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Zoxazolamine
Zoxazolamine (INN, USAN, BAN) (brand name Contrazole, Deflexol, Flexin, Miazol, Uri-Boi, Zoxamine, Zoxine) is a muscle relaxant that is no longer marketed. It was synthesized in 1953 and introduced clinically in 1955 but was withdrawn due to hepatotoxicity. One of its active metabolite An active metabolite, or pharmacologically active metabolite is a biologically active metabolite of a xenobiotic substance, such as a drug or environmental chemical. Active metabolites may produce therapeutic effects, as well as harmful effects. ...s, chlorzoxazone, was found to show less toxicity, and was subsequently marketed in place of zoxazolamine. These drugs activate IKCa channels. References Amines Benzoxazoles Hepatotoxins Muscle relaxants Chloroarenes Withdrawn drugs {{musculoskeletal-drug-stub ...
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Oral Administration
Oral administration is a route of administration whereby a substance is taken through the Human mouth, mouth, swallowed, and then processed via the digestive system. This is a common route of administration for many medications. Oral administration can be easier and less painful than other routes of administration, such as Injection (medicine), injection. However, the onset of action is relatively low, and the effectiveness is reduced if it is not absorbed properly in the digestive system, or if it is broken down by digestive enzymes before it can reach the bloodstream. Some medications may cause gastrointestinal side effects, such as nausea or vomiting, when taken orally. Oral administration can also only be applied to conscious patients, and patients able to swallow. Terminology ''Per os'' (; ''P.O.'') is an adverbial phrase meaning literally from Latin "through the mouth" or "by mouth". The expression is used in medicine to describe a treatment that is taken orally (but not ...
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United States Adopted Name
A United States Adopted Name (USAN) is a unique nonproprietary name assigned to a medication marketed in the United States. Each name is assigned by the USAN Council, which is co-sponsored by the American Medical Association (AMA), the United States Pharmacopeial Convention (USP), and the American Pharmacists Association (APhA). The USAN Program states that its goal is to select simple, informative, and unique nonproprietary names (also called generic names) for drugs by establishing logical nomenclature classifications based on pharmacological or chemical relationships. In addition to drugs, the USAN Council names agents for gene therapy and cell therapy, contact lens polymers, surgical materials, diagnostics, carriers, and substances used as an excipient. The USAN Council works in conjunction with the World Health Organization (WHO) international nonproprietary name (INN) Expert Committee and national nomenclature groups to standardize drug nomenclature and establish rule ...
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British Approved Name
A British Approved Name (BAN) is the official, non-proprietary, or generic name given to a pharmaceutical substance, as defined in the British Pharmacopoeia (BP). The BAN is also the official name used in some countries around the world, because starting in 1953, proposed new names were evaluated by a panel of experts from WHO in conjunction with the BP commission to ensure naming consistency worldwide (an effort leading to the International Nonproprietary Name system). There is also a British Approved Name (Modified) (BANM). Combination preparations BANs are unique in that names are assigned for combination preparations as well as single-drug preparations. For example, the BAN co-amoxiclav is assigned to preparations containing amoxicillin and clavulanic acid. Most other pharmacopoeias simply refer to combination products by both ingredients in the preparation, in this example "amoxicillin with clavulanic acid". The prefix of "co-" is used for many combination drugs, inclu ...
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Muscle Relaxant
A muscle relaxant is a drug that affects skeletal muscle function and decreases the muscle tone. It may be used to alleviate symptoms such as muscle spasms, pain, and hyperreflexia. The term "muscle relaxant" is used to refer to two major therapeutic groups: Neuromuscular-blocking drugs, neuromuscular blockers and Antispasmodic, spasmolytics. Neuromuscular blockers act by interfering with transmission at the neuromuscular end plate and have no central nervous system (CNS) activity. They are often used during surgical procedures and in intensive care and emergency medicine to cause temporary paralysis. Spasmolytics, also known as "centrally acting" muscle relaxant, are used to alleviate musculoskeletal pain and spasms and to reduce spasticity in a variety of neurological conditions. While both neuromuscular blockers and spasmolytics are often grouped together as muscle relaxant,
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List Of Withdrawn Drugs
Medication, Drugs or medicines may be withdrawn from commercial markets because of risks to patients, but also because of commercial reasons (e.g. lack of demand and relatively high production costs) or because it turns out that they are less effective in clinical practice than premarketing efficacy trials suggested. When risks or harms are the cause, withdrawals will usually have been prompted by unexpected adverse effects that were not detected during the early, premaketing, clinical trials, i.e. they became apparent only from postmarketing surveillance data collected from the wider community during routine use over longer periods of time. This list is not limited to drugs that were ever approved by specific jurisdictions. Some of them (lumiracoxib, rimonabant, tolrestat, ximelagatran, and zimeldine, for example) received marketing approval in Europe but had not yet been approved for marketing in the USA when adverse effects became clear and they were withdrawn from the market. S ...
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Hepatotoxicity
Hepatotoxicity (from ''hepatic toxicity'') implies chemical-driven liver damage. Drug-induced liver injury (DILI) is a cause of acute and chronic liver disease caused specifically by medications and the most common reason for a drug to be withdrawn from the market after approval. The liver plays a central role in transforming and clearing chemicals and is susceptible to the toxicity from these agents. Certain medicinal agents, when taken in overdoses (e.g. acetaminophen, paracetamol) and sometimes even when introduced within therapeutic ranges (e.g. halothane), may injure the organ. Other chemical agents, such as those used in laboratories and industries, natural chemicals (e.g., alpha-amanitin), and herbal remedies (two prominent examples being kava, though the causal mechanism is unknown, and comfrey, through pyrrolizidine alkaloid content) can also induce hepatotoxicity. Chemicals that cause liver injury are called hepatotoxins. More than 900 drugs have been implicated ...
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Active Metabolite
An active metabolite, or pharmacologically active metabolite is a biologically active metabolite of a xenobiotic substance, such as a drug or environmental chemical. Active metabolites may produce therapeutic effects, as well as harmful effects. Metabolites of drugs An active metabolite results when a drug is metabolized by the body into a modified form which produces 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 ...
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Chlorzoxazone
Chlorzoxazone (INN) is a centrally acting muscle relaxant used to treat muscle spasm and the resulting pain or discomfort. It can also be administered for acute pain in general and for tension headache (muscle contraction headache). It acts on the spinal cord by depressing reflexes. It is sold under the brand names Lorzone, Paraflex and Muscol and in combination form as Parafon Forte, a combination of chlorzoxazone and acetaminophen (paracetamol). Possible side effects include dizziness, lightheadedness, malaise, nausea, vomiting. In rare cases, chlorzoxazone may cause severe liver dysfunction. On the other hand, chlorzoxazone may reduce the liver toxicity of acetaminophen by competitive inhibition. It is available as a generic medication. Like metaxalone, its mechanism of action is still in question. It is believed that metaxalone works by altering serotonin levels and acting as a mild MAO inhibitor. The mechanism of action of chlorzoxazone is thought to act on GABAA and GABA ...
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IK Channel
The ''I'' channel (KCa3.1), which has a conductance of 20–80 pS, is expressed mainly in peripheral tissues such as those of the haematopoietic system, colon, placenta, lung and pancreas. The KCa3.1 channel in red blood cells was the first Ca2+–sensitive K+ channel to be identified and it has been implicated in a wide range of cell functions, including vasodilation of the microvasculature, K+ flux across endothelial cells of brain capillaries and the phagocytic activity of neutrophils. KCa3.1 is of primary importance in the relationship between K+ channels and cell proliferation. In the latter case, a human ''hIKCa1'' gene encodes the channel found in T cells, which is responsible for the hyperpolarization that is required to keep Ca2+ flowing into the cell through the ''I''CRAC channels. In comparison with the large-conductance (BK) channels, KCa3.1 is much more sensitive to Ca2+ and can thus respond to the global level of Ca2+. This high affinity for Ca2+ depends upon four ...
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Amines
In chemistry, amines (, ) are organic compounds that contain carbon-nitrogen bonds. Amines are formed when one or more hydrogen atoms in ammonia are replaced by alkyl or aryl groups. The nitrogen atom in an amine possesses a lone pair of electrons. Amines can also exist as hetero cyclic compounds. Aniline is the simplest aromatic amine, consisting of a benzene ring bonded to an amino group. Amines are classified into three types: primary (1°), secondary (2°), and tertiary (3°) amines. Primary amines (1°) contain one alkyl or aryl substituent and have the general formula RNH2. Secondary amines (2°) have two alkyl or aryl groups attached to the nitrogen atom, with the general formula R2NH. Tertiary amines (3°) contain three substituent groups bonded to the nitrogen atom, and are represented by the formula R3N. The functional group present in primary amines is called the amino group. Classification of amines Amines can be classified according to the nature and number o ...
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Benzoxazoles
Benzoxazole is an aromatic organic compound with a molecular formula C7H5NO, a benzene-fused oxazole ring structure, and an odor similar to pyridine. Although benzoxazole itself is of little practical value, many derivatives of benzoxazoles are commercially important. Being a heterocyclic compound, benzoxazole finds use in research as a starting material for the synthesis of larger, usually bioactive structures. Its aromaticity makes it relatively stable, although as a heterocycle, it has reactive sites which allow for functionalization. Occurrence and applications It is found within the chemical structures of pharmaceutical drugs such as flunoxaprofen and tafamidis. Benzoxazole derivatives are also of interest for optical brighteners in laundry detergents.E. Smulders, E. Sung "Laundry Detergents, 2. Ingredients and Products" in ''Ullmann's Encyclopedia of Industrial Chemistry'', Wiley-VCH, Weinheim, 2012. Benzoxazoles belong to the group of well-known antifungal agents with an ...
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