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91-424: Heroin , also known as diacetylmorphine and diamorphine among other names, is a morphinan opioid substance synthesized from the dried latex of the opium poppy ; it is mainly used as a recreational drug for its euphoric effects. Heroin is used medically in several countries to relieve pain , such as during childbirth or a heart attack, as well as in opioid replacement therapy . Medical-grade diamorphine

182-400: A maintenance drug to assist the treatment of opiate addiction, normally in long-term chronic intravenous (IV) heroin users. It is only prescribed following exhaustive efforts at treatment via other means. It is sometimes thought that heroin users can walk into a clinic and walk out with a prescription, but the process takes many weeks before a prescription for diamorphine is issued. Though this

273-452: A methylene group via the Wittig reaction to produce 6-Methylenedihydrodesoxymorphine , which is 80× stronger than morphine. Changing morphine into hydromorphone increases its activity and, therefore, makes hydromorphone approximately eight times stronger than morphine on a weight basis, all other things being equal. Changed also is lipid solubility, contributing to hydromorphone's having

364-493: A phenanthrene core structure with the A ring remaining aromatic and the B and C rings being saturated, and an additional nitrogen-containing, six-membered, saturated ring, the D ring, being attached to carbons 9 and 13 of the core, and with the nitrogen being at position 17 of the composite. Of the major naturally occurring opiates of the morphinan type— morphine , codeine and thebaine —thebaine has no therapeutic properties (it causes seizures in mammals), but it provides

455-486: A prodrug for the systemic delivery of morphine. When the drug is injected, however, it avoids this first-pass effect, very rapidly crossing the blood–brain barrier because of the presence of the acetyl groups, which render it much more fat soluble than morphine itself. Once in the brain, it then is deacetylated variously into the inactive 3-monoacetylmorphine and the active 6-monoacetylmorphine (6-MAM), and then to morphine, which bind to μ-opioid receptors , resulting in

546-408: A rush as a forerunner to the high experienced with the use of heroin, which is most pronounced with intravenous use. While the onset of the rush induced by injection can occur in as little as a few seconds, the oral route of administration requires approximately half an hour before the high sets in. Thus, with both higher the dosage of heroin used and faster the route of administration used, the higher

637-603: A vein , but it can also be snorted, smoked, or inhaled. In a clinical context, the route of administration is most commonly intravenous injection ; it may also be given by intramuscular or subcutaneous injection, as well as orally in the form of tablets. The onset of effects is usually rapid and lasts for a few hours. Common side effects include respiratory depression (decreased breathing), dry mouth, drowsiness, impaired mental function, constipation, and addiction . Use by injection can also result in abscesses , infected heart valves , blood-borne infections , and pneumonia . After

728-428: A build-up in levels of hydromorphone-3-glucuronide may produce excitatory neurotoxic effects such as restlessness, myoclonus and hyperalgesia . Patients with compromised kidney function and older patients are at higher risk for metabolite accumulation. With a formula of C 17 H 19 NO 3 and a molecular weight of 285.343, both identical to morphine, hydromorphone can be considered a structural isomer of morphine and

819-474: A fast onset. Snorting heroin becomes an often unwanted route, once a user begins to inject the drug. The user may still get high on the drug from snorting, and experience a nod, but will not get a rush. A "rush" is caused by a large amount of heroin entering the body at once. When the drug is taken in through the nose, the user does not get the rush because the drug is absorbed slowly rather than instantly. Heroin for pain has been mixed with sterile water on site by

910-537: A few addicts who have tried methadone and buprenorphine without success. Beginning in February 2010, addicts in Copenhagen and Odense became eligible to receive free diamorphine. Later in 2010, other cities including Århus and Esbjerg joined the scheme. It was estimated that around 230 addicts would be able to receive free diamorphine. However, Danish addicts would only be able to inject heroin according to

1001-553: A history of long-term use, opioid withdrawal symptoms can begin within hours of the last use. When given by injection into a vein, heroin has two to three times the effect of a similar dose of morphine . It typically appears in the form of a white or brown powder. Treatment of heroin addiction often includes behavioral therapy and medications. Medications can include buprenorphine , methadone , or naltrexone . A heroin overdose may be treated with naloxone . As of 2015, an estimated 17 million people use opiates, of which heroin

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1092-468: A law allowing diamorphine prescription as a standard treatment for addicts; a large-scale trial of diamorphine prescription had been authorized in the country in 2002. On 26 August 2016, Health Canada issued regulations amending prior regulations it had issued under the Controlled Drugs and Substances Act ; the "New Classes of Practitioners Regulations", the "Narcotic Control Regulations", and

1183-399: A low-cost feedstock for the industrial production of at least four semi-synthetic opiate agonists, including hydrocodone , hydromorphone , oxycodone and oxymorphone , and the opioid antagonist naloxone . The physiological behavior of morphinans (naturally occurring and semi-synthetic derivatives) is thought to be associated with the aromatic A ring, the nitrogen-containing D ring and

1274-589: A mix-up between the similar names, either at the time the prescription is written or when the drug is dispensed. This has led to several deaths and calls for hydromorphone to be distributed in distinctly different packaging from morphine to avoid confusion. Massive overdoses are rarely observed in opioid-tolerant individuals, but when they occur, they may lead to circulatory system collapse. Symptoms of overdose include respiratory depression, drowsiness leading to coma and sometimes to death, drooping of skeletal muscles, low heart rate , and decreasing blood pressure . At

1365-606: A more common cause of drug-related deaths. Depending on drug interactions and numerous other factors, death from overdose can take anywhere from several minutes to several hours. Death usually occurs due to lack of oxygen resulting from the lack of breathing caused by the opioid. Heroin overdoses can occur because of an unexpected increase in the dose or purity or because of diminished opioid tolerance. However, many fatalities reported as overdoses are probably caused by interactions with other depressant drugs such as alcohol or benzodiazepines . Since heroin can cause nausea and vomiting,

1456-526: A more rapid onset of action and alterations to the overall absorption, distribution, metabolism, and elimination profile as well as the side effect profile (in general, less nausea and itching) versus that of morphine. The semi-synthetic opiates, of which hydromorphone and its codeine analogue hydrocodone are among the best-known and oldest, include a huge number of drugs of varying strengths and with differences among themselves both subtle and stark, allowing for many different options for treatment. Hydromorphone

1547-570: A natural product of the opium poppy . Internationally, heroin is controlled under Schedules I and IV of the Single Convention on Narcotic Drugs , and it is generally illegal to make, possess, or sell without a license. About 448 tons of heroin were made in 2016. In 2015, Afghanistan produced about 66% of the world's opium. Illegal heroin is often mixed with other substances such as sugar, starch , caffeine , quinine , or other opioids like fentanyl . Bayer 's original trade name of heroin

1638-498: A period of abstinence. If this occurs and the user takes a dose comparable to their previous use, the user may experience drug effects that are much greater than expected, potentially resulting in an overdose. It has been speculated that an unknown portion of heroin-related deaths are the result of an overdose or allergic reaction to quinine , which may sometimes be used as a cutting agent. When taken orally, heroin undergoes extensive first-pass metabolism via deacetylation , making it

1729-406: A precipitate should be discarded. Battery-powered intrathecal drug delivery systems are implanted for chronic pain when other options are ruled out, such as surgery and traditional pharmacotherapy, provided that the patient is considered a suitable fit in terms of any contraindications, both physiological and psychological. An extended-release (once-daily) version of hydromorphone is available in

1820-498: A pure opioid antagonist (i.e., it is also a weak opioid agonist), so naloxone remains a significant therapeutic tool in suspected cases of opioid overdose. See also Bentley compounds . If the D ring is "below" the core ( dextrorotatory ), the analgesic and euphoric properties are eliminated or are dramatically reduced, but the cough-suppressant property is retained, as in dextromethorphan . Immediate derivatives of morphinan include: More distant of derivatives include: As well as

1911-426: A significant increase in respiratory depression, progressing to coma or death. Taking benzodiazepines (e.g., diazepam ) in conjunction with hydromorphone may increase side effects such as dizziness and difficulty concentrating. If simultaneous use of these drugs is required, dose adjustment may be made. A particular problem that may occur with hydromorphone is accidental administration in place of morphine due to

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2002-481: A significant number of deaths attributed to heroin overdose are caused by aspiration of vomit by an unconscious person. Some sources quote the median lethal dose (for an average 75 kg opiate-naive individual) as being between 75 and 600 mg. Illicit heroin is of widely varying and unpredictable purity. This means that the user may prepare what they consider to be a moderate dose while actually taking far more than intended. Also, tolerance typically decreases after

2093-471: A trial diamorphine maintenance program for users that had failed multiple withdrawal programs. The aim of this program was to maintain the health of the user by avoiding medical problems stemming from the illicit use of diamorphine. The first trial in 1994 involved 340 users, although enrollment was later expanded to 1000, based on the apparent success of the program. The trials proved diamorphine maintenance to be superior to other forms of treatment in improving

2184-402: A variable single dose range using a hypodermic needle . The dose of heroin used for recreational purposes is dependent on the frequency and level of use. As with the injection of any drug, if a group of users share a common needle without sterilization procedures, blood-borne diseases, such as HIV/AIDS or hepatitis , can be transmitted. The use of a common dispenser for water for the use in

2275-454: A visibly different refractive index from pure water, isotonic 9‰ (0·9 per cent) saline and the like, especially when stored in clear ampoules and phials may acquire a slight clear amber discolouration upon exposure to light; this reportedly has no effect on the potency of the solution, but 14-dihydromorphinones such as hydromorphone, oxymorphone , and relatives come with instructions to protect from light. Ampoules of solution which have developed

2366-485: Is a hydrogenated ketone thereof. Hydromorphone is made from morphine either by direct re-arrangement (made by reflux heating of alcoholic or acidic aqueous solution of morphine in the presence of platinum or palladium catalyst) or reduction to dihydromorphine (usually via catalytic hydrogenation ), followed by oxidation with benzophenone in presence of potassium tert butoxide or aluminium tert butoxide ( Oppenauer oxidation ). The 6 ketone group may be replaced with

2457-398: Is a rapid-acting painkiller; however, some formulations may last up to several hours. Patients who stop taking this drug abruptly may experience withdrawal symptoms, which may start within hours of taking the last dose of hydromorphone, and last up to several weeks. Withdrawal symptoms in people who stopped taking the opioid may be managed by using opioids or non-opioid adjuncts. Methadone

2548-402: Is an intermediary metabolite in this process; the same goes for codeine being turned into hydrocodone. The process gave rise to various concentrations of hydromorphone, dihydromorphine, hydromorphinol , and oxymorphone during the experiments. Three paths were found: from morphine to hydromorphone with dihydromorphine as the penultimate step, from morphine to hydromorphone with morphinone as

2639-491: Is an opioid commonly used for this kind of therapy. However, the selection of therapy should be tailored to each specific person. Methadone also is used for detoxification in people who have opiate addiction, such as heroin or drugs similar to morphine. It may be given orally or intramuscularly. There is controversy regarding whether any opioid (such as methadone) should be included in the treatment of opioid withdrawal symptoms, since these agents also may cause relapse when therapy

2730-453: Is available as both brand name (Hydro­morph Contin) and generic formu­lations (Apo-Hydro­morphone CR). The chemical modification of the morphine molecule to hydromorphone results in higher lipid solubility and greater ability to cross the blood–brain barrier to produce more rapid and complete central nervous system penetration. On a per milligram basis, hydromorphone is considered to be five times as potent as morphine; although

2821-464: Is clouded; heart function slows, and breathing is also severely slowed, sometimes enough to be life-threatening. Slowed breathing can also lead to coma and permanent brain damage . Heroin use has also been associated with myocardial infarction . Repeated heroin use changes the physical structure and physiology of the brain, creating long-term imbalances in neuronal and hormonal systems that are not easily reversed. Studies have shown some deterioration of

Heroin - Misplaced Pages Continue

2912-665: Is contemplated, the dose of one or both agents should be reduced. Hydromorphone is a semi-synthetic μ-opioid agonist . As a hydrogenated ketone of morphine, it shares the pharmacologic properties typical of opioid analgesics . Hydromorphone and related opioids produce their major effects on the central nervous system and gastrointestinal tract . These include analgesia , drowsiness, mental clouding, changes in mood, euphoria or dysphoria , respiratory depression, cough suppression, decreased gastrointestinal motility, nausea, vomiting, increased cerebrospinal fluid pressure, increased biliary pressure , and increased pinpoint constriction of

3003-414: Is heated by a flame underneath it, with the resulting smoke inhaled through a tube of rolled up foil, a method also known as " chasing the dragon ". Another popular route to intake heroin is insufflation (snorting), where a user crushes the heroin into a fine powder and then gently inhales it (sometimes with a straw or a rolled-up banknote , as with cocaine) into the nose, where heroin is absorbed through

3094-417: Is higher than expected. Users report an intense rush , an acute transcendent state of euphoria , which occurs while diamorphine is being metabolized into 6-monoacetylmorphine (6-MAM) and morphine in the brain. Some believe that heroin produces more euphoria than other opioids; one possible explanation is the presence of 6-monoacetylmorphine, a metabolite unique to heroin – although a more likely explanation

3185-497: Is less common than other methods of administration, mainly because there is little to no "rush", and the effects are less potent. Heroin is entirely converted to morphine by means of first-pass metabolism , resulting in deacetylation when ingested. Heroin's oral bioavailability is both dose-dependent (as is morphine's) and significantly higher than oral use of morphine itself, reaching up to 64.2% for high doses and 45.6% for low doses; opiate-naive users showed far less absorption of

3276-406: Is less than 5 minutes and within 30 minutes of oral administration (immediate release). While other opioids in its class, such as codeine or oxycodone, are metabolized via CYP450 enzymes, hydromorphone is not. Hydromorphone is extensively metabolized in the liver to hydromorphone-3-glucuronide, which has no analgesic effects. As similarly seen with the morphine metabolite, morphine-3-glucuronide,

3367-744: Is listed under the German Betäubungsmittelgesetz as a Betäubungsmittel in the most restricted schedule for medicinal drugs; it is controlled similarly in Austria (Suchtgift) under the SMG and the Swiss BetmG. The Misuse of Drugs Act 1971 (United Kingdom) and comparable French, Canadian, Australian, Italian, Czech, Croatian, Slovenian, Swedish, Polish, Spanish, Greek, Russian, and other laws similarly control it, as do regulations in virtually all other countries. In 2009, Ohio approved

3458-404: Is more fat soluble and therefore more potent by injection, so smaller doses of it are needed for the same effect on pain. Both of these factors are advantageous if giving high doses of opioids via the subcutaneous route, which is often necessary for palliative care. It is also used in the palliative management of bone fractures and other trauma, especially in children. In the trauma context, it

3549-699: Is more common to use morphine or other strong opioids in these situations. In 2004, the National Institute for Health and Clinical Excellence produced guidance on the management of caesarean section , which recommended the use of intrathecal or epidural diamorphine for post-operative pain relief . For women who have had intrathecal opioids, there should be a minimum hourly observation of respiratory rate, sedation and pain scores for at least 12 hours for diamorphine and 24 hours for morphine. Women should be offered diamorphine (0.3–0.4 mg intrathecally) for intra- and postoperative analgesia because it reduces

3640-408: Is more soluble in water than morphine; therefore, hydromorphone solutions may be produced to deliver the drug in a smaller volume of water. The hydrochloride salt is soluble in three parts of water, whereas a gram of morphine hydrochloride dissolves in 16 ml of water; for all common purposes, the pure powder for hospital use can be used to produce solutions of virtually arbitrary concentration. When

3731-414: Is primarily given by nose in hospital; although a prepared nasal spray is available. It has traditionally been made by the attending physician, generally from the same "dry" ampoules as used for injection. In children, Ayendi nasal spray is available at 720 micrograms and 1600 micrograms per 50 microlitres actuation of the spray, which may be preferable as a non-invasive alternative in pediatric care, avoiding

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3822-543: Is reduced abruptly. Intravenous use of heroin (and any other substance) with needles and syringes or other related equipment may lead to: The withdrawal syndrome from heroin may begin within as little as two hours of discontinuation of the drug; however, this time frame can fluctuate with the degree of tolerance as well as the amount of the last consumed dose, and more typically begins within 6–24 hours after cessation. Symptoms may include sweating , malaise , anxiety, depression, akathisia , priapism , extra sensitivity of

3913-515: Is somewhat controversial among proponents of a zero-tolerance drug policy , it has proven superior to methadone in improving the social and health situations of addicts. The UK Department of Health's Rolleston Committee Report in 1926 established the British approach to diamorphine prescription to users, which was maintained for the next 40 years: dealers were prosecuted, but doctors could prescribe diamorphine to users when withdrawing. In 1964,

4004-693: Is suspended. Clonidine is a non-opioid adjunct which may be used in situations where opioid use is not desired, such as in patients with high blood pressure . CNS depressants may enhance the depressant effects of hydromorphone, such as other opioids , anesthetics , sedatives , hypnotics , barbiturates , benzodiazepines , phenothiazines , chloral hydrate , dimenhydrinate , and glutethimide . The depressant effect of hydromorphone also may be enhanced by monoamine oxidase inhibitors (MAO inhibitors), first-generation antihistamines (e.g., brompheniramine , promethazine , diphenhydramine , chlorphenamine ), beta blockers , and alcohol . When combined therapy

4095-623: Is the most common, and opioid use resulted in 122,000 deaths; also, as of 2015, the total number of heroin users worldwide is believed to have increased in Africa, the Americas, and Asia since 2000. In the United States, approximately 1.6 percent of people have used heroin at some point. When people die from overdosing on a drug, the drug is usually an opioid and often heroin. Heroin was first made by C. R. Alder Wright in 1874 from morphine,

4186-410: Is the rapidity of onset. While other opioids of recreational use produce only morphine, heroin also leaves 6-MAM, also a psycho- active metabolite . However, this perception is not supported by the results of clinical studies comparing the physiological and subjective effects of injected heroin and morphine in individuals formerly addicted to opioids; these subjects showed no preference for one drug over

4277-448: Is typically used in non-medical settings. It is used as a recreational drug for the euphoria it induces. Anthropologist Michael Agar once described heroin as "the perfect whatever drug." Tolerance develops quickly, and increased doses are needed in order to achieve the same effects. Its popularity with recreational drug users, compared to morphine , reportedly stems from its perceived different effects. Short-term addiction studies by

4368-413: Is used as a pure hydrochloride salt . Various white and brown powders sold illegally around the world as heroin are routinely diluted with cutting agents . Black tar heroin is a variable admixture of morphine derivatives—predominantly 6-MAM (6-monoacetylmorphine), which is the result of crude acetylation during clandestine production of street heroin. Heroin is typically injected , usually into

4459-516: The Brain Committee recommended that only selected approved doctors working at approved specialized centres be allowed to prescribe diamorphine and cocaine to users. The law was made more restrictive in 1968. Beginning in the 1970s, the emphasis shifted to abstinence and the use of methadone; currently, only a small number of users in the UK are prescribed diamorphine. In 1994, Switzerland began

4550-399: The C ring, may increase potency 1,000 to 10,000 times, or greater, compared to morphine, as in etorphine , and others. The relative potency is thought to be associated with the degree of distortion of the C ring, and is perhaps greatest in diprenorphine , where this group is α,α-dimethyl-6,14-etheno. Diprenorphine (M5050) is the recommended etorphine (M99) antagonist, but it is not

4641-647: The United States , heroin is not accepted as medically useful. Under the generic name diamorphine, heroin is prescribed as a strong pain medication in the United Kingdom , where it is administered via oral , subcutaneous , intramuscular , intrathecal , intranasal or intravenous routes. It may be prescribed for the treatment of acute pain, such as in severe physical trauma , myocardial infarction , post- surgical pain and chronic pain , including end-stage terminal illnesses . In other countries it

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4732-1009: The World Health Organization's List of Essential Medicines . It is available as a generic medication . In 2021, it was the 261st most commonly prescribed medication in the United States, with more than 1   million prescriptions. Adverse effects of hydromorphone are similar to those of other potent opioid analgesics such as morphine and heroin . The major hazards of hydromorphone include dose-related respiratory depression , urinary retention, bronchospasm, and sometimes, circulatory depression. More common side effects include lightheadedness , dizziness , sedation , itching , constipation , nausea , vomiting , headache , perspiration , and hallucinations . These symptoms are common in ambulatory patients and in those not experiencing severe pain. Simultaneous use of hydromorphone with other opioids, muscle relaxants , tranquilizers, sedatives , and general anesthetics may cause

4823-503: The east-coast United States is most commonly found in the hydrochloride salt form, requiring just water (and no heat) to dissolve. Users tend to initially inject in the easily accessible arm veins, but as these veins collapse over time, users resort to more dangerous areas of the body, such as the femoral vein in the groin. Some medical professionals have expressed concern over this route of administration, as they suspect that it can lead to deep vein thrombosis . Intravenous users can use

4914-421: The route of administration . Smoking is the fastest route of drug administration, although intravenous injection results in a quicker rise in blood concentration. These are followed by suppository (anal or vaginal insertion), insufflation (snorting), and ingestion (swallowing). A 2002 study suggests that a fast onset of action increases the reinforcing effects of addictive drugs. Ingestion does not produce

5005-664: The "Food and Drug Regulations", to allow doctors to prescribe diamorphine to people who have a severe opioid addiction who have not responded to other treatments. The prescription heroin can be accessed by doctors through Health Canada 's Special Access Programme (SAP) for "emergency access to drugs for patients with serious or life-threatening conditions when conventional treatments have failed, are unsuitable, or are unavailable." Medicinal uses: Neurological: Psychological: Cardiovascular & Respiratory: Gastrointestinal: Musculoskeletal: Skin: Miscellaneous: The onset of heroin's effects depends upon

5096-440: The "bridge" between these two rings formed by carbons 9, 10 and 11 of the core, with the D ring "above" the core ( levorotatory ). Small groups are usually found on morphinan derivatives at carbons 3 and 6. Many such derivatives have an epoxy group between carbons 4 and 5 (i.e., 4,5α-epoxy), thereby forming an E ring. The substitution of certain bulky groups on nitrogen 17 converts an opioid agonist into an opioid antagonist,

5187-450: The UK. Because significant tolerance to respiratory depression develops quickly with continued use and is lost just as quickly during withdrawal, it is often difficult to determine whether a heroin lethal overdose was accidental, suicide or homicide. Examples include the overdose deaths of Sid Vicious , Janis Joplin , Tim Buckley , Hillel Slovak , Layne Staley , Bradley Nowell , Ted Binion , and River Phoenix . Use of heroin by mouth

5278-555: The United States. Previously, an extended-release version of hydromorphone, Palladone, was available before being voluntarily withdrawn from the market after a July 2005 FDA advisory warned of a high overdose potential 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, In Canada, pre­scrip­tion continuous release hydro­morphone

5369-406: The anus or vagina before the plunger is pushed. The rectum or the vaginal canal is where the majority of the drug would likely be taken up, through the membranes lining their walls. Heroin is classified as a hard drug in terms of drug harmfulness . Like most opioids , unadulterated heroin may lead to adverse effects . The purity of street heroin varies greatly, leading to overdoses when the purity

5460-560: The attending physician, and administered using a syringe with a nebulizer tip. Heroin may be used for fractures, burns, finger-tip injuries, suturing, and wound re-dressing, but is inappropriate in head injuries. Little research has been focused on the suppository (anal insertion) or pessary (vaginal insertion) methods of administration, also known as "plugging". These methods of administration are commonly carried out using an oral syringe . Heroin can be dissolved and withdrawn into an oral syringe which may then be lubricated and inserted into

5551-437: The brain's white matter due to heroin use, which may affect decision-making abilities, the ability to regulate behavior, and responses to stressful situations. Heroin also produces profound degrees of tolerance and physical dependence. Tolerance occurs when more and more of the drug is required to achieve the same effects. With physical dependence , the body adapts to the presence of the drug , and withdrawal symptoms occur if use

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5642-493: The brand name Jurnista as of May 2009. In the United States, the main drug control agency, the Drug Enforcement Administration, reports an increase in annual aggregate production quotas of hydromorphone from 766 kilograms (1,689 pounds) in 1998 to 3,300 kilograms (7,300 lb) in 2006, and an increase in prescriptions in this time of 289%, from about 470,000 to 1,830,000. The 2013 production quota

5733-547: The conversion ratio may vary from 4–8 times, five times is in typical clinical usage. The development of tolerance also may vary among individuals. Patients with renal abnormalities must exercise caution when dosing hydromorphone. In those with renal impairment, the half-life of hydromorphone may increase to as much as 40 hours. The typical half-life of intravenous hydromorphone is 2.3 hours. Peak plasma levels usually occur between 30 and 60 minutes after oral dosing. The onset of action for hydromorphone administered intravenously

5824-401: The dose may result in opioid withdrawal . Generally, use during pregnancy or breastfeeding is not recommended. Hydromorphone is believed to work by activating opioid receptors , mainly in the brain and spinal cord. Hydromorphone 2 mg IV is equivalent to approximately 10 mg morphine IV. Hydromorphone was patented in 1923. Hydromorphone is made from morphine . It is on

5915-641: The drug at low doses, having bioavailabilities of only up to 22.9%. The maximum plasma concentration of morphine following oral administration of heroin was around twice as much as that of oral morphine. Injection , also known as "slamming", "banging", "shooting up", "digging" or "mainlining", is a popular method which carries relatively greater risks than other methods of administration. Heroin base (commonly found in Europe), when prepared for injection, will only dissolve in water when mixed with an acid (most commonly citric acid powder or lemon juice) and heated. Heroin in

6006-477: The drug is suspended. Some people cannot tolerate the symptoms, which results in continuous drug use. Symptoms of opioid withdrawal are not easy to decipher, as there are differences between drug-seeking behaviors and true withdrawal effects. Symptoms associated with hydromorphone withdrawal include: In the clinical setting, excessive secretion of tears, yawning , and dilation of pupils are helpful presentations in diagnosing opioid withdrawal. Hydromorphone

6097-436: The drug's euphoric, analgesic (pain relief), and anxiolytic (anti-anxiety) effects; heroin itself exhibits relatively low affinity for the μ receptor. Analgesia follows from the activation of the μ receptor G-protein coupled receptor , which indirectly hyperpolarizes the neuron, reducing the release of nociceptive neurotransmitters, and hence, causes analgesia and increased pain tolerance. Morphinan Morphinan has

6188-399: The effects of heroin and causes an immediate return of consciousness but may result in withdrawal symptoms. The half-life of naloxone is shorter than some opioids, such that it may need to be given multiple times until the opioid has been metabolized by the body. Between 2012 and 2015, heroin was the leading cause of drug-related deaths in the United States. Since then, fentanyl has been

6279-491: The fear of injection in children. A number of European countries prescribe heroin for treatment of heroin addiction . The initial Swiss HAT ( heroin-assisted treatment ) trial ("PROVE" study) was conducted as a prospective cohort study with some 1,000 participants in 18 treatment centers between 1994 and 1996, at the end of 2004, 1,200 patients were enrolled in HAT in 23 treatment centers across Switzerland. Diamorphine may be used as

6370-417: The following: The following structures are related to morphinan: Hydromorphone Hydromorphone , also known as dihydromorphinone , and sold under the brand name Dilaudid among others, is a morphinan opioid used to treat moderate to severe pain . Typically, long-term use is only recommended for pain due to cancer . It may be used by mouth or by injection into a vein , muscle , or under

6461-425: The genitals in females, general feeling of heaviness, excessive yawning or sneezing, rhinorrhea , insomnia , cold sweats, chills, severe muscle and bone aches, nausea, vomiting, diarrhea, cramps, watery eyes, fever, cramp-like pains, and involuntary spasms in the limbs (thought to be an origin of the term "kicking the habit"). Heroin overdose is usually treated with the opioid antagonist naloxone . This reverses

6552-404: The hospital, individuals with hydromorphone overdose are provided supportive care, such as assisted ventilation to provide oxygen and gut decontamination using activated charcoal through a nasogastric tube. Opioid antagonists , such as naloxone , also may be administered concurrently with oxygen supplementation. Naloxone works by reversing the effects of hydromorphone, and only is administered in

6643-482: The most important of which is naloxone , a non-selective opioid antagonist with no opioid agonist properties whatsoever ( "silent" antagonist ). Additionally, substitution of certain very bulky groups on carbon 6 converts naloxone into a peripherally-selective opioid antagonist with no centrally-selective antagonist properties ( naloxegol ). The addition of a two-carbon bridge between carbons 6 and 14 (e.g., 6,14-ethano, or 6,14-etheno), and which significantly distorts

6734-403: The need for supplemental analgesia after a caesarean section. Epidural diamorphine (2.5–5 mg) is a suitable alternative. Diamorphine continues to be widely used in palliative care in the UK, where it is commonly given by the subcutaneous route, often via a syringe driver if patients cannot easily swallow morphine solution . The advantage of diamorphine over morphine is that diamorphine

6825-461: The other. Equipotent injected doses had comparable action courses, with no difference in subjects' self-rated feelings of euphoria, ambition, nervousness, relaxation, drowsiness, or sleepiness. The rush is usually accompanied by a warm flushing of the skin, dry mouth, and a heavy feeling in the extremities. Nausea , vomiting , and severe itching may also occur. After the initial effects, users usually will be drowsy for several hours; mental function

6916-586: The penultimate step, and from morphine to hydromorphinol to hydromorphone. Hydromorphone was patented in 1923. It was introduced to the mass market in 1926 under the brand name Dilaudid , indicating its derivation and degree of similarity to morphine (by way of laudanum ). Hydromorphone is known in various countries around the world by the brand names Hydal, Dimorphone, Exalgo, Sophidone LP, Dilaudid, Hydrostat, Hydromorfan, Hydromorphan, Hymorphan, Laudicon, Opidol, Palladone, Hydromorph Contin, and others. An extended-release version of hydromorphone, called Palladone,

7007-525: The plant in an unknown percentage of cases under poorly understood conditions. Some bacteria have been shown to be able to turn morphine into closely related drugs, including hydromorphone and dihydromorphine among others. The bacterium Pseudomonas putida serotype M10 produces a naturally-occurring NADH-dependent morphinone reductase that can work on unsaturated 7,8 bonds, with result that, when these bacteria are living in an aqueous solution containing morphine, significant amounts of hydromorphone form, as it

7098-482: The policy set by Danish National Board of Health . Of the estimated 1500 drug users who did not benefit from the then-current oral substitution treatment, approximately 900 would not be in the target group for treatment with injectable diamorphine, either because of "massive multiple drug abuse of non-opioids" or "not wanting treatment with injectable diamorphine". In July 2009, the German Bundestag passed

7189-408: The potential risk for psychological dependence / addiction . Large doses of heroin can cause fatal respiratory depression, and the drug has been used for suicide or as a murder weapon. The serial killer Harold Shipman used diamorphine on his victims, and the subsequent Shipman Inquiry led to a tightening of the regulations surrounding the storage, prescribing and destruction of controlled drugs in

7280-502: The powder appeared on the street, this very small volume of powder needed for a dose means that overdoses are likely for those who mistake it for heroin or other powdered narcotics, especially those that have been diluted prior to consumption. Hydromorphone is made from morphine via catalytic hydrogenation and also is produced in trace amounts by human and other mammalian metabolisms of morphine. It occasionally appears in assays of opium latex in very small quantities, apparently forming in

7371-499: The preparation of the injection, as well as the sharing of spoons and filters can also cause the spread of blood-borne diseases. Many countries now supply small sterile spoons and filters for single use in order to prevent the spread of disease. Smoking heroin refers to vaporizing it to inhale the resulting fumes, rather than burning and inhaling the smoke. It is commonly smoked in glass pipes made from glassblown Pyrex tubes and light bulbs. Heroin may be smoked from aluminium foil that

7462-496: The presence of significant respiratory depression and circulatory depression. Sugar cravings associated with hydromorphone use are the result of a glucose crash after transient hyperglycemia following injection, or a less profound lowering of blood sugar over a period of hours, in common with morphine, heroin , codeine , and other opioids. As with other opioids, hydromorphone (particularly during heavy chronic use) often causes temporary hypogonadism or hormone imbalance . In

7553-506: The pupils. Hydromorphone is available in parenteral, rectal, subcutaneous, and oral formulations, and also can be administered via epidural or intrathecal injection. Hydromorphone also has been administered via nebulization to treat shortness of breath , but it is not used as a route for pain control due to low bioavailability . Transdermal delivery systems are also under consideration to induce local skin analgesia. Concentrated aqueous solutions of hydromorphone hydrochloride have

7644-520: The same researchers demonstrated that tolerance developed at a similar rate to both heroin and morphine. When compared to the opioids hydromorphone , fentanyl , oxycodone , and pethidine (meperidine), former addicts showed a strong preference for heroin and morphine, suggesting that heroin and morphine are particularly susceptible to misuse and causing dependence. Morphine and heroin were also much more likely to produce euphoria and other positive subjective effects when compared to these other opioids. In

7735-401: The setting of prolonged use, high dosage, and/or kidney 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 classes of opioids such as the pethidine class of synthetics in particular. Users of hydromorphone may experience painful symptoms if

7826-472: The skin . Effects generally begin within half an hour and last for up to five hours. A 2016 Cochrane review (updated in 2021) found little difference in benefit between hydromorphone and other opioids for cancer pain. Common side effects include dizziness , sleepiness , nausea , itchiness , and constipation . Serious side effects may include abuse , low blood pressure , seizures , respiratory depression , and serotonin syndrome . Rapidly decreasing

7917-442: The social and health situation for this group of patients. It has also been shown to save money, despite high treatment expenses, as it significantly reduces costs incurred by trials, incarceration, health interventions and delinquency . Patients appear twice daily at a treatment center, where they inject their dose of diamorphine under the supervision of medical staff. They are required to contribute about 450 Swiss francs per month to

8008-427: The soft tissue in the mucous membrane of the sinus cavity and straight into the bloodstream. This method of administration redirects first-pass metabolism , with a quicker onset and higher bioavailability than oral administration, though the duration of action is shortened. This method is sometimes preferred by users who do not want to prepare and administer heroin for injection or smoking but still want to experience

8099-682: The treatment costs. A national referendum in November 2008 showed 68% of voters supported the plan, introducing diamorphine prescription into federal law. The previous trials were based on time-limited executive ordinances. The success of the Swiss trials led German, Dutch, and Canadian cities to try out their own diamorphine prescription programs. Some Australian cities (such as Sydney) have instituted legal diamorphine supervised injecting centers , in line with other wider harm minimization programs. Since January 2009, Denmark has prescribed diamorphine to

8190-661: Was 5,968 kilograms (13,157 lb). Like all opioids used for analgesia, hydromorphone is potentially habit-forming and is listed in Schedule II of the United States Controlled Substances Act of 1970 as well as in similar levels under the drugs laws of practically all other countries and it is listed in the Single Convention On Narcotic Drugs. The DEA ACSCN for hydromorphone is 9150. Hydromorphone

8281-584: Was available for a short time in the United States before being voluntarily withdrawn from the market after a July 2005 FDA advisory warned of a high overdose potential when taken with alcohol. As of March 2010, it is still available in Nepal under the brand name Opidol, in the United Kingdom under the brand name Palladone SR, and in most other European countries. There has also been a once-daily prolonged release version of hydromorphone available in Australia under

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