Hydromorphone , also known as dihydromorphinone , and sold under the trademark Dilaudid , among other things, is a centrally acting painkiller of the opioid class. It's made of morphine. Relatively, hydromorphone is a morphine like hydrocodone is codeine - it is a hydrogenated ketone thereof. In medical terms, it is opioid analgesics, and in legal terms, narcotics. Hydromorphone is commonly used in hospital settings, mostly intravenous (IV) due to its very low oral, rectal, and intranasal bioavailability. Sublingual administration (under the tongue) is usually superior to swallowing for bioavailability and effects; However, the hydromorphone is bitter and hydrophilic like most opiates, not lipophilic, so it is absorbed poorly and slowly through the mouth membrane.
Hydromorphone is much more soluble in water than morphine and, therefore, a hydromorfon solution can be produced to transmit the drug in a smaller volume of water. The salt of hydrochloride dissolves in three parts water, while one gram of soluble morphine hydrochloride in 16 ml of water; for all general purposes, pure powder for hospital use can be used to produce an almost random concentration solution. When the powder has appeared on the road, this very small powder volume is required for doses which means that an overdose is possible for those who think it is for heroin or other powdered narcotics, especially those that have been cut (diluted) before consumption.
A small amount of hydromorphone is detected in opium tests on rare occasions; apparently manufactured by the factory in a state and by a process that is not understood at this time. Similar processes or other metabolic processes at the plant may be particularly responsible for very low amounts of hydrocodones also found on rare occasions in opium and opium-derived alkaloid mixtures. Dihydrocodeine, oxymorphol, oxycodone, oxymorphone, metopon, and possibly other morphine and hydromorphon derivatives are also found in small amounts in opium.
Video Hydromorphone
Side effects
The adverse effects of hydromorphone are similar to other opioid analgesic effects, such as morphine and heroin. The major hazards of hydromorphism include respiratory-related respiratory depression, urinary retention, bronchospasm, and occasionally circulatory depression. More common side effects include dizziness, dizziness, sedation, itching, constipation, nausea, vomiting, headache, perspiration, and hallucinations. These symptoms often occur in outpatients and in those without severe pain.
Simultaneous use of hydromorphone with other opioids, muscle relaxants, tranquilizers, sedatives, and general anesthesia can lead to a significant increase in respiratory depression, progressing into coma or death. Taking benzodiazepines (such as diazepam) in conjunction with hydromorphone can increase side effects such as dizziness and difficulty concentrating. If simultaneous use of these drugs is necessary, dose adjustments may be made.
A particular problem that may occur with hydromorphone is the unintended administration of morphine instead of a mixture of similar names, either at the time the prescription is written or when the drug is removed. This has caused some deaths and calls for hydromorphone to be distributed in different packages of morphine to avoid confusion.
Major overdose is rarely observed in opioid-tolerant individuals, but when they occur they can cause the circulatory system to collapse. Symptoms of overdose include respiratory depression, drowsiness that causes coma and sometimes to death, skeletal muscle decreases, low heart rate and decreased blood pressure. In hospitals, individuals with hydromorphone overdoses provided supportive care such as ventilation assistance to provide oxygen, bowel decontamination using activated charcoal through nasogastric tubes. Opioid antagonists such as naloxone can also be administered together with oxygen supplementation. Naloxone works by reversing the hydromorphone effect. This is given only in the presence of significant respiratory depression and circulatory depression.
The effects of overdose may be exacerbated by a dumping dose if the drug is taken with alcohol.
Sugar cravings associated with hydromorphone use are the result of glucose breakdown after transient hyperglycemia after injection or decreased blood sugar for several hours, similar to morphine, heroin, codeine, and other opiates.
Hormone imbalance
Like other opioids, hydromorphone (especially during heavy chronic use) often leads to hypogonadism or temporary hormone imbalance.
Neurotoxicity
In prolonged use settings, high doses, and/or renal dysfunction, hydromorphone has been associated with neuroexcitatory symptoms such as tremor, myoclonus, agitation, and cognitive dysfunction. This toxicity is less than that associated with other opioid classes such as the pethidine synthetic class in particular.
Withdrawal
Hydromorphone users may experience pain symptoms if the drug is suspended. Some people can not tolerate the symptoms that cause continuous drug use. Opioid withdrawal symptoms are not easily described. There is a difference between drug search behavior and actual withdrawal effects. Symptoms associated with hydromorphone withdrawal include:
- Abdominal pain
- Anxiety/panic attacks
- Depression
- Crooked swanskin
- Inability to enjoy daily activity
- Muscle and joint pain
- Nausea
- A runny nose and excessive tear secretions
- Sweating
- Vomit
In clinical settings, excessive tear secretion, yawning and pupillary dilation help presentations in diagnosing opioid withdrawal. Hydromorphone is a fast pain killer, but some formulations can last up to several hours; patients who stop taking this drug may suddenly experience withdrawal symptoms. It can start within hours after taking the last dose of hydromorphone and can last up to several weeks. Withdrawal symptoms in people who stop using opioids can be managed using opioids or non-opioid additives. Methadone is an opioid commonly used for this kind of therapy. However, the selection of therapy should be tailored for each particular person. Methadone is also used for detoxification in people who are addicted to opioids such as heroin or drugs similar to morphine. It can be given orally or intramuscularly. There is controversy over the use of opioids for people with withdrawal symptoms because these agents can cause relapse in patients when they suspend therapy. Clonidine is a non-opioid addition that can be used in situations where the use of opioids is undesirable, as in patients with high blood pressure.
Maps Hydromorphone
Interactions
CNS depressants can increase the depressant effect of hydromorphone, such as other opioids, anesthesia, sedatives, hypnotics, barbiturates, benzodiazepines, phenothiazines, chloral hydrates, dimenhydrinates, and glutethimide. The effects of depressant hydromorphon can also be enhanced by monoamine oxidase inhibitors (MAO inhibitors) (including procarbazine), first generation antihistamines (brompheniramine, promethazine, diphenhydramine, chlorphenamine), beta blockers, and alcohols. When combined therapy is contemplated, the dosage should be reduced from one or both agents.
Pharmacology
Hydromorphone is a semi-synthetic agonist? -opioid. As the hydrogenated ketone of morphine, it shares the pharmacological properties typical of opioid analgesics. Hydromorfone and associated opioids produce major effects on the central nervous system and gastrointestinal tract. These include analgesia, drowsiness, mental shrinking, mood swings, euphoria or dysphoria, respiratory depression, cough suppress, decreased gastrointestinal motility, nausea, vomiting, increased cerebrospinal fluid pressure, increased biliary pressure, and increased pupillary constriction in the pupil.
Formulation
Hydromorphone is available in parenteral, rectal, subcutaneous, and oral formulations. This can also be given by epidural or intrathecal injection. Hydromorphone has also been administered through nebulation to treat shortness of breath, but it is not used as a route to controlling pain due to low bioavailability.
The concentrated hydromorphic hydrochloride solution has a different refractive index of pure water, isotonic 9? (0 Ã, Â · 9 percent) of salt and the like and especially when stored in ampoules and clear phials can obtain a slight amber color when exposed to light; this is reported to have no effect on potential solutions, but 14-dihydromorphinones such as hydromorphone, oxymorphone and relatives come with instructions to protect from light. Ampoule of the solution which has undergone the precipitate must be discarded.
Battery-powered intrathecal drug delivery systems are implanted for chronic pain when other options are ruled out, such as traditional surgery and pharmacotherapy, provided the patient is considered suitable in terms of contraindications, both physiological and psychological.
Extended hydromorphone versions (once a day) are available in the United States. Previously, the extended-release hydromorphone version, Palladone, was available before being voluntarily withdrawn from the market after the FDA's advisory in July 2005 warned of a high potential for overdose when taken with alcohol. As of March 2010, it is still available in the United Kingdom under the brand name Palladone SR, Nepal under the brand name Opidol, and in most other European countries.
Pharmacokinetics
The chemical modification of the morphine molecules into hydromorphone results in higher lipid solubility and greater ability to cross the blood-brain barrier to produce faster and more complete penetration of the central nervous system. On a per milligram basis, hydromorphone is considered five times stronger than morphine; although the conversion rate may vary from 4-8 times, five times in typical clinical use. The development of tolerance can also vary among individuals.
Patients with kidney disorders should be cautious when administering doses of hydromorphone. In those with renal impairment, the half-life of hydromorphone may increase up to 40 hours. Common half-life of intravenous hydromorphism is 2.3 hours. Peak plasma levels usually occur between 30 and 60 minutes after oral dosing.
The action onset for intravenously administered hydromorphone is less than 5 minutes and within 30 minutes of oral administration (immediately excreted).
Metabolism
While other opioids in the classroom such as codeine or oxycodone are metabolized through the CYP450 enzyme, no hydromorphone. Hydromorphone is extensively metabolized in the liver into hydromorphone-3-glucoronide, which has no analgesic effect. As also seen in morphine metabolites, morphine-3-glucoronide, the buildup in hydromorfone-3-glucoronide levels can produce neurotoxic effects of excitability such as anxiety, myoclonus and hyperalgesia. Patients with impaired renal function and older patients have a higher risk for metabolite accumulation.
Chemistry
Hydromorphone is made of either morphine by direct resetting (made by heating the reflux of an aqueous solution or a morphine aqueous acid in the presence of a platinum or palladium catalyst) or reduction to dihydromorphine (usually by catalytic hydrogenation), followed by oxidation with benzophenone in the presence of potassium tert-butoxide or aluminum tert-butoxide (Oppenauer oxidation). The six groups of ketones can be replaced with methylene groups via Wittig's reaction to produce 6-Methyleneihdrodrodoksonethorphine, which is stronger than morphine.
Turning morphine into hydromorphone increases its activity and, therefore, makes the hydromorphone about eight times stronger than weight-based morphine, all other things being equal. Changed also is lipid solubility, contributing to hydromorphone has a faster onset of action and changes in overall absorption, distribution, metabolism, and elimination profiles and side effect profile (in general, less nausea and itching) compared with morphine. A semi-synthetic opiate, in which hydromorphone and its analogine hydroxide are the most famous and the oldest, including a large number of drugs of varying strength and with their own subtle and cruel differences, allowing many different options for treatment.
Endogenous production
Hydromorphone is made of morphine through catalytic hydrogenation and is also produced in small quantities by the metabolism of human mammals and other mammals and sometimes appears in very small amounts of latex opium tests, apparently formed in factories in an unknown percentage of cases under the less understood conditions.
Bacteria
Some bacteria have been shown to be able to convert morphine into a closely related drug including hydromorphone and dihydromorphine among others. Bacteria Pseudomonas putida serotype M10 produces NADH dependent morphinone reductase which can work on unsaturated 7.8 bonds, with the result that, when these bacteria live in an aqueous solution containing morphine, a significant amount. form of hydromorphone, because it is an intermediate metabolite in this process; the same applies to the codeine converted to hydrocodone.
This process gives rise to various concentrations of hydromorphon, dihydromorphine, hydromorphinol, and oxymorel during the experiment. Three paths are found: from morphine to hydromorphon with dihydromorphine as the second step from the back, from morphine to hydromorphone with morphone as the second step from the back, and from morphine to hydromorphinol to hydromorphone.
History
Hydromorphone was first synthesized and researched in Germany by Knoll (first patent 1922) which introduced it to the mass market in 1926 under the brand name Dilaudid, showing its derivation and similarity with morphine (via laudanum) - compare Dicodid ( hydrocodone), Dihydrin (dihydrocodeine), and Dinarkon (oxycodone). The brand name Dilaudid is more widely known than the general term hydromorphone and, because of this, Dilaudid is commonly used to mean any form of hydromorphone.
Society and culture
Name
Hydromorphone is well known in many countries around the world under the brand name Hydal, Dimorphone, LP Sophidone, Dilaudid, Hydrostat, Hydromorphan, Hydromorphan, Hymorphan, Laudicon, Opidol, Palladone, Hydromorph Contin and others. An extended-release version of the hydromorphone called Palladone is available for a short time in the United States before being voluntarily withdrawn from the market after the FDA advisors in July 2005 warned of a high potential for overdose when taken with alcohol. As of March 2010, it is still available in the United Kingdom under the brand name Palladone SR, Nepal under the brand name Opidol, and in most other European countries.
There is an extended (once daily) Hydromorphone version available (in the United States).
Legal status
In the United States, the main drug regulatory agency, Drug Enforcement Administration, reported an increase in annual aggregate production quota of hydromorphone from 766 kilograms (1,689 lbs) in 1998 to 3,300 kilograms (7.300 pounds) in 2006, and a current prescription increase of 289% about 470,000 to 1,830,000. The production quota of 2013 is 5,968 kilograms (13,157 pounds).
Like all opioids used for analgesia, hydromorphones have the potential to form habits and are listed in Schedule II of the United States Controlled Control Act of 1970 and the same level under the drug laws of virtually all other countries and are registered under the Single Drug Narcotics Convention. DEA ACSCN for hydromorphone is 9150.
Hydromorphone is listed under the German BetÃÆ'¤ubungsmittelgesetz as Suchtgift in the most limited schedule for drugs; it is also controlled in Austria under SMG and Swiss BetmG. Abuse of the Drug Act 1971 (UK) and France, Canada, Australia, Italy, Czech, Croatia, Slovenia, Sweden, Poland, Spain, Greece, Russia, and other laws also control it, as practiced in almost all other countries.
Use in execution
In 2009, Ohio approved the use of intramuscular injection of 500 mg of hydromorphone and supratherapeutic dose of midazolam as a backup means to execute when a suitable vein could not be found for intravenous injection.
Hydromorphone and midazolam were injected intravenously to execute Joseph Wood's double killer in Arizona on July 24, 2014. Wood was deeply anestrated ( surgical anasthesia ) within four minutes from the beginning but it took almost two hours to transition to stage 4 ( cessation of respiration) and death.
References
External links
- Consumer drug information Hydromorphone Drugs.com.
- Exalgo: full recipe information
- An article that discusses the release of long release hydromorphone from the US market
- painCare.ca and Patient Information on Opioid Analgesics (limited access to professionals)
- Dihydromorphinones from morphine & amp; analog
- US DEA Perspective, including statistics on production and prescription levels from 1998 to 2006
- "When did a sick doctor become a medicinal agent?", The New York Times , 17 Jun 2007
Source of the article : Wikipedia
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