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Anti-Anginal Agents. Angina Disease, symptoms Types of Anti-anginal Agents Nitrovasodilators, calcium channel blockers and b -blockers Nitrovasodilators Structure, physical properties, biochemical mechanism of action, metabolism and pharmacokinetics Calcium channel blockers

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slide1

Anti-Anginal Agents

  • Angina

Disease, symptoms

  • Types of Anti-anginal Agents

Nitrovasodilators, calcium channel blockers and b-blockers

  • Nitrovasodilators

Structure, physical properties, biochemical mechanism of action, metabolism and pharmacokinetics

  • Calcium channel blockers

Types, structure, physical properties, biochemical mechanism of action

  • Adverse Effects/Reactions

MEDC 604 Anti-anginals

slide2

QRS Complex

PR Segment

ST Segment

PR Interval

QT Interval

Angina Pectoris

  • Development of Angina
  • Angina is a Symptom, not a disease
  • Types of Angina
  • Stable Angina (typical, atherosclerotic; exertional)
  • Unstable Angina (pre-infarction; at rest)
  • Variant Angina (transient vasospasmatic)

MEDC 604 Anti-anginals

slide3

Nitrovasodilators

MEDC 604 Anti-anginals

slide4

Structure

Nitrate Esters

  • Some nitrate esters are wrongly named, e.g., amylnitrite is actually isoamylnitrite, nitroglycerin is not a nitro compound
  • Nitrate esters are susceptible to hydrolysis! Shelf life is a concern.

MEDC 604 Anti-anginals

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Onset

(min)

Duration of Action (min)

Metabolites

Amyl nitrite

0.25

1

Nitroglycerin

2

30

3

60

Active

Isosorbide dinitrate

Erythrityl tetranitrate

15

180

Pentaerythritol tetranitrate

20

330

Pharmacokinetics of Nitrate Esters

  • Nitrate esters act fast! Think about the size of these molecules.
  • They are rapidly metabolized in the liver (glutathione-nitrate reductase). Yet, can be used in oral prophylactic therapy, especially ISDN, ETN and PETN
  • Number of nitrate groups does not linearly correspond to potency
  • Nitrate esters and possibility of explosion!
  • Nitrovasodilators decrease the blood pressure of patients!!

MEDC 604 Anti-anginals

slide6

Nitrate Ester NO Guanylate Cyclase

Biochemical Mechanism of Action

MEDC 604 Anti-anginals

slide7

Mechanism of Action of __________!!

  • Another less-known use of this drug is in the treatment of pulmonary arterial hypertension!!

MEDC 604 Anti-anginals

slide8

Nitrate Ester NO Guanylate Cyclase

Biochemical Mechanism of Action

MEDC 604 Anti-anginals

slide9

Extensive hydroxylation to inactive species

Calcium channel blockers

  • Types of Calcium Channel Blockers
  • Dihydropyridines  Nifedipine and others
  • Phenylalkylamines  Verapamil and Bepridil
  • Benzothiazipines  Diltiazem

MEDC 604 Anti-anginals

slide10

NOR: ~20% Active

O-deMe

gives inactive

species

Des-Ac

gives

~50%

Structure of Ca+2 channel blockers

MEDC 604 Anti-anginals

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Protein Binding

Duration of Action

Metabolites

Amlodipine

>95%

24 h

phenyl hydroxylations, inactive

Nicardipine

95%

3 h

phenyl hydroxylations, 1 active <1%

Diltiazem

~80%

6 h iv

desacetyl derivative, ~ 50 % active

Bepridil

Extensive inactive metabolites

>90%

24 h

Verapamil

90%

8 h

N-demethyl derivative, ~ 20 % active

Protein Binding of Calcium Channels Blockers

MEDC 604 Anti-anginals

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Adverse Effects of Calcium Channel Blockers

  • Development of Arryhthmia …Bepridil induces new arrhythmias
  • Hypotension … vasodilation’s side-effect; especially with nitrovasodilators
  • Rebound angina … sudden stoppage of drug induces flow of Ca2+ into cells causing coronary arteries to spasm
  • Metabolism by liver … use with caution in patients with hepatic dysfunction
  • Mild to moderate edema … due to vasodilation

MEDC 604 Anti-anginals