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

Stem definition	Drug id	CAS RN
opioid receptor antagonists/agonists related to normorphine	1878	465-65-6

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: naloxone hydrochloride dihydrate naloxone hydrochloride hydrate naloxone hydrobromide evzio naloxone l-naloxone (-)-Naloxone naloxone hydrochloride naloxone HCl	A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors. Molecular weight: 327.38 Formula: C19H21NO4 CLOGP: 0.16 LIPINSKI: 0 HAC: 5 HDO: 2 TPSA: 70 ALOGS: -1.76 ROTB: 2 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

naloxone hydrochloride dihydrate
naloxone hydrochloride hydrate
naloxone hydrobromide
evzio
naloxone
l-naloxone
(-)-Naloxone
naloxone hydrochloride
naloxone HCl

A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.

Molecular weight: 327.38
Formula: C19H21NO4
CLOGP: 0.16
LIPINSKI: 0
HAC: 5
HDO: 2
TPSA: 70
ALOGS: -1.76
ROTB: 2

Status: OFP

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

Drug dosage:

Dose	Unit	Route
75	mg	O

ADMET properties:

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Property	Value	Reference
CL (Clearance)	23 mL/min/kg	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	2 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	1.70 L/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	1.10 hours	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.54 %	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.31 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
EoM (Fraction excreted unchanged in urine)	0 %	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
April 13, 1971	FDA	ADAPT
Nov. 9, 2017	EMA	Mundipharma Corporation (Ireland) Limited

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
Exposure during pregnancy	225.06	15.25	188	9567	155359	63323908
Abortion spontaneous	136.75	15.25	87	9668	47108	63432159
Toxicity to various agents	134.36	15.25	177	9578	247073	63232194
Respiratory depression	133.23	15.25	57	9698	13658	63465609
Drug withdrawal syndrome neonatal	106.61	15.25	30	9725	2051	63477216
Overdose	105.54	15.25	108	9647	114970	63364297
Drug withdrawal syndrome	98.90	15.25	58	9697	27136	63452131
Selective abortion	74.10	15.25	14	9741	155	63479112
Premature delivery	71.12	15.25	49	9706	30232	63449035
Coma	63.69	15.25	63	9692	64301	63414966

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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
Drug withdrawal syndrome	160.19	16.41	81	7627	19753	34929470
Drug withdrawal syndrome neonatal	153.71	16.41	49	7659	3570	34945653
Overdose	133.69	16.41	130	7578	90929	34858294
Unresponsive to stimuli	100.11	16.41	67	7641	27502	34921721
Respiratory depression	90.85	16.41	52	7656	16193	34933030
Miosis	74.18	16.41	38	7670	9497	34939726
Toxicity to various agents	69.78	16.41	143	7565	200219	34749004
Non-cardiogenic pulmonary oedema	64.07	16.41	17	7691	644	34948579
Drug dependence	52.13	16.41	43	7665	24174	34925049
Foetal exposure during pregnancy	42.42	16.41	47	7661	38054	34911169

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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
Respiratory depression	217.66	14.58	103	13792	27527	79702966
Overdose	199.03	14.58	200	13695	184006	79546487
Drug withdrawal syndrome	184.08	14.58	99	13796	34619	79695874
Toxicity to various agents	183.40	14.58	290	13605	421250	79309243
Unresponsive to stimuli	140.77	14.58	99	13796	55689	79674804
Miosis	134.02	14.58	62	13833	15727	79714766
Coma	91.87	14.58	100	13795	100549	79629944
Bradypnoea	88.68	14.58	35	13860	6017	79724476
Depressed level of consciousness	84.69	14.58	94	13801	96558	79633935
Cardiac arrest	73.92	14.58	118	13777	171978	79558515

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	A06AH04	ALIMENTARY TRACT AND METABOLISM DRUGS FOR CONSTIPATION DRUGS FOR CONSTIPATION Peripheral opioid receptor antagonists
ATC	N02AA53	NERVOUS SYSTEM ANALGESICS OPIOIDS Natural opium alkaloids
ATC	N02AA55	NERVOUS SYSTEM ANALGESICS OPIOIDS Natural opium alkaloids
ATC	N02AX51	NERVOUS SYSTEM ANALGESICS OPIOIDS Other opioids
ATC	V03AB15	VARIOUS ALL OTHER THERAPEUTIC PRODUCTS ALL OTHER THERAPEUTIC PRODUCTS Antidotes
CHEBI has role	CHEBI:35488	central nervous system depressants
CHEBI has role	CHEBI:50137	mu-opioid receptor antagonists
CHEBI has role	CHEBI:90755	antidote to opioid overdose
FDA EPC	N0000175691	Opioid Antagonist
FDA MoA	N0000000154	Opioid Antagonists

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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
Pain	indication	22253000
Opioid dependence	indication	75544000	DOID:2559
Poisoning by opiate analgesic drug	indication	241749009
Overdose of opiate	indication	242253008
Prevention of opioid abuse	indication	426928008
Opiate-Induced Respiratory Depression	indication
Suicidal thoughts	contraindication	6471006
Dependent drug abuse	contraindication	6525002
Alcohol withdrawal delirium	contraindication	8635005
Chronic obstructive lung disease	contraindication	13645005	DOID:3083

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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	9.31	acidic
pKa2	7.47	Basic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
0.4MG/0.4ML (0.4MG/0.4ML)	EVZIO	KALEO INC	N205787	April 3, 2014	DISCN	SOLUTION	INTRAMUSCULAR, SUBCUTANEOUS	9724471	May 23, 2027	METHOD FOR CONFIRMING DOSE DELIVERY
0.4MG/0.4ML (0.4MG/0.4ML)	EVZIO	KALEO INC	N205787	April 3, 2014	DISCN	SOLUTION	INTRAMUSCULAR, SUBCUTANEOUS	10322239	Feb. 28, 2031	USE OF A DELIVERY DEVICE TO ADMINISTER A DOSE OF NALOXONE
0.4MG/0.4ML (0.4MG/0.4ML)	EVZIO	KALEO INC	N205787	April 3, 2014	DISCN	SOLUTION	INTRAMUSCULAR, SUBCUTANEOUS	9474869	Feb. 28, 2031	USE OF A DELIVERY DEVICE TO ADMINISTER A DOSE OF NALOXONE
0.4MG/0.4ML (0.4MG/0.4ML)	EVZIO	KALEO INC	N205787	April 3, 2014	DISCN	SOLUTION	INTRAMUSCULAR, SUBCUTANEOUS	10143972	May 24, 2031	USE OF A DELIVERY DEVICE TO DELIVER A DOSE OF NALOXONE
0.4MG/0.4ML (0.4MG/0.4ML)	EVZIO	KALEO INC	N205787	April 3, 2014	DISCN	SOLUTION	INTRAMUSCULAR, SUBCUTANEOUS	9517307	July 18, 2034	USE OF AN AUTO INJECTOR TO ADMINISTER NALOXONE HCL
0.4MG/0.4ML (0.4MG/0.4ML)	EVZIO	KALEO INC	N205787	April 3, 2014	DISCN	SOLUTION	INTRAMUSCULAR, SUBCUTANEOUS	10220158	March 20, 2035	USE OF A DELIVERY DEVICE TO DELIVER A BIOEQUIVALENT DOSE OF A NALOXONE COMPOSITION VIA A NEEDLE
10MG/0.4ML (10MG/0.4ML)	NALOXONE HYDROCHLORIDE (AUTOINJECTOR)	KALEO INC	N215457	Feb. 28, 2022	DISCN	SOLUTION	INTRAMUSCULAR, SUBCUTANEOUS	10322239	Feb. 28, 2031	USE OF A DELIVERY DEVICE TO ADMINISTER A DOSE OF NALOXONE
10MG/0.4ML (10MG/0.4ML)	NALOXONE HYDROCHLORIDE (AUTOINJECTOR)	KALEO INC	N215457	Feb. 28, 2022	DISCN	SOLUTION	INTRAMUSCULAR, SUBCUTANEOUS	9474869	Feb. 28, 2031	USE OF A DELIVERY DEVICE TO ADMINISTER A DOSE OF NALOXONE
10MG/0.4ML (10MG/0.4ML)	NALOXONE HYDROCHLORIDE (AUTOINJECTOR)	KALEO INC	N215457	Feb. 28, 2022	DISCN	SOLUTION	INTRAMUSCULAR, SUBCUTANEOUS	10143792	May 24, 2031	USE OF A DELIVERY DEVICE TO DELIVER A DOSE OF NALOXONE
10MG;20MG	TARGINIQ	PURDUE PHARMA LP	N205777	July 23, 2014	DISCN	TABLET, EXTENDED RELEASE	ORAL	9555000	April 4, 2023	MANAGEMENT OF PAIN SEVERE ENOUGH TO REQUIRE DAILY, AROUND-THE-CLOCK, LONG-TERM OPIOID TREATMENT AND FOR WHICH ALTERNATIVE TREATMENT OPTIONS ARE INADEQUATE

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
4MG/SPRAY	REXTOVY	AMPHASTAR PHARMS INC	N208969	March 7, 2023	RX	SPRAY, METERED	NASAL	March 7, 2026	NEW PRODUCT

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Mu-type opioid receptor	GPCR	P35372	OPRM_HUMAN	ANTAGONIST	Ki	8.81	WOMBAT-PK	CHEMBL
Cytochrome P450 2D6	Enzyme	P10635	CP2D6_HUMAN		IC50	5.70	DRUG MATRIX
Adenosine receptor A3	GPCR	P0DMS8	AA3R_HUMAN		IC50	8.80	CHEMBL
Kappa-type opioid receptor	GPCR	P41145	OPRK_HUMAN	ANTAGONIST	Ki	8.50	WOMBAT-PK
Delta-type opioid receptor	GPCR	P41143	OPRD_HUMAN	ANTAGONIST	Ki	7.27	WOMBAT-PK
Mu-type opioid receptor	GPCR		OPRM_RAT		Kd	9.40	CHEMBL
Mu-type opioid receptor	GPCR		OPRM_MOUSE	ANTAGONIST	Ki	9	IUPHAR
Mu-type opioid receptor	GPCR		OPRM_CAVPO		Ki	9.17	CHEMBL
Delta-type opioid receptor	GPCR		OPRD_MOUSE		Kd	7.30	CHEMBL
Delta-type opioid receptor	GPCR		OPRD_RAT		Kd	7.74	CHEMBL

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External reference:

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ID	Source
001614	NDDF
004661	NDDF
1010598	RXNORM
1526	INN_ID
1638	IUPHAR_LIGAND_ID
2074	MMSL
21518006	SNOMEDCT_US
221948	MMSL
27364	MMSL
357-08-4	SECONDARY_CAS_RN

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Buprenorphine and Naloxone	HUMAN PRESCRIPTION DRUG LABEL	2	0121-1018	TABLET	0.50 mg	SUBLINGUAL	ANDA	31 sections
Buprenorphine and Naloxone	HUMAN PRESCRIPTION DRUG LABEL	2	0121-2036	TABLET	2 mg	SUBLINGUAL	ANDA	31 sections
Buprenorphine and Naloxone	HUMAN PRESCRIPTION DRUG LABEL	2	0228-3154	TABLET	0.50 mg	SUBLINGUAL	ANDA	33 sections
Buprenorphine and Naloxone	HUMAN PRESCRIPTION DRUG LABEL	2	0228-3154	TABLET	0.50 mg	SUBLINGUAL	ANDA	33 sections
Buprenorphine and Naloxone	HUMAN PRESCRIPTION DRUG LABEL	2	0228-3154	TABLET	0.50 mg	SUBLINGUAL	ANDA	33 sections
Buprenorphine and Naloxone	HUMAN PRESCRIPTION DRUG LABEL	2	0228-3154	TABLET	0.50 mg	SUBLINGUAL	ANDA	33 sections
Buprenorphine and Naloxone	HUMAN PRESCRIPTION DRUG LABEL	2	0228-3155	TABLET	2 mg	SUBLINGUAL	ANDA	33 sections
Buprenorphine and Naloxone	HUMAN PRESCRIPTION DRUG LABEL	2	0228-3155	TABLET	2 mg	SUBLINGUAL	ANDA	33 sections
Buprenorphine and Naloxone	HUMAN PRESCRIPTION DRUG LABEL	2	0228-3155	TABLET	2 mg	SUBLINGUAL	ANDA	33 sections
Buprenorphine and Naloxone	HUMAN PRESCRIPTION DRUG LABEL	2	0228-3155	TABLET	2 mg	SUBLINGUAL	ANDA	33 sections

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