Optimal Dosing Regimen of Osteoporosis Drugs in Relation to Food Intake as the Key for the Enhancement of the Treatment Effectiveness—A Concise Literature Review

Abstract

Bisphosphonates and selective estrogen receptor modulators (SERMs) represent the two most important groups of medications taken orally and employed in osteoporosis treatment. Effectiveness of the therapy may be affected by poor patient adherence, in particular, due to the inconvenient dosing regimen of oral bisphosphonates. With this review we aimed to assess the effects that food, beverages, and dietary supplements consumed during treatment, along with the dosing regimens, may have on pharmacokinetics and pharmacodynamics of oral drugs employed in treating osteoporosis; we also aimed to shape the recommendations valuable for professional patients’ counseling and education, to provide appropriate dosing regimens in order to improve adherence to the therapy. Food, beverages such as coffee, juices, and mineral water, as well as dietary supplements containing multivalent cations, e.g., calcium, magnesium, aluminium, iron, showed to have a deleterious effect on the bioavailability of all the investigated oral bisphosphonates, specifically alendronate, risedronate, ibandronate, minodronate, and etidronate. For risedronate, a delayed-release (DR) tablet was designed to solve the malabsorption problem in the presence of food, hence DR risedronate can be ingested following breakfast. For other oral bisphosphonates, the proper interval between drug and food, beverages, and dietary supplements intake should be maintained to minimize the risk of interactions. The effect of food on pharmacokinetic parameters of selective estrogen receptor modulators (SERMs) was found to be clinically irrelevant.

Drug Repurposing for Rare Diseases: A Role for Academia

“…Etidronate is a bisphosphonate and was originally developed to prevent and treat osteoporosis. The product has been replaced by alternative bisphosphonates with a better benefit-risk profile over time ( Wiesner et al, 2021 ). This led to the discontinuation of marketing of virtually all etidronate products in Europe ( Ministerie van Volksgezondheid, Welzijn en Sport, 2018 ).…”

Prevalence of comorbidities and concomitant medication use in acromegaly: analysis of real-world data from the United States

“…Challenges posed by the prescription of multiple oral medications include managing potential drug-drug interactions as well as abiding by any food restrictions [26,27,35]. For example, many of the oral medications used to treat thyroid disorders and bone diseases (prescribed to 35.4% and 2.7% of patients with acromegaly in our analysis, respectively), as well as certain drugs to treat diabetes, are commonly taken while fasting [36][37][38]. Patients taking levothyroxine or alendronate must also generally continue fasting for a period of time before taking any other drugs [37,38], including those to treat acromegaly.…”

“…For example, many of the oral medications used to treat thyroid disorders and bone diseases (prescribed to 35.4% and 2.7% of patients with acromegaly in our analysis, respectively), as well as certain drugs to treat diabetes, are commonly taken while fasting [36][37][38]. Patients taking levothyroxine or alendronate must also generally continue fasting for a period of time before taking any other drugs [37,38], including those to treat acromegaly. Furthermore, proton-pump inhibitors, prescribed in oral form for 22.2% of patients with acromegaly in this study, alter the acidic environment of the stomach and thus can impact absorption of other oral medications [39,40].…”

Severe drug-induced oesophagitis in a young male patient

“…This is because alendronate is very hydrophilic leading to frequent gastrointestinal symptoms and poor patient adherence. [2][3][4] In contrast, intravenous formulations require less frequent dosing and are not associated with gastrointestinal symptoms. 2 Its pathogenic pathway is associated with chemical direct lesion of the oesophageal mucosa caused by the tablet passing through the oesophagus and possibly the reflux of drug-containing gastric content.…”