Pharmacokinetics and bioavailability of denaverine hydrochloride in healthy subjects following intravenous, oral and rectal single doses

European Journal of Pharmaceutical Sciences

Volumn 18, Issue 2, 2003, Pages 121-128

  Staab, Alexander ^a,d   Schug, Barbara S ^a,e   Larsimont, Véronique ^a,f   Elze, Martina ^a,g   Thümmler, Daniela ^b   Mutschler, Ernst ^c   Blume, Henning ^a,e  

^a ABDA Bundesvereinigung Deutscher Apothekerverbande   (Germany)

^b APOGEPHA Arzneimittel GmbH   (Germany)

^c GOETHE UNIVERSITY   (Germany)

^d BOEHRINGER INGELHEIM PHARMA GMBH AND CO KG   (Germany)

^e SocraTec R and D GmbH   (Germany)

^f IMFORM GmbH Intl Clinical Research   (Germany)

^g ClinResearch GmbH   (Germany)

Author keywords

Bioavailability; Denaverine; Denaverine hydrochloride; First pass metabolism; N Monodemethyl denaverine; Pharmacokinetics; Suppository

Indexed keywords

BIOLOGICAL ORGANS; METABOLISM; MUSCLE; PHARMACOKINETICS;

MUSCLE SPASMS;

DRUG PRODUCTS;

DENAVERINE;

ADULT; AQUEOUS SOLUTION; ARTICLE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG FORMULATION; DRUG HALF LIFE; DRUG METABOLISM; DRUG TRANSFORMATION; FEASIBILITY STUDY; FEMALE; FIRST PASS EFFECT; HUMAN; HUMAN EXPERIMENT; MALE; NORMAL HUMAN; PRIORITY JOURNAL; STEADY STATE; SUPPOSITORY;

ADMINISTRATION, ORAL; ADMINISTRATION, RECTAL; ADULT; AREA UNDER CURVE; BENZILATES; BIOLOGICAL AVAILABILITY; CONFIDENCE INTERVALS; CROSS-OVER STUDIES; FEMALE; HUMANS; INFUSIONS, INTRAVENOUS; MALE;

EID: 0037314845     PISSN: 09280987     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0928-0987(02)00225-7     Document Type: Article

References (26)

1. Amon K., Amon I. Experimentelle Untersuchungen eines neuen Spasmoanalgetikums am Rattenuterus und erste klinische Erfahrungen in der Geburtshilfe. Zentralbl. Gynakol. 90:1968;1115-1122.
2. Babul N., Darke A.C. Disposition of morphine and its glucuronide metabolites after oral and rectal administration: evidence of route specificity. Clin. Pharmacol. Ther. 54:1993;286-292.
3. Bredow V. Die Anwendung von Tramadol-versus Pethidin-versus Denaverinsuppositorien unter der Geburt - ein Beitrag zur nichtinvasiven Geburtsschmerztherapie. Zentralbl. Gynakol. 114:1992;551-554.
4. Cid E., Mella F., Lucchini L., Cárcamo M., Monasterio J. Plasma concentrations and bioavailability of propranolol by oral, rectal and intravenous administration in man. Biopharm. Drug Dispos. 7:1986;559-566.
5. de Boer A.G., Breimer D.D., Mattie H., Pronk J., Gubbens-Stibbe J.M. Rectal bioavailability of lidocaine: partial avoidance of first-pass metabolism. Clin. Pharmacol. Ther. 26:1979;701-709.
6. de Boer A.G., de Leede L.G.J., Breimer D.D. Drug absorption by sublingual and rectal routes. Br. J. Anaesth. 56:1984;69-82.
7. de Boer A.G., Moolenaar F., de Leede L.G.J., Breimer D.D. Rectal drug administration, Clinical pharmacokinetic considerations. Clin. Pharmacokinet. 7:1982;285-311.
8. FDA (US Food and Drug Administration), 2001. Guidance: Statistical approaches to establishing bioequivalence.
9. Fischer F.X. Literaturübersicht über die rektale Absorption von Wirkstoffen. Müller B.W. Suppositorien. 1986;208-263 Wissenschaftliche Verlagsgesellschaft, Stuttgart.
10. Gibaldi M., Perrier D. Pharmacokinetics. 1982;Marcel Dekker, New York.
11. Göber B., Lisowski H., Franke P. Zur Analytik und Stabilität von Denaverinhydrochlorid. Pharmazie. 36:1981;812-815.
12. Hellstern A., Hellenbrecht D., Saller R., Gatzen M., Manus B., Achtert G., Brockmann P., Hausleiter H.J., Leuschner U. Absolute bioavailability of metoclopramide given orally or by enema in patients with normal liver function or with cirrhosis of the liver. Drug Res. 37:1987;733-736.
13. Hüller H. Pharmakologie und Klinik von O-(2-Äthylbutoxy)-benzilsäure-2- dimethylaminoäthylesterhydrochlorid (=Spasmalgan). Zentralbl. Pharm. 109:1970;115-139.
14. Hüller H., Scheler W., Oberender W., Peters R. Pharmakologische Vergleichsuntersuchungen mit Derivaten des α,α-Diphenyl-α-(2-äthylbutoxy)-essigsäure- (β-dimethylaminoäthyl) esters. Acta Biol. Med. Ger. 22:1969;751-758.
15. Hughes K.M., Lang J.C.T., Lazare R., Gordon D., Stanton S.L., Malone-Lee J., Geraint M. Measurement of oxybutynin and its N-desethyl metabolite in plasma, and its application to pharmacokinetic studies in young, elderly and frail elderly volunteers. Xenobiotica. 22:1992;859-869.
16. Köpernik H., Schwarz B. Klinische Erfahrungen mit dem Spasmoanalgetikum Spasmalgan in der Geburtshilfe. Z. Arztl. Fortbild. 67:1973;656-658.
17. Lippold B.C. Biopharmazie. 1984;Wissenschaftliche Verlagsgesellschaft, Stuttgart.
18. Neumayer E. Erfahrungen mit Spasmalgan in der Geburtshilfe. Medicamentum. 16:1975;264-266.
19. Sanders S.W., Haering N., Mosberg H., Jaeger H. Pharmacokinetics of ergotamine in healthy volunteers following oral and rectal dosing. Eur. J. Clin. Pharmacol. 30:1986;331-334.
20. Scharein E., Bromm B. The intracutaneous pain model in the assessment of analgesic efficacy. Pain Rev. 5:1998;216-246.
21. Staab A., Scheithauer S., Fieger-Büschges H., Mutschler E., Blume H. A validated high-performance liquid chromatographic assay for the simultaneous determination of denaverine and its N-monodemethyl metabolite in human plasma. J. Chromatogr. B. 751:2001;221-228.
22. Vesper B. Erfahrungen bei der Anwendung von Spasmalgan in der Geburtshilfe. Medicamentum. 12:1971;335-337.
23. van Hoogdalem E.J., de Boer A.G., Breimer D.D. Pharmacokinetics of rectal drug administration. Part I. General considerations and clinical applications of centrally acting drugs. Clin. Pharmacokinet. 21:1991;11-26.
24. van Hoogdalem E.J., de Boer A.G., Breimer D.D. Pharmacokinetics of rectal drug administration. Part II. Clinical applications of peripherally acting drugs, and conclusions. Clin. Pharmacokinet. 21:1991;110-128.
25. Zanke S., Seewald H.J., Michels W., Kunath H., Schubert H. Rechenautomatische Auswertung von Tokogrammen nach Applikationen von Spasmalgan (Denaverin). Zentralbl. Gynakol. 100:1978;1182-1185.
26. Zimmer K., Müller K., Lange J., Schneider W. Erfahrungen bei der Anwendung von Spasmalgan-Ampullen unter der Geburt. Zentralbl. Gynakol. 96:1974;1530-1533.