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Accumulation of nifedipine after multiple doses.
The Journal of Pharmacy and Pharmacology
|June 1, 1986
Summary
Nifedipine pharmacokinetics in patients with peripheral vasospasm show rapid absorption in some individuals. Nifedipine accumulates with repeated dosing every 8 hours, impacting steady-state predictions.
Area of Science:
- Pharmacology
- Clinical Pharmacy
- Cardiovascular Medicine
Background:
- Peripheral vasospasm is a condition affecting blood flow in extremities.
- Understanding nifedipine pharmacokinetics is crucial for effective treatment.
- Nifedipine is a calcium channel blocker used for vasospastic disorders.
Purpose of the Study:
- To investigate the pharmacokinetics of oral nifedipine in patients with peripheral vasospasm.
- To assess nifedipine absorption, bioavailability, and elimination after single and multiple doses.
- To determine the extent of nifedipine accumulation during repeated dosing.
Main Methods:
- Single and multiple oral doses of nifedipine (10 mg and 20 mg) were administered to five patients.
- Pharmacokinetic parameters including Tmax, Cmax, and AUC0-8h were measured.
- Nifedipine elimination rate constant and accumulation extent were calculated.
Main Results:
- Nifedipine showed variable absorption rates (rapid in 3/5 patients).
- Mean bioavailability parameters (Tmax, Cmax, AUC0-8h) were determined for single and multiple doses.
- Nifedipine demonstrated a mean accumulation ratio of 1.3 with 8-hourly dosing, indicating accumulation.
Conclusions:
- Nifedipine pharmacokinetics vary among patients with peripheral vasospasm.
- Nifedipine accumulates in the body when administered every 8 hours.
- Accumulation should be considered when predicting steady-state concentrations and hemodynamic effects from single-dose data.