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Diacetylnalorphine
Diacetylnalorphine ( BAN), also known as ''O''3,''O''6-diacetyl-''N''-allyl-normorphine, is an opioid drug described as an analgesic and antidote which was never marketed. It is the 3,6-diacetyl ester of nalorphine, and therefore the heroin analogue of nalorphine. Diacetylnalorphine may behave as a prodrug to nalorphine, similarly to the cases of heroin (diacetylmorphine) to morphine and diacetyldihydromorphine to dihydromorphine. See also * Nalorphine dinicotinate Nalorphine dinicotinate (trade name Nimelan), also known as ''N''-allylnormorphine dinicotinate, dinicotinoylnalorphine, or niconalorphine, is a semisynthetic, mixed opioid agonist- antagonist which is described as a narcotic antagonist but may ... References Analgesics Antidotes Delta-opioid receptor antagonists 4,5-Epoxymorphinans Kappa-opioid receptor agonists Mu-opioid receptor antagonists Semisynthetic opioids {{Analgesic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nalorphine Dinicotinate
Nalorphine dinicotinate (trade name Nimelan), also known as ''N''-allylnormorphine dinicotinate, dinicotinoylnalorphine, or niconalorphine, is a semisynthetic, mixed opioid agonist- antagonist which is described as a narcotic antagonist but may produce limited analgesia and sedation at higher doses in opioid naive patients (with limited euphoria and dependence liability). It is the 3,6- dinicotinate ester of nalorphine, and is therefore the nalorphine analogue of nicomorphine (which is the 3,6-dinicotinate ester of morphine). As nalorphine dinicotinate is only regulated at the Rx (prescription required) drug, it would be legal to possess with a valid prescription should a patient manage to acquire it. See also * Diacetylnalorphine Diacetylnalorphine (BAN), also known as ''O''3,''O''6-diacetyl-''N''-allyl-normorphine, is an opioid drug described as an analgesic and antidote which was never marketed. It is the 3,6-diacetyl ester of nalorphine, and therefore the heroin analog . ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Nalorphine
Nalorphine () (brand names Lethidrone, Nalline), also known as ''N''-allylnormorphine, is a mixed opioid agonist–antagonist with opioid antagonist and analgesic properties. It was introduced in 1954 and was used as an antidote to reverse opioid overdose and in a challenge test to determine opioid dependence. Nalorphine was the second opioid antagonist to be introduced, preceded by nalodeine (''N''-allylnorcodeine) in 1915 and followed by naloxone in 1960 and naltrexone in 1963. Due to potent activation of the κ-opioid receptor, nalorphine produces side effects such as dysphoria, anxiety, confusion, and hallucinations, and for this reason, is no longer used medically. Pharmacology Pharmacodynamics Nalorphine acts at two opioid receptors — the μ-opioid receptor (MOR) where it has antagonistic effects, and at the κ-opioid receptor (KOR) (Ki = 1.6 nM; EC50 = 483 nM; Emax = 95%) where it exerts high-efficacy partial agonist/near-full agonist characteristics. Chemistry Ana ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Diacetyldihydromorphine
Diacetyldihydromorphine (also known as Paralaudin, dihydroheroin, acetylmorphinol) is a potent opiate derivative developed in Germany in 1928 which is rarely used in some countries for the treatment of severe pain such as that caused by terminal cancer, as another form of diacetylmorphine (also commonly known as Heroin). Diacetyldihydromorphine is fast-acting and longer-lasting than diamorphine, with a duration of action of around 4-7 hours. As an ester/analogue of dihydromorphine, diacetyldihydromorphine is presumably a Schedule I/Narcotic controlled substance in the United States but does not have its own ACSCN or annual production quota. It does appear in the German Betäubungsmittelgesetz and other European controlled-substances laws. Diacetyldihydromorphine is quickly metabolized by plasma esterase enzymes into dihydromorphine, in the same way that diamorphine is metabolized into morphine. Diamorphine is 1.50–1.80 times the potency of morphine. It shares with other opioi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antidotes
An antidote is a substance that can counteract a form of poisoning. The term ultimately derives from the Greek term φάρμακον ἀντίδοτον ''(pharmakon) antidoton'', "(medicine) given as a remedy". Antidotes for anticoagulants are sometimes referred to as reversal agents. The antidotes for some particular toxins are manufactured by injecting the toxin into an animal in small doses and extracting the resulting antibodies from the host animals' blood. This results in an antivenom that can be used to counteract venom produced by certain species of snakes, spiders, and other venomous animals. Some animal venoms, especially those produced by arthropods (such as certain spiders, scorpions, and bees) are only potentially lethal when they provoke allergic reactions and induce anaphylactic shock; as such, there is no "antidote" for these venoms; however anaphylactic shock can be treated (e.g. with epinephrine). Some other toxins have no known antidote. For example, the pois ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Analgesics
An analgesic drug, also called simply an analgesic (American English), analgaesic (British English), pain reliever, or painkiller, is any member of the group of drugs used to achieve relief from pain (that is, analgesia or pain management). It is typically used to induce cooperation with a medical procedure. Analgesics are conceptually distinct from anesthetics, which temporarily reduce, and in some instances eliminate, sensation, although analgesia and anesthesia are neurophysiologically overlapping and thus various drugs have both analgesic and anesthetic effects. Analgesic choice is also determined by the type of pain: For neuropathic pain, traditional analgesics are less effective, and there is often benefit from classes of drugs that are not normally considered analgesics, such as tricyclic antidepressants and anticonvulsants. Various analgesics, such as many NSAIDs, are available over the counter in most countries, whereas various others are prescription drugs owing to t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dihydromorphine
Dihydromorphine (Paramorfan, Paramorphan) is a semi-synthetic opioid structurally related to and derived from morphine. The 7,8-double bond in morphine is reduced to a single bond to get dihydromorphine.Rama Rao Nadendla. Principles Of Organic Medicinal Chemistry pp. 215 Dihydromorphine is a moderately strong analgesic and is used clinically in the treatment of pain and also is an active metabolite of the analgesic opioid drug dihydrocodeine. Dihydromorphine occurs in trace quantities in assays of opium on occasion, as does dihydrocodeine, dihydrothebaine, tetrahydrothebaine, etc. The process for manufacturing dihydromorphine from morphine for pharmaceutical use was developed in Germany in the late 19th century, with the synthesis being published in 1900 and the drug introduced clinically as Paramorfan shortly thereafter. A high-yield synthesis from tetrahydrothebaine was later developed. Uses Medical Dihydromorphine is used for the management of moderate to severe pain such ... [...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-glucopyranosid ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Morphine
Morphine is a strong opiate that is found naturally in opium, a dark brown resin in poppies (''Papaver somniferum''). It is mainly used as a analgesic, pain medication, and is also commonly used recreational drug, recreationally, or to make other illicit drug, illicit opioids. There are numerous methods used to administer morphine: oral; sublingual administration, sublingual; via inhalation; intramuscular, injection into a muscle; by Subcutaneous injection, injection under the skin; intravenously; Intrathecally, injection into the space around the spinal cord; transdermal; or via rectal administration, rectal suppository. It acts directly on the central nervous system (CNS) to induce analgesia and alter perception and emotional response to pain. Physical and psychological dependence and tolerance may develop with repeated administration. It can be taken for both acute pain and chronic pain and is frequently used for pain from myocardial infarction, kidney stones, and during Ch ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
