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

Stem definition	Drug id	CAS RN
opioid receptor antagonists/agonists, morphinan derivates	1999	83-98-7

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
0.12	g	O
0.12	g	P
0.20	g	O
0.20	g	P

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	90 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
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
S (Water solubility)	10 mg/mL	Benet LZ, Broccatelli F, Oprea TI
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
May 10, 1957	FDA

FDA Adverse Event Reporting System (Female)

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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
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

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FDA Adverse Event Reporting System (Male)

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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
Convulsive threshold lowered	32.90	31.85	6	594	532	34955799

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FDA Adverse Event Reporting System (Geriatric)

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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
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

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
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
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

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

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Disease	Relation	SNOMED_ID	DOID
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

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.52	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Sodium channel protein type 9 subunit alpha	Ion channel	Q15858	SCN9A_HUMAN	BLOCKER	IC50	4.76	WOMBAT-PK	CHEMBL
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN	ANTAGONIST	Ki	7.96	WOMBAT-PK	CHEMBL
Sodium channel protein type 10 subunit alpha	Ion channel	Q9Y5Y9	SCNAA_HUMAN	BLOCKER	IC50	5.20	WOMBAT-PK	CHEMBL
Sodium channel protein type 5 subunit alpha	Ion channel	Q14524	SCN5A_HUMAN	BLOCKER	IC50	4.89	WOMBAT-PK	CHEMBL
Sodium channel protein type 1 subunit alpha	Ion channel	P35498	SCN1A_HUMAN	BLOCKER	IC50	4.89	WOMBAT-PK	CHEMBL
Sodium channel protein type 4 subunit alpha	Ion channel	P35499	SCN4A_HUMAN	BLOCKER	Ki	5.66	WOMBAT-PK	CHEMBL
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	5.67	DRUG MATRIX
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	6.55	DRUG MATRIX
5-hydroxytryptamine receptor 6	GPCR	P50406	5HT6R_HUMAN		Ki	6.28	DRUG MATRIX
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		Ki	6.06	DRUG MATRIX

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External reference:

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ID	Source
001648	NDDF
001649	NDDF
001650	NDDF
155039	RXNORM
341-69-5	SECONDARY_CAS_RN
35035001	SNOMEDCT_US
372714007	SNOMEDCT_US
387167001	SNOMEDCT_US
395813009	SNOMEDCT_US
4018819	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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	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

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