Tachyphylaxis with amrinone therapy: association with sequestration and down-regulation of lymphocyte beta-adrenergic receptors

Ann Intern Med. 1989 Feb 1;110(3):195-201. doi: 10.7326/0003-4819-110-3-195.

Abstract

Study objective: To determine whether intravenous therapy with amrinone changes number, location or function of the beta-adrenergic receptors on lymphocytes.

Design: Case series.

Setting: Veterans hospital coronary care unit.

Patients: Eleven patients with decompensated class III or IV heart failure.

Interventions: A bolus of intravenous amrinone followed by a continuous infusion at 10 micrograms/kg.min for 72 hours.

Measurements and main results: At 24 to 36 hours there was a reduction in pulmonary capillary wedge pressure (35%), right atrial pressure (20%), and systemic vascular resistance (25%) with an increase in cardiac output (30%). By 72 hours all these parameters had returned nearly to baseline levels. This partial cardiovascular tolerance to amrinone was accompanied by a 126% increase in the plasma epinephrine, a 182% increase in norepinephrine, a 31% decrease in the number of beta-adrenergic receptors on lymphocytes, and a 36% decrease in isoproterenol-stimulated cyclicadenosine monophosphate on lymphocytes. The number of sequestered receptors doubled during the treatment, and the extent of sequestration correlated well with the extent of receptor down-regulation.

Conclusions: The hemodynamic responses to amrinone had virtually returned to baseline by 72 hours. This tolerance was accompanied by increased plasma catecholamines, and a down-regulation, desensitization, and sequestration of beta-adrenergic receptors on lymphocytes. We suggest that these receptor changes also occur in cardiovascular tissues and may in part account for the tolerance to amrinone.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Aged
  • Amrinone / therapeutic use*
  • Cardiac Output / drug effects
  • Cyclic AMP / analysis
  • Drug Tolerance
  • Female
  • Heart Failure / blood
  • Heart Failure / drug therapy*
  • Humans
  • Infusions, Intravenous
  • Lymphocytes / metabolism*
  • Male
  • Middle Aged
  • Receptors, Adrenergic, beta / drug effects*
  • Receptors, Adrenergic, beta / metabolism
  • Tachyphylaxis*

Substances

  • Receptors, Adrenergic, beta
  • Cyclic AMP
  • Amrinone