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Desfesoterodine
Desfesoterodine (INN, also called 5-hydroxymethyltolterodine) is an antimuscarinic drug. It is the active metabolite An active metabolite is an active form of a drug after it has been processed by the body. Metabolites of drugs An active metabolite results when a drug is metabolized by the body into a modified form which continues to produce effects in the body ... of fesoterodine, its isobutyrate ester. References Muscarinic antagonists Primary alcohols Phenols Diisopropylamino compounds {{genito-urinary-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tolterodine
Tolterodine, sold under the brand name Detrol among others, is a medication used to treat frequent urination, urinary incontinence, or urinary urgency. Effects are seen within an hour. It is taken by mouth. Common side effects include headache, dry mouth, constipation, and dizziness. Serious side effects may include angioedema, urinary retention, and QT prolongation. Use in pregnancy and breastfeeding are of unclear safety. It works by blocking muscarinic receptors in the bladder thus decreasing bladder contractions. Tolterodine was approved for medical use in 1998. It is available as a generic medication. In 2020, it was the 271st most commonly prescribed medication in the United States, with more than 1million prescriptions. Medical uses Detrusor overactivity (DO, contraction of the muscular bladder wall) is the most common form of urinary incontinence (UI) in older adults. It is characterized by uninhibited bladder contractions causing an uncontrollable urge to void. Uri ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antimuscarinic
A muscarinic receptor antagonist (MRA) is a type of anticholinergic agent that blocks the activity of the muscarinic acetylcholine receptor. The muscarinic receptor is a protein involved in the transmission of signals through certain parts of the nervous system, and muscarinic receptor antagonists work to prevent this transmission from occurring. Notably, muscarinic antagonists reduce the activation of the parasympathetic nervous system. The normal function of the parasympathetic system is often summarised as "rest-and-digest", and includes slowing of the heart, an increased rate of digestion, Bronchoconstriction, narrowing of the airways, promotion of urination, and sexual arousal. Muscarinic antagonists counter this parasympathetic "rest-and-digest" response, and also work elsewhere in both the Central nervous system, central and peripheral nervous systems. Drugs with muscarinic antagonist activity are widely used in medicine, in the treatment of Bradycardia, low heart rate, ove ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Active Metabolite
An active metabolite is an active form of a drug after it has been processed by the body. Metabolites of drugs An active metabolite results when a drug is metabolized by the body into a modified form which continues to produce effects in the body. Usually these effects are similar to those of the parent drug but weaker, although they can still be significant (see e.g. 11-hydroxy-THC, morphine-6-glucuronide). Certain drugs such as codeine and tramadol have metabolites (morphine and ''O''-desmethyltramadol respectively) that are stronger than the parent drug and in these cases the metabolite may be responsible for much of the therapeutic action of the parent drug. Sometimes, however, metabolites may produce toxic effects and patients must be monitored carefully to ensure they do not build up in the body. This is an issue with some well-known drugs, such as pethidine (meperidine) and dextropropoxyphene. Prodrugs Sometimes drugs are formulated in an inactive form that is designe ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Fesoterodine
Fesoterodine (INN, used as the fumarate under the brand name Toviaz) is an antimuscarinic drug developed by Schwarz Pharma AG to treat overactive bladder syndrome (OAB). It was approved by the European Medicines Agency in April 2007, the US Food and Drug Administration on October 31, 2008 and Health Canada on February 9, 2012. Fesoterodine is a prodrug. It is broken down into its active metabolite, desfesoterodine, by plasma esterases. Efficacy Fesoterodine has the advantage of allowing more flexible dosage than other muscarinic antagonists A muscarinic receptor antagonist (MRA) is a type of anticholinergic agent that blocks the activity of the muscarinic acetylcholine receptor. The muscarinic receptor is a protein involved in the transmission of signals through certain parts of the .... Its tolerability and side effects are similar to other muscarinic antagonists and as a new drug seems unlikely to make great changes in practices of treatment for overactive bladder. A ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Isobutyric Acid
Isobutyric acid, also known as 2-methylpropanoic acid or isobutanoic acid, is a carboxylic acid with structural formula ( CH3)2CH COOH. It is an isomer of ''n''- butyric acid. It is classified as a short-chain fatty acid. Deprotonation or esterification gives derivatives called isobutyrates. Isobutyric acid is a colorless liquid with a somewhat unpleasant odor. It is soluble in water and organic solvents. It is found naturally in carobs (''Ceratonia siliqua''), in vanilla, and in the root of ''Arnica dulcis'', and as an ethyl ester in croton oil. Production Isobutyric acid is manufactured by the oxidation of isobutyraldehyde, which is a byproduct of the hydroformylation of propylene. It can also be prepared by the high pressure hydrocarboxylation ( Koch reaction) from propylene: :CH3CH=CH2 + CO + H2O → (CH3)2CHCO2H Isobutyric acid can also be manufactured commercially using engineered bacteria with a sugar feedstock. Laboratory methods Many routes are known includ ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Muscarinic Antagonists
A muscarinic receptor antagonist (MRA) is a type of anticholinergic agent that blocks the activity of the muscarinic acetylcholine receptor. The muscarinic receptor is a protein involved in the transmission of signals through certain parts of the nervous system, and muscarinic receptor antagonists work to prevent this transmission from occurring. Notably, muscarinic antagonists reduce the activation of the parasympathetic nervous system. The normal function of the parasympathetic system is often summarised as "rest-and-digest", and includes slowing of the heart, an increased rate of digestion, narrowing of the airways, promotion of urination, and sexual arousal. Muscarinic antagonists counter this parasympathetic "rest-and-digest" response, and also work elsewhere in both the central and peripheral nervous systems. Drugs with muscarinic antagonist activity are widely used in medicine, in the treatment of low heart rate, overactive bladder, respiratory problems such as asthma and ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Primary Alcohols
A primary alcohol is an alcohol in which the hydroxy group In chemistry, a hydroxy or hydroxyl group is a functional group with the chemical formula and composed of one oxygen atom covalently bonded to one hydrogen atom. In organic chemistry, alcohols and carboxylic acids contain one or more hydroxy ... is bonded to a primary carbon atom. It can also be defined as a molecule containing a “–CH2OH” group. In contrast, a secondary alcohol has a formula “–CHROH” and a tertiary alcohol has a formula “–CR2OH”, where “R” indicates a carbon-containing group. Examples of primary alcohols include ethanol and n-Butanol, 1-butanol. Methanol is also generally regarded as a primary alcohol, including the 1911 edition of the Encyclopædia Britannica,. See also * Alcohol (chemistry), Alcohol (especially Nomenclature section for discussion on Secondary and Tertiary alcohols.) * Oxidation of primary alcohols to carboxylic acids References Primary alcohols, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Phenols
In organic chemistry, phenols, sometimes called phenolics, are a class of chemical compounds consisting of one or more hydroxyl groups (— O H) bonded directly to an aromatic hydrocarbon group. The simplest is phenol, . Phenolic compounds are classified as simple phenols or polyphenols based on the number of phenol units in the molecule. Phenols are both synthesized industrially and produced by plants and microorganisms. Properties Acidity Phenols are more acidic than typical alcohols. The acidity of the hydroxyl group in phenols is commonly intermediate between that of aliphatic alcohols and carboxylic acids (their pKa is usually between 10 and 12). Deprotonation of a phenol forms a corresponding negative phenolate ion or phenoxide ion, and the corresponding salts are called phenolates or phenoxides (aryloxides according to the IUPAC Gold Book). Condensation with aldehydes and ketones Phenols are susceptible to Electrophilic aromatic substitutions. Condensation with formald ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
