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labetalol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| aromatic ring -CH(-OH)-CH2-NH-R | 1531 | 36894-69-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A salicylamide derivative that is a non-cardioselective blocker of BETA-ADRENERGIC RECEPTORS and ALPHA-1 ADRENERGIC RECEPTORS.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.60 | g | O |
| 0.60 | g | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 16 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 2.50 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 104.53 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 25 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 4.80 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 23 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.50 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 4.40 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 1.176 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 7.447 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 6.808 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 8.222 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 35.520 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 45.350 | % | High | 1 |
| herg | hERG pIC50 | 4.919 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 8.375 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 23.878 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 40.230 | % | High | 1 |
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 5.212 | High | 1 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 8.790 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 92.897 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 40.500 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 17.947 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 0 | High | 1 | |
| pppb | Pig plasma protein binding (% unbound) | 48.960 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 0.025 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 84.528 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 77.970 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 38.740 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 907.821 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 1, 1984 | FDA | CNTY LINE PHARMS |
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 |
|---|---|---|---|---|---|---|
| Maternal exposure during pregnancy | 386.16 | 16.37 | 288 | 7607 | 359775 | 90260777 |
| Premature delivery | 386.03 | 16.37 | 140 | 7755 | 38622 | 90581930 |
| Exposure during pregnancy | 262.16 | 16.37 | 194 | 7701 | 238216 | 90382336 |
| Pre-eclampsia | 239.96 | 16.37 | 72 | 7823 | 10976 | 90609576 |
| Premature baby | 164.81 | 16.37 | 67 | 7828 | 25010 | 90595542 |
| Foetal growth restriction | 128.35 | 16.37 | 43 | 7852 | 9337 | 90611215 |
| Blood pressure inadequately controlled | 124.12 | 16.37 | 38 | 7857 | 6186 | 90614366 |
| Exercise tolerance decreased | 112.84 | 16.37 | 37 | 7858 | 7514 | 90613038 |
| Caesarean section | 109.72 | 16.37 | 46 | 7849 | 18531 | 90602021 |
| Foetal exposure during pregnancy | 102.13 | 16.37 | 57 | 7838 | 42918 | 90577634 |
| Low birth weight baby | 89.64 | 16.37 | 33 | 7862 | 9434 | 90611118 |
| Diabetes mellitus inadequate control | 86.60 | 16.37 | 39 | 7856 | 18645 | 90601907 |
| Multiple drug therapy | 83.62 | 16.37 | 29 | 7866 | 6980 | 90613572 |
| Treatment noncompliance | 56.35 | 16.37 | 42 | 7853 | 51685 | 90568867 |
| Depressed mood | 52.97 | 16.37 | 40 | 7855 | 50182 | 90570370 |
| Patent ductus arteriosus | 51.03 | 16.37 | 18 | 7877 | 4551 | 90616001 |
| Neonatal respiratory distress | 46.39 | 16.37 | 11 | 7884 | 678 | 90619874 |
| Haemangioma congenital | 43.36 | 16.37 | 10 | 7885 | 546 | 90620006 |
| Medication error | 40.27 | 16.37 | 43 | 7852 | 84609 | 90535943 |
| Cognitive disorder | 39.82 | 16.37 | 39 | 7856 | 69368 | 90551184 |
| Superimposed pre-eclampsia | 39.51 | 16.37 | 6 | 7889 | 29 | 90620523 |
| Premature labour | 32.46 | 16.37 | 18 | 7877 | 13358 | 90607194 |
| Subacute cutaneous lupus erythematosus | 32.12 | 16.37 | 12 | 7883 | 3570 | 90616982 |
| Amnesia | 31.67 | 16.37 | 43 | 7852 | 108462 | 90512090 |
| Neonatal respiratory distress syndrome | 30.05 | 16.37 | 11 | 7884 | 3090 | 90617462 |
| Stillbirth | 29.67 | 16.37 | 14 | 7881 | 7429 | 90613123 |
| Hyperkalaemia | 29.14 | 16.37 | 32 | 7863 | 64932 | 90555620 |
| Pulmonary oedema | 28.58 | 16.37 | 31 | 7864 | 62049 | 90558503 |
| Drug intolerance | 28.38 | 16.37 | 3 | 7892 | 447588 | 90172964 |
| Maternal exposure during delivery | 27.75 | 16.37 | 11 | 7884 | 3835 | 90616717 |
| Oligohydramnios | 27.04 | 16.37 | 13 | 7882 | 7188 | 90613364 |
| Infusion related reaction | 25.90 | 16.37 | 3 | 7892 | 416777 | 90203775 |
| Oedema peripheral | 25.57 | 16.37 | 64 | 7831 | 257851 | 90362701 |
| Gestational diabetes | 25.02 | 16.37 | 14 | 7881 | 10568 | 90609984 |
| Drug ineffective | 24.29 | 16.37 | 204 | 7691 | 1384094 | 89236458 |
| Peptic ulcer perforation | 24.12 | 16.37 | 6 | 7889 | 452 | 90620100 |
| Eclampsia | 23.62 | 16.37 | 6 | 7889 | 492 | 90620060 |
| Renal tubular necrosis | 23.34 | 16.37 | 15 | 7880 | 14540 | 90606012 |
| Proteinuria | 23.34 | 16.37 | 18 | 7877 | 23273 | 90597279 |
| Foetal death | 22.94 | 16.37 | 17 | 7878 | 20706 | 90599846 |
| HELLP syndrome | 22.44 | 16.37 | 7 | 7888 | 1210 | 90619342 |
| Completed suicide | 22.35 | 16.37 | 43 | 7852 | 145015 | 90475537 |
| Ultrasound uterus abnormal | 21.84 | 16.37 | 4 | 7891 | 68 | 90620484 |
| Blood pressure increased | 21.74 | 16.37 | 51 | 7844 | 197166 | 90423386 |
| Dilatation intrahepatic duct acquired | 21.05 | 16.37 | 6 | 7889 | 762 | 90619790 |
| Phaeochromocytoma crisis | 20.22 | 16.37 | 5 | 7890 | 368 | 90620184 |
| Abortion spontaneous | 19.82 | 16.37 | 24 | 7871 | 54032 | 90566520 |
| Live birth | 19.60 | 16.37 | 29 | 7866 | 79078 | 90541474 |
| Systemic lupus erythematosus | 19.32 | 16.37 | 4 | 7891 | 361892 | 90258660 |
| Joint swelling | 19.14 | 16.37 | 10 | 7885 | 503290 | 90117262 |
| Cerebral haemorrhage | 19.05 | 16.37 | 19 | 7876 | 34503 | 90586049 |
| Hypoglycaemia neonatal | 18.80 | 16.37 | 6 | 7889 | 1116 | 90619436 |
| Post transplant lymphoproliferative disorder | 18.66 | 16.37 | 10 | 7885 | 6939 | 90613613 |
| Hypermagnesaemia | 18.17 | 16.37 | 6 | 7889 | 1243 | 90619309 |
| Drug withdrawal syndrome neonatal | 18.02 | 16.37 | 7 | 7888 | 2312 | 90618240 |
| Lipid metabolism disorder | 17.97 | 16.37 | 4 | 7891 | 186 | 90620366 |
| Thymus hypoplasia | 17.77 | 16.37 | 3 | 7892 | 31 | 90620521 |
| Phaeochromocytoma | 17.72 | 16.37 | 5 | 7890 | 612 | 90619940 |
| Arthropathy | 17.68 | 16.37 | 5 | 7890 | 366237 | 90254315 |
| Hepatic enzyme increased | 17.28 | 16.37 | 5 | 7890 | 360731 | 90259821 |
| Pregnancy | 17.20 | 16.37 | 24 | 7871 | 62023 | 90558529 |
| Beta 2 microglobulin increased | 16.60 | 16.37 | 4 | 7891 | 264 | 90620288 |
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 |
|---|---|---|---|---|---|---|
| Premature baby | 252.08 | 21.98 | 93 | 4247 | 23060 | 42593935 |
| Foetal exposure during pregnancy | 179.14 | 21.98 | 90 | 4250 | 47221 | 42569774 |
| Low birth weight baby | 174.06 | 21.98 | 57 | 4283 | 9898 | 42607097 |
| Mechanical ventilation complication | 109.86 | 21.98 | 23 | 4317 | 681 | 42616314 |
| Maternal exposure during pregnancy | 94.49 | 21.98 | 33 | 4307 | 6945 | 42610050 |
| Inspiratory capacity decreased | 81.37 | 21.98 | 24 | 4316 | 2943 | 42614052 |
| Foetal growth restriction | 79.35 | 21.98 | 27 | 4313 | 5256 | 42611739 |
| Adverse reaction | 70.28 | 21.98 | 23 | 4317 | 3970 | 42613025 |
| Haemothorax | 67.96 | 21.98 | 24 | 4316 | 5212 | 42611783 |
| Angiopathy | 63.58 | 21.98 | 23 | 4317 | 5354 | 42611641 |
| Emphysema | 61.37 | 21.98 | 28 | 4312 | 11807 | 42605188 |
| Foetal disorder | 58.88 | 21.98 | 15 | 4325 | 1064 | 42615931 |
| Neutropenia neonatal | 56.21 | 21.98 | 14 | 4326 | 906 | 42616089 |
| Anaphylactic shock | 56.07 | 21.98 | 33 | 4307 | 23484 | 42593511 |
| Hypovolaemia | 52.79 | 21.98 | 25 | 4315 | 11460 | 42605535 |
| Trigemino-cardiac reflex | 51.47 | 21.98 | 11 | 4329 | 360 | 42616635 |
| Face oedema | 48.67 | 21.98 | 25 | 4315 | 13641 | 42603354 |
| Ventricular asystole | 47.95 | 21.98 | 10 | 4330 | 290 | 42616705 |
| Blood pressure increased | 47.33 | 21.98 | 55 | 4285 | 101873 | 42515122 |
| Congenital oesophageal anomaly | 45.27 | 21.98 | 8 | 4332 | 93 | 42616902 |
| Shock haemorrhagic | 44.61 | 21.98 | 25 | 4315 | 16217 | 42600778 |
| Flatulence | 44.02 | 21.98 | 29 | 4311 | 25123 | 42591872 |
| Neonatal respiratory distress | 41.01 | 21.98 | 11 | 4329 | 954 | 42616041 |
| Pneumothorax | 40.85 | 21.98 | 27 | 4313 | 23516 | 42593479 |
| Anaphylactic reaction | 40.35 | 21.98 | 34 | 4306 | 42709 | 42574286 |
| Hypotension | 39.21 | 21.98 | 83 | 4257 | 257548 | 42359447 |
| Neonatal respiratory distress syndrome | 37.77 | 21.98 | 15 | 4325 | 4498 | 42612497 |
| Polyhydramnios | 31.99 | 21.98 | 7 | 4333 | 256 | 42616739 |
| Exposure via breast milk | 30.79 | 21.98 | 11 | 4329 | 2466 | 42614529 |
| Anhedonia | 30.19 | 21.98 | 15 | 4325 | 7625 | 42609370 |
| Anaemia neonatal | 28.87 | 21.98 | 7 | 4333 | 405 | 42616590 |
| Neonatal behavioural syndrome | 28.74 | 21.98 | 6 | 4334 | 175 | 42616820 |
| Patent ductus arteriosus | 27.17 | 21.98 | 11 | 4329 | 3465 | 42613530 |
| Hypospadias | 26.89 | 21.98 | 11 | 4329 | 3556 | 42613439 |
| Newborn persistent pulmonary hypertension | 24.50 | 21.98 | 5 | 4335 | 130 | 42616865 |
| Pyelocaliectasis | 24.32 | 21.98 | 8 | 4332 | 1401 | 42615594 |
| Completed suicide | 23.32 | 21.98 | 38 | 4302 | 96427 | 42520568 |
| Haemorrhage | 22.12 | 21.98 | 29 | 4311 | 60534 | 42556461 |
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 |
|---|---|---|---|---|---|---|
| Maternal exposure during pregnancy | 285.28 | 16.20 | 212 | 9684 | 254671 | 110324732 |
| Premature delivery | 262.90 | 16.20 | 100 | 9796 | 30532 | 110548871 |
| Exposure during pregnancy | 230.23 | 16.20 | 158 | 9738 | 167266 | 110412137 |
| Pre-eclampsia | 228.41 | 16.20 | 66 | 9830 | 8584 | 110570819 |
| Blood pressure inadequately controlled | 119.50 | 16.20 | 39 | 9857 | 7594 | 110571809 |
| Mechanical ventilation complication | 110.71 | 16.20 | 23 | 9873 | 748 | 110578655 |
| Exercise tolerance decreased | 98.46 | 16.20 | 38 | 9858 | 12029 | 110567374 |
| Caesarean section | 90.05 | 16.20 | 37 | 9859 | 13780 | 110565623 |
| Inspiratory capacity decreased | 87.58 | 16.20 | 24 | 9872 | 2571 | 110576832 |
| Multiple drug therapy | 82.77 | 16.20 | 30 | 9866 | 7984 | 110571419 |
| Diabetes mellitus inadequate control | 73.82 | 16.20 | 41 | 9855 | 29734 | 110549669 |
| Blood pressure increased | 64.06 | 16.20 | 96 | 9800 | 258277 | 110321126 |
| Haemothorax | 64.05 | 16.20 | 24 | 9872 | 7007 | 110572396 |
| Angiopathy | 62.46 | 16.20 | 25 | 9871 | 8705 | 110570698 |
| Emphysema | 59.60 | 16.20 | 31 | 9865 | 19725 | 110559678 |
| Trigemino-cardiac reflex | 50.26 | 16.20 | 11 | 9885 | 460 | 110578943 |
| Foetal growth restriction | 49.42 | 16.20 | 16 | 9880 | 3034 | 110576369 |
| Depressed mood | 49.34 | 16.20 | 42 | 9854 | 60767 | 110518636 |
| Treatment noncompliance | 48.46 | 16.20 | 45 | 9851 | 72945 | 110506458 |
| Completed suicide | 46.28 | 16.20 | 80 | 9816 | 242301 | 110337102 |
| Ventricular asystole | 45.67 | 16.20 | 10 | 9886 | 419 | 110578984 |
| Hypovolaemia | 40.88 | 16.20 | 25 | 9871 | 21649 | 110557754 |
| Hypotension | 39.00 | 16.20 | 119 | 9777 | 523730 | 110055673 |
| Pneumothorax | 38.50 | 16.20 | 29 | 9867 | 35256 | 110544147 |
| Medication error | 38.00 | 16.20 | 47 | 9849 | 105319 | 110474084 |
| Stillbirth | 36.83 | 16.20 | 14 | 9882 | 4250 | 110575153 |
| Anaphylactic shock | 36.59 | 16.20 | 33 | 9863 | 51513 | 110527890 |
| Amnesia | 36.39 | 16.20 | 46 | 9850 | 105362 | 110474041 |
| Shock haemorrhagic | 35.66 | 16.20 | 25 | 9871 | 27222 | 110552181 |
| Cognitive disorder | 34.76 | 16.20 | 41 | 9855 | 87470 | 110491933 |
| Face oedema | 33.21 | 16.20 | 26 | 9870 | 33443 | 110545960 |
| Superimposed pre-eclampsia | 32.82 | 16.20 | 5 | 9891 | 24 | 110579379 |
| Adverse reaction | 31.57 | 16.20 | 24 | 9872 | 29570 | 110549833 |
| Subacute cutaneous lupus erythematosus | 31.27 | 16.20 | 13 | 9883 | 4981 | 110574422 |
| Cardiac arrest | 31.26 | 16.20 | 60 | 9836 | 196693 | 110382710 |
| Cerebral haemorrhage | 30.15 | 16.20 | 33 | 9863 | 64935 | 110514468 |
| Premature labour | 29.42 | 16.20 | 15 | 9881 | 9157 | 110570246 |
| Flatulence | 28.68 | 16.20 | 29 | 9867 | 52120 | 110527283 |
| Drug ineffective | 28.34 | 16.20 | 232 | 9664 | 1520308 | 109059095 |
| Anaphylactic reaction | 27.61 | 16.20 | 42 | 9854 | 114258 | 110465145 |
| Premature baby | 24.99 | 16.20 | 11 | 9885 | 4844 | 110574559 |
| Phaeochromocytoma | 24.77 | 16.20 | 7 | 9889 | 838 | 110578565 |
| Drug intolerance | 23.60 | 16.20 | 4 | 9892 | 406508 | 110172895 |
| Anhedonia | 22.17 | 16.20 | 15 | 9881 | 15413 | 110563990 |
| Pleural effusion | 22.10 | 16.20 | 49 | 9847 | 177660 | 110401743 |
| Infusion related reaction | 21.58 | 16.20 | 4 | 9892 | 381158 | 110198245 |
| Maternal exposure during delivery | 21.38 | 16.20 | 9 | 9887 | 3556 | 110575847 |
| Tachycardia | 21.22 | 16.20 | 56 | 9840 | 226589 | 110352814 |
| Oedema peripheral | 21.07 | 16.20 | 71 | 9825 | 328589 | 110250814 |
| Zoonotic bacterial infection | 20.84 | 16.20 | 4 | 9892 | 86 | 110579317 |
| Nephrogenic systemic fibrosis | 20.64 | 16.20 | 10 | 9886 | 5473 | 110573930 |
| Peptic ulcer perforation | 20.41 | 16.20 | 6 | 9890 | 827 | 110578576 |
| Dilatation intrahepatic duct acquired | 20.34 | 16.20 | 6 | 9890 | 837 | 110578566 |
| Pulmonary oedema | 20.20 | 16.20 | 34 | 9862 | 100625 | 110478778 |
| HELLP syndrome | 20.11 | 16.20 | 6 | 9890 | 870 | 110578533 |
| Eclampsia | 20.09 | 16.20 | 5 | 9891 | 367 | 110579036 |
| Foetal death | 19.33 | 16.20 | 14 | 9882 | 16031 | 110563372 |
| Haemodynamic instability | 18.95 | 16.20 | 16 | 9880 | 22872 | 110556531 |
| Live birth | 18.89 | 16.20 | 27 | 9869 | 69457 | 110509946 |
| Abortion spontaneous | 18.73 | 16.20 | 19 | 9877 | 34263 | 110545140 |
| Phaeochromocytoma crisis | 18.49 | 16.20 | 5 | 9891 | 509 | 110578894 |
| Hypertensive encephalopathy | 18.19 | 16.20 | 6 | 9890 | 1205 | 110578198 |
| Product use issue | 17.96 | 16.20 | 65 | 9831 | 311630 | 110267773 |
| Haemorrhage | 17.50 | 16.20 | 33 | 9863 | 106659 | 110472744 |
| Hypoaldosteronism | 17.19 | 16.20 | 5 | 9891 | 664 | 110578739 |
| Abortion induced | 17.07 | 16.20 | 10 | 9886 | 8009 | 110571394 |
| Beta 2 microglobulin increased | 16.96 | 16.20 | 5 | 9891 | 696 | 110578707 |
| Premature separation of placenta | 16.63 | 16.20 | 6 | 9890 | 1574 | 110577829 |
| Mycobacterium marinum infection | 16.53 | 16.20 | 5 | 9891 | 760 | 110578643 |
| Hypermagnesaemia | 16.47 | 16.20 | 6 | 9890 | 1617 | 110577786 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | C07AG01 | CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS Alpha and beta blocking agents |
| ATC | C07BG01 | CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS AND THIAZIDES Alpha and beta blocking agents and thiazides |
| ATC | C07CG01 | CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS AND OTHER DIURETICS Alpha and beta blocking agents and other diuretics |
| FDA MoA | N0000000161 | Adrenergic beta-Antagonists |
| FDA EPC | N0000175556 | beta-Adrenergic Blocker |
| MeSH PA | D000317 | Adrenergic alpha-Antagonists |
| MeSH PA | D000319 | Adrenergic beta-Antagonists |
| MeSH PA | D000959 | Antihypertensive Agents |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D013566 | Sympathomimetics |
| 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:35480 | analgesic |
| CHEBI has role | CHEBI:35530 | β-adrenergic antagonist |
| CHEBI has role | CHEBI:35554 | cardiovascular drug |
| CHEBI has role | CHEBI:35674 | antihypertensive agent |
| CHEBI has role | CHEBI:37890 | α-adrenergic antagonist |
| CHEBI has role | CHEBI:66991 | sympatholytic agent |
Related Drugs by ATC class:
C07AG Alpha and beta blocking agents 1 drug
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Hypertensive disorder | indication | 38341003 | DOID:10763 |
| Angina pectoris | off-label use | 194828000 | |
| Pheochromocytoma Adjunct Therapy | off-label use | ||
| Anuria | contraindication | 2472002 | DOID:2983 |
| Bronchospasm | contraindication | 4386001 | |
| Hypercholesterolemia | contraindication | 13644009 | |
| Secondary angle-closure glaucoma | contraindication | 21571006 | |
| Complete atrioventricular block | contraindication | 27885002 | |
| Hypovolemia | contraindication | 28560003 | |
| Dehydration | contraindication | 34095006 | |
| Depressive disorder | contraindication | 35489007 | |
| Hyperuricemia | contraindication | 35885006 | DOID:1920 |
| Hypokalemia | contraindication | 43339004 | |
| Low blood pressure | contraindication | 45007003 | |
| Sinus bradycardia | contraindication | 49710005 | |
| Systemic lupus erythematosus | contraindication | 55464009 | DOID:9074 |
| Sympathectomy | contraindication | 57071006 | |
| Hepatic failure | contraindication | 59927004 | |
| Hypercalcemia | contraindication | 66931009 | DOID:12678 |
| Hyperparathyroidism | contraindication | 66999008 | DOID:13543 |
| Hypochloremic alkalosis | contraindication | 70134007 | |
| Hepatic coma | contraindication | 72836002 | DOID:12550 |
| Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
| Pulmonary emphysema | contraindication | 87433001 | |
| Cardiogenic shock | contraindication | 89138009 | |
| Hyponatremia | contraindication | 89627008 | |
| Gout | contraindication | 90560007 | DOID:13189 |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Hypomagnesemia | contraindication | 190855004 | |
| Partial atrioventricular block | contraindication | 195039008 | |
| Decompensated cardiac failure | contraindication | 195111005 | |
| Acute pancreatitis | contraindication | 197456007 | DOID:2913 |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Neonatal hyperbilirubinemia | contraindication | 281610001 | |
| Intraoperative floppy iris syndrome | contraindication | 418801006 | |
| Azotemia | contraindication | 445009001 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 8.81 | acidic |
| pKa2 | 12.65 | acidic |
| pKa3 | 8.23 | 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]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Beta-1 adrenergic receptor | GPCR | ANTAGONIST | Ki | 8.23 | DRUG MATRIX | CHEMBL | |||
| Beta-2 adrenergic receptor | GPCR | ANTAGONIST | Ki | 7.96 | DRUG MATRIX | CHEMBL | |||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | Ki | 6.12 | DRUG MATRIX | |||||
| Sodium-dependent noradrenaline transporter | Transporter | Ki | 5.48 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 6.65 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 2B | GPCR | Ki | 5.71 | DRUG MATRIX | |||||
| Alpha-1A adrenergic receptor | GPCR | ANTAGONIST | IC50 | 7.90 | IUPHAR | ||||
| Sodium-dependent dopamine transporter | Transporter | Ki | 5.89 | DRUG MATRIX | |||||
| Cytochrome P450 2D6 | Enzyme | IC50 | 6.10 | DRUG MATRIX | |||||
| Alpha-1D adrenergic receptor | GPCR | ANTAGONIST | Ki | 7.64 | DRUG MATRIX | ||||
| Alpha-1B adrenergic receptor | GPCR | Ki | 6.49 | DRUG MATRIX | |||||
| Alpha-1A adrenergic receptor | GPCR | IC50 | 7.24 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | IC50 | 6.41 | CHEMBL | |||||
| CAAX prenyl protease 1 | Enzyme | AC50 | 5.11 | CHEMBL | |||||
| CAAX prenyl protease 2 | Enzyme | AC50 | 4.82 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019797 | VUID |
| N0000147886 | NUI |
| D00600 | KEGG_DRUG |
| 32780-64-6 | SECONDARY_CAS_RN |
| 4018799 | VANDF |
| 4019797 | VANDF |
| C0022860 | UMLSCUI |
| CHEBI:6343 | CHEBI |
| CHEMBL429 | ChEMBL_ID |
| CHEMBL1200323 | ChEMBL_ID |
| DB00598 | DRUGBANK_ID |
| D007741 | MESH_DESCRIPTOR_UI |
| 3869 | PUBCHEM_CID |
| 7207 | IUPHAR_LIGAND_ID |
| 3941 | INN_ID |
| R5H8897N95 | UNII |
| 202693 | RXNORM |
| 11828 | MMSL |
| 201477 | MMSL |
| 4950 | MMSL |
| d00016 | MMSL |
| 001839 | NDDF |
| 004368 | NDDF |
| 372750000 | SNOMEDCT_US |
| 46547007 | SNOMEDCT_US |
| 50627005 | SNOMEDCT_US |
| CHEMBL1204165 | ChEMBL_ID |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Labetalol Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9183 | INJECTION, SOLUTION | 5 mg | INTRAVENOUS | NDA | 26 sections |
| Labetalol Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9320 | INJECTION | 5 mg | INTRAVENOUS | ANDA | 24 sections |
| Labetalol HCl in Sodium Chloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9363 | INJECTION | 1 mg | INTRAVENOUS | NDA | 26 sections |
| Labetalol HCl in Sodium Chloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9364 | INJECTION | 1 mg | INTRAVENOUS | NDA | 26 sections |
| Labetalol HCl in Sodium Chloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9365 | INJECTION | 1 mg | INTRAVENOUS | NDA | 26 sections |
| Labetalol HCl in Dextrose | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9366 | INJECTION | 1 mg | INTRAVENOUS | NDA | 26 sections |
| Labetalol Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9622 | INJECTION | 5 mg | INTRAVENOUS | ANDA | 23 sections |
| Labetalol Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9623 | INJECTION | 5 mg | INTRAVENOUS | ANDA | 23 sections |
| Labetalol Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0409-0125 | INJECTION, SOLUTION | 5 mg | INTRAVENOUS | ANDA | 12 sections |
| Labetalol Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0409-2267 | INJECTION, SOLUTION | 5 mg | INTRAVENOUS | ANDA | 12 sections |
| Labetalol Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0409-2339 | INJECTION, SOLUTION | 5 mg | INTRAVENOUS | ANDA | 12 sections |
| Labetalol hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-0605 | TABLET, FILM COATED | 100 mg | ORAL | ANDA | 22 sections |
| Labetalol hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-0605 | TABLET, FILM COATED | 100 mg | ORAL | ANDA | 22 sections |
| Labetalol hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-0606 | TABLET, FILM COATED | 200 mg | ORAL | ANDA | 22 sections |
| Labetalol hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-0606 | TABLET, FILM COATED | 200 mg | ORAL | ANDA | 22 sections |
| Labetalol hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-0607 | TABLET, FILM COATED | 300 mg | ORAL | ANDA | 22 sections |
| Labetalol hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-0607 | TABLET, FILM COATED | 300 mg | ORAL | ANDA | 22 sections |
| Labetalol Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0615-8512 | TABLET, FILM COATED | 100 mg | ORAL | ANDA | 23 sections |
| Labetalol Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0615-8513 | TABLET, FILM COATED | 200 mg | ORAL | ANDA | 23 sections |
| Labetalol Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0904-7451 | TABLET, FILM COATED | 100 mg | ORAL | ANDA | 23 sections |
| Labetalol Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0904-7452 | TABLET, FILM COATED | 200 mg | ORAL | ANDA | 23 sections |
| Labetalol Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0904-7453 | TABLET, FILM COATED | 300 mg | ORAL | ANDA | 23 sections |
| Labetalol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10135-641 | TABLET, FILM COATED | 100 mg | ORAL | ANDA | 23 sections |
| Labetalol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10135-642 | TABLET, FILM COATED | 200 mg | ORAL | ANDA | 23 sections |
| Labetalol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10135-643 | TABLET, FILM COATED | 300 mg | ORAL | ANDA | 23 sections |
| Labetalol Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10135-711 | TABLET, FILM COATED | 100 mg | ORAL | ANDA | 24 sections |
| Labetalol Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10135-712 | TABLET, FILM COATED | 200 mg | ORAL | ANDA | 24 sections |
| Labetalol Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10135-713 | TABLET, FILM COATED | 300 mg | ORAL | ANDA | 24 sections |
| LABETALOL HYDROCHLORIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16590-994 | TABLET, FILM COATED | 300 mg | ORAL | ANDA | 24 sections |
| Labetalol Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 17478-420 | INJECTION, SOLUTION | 5 mg | INTRAVENOUS | ANDA | 26 sections |