Dipyridamole kinetics

Mahony, Cheryl; Wolfram, Katherine M.; Cocchetto, David M.; Bjornsson, Thorir D.

doi:10.1038/clpt.1982.42

Cited by 90 publications

(27 citation statements)

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“…Contrary to Mahony et al (1982), who reported this phenomenon only in females, we observed this rise in males as well, and our findings thus concur with those of Rosenfeld et al (1983).…”

Section: Discussionsupporting

confidence: 78%

“…The mean t½,z found in our subjects was longer than that previously reported by those workers who have recently recognized the biphasic decline of plasma dipyridamole concentration (Mahony et al, 1982;Rosenfeld et al, 1983). The reason for this discrepancy is unclear, since we employed the same assay method as Mahony et al (1982). We did not administer dipyridamole intravenously to our volunteers and therefore could not calculate the distribution volume and clearance.…”

Section: Discussioncontrasting

confidence: 46%

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Dipyridamole: pharmacokinetics and effects on aspects of platelet function in man.

Gregov

Jenkins

Duncan

et al. 1987

Brit J Clinical Pharma

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1. The effect of dipyridamole on platelet function was measured in twelve normal subjects given 150 or 200 mg tablets as single and multiple doses, and in six subjects given single doses of 25, 50 and 100 mg and multiple doses of 50 mg 8 hourly. 2. Platelet aggregation was measured in response to ADP and collagen. In the subjects given 150/200 mg, the platelets were assayed for content of cyclic AMP and for formation of thromboxane after addition of collagen. The responses to ADP and collagen and the cyclic AMP content were assessed in both the presence and absence of added PGE1. The pharmacokinetics of dipyridamole were studied in all subjects. 3. One hour after 150/200 mg single doses of dipyridamole there was significant inhibition of platelet aggregation in response to both collagen and ADP. There was no detectable effect on aggregation at other time points or with lower doses of dipyridamole. The addition of PGE1 to platelets prior to testing did not enhance the effect of dipyridamole on platelet aggregation. 4. In multiple doses, dipyridamole (150/200 mg twice daily for 11 days) had no detectable effect on platelet aggregation. 5. Dipyridamole did not have any effect on platelet cyclic AMP content, whether or not PGE1 was added prior to assay. 6. Dipyridamole did not affect platelet thromboxane formation. 7. Plasma dipyridamole concentrations were maximal 1‐2 h after ingestion, at the same time that inhibition of platelet aggregation was detected. The concentrations declined in a biexponential fashion, with a terminal half life of 24.1 +/‐ 1.9 h (mean +/‐ s.e. mean). In six of the 17 subjects, the mean steady state plasma concentration was less than 75% of the value predicted from the single dose data.

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“…Contrary to Mahony et al (1982), who reported this phenomenon only in females, we observed this rise in males as well, and our findings thus concur with those of Rosenfeld et al (1983).…”

Section: Discussionsupporting

confidence: 78%

Section: Discussioncontrasting

confidence: 46%

Dipyridamole: pharmacokinetics and effects on aspects of platelet function in man.

Gregov

Jenkins

Duncan

et al. 1987

Brit J Clinical Pharma

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“…However, attempts to use DP clinically to potentiate antimetabolite activity have so far proved unsuccessful (Wadler et al, 1987;Wilson et al, 1989). A significant problem with the clinical use of DP is the avid binding of DP to the serum protein α 1 acid glycoprotein (Mahoney et al, 1982). There is a wide variation in α 1 acid glycoprotein in humans, with normal levels between 0.5 and 1 mg ml -1 and levels in cancer patients generally being elevated to 1-3 mg ml -1 (Kremer et al, 1988).…”

Section: Cell Linementioning

confidence: 99%

Dipyridamole potentiates the in vitro activity of MTA (LY231514) by inhibition of thymidine transport

et al. 2000

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The novel pyrrolopyrimidine-based antifolate LY231514 (MTA), inhibits multiple folate-requiring enzymes including thymidylate synthase, glycinamide ribonucleotide formyltransferase and dihydrofolate reductase. Both thymidine and hypoxanthine are required to reverse MTA growth inhibition in leukaemia and colon cancer cells. Prevention of MTA growth inhibition by thymidine and/or hypoxanthine was investigated in two human lung (A549, COR L23) and two breast (MCF7, T47D) tumour cell lines, and the effect of the nucleoside/base transport inhibitor dipyridamole (DP) on thymidine and hypoxanthine rescue defined. MTA IC 50 values (continuous exposure three population doublings) were: A549–640 n M , COR L23–28 n M , MCF7–52 n M and T47D–46 n M . Thymidine (1 μ M ) completely prevented growth inhibition at the MTA IC 50 in all cell lines. At 10 × IC 50 , growth inhibition was only partially reversed by thymidine (≤ 10 μ M ); both thymidine and hypoxanthine (30 μ M ) being required for complete reversal, reflecting the multi-targeted nature of MTA. Growth inhibition by MTA was not affected by hypoxanthine alone. A non-toxic concentration (1 μ M ) of DP prevented thymidine/hypoxanthine rescue of MTA indicating that DP may potentiate MTA activity by preventing nucleoside and/or base salvage. Thymidine transport was inhibited by ≥ 89% by 1 μ M DP in all cell lines, whereas hypoxanthine transport was inhibited only in A549 and MCF7 cells. Therefore, prevention of end-product reversal of MTA-induced growth inhibition by DP can be explained by inhibition of thymidine transport alone. © 2000 Cancer Research Campaign

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“…Its concentration decreases in a triexponential fashion following intravenous infusion, with half-lives of approximately 12 minutes, 62 minutes, and 11.6 hours. 7,8 Its peak cardiac vasodilatory effect occurs 9 minutes after infusion. 6 Aminophylline is an antidote for dipyridamole as it antagonizes the adenosine receptor.…”

Section: Discussionmentioning

confidence: 99%

Surviving a stressful MIBI scan

Gooch

Bryski

Courvoisier-Grzywacz

2013

CJEM

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Dipyridamole/technetium sestamibi scans (more commonly known as MIBI scans, an acronym for methoxyisobutyl isonitrile) are used commonly for the diagnosis and risk stratification of coronary artery disease. Adverse events from MIBI scans are extremely rare. We present the case of a 64-year-old man who was successfully resuscitated after two asystolic episodes following dipyridamole infusion for a MIBI scan. The second asystolic episode occurred in the emergency department 40 minutes after the patient had been transferred from the Cardiac Stress Test Laboratory. To our knowledge, there are no previous reports of patients having two discrete asystolic episodes or an asystolic episode as delayed as we report after a MIBI scan. Our case illustrates why emergency physicians should be aware of the potential for asystole following MIBI scanning and why aminophylline, the antidote for dipyridamole, should be readily available in emergency departments that could see patients after pharmacologic stress testing. Patients who become asystolic following dipyridamole infusion likely require prolonged cardiac monitoring, given the potential for further episodes after periods of hemodynamic stability. RÉ SUMÉLes scintigraphies au dipyridamole-techné tium sestamibi (mieux connues sous le nom de scintigraphies au MIBI, acronyme anglais de mé thoxy-isobutyl-isonitrile) servent souvent au diagnostic et à la classification du risque de maladie coronarienne. Les é vé nements indé sirables dé coulant des scintigraphies au MIBI sont extrê mement rares. Nous exposons le cas d'un homme de 64 ans qui a é té ré animé avec succè s à la suite de deux é pisodes d'asystole, consé cutifs à la perfusion de dipyridamole en vue d'une scintigraphie au MIBI. Le deuxiè me é pisode est survenu au service des urgences, 40 minutes aprè s la mutation du patient du laboratoire d'é preuves d'effort cardiaque. À notre connaissance, il n'existe pas de rapport anté rieur de deux é pisodes distincts d'asystole ou tout au moins d'un é pisode d'asystole survenu aussi tardivement aprè s une scintigraphie au MIBI. Le cas dé crit dé montre trè s bien pourquoi les mé decins d'urgence devraient ê tre conscients du risque d'asystole à la suite d'une scintigraphie au MIBI et pourquoi il faudrait que les services d'urgence susceptibles de recevoir des patients aprè s une é preuve d'effort mé dicamenteuse aient à la porté e de la main de l'aminophylline, l'antidote du dipyridamole. Il ne fait aucun doute que les patients qui subissent un é pisode d'asystole aprè s une perfusion de dipyridamole doivent faire l'objet d'une surveillance cardiaque prolongé e, compte tenu du risque d'é pisodes ulté rieurs d'arrê t cardiaque aprè s des pé riodes de stabilité hé modynamique.Keywords: aminophylline, asystole, dipyridamole, MIBI Dipyridamole/technetium sestamibi scans (more commonly known as MIBI scans, an acronym for methoxyisobutyl isonitrile) are used commonly for the diagnosis and risk stratification of coronary artery disease. Adverse events from MIBI scans are extre...

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Dipyridamole kinetics

Cited by 90 publications

References 0 publications

Dipyridamole: pharmacokinetics and effects on aspects of platelet function in man.

Dipyridamole: pharmacokinetics and effects on aspects of platelet function in man.

Dipyridamole potentiates the in vitro activity of MTA (LY231514) by inhibition of thymidine transport

Surviving a stressful MIBI scan

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