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17 Cards in this Set
- Front
- Back
Central Sympatholytics: MOA
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-Central mediated inhibition of sympathetic activity
-Stimulation of postsynaptic A2 receptors (A2a subtype) -Possible role of imidazoline receptors (I1, I2, I3 receptors) -Endogenous substrate (clonidine displacing substrate) |
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Central Sympatholytics: Probable Sites of Action in Brain
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-Nucleus of solitary tract (NTS)
-Ventral lateral medulla (VLM) -Activation of these sites: decreases sympathetic nerve activity |
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Central Sympatholytics: General Hemodynamic Effects
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-Decreased TPR
-Decreased HR -Decreased CO -Slight increase in sodium retention -Slight decrease in renin release |
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Central Sympatholytics: Advantages
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-Decreased TPR w/modest decrease in CO
-Efficacy independent of age, race, gender -Suitable for monotherapy -Works well in elderly -No negative effects on lipids |
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Central Sympatholytics: General Side Effects
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-Drowsiness/sedation (CNS)
-Dry mouth (CNS) -Sexual dysfunction -Narrow therapeutic range -Abrupt withdrawal hypertension |
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Alpha-Methyldopa
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-Potent A2 agonist
-Metabolized to a-methylnorepinephrine -Taken up by reuptake pump, converted by normal enzymes in NE synthesis |
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Alpha-Methyldopa: Side Effects
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-Sodium, fluid retention
-Positive Combs test in 20%, only 5% have true autoimmune response -Hepatotoxicity (2%) -Fever -Allergic skin reactions -Hemolytic anemia -Can be used during pregnancy -2nd to 3rd line therapy |
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Clonidine
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-A2 agonist, Imidazoline agonist
-Acute pressor response -Lipid sol of analogues predicts potency -Decrease SNS activity, increase PNS activity -Increase blood glucose (inhibits insulin secretion) -Decrease ADH secretion -Causes Na+ retention (often given w/diuretic) -Dry mouth (central effect) -Analgesic activity - blunts opiate withdrawal reactions |
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Clonidine: Additional Side Effects
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-Withdrawal reactions (may be severe)
-Orthostatic hypotension -Impotence -Bradycardia |
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Clonidine Analogues: Apraclonidine
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-Apraclonidine:
-selective A2 agonist -doesn't cross BBB -decreases A2 mediated aqueous humor production -short-term after laser surgery -can be used w/other agents when pressure not well controlled |
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Clonidine Analogues: Brimonidine
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-decreases A2-mediated aqueous humor production
-increases aqueous humor outflow -crosses BBB, hypotension, sedation |
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Guanabenz
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-Less Na+/water retention
-More selectve for A2 receptors than Clonidine -Sedation -Dry mouth |
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Guanfacine
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-Less potent than Clonidine
-Most selective (A2>>A1) -Less sedation -Occasional withdrawal syndrome |
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Rilmenidine
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-I1 receptor agonist (RVLM, NTS)
-Antihypertensive actions -Few classical A2-adrenergic effects: -Less dry mouth -Minor sedation -Little Na+/water retention -No withdrawal syndrome -No orthostatic hypotension *Available in Europe only |
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Reserpine
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-Blocks transport into vesicles, new synthesis of vesicles
-Depletes NE stores -Decrease CO, TPR, HR, Renin -Effective in elderly w/diuretic -Both central and peripheral effects |
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Reserpine: Side Effects
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-Sedation, drowsiness, fatigue
-Dysrhythmias -Depression and suicide: -Gradual onset, withdraw drug |
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Guanadrel
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-Guanethidine analog
-Slow displacement of vesicles: -Orhostatic hypotension, CHF -Weakness, fatigue, confusion, depression -Sexual problems -Withdrawal syndrome |