Disease relevance of Pafenolol

• Pafenolol in hypertension: a double-blind randomized trial of a new beta 1-selective adrenoceptor blocker [1].

High impact information on Pafenolol

• Displacement of specific binding by the beta 1-adrenoceptor antagonist pafenolol and the beta 2-adrenoceptor antagonist ICI 118.551 revealed that the colon preparation possessed a heterogenous beta-adrenoceptor population [2].
• The 24-hour blood pressure and heart rate recordings showed a clear dose-response relationship for pafenolol that could not be detected by ordinary casual readings [3].
• A daily dose of 25 mg of pafenolol significantly reduced blood pressure during the 9 hours after tablet intake (p less than 0.01), while 50 mg per day of pafenolol resulted in a significant reduction throughout the 24-hour period (p less than 0.01) [3].
• A separately reported exercise study in the same patients showed that 5 mg pafenolol and 15 mg metoprolol were equipotent with respect to beta 1-adrenoceptor blockade, whereas 7.5 mg pafenolol tended to increase the blockade [4].
• After iv administration of pafenolol, the excretion of unchanged drug into urine and feces was about 50 and 25-30% of the given dose, respectively [5].

Biological context of Pafenolol

• The pharmacokinetics of pafenolol were studied in eight young healthy individuals [6].
• The gastrointestinal absorption characteristics of pafenolol following oral administration as a solution in man and rat has previously been found to be a double-peak phenomenon and exhibited dose-dependent bioavailability, despite negligible presystemic metabolism [7].
• We addressed the question whether the intestinal absorption of pafenolol was affected by bile depletion in the gut lumen of rats [8].
• Further, the hypothesis that variable gastric emptying accounts for double peaks in blood was tested by duodenal administration of pafenolol [8].

Anatomical context of Pafenolol

• The beta 1-antagonists pafenolol and pamatolol in concentrations higher than those, which blocked the effects of the agonists on beating rate, were devoid of inhibitory effects in the uterus [9].
• These results suggest that the low bioavailability of pafenolol is due to a complexation between bile and pafenolol in the gut lumen, preventing intestinal uptake in the major part of the small intestine [8].

Associations of Pafenolol with other chemical compounds

• The origin of the presystemic metabolism was studied in rats after oral and intraperitoneal administration of tritium-labeled pafenolol with reference to the intravenous route by means of urinary excretion data of pafenolol and metabolites specifically assayed by HPLC and radioisotope detection [10].

Analytical, diagnostic and therapeutic context of Pafenolol

• After single oral doses of pafenolol 25 to 100 mg, there was a marked reduction in heart rate and systolic blood pressure during exercise tests [11].

References