Pindolol‐a beta‐adrenoceptor blocking drug with partial agonist activity: clinical pharmacological considerations.

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Abstract
1 Pindolol is a beta‐adrenoceptor antagonist equally effective on beta 1‐ and beta 2‐adrenoceptors which has a relatively long duration of action. It is practically completely absorbed and, unlike most other beta‐adrenoceptor blockers, is only metabolized to a small extent during the first passage through the liver. 2 Pindolol possesses partial agonist activity (intrinsic sympathomimetic activity, ISA). This means that apart from blocking beta‐adrenoceptors it produces some stimulation. Pindolol therefore only slightly influences normal sympathetic drive at rest but effectively reduces the effects of elevated sympathetic activity. 3 Various therapeutic advantages have been attributed to the partial agonist activity of pindolol: no or only slight alterations in normal cardiac output, heart rate and peripheral blood flow occur. Peripheral resistance is reduced during chronic oral therapy. No alteration of HDL/LDL cholesterol ratio has been observed. Rebound phenomena on sudden withdrawal of therapy and bronchoconstriction in susceptible patients are less likely than with drugs devoid of ISA.

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