Showing posts with label Nonselective b-Blocking Agent. Show all posts
Showing posts with label Nonselective b-Blocking Agent. Show all posts

Timolol (Blocadren)

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Name: Timolol (Blocadren)

Class: Nonselective b-Blocking Agent

Mechanism: Competitive blockade of b1 and b2 receptors. No a effect.

Absorption: Good oral (>90%). High bioavailability ~75%. Plasma levels vary 7x btwn. patients. b-blocking plasma conc. 5-10 ng/mL (low). Eye drops.

Dist.: 10% bound to protein. Excretion, t½: Hepatic, renal. 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. Eyedrops for open-angle glaucoma (¯ production of aqueous humor).

Spec. Features: Abrupt w/drawal may trigger MI. 6-10x as potent orally as others.

 

Nadolol (Corgard)

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Name: Nadolol (Corgard)

Class: Nonselective b-Blocking Agent

Mechanism: Competitive blockade of b1 and b2 receptors. No a effect.

Absorp.: Poor oral (>30%). Low bioavail: ~30%. Plasma levels vary 7x btwn. pts.

Dist.: 30% bound to protein.

Metabolism.: Excretion, : Renal. Long t½ (14-24 hr). Unchanged in urine.

Toxicity/S.E.s: CV—hypotension, bradycardia, c/i for AV block. May exacerbate angina (unopposed a receptor action). 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. Better pt. compliance than w/propranolol.

 

Propranolol (Inderal)

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Name: Propranolol (Inderal)

Class: Nonselective b-Blocking Agent

Mechanism: Competitive blockade of b1 and b2 receptors. No a effect. Decreases conversion of T4 to T3 by inhibiting hepatic monodeiodinase.

Absorp.: Good oral (>90%). Low bioavail.: ~30%. Plasma levels vary 20x btwn. patients.

Dist.:93% bound to protein. Enters CNS. Metabolism.: Hepatic Excret., : Short t½ (3.5-6 hr).

Toxicity/S.E.s: CV—hypotension, bradycardia. C/i for AV. May exacerbate angina (unopposed a receptor action). 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: Mild-mod HTN (¯ CO ® ¯ BP; blocks renin release). Adjunct to direct vasodilators for severe HTN (prevents reflex tachycardia). Angina pectoris (prophylactic ® ­ exercise tolerance 2° to ¯ O2 demand). Cardiac arrhythmias (esp. supravent. tachyarrhyths). Acute MI (prophylaxis & reduction of infarct size and failure). Modifies risk factors assoc. w/atherosclerosis. Increases O2 delivery to ischemic cardiac tissue.

Special Features: Abrupt w/drawal may trigger MI. Not as effective against variant angina as channel blockers and nitrates. Long-term antiarrhythmic b-blocker Rx ® ¯ mortality.

 

Propranolol (Inderal)

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Name: Propranolol (Inderal)

Class: Nonselective b-Blocking Agent

Mechanism: Competitive blockade of b1 and b2 receptors. No a effect. Decreases conversion of T4 to T3 by inhibiting hepatic monodeiodinase.

Absorption: Good oral (>90%). But low bioavailability ~30%. Plasma levels vary 20x btwn. patients.

Dist.:93% bound to protein. Enters CNS. Metabolism.: Hepatic Excret., : Short t½ (3.5-6 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 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. Thyrotoxicosis—Suppression of signs/symptoms of thyrotoxicosis. Most effective drug for treatment of thyrotoxic crisis or thyroid storm (usu. used in comb w/a thioamide and/or iodide. Can be used preop. for thyroid surg. Controversial Rx of hyperthyroid symptoms while awaiting effects of thioamide or iodide.

Special Features: Abrupt w/drawal may trigger MI.

 

Nadolol (Corgard)

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Name: Nadolol (Corgard)

Class: Nonselective b-Blocking Agent

Mechanism: Competitive blockade of b1 and b2 receptors. No a effect.

Absorp.: Poor oral (>30%). Low bioavail: ~30%. Plasma levels vary 7x btwn. pts.

Dist.: 30% bound to protein.

Metabolism.: Excretion, : Renal. Long t½ (14-24 hr). Unchanged in urine.

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. Better pt. compliance than w/propranolol.

 

Timolol (Blocadren)

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Name: Timolol (Blocadren)

Class: Nonselective b-Blocking Agent

Mechanism: Competitive blockade of b1 and b2 receptors. No a effect.

Absorption: Good oral (>90%). High bioavailability ~75%. Plasma levels vary 7x btwn. patients. b-blocking plasma conc. 5-10 ng/mL (low). Eye drops.

Dist.: 10% bound to protein. Excretion, t½: Hepatic, renal. 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. Eyedrops for open-angle glaucoma (¯ production of aqueous humor).

Spec. Features: Abrupt w/drawal may trigger MI. 6-10x as potent orally as others.

 

Propranolol (Inderal)

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Name: Propranolol (Inderal)

Class: Nonselective b-Blocking Agent

Mechanism: Competitive blockade of b1 and b2 receptors. No a effect. Decreases conversion of T4 to T3 by inhibiting hepatic monodeiodinase.

Absorp.: Good oral (>90%). Low bioavail.: ~30%. Plasma levels vary 20x btwn. patients.

Dist.:93% bound to protein. Enters CNS. Metabolism.: Hepatic Excret., : Short t½ (3.5-6 hr).

Toxicity/S.E.s: CV—hypotension, bradycardia, c/i for CHF[KLW1] 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: Mild-mod HTN (¯ CO ® ¯ BP; blocks renin release). Adjunct to direct vasodilators for severe HTN (prevents reflex tachycardia). Angina pectoris (prophylactic ® ­ exercise tolerance 2° ¯ O2 demand). Cardiac arrhythmias (esp. supravent. tachyarrhyths). Acute MI (prophylaxis & reduction of infarct size and failure). Pheochromocytoma (in comb. w/a -blocker). Essential tremor. Migraine headache (prophylaxis). Performance anxiety. Thyrotoxicosis—Suppression of signs/symptoms. Most effective drug for Rx of thyrotoxic crisis or thyroid storm (usu. in comb w/thioamide and/or iodide. Can be used preoperatively. Controversial Rx of hyperthyroid symptoms while awaiting effects of thioamides or iodide.

Special Features: Abrupt w/drawal may trigger MI.