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Tilidine Synthesis
Tilidine, or tilidate (brand names: Tilidin, Valoron, Tetova and Valtran) is a synthetic opioid painkiller, used mainly in Belgium, Bulgaria, Germany, Luxembourg, South Africa and Switzerland for the treatment of moderate to severe pain, both acute and chronic. Its onset of pain relief after oral administration is about 10–15 minutes and peak relief from pain occurs about 25–50 minutes after oral administration. Medical uses Tilidine is used in the form of hydrochloride or phosphate salt. In Germany, tilidine is available in a fixed combination with naloxone for oral administration (Valoron N and generics); the mixture of naloxone is claimed to lower the abuse liability of the opioid analgesic. This is so that if people take the medication orally (which is the way they are meant to) the opioid blocker, naloxone, has minimal effects on them but if they inject it the naloxone becomes bioavailable and hence antagonises the effects of the tilidine producing withdrawal effects. I ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
CYP3A4
Cytochrome P450 3A4 (abbreviated CYP3A4) () is an important enzyme in the body, mainly found in the liver and in the intestine. It oxidizes small foreign organic molecules ( xenobiotics), such as toxins or drugs, so that they can be removed from the body. It is highly homologous to CYP3A5, another important CYP3A enzyme. While many drugs are deactivated by CYP3A4, there are also some drugs which are ''activated'' by the enzyme. Some substances, such as some drugs and furanocoumarins present in grapefruit juice, interfere with the action of CYP3A4. These substances will therefore either amplify or weaken the action of those drugs that are modified by CYP3A4. CYP3A4 is a member of the cytochrome P450 family of oxidizing enzymes. Several other members of this family are also involved in drug metabolism, but CYP3A4 is the most common and the most versatile one. Like all members of this family, it is a hemoprotein, i.e. a protein containing a heme group with an iron atom. In humans, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Prodrug
A prodrug is a medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug. Instead of administering a drug directly, a corresponding prodrug can be used to improve how the drug is absorbed, distributed, metabolized, and excreted ( ADME). Prodrugs are often designed to improve bioavailability when a drug itself is poorly absorbed from the gastrointestinal tract. A prodrug may be used to improve how selectively the drug interacts with cells or processes that are not its intended target. This reduces adverse or unintended effects of a drug, especially important in treatments like chemotherapy, which can have severe unintended and undesirable side effects. History Many herbal extracts historically used in medicine contain glycosides (sugar derivatives) of the active agent, which are hydrolyzed in the intestines to release the active and more bioavailable aglycone. For example, salicin is a β-D-gluco ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Isomer
In chemistry, isomers are molecules or polyatomic ions with identical molecular formulae – that is, same number of atoms of each element – but distinct arrangements of atoms in space. Isomerism is existence or possibility of isomers. Isomers do not necessarily share similar chemical or physical properties. Two main forms of isomerism are structural or constitutional isomerism, in which '' bonds'' between the atoms differ; and stereoisomerism or spatial isomerism, in which the bonds are the same but the ''relative positions'' of the atoms differ. Isomeric relationships form a hierarchy. Two chemicals might be the same constitutional isomer, but upon deeper analysis be stereoisomers of each other. Two molecules that are the same stereoisomer as each other might be in different conformational forms or be different isotopologues. The depth of analysis depends on the field of study or the chemical and physical properties of interest. The English word "isomer" () is a bac ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dimethylamine
Dimethylamine is an organic compound with the formula (CH3)2NH. This secondary amine is a colorless, flammable gas with an ammonia-like odor. Dimethylamine is commonly encountered commercially as a solution in water at concentrations up to around 40%. An estimated 270,000 tons were produced in 2005. Structure and synthesis The molecule consists of a nitrogen atom with two methyl substituents and one proton. Dimethylamine is a weak base and the pKa of the ammonium CH3--CH3 is 10.73, a value above methylamine (10.64) and trimethylamine (9.79). Dimethylamine reacts with acids to form salts, such as dimethylamine hydrochloride, an odorless white solid with a melting point of 171.5 °C. Dimethylamine is produced by catalytic reaction of methanol and ammonia at elevated temperatures and high pressure: :2 CH3OH + NH3 → (CH3)2NH + 2 H2O Natural occurrence Dimethylamine is found quite widely distributed in animals and plants, and is present in many foods at the level ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Crotonaldehyde
Crotonaldehyde is a chemical compound with the formula CH3CH=CHCHO. The compound is usually sold as a mixture of the ''E''- and ''Z''-isomers, which differ with respect to the relative position of the methyl and formyl groups. The ''E''-isomer is more common (data given in Table is for the ''E''-isomer). This lachrymatory liquid is moderately soluble in water and miscible in organic solvents. As an unsaturated aldehyde, crotonaldehyde is a versatile intermediate in organic synthesis. It occurs in a variety of foodstuffs, e.g. soybean oils. Production and reactivity Crotonaldehyde is produced by the aldol condensation of acetaldehyde: :2 CH3CHO → CH3CH=CHCHO + H2O Crotonaldehyde is a multifunctional molecule that exhibits diverse reactivity. It is a prochiral dienophile. It is a Michael acceptor. Addition of methylmagnesium chloride produces 3-penten-2-ol. Polyurethane catalyst ''N'',''N'',''N''′,''N''′-tetramethyl-1,4-butanediamine (also known as NIAX TM ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tilidine Synthesis
Tilidine, or tilidate (brand names: Tilidin, Valoron, Tetova and Valtran) is a synthetic opioid painkiller, used mainly in Belgium, Bulgaria, Germany, Luxembourg, South Africa and Switzerland for the treatment of moderate to severe pain, both acute and chronic. Its onset of pain relief after oral administration is about 10–15 minutes and peak relief from pain occurs about 25–50 minutes after oral administration. Medical uses Tilidine is used in the form of hydrochloride or phosphate salt. In Germany, tilidine is available in a fixed combination with naloxone for oral administration (Valoron N and generics); the mixture of naloxone is claimed to lower the abuse liability of the opioid analgesic. This is so that if people take the medication orally (which is the way they are meant to) the opioid blocker, naloxone, has minimal effects on them but if they inject it the naloxone becomes bioavailable and hence antagonises the effects of the tilidine producing withdrawal effects. I ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
First Pass Effect
The first pass effect (also known as first-pass metabolism or presystemic metabolism) is a phenomenon of drug metabolism whereby the concentration of a drug, specifically when administered orally, is greatly reduced before it reaches the systemic circulation. It is the fraction of drug lost during the process of absorption which is generally related to the liver and gut wall. Notable drugs that experience a significant first-pass effect are buprenorphine, chlorpromazine, cimetidine, diazepam, ethanol (drinking alcohol), imipramine, insulin, lidocaine, midazolam, morphine, pethidine, propranolol, and tetrahydrocannabinol (THC). First pass metabolism may occur in the liver (for propranolol, lidocaine, clomethiazole, and NTG) or in the gut (for benzylpenicillin and insulin). After a drug is swallowed, it is absorbed by the digestive system and enters the hepatic portal system. It is carried through the portal vein into the liver before it reaches the rest of the body. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bisnortilidine
Bisnortilidine is an opioid Opioids are substances that act on opioid receptors to produce morphine-like effects. Medically they are primarily used for pain relief, including anesthesia. Other medical uses include suppression of diarrhea, replacement therapy for opioi ... metabolite. It is formed from tilidine by demethylation in the liver. References {{organic-compound-stub Human metabolites Cyclohexenes ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nortilidine
Nortilidine is the major active metabolite of tilidine. It is formed from tilidine by demethylation in the liver. The racemate has opioid analgesic effects roughly equivalent in potency to that of morphine. The (1R,2S) isomer has NMDA antagonist activity. The drug also acts as a dopamine reuptake inhibitor. The reversed-ester of nortilidine is also known, as is the corresponding analogue with the cyclohexene ring replaced by cyclopentane, which have almost identical properties to nortilidine. Use Nortilidine has been sold as a designer drug A designer drug is a structural or functional analog of a controlled substance that has been designed to mimic the pharmacological effects of the original drug, while avoiding classification as illegal and/or detection in standard drug tests. Des ..., first being identified in Poland in May 2020. See also * Desmetramadol, another opioid metabolite with additional (non-opioid) mechanisms of analgesia, which has also been sold as a designe ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Injection (medicine)
An injection (often and usually referred to as a "shot" in US English, a "jab" in UK English, or a "jag" in Scottish English and Scots) is the act of administering a liquid, especially a drug, into a person's body using a needle (usually a hypodermic needle) and a syringe. An injection is considered a form of parenteral drug administration; it does not involve absorption in the digestive tract. This allows the medication to be absorbed more rapidly and avoid the first pass effect. There are many types of injection, which are generally named after the body tissue the injection is administered into. This includes common injections such as subcutaneous, intramuscular, and intravenous injections, as well as less common injections such as intraperitoneal, intraosseous, intracardiac, intraarticular, and intracavernous injections. Injections are among the most common health care procedures, with at least 16 billion administered in developing and transitional countries each ye ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Suppository
A suppository is a dosage form used to deliver medications by insertion into a body orifice where it dissolves or melts to exert local or systemic effects. There are three types of suppositories, each to insert into a different sections: rectal suppositories into the rectum, vaginal suppositories into the vagina, and urethral suppositories into the urethra of a male. Suppositories are ideal for infants, elderly individuals and post-operative patients, who are unable to swallow oral medications, and for individuals experiencing severe nausea and/or vomiting. Composition Several different ingredients can be used to form the base of a suppository: cocoa butter or a similar substitute, polyethylene glycol, hydrogels, and glycerinated gelatin. The type of material used depends on the type of suppository, the type of drug, and the conditions in which the suppository will be stored. Rectal suppositories In 1991, a study on suppository insertion in ''The Lancet'' found that the "to ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
