Pharmacology of Adrenaline and Beta-Blockers
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Questions and Answers

What condition is adrenaline primarily used to treat in severe allergic reactions?

  • Cardiac arrest
  • Hypertension
  • Asthma
  • Anaphylaxis (correct)
  • What physiological effect does adrenaline have on the smooth muscles in the airways?

  • Constricts the muscles
  • Paralyzes the muscles
  • Relaxes the muscles (correct)
  • Inflates the muscles
  • Which of the following conditions contraindicates the use of adrenaline?

  • Asthma
  • Heart failure
  • Hypertension (correct)
  • Anaphylaxis
  • What is one effect of adrenaline on the cardiovascular system?

    <p>Increased heart rate (A)</p> Signup and view all the answers

    What type of beta-blocker blocks both beta 1 and beta 2 receptors?

    <p>Non-selective beta-blocker (C)</p> Signup and view all the answers

    What type of adrenergic receptor is responsible for bronchodilation?

    <p>Beta 2 receptor (B)</p> Signup and view all the answers

    In which condition are beta-blockers NOT typically used as a treatment?

    <p>Diabetes (B)</p> Signup and view all the answers

    Which receptor is associated with the hydrolysis of PIP2?

    <p>Alpha 1 receptor (C)</p> Signup and view all the answers

    What primary effect occurs when adrenaline stimulates alpha 1 receptors in blood vessels?

    <p>Vasoconstriction (D)</p> Signup and view all the answers

    Which of the following is a common side effect of beta blockers?

    <p>Fatigue (A)</p> Signup and view all the answers

    How do beta-blockers primarily affect heart function in patients with heart failure?

    <p>Decrease heart workload (D)</p> Signup and view all the answers

    Why should adrenaline be avoided in patients with heart disease?

    <p>It can worsen heart disease (C)</p> Signup and view all the answers

    Which condition should beta blockers be avoided in?

    <p>Asthma (B)</p> Signup and view all the answers

    Which adrenergic receptor type is coupled to the Gs protein?

    <p>Beta 2 receptor (B)</p> Signup and view all the answers

    How does adrenaline affect the gastrointestinal tract?

    <p>Slows down the digestion process (D)</p> Signup and view all the answers

    What is one major action of adrenaline in the body?

    <p>Increasing heart rate (C)</p> Signup and view all the answers

    Which of the following is TRUE about beta blockers?

    <p>They are effective in managing arrhythmias (C)</p> Signup and view all the answers

    What is a contraindication for using beta blockers?

    <p>Heart block (C)</p> Signup and view all the answers

    What is the result of adrenaline binding to beta 1 receptors?

    <p>Increased heart rate and contractility (D)</p> Signup and view all the answers

    What occurs as a result of adrenaline affecting the urinary bladder?

    <p>Constriction of the bladder sphincter (C)</p> Signup and view all the answers

    What effect do beta blockers have on the heart rate?

    <p>Decrease it (A)</p> Signup and view all the answers

    Which drug class mimics the effects of the sympathetic nervous system?

    <p>Sympathomimetics (C)</p> Signup and view all the answers

    Which condition is NOT treated by beta blockers?

    <p>Asthma (A)</p> Signup and view all the answers

    What is the primary function of the sympathetic nervous system?

    <p>To regulate heart rate and blood pressure during stress (A)</p> Signup and view all the answers

    Which of the following is a side effect of beta blockers?

    <p>Dry cough (C)</p> Signup and view all the answers

    Which of the following is NOT a function of the sympathetic nervous system?

    <p>Decreasing heart rate (A)</p> Signup and view all the answers

    What type of drug mimics the effects of the sympathetic nervous system?

    <p>Sympathomimetic drugs (C)</p> Signup and view all the answers

    Which response is primarily controlled by the parasympathetic nervous system?

    <p>Rest and digest (C)</p> Signup and view all the answers

    How does adrenaline function in the body during stress?

    <p>By stimulating adrenergic receptors (A)</p> Signup and view all the answers

    In comparison to the sympathetic nervous system, what is a key characteristic of the parasympathetic nervous system?

    <p>Conserves energy and promotes relaxation (D)</p> Signup and view all the answers

    What role do adrenergic receptors play in the sympathetic nervous system?

    <p>Receive signals from the sympathetic nervous system (B)</p> Signup and view all the answers

    During a 'fight or flight' situation, which physiological change is most likely to occur?

    <p>Increased oxygen consumption (A)</p> Signup and view all the answers

    Flashcards

    Sympathetic nervous system

    Part of the autonomic nervous system; controls 'fight or flight' response.

    Autonomic nervous system

    Controls involuntary bodily functions like heart rate and digestion.

    'fight or flight' response

    Physiological changes preparing the body for a stressful situation.

    Sympathomimetic drugs

    Drugs mimicking the sympathetic nervous system's effects.

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    Adrenaline

    A well-known sympathomimetic drug released during stress.

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    Parasympathetic nervous system

    Branch of ANS; controls 'rest and digest' response, opposite of sympathetic

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    Adrenergic receptors

    Cells responding to adrenaline and other sympathomimetic drugs.

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    Heart rate regulation

    Both sympathetic and parasympathetic nervous systems affect heart rate.

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    Adrenaline effects

    Adrenaline increases heart rate and blood pressure, relaxes airways, constricts blood vessels, causes sweating, and dilates pupils.

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    Alpha receptors

    Alpha 1 and alpha 2 receptors are responsible for vasoconstriction, pupillary dilation, and contraction of the urinary and pyloric sphincters.

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    Beta receptors

    Beta 1, beta 2, and beta 3 receptors regulate heart rate, bronchodilation, smooth muscle relaxation, glycogenolysis, lipolysis, and thermogenesis.

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    How does alpha 1 work?

    Alpha 1 receptors are coupled to Gq proteins, activating phospholipase C (PLC). PLC breaks down PIP2 into DAG and IP3, which trigger smooth muscle contraction.

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    How does beta 1 work?

    Beta 1 receptors activate Gs proteins, which activate adenylyl cyclase (AC). AC converts ATP to cAMP, leading to increased heart rate and contractility.

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    How does beta 2 work?

    Beta 2 receptors also activate Gs proteins, leading to cAMP production, which relaxes airways and smooth muscles.

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    Adrenaline's heart effect

    Adrenaline binds to beta 1 receptors in the heart, increasing heart rate and force of contraction, leading to increased cardiac output.

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    Adrenaline's blood vessel effect

    Adrenaline causes vasoconstriction by stimulating alpha 1 receptors. However, it can also cause vasodilation in skeletal muscle by stimulating a2 receptors.

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    Alpha 1 receptors in bladder

    These receptors in the bladder wall are stimulated by adrenaline, causing muscle contraction and a feeling of urgency to urinate.

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    Sweat glands and adrenaline

    When adrenaline is released, it activates sweat glands, producing perspiration. This helps cool the body during stress.

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    Hair erection and alpha 1 receptors

    Adrenaline stimulates alpha 1 receptors in hair follicles, causing the hair to stand on end. This is also known as 'piloerection'.

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    Anaphylaxis and adrenaline

    This severe allergic reaction is treated with adrenaline as the first-line response. It reverses the allergic effects quickly, preventing life-threatening consequences.

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    Asthma and adrenaline

    Adrenaline is used to treat acute asthma attacks. It relaxes the muscles in the airways, making it easier to breathe.

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    Cardiac arrest and adrenaline

    Adrenaline helps revive the heart during cardiac arrest by stimulating it to beat again. It's crucial for restoring heart function.

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    Beta blockers: general function

    These drugs block the effects of the sympathetic nervous system by targeting beta receptors in the body.

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    Non-selective vs Selective beta-blockers

    Non-selective beta-blockers block both beta 1 and beta 2 receptors, while selective ones only target beta 1 receptors.

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    Beta Blockers and Bradycardia

    Beta blockers can slow down the heart rate, which can lead to bradycardia (slow heart rate).

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    Beta Blockers and Asthma

    Beta blockers can worsen asthma symptoms, so they are generally contraindicated in people with asthma.

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    Beta Blockers and Heart Block

    Beta blockers can disrupt the electrical signals that control heart rhythm, potentially worsening heart block.

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    Adrenaline and Local Anesthetics

    Adrenaline is added to local anesthetics to prolong their effect, decrease bleeding, reduce systemic toxicity and delay absorption.

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    Adrenaline and Histamine

    Adrenaline acts as a physiological antagonist to histamine, meaning it has opposing effects.

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    Beta Blockers and Hypertension

    Beta blockers are commonly used in the treatment of hypertension (high blood pressure) by slowing down the heart rate and reducing the force of contractions.

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    False: Adrenaline for Hypertension?

    Adrenaline is not used to treat hypertension (high blood pressure) because it can actually increase blood pressure.

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    4 Uses of Adrenaline

    Adrenaline is commonly used for a variety of conditions, including anaphylaxis, asthma, cardiac arrest and as an additive for local anesthetics.

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    Study Notes

    Adrenaline

    • Adrenaline is a sympathomimetic catecholamine
    • It is present in the adrenal medulla (80% of secretions) and some CNS tracts
    • Not absorbed orally

    Adrenaline Kinetics

    • Routes of administration: subcutaneous (1/2 mL of 1/1000 solution), inhalation (1/100 solution by nebulizer or atomizer), eye drops (2% solution), intra-cardiac (in cardiac resuscitation)
    • Subcutaneous administration causes vasoconstriction, which slows absorption
    • Inhalation is used in bronchial asthma
    • Eye drops are used in open-angle glaucoma
    • Intra-cardiac use is for impaired circulation during cardiac resuscitation

    Adrenaline Fate

    • Distribution: does not pass the blood-brain barrier
    • Reuptake: by nerve endings and tissues (80%)
    • Metabolism: by MAO (Monoamine oxidase) and COMT (Catechol-O-methyltransferase) (18%)
    • Excretion: unchanged in urine (2%)

    Adrenaline Actions

    • Systemic actions:
      • Heart: increases heart rate and force of contraction
      • Blood vessels: constriction of skin, mucous membranes, and renal blood vessels, dilation of skeletal and coronary blood vessels.
      • Blood pressure: increase in systolic blood pressure (SBP) due to increased cardiac output (COP) and increased venous return, decrease in diastolic blood pressure (DBP) due to vasodilation of skeletal vessels and reduced peripheral resistance.
      • Respiratory: decongestion of bronchial mucosa, bronchodilation
      • Gastrointestinal Tract: constriction of sphincters and relaxation of intestinal wall.
      • Urinary Bladder: constriction of bladder sphincter, relaxation of bladder wall causing urine retention.
      • Uterus: contraction in early pregnancy, relaxation in late pregnancy
      • Skeletal Muscles: vasodilation, facilitation of neuromuscular transmission, anti-fatigue
      • Metabolic: hyperglycemia
      • Other: anxiety; physiological antagonist of histamine
    • Local actions
      • Skin: localized vasoconstriction via alpha-1 receptors
      • Mucous membranes: (e.g., nasal): vasoconstriction via alpha-1 receptors - decongestion and homeostasis

    Adrenaline Local Uses

    • Open-angle glaucoma
    • Haemostatic nasal pack in epistaxis (not in hypertension patients)
    • With local anaesthetics (except cocaine): slows absorption, increases duration, reduces systemic toxicity and bleeding

    Adrenaline Systemic Uses

    • Anaphylactic shock and urticaria
    • Acute bronchial asthma
    • Acute insulin hypoglycemia
    • Cardiac resuscitation
    • Contracting ring of uterus during labor

    Adrenaline Contraindications

    • Around-the-finger and toe gangrene
    • Hypertension
    • Hemorrhagic shock
    • Thyrotoxicosis
    • Pulmonary embolism
    • Digitalis administration, general anaesthesia causing cardiac arrhythmias
    • Non selective beta blocker

    Beta-Adrenergic Blockers

    • Mechanism: competitive blocking of beta-adrenergic receptors
    • Intrinsic Sympathetic Activity (ISA): partial agonist activity
    • Classification:
      • Non-selective: blocks β1 and β2 receptors, e.g., propranolol, sotalol, timolol, pindolol; Additional a-blocking effect (e.g., labetalol and carvedilol)
      • Selective: blocks primarily β1 receptors, e.g., metoprolol, atenolol, bisoprolol, esmolol

    Beta-Blockers Kinetics

    • Absorption: orally and parenterally
    • Distribution: throughout the body; highly lipophilic drugs like propranolol and timolol cross the BBB.
    • Propranolol: extensive hepatic metabolism; short duration of action, given t.d.s (three times a day)
    • Esmolol: rapid metabolism by RBC esterase; given by IV infusion; suitable for patients with renal or hepatic diseases

    Beta-Blockers Pharmacodynamics

    • Heart: decreases heart rate and force of contraction (by beta1)
    • Blood vessels: vasodilation of skeletal muscles and coronary blood vessels (by beta2), vasoconstriction of skin, mucous membranes, and renal blood vessels (by alpha1)
    • Anti-hypertensive: by decreasing sympathetic outflow and reducing renin secretion
    • IOP: reduced formation of aqueous humor
    • Bronchi: bronchospasm (by beta2 blockade)
    • Metabolism: hypoglycemic effect, masks symptoms of hypoglycemia

    Beta-Blockers Uses

    • Heart: arrhythmias, angina, myocardial infarction (MI), hypertension, heart failure
    • Other: pheochromocytoma, portal hypertension, thyrotoxicosis, glaucoma, migraine headache, anxiety

    Beta-Blockers Side Effects

    • Heart: bradycardia, heart block, angina pain
    • Other: cold extremities, intermittent claudication, acute bronchial asthma

    Beta-Blockers Contraindications

    • Heart: bradycardia (< 60 bpm), heart block, advanced stages of heart failure, vasospastic angina.
    • Other: bronchial asthma, diabetic patients, pregnancy

    MCQs

    • Adrenaline addition to local anaesthetics: delays absorption, prolongs duration, and reduces toxicity
    • Physiological antagonist of adrenaline: acetylcholine
    • Beta-blockers use: hypertension, heart block, angina

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    Description

    This quiz covers the key concepts related to the use of adrenaline and beta-blockers in medical treatments. It explores their physiological effects, contraindications, and the specific receptors involved in their actions. Test your knowledge on these crucial pharmacological agents.

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