Antihypertensives
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Questions and Answers

What is the diastolic blood pressure range for Stage 2 hypertension?

  • 80 - 89 mmHg
  • 100 - 109 mmHg (correct)
  • > 110 mmHg
  • 90 - 99 mmHg

    • Which class of antihypertensive drugs primarily works by blocking CNS output?

  • Sympathoplegics (correct)
  • Calcium channel blockers
  • Diuretics
  • ACE inhibitors

    • Which of the following drugs is classified as a loop diuretic?

  • Metoprolol
  • Hydrochlorothiazide
  • Furosemide (correct)
  • Spironolactone

    • In what scenario is polydrug therapy required?

    <p>Stage 2 and 3 hypertension</p> Signup and view all the answers

    Which of the following is NOT categorized as a beta adrenoceptor blocker?

    <p>Verapamil</p> Signup and view all the answers

    What mechanism do ACE inhibitors use to lower blood pressure?

    <p>Decrease Angiotensin II production</p> Signup and view all the answers

    What is the primary effect of alpha 2 agonists like clonidine and methyldopa on sympathetic outflow?

    <p>Decrease sympathetic outflow</p> Signup and view all the answers

    How does methyldopa function as a prodrug in the treatment of hypertension?

    <p>It is metabolized into an agonist that decreases adrenergic outflow</p> Signup and view all the answers

    Which side effect is commonly associated with the use of methyldopa?

    <p>Parkinson-like symptoms</p> Signup and view all the answers

    What is the mechanism of action of clonidine in the treatment of hypertension?

    <p>It activates presynaptic alpha 2 receptors, inhibiting norepinephrine release</p> Signup and view all the answers

    What does the drug reserpine do in the context of sympathetic nervous system function?

    <p>It depletes norepinephrine stores</p> Signup and view all the answers

    What effect does activation of presynaptic alpha 2 receptors have on norepinephrine release?

    <p>It inhibits norepinephrine release</p> Signup and view all the answers

    Which of the following is NOT a characteristic of centrally acting antihypertensive agents like clonidine?

    <p>They directly block alpha 1 receptors</p> Signup and view all the answers

    Which of the following describes the mechanism of action of hydralazine?

    <p>Releases nitric oxide from endothelial cells</p> Signup and view all the answers

    What is a potential side effect of using hydralazine in high doses?

    <p>Tachycardia</p> Signup and view all the answers

    How does minoxidil exert its therapeutic effects?

    <p>It opens potassium channels in smooth muscle</p> Signup and view all the answers

    What is a notable characteristic of calcium channel blockers (CCBs) in their action?

    <p>They block voltage-gated L-Type calcium channels</p> Signup and view all the answers

    What is the primary action of nitroprusside in managing hypertension?

    <p>Releases nitric oxide to cause vasodilation</p> Signup and view all the answers

    Which of the following compounds is a dopamine D1 receptor agonist used for hypertensive crisis?

    <p>Fenoldopam</p> Signup and view all the answers

    Captopril and enalapril are classified as which type of antihypertensive agents?

    <p>ACE inhibitors</p> Signup and view all the answers

    What is the metabolite of nitroprusside that is cleared by the kidneys?

    <p>Thiocyanate</p> Signup and view all the answers

    What role does renin play in the renin-angiotensin system?

    <p>It converts angiotensinogen to Angiotensin I.</p> Signup and view all the answers

    What is a key difference between ACE inhibitors and Angiotensin II receptor blockers?

    <p>ACE inhibitors have a higher incidence of cough compared to ARBs.</p> Signup and view all the answers

    Which of the following correctly describes the effects of Angiotensin II?

    <p>It promotes sodium and water retention.</p> Signup and view all the answers

    What is a common side effect of ACE inhibitors experienced by some patients?

    <p>Chronic cough</p> Signup and view all the answers

    Which statement is true regarding the safety of ACE inhibitors during pregnancy?

    <p>They can cause renal damage to the fetus.</p> Signup and view all the answers

    What is the primary clinical effect of angiotensin II receptor blockers (ARBs)?

    <p>They provide the same clinical effects as ACE inhibitors.</p> Signup and view all the answers

    What is the function of aminopeptidase in relation to Angiotensin II?

    <p>It converts Ang II to inactive fragments.</p> Signup and view all the answers

    Which of the following drugs is considered an ACE inhibitor?

    <p>Captopril</p> Signup and view all the answers

    What is the primary role of Atrial natriuretic peptide (ANP)?

    <p>To counterbalance the renin-angiotensin-aldosterone system</p> Signup and view all the answers

    What does BNP specifically target to achieve its effects?

    <p>Lowered blood pressure</p> Signup and view all the answers

    Which of the following is true about BiDil®?

    <p>It contains isosorbide and hydralazine</p> Signup and view all the answers

    How does isosorbide enhance its cardiovascular effects?

    <p>By producing nitric oxide</p> Signup and view all the answers

    What genetic factor contributes to the differences in medication efficacy between African American patients and whites regarding ACE inhibitors?

    <p>Genetic polymorphism in the MSD720 gene</p> Signup and view all the answers

    Which of the following statements correctly characterizes the renin-angiotensin-aldosterone system's effect?

    <p>It raises blood pressure.</p> Signup and view all the answers

    What is a primary reason for noncompliance among patients taking antihypertensives?

    <p>Forgetfulness about medication</p> Signup and view all the answers

    What term describes when a patient correctly takes medication only for five days prior to a doctor's appointment?

    <p>White-coat adherence</p> Signup and view all the answers

    Which of the following best describes the '1/6th Rule' related to patient adherence?

    <p>Classifications from perfect to none</p> Signup and view all the answers

    According to the survey of patients, which of these was reported as a reason for not filling prescriptions?

    <p>Delays in prescription filling</p> Signup and view all the answers

    What is the mechanism of action (MOA) of enalapril?

    <p>Inhibition of angiotensin-converting enzyme (ACE)</p> Signup and view all the answers

    What is the mechanism of action (MOA) of losartan?

    <p>Angiotensin II receptor antagonist</p> Signup and view all the answers

    What role does aldosterone play in the renin-angiotensin system's control of blood pressure?

    <p>It increases sodium reabsorption in the kidneys, leading to increased blood volume.</p> Signup and view all the answers

    Which of the following is an aim of drug treatment for hypertension? (Select all that apply)

    <p>Restrict dietary sodium intake, reduce blood volume (remove water)</p> Signup and view all the answers

    What do diuretics do?

    <p>Lower blood volume</p> Signup and view all the answers

    Which drugs alter water and sodium concentrations?

    <p>Diuretics</p> Signup and view all the answers

    Which of the following drugs alter sympathetic outflow? (Select all that apply)

    <p>Methyldopa</p> Signup and view all the answers

    What drugs are adrenergic neuron-blocking drugs? (Select all that apply)

    <p>reserpine</p> Signup and view all the answers

    Which drug is an adrenoceptor antagonist (alpha 1 blocker)?

    <p>Prazosin</p> Signup and view all the answers

    Which drugs are calcium channel blockers? (Select all that apply)

    <p>Diltiazem</p> Signup and view all the answers

    Which drugs are ACE inhibitors? (Select all that apply)

    <p>captopril</p> Signup and view all the answers

    What is the stem for Angiotensin II blockers?

    <p>-sartan</p> Signup and view all the answers

    Which of the following is an example of a thiazide?

    <p>hydrochlorothiazide</p> Signup and view all the answers

    Which drug blocks norepinephrine (NE) stores from being released?

    <p>Guanethidine</p> Signup and view all the answers

    Guanethidine crosses the blood-brain barrier (BBB).

    <p>False</p> Signup and view all the answers

    What is the major adverse drug reaction (ADR) of reserpine?

    <p>Depression</p> Signup and view all the answers

    What are the two primary actions of beta blocker drugs?

    <p>Reduce cardiac output and decrease vascular resistance</p> Signup and view all the answers

    Which of the following are oral vasodilators? (Select all that apply)

    <p>hydralazine</p> Signup and view all the answers

    Which of the following drugs are parenteral vasodilators?

    <p>nitroprusside</p> Signup and view all the answers

    Which of the following are actions of vasodilators? (Select all that apply)

    <p>Release of Nitric Oxide (NO)</p> Signup and view all the answers

    Describe the Renin, ACE, angiotensin pathway?

    <p>Low renal arterial pressure --&gt; release of renin by kidneys --&gt; converts angiotensinogen to angiotensin I --&gt; ACE converts to angiotensin II</p> Signup and view all the answers

    Which class of drugs should never be used in pregnancy?

    <p>ACE inhibitors</p> Signup and view all the answers

    What does Losartan do?

    <p>Block the receptor for Angiotensin II</p> Signup and view all the answers

    What is primary hypertension?

    <p>Hypertension for which the cause is unknown</p> Signup and view all the answers

    What is secondary hypertension?

    <p>A cause (like an adrenal tumor) is found, removed and hypertension cured</p> Signup and view all the answers

    Which drug is used to lower blood pressure in pregnancy?

    <p>Methyldopa</p> Signup and view all the answers

    What does Labetalol do and what does it treat?

    <p>blocks alpha and beta receptors and can be used to treat pheochromocytoma (adrenal tumor).</p> Signup and view all the answers

    How is esmolol administered?

    <p>Continuous slow IV infusion</p> Signup and view all the answers

    What is a common adverse drug reaction (ADR) of hydralazine?

    <p>Skin rashes and fever that resembles lupus erythematosus (LE), an autoimmune disorder</p> Signup and view all the answers

    What is an ADR of minoxidil (potassium channel enhancer)?

    <p>hypertrichosis</p> Signup and view all the answers

    Study Notes

    Pharmacology I - Chapter 11: Antihypertensives

    • A 35-year-old male patient, with a blood pressure of 150/95 mmHg, drinks alcohol, is sedentary, and does not smoke. He has a family history of hypertension and is moderately obese. His total cholesterol is 220 mg/dL, HDL is 40 mg/dL, and FBS is 105 mg/dL. Treatment needs to be considered.

    Case Study Treatment Recommendations

    • Treat first with behavioral changes: diet, exercise, and reduced alcohol consumption.
    • Initiate low-dose thiazide diuretic.
    • Monitor for a few months. If needed, add a second drug such as a calcium channel blocker or an ACE inhibitor.

    Hypertension Staging

    • Normal blood pressure is defined as 120/80 mmHg.
    • Hypertension is diagnosed when blood pressure is 140/90 mmHg or higher.
    • DBP (diastolic blood pressure) is used to stage hypertension.
      • Mild: DBP 90-104 mmHg
      • Moderate: DBP 105-114 mmHg
      • Severe: DBP > 115 mmHg

    Antihypertensive Agents

    • Drugs target various sites in the body to lower blood pressure. The figure illustrates different targets.

    Types of Hypertension

    • Primary hypertension (essential): accounts for over 95% of all cases. Cause is unknown. Approximately 27% of the US population has high blood pressure.
    • Secondary hypertension: accounts for less than 5% of cases. Caused by specific disorders affecting control mechanisms, including the renin system or tumors.

    Aims of Drug Treatment

    • Lower blood volume: diuretics restrict dietary sodium intake and reduce blood volume.
    • Reduce peripheral resistance: sympatholytics reduce peripheral resistance.
    • Relax smooth muscle: direct vasodilators relax smooth muscle.
    • Block or decrease Angiotensin II production: drugs target the renin-angiotensin system.

    Blood Pressure Monitoring

    • Using home blood pressure monitors helps eliminate "white coat" hypertension in some patients.
    • Approximately 20% of patients with elevated blood pressure have "white coat" hypertension.

    Staging Primary Hypertension

    • Stage 1: diastolic BP 90-99
    • Stage 2: diastolic BP 100-109
    • Stage 3: diastolic BP >110
    • Reducing diastolic blood pressure by 5-6 mmHg decreases the risk of stroke by 40%, risk of coronary disease by 16%, and risk of death from any cardiovascular cause by 20%.

    Antihypertensive Drug Classes

    • Diuretics: lower blood volume.
    • Sympatholytics: block CNS output, reduce peripheral resistance.
    • Direct vasodilators: relax smooth muscles, induce vasodilation.
    • Block Angiotensin: decrease Angiotensin II production.

    Drug Treatment of Hypertension

    • Drug treatment lowers systolic blood pressure by 10-15%.
    • Monotherapy is effective in approximately 50% of patients.
    • Using multiple drugs at lower doses may produce fewer side effects than using a single drug at high doses.
    • Patients with stage 2 and 3 hypertension often require poly-drug therapy.

    List of Drugs

    • Alter water and sodium: diuretics
    • Alter sympathetic outflow: methyldopa, clonidine
    • Adrenergic neuron blockers: guanethidine, reserpine
    • Alpha blockers: prazosin
    • Beta blockers: metoprolol, propranolol, bisoprolol
    • Calcium channel blockers: verapamil, diltiazem, nifedipine
    • ACE inhibitors: captopril, enalapril, benazepril
    • ANG II receptor blockers: losartan, valsartan, candesartan
    • Vasodilators: hydralazine, minoxidil, nitroprusside, fenoldopam
    • BNP agonist: nesiritide
    • BiDil: isosorbide/hydralazine

    Vasodilators

    • Drugs that dilate blood vessels through different mechanisms.
    • Some examples are hydralazine, minoxidil, nitroprusside, and fenoldopam.

    Calcium Channel Blockers (CCBs)

    • Block voltage-gated L-type calcium channels in cardiac and smooth muscle.
    • Calcium influx is blocked, preventing muscle contraction, causing vasodilation.

    Nitroprusside

    • Releases NO, stimulates guanylyl cyclase which increases cGMP, leading to myosin light chain dephosphorylation, and muscle relaxation.
    • Used as an IV drug in emergencies to lower blood pressure.

    Dopamine D1 Receptor Agonist

    • Fenoldopam results in arterial vasodilation.
    • IV administration is typically used for hypertensive crisis.

    ACE Inhibitors

    • Captopril, enalapril block ACE (angiotensin-converting enzyme), reducing Angiotensin II levels and aldosterone levels.

    ACE Inhibitors Mechanism of Action

    • Reduced renal arterial pressure releases renin from the kidney.
    • Renin converts angiotensinogen to angiotensin I.
    • ACE converts angiotensin I to angiotensin II.
    • Angiotensin II is a potent vasoconstrictor.
    • Aminopeptidase converts angiotensin II to inactive fragments.

    Angiotensin Antagonists - ACE Inhibitors

    • Block the formation of angiotensin II.
    • A second class of drugs that directly act on the renin-angiotensin system.

    Angiotensin II Receptor Blockers (ARBs)

    • Block the receptor for angiotensin II.
    • Similar clinical effects to ACE inhibitors but with lower incidence of cough.
    • Still may cause fetal kidney damage and should not be used in pregnancy.

    BNP Agonists

    • Brain natriuretic peptide (BNP) and Atrial natriuretic peptide (ANP) act to counter-balance the renin-angiotensin-aldosterone system (RAAS).
    • Nesiritide (Natrecor®) is a BNP agonist used as a slow IV drip to lower blood pressure.

    BiDil

    • First drug FDA approved for a specific ethnic group.
    • A combination of isosorbide dinitrate and hydralazine.
    • Both drugs were already widely used and available.
    • Data from clinical trials supported its use in African Americans.
    • Hydralazine acts by releasing NO from endothelial cells.

    Patient Compliance

    • Adherence to medication is crucial for efficacy.
    • Rates of adherence vary depending on the condition. Some patients have higher adherence rates for acute conditions than chronic ones, but chronic patients typically show adherence rates between 43 and 78%.
    • Poor compliance is also a major cost driver related to hospital admissions, estimated at $100 billion annually in the US.
    • Methods to measure or increase compliance include direct observation, indirect measures such as counting pills, medication monitoring devices, patient diaries, and support from family or nurses.
    • Factors like forgetting to take medication, or adverse effects, and high cost are among the reasons that patients cite for poor compliance.

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    PM716 C11 Antihypertensives Slides PDF

    Description

    This quiz covers the key concepts from Chapter 11 of Pharmacology I, focusing on antihypertensive treatments and guidelines. Explore the classification and management strategies for hypertension, along with the pharmacological agents used in treatment. Test your knowledge on dietary changes, medication options, and staging of hypertension.

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