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Metoprolol is a beta blocker, or an antagonist of the β-adrenergic receptors. It is specifically a selective antagonist of the β 1-adrenergic receptor and has no intrinsic sympathomimetic activity. [37] Metoprolol exerts its effects by blocking the action of certain neurotransmitters, specifically adrenaline and noradrenaline.
According to the Biopharmaceutics Classification System (BCS) drug substances are classified to four classes upon their solubility and permeability: [1] Class I – high permeability, high solubility. Example: metoprolol, paracetamol [2] Those compounds are well absorbed and their absorption rate is usually higher than excretion.
This is generally defined by the range between the minimum effective dose (MED) and the maximum tolerated dose (MTD). The MED is defined as the lowest dose level of a pharmaceutical product that provides a clinically significant response in average efficacy, which is also statistically significantly superior to the response provided by the ...
The maximum dose is used, rather than a lower dose, to reduce the number of test subjects (and, among other things, the cost of testing), to detect an effect that might occur only rarely. This type of analysis is also used in establishing chemical residue tolerances in foods. Maximum tolerated dose studies are also done in clinical trials.
A highly potent drug (e.g., fentanyl, clonazepam, risperidone, benperidol, bumetanide) evokes a given response at low concentrations, while a drug of lower potency (e.g. morphine, alprazolam, ziprasidone, haloperidol, furosemide) evokes the same response only at higher concentrations.
Drug Trade name Type Main indications Company Sales (USD millions/year) ∆ vs 2014 1 Adalimumab: Humira Biologic Rheumatoid arthritis: AbbVie Inc. 14,012 1,469 2 Ledipasvir/sofosbuvir: Harvoni Small molecule Hepatitis C: Gilead Sciences: 13,864 11,737 3 Etanercept: Enbrel Biologic Rheumatoid arthritis: Amgen. Pfizer. 8,697 4,009 4 Infliximab ...
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Beta blockers counter this inappropriately high sympathetic activity, eventually leading to an improved ejection fraction, despite an initial reduction in ejection fraction. [citation needed] Trials have shown beta blockers reduce the absolute risk of death by 4.5% over a 13-month period.