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Metoprolol

Trade names Lopressor, Toprol-XL

Routes of administration oral and IV.

Selective β receptor blocker used in treatment of several diseases of the cardiovascular system, especially hypertension.

Utilized as either metoprolol succinate or metoprolol tartrate.

Used for: hypertension, angina, acute myocardial infarction, supraventricular tachycardia, ventricular tachycardia, CHF, and prevention of migraine headache, treatment of heart failure, vasovagal syncope, as an adjunctive treatment of hyperthyroidism, Long QT syndrome, especially for patients with asthma, as metoprolol’s β1 selectivity tends to interfere less with asthma drugs which are often β2-adrenergic receptor-agonist drugs.

Also prescribed for use in anxiety disorders.

Without intrinsic sympathomimetic activity.

A selective β1 receptor blocker used in treatment of several diseases of the cardiovascular system, especially hypertension.

Trade names are Lopressor, Toprol-XL

Can be given orally or intravenously.

Bioavailability of 12% with hepatic metabolism via CYP2D6, CYP3A4.

Half-life 3-7 hours

Excretion Renal

The active substance metoprolol is employed either as metoprolol succinate or metoprolol tartrate.

100 mg metoprolol tartrate corresponds to 95 mg metoprolol succinate.

The tartrate is an immediate-release and the succinate is an extended-release formulation.

Metoprolol is used for a number of conditions including: hypertension, angina, acute myocardial infarction, supraventricular tachycardia, ventricular tachycardia, congestive heart failure, and prevention of migraine headaches, adjunct treatment of hyperthyroidism, Long QT syndrome, for patients with asthma, as metoprolol’s β1 selectivity tends to interfere less with asthma drugs, which are often β2-adrenergic receptor-agonist drugs, and anxiety disorders.

Side effects include: dizziness, drowsiness, fatigue, diarrhea, unusual dreams, ataxia, trouble sleeping, depression, vision problems, reduction in blood flow to the hands and feet, causing them to feel numb and cold.

Lipophilic beta blockers such as metoprolol are more likely than other less lipophilic beta blockers to cause sleep disturbances such as insomnia and vivid dreams and nightmares.

Serious side-effects include: symptoms of bradycardia, dizziness, fainting and unusual fatigue, bluish discoloration of the fingers and toes, numbness/tingling/swelling of the hands or feet, sexual dysfunction, erectile dysfunction, hair loss, mental/mood changes, depression, trouble breathing, cough, dyslipidemia, and increased thirst.

Symptoms of an allergic reaction include: rash, itching, swelling, and severe dizziness.

Coadministration with alcohol may cause mild body rashes and is not recommended.

May worsen the symptoms of heart failure in some patients.

This medicine may cause changes in blood sugar levels or cover up signs of low blood sugar.

May cause impaired alertness.

Excessive doses can cause severe hypotension, bradycardia, metabolic acidosis, seizures and cardiorespiratory arrest.

Blood or plasma concentrations may be measured and are usually less than 200 μg/L during therapeutic administration, but can range from 1–20 mg/L in overdose situations.

A weak membrane stabilizing activity.

Has a short half-life and must be taken at least twice daily or as a slow-release preparation.

Decreases heart rate, contractility and cardiac output.

Decreases blood pressure.

Metabolized in the liver to inactive metabolite.

Moderately lipophilic.

Has weak membrane stabilizing activitty.

Has a short half-life, therefore must be taken at least twice daily or as a slow-release preparation.

Side effects include: ataxia, bradycardia, cough, diarrhea, depression, dizziness, drowsiness, fatigue, sexual dysfunction, erectile dysfunction, , mood disturbances, unusual dreams, shortness of breath, thirst, trouble sleeping, and vision problems.

Metoprolol may reduce blood flow to the hands and feet, causing them to feel numb and cold.

Due to the high penetration across the blood brain barrier, lipophilic beta blocker metoprolol is more likely than other less lipophilic beta blockers to cause sleep disturbances such as insomnia and vivid dreams and nightmares.

Serious side effects include bradycardia, dizziness, fainting, fatigue, bluish discoloration of the fingers and toes, numbness/tingling/swelling of the hands or feet, sexual dysfunction, erectile dysfunction, hair loss, mental/mood changes, depression, trouble breathing, cough, dyslipidemia, and increased thirst.

Rare symptoms include easy bruising or bleeding, sore throat, fever, yellowing skin or eyes, stomach pain, dark urine, and persistent nausea.

Allergic reaction include: rash, itching, swelling, and severe dizziness.

Administration with alcohol may cause mild body rashes and is not recommended.

May worsen the symptoms of heart failure in some patients.

May cause changes in blood sugar levels and diminish signs of low blood sugar, such as a rapid pulse rate.

May cause some people to become less alert.

Excessive doses can cause severe hypotension, bradycardia, metabolic acidosis, seizures and cardiorespiratory arrest.

Blood or plasma concentrations are usually less than 200 μg/L during therapeutic administration.

Metoprolol undergoes a-hydroxylation and O-demethylation by the cytochrome liver enzymes CYP2D6 [11] and a small percentage by CYP3A4.

Metabolized in the liver to an inactive agent.

Has bioavailability of 12%, with hepatic metabolism via CYP2D6, CYP3A4 enzymes.

Metabolized in the liver to inactive metabolite.

Half-life of 3-7 hours, with renal excretion.

A selective β1 receptor blocker used in treatment of several diseases of the cardiovascular system, especially hypertension.

100 mg metoprolol tartrate corresponds to 95 mg metoprolol succinate

The tartrate is an immediate-release and the succinate is an extended-release formulation.

Used as an adjunct therapy for hyperthyroidism.

Its β1 selectivity tends to interfere less with asthma drugs which are often β2-adrenergic receptor-agonist drugs.

Due to its selectivity in blocking the beta1 receptors in the heart, is also prescribed for use in anxiety, social anxiety disorder, and other anxiety disorders.

May be associated with cold hands and feet related to reduced blood flow.

A lipophilic beta blocker and has a high penetration rate across the blood brain barrier causing sleep insomnia and vivid dreams and nightmares.

May impair recognition of hypoglycemic symptoms.

May impair alertness.

Excessive doses associated with hypotension, bradycardia, metabolic acidosis, seizures and cardiorespiratory arrest.

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