Beta Adrenergic Receptor Antagonists Flashcards
Esmolol
1) Indications
2) Onset, DOA, Half Life, & VD
3) Metabolism
1) "Blunt SNS response to dVL and surgical stimuli or emergence. Tachycardia HTN For controlled hypotension with drip SVT"
2) "Onset: 30-60 sec DOA = 10-15mins E1/2t = 9 mins High Vd 55% PB"
3) Plasma esterases and excretion in the urine
Esmolol
1) Class
2) Action
1) Selective Beta 1 adrenergic antagonist
2) Reversibly binds to beta1 adrenergic receptor antagonists to inhibit the binding of NE, EPI, and other beta agonist, preventing the stimulation of G-coupled protein receptors, adenylate cyclase, and cAMP.
Slows SA rate, conduction through the AV node, decreases contractility = decreased cardiac O2 demand
Esmolol: Adverse Effects
Severe bradycardia Hypotension Heart block Syncope/dizziness Head ache CHF and pulmonary edema POI – propylene glycol"
Esmolol:
1) Contraindications
2) Dosage
1) "hypersensitivity CHF With CCB = complete heart block SSS Severe hypotension Pts who are heart rate dependent Asthma and COPD in high doses Pregnancy"
2) “5-10mg IV Q3-5mins to total dose of 80mg
0. 5mg/kg IV (10-180 mg IV)
Labetalol
1) Class
2) Action
1) Beta1, Beta 2, Alpha1 adrenergic antagonist
2) Reversibly binds to beta1, beta2, alpha1 adrenergic receptor antagonists to inhibit the binding of NE, EPI, and other beta agonist, preventing the stimulation of G-coupled protein receptors, adenylate cyclase, cAMP.
Slows SA node rate, conduction through the AV node, decreases contractility, causes peripheral, cerebral, and coronary vasodilation.
Labetalol
1) Indications
2) Onset, DOA, Half Life & VD
3) Metabolism
1) "HTN crisis Angina Aortic dissection Tachyarrthymias Clonidine withdrawal (beta 2 blocker) Pre-eclampsia"
2) "Onset = 3-5 mins Peak effect 5-10mins (redose 5-10mins) E1/2t = 5-8hrs Vd 7L/kg 50% PB"
3) Hepatic microsomal enzymes – conjugated to urine 50% - fecal 50%
Labetalol: Adverse Effects
"Severe bradycardia Hypotension Heart block Syncope/dizziness Headache Bronchospasm! Fluid retention! Hypoglycemia – prevents the inhibitory effects of NE on insulin secretion"
Labetalol
1) Contraindications
2) Dosage
1) "Hypersensitivity Asthma/COPD Severe CHF With CCB= complete heart block Severe hypotension or bradycardia SSS"
2) “5-10mg IV Q5-10mins up to 300mg total
0.1-0.5 mg/kg
PO 200-400mg BID”
Metoprolol
1) Class
2) Action
1) Selective Beta 1 adrenergic antagonist
2) Reversibly binds to beta1 adrenergic receptor antagonists to inhibit the binding of NE, EPI, and other beta agonist, preventing the stimulation of G-coupled protein receptors, adenylate cyclase, and cAMP.
“Slows SA rate, conduction through the AV node, decreases contractility = decreased cardiac O2 demand.”
Metoprolol
1) Indications
2) Onset & Half Life
3) Metabolism
1) "Blunt SNS response to DVL and invasive surgical stimuli. Pheochromocytoma, HTN, tachyarrthymias CAD, heart failure Angina, MI"
2) “Onset Rapid
E1/2 life = 3-7hrs
12% PB”
3) “Hepatic renal”
Metoprolol: Adverse Effects
"Severe bradycardia Cardiac failure- asystole SOB Heart block Peripheral edema Arterial insufficiency"
Metoprolol
1) Contraindications
2) Dosage
1) "Hypersensitivity SSS With CCB – complete heart block Asthma and COPD in HIGH doses HR dependent pts."
2) “1.25-5mg IV Q2-5mins to max of 15mg
1-15mg IV
50-400mg PO
Titrate to BP and HR”
Propanolol
1) Class
2) Action
1) Beta1, beta2 adrenergic antagonist
2) Reversibly binds to beta1, and beta2 adrenergic receptor antagonists to inhibit the binding of NE, EPI, and other beta agonist, preventing the stimulation of G-coupled protein receptors, adenylate cyclase, cAMP.
Slows SA rate, conduction through the AV node, decreases contractility. Causes peripheral, cerebral, and coronary vasodilation.
Propanolol
1) Indications
2) VD & Half life
3) Metabolism
1) "Blunt SNS response to DVL and invasive surgical stim. Pheochromoctyoma HTN, tachyarrythmias CAD,MI, angina THYROTOXICOSIS Migraines and tremors!"
2) “Vd 4L/kg
90%PB
E1/2t = 4hrs”
3) “1st pass effect & pulmonary uptake,
Hydroxypropanolol (decreased activity)»_space; urine.”
Propanolol: Adverse Effects
"Bronchospasm! Hypoglycemia! = prevents the inhibitory effects of NE on insulin secretion Severe bradycardia Severe hypotension Heart Block Rebound tachycardia with rapid withdrawal Syncope/dizziness "