Lack of a pharmacokinetic interaction between carvedilol and digitoxin or phenprocoumon. 1993

S Harder, and R Brei, and S Caspary, and P G Merz
Department of Clinical Pharmacology, University Hospital Frankfurt/Main, Germany.

The possibility of a pharmacokinetic interaction between carvedilol and digitoxin (Study I) or phenprocoumon (Study II) has been evaluated in groups of 12 healthy volunteers. The bioavailability (Cmax, tmax, AUC) of digitoxin and phenprocoumon were assessed after a single dose, given once alone and once on day 6 of treatment with carvedilol 25 mg o.d. Cmax, tmax, AUC and Ut of carvedilol and desmethylcarvedilol were also investigated after the fifth dose of carvedilol and after the sixth dose given concomitantly with digitoxin or phenprocoumon. In Study I, the 95% confidence intervals of the ratio test versus the reference findings were; digitoxin Cmax 0.80-1.20, tmax 0.56-1.14, AUC 0.97-1.33, and for carvedilol Cmax 0.81-1.22; tmax 0.66-1.23; AUC 0.91-1.17. Formation of the active metabolite desmethylcarvedilol and the urinary recovery of carvedilol and desmethylcarvedilol were not influenced by digitoxin. In Study II Cmax and AUC of phenprocoumon were not changed after carvedilol. Cmax of carvedilol was decreased after phenprocoumon. The kinetic parameters of phenprocoumon were Cmax 0.80-1.05, tmax 0.47-2.00, AUC 0.78-1.05, and for carvedilol Cmax 0.59-1.06, tmax 0.71-1.73; AUC 0.80-1.08, respectively. The plasma levels of desmethylcarvedilol and the urinary recovery of carvedilol and desmethylcarvedilol were not influenced by phenprocoumon. The blood pressure and heart rate after carvedilol alone were not affected by concomitant administration of digitoxin or phenprocoumon.

UI MeSH Term Description Entries
D008297 Male Males
D010644 Phenprocoumon Coumarin derivative that acts as a long acting oral anticoagulant. Phenprocoumalol,Phenprocoumarol,Phenylpropylhydroxycumarinum,Falithrom,Liquamar,Marcoumar,Marcumar,Phenprogramma
D011412 Propanolamines AMINO ALCOHOLS containing the propanolamine (NH2CH2CHOHCH2) group and its derivatives. Aminopropanols
D002227 Carbazoles Benzo-indoles similar to CARBOLINES which are pyrido-indoles. In plants, carbazoles are derived from indole and form some of the INDOLE ALKALOIDS.
D004074 Digitoxin A cardiac glycoside sometimes used in place of DIGOXIN. It has a longer half-life than digoxin; toxic effects, which are similar to those of digoxin, are longer lasting. (From Martindale, The Extra Pharmacopoeia, 30th ed, p665) Coramedan,Digimed,Digimerck,Digitaline Nativelle,Digitoxin AWD,Digitoxin Bürger,Digitoxin Didier,Digitoxin-Philo,Digophton,AWD, Digitoxin,Bürger, Digitoxin,Didier, Digitoxin,Digitoxin Philo,Nativelle, Digitaline
D004347 Drug Interactions The action of a drug that may affect the activity, metabolism, or toxicity of another drug. Drug Interaction,Interaction, Drug,Interactions, Drug
D005260 Female Females
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000077261 Carvedilol A carbazole and propanol derivative that acts as a non-cardioselective beta blocker and vasodilator. It has blocking activity for ALPHA 1 ADRENERGIC RECEPTORS and, at higher doses, may function as a blocker of CALCIUM CHANNELS; it also has antioxidant properties. Carvedilol is used in the treatment of HYPERTENSION; ANGINA PECTORIS; and HEART FAILURE. It can also reduce the risk of death following MYOCARDIAL INFARCTION. BM 14190,BM-14190,Carvedilol Hydrochloride,Carvedilol, (+),Carvedilol, (+)-isomer,Carvedilol, (+-)-isomer,Carvedilol, (-),Carvedilol, (-)-isomer,Carvedilol, (R)-isomer,Carvedilol, (S)-isomer,Carvedilol, 14C-labeled,Coreg,Coropres,Dilatrend,Eucardic,Kredex,Querto,14C-labeled Carvedilol,BM14190,Carvedilol, 14C labeled
D000328 Adult A person having attained full growth or maturity. Adults are of 19 through 44 years of age. For a person between 19 and 24 years of age, YOUNG ADULT is available. Adults

Related Publications

S Harder, and R Brei, and S Caspary, and P G Merz
January 1996, European journal of clinical pharmacology,
S Harder, and R Brei, and S Caspary, and P G Merz
March 2000, Alimentary pharmacology & therapeutics,
S Harder, and R Brei, and S Caspary, and P G Merz
January 1984, Biomedica biochimica acta,
S Harder, and R Brei, and S Caspary, and P G Merz
September 2004, The Annals of pharmacotherapy,
S Harder, and R Brei, and S Caspary, and P G Merz
January 1984, British journal of clinical pharmacology,
S Harder, and R Brei, and S Caspary, and P G Merz
November 1980, Annals of internal medicine,
S Harder, and R Brei, and S Caspary, and P G Merz
December 1981, Journal of veterinary pharmacology and therapeutics,
S Harder, and R Brei, and S Caspary, and P G Merz
August 1994, Journal of clinical pharmacy and therapeutics,
S Harder, and R Brei, and S Caspary, and P G Merz
January 1990, European journal of clinical pharmacology,
S Harder, and R Brei, and S Caspary, and P G Merz
June 1999, European journal of clinical pharmacology,
Copied contents to your clipboard!