Mephenesin
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Mephenesin
Mephenesin (INN) is a centrally acting muscle relaxant. It can be used as an antidote for strychnine poisoning. Mephenesin however presents with the major drawbacks of having a short duration of action and a much greater effect on the spinal cord than the brain, resulting in pronounced respiratory depression at clinical doses and therefore a very low therapeutic index. It is especially dangerous and potentially fatal in combination with alcohol and other depressants. Mephenesin was used by Bernard Ludwig and Frank Berger to synthesize meprobamate, the first tranquilizer to see widespread clinical use. Mephenesin is no longer available in North America but is used in Italy and a few other countries. Its use has largely been replaced by the related drug methocarbamol, which is better absorbed. Mephenesin may be an NMDA receptor antagonist. Mephenesin was previously used in France as an OTC muscle relaxant called Décontractyl but was taken out of production by Sanofi Aventis and ...
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Meprobamate
Meprobamate—marketed as Miltown by Wallace Laboratories and Equanil by Wyeth, among others—is a carbamate derivative used as an anxiolytic drug. It was the best-selling minor tranquilizer for a time, but has largely been replaced by the benzodiazepines due to their wider therapeutic index (lower risk of toxicity at therapeutically prescribed doses) and lower incidence of serious side effects. History Frank Berger was working in a laboratory of a British drug company, looking for a preservative for penicillin, when he noticed that a compound called mephenesin calmed laboratory rodents without actually sedating them. Berger subsequently referred to this “tranquilizing” effect in a now-historic article, published by the ''British Journal of Pharmacology'' in 1946. However, three major drawbacks existed to the use of mephenesin as a tranquilizer: a very short duration of action, greater effect on the spinal cord than on the brain (resulting in a very low therapeutic index), ...
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Prenderol
Prenderol (Diethylpropanediol) is a simple alkyl diol which has sedative, anticonvulsant and muscle relaxant effects. It is closely related in structure to meprobamate and numerous other alkyl alcohols and diols with generally comparable activity.Reyes Q., Aaurelio; Mascetti V., G.; Martinez J., Rolando. Synthesis of polyhydroxylated alcohols. ''Revista Latinoamericana de Quimica'' 1984; 15 (1): 29-30. ISSN: 0370-5943. See also * 1,4-Butanediol * 1,6-Dioxecane-2,7-dione * 1-Ethynylcyclohexanol * 2-Methyl-2-propyl-1,3-propanediol * 2-Methyl-2-butanol * 2-Methyl-2-pentanol * 3-Methyl-3-pentanol * 3-Hydroxybutanal * Ethchlorvynol * Phenaglycodol Phenaglycodol (brand names Acalmid, Acalo, Alterton, Atadiol, Felixyn, Neotran, Pausital, Remin, Sedapsin, Sinforil, Stesil, Ultran) is a drug described as a tranquilizer or sedative which has anxiolytic and anticonvulsant properties. It is relat ... References Alkanediols Muscle relaxants {{musculoskeletal-drug-stub ...
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Frank Berger
Frank Milan Berger (June 25, 1913 - March 18, 2008) was a Czechoslovakian pharmacologist who discovered meprobamate, carisoprodol, and felbamate, while working at Wallace Laboratories. He also discovered the 'tranquilising' effects of mephenesin in rodents while working at a laboratory in the United Kingdom The United Kingdom of Great Britain and Northern Ireland, commonly known as the United Kingdom (UK) or Britain, is a country in Europe, off the north-western coast of the continental mainland. It comprises England, Scotland, Wales and North ..., and campaigned against the advertising of medications in the mass media. References {{DEFAULTSORT:Berger, Frank 1913 births 2008 deaths Scientists from Plzeň Czechoslovak pharmacologists Charles University alumni ...
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Methocarbamol
Methocarbamol, sold under the brand name Robaxin among others, is a medication used for short-term musculoskeletal pain. It may be used together with rest, physical therapy, and pain medication. It is less preferred in low back pain. It has limited use for rheumatoid arthritis and cerebral palsy. Effects generally begin within half an hour. It is taken by mouth or injection into a vein. Common side effect include headaches, sleepiness, and dizziness. Serious side effects may include anaphylaxis, liver problems, confusion, and seizures. Use is not recommended in pregnancy and breastfeeding. Because of risk of injury, skeletal muscle relaxants should generally be avoided in geriatric patients. Methocarbamol is a centrally acting muscle relaxant. How it works is unclear, but it does not appear to affect muscles directly. History and culture Methocarbamol was developed in 1956 in the laboratories of A. H. Robins (later acquired by Pfizer). Studies were directed towards the deve ...
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Methocarbamol
Methocarbamol, sold under the brand name Robaxin among others, is a medication used for short-term musculoskeletal pain. It may be used together with rest, physical therapy, and pain medication. It is less preferred in low back pain. It has limited use for rheumatoid arthritis and cerebral palsy. Effects generally begin within half an hour. It is taken by mouth or injection into a vein. Common side effect include headaches, sleepiness, and dizziness. Serious side effects may include anaphylaxis, liver problems, confusion, and seizures. Use is not recommended in pregnancy and breastfeeding. Because of risk of injury, skeletal muscle relaxants should generally be avoided in geriatric patients. Methocarbamol is a centrally acting muscle relaxant. How it works is unclear, but it does not appear to affect muscles directly. History and culture Methocarbamol was developed in 1956 in the laboratories of A. H. Robins (later acquired by Pfizer). Studies were directed towards the deve ...
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Mephenoxalone
Mephenoxalone (trade names Dorsiflex, Moderamin, Control-OM) is a muscle relaxant and mild anxiolytic. MIMSMephenoxalone/ref> It inhibits neuron transmission, relaxing skeletal muscles by inhibiting the reflex arc. As the effect of muscle relaxation, mephenoxalone affects mental condition, and is also a treatment for nervousness and anxiety. See also * Chlorphenesin * Guaifenesin * Mephenesin * Metaxalone * Methocarbamol Methocarbamol, sold under the brand name Robaxin among others, is a medication used for short-term musculoskeletal pain. It may be used together with rest, physical therapy, and pain medication. It is less preferred in low back pain. It has l ... References Carbamates Drugs with unknown mechanisms of action Oxazolidines Phenol ethers Methoxy compounds {{sedative-stub ...
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Drugs With Unknown Mechanisms Of Action
A drug is any chemical substance that causes a change in an organism's physiology or psychology when consumed. Drugs are typically distinguished from food and substances that provide nutritional support. Consumption of drugs can be via inhalation, injection, smoking, ingestion, absorption via a patch on the skin, suppository, or dissolution under the tongue. In pharmacology, a drug is a chemical substance, typically of known structure, which, when administered to a living organism, produces a biological effect. A pharmaceutical drug, also called a medication or medicine, is a chemical substance used to treat, cure, prevent, or diagnose a disease or to promote well-being. Traditionally drugs were obtained through extraction from medicinal plants, but more recently also by organic synthesis. Pharmaceutical drugs may be used for a limited duration, or on a regular basis for chronic disorders. Pharmaceutical drugs are often classified into drug classes—groups of related drugs ...
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Diols
A diol is a chemical compound containing two hydroxyl groups ( groups). An aliphatic diol is also called a glycol. This pairing of functional groups is pervasive, and many subcategories have been identified. The most common industrial diol is ethylene glycol. Examples of diols in which the hydroxyl functional groups are more widely separated include 1,4-butanediol and propylene-1,3-diol, or beta propylene glycol, . Synthesis of classes of diols Geminal diols A geminal diol has two hydroxyl groups bonded to the same atom. These species arise by hydration of the carbonyl compounds. The hydration is usually unfavorable, but a notable exception is formaldehyde which, in water, exists in equilibrium with methanediol H2C(OH)2. Another example is (F3C)2C(OH)2, the hydrated form of hexafluoroacetone. Many gem-diols undergo further condensation to give dimeric and oligomeric derivatives. This reaction applies to glyoxal and related aldehydes. Vicinal diols In a vicinal diol, t ...
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NMDA Receptor Antagonist
NMDA receptor antagonists are a class of drugs that work to antagonize, or inhibit the action of, the ''N''-Methyl-D-aspartate receptor (NMDAR). They are commonly used as anesthetics for animals and humans; the state of anesthesia they induce is referred to as dissociative anesthesia. Several synthetic opioids function additionally as NMDAR-antagonists, such as pethidine, levorphanol, methadone, dextropropoxyphene, tramadol and ketobemidone. Some NMDA receptor antagonists, such as ketamine, dextromethorphan (DXM), phencyclidine (PCP), methoxetamine (MXE), and nitrous oxide (N2O), are sometimes used as recreational drugs, for their dissociative, hallucinogenic, and euphoriant properties. When used recreationally, they are classified as dissociative drugs. Uses and effects NMDA receptor antagonists induce a state called dissociative anesthesia, marked by catalepsy, amnesia, and analgesia. Ketamine is a favored anesthetic for emergency patients with unknown medical history and i ...
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Guaifenesin
Guaifenesin, also known as glyceryl guaiacolate, is an expectorant medication that aids in the elimination of sputum from the respiratory tract. Chemically it is an ether of guaiacol and glycerine. It is often used in combination with other medications. It is taken by mouth. Side effects may include dizziness, sleepiness, skin rash, and nausea. While it has not been properly studied in pregnancy, it appears to be safe. It is believed to work by making airway secretions more liquid. Guaifenesin has been used medically since at least 1933. It is available as a generic medication and over the counter. In 2020, it was the 324th most commonly prescribed medication in the United States, with more than 800,000 prescriptions. Medical use Guaifenesin is used to try to help with coughing up thick mucus and is sometimes combined with dextromethorphan, an antitussive (cough suppressant), such as in Mucinex DM or Robitussin DM. It is also combined with ephedrine to produce Primatene and ...
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Chlorphenesin
Chlorphenesin carbamate (Maolate, Musil) is a centrally acting muscle relaxant used to treat muscle pain and spasms. Chlorphenesin is no longer used for this purpose in most developed nations due to the availability of much safer spasmolytics such as benzodiazepines. Other central effects include sedation, anxiolysis, and dizziness. It also has antifungal and some antibacterial properties and is thus classified as an antifungal for topical use by the WHO. Safety The major adverse effect from this preservative on skin is allergic contact sensitivity. Systemic intoxication from transdermal Transdermal is a route of administration wherein active ingredients are delivered across the skin for systemic distribution. Examples include transdermal patches used for medicine delivery. The drug is administered in the form of a patch or ointme ... use has not been observed, although the FDA discourages its use as an ingredient in nipple cream for nursing mothers. References {{Muscle ...
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