Piperidione
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Piperidione
Piperidione (trade name Sedulon) is a sedative drug, structurally related to methyprylon and pyrithyldione. It used to be marketed by Roche as a cough medicine available in liquid form. In the US, it was approved by the FDA on grounds of safety alone in 1947. After Roche failed to submit evidence of efficacy to the Drug Efficacy Study Implementation program in 1972, it was withdrawn from the US market. See also *Glutethimide Glutethimide is a hypnotic sedative that was introduced by Ciba in 1954 as a safe alternative to barbiturates to treat insomnia. Before long, however, it had become clear that glutethimide was just as likely to cause addiction and caused simila ... References Withdrawn drugs Antitussives 2-Piperidinones GABAA receptor positive allosteric modulators Sedatives 4-Piperidinones {{respiratory-system-drug-stub ...
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Methyprylon
Methyprylon, or Noludar, is a sedative of the piperidinedione derivative family first developed by Hoffmann-La Roche. This medicine was used for treating insomnia, but is now rarely used as it has been replaced by newer drugs with fewer side effects, such as benzodiazepines. Methyprylon was withdrawn from the US market in June 1975 and the Canadian market in September 1990. Some other trade names are Noctan and Dimerin. Adverse effects Side effects can include skin rash, fever, depression, ulcers or sores in mouth or throat, unusual bleeding or bruising, confusion, fast heartbeat, respiratory depression, swelling of feet or lower legs, dizziness, drowsiness, headache, double vision, clumsiness, constipation, diarrhea, nausea, vomiting, unusual weakness. Pharmacokinetics A study of single oral doses of 300 mg in healthy volunteers found that the zero-order absorption model fit the data best. Mean (+/- SD) values for the half-life (9.2 +/- 2.2 h), apparent clearance, (11.91 ...
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Pyrithyldione
Pyrithyldione (Presidon, Persedon) is a psychoactive drug invented in 1949. An improved method of manufacture was patented by Roche in 1959. It was used as a hypnotic or sedative and presumed to be less toxic than barbiturates. Today, this substance is no longer used. Agranulocytosis was sometimes reported as adverse effect An adverse effect is an undesired harmful effect resulting from a medication or other intervention, such as surgery. An adverse effect may be termed a " side effect", when judged to be secondary to a main or therapeutic effect. The term compl .... Pyrithyldione is also a CYP2D6 inducer but is not as potent as glutethimide s pyrithyldione (Benedorm) an enzyme inducer (author's transl)Pharmazie. 1982 Jan;37(1):69. In studies, it increased the O-Demethylation of codeine by 20%. See also * Methyprylon * Piperidione * Glutethimide References Hypnotics Lactams Ketones GABAA receptor positive allosteric modulators Abandoned drugs {{se ...
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Glutethimide
Glutethimide is a hypnotic sedative that was introduced by Ciba in 1954 as a safe alternative to barbiturates to treat insomnia. Before long, however, it had become clear that glutethimide was just as likely to cause addiction and caused similar withdrawal symptoms. Doriden was the brand-name version. Current production levels in the United States (the annual quota for manufacturing imposed by the DEA has been three grams, enough for six Doriden tablets, for a number of years) point to its use only in small-scale research. Manufacturing of the drug was discontinued in the US in 1993 and discontinued in several eastern European countries in 2006. Long term use Long-term use rebound effects, which resembled those seen in withdrawal, have anecdotally been described in patients who were still taking a stable dose of the drug. The symptoms included delirium, hallucinosis, convulsions and fever. Recreational use Glutethimide is a CYP2D6 enzyme inducer. When taken with codeine, (kn ...
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Sedative
A sedative or tranquilliser is a substance that induces sedation by reducing irritability or excitement. They are CNS depressants and interact with brain activity causing its deceleration. Various kinds of sedatives can be distinguished, but the majority of them affect the neurotransmitter gamma-aminobutyric acid (GABA). In spite of the fact that each sedative acts in its own way, most produce relaxing effects by increasing GABA activity. This group is related to hypnotics. The term ''sedative'' describes drugs that serve to calm or relieve anxiety, whereas the term ''hypnotic'' describes drugs whose main purpose is to initiate, sustain, or lengthen sleep. Because these two functions frequently overlap, and because drugs in this class generally produce dose-dependent effects (ranging from anxiolysis to loss of consciousness) they are often referred to collectively as ''sedative-hypnotic'' drugs. Sedatives can be used to produce an overly-calming effect ( alcohol being the m ...
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Hoffmann-La Roche
F. Hoffmann-La Roche AG, commonly known as Roche, is a Swiss multinational healthcare company that operates worldwide under two divisions: Pharmaceuticals and Diagnostics. Its holding company, Roche Holding AG, has shares listed on the SIX Swiss Exchange. The company headquarters are located in Basel. Roche is the fifth largest pharmaceutical company in the world by revenue, and the leading provider of cancer treatments globally. The company controls the American biotechnology company Genentech, which is a wholly owned affiliate, and the Japanese biotechnology company Chugai Pharmaceuticals, as well as the United States-based companies Ventana and Foundation Medicine. Roche's revenues during fiscal year 2020 were 58.32 billion Swiss francs. Descendants of the founding Hoffmann and Oeri families own slightly over half of the bearer shares with voting rights (a pool of family shareholders 45%, and Maja Oeri a further 5% apart), with Swiss pharma firm Novartis owning a furth ...
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Cough Suppressant
Cold medicines are a group of medicinal, medications taken individually or in Combination drug, combination as a Symptomatic treatment, treatment for the symptoms of the common cold and similar conditions of the upper respiratory tract. The term encompasses a broad array of drugs, including analgesics, antihistamines and decongestants, among many others. It also includes drugs which are marketed as cough suppressants or antitussives, but their effectiveness in reducing cough symptoms is unclear or minimal. While they have been used by 10% of American children in any given week, they are not recommended in Canada or the United States in children six years or younger because of lack of evidence showing effect and concerns of harm. In 2020, one version containing codeine and guaifenesin was the 377th most commonly prescribed medication in the United States with more than 400thousand prescriptions. Types There are a number of different cough and cold medications, which may be use ...
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Drug Efficacy Study Implementation
Drug Efficacy Study Implementation (DESI) was a program begun by the Food and Drug Administration (FDA) in the 1960s after the requirement (in the Kefauver-Harris Drug Control Act) that all drugs be efficacious as well as safe, was made part of US law. The DESI program was intended to classify all pre-1962 drugs that were already on the market as either effective, ineffective, or needing further study.Pharmacy Today. August 2008.FDA aims to remove unapproved drugs from market: Risk-based enforcement program focuses on removing potentially harmful products/ref> The Drug Efficacy Study Implementation (DESI) evaluated over 3,000 separate products and over 16,000 therapeutic claims. By 1984, final action had been completed on 3,443 products; of these, 2,225 were found to be effective, 1,051 were found not effective, and 167 were pending. One of the early effects of the DESI study was the development of the Abbreviated New Drug Application (ANDA). See also * Estes Kefauver * Federal ...
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Withdrawn Drugs
Withdrawal means "an act of taking out" and may refer to: * Anchoresis (withdrawal from the world for religious or ethical reasons) * ''Coitus interruptus'' (the withdrawal method) * Drug withdrawal * Social withdrawal * Taking of money from a bank * Water withdrawal * Withdrawal (military) * Withdrawal reflex * ''Withdrawal'', Twista Carl Terrell Mitchell (born November 27, 1973), better known by his stage name Twista (formerly Tung Twista), is an American rapper and record producer. He is best known for his Chopper (rap), chopper style of rapping and for once holding the t .../ Do or Die EP * "Withdrawals" (Tyler Farr song) See also

* * {{disambiguation ...
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Antitussives
Cold medicines are a group of medications taken individually or in combination as a treatment for the symptoms of the common cold and similar conditions of the upper respiratory tract. The term encompasses a broad array of drugs, including analgesics, antihistamines and decongestants, among many others. It also includes drugs which are marketed as cough suppressants or antitussives, but their effectiveness in reducing cough symptoms is unclear or minimal. While they have been used by 10% of American children in any given week, they are not recommended in Canada or the United States in children six years or younger because of lack of evidence showing effect and concerns of harm. In 2020, one version containing codeine and guaifenesin was the 377th most commonly prescribed medication in the United States with more than 400thousand prescriptions. Types There are a number of different cough and cold medications, which may be used for various coughing symptoms. The commercially a ...
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GABAA Receptor Positive Allosteric Modulators
In pharmacology, GABAA receptor positive allosteric modulators are positive allosteric modulator (PAM) molecules that increase the activity of the GABAA receptor protein in the vertebrate central nervous system. GABA is a major inhibitory neurotransmitter in the central nervous system. Upon binding, it triggers the GABAA receptor to open its chloride channel to allow chloride ions into the neuron, making the cell hyperpolarized and less likely to fire. GABAA PAMs increase the effect of GABA by making the channel open more frequently or for longer periods. However, they have no effect if GABA or another agonist is not present. Unlike GABAA receptor agonists, GABAA PAMs do not bind at the same active site as the γ-Aminobutyric acid (GABA) neurotransmitter molecule: they affect the receptor by binding at a different site on the protein. This is called allosteric modulation. In psychopharmacology, GABAA receptor PAMs used as drugs have mainly sedative and anxiolytic effects. ...
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Sedatives
A sedative or tranquilliser is a substance that induces sedation by reducing irritability or excitement. They are CNS depressants and interact with brain activity causing its deceleration. Various kinds of sedatives can be distinguished, but the majority of them affect the neurotransmitter gamma-aminobutyric acid (GABA). In spite of the fact that each sedative acts in its own way, most produce relaxing effects by increasing GABA activity. This group is related to hypnotics. The term ''sedative'' describes drugs that serve to calm or relieve anxiety, whereas the term ''hypnotic'' describes drugs whose main purpose is to initiate, sustain, or lengthen sleep. Because these two functions frequently overlap, and because drugs in this class generally produce dose-dependent effects (ranging from anxiolysis to loss of consciousness) they are often referred to collectively as ''sedative-hypnotic'' drugs. Sedatives can be used to produce an overly-calming effect (alcohol being the most ...
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