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Presynaptic Adrenergic Release Inhibitor

Aka: Presynaptic Adrenergic Release Inhibitor, Alpha Adrenergic Central Agonist, Central Adrenergic Agonist, Central Alpha 2 Adrenergic Agonist, Peripheral Acting Presynaptic Adrenergic Antagonist, Peripheral Presynaptic Adrenergic Antagonist, Peripheral Presynaptic Alpha Adrenergic Antagonist
  1. See Also
    1. Sympathetic Nervous System
    2. Alpha Adrenergic Receptor
    3. Beta Adrenergic Receptor
    4. Guanabenz (Wytensin)
    5. Guanfacine (Tenex)
    6. Alpha Methyldopa (Aldomet)
    7. Clonidine
    8. Clonidine Withdrawal
    9. Clonidine Overdose
    10. Alpha Adrenergic Antagonist (e.g. Prazosin)
    11. Reserpine (Serpasil)
    12. Guanethidine (Ismelin)
    13. Guanadrel (Hylorel)
  2. Background
    1. Adrenergic ReceptorAgonists increase Blood Pressure
      1. Alpha 1 Adrenergic Receptor binding increases Vasoconstriction
      2. Beta 1 Adrenergic Receptor binding increases myocardial contractility
    2. Presynaptic Adrenergic Release Inhibitors lower Blood Pressure
      1. Central Acting Adrenergic Agonists
        1. Activate alpha-2 receptors that inhibit CNS sympathetic signals
        2. Results in increased parasympathetic effects and side effects
      2. Peripheral Acting Adrenergic Antagonists
        1. Block peripheral Norepinephrine release
  3. Preparations: Central Acting Adrenergic Agonists
    1. Mechanism
      1. See Alpha Adrenergic Receptor
      2. Bind central alpha-2 receptors (vasomotor receptors) to inhibit sympathetic outflow
        1. Decreases Peripheral Vascular Resistance (and Blood Pressure)
        2. Decreases Heart Rate
    2. Non-selective Preparations
      1. Clonidine (Catapres)
      2. Alpha Methyldopa (Aldomet)
      3. Guanabenz (Wytensin)
      4. Guanfacine (Tenex)
    3. Selective Preparations: Alpha-2a (for Opioid Withdrawal symptoms)
      1. Lofexidine
  4. Preparations: Peripheral Acting Adrenergic Antagonists
    1. Mechanism
      1. Peripheral Presynaptic Adrenergic Antagonists block Norepinephrine release from postganglionic nerve terminals
      2. Contrast with Postsynaptic Adrenergic Antagonists that block peripheral alpha receptors
    2. Agents
      1. Reserpine (Serpasil)
      2. Guanethidine (Ismelin)
      3. Guanadrel (Hylorel)

Central alpha-adrenoceptor agonist (C0360167)

Concepts Pharmacologic Substance (T121)
SnomedCT 349933002, 372623002
English Central alpha-adrenocep agon., Central alpha-adrenoceptor agonist, Central alpha-adrenoceptor agonist (product), Central alpha-adrenoceptor agonist (substance)
Spanish agonista central alfa adrenérgico (producto), agonista central alfa adrenérgico (sustancia), agonista central alfa adrenérgico, agonista de adrenorreceptor alfa central (sustancia), agonista de adrenorreceptor alfa central
Sources
Derived from the NIH UMLS (Unified Medical Language System)


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