p.32
Treatment of Hypertension and Heart Conditions
What are some secondary agents for hypertension management?
α1 antagonists, β-blockers, α2 agonists, loop diuretics, and potassium-sparing diuretics.
p.4
Norepinephrine Metabolism and Stability
Which enzymes metabolize norepinephrine?
COMT (Catechol-O-methyltransferase) and MAO (Monoamine oxidase).
p.7
Direct-Acting Adrenergic Agonists
What are some clinical applications of Epinephrine?
Used in nasal spray for rhinitis and for hypotension.
p.15
Prodrugs and Their Mechanisms
What is the role of prodrugs in pharmacology?
They undergo enzymatic and/or chemical transformation to exert the desired pharmacologic effect.
p.5
Norepinephrine Metabolism and Stability
What are the primary metabolites of norepinephrine?
Dihydroxyphenylglycol (DHPG) and vanillylmandelic acid (VMA).
What is the significance of clinically useful mustards?
They are a class of alkylating agents used in cancer treatment.
p.8
Norepinephrine Metabolism and Stability
What can ortho-quinone react with?
DNA, protein, GSH, and others.
p.9
Clinical Applications of Epinephrine
What is a common effect of poison IV on the body?
It can lead to severe toxicity and potentially fatal outcomes.
p.3
α and β Adrenergic Receptor Functions
What receptors does norepinephrine primarily act on?
Alpha and beta adrenergic receptors.
p.3
Sympathetic Nervous System Functions
What is the role of norepinephrine in the body?
To prepare the body for 'fight or flight' responses.
p.7
Direct-Acting Adrenergic Agonists
What effect does Epinephrine have on blood vessels in the mucous membranes?
Causes vasoconstriction and reduces nasal congestion.
p.54
α and β Adrenergic Receptor Functions
What are common side effects of alpha blockers?
Dizziness, fainting, low blood pressure, and sudden blood pressure changes when standing after sitting.
p.5
Norepinephrine Metabolism and Stability
What happens to norepinephrine after it is released into the synaptic cleft?
It can bind to receptors, be reabsorbed by neurons, or be metabolized.
p.56
β Blockers and Their Therapeutic Uses
What are β blockers also known as?
β-adrenergic blocking agents.
p.27
Adrenergic Drug Mechanisms
What is the role of 2-Arylimidazoline?
Used as nasal decongestants.
p.3
Clinical Applications of Epinephrine
What effect does norepinephrine have on blood vessels?
It causes vasoconstriction, increasing blood pressure.
p.7
Direct-Acting Adrenergic Agonists
How is Epinephrine formulated for stability?
In combination with antioxidants and must be stored away from light.
p.54
α and β Adrenergic Receptor Functions
What condition can cause sudden blood pressure changes when standing?
Orthostatic hypotension, which is a concern with alpha blockers.
p.6
α and β Adrenergic Receptor Functions
What happens when norepinephrine binds to α2 receptors?
It inhibits further release of norepinephrine, serving as a negative feedback mechanism.
p.9
Clinical Applications of Epinephrine
What should be done in case of a poison IV exposure?
Seek immediate medical attention.
What type of medication is Claritin-D?
An allergy and congestion medication.
p.3
Norepinephrine Metabolism and Stability
What is the significance of norepinephrine in mood regulation?
It plays a role in mood and arousal, affecting conditions like depression.
p.51
Clinical Applications of Epinephrine
What conditions is 5.13 mainly used to treat?
Chronic lymphocytic leukemia and lymphomas.
p.41
Direct-Acting Adrenergic Agonists
How long do the bronchodilation effects of inhaled adrenergic agonists last?
Duration can range from 4 to 12 hours, depending on the specific agonist.
p.41
Direct-Acting Adrenergic Agonists
What factors can influence the onset and duration of bronchodilation from inhaled adrenergic agonists?
Type of agonist, dosage, and individual patient response.
p.16
Direct-Acting Adrenergic Agonists
What type of activity do α 1 selective adrenergic receptor agonists have?
Vasoconstrictor/vasopressor activity.
p.25
Clinical Applications of Epinephrine
What are some clinical uses of α2 agonists?
Antihypertensive, treatment of glaucoma, sedative, and treatment of opiate dependence and alcohol withdrawal symptoms.
p.62
Mixed α/β Blockers and Their Applications
What type of adrenergic receptors do labetalol and carvedilol block?
Both α1- and β-adrenergic receptors.
p.32
Treatment of Hypertension and Heart Conditions
What are the first-line therapies recommended by the ACC/AHA for managing hypertension?
Thiazide diuretics, calcium channel blockers, and angiotensin-converting enzymes or angiotensin receptor blockers.
In what forms does Claritin-D come?
12-hour and 24-hour tablets.
p.5
Norepinephrine Metabolism and Stability
Where is norepinephrine primarily produced?
In the adrenal medulla and sympathetic nerve endings.
p.5
Norepinephrine Metabolism and Stability
What is the role of catechol-O-methyltransferase (COMT) in norepinephrine metabolism?
It metabolizes norepinephrine in the synaptic cleft.
p.5
Norepinephrine Metabolism and Stability
How does norepinephrine affect the body?
It increases heart rate, blood pressure, and blood flow to muscles.
p.11
Clinical Applications of Epinephrine
What potential adverse effects of epinephrine should John be counseled about?
Increased or irregular heartbeat, sweating, weakness, shakiness, paleness, anxiety, dizziness, breathing problems, or nausea.
p.56
β Blockers and Their Therapeutic Uses
When are β blockers not recommended as a first treatment?
In people who have only high blood pressure.
p.35
β Blockers and Their Therapeutic Uses
What is a key difference between selective and non-selective β blockers?
Selective β blockers have less effect on bronchoconstriction compared to non-selective β blockers.
p.38
Treatment of Hypertension and Heart Conditions
What are the two types of β agonists used in COPD/asthma treatment?
Short-acting and long-acting β agonists.
p.59
β Blockers and Their Therapeutic Uses
How does Metoprolol affect the risk of death after a heart attack?
It may lower the risk of death after a heart attack.
p.9
Clinical Applications of Epinephrine
What is the primary route of administration for poison IV?
Intravenous (IV) injection.
p.9
Clinical Applications of Epinephrine
What is a potential treatment for poison IV exposure?
Administration of antidotes or supportive care.
p.32
Treatment of Hypertension and Heart Conditions
What should patients with stage II hypertension be started on?
Two medications from different classes.
p.3
Sympathetic Nervous System Functions
Where is norepinephrine primarily released?
From sympathetic nerve endings.
p.4
Norepinephrine Metabolism and Stability
Why is norepinephrine not typically used as a drug?
Because it is metabolically unstable.
Is Claritin-D available over-the-counter?
Yes, but it must be obtained from the pharmacist.
p.6
α and β Adrenergic Receptor Functions
Where are α2-adrenergic receptors primarily located?
On the presynaptic neuron.
p.8
Norepinephrine Metabolism and Stability
What happens to epinephrine and other catechols in the presence of oxygen and oxidizing agents?
They quickly decompose to inactive quinones.
p.8
Norepinephrine Metabolism and Stability
How are catechol-containing drugs stabilized?
With antioxidants and dispensed in air-tight amber containers.
p.12
α and β Adrenergic Receptor Functions
What does an α1 agonist stimulate?
Phospholipase C activity.
p.25
Sympathetic Nervous System Functions
How do α2 agonists affect the brainstem?
They reduce CNS activation mediated by the vasomotor center.
p.16
Direct-Acting Adrenergic Agonists
What is the significance of the imidazoline ring in arylimidazoline agonists?
It has a pKa range of 10 - 11.
p.12
Direct-Acting Adrenergic Agonists
What are the two types of α1 selective adrenergic receptor agonists?
Phenylethanolamine and 2-arylimidazoline analogues.
p.56
β Blockers and Their Therapeutic Uses
Under what circumstances are β blockers usually prescribed for high blood pressure?
When other medications, such as diuretics, haven't worked well.
p.16
Direct-Acting Adrenergic Agonists
What is the nature of arylimidazoline adrenergic agonists?
They are highly ionic in nature.
p.64
β Blockers and Their Therapeutic Uses
In what form is Levobunolol administered?
Topically in the form of eye drops.
p.22
Clinical Applications of Epinephrine
What is the primary function of antihistamines?
To block the action of histamine and reduce allergy symptoms.
p.61
β Blockers and Their Therapeutic Uses
How does atenolol differ from practolol?
Atenolol does not possess severe oculomucocutaneous side effects.
p.22
Clinical Applications of Epinephrine
What are some side effects of antihistamines?
Drowsiness, dry mouth, and dizziness.
p.36
Direct-Acting Adrenergic Agonists
What activity does the S - (−) - enantiomer of dobutamine exhibit?
β 1 - agonist activity and is also an α 1 - agonist and vasopressor.
p.3
Norepinephrine Metabolism and Stability
What is norepinephrine?
A neurotransmitter involved in the sympathetic nervous system.
p.7
Direct-Acting Adrenergic Agonists
What is the oral bioavailability of Epinephrine (EPI)?
Poor, due to extensive metabolism by MAO and COMT.
p.52
Norepinephrine Metabolism and Stability
What is the most nucleophilic atom in DNA?
The N-7 nitrogen of guanine.
p.15
Prodrugs and Their Mechanisms
What are prodrugs?
Bioreversible derivatives of drug molecules that transform in vivo to release the active parent drug.
p.24
α and β Adrenergic Receptor Functions
What does the activation of α2-adrenoreceptor inhibit?
The enzyme adenylate cyclase.
What type of agent is 5.13?
An orally administered alkylating agent.
p.24
Sympathetic Nervous System Functions
What physiological effects result from the activation of α2-adrenoreceptors?
Induces smooth muscle and blood vessel constriction, reducing blood pressure.
p.11
Clinical Applications of Epinephrine
What symptoms of anaphylaxis should John be aware of?
Trouble breathing, wheezing, facial swelling, throat closing, fast heartbeat, anxiousness, or hives.
p.12
α and β Adrenergic Receptor Functions
What are the effects of α1 agonists?
Vasoconstriction and mydriasis.
p.1
Sympathetic Nervous System Functions
What are adrenergic drugs primarily used for?
They are used to mimic the effects of the sympathetic nervous system.
p.2
Sympathetic Nervous System Functions
What effect does the sympathetic nervous system have on the pupils?
It enlarges the pupils to let more light in and improve vision.
p.1
Adrenergic Drug Mechanisms
What is the significance of medicinal chemistry in the development of adrenergic drugs?
It involves the design and optimization of drugs that target adrenergic receptors.
p.59
β Blockers and Their Therapeutic Uses
What is the main difference between Metoprolol tartrate and Metoprolol succinate?
Metoprolol tartrate is an immediate-release tablet taken several times a day, while Metoprolol succinate is an extended-release tablet taken once a day.
p.2
Sympathetic Nervous System Functions
What effect does the sympathetic nervous system have on digestion?
It slows down digestion to divert energy to other areas of the body.
p.2
Sympathetic Nervous System Functions
How does the sympathetic nervous system affect the liver?
It activates energy stores in the liver for quick use.
p.61
β Blockers and Their Therapeutic Uses
What modification led to the discovery of atenolol?
Replacement of the acetamide -NHCOCH3 with -CH2CONH2 at the para position.
p.67
Treatment of Hypertension and Heart Conditions
What are the possible reasons for the patient's pulmonary congestion and peripheral edema?
Worsening heart failure, non-adherence to a low-salt diet, or not taking diuretics as prescribed.
p.36
Direct-Acting Adrenergic Agonists
What happens when the racemate of dobutamine is used clinically?
The α - effects of the enantiomers cancel each other, leaving primarily the β 1 - effects.
p.20
Norepinephrine Metabolism and Stability
Why is ephedrine not metabolized by MAO?
Due to the presence of an α-methyl group that hinders metabolism.
p.54
α and β Adrenergic Receptor Functions
Who should not be prescribed alpha blockers?
Patients with a history of orthostatic hypotension, heart failure, liver or kidney problems, or Parkinson’s disease.
p.11
Clinical Applications of Epinephrine
What should John do after removing the EpiPen?
Massage the injection site for an additional 10 seconds.
p.25
α and β Adrenergic Receptor Functions
What is the primary action of α2 agonists?
Inhibit adenylyl cyclase activity.
p.35
β Blockers and Their Therapeutic Uses
What is the therapeutic use of β3 agonists?
Treatment of overactive bladder.
p.31
Treatment of Hypertension and Heart Conditions
How can high blood pressure be managed?
Through lifestyle changes, medication, and regular monitoring.
p.1
α and β Adrenergic Receptor Functions
What is the role of adrenergic receptors?
They mediate the effects of catecholamines like epinephrine and norepinephrine.
p.56
β Blockers and Their Therapeutic Uses
What conditions are β blockers used to treat?
Irregular heart rhythm, heart failure, chest pain, heart attacks, migraine, certain types of tremors, and glaucoma.
p.2
Sympathetic Nervous System Functions
How does the sympathetic nervous system affect the heart?
It increases the heart rate to improve the delivery of oxygen to the body.
p.1
Direct-Acting Adrenergic Agonists
How do adrenergic agonists function?
They activate adrenergic receptors to produce physiological responses.
p.16
Clinical Applications of Epinephrine
In what preparations are arylimidazoline agonists widely used?
Topical preparations as nasal decongestants and eye drops.
p.58
β Blockers and Their Therapeutic Uses
What is the chemical structure of the majority of clinically available selective β 1 - blockers?
Aryloxypropanolamine derivatives.
p.62
β Blockers and Their Therapeutic Uses
What unique group does sotalol contain?
A sulfonamide group at the para position.
p.58
β Blockers and Their Therapeutic Uses
What type of substitutions do most selective β 1 - blockers have?
Substitutions at the para position.
p.20
Adrenergic Drug Mechanisms
What is the mechanism of action for mixed-acting sympathomimetics?
They bind to both α- and β-adrenoceptors and increase NE concentration through displacing NE or reuptake inhibition.
p.65
β Blockers and Their Therapeutic Uses
What is Carvedilol primarily used to treat?
Congestive heart failure.
p.55
β Blockers and Their Therapeutic Uses
What is the role of β3 agonists?
Treatment of overactive bladder.
p.50
Mixed α/β Blockers and Their Applications
What is the administration route for phentolamine?
Usually administered intravenously.
p.10
Clinical Applications of Epinephrine
What is bradycardia?
A type of arrhythmia where the heart beats slower than 60 beats per minute.
p.43
β Blockers and Their Therapeutic Uses
What are long-acting β2 agonists used for?
Prophylaxis and treatment of asthma and COPD.
p.67
Treatment of Hypertension and Heart Conditions
What alternative is suggested if a calcium channel blocker is needed for angina?
A dihydropyridine calcium channel blocker with minimal effects on left ventricular function.
p.28
Adrenergic Drug Mechanisms
What does the phenyl ring require for activity in guanfacine and guanabenz?
At least one ortho chlorine or methyl group.
p.3
Norepinephrine Metabolism and Stability
How is norepinephrine metabolized in the body?
Through reuptake into nerve terminals and enzymatic degradation.
p.5
Norepinephrine Metabolism and Stability
What is norepinephrine?
A neurotransmitter and hormone involved in the body's 'fight or flight' response.
p.24
GPCR signaling mediated by cAMP
What is the effect of inactivating adenylate cyclase?
It leads to the inactivation of cyclic adenosine monophosphate (cAMP).
p.41
Direct-Acting Adrenergic Agonists
What is the onset time for bronchodilation effects of inhaled adrenergic agonists?
Typically within minutes.
p.6
α and β Adrenergic Receptor Functions
How does the activation of α2 receptors affect the protein Gs?
It produces an opposite effect compared to α1 receptors and causes negative feedback on the effect of protein Gs.
p.11
Clinical Applications of Epinephrine
What should John do if symptoms continue after the first EpiPen injection?
Use a second injection and seek emergency medical care.
p.56
β Blockers and Their Therapeutic Uses
What is the primary effect of β blockers?
They reduce blood pressure.
p.35
β Blockers and Their Therapeutic Uses
What is the role of selective β1 blockers?
They are preferred in patients with respiratory conditions due to reduced bronchoconstriction.
p.27
Adrenergic Drug Mechanisms
What is the role of 2-Aminoimidazoline?
Used in the treatment of hypertension and glaucoma.
p.16
Direct-Acting Adrenergic Agonists
What is essential for the activity of arylimidazoline adrenergic agonists?
Lipophilic substitution at the ortho position on the phenyl ring.
p.53
Adrenergic Drug Mechanisms
What is a key difference between tolazoline and α1-agonists?
Tolazoline lacks the lipophilic substituents required for agonist activity.
p.63
β Blockers and Their Therapeutic Uses
What type of adrenergic receptor antagonist is propranolol?
Non-selective β-adrenergic receptor antagonist.
p.38
Treatment of Hypertension and Heart Conditions
What are combination inhalers used for in COPD/asthma treatment?
They combine different classes of medications for better management.
p.18
Norepinephrine Metabolism and Stability
Which amino acids have side chains that can be negatively charged?
Aspartic acid (Asp) and Glutamic acid (Glu).
p.70
Norepinephrine Metabolism and Stability
What is Metyrosine's mechanism of action?
It is a competitive inhibitor of tyrosine hydroxylase, inhibiting catecholamine production.
p.22
Clinical Applications of Epinephrine
Why should decongestants be used with caution?
They can raise blood pressure and cause insomnia.
p.13
Adrenergic Drug Mechanisms
List two other α 1 selective adrenergic receptor agonists besides Phenylephrine.
Metaraminol and midodrine.
p.44
Clinical Applications of Epinephrine
What is Mirabegron?
An orally bioavailable β 3 adrenergic receptor agonist approved for overactive bladder.
p.37
Clinical Applications of Epinephrine
What are short-acting β2 adrenergic agonists used for?
Long-term treatment of obstructive airway diseases and asthma, and for treatment of acute bronchospasm.
p.46
α and β Adrenergic Receptor Functions
What are common side effects of Doxazosin?
Dizziness, sleepiness, swelling, nausea, shortness of breath, and abdominal pain.
p.60
β Blockers and Their Therapeutic Uses
What type of drug is Esmolol (Brevibloc)?
An ultrashort-acting selective β-blocker.
p.14
Treatment of Hypertension and Heart Conditions
What is Midodrine indicated for?
Symptomatic orthostatic hypotension.
p.47
α and β Adrenergic Receptor Functions
How does Alfuzosin work in the body?
By relaxing the muscles in the prostate and bladder neck, making it easier to urinate.
p.11
Clinical Applications of Epinephrine
What is the purpose of the EpiPen prescribed to John?
To treat emergency allergic reactions, specifically anaphylaxis.
What are β-Haloalkylamines?
Highly reactive alkylating agents present in nitrogen mustard anticancer agents.
p.27
Treatment of Hypertension and Heart Conditions
What are the primary treatment options for glaucoma?
Prostaglandin analogues, muscarinic agonists, β-blockers, adrenergic α-agonists, and carbonic anhydrases.
p.63
β Blockers and Their Therapeutic Uses
What conditions can propranolol treat?
High blood pressure, chest pain (angina), arrhythmias, migraine headaches, and anxiety.
p.12
Clinical Applications of Epinephrine
What are some clinical uses of α1 agonists?
Treatment of hypotension, nasal decongestants, and during eye exams.
p.59
β Blockers and Their Therapeutic Uses
What conditions can Metoprolol treat?
High blood pressure, chest pain (angina), and heart failure.
p.1
β Blockers and Their Therapeutic Uses
What is the therapeutic application of β blockers?
They are used to manage hypertension and heart conditions.
p.19
Norepinephrine Metabolism and Stability
What does pKa represent in relation to amines?
The acidity of the amine's conjugate acid.
p.50
Adrenergic Drug Mechanisms
What is a pheochromocytoma?
A vascular tumor of chromaffin tissue that produces and secretes norepinephrine and epinephrine.
p.44
β Blockers and Their Therapeutic Uses
What type of receptor does Vibegron act on?
Selective bladder β 3 adrenergic receptor (β 3 - AR).
p.20
Clinical Applications of Epinephrine
How do mixed-acting sympathomimetics compare to topical decongestants?
They have a slower onset but longer duration of action and do not cause nasal irritation or rebound congestion.
p.70
Clinical Applications of Epinephrine
What condition is Metyrosine used to help control?
Hypertensive episodes and symptoms of catecholamine overproduction in pheochromocytoma.
p.37
Direct-Acting Adrenergic Agonists
Name a few examples of short-acting β2 adrenergic agonists.
Metaproterenol, albuterol, Levalbuterol, Pirbuterol, Terbutaline, Isotharine, Fenoterol, Procaterol.
p.36
Norepinephrine Metabolism and Stability
How is dobutamine metabolized and what is its duration of action?
As a catechol, dobutamine is readily metabolized by COMT and has a short duration of action with no oral activity.
p.49
α and β Adrenergic Receptor Functions
What type of drug is Phenoxybenzamine?
A non-selective, irreversible α blocker.
p.14
Prodrugs and Their Mechanisms
What is unique about Midodrine as a drug?
It is a prodrug that forms an active metabolite, desglymidodrine.
p.69
Mixed α/β Blockers and Their Applications
What is unique about the administration of carvedilol?
It is administered as its racemate.
p.52
Norepinephrine Metabolism and Stability
What is an example of an alkylating agent mentioned?
Chloroethylamine (Cl(CH2)2NR2).
p.11
Clinical Applications of Epinephrine
Where should John inject the EpiPen if he experiences anaphylaxis?
Into the middle of his outer thigh.
p.6
Adrenergic Drug Mechanisms
What is the effect of inactivating adenylate cyclase?
It leads to the inactivation of cyclic adenosine monophosphate (cAMP) and inhibits further release of norepinephrine.
p.31
Treatment of Hypertension and Heart Conditions
What are some common causes of high blood pressure?
Obesity, lack of physical activity, high salt intake, and stress.
p.31
Treatment of Hypertension and Heart Conditions
What are the potential health risks associated with untreated high blood pressure?
Heart disease, stroke, and kidney damage.
p.11
Clinical Applications of Epinephrine
How long should the adverse effects of epinephrine last?
They should subside with time.
p.31
Treatment of Hypertension and Heart Conditions
What lifestyle changes can help lower high blood pressure?
Eating a balanced diet, exercising regularly, and reducing alcohol intake.
p.64
β Blockers and Their Therapeutic Uses
What type of drug is Levobunolol?
A non-selective β blocker.
p.22
Clinical Applications of Epinephrine
What are common types of allergic/cold drugs?
Antihistamines, decongestants, and expectorants.
p.59
β Blockers and Their Therapeutic Uses
What type of adrenergic antagonist is Metoprolol?
Selective β 1 - adrenergic antagonist.
p.18
Norepinephrine Metabolism and Stability
What is the nature of the N-terminal amine in amino acids?
It is a basic functional group.
p.45
Treatment of Hypertension and Heart Conditions
What class of drugs is commonly used to treat overactive bladder?
Antimuscarinics (Anticholinergics).
p.22
Clinical Applications of Epinephrine
What is the role of expectorants in cold medications?
To help loosen mucus and phlegm in the airways.
p.18
Norepinephrine Metabolism and Stability
What is the significance of pKa in drug functional groups?
It indicates the strength of an acid or base and affects drug solubility and absorption.
p.26
α and β Adrenergic Receptor Functions
What are α2 selective adrenergic receptor agonists used for?
Antihypertensives, antiglaucoma, and analgesics.
p.13
Adrenergic Drug Mechanisms
What is the role of methoxamine in adrenergic pharmacology?
It is an α 1 selective adrenergic receptor agonist used as a vasoconstrictor.
p.46
α and β Adrenergic Receptor Functions
What condition is Doxazosin primarily used to treat?
Benign prostatic hyperplasia and hypertension.
p.39
Clinical Applications of Epinephrine
What are short-acting β2 adrenergic agonists used for?
Symptomatic relief of bronchospasm in asthma and COPD.
p.70
Norepinephrine Metabolism and Stability
What enzyme does Carbidopa inhibit?
Aromatic L-amino acid decarboxylase.
p.55
β Blockers and Their Therapeutic Uses
Why are selective β1 blockers preferred in patients with respiratory conditions?
They have a reduced effect on bronchoconstriction compared to non-selective β blockers.
p.67
Treatment of Hypertension and Heart Conditions
What medication might be worsening the patient's heart failure?
Verapamil, a calcium channel blocker that can lower left ventricular function.
p.26
Clinical Applications of Epinephrine
Why is Apraclonidine a good candidate for treating glaucoma?
It is highly ionized at physiological pH and does not cross the blood-brain barrier readily.
p.39
Clinical Applications of Epinephrine
What is Levalbuterol?
The R-enantiomer of albuterol, used to treat asthma and COPD.
p.14
Norepinephrine Metabolism and Stability
Why do α1 agonists have a longer duration of action than norepinephrine?
They are not substrates for catechol-O-methyltransferase (COMT) and do not contain catechol.
p.24
Clinical Applications of Epinephrine
How does α2-adrenoreceptor activation affect norepinephrine release?
It inhibits the release of norepinephrine.
p.25
Direct-Acting Adrenergic Agonists
What type of adrenergic receptor do α2 agonists selectively target?
α2 selective adrenergic receptors.
p.63
β Blockers and Their Therapeutic Uses
How does propranolol's lipophilicity affect its function?
It allows better penetration of the CNS, explaining its effect in preventing migraines.
p.63
β Blockers and Their Therapeutic Uses
How much more potent is S(−)-propranolol compared to R(+)-propranolol?
About 100 times more potent.
p.53
Treatment of Hypertension and Heart Conditions
What condition is tolazoline primarily used to control?
Hypertensive emergencies, especially due to pheochromocytoma.
p.61
β Blockers and Their Therapeutic Uses
What severe side effects were associated with practolol?
Vision loss, fibrous or plastic peritonitis, mucosal and nasal ulceration, otitis media, and rashes.
p.22
Clinical Applications of Epinephrine
What do decongestants do?
They relieve nasal congestion by constricting blood vessels in the nasal passages.
p.18
Norepinephrine Metabolism and Stability
What is the nature of the N-terminal carboxylic acid in amino acids?
It is an acidic functional group.
p.44
α and β Adrenergic Receptor Functions
Where is the β 3 adrenergic receptor located?
In the kidneys, urinary tract, and bladder tissue.
p.10
Clinical Applications of Epinephrine
What is anaphylaxis?
A severe, potentially life-threatening allergic reaction.
p.50
Treatment of Hypertension and Heart Conditions
Why is phenoxybenzamine preferred preoperatively?
It is longer acting than phentolamine and helps control symptoms.
p.67
Treatment of Hypertension and Heart Conditions
What medications is the patient currently taking?
Aspirin, furosemide, lisinopril, lovastatin, metoprolol, and verapamil.
p.43
β Blockers and Their Therapeutic Uses
With which medications is vilanterol commonly used in combination?
Fluticasone furoate or umeclidinium bromide.
p.10
Clinical Applications of Epinephrine
What is the role of epinephrine infusions in bradycardia?
They may be used for symptomatic treatment.
p.30
Treatment of Hypertension and Heart Conditions
What does diastolic pressure measure?
The resting state in between heartbeats.
p.68
β Blockers and Their Therapeutic Uses
What should be considered when treating patients with congestive heart failure with β receptor antagonists?
Treatment should only be undertaken by experienced physicians.
p.57
β Blockers and Their Therapeutic Uses
What conditions do β blockers help treat?
Chest pain, high blood pressure, and irregular heartbeat.
p.30
Treatment of Hypertension and Heart Conditions
How is high blood pressure defined for adults?
Systolic pressure of 140 mm Hg or greater and/or diastolic pressure of 90 mm Hg or greater.
p.53
Mixed α/β Blockers and Their Applications
What type of drugs are tolazoline and phentolamine?
Non-selective α-antagonists with antihypertensive activity.
p.62
β Blockers and Their Therapeutic Uses
Name some nonselective β-blockers.
Carteolol, nadolol, penbutolol, pindolol, propranolol, sotalol, timolol, carvedilol, and labetalol.
p.64
β Blockers and Their Therapeutic Uses
What conditions is Levobunolol used to manage?
Ocular hypertension and open-angle glaucoma.
p.61
β Blockers and Their Therapeutic Uses
Why was practolol withdrawn from clinical use?
Due to adverse oculomucocutaneous syndrome, including vision loss and other severe side effects.
p.62
β Blockers and Their Therapeutic Uses
What are many β-blockers derived from?
Aryloxypropanolamine derivatives.
p.19
Norepinephrine Metabolism and Stability
What is the significance of a lower pKa value for an amine?
Indicates a stronger acid and a weaker base.
p.50
β Blockers and Their Therapeutic Uses
What is the role of phenoxybenzamine in managing pheochromocytoma?
It is an α1-antagonist that reverses vasoconstriction, lowering arterial blood pressure and increasing intravascular volume.
p.65
β Blockers and Their Therapeutic Uses
In addition to congestive heart failure, what other conditions is Carvedilol effective for?
Mild to moderate hypertension and ischaemic heart disease.
p.10
Clinical Applications of Epinephrine
What can happen if anaphylaxis is not treated promptly?
It can result in unconsciousness or death.
p.26
Clinical Applications of Epinephrine
In what forms is Clonidine available?
Oral tablets, injection, or a transdermal system.
p.37
Norepinephrine Metabolism and Stability
Why are short-acting β2 adrenergic agonists resistant to methylation by COMT?
They contain a resorcinol ring.
p.48
Treatment of Hypertension and Heart Conditions
What complications can arise from untreated BPH?
Bladder stones, infections, and kidney failure.
p.49
Sympathetic Nervous System Functions
What condition is caused by tumors of chromaffin cells in the adrenal medulla?
Pheochromocytoma, which produces large amounts of epinephrine and norepinephrine.
p.48
β Blockers and Their Therapeutic Uses
How do α-blockers help in treating BPH?
They relax the prostate muscle, making it easier for urine to pass through.
p.66
β Blockers and Their Therapeutic Uses
What are the common groups attached to the amine in β-blockers?
Isopropyl or tertiary butyl groups.
p.57
Clinical Applications of Epinephrine
What happens to the heart when arteries become narrowed?
The heart compensates by pumping harder and faster, increasing oxygen demand.
p.49
β Blockers and Their Therapeutic Uses
Why is the use of Phenoxybenzamine limited?
Due to its receptor nonselectivity and toxicity.
p.66
β Blockers and Their Therapeutic Uses
What type of derivatives do the majority of selective β1-blockers belong to?
Aryloxypropanolamine derivatives with substitutions at the para position.
p.40
Adrenergic Drug Mechanisms
What contributes to the long duration of action of long-acting β2 agonists?
Higher lipophilicity and greater receptor affinity compared to short-acting agonists.
p.1
α and β Adrenergic Receptor Functions
What are the two main types of adrenergic receptors?
Alpha (α) and beta (β) receptors.
p.53
Adrenergic Drug Mechanisms
What structural similarities does tolazoline have?
It has similarities to imidazoline α1-agonists like naphazoline and xylometazoline.
p.2
Sympathetic Nervous System Functions
What happens to the airway muscles in the lungs under sympathetic nervous system activation?
They relax to improve oxygen delivery to the lungs.
p.58
β Blockers and Their Therapeutic Uses
What are selective β 1 - adrenergic antagonists commonly known as?
Cardio-selective β 1 - blockers.
p.64
β Blockers and Their Therapeutic Uses
What is Levobunolol reduced to in the eye's tissues?
Dihydrolevobunolol, which is equally active.
p.45
Treatment of Hypertension and Heart Conditions
Name two antimuscarinic drugs used for overactive bladder.
Oxybutynin and Tolterodine.
p.10
Clinical Applications of Epinephrine
What conditions can epinephrine treat?
Anaphylaxis, cardiac arrest, asthma, and superficial bleeding.
p.50
Clinical Applications of Epinephrine
How does phenoxybenzamine affect glucose intolerance?
It often corrects glucose intolerance.
p.20
Clinical Applications of Epinephrine
What are some indications for ephedrine?
Bronchodilator, vasopressor, cardiac stimulant, and nasal decongestant.
p.36
Clinical Applications of Epinephrine
What is dobutamine used for?
As a cardiac stimulant after surgery or congestive heart failure (IV only).
p.67
Treatment of Hypertension and Heart Conditions
How do ACE inhibitors like lisinopril help in heart failure?
They dilate blood vessels to improve blood flow and decrease the heart's workload.
p.65
β Blockers and Their Therapeutic Uses
What is unique about the composition of Carvedilol?
It is a racemic mixture with nonselective β-adrenoreceptor blocking in the S(-) enantiomer and α 1-adrenergic blocking in both R(+) and S(-) enantiomers.
p.49
Mixed α/β Blockers and Their Applications
What is Phenoxybenzamine used for?
Treatment of hypertension due to pheochromocytoma and benign prostate hyperplasia.
p.60
β Blockers and Their Therapeutic Uses
What is the primary use of Esmolol in acute critical care settings?
To terminate supraventricular tachycardia during surgery.
p.39
Norepinephrine Metabolism and Stability
Which enzyme are short-acting β2 adrenergic agonists resistant to?
COMT (Catechol-O-methyltransferase).
p.57
β Blockers and Their Therapeutic Uses
What is the leading cause of death in the United States?
Heart disease, killing 1 in every 4 people.
p.28
Treatment of Hypertension and Heart Conditions
What is methyldopa used for?
The management of moderate to severe hypertension.
p.29
α and β Adrenergic Receptor Functions
What is Lofexidine used for?
Treatment of opioid withdrawal symptoms in adults.
p.68
β Blockers and Their Therapeutic Uses
What is one proposed mechanism of action for carvedilol in heart failure?
Inhibition of β1 receptor activation may help preserve myocardial function.
p.40
β Blockers and Their Therapeutic Uses
What is a key characteristic of Salmeterol?
It is a lipophilic β2-selective agonist with a prolonged duration of action (>12 h).
p.47
Clinical Applications of Epinephrine
Why should Tamsulosin be avoided in some patients?
Due to the presence of aryl sulfonamide, it should be avoided in patients with severe sulfa allergies.
p.57
Clinical Applications of Epinephrine
What condition can result from the heart pumping harder due to narrowed arteries?
Angina, which is chest pain.
p.47
α and β Adrenergic Receptor Functions
What is the selectivity of Tamsulosin, Alfuzosin, and Silodosin?
They are more selective for the α 1A adrenergic receptor subtype found in the prostate gland.
p.18
Norepinephrine Metabolism and Stability
What type of side chain does lysine have?
A positively charged amino side chain.
p.64
β Blockers and Their Therapeutic Uses
What is the pharmacological activity of Levobunolol compared to R-bunolol?
Levobunolol has more than 60 times the pharmacological activity of R-bunolol.
p.20
Clinical Applications of Epinephrine
What are mixed-acting sympathomimetics commonly used for?
As ingredients in many cold medications and oral decongestant formulations.
p.43
β Blockers and Their Therapeutic Uses
What are the names of the very long-acting β2 adrenergic agonists approved for COPD?
Indacaterol, olodaterol, and vilanterol.
p.61
β Blockers and Their Therapeutic Uses
What type of drug is atenolol?
A selective β1-adrenergic receptor antagonist.
p.65
β Blockers and Their Therapeutic Uses
What type of receptors does Carvedilol block?
β 1, β 2, and α 1 receptors.
p.44
Clinical Applications of Epinephrine
How do β 3 adrenergic agonists compare to muscarinic antagonists?
They are similar in treating overactive bladder.
p.20
Norepinephrine Metabolism and Stability
Is ephedrine a substrate for COMT?
No, ephedrine is not a substrate for COMT.
p.70
Norepinephrine Metabolism and Stability
Was a drug developed for dopamine β-hydroxylase or phenylethanolamine N-methyltransferase?
No, no drug was developed for these enzymes.
p.55
β Blockers and Their Therapeutic Uses
What distinguishes selective β blockers from non-selective β blockers?
Selective β blockers primarily target β1 receptors, while non-selective affect both β1 and β2 receptors.
p.30
Treatment of Hypertension and Heart Conditions
What does systolic pressure measure?
The pressure when blood is pumped out of the heart.
p.69
Mixed α/β Blockers and Their Applications
What are the two available mixed α/β-receptor blockers?
Carvedilol and labetalol.
p.66
β Blockers and Their Therapeutic Uses
What functional groups are β-blockers devoid of?
Catechol functional groups.
p.30
Treatment of Hypertension and Heart Conditions
Why is high blood pressure referred to as a 'silent killer'?
Because it often has no symptoms but can lead to serious health issues.
p.37
Clinical Applications of Epinephrine
What is the status of Terbutaline in current medical use?
It has been withdrawn and is no longer used.
p.26
Clinical Applications of Epinephrine
What side effects can Brimonidine cause?
Fatigue and/or drowsiness in some patients.
p.40
Norepinephrine Metabolism and Stability
Why does Salmeterol have a long duration of action?
It is resistant to both MAO and COMT and is lipophilic.
p.68
β Blockers and Their Therapeutic Uses
What effect can activation of β receptors and elevation of cellular cyclic AMP have?
They may promote myocardial cell death by apoptosis.
p.29
α and β Adrenergic Receptor Functions
What condition is Tizanidine used to treat?
Muscle spasticity due to spinal cord injury or multiple sclerosis.
p.53
Mixed α/β Blockers and Their Applications
What type of receptor antagonists are tolazoline and phentolamine?
Non-selective α-adrenergic receptor antagonists.
p.16
Clinical Applications of Epinephrine
What conditions are treated with arylimidazoline adrenergic agonists?
Common cold, influenza, sinusitis, allergic and nonallergic rhinitis, and upper respiratory tract infections.
p.19
Norepinephrine Metabolism and Stability
How does the structure of an amine affect its pKa?
Electron-donating groups increase basicity, lowering pKa; electron-withdrawing groups decrease basicity, raising pKa.
p.50
Sympathetic Nervous System Functions
What symptoms might a patient with pheochromocytoma experience?
Paroxysmal attacks of headache, hypertension, sweating, and palpitations.
p.45
Treatment of Hypertension and Heart Conditions
What is the role of β 3 adrenergic agonists in treating overactive bladder?
They help relax the bladder muscle.
p.36
Direct-Acting Adrenergic Agonists
What is the effect of the R - (+) - isomer of dobutamine?
It is an α 1 - antagonist and general β 1 β 2 - agonist.
p.42
β Blockers and Their Therapeutic Uses
What are the names of the very long-acting β2 adrenergic agonists approved for COPD?
Indacaterol, olodaterol, and vilanterol.
p.70
Treatment of Hypertension and Heart Conditions
What is Carbidopa used for?
To inhibit the metabolism of exogenous L-DOPA in Parkinson disease treatment.
p.55
β Blockers and Their Therapeutic Uses
What is a common use of β blockers?
Treatment of hypertension.
p.48
Treatment of Hypertension and Heart Conditions
What is benign prostatic hyperplasia (BPH)?
A condition that causes the prostate gland to enlarge, making it hard to urinate.
p.68
β Blockers and Their Therapeutic Uses
Why might the new physician question the use of a β blocker in treating heart failure?
Because β receptor antagonists can worsen or precipitate congestive heart failure in compensated patients with heart disease.
p.47
Treatment of Hypertension and Heart Conditions
What condition is Alfuzosin used to treat?
Benign prostatic hyperplasia (BPH).
p.42
Norepinephrine Metabolism and Stability
What is a zwitterion?
A molecule having a net formal charge of zero, but with negative and positive formal charges on individual atoms.
p.67
Treatment of Hypertension and Heart Conditions
What should be assessed to relieve the patient's symptoms?
Adherence to a low-salt diet and proper intake of diuretics and other medications.
p.47
Prodrugs and Their Mechanisms
What is the stereochemical nature of Alfuzosin?
It is chiral and contains a stereocenter.
p.39
α and β Adrenergic Receptor Functions
How does R-albuterol (levalbuterol) compare to S-albuterol in terms of receptor affinity?
R-albuterol binds to β2 adrenergic receptor with 100-fold higher affinity than S-albuterol.
p.60
β Blockers and Their Therapeutic Uses
What is the therapeutic effect duration of Esmolol after discontinuation?
It quickly dissipates in 30 minutes.
p.29
α and β Adrenergic Receptor Functions
What effects does Dexmedetomidine have on blood pressure and heart rate?
It decreases both blood pressure and heart rate.
p.57
β Blockers and Their Therapeutic Uses
Who should not be prescribed β blockers?
Patients with slow heart rate or low blood pressure.
p.10
Clinical Applications of Epinephrine
What are common symptoms of anaphylaxis?
Skin rash, nausea, vomiting, difficulty breathing, and shock.
p.43
β Blockers and Their Therapeutic Uses
What is unique about vilanterol compared to other β2 adrenergic agonists?
It is an ultra-long acting β2 adrenergic receptor agonist.
p.45
Treatment of Hypertension and Heart Conditions
What is the purpose of botulinum toxin injections in overactive bladder treatment?
To relax the bladder muscle.
p.50
Adrenergic Drug Mechanisms
What is a limitation of phentolamine compared to other hypotensive agents?
It has a slow onset and long duration of action, and is no longer widely available.
p.10
Clinical Applications of Epinephrine
How is epinephrine usually administered for acute asthmatic attacks?
Slowly by intravenous (IV) injection.
p.65
β Blockers and Their Therapeutic Uses
What type of adrenergic receptor antagonist is Carvedilol?
Non-selective β-adrenergic receptor antagonist.
p.68
β Blockers and Their Therapeutic Uses
What is a common clinical observation regarding β receptor antagonists and heart failure?
They can worsen or precipitate congestive heart failure in compensated patients.
p.37
Norepinephrine Metabolism and Stability
What is unique about Terbutaline in terms of metabolism?
It is resistant to metabolism by MAO but is a good substrate for COMT.
p.48
Treatment of Hypertension and Heart Conditions
What are common signs of prostate problems?
Frequent urge to urinate, blood in urine, painful urination, difficulty urinating, or inability to urinate.
p.40
Clinical Applications of Epinephrine
What are long-acting β2 adrenergic agonists used for?
Treatment of COPD and asthma.
p.46
α and β Adrenergic Receptor Functions
What is the relationship between hydrophobicity and duration of action for these medications?
Duration of action is correlated with hydrophobicity: Doxazosin > Terazosin > Prazosin.
p.30
Treatment of Hypertension and Heart Conditions
What are some risks associated with high blood pressure?
Heart attack, heart failure, stroke, dementia, vision loss, and kidney failure.
p.47
Treatment of Hypertension and Heart Conditions
What is Tamsulosin used for?
It is a first-line drug for the treatment of BPH.
p.39
Clinical Applications of Epinephrine
What is the primary use of short-acting β2 adrenergic agonists?
Treatment or prevention of bronchospasm in reversible obstructive airway disease.
p.69
Mixed α/β Blockers and Their Applications
What is dilevalol?
The R,R diastereomer of labetalol, not approved by the FDA due to hepatotoxicity.
p.40
α and β Adrenergic Receptor Functions
What is the significance of the (R,R) stereoisomer of Formoterol?
It has a 1,000-fold higher affinity than the (S,S) stereoisomer.
p.28
Treatment of Hypertension and Heart Conditions
What are guanfacine, guanabenz, and moxonidine used for?
The treatment of hypertension.
p.46
α and β Adrenergic Receptor Functions
What additional condition can Prazosin treat besides high blood pressure?
Nightmares related to post-traumatic stress disorder (PTSD).
p.66
β Blockers and Their Therapeutic Uses
What is a common structural feature of clinically available β-blockers?
At least one aromatic and/or heteroaromatic ring system.
p.68
β Blockers and Their Therapeutic Uses
Which β blockers have been shown to reduce mortality in chronic heart failure?
Carvedilol, metoprolol, and bisoprolol.
p.42
Norepinephrine Metabolism and Stability
What must charged atoms in a zwitterion be joined by?
One or more covalent bonds.
p.66
β Blockers and Their Therapeutic Uses
What type of side chain is attached to the aromatic ring in β-blockers?
An alkyl side chain containing a chiral secondary hydroxyl group and an amine.
p.47
Prodrugs and Their Mechanisms
What are the two enantiomeric forms of Alfuzosin?
(R)-alfuzosin and (S)-alfuzosin.
p.46
α and β Adrenergic Receptor Functions
What common structural feature do Prazosin, Terazosin, Doxazosin, and Alfuzosin share?
They all bear a 4-amino-6,7-dimethoxyquinazoline ring system attached to a piperazine ring.
p.60
β Blockers and Their Therapeutic Uses
What happens to Esmolol after administration?
It is rapidly hydrolyzed by red blood cells esterases into a carboxylic acid metabolite and methanol.
p.48
β Blockers and Their Therapeutic Uses
What is a benefit of prostate gland-selective α-blockers?
They have fewer systemic side effects than non-selective ones.
p.57
β Blockers and Their Therapeutic Uses
How do β blockers affect the heart's function?
They slow down the heart, allowing it to relax and reducing blood pressure.
p.69
Mixed α/β Blockers and Their Applications
Which diastereomers of labetalol are inactive?
S(CH3),S(OH) and R(CH3),S(OH).
p.29
α and β Adrenergic Receptor Functions
How does Tizanidine reduce spasticity?
By increasing presynaptic inhibition of motor neurons.
p.69
Mixed α/β Blockers and Their Applications
What are the functions of the S-(−) enantiomer of carvedilol?
It is both an α- and nonselective β-blocker.
p.68
β Blockers and Their Therapeutic Uses
How might β receptor antagonism affect cardiac remodeling?
It may attenuate cardiac remodeling, which can have deleterious effects on cardiac function.
p.30
Treatment of Hypertension and Heart Conditions
How are blood pressure thresholds determined?
Based on the average of at least two measurements obtained in an office setting on at least two separate occasions.
p.49
Norepinephrine Metabolism and Stability
What is the duration of action for Phenoxybenzamine?
It has a long-lasting action.
p.29
α and β Adrenergic Receptor Functions
What forms is Dexmedetomidine available in?
Oral tablets, injection, or a transdermal system.
p.57
β Blockers and Their Therapeutic Uses
What are some possible side effects of β blockers?
Tiredness, dizziness, and generally feeling unwell.
p.40
Direct-Acting Adrenergic Agonists
Name three long-acting β2 adrenergic agonists.
Salmeterol, Formoterol, Arformoterol.
p.48
β Blockers and Their Therapeutic Uses
Name some approved α-blockers for BPH.
Alfuzosin, Doxazosin, Silodosin, Tamsulosin, Terazosin.
p.68
β Blockers and Their Therapeutic Uses
What role does chronic excess catecholamines play in heart failure?
They may be toxic to the heart, especially through activation of β1 receptors.
p.68
β Blockers and Their Therapeutic Uses
What is a potential benefit of afterload reduction by carvedilol?
It may be clinically relevant in the treatment of heart failure.
p.57
β Blockers and Their Therapeutic Uses
What was a characteristic of the initial β blockers?
They were non-selective, blocking adrenaline receptors in multiple organs.
p.66
β Blockers and Their Therapeutic Uses
What are the exceptions to the racemic mixture administration of β-blockers?
Timolol, which is only available as S(−) - timolol, and levobunolol.
p.48
β Blockers and Their Therapeutic Uses
What types of medications are used to treat overactive bladder?
Muscarinic antagonists and β3-adrenergic agonists.
p.49
Adrenergic Drug Mechanisms
What is unique about the neutral isomer of Phenoxybenzamine?
It forms a highly reactive aziridinium that covalently modifies α receptors.
p.69
Mixed α/β Blockers and Their Applications
What is the active diastereomer of labetalol?
R(CH3),R(OH) with minimal α1-blocking activity.
p.40
Clinical Applications of Epinephrine
What is the role of inhaled formoterol fumarate?
Acts locally in the lung as a bronchodilator.
p.57
β Blockers and Their Therapeutic Uses
What advancements have been made in β blockers over the decades?
They have become more targeted, focusing on adrenaline receptors in the heart.
p.66
β Blockers and Their Therapeutic Uses
What type of derivatives do many non-selective β-blockers belong to?
Aryloxypropanolamine derivatives.
p.66
β Blockers and Their Therapeutic Uses
What is the exception among non-selective β-blockers?
Sotalol, which is a phenylethanolamine derivative containing a sulfonamide group at the para position.
p.60
β Blockers and Their Therapeutic Uses
What is the nature of the carboxylic acid metabolite of Esmolol?
It is essentially inactive.
p.47
Treatment of Hypertension and Heart Conditions
What is a key advantage of Tamsulosin, Alfuzosin, and Silodosin over terazosin and doxazosin?
They have fewer cardiovascular side effects when treating BPH.
p.40
Mixed α/β Blockers and Their Applications
How do long-acting β2 adrenergic agonists differ from short-acting ones?
They have larger hydrophobic substitutions.
