Pharmacology Chapter on Sympathomimetics
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Questions and Answers

Why should patients taking MAOIs avoid foods high in tyramine?

  • Tyramine blocks the reuptake of catecholamines which leads to reduced sympathetic stimulation.
  • Tyramine's effect is potentiated by MAOIs, causing a rapid decrease in blood pressure.
  • Tyramine directly stimulates adrenergic receptors, leading to hypotension.
  • MAOIs prevent the breakdown of tyramine, leading to a buildup and significant blood pressure increase. (correct)
  • How does cocaine induce its sympathomimetic effects?

  • By increasing the breakdown rate of norepinephrine and dopamine.
  • By directly activating adrenergic receptors in the central nervous system.
  • By blocking the reuptake of norepinephrine and dopamine. (correct)
  • By promoting the reuptake of norepinephrine and dopamine.
  • What is the primary mechanism through which tyramine exerts its effects?

  • It inhibits the release of catecholamines.
  • It antagonizes the actions of norepinephrine.
  • It causes the release of stored catecholamines. (correct)
  • It directly activates postsynaptic adrenergic receptors.
  • Why would orally administered tyramine not have a pronounced sympathomimetic effect in a patient with a normally functioning liver?

    <p>It is rapidly metabolized by monoamine oxidase (MAO) during the first pass metabolism. (C)</p> Signup and view all the answers

    Which of these statements best describes the difference between the effects of cocaine and amphetamine on the central nervous system?

    <p>Cocaine produces a more intense effect than amphetamine, with a shorter duration. (D)</p> Signup and view all the answers

    Which term describes a drug that mimics the effects of the sympathetic nervous system?

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

    What is the primary action of a decongestant?

    <p>Constricting blood vessels in the submucosal tissue (B)</p> Signup and view all the answers

    A drug that causes pupil dilation is classified as which of the following?

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

    Which of the following best describes an indirect agonist?

    <p>Activates the receptor by binding to another molecule and increasing neurotransmitter concentration (indirectly) (D)</p> Signup and view all the answers

    What does the term 'catecholaminergic' refer to?

    <p>Effects related to norepinephrine, epinephrine, or dopamine (C)</p> Signup and view all the answers

    What is the primary mechanism of action of a reuptake inhibitor?

    <p>Inhibiting the reuptake of a neurotransmitter, increasing its synaptic concentration (A)</p> Signup and view all the answers

    What distinguishes a 'selective' alpha or beta adrenergic agonist from a non-selective one?

    <p>It has relatively greater effects on either alpha or beta adrenergic receptors (C)</p> Signup and view all the answers

    A drug that increases the activity of a neurotransmitter in the synapse by blocking its reuptake is acting as a what?

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

    Which of the following best describes the primary mechanism of action of beta-blocking agents in treating glaucoma?

    <p>Decreasing aqueous humor production. (D)</p> Signup and view all the answers

    Which medication is NOT typically used as a tocolytic agent to suppress premature labor?

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

    Which of the following is the most appropriate treatment for priapism?

    <p>Injection of phenylephrine into the penis. (A)</p> Signup and view all the answers

    What primary neurotransmitter systems are modulated by stimulant medications used to treat ADHD?

    <p>Dopamine and norepinephrine. (C)</p> Signup and view all the answers

    Clonidine is used to reduce addiction craving for which of the following substances?

    <p>Narcotics, ethanol, and nicotine. (A)</p> Signup and view all the answers

    Which of the following best describes the mechanism of action of an indirect sympathomimetic drug?

    <p>Displacing stored catecholamines from adrenergic nerve endings. (A)</p> Signup and view all the answers

    What is the primary cardiovascular effect of a pure alpha-1 agonist such as phenylephrine?

    <p>Increased arterial resistance and decreased heart rate (C)</p> Signup and view all the answers

    Which of the following is NOT a typical effect of beta-1 receptor activation in the heart?

    <p>Decreased conduction velocity at the AV node (C)</p> Signup and view all the answers

    Which receptor subtype primarily mediates vasodilation in the renal, splanchnic, coronary and cerebral vascular beds?

    <p>Dopamine (D1) receptors (C)</p> Signup and view all the answers

    Which of the following actions is characteristic of a mixed-acting sympathomimetic drug, like amphetamine?

    <p>Exhibits both direct and indirect adrenergic activities (B)</p> Signup and view all the answers

    According to the content, which vascular bed is primarily impacted by alpha receptor activation?

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

    Which of the following is true regarding an isoproterenol?

    <p>It primarily increases cardiac output due to beta-1 activation. (A)</p> Signup and view all the answers

    Smooth muscle relaxation in which of these locations occurs due to beta-2 receptor activation?

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

    What effect does increased calcium influx in cardiac cells typically have?

    <p>Positive chronotropic effect (D)</p> Signup and view all the answers

    What is the effect on vascular smooth muscle tone of dopamine activation at the D1 receptor?

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

    Which of the following is a primary effect of ergotamine?

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

    What is a primary therapeutic use of atomoxetine?

    <p>Management of attention deficit disorders (ADHD) (D)</p> Signup and view all the answers

    Which medication is specifically identified as a selective serotonin and norepinephrine reuptake inhibitor?

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

    What is the primary reason direct-acting alpha agonists like norepinephrine or phenylephrine are considered in cases of acute hypotension?

    <p>To achieve vasoconstriction (B)</p> Signup and view all the answers

    Under what circumstances might the administration of vasoconstrictive drugs in shock be potentially harmful?

    <p>When it increases cardiac oxygen demand (C)</p> Signup and view all the answers

    What class of drugs is commonly used as positive inotropic agents in cases of cardiogenic shock?

    <p>Beta-1 agonists (C)</p> Signup and view all the answers

    Which drug is identified as the primary treatment for anaphylactic reactions?

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

    What is the primary mechanism through which epinephrine and dipivefrin lower intraocular pressure in the treatment of glaucoma?

    <p>Increasing the outflow of aqueous humor (D)</p> Signup and view all the answers

    Which medication is now often used to replace ephedrine in the treatment of chronic orthostatic hypotension?

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

    What is the primary goal when using positive inotropic agents in cardiogenic shock?

    <p>Optimizing tissue perfusion (D)</p> Signup and view all the answers

    What is the primary characteristic of asthma's pathophysiology?

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

    Which medication is classified as a selective norepinephrine reuptake inhibitor?

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

    What is the 3rd leading cause of death in the US?

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

    Which therapeutic approach is used as a long-term controller for asthma?

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

    What is a common clinical symptom of asthma?

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

    What kind of medication provides symptomatic relief but does not address underlying inflammation in asthma?

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

    Which option is true about the use of long-acting β2-adrenoceptor agonists?

    <p>They improve lung function. (A)</p> Signup and view all the answers

    Which of the following agents is not considered selective for β2 receptors?

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

    Flashcards

    Direct Agonist

    A drug that directly binds to and activates a receptor, initiating a response.

    Mydriatic

    A drug that causes dilation of the pupil, making it larger.

    Reuptake Inhibitor

    A drug that increases the activity of a neurotransmitter by inhibiting its reuptake into the nerve terminal.

    Decongestant

    A drug that causes constriction of blood vessels, particularly in the nasal or oropharyngeal mucosa.

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    Sympathomimetic

    A drug that mimics the effects of the sympathetic nervous system, often by affecting adrenergic receptors.

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    Selective Alpha or Beta Adrenergic Agonist

    A drug that has relatively greater effects on either alpha or beta adrenergic receptors, although not absolutely specific.

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    Catecholaminergic

    Relating to or influenced by norepinephrine, epinephrine, or dopamine.

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    Indirect Agonist

    A drug that brings about receptor activation indirectly, by affecting another molecule that regulates the neurotransmitter.

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    Direct sympathomimetics

    Sympathomimetic drugs that act directly on adrenergic receptors, causing activation by binding directly to the receptor.

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    Indirect sympathomimetics

    Sympathomimetic drugs that indirectly increase the release of catecholamines from nerve endings, indirectly activating adrenergic receptors.

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    Mixed sympathomimetics

    Sympathomimetic drugs that possess both direct and indirect modes of action, they can bind to receptors directly and also increase the release of neurotransmitters.

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    Receptor affinity

    The ability of a drug to bind to a specific receptor.

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    Intrinsic activity

    The ability of a drug to activate a receptor once it is bound.

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    Cardiovascular effects of sympathomimetics

    The effects of a sympathomimetic drug on the cardiovascular system are complex and may differ depending on which adrenergic receptor is dominant in the tissue and the specificity of the drug.

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    Alpha-1 receptors in blood vessels

    The alpha-1 adrenergic receptors in blood vessels, primarily found in skin vessels, splanchnic vessels, and some skeletal muscle vessels, cause vasoconstriction when activated.

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    Beta-2 receptors in blood vessels

    The beta-2 adrenergic receptors in blood vessels, primarily found in some skeletal muscle vessels, cause vasodilation when activated.

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    Beta-1 receptors in the heart

    The beta-1 adrenergic receptors in the heart cause increased heart rate (positive chronotropic effect), increased conduction velocity through the AV node, decreased refractory period, and increased contractility (positive inotropic effect) when activated.

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    Dopamine receptors in blood vessels

    The dopamine receptors in renal, splanchnic, coronary, and cerebral blood vessels cause vasodilation when activated.

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    Tyramine

    A naturally occurring substance found in fermented food such as cheese and wine, and metabolized by the liver enzyme monoamine oxidase (MAO).

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    Adrenergic Agonist

    A category of medications that stimulate the sympathetic nervous system, potentially leading to increased heart rate, blood pressure, and alertness.

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    Monoamine Oxidase Inhibitors (MAOIs)

    A class of drugs that inhibit the breakdown of neurotransmitters like norepinephrine and dopamine, leading to increased levels of these neurotransmitters in the brain.

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    Cocaine

    A type of drug that acts as a local anesthetic by blocking sodium channels, and also has sympathomimetic effects by inhibiting the reuptake of norepinephrine and dopamine. It is known for its addictive properties due to its action on the brain's reward system.

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    How do alpha-2 agonists help with glaucoma?

    Alpha-2 adrenergic agonists, like apraclonidine and brimonidine, work by increasing the outflow of aqueous humor from the eye, reducing intraocular pressure. They are used in the treatment of glaucoma.

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    How do beta blockers work in glaucoma?

    Beta blockers, such as timolol, betaxolol, and carteolol, reduce the production of aqueous humor in the eye, contributing to decreased intraocular pressure. They are widely used for glaucoma management.

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    What do beta-2 agonists do in pregnancy?

    Beta-2 selective agents, like ritodrine and terbutaline, are used to relax the uterus to suppress preterm labor. They work by stimulating beta-2 receptors, leading to uterine muscle relaxation.

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    How do amphetamines help with ADHD?

    Amphetamines and amphetamine-like drugs have a stimulant effect on the nervous system, improving concentration and attention in individuals with ADHD by modulating neurotransmitter activity.

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    What does modafinil do for narcolepsy?

    Modafinil is a stimulant drug approved for narcolepsy. It acts on various neurotransmitter receptors (alpha1b, GABA, serotonin, and glutamate) to improve alertness and reduce sleepiness associated with the condition.

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    Ergot Alkaloids (Ergotamine, Ergonovine)

    Drugs like ergotamine and ergonovine that primarily act as alpha agonists, but also influence other receptors like serotonin and acetylcholine.

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    Ergotism

    A condition caused by ergot alkaloids characterized by effects on the central nervous system, leading to hallucinations and other neurological disturbances.

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    Orthostatic Hypotension

    A condition involving a significant drop in blood pressure upon standing, often causing lightheadedness or fainting.

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    Shock

    A severe medical condition characterized by inadequate perfusion of tissues and organs, leading to an inability to meet metabolic demands.

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    Cardiogenic Shock

    A type of shock caused by a weakened heart unable to pump blood effectively.

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    Congestive Heart Failure

    A type of heart failure characterized by a buildup of fluid in the lungs and other parts of the body.

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    Anaphylaxis

    A serious allergic reaction causing widespread swelling, difficulty breathing, and a drop in blood pressure.

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    Glaucoma

    A condition affecting the eye, characterized by increased pressure within the eye.

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    Increasing Aqueous Outflow

    The process of increasing the flow of fluid from the eye, which can help to reduce intraocular pressure.

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    Bronchial Asthma

    A chronic respiratory illness marked by recurrent episodes of wheezing, coughing, chest tightness, and shortness of breath. Often triggered by allergens or irritants, resulting in inflammation and narrowing of the airways.

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    COPD (Chronic Obstructive Pulmonary Disease)

    A group of lung diseases that block airflow and make it difficult to breathe. Characterized by persistent airflow limitation that is not fully reversible, typically caused by long-term exposure to irritants like smoke or dust.

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    Short-Acting Beta-Adrenoceptor Agonists (SABAs)

    Medications that quickly relieve asthma symptoms by widening the airways. They act on beta-adrenergic receptors in the lungs, causing smooth muscle relaxation.

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    Inhaled Corticosteroids

    Medications primarily used to help control long-term asthma symptoms by reducing inflammation in the airways. They are usually administered as inhalants and include corticosteroid medications.

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    Inhibitors of Mast Cell Degranulation

    Medications that block the release of histamine from mast cells, preventing an allergic reaction that can trigger asthma symptoms.

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    Leukotriene Antagonists

    Medications that specifically block the action of leukotrienes, chemicals involved in airway inflammation and constriction.

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    Methylxanthines (Theophylline)

    A type of medication that relaxes smooth muscles in the airways, often used to treat asthma. They act by inhibiting the breakdown of cyclic AMP, which promotes relaxation.

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    Long-Acting Beta-Adrenoceptor Agonists (LABAs)

    Medications that provide long-lasting relief from asthma symptoms by promoting bronchodilation. They are often used in combination with inhaled corticosteroids for effective long-term control.

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    Study Notes

    Adrenoreceptor Activating Drugs (Agonists)

    • Required Reading: Foye's, Sixth Edition - Chapter 13, pages 392-416; Foye's, Fifth Edition Online - Chapter 10. Recommended: Katzung, Eleventh Edition - Chapter 9, pages 127-148.

    Definitions

    • Catecholaminergic: Relating to norepinephrine, epinephrine, or dopamine effects.
    • Decongestant: A drug that reduces nasal or oropharyngeal swelling, typically by constricting blood vessels in the submucosal tissue.
    • Direct Agonist: Directly binds to and activates the receptor, causing the agonist effect.
    • Indirect Agonist: Brings about receptor activation by binding to another molecule (e.g., a reuptake carrier or enzyme), increasing the synaptic concentration of the normal neurotransmitter.
    • Mydriatic: A drug that causes pupil dilation; the opposite of miotic.
    • "Selective" alpha or beta adrenergic agonist: Drugs having a greater effect on a specific alpha or beta adrenergic receptor; however, none are completely selective.
    • Sympathomimetic: A drug that mimics the effects of stimulating the sympathetic autonomic nervous system (SNS).
    • Reuptake Inhibitor: An indirectly acting drug that increases neurotransmitter activity in the synapse by inhibiting its reuptake back into the presynaptic nerve terminal. It may act on more than one transporter at a time (e.g., norepinephrine and serotonin) and is considered an indirect agonist.

    Sympathomimetic Drugs/Adrenergic Agonists

    • Spectrum of Action: A branching diagram showing categories of adrenergic agonists based on direct/indirect action and receptor selectivity (alpha or beta). Specific examples of drugs are also listed. Categorization includes: a agonists/direct-acting, B agonists/direct-acting, indirect-acting (releasers), and reuptake inhibitors.

    Direct, Indirect, and Mixed Modes of Action

    • Direct: Binds to and directly activates adrenergic receptors.
    • Indirect: Displace stored catecholamines from adrenergic nerve endings (e.g., tyramine) or inhibit reuptake (e.g., cocaine and TCAs).
    • Mixed: Possess both direct and indirect modes of action (e.g., amphetamine).

    Organ System Effect - Receptor Specificity

    • Overall Effect: Determined by receptor affinity and intrinsic activity, alongside compensatory reflexes. Provides a table indicating the various receptor types (e.g α₁, β₁, β₂, β₃; and even D₁) and their target tissues (e.g. vascular smooth muscle, heart, platelets). These effects can vary based on relative receptor activation.

    Receptor Specificity of Direct Sympathomimetics

    • A table showing the receptor selectivity profiles of different direct-acting sympathomimetic drugs (e.g., norepinephrine, epinephrine, phenylephrine, and dobutamine) across various receptor subtypes (α₁, α₂, β₁, β₂).

    Cardiovascular System Effects

    • Blood Vessels: Responses vary depending on the dominant receptor subtype (α₁, β₂) leading to vasoconstriction or vasodilation, impacting blood pressure. Different vascular beds (skin vessels, skeletal muscle, etc.) exhibit distinct receptor profiles that affect outcomes.
    • Heart: Increase in calcium influx, positive chronotropic effect (increasing pacemaker rate), increased conduction velocity, decreased refractory period, and positive inotropic effects (increased contractility).
    • Blood Pressure: Pure alpha agonists (like phenylephrine) increase peripheral resistance and decrease venous capacitance, leading to a rise in blood pressure. Pure beta agonists (like isoproterenol) increase cardiac output and can have a varying effect on blood pressure, with effects dependent on other factors like vasodilatory effects.

    Visual System Effects

    • Eye: α₂ agonists decrease aqueous humor outflow, while β agonists increase aqueous humor production. α₁ agonists constrict the pupillary dilatory muscles, causing pupil dilation (mydriasis).

    Respiratory System Effects

    • Respiratory Tract: ẞ₂ agonists lead to bronchodilation, while α₁ agonists constrict blood vessels in the upper respiratory tract, which is a basis of decongestant action.

    Gastrointestinal & Genitourinary Effects

    • Gastrointestinal: α₁ and β₂ agonists typically relax GI smooth muscles.
    • Genitourinary: ẞ₂ mediates uterine relaxation (useful in pregnancy) and promotes urinary continence or retention. α₁ promotes contraction. Ejaculation relies on a receptor activation.

    Metabolic Effects

    • Metabolism: ẞ₃ activation (in fat cells) results in lipolysis, while a₂ inhibits lipolysis (in adipocytes ) by a decrease in intracellular cAMP. Sympathomimetics increase glycogenolysis in the liver (mostly affected by β receptors), but alpha receptors also play a role. Beta2 receptors stimulate potassium uptake in cells which leads to decrease in extracellular fluid potassium levels. Different organs respond differently to various adrenergic receptor types and actions.

    Exocrine and Endocrine Glands

    • Exocrine: Clonidine is associated with a dry mouth; the mechanism isn't fully understood.
    • Endocrine: β2 receptor activation in islet cells of the pancreas increases insulin secretion. This response is often modulated by simultaneous a2 receptor activation. Renin release is stimulated by β₁ receptors but inhibited by α₂ receptors.

    Central Nervous System Effects

    • CNS: Various effects depend on the ability of catecholamines to cross the blood-brain barrier (BBB). They tend to not cross the BBB based on their charge, with few effects observed in the brain during low rates of infusion; however, effects at higher rates can be felt. Beta-agonists can elicit effects similar to anxious somatic feelings. Beta-antagonists can be beneficial in migraines and tension headaches. Amphetamine usage enhances dopamine function in the central nervous system, influencing mood, attention, and alertness.

    CNS Effects - Amphetamine

    • Amphetamine: At low concentrations, amphetamine blocks dopamine/norepinephrine reuptake, while high concentrations disrupt neurotransmission.

    Dominant Effects of Adrenergic Drugs

    • Blood Vessels: α₁ primarily causes vasoconstriction, increasing blood pressure initially, followed by compensatory reflex slowing of heart rate.
    • Heart: β₁ increases heart rate and force, increasing initial blood pressure.
    • Bronchial Smooth Muscle: β₂ relaxes muscles and opens airways.
    • Eye: α₁ constricts pupils and nasal mucosa.
    • CNS: Diverse effects.

    Catecholamines - Receptor Selectivity

    • Epinephrine (Adrenaline): Primarily affects alpha and beta receptors (α₁ = α₂, β₁ = β₂).
    • Norepinephrine (Noradrenaline): Significantly effects alpha and beta receptors with a greater effect on β₁ than β₂.
    • Isoproterenol: Strong effects on β₁ and β₂ receptors, with comparatively less effect on alpha receptors.
    • Dopamine: Primarily affects dopamine receptors D₁ and D₂, with minimal effect on other adrenergic receptors.

    Catecholamines - Cardiovascular Effects

    • Contraction of Arterial Strips: Graph showing receptor activation and resulting potency, comparing epinephrine, norepinephrine, and isoproterenol at different concentrations.
    • Relaxation of Bronchial Smooth Muscle: Comparison of epinephrine, norepinephrine, and isoproterenol.
    • Augmented Contraction of Heart Tissue: Same graph comparison as above.

    Dopamine & Sympathomimetics

    • Dopamine: D₁=D₂ >> β₁ > α₁, primarily causing vasodilation, vital for renal blood flow and shock, and it suppresses norepinephrine release via presynaptic D₂ activation.
    • Higher Doses: Can mimic the actions of epinephrine which leads to vasoconstriction, and their combined effect impacts tissue perfusion.

    Adrenergic Agonists - α Receptors

    • Phenylephrine: Strong α₁ effect, with minimal β effects; important for mydriasis, decongestants, and raising blood pressures; longer duration of action.
    • Midodrine: α₁ selective agonist, a prodrug, commonly used clinically for chronic orthostatic hypotension.
    • Methoxamine: Strong α₁ effect with minimal β effects. Pharmacologically similar to ephedrine, useful under hypotensive conditions.
    • Xylometazoline and Oxymetazoline: Alpha-selective agonists, used topically as nasal decongestants, however prolonged usage can lead to rebound congestion.

    Alpha2 Receptor Selective Drugs

    • Decrease blood pressure: Through a central effect and reducing sympathetic outflow.
    • Antihypertensive effect: Mediated by binding to non-adrenergic receptors (e.g., imidazoline receptors), and may be involved in the overall antihypertensive effect.
    • Local application: Causes vasoconstriction.
    • Clinical examples: Clonidine, Methyldopa, Guanfacine, and Guanabenz. Dexmedetomidine is indicated for sedation.

    α₂ Receptor Agonists - Mechanism of Action

    • Baroreceptor Reflex: Diagram illustrating the interaction between blood pressure, heart rate, sympathomimetic actions, and consequent drug effects on the CNS and cardiovascular systems when a2 agonists are given.

    Adrenergic Agonists - β Receptors

    • Isoproterenol: Strong β₁ and β₂ effects, primarily used for its effects on the heart and bronchi. Not very selective; minimal alpha effects.
    • Dobutamine: Primarily a selective β₁ agonist with some β₂ effect but minimal alpha effects. Its significant vaso-constrictive effect compared to other B-selective drugs.

    ẞ₂ Selective Agonists Used for Asthma/Uterine Relaxation

    • Short-Acting: Albuterol, Bitolterol, Metaproterenol, Pirbuterol, Terbutaline, and Lavalbuterol.
    • Long-Acting: Salmeterol and Formoterol, useful for maintaining the effects. ẞ₂-selective agonists reduce pulmonary vascular tone and uterine contraction. Commonly used in asthma.

    Adrenergic Agonists - Mixed Agonists

    • Ephedrine: Mixed agonist, releasing stored catecholamines and exhibiting some direct action. Often used as a nasal decongestant, pressor agent, and for the treatment of stress incontinence.
    • Pseudoephedrine: Indirect agonist, primarily relieving nasal decongestion. May also resolve stress incontinence.

    Adrenergic Agonists - Indirect Agonists

    • Amphetamine and Methylphenidate: Indirect agonists; primarily affect the central nervous system. Their usage includes treating ADHD, mood enhancement, and as appetite suppressants in short term use.

    Adrenergic Agonists - Receptor Selectivity for Indirect Agonists

    • Substrate/Inhibitors: Categorizes neurotransmitter substrates and inhibitors that influence various neurotransmitter transporters (e.g., norepinephrine, dopamine, serotonin) and their associated effects. Ephedrine, Tyramine, Amphetamine, and Cocaine are mentioned as important mediators for release. The relevant inhibitory effects for reuptake are also listed.

    Adrenergic Agonists - "Selective" Reuptake Inhibitors

    • Atomoxetine: Selective norepinephrine reuptake inhibitor, used to treat ADHD.
    • Reboxetine: Similar to Atomoxetine. Reuptake Inhibitor.
    • Sibutramine: Selective serotonin and norepinephrine reuptake inhibitor, initially for appetite suppression but is no longer in use due to complications.
    • Duloxetine: Similar to an SSRI, also acts as an inhibitor for both norepinephrine and serotonin reuptake, used for depression and other conditions.

    Catecholamines & Non-catecholamines

    • Categorises drugs into Catecholamines and non-catecholamines based on structural and functional differences and receptor specificity. A table lists some important drugs and their relevant applications. (E.g., Epinephrine use in asthma, acute asthma, and shock.)

    Adrenergic Agonists - Therapeutic Applications

    • Acute Hypotension and/or shock: Use epinephrine, dopamine, and other agonists to increase blood pressure and maintain organ perfusion.
    • Chronic Orthostatic Hypotension: Midodrine, a selective α₁ agonist, is often used. Certain blood pressure maintaining mechanisms in the body, should be targeted to counteract shock related effects.
    • Cardiac Applications: Dopamine and dobutamine are positive inotropic agents.
    • Pulmonary Applications (Asthma): Beta₂ selective agonists are used as bronchodilators.
    • CNS Applications: Various agents have different applications in cases of narcolepsy and ADHD. Clonidine can be helpful in treatment of addiction cravings.
    • Other: Applications for glaucoma, anaphylaxis, and inducing local vasoconstriction are also detailed.

    Adrenergic Agents - Toxicity

    • Cardiovascular: Causes adverse effects like marked blood pressure elevation, cerebral hemorrhage, pulmonary edema, increased cardiac work, angina, myocardial infarction, sinus tachycardia, ventricular arrhythmia, and myocardial damage from long infusions.
    • CNS: Cocaine can cause convulsions, cerebral hemorrhages, and arrhythmias, as well as myocardial infarctions. Monitoring is crucial.

    Glaucoma

    • Epinephrine and Dipivefrin: Lower intraocular pressure by influencing aqueous outflow.
    • Alpha2 Selective Agonists: Apraclonidine and Brimonidine are second and first line treatment against glaucoma.
    • **Beta-Blocking Agents:**Timolol, Beta-xolol, Carteolol, Levobunolol, and Metipranolol are now the primary treatment for decreasing aqueous humor production.

    Genitourinary Applications

    • Suppress Premature Labor: ẞ2 selective agonists, like Ritodrine and Terbutaline, are tocolytic agents and help relax the uterus.
    • Stress Incontinence: Oral ephedrine or pseudoephedrine might be used. Priapism management addresses a different target.

    Central Nervous System Applications

    • Addiction Craving: Treatments like clonidine are used to decrease cravings.
    • Narcolepsy: Agents like Modafinil are used as treatment due to their effects on the central nervous system.
    • Appetite Suppression: Amphetamine-like drugs (e.g., methylphenidate) can suppress appetite but are used carefully due to risks.

    Attention Deficit and Hyperactivity Disorder (ADHD)

    • Treatment: Amphetamine and methylphenidate, and even atomoxetine, are commonly presented as treatments. Many also require multimodal therapies.

    Bronchial Asthma & COPD

    • Asthma: A chronic inflammatory disorder associated with bronchial hyperactivity, bronchoconstriction, and bronchospasm.
    • COPD: Structural disorder in the airways not associated with inflammation, however, has increased incidence with smoking or other environmental exposures.
    • Treatment: Short and long-term approaches are reviewed. Short term treatments include β₂-adrenoceptor agonists (e.g., albuterol). Long term approaches include inhaled corticosteroids (e.g., fluticasone), inhibitors of mast cell degranulation, and leukotriene antagonists.

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    Test your knowledge on the pharmacological aspects of sympathomimetic drugs, including the role of MAOIs, cocaine, and various agonists. This quiz will cover mechanisms of action, effects of different drugs, and the biochemical principles governing these interactions.

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