Sympatholytics Flashcards
Types of cholinergic receptors and sites of action
1) Nicotinic: ganglia and skeletal muscle
2) Muscarinic: glands (lacrimal, salivary, gastric), smooth muscle (bronchial, GI, bladder, and vessels), and heart (SA and AV node)
All preganglionic neurons release what neurotransmitters? Is it excitatory or inhibitory?
Acetylcholine. Excitatory.
What is the rate-limiting step in the synthesis of epi and norepi in the adrenal medulla?
tyrosine hydoxylase
Ratio of Epi/norepi synthesis in the adrenal medulla
80/20
What neurotransmitter precedes the synthesis of norepinephrine?
dopamine
Metabolism of norepi and epi
Metabolic degradation by MOA and COMT. However, 80% is reuptake.
Beta-1 selective antagonists
atenolol, esmolol, and metoprolol
Beta-blockers with alpha effects
labetalol and carvedilol
Phentolamine MOA and SE
nonselective reversible IV alpha-blocker. Produces vasodilation. Produces baroceptor-mediated increases in CO and HR. May cause dysrhythmias and angina, as well as hyperperistalsis, abdominal pain, and diarrhea due to the predominance of parasympathetic activity.
Clinical uses for phentolamine
Intraop management of pheochromocytoma, autonomic dysreflexia (SCI), and extravasation of IV sympathomimetic.
Phenoxybenzamine MOA and SE
nonselective IRREVERSIBLE alpha-blocker. Profound hypotension in the presence of hypovolemia, blood loss, vasodilators, and inhalation agents. Noncardiac effects include miosis, nasal stuffiness, and sedation.
Phenoxybenzamine clinical uses
Preoperative management of pheochromocytoma, inoperable adrenal tumors, Raynaud’s diseases (more effective in cutaneous vasoconstriction rather than skeletal muscle flow)
Preoperative management of pheochromocytoma with phenoxybenzamine
0.5-1 mg/kg PO beginning two weeks prior to surgery. Make sure intravascular volume is adequate. Prazosin as an alternative.
Yohimbine MOA
Selective presynaptic alpha-2 antagonist. Enhances the release of norepinephrine.
Yohimbine clinical uses
idiopathic orthostatic hypotension, former treatment for impotence.
Prazosin MOA
selective post-synaptic alpha-1 antagonist. Dilates both arterioles and veins. Reflex tachycardia less common because drug has no inhibitory effect on alpha-2 receptors.