CNS - Cholinergics A ntagonists - INTRO - Sympatholytic

33 important questions on CNS - Cholinergics A ntagonists - INTRO - Sympatholytic

What are the three categories of adrenergic antagonists under sympatholytics?

  • a-blockers: e.g., Prazocin, Doxazocin, Phentamine, Phenoxabenzamine
  • Beta-Blockers: e.g., Propranolol, Atenolol, Acetabutolol, Labetalol, Pindolol, Metoprolol
  • Drugs affecting Neurotransmitters: e.g., Methyldopa, Reserpine, Guanethidine

What are the alpha-blockers listed under other adrenergic antagonist drugs?

The alpha-blockers listed under other adrenergic antagonist drugs include:
  • Labetalol

What drugs are used for hypertension and what is their pharmacological effect?

  • Drugs used: Atenolol, Nadolol, Metoprolol, etc.
  • Pharmacological effect: Reduce cardiac output, reduce RAAS activation, etc.
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Name the beta-blockers mentioned in the list of other adrenergic antagonist drugs.

The beta-blockers mentioned include:
  • Labetalol
  • Sotalol
  • Pindolol
  • Timolol
  • Metoprolol
  • Acebutolol
  • Nadolol, etc

What do adrenergic antagonists do when they bind to adrenergic receptors?

Adrenergic antagonists bind to adrenergic receptors but do NOT activate the receptors and block the receptors-mediated effects of endogenous catecholamines (and exogenous agonists).

Which drug is used for angina pectoris and what is its effect?

  • Drugs used: Propranolol, etc.
  • Pharmacological effect: Reduce cardiac workload, rate & force.

What is the pharmacological effect of Esmolol and Propranolol in arrhythmia prophylaxis?

  • Drugs used: Esmolol, Propranolol, etc.
  • Pharmacological effect: Reduce automaticity and SA node rate.

Which drugs are used for chronic heart failure and what is their effect?

  • Drugs used: Carvedilol, Labetalol, Metoprolol
  • Pharmacological effect: Intrinsic vasodilator effect, reduce cardiac workload.

What is the effect of Propranolol and Nadolol on portal hypertension and esophageal varices?

  • Drugs used: Propranolol, Nadolol
  • Pharmacological effect: Vasoconstriction decreases pressure inside varices reducing risks of bleeding.

How does Propranolol affect familial tremor ('stage freight')?

  • Drugs used: Propranolol
  • Pharmacological effect: CNS effect & reduces β2 alteration of NMJ transmission.

What is the pharmacological effect of Propranolol and Esmolol in thyrotoxicosis?

  • Drugs used: Propranolol, Esmolol
  • Pharmacological effect: Reduce conversion of T4 to T3; reduce cardiac rate & workload.

What is carvedilol used for in chronic therapy?

Carvedilol is used for chronic therapy of CHF with reduced ejection fraction. It helps manage heart failure by improving heart function and reducing symptoms.

Which beta-blocker is approved by the FDA for CHF due to its cardio-selective nature and minimal side effects?

Betablockers approved by FDA for CHF are mostly cardio-selective for minimum side effects, specifically bisoprolol.

How does carvedilol help patients with HBP and left ventricular dysfunction?

Carvedilol is used for HBP and left ventricular dysfunction following MI in clinically stable patients. It aids in stabilizing heart function post-myocardial infarction.

What do B-blockers cause that interferes with metabolic and autonomic responses?

B-blockers cause glucose tolerance and interfere with metabolic and autonomic responses to hypoglycemia.

What benefits do carvedilol and metoprolol studies show for long-term use in CHF patients?

Carvedilol and metoprolol studies show long-term use improves ventricular function and symptoms of CHF and reduces hospital re-admission and decreases mortality.

What role do b-blockers play in treating angina?

B-blockers reduce cardiac work, improving exercise tolerance and relieving symptoms. Short acting nitrates are good for rapid symptomatic relief.

In asthma, where are Beta-blockers contraindicated, which selective Beta-blockers are used?

In asthma, where Beta-blockers are contraindicated, Selective B1 blockers with less effect on Beta 2, such as atenolol, bisoprolol, metoprolol, nebivolol, esmolol, acebutolol, and betaxolol, are used.

In which patients should B-blockers be avoided, especially when combined with thiazide diuretics?

Avoid in diabetic patients with frequent episodes of hypoglycemia, especially when combined with thiazide diuretics that also cause glucose tolerance.

How does carvedilol differ from cardioselective beta-blockers like metoprolol in its action on heart failure?

Carvedilol is complex non-selective, representing comprehensive antagonism of heart failure. It affects alpha-1 receptors, blocking stress responses that increase heart rate and BP, enhancing cardioprotection.

What are long acting nitrates used for, and what is their onset?

Long acting nitrates like isosorbide dinitrate/mononitrate have a slower onset and are used for prophylaxis, especially in sustained release formulations (duration 12 hours or more).

Why are B-blockers contraindicated in patients with certain heart conditions?

They slow the heart and depress the myocardium, hence contraindicated in patients with second or third degree of heart block.

Why must cardio-selective Beta-blockers be used with monitoring and supervision by a specialist?

Cardio-selective Beta-blockers are not cardio-specific and still express side effects, hence they can be used with monitoring and supervision by the specialist.

Why should thiazides and B-blockers be avoided together in hypertension and diabetes?

Thiazides and B-blockers combined in hypertension and diabetes should be avoided due to comorbidities drug interaction and risks of developing diabetes.

What is a noted use of B-blockers despite their contraindications?

B-blockers can be used to control the pulse rate.

What are the characteristics of water-soluble beta blockers?

Water-soluble beta blockers like atenolol, nadolol, celiprolol, and sotalol cannot pass through the BBB, causing less sleep disturbance and nightmares. They are excreted by the kidneys, requiring dose reduction in renal impairment.

What factors affect the choice of beta blockers in treating diseases or patients?

Differences between beta blockers may affect choice in treating particular diseases or individual patients. Selection is determined by co-morbidities, prescriber experience, and patient preference for dosing frequency and adherence.

How are long-acting beta blockers administered?

Long-acting beta blockers such as atenolol, bisoprolol, cavedilol, nadolol, and celiprolol have a longer duration of action. They are given once a day or modified release and given twice daily in angina.

What effect can Sotalol have on the QT interval and ventricular arrhythmias?

Sotalol may prolong the QT interval and occasionally cause life-threatening ventricular arrhythmias. Care is required to avoid hypokalaemia in patients on sotalol.

How often are beta blockers with short duration administered?

Beta blockers with short duration are given twice or three times daily.

What activities do intrinsic sympathomimetic and partial agonist activities represent?

Intrinsic sympathomimetic activity and partial agonist activity represent the capacity to stimulate as well as to block adrenergic receptors. Carvedilol, Pindolol, celiprolol, and acebutolol have intrinsic sympathomimetic activity.

What additional effects do Labetalol, carvedilol, and nebivolol have?

Labetalol, carvedilol, nebivolol have in addition an arteriolar vasodilation thus lower peripheral resistance by diverse mechanism e.g. some act on alpha receptors.

How do beta blockers with intrinsic sympathomimetic activity affect bradycardia?

Beta blockers with intrinsic sympathomimetic activity cause less bradycardia than other beta blockers. They reduce resting heart rate more than others, hence avoided or used with caution in CHF and angina.

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