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Autonomic Nervous System: Parasympathetic vs Sympathetic Activity

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What are the two opposing branches of the autonomic nervous system (ANS) that maintain the resting activity of organs?

Sympathetic nervous system and parasympathetic nervous system

Which neurotransmitter is associated with the parasympathetic nervous system (PNS)?

Acetylcholine

How can changes in resting activity occur in organs according to the text?

By decreasing the activity of either the PNS or the SNS

Which statement about adverse drug effects (ADRs) is accurate based on the text?

ADRs may have a therapeutic effect on target organs and an adverse effect on ancillary organs

What is the primary focus of this chapter according to the text?

Use of drugs in primary care by advanced practice nurses to treat various conditions

Which type of drugs target the sympathetic nervous system (SNS) by direct receptor binding or mimicking the action of norepinephrine (NE) or epinephrine?

Peripherally acting alpha-adrenergic agonists

Which of the following is NOT a common adverse reaction in trials of methyldopa?

Insomnia

What is the metabolic fate of approximately 50% of guanfacine's oral dose?

Converted to inactive sulfate metabolites

In patients with renal failure, why do adverse effects of methyldopa increase?

Accumulation of methyldopa and its metabolites

Which of the following drugs has a significant first-pass effect?

Guanfacine

What is the primary reason for cautious use of clonidine in patients with a history of bradycardia?

Risk of mental depression

Why should methyldopa and clonidine be used cautiously in patients with cerebrovascular disease?

They cross the blood-brain barrier

What is the effect of stimulation of central alpha2 receptors by methyldopa's active metabolite?

Decrease in sympathetic outflow to the heart

Which of the following receptors are primarily associated with excitation or stimulation?

Alpha1 receptors

Where are alpha2 receptors primarily located?

Presynaptic nerve terminals of smooth muscles and islet cells of the pancreas

What is the primary function of beta1 receptors?

Stimulation of adenylyl cyclase to increase cAMP production

Which of the following receptors are stimulated by both norepinephrine (NE) and epinephrine?

Alpha1, alpha2, beta1, and beta2 receptors

What is the primary use of alpha1 agonists?

Decongestants

Which of the following is a central effect of alpha2 agonists?

Inhibition of cardioacceleration and vasoconstriction centers in the brain

Which of the following is a potential adverse effect of centrally acting alpha2 agonists used for hypertension?

Dry mouth

What is a potential consequence of abruptly stopping centrally acting alpha2 agonists?

Impaired homeostatic balance regulating SNS action

Which of the following is an approved use for guanfacine?

Both A and B

How does guanfacine reduce blood pressure?

By reducing sympathetic outflow by activating alpha2 receptors in the brain

Which alpha1 receptor subtype is the most prevalent in the prostate?

alpha1a

Which statement regarding the metabolism of tamsulosin is accurate?

It is extensively metabolized by CYP450 enzymes, with less than 10% eliminated unchanged.

Which of the following statements about alfuzosin metabolism is correct?

Approximately 11% of the administered drug is eliminated unchanged in the urine.

What is the primary reason that selective alpha1a receptor antagonists are advantageous for treating BPH?

They demonstrate fewer adverse drug reactions (ADRs)

Which enzyme is involved in the metabolism of silodosin?

CYP3A4

Which of the following is NOT a characteristic of the pharmacokinetics of the alpha1 antagonist drugs?

Demonstrate low protein binding

Which of the following alpha1 antagonist drugs has the lowest bioavailability?

Silodosin

Based on the information provided, what is true about the active metabolite of silodosin?

It has a half-life of approximately 24 hours.

Which alpha1 antagonist drug is known to accumulate in breast milk at a concentration 20 times that in maternal plasma?

Doxazosin

Which of the following statements about drug interactions with alpha-blockers is accurate?

They can lead to additive hypotension, with increased risk.

What is the primary reason that the absorption of alfuzosin is reduced when taken in a fasting state?

Alfuzosin should be administered with food

Which statement about the metabolism and excretion of doxazosin is true?

Doxazosin exhibits biphasic plasma elimination

What is the primary mechanism by which selective alpha1a receptor antagonists are thought to relieve lower urinary tract symptoms (LUTS) in BPH?

By a mechanism unrelated to prostate smooth-muscle relaxation

Which alpha1 antagonist drug demonstrates the highest selectivity for the alpha1a receptor subtype?

Silodosin

How does taking tamsulosin in a fasting state affect its pharmacokinetics?

Increases bioavailability by 30% and increases Cmax by 40-70%

Which of the following statements about clonidine is correct?

It can cause nightmares and insomnia as an adverse reaction.

Which drugs are well-suited for monotherapy in treating hypertension according to the text?

None of the drugs mentioned are well-suited for monotherapy

Which of the following statements about methyldopa is true?

It is the first-line therapy for hypertension in pregnant patients.

How can methyldopa and clonidine be used effectively for treating hypertension?

By combining them with a diuretic to address sodium and water retention

Which of the following adverse reactions is NOT associated with centrally acting alpha2 agonists?

Hypoglycemia

What is the recommended approach for dosing methyldopa and clonidine in treating hypertension?

Start with the lowest recommended dose and increase gradually

How can the sedation side effect associated with clonidine and methyldopa be minimized?

By dividing the dose with a higher dose in the evening

Which drug interaction is mentioned in the text for centrally acting alpha2 agonists?

Beta-adrenergic blockers should not be used concurrently with them.

Which of the following statements about the use of centrally acting alpha2 agonists in children is correct?

Methyldopa can be safely used in children, but clonidine cannot.

Which drug in this class is approved by the FDA for the treatment of ADHD in children?

Clonidine

For which age group is clonidine considered to work better in treating hypertension?

Adults

Which of the following adverse reactions is specifically associated with guanabenz?

Abdominal pain and vomiting

What should be done if a patient needs to discontinue both a centrally acting alpha2 agonist and a beta-adrenergic blocker?

Discontinue the beta-adrenergic blocker first.

Which drug formulation is available for patients who have difficulty taking pills or remembering frequent doses?

Transdermal clonidine

Which of the following is NOT a recommended monitoring parameter for patients taking methyldopa?

Liver function tests

What should be monitored for patients taking clonidine or methyldopa, especially those with renal impairment?

Serum creatinine levels

Which drug was traditionally considered the drug of choice for pregnant women with hypertension?

Methyldopa

Which of the following statements about the use of centrally acting alpha2 agonists in hypertension is correct?

They are used as second-line drugs when other drugs are not effective in achieving blood pressure control.

What is the recommended approach for monitoring blood pressure when using clonidine or methyldopa?

Take baseline blood pressure before initiating therapy and monitor with each dosage change

Which of the following adverse reactions is specifically associated with clonidine?

Pruritic rash

What is the primary reason for conducting liver function studies before and during methyldopa therapy?

To monitor for potential hepatotoxicity associated with methyldopa

How should patients take methyldopa to ensure proper dosing?

Take the missed dose as soon as possible, unless it's almost time for the next dose

What is a potential consequence of missing doses of methyldopa?

Increased risk of experiencing rebound hypertension

What should patients be aware of regarding potential drug-herbal interactions with methyldopa?

Methyldopa may interact with certain herbal supplements, so patients should inform their prescribers about any herbal use

How should patients apply the transdermal clonidine patch?

Apply the patch to a hairless area of intact skin on the upper arm or torso once every 7 days, using a different site from the previous application

What is the most common adverse reaction associated with methyldopa and clonidine?

Hypotension (low blood pressure)

What should patients do to minimize the risk of hypotension while taking methyldopa or clonidine?

Avoid alcohol and other CNS depressants, and drink an adequate amount of non-caffeinated fluids

What should patients report to their healthcare provider while taking methyldopa?

Any weight gain of more than 2 lb (1 kg) in 1 day, which may indicate fluid retention

What should patients be encouraged to do in addition to taking medication for hypertension management?

Adhere to lifestyle interventions such as weight loss, exercise, low-sodium diet, smoking cessation, and stress management

What is the primary mechanism of action of adrenergic antagonists in the treatment of hypertension?

They block adrenergic receptors or decrease norepinephrine release within sympathetic nervous system terminals

What is the main reason nonselective alpha antagonists are not used in the treatment of hypertension?

They block presynaptic alpha2 receptors resulting in reflex cardiac stimulation

Which statement about selective alpha1 antagonists is true?

Tamsulosin, alfuzosin, and silodosin have minimal effect on blood pressure

What is the primary pharmacodynamic effect of reversible alpha1 antagonists?

Decrease in peripheral vascular resistance

Why are prazosin and terazosin less likely to cause reflex tachycardia compared to other alpha1 antagonists?

They are more selective for alpha1 receptors in the vasculature

Which drug was found to have an increased risk of heart failure (HF) in comparison to chlorthalidone according to the ALLHAT trial?

Doxazosin

What is one of the reasons tamsulosin, silodosin, and alfuzosin have not been approved for hypertension treatment?

Increased selectivity for alpha1 receptors in the prostate

Learn about how the parasympathetic and sympathetic branches of the autonomic nervous system work together to maintain the resting activity of organs. Discover how changes in activities of these systems can affect organ functions.

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