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nefopam 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 1891 | 13669-70-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Non-narcotic analgesic chemically similar to ORPHENADRINE. Its mechanism of action is unclear. It is used for the relief of acute and chronic pain. (From Martindale, The Extra Pharmacopoeia, 30th ed, p26)
|
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 34 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 3 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 1.04 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 36 % | 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) | 12 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 5 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 | 2.093 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.665 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 29.854 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 46.452 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 46.210 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 55.620 | % | High | 1 |
| herg | hERG pIC50 | 4.799 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 4.266 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 18.365 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 46.440 | % | High | 1 |
| kinase-safety-class | ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,MAPK7,MAPKAPK2,NTRK2,PDK4,PRKDC | 17 | |||
| kinase-selectivity-class | AXL,GRK2,PDK4 | 3 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.462 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 133.045 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 52.700 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 0.474 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 59.330 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 163.682 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 80.720 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 49.370 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 448.745 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 1, 1978 | YEAR INTRODUCED |
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 |
|---|---|---|---|---|---|---|
| Hepatocellular injury | 408.17 | 27.03 | 135 | 7629 | 28823 | 90591860 |
| Cholestasis | 393.50 | 27.03 | 139 | 7625 | 36160 | 90584523 |
| Hepatic cytolysis | 277.36 | 27.03 | 103 | 7661 | 30813 | 90589870 |
| Acute generalised exanthematous pustulosis | 234.15 | 27.03 | 74 | 7690 | 13629 | 90607054 |
| Acute kidney injury | 191.30 | 27.03 | 182 | 7582 | 320205 | 90300478 |
| Coma | 154.45 | 27.03 | 89 | 7675 | 72543 | 90548140 |
| Drug reaction with eosinophilia and systemic symptoms | 125.85 | 27.03 | 65 | 7699 | 42693 | 90577990 |
| Thrombocytopenia | 102.83 | 27.03 | 107 | 7657 | 208618 | 90412065 |
| Mixed liver injury | 93.26 | 27.03 | 32 | 7732 | 7591 | 90613092 |
| Drug dependence | 87.47 | 27.03 | 45 | 7719 | 29282 | 90591401 |
| Peripheral nerve injury | 78.16 | 27.03 | 17 | 7747 | 722 | 90619961 |
| Pancreatitis acute | 78.07 | 27.03 | 43 | 7721 | 32072 | 90588611 |
| Metabolic acidosis | 77.14 | 27.03 | 52 | 7712 | 55624 | 90565059 |
| Anaphylactic shock | 75.94 | 27.03 | 42 | 7722 | 31575 | 90589108 |
| Rash maculo-papular | 73.46 | 27.03 | 45 | 7719 | 40888 | 90579795 |
| Foetal megacystis | 70.85 | 27.03 | 10 | 7754 | 26 | 90620657 |
| Toxic skin eruption | 70.68 | 27.03 | 32 | 7732 | 15742 | 90604941 |
| Eosinophilia | 68.79 | 27.03 | 38 | 7726 | 28495 | 90592188 |
| Spinal epidural haemorrhage | 67.93 | 27.03 | 13 | 7751 | 288 | 90620395 |
| Epidural haemorrhage | 67.39 | 27.03 | 13 | 7751 | 301 | 90620382 |
| Fatigue | 62.05 | 27.03 | 12 | 7752 | 1154011 | 89466672 |
| Schizencephaly | 60.19 | 27.03 | 12 | 7752 | 331 | 90620352 |
| Cerebral haemorrhage foetal | 60.01 | 27.03 | 12 | 7752 | 336 | 90620347 |
| Somnolence | 59.40 | 27.03 | 81 | 7683 | 209003 | 90411680 |
| Tonic clonic movements | 59.15 | 27.03 | 16 | 7748 | 1706 | 90618977 |
| Myoclonus | 58.85 | 27.03 | 30 | 7734 | 19138 | 90601545 |
| Miosis | 58.10 | 27.03 | 24 | 7740 | 9460 | 90611223 |
| Symmetrical drug-related intertriginous and flexural exanthema | 52.66 | 27.03 | 13 | 7751 | 966 | 90619717 |
| Anticholinergic syndrome | 51.78 | 27.03 | 16 | 7748 | 2727 | 90617956 |
| Hyperkalaemia | 50.58 | 27.03 | 43 | 7721 | 64921 | 90555762 |
| Drug ineffective | 49.27 | 27.03 | 29 | 7735 | 1384269 | 89236414 |
| Poisoning deliberate | 48.29 | 27.03 | 25 | 7739 | 16461 | 90604222 |
| Foetal heart rate abnormal | 47.86 | 27.03 | 12 | 7752 | 950 | 90619733 |
| Drug interaction | 47.55 | 27.03 | 85 | 7679 | 276368 | 90344315 |
| Drug use disorder | 47.37 | 27.03 | 20 | 7744 | 8323 | 90612360 |
| Encephalopathy | 47.34 | 27.03 | 36 | 7728 | 46408 | 90574275 |
| Agranulocytosis | 46.82 | 27.03 | 32 | 7732 | 34970 | 90585713 |
| Shock haemorrhagic | 43.01 | 27.03 | 21 | 7743 | 12224 | 90608459 |
| Epidural analgesia | 42.44 | 27.03 | 8 | 7756 | 163 | 90620520 |
| Status epilepticus | 42.39 | 27.03 | 24 | 7740 | 18850 | 90601833 |
| Reversible cerebral vasoconstriction syndrome | 41.57 | 27.03 | 15 | 7749 | 4115 | 90616568 |
| Hyponatraemia | 41.36 | 27.03 | 54 | 7710 | 133484 | 90487199 |
| Posterior reversible encephalopathy syndrome | 41.19 | 27.03 | 25 | 7739 | 22314 | 90598369 |
| Urinary bladder rupture | 41.15 | 27.03 | 8 | 7756 | 193 | 90620490 |
| Purpura | 39.27 | 27.03 | 21 | 7743 | 14757 | 90605926 |
| Hypotension | 38.98 | 27.03 | 86 | 7678 | 325311 | 90295372 |
| Pain | 38.10 | 27.03 | 19 | 7745 | 996322 | 89624361 |
| Cell death | 38.04 | 27.03 | 13 | 7751 | 3042 | 90617641 |
| Shock | 37.75 | 27.03 | 26 | 7738 | 28752 | 90591931 |
| Agitation | 37.71 | 27.03 | 37 | 7727 | 67061 | 90553622 |
| Prescription drug used without a prescription | 37.24 | 27.03 | 13 | 7751 | 3242 | 90617441 |
| Hallucination | 36.37 | 27.03 | 36 | 7728 | 65923 | 90554760 |
| Tachycardia | 35.84 | 27.03 | 55 | 7709 | 157618 | 90463065 |
| Urinary retention | 35.72 | 27.03 | 28 | 7736 | 37716 | 90582967 |
| Hepatitis fulminant | 34.80 | 27.03 | 13 | 7751 | 3932 | 90616751 |
| Granulomatous liver disease | 33.45 | 27.03 | 9 | 7755 | 940 | 90619743 |
| Pancreatic pseudoaneurysm | 33.14 | 27.03 | 6 | 7758 | 97 | 90620586 |
| Cutaneous T-cell lymphoma | 32.92 | 27.03 | 10 | 7754 | 1610 | 90619073 |
| Neutropenia | 32.23 | 27.03 | 64 | 7700 | 224840 | 90395843 |
| Cardio-respiratory arrest | 32.14 | 27.03 | 33 | 7731 | 63107 | 90557576 |
| Naevus haemorrhage | 31.98 | 27.03 | 6 | 7758 | 119 | 90620564 |
| Alopecia | 31.57 | 27.03 | 3 | 7761 | 495068 | 90125615 |
| Hyperlactacidaemia | 30.63 | 27.03 | 12 | 7752 | 4124 | 90616559 |
| Abdominal discomfort | 30.15 | 27.03 | 3 | 7761 | 477325 | 90143358 |
| Term birth | 30.04 | 27.03 | 6 | 7758 | 167 | 90620516 |
| Hallucinations, mixed | 29.75 | 27.03 | 13 | 7751 | 5876 | 90614807 |
| Febrile bone marrow aplasia | 29.19 | 27.03 | 15 | 7749 | 9723 | 90610960 |
| Altered state of consciousness | 28.99 | 27.03 | 23 | 7741 | 31509 | 90589174 |
| Porphyria | 28.94 | 27.03 | 6 | 7758 | 202 | 90620481 |
| Blood phosphorus decreased | 28.35 | 27.03 | 12 | 7752 | 5022 | 90615661 |
| Stevens-Johnson syndrome | 28.24 | 27.03 | 22 | 7742 | 29354 | 90591329 |
| Pneumonia | 27.81 | 27.03 | 10 | 7754 | 638049 | 89982634 |
| Skin reaction | 27.29 | 27.03 | 18 | 7746 | 18535 | 90602148 |
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 |
|---|---|---|---|---|---|---|
| Agranulocytosis | 224.49 | 29.71 | 101 | 5789 | 30511 | 42584934 |
| Cholestasis | 177.94 | 29.71 | 88 | 5802 | 32791 | 42582654 |
| Rash maculo-papular | 161.32 | 29.71 | 86 | 5804 | 37417 | 42578028 |
| Eosinophilia | 154.45 | 29.71 | 80 | 5810 | 32819 | 42582626 |
| Drug reaction with eosinophilia and systemic symptoms | 149.35 | 29.71 | 85 | 5805 | 41990 | 42573455 |
| Hepatic cytolysis | 139.71 | 29.71 | 70 | 5820 | 26774 | 42588671 |
| Hepatocellular injury | 123.95 | 29.71 | 62 | 5828 | 23616 | 42591829 |
| Confusional state | 104.71 | 29.71 | 122 | 5768 | 167475 | 42447970 |
| Alveolar lung disease | 89.31 | 29.71 | 19 | 5871 | 443 | 42615002 |
| Pulmonary interstitial emphysema syndrome | 85.57 | 29.71 | 19 | 5871 | 544 | 42614901 |
| Acute kidney injury | 82.59 | 29.71 | 166 | 5724 | 367171 | 42248274 |
| Toxic skin eruption | 77.90 | 29.71 | 38 | 5852 | 13692 | 42601753 |
| Anti factor V antibody | 66.89 | 29.71 | 14 | 5876 | 301 | 42615144 |
| Acute generalised exanthematous pustulosis | 61.73 | 29.71 | 28 | 5862 | 8567 | 42606878 |
| Diffuse alveolar damage | 60.84 | 29.71 | 20 | 5870 | 2572 | 42612873 |
| Mixed liver injury | 57.24 | 29.71 | 22 | 5868 | 4452 | 42610993 |
| Hyperleukocytosis | 56.72 | 29.71 | 19 | 5871 | 2589 | 42612856 |
| Urethral valves | 51.97 | 29.71 | 11 | 5879 | 250 | 42615195 |
| Pancreatitis acute | 50.93 | 29.71 | 40 | 5850 | 33524 | 42581921 |
| Pancytopenia | 50.13 | 29.71 | 71 | 5819 | 117672 | 42497773 |
| Ischaemic stroke | 48.49 | 29.71 | 33 | 5857 | 22200 | 42593245 |
| Drug ineffective | 47.96 | 29.71 | 14 | 5876 | 630183 | 41985262 |
| Hyperammonaemia | 45.29 | 29.71 | 22 | 5868 | 7844 | 42607601 |
| Eosinophilic pneumonia | 45.16 | 29.71 | 19 | 5871 | 4855 | 42610590 |
| Cell death | 43.10 | 29.71 | 16 | 5874 | 2943 | 42612502 |
| Fatigue | 43.02 | 29.71 | 5 | 5885 | 435636 | 42179809 |
| Oesophageal achalasia | 40.79 | 29.71 | 10 | 5880 | 444 | 42615001 |
| Anaphylactic shock | 39.99 | 29.71 | 30 | 5860 | 23487 | 42591958 |
| Cerebral haematoma | 39.41 | 29.71 | 18 | 5872 | 5592 | 42609853 |
| Urinary retention | 39.13 | 29.71 | 38 | 5852 | 42176 | 42573269 |
| Enterobacter pneumonia | 38.68 | 29.71 | 10 | 5880 | 551 | 42614894 |
| Consciousness fluctuating | 38.48 | 29.71 | 12 | 5878 | 1303 | 42614142 |
| Secondary adrenocortical insufficiency | 36.74 | 29.71 | 13 | 5877 | 2086 | 42613359 |
| Generalised oedema | 34.00 | 29.71 | 23 | 5867 | 15313 | 42600132 |
| Haemolytic anaemia | 33.80 | 29.71 | 21 | 5869 | 12106 | 42603339 |
| Hepatic encephalopathy | 32.55 | 29.71 | 23 | 5867 | 16419 | 42599026 |
| Hallucination, visual | 31.76 | 29.71 | 25 | 5865 | 20995 | 42594450 |
| Hallucination | 31.07 | 29.71 | 39 | 5851 | 57468 | 42557977 |
| Pyroglutamic acidosis | 30.88 | 29.71 | 9 | 5881 | 776 | 42614669 |
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 |
|---|---|---|---|---|---|---|
| Cholestasis | 539.61 | 23.58 | 225 | 13231 | 64293 | 110511550 |
| Hepatocellular injury | 493.09 | 23.58 | 197 | 13259 | 50445 | 110525398 |
| Hepatic cytolysis | 397.22 | 23.58 | 173 | 13283 | 54880 | 110520963 |
| Acute generalised exanthematous pustulosis | 273.89 | 23.58 | 102 | 13354 | 21562 | 110554281 |
| Drug reaction with eosinophilia and systemic symptoms | 264.38 | 23.58 | 149 | 13307 | 81946 | 110493897 |
| Agranulocytosis | 251.53 | 23.58 | 131 | 13325 | 61629 | 110514214 |
| Acute kidney injury | 251.01 | 23.58 | 345 | 13111 | 635085 | 109940758 |
| Rash maculo-papular | 226.27 | 23.58 | 130 | 13326 | 74092 | 110501751 |
| Eosinophilia | 222.00 | 23.58 | 118 | 13338 | 57818 | 110518025 |
| Coma | 158.27 | 23.58 | 124 | 13332 | 117745 | 110458098 |
| Toxic skin eruption | 146.33 | 23.58 | 70 | 13386 | 27445 | 110548398 |
| Mixed liver injury | 138.59 | 23.58 | 53 | 13403 | 12026 | 110563817 |
| Pancreatitis acute | 128.37 | 23.58 | 84 | 13372 | 60190 | 110515653 |
| Thrombocytopenia | 110.33 | 23.58 | 171 | 13285 | 348714 | 110227129 |
| Fatigue | 106.50 | 23.58 | 12 | 13444 | 1215946 | 109359897 |
| Anaphylactic shock | 105.29 | 23.58 | 70 | 13386 | 51476 | 110524367 |
| Confusional state | 97.57 | 23.58 | 191 | 13265 | 468489 | 110107354 |
| Alveolar lung disease | 88.74 | 23.58 | 20 | 13436 | 699 | 110575144 |
| Pulmonary interstitial emphysema syndrome | 87.56 | 23.58 | 19 | 13437 | 556 | 110575287 |
| Drug dependence | 83.49 | 23.58 | 60 | 13396 | 49960 | 110525883 |
| Drug ineffective | 83.01 | 23.58 | 41 | 13415 | 1520499 | 109055344 |
| Cell death | 75.84 | 23.58 | 28 | 13428 | 5763 | 110570080 |
| Urinary retention | 73.96 | 23.58 | 64 | 13392 | 69619 | 110506224 |
| Symmetrical drug-related intertriginous and flexural exanthema | 69.48 | 23.58 | 20 | 13436 | 1877 | 110573966 |
| Encephalopathy | 69.44 | 23.58 | 66 | 13390 | 80989 | 110494854 |
| Anti factor V antibody | 68.35 | 23.58 | 14 | 13442 | 308 | 110575535 |
| Shock haemorrhagic | 68.01 | 23.58 | 42 | 13414 | 27205 | 110548638 |
| Pancytopenia | 66.50 | 23.58 | 103 | 13353 | 209510 | 110366333 |
| Peripheral nerve injury | 64.78 | 23.58 | 17 | 13439 | 1131 | 110574712 |
| Hallucination | 63.95 | 23.58 | 70 | 13386 | 101362 | 110474481 |
| Tonic clonic movements | 60.77 | 23.58 | 20 | 13436 | 2932 | 110572911 |
| Miosis | 60.30 | 23.58 | 36 | 13420 | 21947 | 110553896 |
| Epidural haemorrhage | 59.28 | 23.58 | 13 | 13443 | 400 | 110575443 |
| Metabolic acidosis | 56.32 | 23.58 | 65 | 13391 | 99679 | 110476164 |
| Spinal epidural haemorrhage | 56.16 | 23.58 | 12 | 13444 | 326 | 110575517 |
| Myoclonus | 56.02 | 23.58 | 40 | 13416 | 32958 | 110542885 |
| Diffuse alveolar damage | 54.59 | 23.58 | 20 | 13436 | 4027 | 110571816 |
| Hyperleukocytosis | 53.93 | 23.58 | 19 | 13437 | 3420 | 110572423 |
| Haemolytic anaemia | 51.58 | 23.58 | 32 | 13424 | 20888 | 110554955 |
| Status epilepticus | 50.69 | 23.58 | 37 | 13419 | 31534 | 110544309 |
| Pain | 50.09 | 23.58 | 27 | 13429 | 954928 | 109620915 |
| Cerebral haematoma | 49.66 | 23.58 | 24 | 13432 | 9608 | 110566235 |
| Cardio-respiratory arrest | 48.55 | 23.58 | 65 | 13391 | 115771 | 110460072 |
| Drug interaction | 48.30 | 23.58 | 152 | 13304 | 500031 | 110075812 |
| Ischaemic stroke | 48.08 | 23.58 | 40 | 13416 | 41223 | 110534620 |
| Foetal heart rate abnormal | 47.90 | 23.58 | 12 | 13444 | 663 | 110575180 |
| Neutropenia | 46.92 | 23.58 | 125 | 13331 | 374495 | 110201348 |
| Somnolence | 46.46 | 23.58 | 108 | 13348 | 297341 | 110278502 |
| Febrile bone marrow aplasia | 46.35 | 23.58 | 28 | 13428 | 17437 | 110558406 |
| Posterior reversible encephalopathy syndrome | 46.19 | 23.58 | 36 | 13420 | 33825 | 110542018 |
| Cholestatic liver injury | 46.12 | 23.58 | 21 | 13435 | 7355 | 110568488 |
| Drug use disorder | 45.46 | 23.58 | 28 | 13428 | 18046 | 110557797 |
| Poisoning deliberate | 44.88 | 23.58 | 32 | 13424 | 26299 | 110549544 |
| Lichenoid keratosis | 42.77 | 23.58 | 19 | 13437 | 6283 | 110569560 |
| Gamma-glutamyltransferase increased | 41.60 | 23.58 | 44 | 13412 | 61265 | 110514578 |
| Hepatitis | 41.57 | 23.58 | 53 | 13403 | 90001 | 110485842 |
| Agitation | 40.74 | 23.58 | 59 | 13397 | 112992 | 110462851 |
| Eosinophilic pneumonia | 40.28 | 23.58 | 19 | 13437 | 7208 | 110568635 |
| Pneumonia | 40.13 | 23.58 | 29 | 13427 | 876685 | 109699158 |
| Epidural analgesia | 39.55 | 23.58 | 8 | 13448 | 165 | 110575678 |
| Anticholinergic syndrome | 39.33 | 23.58 | 16 | 13440 | 4264 | 110571579 |
| Hallucination, visual | 39.25 | 23.58 | 35 | 13421 | 39570 | 110536273 |
| Hyperammonaemia | 39.00 | 23.58 | 23 | 13433 | 13709 | 110562134 |
| Hepatitis acute | 37.13 | 23.58 | 25 | 13431 | 18741 | 110557102 |
| Hepatic encephalopathy | 36.30 | 23.58 | 29 | 13427 | 28227 | 110547616 |
| Hyperbilirubinaemia | 36.29 | 23.58 | 30 | 13426 | 30641 | 110545202 |
| Anaphylactic reaction | 35.98 | 23.58 | 56 | 13400 | 114244 | 110461599 |
| Headache | 35.64 | 23.58 | 33 | 13423 | 882344 | 109693499 |
| Secondary adrenocortical insufficiency | 35.42 | 23.58 | 15 | 13441 | 4419 | 110571424 |
| Reversible cerebral vasoconstriction syndrome | 34.40 | 23.58 | 15 | 13441 | 4746 | 110571097 |
| Enterobacter pneumonia | 34.33 | 23.58 | 9 | 13447 | 596 | 110575247 |
| Hyperthermia | 34.30 | 23.58 | 25 | 13431 | 21247 | 110554596 |
| Bradypnoea | 34.17 | 23.58 | 18 | 13438 | 8631 | 110567212 |
| Nasopharyngitis | 34.12 | 23.58 | 4 | 13452 | 394357 | 110181486 |
| Hallucinations, mixed | 34.09 | 23.58 | 18 | 13438 | 8675 | 110567168 |
| Abdominal discomfort | 34.06 | 23.58 | 4 | 13452 | 393854 | 110181989 |
| Oesophageal achalasia | 34.01 | 23.58 | 10 | 13446 | 1011 | 110574832 |
| Consciousness fluctuating | 33.93 | 23.58 | 12 | 13444 | 2184 | 110573659 |
| Cytokine release syndrome | 33.43 | 23.58 | 42 | 13414 | 70264 | 110505579 |
| Altered state of consciousness | 33.27 | 23.58 | 38 | 13418 | 57588 | 110518255 |
| Weight increased | 32.29 | 23.58 | 6 | 13450 | 419638 | 110156205 |
| Pancreatic pseudoaneurysm | 31.10 | 23.58 | 6 | 13450 | 96 | 110575747 |
| Transaminases increased | 30.35 | 23.58 | 38 | 13418 | 63352 | 110512491 |
| Drug hypersensitivity | 30.00 | 23.58 | 9 | 13447 | 454081 | 110121762 |
| Naevus haemorrhage | 29.88 | 23.58 | 6 | 13450 | 119 | 110575724 |
| Prothrombin time ratio decreased | 29.64 | 23.58 | 10 | 13446 | 1582 | 110574261 |
| Weight decreased | 29.64 | 23.58 | 10 | 13446 | 468047 | 110107796 |
| Purpura | 29.15 | 23.58 | 24 | 13432 | 24364 | 110551479 |
| Hyponatraemia | 28.61 | 23.58 | 74 | 13382 | 217579 | 110358264 |
| Generalised oedema | 28.20 | 23.58 | 26 | 13430 | 30678 | 110545165 |
| Infusion related reaction | 28.17 | 23.58 | 6 | 13450 | 381156 | 110194687 |
| Renal failure | 27.71 | 23.58 | 75 | 13381 | 226499 | 110349344 |
| Lactic acidosis | 27.17 | 23.58 | 44 | 13412 | 92767 | 110483076 |
| Peripheral swelling | 26.70 | 23.58 | 8 | 13448 | 404026 | 110171817 |
| Prescription drug used without a prescription | 26.25 | 23.58 | 13 | 13443 | 5483 | 110570360 |
| Arthralgia | 26.11 | 23.58 | 34 | 13422 | 779598 | 109796245 |
| Porphyria | 25.88 | 23.58 | 6 | 13450 | 238 | 110575605 |
| Disorientation | 25.62 | 23.58 | 37 | 13419 | 70634 | 110505209 |
| Rash pustular | 25.16 | 23.58 | 17 | 13439 | 12812 | 110563031 |
| Anuria | 25.09 | 23.58 | 22 | 13434 | 24319 | 110551524 |
| Respiratory distress | 24.88 | 23.58 | 36 | 13420 | 68838 | 110507005 |
| Abdominal pain upper | 24.78 | 23.58 | 6 | 13450 | 349105 | 110226738 |
| Alopecia | 24.51 | 23.58 | 7 | 13449 | 364746 | 110211097 |
| Seizure | 23.90 | 23.58 | 70 | 13386 | 221115 | 110354728 |
| Hyperlactacidaemia | 23.85 | 23.58 | 14 | 13442 | 8272 | 110567571 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N02BG06 | NERVOUS SYSTEM ANALGESICS OTHER ANALGESICS AND ANTIPYRETICS Other analgesics and antipyretics |
| MeSH PA | D000700 | Analgesics |
| MeSH PA | D018689 | Sensory System Agents |
| MeSH PA | D018712 | Analgesics, Non-Narcotic |
| CHEBI has role | CHEBI:35481 | non-narcotic analgesic |
| CHEBI has role | CHEBI:35640 | adrenergic uptake inhibitor |
| CHEBI has role | CHEBI:50949 | serotonin uptake inhibitor |
| CHEBI has role | CHEBI:51039 | dopamine uptake inhibitor |
| CHEBI has role | CHEBI:35480 | analgesic |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
Related Drugs by ATC class:
N02BG Other analgesics and antipyretics 8 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
None
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 7.85 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Sodium channel protein type 5 subunit alpha | Ion channel | WOMBAT-PK | |||||||
| Sodium-dependent serotonin transporter | Transporter | Ki | 7.54 | PDSP | |||||
| Sodium-dependent noradrenaline transporter | Transporter | Ki | 7.48 | PDSP | |||||
| 5-hydroxytryptamine receptor 2A | GPCR | Ki | 5.77 | PDSP | |||||
| 5-hydroxytryptamine receptor 2B | GPCR | Ki | 6.48 | PDSP | |||||
| 5-hydroxytryptamine receptor 2C | GPCR | Ki | 7.25 | PDSP | |||||
| Sodium-dependent dopamine transporter | Transporter | Ki | 6.28 | PDSP |
External reference:
| ID | Source |
|---|---|
| N0000167217 | NUI |
| D05133 | KEGG_DRUG |
| C0027556 | UMLSCUI |
| CHEBI:88316 | CHEBI |
| CHEMBL465026 | ChEMBL_ID |
| DB12293 | DRUGBANK_ID |
| CHEMBL1407915 | ChEMBL_ID |
| D009340 | MESH_DESCRIPTOR_UI |
| 4450 | PUBCHEM_CID |
| 3018 | INN_ID |
| 23327-57-3 | SECONDARY_CAS_RN |
| 4UP8060B7J | UNII |
| 4324 | RXNORM |
| 001582 | NDDF |
| 004636 | NDDF |
| 322300008 | SNOMEDCT_US |
| 350324006 | SNOMEDCT_US |
| 419768004 | SNOMEDCT_US |
| 4UP8060B7J | INXIGHT DRUGS |
Pharmaceutical products:
None