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

Stem definition	Drug id	CAS RN
monoamine oxydase (MAO)-inhibitors type B	2429	14611-51-9

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: selegiline (-)-deprenil (-)-deprenyl (-)-selegiline (r)-(-)-deprenyl (r)-selegiline anipryl l-deprenyl selegina selgene zelapar selegiline hydrochloride selegiline HCl	A selective, irreversible inhibitor of Type B monoamine oxidase that is used for the treatment of newly diagnosed patients with PARKINSON DISEASE, and for the treatment of depressive disorders. The compound without isomeric designation is Deprenyl. Molecular weight: 187.29 Formula: C13H17N CLOGP: 2.84 LIPINSKI: 0 HAC: 1 HDO: 0 TPSA: 3.24 ALOGS: -3.87 ROTB: 4 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

selegiline
(-)-deprenil
(-)-deprenyl
(-)-selegiline
(r)-(-)-deprenyl
(r)-selegiline
anipryl
l-deprenyl
selegina
selgene
zelapar
selegiline hydrochloride
selegiline HCl

A selective, irreversible inhibitor of Type B monoamine oxidase that is used for the treatment of newly diagnosed patients with PARKINSON DISEASE, and for the treatment of depressive disorders. The compound without isomeric designation is Deprenyl.

Molecular weight: 187.29
Formula: C13H17N
CLOGP: 2.84
LIPINSKI: 0
HAC: 1
HDO: 0
TPSA: 3.24
ALOGS: -3.87
ROTB: 4

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
5	mg	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0.10 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.89 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	4.40 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	1.90 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	20 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.13 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	1.30 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
June 5, 1989	FDA	SOMERSET

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
Application site rash	181.48	27.41	35	1661	2388	56287983
Application site erythema	170.27	27.41	37	1659	4563	56285808
Application site pruritus	99.12	27.41	23	1673	3796	56286575
Application site reaction	90.52	27.41	16	1680	670	56289701
Dyskinesia	80.67	27.41	31	1665	29077	56261294
Application site urticaria	75.97	27.41	12	1684	250	56290121
Hallucination	74.34	27.41	34	1662	49115	56241256
Hallucination, visual	68.37	27.41	24	1672	17444	56272927
Parkinsonism hyperpyrexia syndrome	67.96	27.41	10	1686	127	56290244
Application site irritation	59.45	27.41	13	1683	1639	56288732
Drug interaction	36.79	27.41	38	1658	209717	56080654
Application site pain	30.14	27.41	9	1687	3911	56286460
Impulse-control disorder	27.74	27.41	6	1690	717	56289654
Delusion	27.68	27.41	11	1685	11204	56279167

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
Hallucination	161.72	29.13	76	2341	46334	31648593
Dyskinesia	127.83	29.13	51	2366	20859	31674068
Hallucination, visual	87.77	29.13	36	2381	15758	31679169
Impulse-control disorder	86.69	29.13	20	2397	1256	31693671
Hypersexuality	84.59	29.13	20	2397	1398	31693529
Gambling disorder	77.09	29.13	19	2398	1583	31693344
Dopamine dysregulation syndrome	73.90	29.13	14	2403	332	31694595
Application site rash	68.14	29.13	15	2402	761	31694166
On and off phenomenon	67.14	29.13	18	2399	2092	31692835
Delusion	62.07	29.13	26	2391	11971	31682956
Application site erythema	44.18	29.13	13	2404	2116	31692811
Parkinsonism hyperpyrexia syndrome	41.67	29.13	7	2410	81	31694846
Binge eating	32.74	29.13	6	2411	118	31694809
Impulsive behaviour	31.94	29.13	10	2407	2003	31692924
Orthostatic hypotension	29.64	29.13	20	2397	24099	31670828

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
Hallucination	179.90	24.75	83	3354	76177	70848830
Application site rash	165.36	24.75	34	3403	1975	70923032
Dyskinesia	164.17	24.75	65	3372	41009	70883998
Hallucination, visual	151.58	24.75	56	3381	29281	70895726
Application site erythema	131.17	24.75	33	3404	4728	70920279
Parkinsonism hyperpyrexia syndrome	107.59	24.75	17	3420	214	70924793
Impulse-control disorder	101.35	24.75	22	3415	1657	70923350
Gambling disorder	87.38	24.75	20	3417	1918	70923089
Hypersexuality	86.10	24.75	19	3418	1544	70923463
Dopamine dysregulation syndrome	75.37	24.75	14	3423	476	70924531
Delusion	75.31	24.75	30	3407	19135	70905872
Application site pruritus	61.06	24.75	17	3420	3584	70921423
Application site urticaria	50.74	24.75	9	3428	235	70924772
Application site irritation	43.48	24.75	11	3426	1606	70923401
Parkinson's disease	42.34	24.75	11	3426	1784	70923223
On and off phenomenon	42.00	24.75	12	3425	2774	70922233
Muscle rigidity	36.80	24.75	18	3419	18632	70906375
Application site reaction	35.49	24.75	8	3429	715	70924292
Orthostatic hypotension	35.07	24.75	25	3412	51718	70873289
Drug interaction	31.80	24.75	62	3375	381379	70543628
Sudden onset of sleep	31.12	24.75	7	3430	620	70924387
Insomnia	30.98	24.75	45	3392	217761	70707246
Psychotic disorder	29.74	24.75	20	3417	37681	70887326
Sleep talking	27.59	24.75	7	3430	1034	70923973
Binge eating	27.26	24.75	6	3431	481	70924526
Tremor	26.38	24.75	35	3402	155589	70769418
Choking	25.86	24.75	12	3425	11048	70913959
Agitation	25.83	24.75	27	3410	93348	70831659
Marital problem	25.68	24.75	5	3432	219	70924788
Application site pain	24.91	24.75	9	3428	4393	70920614
Impulsive behaviour	24.89	24.75	8	3429	2746	70922261
Pneumonia aspiration	24.77	24.75	22	3415	62267	70862740

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	N04BD01	NERVOUS SYSTEM ANTI-PARKINSON DRUGS DOPAMINERGIC AGENTS Monoamine oxidase B inhibitors
FDA MoA	N0000000184	Monoamine Oxidase Inhibitors
MeSH PA	D018726	Anti-Dyskinesia Agents
MeSH PA	D000928	Antidepressive Agents
MeSH PA	D000978	Antiparkinson Agents
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D008996	Monoamine Oxidase Inhibitors
MeSH PA	D018696	Neuroprotective Agents
MeSH PA	D020011	Protective Agents
MeSH PA	D011619	Psychotropic Drugs
CHEBI has role	CHEBI:176497	geroprotectors
CHEBI has role	CHEBI:38623	monoamine oxidase inhibitors
CHEBI has role	CHEBI:48407	antiparkinson agent
CHEBI has role	CHEBI:48560	dopaminergic agents
FDA EPC	N0000175744	Monoamine Oxidase Inhibitor
FDA MoA	N0000175761	Monoamine Oxidase-B Inhibitors
FDA EPC	N0000175762	Monoamine Oxidase Type B Inhibitor

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

Disease	Relation	SNOMED_ID	DOID
Parkinson's disease	indication	49049000	DOID:14330
Major depressive disorder	indication	370143000
Suicidal thoughts	contraindication	6471006
Bipolar disorder	contraindication	13746004	DOID:3312
Orthostatic hypotension	contraindication	28651003
Conduction disorder of the heart	contraindication	44808001
Psychotic disorder	contraindication	69322001
Kidney disease	contraindication	90708001	DOID:557
Tardive dyskinesia	contraindication	102449007
Angina pectoris	contraindication	194828000
Mania	contraindication	231494001
Disease of liver	contraindication	235856003	DOID:409
Pheochromocytoma	contraindication	302835009
Malignant melanoma	contraindication	372244006

🐶 Veterinary Drug Use

Species	Use	Relation
Dogs	Cognitive dysfunction syndrome (CDS)	Indication
Dogs	Pituitary dependent hyperadrenocorticism (PDH)	Indication

🐶 Veterinary products

Product	Applicant	Ingredients
Anipryl	Zoetis Inc.	1

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	7.6	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])	Bioact source	MoA source
Amine oxidase [flavin-containing] B	Enzyme	P27338	AOFB_HUMAN	INHIBITOR	Ki	7.26	CHEMBL	CHEMBL
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		Ki	6.76	DRUG MATRIX
Amine oxidase [flavin-containing] A	Enzyme	P21397	AOFA_HUMAN		Ki	5.04	CHEMBL
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	6.17	DRUG MATRIX
Alpha-synuclein	Transporter	P37840	SYUA_HUMAN		IC50	6.57	CHEMBL
Amine oxidase [flavin-containing] B	Enzyme		AOFB_RAT		Ki	5.87	CHEMBL
Amine oxidase [flavin-containing] A	Enzyme		AOFA_RAT		Ki	4.98	CHEMBL
Amine oxidase [flavin-containing] A	Enzyme		AOFA_BOVIN		Ki	5.42	CHEMBL
Amine oxidase [flavin-containing] B	Enzyme		AOFB_BOVIN		Ki	6.01	CHEMBL
Monoamine oxidase	Enzyme		AOFB_RAT AOFA_RAT		IC50	7.89	CHEMBL

External reference:

ID	Source
4019929	VUID
N0000148014	NUI
D00785	KEGG_DRUG
14611-52-0	SECONDARY_CAS_RN
4019485	VANDF
4019929	VANDF
C0036579	UMLSCUI
CHEBI:50217	CHEBI
CHEMBL972	ChEMBL_ID
DB01037	DRUGBANK_ID
CHEMBL1200904	ChEMBL_ID
D012642	MESH_DESCRIPTOR_UI
26757	PUBCHEM_CID
4436	INN_ID
6639	IUPHAR_LIGAND_ID
2K1V7GP655	UNII
203137	RXNORM
1551	MMSL
21238	MMSL
53269	MMSL
5448	MMSL
63129	MMSL
d00976	MMSL
003465	NDDF
004599	NDDF
108466000	SNOMEDCT_US
108467009	SNOMEDCT_US
372497003	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
ZELAPAR	HUMAN PRESCRIPTION DRUG LABEL	1	0187-0453	TABLET, ORALLY DISINTEGRATING	1.25 mg	ORAL	NDA	25 sections
Selegiline Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	10135-737	CAPSULE	5 mg	ORAL	ANDA	20 sections
Selegiline Hydrochloride	Human Prescription Drug Label	1	16571-659	CAPSULE	5 mg	ORAL	ANDA	19 sections
EMSAM	HUMAN PRESCRIPTION DRUG LABEL	1	49502-900	PATCH	6 mg	TRANSDERMAL	NDA	31 sections
EMSAM	HUMAN PRESCRIPTION DRUG LABEL	1	49502-901	PATCH	9 mg	TRANSDERMAL	NDA	31 sections
EMSAM	HUMAN PRESCRIPTION DRUG LABEL	1	49502-902	PATCH	12 mg	TRANSDERMAL	NDA	31 sections
Selegiline Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	50090-2918	TABLET	5 mg	ORAL	ANDA	19 sections
Selegiline Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	60429-176	TABLET	5 mg	ORAL	ANDA	20 sections
SELEGILINE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	60505-0055	CAPSULE	5 mg	ORAL	ANDA	13 sections
Selegiline Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	60505-3438	TABLET	5 mg	ORAL	ANDA	20 sections
SELEGILINE HYDROCHLORIDE	HUMAN PRESCRIPTION DRUG LABEL	1	68151-2649	CAPSULE	5 mg	ORAL	ANDA	19 sections
Selegiline Hydrochloride	Human Prescription Drug Label	1	70954-504	CAPSULE	5 mg	ORAL	ANDA	20 sections
Selegiline Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	71205-888	CAPSULE	5 mg	ORAL	ANDA	19 sections
Selegiline Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	71205-888	CAPSULE	5 mg	ORAL	ANDA	19 sections
Selegiline Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	72319-006	TABLET	5 mg	ORAL	ANDA	15 sections