 | 9897 | 1575 | 110577814 |
| Hyperammonaemia | 45.60 | 23.40 | 23 | 9887 | 13709 | 110565680 |
| Suicide attempt | 45.34 | 23.40 | 51 | 9859 | 103343 | 110476046 |
| Nephrogenic diabetes insipidus | 44.43 | 23.40 | 14 | 9896 | 2431 | 110576958 |
| Disturbance in attention | 42.62 | 23.40 | 39 | 9871 | 61956 | 110517433 |
| Product dose omission issue | 42.61 | 23.40 | 91 | 9819 | 321691 | 110257698 |
| Distributive shock | 42.53 | 23.40 | 17 | 9893 | 5887 | 110573502 |
| Syncope | 41.43 | 23.40 | 69 | 9841 | 202467 | 110376922 |
| Behaviour disorder | 40.59 | 23.40 | 19 | 9891 | 9628 | 110569761 |
| Oromandibular dystonia | 39.85 | 23.40 | 11 | 9899 | 1208 | 110578181 |
| Affective disorder | 37.83 | 23.40 | 19 | 9891 | 11222 | 110568167 |
| Off label use | 37.72 | 23.40 | 246 | 9664 | 1499939 | 109079450 |
| Mood swings | 37.18 | 23.40 | 24 | 9886 | 22788 | 110556601 |
| Withdrawal syndrome | 36.91 | 23.40 | 27 | 9883 | 31353 | 110548036 |
| Emotional disorder | 36.63 | 23.40 | 21 | 9889 | 16139 | 110563250 |
| Priapism | 35.82 | 23.40 | 15 | 9895 | 5846 | 110573543 |
| Hypertensive urgency | 35.80 | 23.40 | 10 | 9900 | 1147 | 110578242 |
| Device mechanical issue | 34.34 | 23.40 | 11 | 9899 | 2013 | 110577376 |
| Pain | 33.90 | 23.40 | 22 | 9888 | 954933 | 109624456 |
| Distractibility | 33.51 | 23.40 | 9 | 9901 | 892 | 110578497 |
| Sinus arrest | 33.31 | 23.40 | 13 | 9897 | 4229 | 110575160 |
| Insomnia | 32.64 | 23.40 | 88 | 9822 | 360502 | 110218887 |
| Seizure | 32.12 | 23.40 | 65 | 9845 | 221120 | 110358269 |
| Homicidal ideation | 31.64 | 23.40 | 12 | 9898 | 3615 | 110575774 |
| Disturbance in social behaviour | 31.09 | 23.40 | 13 | 9897 | 5045 | 110574344 |
| Anaemia | 30.52 | 23.40 | 6 | 9904 | 547080 | 110032309 |
| Completed suicide | 30.30 | 23.40 | 67 | 9843 | 242314 | 110337075 |
| Atrioventricular dissociation | 30.07 | 23.40 | 7 | 9903 | 387 | 110579002 |
| Tachycardia | 29.86 | 23.40 | 64 | 9846 | 226581 | 110352808 |
| Electrocardiogram QRS complex prolonged | 29.72 | 23.40 | 17 | 9893 | 13004 | 110566385 |
| Orthostatic hypotension | 29.58 | 23.40 | 33 | 9877 | 66216 | 110513173 |
| Joint swelling | 29.01 | 23.40 | 3 | 9907 | 442842 | 110136547 |
| Arrhythmia | 28.26 | 23.40 | 33 | 9877 | 69542 | 110509847 |
| Oppositional defiant disorder | 28.16 | 23.40 | 7 | 9903 | 511 | 110578878 |
| Respiratory depression | 27.77 | 23.40 | 23 | 9887 | 31978 | 110547411 |
| Defiant behaviour | 27.62 | 23.40 | 5 | 9905 | 77 | 110579312 |
| Drug dose titration not performed | 27.53 | 23.40 | 8 | 9902 | 1057 | 110578332 |
| Cerebral disorder | 27.35 | 23.40 | 13 | 9897 | 6813 | 110572576 |
| Gaming disorder | 27.05 | 23.40 | 4 | 9906 | 15 | 110579374 |
| Hallucination | 26.94 | 23.40 | 39 | 9871 | 101393 | 110477996 |
| Restlessness | 26.81 | 23.40 | 29 | 9881 | 56230 | 110523159 |
| Depressed level of consciousness | 26.71 | 23.40 | 41 | 9869 | 112237 | 110467152 |
| No adverse event | 26.68 | 23.40 | 33 | 9877 | 73806 | 110505583 |
| Presyncope | 26.51 | 23.40 | 27 | 9883 | 48860 | 110530529 |
| Arthralgia | 26.26 | 23.40 | 19 | 9891 | 779613 | 109799776 |
| Self-injurious ideation | 26.15 | 23.40 | 11 | 9899 | 4335 | 110575054 |
| Disruptive mood dysregulation disorder | 25.80 | 23.40 | 4 | 9906 | 22 | 110579367 |
| Sinus arrhythmia | 25.71 | 23.40 | 9 | 9901 | 2161 | 110577228 |
| Wrong technique in product usage process | 25.29 | 23.40 | 35 | 9875 | 87313 | 110492076 |
| Coma | 25.22 | 23.40 | 41 | 9869 | 117828 | 110461561 |
| Activation syndrome | 25.07 | 23.40 | 6 | 9904 | 374 | 110579015 |
| Mania | 24.70 | 23.40 | 18 | 9892 | 20778 | 110558611 |
| Anxiety | 24.28 | 23.40 | 77 | 9833 | 345001 | 110234388 |
| Diarrhoea | 23.89 | 23.40 | 41 | 9869 | 1139464 | 109439925 |
| Obsessive-compulsive disorder | 23.66 | 23.40 | 12 | 9898 | 7229 | 110572160 |
| Accidental overdose | 23.45 | 23.40 | 26 | 9884 | 51808 | 110527581 |
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:35469 | antidepressant |
| CHEBI has role | CHEBI:35674 | antihypertensive agent |
| CHEBI has role | CHEBI:176497 | geroprotector |
| MeSH PA | D000316 | Adrenergic alpha-Agonists |
| MeSH PA | D000959 | Antihypertensive Agents |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018663 | Adrenergic Agents |
| MeSH PA | D058647 | Adrenergic alpha-2 Receptor Agonists |
| 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 |
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 2B | GPCR | Ki | 5.88 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 2C | GPCR | Ki | 6.12 | DRUG MATRIX | |||||
| Alpha-1A adrenergic receptor | GPCR | Ki | 5.33 | CHEMBL | |||||
| 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 |
| 30OMY4G3MK | INXIGHT DRUGS |
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| 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 Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24979-198 | TABLET | 1 mg | ORAL | ANDA | 13 sections |
| Guanfacine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24979-199 | TABLET | 2 mg | ORAL | ANDA | 13 sections |
| Guanfacine Extended-Release | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24979-533 | TABLET, EXTENDED RELEASE | 1 mg | ORAL | ANDA | 28 sections |
| Guanfacine Extended-Release | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24979-534 | TABLET, EXTENDED RELEASE | 2 mg | ORAL | ANDA | 28 sections |
| Guanfacine Extended-Release | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24979-536 | TABLET, EXTENDED RELEASE | 3 mg | ORAL | ANDA | 28 sections |
| Guanfacine Extended-Release | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24979-538 | TABLET, EXTENDED RELEASE | 4 mg | ORAL | ANDA | 28 sections |
| Guanfacine | Human Prescription Drug Label | 1 | 27241-242 | TABLET | 1 mg | ORAL | ANDA | 10 sections |
| Guanfacine | Human Prescription Drug Label | 1 | 27241-243 | TABLET | 2 mg | ORAL | ANDA | 10 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 | HUMAN PRESCRIPTION DRUG LABEL | 1 | 29300-460 | TABLET, EXTENDED RELEASE | 1 mg | ORAL | ANDA | 26 sections |
| Guanfacine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 29300-461 | TABLET, EXTENDED RELEASE | 2 mg | ORAL | ANDA | 26 sections |
| Guanfacine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 29300-462 | TABLET, EXTENDED RELEASE | 3 mg | ORAL | ANDA | 26 sections |
| Guanfacine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 29300-463 | TABLET, EXTENDED RELEASE | 4 mg | ORAL | ANDA | 26 sections |
| Guanfacine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42291-310 | TABLET | 1 mg | ORAL | ANDA | 13 sections |
| guanfacine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42291-324 | TABLET, EXTENDED RELEASE | 1 mg | ORAL | ANDA | 29 sections |