Pharmacokinetics of Cardiovascular Drugs in Heart Failure

Heart failure induces profound alterations in the absorption, distribution, metabolism and excretion of cardiovascular agents. Reduced cardiac output and splanchnic perfusion may delay gastrointestinal uptake, while oedema and hypoalbuminaemia modify plasma protein binding and increase the apparent volume of distribution of lipophilic compounds. Hepatic metabolism of prodrugs and high-extraction agents is frequently impaired by diminished liver blood flow, necessitating dose adjustments to avoid accumulation or subtherapeutic exposure. Renal clearance of diuretics and renin–angiotensin inhibitors often declines in cardiorenal syndrome, emphasising the need to monitor glomerular filtration rate and adjust dosing intervals. Key pharmacokinetic parameters such as peak plasma concentration and overall exposure inform titration of β-blockers, angiotensin receptor-neprilysin inhibitors, mineralocorticoid receptor antagonists and newer sodium–glucose co-transporter-2 inhibitors. An integrated understanding of drug–drug and drug–disease interactions is essential to optimise efficacy, minimise toxicity and improve adherence in a population characterised by polypharmacy and comorbidity.

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Pharmacokinetics of Cardiovascular Drugs in Heart Failure publication trend

The graph below shows the total number of articles in pharmacokinetics of cardiovascular drugs in heart failure across all publications each year (not limited to Nature Index journals).

Technical terms

Pharmacokinetics: The study of how a drug is absorbed, distributed, metabolised and excreted by the body.

Bioavailability: The proportion of an administered dose that reaches the systemic circulation intact.

Cmax: The maximum concentration of a drug observed in plasma after dosing.

AUC (Area Under the Curve): The integral of plasma drug concentration over time, reflecting overall exposure.

Prodrug: An inactive precursor that is converted by metabolic processes into an active pharmacological agent.

Fixed-dose combination: A single pharmaceutical formulation that contains two or more active drugs at predetermined doses.

References

1. Potential pharmacokinetic interactions in fixed-dose combinations of perindopril/indapamide/amlodipine compared with perindopril/indapamide and amlodipine in healthy Chinese volunteers. Acta Materia Medica (2023).
2. An Up-to-Date Article Regarding Particularities of Drug Treatment in Patients with Chronic Heart Failure. Journal of Clinical Medicine (2022).
3. Bioavailability study of fixed-dose tablet versus capsule formulation of amlodipine plus benazepril: A randomized, single-dose, two-sequence, two-period, open-label, crossover study in healthy volunteers. Current Therapeutic Research (2005).