Sympathomimetic Agents

  • Sympathomimetic Agents the actions of endogenous catecholamines.
  • They are broadly classified into three groups based on their mechanism of action:

Classification of Sympathomimetic Agents

  • Sympathomimetic agents are drugs that mimic the actions of the sympathetic (adrenergic) nervous system.
  • They are classified based on their mechanism of action in activating adrenergic receptors.
  • Classification of Sympathomimetic Agents
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1. Direct-Acting Sympathomimetics

  1. Mechanism:

    • These agents directly bind to and stimulate adrenergic receptors (α and/or β), reproducing the effects of endogenous catecholamines.
  2. Key Points:

    • Their action is receptor-mediated.
    • They can have selectivity for α-receptors, β-receptors, or both.
    • Some of these drugs also have central effects.
  3. Examples:

    1. Non-Selective Adrenergic Agonists (α and β receptors):
      • Norepinephrine
      • Epinephrine
      • Dopamine
    2. Selective α-Agonists:
      • Phenylephrine (α₁-selective)
      • Methyldopa (α₂-selective, centrally acting)
      • Clonidine (α₂-selective, centrally acting)
      • Naphazoline (α₁-selective, used as a decongestant)
      • Oxymetazoline (α₁ and partial α₂-selective, used as a decongestant)
      • Xylometazoline (α₁ and partial α₂-selective, used as a decongestant)
    3. Selective β-Agonists:
      • Dobutamine (β₁-selective, used in heart failure)
      • Isoproterenol (non-selective β₁ and β₂ agonist)
      • Terbutaline (β₂-selective, used in asthma & preterm labor)
      • Salbutamol (Albuterol) (β₂-selective, used in asthma)
      • Bitolterol (β₂-selective, used in asthma)

2. Indirect-Acting Sympathomimetics

  1. Mechanism:

    • These drugs do not directly activate adrenergic receptors but instead:
    • Promote the release of endogenous catecholamines (norepinephrine, dopamine, epinephrine).
    • Inhibit the reuptake of catecholamines, thereby enhancing the sympathetic response.
  2. Key Points:

    • Their effect depends on the presence of stored catecholamines.
    • They indirectly increase the stimulation of adrenergic receptors.
  3. Examples:

    • Hydroxyamphetamine (induces norepinephrine release, used in pupil dilation)
    • Pseudoephedrine (induces norepinephrine release, used as a decongestant)
    • Propylhexedrine (causes norepinephrine release, used as a nasal decongestant)
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3. Mixed-Acting Sympathomimetics

  1. Mechanism:

    • These agents have both direct receptor agonist activity and the ability to stimulate the release of endogenous catecholamines.
  2. Key Points:

    • They provide a dual mechanism of action (direct activation + indirect release of catecholamines).
    • This can lead to a broader range of effects compared to purely direct-acting or indirect-acting agents.
  3. Examples:

    • Ephedrine (directly activates α and β receptors & releases norepinephrine)
    • Metaraminol (direct α₁ agonist & causes norepinephrine release, used in hypotension)

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