Cardio Pharm - Calcium Channel Blockers, Β-Adrenergic, Α1-Adrenergic

Front 1

What are the types of Calcium Channel Blockers?

Back 1

1,4 - dihyrdopyridines
Phenalkylamines
Benzothiazepines

Front 2

1,4 - dihydropyridines
Included drugs

Back 2

Amiodipine
Nifedipine

Front 3

Calcium Channel Blockers
MOA

Back 3

- Inhibit alpha1 subunit of L-type voltage gated Calcium Channels
- Decrease transmembrane Ca current by reducing the frequency of opening
- Relax arteriolar smooth muscle
- Enhance GFR and natriuresis
- Minimal effect on venous beds (no change in preload)

Front 4

1,4 - Dihydropyridines
MOA

Back 4

Vasoselective - Peripheral vascular effects

Front 5

1, 4 - Dihydropyridines
Adverse Effects

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• Rapid BP↓:
- Avoid short-acting dyhydropyridines
• Reflex tachycardia

Front 6

Calcium Channel Blockers
Long vs Short

Back 6

Avoid short acting as they are related to more cardiovascular complications

Front 7

Phenalkylamines
Included Drugs

Back 7

Verapamil

Front 8

Phenalkylamines
MOA

Back 8

Cardioselective:
• Inhibit SA and AV nodes
→ HR↓

Front 9

Benzothiazepines
Included Drugs

Back 9

- Diltiazim
- Verapamil

Front 10

Dihydropyridines
Vascular Selective

Back 10

Greatest effect on BP
Minimal effect on HR
Reflex tachycardia

Front 11

Phenalkylamines
Cardioselective

Back 11

Weaker BP effect
Inhibit AV & SA node
Blunt reflex tachycardia

Front 12

Calcium Channel Blockers
Pharmacology

Back 12

Highly Absorbed
Reduced bioavailability due to hepatic 1st pass

Front 13

Benzothiazepines
MOA

Back 13

Vasoselective and Cardioselective balance
- Peripheral vascular effects
- Decrease HR

Front 14

β-Adrenergic Blockers
MOA

Back 14

Block β-adrenergic receptors:
→ HR↓, contractility↓
→ CO↓

Block catecholamine binding to β1 receptors on juxtaglomerular cells
↓Renin secretion
→ Angiotensin I, Angiotensin II↓

Front 15

β-Adrenergic Blockers
ADME

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• Absorption: Highly absorbed
• Distribution:
• Metabolism:
• Elimination:
- Hepatic 1st pass (lipid soluble)
→ Reduced bioavailability
- Renal (H20 soluble)

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β-Adrenergic Blockers
Clinical Use

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• Cardiovascular disease:
- Stable heart failure
- Arrhythmia
• Stage 2 hypertension (1 of 2 drugs)
• Migraine
• Essential tremor

Front 17

β-Adrenergic Blockers
Adverse Effects

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Common:
• Metabolic:
- ↑glucose, ↑ triglycerides, ↓HDL
• Attenuated recovery from hypoglycemia
• CNS:
- Depression, nightmares, hallucination

Life-threatening:
• Heart block
• Bronchospasm

Front 18

β-Adrenergic Blockers
Contraindications and Interactions

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Interactions:
↑↑ BP of on medication binding α-receptor to ↑BP
- Unopposed α1-induced vasoconstriction
- Ephidrine, pseudoephidrine, phenylpropanolamine, cocaine

Front 19

β-Adrenergic Blockers
Included Drugs

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- Propanolol
- Atenolol
- Metoprolol
- Nebivolol
- Labetalol

Front 20

β-Adrenergic Blockers
Non-Selective Drugs

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Propanolol

Front 21

β-Adrenergic Blockers
Selective Drugs (β1)

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- Atenolol
- Metoprolol
- Nebivolol

Front 22

β-Adrenergic Blockers
With α-blocking activity

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- Labetalol

Front 23

α1-Adrenergic Blockers
MOA

Back 23

Block α1-receptors, preventing norepinephrine binding
→ BP↓

Front 24

α1-Adrenergic Blockers
Included Drugs

Back 24

Doxazosin