3455. Drotaverine

Nomenclature

CAS number: 14009-24-6
1-[(3,4-Diethoxyphenyl)methylene]-6,7-diethoxy-1,2,3,4-tetrahydroisoquinoline; 1-(3,4-diethoxybenzylidene)-6,7-diethoxy-1,2,3,4-tetrahydroisoquinoline; isodihydroperparine.
C24H31NO4; mol wt 397.51.
C 72.52%, H 7.86%, N 3.52%, O 16.10%.

Description and references

Analogue of papaverine, q.v. Prepn: BE 621917 (1962 to Chinoin), C.A. 59, 8713g (1963). Synthesis: E. Koltai et al., J. Labelled Compd. Radiopharm. 16, 351 (1979). Crystal structure: Z. B"ocksei et al., Acta Crystallogr. C51, 1587 (1995). Absorption study: P. Szentmiklosi, S. Marton, Pharmazie 38, 611 (1983). Platelet aggregation and hemorrheological effects: Z. Kapui et al., Thromb. Res. 66, 693 (1992). Clinical pharmacokinetics and bioavailability: O. O. Bolaji et al., Eur. J. Drug Metab. Pharmacokinet. 21, 217 (1996). HPLC determn in biological fluids: eidem, J. Chromatogr. 622, 93 (1993). Clinical evaluation: D. Vecsey, Ther. Hung. 32, 127 (1984). Clinical effects on fetal development: A. E. Czeizel, M. Rockenbauer, Prenatal Neonat. Med. 1, 137 (1996).

Chemical structure

Derivative

Acephyllinate.

Nomenclature

CAS number: 61954-97-0
Drotaverine theophylline-7-acetic acid; 6,7,3′,4′-tetraethoxy-1-benzyl-3,4-dihydroisoquinoline xanthine-7-acetate; DRA; Depogen (Chinoin).
C24H31NO4.C9H10N4O4; mol wt 635.71.
C 62.35%, H 6.50%, N 11.02%, O 20.13%.

Properties

Exists as monohydrate.

Derivative

Hydrochloride.

Nomenclature

CAS number: 985-12-6
No-Spa (Chinoin).

Properties

Pale yellow crystals from ethanol, mp 197-200° (uncorr).

Therapeutic Category

Antispasmodic.

Keywords

Antispasmodic