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Questions and Answers
Which adrenergic receptor type is primarily responsible for vasoconstriction?
Which adrenergic receptor type is primarily responsible for vasoconstriction?
What is the primary effect of Beta 2 adrenergic receptor activation?
What is the primary effect of Beta 2 adrenergic receptor activation?
What is the main outcome of the re-uptake of norepinephrine into the neuron?
What is the main outcome of the re-uptake of norepinephrine into the neuron?
How does Alpha 2 adrenergic receptor activation affect insulin release?
How does Alpha 2 adrenergic receptor activation affect insulin release?
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Which of the following is classified as a direct-acting adrenergic drug?
Which of the following is classified as a direct-acting adrenergic drug?
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Which adrenergic drug class is known for stimulating norepinephrine release?
Which adrenergic drug class is known for stimulating norepinephrine release?
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What physiological effect results from Beta 1 receptor activation?
What physiological effect results from Beta 1 receptor activation?
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What role does MAO have in the control of norepinephrine levels?
What role does MAO have in the control of norepinephrine levels?
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What is the primary role of beta 2 receptors in the body?
What is the primary role of beta 2 receptors in the body?
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Which of the following statements about sympathomimetic drugs is true?
Which of the following statements about sympathomimetic drugs is true?
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What is the effect of dopamine on renal blood vessels?
What is the effect of dopamine on renal blood vessels?
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Which mechanism is primarily associated with indirect agonists in the context of neurotransmitter release?
Which mechanism is primarily associated with indirect agonists in the context of neurotransmitter release?
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What effect do beta 2 receptors have on pancreatic beta cells?
What effect do beta 2 receptors have on pancreatic beta cells?
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Which drug is classified as an indirect acting agonist?
Which drug is classified as an indirect acting agonist?
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Which receptor subtype has a higher affinity for epinephrine over norepinephrine?
Which receptor subtype has a higher affinity for epinephrine over norepinephrine?
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Which mechanism is affected by Agonist drug binding to adrenergic receptors?
Which mechanism is affected by Agonist drug binding to adrenergic receptors?
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What is the primary action of beta adrenergic agonists on muscle cells?
What is the primary action of beta adrenergic agonists on muscle cells?
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Which of the following is not classified as a sympathomimetic?
Which of the following is not classified as a sympathomimetic?
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Which substance is primarily known as a beta-agonist used for respiratory issues?
Which substance is primarily known as a beta-agonist used for respiratory issues?
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Which sympathomimetic drug is primarily used as a vasoconstrictor?
Which sympathomimetic drug is primarily used as a vasoconstrictor?
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Which of the following receptor types binds norepinephrine equally to epinephrine?
Which of the following receptor types binds norepinephrine equally to epinephrine?
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What is the primary clinical effect of phenylephrine when it acts as an alpha 1 agonist?
What is the primary clinical effect of phenylephrine when it acts as an alpha 1 agonist?
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Which drug is indicated for increasing blood pressure through alpha 1 receptor stimulation?
Which drug is indicated for increasing blood pressure through alpha 1 receptor stimulation?
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Which beta agonist is primarily used to relieve bronchoconstriction?
Which beta agonist is primarily used to relieve bronchoconstriction?
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What is the role of isoproterenol in terms of receptor interaction?
What is the role of isoproterenol in terms of receptor interaction?
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What is the primary action of epinephrine during anaphylactic shock?
What is the primary action of epinephrine during anaphylactic shock?
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Which of the following drugs is classified as a pure beta agonist?
Which of the following drugs is classified as a pure beta agonist?
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Which beta agonist is commonly used for acute asthmatic bronchoconstriction?
Which beta agonist is commonly used for acute asthmatic bronchoconstriction?
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What pharmacological effect does clonidine have through alpha 2 receptor agonism?
What pharmacological effect does clonidine have through alpha 2 receptor agonism?
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What is the primary therapeutic use of amphetamines?
What is the primary therapeutic use of amphetamines?
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Which type of medication is used topically for reducing conjunctival itching caused by allergies?
Which type of medication is used topically for reducing conjunctival itching caused by allergies?
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Which adrenergic receptors are primarily involved in suppressing premature labor?
Which adrenergic receptors are primarily involved in suppressing premature labor?
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What can beta activation lead to in terms of blood pressure regulation?
What can beta activation lead to in terms of blood pressure regulation?
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Which action is associated with alpha agonists in the management of eye conditions?
Which action is associated with alpha agonists in the management of eye conditions?
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In the genitourinary tract, which receptor type promotes contraction of the bladder?
In the genitourinary tract, which receptor type promotes contraction of the bladder?
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Which of the following effects do beta receptors on fat cells primarily have?
Which of the following effects do beta receptors on fat cells primarily have?
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What effect do beta 2 agonists have on bronchial smooth muscle?
What effect do beta 2 agonists have on bronchial smooth muscle?
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What is the primary effect of epinephrine?
What is the primary effect of epinephrine?
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Which of the following correctly describes isoproterenol?
Which of the following correctly describes isoproterenol?
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In the context of anaphylaxis, which of the following actions is attributed to epinephrine?
In the context of anaphylaxis, which of the following actions is attributed to epinephrine?
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What is a potential cardiovascular adverse effect of sympathomimetic drugs?
What is a potential cardiovascular adverse effect of sympathomimetic drugs?
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Which receptors are primarily activated by norepinephrine and epinephrine?
Which receptors are primarily activated by norepinephrine and epinephrine?
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What role does modafinil have in the context of sympathomimetic drugs?
What role does modafinil have in the context of sympathomimetic drugs?
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Which of the following sympathomimetic drugs is used for local anesthesia in combination with norepinephrine?
Which of the following sympathomimetic drugs is used for local anesthesia in combination with norepinephrine?
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What outcome is associated with the action of alpha 1 activation from sympathomimetic drugs?
What outcome is associated with the action of alpha 1 activation from sympathomimetic drugs?
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Metoprolol is selective for which adrenoceptors?
Metoprolol is selective for which adrenoceptors?
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What effects does metoprolol have on the cardiovascular system?
What effects does metoprolol have on the cardiovascular system?
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In which organ is metoprolol primarily metabolized (biotransformed)?
In which organ is metoprolol primarily metabolized (biotransformed)?
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Why must beta-adrenergic antagonists be used with caution in asthmatics?
Why must beta-adrenergic antagonists be used with caution in asthmatics?
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Which of the following are reversible alpha receptor agonists?
Which of the following are reversible alpha receptor agonists?
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Which of the following is an irreversible alpha receptor antagonist?
Which of the following is an irreversible alpha receptor antagonist?
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Match each alpha blocker drug to its description
Match each alpha blocker drug to its description
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Match each alpha blocker drug to its description
Match each alpha blocker drug to its description
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What are non-selective alpha blockers used to treat?
What are non-selective alpha blockers used to treat?
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Which drug has a high bioavailability following oral dosing?
Which drug has a high bioavailability following oral dosing?
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Which drug has a short half-life of 10 minutes?
Which drug has a short half-life of 10 minutes?
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Which drug is highly lipid soluble and can enter the CNS?
Which drug is highly lipid soluble and can enter the CNS?
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What is the mechanism of action (MOA) of all local anesthetics?
What is the mechanism of action (MOA) of all local anesthetics?
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Match each drug to its selectivity, partial agonist activity and lipid solubility
Match each drug to its selectivity, partial agonist activity and lipid solubility
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Match each drug to its lipid solubility and half life
Match each drug to its lipid solubility and half life
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What drug is used for both performance anxiety and migraines?
What drug is used for both performance anxiety and migraines?
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Which of the following displaces stored biogenic amines from nerve terminals?
Which of the following displaces stored biogenic amines from nerve terminals?
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Which of the following block the reuptake of the amine back into storage in the neuron?
Which of the following block the reuptake of the amine back into storage in the neuron?
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Which of the following are antagonists to phenylephrine? (Select all that apply)
Which of the following are antagonists to phenylephrine? (Select all that apply)
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Which of the following is an antagonist to isoproterenol?
Which of the following is an antagonist to isoproterenol?
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Match each receptor type to its description
Match each receptor type to its description
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Which desensitization is described below:
caused by repeated exposure to agonist drug
Which desensitization is described below: caused by repeated exposure to agonist drug
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Which desensitization is described below: receptor A undergoes homologous desensitization which
causes receptor B which never saw the agonist drug but it becomes desensitized
also
Which desensitization is described below: receptor A undergoes homologous desensitization which causes receptor B which never saw the agonist drug but it becomes desensitized also
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What is a good example of a drug that inhibits the NET and raises NE, which stimulates alpha and beta receptors?
What is a good example of a drug that inhibits the NET and raises NE, which stimulates alpha and beta receptors?
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Which alpha 1 agonist leads to urinary retention? It is also used to treat orthostatic hypertension
Which alpha 1 agonist leads to urinary retention? It is also used to treat orthostatic hypertension
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Which drug is both an agonist and antagonist at alpha 2 receptors and stops NE from binding or being produced?
Which drug is both an agonist and antagonist at alpha 2 receptors and stops NE from binding or being produced?
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What is the most common clinical presentation of a pheochromocytoma?
What is the most common clinical presentation of a pheochromocytoma?
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Which of the following alpha blockers is indicated for the treatment of urinary obstruction in benign prostatic hyperplasia (BPH)?
Which of the following alpha blockers is indicated for the treatment of urinary obstruction in benign prostatic hyperplasia (BPH)?
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What commonly occurs during postural changes associated with alpha blocker use?
What commonly occurs during postural changes associated with alpha blocker use?
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What is a common side effect seen with the use of alpha antagonists?
What is a common side effect seen with the use of alpha antagonists?
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Which of the following conditions is NOT primarily treated with alpha blockers?
Which of the following conditions is NOT primarily treated with alpha blockers?
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Which drug is specifically mentioned as the drug of choice for managing pheochromocytoma post-operatively?
Which drug is specifically mentioned as the drug of choice for managing pheochromocytoma post-operatively?
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What is the mechanism by which ergot derivatives primarily help in the treatment of migraines?
What is the mechanism by which ergot derivatives primarily help in the treatment of migraines?
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What is a notable clinical use of selective alpha1 antagonists?
What is a notable clinical use of selective alpha1 antagonists?
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In what way do sympatholytics primarily exert their effects?
In what way do sympatholytics primarily exert their effects?
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What is the primary therapeutic use of clonidine, an alpha 2 agonist?
What is the primary therapeutic use of clonidine, an alpha 2 agonist?
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What is primarily released by pheochromocytomas that leads to symptoms of palpitations and sweating?
What is primarily released by pheochromocytomas that leads to symptoms of palpitations and sweating?
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Which factor affects the duration of action of reversible alpha antagonists?
Which factor affects the duration of action of reversible alpha antagonists?
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Which adrenoceptor antagonist is classified as a non-selective beta blocker?
Which adrenoceptor antagonist is classified as a non-selective beta blocker?
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How might beta blockers affect individuals who are insulin-dependent?
How might beta blockers affect individuals who are insulin-dependent?
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Which of these drugs is specifically indicated for heart rate reduction?
Which of these drugs is specifically indicated for heart rate reduction?
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What adverse effect is associated with high lipid solubility beta antagonists?
What adverse effect is associated with high lipid solubility beta antagonists?
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Which muscarinic agonist is mentioned in the context of parasympathetic activity?
Which muscarinic agonist is mentioned in the context of parasympathetic activity?
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What effect is commonly associated with the use of atenolol compared to other beta blockers?
What effect is commonly associated with the use of atenolol compared to other beta blockers?
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What is the effect of beta antagonists on intraocular pressure in patients with glaucoma?
What is the effect of beta antagonists on intraocular pressure in patients with glaucoma?
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Which drug is primarily indicated for the treatment of hypertension combined with diuretics and/or vasodilators?
Which drug is primarily indicated for the treatment of hypertension combined with diuretics and/or vasodilators?
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How do beta 2 selective beta blockers affect metabolism, particularly in diabetes patients?
How do beta 2 selective beta blockers affect metabolism, particularly in diabetes patients?
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What is the primary therapeutic use of metoprolol in clinical practice?
What is the primary therapeutic use of metoprolol in clinical practice?
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In treating hyperthyroidism, which effect do beta blockers like propranolol exhibit?
In treating hyperthyroidism, which effect do beta blockers like propranolol exhibit?
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Study Notes
Pharmacology I, Chapter 9: NE Agonists (Sympathomimetics)
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Case Study: A 68-year-old male presented with lightheadedness upon standing, worsened by meals, decreased sweating, and urinary retention. He was taking the alpha-1 antagonist, tamsulosin, for urinary retention, but it worsened his orthostatic hypotension. His supine blood pressure was 167/84 mmHg and standing blood pressure was 106/55 mmHg. Heart rate did not compensate. The diagnosis was pure autonomic failure, unrelated to other diseases or drugs.
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Case Study (continued): The patient had lost sympathetic tone. Tamsulosin, an alpha blocker, worsened his condition. Midodrine, an alpha agonist, might be helpful. The patient should avoid over-the-counter sympathomimetics and sympatholytics.
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Catecholamines: Adrenergic neurotransmitters include norepinephrine, epinephrine, and dopamine. Chemical structures of each are shown.
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Adrenergic Neurotransmitter Discovery: J. Axelrod (1912-2004) won the Nobel Prize in 1970 for discovering the uptake and release of catecholamine neurotransmitters.
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Sympathomimetics (Adrenergic Agonists): These drugs mimic the actions of the sympathetic nervous system. Adrenal glands (L. add + renal), sympathetic nervous system, and adrenergic neurons release norepinephrine (NE). Locations are in the CNS and linking between ganglia and effector organs within the peripheral nervous system (PNS).
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Sympathetic Drugs/Terms: Norepinephrine (NE), Epinephrine (EP), Dopamine (DA) are catecholamines. Derived from the amino acid tyrosine. Adrenergics (Gr. work) NE, EP, DA. (Commonly used terms to refer to these substances)
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Receptor Organization, Sympathetic/Parasympathetic Pathway: The information presented in diagram form, showing the CNS, ACh, NE, adrenergic receptors (α1, α2, β1, β2). Diagram also presents the parasympathetic and somatic pathways.
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NE at Adrenergic Neurons: Steps 1-6 in the synthesis, storage, release, receptor binding, re-uptake, and removal of NE from the synapse.
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Adrenergic Receptors: Alpha1: Actions include vasoconstriction, increased peripheral resistance, increased blood pressure (BP), mydriasis, increased closure of the bladder sphincter.
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Adrenergic Receptors: Alpha2: Actions include inhibition of NE release, inhibition of insulin release.
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Adrenergic Receptors: Beta1: Actions include tachycardia, increased lipolysis, increased myocardial contractility, increased renin release.
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Adrenergic Receptors: Beta2: Actions include vasodilation, decreased peripheral resistance, bronchodilation, relaxation of uterine smooth muscle.
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Adrenoceptor Agonists & Sympathomimetics Drugs (Table 9-1): This table lists receptor type, agonist, antagonist, G protein, effects, and chromosome location. (Detailed Table)
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Adrenergic Drugs (Direct-Acting/Indirect-Acting): A direct-acting drug binds to receptors (e.g., epinephrine, norepinephrine, isoproterenol, phenylephrine). An indirect-acting drug causes the release of norepinephrine (e.g., tyramine, amphetamine).
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Adrenergic Drugs (Mixed Action): This category includes drugs with both direct- and indirect-acting effects (e.g., ephedrine, metaraminol).
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Cardiac Innervation: Parasympathetic (ACh) and sympathetic (NE) systems. NE causes constriction (+), ACh causes relaxation (-). Diagram also presents blood vessels and the heart.
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Sympathomimetics: This section explains the categories and different type of drugs.
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Relative receptor affinities of Adrenergic Agonists (Table 9-2): This table provides details on the relative binding affinities of various agonists to different receptor subtypes (e.g., α1, α2, β1, β2). (Detailed Table)
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Distribution of adrenoceptor subtypes (Table 9-3): Details on the presence and actions of receptor subtypes on various tissues and organs. (Detailed Table)
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Alpha 1 Receptors: Locations (vascular smooth muscle, pupil dilator muscle, pilomotor smooth muscle), effect of activation (contraction).
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Alpha 2 Receptors: Locations (adrenal and cholinergic nerve terminals, platelets, smooth muscle, fat cells), effect of activation (inhibition of NE release, inhibition of insulin release, inhibition of lipolysis)
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Beta 1 Receptors: Location (heart, juxtaglomerular cells), effect of activation (increase heart rate/force).
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Beta 2 Receptors: Location (smooth muscle, skeletal muscle, liver), effect of activation (muscle relaxation, glycogenolysis).
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Dopamine Receptors: Locations and functions. Different types and effects. Activation stimulates adenyl cyclase and increases cAMP second messenger.
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Receptor Desensitization: Repeated exposure leads to a decrease in receptor response. There are homologous (in the exposed receptor) and heterologous (in other receptors) forms
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Points to Remember: Important features and locations of Alpha 1, Beta 1, and Beta 2 receptors highlighted, summarizing their functions.
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Pharmacokinetics of Isoproterenol/Methoxamine: Includes information on absorption and distribution depending on substitutions in the chemical structure.
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Beta Agonists (Table): A table with examples, receptor subtypes, and clinical effects. List includes examples of drug names.
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Alpha Receptor Agonists (Table): Another table with examples, receptor subtypes, and clinical effects. List includes example of drug names.
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Anaphylaxis: Epinephrine is the treatment of choice.
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Bronchi (asthma): Beta agonists (mostly Beta 2) treat acute asthmatic bronchoconstriction with short-acting examples such as terbutaline, albuterol, and metaproterenol.
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Cardiovascular: NE increases blood flow in acute heart failure and some types of shock. Beta 1 agonists useful here.
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CNS effects of Amphetamines: Weight loss, attention-deficit disorder, narcolepsy, mood altering effects.
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Eye drug effects: Alpha agonists are used topically for conjunctival itching and for glaucoma.
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Genitourinary Tract: Beta 2 agonists used to suppress premature labor and ephedrine for continence problems. Alpha receptors are also involved in the bladder.
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Summary I and Summary 2: These pages include summary points on various aspects of adrenergic agonists, and how to organize, classify, or categorize them.
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Cardiovascular Effects of NE: NE causes total peripheral resistance increase, leading to arterial pressure elevation. Also causes vascular bed constriction and a subsequent increase in BP. In response to higher BP, the body activates parasympathetic output to the heart, increasing the heartbeat. Despite this, norepinephrine activation of beta 1 receptors causes a decrease in the heart rate.
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Specific Sympathomimetic Drugs: Clinically relevant drugs, their classifications, and use cases described more specifically.
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Selective Sympathomimetics: Including dexmedetomidine, tyramine, and others, based on specificity and use.
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Clonidine (Catapres®): An alpha 2 agonist, lowering sympathetic outflow, reducing heart rate, and having multiple functions with a presynaptic/postsynaptic effect.
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Dopamine (Intropin®): A dopamine receptor agonist, primarily used as a vasodilator at low doses for renal and coronary blood vessels. In high doses, it functions more like noradrenaline. Activates beta 1 receptors.
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Importance of Receptor Type in Clinical Practice: Focuses on a patient with reactive airway disease and a mild heart attack. The need to use beta 2 receptor agonists targeting the lung but not stimulating the heart is emphasized.
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Epinephrine (Adrenalin): Potent vasoconstrictor and cardiac stimulant, increasing blood pressure.
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Norepinephrine: Similar effects to epinephrine.
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Isoproterenol: Potent beta agonist primarily, with limited effect on alpha receptors, and a potent vasodilator effect.
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Sympathomimetic Drugs (General): Raising blood pressure via drug reactions, decreased blood volume, and infections via reduced blood flow in surgery and local anesthesia, to reduce diffusion and efficacy. Shock is also mentioned.
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Sympathomimetics (Effects): Anaphylactic shock, caused by immediate IgE-mediated reactions, addressed and reversed by epinephrine (EP). CNS effects are discussed for drug use, like modafinil (amphetamine analog) in narcolepsy and for ADHD (methylphenidate, clonidine).
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Sympathomimetic Receptors, General (Summary): Describes receptor subtypes, specificity, and activation effects, like varying receptor subtypes and their varied activation pathways to achieve activation/inactivation of an action.
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Agonist Drug Binding Mechanism: Detailed mechanism to achieve activation (e.g., activation of G proteins and cAMP, downstream signaling pathways).
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