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Chlorzoxazone

Index Chlorzoxazone

Chlorzoxazone (INN) is a centrally acting muscle relaxant used to treat muscle spasm and the resulting pain or discomfort. It acts on the spinal cord by depressing reflexes. It is sold under the trade 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 hepatoxicity, which is why the combination is not recommended. It can also be administered for acute pain in general and for tension headache (muscle contraction headache). Like metaxalone, no specific mechanism of action has been identified for chlorzoxazone, with general central nervous system depression being the only currently accepted aspect to its medical benefits. Search for the exact mechanism of action is ongoing but limited due to the existence of more-effective safe muscle relaxers (ex. diazepam, cyclobenzaprine, tizanidine) greatly limiting the potential benefit of identifying novel compounds which share chlozoxazone's mechanism of action. As of 2015 the cost for a typical course of medication in the United States is less than 25 USD. [1]

17 relations: Central nervous system, Cyclobenzaprine, Depressant, Diazepam, Dizziness, Hepatotoxicity, International nonproprietary name, Lightheadedness, Malaise, Metaxalone, Muscle relaxant, Nausea, Paracetamol, Spasm, Tizanidine, Vomiting, Zoxazolamine.

Central nervous system

The central nervous system (CNS) is the part of the nervous system consisting of the brain and spinal cord.

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Cyclobenzaprine

Cyclobenzaprine, sold under the brand name Flexeril among others, is a muscle relaxer medication used to relieve skeletal muscle spasms and associated pain in acute musculoskeletal conditions.

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Depressant

A depressant, or central depressant, is a drug that lowers neurotransmission levels, which is to depress or reduce arousal or stimulation, in various areas of the brain.

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Diazepam

Diazepam, first marketed as Valium, is a medicine of the benzodiazepine family that typically produces a calming effect.

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Dizziness

Dizziness is an impairment in spatial perception and stability.

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Hepatotoxicity

Hepatotoxicity (from hepatic toxicity) implies chemical-driven liver damage.

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International nonproprietary name

The International Nonproprietary Name (INN) is an official generic and non-proprietary name given to a pharmaceutical drug or an active ingredient.

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Lightheadedness

Lightheadedness is a common and typically unpleasant sensation of dizziness and/or a feeling that one may faint.

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Malaise

Malaise is a feeling of general discomfort, uneasiness or pain, often the first indication of an infection or other disease.

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Metaxalone

Metaxalone (marketed by King Pharmaceuticals under the brand name Skelaxin) is a muscle relaxant used to relax muscles and relieve pain caused by strains, sprains, and other musculoskeletal conditions.

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Muscle relaxant

A muscle relaxant is a drug that affects skeletal muscle function and decreases the muscle tone.

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Nausea

Nausea or queasiness is an unpleasant sense of unease, discomfort, and revulsion towards food.

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Paracetamol

--> Acetanilide was the first aniline derivative serendipitously found to possess analgesic as well as antipyretic properties, and was quickly introduced into medical practice under the name of Antifebrin by A. Cahn and P. Hepp in 1886. But its unacceptable toxic effects, the most alarming being cyanosis due to methemoglobinemia, prompted the search for less toxic aniline derivatives. Harmon Northrop Morse had already synthesised paracetamol at Johns Hopkins University via the reduction of ''p''-nitrophenol with tin in glacial acetic acid in 1877, but it was not until 1887 that clinical pharmacologist Joseph von Mering tried paracetamol on humans. In 1893, von Mering published a paper reporting on the clinical results of paracetamol with phenacetin, another aniline derivative. Von Mering claimed that, unlike phenacetin, paracetamol had a slight tendency to produce methemoglobinemia. Paracetamol was then quickly discarded in favor of phenacetin. The sales of phenacetin established Bayer as a leading pharmaceutical company. Overshadowed in part by aspirin, introduced into medicine by Heinrich Dreser in 1899, phenacetin was popular for many decades, particularly in widely advertised over-the-counter "headache mixtures", usually containing phenacetin, an aminopyrine derivative of aspirin, caffeine, and sometimes a barbiturate. Paracetamol is the active metabolite of phenacetin and acetanilide, both once popular as analgesics and antipyretics in their own right. However, unlike phenacetin, acetanilide and their combinations, paracetamol is not considered carcinogenic at therapeutic doses. Von Mering's claims remained essentially unchallenged for half a century, until two teams of researchers from the United States analyzed the metabolism of acetanilide and paracetamol. In 1947 David Lester and Leon Greenberg found strong evidence that paracetamol was a major metabolite of acetanilide in human blood, and in a subsequent study they reported that large doses of paracetamol given to albino rats did not cause methemoglobinemia. In three papers published in the September 1948 issue of the Journal of Pharmacology and Experimental Therapeutics, Bernard Brodie, Julius Axelrod and Frederick Flinn confirmed using more specific methods that paracetamol was the major metabolite of acetanilide in human blood, and established that it was just as efficacious an analgesic as its precursor. They also suggested that methemoglobinemia is produced in humans mainly by another metabolite, phenylhydroxylamine. A follow-up paper by Brodie and Axelrod in 1949 established that phenacetin was also metabolised to paracetamol. This led to a "rediscovery" of paracetamol. It has been suggested that contamination of paracetamol with 4-aminophenol, the substance von Mering synthesised it from, may be the cause for his spurious findings. Paracetamol was first marketed in the United States in 1950 under the name Triagesic, a combination of paracetamol, aspirin, and caffeine. Reports in 1951 of three users stricken with the blood disease agranulocytosis led to its removal from the marketplace, and it took several years until it became clear that the disease was unconnected. Paracetamol was marketed in 1953 by Sterling-Winthrop Co. as Panadol, available only by prescription, and promoted as preferable to aspirin since it was safe for children and people with ulcers. In 1955, paracetamol was marketed as Children's Tylenol Elixir by McNeil Laboratories. In 1956, 500 mg tablets of paracetamol went on sale in the United Kingdom under the trade name Panadol, produced by Frederick Stearns & Co, a subsidiary of Sterling Drug Inc. In 1963, paracetamol was added to the British Pharmacopoeia, and has gained popularity since then as an analgesic agent with few side-effects and little interaction with other pharmaceutical agents. Concerns about paracetamol's safety delayed its widespread acceptance until the 1970s, but in the 1980s paracetamol sales exceeded those of aspirin in many countries, including the United Kingdom. This was accompanied by the commercial demise of phenacetin, blamed as the cause of analgesic nephropathy and hematological toxicity. In 1988 Sterling Winthrop was acquired by Eastman Kodak which sold the over the counter drug rights to SmithKline Beecham in 1994. Available without a prescription since 1959, it has since become a common household drug. Patents on paracetamol have long expired, and generic versions of the drug are widely available.

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Spasm

A spasm is a sudden involuntary contraction of a muscle, a group of muscles, or a hollow organ such as the heart.

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Tizanidine

Tizanidine (trade names Zanaflex (Acorda Therapeutics), Sirdalud (Novartis), Relentus (Beximco Pharma) Is a centrally acting α2 adrenergic agonist used as a muscle relaxant. It is used to treat the spasms, cramping, and tightness of muscles caused by medical problems such as multiple sclerosis, ALS, spastic diplegia, back pain, or certain other injuries to the spine or central nervous system. It is also prescribed off-label for migraine headaches, as a sleep aid, and as an anticonvulsant. It is also prescribed for some symptoms of fibromyalgia. Tizanidine has been found to be as effective as other antispasmodic drugs and is more tolerable than baclofen and diazepam. Tizanidine can be very strong even at the 2 mg dose and may cause hypotension, so caution is advised when it is used in patients who have a history of orthostatic hypotension, or when switching from gel cap to tablet form and vice versa. Tizanidine can occasionally cause acute liver failure. Clinical trials show that up to 5% of patients treated with tizanidine had elevated liver function test values, though symptoms disappeared upon withdrawal of the drug. Care should be used when first beginning treatment with tizanidine with regular liver tests for the first six months of treatment. As of 2015 the cost for a typical month of medication in the United States is US$100200.

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Vomiting

Vomiting, also known as emesis, puking, barfing, throwing up, among other terms, is the involuntary, forceful expulsion of the contents of one's stomach through the mouth and sometimes the nose.

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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.

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Redirects here:

ATC code M03BB03, ATCvet code QM03BB03, Biomioran, C7H4ClNO2, Chlorzoxazon, EZE-DS, Escoflex, Flexazone, Klorzoxazon, Mioran, Miotran, Muscol, Myoflexin, Myoflexine, Neoflex, Paraflex, Parafon Forte, Parafon Forte Dsc, Pathorysin, Relaxazone, Remular, Remular-S, Solaxin, Strifon Forte Dsc, Usaf Ma-10.

References

[1] https://en.wikipedia.org/wiki/Chlorzoxazone

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