metoprolol (Lopressor Toprol XL, Kapspargo)
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Introduction
Tradename: Lopressor, Toprol XL. A selective beta-1 antagonist.
Indications
- hypertension
- chronic stable angina
- unstable angina[8]
- secondary prevention in patients with cardiovascular disease
- reduces risk of cardiovascular mortality in hemodynamically stable patients with acute myocardial infarction
- supraventricular tachycardia
- paroxysmal supraventricular tachycardia
- multifocal atrial tachycardia
- control of ventricular rate in atrial fibrillation or atrial flutter
- long QT syndrome[8]
- mitral valve prolapse[8]
- pheochromocytoma[8]
- thyrotoxicosis
- reduces mortality in high-risk patients indgoing non-cardiac surgery
- heart failure (Toprol XL is FDA approved)
- migraine prophylaxis[8]
Contraindications
Dosage
- acute MI: 5 mg increments IV every 2 hours up to 15 mg
- hypertension: start 50 mg PO BID, max 450 mg/day
Tabs: 50 100 mg.
metoprolol succinate, Toprol XL*, Kapspargo (extended release):
- start 50-100 mg PO QD, max 400 mg/day
- heart failure:[5]
Tabs: 25 mg (scored), 50, 100, 200 mg.
* ok to crush, except XL.
* generic extended-release metoprolol succinate may have different pharmacokinetics than Toprol-XL[9]
* Kapspargo available in sprinkle
Pharmacokinetics
- 1st pass hepatic metabolism with oral administration
- 11% of the drug is bound to plasma proteins
- 78% crosses blood-brain barrier
- excreted in the urine
- elimination 1/2life is 3-4 hours
- dialyzable[12]
- no good correlation between serum levels & therapeutic effect
elimination via liver
1/2life = 3.0-3.4 hours
protein binding = 13 %
elimination by hemodialysis = +
Adverse effects
- common (> 10%)
- less common (1-10%)
- bradycardia, wheezing, irregular heartbeat, diminished peripheral circulation, heartburn
- uncommon (< 1%)
- other
- drug adverse effects of beta-adrenergic receptor antagonists
- drug adverse effects of beta-1 adrenergic receptor antagonists
- drug adverse effects of renin-angiotensin-aldosterone system inhibitors (RAAS inhibitors)
- drug adverse effects of antihypertensive agents
Drug interactions
- blocks bronchodilator effects of beta adrenergic agonists
- barbiturates may enhance metoprolol metabolism
- phenothiazines & cimetidine may increase plasma concentrations
- any pharmaceutical agent that inhibits cyt P450 2D6 may increase levels of metoprolol
- drug interaction(s) of antiarrhythmic agents in combination with diuretics
- drug interaction(s) of beta-2 adrenergic receptor agonists with beta adrenergic receptor antagonists
- drug interaction(s) of renin-angiotensin-aldosterone inhibitors with trimethoprim-sulfamethoxazole
- drug interaction(s) of beta-adrenergic receptor antagonists with thyroid hormone
- drug interaction(s) of beta-adrenergic receptor antagonists with sulfinpyrazone
- drug interaction(s) of beta-adrenergic receptor antagonists with salicylate
- drug interaction(s) of beta-adrenergic receptor antagonists with rifampin
- drug interaction(s) of beta-adrenergic receptor antagonists with ampicillin
- drug interaction(s) of beta-adrenergic receptor antagonists with colestipol
- drug interaction(s) of beta-adrenergic receptor antagonists with cholestyramine
- drug interaction(s) of beta-adrenergic receptor antagonists with barbiturates
- drug interaction(s) of beta-adrenergic receptor antagonists with calcium salts
- drug interaction(s) of beta-adrenergic receptor antagonists with aluminum carbonate
- drug interaction(s) of beta-adrenergic receptor antagonists with aluminum hydroxide
- drug interaction(s) of beta-adrenergic receptor antagonists with prazosin
- drug interaction(s) of beta-adrenergic receptor antagonists with lidocaine
- drug interaction(s) of beta-adrenergic receptor antagonists with ergot alkaloids
- drug interaction(s) of beta-adrenergic receptor antagonists with clonidine
- drug interaction(s) of beta-adrenergic receptor antagonists with benzodiazepines
- drug interaction(s) of beta-adrenergic receptor antagonists (except atenolol) with benzodiazepines
- drug interaction(s) of beta-adrenergic receptor antagonists with quinolones
- drug interaction(s) of beta-adrenergic receptor antagonists with quinidine
- drug interaction(s) of beta-adrenergic receptor antagonists with propafenone
- drug interaction(s) of beta-adrenergic receptor antagonists with phenothiazines
- drug interaction(s) of beta-adrenergic receptor antagonists with MAO inhibitors
- drug interaction(s) of beta-adrenergic receptor antagonists with loop diuretics
- drug interaction(s) of beta-adrenergic receptor antagonists with hydralazine
- drug interaction(s) of beta-adrenergic receptor antagonists with histamine H2 receptor antagonists
- drug interaction(s) of beta-adrenergic receptor antagonists with haloperidol
- drug interaction(s) of beta-adrenergic receptor antagonists with flecainide
- drug interaction(s) of beta-adrenergic receptor antagonists with oral contraceptives
- drug interaction(s) of beta-adrenergic receptor antagonists with calcium channel blockers
- drug interaction(s) of beta-adrenergic receptor antagonists with sulfonylureas
- drug interaction(s) of beta blockers with ACE inhibitors
- drug interaction(s) of spironolactone with beta blockers
- drug interaction(s) of NSAIDs with beta blockers
- drug interaction(s) of NSAIDs & antihypertensives
Laboratory
- specimen:
- methods:
Mechanism of action
- selective beta-1 adrenergic receptor antagonist
- at higher doses, beta-2 adenergic receptor antagonism occurs
More general terms
Additional terms
- African American Study of Kidney Disease & Hypertension (AASK)
- cytochrome P450 2D6 (cytochrome P450 2D, cytochrome P450 DB1, debrisoquine-4-hydroxylase, CYP2D6)
Component of
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ Clinical Guide to Laboratory Tests, NW Tietz (ed) 3rd ed, WB Saunders, Philadelpha 1995
- ↑ 5.0 5.1 Prescriber's Letter 8(4):20 2001
- ↑ Prescriber's Letter 13(3): 2006 Cytochrome P450 drug interactions Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=220233&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Alessi C In: Intensive Course in Geriatric Medicine & Board Review, Marina Del Ray, CA, Sept 29-Oct 2, 2004
- ↑ 8.0 8.1 8.2 8.3 8.4 8.5 Deprecated Reference
- ↑ 9.0 9.1 Orciari Herman A FDA Planning Study of Generic Metoprolol Over Safety, Efficacy Concerns. NEJM Journal Watch. May 9, 2014 Massachusetts Medical Society (subscription needed) http://www.jwatch.org
- ↑ 10.0 10.1 10.2 Geriatric Review Syllabus, 8th edition (GRS8) Durso SC and Sullivan GN (eds) American Geriatrics Society, 2013
- ↑ 11.0 11.1 11.2 Habbab KM, Moles DR, Porter SR. Potential oral manifestations of cardiovascular drugs. Oral Dis. 2010 Nov;16(8):769-73. PMID: https://www.ncbi.nlm.nih.gov/pubmed/20604876
- ↑ 12.0 12.1 Zhou H et al beta-blocker use and risk of mortality in heart failure patients initiating maintenance dialysis. Am J Kidney Dis 2021 May; 77:704 PMID: https://www.ncbi.nlm.nih.gov/pubmed/33010357 https://www.ajkd.org/article/S0272-6386(20)31001-5/fulltext
Database
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=441308
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=4171
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=62937
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=157620
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=41860
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=3043945