Metoprolol , marketed under the trade name Lopressor among others, is a drug of a selective type of receptor blocker? 1 . It is used to treat high blood pressure, chest pain due to poor blood flow to the heart, and a number of conditions involving an abnormally fast heartbeat. It is also used to prevent further heart problems after myocardial infarction and to prevent headaches in those with migraines.
Metoprolol is sold in a formulation which can be drunk or administered intravenously. The medicine is often taken twice a day. Extended release formulations are taken once per day. Metoprolol can be combined with hydrochlorothiazide (diuretics) in one tablet.
Common side effects include difficulty sleeping, feeling tired, feeling fainted, and abdominal discomfort. Large doses can cause serious toxicity. The risk of pregnancy has not been ruled out. Seems to be safe in breastfeeding. Greater care is required with use in those with liver or asthma issues. Stopping this drug should be done slowly to reduce the risk of further health problems.
Metoprolol was first made in 1969. This is the List of Essential Medicines of the World Health Organization, the most important drugs needed in basic health systems. It is available as a generic drug. By 2013, metoprolol is the 19th most widely prescribed drug in the United States.
Video Metoprolol
Medical use
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.
- Treatment of heart failure
- Vasovagal syncope
- Adjunct in the treatment of hyperthyroidism
- Long QT syndrome, especially for patients with asthma, because 1 selectivity of metoprolol tends to be less disturbing with asthma medication, which is often? 2-drug adrenergic receptor-agonist
- Relapse prevention into atrial fibrillation (release/controlled release)
Because of its selectivity in blocking the beta receptor 1 in the heart, metoprolol is also prescribed for off-label use in performance anxiety, social anxiety disorder, and other anxiety disorders.
Available form
Metoprolol is sold in a formulation which can be drunk or administered intravenously. The medicine is often taken twice a day. Extended release formulations are taken once per day. Metoprolol can be combined with hydrochlorothiazide (diuretics) in one tablet.
Maps Metoprolol
Adverse effects
Side effects, especially with higher doses, include dizziness, drowsiness, fatigue, diarrhea, unusual dreams, sleeping difficulties, depression, and vision problems. Metoprolol can also reduce blood flow to the hands or feet, causing them to feel numb and cold; smoking can aggravate this effect. Because of the high penetration in the blood-brain barrier, lipophilic beta inhibitors such as propranolol and metoprolol are more likely than other lipophilic lipid beta, which causes sleep disorders such as insomnia and dreams and nightmares.
Serious adverse events suggested for immediate reported symptoms include bradycardia (resting heart rate slower than 60 beats per minute), persistent dizziness, unconsciousness and unusual fatigue, bluish discoloration of the fingers and toes, numbness/tingling/swelling of hands or feet, sexual dysfunction, erectile dysfunction, hair loss, mental/mood changes, depression, trouble breathing, cough, dyslipidemia and increased thirst. Consuming alcohol while using metoprolol can cause mild and not recommended body rashes.
Precautions
Metoprolol may worsen the symptoms of heart failure in some patients, who may have chest pain or discomfort, dilated neck veins, extreme fatigue, irregular breathing, irregular heartbeat, shortness of breath, facial swelling, fingers, legs, or lower legs. , weight gain, or wheezing.
These drugs can cause changes in blood sugar levels or cover up signs of low blood sugar, such as rapid pulse. It can also cause some people to become less alert than usual, making it dangerous for them to drive or use the machine.
Greater care is required with use in those with liver or asthma issues. Stopping this drug should be done slowly to reduce the risk of further health problems.
Pregnancy and breastfeeding
The risk to the fetus has not been ruled out, as per the category of pregnancy C in the United States. Metoprolol is a category C in Australia, which means that it can be suspected to cause harmful effects on the human fetus (but no malformations). Seems to be safe in breastfeeding.
Overdose
Excessive doses of metoprolol may cause severe hypotension, bradycardia, metabolic acidosis, seizures, and cardiorespiratory arrest. Blood or plasma concentrations can be measured to confirm the diagnosis of overdose or poisoning in hospitalized patients or to assist in the investigation of medicolegal deaths. Plasma levels are usually less than 200 μg/l during therapeutic administration, but can range from 1-20Ã, mg/l in overdose victims.
Pharmacology
General pharmacological principles of metoprolol:
- beta-1 selectively
- is quite lipophilic
- without intrinsic sympathomimetic activity
- with weak membrane stabilization activity
- lowers heart rate, contractility, and cardiac output, thereby lowering blood pressure
Action mechanism
Metoprolol blocking? 1 adrenergic receptor in cardiac muscle cells, thus decreasing the slope of phase 4 in nodal action potential (reducing Na uptake) and extending phase 3 repolarization (slowing K release). It also suppresses an increase in induction caused by norepinephrine in Ca leopoplasma (SR) Ca 2 leak and spontaneous release of SR Ca 2 , which is a major trigger for atrial fibrillation..
Pharmacokinetics
Metoprolol has a short half-life of 3 to 7 hours, so drink at least twice a day or as a slow release preparation.
This experience? -hydroxylation and O-demethylation as the substrate of cytochrome CYP2D6 liver enzyme and a small percentage by CYP3A4, resulting in inactive metabolites.
Chemistry
Metoprolol has a very low melting point; about 120 Ã, Â ° C (248Ã, Â ° F) for tartrate, and about 136Ã, Â ° C (277Ã, Â ° F) for succinate. Because of this, metoprolol is always produced in salt-based solutions, because drugs with low melting points are difficult to work with in the manufacturing environment. The free base exists as a white solid of wax, and the tartrate salt is a finer crystal material.
Metoprolol active substance is used either as metoprolol succinate or as tartrate metoprolol (where 100mg metoprolol tartrate corresponds to 95 mg of metoprolol succinate). Tartrate is a formulation of direct release and succinate is an extended release formulation.
Stereochemistry
Metoprolol contains stereocenter and consists of two enansiomers. This is a rashem, a mixture of 1: 1 ( R ) - and ( S ) - a form:
History
Metoprolol was first made in 1969.
Society and culture
Metoprolol is on the World Health Organization's Essential Drug List, the most important drug needed in a basic health system. It is available as a generic drug. By 2013, metoprolol is the 19th most widely prescribed drug in the United States.
Legal status
In the UK metoprolol is classified as a prescription drug-only in the beta-blocker class and is regulated by the Regulatory Agency for Medicines and Health Products (MHRA). MHRA is a government body established in 2003 and is responsible for regulating drugs, medical equipment, and equipment used in health care. MHRA recognizes that no product is completely risk-free but takes into account research and evidence to ensure that the associated risks are minimal.
The use of beta blockers such as metoprolol was approved in the US by the FDA (Food and Drug Administration) in 1967. The FDA has approved beta blockers for the treatment of cardiac arrhythmias, hypertension, migraines, and others. The prescription may choose to prescribe beta blockers for other treatments if there is only cause although not approved by the FDA. Drug manufacturers, however, can not advertise beta blockers for other purposes that have not been approved by the FDA. Because the FDA does not regulate the practice of medicine after the drug is approved, it is legal to prescribe beta blockers for other treatments such as performance anxiety.
Legislation
MHRA provides Limited Marketing Authorization Intas Pharmaceuticals (licensed) for metoprolol tartrate (tablets 50mg and 100mg) for prescription only on 23 September 2011; this is once established that there are no new or unexpected safety issues and that the benefits of tartrate metoprolol outweigh the risks. Metoprolol tartrate is a generic version of Lopressor, which was licensed and authorized on June 6, 1997 for Novartis Pharmaceuticals.
In sports
Metoprolol is a beta blocker and is banned by the world's anti-doping bodies in some sports. Beta blockers can be used to reduce heart rate and minimize vibration, which can improve performance in sports such as archery. All beta blockers are banned during and out of competition for archery and shooting. In some sports like all forms of billiards, archery, and golf, beta blockers are banned during competition only. Furthermore, any form of beta blocker is prohibited in the riflery competition by the National Collegiate Athletic Association.
To detect whether beta blockers have been used the analysis of human urine traces was analyzed. Uncharged drugs and/or beta blocker metabolites can be analyzed by gas-chromatographic mass spectrometry in the monitoring of selected ions (GC-MS-SIM). However, in modern times it is increasingly difficult to detect the presence of beta blockers used for sports doping purposes. The disadvantage of using GC-MS-SIM is that prior knowledge of the molecular structure of target drug/metabolite is required. Modern times have shown a difference in the structure and hence the new beta blocker can not be detected.
Claim
In 2012, a $ 11 million settlement was achieved with Toprol XL (release version of time-release from metoprolol) and generic equivalent metoprolol. The lawsuit involved the pharmaceutical company AstraZeneca AB, LP AstraZeneca, LP AstraZeneca Pharmaceuticals, and Aktiebolaget Hassle. Claim claims suggest that manufacturers violate antitrust and consumer protection laws. Claiming that to increase earnings, low-cost generic versions of Toprol XL are deliberately kept out of the market. This claim was later rejected by the defendants.
References
External links
- US. National Library of Medicine: Drug Information Portal - Metoprolol
Source of the article : Wikipedia
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