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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 It was synthesized in 1953 and introduced clinically in 1955 but was withdrawn due to hepatotoxicity.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 metabolites, 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 th ..., 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 References Amines Benzoxazoles Hepatotoxins Muscle relaxants Organochlorides Withdrawn drugs {{musculoskeletal-drug-stub ...
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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, and liver dysfunction. Used with acetaminophen it has added risk of hepatotoxicity,. 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 chlorzoaxazone is thought to act on Gaba-A & B receptors and voltage-gated calcium channels to a degree. General central nervous system depression is the only currently accepted ...
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Oral Administration
Oral administration is a route of administration where a substance is taken through the mouth. Per os abbreviated to P.O. is sometimes used as a direction for medication to be taken orally. Many medications are taken orally because they are intended to have a systemic effect, reaching different parts of the body via the bloodstream, for example. Oral administration can be easier and less painful than other routes, such as 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 willing and able to swallow. Terminology ''Per os'' (; ''P.O.'') is an adverbial phrase meaning literally from Latin "through the mouth" or "by mouth ...
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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, List of soft contact lens materials, 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 ...
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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, including ...
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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 blockers and 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
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). Where risks or harms is the reason for withdrawal, this will usually have been prompted by unexpected adverse effects that were not detected during Phase III clinical trials, i.e. they were only made apparent from postmarketing surveillance data collected from the wider community over longer periods of time. This list is not limited to drugs that were ever approved by the FDA. Some of them (lumiracoxib, rimonabant, tolrestat, ximelagatran and ximelidine, for example) were approved to be marketed in Europe but had not yet been approved for marketing in the US, when side effects became clear and their developers pulled them from the market. Some drugs in this list (e.g. LSD) were never approved for marketing in the US or Europe. Significant withdrawals Withdrawn clinical trial drugs *RG7795, ...
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Hepatotoxicity
Hepatotoxicity (from ''hepatic toxicity'') implies chemical-driven liver damage. Drug-induced liver injury 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. 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., microcystins), and herbal remedies (two prominent examples being kava, mechanism unknown, and comfrey, through its pyrrolizidine alkaloid content) can also induce hepatotoxicity. Chemicals that cause liver injury are called hepatotoxins. More than 900 drugs have been implicated in causing liver injury (see LiverTox, exter ...
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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 ...
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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 compounds and functional groups that contain a basic nitrogen atom with a lone pair. Amines are formally derivatives of ammonia (), wherein one or more hydrogen atoms have been replaced by a substituent such as an alkyl or aryl group (these may respectively be called alkylamines and arylamines; amines in which both types of substituent are attached to one nitrogen atom may be called alkylarylamines). Important amines include amino acids, biogenic amines, trimethylamine, and aniline; Inorganic derivatives of ammonia are also called amines, such as monochloramine (). The substituent is called an amino group. Compounds with a nitrogen atom attached to a carbonyl group, thus having the structure , are called amides and have different chemical properties from amines. Classification of amines Amines can be classified according to the nature and number of substituents on nitrogen. Aliphatic amines contain only H and alkyl substituents. Aromatic ...
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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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