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

Stem definition	Drug id	CAS RN
prednisone and prednisolone derivatives	294	5534-09-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: rhinocort beclometasone dipropionate beclomethasone dipropionate beclomethasone dipropionate monohydrate	An anti-inflammatory, synthetic glucocorticoid. It is used topically as an anti-inflammatory agent and in aerosol form for the treatment of ASTHMA. Molecular weight: 521.05 Formula: C28H37ClO7 CLOGP: 4.26 LIPINSKI: 1 HAC: 7 HDO: 1 TPSA: 106.97 ALOGS: -5.40 ROTB: 8 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

rhinocort
beclometasone dipropionate
beclomethasone dipropionate
beclomethasone dipropionate monohydrate

An anti-inflammatory, synthetic glucocorticoid. It is used topically as an anti-inflammatory agent and in aerosol form for the treatment of ASTHMA.

Molecular weight: 521.05
Formula: C28H37ClO7
CLOGP: 4.26
LIPINSKI: 1
HAC: 7
HDO: 1
TPSA: 106.97
ALOGS: -5.40
ROTB: 8

Status: OFP

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

Drug dosage:

Dose	Unit	Route
0.40	mg	N
0.80	mg	Inhal.aerosol
0.80	mg	Inhal.powder
1.50	mg	Inhal.solution

ADMET properties:

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Property	Value	Reference
CL (Clearance)	36 mL/min/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ
t_half (Half-life)	0.50 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.29 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.13 %	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.05 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
S (Water solubility)	0.00 mg/mL	Bocci G, Oprea TI, Benet LZ

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Approvals:

Date	Agency	Company	Orphan
May 12, 1976	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
Asthma	433.20	12.69	382	25553	127179	63335908
Wheezing	208.75	12.69	225	25710	95370	63367717
Bacterial disease carrier	141.15	12.69	42	25893	1289	63461798
Bronchial secretion retention	129.27	12.69	47	25888	2726	63460361
Bronchospasm	128.73	12.69	83	25852	17197	63445890
Superinfection	113.44	12.69	42	25893	2565	63460522
Aggression	112.28	12.69	86	25849	23412	63439675
Dyspnoea	109.12	12.69	545	25390	660768	62802319
Nightmare	104.56	12.69	76	25859	19118	63443969
Drug ineffective	99.74	12.69	172	25763	1044593	62418494

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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
Asthma	326.57	13.44	209	14249	42447	34900026
Wheezing	143.01	13.44	126	14332	41276	34901197
Dyspnoea	85.47	13.44	344	14114	376438	34566035
Nightmare	71.12	13.44	54	14404	14337	34928136
Anger	70.97	13.44	50	14408	11834	34930639
Lip swelling	63.73	13.44	53	14405	16027	34926446
Ballismus	54.95	13.44	12	14446	98	34942375
Sleep terror	51.06	13.44	23	14435	2295	34940178
Lower respiratory tract infection	49.19	13.44	63	14395	31574	34910899
Abnormal behaviour	49.07	13.44	56	14402	24913	34917560

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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
Asthma	601.05	11.72	486	34292	134609	79575001
Wheezing	303.87	11.72	311	34467	116353	79593257
Nightmare	189.56	11.72	126	34652	25735	79683875
Dyspnoea	166.27	11.72	775	34003	856250	78853360
Bacterial disease carrier	136.38	11.72	43	34735	1503	79708107
Lip swelling	130.54	11.72	122	34656	40789	79668821
Depressed mood	122	11.72	127	34651	48353	79661257
Bronchospasm	111.41	11.72	90	34688	24769	79684841
Bronchial secretion retention	108.42	11.72	47	34731	4057	79705553
Swollen tongue	104.40	11.72	110	34668	42460	79667150

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	A07EA07	ALIMENTARY TRACT AND METABOLISM ANTIDIARRHEALS, INTESTINAL ANTIINFLAMMATORY/ANTIINFECTIVE AGENTS INTESTINAL ANTIINFLAMMATORY AGENTS Corticosteroids acting locally
ATC	D07AC15	DERMATOLOGICALS CORTICOSTEROIDS, DERMATOLOGICAL PREPARATIONS CORTICOSTEROIDS, PLAIN Corticosteroids, potent (group III)
ATC	D07CC04	DERMATOLOGICALS CORTICOSTEROIDS, DERMATOLOGICAL PREPARATIONS CORTICOSTEROIDS, COMBINATIONS WITH ANTIBIOTICS Corticosteroids, potent, combinations with antibiotics
ATC	R01AD01	RESPIRATORY SYSTEM NASAL PREPARATIONS DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE Corticosteroids
ATC	R03AK08	RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES ADRENERGICS, INHALANTS Adrenergics in combination with corticosteroids or other drugs, excl. anticholinergics
ATC	R03AK13	RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES ADRENERGICS, INHALANTS Adrenergics in combination with corticosteroids or other drugs, excl. anticholinergics
ATC	R03AL09	RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES ADRENERGICS, INHALANTS Adrenergics in combination with anticholinergics incl. triple combinations with corticosteroids
ATC	R03BA01	RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES OTHER DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES, INHALANTS Glucocorticoids
CHEBI has role	CHEBI:35472	anti-inflammatory drugs
CHEBI has role	CHEBI:49167	anti-asthmatic drugs

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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
Vasomotor rhinitis	indication	8229003	DOID:4730
Nasal polyp	indication	52756005
Allergic rhinitis	indication	61582004
Rhinitis	indication	70076002	DOID:4483
Asthma	indication	195967001	DOID:2841
Asthma management	indication	406162001
Severe chronic obstructive pulmonary disease	off-label use	313299006
Mycosis	contraindication	3218000	DOID:1564
Ocular hypertension	contraindication	4210003	DOID:9282
Inactive tuberculosis	contraindication	11999007

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

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Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	12.01	acidic

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
Glucocorticoid receptor	Nuclear hormone receptor	P04150	GCR_HUMAN	AGONIST	Ki	8.43	DRUG MATRIX	CHEMBL
Interleukin-5	Cytokine	P05113	IL5_HUMAN		IC50	4.57	CHEMBL
Mineralocorticoid receptor	Nuclear hormone receptor	P08235	MCR_HUMAN		EC50	8.32	CHEMBL
Matrix metalloproteinase-9	Enzyme	P14780	MMP9_HUMAN		IC50	5.70	CHEMBL
Probable G-protein coupled receptor 97	GPCR	Q86Y34	AGRG3_HUMAN	AGONIST	EC50	8.50	IUPHAR
Progesterone receptor	Nuclear hormone receptor	P06401	PRGR_HUMAN		IC50	7.55	CHEMBL
Androgen receptor	Transcription factor		ANDR_RAT		Ki	5.96	CHEMBL
Progesterone receptor	Transcription factor		Q690N0_BOVIN		Ki	7.57	CHEMBL
Glucocorticoid receptor	Transcription factor		GCR_RAT		IC50	8.54	CHEMBL
Interleukin-5	Unclassified		IL5_MOUSE		IC50	4.58	CHEMBL

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External reference:

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ID	Source
002179	NDDF
004947	NDDF
116574000	SNOMEDCT_US
116575004	SNOMEDCT_US
1167	MMSL
1347	RXNORM
1389007	SNOMEDCT_US
20469	PUBCHEM_CID
21700	PUBCHEM_CID
2307	INN_ID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
BECONASE AQ	HUMAN PRESCRIPTION DRUG LABEL	1	16590-030	SPRAY, SUSPENSION	42 ug	NASAL	NDA	13 sections
BECONASEAQ	HUMAN PRESCRIPTION DRUG LABEL	1	0173-0388	SPRAY, SUSPENSION	42 ug	NASAL	NDA	20 sections
BECONASEAQ	HUMAN PRESCRIPTION DRUG LABEL	1	0173-0388	SPRAY, SUSPENSION	42 ug	NASAL	NDA	20 sections
BECONASEAQ	HUMAN PRESCRIPTION DRUG LABEL	1	0173-0388	SPRAY, SUSPENSION	42 ug	NASAL	NDA	20 sections
QNASL	HUMAN PRESCRIPTION DRUG LABEL	1	59310-406	AEROSOL, METERED	40 ug	NASAL	NDA	27 sections
QNASL	HUMAN PRESCRIPTION DRUG LABEL	1	59310-406	AEROSOL, METERED	40 ug	NASAL	NDA	27 sections
QNASL	HUMAN PRESCRIPTION DRUG LABEL	1	59310-406	AEROSOL, METERED	40 ug	NASAL	NDA	27 sections
QNASL	HUMAN PRESCRIPTION DRUG LABEL	1	59310-410	AEROSOL, METERED	80 ug	NASAL	NDA	27 sections
QNASL	HUMAN PRESCRIPTION DRUG LABEL	1	59310-410	AEROSOL, METERED	80 ug	NASAL	NDA	27 sections
QNASL	HUMAN PRESCRIPTION DRUG LABEL	1	59310-410	AEROSOL, METERED	80 ug	NASAL	NDA	27 sections

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