Overview of Novel Renal Properties of Tertatolol

Abstract

The renal vasodilatating properties of tertatolol demonstrated in animals have been confirmed in man. In a first study [Paillard et al., 1986], tertatolol (T) 5 mg and propranolol (Pr) 160 mg (SR) were given orally for 15 days to 2 groups of 9 patients with essential hypertension. Glomerular filtration rate (GFR), measured by inulin clearance and renal plasma flow (RPF) measured by PAH clearance increased in T group (+8.9%, p = 0.038 and +13.0%, p = 0.007, respectively) and decreased in Pr group (-2.8%, NS and -13.4%, p < 0.001, respectively). Two clinical pharmacology studies [Leeman et al, 1986; Nitenberg et al, 1990] have shown specific and selective effects of tertatolol on the renal vasculature. In 8 hypertensive patients with chronic renal failure, the effects of tertatolol 5 mg were evaluated before and after 3 months of treatment on GFR using inulin clearance, and RPF, using PAH clearance [Hannedouche et al, 1991]. After 3 months of treatment, GFR and effective RPF increased significantly by 10 and 13%, respectively, whereas RVR decreased by 16% and the filtration fraction was unchanged. In summary, tertatolol 5 mg, contrasting with other beta-blockers, possesses a selective effect on the renal circulation beneficial to hypertensive patients. The mechanisms of this renal vasodilatation are not fully understood but might involve renal 5-HT_1A receptor stimulation.

Stereoselective HPLC analysis of tertatolol in rat plasma using macrocyclic antibiotic chiral stationary phase

“…It does not induce withdrawal syndrome after abrupt cessation and it preserves renal function. [17][18][19] Tertatolol was devoid of any atherogenic effect. 20 With respect to tertatolol enantiomers, the (1)-tertatolol showed a lower total clearance and volume of distribution, compared to the (2)-enantiomer.…”