dexmedetomidine ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
835 113775-47-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • dexmedetomidine
  • (S)-Medetomidine
  • dexmedetomidine hydrochloride
  • dexdor
  • dexmedetomidine HCl
  • MPV1440
  • precedex
A imidazole derivative that is an agonist of ADRENERGIC ALPHA-2 RECEPTORS. It is closely-related to MEDETOMIDINE, which is the racemic form of this compound.
  • Molecular weight: 200.29
  • Formula: C13H16N2
  • CLOGP: 3.10
  • LIPINSKI: 0
  • HAC: 2
  • HDO: 1
  • TPSA: 28.68
  • ALOGS: -3.06
  • ROTB: 2

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
1 mg P

ADMET properties:

PropertyValueReference
BA (Bioavailability) 16 %
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.09 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution) 1.60 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 11 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) 2.20 hours Lombardo F, Berellini G, Obach RS
S (Water solubility) 20 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2A,ACVR2B,AKT3,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK1,JAK2,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPK9,MAPKAPK2,MARK4,MET,MTOR,NTRK2,PDK4,PIK3CB,PIK3CG,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,TEK,TTK,ULK1 44
kinase-selectivity-class AXL,BRAF,CSF1R,DDR1,EPHB4,ERBB2,GRK2,PDK4,PIK3CB,PIK3CD,SIK2 11
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
Dec. 17, 1999 FDA HOSPIRA
Jan. 29, 2001 PMDA Abbott Japan, Maruishi Pharmaceutical
Sept. 15, 2011 EMA Orion Corporation

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Bradycardia 310.88 31.01 140 6227 83707 90538373
Agitation 154.53 31.01 81 6286 67017 90555063
Product administered to patient of inappropriate age 152.73 31.01 40 6327 4613 90617467
Anaesthetic complication neurological 141.89 31.01 27 6340 714 90621366
Cardiac arrest 113.77 31.01 78 6289 104857 90517223
Hypotension 112.77 31.01 126 6241 325271 90296809
Phaeochromocytoma crisis 106.19 31.01 19 6348 354 90621726
Withdrawal syndrome 104.04 31.01 44 6323 22480 90599600
Off label use 101.92 31.01 232 6135 1102020 89520060
Sinus arrest 97.88 31.01 24 6343 2122 90619958
Myoclonus 93.73 31.01 39 6328 19129 90602951
Torsade de pointes 91.85 31.01 36 6331 15146 90606934
Respiratory acidosis 89.52 31.01 30 6337 8089 90613991
Upper airway obstruction 86.90 31.01 19 6348 1013 90621067
Respiratory depression 84.02 31.01 34 6333 15541 90606539
Drug interaction 78.90 31.01 97 6270 276356 90345724
Glossoptosis 77.10 31.01 12 6355 90 90621990
Delirium 75.80 31.01 61 6306 104298 90517782
Respiratory failure 75.14 31.01 64 6303 118354 90503726
Floppy iris syndrome 74.95 31.01 12 6355 110 90621970
Apnoea 73.87 31.01 27 6340 9387 90612693
Paradoxical drug reaction 70.35 31.01 23 6344 5743 90616337
Drug ineffective for unapproved indication 68.55 31.01 48 6319 66596 90555484
Generalised tonic-clonic seizure 65.96 31.01 37 6330 34866 90587214
Hyperthermia 60.72 31.01 24 6343 10311 90611769
Atrioventricular block second degree 59.37 31.01 19 6348 4433 90617647
Sinus bradycardia 58.51 31.01 27 6340 16925 90605155
Electrocardiogram QT prolonged 58.29 31.01 45 6322 72411 90549669
Drug reaction with eosinophilia and systemic symptoms 56.50 31.01 36 6331 42722 90579358
Maternal exposure during delivery 53.70 31.01 17 6350 3829 90618251
Sedation complication 52.35 31.01 25 6342 16919 90605161
Hypoxia 51.86 31.01 42 6325 72357 90549723
Hyperthermia malignant 51.58 31.01 13 6354 1285 90620795
Laryngeal stenosis 51.18 31.01 13 6354 1326 90620754
Tachyphylaxis 50.03 31.01 10 6357 343 90621737
Transcranial electrical motor evoked potential monitoring abnormal 49.53 31.01 7 6360 24 90622056
Posterior reversible encephalopathy syndrome 48.61 31.01 26 6341 22313 90599767
Product appearance confusion 46.99 31.01 8 6359 110 90621970
Hypocapnia 46.15 31.01 10 6357 511 90621569
Drug ineffective 45.29 31.01 204 6163 1384094 89237986
Stress cardiomyopathy 45.24 31.01 21 6346 13334 90608746
Drug withdrawal syndrome 45.10 31.01 27 6340 28696 90593384
Hepatic function abnormal 44.49 31.01 32 6335 46256 90575824
Product closure removal difficult 42.82 31.01 6 6361 19 90622061
Myocardial calcification 41.32 31.01 8 6359 232 90621848
Acute respiratory distress syndrome 40.01 31.01 25 6342 28661 90593419
Toxicity to various agents 39.87 31.01 72 6295 287774 90334306
Tachycardia 39.62 31.01 52 6315 157621 90464459
Human herpesvirus 6 infection reactivation 38.83 31.01 9 6358 625 90621455
Mental status changes 38.67 31.01 29 6338 44650 90577430
Ventricular dysfunction 38.03 31.01 13 6354 3718 90618362
Arthralgia 37.93 31.01 5 6362 778517 89843563
Arteriospasm coronary 37.82 31.01 14 6353 5036 90617044
Anaphylactic shock 37.78 31.01 25 6342 31592 90590488
Unwanted awareness during anaesthesia 37.05 31.01 8 6359 402 90621678
Abdominal compartment syndrome 36.94 31.01 9 6358 774 90621306
Aplastic anaemia 36.25 31.01 18 6349 13251 90608829
Serotonin syndrome 35.96 31.01 26 6341 37861 90584219
Postoperative delirium 35.96 31.01 7 6360 209 90621871
Laryngospasm 35.49 31.01 12 6355 3321 90618759
Ventricular fibrillation 35.28 31.01 18 6349 14026 90608054
Intensive care unit acquired weakness 34.66 31.01 9 6358 1002 90621078
Delayed recovery from anaesthesia 34.49 31.01 9 6358 1021 90621059
Device pacing issue 33.99 31.01 6 6361 103 90621977
Confusional arousal 33.46 31.01 7 6360 302 90621778
Apgar score low 33.10 31.01 9 6358 1194 90620886
Echolalia 32.94 31.01 7 6360 326 90621754
Accidental overdose 32.92 31.01 22 6345 28251 90593829
Fatigue 31.99 31.01 21 6346 1154002 89468078
Polyuria 31.58 31.01 15 6352 10025 90612055
Local anaesthetic systemic toxicity 31.06 31.01 11 6356 3489 90618591
Airway complication of anaesthesia 31.06 31.01 7 6360 429 90621651

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Bradycardia 470.86 22.53 263 8457 85221 42527394
Diabetes insipidus 389.33 22.53 100 8620 3613 42609002
Cardiac arrest 251.36 22.53 195 8525 109125 42503490
Arteriospasm coronary 188.70 22.53 60 8660 4678 42607937
Drug withdrawal syndrome 147.95 22.53 77 8643 21472 42591143
Hyperthermia 147.71 22.53 65 8655 12509 42600106
Product administered to patient of inappropriate age 144.09 22.53 49 8671 4712 42607903
Anaesthetic complication neurological 134.35 22.53 31 8689 705 42611910
Intestinal pseudo-obstruction 130.17 22.53 38 8682 2217 42610398
Hyperthermia malignant 115.55 22.53 36 8684 2622 42609993
Seizure like phenomena 112.25 22.53 29 8691 1068 42611547
Delirium 103.94 22.53 86 8634 52433 42560182
Hypotension 98.47 22.53 183 8537 257448 42355167
Respiratory failure 84.71 22.53 117 8603 128015 42484600
Off label use 84.35 22.53 303 8417 638032 41974583
Withdrawal syndrome 79.65 22.53 45 8675 14730 42597885
Agitation 74.21 22.53 78 8642 64236 42548379
Drug ineffective for unapproved indication 73.91 22.53 67 8653 46096 42566519
Sedation complication 72.75 22.53 26 8694 2893 42609722
Polyuria 69.31 22.53 36 8684 9975 42602640
Sinus arrest 68.41 22.53 23 8697 2133 42610482
Postoperative ileus 68.11 22.53 18 8702 725 42611890
Tachypnoea 63.83 22.53 45 8675 21617 42590998
Torsade de pointes 62.66 22.53 32 8688 8562 42604053
Tachycardia 61.84 22.53 89 8631 100998 42511617
Serotonin syndrome 56.74 22.53 45 8675 25800 42586815
Fatigue 55.47 22.53 11 8709 435630 42176985
Neuroleptic malignant syndrome 55.05 22.53 41 8679 21431 42591184
Acute motor axonal neuropathy 53.22 22.53 10 8710 78 42612537
Burkholderia test positive 48.92 22.53 15 8705 1035 42611580
Hypocapnia 47.39 22.53 12 8708 407 42612208
Upper airway obstruction 44.14 22.53 13 8707 781 42611834
Haemodynamic instability 43.90 22.53 29 8691 12528 42600087
Electrocardiogram QT prolonged 42.98 22.53 51 8669 47894 42564721
Ventricular tachycardia 42.89 22.53 41 8679 30119 42582496
Epidermolysis bullosa 42.53 22.53 9 8711 135 42612480
Drug interaction 42.14 22.53 135 8585 266864 42345751
Myoclonus 38.06 22.53 30 8690 17035 42595580
Methaemoglobinaemia 37.78 22.53 20 8700 5754 42606861
Laryngomalacia 34.89 22.53 9 8711 329 42612286
Hypernatraemia 34.66 22.53 23 8697 10009 42602606
Atrioventricular block complete 34.38 22.53 24 8696 11340 42601275
Product use issue 33.59 22.53 58 8662 76693 42535922
Product use in unapproved indication 33.47 22.53 98 8622 184358 42428257
Respiratory depression 33.38 22.53 29 8691 18839 42593776
Diarrhoea 32.55 22.53 28 8692 460821 42151794
Malignant catatonia 32.16 22.53 9 8711 450 42612165
Hyperaesthesia 31.72 22.53 18 8702 5934 42606681
Weight decreased 31.68 22.53 3 8717 207945 42404670
Hypercapnia 30.71 22.53 17 8703 5344 42607271
Floppy iris syndrome 30.42 22.53 8 8712 316 42612299
Asthenia 30.10 22.53 10 8710 280783 42331832
Hypothermia 30.08 22.53 23 8697 12492 42600123
Hypoxia 29.57 22.53 52 8668 69734 42542881
Arthralgia 28.67 22.53 4 8716 205234 42407381
Stress cardiomyopathy 28.24 22.53 13 8707 2772 42609843
Urinary bladder rupture 27.87 22.53 6 8714 98 42612517
Delayed recovery from anaesthesia 27.58 22.53 10 8710 1159 42611456
Renal ischaemia 27.54 22.53 11 8709 1659 42610956
Endotracheal intubation 27.31 22.53 14 8706 3771 42608844
Oxygen saturation decreased 27.15 22.53 48 8672 64639 42547976
Lung assist device therapy 26.96 22.53 5 8715 36 42612579
Cardiac arrest neonatal 26.96 22.53 5 8715 36 42612579
Hypotonia 26.28 22.53 19 8701 9480 42603135
Phrenic nerve injury 25.59 22.53 4 8716 8 42612607
Generalised tonic-clonic seizure 25.19 22.53 29 8691 26350 42586265
Death 25.15 22.53 36 8684 471149 42141466
Headache 24.82 22.53 9 8711 239360 42373255
Dizziness 24.80 22.53 10 8710 249244 42363371
Sinus bradycardia 24.61 22.53 22 8698 14831 42597784
Transcranial electrical motor evoked potential monitoring abnormal 24.44 22.53 4 8716 12 42612603
Abdominal compartment syndrome 24.39 22.53 9 8711 1096 42611519
Drug ineffective 24.30 22.53 215 8505 629982 41982633
Glossoptosis 24.25 22.53 6 8714 185 42612430
Multiple organ dysfunction syndrome 24.12 22.53 58 8662 96977 42515638
Blood pressure decreased 24.11 22.53 43 8677 58289 42554326
Locked-in syndrome 24.11 22.53 7 8713 400 42612215
Porphyria acute 23.96 22.53 7 8713 409 42612206
Respiratory alkalosis 23.95 22.53 11 8709 2333 42610282
Ileus 23.45 22.53 24 8696 19115 42593500

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Bradycardia 668.37 25.35 345 13573 155172 110420209
Diabetes insipidus 409.70 25.35 106 13812 6464 110568917
Cardiac arrest 371.03 25.35 257 13661 196496 110378885
Product administered to patient of inappropriate age 236.30 25.35 72 13846 7964 110567417
Hyperthermia 215.31 25.35 86 13832 21186 110554195
Agitation 199.51 25.35 142 13776 112909 110462472
Drug withdrawal syndrome 196.90 25.35 96 13822 37958 110537423
Arteriospasm coronary 194.78 25.35 64 13854 9036 110566345
Hypotension 194.00 25.35 281 13637 523568 110051813
Withdrawal syndrome 167.86 25.35 81 13837 31299 110544082
Respiratory failure 151.84 25.35 160 13758 215172 110360209
Torsade de pointes 150.84 25.35 68 13850 22532 110552849
Hyperthermia malignant 149.89 25.35 43 13875 3857 110571524
Delirium 143.86 25.35 126 13792 134899 110440482
Sinus arrest 141.94 25.35 42 13876 4200 110571181
Intestinal pseudo-obstruction 137.97 25.35 39 13879 3317 110572064
Off label use 135.72 25.35 454 13464 1499731 109075650
Respiratory depression 128.37 25.35 68 13850 31933 110543448
Drug ineffective for unapproved indication 128.06 25.35 105 13813 102733 110472648
Drug interaction 126.79 25.35 226 13692 499957 110075424
Upper airway obstruction 111.94 25.35 29 13889 1773 110573608
Myoclonus 107.18 25.35 61 13857 32937 110542444
Electrocardiogram QT prolonged 104.77 25.35 96 13822 108864 110466517
Polyuria 104.66 25.35 49 13869 17689 110557692
Seizure like phenomena 103.22 25.35 29 13889 2412 110572969
Sedation complication 102.39 25.35 50 13868 19805 110555576
Postoperative ileus 102.09 25.35 25 13893 1215 110574166
Serotonin syndrome 96.71 25.35 71 13847 59082 110516299
Respiratory acidosis 93.52 25.35 42 13876 13784 110561597
Tachypnoea 92.18 25.35 59 13859 39336 110536045
Generalised tonic-clonic seizure 90.22 25.35 66 13852 54614 110520767
Phaeochromocytoma crisis 89.05 25.35 19 13899 495 110574886
Drug ineffective 84.88 25.35 396 13522 1520144 109055237
Tachycardia 82.68 25.35 121 13797 226524 110348857
Glossoptosis 81.65 25.35 16 13902 269 110575112
Neuroleptic malignant syndrome 79.66 25.35 51 13867 34008 110541373
Sinus bradycardia 78.66 25.35 48 13870 29435 110545946
Fatigue 78.04 25.35 28 13890 1215930 109359451
Atrioventricular block second degree 75.61 25.35 31 13887 8150 110567231
Ventricular tachycardia 74.99 25.35 57 13861 49952 110525429
Delayed recovery from anaesthesia 74.40 25.35 22 13896 2193 110573188
Haemodynamic instability 73.48 25.35 42 13876 22846 110552535
Transcranial electrical motor evoked potential monitoring abnormal 71.59 25.35 11 13907 37 110575344
Arthralgia 70.36 25.35 8 13910 779624 109795757
Hypoxia 70.20 25.35 84 13834 129431 110445950
Hypernatraemia 66.19 25.35 36 13882 17797 110557584
Stress cardiomyopathy 64.54 25.35 34 13884 15772 110559609
Oxygen saturation decreased 61.89 25.35 87 13831 156895 110418486
Ventricular fibrillation 61.74 25.35 47 13871 41266 110534115
Malaise 60.33 25.35 7 13911 671812 109903569
Abdominal compartment syndrome 59.78 25.35 18 13900 1909 110573472
Paradoxical drug reaction 57.54 25.35 27 13891 9790 110565591
Atrioventricular block complete 56.94 25.35 34 13884 20048 110555333
Multiple organ dysfunction syndrome 53.84 25.35 80 13838 151630 110423751
Headache 53.72 25.35 22 13896 882355 109693026
Diarrhoea 52.72 25.35 40 13878 1139465 109435916
Acute motor axonal neuropathy 52.04 25.35 10 13908 151 110575230
Nausea 51.51 25.35 48 13870 1235642 109339739
Drug reaction with eosinophilia and systemic symptoms 49.05 25.35 56 13862 82039 110493342
Mental status changes 49.03 25.35 54 13864 76068 110499313
Apnoea 46.40 25.35 26 13892 13613 110561768
Asthenia 45.58 25.35 15 13903 688984 109886397
Decreased appetite 45.18 25.35 4 13914 475842 110099539
Blood pressure decreased 44.18 25.35 63 13855 115028 110460353
Product use in unapproved indication 44.08 25.35 140 13778 447237 110128144
Pain in extremity 43.89 25.35 5 13913 487113 110088268
Postoperative delirium 43.88 25.35 12 13906 903 110574478
Laryngeal stenosis 43.12 25.35 13 13905 1385 110573996
Posterior reversible encephalopathy syndrome 43.00 25.35 35 13883 33826 110541555
Acute respiratory distress syndrome 41.86 25.35 42 13876 53156 110522225
Maternal exposure during delivery 41.64 25.35 16 13902 3549 110571832
Dizziness 41.51 25.35 18 13900 698175 109877206
Pruritus 41.48 25.35 11 13907 581549 109993832
Anaphylactic shock 41.12 25.35 41 13877 51505 110523876
Hypercapnia 39.95 25.35 22 13896 11137 110564244
Cardio-respiratory arrest 39.54 25.35 60 13858 115776 110459605
Acute respiratory failure 39.42 25.35 48 13870 75212 110500169
Methaemoglobinaemia 38.22 25.35 20 13898 9148 110566233
Epidermolysis bullosa 37.93 25.35 9 13909 382 110574999
Airway complication of anaesthesia 37.64 25.35 10 13908 674 110574707
Product closure removal difficult 37.55 25.35 5 13913 3 110575378
Laryngospasm 37.47 25.35 16 13902 4652 110570729
Hypothermia 37.27 25.35 29 13889 26273 110549108
Unresponsive to stimuli 37.24 25.35 43 13875 63747 110511634
Myocardial calcification 35.85 25.35 8 13910 258 110575123
Septic shock 35.72 25.35 68 13850 157460 110417921
Weight decreased 35.03 25.35 8 13910 468049 110107332
Shock 34.48 25.35 38 13880 53550 110521831
Rebound effect 34.19 25.35 22 13896 14784 110560597
Burkholderia test positive 33.76 25.35 9 13909 615 110574766
Hypotonia 32.95 25.35 22 13896 15723 110559658
Back pain 32.93 25.35 4 13914 370992 110204389
Confusional arousal 32.78 25.35 7 13911 183 110575198
Aplastic anaemia 32.72 25.35 26 13892 24282 110551099
Malignant catatonia 32.65 25.35 9 13909 697 110574684
Hyperpyrexia 31.93 25.35 17 13901 8052 110567329
Hepatic function abnormal 31.53 25.35 47 13871 89248 110486133
Respiratory distress 31.42 25.35 41 13877 68833 110506548
Aggression 31.39 25.35 38 13880 59172 110516209
Ileus 31.32 25.35 28 13890 30701 110544680
Hypersensitivity 30.03 25.35 7 13911 403991 110171390
Drug hypersensitivity 29.80 25.35 10 13908 454080 110121301
Fall 29.38 25.35 20 13898 603462 109971919
Renal ischaemia 29.20 25.35 11 13907 2312 110573069
Intensive care unit acquired weakness 29.04 25.35 11 13907 2348 110573033
Dyspnoea 28.99 25.35 60 13858 1106812 109468569
Human herpesvirus 6 infection reactivation 28.48 25.35 9 13909 1120 110574261
Swelling 28.34 25.35 5 13913 351036 110224345
Pain 28.32 25.35 48 13870 954907 109620474
Negative pressure pulmonary oedema 28.17 25.35 8 13910 691 110574690
Autonomic nervous system imbalance 28.14 25.35 14 13904 5766 110569615
Device pacing issue 27.98 25.35 6 13912 160 110575221
Overdose 27.55 25.35 78 13840 233716 110341665
Phrenic nerve injury 27.53 25.35 4 13914 8 110575373
Hyperaesthesia 27.09 25.35 19 13899 14708 110560673
Acute chest syndrome 26.59 25.35 10 13908 2093 110573288
Electrocardiogram R on T phenomenon 25.91 25.35 4 13914 14 110575367
Hypercapnic coma 25.84 25.35 7 13911 508 110574873
Echolalia 25.37 25.35 7 13911 544 110574837

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N05CM18 NERVOUS SYSTEM
PSYCHOLEPTICS
HYPNOTICS AND SEDATIVES
Other hypnotics and sedatives
FDA MoA N0000009918 Adrenergic alpha2-Agonists
FDA EPC N0000175554 Central alpha-2 Adrenergic Agonist
CHEBI has role CHEBI:35474 anxiolytic drug
CHEBI has role CHEBI:35480 analgesic
CHEBI has role CHEBI:35481 non-narcotic analgesic
CHEBI has role CHEBI:35554 cardiovascular drug
CHEBI has role CHEBI:35569 ฮฑ-adrenergic agonist
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:35623 anticonvulsant
CHEBI has role CHEBI:35674 antihypertensive agent
CHEBI has role CHEBI:35717 sedative
CHEBI has role CHEBI:38070 anti-arrhythmia drug
CHEBI has role CHEBI:51177 antitussive
CHEBI has role CHEBI:63726 neuroprotective agent
CHEBI has role CHEBI:67079 anti-inflammatory agent
CHEBI has role CHEBI:73336 vulnerary
CHEBI has role CHEBI:74518 anti-obesity agent
CHEBI has role CHEBI:231911 renoprotective agent
FDA PE N0000175975 General Anesthesia
MeSH PA D000316 Adrenergic alpha-Agonists
MeSH PA D000700 Analgesics
MeSH PA D002492 Central Nervous System Depressants
MeSH PA D006993 Hypnotics and Sedatives
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018663 Adrenergic Agents
MeSH PA D018689 Sensory System Agents
MeSH PA D018712 Analgesics, Non-Narcotic
MeSH PA D058647 Adrenergic alpha-2 Receptor Agonists
CHEBI has role CHEBI:35476 antipsychotic agent

Related Drugs by ATC class:

N05CM Other hypnotics and sedatives 13 drugs

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Conscious sedation indication 314271007
Complete atrioventricular block contraindication 27885002
Hypovolemia contraindication 28560003
Hypertensive disorder contraindication 38341003 DOID:10763
Low blood pressure contraindication 45007003
Chronic heart failure contraindication 48447003
Bradycardia contraindication 48867003
Diabetes mellitus contraindication 73211009 DOID:9351
Kidney disease contraindication 90708001 DOID:557
Disease of liver contraindication 235856003 DOID:409
Cardiac Decompensation contraindication




๐Ÿถ Veterinary Drug Use

SpeciesUseRelation
Cats Preanesthesia to general anesthesia Indication
Cats Sedation and analgesia Indication
Dogs Preanesthesia to general anesthesia Indication
Dogs Sedation and analgesia Indication
Dogs Noise aversion Indication

๐Ÿถ Veterinary products

ProductApplicantIngredients
Dexdomitor Orion Corp. 1
SILEO Orion Corp. 1
Dexmedesed Dechra Veterinary Products LLC 1
Dexmedetomidine Hydrochloride Injection Akorn Animal Health Inc. 1

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.36 acidic
pKa2 6.76 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 200MCG BASE/50ML (EQ 4MCG BASE/ML) PRECEDEX HOSPIRA N021038 March 13, 2013 RX INJECTABLE INJECTION 8455527 Jan. 4, 2032 USE FOR SEDATION
EQ 400MCG BASE/100ML (EQ 4MCG BASE/ML) PRECEDEX HOSPIRA N021038 March 13, 2013 RX INJECTABLE INJECTION 8455527 Jan. 4, 2032 USE FOR SEDATION
EQ 80MCG BASE/20ML (EQ 4MCG BASE/ML) PRECEDEX HOSPIRA N021038 Nov. 14, 2014 RX INJECTABLE INJECTION 8455527 Jan. 4, 2032 USE FOR SEDATION
EQ 0.12MG BASE IGALMI BIOXCEL N215390 April 5, 2022 RX FILM BUCCAL, SUBLINGUAL 11786508 Dec. 29, 2037 ACUTE TREATMENT OF AGITATION ASSOCIATED WITH SCHIZOPHRENIA BY SUBLINGUAL OR BUCCAL ADMINISTRATION
EQ 0.12MG BASE IGALMI BIOXCEL N215390 April 5, 2022 RX FILM BUCCAL, SUBLINGUAL 11839604 Dec. 29, 2037 ACUTE TREATMENT OF AGITATION ASSOCIATED WITH BIPOLAR I OR II DISORDER BY SUBLINGUAL OR BUCCAL ADMINISTRATION
EQ 0.18MG BASE IGALMI BIOXCEL N215390 April 5, 2022 RX FILM BUCCAL, SUBLINGUAL 11786508 Dec. 29, 2037 ACUTE TREATMENT OF AGITATION ASSOCIATED WITH SCHIZOPHRENIA BY SUBLINGUAL OR BUCCAL ADMINISTRATION
EQ 0.18MG BASE IGALMI BIOXCEL N215390 April 5, 2022 RX FILM BUCCAL, SUBLINGUAL 11839604 Dec. 29, 2037 ACUTE TREATMENT OF AGITATION ASSOCIATED WITH BIPOLAR I OR II DISORDER BY SUBLINGUAL OR BUCCAL ADMINISTRATION
EQ 0.12MG BASE IGALMI BIOXCEL N215390 April 5, 2022 RX FILM BUCCAL, SUBLINGUAL 10792246 June 26, 2039 ACUTE TREATMENT OF AGITATION ASSOCIATED WITH SCHIZOPHRENIA OR BIPOLAR I OR II DISORDER BY SUBLINGUAL ADMINISTRATION
EQ 0.12MG BASE IGALMI BIOXCEL N215390 April 5, 2022 RX FILM BUCCAL, SUBLINGUAL 11497711 June 26, 2039 ACUTE TREATMENT OF AGITATION ASSOCIATED WITH SCHIZOPHRENIA OR BIPOLAR I OR II DISORDER BY BUCCAL ADMINISTRATION
EQ 0.12MG BASE IGALMI BIOXCEL N215390 April 5, 2022 RX FILM BUCCAL, SUBLINGUAL 11517524 June 26, 2039 ACUTE TREATMENT OF AGITATION ASSOCIATED WITH SCHIZOPHRENIA OR BIPOLAR I OR II DISORDER BY BUCCAL ADMINISTRATION
EQ 0.18MG BASE IGALMI BIOXCEL N215390 April 5, 2022 RX FILM BUCCAL, SUBLINGUAL 10792246 June 26, 2039 ACUTE TREATMENT OF AGITATION ASSOCIATED WITH SCHIZOPHRENIA OR BIPOLAR I OR II DISORDER BY SUBLINGUAL ADMINISTRATION
EQ 0.18MG BASE IGALMI BIOXCEL N215390 April 5, 2022 RX FILM BUCCAL, SUBLINGUAL 11497711 June 26, 2039 ACUTE TREATMENT OF AGITATION ASSOCIATED WITH SCHIZOPHRENIA OR BIPOLAR I OR II DISORDER BY BUCCAL ADMINISTRATION
EQ 0.18MG BASE IGALMI BIOXCEL N215390 April 5, 2022 RX FILM BUCCAL, SUBLINGUAL 11517524 June 26, 2039 ACUTE TREATMENT OF AGITATION ASSOCIATED WITH SCHIZOPHRENIA OR BIPOLAR I OR II DISORDER BY BUCCAL ADMINISTRATION
EQ 0.12MG BASE IGALMI BIOXCEL N215390 April 5, 2022 RX FILM BUCCAL, SUBLINGUAL 11890272 July 17, 2040 ACUTE TREATMENT OF AGITATION ASSOCIATED WITH BIPOLAR I OR II DISORDER BY SUBLINGUAL OR BUCCAL ADMINISTRATION
EQ 0.12MG BASE IGALMI BIOXCEL N215390 April 5, 2022 RX FILM BUCCAL, SUBLINGUAL 11890272 July 17, 2040 ACUTE TREATMENT OF AGITATION ASSOCIATED WITH SCHIZOPHRENIA OR BIPOLAR I OR II DISORDER BY SUBLINGUAL OR BUCCAL ADMINISTRATION
EQ 0.12MG BASE IGALMI BIOXCEL N215390 April 5, 2022 RX FILM BUCCAL, SUBLINGUAL 11998529 July 17, 2040 ACUTE TREATMENT OF AGITATION ASSOCIATED WITH SCHIZOPHRENIA OR BIPOLAR I OR II DISORDER BY SUBLINGUAL OR BUCCAL ADMINISTRATION
EQ 0.12MG BASE IGALMI BIOXCEL N215390 April 5, 2022 RX FILM BUCCAL, SUBLINGUAL 12109196 July 17, 2040 ACUTE TREATMENT OF AGITATION ASSOCIATED WITH SCHIZOPHRENIA OR BIPOLAR I OR II DISORDER BY SUBLINGUAL OR BUCCAL ADMINISTRATION
EQ 0.18MG BASE IGALMI BIOXCEL N215390 April 5, 2022 RX FILM BUCCAL, SUBLINGUAL 11890272 July 17, 2040 ACUTE TREATMENT OF AGITATION ASSOCIATED WITH BIPOLAR I OR II DISORDER BY SUBLINGUAL OR BUCCAL ADMINISTRATION
EQ 0.18MG BASE IGALMI BIOXCEL N215390 April 5, 2022 RX FILM BUCCAL, SUBLINGUAL 11890272 July 17, 2040 ACUTE TREATMENT OF AGITATION ASSOCIATED WITH SCHIZOPHRENIA OR BIPOLAR I OR II DISORDER BY SUBLINGUAL OR BUCCAL ADMINISTRATION
EQ 0.18MG BASE IGALMI BIOXCEL N215390 April 5, 2022 RX FILM BUCCAL, SUBLINGUAL 11998529 July 17, 2040 ACUTE TREATMENT OF AGITATION ASSOCIATED WITH SCHIZOPHRENIA OR BIPOLAR I OR II DISORDER BY SUBLINGUAL OR BUCCAL ADMINISTRATION
EQ 0.18MG BASE IGALMI BIOXCEL N215390 April 5, 2022 RX FILM BUCCAL, SUBLINGUAL 12109196 July 17, 2040 ACUTE TREATMENT OF AGITATION ASSOCIATED WITH SCHIZOPHRENIA OR BIPOLAR I OR II DISORDER BY SUBLINGUAL OR BUCCAL ADMINISTRATION
EQ 0.12MG BASE IGALMI BIOXCEL N215390 April 5, 2022 RX FILM BUCCAL, SUBLINGUAL 11806334 Jan. 12, 2043 ACUTE TREATMENT OF AGITATION ASSOCIATED WITH SCHIZOPHRENIA OR BIPOLAR I OR II DISORDER BY SUBLINGUAL OR BUCCAL ADMINISTRATION IN PATIENTS WITH SEVERE HEPATIC IMPAIRMENT
EQ 0.12MG BASE IGALMI BIOXCEL N215390 April 5, 2022 RX FILM BUCCAL, SUBLINGUAL 11998528 Jan. 12, 2043 ACUTE TREATMENT OF AGITATION ASSOCIATED WITH SCHIZOPHRENIA OR BIPOLAR I OR II DISORDER BY SUBLINGUAL OR BUCCAL ADMINISTRATION
EQ 0.12MG BASE IGALMI BIOXCEL N215390 April 5, 2022 RX FILM BUCCAL, SUBLINGUAL 12090140 Jan. 12, 2043 A METHOD OF TREATING AGITATION ASSOCIATED WITH SCHIZOPHRENIA OR BIPOLAR I OR II DISORDER
EQ 0.12MG BASE IGALMI BIOXCEL N215390 April 5, 2022 RX FILM BUCCAL, SUBLINGUAL 12138247 Jan. 12, 2043 ACUTE TREATMENT OF AGITATION IN PATIENTS WITH SEVERE HEPATIC IMPAIRMENT
EQ 0.12MG BASE IGALMI BIOXCEL N215390 April 5, 2022 RX FILM BUCCAL, SUBLINGUAL 12364683 Jan. 12, 2043 ACUTE TREATMENT OF AGITATION IN PATIENTS WITH SEVERE HEPATIC IMPAIRMENT
EQ 0.18MG BASE IGALMI BIOXCEL N215390 April 5, 2022 RX FILM BUCCAL, SUBLINGUAL 11806334 Jan. 12, 2043 ACUTE TREATMENT OF AGITATION ASSOCIATED WITH SCHIZOPHRENIA OR BIPOLAR I OR II DISORDER BY SUBLINGUAL OR BUCCAL ADMINISTRATION IN PATIENTS WITH SEVERE HEPATIC IMPAIRMENT
EQ 0.18MG BASE IGALMI BIOXCEL N215390 April 5, 2022 RX FILM BUCCAL, SUBLINGUAL 11998528 Jan. 12, 2043 ACUTE TREATMENT OF AGITATION ASSOCIATED WITH SCHIZOPHRENIA OR BIPOLAR I OR II DISORDER BY SUBLINGUAL OR BUCCAL ADMINISTRATION
EQ 0.18MG BASE IGALMI BIOXCEL N215390 April 5, 2022 RX FILM BUCCAL, SUBLINGUAL 12090140 Jan. 12, 2043 A METHOD OF TREATING AGITATION ASSOCIATED WITH SCHIZOPHRENIA OR BIPOLAR I OR II DISORDER
EQ 0.18MG BASE IGALMI BIOXCEL N215390 April 5, 2022 RX FILM BUCCAL, SUBLINGUAL 12138247 Jan. 12, 2043 ACUTE TREATMENT OF AGITATION IN PATIENTS WITH SEVERE HEPATIC IMPAIRMENT
EQ 0.18MG BASE IGALMI BIOXCEL N215390 April 5, 2022 RX FILM BUCCAL, SUBLINGUAL 12364683 Jan. 12, 2043 ACUTE TREATMENT OF AGITATION IN PATIENTS WITH SEVERE HEPATIC IMPAIRMENT

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 0.12MG BASE IGALMI BIOXCEL N215390 April 5, 2022 RX FILM BUCCAL, SUBLINGUAL Nov. 19, 2028 LABELING REVISIONS RELATED TO CLINICAL STUDIES
EQ 0.18MG BASE IGALMI BIOXCEL N215390 April 5, 2022 RX FILM BUCCAL, SUBLINGUAL Nov. 19, 2028 LABELING REVISIONS RELATED TO CLINICAL STUDIES

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Alpha-2B adrenergic receptor GPCR AGONIST Ki 9.70 IUPHAR CHEMBL
Alpha-2C adrenergic receptor GPCR AGONIST Ki 9.30 IUPHAR CHEMBL
Alpha-2A adrenergic receptor GPCR AGONIST EC50 8.82 CHEMBL CHEMBL
Alpha-1A adrenergic receptor GPCR Ki 6.70 PDSP
Alpha-1D adrenergic receptor GPCR Ki 10.82 CHEMBL
Alpha-1B adrenergic receptor GPCR Ki 6.50 PDSP
Sodium-dependent noradrenaline transporter Transporter Ki 5.49 CHEMBL
5-hydroxytryptamine receptor 7 GPCR Ki 6.04 CHEMBL
Alpha-2A adrenergic receptor GPCR Ki 10.82 CHEMBL
Alpha-1A adrenergic receptor GPCR EC50 6.42 CHEMBL
Adrenergic receptor alpha-2 GPCR Ki 10.82 CHEMBL
Adrenergic receptor alpha-1 GPCR Ki 8.30 CHEMBL
Alpha-1B adrenergic receptor GPCR EC50 6.44 CHEMBL

External reference:

IDSource
4021214 VUID
N0000148660 NUI
D00514 KEGG_DRUG
145108-58-3 SECONDARY_CAS_RN
228054 RXNORM
4021214 VANDF
4021215 VANDF
C0113293 UMLSCUI
CHEBI:4466 CHEBI
CZX PDB_CHEM_ID
CHEMBL778 ChEMBL_ID
DB00633 DRUGBANK_ID
CHEMBL2106195 ChEMBL_ID
D020927 MESH_DESCRIPTOR_UI
5311068 PUBCHEM_CID
521 IUPHAR_LIGAND_ID
6277 INN_ID
67VB76HONO UNII
227894 MMSL
29394 MMSL
31641 MMSL
8598 MMSL
d04505 MMSL
008084 NDDF
008085 NDDF
116348007 SNOMEDCT_US
437750002 SNOMEDCT_US
438079000 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Dexmedetomidine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0143-9198 INJECTION, SOLUTION 4 ug INTRAVENOUS ANDA 30 sections
Dexmedetomidine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0143-9525 INJECTION, SOLUTION 4 ug INTRAVENOUS ANDA 30 sections
Dexmedetomidine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 0143-9526 INJECTION, SOLUTION 4 ug INTRAVENOUS ANDA 30 sections
Dexmedetomidine HCl HUMAN PRESCRIPTION DRUG LABEL 1 0143-9532 INJECTION 100 ug INTRAVENOUS ANDA 29 sections
DEXMEDETOMIDINE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 0338-9555 INJECTION 200 ug INTRAVENOUS ANDA 29 sections
DEXMEDETOMIDINE HYDROCHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 0338-9557 INJECTION 400 ug INTRAVENOUS ANDA 29 sections
PRECEDEX HUMAN PRESCRIPTION DRUG LABEL 1 0404-9938 INJECTION, SOLUTION, CONCENTRATE 100 ug INTRAVENOUS NDA 18 sections
Precedex HUMAN PRESCRIPTION DRUG LABEL 1 0409-0155 INJECTION, SOLUTION 4 ug INTRAVENOUS NDA 31 sections
Precedex HUMAN PRESCRIPTION DRUG LABEL 1 0409-1174 INJECTION, SOLUTION 4 ug INTRAVENOUS NDA 34 sections
Precedex HUMAN PRESCRIPTION DRUG LABEL 1 0409-1434 INJECTION, SOLUTION 4 ug INTRAVENOUS NDA 34 sections
Precedex HUMAN PRESCRIPTION DRUG LABEL 1 0409-1454 INJECTION, SOLUTION 4 ug INTRAVENOUS NDA 34 sections
Precedex HUMAN PRESCRIPTION DRUG LABEL 1 0409-1596 INJECTION, SOLUTION 4 ug INTRAVENOUS NDA 34 sections
Precedex HUMAN PRESCRIPTION DRUG LABEL 1 0409-1638 INJECTION, SOLUTION, CONCENTRATE 100 ug INTRAVENOUS NDA 34 sections
Precedex HUMAN PRESCRIPTION DRUG LABEL 1 0409-1660 INJECTION, SOLUTION 4 ug INTRAVENOUS NDA 34 sections
Precedex HUMAN PRESCRIPTION DRUG LABEL 1 0409-2815 INJECTION, SOLUTION 4 ug INTRAVENOUS NDA 34 sections
Precedex HUMAN PRESCRIPTION DRUG LABEL 1 0409-3301 INJECTION, SOLUTION 4 ug INTRAVENOUS NDA 34 sections
Precedex HUMAN PRESCRIPTION DRUG LABEL 1 0409-4596 INJECTION, SOLUTION 4 ug INTRAVENOUS NDA 31 sections
Precedex HUMAN PRESCRIPTION DRUG LABEL 1 0409-7838 INJECTION, SOLUTION 4 ug INTRAVENOUS NDA 34 sections
Precedex HUMAN PRESCRIPTION DRUG LABEL 1 0409-7853 INJECTION, SOLUTION 4 ug INTRAVENOUS NDA 34 sections
Precedex HUMAN PRESCRIPTION DRUG LABEL 1 0409-7875 INJECTION, SOLUTION 4 ug INTRAVENOUS NDA 34 sections
DEXMEDETOMIDINE HYDROCHLORIDE IN 0.9% SODIUM CHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 0781-3493 INJECTION 4 ug INTRAVENOUS ANDA 29 sections
DEXMEDETOMIDINE HYDROCHLORIDE IN 0.9% SODIUM CHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 0781-3494 INJECTION 4 ug INTRAVENOUS ANDA 29 sections
DEXMEDETOMIDINE HYDROCHLORIDE IN 0.9% SODIUM CHLORIDE HUMAN PRESCRIPTION DRUG LABEL 1 0781-3495 INJECTION 4 ug INTRAVENOUS ANDA 29 sections
Dexmedetomidine HUMAN PRESCRIPTION DRUG LABEL 1 16729-239 INJECTION, SOLUTION 100 ug INTRAVENOUS ANDA 27 sections
DEXMEDETOMIDINE HUMAN PRESCRIPTION DRUG LABEL 1 16729-432 INJECTION, SOLUTION 100 ug INTRAVENOUS ANDA 28 sections
Dexmedetomidine HUMAN PRESCRIPTION DRUG LABEL 1 17478-055 INJECTION, SOLUTION, CONCENTRATE 100 ug INTRAVENOUS ANDA 32 sections
Dexmedetomidine Hydrochloride in 0.9% Sodium Chloride HUMAN PRESCRIPTION DRUG LABEL 1 25021-615 INJECTION, SOLUTION 4 ug INTRAVENOUS ANDA 32 sections
Dexmedetomidine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 25021-617 INJECTION 4 ug INTRAVENOUS ANDA 33 sections
Dexmedetomidine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 36000-262 INJECTION, SOLUTION, CONCENTRATE 100 ug INTRAVENOUS ANDA 28 sections
Dexmedetomidine Hydrochloride HUMAN PRESCRIPTION DRUG LABEL 1 42023-146 INJECTION, SOLUTION, CONCENTRATE 100 ug INTRAVENOUS ANDA 31 sections