Nifedipine: Kinetics and dynamics in healthy subjects

Kleinbloesem, C. H.; Brummelen, P. Van; Linde, J A Van De; Voogd, P. J.; Breimer, D.D.

doi:10.1038/clpt.1984.105

Cited by 217 publications

(86 citation statements)

References 0 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…The present study demonstrated that the fractions of dose absorbed (F) in both forms are rather low (0.18-0.63). These values of pharmacokinetic parameters are essentially similar to those reported previously (Brennan et al 1983;Raemsch and Sommer 1983;Taburet et al 1983;Kleinbloesem et al 1984). The values of systemic availability of nifedipine suggest that the absorption is incomplete or this substance is subjected to the first pass effect, or both.…”

Section: Discussionsupporting

confidence: 78%

Pharmacokinetics and pharmacodynamics of conventional and slow release forms of nifedipine in essential hypertensive patients.

Imai

Abe

Sasaki

et al. 1986

Tohoku J. Exp. Med.

View full text Add to dashboard Cite

In patients with essential hypertension, the pharmacokinetics of nifedipine in 2 forms (capsule, 10 mg nifedipine dissolved in an organic solvent ; slow release tablet, 20 mg nifedipine) and their pharmacodynamic effectiveness on arterial pressure were studied. The maximum plasma concentration was higher and achieved more rapidly after application of the capsule than after the retard tablet (p <0.01). The plasma half-time of nifedipine in the capsule was shorter than that in the retard tablet (p <0.05). The absorption rate of nifedipine from the capsule tended to be larger than that from the retard tablet. Plasma concentrations of nifedipine, measured 12 hr after the dosing of the retard tablet during chronic treatment, were not different from those after the acute administration of the retard tablet, suggesting that no accumulation of nifedipine occurs. The capsule of nifedipine elicited prompt and profound hypotension with short duration, while the retard tablet produced a hypotensive effect with relatively slow onset and long duration. Arterial pressure reduction was maintained throughout the day using 12 hourly dose of the retard tablet. During the chronic treatment the maximum hypotensive effect was observed 4 weeks after the start of treatment. Twelve hourly administration of the retard tablet is a convenient regimen for the long-term control of mild to severe essential hypertension.nifedipine ; slow release form ; conventional form ; antihypertensive therapy ; essential hypertension Nifedipine is a potent vasodilator, which relaxes vascular smooth muscle probably by its inhibitory effect on the transmembrane influx of calcium (Fleckenstein et al. 1972 ). It has been demonstrated that this drug exerts a prompt and marked hypotensive effect when administered to hypertensive patients (Murakami et al, 1972;Aoki et al, 1976;Guazzi et al. 1977;Pedersen and Mikkelsen 1978;Imai et al. 1980) and the drug has been accepted as a critical therapeutic for several forms of hypertension (Guazzi et al. 1983;Massie et al. 1984; Muhller et

show abstract

Section: Discussionsupporting

confidence: 78%

Pharmacokinetics and pharmacodynamics of conventional and slow release forms of nifedipine in essential hypertensive patients.

Imai

Abe

Sasaki

et al. 1986

Tohoku J. Exp. Med.

View full text Add to dashboard Cite

show abstract

“…Nifedipine usually shows no marked antihypertensive eŠect in normal individuals, because the diastaltic sympathicotonia through pressoreceptor with decreases of peripheral arterial resistance induces the increases of heart rate, and prevents blood pressure decreases. 20) However, there have been reports [21][22][23][24][25][26][27][28] that nifedipine signiˆcantly reduced the blood pressure by oral and sublingual administration and that the serum nifedipine concentration was correlated with the antihypertensive eŠect in normal individuals. In our study, also, the serum concentration was correlated with blood pressure, especially DBP, by each administration method.…”

Section: Discussionmentioning

confidence: 99%

Evaluation of the Method for Nifedipine Administration for a Rapid Onset of Clinical Effect: A Clinical Study in Normal Volunteers.

2001

View full text Add to dashboard Cite

Nifedipine is frequently used for patients who require an immediate reduction of blood pressure elevated temporarily by various administration techniques including sublingual route without administrating intravenous infusion of vasodilator. A cross-over clinical study was conducted to investigate the optimal administration metho of nifedipine for rapid management of hypertension. Four method of administering 10 mg nifedipine (the capsule was bitten and swallowed, sublingually with a hole in it or the contents administered orally or intranasally with a syringe) were evaluated with regarded e‹cacy, safety, and usefulness in 6 normal volunteers. Systolic and diastolic blood pressures were correlated with the nifedipine serum concentration in each method. Nifedipine pharmacokinetic parameters diŠered among the 4 administration methods. Nifedipine was absorbed rapidly by not only intestinal mucosa but also the nasal or oral mucosa. The pharmacological eŠect of intranasal or sublingual administration was superior. However, mint oil which is present in nifedipine capsules stimulates nasal mucosa when administered intranasally. For clinical usage, nifedipine capsules in which a hole is made with a needle, administered sublingually, can be eŠectively and safely used for rapid management of systemic hypertension.

show abstract

“…However, this proposed mechanism does not explain the increased plasma level of nifedipine associated with concomitant administration of diltiazem. Such a mechanism would also raise the diltiazem plasma concentration, since nifedipine is a stronger vasodilator than diltiazem and diltiazem undergoes more extensive first-pass metabolism than does nifedipine (their bioavailabilities are 42%33 and 55% to 63%, 34 In summary, the results of this study indicate that, in patients with effort angina, exercise tolerance is increased by the concomitant administration of diltiazem and nifedipine. This effect appears to be partly a consequence of an increase in the nifedipine plasma concentration as an expression of drug interaction.…”

Section: Resultsmentioning

confidence: 59%

Combination therapy with diltiazem and nifedipine in patients with effort angina pectoris.

et al. 1988

View full text Add to dashboard Cite

The antianginal effects of diltiazem and nifedipine alone and in combination were evaluated in a double-blind, randomized, placebo-controlled trial in 11 patients (nine men and two women, 57 + 8 years old) with stable effort angina. Each Subjects and methodsStudy patients. The study group consisted of 11 patients (nine men and two women, average age 57 years, range 39 to 68) with stable effort angina. All of the patients had already performed at least two exercise tests before participation in this study. All patients showed reproducible positive results on the exercise test with regard to exercise-induced chest pain and ischemic electrocardiographic changes (horizontal or downsloping ST segment depression .0.1 mV for at least 0.08 sec after the J point). Selective coronary angiography demonstrated that every patient had significant coronary artery disease, defined as greater than 75% narrowing of the luminal diameter. Five patients had one-vessel, three patients had two-vessel, and three patients had three-vessel coronary artery disease. Two patients had a history of myocardial infarction, but were without episodes within the 6 months preceding the study.Protocol. During the study period, all patients were admitted to the hospital and all antianginal medications other than sublingual isosorbide dinitrate (5 mg) were discontinued for at least 72 hr before the study. The study protocol consisted of four different treatment periods of 1 week each, and every patient underwent all four treatments in succession. Assignment to a specific sequence of treatments was random. The drugs and dosages were: placebo four times daily, 30 mg diltiazem four times daily, 10 mg nifedipine four times daily, and a combination of 30 mg diltiazem plus 10 mg nifedipine four times daily. Placebo or drugs were taken at 6 hr intervals starting at 5:00 A.M. (5 A.M., 11 A.M., 5 P.M., and 11 P.M.).At 4 P.M. on the seventh (final) day of each treatment period, the patients performed a symptom-limited treadmill exercise CIRCULATION

show abstract

Nifedipine: Kinetics and dynamics in healthy subjects

Cited by 217 publications

References 0 publications

Pharmacokinetics and pharmacodynamics of conventional and slow release forms of nifedipine in essential hypertensive patients.

Pharmacokinetics and pharmacodynamics of conventional and slow release forms of nifedipine in essential hypertensive patients.

Evaluation of the Method for Nifedipine Administration for a Rapid Onset of Clinical Effect: A Clinical Study in Normal Volunteers.

Combination therapy with diltiazem and nifedipine in patients with effort angina pectoris.

Contact Info

Product

Resources

About