Fenspiride

Fenspiride
Clinical data
Trade names	Eurespal, Pneumorel
AHFS/Drugs.com	International Drug Names
Routes of; administration	Oral
ATC code	R03BX01 (WHO) R03DX03 (WHO);
Legal status
Legal status	In general: ℞ (Prescription only);
Pharmacokinetic data
Bioavailability	90%
Elimination half-life	14–16 hours
Excretion	Urine (90%), feces (~10%)
Identifiers
	IUPAC name 8-(2-phenylethyl)-1-oxa-3,8-diazaspiro[4.5]decan-2-one;
CAS Number	5053-06-5 ;
PubChem CID	68626;
DrugBank	DB08979 ;
ChemSpider	3227 ;
UNII	S983QC7HKM;
KEGG	D07949 ;
ChEMBL	ChEMBL576127 ;
CompTox Dashboard (EPA)	DTXSID4023048 ;
ECHA InfoCard	100.023.411
Chemical and physical data
Formula	C15H20N2O2
Molar mass	260.337 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES c1ccc(cc1)CCN2CCC3(CC2)CN=C(O3)O;
	InChI InChI=1S/C15H20N2O2/c18-14-16-12-15(19-14)7-10-17(11-8-15)9-6-13-4-2-1-3-5-13/h1-5H,6-12H2,(H,16,18) ; Key:FVNFBBAOMBJTST-UHFFFAOYSA-N ;
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Fenspiride (INN, brand names Eurespal, Pneumorel and others) is an oxazolidinone spiro compound used as a drug in the treatment of certain respiratory diseases.^[2] The pharmacotherapeutic classification is antitussives. In Russia it was approved for the treatment of acute and chronic inflammatory diseases of ENT organs (ear, nose, throat) and the respiratory tract (like rhinopharyngitis, laryngitis, tracheobronchitis, otitis and sinusitis), as well as for maintenance treatment of asthma.^[3] Russia, Romania, France and other European countries withdrew fenspiride-based drugs from the market due to the risk of QT prolongation and torsades de pointes.^[4] Fenspiride is known to have activity as an alpha-1 blocker, H1 antagonist, it also inhibits PDE3, PDE4, PDE5 with -logIC50 values of 3.44, 4.16, 3.8 respectively.^[5]

References

^ Montes B, Catalan M, Roces A, Jeanniot JP, Honorato JM (1993). "Single dose pharmacokinetics of fenspiride hydrochloride: phase I clinical trial". European Journal of Clinical Pharmacology. 45 (2): 169–72. doi:10.1007/bf00315501. PMID 7901024. S2CID 20605939.
^ Płusa T, Nawacka D (December 1998). "[Efficacy and tolerance of fenspiride in adult patients with acute respiratory tract infections]". Polski Merkuriusz Lekarski. 5 (30): 368–71. PMID 10101527.
^ "Эреспал (Eurespal) Prescribing Information. VIDAL Drug Compendium" (in Russian). Retrieved 6 February 2014.
^ "Fenspiride containing medicinal products". European Medicines Agency. 2019-02-15. Retrieved 2019-06-12.
^ Jankowski R (September 2002). "[ENT inflammation and importance of fenspiride]". Presse Med (in French). 31 Spec No 1: HS7–10. PMID 12378970.

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[1] Montes B, Catalan M, Roces A, Jeanniot JP, Honorato JM (1993). "Single dose pharmacokinetics of fenspiride hydrochloride: phase I clinical trial". European Journal of Clinical Pharmacology. 45 (2): 169–72. doi:10.1007/bf00315501. PMID 7901024. S2CID 20605939.

[2] Płusa T, Nawacka D (December 1998). "[Efficacy and tolerance of fenspiride in adult patients with acute respiratory tract infections]". Polski Merkuriusz Lekarski. 5 (30): 368–71. PMID 10101527.

[PI-3] "Эреспал (Eurespal) Prescribing Information. VIDAL Drug Compendium" (in Russian). Retrieved 6 February 2014.

[4] "Fenspiride containing medicinal products". European Medicines Agency. 2019-02-15. Retrieved 2019-06-12.

[pmid12378970-5] Jankowski R (September 2002). "[ENT inflammation and importance of fenspiride]". Presse Med (in French). 31 Spec No 1: HS7–10. PMID 12378970.

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References

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