Effects of calcium channel blockers on gastric emptying and acid secretion of the rat <i>in vivo</i>

R, Brage; Cortijo, Julio; Esplugues, Juan V.; Martí-Bonmatí, E.; Rodríguez, Carlos Larrinaga

doi:10.1111/j.1476-5381.1986.tb11166.x

Cited by 31 publications

(11 citation statements)

References 26 publications

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“…The fact that AUC values of CsA were decreased by diltiazem where as the t l / 2 values were not changed suggests that diltiazem affects the absorption but not the systemic elimination of CsA. Brage et al showed that oral administration of diltiazem caused a delay in the gastric emptying in the rat in vivo (30). Absorption of CsA is also affected by food intake and gastrointestinal motility.…”

Section: Resultsmentioning

confidence: 99%

The interaction of the diltiazem with oral and intravenous cyclosporine in rats

Kalkan

Gümüştekin

Aygoren

et al. 2004

European Journal of Drug Metabolism and Pharmacokinetics

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This study investigated the effect of diltiazem on the bioavailability of oral and intravenous cyclosporine (CsA) in rats. While control rats received normal saline, experimental groups received 60 or 90 mg/kg diltiazem orally for 3 days. Each group divided into 2 equal groups that received a single oral dose or i.v. injection of CsA. Pharmacokinetic parameters were analyzed by nonparametric analysis of variance. Pretreatment with 60 or 90 mg/kg diltiazem decreased the area under the blood CsA concentration-time curve (AUC) of oral CsA compared to control group (54.5% and 65.5% for AUC(0-24), 57.6% and 62.2% for AUC(0-infinity), respectively, p<0.05). Mean CsA maximum concentration (Cmax) decreased from 0.4 +/- 0.1 microg/ml to 0.1 +/- 0.0 microg/mL in rats pretreated with 90 mg/kg diltiazem (p<0.05). The absolute bioavailability after oral administration (F(p.o.)) in the 60 or 90 mg/kg diltiazem groups were lower than the control group (9.6% and 8.5% versus 22.6%). Pretreatment with 90 mg/kg but not 60 mg/kg of diltiazem increased the AUC(0-infinity), elimination half-life (t1/2) of intravenous CsA (116.0%, 219.2%, respectively, p<0.05) and decreased the intravenous CsA clearence (CL(i.v.)) (62.9%, p<0.05). Diltiazem decreased the bioavailability of oral CsA, while it increased the bioavailability of intravenous CsA. One must consider this interaction when administering oral or intravenous CsA concomitantly with diltiazem.

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Section: Resultsmentioning

confidence: 99%

The interaction of the diltiazem with oral and intravenous cyclosporine in rats

Kalkan

Gümüştekin

Aygoren

et al. 2004

European Journal of Drug Metabolism and Pharmacokinetics

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“…Although verapamil has been shown to moderately inhibit gastric acid secretion [Brage et al, 1986;Kirkegaard et al, 1982], this action is unlikely to be responsible for the antiulcer effect exhibited in the reserpine model. If so, verapamil should also inhibit histamine-and compound 48/80-induced gastric damage in which acid has been pro posed to play a certain role [Esplugues et al, 1982].…”

Section: Discussionmentioning

confidence: 99%

“…Verapamil, clinically one of the most widely used calcium channel blockers, has been shown to diminish gastric acid secre tion both in vivo [Brage et al, 1986] and in vitro [Kirkegaard et al, 1982], to decrease gastric motility [Brage et al, 1986] and to inhibit gastric mast cell degranulation [Ogle et al, 1985]. Although similar effects to these have been held responsible for the an tiulcer properties of different drugs, the pos sible influence of verapamil on gastric le sions is poorly understood.…”

Section: Introductionmentioning

confidence: 99%

Differential Effects of Verapamil on Various Gastric Lesions in Rats

Esplugues

R²,

Cortijo³

et al. 1988

Pharmacology

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Verapamil (3, 10, 20 mg/kg^–1) increases the necrotizing effects of oral 25% NaCl or 100% ethanol. Damage by 0.6 N HCl was not equally affected since 1 mg/kg^–1 of verapamil decreased the ulcer index whereas the higher doses augmented it. Pharmacologically induced gastric lesions were also differently affected by verapamil, ulcers produced by histamine being greatly enhanced and those of reserpine inhibited. Neither indomethacin nor compound 48/80 ulcers were modified. These results suggest that verapamil modifies the susceptibility of the gastric mucosa to damage.

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“…This was sug gested to be possibly due to the uncertainty concerning the existence, function, type, or state of voltage-dependent calcium channels in the secretory or contractile elements of the stomach [9]. It was concluded that decreased amine release from the mast cells, stomach wall relaxation and reduced gastric acid were responsible for the ulcer-antagonizing effects of the calcium-entry blocker [4], A previous in vivo study showed that calcium antagonists delayed gastric emptying in the rat [10]. Pre vious studies have shown that antiulcer activ ity of some calcium antagonists may be attrib uted mostly to their inhibitory effect on gas tric motility [11], which was found to be accel erated in stressful conditions.…”

Section: Introductionmentioning

confidence: 99%

Influence of Gallopamil on the Gastric Effects of Stress in Conscious Rats

Coşkun

Ali̇can²,

Gürbüz³

et al. 1996

Pharmacology

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The influence of the calcium-channel blocker gallopamil on cold-restraint stress (CRS)-induced gastric effects was investigated in conscious rats with gastric cannula. CRS, while leading to multiple gastric lesions, reduced gastric acid output and mast cell count, but increased the gastric emptying rate of acid solutions. Intraperitoneally injected gallopamil (1 mg/kg), given 1 h before CRS administration, prevented gastric lesion formation and partially reversed mast cell count and the emptying of acid solutions, but had no further effect on acid output. However, gallopamil in unrestrained rats did not significantly affect acid emptying or mast cell count. Regarding calcium involvement in the pathophysiology of stress-induced gastric lesions, the possible antiulcer actions of gallopamil involved in the prevention of CRS-induced lesion formation may be attributed to its putative stabilizing effect on mast cells and gastric emptying.

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Effects of calcium channel blockers on gastric emptying and acid secretion of the rat in vivo

Cited by 31 publications

References 26 publications

The interaction of the diltiazem with oral and intravenous cyclosporine in rats

The interaction of the diltiazem with oral and intravenous cyclosporine in rats

Differential Effects of Verapamil on Various Gastric Lesions in Rats

Influence of Gallopamil on the Gastric Effects of Stress in Conscious Rats

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