Pharmacology of Adrenergic Agents
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Questions and Answers

What are the different types of adrenergic agents mentioned in the content?

Adrenopositive agents and Adrenonegative agents

Which adrenergic receptor does Epinephrine primarily act on?

  • α2 adrenoreceptor
  • α1 adrenoreceptor
  • β adrenoreceptor (correct)
  • β2 adrenoreceptor
  • Norepinephrine, Epinephrine, and Isoprenaline are examples of __________.

    Catecholamines

    Epinephrine causes bronchodilation.

    <p>False</p> Signup and view all the answers

    What effect does Isoprenaline have on Mean Blood Pressure (MBP)?

    <p>reduces</p> Signup and view all the answers

    What effect does Epinephrine have on Systolic Blood Pressure (SBP) in a dose-dependent manner?

    <p>Increases</p> Signup and view all the answers

    Phenylephrine causes vasoconstriction in nasal mucosa as a ____________ action vasoconstrictor.

    <p>local</p> Signup and view all the answers

    Selective alpha 2 adrenoreceptor agonists can have a very fast-acting hypotensive effect.

    <p>True</p> Signup and view all the answers

    Match the following clinical uses with the respective drug:

    1. Acute rhinitis, nose bleeding, paroxysmal ventricular tachycardia
    2. Coronary artery disease, tachycardia, thyrotoxicosis
    3. Glaucoma

    <p>Phenylephrine = 1 Propranolol = 2 Timolol = 3</p> Signup and view all the answers

    What is the clinical use of carvedilol?

    <p>Chronic heart failure, CAD, hypertension</p> Signup and view all the answers

    What is the mechanism of toxicity of beta blockers?

    <p>All of the above</p> Signup and view all the answers

    Central nervous system toxicity, including convulsions and coma, is commonly seen with beta blockers.

    <p>True</p> Signup and view all the answers

    Beta blockers may cause ____, hypotension, and bradycardia as cardiac disturbances in poisoning.

    <p>first degree heart block</p> Signup and view all the answers

    Match the following toxicology treatment with their associated actions:

    <p>Atropine = May be ineffective for beta blocker-associated bradycardia Glucagon IV = Administered for bradycardia resistant to basic supportive measures Vasopressors = Often needed to manage shock from beta blocker overdose</p> Signup and view all the answers

    Study Notes

    Adrenopositive Agents

    • Adrenopositive agents are also known as adrenomimetic or sympathomimetic agents
    • Examples include Epinephrine, Isoprenaline, Norepinephrine, and Clonidine
    • These agents stimulate adrenergic receptors, leading to various physiological effects

    Alpha 1 Adrenergic Receptors

    • Found in smooth muscle, especially in blood vessels, eyes, and urinary bladder
    • Stimulation leads to:
      • Contraction of smooth muscle in blood vessels, eyes, and urinary bladder
      • Vasoconstriction, increasing diastolic blood pressure and heart preload
      • Mydriasis, increasing intraocular pressure

    Alpha 2 Adrenergic Receptors

    • Found in pancreatic beta cells, nerve endings, and eyes
    • Stimulation leads to:
      • Decreased insulin secretion from pancreatic beta cells
      • Decreased norepinephrine release from nerve endings
      • Decreased intraocular fluid secretion from eyes

    Beta 1 Adrenergic Receptors

    • Found in heart, kidneys, and adipose tissue
    • Stimulation leads to:
      • Increased heart rate and contractility
      • Increased conduction velocity in the heart
      • Increased renin release from kidneys
      • Lipolysis in adipose tissue

    Beta 2 Adrenergic Receptors

    • Found in smooth muscle, especially in lungs, blood vessels, and uterus
    • Stimulation leads to:
      • Relaxation of smooth muscle in lungs, blood vessels, and uterus
      • Bronchodilation, decreasing airway resistance
      • Vasodilation, decreasing diastolic blood pressure and heart preload
      • Tocolytic effect, inhibiting uterine contractions

    Adrenonegative Agents

    • Adrenonegative agents are also known as adrenergic blockers or sympatholytics
    • Examples include Propranolol, Doxazosin, and Clonidine
    • These agents block adrenergic receptors, leading to various physiological effects

    Alpha 1 Adrenoreceptor Antagonists

    • Examples include Doxazosin and Prazosin
    • Clinical use: treatment of hypertension and symptoms of benign prostatic hyperplasia

    Beta Adrenoreceptor Antagonists (BAB)

    • Examples include Propranolol and Metoprolol

    • Clinical use: treatment of hypertension, angina pectoris, cardiac arrhythmias, and thyrotoxicosis

    • Side effects: bradycardia, decreased exercise tolerance, and rebound effect upon sudden withdrawal### Beta Adrenoreceptor Antagonists

    • Nonselective beta blockers (BAB) may mask initial symptoms of insulin overdose, including tachycardia, tremor, and anxiety.

    • Cardioselective BAB are safer for patients with diabetes mellitus (DM).

    Side Effects and Interactions

    • Side effects of BAB include bradycardia, AV block, risk of bronchial obstruction, sexual dysfunction, and Raynaud syndrome.
    • Interactions: Non-selective action may affect the effects of adrenopositive agents.

    Nonselective Beta Adrenoreceptor Antagonists

    • Examples: Timolol eye drops, which reduce intraocular fluid secretion in the ciliary body and decrease intraocular pressure.
    • Clinical use: Glaucoma.
    • Target structures in the eye: three muscles (pupil dilator, pupil constrictor muscle, ciliary muscle) and ciliary body epithelium.

    Selective Beta 1 Adrenoreceptor Antagonists

    • Examples: Metoprolol, Bisoprolol, which are highly selective β1 adrenoblockers.
    • Clinical use: Coronary artery disease (CAD), hypertension, atrial fibrillation, chronic heart failure (CHF), and prophylaxis of migraine attacks.
    • Lipophilic BAB cause vasoconstriction.
    • Cardioslectivity β1: less impact on β/vascular smooth muscle, bronchi, uterus, and electrolyte balance (lower risk of hyperkalemia).

    Selective Alpha 1, Nonselective Beta Adrenoreceptor Antagonists

    • Examples: Carvedilol, which has cardiodepressant and antioxidant properties, and reduces peripheral vascular resistance.
    • Clinical use: Chronic heart failure, CAD, and hypertension.
    • BAB effect on renin is not clinically important, as it will compensate.

    Raynaud Syndrome

    • Characterized by episodic stenosis of limb arteries and arterioles, usually provoked by cold or stress.
    • Manifested as sudden paleness or cyanosis of the fingers and toes, including the earlobe and nose.
    • β2 blockage causes peripheral vasoconstriction, leading to limb freezing.

    Beta Adrenoreceptor Antagonist Toxicology

    • Mechanism of toxicity: All beta blockers antagonize beta1 adrenoreceptors, decreasing heart rate and cardiac contractility.
    • Nonselective beta blockers also antagonize beta2 receptors, leading to bronchoconstriction, hypoglycemia, and hyperkalemia.

    Clinical Presentation

    • Cardiac disturbances: first-degree heart block, hypotension, and bradycardia.
    • Central nervous system toxicity: convulsions, coma, and respiratory arrest.
    • Bronchospasm: most common in patients with preexisting asthma or chronic bronchospastic disease.
    • Hypoglycemia and hyperkalemia may occur.

    Treatment

    • Emergency and supportive measures: maintain an open airway, assist ventilation, and treat coma, seizures, hypotension, hyperkalemia, and hypoglycemia.
    • Specific drugs and antidotes: glucagon, calcium chloride, high-dose insulin euglycemic therapy, sodium bicarbonate, and vasopressors.

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