orphenadrine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
opioid receptor antagonists/agonists, morphinan derivates 1999 83-98-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • disipal
  • orphenadrine
  • orphenadine
  • orphenadrin
  • orphenadrine citrate
  • orphenadrine hydrochloride
  • orphenadrine (chloride)
  • orphenadrine HCl
A muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm.
  • Molecular weight: 269.39
  • Formula: C18H23NO
  • CLOGP: 3.90
  • LIPINSKI: 0
  • HAC: 2
  • HDO: 0
  • TPSA: 12.47
  • ALOGS: -3.95
  • ROTB: 6
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.12 g O
0.12 g P
0.20 g O
0.20 g P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 10 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 8 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 21.21 µM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 90 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

DateAgencyCompanyOrphan
May 10, 1957 FDA

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
Pneumonia viral 468.60 26.48 112 5004 7810 63476096
Soft tissue disorder 354.09 26.48 80 5036 4342 63479564
Herpes zoster 282.86 26.48 136 4980 82326 63401580
Oral pain 228.87 26.48 86 5030 28308 63455598
Liver function test abnormal 200.68 26.48 91 5025 48090 63435816
Leukopenia 181.91 26.48 99 5017 77191 63406715
Fibromyalgia 178.23 26.48 99 5017 80321 63403585
Blood cholesterol increased 163.83 26.48 99 5017 93933 63389973
Peripheral swelling 149.40 26.48 142 4974 265800 63218106
Arthritis 140.11 26.48 97 5019 115824 63368082
Synovitis 99.39 26.48 97 5019 186821 63297085
Sternal fracture 93.45 26.48 24 5092 2230 63481676
Libido increased 89.75 26.48 21 5095 1324 63482582
Soft tissue injury 85.46 26.48 21 5095 1631 63482275
Hostility 82.85 26.48 21 5095 1851 63482055
Post-traumatic neck syndrome 80.71 26.48 21 5095 2053 63481853
Infection 78.00 26.48 94 5022 229079 63254827
Tenderness 73.40 26.48 36 5080 22542 63461364
Anaemia 68.42 26.48 100 5016 293330 63190576
Nightmare 60.58 26.48 30 5086 19164 63464742
Personality disorder 59.38 26.48 21 5095 5790 63478116
Therapeutic product effect incomplete 53.81 26.48 58 5058 124998 63358908
Joint swelling 52.22 26.48 94 5022 327572 63156334
Concussion 49.91 26.48 21 5095 9223 63474683
Middle insomnia 49.75 26.48 23 5093 12620 63471286
Muscle twitching 45.60 26.48 25 5091 19643 63464263
Soft tissue swelling 45.54 26.48 12 5104 1232 63482674
Oculogyric crisis 37.26 26.48 11 5105 1710 63482196
Rib fracture 34.68 26.48 22 5094 22575 63461331
Poor quality sleep 34.63 26.48 21 5095 19914 63463992
Body temperature increased 33.22 26.48 26 5090 37166 63446740
Irritability 27.97 26.48 22 5094 31672 63452234

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
Convulsive threshold lowered 32.90 31.85 6 594 532 34955799

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
Pneumonia viral 315.90 25.88 78 4342 9080 79730888
Soft tissue disorder 216.78 25.88 48 4372 3467 79736501
Herpes zoster 142.34 25.88 79 4341 93004 79646964
Fibromyalgia 127.68 25.88 65 4355 64275 79675693
Oral pain 126.05 25.88 52 4368 31746 79708222
Liver function test abnormal 101.99 25.88 56 4364 64419 79675549
Blood cholesterol increased 101.14 25.88 61 4359 83659 79656309
Sternal fracture 99.63 25.88 24 4396 2506 79737462
Leukopenia 94.27 25.88 66 4354 116447 79623521
Soft tissue injury 91.71 25.88 21 4399 1760 79738208
Arthritis 90.44 25.88 64 4356 114816 79625152
Libido increased 89.28 25.88 21 4399 1980 79737988
Post-traumatic neck syndrome 88.33 25.88 21 4399 2073 79737895
Hostility 86.28 25.88 21 4399 2289 79737679
Peripheral swelling 80.02 25.88 86 4334 269531 79470437
Tenderness 71.67 25.88 32 4388 23610 79716358
Synovitis 68.94 25.88 61 4359 150673 79589295
Personality disorder 65.94 25.88 21 4399 6125 79733843
Therapeutic product effect incomplete 62.14 25.88 56 4364 141589 79598379
Nightmare 59.73 25.88 29 4391 25832 79714136
Concussion 56.97 25.88 21 4399 9482 79730486
Middle insomnia 46.30 25.88 21 4399 16048 79723920
Infection 43.60 25.88 60 4360 241652 79498316
Soft tissue swelling 42.83 25.88 11 4409 1490 79738478
Sedation 40.97 25.88 29 4391 51866 79688102
Poor quality sleep 39.40 25.88 21 4399 22701 79717267
Rib fracture 37.97 25.88 22 4398 27925 79712043
Muscle twitching 37.70 25.88 21 4399 24743 79715225
Oculogyric crisis 35.47 25.88 11 4409 2941 79737027
Body temperature increased 35.47 25.88 25 4395 44395 79695573
Anxiety 35.12 25.88 55 4365 248457 79491511
Arthralgia 34.96 25.88 89 4331 571714 79168254
Joint swelling 34.21 25.88 59 4361 288587 79451381
Migraine 31.44 25.88 31 4389 87462 79652506
C-reactive protein abnormal 29.16 25.88 23 4397 48344 79691624
Feeling hot 28.91 25.88 25 4395 59709 79680259
Incorrect route of product administration 28.68 25.88 20 4400 34909 79705059
Irritability 27.94 25.88 21 4399 41123 79698845

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC M03BC01 MUSCULO-SKELETAL SYSTEM
MUSCLE RELAXANTS
MUSCLE RELAXANTS, CENTRALLY ACTING AGENTS
Ethers, chemically close to antihistamines
ATC M03BC51 MUSCULO-SKELETAL SYSTEM
MUSCLE RELAXANTS
MUSCLE RELAXANTS, CENTRALLY ACTING AGENTS
Ethers, chemically close to antihistamines
ATC N04AB02 NERVOUS SYSTEM
ANTI-PARKINSON DRUGS
ANTICHOLINERGIC AGENTS
Ethers chemically close to antihistamines
MeSH PA D018726 Anti-Dyskinesia Agents
MeSH PA D000978 Antiparkinson Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D018678 Cholinergic Agents
MeSH PA D018680 Cholinergic Antagonists
MeSH PA D065686 Cytochrome P-450 CYP2B6 Inhibitors
MeSH PA D065607 Cytochrome P-450 Enzyme Inhibitors
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D065606 Metabolic Side Effects of Drugs and Substances
MeSH PA D018727 Muscarinic Antagonists
MeSH PA D009125 Muscle Relaxants, Central
MeSH PA D009465 Neuromuscular Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D010276 Parasympatholytics
MeSH PA D018373 Peripheral Nervous System Agents
CHEBI has role CHEBI:37955 H1 receptor antagonists
CHEBI has role CHEBI:48407 antiparkinson agent
CHEBI has role CHEBI:48876 muscarinic antagonists
CHEBI has role CHEBI:50370 parasympatholytics
CHEBI has role CHEBI:51371 muscle relaxants
CHEBI has role CHEBI:60643 N-methyl-D-aspartate receptor antagonists
CHEBI has role CHEBI:66956 antidyskinetic agent
FDA PE N0000175730 Centrally-mediated Muscle Relaxation
FDA EPC N0000175737 Muscle Relaxant

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

DiseaseRelationSNOMED_IDDOID
Parkinsonism indication 32798002
Spasticity indication 221360009
Necrotizing enterocolitis in fetus OR newborn contraindication 2707005
Tachyarrhythmia contraindication 6285003
Alcoholism contraindication 7200002
Peptic ulcer contraindication 13200003 DOID:750
Glaucoma contraindication 23986001 DOID:1686
Hypertensive disorder contraindication 38341003 DOID:10763
Gastrointestinal ulcer contraindication 40845000
Conduction disorder of the heart contraindication 44808001
Achalasia of esophagus contraindication 45564002 DOID:9164
Vitamin K deficiency contraindication 52675005 DOID:11249
Nasal polyp contraindication 52756005
Acute nephropathy contraindication 58574008
Hepatic failure contraindication 59927004
Poisoning by acetaminophen contraindication 70273001
Agoraphobia contraindication 70691001 DOID:593
Factor II deficiency contraindication 73975000
Reye's syndrome contraindication 74351001 DOID:14525
Gastrointestinal hemorrhage contraindication 74474003
Thrombotic thrombocytopenic purpura contraindication 78129009 DOID:10772
Gout contraindication 90560007 DOID:13189
Kidney disease contraindication 90708001 DOID:557
Hemophilia contraindication 90935002
Myasthenia gravis contraindication 91637004 DOID:437
Obstruction of duodenum contraindication 95532008 DOID:3558
Anemia due to enzyme deficiency contraindication 111577008
von Willebrand disorder contraindication 128105004 DOID:12531
Seizure disorder contraindication 128613002
Obsessive-compulsive disorder contraindication 191736004 DOID:10933
Insomnia contraindication 193462001
Decompensated cardiac failure contraindication 195111005
Impaired renal function disorder contraindication 197663003
Disease of liver contraindication 235856003 DOID:409
Bladder outflow obstruction contraindication 236645006
Pyloric obstruction contraindication 244815007
Benign prostatic hyperplasia contraindication 266569009
Anemia contraindication 271737000 DOID:2355
Pregnancy, function contraindication 289908002
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Panic disorder contraindication 371631005 DOID:594
Breastfeeding (mother) contraindication 413712001
Chronic myocardial ischemia contraindication 413844008 DOID:3393
Myocardial ischemia contraindication 414795007 DOID:3393
Myocardial infarction in recovery phase contraindication 418044006
Acute erosive gastritis contraindication 444926003




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.52 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Sodium channel protein type 9 subunit alpha Ion channel BLOCKER IC50 4.76 WOMBAT-PK CHEMBL
Histamine H1 receptor GPCR ANTAGONIST Ki 7.96 WOMBAT-PK CHEMBL
Sodium channel protein type 10 subunit alpha Ion channel BLOCKER IC50 5.20 WOMBAT-PK CHEMBL
Sodium channel protein type 5 subunit alpha Ion channel BLOCKER IC50 4.89 WOMBAT-PK CHEMBL
Sodium channel protein type 1 subunit alpha Ion channel BLOCKER IC50 4.89 WOMBAT-PK CHEMBL
Sodium channel protein type 4 subunit alpha Ion channel BLOCKER Ki 5.66 WOMBAT-PK CHEMBL
5-hydroxytryptamine receptor 2B GPCR Ki 5.67 DRUG MATRIX
5-hydroxytryptamine receptor 2C GPCR Ki 6.55 DRUG MATRIX
5-hydroxytryptamine receptor 6 GPCR Ki 6.28 DRUG MATRIX
Alpha-2B adrenergic receptor GPCR Ki 6.06 DRUG MATRIX
Histamine H2 receptor GPCR Ki 5.17 DRUG MATRIX
Muscarinic acetylcholine receptor M2 GPCR Ki 6.87 DRUG MATRIX
Muscarinic acetylcholine receptor M3 GPCR Ki 7.43 DRUG MATRIX
Muscarinic acetylcholine receptor M4 GPCR Ki 7.77 DRUG MATRIX
Muscarinic acetylcholine receptor M5 GPCR Ki 7.70 DRUG MATRIX
Cytochrome P450 2D6 Enzyme IC50 6.40 DRUG MATRIX
Solute carrier family 22 member 1 Transporter IC50 4.90 CHEMBL
Muscarinic acetylcholine receptor M1 GPCR Ki 7.39 WOMBAT-PK
Glutamate [NMDA] receptor Ion channel Ki 5.22 CHEMBL
Alpha-2A adrenergic receptor GPCR Ki 6.09 DRUG MATRIX
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 5.17 WOMBAT-PK
Sodium-dependent serotonin transporter Transporter Ki 6.61 DRUG MATRIX
Sodium-dependent noradrenaline transporter Transporter INHIBITOR Ki 5.58 DRUG MATRIX
5-hydroxytryptamine receptor 2A GPCR Ki 6.90 DRUG MATRIX
Histamine H1 receptor GPCR IC50 6.79 CHEMBL

External reference:

IDSource
4019866 VUID
N0000147952 NUI
D00774 KEGG_DRUG
4682-36-4 SECONDARY_CAS_RN
341-69-5 SECONDARY_CAS_RN
4018819 VANDF
4018820 VANDF
4019866 VANDF
C0029309 UMLSCUI
CHEBI:7789 CHEBI
CHEMBL900 ChEMBL_ID
CHEMBL1201023 ChEMBL_ID
DB01173 DRUGBANK_ID
CHEMBL1200395 ChEMBL_ID
D009966 MESH_DESCRIPTOR_UI
4601 PUBCHEM_CID
7251 IUPHAR_LIGAND_ID
658 INN_ID
AL805O9OG9 UNII
155039 RXNORM
4456 MMSL
5206 MMSL
d00966 MMSL
001648 NDDF
001649 NDDF
001650 NDDF
35035001 SNOMEDCT_US
372714007 SNOMEDCT_US
387167001 SNOMEDCT_US
395813009 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Orphenadrine Citrate HUMAN PRESCRIPTION DRUG LABEL 1 0115-2011 TABLET, EXTENDED RELEASE 100 mg ORAL ANDA 10 sections
Orphenadrine Citrate HUMAN PRESCRIPTION DRUG LABEL 1 0185-0022 TABLET, EXTENDED RELEASE 100 mg ORAL ANDA 13 sections
Orphenadrine Citrate HUMAN PRESCRIPTION DRUG LABEL 1 0185-0022 TABLET, EXTENDED RELEASE 100 mg ORAL ANDA 13 sections
Orphenadrine Citrate HUMAN PRESCRIPTION DRUG LABEL 1 0591-3222 INJECTION 30 mg INTRAMUSCULAR ANDA 11 sections
Orphenadrine citrate HUMAN PRESCRIPTION DRUG LABEL 1 0641-6182 INJECTION 60 mg INTRAMUSCULAR ANDA 15 sections
Orphenadrine citrate HUMAN PRESCRIPTION DRUG LABEL 1 0641-6182 INJECTION 60 mg INTRAMUSCULAR ANDA 15 sections
Orphenadrine Citrate HUMAN PRESCRIPTION DRUG LABEL 1 10544-283 TABLET, EXTENDED RELEASE 100 mg ORAL ANDA 12 sections
ORPHENADRINE CITRATE HUMAN PRESCRIPTION DRUG LABEL 1 16590-177 TABLET, EXTENDED RELEASE 100 mg ORAL ANDA 9 sections
Orphenadrine Citrate HUMAN PRESCRIPTION DRUG LABEL 1 17478-538 INJECTION 30 mg INTRAMUSCULAR ANDA 15 sections
Orphenadrine Citrate HUMAN PRESCRIPTION DRUG LABEL 1 17478-538 INJECTION 30 mg INTRAMUSCULAR ANDA 15 sections
Orphenadrine Citrate HUMAN PRESCRIPTION DRUG LABEL 1 21695-099 TABLET, EXTENDED RELEASE 100 mg ORAL ANDA 16 sections
Orphenadrine Citrate, Aspirin and Caffeine HUMAN PRESCRIPTION DRUG LABEL 3 21695-726 TABLET, MULTILAYER 50 mg ORAL ANDA 12 sections
Orphenadrine Citrate HUMAN PRESCRIPTION DRUG LABEL 1 33261-088 TABLET, EXTENDED RELEASE 100 mg ORAL ANDA 16 sections
Orphenadrine Citrate HUMAN PRESCRIPTION DRUG LABEL 1 33358-274 TABLET, EXTENDED RELEASE 100 mg ORAL ANDA 12 sections
ORPHENADRINE CITRATE HUMAN PRESCRIPTION DRUG LABEL 1 42549-559 TABLET, EXTENDED RELEASE 100 mg ORAL ANDA 11 sections
ORPHENADRINE CITRATE HUMAN PRESCRIPTION DRUG LABEL 1 43063-407 TABLET, EXTENDED RELEASE 100 mg ORAL ANDA 14 sections
ORPHENADRINE CITRATE HUMAN PRESCRIPTION DRUG LABEL 1 43063-407 TABLET, EXTENDED RELEASE 100 mg ORAL ANDA 14 sections
ORPHENADRINE CITRATE HUMAN PRESCRIPTION DRUG LABEL 1 43063-407 TABLET, EXTENDED RELEASE 100 mg ORAL ANDA 14 sections
ORPHENADRINE CITRATE HUMAN PRESCRIPTION DRUG LABEL 1 43386-480 TABLET, EXTENDED RELEASE 100 mg ORAL ANDA 14 sections
Orphenadrine Citrate HUMAN PRESCRIPTION DRUG LABEL 1 45865-363 TABLET 100 mg ORAL ANDA 13 sections
Orphenadrine Citrate HUMAN PRESCRIPTION DRUG LABEL 1 49999-046 TABLET, EXTENDED RELEASE 100 mg ORAL ANDA 16 sections
Orphenadrine Citrate HUMAN PRESCRIPTION DRUG LABEL 1 49999-046 TABLET, EXTENDED RELEASE 100 mg ORAL ANDA 16 sections
Orphenadrine Citrate HUMAN PRESCRIPTION DRUG LABEL 1 50090-0169 TABLET, EXTENDED RELEASE 100 mg ORAL ANDA 14 sections
Orphenadrine Citrate HUMAN PRESCRIPTION DRUG LABEL 1 50090-0169 TABLET, EXTENDED RELEASE 100 mg ORAL ANDA 14 sections
Orphenadrine Citrate HUMAN PRESCRIPTION DRUG LABEL 1 50090-2438 INJECTION 30 mg INTRAMUSCULAR ANDA 14 sections
Orphenadrine Citrate HUMAN PRESCRIPTION DRUG LABEL 1 50090-3150 TABLET, EXTENDED RELEASE 100 mg ORAL ANDA 14 sections
Orphenadrine Citrate Aspirin Caffeine HUMAN PRESCRIPTION DRUG LABEL 3 50564-554 TABLET 25 mg ORAL ANDA 10 sections
Orphenadrine Citrate Aspirin Caffeine HUMAN PRESCRIPTION DRUG LABEL 3 50564-555 TABLET 50 mg ORAL ANDA 10 sections
Norgesic Forte HUMAN PRESCRIPTION DRUG LABEL 3 50991-999 TABLET, MULTILAYER 50 mg ORAL ANDA 12 sections
Norgesic Forte HUMAN PRESCRIPTION DRUG LABEL 3 50991-999 TABLET, MULTILAYER 50 mg ORAL ANDA 12 sections