Podcast
Questions and Answers
Which adrenergic receptor type is primarily responsible for vasoconstriction?
Which adrenergic receptor type is primarily responsible for vasoconstriction?
- Beta 2
- Alpha 2
- Beta 1
- Alpha 1 (correct)
What is the primary effect of Beta 2 adrenergic receptor activation?
What is the primary effect of Beta 2 adrenergic receptor activation?
- Increased heart rate
- Vasoconstriction
- Bronchodilation (correct)
- Increased peripheral resistance
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?
- Activation of muscle contraction
- Decreased norepinephrine levels in the synapse (correct)
- Enhanced adrenergic receptor sensitivity
- Increased blood pressure
How does Alpha 2 adrenergic receptor activation affect insulin release?
How does Alpha 2 adrenergic receptor activation affect insulin release?
Which of the following is classified as a direct-acting adrenergic drug?
Which of the following is classified as a direct-acting adrenergic drug?
Which adrenergic drug class is known for stimulating norepinephrine release?
Which adrenergic drug class is known for stimulating norepinephrine release?
What physiological effect results from Beta 1 receptor activation?
What physiological effect results from Beta 1 receptor activation?
What role does MAO have in the control of norepinephrine levels?
What role does MAO have in the control of norepinephrine levels?
What is the primary role of beta 2 receptors in the body?
What is the primary role of beta 2 receptors in the body?
Which of the following statements about sympathomimetic drugs is true?
Which of the following statements about sympathomimetic drugs is true?
What is the effect of dopamine on renal blood vessels?
What is the effect of dopamine on renal blood vessels?
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?
What effect do beta 2 receptors have on pancreatic beta cells?
What effect do beta 2 receptors have on pancreatic beta cells?
Which drug is classified as an indirect acting agonist?
Which drug is classified as an indirect acting agonist?
Which receptor subtype has a higher affinity for epinephrine over norepinephrine?
Which receptor subtype has a higher affinity for epinephrine over norepinephrine?
Which mechanism is affected by Agonist drug binding to adrenergic receptors?
Which mechanism is affected by Agonist drug binding to adrenergic receptors?
What is the primary action of beta adrenergic agonists on muscle cells?
What is the primary action of beta adrenergic agonists on muscle cells?
Which of the following is not classified as a sympathomimetic?
Which of the following is not classified as a sympathomimetic?
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?
Which sympathomimetic drug is primarily used as a vasoconstrictor?
Which sympathomimetic drug is primarily used as a vasoconstrictor?
Which of the following receptor types binds norepinephrine equally to epinephrine?
Which of the following receptor types binds norepinephrine equally to epinephrine?
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?
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?
Which beta agonist is primarily used to relieve bronchoconstriction?
Which beta agonist is primarily used to relieve bronchoconstriction?
What is the role of isoproterenol in terms of receptor interaction?
What is the role of isoproterenol in terms of receptor interaction?
What is the primary action of epinephrine during anaphylactic shock?
What is the primary action of epinephrine during anaphylactic shock?
Which of the following drugs is classified as a pure beta agonist?
Which of the following drugs is classified as a pure beta agonist?
Which beta agonist is commonly used for acute asthmatic bronchoconstriction?
Which beta agonist is commonly used for acute asthmatic bronchoconstriction?
What pharmacological effect does clonidine have through alpha 2 receptor agonism?
What pharmacological effect does clonidine have through alpha 2 receptor agonism?
What is the primary therapeutic use of amphetamines?
What is the primary therapeutic use of amphetamines?
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?
Which adrenergic receptors are primarily involved in suppressing premature labor?
Which adrenergic receptors are primarily involved in suppressing premature labor?
What can beta activation lead to in terms of blood pressure regulation?
What can beta activation lead to in terms of blood pressure regulation?
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?
In the genitourinary tract, which receptor type promotes contraction of the bladder?
In the genitourinary tract, which receptor type promotes contraction of the bladder?
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?
What effect do beta 2 agonists have on bronchial smooth muscle?
What effect do beta 2 agonists have on bronchial smooth muscle?
What is the primary effect of epinephrine?
What is the primary effect of epinephrine?
Which of the following correctly describes isoproterenol?
Which of the following correctly describes isoproterenol?
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?
What is a potential cardiovascular adverse effect of sympathomimetic drugs?
What is a potential cardiovascular adverse effect of sympathomimetic drugs?
Which receptors are primarily activated by norepinephrine and epinephrine?
Which receptors are primarily activated by norepinephrine and epinephrine?
What role does modafinil have in the context of sympathomimetic drugs?
What role does modafinil have in the context of sympathomimetic drugs?
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?
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?
Metoprolol is selective for which adrenoceptors?
Metoprolol is selective for which adrenoceptors?
What effects does metoprolol have on the cardiovascular system?
What effects does metoprolol have on the cardiovascular system?
In which organ is metoprolol primarily metabolized (biotransformed)?
In which organ is metoprolol primarily metabolized (biotransformed)?
Why must beta-adrenergic antagonists be used with caution in asthmatics?
Why must beta-adrenergic antagonists be used with caution in asthmatics?
Which of the following are reversible alpha receptor agonists?
Which of the following are reversible alpha receptor agonists?
Which of the following is an irreversible alpha receptor antagonist?
Which of the following is an irreversible alpha receptor antagonist?
Match each alpha blocker drug to its description
Match each alpha blocker drug to its description
Match each alpha blocker drug to its description
Match each alpha blocker drug to its description
What are non-selective alpha blockers used to treat?
What are non-selective alpha blockers used to treat?
Which drug has a high bioavailability following oral dosing?
Which drug has a high bioavailability following oral dosing?
Which drug has a short half-life of 10 minutes?
Which drug has a short half-life of 10 minutes?
Which drug is highly lipid soluble and can enter the CNS?
Which drug is highly lipid soluble and can enter the CNS?
What is the mechanism of action (MOA) of all local anesthetics?
What is the mechanism of action (MOA) of all local anesthetics?
Match each drug to its selectivity, partial agonist activity and lipid solubility
Match each drug to its selectivity, partial agonist activity and lipid solubility
Match each drug to its lipid solubility and half life
Match each drug to its lipid solubility and half life
What drug is used for both performance anxiety and migraines?
What drug is used for both performance anxiety and migraines?
Which of the following displaces stored biogenic amines from nerve terminals?
Which of the following displaces stored biogenic amines from nerve terminals?
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?
Which of the following are antagonists to phenylephrine? (Select all that apply)
Which of the following are antagonists to phenylephrine? (Select all that apply)
Which of the following is an antagonist to isoproterenol?
Which of the following is an antagonist to isoproterenol?
Match each receptor type to its description
Match each receptor type to its description
Which desensitization is described below:
caused by repeated exposure to agonist drug
Which desensitization is described below: caused by repeated exposure to agonist drug
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
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?
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
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?
What is the most common clinical presentation of a pheochromocytoma?
What is the most common clinical presentation of a pheochromocytoma?
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)?
What commonly occurs during postural changes associated with alpha blocker use?
What commonly occurs during postural changes associated with alpha blocker use?
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?
Which of the following conditions is NOT primarily treated with alpha blockers?
Which of the following conditions is NOT primarily treated with alpha blockers?
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?
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?
What is a notable clinical use of selective alpha1 antagonists?
What is a notable clinical use of selective alpha1 antagonists?
In what way do sympatholytics primarily exert their effects?
In what way do sympatholytics primarily exert their effects?
What is the primary therapeutic use of clonidine, an alpha 2 agonist?
What is the primary therapeutic use of clonidine, an alpha 2 agonist?
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?
Which factor affects the duration of action of reversible alpha antagonists?
Which factor affects the duration of action of reversible alpha antagonists?
Which adrenoceptor antagonist is classified as a non-selective beta blocker?
Which adrenoceptor antagonist is classified as a non-selective beta blocker?
How might beta blockers affect individuals who are insulin-dependent?
How might beta blockers affect individuals who are insulin-dependent?
Which of these drugs is specifically indicated for heart rate reduction?
Which of these drugs is specifically indicated for heart rate reduction?
What adverse effect is associated with high lipid solubility beta antagonists?
What adverse effect is associated with high lipid solubility beta antagonists?
Which muscarinic agonist is mentioned in the context of parasympathetic activity?
Which muscarinic agonist is mentioned in the context of parasympathetic activity?
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?
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?
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?
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?
What is the primary therapeutic use of metoprolol in clinical practice?
What is the primary therapeutic use of metoprolol in clinical practice?
In treating hyperthyroidism, which effect do beta blockers like propranolol exhibit?
In treating hyperthyroidism, which effect do beta blockers like propranolol exhibit?
Flashcards
Adrenergic Receptors
Adrenergic Receptors
Neuroreceptors that bind to norepinephrine (NE) and epinephrine, triggering various physiological responses.
Alpha1 Adrenergic Receptors
Alpha1 Adrenergic Receptors
Cause vasoconstriction, increased blood pressure, and mydriasis (pupil dilation).
Alpha2 Adrenergic Receptors
Alpha2 Adrenergic Receptors
Inhibit NE release and insulin release.
Beta1 Adrenergic Receptors
Beta1 Adrenergic Receptors
Cause tachycardia (increased heart rate), increased lipolysis, and increased myocardial contractility.
Signup and view all the flashcards
Beta2 Adrenergic Receptors
Beta2 Adrenergic Receptors
Cause vasodilation, bronchodilation, and relaxation of uterine smooth muscle.
Signup and view all the flashcards
Direct-Acting Adrenergic Drugs
Direct-Acting Adrenergic Drugs
Drugs that directly bind and activate adrenergic receptors.
Signup and view all the flashcards
Indirect-Acting Adrenergic Drugs
Indirect-Acting Adrenergic Drugs
Drugs that cause the release of norepinephrine (NE).
Signup and view all the flashcards
Mixed-Action Adrenergic Drugs
Mixed-Action Adrenergic Drugs
Drugs that directly activate adrenergic receptors and cause the release of NE.
Signup and view all the flashcards
Adrenoceptor Agonists
Adrenoceptor Agonists
Drugs that activate adrenoceptors, mimicking the effects of norepinephrine (NE) and epinephrine (EP).
Signup and view all the flashcards
Beta 2 Receptors
Beta 2 Receptors
Stimulation causes relaxation of smooth muscles in the lungs, uterus, and blood vessels.
Signup and view all the flashcards
Dopamine Receptors
Dopamine Receptors
Located in the kidneys and other areas; cause dilation of blood vessels and decreased blood pressure.
Signup and view all the flashcards
Sympathomimetic Drugs
Sympathomimetic Drugs
Drugs that mimic the actions of norepinephrine (NE) and epinephrine (EP).
Signup and view all the flashcards
Indirect Agonists
Indirect Agonists
Drugs that release norepinephrine (NE) from nerve terminals, having widespread, nonspecific effects.
Signup and view all the flashcards
Sympathomimetics
Sympathomimetics
Drugs that mimic the effects of the sympathetic nervous system (SNS) by activating adrenergic receptors.
Signup and view all the flashcards
What is the effect of activating Adenylate Cyclase?
What is the effect of activating Adenylate Cyclase?
Adenylate cyclase converts ATP to cAMP, which activates kinases, leading to phosphorylation and ultimately muscle contraction.
Signup and view all the flashcards
What is the difference between Alpha and Beta Adrenergic Receptors?
What is the difference between Alpha and Beta Adrenergic Receptors?
Alpha receptors are primarily involved in vasoconstriction and other responses while Beta receptors are involved in bronchodilation, increased heart rate and other responses.
Signup and view all the flashcards
What are some examples of sympathomimetic medications?
What are some examples of sympathomimetic medications?
Examples include epinephrine, norepinephrine, dopamine, phenylephrine, albuterol, and many others.
Signup and view all the flashcards
Alpha 1 Agonist Action
Alpha 1 Agonist Action
Alpha 1 agonists primarily cause vasoconstriction, leading to increased blood pressure and potential for nasal decongestion.
Signup and view all the flashcards
Phenylephrine
Phenylephrine
A classic alpha 1 agonist used for nasal decongestion, it directly activates alpha 1 receptors causing vasoconstriction in the nasal passages.
Signup and view all the flashcards
Isoproterenol (Isuprel®)
Isoproterenol (Isuprel®)
This drug is a potent beta 1 and beta 2 agonist, widely used in emergency situations due to its strong effect on the heart and lungs.
Signup and view all the flashcards
Beta 2 Agonist Use
Beta 2 Agonist Use
Beta 2 agonists are the primary treatment for acute asthmatic bronchoconstriction. Their action relaxes airway smooth muscle, opening up the airways.
Signup and view all the flashcards
Albuterol (Proventil®)
Albuterol (Proventil®)
A commonly used beta 2 agonist, it relieves bronchoconstriction and improves breathing in asthma patients by selectively activating beta 2 receptors.
Signup and view all the flashcards
Epinephrine in Anaphylaxis
Epinephrine in Anaphylaxis
Epinephrine is the drug of choice to treat anaphylactic shock, a severe allergic reaction. It acts by stimulating both alpha and beta receptors to counteract the life-threatening symptoms.
Signup and view all the flashcards
Clonidine (Catapres®)
Clonidine (Catapres®)
This alpha 2 agonist acts in the central nervous system (CNS) to lower blood pressure by reducing the release of norepinephrine.
Signup and view all the flashcards
Midodrine (ProAmatine®)
Midodrine (ProAmatine®)
A direct-acting alpha 1 agonist that increases blood pressure by constricting blood vessels.
Signup and view all the flashcards
Adrenoceptor Agonists: CNS
Adrenoceptor Agonists: CNS
Drugs that stimulate adrenergic receptors in the central nervous system (CNS), often used for weight loss, attention deficit disorder, narcolepsy, and sometimes abused for mood-altering effects.
Signup and view all the flashcards
Adrenoceptor Agonists: Eye
Adrenoceptor Agonists: Eye
Drugs that stimulate adrenergic receptors in the eye, used to reduce conjunctival itching caused by allergies (phenylephrine) and treat glaucoma (epinephrine).
Signup and view all the flashcards
Adrenoceptor Agonists: Genitourinary Tract
Adrenoceptor Agonists: Genitourinary Tract
Drugs that stimulate adrenergic receptors in the genitourinary tract, primarily beta 2 agonists used to suppress premature labor (ritodrine, terbutaline) and alpha agonists (like ephedrine) to improve urinary continence.
Signup and view all the flashcards
Sympathomimetics: Cardiovascular Effects
Sympathomimetics: Cardiovascular Effects
Drugs that mimic the sympathetic nervous system, affecting blood vessels (alpha for constriction, beta 2 for relaxation), heart (beta 1 for increased heart rate and contractility), and blood pressure (alpha raises, beta lowers).
Signup and view all the flashcards
Sympathomimetics: Eye Effects
Sympathomimetics: Eye Effects
Drugs that mimic the sympathetic nervous system, affecting the eye by increasing aqueous humor outflow (alpha) and decreasing its production (beta), influencing eye pressure.
Signup and view all the flashcards
Sympathomimetics: Respiratory Effects
Sympathomimetics: Respiratory Effects
Drugs that mimic the sympathetic nervous system, affecting the respiratory system primarily through beta 2 receptors, causing relaxation of bronchial smooth muscle, leading to bronchodilation.
Signup and view all the flashcards
Sympathomimetics: GI Effects
Sympathomimetics: GI Effects
Drugs that mimic the sympathetic nervous system, affecting the gastrointestinal (GI) tract by relaxing smooth muscles (beta) and decreasing acetylcholine release (alpha 2), affecting digestion and motility.
Signup and view all the flashcards
Sympathomimetics: Other Effects
Sympathomimetics: Other Effects
Drugs that mimic the sympathetic nervous system, affecting various systems including the uterus (beta for relaxation, alpha for contraction), exocrine glands (controlling secretions), and fat cells (increasing lipolysis).
Signup and view all the flashcards
Epinephrine (Adrenaline)
Epinephrine (Adrenaline)
A potent vasoconstrictor and cardiac stimulant that increases blood pressure.
Signup and view all the flashcards
Norepinephrine
Norepinephrine
Similar effects to epinephrine, but slightly less potent.
Signup and view all the flashcards
Isoproterenol
Isoproterenol
A strong beta agonist, primarily affecting beta receptors. Dilates blood vessels.
Signup and view all the flashcards
How do Sympathomimetics Raise Blood Pressure?
How do Sympathomimetics Raise Blood Pressure?
Direct-acting drugs like phenylephrine or methoxamine increase blood pressure by constricting blood vessels.
Signup and view all the flashcards
Sympathomimetics for Anaphylaxis
Sympathomimetics for Anaphylaxis
Epinephrine (EP) is used to counter the effects of anaphylaxis by reversing low blood pressure, bronchospasm, and congestion.
Signup and view all the flashcards
General Cardiovascular Adverse Effects of Sympathomimetics
General Cardiovascular Adverse Effects of Sympathomimetics
These drugs can lead to hypertension, increased risk of heart problems, and cardiac failure.
Signup and view all the flashcards
Sympathomimetics and the CNS
Sympathomimetics and the CNS
Only drugs like cocaine and amphetamine can cross the blood-brain barrier easily, leading to central nervous system side effects.
Signup and view all the flashcards
Alpha Antagonists
Alpha Antagonists
Drugs that block alpha receptors, primarily found on vascular smooth muscle, leading to a decrease in blood pressure.
Signup and view all the flashcards
Phentolamine
Phentolamine
Non-selective alpha antagonist that blocks both alpha 1 and alpha 2 receptors, used to lower blood pressure and treat pheochromocytoma.
Signup and view all the flashcards
Epinephrine Reversal
Epinephrine Reversal
A phenomenon where activating alpha and beta receptors in the same tissue leads to opposing effects on blood pressure. For example, epinephrine increases blood pressure by activating both alpha and beta receptors, but a selective alpha 1 antagonist blocks both alpha and beta actions of epinephrine, resulting in lowered blood pressure.
Signup and view all the flashcards
Pheochromocytoma
Pheochromocytoma
A tumor of the sympathetic nervous system that produces excessive norepinephrine and epinephrine, leading to hypertensive crisis.
Signup and view all the flashcards
Alpha 2 Agonists
Alpha 2 Agonists
Drugs that activate alpha 2 receptors, ultimately reducing sympathetic outflow from the brain and norepinephrine release from neurons, lowering blood pressure.
Signup and view all the flashcards
Clonidine
Clonidine
An alpha 2 agonist used to treat hypertension by reducing sympathetic activity.
Signup and view all the flashcards
Sympatholytics
Sympatholytics
Drugs that reduce sympathetic activity, generally by blocking adrenergic receptors.
Signup and view all the flashcards
Alpha 1 Selective Antagonists
Alpha 1 Selective Antagonists
Drugs that specifically block alpha 1 receptors, leading to vasodilation and lower blood pressure.
Signup and view all the flashcards
What are Sympatholytics?
What are Sympatholytics?
Drugs that block the effects of the sympathetic nervous system by antagonizing adrenergic receptors. They can be selective for specific receptor subtypes or non-selective, affecting multiple receptors.
Signup and view all the flashcards
What is Pheochromocytoma?
What is Pheochromocytoma?
A tumor of the adrenal medulla that releases excessive amounts of catecholamines (epinephrine and norepinephrine), causing high blood pressure, sweating, palpitations, and headaches.
Signup and view all the flashcards
What are Non-Selective Alpha Antagonists used for?
What are Non-Selective Alpha Antagonists used for?
These drugs are primarily used for treating Pheochromocytoma, a rare tumor. They are not selective and block both alpha 1 and alpha 2 receptors.
Signup and view all the flashcards
What are Alpha-1 Selective Antagonists used for?
What are Alpha-1 Selective Antagonists used for?
These drugs are used for treating hypertension and benign prostatic hyperplasia (BPH). They specifically block alpha 1 receptors, which are linked to vasoconstriction and prostate function.
Signup and view all the flashcards
What are Beta Antagonists used for?
What are Beta Antagonists used for?
These drugs are used for treating various conditions, including hypertension, ischemic heart disease, and neurological disorders. They block beta receptors, affecting heart rate, blood pressure, and other bodily functions.
Signup and view all the flashcards
What's the difference between Reversible and Irreversible Alpha Antagonists?
What's the difference between Reversible and Irreversible Alpha Antagonists?
Reversible alpha antagonists have a duration of action tied to their half-life, while irreversible alpha antagonists form a strong bond with the receptor and their effects last for days. They require new receptor synthesis to restore function.
Signup and view all the flashcards
Which drug is used to stabilize patients before surgery for Pheochromocytoma?
Which drug is used to stabilize patients before surgery for Pheochromocytoma?
Phenoxybenzamine is an irreversible alpha blocker used pre-operatively to control the high blood pressure and other symptoms caused by the tumor's catecholamine release.
Signup and view all the flashcards
What is Phentolamine used for?
What is Phentolamine used for?
Phentolamine is a reversible alpha blocker that is used to treat hypertensive episodes associated with Pheochromocytoma. It can also be administered intravenously to reverse the effects of alpha agonists.
Signup and view all the flashcards
Pheochromocytoma Location
Pheochromocytoma Location
A tumor most often found in the adrenal gland that releases excessive amounts of norepinephrine and epinephrine, causing high blood pressure, sweating, palpitations, and headaches.
Signup and view all the flashcards
Pheochromocytoma Symptoms
Pheochromocytoma Symptoms
A condition characterized by high blood pressure, sweating, palpitations, and headaches due to excessive release of norepinephrine and epinephrine from a tumor in the adrenal gland.
Signup and view all the flashcards
Alpha Blockers and Blood Pressure?
Alpha Blockers and Blood Pressure?
Alpha blockers cause vasodilation, leading to a decrease in blood pressure. This effect is more pronounced when standing due to the increased need for norepinephrine to maintain blood pressure.
Signup and view all the flashcards
Alpha Blockers Side Effects
Alpha Blockers Side Effects
Alpha blockers can cause postural hypotension (low blood pressure upon standing) and reflex tachycardia (increased heart rate as a response to lowered blood pressure).
Signup and view all the flashcards
Phenoxybenzamine
Phenoxybenzamine
An irreversible alpha blocker with a long duration of action (14-48+ hours), used to treat pheochromocytoma and other conditions.
Signup and view all the flashcards
Prazosin
Prazosin
A selective alpha 1 blocker with a relatively low incidence of tachycardia, used to treat hypertension and benign prostatic hyperplasia (BPH).
Signup and view all the flashcards
Terazosin
Terazosin
A reversible alpha 1 antagonist with a long half-life, used to treat hypertension and benign prostatic hyperplasia (BPH).
Signup and view all the flashcards
Doxazosin
Doxazosin
A long-acting alpha 1 blocker with a half-life of 22 hours, used to treat hypertension and benign prostatic hyperplasia (BPH).
Signup and view all the flashcards
Beta Blockers: Cardiovascular Action
Beta Blockers: Cardiovascular Action
Beta blockers decrease blood pressure by reducing heart rate, constricting blood vessels, and inhibiting the renin-angiotensin system.
Signup and view all the flashcards
Beta Blockers: Respiratory Action
Beta Blockers: Respiratory Action
Beta blockers can cause airway constriction by blocking the beta 2 receptors. Selective beta 1 blockers have less effect on the lungs.
Signup and view all the flashcards
Beta Blockers: Eye Action
Beta Blockers: Eye Action
Beta blockers increase pressure in the eye, potentially leading to glaucoma. They are also used topically to treat glaucoma.
Signup and view all the flashcards
Beta Blockers: Metabolic Effects
Beta Blockers: Metabolic Effects
Beta blockers can inhibit lipolysis (fat breakdown) and reduce glycogenolysis in the liver. Caution is advised with diabetes patients.
Signup and view all the flashcards
Beta Blockers: Common Uses
Beta Blockers: Common Uses
Beta blockers are widely used to treat hypertension, ischemic heart disease, cardiac arrhythmias, and glaucoma.
Signup and view all the flashcards
Beta Blockers: Neurological Uses
Beta Blockers: Neurological Uses
Beta blockers, especially propranolol, are used to treat migraines and other neurological conditions.
Signup and view all the flashcards
Propranolol
Propranolol
The first beta blocker drug, non-selective, with numerous effects on the central nervous system.
Signup and view all the flashcards
Timolol
Timolol
A non-selective beta blocker used topically for the treatment of glaucoma.
Signup and view all the flashcards
Alpha Blockers: Clinical Use
Alpha Blockers: Clinical Use
Alpha blockers are used primarily to treat hypertension (high blood pressure) and pheochromocytoma (a tumor that releases excessive catecholamines).
Signup and view all the flashcards
Beta Blockers: Clinical Use
Beta Blockers: Clinical Use
Beta blockers are used to treat hypertension, angina (chest pain), heart failure, and other conditions associated with the cardiovascular system. They are also used to manage stage fright.
Signup and view all the flashcards
Non-selective Beta Blockers: Risks
Non-selective Beta Blockers: Risks
Non-selective beta blockers can worsen asthma due to their blocking of beta-2 receptors in the lungs, and they can exacerbate hypoglycemia in insulin-dependent patients.
Signup and view all the flashcards
Beta Blockers: CNS Effects
Beta Blockers: CNS Effects
Beta blockers, particularly non-selective and high lipid-soluble ones, can cause CNS side effects like sedation, sleep disturbance, and depression.
Signup and view all the flashcards
Reversible vs. Irreversible Alpha Blockers
Reversible vs. Irreversible Alpha Blockers
Reversible alpha blockers have a duration of action tied to their half-life, while irreversible alpha blockers form a strong bond with the receptor and their effects last for days. They require new receptor synthesis to restore function.
Signup and view all the flashcards
What are beta blockers?
What are beta blockers?
Drugs that block beta receptors, resulting in effects such as reduced heart rate, blood pressure control, and other physiological changes.
Signup and view all the flashcards
What are beta blockers used for?
What are beta blockers used for?
Beta blockers are widely used for conditions like hypertension, angina, heart failure, and even to manage stage fright.
Signup and view all the flashcards
What are alpha blockers used for?
What are alpha blockers used for?
Alpha blockers are primarily used to treat hypertension and pheochromocytoma, a tumor that releases excessive catecholamines.
Signup and view all the flashcards
What are the effects of beta blockers on the heart?
What are the effects of beta blockers on the heart?
Beta blockers decrease heart rate and blood pressure by blocking beta receptors in the heart.
Signup and view all the flashcards
What are the effects of alpha blockers on blood vessels?
What are the effects of alpha blockers on blood vessels?
Alpha blockers cause vasodilation (widening of blood vessels) leading to a decrease in blood pressure.
Signup and view all the flashcards
What are some examples of beta blockers?
What are some examples of beta blockers?
Common beta blockers include propranolol, atenolol, metoprolol, and timolol. Each has specific properties and uses.
Signup and view all the flashcardsStudy Notes
Pharmacology I, Chapter 9: NE Agonists (Sympathomimetics)
-
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.
-
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.
-
Catecholamines: Adrenergic neurotransmitters include norepinephrine, epinephrine, and dopamine. Chemical structures of each are shown.
-
Adrenergic Neurotransmitter Discovery: J. Axelrod (1912-2004) won the Nobel Prize in 1970 for discovering the uptake and release of catecholamine neurotransmitters.
-
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).
-
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)
-
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.
-
NE at Adrenergic Neurons: Steps 1-6 in the synthesis, storage, release, receptor binding, re-uptake, and removal of NE from the synapse.
-
Adrenergic Receptors: Alpha1: Actions include vasoconstriction, increased peripheral resistance, increased blood pressure (BP), mydriasis, increased closure of the bladder sphincter.
-
Adrenergic Receptors: Alpha2: Actions include inhibition of NE release, inhibition of insulin release.
-
Adrenergic Receptors: Beta1: Actions include tachycardia, increased lipolysis, increased myocardial contractility, increased renin release.
-
Adrenergic Receptors: Beta2: Actions include vasodilation, decreased peripheral resistance, bronchodilation, relaxation of uterine smooth muscle.
-
Adrenoceptor Agonists & Sympathomimetics Drugs (Table 9-1): This table lists receptor type, agonist, antagonist, G protein, effects, and chromosome location. (Detailed Table)
-
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).
-
Adrenergic Drugs (Mixed Action): This category includes drugs with both direct- and indirect-acting effects (e.g., ephedrine, metaraminol).
-
Cardiac Innervation: Parasympathetic (ACh) and sympathetic (NE) systems. NE causes constriction (+), ACh causes relaxation (-). Diagram also presents blood vessels and the heart.
-
Sympathomimetics: This section explains the categories and different type of drugs.
-
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)
-
Distribution of adrenoceptor subtypes (Table 9-3): Details on the presence and actions of receptor subtypes on various tissues and organs. (Detailed Table)
-
Alpha 1 Receptors: Locations (vascular smooth muscle, pupil dilator muscle, pilomotor smooth muscle), effect of activation (contraction).
-
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)
-
Beta 1 Receptors: Location (heart, juxtaglomerular cells), effect of activation (increase heart rate/force).
-
Beta 2 Receptors: Location (smooth muscle, skeletal muscle, liver), effect of activation (muscle relaxation, glycogenolysis).
-
Dopamine Receptors: Locations and functions. Different types and effects. Activation stimulates adenyl cyclase and increases cAMP second messenger.
-
Receptor Desensitization: Repeated exposure leads to a decrease in receptor response. There are homologous (in the exposed receptor) and heterologous (in other receptors) forms
-
Points to Remember: Important features and locations of Alpha 1, Beta 1, and Beta 2 receptors highlighted, summarizing their functions.
-
Pharmacokinetics of Isoproterenol/Methoxamine: Includes information on absorption and distribution depending on substitutions in the chemical structure.
-
Beta Agonists (Table): A table with examples, receptor subtypes, and clinical effects. List includes examples of drug names.
-
Alpha Receptor Agonists (Table): Another table with examples, receptor subtypes, and clinical effects. List includes example of drug names.
-
Anaphylaxis: Epinephrine is the treatment of choice.
-
Bronchi (asthma): Beta agonists (mostly Beta 2) treat acute asthmatic bronchoconstriction with short-acting examples such as terbutaline, albuterol, and metaproterenol.
-
Cardiovascular: NE increases blood flow in acute heart failure and some types of shock. Beta 1 agonists useful here.
-
CNS effects of Amphetamines: Weight loss, attention-deficit disorder, narcolepsy, mood altering effects.
-
Eye drug effects: Alpha agonists are used topically for conjunctival itching and for glaucoma.
-
Genitourinary Tract: Beta 2 agonists used to suppress premature labor and ephedrine for continence problems. Alpha receptors are also involved in the bladder.
-
Summary I and Summary 2: These pages include summary points on various aspects of adrenergic agonists, and how to organize, classify, or categorize them.
-
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.
-
Specific Sympathomimetic Drugs: Clinically relevant drugs, their classifications, and use cases described more specifically.
-
Selective Sympathomimetics: Including dexmedetomidine, tyramine, and others, based on specificity and use.
-
Clonidine (Catapres®): An alpha 2 agonist, lowering sympathetic outflow, reducing heart rate, and having multiple functions with a presynaptic/postsynaptic effect.
-
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.
-
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.
-
Epinephrine (Adrenalin): Potent vasoconstrictor and cardiac stimulant, increasing blood pressure.
-
Norepinephrine: Similar effects to epinephrine.
-
Isoproterenol: Potent beta agonist primarily, with limited effect on alpha receptors, and a potent vasodilator effect.
-
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.
-
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).
-
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.
-
Agonist Drug Binding Mechanism: Detailed mechanism to achieve activation (e.g., activation of G proteins and cAMP, downstream signaling pathways).
Studying That Suits You
Use AI to generate personalized quizzes and flashcards to suit your learning preferences.