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Closed channel blockers

Chlorisondamine - An Open And Closed Channel Blocker With Complex Blocking Kinetics... [Pg.307]

With mechanisms such as these, it is often possible to simplify the analysis of the action of a channel blocker by assuming that agonist binding is much faster than channel opening and closing and then combining several closed states together so that the mechanism approximates a three-state system ... [Pg.197]

The reaction of ethyl acetoacetate, benzaldehyde, and urea leads to ethyl 1,2,3,4-tetrahydro-6-methyl-2-oxo-4-phenyl-5-pyrimidinecarboxylate. This reaction (the so called Biginelli reaction) was discovered over 100 years ago [93T6937], Interest in these dihydropyrimidines has increased rapidly mainly due to their close structural relationship to the pharmacologically important dihydropyridine calcium channel blockers of the nifedipine-type [93T6937], The dibromo (51) and monobromo derivatives (55) of the most simple Biginelli compounds mentioned above are readily obtained by bromination [93T6937], and the reactions of these derivatives with sodium azide have been studied recently [90LA505] [91 JCS(P1)1342],... [Pg.9]

AMIODARONE CALCIUM CHANNEL BLOCKERS Risk of bradycardia, AV block and 1 BP when amiodarone coadministered with diltiazem or verapamil Additive negative inotropic and chronotropic effect. Also, amiodarone inhibits intestinal P-gp, which t the bioavailability of diltiazem and verapamil Monitor PR, BP and ECG closely watch for heart failure... [Pg.12]

AMIODARONE POTASSIUM-SPARING DIURETICS Risk of T levels of eplerenone with amiodarone risk of hyperkalaemia directly related to serum levels Calcium channel blockers inhibit CYP3A4-mediated metabolism of eplerenone Restrict dose of eplerenone to 25mg/day. Monitor serum potassium concentrations closely watch for hyperkalaemia... [Pg.13]

CALCIUM CHANNEL BLOCKERS ALCOHOL 1. Acute alcohol ingestion may t hypotensive effect. Chronic moderate/heavy drinking 1 hypotensive effect 2. Verapamil may t peak serum concentration and prolong the effects of alcohol 1. Additive hypotensive effect with acute alcohol excess. Chronic alcohol excess is associated with hypertension 2. Uncertain at present, but presumed to be due to an inhibition of hepatic metabolism of alcohol 1. Monitor BP closely as unpredictable responses can occur. Advise patients to drink only in moderation and avoid large variations in the amount of alcohol drunk 2. Warn the patient about the potentiation of the effects of alcohol, particularly the risks of driving... [Pg.78]

CALCIUM CHANNEL BLOCKERS ANAESTHETICS -GENERAL, INHALATIONAL t hypotensive effects of dihydropyridines, and hypotensive/bradycardic effects of diltiazem and verapamil Additive hypotensive and negative inotropic effects. General anaesthetics tend to be myocardial depressants and vasodilators they also 1 sinus automaticity and AV conduction Monitor BP and ECG closely... [Pg.78]

CALCIUM CHANNEL BLOCKERS ANAESTHETICS - LOCAL Case reports of severe 1 BP when bupivacaine epidural was administered to patients on calcium channel blockers Additive hypotensive effect both bupivacaine and calcium channel blockers are cardiodepressant in addition, epidural anaesthesia causes sympathetic block in the lower limbs, which leads to vasodilatation and 1 BP Monitor BP closely. Preload intravenous fluids prior to the epidural... [Pg.78]

CALCIUM CHANNEL BLOCKERS DISOPYRAMIDE Risk of myocardial depression and asystole when disopyramide is co-administered with verapamil, particularly in the presence of heart failure Disopyramide is a myocardial depressant like verapamil and can cause ventricular tachycardia, ventricular fibrillation or torsades de pointes Avoid co-administering verapamil with disopyramide if possible. If single-agent therapy is ineffective, monitor PR, BP and ECG closely watch for heart failure... [Pg.79]

CALCIUM CHANNEL BLOCKERS MACROLIDES t plasma concentrations of felodipine when co-administered with erythromycin cases of adverse effects of verapamil (bradycardia and 1 BP) with both erythromycin and clarithromycin Erythromycin inhibits CYP3A4-mediated metabolism of felodipine and verapamil. Clarithromycin and erythromycin inhibit intestinal P-gp, which may t the bioavailability of verapamil Monitor PR and BP closely watch for bradycardia and 1 BP. Consider reducing the dose of calcium channel blocker during macrolide therapy... [Pg.80]

CALCIUM CHANNEL BLOCKERS RIFAMPICIN Plasma concentrations of calcium channel blockers may be 1 by rifampicin Rifampicin induces CYP3A4-mediated metabolism of calcium channel blockers. It also induces CYP2C9-mediated metabolism of verapamil and induces intestinal P-gp, which may 1 the bioavailability of verapamil Monitor BP closely watch for 1 effect of calcium channel blockers... [Pg.80]

CALCIUM CHANNEL BLOCKERS QUINUPRISTIN/ DALFOPRISTIN Plasma levels of nifedipine may be T by qu in upristi n—dalfopristi n Quinupristin inhibits CYP3A4-mediated metabolism of calcium channel blockers Monitor BP closely watch for 1 BP... [Pg.80]

CALCIUM CHANNEL BLOCKERS EPIRUBICIN Cases of T bone marrow suppression when verapamil is added to epirubicin Uncertain at present Monitor FBC closely... [Pg.81]

CALCIUM CHANNEL BLOCKERS CICLOSPORIN 1. Plasma concentrations of ciclosporin are t when co-administered with diltiazem, nicardipine, verapamil and possibly amlodipine and nisoldipine. However, calcium channel blockers seem to protect renal function 2. Ciclosporin t nifedipine levels 1. Uncertain presumed to be due to impaired hepatic metabolism. Also, diltiazem and verapamil inhibit intestinal P-gp, which may t the bioavailability of ciclosporin. Uncertain mechanism of renal protection 2. Uncertain effect of ciclosporin on nifedipine 1. Monitor ciclosporin levels and i dose accordingly (possibly by up to 25-50% with nicardipine) 2. Monitor BP closely and warn patients to watch for signs of nifedipine toxicity... [Pg.83]

CALCIUM CHANNEL BLOCKERS SIROUMUS Plasma concentrations of sirolimus are t when given with diltiazem. Plasma levels of both drugs are t when verapamil and sirolimus are coadministered Diltiazem and verapamil inhibit intestinal CYP3A4, which is the main site of sirolimus metabolism Watch for side-effects of sirolimus when it is co-administered with diltiazem or verapamil monitor renal and hepatic function. Monitor PR and BP closely when sirolimus is given with verapamil... [Pg.84]

CALCIUM CHANNEL BLOCKERS LITHIUM Small number of cases of neurotoxicity when co-administered with diltiazem or verapamil Uncertain, but thought to be due to an additive effect on neurotransmission Monitor closely for side-effects... [Pg.84]

CALCIUM CHANNEL BLOCKERS CARBAMAZEPINE 1. Diltiazem and verapamil T plasma concentrations of carbamazepine (cases of toxicity) 2.1 plasma concentrations of felodipine, nifedipine and possibly nimodipine and nisoldipine 1. Diltiazem and verapamil inhibit CYP3A4-mediated metabolism of carbamazepine. They also inhibit intestinal P-gp, which may t the bioavailability of carbamazepine 2. Carbamazepine, in turn, induces CYP3A4, which metabolizes calcium channel blockers 1. Monitor carbamazepine levels when initiating calcium channel blockers, particularly diltiazem and verapamil 2. Monitor PR and BP closely watch for T BP when starting carbamazepine in patients already on calcium channel blockers... [Pg.86]

See other pages where Closed channel blockers is mentioned: [Pg.140]    [Pg.215]    [Pg.887]    [Pg.887]    [Pg.140]    [Pg.215]    [Pg.887]    [Pg.887]    [Pg.296]    [Pg.296]    [Pg.406]    [Pg.567]    [Pg.407]    [Pg.475]    [Pg.101]    [Pg.95]    [Pg.354]    [Pg.118]    [Pg.120]    [Pg.250]    [Pg.9]    [Pg.403]    [Pg.234]    [Pg.286]    [Pg.223]    [Pg.198]    [Pg.171]    [Pg.135]    [Pg.122]    [Pg.227]    [Pg.174]    [Pg.296]    [Pg.296]   


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Channel blockers

Channels closed

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