Showing posts with label Cardioselective b1-Blocking Agent. Show all posts
Showing posts with label Cardioselective b1-Blocking Agent. Show all posts

Metoprolol (Lopressor)

Post a comment

Name: Metoprolol (Lopressor)

Class: Cardioselective b1-Blocking Agent

Mechanism: Selective blockade of b1 (heart, kidney) w/rel. sparing of b2. No a effect.

Absorption: Good oral (>95%). Bioavailability ~50%. Plasma levels vary 10x btwn. patients.

Dist.: 12% bound to protein. Metabolism.: Hepatic Excretion, : Short t½ (3-4 hr).

Toxicity/S.E.s: CV—hypotension, bradycardia, c/i for AV block. Resp—c/i in asthmatics, COPD, bronchitis, allergic rhinitis. Metabolism—caution w/diabetics (masks sign of hypoglycemia: tachycardia). CNS—weakness, fatigue, nightmares, depression. GI—n/v (uncommon). Hypersens—rash, hematologic disorders (rare).

Utility: Hypertension (¯ CO ® ¯ BP; blocks renin release). Angina pectoris (prophylactic ® ­ exercise tolerance due to ¯ O2 demand). Cardiac arrhythmias (esp. supravent. tachyarrhyths). Acute MI (prophylaxis and reduction of infarct size and failure). Pheochromocytoma (in comb. w/alpha blocker). Essential tremor. Migraine headache (prophylaxis). Performance anxiety.

Special Features: Abrupt w/drawal may trigger MI. Cardioselectivity not great. May be advantageous in asthmatic or diabetic hypertensives.

 

Esmolol (Breviblock)

Post a comment

Name: Esmolol (Breviblock)

Class: Cardioselective b1-Blocking Agent

Mechanism: Selective blockade of b1 (heart, kidney) w/rel. sparing of b2. No a effect.

Absorption: IV

Dist.:

Metabolism.: RBC esterases Excretion, : Ultrashort (10 min.).

Toxicity/S.E.s: CV—hypotension, bradycardia, c/i for CHF or AV block. Resp—c/i in asthmatics, COPD, bronchitis, allergic rhinitis. Metabolism—caution w/diabetics (masks signs of hypoglycemia: tachycardia). CNS—weakness, fatigue, nightmares, depression. GI—n/v (uncommon). Hypersens—rash, hematologic disorders (rare).

Utility: Acute cardiac arrhythmias (esp. supravent. tachyarrhythmias)—general anesthetics, thyrotoxicosis, digitalis toxicity. Perioperative hypertension. Acute MI (reduction of infarct size and failure).

Special Features: Ultrashort t½. Cardioselectivity not great.

 

Atenolol (Tenormin)

Post a comment

Name: Atenolol (Tenormin)

Class: Cardioselective b1-Blocking Agent

Mechanism: Selective blockade of b1 (heart, kidney) w/rel. sparing of b2. No a effect.

Absorption: Oral (>50%). Bioavailability ~40%. Plasma levels vary 4x btwn. patients.

Dist.: <5%>

Metabolism.: Excretion, : Renal (mostly unchanged). Long t½ (6-9 hr.)

Toxicity/S.E.s: CV—hypotension, bradycardia, c/i for CHF or AV block. Resp—c/i in asthmatics, COPD, bronchitis, allergic rhinitis. Metabolism—caution w/diabetics (masks signs of hypoglycemia: tachycardia). CNS—weakness, fatigue, nightmares, depression. GI—n/v (uncommon). Hypersens—rash, hematologic disorders (rare).

Utility: Hypertension (¯ CO ® ¯ BP; blocks renin release). Angina pectoris (prophylactic ® ­ exercise tolerance due to ¯ O2 demand). Cardiac arrhythmias (esp. supravent. tachyarrhyths). Acute MI (prophylaxis and reduction of infarct size and failure). Pheochromocytoma (in comb. w/alpha blocker). Essential tremor. Migraine headache (prophylaxis). Performance anxiety.

Special Features: Abrupt w/drawal may trigger MI. Cardioselectivity not great.

 

Metoprolol (Lopressor)

Post a comment

Name: Metoprolol (Lopressor)

Class: Cardioselective b1-Blocking Agent

Mechanism: Selective blockade of b1 (heart, kidney) w/rel. sparing of b2. No a effect.

Absorption: Good oral (>95%). Bioavailability ~50%. Plasma levels vary 10x btwn. patients.

Dist.: 12% bound to protein. Metabolism.: Hepatic Excretion, : Short t½ (3-4 hr).

Toxicity/S.E.s: CV—hypotension, bradycardia, c/i for CHF or AV block. Resp—c/i in asthmatics, COPD, bronchitis, allergic rhinitis. Metabolism—caution w/diabetics (masks signs of hypoglycemia: tachycardia). CNS—weakness, fatigue, nightmares, depression. GI—n/v (uncommon). Hypersens—rash, hematologic disorders (rare).

Utility: Hypertension (¯ CO ® ¯ BP; blocks renin release). Angina pectoris (prophylactic ® ­ exercise tolerance due to ¯ O2 demand). Cardiac arrhythmias (esp. supravent. tachyarrhyths). Acute MI (prophylaxis and reduction of infarct size and failure). Pheochromocytoma (in comb. w/alpha blocker). Essential tremor. Migraine headache (prophylaxis). Performance anxiety.

Special Features: Abrupt w/drawal may trigger MI. Cardioselectivity not great. May be advantageous in asthmatic or diabetic hypertensives.