Lecture 26: CV effects of Autonomic ANTAGONIST drugs Flashcards
What are the parasympathetic agonists? Antagonists?
Parasympathetic agonists i. Acetylcholine ii. Edrophonium Parasympathetic antagonists i. Atropine ii. Scopolamine
What is the MoA for Atropine?
Competitive antagonist for the muscarinic receptor’s acetylcholine binding site
What is the difference between atropine and scopolamine?
Both are competitive antagonists for muscarinic receptors
However, scopolamine acts on CNS
Atropine cannot act on CNS
What are the circulatory effects of atropine?
Increases heart rate by withdrawal of vagal influence
i. Decreases AV nodal refractoriness
ii. increases SA node conduction
Decreases parasympathetic systemic arteriolar vasodilation (in areas such as the skin and GI tract)
Decreases vasodilation
What are the clinical uses for atropine?
- Prevention of vagal reaction
- Restore AV conduction in conditions with prolonged AV nodal refractoriness such as inferior wall MI and digitalis intoxication
What are the side effects for atropine?
- Dry mouth/skin
- delirium
- Tachycardia
- flushing
What are the sympathetic antagonists?
i. Prazosin
ii. Carvedilol
iii. Atenolol
iv. Metoprolol
v. Propanolol
What are the alpha adrenergic antagonists?
- Prazosin (prazocin)a
- Doxazosin
- Terazosin
What is the MoA of Prazosin?
Alpha 1 receptor antagonist»_space; alpha 2 antagonist
Results in decreased SVR and decreased blood pressure
Inhibition of vasoconstriction
What are the indications for use of Prazosin/Prazocin?
Hypertension (to decrease peripheral vascular resistance by vasodilation)
Urinary bladder obstruction
What are the side effects of Prazocin?
Hypotension
Dizziness
Headache
Fatigue
What are the characteristics of doxazosin and terazosin?
Similar to prazosin but are pure alpha1 blockers and have no alpha2 activity
What are the Beta adrenergic antagnoists?
- Propranolol
- Metoprolol
- Atenolol
- Esmolol
- Carvedilol
What are the classification schemes for beta adrenergic antagonists?
- Beta1 selectivity
- B2 blockers can cause bronchoconsriction
- Intrinsic sympathomimetic activity (ISA)
- B-blockers with ISA are partial agonists that may produce blocked by shielding receptors from more potent agonists
- lipid solubility
- duration of activity
What beta blockers are lipid soluble? Significance?
- Propranolol
- Metoprolol
Readily absorbed by GI tract
Metabolized by liver
Short half life
What beta blockers are water soluble? Significance?
Atenolol
Not as readily absorbed or metabolized
Longer halflifes and metabolized in kidney