Overview of novel renal properties of tertatolol.
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-HT1A receptor stimulation.
Guillet
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Institut de Recherches Internationales Servier, Courbevoie, France.
D000319:Adrenergic beta-Antagonists / Q000627:therapeutic use*; D000959:Antihypertensive Agents / Q000627:therapeutic use*; D006801:Humans; D006973:Hypertension / Q000150:complications / Q000188:drug therapy*; D007668:Kidney / Q000187:drug effects*; D011412:Propanolamines / Q000627:therapeutic use*; D012079:Renal Circulation / Q000187:drug effects*; D051437:Renal Insufficiency / Q000150:complications; D013876:Thiophenes
D000319:Adrenergic beta-Antagonists; D000959:Antihypertensive Agents; D011412:Propanolamines; D013876:Thiophenes; C005632:tertatolol