Metoprolol

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Brand names: Lopressor®, Toprol XL®

Chemical formula:

Drug Forms:
• Metoprolol Tartrate Oral tablet (below)
• Metoprolol Tartrate Solution for injection
• Metoprolol tablets or extended-release tablets
• Metoprolol injection
• Metoprolol Succinate Oral tablet, extended-release

Español:
• Metoprolol Tartrato, Tableta oral
• Tartrato de metoprolol, Solución para inyección
• Tabletas normales o de liberación prolongada de metoprolol
• Inyección de metoprolol
• Succinato de Metoprolol, Tableta oral de liberación prolongada

Metoprolol Tartrate Oral tablet

What is this medicine?

METOPROLOL is a beta-blocker. Beta-blockers reduce the workload on the heart and help it to beat more regularly. This medicine is used to treat high blood pressure and to prevent chest pain. It is also used to after a heart attack and to prevent an additional heart attack from occurring.

This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
• diabetes
• heart or vessel disease like slow heart rate, worsening heart failure, heart block, sick sinus syndrome or Raynaud's disease
• kidney disease
• liver disease
• lung or breathing disease, like asthma or emphysema
• pheochromocytoma
• thyroid disease
• an unusual or allergic reaction to metoprolol, other beta-blockers, medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding

How should I use this medicine?

Take this medicine by mouth with a drink of water. Follow the directions on the prescription label. Take this medicine immediately after meals. Take your doses at regular intervals. Do not take more medicine than directed. Do not stop taking this medicine suddenly. This could lead to serious heart-related effects.

Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.

Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.

What may interact with this medicine?

Do not take this medicine with any of the following medications:
• sotalol

This medicine may also interact with the following medications:
• clonidine
• digoxin
• dobutamine
• epinephrine
• isoproterenol
• medicine to control heart rhythm like quinidine, propafenone
• medicine for depression like monoamine oxidase (MAO) inhibitors, fluoxetine, and paroxetine
• medicine for high blood pressure like calcium channel blockers
• reserpine

This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.

What should I watch for while using this medicine?

Visit your doctor or health care professional for regular check ups. Contact your doctor right away if your symptoms worsen. Check your blood pressure and pulse rate regularly. Ask your health care professional what your blood pressure and pulse rate should be, and when you should contact them.

You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. Do not sit or stand up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells. Contact your doctor if these symptoms continue. Alcohol may interfere with the effect of this medicine. Avoid alcoholic drinks.

What side effects may I notice from receiving this medicine?

Side effects that you should report to your doctor or health care professional as soon as possible:
• allergic reactions like skin rash, itching or hives
• cold or numb hands or feet
• depression
• difficulty breathing
• faint
• fever with sore throat
• irregular heartbeat, chest pain
• rapid weight gain
• swollen legs or ankles

Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
• anxiety or nervousness
• change in sex drive or performance
• dry skin
• headache
• nightmares or trouble sleeping
• short term memory loss
• stomach upset or diarrhea
• unusually tired

This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Where should I keep my medicine?

Keep out of the reach of children.

Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Throw away any unused medicine after the expiration date.

Last updated: 7/1/2002

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

A cardioselective beta-blocker having a greater effect on β₁-adrenergic receptors of the heart than on β₂-adrenergic receptors of the bronchi and blood vessels. Used as the tartrate.

The noun has one meaning:

Meaning #1: beta blocker (trade name Lopressor) used in treating hypertension and angina and arrhythmia and acute myocardial infarction; has adverse side effects (depression and exacerbation of congestive heart failure etc.)
  Synonym: Lopressor

Metoprolol
Systematic (IUPAC) name
(RS)-1-(isopropylamino)-3-[4-(2-methoxyethyl)phenoxy]propan-2-ol
Identifiers
CAS number	37350-58-6
ATC code	C07AB02
PubChem	4171
DrugBank	APRD00208
ChemSpider	4027
Chemical data
Formula	C15H25NO3
Mol. mass	267.364 g/mol
SMILES	eMolecules & PubChem
Pharmacokinetic data
Bioavailability	12%
Metabolism	Hepatic
Half life	3-7 hours
Excretion	Renal
Therapeutic considerations
Licence data	US FDA:link
Pregnancy cat.	C(AU) C(US)
Legal status	℞ Prescription only
Routes	oral iv

"Minax" redirects here. For Ultima game character, see Minax (Ultima).

Metoprolol is a selective β₁ receptor blocker used in treatment of several diseases of the cardiovascular system, especially hypertension. It is marketed under the brand name Lopressor by Novartis, and Toprol-XL (in the USA); Selokeen (in the Netherlands); as Minax by Alphapharm (in Australia), Metrol by Arrow Pharmaceuticals (in Australia), as Betaloc by AstraZeneca, as Neobloc by Unipharm (in Israel) and as Corvitol by Berlin-Chemie AG. A number of generic products are available as well. The active substance metoprolol is employed either as metoprolol succinate or metoprolol tartrate (whereas 100 mg metoprolol tartrate corresponds to 95 mg metoprolol succinate), respectively as prolonged-release or conventional-release formulation.

Contents 1 Physical properties 2 Pharmacology 3 Indications 4 Precautions 5 Side effects 6 References 7 External links

Physical properties

Metoprolol has a very low melting point, around 45 degrees Celsius (as determined by Differential scanning calorimetry). Because of this metoprolol is always manufactured in a salt-based solution, as drugs with melting points below 100 degrees Celsius are difficult to work with in a manufacturing environment. The free base exists as a waxy white solid, where the tartrate salt is finer crystalline material.

Pharmacology

• Selective
• Moderately Lipophilic
• Without intrinsic sympathomimetic activity (ISA)
• With weak membrane stabilizing activity
• Short half-life, therefore must be taken at least twice daily or as a Slow-release preparation.
• Decreases Heart Rate, Contractility and Cardiac Output, therefore decreasing blood pressure

Indications

• Essential hypertension
• Tachycardia
• Coronary heart disease (prevention of angina attacks)
• Secondary prevention after a myocardial infarction
• Treatment of heart failure.^[1]
• Migraine prophylaxis
• Vasovagal syncope^[2]
• Adjunct in 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.

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

Toprol XL 50mg

Precautions

Metoprolol may worsen the symptoms of heart failure in some patients. Check with your doctor right away if you are having chest pain or discomfort; dilated neck veins; extreme fatigue; irregular breathing; an irregular heartbeat; shortness of breath; swelling of the face, fingers, feet, or lower legs; weight gain; or wheezing.^[3]

This medicine may cause changes in your blood sugar levels. Also, this medicine may cover up signs of low blood sugar, such as a rapid pulse rate. Check with your doctor if you have these problems or if you notice a change in the results of your blood or urine sugar tests.^[3]

This medicine may cause some people to become less alert than they are normally. If this side effect occurs, do not drive, use machines, or do anything else that could be dangerous if you are not alert while taking metoprolol .^[3]

Side effects

Transient effects include dizziness, lightheadedness, drowsiness, tiredness, diarrhea, unusual dreams, ataxia, trouble sleeping, depression, and vision problems. It may also reduce blood flow to the hands and feet, causing them to feel numb and cold; smoking may worsen this effect.^[4]

Serious side effects that are not to be tolerated for any length of time include symptoms of a very slow heartbeat (less than 50 bpm) (e.g. persistent dizziness, fainting, unusual fatigue), bluish discoloration of the fingers and toes, numbness/tingling/swelling of the hands or feet, sexual dysfunction, erectile dysfunction (impotence), hair loss, mental/mood changes, trouble breathing, cough, dyslipidemia, and increased thirst. Other highly unlikely symptoms include easy bruising or bleeding, persistent sore throat or fever, yellowing skin or eyes, stomach pain, dark urine, and persistent nausea. Symptoms of an allergic reaction include: rash, itching, swelling, severe dizziness. Taking it with alcohol might cause mild body rashes and therefore is not recommended.^[4]

References

1. ^ "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. June 12 1999. doi:10.1016/S0140-6736(99)04440-2. PMID 10376614. 
2. ^ Zhang Q, Jin H, Wang L, Chen J, Tang C, Du J (April 2008). "Randomized comparison of metoprolol versus conventional treatment in preventing recurrence of vasovagal syncope in children and adolescents". Medical science monitor : international medical journal of experimental and clinical research 14 (4): CR199–203. PMID 18376348. http://www.medscimonit.com/fulltxt.php?ICID=850297. 
3. ^ ^{a b c} MayoClinic.com Drug Information Metoprolol Precautions
4. ^ ^{a b} Canadian Online Pharmacy website: Metoprolol

External links

• AstraZeneca's page for Toprol-XL
• Novartis's page for Lopresor (PDF)

v • d • e Adrenergic antagonists α α1 selective Doxazosin • Prazosin • Alfuzosin • Terazosin • Indoramin • Urapidil • Trimazosin • Moxisylyte • Nantenine • 1A (Tamsulosin • Silodosin) α2 selective Atipamezole • Efaroxan • Idazoxan • Mianserin • Mirtazapine • NAN-190 • Rauwolscine • SB-269,970 • Yohimbine Non-selective α reversible (Phentolamine) • irreversible (Phenoxybenzamine) Ungrouped Tolazoline β β1 selective (cardioselective) Atenolol #  • Celiprolol • Betaxolol • Bisoprolol • Esmolol • Metoprolol • Nebivolol • intrinsic sympatheticomimetic activity (Acebutolol) β2 selective Butaxamine • ICI 118551 β3 selective SR 59230A Non-selective β Alprenolol • Amosulalol • Bupranolol • Metipranolol • Nadolol • Oxprenolol • Penbutolol • Propranolol • Tertatolol • Timolol • Tilisolol • Sotalol • intrinsic sympatheticomimetic activity (Pindolol) Mixed α1/β Carvedilol • Labetalol • Arotinolol Indirect tyrosine hydroxylase inhibitor (Metirosine) • vesicle storage inhibitor (Reserpine) • neurotransmitter release blocker (Guanethidine, Bretylium) #WHO-EM. †Undergoing clinical trials, not FDA approved. ‡Withdrawn from market. §Development halted.

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