Podcast
Questions and Answers
What is the active moiety of penicillins?
What is the active moiety of penicillins?
- Three-member ring
- Five-member ring
- Six-member ring
- Four-member ring (correct)
Which type of antibiotics contain the beta-lactam ring, similar to penicillins?
Which type of antibiotics contain the beta-lactam ring, similar to penicillins?
- Cephalosporins (correct)
- Aminoglycosides
- Quinolones
- Macrolides
At what concentration are beta-lactam antibiotics bactericidal against most organisms?
At what concentration are beta-lactam antibiotics bactericidal against most organisms?
- Equal to the MIC
- Exceeding the minimum inhibitory concentration (MIC) (correct)
- Unrelated to the MIC
- Below the MIC
When are beta-lactam antibiotics most effective?
When are beta-lactam antibiotics most effective?
Where are monobactams and carbapenems commonly used?
Where are monobactams and carbapenems commonly used?
Why are beta-lactamase inhibitors described with penicillins?
Why are beta-lactamase inhibitors described with penicillins?
Why are oral penicillin formulations generally limited to mild to moderate infections?
Why are oral penicillin formulations generally limited to mild to moderate infections?
Which statement is true regarding penicillin V and dicloxacillin?
Which statement is true regarding penicillin V and dicloxacillin?
Why is it recommended to use amoxicillin instead of ampicillin for oral administration?
Why is it recommended to use amoxicillin instead of ampicillin for oral administration?
Why should penicillin G procaine and penicillin G benzathine depot formulations not be injected near an artery or vein?
Why should penicillin G procaine and penicillin G benzathine depot formulations not be injected near an artery or vein?
What is the primary route of excretion for most penicillins, except nafcillin and oxacillin?
What is the primary route of excretion for most penicillins, except nafcillin and oxacillin?
How does probenecid affect the pharmacokinetics of penicillins when administered concurrently?
How does probenecid affect the pharmacokinetics of penicillins when administered concurrently?
What is the main mechanism of action of penicillins against bacteria?
What is the main mechanism of action of penicillins against bacteria?
Which subclass of penicillins is known for its activity against aerobic, gram-positive organisms like Streptococcus species?
Which subclass of penicillins is known for its activity against aerobic, gram-positive organisms like Streptococcus species?
Why are penicillins considered effective mainly during active cellular multiplication?
Why are penicillins considered effective mainly during active cellular multiplication?
Which bacterium is Penicillin G specifically reliable for treating?
Which bacterium is Penicillin G specifically reliable for treating?
Which group of organisms has reduced the range of bacterial species that penicillins can effectively treat?
Which group of organisms has reduced the range of bacterial species that penicillins can effectively treat?
Why do aminopenicillins have greater activity against gram-negative bacteria compared to natural penicillins?
Why do aminopenicillins have greater activity against gram-negative bacteria compared to natural penicillins?
What is a common reason for combining amoxicillin and ampicillin with beta-lactamase inhibitors like clavulanic acid?
What is a common reason for combining amoxicillin and ampicillin with beta-lactamase inhibitors like clavulanic acid?
Which factor contributed to the decreased concern with penicillin-resistant S. pneumoniae strains?
Which factor contributed to the decreased concern with penicillin-resistant S. pneumoniae strains?
Why are penicillins considered bactericidal against sensitive organisms?
Why are penicillins considered bactericidal against sensitive organisms?
Why are aminopenicillins considered more effective against gram-negative bacteria than natural penicillins?
Why are aminopenicillins considered more effective against gram-negative bacteria than natural penicillins?
How do beta-lactamase inhibitors prevent the destruction of beta-lactam antibiotics?
How do beta-lactamase inhibitors prevent the destruction of beta-lactam antibiotics?
What is the result of altering target PBPs on the bacterial cell wall in terms of resistance to penicillins?
What is the result of altering target PBPs on the bacterial cell wall in terms of resistance to penicillins?
Which organisms are resistant to all penicillins, cephalosporins, and carbapenems, except for ceftaroline?
Which organisms are resistant to all penicillins, cephalosporins, and carbapenems, except for ceftaroline?
What is the mechanism by which beta-lactamase inhibitors like clavulanate, sulbactam, and tazobactam work?
What is the mechanism by which beta-lactamase inhibitors like clavulanate, sulbactam, and tazobactam work?
What type of resistance mechanism is responsible for methicillin resistance in staphylococci and penicillin resistance in pneumococci?
What type of resistance mechanism is responsible for methicillin resistance in staphylococci and penicillin resistance in pneumococci?
Which group of organisms produce extended-spectrum beta-lactamases (ESBLs) that can hydrolyze both penicillins and cephalosporins?
Which group of organisms produce extended-spectrum beta-lactamases (ESBLs) that can hydrolyze both penicillins and cephalosporins?
What role do antipseudomonal penicillins like piperacillin/tazobactam play in antimicrobial therapy?
What role do antipseudomonal penicillins like piperacillin/tazobactam play in antimicrobial therapy?
Which enzymes irreversibly inactivate beta-lactamase enzymes produced by bacteria?
Which enzymes irreversibly inactivate beta-lactamase enzymes produced by bacteria?
What is the main reason for resistance to penicillins due to alteration in the outer membrane of the cell wall?
What is the main reason for resistance to penicillins due to alteration in the outer membrane of the cell wall?
What is the unique spectrum of activity of Nafcillin, oxacillin, and dicloxacillin?
What is the unique spectrum of activity of Nafcillin, oxacillin, and dicloxacillin?
How can changes in resting activity occur in organs?
How can changes in resting activity occur in organs?
Which neurotransmitter is associated with the parasympathetic nervous system?
Which neurotransmitter is associated with the parasympathetic nervous system?
Which branch of the autonomic nervous system is targeted by adrenergic agonists?
Which branch of the autonomic nervous system is targeted by adrenergic agonists?
What is the primary function of peripherally acting alpha-adrenergic agonists?
What is the primary function of peripherally acting alpha-adrenergic agonists?
Which type of receptor is NOT involved in adrenergic agonists' action?
Which type of receptor is NOT involved in adrenergic agonists' action?
Where are intravenous forms of drugs generally NOT used according to the text?
Where are intravenous forms of drugs generally NOT used according to the text?
What is the most common adverse reaction reported in monotherapy trials of the drug discussed?
What is the most common adverse reaction reported in monotherapy trials of the drug discussed?
What percentage of patients experienced adverse reactions that resulted in their being discontinued from monotherapy trials?
What percentage of patients experienced adverse reactions that resulted in their being discontinued from monotherapy trials?
What is the most common adverse reaction reported in trials of adjunctive therapy?
What is the most common adverse reaction reported in trials of adjunctive therapy?
What percentage of patients experienced adverse reactions leading to discontinuation from trials of adjunctive therapy?
What percentage of patients experienced adverse reactions leading to discontinuation from trials of adjunctive therapy?
What is the mechanism of action of the drug's active metabolite, alpha-methyl-norepinephrine?
What is the mechanism of action of the drug's active metabolite, alpha-methyl-norepinephrine?
What is the end result from the use of the drug discussed?
What is the end result from the use of the drug discussed?
What is the primary route of excretion for the drugs in this class?
What is the primary route of excretion for the drugs in this class?
What is the main reason for cautious use of these drugs in patients with renal function impairment?
What is the main reason for cautious use of these drugs in patients with renal function impairment?
What is the primary reason these drugs should be used with caution in populations like older adults?
What is the primary reason these drugs should be used with caution in populations like older adults?
What is the primary reason guanabenz and clonidine are classified as Pregnancy Category C drugs?
What is the primary reason guanabenz and clonidine are classified as Pregnancy Category C drugs?
What percentage of the administered dose of tamsulosin is typically eliminated unchanged in the urine?
What percentage of the administered dose of tamsulosin is typically eliminated unchanged in the urine?
What is the main route of elimination for the metabolites of alfuzosin?
What is the main route of elimination for the metabolites of alfuzosin?
Which enzyme is responsible for the metabolism of silodosin?
Which enzyme is responsible for the metabolism of silodosin?
What is the half-life of the active metabolite of silodosin?
What is the half-life of the active metabolite of silodosin?
What is the primary consequence of major drug interactions with these alpha-blocker medications?
What is the primary consequence of major drug interactions with these alpha-blocker medications?
Which of the following is the main reason for using clonidine in combination with a diuretic for hypertension treatment?
Which of the following is the main reason for using clonidine in combination with a diuretic for hypertension treatment?
What is the primary reason for the use of the transdermal formulation of clonidine?
What is the primary reason for the use of the transdermal formulation of clonidine?
Which of the following is the main reason for the reduced sedation with clonidine when the dose is divided?
Which of the following is the main reason for the reduced sedation with clonidine when the dose is divided?
What is the primary reason for the use of clonidine in the treatment of ADHD?
What is the primary reason for the use of clonidine in the treatment of ADHD?
Why are smaller doses of clonidine and methyldopa required in patients with renal impairment?
Why are smaller doses of clonidine and methyldopa required in patients with renal impairment?
What is the primary advantage of using the low end of the dose range for guanfacine in patients with renal insufficiency?
What is the primary advantage of using the low end of the dose range for guanfacine in patients with renal insufficiency?
Why is consultation with a pediatric mental health professional recommended for the safe administration of clonidine for ADHD?
Why is consultation with a pediatric mental health professional recommended for the safe administration of clonidine for ADHD?
Which statement is true regarding the use of clonidine and methyldopa in older adult patients?
Which statement is true regarding the use of clonidine and methyldopa in older adult patients?
What is the primary reason for the increased use of medications other than methyldopa for the treatment of hypertension during pregnancy?
What is the primary reason for the increased use of medications other than methyldopa for the treatment of hypertension during pregnancy?
What is the primary purpose of monitoring weight and other indicators of fluid status in patients taking clonidine and methyldopa?
What is the primary purpose of monitoring weight and other indicators of fluid status in patients taking clonidine and methyldopa?
Which receptors are mostly associated with excitation or stimulation?
Which receptors are mostly associated with excitation or stimulation?
What is the primary mechanism of action of centrally acting alpha2 agonists in reducing blood pressure?
What is the primary mechanism of action of centrally acting alpha2 agonists in reducing blood pressure?
Which class of drugs may be inappropriate for use in geriatric patients, according to the Beers Criteria?
Which class of drugs may be inappropriate for use in geriatric patients, according to the Beers Criteria?
What is the primary reason for gradually tapering the dose when discontinuing centrally acting alpha2 agonists?
What is the primary reason for gradually tapering the dose when discontinuing centrally acting alpha2 agonists?
Which medication in the class of centrally acting alpha2 agonists is approved for the treatment of attention deficit-hyperactivity disorder (ADHD)?
Which medication in the class of centrally acting alpha2 agonists is approved for the treatment of attention deficit-hyperactivity disorder (ADHD)?
Which receptors are associated with relaxation or inhibition of norepinephrine release?
Which receptors are associated with relaxation or inhibition of norepinephrine release?
Which receptors are found mostly in the heart, brain, kidney, and lipocytes, and are associated with stimulation of adenylyl cyclase?
Which receptors are found mostly in the heart, brain, kidney, and lipocytes, and are associated with stimulation of adenylyl cyclase?
Which receptors are located in the smooth muscle of the eyes, arterioles, venules, bronchioles, liver, pancreas, and GI and GU systems?
Which receptors are located in the smooth muscle of the eyes, arterioles, venules, bronchioles, liver, pancreas, and GI and GU systems?
Which neurotransmitter stimulates all four types of adrenergic receptors (alpha1, alpha2, beta1, and beta2)?
Which neurotransmitter stimulates all four types of adrenergic receptors (alpha1, alpha2, beta1, and beta2)?
Which class of drugs is used mainly for their bronchodilating effects?
Which class of drugs is used mainly for their bronchodilating effects?
What is the proper way to handle a missed dose of methyldopa?
What is the proper way to handle a missed dose of methyldopa?
What is the most common adverse reaction associated with methyldopa?
What is the most common adverse reaction associated with methyldopa?
How should patients using the transdermal clonidine system apply the patch?
How should patients using the transdermal clonidine system apply the patch?
What lifestyle changes are recommended for hypertension management in addition to drug therapy?
What lifestyle changes are recommended for hypertension management in addition to drug therapy?
What should patients do if they experience more than a 2 lb weight gain in a day?
What should patients do if they experience more than a 2 lb weight gain in a day?
What is the recommended approach to prevent rebound hypertension when withdrawing drugs like methyldopa?
What is the recommended approach to prevent rebound hypertension when withdrawing drugs like methyldopa?
How can dry mouth be minimized for patients on medications like methyldopa?
How can dry mouth be minimized for patients on medications like methyldopa?
What should patients do if they suspect hepatotoxicity from methyldopa use?
What should patients do if they suspect hepatotoxicity from methyldopa use?
What is indicated by swelling in the feet and ankles in patients on drugs like methyldopa?
What is indicated by swelling in the feet and ankles in patients on drugs like methyldopa?
Which of the following is NOT a recommended approach for decreasing adverse reactions to drugs like methyldopa?
Which of the following is NOT a recommended approach for decreasing adverse reactions to drugs like methyldopa?
Which category does methyldopa fall under in an injectable form?
Which category does methyldopa fall under in an injectable form?
What is a major adverse reaction common to all drugs in the category of centrally acting alpha2 agonists?
What is a major adverse reaction common to all drugs in the category of centrally acting alpha2 agonists?
What is a common adverse effect associated with clonidine use?
What is a common adverse effect associated with clonidine use?
Why should all patients given these drugs be warned about a particular possibility?
Why should all patients given these drugs be warned about a particular possibility?
Which adverse reaction has been associated with guanabenz and clonidine but not with methyldopa?
Which adverse reaction has been associated with guanabenz and clonidine but not with methyldopa?
What is the clinical use of centrally acting alpha2 agonists like clonidine and methyldopa?
What is the clinical use of centrally acting alpha2 agonists like clonidine and methyldopa?
Which drug interaction can result in toxicity, psychoses, or excessive SNS stimulation when interacting with centrally acting alpha2 agonists?
Which drug interaction can result in toxicity, psychoses, or excessive SNS stimulation when interacting with centrally acting alpha2 agonists?
Which category do all drugs in this class belong to when it comes to pruritic rashes?
Which category do all drugs in this class belong to when it comes to pruritic rashes?
What is recommended if the withdrawal of a drug from this class is necessary?
What is recommended if the withdrawal of a drug from this class is necessary?
What baseline test should be performed prior to initiating therapy with methyldopa?
What baseline test should be performed prior to initiating therapy with methyldopa?
What is a distinguishing characteristic between phenoxybenzamine and phentolamine in terms of their blockade of receptors?
What is a distinguishing characteristic between phenoxybenzamine and phentolamine in terms of their blockade of receptors?
Why are nonselective alpha antagonists like phentolamine and phenoxybenzamine not recommended for the treatment of hypertension?
Why are nonselective alpha antagonists like phentolamine and phenoxybenzamine not recommended for the treatment of hypertension?
Which class of alpha antagonists is specifically used for relieving symptoms associated with benign prostatic hypertrophy (BPH)?
Which class of alpha antagonists is specifically used for relieving symptoms associated with benign prostatic hypertrophy (BPH)?
How do reversible alpha1 antagonists affect peripheral vascular resistance?
How do reversible alpha1 antagonists affect peripheral vascular resistance?
Which adverse effect is minimal in patients taking tamsulosin, alfuzosin, and silodosin compared to other alpha antagonists?
Which adverse effect is minimal in patients taking tamsulosin, alfuzosin, and silodosin compared to other alpha antagonists?
Why is prazosin not typically used for treating benign prostatic hypertrophy (BPH)?
Why is prazosin not typically used for treating benign prostatic hypertrophy (BPH)?
How do selective alpha1 antagonists like doxazosin lower blood pressure?
How do selective alpha1 antagonists like doxazosin lower blood pressure?
Which type of patients might experience orthostatic hypotension as a side effect of taking reversible alpha1 antagonists?
Which type of patients might experience orthostatic hypotension as a side effect of taking reversible alpha1 antagonists?
What subtype of alpha1 receptors are approximately 70% localized to the prostatic stroma in the prostate?
What subtype of alpha1 receptors are approximately 70% localized to the prostatic stroma in the prostate?
Which alpha1 antagonist demonstrates the highest selectivity for the alpha1a receptor subtype among the listed drugs?
Which alpha1 antagonist demonstrates the highest selectivity for the alpha1a receptor subtype among the listed drugs?
Why is tamsulosin recommended to be administered with food?
Why is tamsulosin recommended to be administered with food?
Which reversible alpha1 antagonist has significant first-pass metabolism?
Which reversible alpha1 antagonist has significant first-pass metabolism?
Which alpha1 antagonist is eliminated in feces and has plasma elimination which is biphasic?
Which alpha1 antagonist is eliminated in feces and has plasma elimination which is biphasic?
What is the primary route of elimination for prazosin?
What is the primary route of elimination for prazosin?
Which drug has active metabolites that contribute to its pharmacological effect, especially in the presence of renal failure?
Which drug has active metabolites that contribute to its pharmacological effect, especially in the presence of renal failure?
That should be administered with a meal to increase bioavailability and decrease the risk for adverse effects?
That should be administered with a meal to increase bioavailability and decrease the risk for adverse effects?
Which neurotransmitter is associated with the parasympathetic nervous system?
Which neurotransmitter is associated with the parasympathetic nervous system?
How can changes in resting activity occur in organs?
How can changes in resting activity occur in organs?
Which receptors are located in the smooth muscle of the eyes, arterioles, venules, bronchioles, liver, pancreas, and GI and GU systems?
Which receptors are located in the smooth muscle of the eyes, arterioles, venules, bronchioles, liver, pancreas, and GI and GU systems?
Where are intravenous forms of drugs generally NOT used according to the text?
Where are intravenous forms of drugs generally NOT used according to the text?
Which receptors are NOT involved in adrenergic agonists' action?
Which receptors are NOT involved in adrenergic agonists' action?
Which neurotransmitter, along with epinephrine and norepinephrine, is released by the sympathetic nervous system?
Which neurotransmitter, along with epinephrine and norepinephrine, is released by the sympathetic nervous system?
What is the primary metabolite of methyldopa that is stored in adrenergic nerve vesicles?
What is the primary metabolite of methyldopa that is stored in adrenergic nerve vesicles?
Which drug in the class of centrally acting alpha2 agonists should be avoided in patients with a history of bradycardia?
Which drug in the class of centrally acting alpha2 agonists should be avoided in patients with a history of bradycardia?
Which drug demonstrates significant first-pass metabolism and is metabolized by CYP 3A4 to inactive sulfate metabolites?
Which drug demonstrates significant first-pass metabolism and is metabolized by CYP 3A4 to inactive sulfate metabolites?
In what way do patients with renal failure experience increased adverse effects related to methyldopa?
In what way do patients with renal failure experience increased adverse effects related to methyldopa?
Which drug in this class is not completely absorbed in the gut and is absorbed via an aromatic amino acid transport system?
Which drug in this class is not completely absorbed in the gut and is absorbed via an aromatic amino acid transport system?
What is the primary pharmacotherapeutic precaution for the use of methyldopa and clonidine in patients with cerebrovascular disease?
What is the primary pharmacotherapeutic precaution for the use of methyldopa and clonidine in patients with cerebrovascular disease?
Which enzyme is primarily responsible for the metabolism of silodosin?
Which enzyme is primarily responsible for the metabolism of silodosin?
What is the primary route of elimination for the metabolites of alfuzosin?
What is the primary route of elimination for the metabolites of alfuzosin?
What percentage of the administered dose of tamsulosin is eliminated unchanged in the urine?
What percentage of the administered dose of tamsulosin is eliminated unchanged in the urine?
What is the half-life of the active metabolite of silodosin?
What is the half-life of the active metabolite of silodosin?
Which of the following enzymes is responsible for the metabolism of alfuzosin?
Which of the following enzymes is responsible for the metabolism of alfuzosin?
What is the primary mechanism by which selective alpha1 antagonists like doxazosin reduce bladder outflow obstruction?
What is the primary mechanism by which selective alpha1 antagonists like doxazosin reduce bladder outflow obstruction?
Which subtype of the alpha1 receptors is the most predominant in the prostate, making up approximately 70% of the alpha1 receptors?
Which subtype of the alpha1 receptors is the most predominant in the prostate, making up approximately 70% of the alpha1 receptors?
Which alpha1 antagonist demonstrates the highest selectivity for the alpha1a receptor subtype?
Which alpha1 antagonist demonstrates the highest selectivity for the alpha1a receptor subtype?
Which pharmacokinetic property of tamsulosin is different from the other alpha1 antagonists discussed?
Which pharmacokinetic property of tamsulosin is different from the other alpha1 antagonists discussed?
What is the primary route of elimination for prazosin?
What is the primary route of elimination for prazosin?
Which of the following is a common adverse effect associated with the use of centrally acting alpha2 agonists like clonidine and methyldopa?
Which of the following is a common adverse effect associated with the use of centrally acting alpha2 agonists like clonidine and methyldopa?
What is the primary reason for the increased use of medications other than methyldopa for the treatment of hypertension during pregnancy?
What is the primary reason for the increased use of medications other than methyldopa for the treatment of hypertension during pregnancy?
What is the primary reason for the use of the transdermal formulation of clonidine?
What is the primary reason for the use of the transdermal formulation of clonidine?
Which class of alpha antagonists is specifically used for relieving symptoms associated with benign prostatic hypertrophy (BPH)?
Which class of alpha antagonists is specifically used for relieving symptoms associated with benign prostatic hypertrophy (BPH)?
What is the primary consequence of major drug interactions with these alpha-blocker medications?
What is the primary consequence of major drug interactions with these alpha-blocker medications?
Which class of receptors are mostly associated with excitation or stimulation?
Which class of receptors are mostly associated with excitation or stimulation?
What is the primary mechanism of action of centrally acting alpha2 agonists like clonidine?
What is the primary mechanism of action of centrally acting alpha2 agonists like clonidine?
Why is it important to gradually taper the dose when discontinuing centrally acting alpha2 agonists?
Why is it important to gradually taper the dose when discontinuing centrally acting alpha2 agonists?
Which neurotransmitter stimulates all four types of adrenergic receptors (alpha1, alpha2, beta1, and beta2)?
Which neurotransmitter stimulates all four types of adrenergic receptors (alpha1, alpha2, beta1, and beta2)?
Which class of drugs is used mainly for their bronchodilating effects?
Which class of drugs is used mainly for their bronchodilating effects?
What is the primary reason for using the transdermal formulation of clonidine?
What is the primary reason for using the transdermal formulation of clonidine?
Which class of alpha antagonists is specifically used for relieving symptoms associated with benign prostatic hypertrophy (BPH)?
Which class of alpha antagonists is specifically used for relieving symptoms associated with benign prostatic hypertrophy (BPH)?
Which branch of the autonomic nervous system is targeted by adrenergic agonists?
Which branch of the autonomic nervous system is targeted by adrenergic agonists?
What is the primary function of peripherally acting alpha-adrenergic agonists?
What is the primary function of peripherally acting alpha-adrenergic agonists?
Which statement is true regarding the use of clonidine and methyldopa in older adult patients?
Which statement is true regarding the use of clonidine and methyldopa in older adult patients?
What is a common adverse reaction associated with clonidine and methyldopa at higher doses?
What is a common adverse reaction associated with clonidine and methyldopa at higher doses?
Why are clonidine and methyldopa not well suited for monotherapy?
Why are clonidine and methyldopa not well suited for monotherapy?
In which age group do clonidine and methyldopa have pediatric doses approved for use?
In which age group do clonidine and methyldopa have pediatric doses approved for use?
Which drug is specifically available in a transdermal formulation for better adherence to treatment regimens?
Which drug is specifically available in a transdermal formulation for better adherence to treatment regimens?
What is the primary reason for starting clonidine and methyldopa at the lowest recommended dose?
What is the primary reason for starting clonidine and methyldopa at the lowest recommended dose?
Which drug works better in adults but should be used cautiously in older adult patients?
Which drug works better in adults but should be used cautiously in older adult patients?
How is clonidine now available for children (ages 6 to 17) for treating ADHD?
How is clonidine now available for children (ages 6 to 17) for treating ADHD?
What has resulted in improved concentration and reduced behavioral symptoms in some children with ADHD?
What has resulted in improved concentration and reduced behavioral symptoms in some children with ADHD?
What should be done for safe administration when using clonidine for treating ADHD?
What should be done for safe administration when using clonidine for treating ADHD?
What is the primary advantage of using a transdermal system for clonidine administration?
What is the primary advantage of using a transdermal system for clonidine administration?
What is the Pregnancy Category of methyldopa in an injectable form?
What is the Pregnancy Category of methyldopa in an injectable form?
Which symptom has been specifically associated with guanabenz among the centrally acting alpha2 agonists?
Which symptom has been specifically associated with guanabenz among the centrally acting alpha2 agonists?
What is the major adverse reaction related to centrally acting alpha2 agonists like clonidine and methyldopa?
What is the major adverse reaction related to centrally acting alpha2 agonists like clonidine and methyldopa?
Which drug interaction can result in potentially life-threatening hypertension if abruptly discontinued with clonidine or methyldopa?
Which drug interaction can result in potentially life-threatening hypertension if abruptly discontinued with clonidine or methyldopa?
What is a common adverse reaction associated with guanabenz and clonidine but not with methyldopa?
What is a common adverse reaction associated with guanabenz and clonidine but not with methyldopa?
Which drug should be withdrawn first to prevent excessive unopposed stimulation of alpha2 receptors that can result in a hypertensive crisis?
Which drug should be withdrawn first to prevent excessive unopposed stimulation of alpha2 receptors that can result in a hypertensive crisis?
What is the primary reason for the cautious use of centrally acting alpha2 agonists in patients with renal function impairment?
What is the primary reason for the cautious use of centrally acting alpha2 agonists in patients with renal function impairment?
Which symptom is NOT more commonly associated with guanabenz compared to other centrally acting alpha2 agonists?
Which symptom is NOT more commonly associated with guanabenz compared to other centrally acting alpha2 agonists?
What major body system are the adverse reactions related to centrally acting alpha2 agonists mainly affecting?
What major body system are the adverse reactions related to centrally acting alpha2 agonists mainly affecting?
In what form has clonidine been associated with a rash that is an allergic reaction to the adhesive on the patch?
In what form has clonidine been associated with a rash that is an allergic reaction to the adhesive on the patch?
What is the most common adverse reaction associated with drugs that control hypertension?
What is the most common adverse reaction associated with drugs that control hypertension?
How should patients on transdermal clonidine systems address a loosened patch?
How should patients on transdermal clonidine systems address a loosened patch?
What action should be taken if a patient on methyldopa experiences significant weight gain within a day?
What action should be taken if a patient on methyldopa experiences significant weight gain within a day?
What is the recommended approach to prevent rebound hypertension when withdrawing drugs like methyldopa?
What is the recommended approach to prevent rebound hypertension when withdrawing drugs like methyldopa?
What is the primary reason for instructing patients not to cut or trim transdermal clonidine patches?
What is the primary reason for instructing patients not to cut or trim transdermal clonidine patches?
What lifestyle changes are encouraged in addition to drug therapy for hypertension management?
What lifestyle changes are encouraged in addition to drug therapy for hypertension management?
Which of the following is a key difference between phentolamine and phenoxybenzamine?
Which of the following is a key difference between phentolamine and phenoxybenzamine?
Why are nonselective alpha antagonists like phentolamine and phenoxybenzamine not used for the treatment of hypertension?
Why are nonselective alpha antagonists like phentolamine and phenoxybenzamine not used for the treatment of hypertension?
How do selective alpha1 antagonists like doxazosin lower blood pressure?
How do selective alpha1 antagonists like doxazosin lower blood pressure?
Which of the following statements is true regarding the use of selective alpha1 antagonists like tamsulosin, alfuzosin, and silodosin?
Which of the following statements is true regarding the use of selective alpha1 antagonists like tamsulosin, alfuzosin, and silodosin?
What is the primary reason the ALLHAT trial found an increased risk of heart failure with the use of the alpha1 antagonist doxazosin?
What is the primary reason the ALLHAT trial found an increased risk of heart failure with the use of the alpha1 antagonist doxazosin?
How do selective alpha1 antagonists like tamsulosin, alfuzosin, and silodosin relieve the symptoms of benign prostatic hyperplasia (BPH)?
How do selective alpha1 antagonists like tamsulosin, alfuzosin, and silodosin relieve the symptoms of benign prostatic hyperplasia (BPH)?
What is the primary reason that the nonselective alpha antagonists phentolamine and phenoxybenzamine are used in the treatment of pheochromocytoma?
What is the primary reason that the nonselective alpha antagonists phentolamine and phenoxybenzamine are used in the treatment of pheochromocytoma?
Which of the following is a potential adverse effect associated with the use of nonselective alpha antagonists like phentolamine and phenoxybenzamine?
Which of the following is a potential adverse effect associated with the use of nonselective alpha antagonists like phentolamine and phenoxybenzamine?
Flashcards are hidden until you start studying
Study Notes
Penicillin Subclasses
- There are four penicillin subclasses:
- Penicillinase-sensitive or natural penicillins
- Aminopenicillins
- Penicillinase-resistant or antistaphylococcal penicillins
- Antipseudomonal or extended-spectrum penicillins
Pharmacodynamics
- Penicillins inhibit bacterial cell wall formation by binding to penicillin-binding proteins (PBPs)
- PBPs include transpeptidase, carboxypeptidase, and endopeptidase enzymes
- Penicillins are bactericidal against sensitive organisms and are most effective during active cellular multiplication
- Human cells lack a cell wall, so there is virtually no action against host cells
Natural Penicillins
- There are four commercially available natural penicillins:
- Penicillin V (administered orally)
- Procaine penicillin and benzathine penicillin (administered intramuscularly)
- Penicillin G (administered intravenously)
- Active against aerobic, gram-positive organisms, including Streptococcus species, Enterococcus, and some non-penicillinase-producing staphylococci
- Only 5-15% of community-acquired Staphylococcus aureus remains susceptible to natural penicillins
Aminopenicillins
- Have reliable activity against gram-positive organisms, including Streptococcus and Enterococcus species
- Have greater activity against gram-negative bacteria due to enhanced ability to penetrate the outer membrane
- Available aminopenicillins:
- Ampicillin
- Amoxicillin
- Often combined with beta-lactamase inhibitors (clavulanic acid and sulbactam, respectively) for enhanced gram-negative and anaerobic activity
- Have excellent activity against methicillin-susceptible Staphylococcus aureus, Streptococcus and Enterococcus species, and others
Penicillinase-Resistant Penicillins
- Active against Streptococcus species, methicillin-susceptible Staphylococcus aureus, and some coagulase-negative staphylococci
- Not active against Enterococcus species, Listeria, gram-negative bacteria, and most anaerobes
- Chemical modifications of penicillin yields this class of antibiotics that is stable in the presence of penicillinase produced by staphylococci
Antipseudomonal Penicillins
- Comprised of piperacillin combined with a beta-lactamase inhibitor, tazobactam
- Has enhanced activity against gram-negative bacilli, particularly Pseudomonas aeruginosa and others
- Retains activity against ampicillin-sulbactam-susceptible organisms
Resistance to Penicillins
- Due to:
- Inactivation by beta-lactamases
- Alteration in target PBPs on the bacterial cell wall
- Alteration in the outer membrane of the cell wall that decreases permeability to the site of action
- Beta-lactamase production is the most common mechanism
- Beta-lactamase inhibitors (clavulanate, sulbactam, and tazobactam) have minimal antibacterial activity but irreversibly inactivate beta-lactamase enzymes produced by bacteria
Pharmacokinetics
- Absorption and distribution of penicillins depend on the specific structure of the antibiotic, pH of the stomach and intestine, and presence of food
- Penicillin V and dicloxacillin are the only natural and penicillinase-resistant penicillins that have oral absorption adequate to be recommended
- Amoxicillin is more completely absorbed than ampicillin
- Penicillins are bound to plasma proteins to varying degrees and are well-distributed to most tissues and body fluids
- Inflammation enhances penetration of the meninges, joints, and eye fluids, which are otherwise poorly penetrated### Centrally Acting Alpha2 Agonists
- Clonidine, guanfacine, and methyldopa are centrally acting alpha2 agonists used to treat hypertension and ADHD.
- They decrease sympathetic outflow from the CNS, leading to decreased blood pressure and heart rate.
Pregnancy and Lactation
- Clonidine crosses the placenta, but no well-controlled studies have been done in pregnant women.
- Methyldopa and guanfacine are Category B in oral form, but methyldopa is Category C in injectable form.
- Methyldopa appears in breast milk and should be used with caution in nursing women.
- Long-term follow-up of children born to women treated with methyldopa did not find any significant effects.
Adverse Drug Reactions
- Major adverse reactions include:
- Drowsiness
- Dry mouth
- Constipation
- Urinary retention
- Impotence
- Nightmares and insomnia (associated with clonidine)
- Cardiac symptoms (hypotension, chest pain, bradycardia)
- GI symptoms (abdominal pain, vomiting, anorexia, altered taste)
- Gynecomastia (associated with guanabenz and clonidine)
- Life-threatening rebound hypertension (HTN) after sudden withdrawal
- All patients should be warned about the possibility of rebound HTN and should be tapered gradually.
Drug Interactions
- Additive sedative effects with CNS depressants
- Additive hypotensive effects with other drugs that reduce blood pressure
- Tricyclic antidepressant (TCA) agents decrease the antihypertensive effects
- Beta-adrenergic blockers interact with clonidine and methyldopa to produce potentially life-threatening HTN
Clinical Use and Dosing
- Centrally acting alpha2 agonists are used to treat mild to moderate HTN and are second-line drugs.
- Methyldopa is first-line therapy for pregnant patients.
- Clonidine and methyldopa can be used effectively with a diuretic to address sodium and water retention.
- Doses vary with each drug, but adverse reactions occur at higher doses and with older adults.
Unlabeled Uses of Clonidine
- Clonidine has been evaluated for many off-label uses, including:
- Lowering adrenergic stimulation associated with alcohol, heroin, and nicotine withdrawal
- Reducing symptoms of withdrawal
Rational Drug Selection
- Age: Only clonidine and methyldopa have pediatric doses and are approved for use in children.
- Pregnancy: Methyldopa was traditionally the drug of choice for pregnant women, but now other medications are also selected.
- Route of administration: Clonidine is available in a transdermal formulation.
Monitoring
- Clinical monitoring of blood pressure is appropriate for all drugs in this class.
- Baseline blood pressure should be taken before initiating therapy and with each change in dosage.
- Weight and other indicators of fluid status should also be monitored.
Patient Education
- Administration: Take the drug exactly as prescribed, at the same time each day.
- Missed doses: Take as soon as remembered, unless it's almost time for the next dose.
- Withdrawal: Must be withdrawn slowly over 2-3 days to prevent rebound hypertension.
- Interactions: Avoid concurrent use of alcohol or other CNS depressants.
- Adverse reactions: Report any weight gain, swelling, or other symptoms to the healthcare provider.
Adrenergic Antagonists
- Act directly by blocking adrenergic receptors or indirectly by decreasing NE release within SNS terminals.
- Most clinically useful actions result from the blockade of alpha1 receptors in blood vessels, beta1 receptors in the heart, and alpha1 receptors in the bladder neck and prostate gland.
Alpha1 Antagonists
- Nonselective alpha antagonists: Phentolamine and phenoxybenzamine
- Selective alpha1 antagonists: Doxazosin, prazosin, terazosin, tamsulosin, alfuzosin, and silodosin
- Used to treat hypertension and relieve outflow obstruction secondary to benign prostatic hypertrophy (BPH)### Alpha1 Receptors and Selective Blockers
- Alpha1 receptors are found in the prostate, bladder, and other smooth muscles, and are involved in the regulation of bladder outflow obstruction and prostate smooth muscle contraction.
- Three subtypes of alpha1 receptors have been identified: alpha1a, alpha1b, and alpha1d.
- Approximately 70% of alpha1 receptors in the prostate are of the subtype 1a, which are localized to the prostatic stroma.
- Development of a selective alpha1a receptor antagonist would be advantageous in treating BPH, as it would reduce ADRs theoretically mediated by alpha1b and alpha1d receptor subtypes.
Alpha1 Antagonists
- Alpha1 antagonists are used to treat BPH and reduce bladder outflow obstruction without affecting bladder contractility.
- Large numbers of alpha1 receptors are found in the base of the bladder and prostate.
- Doxazosin, terazosin, and alfuzosin are selective for alpha1a, alpha1b, and alpha1d receptors, respectively.
- Silodosin demonstrates a 583-fold selectivity for the alpha1a receptor subtype and 56-fold selectivity for the alpha1d receptor subtype.
Pharmacokinetics and Pharmacodynamics
- Five of the alpha1 antagonists are well absorbed after oral administration, except for silodosin.
- Absorption of alfuzosin is reduced by 50% in a fasting state, and taking tamsulosin in a fasting state increases bioavailability and Cmax.
- All drugs in this class are widely distributed in the body and are highly protein bound.
- Doxazosin accumulates in breast milk, while prazosin is found in small amounts, and it is not known if terazosin is excreted in breast milk.
- Reversible alpha1 antagonists are extensively metabolized by the liver and excreted in both feces and urine.
Adrenergic Agonists
- Adrenergic agonists target the sympathetic nervous system (SNS) by direct receptor binding to organs or tissues, promotion of NE release, or mimicking the action of NE or epinephrine.
- The four main receptor types involved in this process are alpha1, alpha2, beta1, and beta2.
Centrally Acting Alpha2 Agonists
- Centrally acting alpha2 agonists are used to treat hypertension and ADHD.
- They activate alpha2 receptors in the brain, reducing sympathetic tone and increasing parasympathetic tone.
- They decrease peripheral resistance, heart rate, blood pressure, and renal vascular resistance.
- Examples of centrally acting alpha2 agonists include clonidine, guanabenz, and guanfacine.
Clonidine
- Clonidine is used to treat hypertension, ADHD, and symptoms of opioid or alcohol withdrawal.
- It is available in oral and transdermal forms.
- It is used off-label to treat symptoms of nicotine withdrawal and to reduce adrenergic stimulation associated with heroin withdrawal.
- It is used as an adjunct therapy or monotherapy to treat ADHD in children and adults.
Methyldopa
- Methyldopa is used to treat hypertension, especially in pregnant women.
- It is used off-label to treat ADHD and symptoms of opioid or alcohol withdrawal.
- It is used in combination with a diuretic to address sodium and water retention.
Guanabenz and Guanfacine
- Guanabenz and guanfacine are used to treat hypertension and ADHD.
- They are used off-label to treat symptoms of opioid or alcohol withdrawal.
- Guanfacine is available in an extended-release form and is used to treat ADHD in children and adults.
Studying That Suits You
Use AI to generate personalized quizzes and flashcards to suit your learning preferences.
