Clinical pharmacokinetics of terbutaline in humans: a systematic review

Naunyn Schmiedebergs Arch Pharmacol. 2023 Feb;396(2):213-227. doi: 10.1007/s00210-022-02304-5. Epub 2022 Oct 13.

Abstract

Terbutaline is used for the management of bronchospasm associated with asthma, bronchitis, emphysema, and chronic obstructive pulmonary disease. A systematic review would be beneficial to assess the impact of routes of administration, stereoisomerism, disease states, smoking, age, exercise, and chronobiology on pharmacokinetics (PK) of terbutaline in humans. PubMed and Google Scholar databases were searched to screen all the relevant articles consisting of at least one of the PK parameters after administration of oral, inhaled, and intravenous (IV) terbutaline in humans. Oral studies of terbutaline depicted a linear relationship between plasma concentration (Cp) and the administered dose. The IV studies demonstrated multi-exponential behavior for disposition and renal clearance. Higher systemic availability was observed with inhaled as compared to oral route, and chrono-pharmacokinetic behavior was notable. Time to reach maximum plasma concentration (Tmax) was prolonged, and maximum plasma concentration (Cmax) was lowered after exercise. The primary route of excretion in chronic kidney disease (CKD) patients is reported to be nonrenal. In pregnant women, the Cp of terbutaline is lowered and clearance is increased. The addition of theophylline to terbutaline did not affect the PK of terbutaline; hence, both can be used without dose adjustment. This review summarizes all the available PK parameters of terbutaline, and it may be helpful for researchers in the development and evaluation of PK models as well as in designing optimal dosage regimens in different clinical conditions.

Keywords: Beta-2 agonists; Intravenous (IV); Pharmacokinetics (PK); Plasma concentration (C p); Terbutaline.

Publication types

  • Systematic Review
  • Review

MeSH terms

  • Administration, Intravenous
  • Asthma* / drug therapy
  • Female
  • Humans
  • Kinetics
  • Pregnancy
  • Terbutaline* / pharmacokinetics
  • Theophylline / pharmacokinetics
  • Theophylline / therapeutic use

Substances

  • Terbutaline
  • Theophylline