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

Stem definitionDrug idCAS RN
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 472.16 31.40 112 4753 7046 56280156
Soft tissue disorder 351.11 31.40 80 4785 4202 56283000
Herpes zoster 284.63 31.40 136 4729 75753 56211449
Oral pain 229.48 31.40 86 4779 26207 56260995
Fibromyalgia 202.68 31.40 100 4765 59503 56227699
Liver function test abnormal 199.28 31.40 91 4774 45580 56241622
Leukopenia 183.42 31.40 99 4766 70841 56216361
Blood cholesterol increased 181.30 31.40 99 4766 72480 56214722
Peripheral swelling 156.15 31.40 142 4723 234584 56052618
Arthritis 147.13 31.40 97 4768 99755 56187447
Synovitis 105.83 31.40 97 4768 161208 56125994
Libido increased 88.81 31.40 21 4844 1291 56285911
Soft tissue injury 84.68 31.40 21 4844 1578 56285624
Sternal fracture 83.88 31.40 22 4843 2068 56285134
Infection 83.00 31.40 94 4771 200112 56087090
Hostility 81.85 31.40 21 4844 1810 56285392
Post-traumatic neck syndrome 80.25 31.40 21 4844 1957 56285245
Tenderness 74.89 31.40 36 4829 20119 56267083
Anaemia 70.18 31.40 100 4765 267411 56019791
Nightmare 62.34 31.40 30 4835 16796 56270406
Personality disorder 60.33 31.40 21 4844 5152 56282050
Therapeutic product effect incomplete 58.43 31.40 58 4807 105973 56181229
Joint swelling 55.86 31.40 94 4771 289706 55997496
Concussion 50.80 31.40 21 4844 8225 56278977
Muscle twitching 48.46 31.40 25 4840 16217 56270985
Soft tissue swelling 46.55 31.40 12 4853 1053 56286149
Middle insomnia 45.08 31.40 21 4844 10929 56276273
Oculogyric crisis 37.82 31.40 11 4854 1513 56285689
Poor quality sleep 35.52 31.40 21 4844 17734 56269468
Rib fracture 35.42 31.40 22 4843 20287 56266915
Body temperature increased 33.52 31.40 26 4839 34216 56252986

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 32.85 32.30 6 567 509 31696262

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 318.33 28.69 78 4132 8214 70916020
Soft tissue disorder 215.48 28.69 48 4162 3326 70920908
Herpes zoster 143.82 28.69 79 4131 85156 70839078
Fibromyalgia 141.76 28.69 65 4145 47809 70876425
Oral pain 127.13 28.69 52 4158 29014 70895220
Blood cholesterol increased 112 28.69 61 4149 64543 70859691
Liver function test abnormal 101.19 28.69 56 4154 61090 70863144
Arthritis 100.57 28.69 66 4144 97914 70826320
Leukopenia 95.53 28.69 66 4144 106494 70817740
Soft tissue injury 90.98 28.69 21 4189 1701 70922533
Sternal fracture 89.53 28.69 22 4188 2329 70921905
Libido increased 89.27 28.69 21 4189 1848 70922386
Post-traumatic neck syndrome 88.14 28.69 21 4189 1952 70922282
Hostility 85.35 28.69 21 4189 2234 70922000
Peripheral swelling 84.52 28.69 86 4124 236477 70687757
Synovitis 73.49 28.69 61 4149 129167 70795067
Tenderness 72.91 28.69 32 4178 21178 70903056
Therapeutic product effect incomplete 66.93 28.69 56 4154 119826 70804408
Personality disorder 66.64 28.69 21 4189 5527 70918707
Nightmare 62.12 28.69 29 4181 22127 70902107
Concussion 57.84 28.69 21 4189 8488 70915746
Middle insomnia 47.63 28.69 21 4189 14032 70910202
Infection 46.84 28.69 60 4150 210725 70713509
Soft tissue swelling 44.49 28.69 11 4199 1193 70923041
Sedation 41.92 28.69 29 4181 46702 70877532
Muscle twitching 40.74 28.69 21 4189 19806 70904428
Poor quality sleep 40.22 28.69 21 4189 20328 70903906
Rib fracture 38.56 28.69 22 4188 25334 70898900
Joint swelling 36.95 28.69 59 4151 253152 70671082
Body temperature increased 36.38 28.69 25 4185 39809 70884425
Anxiety 35.85 28.69 54 4156 220276 70703958
Oculogyric crisis 35.70 28.69 11 4199 2687 70921547
Arthralgia 33.06 28.69 84 4126 503306 70420928
C-reactive protein abnormal 32.40 28.69 23 4187 38556 70885678
Incorrect route of product administration 29.95 28.69 19 4191 26473 70897761

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 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
Sodium channel protein type 5 subunit alpha Ion channel BLOCKER IC50 4.89 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 M1 GPCR Ki 7.39 WOMBAT-PK
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
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
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
341-69-5 SECONDARY_CAS_RN
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 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
Orphenadrine Citrate HUMAN PRESCRIPTION DRUG LABEL 1 52959-527 TABLET, EXTENDED RELEASE 100 mg ORAL ANDA 13 sections