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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	182.44	27.57	35	1769	2463	63484755
Application site erythema	170.57	27.57	37	1767	4798	63482420
Application site pruritus	99.48	27.57	23	1781	3961	63483257
Parkinsonism hyperpyrexia syndrome	91.09	27.57	13	1791	140	63487078
Application site reaction	90.03	27.57	16	1788	734	63486484
Dyskinesia	79.56	27.57	31	1773	31971	63455247
Application site urticaria	76.62	27.57	12	1792	251	63486967
Hallucination	75.80	27.57	35	1769	54782	63432436
Hallucination, visual	67.40	27.57	24	1780	19274	63467944
Application site irritation	59.46	27.57	13	1791	1737	63485481
Drug interaction	41.29	27.57	41	1763	229090	63258128
Rapid eye movement sleep behaviour disorder	39.42	27.57	7	1797	319	63486899
Application site pain	30.09	27.57	9	1795	4173	63483045
Delusion	27.57	27.57	11	1793	12006	63475212

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	183.46	28.86	85	2519	51413	34902914
Dyskinesia	142.96	28.86	56	2548	22357	34931970
Hallucination, visual	91.11	28.86	38	2566	17753	34936574
Impulse-control disorder	86.77	28.86	20	2584	1281	34953046
Hypersexuality	84.03	28.86	20	2584	1473	34952854
Gambling disorder	81.92	28.86	20	2584	1640	34952687
On and off phenomenon	78.53	28.86	21	2583	2476	34951851
Dopamine dysregulation syndrome	70.37	28.86	14	2590	442	34953885
Application site rash	67.00	28.86	15	2589	842	34953485
Delusion	61.35	28.86	26	2578	12609	34941718
Application site erythema	43.28	28.86	13	2591	2323	34952004
Parkinsonism hyperpyrexia syndrome	41.75	28.86	7	2597	82	34954245
Binge eating	32.73	28.86	6	2598	121	34954206
Impulsive behaviour	31.47	28.86	10	2594	2152	34952175
Tremor	30.43	28.86	34	2570	82553	34871774

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	201.97	25.85	92	3609	85653	79655034
Dyskinesia	171.86	25.85	68	3633	44705	79695982
Application site rash	164.80	25.85	34	3667	2098	79738589
Hallucination, visual	155.21	25.85	58	3643	32671	79708016
Application site erythema	130.26	25.85	33	3668	5077	79735610
Parkinsonism hyperpyrexia syndrome	129.27	25.85	20	3681	228	79740459
Impulse-control disorder	101.08	25.85	22	3679	1752	79738935
Gambling disorder	92.74	25.85	21	3680	2005	79738682
Hypersexuality	85.55	25.85	19	3682	1661	79739026
Dopamine dysregulation syndrome	75.22	25.85	14	3687	503	79740184
Delusion	74.71	25.85	30	3671	20393	79720294
Application site pruritus	60.83	25.85	17	3684	3793	79736894
On and off phenomenon	54.22	25.85	15	3686	3225	79737462
Application site urticaria	50.98	25.85	9	3692	239	79740448
Application site irritation	43.13	25.85	11	3690	1733	79738954
Neuroleptic malignant syndrome	39.10	25.85	21	3680	27538	79713149
Muscle rigidity	36.44	25.85	18	3683	19864	79720823
Drug interaction	36.08	25.85	67	3634	415116	79325571
Application site reaction	35.27	25.85	8	3693	768	79739919
Orthostatic hypotension	34.20	25.85	25	3676	56139	79684548
Rapid eye movement sleep behaviour disorder	33.49	25.85	7	3694	459	79740228
Sudden onset of sleep	31.23	25.85	7	3694	637	79740050
Psychotic disorder	31.19	25.85	21	3680	41381	79699306
Insomnia	28.40	25.85	45	3656	245125	79495562
Tremor	28.17	25.85	37	3664	170046	79570641
Sleep talking	27.53	25.85	7	3694	1089	79739598
Binge eating	27.25	25.85	6	3695	503	79740184
Marital problem	25.89	25.85	5	3696	219	79740468

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	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	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
Selegiline Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	72319-006	TABLET	5 mg	ORAL	ANDA	15 sections