promethazine Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2286 | 60-87-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A phenothiazine derivative with histamine H1-blocking, antimuscarinic, and sedative properties. It is used as an antiallergic, in pruritus, for motion sickness and sedation, and also in animals.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 25 | mg | O |
| 25 | mg | P |
| 25 | mg | R |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 2 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 5.03 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) | 14 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 14 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.09 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 14 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 29, 1951 | FDA | DELCOR ASSET CORP |
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 |
|---|---|---|---|---|---|---|
| Intentional self-injury | 6053.80 | 9.99 | 2023 | 72462 | 22143 | 46589434 |
| Intentional overdose | 4875.76 | 9.99 | 2271 | 72214 | 62673 | 46548904 |
| Akathisia | 500.48 | 9.99 | 245 | 74240 | 7469 | 46604108 |
| Depressed level of consciousness | 375.28 | 9.99 | 420 | 74065 | 47149 | 46564428 |
| Tachycardia | 361.30 | 9.99 | 603 | 73882 | 99019 | 46512558 |
| Mydriasis | 268.26 | 9.99 | 182 | 74303 | 10371 | 46601206 |
| Cholecystitis chronic | 252.53 | 9.99 | 175 | 74310 | 10324 | 46601253 |
| Drug ineffective | 224.02 | 9.99 | 468 | 74017 | 677370 | 45934207 |
| Rheumatoid arthritis | 186.55 | 9.99 | 75 | 74410 | 240140 | 46371437 |
| Anxiety | 151.55 | 9.99 | 633 | 73852 | 181324 | 46430253 |
| Toxicity to various agents | 147.93 | 9.99 | 699 | 73786 | 211067 | 46400510 |
| Drug abuse | 129.73 | 9.99 | 302 | 74183 | 63106 | 46548471 |
| Hallucination | 111.16 | 9.99 | 246 | 74239 | 49705 | 46561872 |
| Treatment failure | 109.01 | 9.99 | 11 | 74474 | 93076 | 46518501 |
| Suicide attempt | 108.08 | 9.99 | 258 | 74227 | 54778 | 46556799 |
| Injury | 99.28 | 9.99 | 218 | 74267 | 43809 | 46567768 |
| Nausea | 98.51 | 9.99 | 1589 | 72896 | 685865 | 45925712 |
| Contraindicated product administered | 94.78 | 9.99 | 9 | 74476 | 79938 | 46531639 |
| Poisoning | 94.25 | 9.99 | 114 | 74371 | 13880 | 46597697 |
| Off label use | 92.22 | 9.99 | 305 | 74180 | 379536 | 46232041 |
| Vomiting | 91.51 | 9.99 | 1113 | 73372 | 451681 | 46159896 |
| Somnolence | 89.72 | 9.99 | 489 | 73996 | 156032 | 46455545 |
| Biliary dyskinesia | 80.58 | 9.99 | 52 | 74433 | 2721 | 46608856 |
| Drug intolerance | 78.93 | 9.99 | 71 | 74414 | 146978 | 46464599 |
| Gallbladder disorder | 77.19 | 9.99 | 116 | 74369 | 17382 | 46594195 |
| Sinus tachycardia | 76.91 | 9.99 | 130 | 74355 | 21519 | 46590058 |
| Agitation | 74.65 | 9.99 | 226 | 74259 | 55189 | 46556388 |
| Gallbladder injury | 72.60 | 9.99 | 38 | 74447 | 1336 | 46610241 |
| Joint swelling | 69.68 | 9.99 | 98 | 74387 | 165975 | 46445602 |
| Synovitis | 69.50 | 9.99 | 8 | 74477 | 61067 | 46550510 |
| Emotional distress | 69.16 | 9.99 | 152 | 74333 | 30555 | 46581022 |
| Completed suicide | 67.52 | 9.99 | 431 | 74054 | 145489 | 46466088 |
| Migraine | 67.30 | 9.99 | 255 | 74230 | 69771 | 46541806 |
| Muscle twitching | 50.65 | 9.99 | 87 | 74398 | 14585 | 46596992 |
| Accidental overdose | 50.58 | 9.99 | 104 | 74381 | 19962 | 46591615 |
| Cholelithiasis | 49.52 | 9.99 | 155 | 74330 | 38526 | 46573051 |
| Snoring | 48.95 | 9.99 | 42 | 74443 | 3400 | 46608177 |
| Incoherent | 46.53 | 9.99 | 46 | 74439 | 4466 | 46607111 |
| Dependence | 45.98 | 9.99 | 32 | 74453 | 1899 | 46609678 |
| Serotonin syndrome | 45.87 | 9.99 | 112 | 74373 | 24108 | 46587469 |
| Opisthotonus | 45.74 | 9.99 | 18 | 74467 | 319 | 46611258 |
| Therapeutic product effect incomplete | 45.28 | 9.99 | 35 | 74450 | 78118 | 46533459 |
| Arthralgia | 44.60 | 9.99 | 370 | 74115 | 364233 | 46247344 |
| Glossodynia | 43.26 | 9.99 | 9 | 74476 | 44364 | 46567213 |
| Accidental death | 42.74 | 9.99 | 30 | 74455 | 1805 | 46609772 |
| Formication | 42.04 | 9.99 | 41 | 74444 | 3915 | 46607662 |
| Hand deformity | 40.68 | 9.99 | 4 | 74481 | 34570 | 46577007 |
| Cardiac failure | 37.85 | 9.99 | 43 | 74442 | 79905 | 46531672 |
| Respiratory arrest | 37.44 | 9.99 | 129 | 74356 | 33687 | 46577890 |
| Therapeutic product effect decreased | 37.42 | 9.99 | 46 | 74439 | 82555 | 46529022 |
| Lethargy | 37.12 | 9.99 | 171 | 74314 | 51000 | 46560577 |
| Hepatic enzyme increased | 34.53 | 9.99 | 48 | 74437 | 81739 | 46529838 |
| Mental status changes | 34.37 | 9.99 | 136 | 74349 | 37952 | 46573625 |
| Abdominal pain | 33.83 | 9.99 | 535 | 73950 | 229496 | 46382081 |
| Electrocardiogram QRS complex shortened | 33.66 | 9.99 | 15 | 74470 | 367 | 46611210 |
| Rash | 33.38 | 9.99 | 386 | 74099 | 356126 | 46255451 |
| Dysarthria | 33.12 | 9.99 | 133 | 74352 | 37365 | 46574212 |
| Pupillary reflex impaired | 33.06 | 9.99 | 27 | 74458 | 2041 | 46609536 |
| Abdominal discomfort | 32.81 | 9.99 | 127 | 74358 | 151038 | 46460539 |
| Infusion related reaction | 32.19 | 9.99 | 71 | 74414 | 101137 | 46510440 |
| Lower respiratory tract infection | 31.49 | 9.99 | 25 | 74460 | 55064 | 46556513 |
| Exposure via ingestion | 31.48 | 9.99 | 33 | 74452 | 3434 | 46608143 |
| Hereditary angioedema | 30.90 | 9.99 | 41 | 74444 | 5475 | 46606102 |
| Arthropathy | 30.74 | 9.99 | 55 | 74430 | 84645 | 46526932 |
| Loss of consciousness | 29.07 | 9.99 | 282 | 74203 | 107956 | 46503621 |
| Suicidal ideation | 28.84 | 9.99 | 171 | 74314 | 56211 | 46555366 |
| Drug reaction with eosinophilia and systemic symptoms | 28.79 | 9.99 | 6 | 74479 | 29542 | 46582035 |
| Nasopharyngitis | 28.75 | 9.99 | 137 | 74348 | 153861 | 46457716 |
| C-reactive protein increased | 28.29 | 9.99 | 31 | 74454 | 58559 | 46553018 |
| Anticholinergic syndrome | 27.66 | 9.99 | 23 | 74462 | 1783 | 46609794 |
| Fatigue | 27.39 | 9.99 | 1209 | 73276 | 607488 | 46004089 |
| Infection | 26.63 | 9.99 | 116 | 74369 | 133476 | 46478101 |
| Drug hypersensitivity | 26.60 | 9.99 | 541 | 73944 | 243284 | 46368293 |
| Deep vein thrombosis | 25.58 | 9.99 | 216 | 74269 | 79557 | 46532020 |
| Cholestasis | 25.11 | 9.99 | 6 | 74479 | 26887 | 46584690 |
| Drug screen positive | 25.07 | 9.99 | 31 | 74454 | 3860 | 46607717 |
| Product counterfeit | 24.87 | 9.99 | 9 | 74476 | 125 | 46611452 |
| Acute kidney injury | 24.59 | 9.99 | 249 | 74236 | 235606 | 46375971 |
| Drug abuser | 24.53 | 9.99 | 28 | 74457 | 3205 | 46608372 |
| Depression | 24.00 | 9.99 | 393 | 74092 | 169711 | 46441866 |
| Systemic lupus erythematosus | 23.94 | 9.99 | 42 | 74443 | 65138 | 46546439 |
| Renal impairment | 23.79 | 9.99 | 52 | 74433 | 74320 | 46537257 |
| Restlessness | 23.72 | 9.99 | 92 | 74393 | 25432 | 46586145 |
| Neutropenia | 23.03 | 9.99 | 134 | 74351 | 143070 | 46468507 |
| Product use issue | 22.86 | 9.99 | 76 | 74409 | 94568 | 46517009 |
| Arthritis | 22.38 | 9.99 | 57 | 74428 | 77259 | 46534318 |
| Device expulsion | 22.32 | 9.99 | 8 | 74477 | 27534 | 46584043 |
| Fall | 22.01 | 9.99 | 381 | 74104 | 328716 | 46282861 |
| Somatic delusion | 21.61 | 9.99 | 13 | 74472 | 600 | 46610977 |
| Pancreatitis chronic | 21.57 | 9.99 | 20 | 74465 | 1793 | 46609784 |
| Melaena | 20.97 | 9.99 | 9 | 74476 | 27763 | 46583814 |
| Poor feeding infant | 20.83 | 9.99 | 9 | 74476 | 204 | 46611373 |
| Therapeutic response decreased | 20.64 | 9.99 | 23 | 74462 | 43122 | 46568455 |
| Hyperreflexia | 20.61 | 9.99 | 33 | 74452 | 5221 | 46606356 |
| Gallbladder hypofunction | 20.57 | 9.99 | 12 | 74473 | 523 | 46611054 |
| Cholecystitis | 20.41 | 9.99 | 60 | 74425 | 14406 | 46597171 |
| Mental disorder | 20.17 | 9.99 | 80 | 74405 | 22345 | 46589232 |
| Overdose | 20.14 | 9.99 | 250 | 74235 | 101729 | 46509848 |
| Hepatocellular injury | 20.11 | 9.99 | 11 | 74474 | 29511 | 46582066 |
| Dehydration | 20.11 | 9.99 | 362 | 74123 | 159178 | 46452399 |
| Hypopnoea | 20.09 | 9.99 | 22 | 74463 | 2406 | 46609171 |
| Hyponatraemia | 19.58 | 9.99 | 89 | 74396 | 101243 | 46510334 |
| Peripheral swelling | 19.45 | 9.99 | 160 | 74325 | 157911 | 46453666 |
| Impaired gastric emptying | 19.36 | 9.99 | 41 | 74444 | 8031 | 46603546 |
| Pericarditis | 19.31 | 9.99 | 7 | 74478 | 23920 | 46587657 |
| Wound | 19.21 | 9.99 | 24 | 74461 | 42778 | 46568799 |
| Alopecia | 18.82 | 9.99 | 167 | 74318 | 162247 | 46449330 |
| Gallbladder cholesterolosis | 18.73 | 9.99 | 13 | 74472 | 768 | 46610809 |
| Cholecystectomy | 18.40 | 9.99 | 43 | 74442 | 8999 | 46602578 |
| Helplessness | 17.33 | 9.99 | 8 | 74477 | 213 | 46611364 |
| Cough | 17.22 | 9.99 | 261 | 74224 | 229988 | 46381589 |
| General physical health deterioration | 17.22 | 9.99 | 111 | 74374 | 115658 | 46495919 |
| Cholesterosis | 17.16 | 9.99 | 10 | 74475 | 435 | 46611142 |
| Cardiac arrest | 17.16 | 9.99 | 220 | 74265 | 90179 | 46521398 |
| Base excess increased | 17.07 | 9.99 | 4 | 74481 | 9 | 46611568 |
| Cytomegalovirus infection | 17.04 | 9.99 | 4 | 74481 | 18140 | 46593437 |
| Interstitial lung disease | 17.02 | 9.99 | 38 | 74447 | 53911 | 46557666 |
| Product use in unapproved indication | 17.02 | 9.99 | 80 | 74405 | 90193 | 46521384 |
| Illness anxiety disorder | 16.96 | 9.99 | 7 | 74478 | 141 | 46611436 |
| Pupil fixed | 16.75 | 9.99 | 17 | 74468 | 1703 | 46609874 |
| Coma blister | 16.65 | 9.99 | 7 | 74478 | 148 | 46611429 |
| Herpes zoster | 16.05 | 9.99 | 55 | 74430 | 67817 | 46543760 |
| Drug resistance | 15.97 | 9.99 | 4 | 74481 | 17364 | 46594213 |
| Differential white blood cell count abnormal | 15.79 | 9.99 | 11 | 74474 | 654 | 46610923 |
| Dyspnoea | 15.68 | 9.99 | 668 | 73817 | 514880 | 46096697 |
| Drug withdrawal syndrome | 15.27 | 9.99 | 85 | 74400 | 27299 | 46584278 |
| Blastocystis infection | 15.16 | 9.99 | 4 | 74481 | 17 | 46611560 |
| Biliary colic | 15.15 | 9.99 | 23 | 74462 | 3475 | 46608102 |
| Pneumocystis jirovecii pneumonia | 15.05 | 9.99 | 3 | 74482 | 15245 | 46596332 |
| Miosis | 15.04 | 9.99 | 33 | 74452 | 6624 | 46604953 |
| Paranoia | 15.00 | 9.99 | 44 | 74441 | 10553 | 46601024 |
| Electrocardiogram QT prolonged | 14.90 | 9.99 | 136 | 74349 | 51189 | 46560388 |
| Blood pressure fluctuation | 14.82 | 9.99 | 16 | 74469 | 30432 | 46581145 |
| Drug interaction | 14.58 | 9.99 | 232 | 74253 | 202862 | 46408715 |
| Mobility decreased | 14.39 | 9.99 | 49 | 74436 | 60545 | 46551032 |
| Hypoglycaemia | 14.28 | 9.99 | 42 | 74443 | 54307 | 46557270 |
| Uterine perforation | 14.18 | 9.99 | 34 | 74451 | 7233 | 46604344 |
| Cardio-respiratory arrest | 14.15 | 9.99 | 152 | 74333 | 59717 | 46551860 |
| Inflammation | 14.08 | 9.99 | 36 | 74449 | 48745 | 46562832 |
| Ureteric stenosis | 14.05 | 9.99 | 10 | 74475 | 615 | 46610962 |
| Injection site erythema | 14 | 9.99 | 66 | 74419 | 74361 | 46537216 |
| Maternal exposure during pregnancy | 13.92 | 9.99 | 101 | 74384 | 102448 | 46509129 |
| Thrombocytopenia | 13.86 | 9.99 | 132 | 74353 | 126449 | 46485128 |
| pH body fluid increased | 13.79 | 9.99 | 3 | 74482 | 4 | 46611573 |
| Breast cancer | 13.60 | 9.99 | 33 | 74452 | 45485 | 46566092 |
| Red blood cell sedimentation rate increased | 13.57 | 9.99 | 10 | 74475 | 22879 | 46588698 |
| Hepatitis | 13.50 | 9.99 | 19 | 74466 | 32196 | 46579381 |
| Jaw clicking | 13.50 | 9.99 | 4 | 74481 | 28 | 46611549 |
| Basal cell carcinoma | 13.43 | 9.99 | 8 | 74477 | 20479 | 46591098 |
| Sports injury | 13.26 | 9.99 | 4 | 74481 | 30 | 46611547 |
| Blood potassium decreased | 13.24 | 9.99 | 105 | 74380 | 37958 | 46573619 |
| Attention-seeking behaviour | 12.95 | 9.99 | 5 | 74480 | 84 | 46611493 |
| Vasoplegia syndrome | 12.90 | 9.99 | 12 | 74473 | 1080 | 46610497 |
| Osteonecrosis of jaw | 12.78 | 9.99 | 22 | 74463 | 34380 | 46577197 |
| Agranulocytosis | 12.76 | 9.99 | 10 | 74475 | 22175 | 46589402 |
| Ventricular septal defect | 12.73 | 9.99 | 23 | 74462 | 4011 | 46607566 |
| Fallot's tetralogy | 12.58 | 9.99 | 5 | 74480 | 91 | 46611486 |
| Bradycardia | 12.35 | 9.99 | 59 | 74426 | 66239 | 46545338 |
| Hypersensitivity | 12.06 | 9.99 | 168 | 74317 | 150153 | 46461424 |
| Heart rate decreased | 12.05 | 9.99 | 20 | 74465 | 31703 | 46579874 |
| Water intoxication | 11.83 | 9.99 | 8 | 74477 | 453 | 46611124 |
| Ischaemic stroke | 11.73 | 9.99 | 6 | 74479 | 16716 | 46594861 |
| Femur fracture | 11.72 | 9.99 | 26 | 74459 | 36971 | 46574606 |
| Pancytopenia | 11.43 | 9.99 | 84 | 74401 | 84974 | 46526603 |
| Acute lung injury | 11.36 | 9.99 | 12 | 74473 | 1259 | 46610318 |
| Atrial fibrillation | 11.34 | 9.99 | 108 | 74377 | 103482 | 46508095 |
| Product quality issue | 11.33 | 9.99 | 25 | 74460 | 35623 | 46575954 |
| Intentional product misuse | 11.30 | 9.99 | 120 | 74365 | 47008 | 46564569 |
| Drug dependence | 11.25 | 9.99 | 62 | 74423 | 19839 | 46591738 |
| Gamma-glutamyltransferase increased | 11.16 | 9.99 | 21 | 74464 | 31719 | 46579858 |
| Lipase decreased | 11.16 | 9.99 | 4 | 74481 | 54 | 46611523 |
| Injection site reaction | 11.16 | 9.99 | 39 | 74446 | 47810 | 46563767 |
| Swelling | 11.15 | 9.99 | 136 | 74349 | 124375 | 46487202 |
| Seizure | 11.15 | 9.99 | 266 | 74219 | 122788 | 46488789 |
| Anhedonia | 11.07 | 9.99 | 39 | 74446 | 10296 | 46601281 |
| Fear of disease | 11.01 | 9.99 | 11 | 74474 | 1081 | 46610496 |
| Heart rate increased | 10.98 | 9.99 | 174 | 74311 | 74617 | 46536960 |
| Infusion site macule | 10.98 | 9.99 | 3 | 74482 | 15 | 46611562 |
| Skin ulcer | 10.96 | 9.99 | 22 | 74463 | 32436 | 46579141 |
| Osteoporosis | 10.94 | 9.99 | 31 | 74454 | 40577 | 46571000 |
| Finger amputation | 10.86 | 9.99 | 8 | 74477 | 519 | 46611058 |
| Neonatal tachycardia | 10.82 | 9.99 | 3 | 74482 | 16 | 46611561 |
| Musculoskeletal stiffness | 10.80 | 9.99 | 102 | 74383 | 97891 | 46513686 |
| Jugular vein thrombosis | 10.79 | 9.99 | 17 | 74468 | 2653 | 46608924 |
| Injection site pain | 10.78 | 9.99 | 114 | 74371 | 107038 | 46504539 |
| Hyperkalaemia | 10.74 | 9.99 | 43 | 74442 | 50666 | 46560911 |
| Prolonged rupture of membranes | 10.60 | 9.99 | 4 | 74481 | 63 | 46611514 |
| Lentigo | 10.53 | 9.99 | 6 | 74479 | 250 | 46611327 |
| Toxic epidermal necrolysis | 10.52 | 9.99 | 12 | 74473 | 22266 | 46589311 |
| Psoriasis | 10.38 | 9.99 | 78 | 74407 | 78526 | 46533051 |
| Hyperkinetic heart syndrome | 10.38 | 9.99 | 3 | 74482 | 19 | 46611558 |
| Retroplacental haematoma | 10.37 | 9.99 | 5 | 74480 | 147 | 46611430 |
| Arm amputation | 10.25 | 9.99 | 3 | 74482 | 20 | 46611557 |
| Unresponsive to stimuli | 10.24 | 9.99 | 87 | 74398 | 32087 | 46579490 |
| Patient uncooperative | 10.22 | 9.99 | 5 | 74480 | 152 | 46611425 |
| Respiratory rate decreased | 10.16 | 9.99 | 18 | 74467 | 3092 | 46608485 |
| Myocardial infarction | 10.13 | 9.99 | 103 | 74382 | 97425 | 46514152 |
| Intestinal ischaemia | 10.04 | 9.99 | 29 | 74456 | 6896 | 46604681 |
| Condition aggravated | 10.03 | 9.99 | 306 | 74179 | 244746 | 46366831 |
| Pain | 10.02 | 9.99 | 887 | 73598 | 476061 | 46135516 |
| Radial pulse abnormal | 10.00 | 9.99 | 3 | 74482 | 22 | 46611555 |
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 |
|---|---|---|---|---|---|---|
| Intentional self-injury | 1949.24 | 11.04 | 663 | 28774 | 12869 | 29910172 |
| Intentional overdose | 1507.08 | 11.04 | 758 | 28679 | 40723 | 29882318 |
| Akathisia | 154.48 | 11.04 | 87 | 29350 | 5817 | 29917224 |
| Depressed level of consciousness | 103.92 | 11.04 | 156 | 29281 | 38066 | 29884975 |
| Tachycardia | 80.94 | 11.04 | 205 | 29232 | 73534 | 29849507 |
| Agitation | 65.32 | 11.04 | 156 | 29281 | 53917 | 29869124 |
| Neuroleptic malignant syndrome | 64.77 | 11.04 | 80 | 29357 | 16215 | 29906826 |
| Vomiting | 64.28 | 11.04 | 402 | 29035 | 219416 | 29703625 |
| Nausea | 62.88 | 11.04 | 502 | 28935 | 296455 | 29626586 |
| Respiratory arrest | 61.15 | 11.04 | 106 | 29331 | 29152 | 29893889 |
| Sinus tachycardia | 59.83 | 11.04 | 75 | 29362 | 15429 | 29907612 |
| Mydriasis | 59.67 | 11.04 | 49 | 29388 | 6094 | 29916947 |
| Drug ineffective | 59.30 | 11.04 | 157 | 29280 | 340230 | 29582811 |
| Somnolence | 56.55 | 11.04 | 216 | 29221 | 96547 | 29826494 |
| Poisoning | 47.04 | 11.04 | 57 | 29380 | 11325 | 29911716 |
| Off label use | 44.85 | 11.04 | 113 | 29324 | 249177 | 29673864 |
| Toxicity to various agents | 43.83 | 11.04 | 311 | 29126 | 176872 | 29746169 |
| Product counterfeit | 38.65 | 11.04 | 12 | 29425 | 170 | 29922871 |
| Lethargy | 38.34 | 11.04 | 105 | 29332 | 39414 | 29883627 |
| Exposure during pregnancy | 36.04 | 11.04 | 45 | 29392 | 9216 | 29913825 |
| Overdose | 35.86 | 11.04 | 171 | 29266 | 84166 | 29838875 |
| Drug abuse | 33.16 | 11.04 | 164 | 29273 | 81908 | 29841133 |
| Dysarthria | 31.57 | 11.04 | 83 | 29354 | 30407 | 29892634 |
| Hallucination | 30.68 | 11.04 | 112 | 29325 | 48947 | 29874094 |
| Consciousness fluctuating | 29.81 | 11.04 | 16 | 29421 | 972 | 29922069 |
| Loss of consciousness | 28.17 | 11.04 | 153 | 29284 | 79222 | 29843819 |
| Anxiety | 27.81 | 11.04 | 167 | 29270 | 89704 | 29833337 |
| Cardio-respiratory arrest | 25.66 | 11.04 | 118 | 29319 | 57188 | 29865853 |
| Pyomyositis | 24.10 | 11.04 | 8 | 29429 | 142 | 29922899 |
| Interstitial lung disease | 23.61 | 11.04 | 15 | 29422 | 60182 | 29862859 |
| Dehydration | 22.87 | 11.04 | 203 | 29234 | 123336 | 29799705 |
| Opisthotonus | 22.81 | 11.04 | 10 | 29427 | 388 | 29922653 |
| Dextrocardia | 22.80 | 11.04 | 8 | 29429 | 169 | 29922872 |
| Dystonia | 22.65 | 11.04 | 37 | 29400 | 9690 | 29913351 |
| Acute kidney injury | 22.14 | 11.04 | 168 | 29269 | 273674 | 29649367 |
| Atrial septal defect | 22.08 | 11.04 | 30 | 29407 | 6671 | 29916370 |
| Foetal alcohol syndrome | 21.47 | 11.04 | 8 | 29429 | 202 | 29922839 |
| Suicide attempt | 21.46 | 11.04 | 82 | 29355 | 36615 | 29886426 |
| General physical health deterioration | 20.60 | 11.04 | 42 | 29395 | 99902 | 29823139 |
| Sedation | 20.57 | 11.04 | 48 | 29389 | 16325 | 29906716 |
| Renal impairment | 20.38 | 11.04 | 32 | 29405 | 84152 | 29838889 |
| Paralysis | 20.34 | 11.04 | 27 | 29410 | 5874 | 29917167 |
| Exposure via ingestion | 19.63 | 11.04 | 18 | 29419 | 2593 | 29920448 |
| Hepatic ischaemia | 19.47 | 11.04 | 9 | 29428 | 396 | 29922645 |
| Failure to thrive | 19.25 | 11.04 | 31 | 29406 | 8023 | 29915018 |
| Breathing-related sleep disorder | 18.89 | 11.04 | 7 | 29430 | 174 | 29922867 |
| General symptom | 18.48 | 11.04 | 11 | 29426 | 815 | 29922226 |
| Confusional state | 18.39 | 11.04 | 208 | 29229 | 134626 | 29788415 |
| Respiratory depression | 18.19 | 11.04 | 37 | 29400 | 11466 | 29911575 |
| Serotonin syndrome | 17.80 | 11.04 | 48 | 29389 | 17843 | 29905198 |
| Treatment failure | 17.67 | 11.04 | 6 | 29431 | 34673 | 29888368 |
| Angioedema | 17.44 | 11.04 | 6 | 29431 | 34378 | 29888663 |
| Rheumatoid arthritis | 16.52 | 11.04 | 10 | 29427 | 41187 | 29881854 |
| Pupil fixed | 16.52 | 11.04 | 14 | 29423 | 1818 | 29921223 |
| Completed suicide | 16.15 | 11.04 | 159 | 29278 | 99333 | 29823708 |
| Red blood cells urine positive | 15.91 | 11.04 | 13 | 29424 | 1604 | 29921437 |
| Conduction disorder | 15.75 | 11.04 | 14 | 29423 | 1937 | 29921104 |
| Drug withdrawal syndrome | 15.71 | 11.04 | 49 | 29388 | 19760 | 29903281 |
| Fatigue | 15.67 | 11.04 | 419 | 29018 | 320254 | 29602787 |
| Myocardial infarction | 15.56 | 11.04 | 67 | 29370 | 125558 | 29797483 |
| Inappropriate schedule of product administration | 15.44 | 11.04 | 10 | 29427 | 39718 | 29883323 |
| Obsessive thoughts | 15.18 | 11.04 | 9 | 29428 | 662 | 29922379 |
| Condition aggravated | 15.04 | 11.04 | 77 | 29360 | 137789 | 29785252 |
| Patent ductus arteriosus | 14.97 | 11.04 | 17 | 29420 | 3152 | 29919889 |
| Drug withdrawal syndrome neonatal | 14.94 | 11.04 | 17 | 29420 | 3158 | 29919883 |
| Fallot's tetralogy | 14.77 | 11.04 | 6 | 29431 | 192 | 29922849 |
| Skin swelling | 14.68 | 11.04 | 10 | 29427 | 937 | 29922104 |
| Drug hypersensitivity | 13.92 | 11.04 | 115 | 29322 | 68404 | 29854637 |
| Hepatocellular injury | 13.71 | 11.04 | 4 | 29433 | 25467 | 29897574 |
| Protein urine present | 13.69 | 11.04 | 20 | 29417 | 4755 | 29918286 |
| Psoriasis | 13.61 | 11.04 | 13 | 29424 | 42493 | 29880548 |
| Poor quality product administered | 13.52 | 11.04 | 12 | 29425 | 1657 | 29921384 |
| Incision site pain | 13.51 | 11.04 | 13 | 29424 | 1991 | 29921050 |
| Foetal death | 13.37 | 11.04 | 6 | 29431 | 246 | 29922795 |
| Hyperkalaemia | 13.37 | 11.04 | 28 | 29409 | 65982 | 29857059 |
| Unresponsive to stimuli | 13.02 | 11.04 | 56 | 29381 | 26363 | 29896678 |
| Foetal exposure during pregnancy | 13.01 | 11.04 | 71 | 29366 | 36800 | 29886241 |
| Snoring | 12.80 | 11.04 | 15 | 29422 | 2876 | 29920165 |
| Cardiomegaly | 12.55 | 11.04 | 37 | 29400 | 14472 | 29908569 |
| Acute chest syndrome | 12.53 | 11.04 | 6 | 29431 | 286 | 29922755 |
| Therapeutic product effect incomplete | 12.50 | 11.04 | 9 | 29428 | 33825 | 29889216 |
| Environmental exposure | 12.47 | 11.04 | 6 | 29431 | 289 | 29922752 |
| Restlessness | 12.00 | 11.04 | 49 | 29388 | 22550 | 29900491 |
| Cardiac arrest | 11.65 | 11.04 | 141 | 29296 | 92709 | 29830332 |
| Cholestasis | 11.58 | 11.04 | 5 | 29432 | 24945 | 29898096 |
| Disorganised speech | 11.48 | 11.04 | 7 | 29430 | 542 | 29922499 |
| Product use in unapproved indication | 11.28 | 11.04 | 36 | 29401 | 73657 | 29849384 |
| Drug resistance | 11.13 | 11.04 | 3 | 29434 | 20130 | 29902911 |
| Myocarditis | 11.13 | 11.04 | 28 | 29409 | 9983 | 29913058 |
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | D04AA10 | DERMATOLOGICALS ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. Antihistamines for topical use |
| ATC | R06AD02 | RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Phenothiazine derivatives |
| ATC | R06AD52 | RESPIRATORY SYSTEM ANTIHISTAMINES FOR SYSTEMIC USE ANTIHISTAMINES FOR SYSTEMIC USE Phenothiazine derivatives |
| ATC | V03AB05 | VARIOUS ALL OTHER THERAPEUTIC PRODUCTS ALL OTHER THERAPEUTIC PRODUCTS Antidotes |
| FDA CS | M0016525 | Phenothiazines |
| FDA EPC | N0000175746 | Phenothiazine |
| MeSH PA | D018926 | Anti-Allergic Agents |
| MeSH PA | D000982 | Antipruritics |
| MeSH PA | D003879 | Dermatologic Agents |
| MeSH PA | D018494 | Histamine Agents |
| MeSH PA | D006633 | Histamine Antagonists |
| MeSH PA | D006634 | Histamine H1 Antagonists |
| MeSH PA | D018377 | Neurotransmitter Agents |
| CHEBI has role | CHEBI:35717 | sedatives |
| CHEBI has role | CHEBI:36333 | local anesthetics |
| CHEBI has role | CHEBI:37955 | h1-receptor blockers |
| CHEBI has role | CHEBI:50857 | anti-allergic agents |
| CHEBI has role | CHEBI:50919 | antiemetico |
| CHEBI has role | CHEBI:59683 | anti-itching drug |
| CHEBI has role | CHEBI:149553 | anti-coronaviral agents |
Drug Use (View source of the data)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Vasomotor rhinitis | indication | 8229003 | DOID:4730 |
| Nausea and vomiting | indication | 16932000 | |
| General anesthesia | indication | 50697003 | |
| Sedation | indication | 72641008 | |
| Urticaria | indication | 126485001 | |
| Seasonal allergic rhinitis | indication | 367498001 | |
| Allergic conjunctivitis | indication | 473460002 | DOID:11204 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.19 | Basic |
| pKa2 | 3.55 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Histamine H1 receptor | GPCR | ANTAGONIST | Ki | 9.62 | WOMBAT-PK | CHEMBL | |||
| D(1A) dopamine receptor | GPCR | Ki | 5.86 | DRUG MATRIX | |||||
| Alpha-2A adrenergic receptor | GPCR | Ki | 6.59 | DRUG MATRIX | |||||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | Ki | 6.92 | DRUG MATRIX | |||||
| Sodium-dependent noradrenaline transporter | Transporter | Ki | 5.38 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 5.83 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 2B | GPCR | Ki | 7.37 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 2C | GPCR | Ki | 8.19 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 6 | GPCR | Ki | 5.95 | DRUG MATRIX | |||||
| Alpha-2B adrenergic receptor | GPCR | Ki | 7.62 | DRUG MATRIX | |||||
| D(3) dopamine receptor | GPCR | Ki | 6.72 | DRUG MATRIX | |||||
| Histamine H2 receptor | GPCR | Ki | 5.94 | DRUG MATRIX | |||||
| Muscarinic acetylcholine receptor M1 | GPCR | Ki | 8.48 | DRUG MATRIX | |||||
| Muscarinic acetylcholine receptor M2 | GPCR | Ki | 7.92 | DRUG MATRIX | |||||
| Muscarinic acetylcholine receptor M3 | GPCR | Ki | 8.38 | DRUG MATRIX | |||||
| Muscarinic acetylcholine receptor M4 | GPCR | Ki | 8.97 | DRUG MATRIX | |||||
| Muscarinic acetylcholine receptor M5 | GPCR | Ki | 8.48 | DRUG MATRIX | |||||
| Alpha-2C adrenergic receptor | GPCR | Ki | 6.45 | DRUG MATRIX | |||||
| Alpha-1D adrenergic receptor | GPCR | Ki | 7.49 | DRUG MATRIX | |||||
| Solute carrier family 22 member 1 | Transporter | IC50 | 4.45 | CHEMBL | |||||
| Sodium channel alpha subunits; brain (Types I, II, III) | Ion channel | IC50 | 5.16 | CHEMBL | |||||
| Major prion protein | Surface antigen | EC50 | 5.10 | CHEMBL | |||||
| Sodium-dependent serotonin transporter | Transporter | IC50 | 5.12 | CHEMBL | |||||
| Cholinesterase | Enzyme | Ki | 7.10 | WOMBAT-PK | |||||
| Alpha-1A adrenergic receptor | GPCR | WOMBAT-PK | |||||||
| 5-hydroxytryptamine receptor 2A | GPCR | Ki | 6.77 | WOMBAT-PK | |||||
| Aldehyde oxidase | Enzyme | IC50 | 6.29 | WOMBAT-PK | |||||
| Histamine H4 receptor | GPCR | Ki | 6.82 | WOMBAT-PK | |||||
| D(2) dopamine receptor | GPCR | Ki | 6.61 | WOMBAT-PK | |||||
| Cytochrome P450 2D6 | Enzyme | Ki | 5.42 | WOMBAT-PK | |||||
| FAD-linked sulfhydryl oxidase ALR | Enzyme | AC50 | 6.44 | CHEMBL | |||||
| Alpha-1B adrenergic receptor | GPCR | Ki | 7.68 | DRUG MATRIX | |||||
| Chloroquine resistance transporter | Unclassified | IC50 | 4.07 | CHEMBL | |||||
| Pleiotropic ABC efflux transporter of multiple drugs | Transporter | IC50 | 4.75 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | IC50 | 5.59 | CHEMBL | |||||
| Alpha-1A adrenergic receptor | GPCR | IC50 | 7.10 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019910 | VUID |
| N0000147995 | NUI |
| D00480 | KEGG_DRUG |
| 58-33-3 | SECONDARY_CAS_RN |
| 4017846 | VANDF |
| 4019910 | VANDF |
| C0699114 | UMLSCUI |
| CHEBI:8461 | CHEBI |
| CHEMBL643 | ChEMBL_ID |
| CHEMBL251904 | ChEMBL_ID |
| CHEMBL1200750 | ChEMBL_ID |
| D011398 | MESH_DESCRIPTOR_UI |
| DB01069 | DRUGBANK_ID |
| 4927 | PUBCHEM_CID |
| 7282 | IUPHAR_LIGAND_ID |
| 516 | INN_ID |
| FF28EJQ494 | UNII |
| 142445 | RXNORM |
| 2141 | MMSL |
| 5367 | MMSL |
| d00787 | MMSL |
| 001483 | NDDF |
| 004459 | NDDF |
| 14905007 | SNOMEDCT_US |
| 372871004 | SNOMEDCT_US |
| 8372007 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| PROMETHAZINE HYDROCHLORIDE AND CODEINE PHOSPHATE | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0121-0547 | SYRUP | 6.25 mg | ORAL | ANDA | 30 sections |
| Promethazine VC with Codeine Oral Solution | HUMAN PRESCRIPTION DRUG LABEL | 3 | 0121-0925 | SOLUTION | 6.25 mg | ORAL | ANDA | 29 sections |
| Promethazine VC | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0121-0926 | SOLUTION | 6.25 mg | ORAL | ANDA | 25 sections |
| Promethazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0121-0927 | SOLUTION | 6.25 mg | ORAL | ANDA | 25 sections |
| Promethazine with Codeine | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0121-0928 | SOLUTION | 6.25 mg | ORAL | ANDA | 29 sections |
| Promethazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0440-5195 | TABLET | 25 mg | ORAL | ANDA | 11 sections |
| Promethazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0440-8195 | TABLET | 25 mg | ORAL | ANDA | 12 sections |
| PHENULLDOZ | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-2985 | SUPPOSITORY | 12.50 mg | RECTAL | ANDA | 25 sections |
| PHENULLDOZ | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-2992 | SUPPOSITORY | 25 mg | RECTAL | ANDA | 25 sections |
| Promethazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-5307 | TABLET | 25 mg | ORAL | ANDA | 24 sections |
| Promethazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-5319 | TABLET | 50 mg | ORAL | ANDA | 24 sections |
| Promethazine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0615-1539 | TABLET | 12.50 mg | ORAL | ANDA | 18 sections |
| promethazine hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0615-7668 | TABLET | 25 mg | ORAL | ANDA | 24 sections |
| Promethazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0615-8154 | TABLET | 25 mg | ORAL | ANDA | 21 sections |
| Promethazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0641-0928 | INJECTION | 25 mg | INTRAMUSCULAR | ANDA | 25 sections |
| Promethazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0641-0929 | INJECTION | 50 mg | INTRAMUSCULAR | ANDA | 25 sections |
| Promethazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0641-0948 | INJECTION | 25 mg | INTRAMUSCULAR | ANDA | 25 sections |
| Promethazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0641-0949 | INJECTION | 50 mg | INTRAMUSCULAR | ANDA | 25 sections |
| Promethazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0641-0955 | INJECTION | 25 mg | INTRAMUSCULAR | ANDA | 25 sections |
| Promethazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0641-0956 | INJECTION | 50 mg | INTRAMUSCULAR | ANDA | 25 sections |
| Promethazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0641-1495 | INJECTION | 25 mg | INTRAMUSCULAR | ANDA | 25 sections |
| Promethazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0641-1496 | INJECTION | 50 mg | INTRAMUSCULAR | ANDA | 25 sections |
| PHENERGAN | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0641-6082 | INJECTION | 25 mg | INTRAMUSCULAR | ANDA | 25 sections |
| PHENERGAN | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0641-6083 | INJECTION | 50 mg | INTRAMUSCULAR | ANDA | 25 sections |
| PHENERGAN | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0641-6084 | INJECTION | 25 mg | INTRAMUSCULAR | ANDA | 26 sections |
| PHENERGAN | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0641-6085 | INJECTION | 50 mg | INTRAMUSCULAR | ANDA | 26 sections |
| Promethazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0641-6099 | INJECTION | 25 mg | INTRAMUSCULAR | ANDA | 26 sections |
| Promethazine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0641-6208 | INJECTION | 25 mg | INTRAMUSCULAR | ANDA | 25 sections |
| PROMETHEGAN | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0713-0132 | SUPPOSITORY | 50 mg | RECTAL | ANDA | 21 sections |
| PROMETHEGAN | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0713-0526 | SUPPOSITORY | 25 mg | RECTAL | ANDA | 21 sections |