A Review on Pharmacokinetic and Pharmacodynamic Drug Interactions of Adrenergic β-blockers with Clinically Relevant Drugs-An Overview

Abstract

: Adrenergic β-blockers are used to treat many conditions, including hypertension, cardiac arrhythmias, heart failure, angina pectoris, migraine, and tremors. The majority of the β-blockers, including propranolol, metoprolol, acebutolol, alprenolol, betaxolol, carvedilol, nebivolol, and oxprenolol are metabolised majorly by CYP2D6, and bisoprolol is primarily metabolised by CYP3A4 enzymes. The drugs inhibiting or inducing them may alter the pharmacokinetics of those β-blockers. The plasma concentrations of propranolol might be elevated by the concomitant use of drugs such as SSRIs (Fluoxetine, Paroxetine), SNRIs (Duloxetine), and cimetidine, while the plasma concentrations of metoprolol are increased by the concurrent use of SSRIs (Fluoxetine, Paroxetine), amiodarone, celecoxib, cimetidine, terbinafine, and diphenhydramine. β-blockers can also interact pharmacodynamically with drugs, including fluoroquinolones, antidiabetic agents, and NSAIDs. In addition, β-blockers may interact with herbs such as curcumin, Ginkgo biloba, Schisandra chinensis, green tea, guggul, hawthorn, St. John’s wort, and Yohimbine . This article focuses on clinically relevant drug interactions of β-blockers with commonly prescribed medications. In addition to pharmacokinetics and pharmacodynamics of the drug interactions, recommendations for clinical practice are highlighted. The prescribers and the pharmacists are needed to be aware of the drugs interacting with β-blockers to prevent possible adverse drug interactions.

A HPLC-MS/MS method for the determination of Nadolol in rat plasma: Development, validation, and application to pharmacokinetic study

“…[2][3][4][5] Nadolol, like other β-adrenoceptor-blocking drugs, significantly reduces resting heart rate in patients with coronary artery disease and hypertension. 6,7 Moderate oral doses of Nadolol and propranolol (10-80 mg) inhibit the double product (heart rate × systolic blood pressure) in a dose-related manner. 8 Oral Nadolol is more potent than Atenolol in blocking exercise tachycardia in healthy subjects.…”

Pharmacokinetics and Pharmacodynamics: A Comprehensive Analysis of the Absorption, Distribution, Metabolism, and Excretion of Psychiatric Drugs

“…The conditions above include anxiety disorders, obsessive–compulsive disorders, and premenstrual dysphoric disorders. Hence, the use of selective serotonin reuptake inhibitors (SSRIs) may be regarded as a rational and mechanism-based therapeutic strategy [ 6 ].…”

Influence of β- blockers on the activity of some anti-epileptic drugs on convulsions induced by picrotoxin in mice

“…Most of β-blockers are metabolized majorly by CYP2D6, such as propranolol and metoprolol. Therefore the bioavailability of drugs that metabolized by the same enzyme could be altered and as a consequence their pharmacological effect (Maideen et al 2021). Anti-epileptic drugs exert their action mainly through the inhibition of the central nervous system to decrease the firing and the excitability of neurons.…”