Metoprolol
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Metoprolol
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Systematic (IUPAC) name | |
1-[4-(2-methoxyethyl)phenoxy] -3-propan-2-ylamino-propan-2-ol |
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Identifiers | |
CAS number | |
ATC code | C07 |
PubChem | |
DrugBank | |
Chemical data | |
Formula | C15H25NO3 |
Mol. mass | 267.364 g/mol |
Pharmacokinetic data | |
Bioavailability | 12% |
Metabolism | Hepatic |
Half life | 3-7 hours |
Excretion | Renal |
Therapeutic considerations | |
Pregnancy cat. | |
Legal status |
℞ Prescription only |
Routes | oral iv |
Metoprolol is a selective beta1 receptor blocker used in treatment of several diseases of the cardiovascular system. It is marketed under the brand name Lopressor® by Novartis, and Toprol-XL® (in the USA); Seleken® or Selokeen® (elsewhere); as Minax® by Alphapharm (in Australia), as Betaloc® by AstraZeneca and as Corvitol® by Berlin-Chemie AG.
It should be noted that Lopressor® refers to metoprolol tartrate, while Toprol-XL® refers to metoprolol succinate, the sustained release formulation.
Contents |
[edit] Pharmacology
- Cardioselective
- Lipophilic
- Without intrinsic sympathomimetic activity (ISA)
- Without membrane stabilizing activity
- Short half-life must be taken at least twice daily or as an SR preparation.
[edit] Indications
- Essential hypertension
- Arrhythmias
- Coronary heart disease (prevention of angina attacks)
- Secondary prevention after a myocardial infarction
- Low dose in treatment of some forms of heart failure.[1]
- Migraine prophylaxis
- Adjunct in treatment of hyperthyroidism
[edit] Side effects
Transient effects include dizziness, lightheadedness, drowsiness, tiredness, diarrhea, unusual dreams, ataxia, trouble sleeping, and vision problems. If negative symptoms become worse or are persistent, then they may be a sign of something more serious. This drug may reduce blood flow to the hands and feet, causing them to feel cold. Smoking may worsen this effect.
Serious but unlikely side effects that are not to be tolerated for any length of time include: symptoms of a very slow heartbeat (e.g.,persistent dizziness, fainting, unusual fatigue), bluish discoloration of the fingers and toes, numbness/tingling/swelling of the hands or feet, decreased sexual ability, reversible hair loss, mental/mood changes, trouble breathing, cough, unexplained or sudden weight gain, increased thirst, increased urination. Even more highly unlikely are: easy bruising or bleeding, persistent sore throat or fever, yellowing skin or eyes, stomach pain, dark urine, persistent nausea. Symptoms of an allergic reaction include: rash, itching, swelling, severe dizziness.
[edit] Footnotes
- ^ (June 12 1999) "Effect of metoprolol CR/XL in chronic heart failure: Metoprolol CR/XL Randomised Intervention Trial in Congestive Heart Failure (MERIT-HF)". Lancet 353 (9169): 2001-7. PMID 10376614.
[edit] External links
Beta blockers (C07) | |
---|---|
Non-selective β antagonists (C07AA) | Metipranolol, Nadolol, Oxprenolol, Penbutolol, Pindolol, Propranolol, Timolol, Sotalol |
β1 antagonists (cardioselective) (C07AB) | Atenolol, Acebutolol, Betaxolol, Bisoprolol, Esmolol, Metoprolol, Nebivolol |
Mixed α1/β antagonists (C07AG) | Carvedilol, Labetalol |