Scroll

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

Stem definition	Drug id	CAS RN
	228	58-00-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: apomorphine (-)-Apomorphine apomorphin L-Apomorphine apomorphine hydrochloride apomorphine hydrochloride hydrate apomorphine hydrochloride hemihydrate apomorphine HCl apomorphine chloride	A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use. Molecular weight: 267.33 Formula: C17H17NO2 CLOGP: 2.49 LIPINSKI: 0 HAC: 3 HDO: 2 TPSA: 43.70 ALOGS: -2.72 ROTB: 0 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

apomorphine
(-)-Apomorphine
apomorphin
L-Apomorphine
apomorphine hydrochloride
apomorphine hydrochloride hydrate
apomorphine hydrochloride hemihydrate
apomorphine HCl
apomorphine chloride

A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use.

Molecular weight: 267.33
Formula: C17H17NO2
CLOGP: 2.49
LIPINSKI: 0
HAC: 3
HDO: 2
TPSA: 43.70
ALOGS: -2.72
ROTB: 0

Status: OFP

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

Drug dosage:

Dose	Unit	Route
2	mg	SL
20	mg	P

ADMET properties:

Show entries

Search:

Property	Value	Reference
CL (Clearance)	40 mL/min/kg	Lombardo F, Berellini G, Obach RS
S (Water solubility)	20 mg/mL	Benet LZ, Broccatelli F, Oprea TI
BA (Bioavailability)	10 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	1.60 L/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)	0.68 hours	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.32 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
EoM (Fraction excreted unchanged in urine)	0.30 %	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.05 %	Lombardo F, Berellini G, Obach RS

Showing 1 to 9 of 9 entries

Previous1Next

Approvals:

Date	Agency	Company	Orphan
April 20, 2004	FDA	US WORLDMEDS

FDA Adverse Event Reporting System (Female)

Show entries

Search:

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
Somnolence	358.12	39.76	179	3241	178506	63307096
Nausea	329.98	39.76	306	3114	854165	62631437
Blood pressure decreased	260.51	39.76	106	3314	64916	63420686
Dizziness	197.30	39.76	171	3249	429754	63055848
Yawning	170.13	39.76	32	3388	1048	63484554
Orthostatic hypotension	95.38	39.76	44	3376	36116	63449486
Feeling abnormal	92.65	39.76	71	3349	148321	63337281
Dyskinesia	90.88	39.76	41	3379	31961	63453641
Product taste abnormal	89.21	39.76	21	3399	2046	63483556
Dysgeusia	81.81	39.76	43	3377	46667	63438935

Showing 1 to 10 of 26 entries

Previous1 2 3Next

FDA Adverse Event Reporting System (Male)

Show entries

Search:

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
Somnolence	433.83	35.47	244	4970	110872	34840845
Dizziness	398.72	35.47	297	4917	218224	34733493
Blood pressure decreased	372.95	35.47	172	5042	51343	34900374
Nausea	369.92	35.47	342	4872	339566	34612151
Yawning	310.66	35.47	56	5158	486	34951231
Orthostatic hypotension	191.56	35.47	88	5126	25831	34925886
Hyperhidrosis	150.37	35.47	109	5105	75583	34876134
Dyskinesia	119.81	35.47	61	5153	22352	34929365
Feeling abnormal	107.46	35.47	83	5131	63152	34888565
On and off phenomenon	106.53	35.47	31	5183	2466	34949251

Showing 1 to 10 of 30 entries

Previous1 2 3Next

FDA Adverse Event Reporting System (Geriatric)

Show entries

Search:

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
Somnolence	695.14	34.11	366	6936	238615	79498471
Nausea	585.89	34.11	562	6740	956634	78780452
Blood pressure decreased	577.86	34.11	246	7056	99220	79637866
Dizziness	498.95	34.11	398	6904	526043	79211043
Yawning	424.51	34.11	78	7224	1288	79735798
Orthostatic hypotension	260.88	34.11	119	7183	56045	79681041
Hyperhidrosis	187.07	34.11	135	7167	151357	79585729
On and off phenomenon	171.40	34.11	43	7259	3197	79733889
Feeling abnormal	148.31	34.11	120	7182	159079	79578007
Dyskinesia	147.44	34.11	75	7227	44698	79692388

Showing 1 to 10 of 36 entries

Previous1 2 3 4Next

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Show entries

Search:

Source	Code	Description
ATC	G04BE07	GENITO URINARY SYSTEM AND SEX HORMONES UROLOGICALS UROLOGICALS Drugs used in erectile dysfunction
ATC	N04BC07	NERVOUS SYSTEM ANTI-PARKINSON DRUGS DOPAMINERGIC AGENTS Dopamine agonists
CHEBI has role	CHEBI:48278	serotonergic drugs
CHEBI has role	CHEBI:48407	antiparkinson agent
CHEBI has role	CHEBI:48539	alpha-adrenergic drugs
CHEBI has role	CHEBI:51065	Dopamine receptor agonist
CHEBI has role	CHEBI:66956	antidyskinetic agent
CHEBI has role	CHEBI:149552	emetics
FDA EPC	N0000175580	Dopaminergic Agonist
FDA MoA	N0000000117	Dopamine Agonists

Showing 1 to 10 of 17 entries

Previous1 2Next

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

Show entries

Search:

Disease	Relation	SNOMED_ID	DOID
Parkinson's disease	indication	49049000	DOID:14330
Priapism	contraindication	6273006	DOID:9286
Alcoholism	contraindication	7200002
Dyskinesia	contraindication	9748009
Acute vomiting	contraindication	23971007
Alcohol intoxication	contraindication	25702006
Orthostatic hypotension	contraindication	28651003
Torsades de pointes	contraindication	31722008
Hypokalemia	contraindication	43339004
Acute nephropathy	contraindication	58574008

Showing 1 to 10 of 22 entries

Previous1 2 3Next

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.88	acidic
pKa2	12.98	acidic
pKa3	8.36	Basic

Orange Book patent data (new drug applications)

Show entries

Search:

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
10MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	10420763	June 11, 2030	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
10MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	9283219	June 11, 2030	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
10MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	9326981	June 11, 2030	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
10MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	9669019	June 11, 2030	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
10MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	9669021	June 11, 2030	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
10MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	11419769	Dec. 16, 2031	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
10MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	8414922	Dec. 16, 2031	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
10MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	8846074	Dec. 16, 2031	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
10MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	10449146	April 19, 2036	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE
10MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	10959943	April 19, 2036	TREATMENT OF OFF EPISODES IN PATIENTS WITH PARKINSONS DISEASE

Showing 1 to 10 of 50 entries

Previous1 2 3 4 5Next

Orange Book exclusivity data (new drug applications)

Show entries

Search:

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
10MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	May 21, 2023	NEW PRODUCT
15MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	May 21, 2023	NEW PRODUCT
20MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	May 21, 2023	NEW PRODUCT
25MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	May 21, 2023	NEW PRODUCT
30MG	KYNMOBI	SUMITOMO PHARMA AM	N210875	May 21, 2020	DISCN	FILM	SUBLINGUAL	May 21, 2023	NEW PRODUCT

Showing 1 to 5 of 5 entries

Previous1Next

Bioactivity Summary:

Show entries

Search:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN	AGONIST	Ki	9.21	CHEMBL	CHEMBL
D(4) dopamine receptor	GPCR	P21917	DRD4_HUMAN	AGONIST	Ki	8.05	CHEMBL
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	8.34	CHEMBL
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN	AGONIST	Ki	6.90	IUPHAR
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	6.53	CHEMBL
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN	ANTAGONIST	Ki	6.90	IUPHAR
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN	ANTAGONIST	Ki	6.90	IUPHAR
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN	ANTAGONIST	Ki	7	IUPHAR
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN		Ki	5.70	PDSP
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN	ANTAGONIST	Ki	7.20	IUPHAR

Showing 1 to 10 of 37 entries

Previous1 2 3 4Next

External reference:

Show entries

Search:

ID	Source
5RL	PDB_CHEM_ID
001665	NDDF
004677	NDDF
1043	RXNORM
17790	MMSL
33	IUPHAR_LIGAND_ID
387375001	SNOMEDCT_US
4017524	VANDF
4019618	VUID
4019618	VANDF

Showing 1 to 10 of 27 entries

Previous1 2 3Next

Pharmaceutical products:

Show entries

Search:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
APOKYN	HUMAN PRESCRIPTION DRUG LABEL	1	27505-004	INJECTION	30 mg	SUBCUTANEOUS	NDA	35 sections
APOKYN	HUMAN PRESCRIPTION DRUG LABEL	1	27505-004	INJECTION	30 mg	SUBCUTANEOUS	NDA	35 sections
APOKYN	HUMAN PRESCRIPTION DRUG LABEL	1	27505-004	INJECTION	30 mg	SUBCUTANEOUS	NDA	35 sections
APOKYN	HUMAN PRESCRIPTION DRUG LABEL	1	27505-004	INJECTION	30 mg	SUBCUTANEOUS	NDA	35 sections
apomorphine hydrocloride	HUMAN PRESCRIPTION DRUG LABEL	1	52817-720	INJECTION	30 mg	SUBCUTANEOUS	ANDA	33 sections
KYNMOBI	HUMAN PRESCRIPTION DRUG LABEL	1	63402-010	FILM, SOLUBLE	10 mg	SUBLINGUAL	NDA	34 sections
KYNMOBI	HUMAN PRESCRIPTION DRUG LABEL	1	63402-010	FILM, SOLUBLE	10 mg	SUBLINGUAL	NDA	34 sections
KYNMOBI	HUMAN PRESCRIPTION DRUG LABEL	1	63402-010	FILM, SOLUBLE	10 mg	SUBLINGUAL	NDA	34 sections
KYNMOBI	HUMAN PRESCRIPTION DRUG LABEL	1	63402-015	FILM, SOLUBLE	15 mg	SUBLINGUAL	NDA	34 sections
KYNMOBI	HUMAN PRESCRIPTION DRUG LABEL	1	63402-015	FILM, SOLUBLE	15 mg	SUBLINGUAL	NDA	34 sections

Showing 1 to 10 of 30 entries

Previous1 2 3Next