Podcast
Questions and Answers
Which subunit of the voltage-gated calcium channel do Calcium Antagonists bind to?
Which subunit of the voltage-gated calcium channel do Calcium Antagonists bind to?
What is the mechanism of action of Calcium Antagonists in preventing the diffusion of Ca2+ through the pore in an open channel?
What is the mechanism of action of Calcium Antagonists in preventing the diffusion of Ca2+ through the pore in an open channel?
Which type of Calcium Channel Blocker is preferentially acting on the heart?
Which type of Calcium Channel Blocker is preferentially acting on the heart?
What is one example of a Benzothiazepine Calcium Channel Blocker?
What is one example of a Benzothiazepine Calcium Channel Blocker?
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In which type of angina would reducing coronary artery spasm be beneficial?
In which type of angina would reducing coronary artery spasm be beneficial?
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What is the main pharmacological effect in smooth muscles caused by Calcium Channel Blockers?
What is the main pharmacological effect in smooth muscles caused by Calcium Channel Blockers?
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What is the primary reason for the contraindication of Calcium Channel Blockers (CCB) in heart failure?
What is the primary reason for the contraindication of Calcium Channel Blockers (CCB) in heart failure?
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What is the mechanism behind the reflex increase in sympathetic activity caused by Calcium Channel Blockers (CCB)?
What is the mechanism behind the reflex increase in sympathetic activity caused by Calcium Channel Blockers (CCB)?
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Which of the following is an adverse drug reaction associated with Calcium Channel Blockers?
Which of the following is an adverse drug reaction associated with Calcium Channel Blockers?
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How does grapefruit interact with Calcium Channel Blockers?
How does grapefruit interact with Calcium Channel Blockers?
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Which of the following statements is true regarding the clinical use of Dihydropyridine Calcium Channel Blockers?
Which of the following statements is true regarding the clinical use of Dihydropyridine Calcium Channel Blockers?
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What is a characteristic of Calcium Antagonists' pharmacokinetics?
What is a characteristic of Calcium Antagonists' pharmacokinetics?
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What is a contraindication for all calcium channel blockers in the presence of overt heart failure?
What is a contraindication for all calcium channel blockers in the presence of overt heart failure?
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What adverse drug reaction is most frequently associated with nifedipine among the calcium channel blockers?
What adverse drug reaction is most frequently associated with nifedipine among the calcium channel blockers?
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Which calcium antagonist does not increase mortality in patients with heart failure due to nonischemic left ventricular systolic dysfunction?
Which calcium antagonist does not increase mortality in patients with heart failure due to nonischemic left ventricular systolic dysfunction?
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What type of interaction occurs between calcium channel blockers and grapefruit?
What type of interaction occurs between calcium channel blockers and grapefruit?
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Which clinical condition is not a common use for calcium channel blockers?
Which clinical condition is not a common use for calcium channel blockers?
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Which calcium antagonist has a long half-life and is typically dosed once daily?
Which calcium antagonist has a long half-life and is typically dosed once daily?
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Study Notes
Calcium Antagonists Overview
- Bind primarily to the alpha-1 subunit of voltage-gated calcium channels.
- Mechanism of action involves blocking the Ca2+ influx by preventing channel opening, thereby inhibiting calcium entry during depolarization.
Types and Examples
- Dihydropyridine calcium channel blockers preferentially affect vascular smooth muscle, reducing blood pressure.
- An example of a Benzothiazepine calcium channel blocker is diltiazem.
Clinical Applications
- Reducing coronary artery spasm is beneficial in Prinzmetal's angina.
- Calcium channel blockers primarily cause vasodilation in smooth muscles, decreasing overall vascular resistance.
Contraindications and Considerations
- Contraindicated in patients with heart failure due to potential for worsening symptoms and increasing preload.
- Reflex sympathetic activity is stimulated due to decreased blood pressure, as the body compensates with increased heart rate and contractility.
Adverse Effects and Interactions
- Common adverse drug reactions include peripheral edema, flush, and hypotension; especially noted with nifedipine.
- Grapefruit juice can significantly increase plasma concentrations of calcium channel blockers, enhancing effects and side effects.
Clinical Use and Pharmacokinetics
- Dihydropyridine calcium channel blockers are primarily used for hypertension and angina.
- Calcium antagonists exhibit varied pharmacokinetics; for instance, amlodipine has a long half-life, allowing for once-daily dosing.
- All calcium channel blockers are contraindicated in overt heart failure cases to avoid exacerbation.
Notable Conditions and Interactions
- Calcium channel blockers are not typically used for heart failure management.
- No calcium antagonist has been shown to increase mortality in patients with nonischemic left ventricular systolic dysfunction.
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Description
Test your knowledge on Calcium Channel Blockers including the classes, mechanisms of action, and pharmacological effects of calcium antagonists such as phenylalkylamines, dihydropyridines, and benzothizepines.