|
Dihydroetorphine
Dihydroetorphine was developed by K. W. Bentley at McFarlan-Smith in the 1960s and is a potent opioid analgesic used mainly in China. It is a derivative of the better-known opioid etorphine, a very potent veterinary painkiller and anesthetic medication used primarily for the sedation of large animals such as elephants, giraffes, and rhinos. Dihydroetorphine is a semi- synthetic opioid used mainly as a strong painkiller for humans. It is several thousand times stronger than morphine (between 1000x and 12000x more potent depending what method is used for comparison), although it is poorly absorbed when taken orally. Sublingual forms of dihydroetorphine are used in China at doses ranging from 20 to 40 μg repeated every 3-4 hours, and are reported to cause strong analgesia and relatively mild side effects compared to other opioids, although all the usual opioid side effects such as dizziness, sedation, nausea, constipation, and respiratory depression can occur. Transdermal patche ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 opioid use disorder, reversing opioid overdose, and suppressing cough. Extremely potent opioids such as carfentanil are approved only for veterinary use. Opioids are also frequently used non-medically for their euphoric effects or to prevent withdrawal. Opioids can cause death and have been used for executions in the United States. Side effects of opioids may include itchiness, sedation, nausea, respiratory depression, constipation, and euphoria. Long-term use can cause tolerance, meaning that increased doses are required to achieve the same effect, and physical dependence, meaning that abruptly discontinuing the drug leads to unpleasant withdrawal symptoms. The euphoria attracts recreational use, and frequent, escalating recreational use of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Semisynthetic Opioids
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 opioid use disorder, reversing opioid overdose, and suppressing cough. Extremely potent opioids such as carfentanil are approved only for veterinary use. Opioids are also frequently used non-medically for their euphoric effects or to prevent withdrawal. Opioids can cause death and have been used for executions in the United States. Side effects of opioids may include itchiness, sedation, nausea, respiratory depression, constipation, and euphoria. Long-term use can cause tolerance, meaning that increased doses are required to achieve the same effect, and physical dependence, meaning that abruptly discontinuing the drug leads to unpleasant withdrawal symptoms. The euphoria attracts recreational use, and frequent, escalating recreational use of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Etorphine
Etorphine (M99) is a semi-synthetic opioid possessing an analgesic potency approximately 1,000–3,000 times that of morphine. It was first prepared in 1960 from oripavine, which does not generally occur in opium poppy extract but rather the related plants ''Papaver orientale'' and ''Papaver bracteatum''. It was later reproduced in 1963 by a research group at MacFarlan Smith in Gorgie, Edinburgh, led by Kenneth Bentley. It can also be produced from thebaine. Veterinary use Etorphine is available legally only for veterinary use and is strictly governed by law. It is often used to immobilize elephants and other large mammals. Diprenorphine (Revivon) is an opioid receptor antagonist that can be administered in proportion to the amount of etorphine used (1.3 times) to reverse its effects. Veterinary-strength etorphine is fatal to humans. For this reason the package as supplied to vets always includes the human antidote along with the etorphine. The human antidote is generally na ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Equianalgesic
An equianalgesic chart is a conversion chart that lists equivalent doses of analgesics (drugs used to relieve pain). Equianalgesic charts are used for calculation of an equivalent dose (a dose which would offer an equal amount of analgesia) between different analgesics. Tables of this general type are also available for NSAIDs, benzodiazepines, depressants, stimulants, anticholinergics and others as well. Format Equianalgesic tables are available in different formats, such as pocket-sized cards for ease of reference. A frequently-seen format has the drug names in the left column, the route of administration in the center columns and any notes in the right column. Purpose There are several reasons for switching a patient to a different pain medication. These include practical considerations such as lower cost or unavailability of a drug at the patient's preferred pharmacy, or medical reasons such as lack of effectiveness of the current drug or to minimize adverse effects. Some pa ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Thienorphine
Thienorphine is a very potent, extremely long-acting, orally-active opioid analgesic with mixed agonist–antagonist properties which was developed by the Beijing Institute of Pharmacology and Toxicology as a potential treatment for opioid dependence. It is a high-affinity, balanced ligand of the μ- (Ki = 0.22 nM), δ- (Ki = 0.69 nM), and κ-opioid receptors (Ki = 0.14 nM), behaving as a partial agonist of the μ- ( Emax = 19%–28%) and κ-opioid receptors (Emax = 65–75%) and as an antagonist of the δ-opioid receptor. It also possesses relatively low affinity for the nociceptin receptor (Ki = 36.5 nM), where it acts as an antagonist. See also * Buprenorphine * Etorphine * Dihydroetorphine * Diprenorphine Diprenorphine (brand name Revivon; former developmental code name M5050), also known as diprenorfin, is a non-selective, high- affinity, weak partial agonist of the μ- (MOR), κ- (KOR), and δ-opioid receptor (DOR) (with equal affinity) which ... References D ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Acetorphine
Acetorphine is a potent opioid analgesic, up to 8700 times stronger than morphine by weight. It is a derivative of the more well-known opioid etorphine, which is used as a very potent veterinary painkiller and anesthetic medication, primarily for the sedation of large animals such as elephants, giraffes and rhinos. Acetorphine was developed in 1966 by the Reckitt research group that developed etorphine. Acetorphine was developed for the same purpose as etorphine itself, namely as a strong tranquilizer for use in immobilizing large animals in veterinary medicine. Despite showing some advantages over etorphine, for instance producing less toxic side effects in giraffes, acetorphine was never widely adopted for veterinary use, and etorphine (along with other tranquilizers such as carfentanil and azaperone) remains the drug of choice in this application. Legal Status Australia Acetorphine is a schedule 9 substance in Australia under the Poisons Standard (February 2017). A schedule ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Substance Use Disorder
Substance use disorder (SUD) is the persistent use of drugs (including alcohol) despite substantial harm and adverse consequences as a result of their use. Substance use disorders are characterized by an array of mental/emotional, physical, and behavioral problems such as chronic guilt; an inability to reduce or stop consuming the substance(s) despite repeated attempts; operating vehicles while intoxicated; and physiological withdrawal symptoms. Drug classes that are commonly involved in SUD include: alcohol (alcoholism); cannabis; opioids; stimulants such as nicotine (including tobacco), cocaine and amphetamines; benzodiazepines; barbiturates; and other or unknown substances. In the Diagnostic and Statistical Manual of Mental Disorders 5th edition (2013), also known as DSM-5, the DSM-IV diagnoses of substance abuse and substance dependence were merged into the category of substance use disorders. The severity of substance use disorders can vary widely; in the DSM-5 diagnosi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Phenols
In organic chemistry, phenols, sometimes called phenolics, are a class of chemical compounds consisting of one or more hydroxyl groups (— O H) bonded directly to an aromatic hydrocarbon group. The simplest is phenol, . Phenolic compounds are classified as simple phenols or polyphenols based on the number of phenol units in the molecule. Phenols are both synthesized industrially and produced by plants and microorganisms. Properties Acidity Phenols are more acidic than typical alcohols. The acidity of the hydroxyl group in phenols is commonly intermediate between that of aliphatic alcohols and carboxylic acids (their pKa is usually between 10 and 12). Deprotonation of a phenol forms a corresponding negative phenolate ion or phenoxide ion, and the corresponding salts are called phenolates or phenoxides (aryloxides according to the IUPAC Gold Book). Condensation with aldehydes and ketones Phenols are susceptible to Electrophilic aromatic substitutions. Condensation with formald ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
List Of Fentanyl Analogues
This is a list of fentanyl analogues (sometimes referred to as Fentalogs), including both compounds developed by pharmaceutical companies for legitimate medical use, and those which have been sold as designer drugs and reported to national drug control agencies such as the DEA, or transnational agencies such as the EMCDDA and UNODC. This is not a comprehensive listing of fentanyl analogues, as more than 1400 compounds from this family have been described in the scientific and patent literature, but it includes all notable compounds that have reached late-stage human clinical trials, or which have been identified as having been sold as designer drugs, as well as representative examples of significant structural variations reported in the scientific and patent literature. In the United States, the Drug Enforcement Administration placed the broadly defined class of "Fentanyl-Related Substances" on the list of Schedule I drugs in 2018, making it illegal to manufacture, distribute, or p ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Carfentanil
Carfentanil or carfentanyl, sold under the brand name Wildnil, is a very potent opioid analgesic which is used in veterinary medicine to anesthetize large animals such as elephants and rhinoceroses. It is typically administered in this context by tranquilizer dart. Carfentanil has also been used in humans for imaging of opioid receptors. It has additionally been used as a recreational drug, typically by injection, insufflation, or inhalation. Deaths have been reported in association with carfentanil. Effects and side effects of carfentanil in humans are similar to those of other opioids and include euphoria, relaxation, pain relief, pupil constriction, drowsiness, sedation, slowed heart rate, low blood pressure, lowered body temperature, loss of consciousness, and suppression of breathing. The effects of carfentanil, including overdose, can be reversed by the opioid antagonists naloxone and naltrexone, though higher or multiple doses than usual may be necessary compared ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
