In man, absorption of Metolar is rapid and complete. Plasma levels following oral administration of conventional Metolar tablets, however, approximate 50% of levels following intravenous administration, indicating about 50% first-pass metabolism. Metolar crosses the bloodbrain barrier and has been reported in the CSF in a concentration 78% of the simultaneous plasma concentration.
Plasma levels achieved are highly variable after oral administration. Only a small fraction of the drug (about 12%) is bound to human serum albumin. Metolar is a racemic mixture of R- and Senantiomers, and is primarily metabolized by CYP2D6. When administered orally, it exhibits stereoselective metabolism that is dependent on oxidation phenotype. Elimination is mainly by biotransformation in the liver, and the plasma half-life ranges from approximately 3 to 7 hours. Less than 5% of an oral dose of Metolar is recovered unchanged in the urine; the rest is excreted by the kidneys as metabolites that appear to have no beta-blocking activity.
Following intravenous administration of Metolar, the urinary recovery of unchanged drug is approximately 10%. The systemic availability and half-life of Metolar in patients with renal failure do not differ to a clinically significant degree from those in normal subjects. Consequently, no reduction in Metolar succinate dosage is usually needed in patients with chronic renal failure.
Metolar is metabolized predominantly by CYP2D6, an enzyme that is absent in about 8% of Caucasians (poor metabolizers) and about 2% of most other populations. CYP2D6 can be inhibited by a number of drugs. Poor metabolizers and extensive metabolizers who concomitantly use CYP2D6 inhibiting drugs will have increased (several-fold) Metolar blood levels, decreasing Metolar's cardioselectivity .
In comparison to conventional Metolar, the plasma Metolar levels following administration of TOPROL-XL are characterized by lower peaks, longer time to peak and significantly lower peak to trough variation. The peak plasma levels following once-daily administration of TOPROL-XL average one-fourth to one-half the peak plasma levels obtained following a corresponding dose of conventional Metolar, administered once daily or in divided doses. At steady state the average bioavailability of Metolar following administration of TOPROL-XL, across the dosage range of 50 to 400 mg once daily, was 77% relative to the corresponding single or divided doses of conventional Metolar. Nevertheless, over the 24-hour dosing interval, β1 -blockade is comparable and dose-related. The bioavailability of Metolar shows a dose-related, although not directly proportional, increase with dose and is not significantly affected by food following TOPROLXL administration.
Rated Metolar (Lopressor) for Atrial Fibrillation Report
Taken for afib. 25 once a day. Stopped from be able to orgasm right away. Felt tired. I cut it in half. Was a bit better. 4th cardiologist told me to stop taking it and see what happens. If I go into afib he said to take one. Am on Xarelto so if I go into afib I am protected. First day and I feel better. These doctors say the exact same thing to each person. Never treat you like a human being. Question everything they tell you to do. Go to multiple specialists. Many of these drugs they put you on you do not need to take. I have to take a stinkin blood thinner. But, I do not have to take this crap. First Doc put me on a big dose of Crestor. I asked if he knew my cholesterol numbers. He did not and said it did not matter. My numbers are good. Crap darn near crippled me. Stop taking it also. Remember quality of life not quantity.
You should not use Metolar if you have a serious heart problem (heart block, sick sinus syndrome, slow heart rate), severe circulation problems, severe heart failure, or a history of slow heart beats that caused fainting.
Q: Can Metolar cause excessive drooling?
A: Metolar is in a class of medications called beta blockers. Metolar is used in the treatment of high blood pressure. Metolar is also used to treat angina. Metolar extended release tablets are indicated also for the treatment of heart failure. Metolar works by slowing the heart rate and relaxing blood vessels, which helps to improve blood flow. Metolar may also be used for conditions that are not mentioned here. Some of the side effects of Metolar include slow heart rate, dizziness, fatigue, depression, low blood pressure, and diarrhea. There was no listing of drooling being reported as a side effect in the prescribing information for Metolar. Please consult with your health care provider in regards to the symptoms you are experiencing. Kristen Dore, PharmD
Q: Is it possible to get joint pain, ie, wrist, shoulder, knee and muscle pain from taking Metolar?
A: Metolar is in a drug class called beta blockers. Metolar is used alone or combined with other medications to lower high blood pressure. In addition, Metolar is used to prevent angina and to increase the chance that a person will live longer after a heart attack. Metolar works by slowing the heart rate and relaxing blood vessels, thereby allowing for smoother blood flow and decreased blood pressure. The most common side effects with Metolar are low blood pressure; slow heart rate; dizziness; fatigue; depression; itchy skin; rash; and diarrhea. Pain in the muscles, tendons, ligaments, nerves, and bones have been reported with Metolar. There have been very rare reports of arthritis in people who have taken Metolar; however, the relationship to Metolar is unknown. This is not a complete list of the side effects associated with Metolar. When your doctor prescribes a new medication, be sure to discuss all your prescription and over-the-counter drugs, including dietary supplements, vitamins, botanicals, minerals, and herbals, as well as the foods you eat. Always keep a current list of the drugs and supplements you take and review it with your healthcare providers and your pharmacist. If possible, use one pharmacy for all your prescription medications and over-the-counter products. This allows your pharmacist to keep a complete record of all your prescription drugs and to advise you about drug interactions and side effects. Tell your health-care provider about any negative side effects from prescription drugs. You can also report them to the U.S. Food and Drug Administration by visiting www.fda.gov/medwatch or by calling 1-800-FDA-1088. There are many factors that can cause joint pain and muscle pain. For more specific information, consult with your doctor or pharmacist for guidance based on your health status and current medications, particularly before taking any action. Derek Dore, PharmD
Q: I have begun taking 100 mg Metolar for high blood pressure. Will this medication make my triglycerides rise?
A: Metolar can slightly increase triglycerides and decrease high-density lipoprotein (HDL, or "good") cholesterol. Typically, this occurs in people who have a cluster of conditions (metabolic syndrome) that includes: high blood pressure, high blood sugar, excess weight around the abdomen, and high cholesterol. Newer beta blockers, such as carvedilol (Coreg) and nebivolol (Bystolic), are less likely to affect your cholesterol levels. If you have been stable and have good results with Metolar and your triglycerides have been in the normal range, then you can remain on this medication while under the supervision of you health care provider. They will monitor your triglycerides to see that are in the the proper range. Hope this has been of some help to you. For more information, you can go to //www.everydayhealth.com/heart-health/understanding-triglycerides.aspx. Gerald R. Levy, RPh
Dipyridamole is used for heart testing. Because Metolar affects your heart rate, you should stop taking it before you’re given dipyridamole to help ensure an accurate test result.
All possible dosages and forms may not be included here. Your dosage, form, and how often you take the drug will depend on:
- your age
- the condition being treated
- how severe your condition is
- other medical conditions you have
- how you react to the first dose
Concomitant administration of hydralazine may inhibit presystemic metabolism of Metolar leading to increased concentrations of Metolar.
Rated Metolar (Lopressor) for Generalized anxiety disorder (GAD) Report
Knocked my sex life out. Ed made heart beat fast and irregular made me have real bad nerves cold feet sleepless nights due to uncomfortable heart beating. Nothing good for me