~Oxymorphone - Numorphan - Numorphone - 14-Hydroxydihydromorphinone~
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From Wikipedia, the free encyclopedia
--->What is Opana?
Brand Name: O P A N A Chemical/Generic Name: O X Y M O R P H O N E Oxymorphone is a powerful semi-synthetic opioid analgesic first developed in Germany circa 1914, patented in the USA by Endo Pharmaceuticals in 1955 and introduced to the United States market in January 1959 and other countries around the same time. It (along with hydromorphone) was designed to have less incidence of side effects than morphine and heroin. It was a success as it differs from morphine and heroin in its effects in that it generates less euphoria, sedation, itching and other histamine effects at equianalgesic doses. This also means a lower dependence liability. The brand name Numorphan is derived by analogy to the Nucodan name for an oxycodone product (or vice versa) as well as Paramorphan / Paramorfan for dihydromorphine and Paracodin (dihydrocodeine). The only commercially available salt of oxymorphone in most of the world at this time is the hydrochloride, which has a free base conversion ratio of 0.891. In some countries, hydromorphinol is distributed under the trade names Numorphan and Numorphan Oral. This is a relatively rare exception and the two drugs, whilst both being strong opioid analgesics, are notably different from one another. Oxymorphone is administered as its hydrochloride salt via injection, or suppository; typically in dosages of 1 mg (injected) to 5 mg (suppository). Endo has been the major distributor of oxymorphone throughout the world and currently markets oxymorphone in the United States and elsewhere as Opana and Opana ER. Opana is available as 5 mg and 10 mg tablets; Opana ER, an extended-release form of oxymorphone, is available as tablets in strengths of 5 mg,10 mg, 20 mg, 30 mg, and 40 mg. The 7½ mg and 15 mg strengths of Opana ER have been discontinued as of March 1, 2011. Some resources assert that 2, 12 and/or 15 mg IR tablets and 25, 36 and 50 mg extended release tablets will be introduced although apparently the timeline on that is not known to the public at this time. Opana Extended-Release tablets are based on the TIMERx system developed by a consortium led by Endo and Penwest. Some of these strengths (notably not the 7.5 mg) are available in an Opana IR–immediate release–form for breakthrough pain to be used by patients already on 24/7 opioid care such as fentanyl patches and sustained-relief morphine drugs like Avinza. In addition to the sustained-release version for Opana, other versions of TIMERx are available and being developed for other protocols such as increasing, decreasing, stepwise increasing, and stepwise decreasing dose delivery over time, single and multiple bursts of medication, and combinations of the above. Specifically, the apparent extension of the duration of effect of the IR tablets (all other things being equal, oxymorphone has a duration of action of 5 to 8 hours in most patients) versus similar drugs in commonly used immediate-release forms-for example Dilaudid (hydromorphone),morphine Vilan (nicomorphine), and Paramorfan (dhydromorphne) as well as prodrugs for this group such as hydrocodone, nicocodeine, codeine, dihydrocodeine, and others—is often attributed to marginal extended-release effect from various excipients, particularly those that are hydrophilic and form a gel-like substance at the pH levels in the stomach and duodenum. Both as the result of this and the pharmacokinetics of oxymorphone, the IR tablets have a de facto duration of action of 5 to 13 hours (the mean would seem to be around 7 hours with a moderatly small standard deviation and a left-skewed and leptokurt- ic frequency distribution) in patients with normal kidney and liver function. As a result, patients who go on to extended - release oxymorphone preparations from other opioids may very well need the Opana IR tablets, Numorphan ampoules or phials with hypodermic needles and/or a PCA pump, or immediate-release formulations of hydromorphone, dihydromorphine, high dose oxycodone, nicomorphine hydromorphinol, diamorphine, or morphine for breakthrough pain incidents already in progress. An oxymorphone nasal spray is reportedly in development, along with a possible hydromorphone nasal spray and implantable osmotic pumps for both drugs. The duration of action and metabolic half-life of oxymorphone mean that immediate-release tablets are more similar to analgesic preparations of methadone, levorphenol, piritramide, and existing extended-release forms of morphine, oxycodone, ketobimodone and so on. The extended-release Opana tablets can provide detectable analgesia for anywhere from 6 to 36+ hours (the mean appears to be very close to the lower end of the continuum), largely contingent on things that can alter the drug's liberation, absorption, distribution, metabolism, and elimination profile. One cause is unusual conditions in the upper and middle GI tract, such as created by misoprostol and Arthrotec (misoprostol plus diclofenac). Among other things, misoprostol is a smooth muscle agent with both a contact and systemic mucousagogue that coats the stomach and adjacent areas with increasing amounts of mucus. This can result in everything from even slower onset of action to intact tablets being passed with stool. Oxymorphone is also produced within the human body when the liver metabolises oxycodone by means of O demethylation catalysed by the CYP2D6 enzyme. Approximately 10% of the dose is processed by the endocrine system in this respect; this can vary widely from person to person. The codeine-hydrocodone group and morphinans exhibit the same characteristics. Consuming alcohol with Opana extended-release tablets can be an extremely dangerous situation. The absorption of oxymorphone can vary wildly in the presence of alcohol. Plasma concentrations were found to be as low as 50% of expected to as much as 270% more than expected. Elevated plasma levels could result in overdose. Opana ER does not cause "dose dumping," which creates a blast of drug release that plagues other long acting opioids.- -------------------------------------------------------------------------------------- O p i a t e s
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* P h a r m a c o k i n e t i c D a t a *
opana ER tabs
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PAINKILLER, OPANA, NEW SCOURGE OF RURAL AMERICA
By Mary Wisniewski
AUSTIN, Indiana | Tue Mar 27, 2012 2:48am EDT
AUSTIN, Indiana (Reuters) - Back in high school in Houston, Texas, C.J. Coomer got good grades and played football. He was dark-haired and handsome, popular with his friends and doted on by his family.
But when his mother got divorced and moved to be near family in rural Scott County, Indiana, Coomer began running with a crowd there that abused prescription painkillers to get high. His weight dropped from 210 pounds to just 140 pounds (64 kg), he couldn't work, and was constantly borrowing money.
One night last July, Coomer tried something new -- Opana, a powerful opioid painkiller containing oxymorphone. He overdosed and died at the age of 24.
"It's a nightmare every single day," said his mother, Melissa Himmelheber, 43, who wiped away tears as she showed pictures of her lost son. "This is a family that was extremely close. Now we're just picking up the shattered pieces."
Prescription drug abuse is the new scourge of rural America. It now leads to more deaths in the United States than heroin and cocaine combined, and rural residents are nearly twice as likely to overdose on pills than people in big cities, according to the Centers for Disease Control.
While methamphetamine addiction has long been associated with small towns, prescription painkillers have overtaken meth as the most abused drugs in places such as southern Indiana, according to local authorities.
Opana is the hot new prescription drug of abuse, sometimes with tragic consequences.
At least nine people have died so far this year from prescription drug overdoses in Scott County, Indiana. Most of the fatalities involved Opana, according to county coroner Kevin Collins.
Before 2011, only about 20 percent of the cases referred to the coroner were overdose deaths, and most of those were suicides rather than accidents. Last year, prescription drug overdoses accounted for 19 deaths, or about half of all deaths referred to the coroner in this county of just 24,000 on the southern tip of Indiana, about 30 miles from Louisville, Kentucky.
"We're seeing a lot of 25-year-olds who are dead for no apparent reason," said Collins, who is so disheartened by the overdoses that it is one reason he won't run for reelection in May.
POTENT, DEADLY
Law enforcement officials are alarmed by the rise of Opana abuse, which they said started after Oxycontin was changed in late 2010 to make that drug more difficult to snort or inject for a heroin-like high. Oxycontin is a brand of oxycodone.
Opana abuse can be deadly because it is more potent, per milligram, than Oxycontin, and users who are not familiar with how strong it is may be vulnerable to overdosing.
Opana, known by such street names as "stop signs," "the O bomb," and "new blues," is crushed and either snorted or injected. Crushing defeats the pill's "extended release" design, releasing the drug all at once.
"This Opana pill has really kicked us in the rear," said Indiana State Police Sergeant Jerry Goodin. "We've never seen an addiction like this."
Oxycontin's new pills make it harder to crush them into a powder as they instead become gummy and cannot be readily snorted or injected. This drove abusers to switch to Opana or to generic, immediate-release forms of oxycodone, according to John Burke, president of the National Association of Drug Diversion Investigators. Drug abuse experts have also found an increase in heroin use.
Endo Pharmaceuticals, which produces Opana, announced in December that it would reformulate Opana. The new pill is being manufactured now.
The new formulation makes it difficult to crush and it turns viscous or "gooey" if an abuser tries to add liquid to it, said company spokesman Kevin Wiggins. When used properly, Opana is indicated for chronic low back and osteoarthritis pain, and cancer pain.
But the old form of Opana is still available, and pharmacy and home robberies are on the rise as addicts search for a way to get their fix, according to police.
"We're pretty much consumed by it," Shane McHenry, a detective with the Dearborn County Sheriff's Department in southern Indiana, said of Opana. He said users who cannot afford Opana sometimes travel to Cincinnati to get heroin, which is cheaper in smaller amounts.
Fort Wayne, Indiana reported about 11 pharmacy robberies related to Opana since Endo announced the reformulation, according to Fort Wayne police spokeswoman Raquel Foster. The thief would hand the pharmacist a note, as in a bank robbery, threatening harm if Opana was not delivered.
MANY SOURCES
The Opana problem has been reported by abuse experts around the country. In Florida, for example, the number of oxymorphone-related deaths rose to 493 in 2010, an increase of 109 percent from the previous year, according to Jim Hall, director of a drug abuse center at Nova Southeastern University in Florida.
Some users and dealers get painkillers from so-called "pill mills" -- storefront pain clinics that sell drugs for cash up front, often to out of-state buyers who take them for resale.
But the other way users get pills is from their doctors, or by buying from seniors looking to supplement a fixed income. One Opana pill brings up to $90 on the street depending on dosage, so it is tempting to sell, said Scott County Sheriff Dan McClain.
A woman in her late 70s was arrested in Austin, Indiana for exchanging pills for work around her house, McClain said.
"Most of what I see is people with a prescription from their doctors and they need the money," said Austin, Indiana Police Detective Lonnie Noble. He said the appetite for Opana is "more aggressive" than it was for Oxycontin.
Nashville, Tennessee Detective Michael Donaldson, who also has seen an increase in Opana abuse, said many small towns have "dirty doctors" willing to give out unneeded prescriptions.
Scott County is one of the poorest areas in Indiana, with a median household income of $39,588 in 2010. It was a hot spot for oxycodone retail distribution in 2010, with 48.79 per capita dosage units -- the highest in the state, according to Lori Croasdell, a coordinator for CEASe of Scott County, a drug abuse prevention group.
A northern section of Austin in Scott County showed signs of poverty and neglect. Run-down trailers and houses with broken windows and peeling paint were mixed in among well-kept homes and tidy gardens.
McClain said the drugs cause a vicious cycle of poverty, since abusers cannot hold a job. "Most of them sleep until noon, get up, and try to find a way to get another pill," said McClain.
One reason for the rise in prescription pill abuse is that Americans feel they can fix any problem - pain, depression, anxiety, hopelessness - with a pill, according to Shane Avery, a Scott County doctor. And some doctors, who may mean well but fear being sued for undertreating pain, give out pills better suited for cancer patients to soothe a backache, Avery said.
"The people who abuse prescription medications know how to doctor shop," said Collins, the Scott County coroner.
(Reporting By Mary Wisniewski; Additional reporting by Tim Ghianni in Nashville, Tennesee; Editing by Greg McCune and Tim Dobbyn)
AUSTIN, Indiana | Tue Mar 27, 2012 2:48am EDT
AUSTIN, Indiana (Reuters) - Back in high school in Houston, Texas, C.J. Coomer got good grades and played football. He was dark-haired and handsome, popular with his friends and doted on by his family.
But when his mother got divorced and moved to be near family in rural Scott County, Indiana, Coomer began running with a crowd there that abused prescription painkillers to get high. His weight dropped from 210 pounds to just 140 pounds (64 kg), he couldn't work, and was constantly borrowing money.
One night last July, Coomer tried something new -- Opana, a powerful opioid painkiller containing oxymorphone. He overdosed and died at the age of 24.
"It's a nightmare every single day," said his mother, Melissa Himmelheber, 43, who wiped away tears as she showed pictures of her lost son. "This is a family that was extremely close. Now we're just picking up the shattered pieces."
Prescription drug abuse is the new scourge of rural America. It now leads to more deaths in the United States than heroin and cocaine combined, and rural residents are nearly twice as likely to overdose on pills than people in big cities, according to the Centers for Disease Control.
While methamphetamine addiction has long been associated with small towns, prescription painkillers have overtaken meth as the most abused drugs in places such as southern Indiana, according to local authorities.
Opana is the hot new prescription drug of abuse, sometimes with tragic consequences.
At least nine people have died so far this year from prescription drug overdoses in Scott County, Indiana. Most of the fatalities involved Opana, according to county coroner Kevin Collins.
Before 2011, only about 20 percent of the cases referred to the coroner were overdose deaths, and most of those were suicides rather than accidents. Last year, prescription drug overdoses accounted for 19 deaths, or about half of all deaths referred to the coroner in this county of just 24,000 on the southern tip of Indiana, about 30 miles from Louisville, Kentucky.
"We're seeing a lot of 25-year-olds who are dead for no apparent reason," said Collins, who is so disheartened by the overdoses that it is one reason he won't run for reelection in May.
POTENT, DEADLY
Law enforcement officials are alarmed by the rise of Opana abuse, which they said started after Oxycontin was changed in late 2010 to make that drug more difficult to snort or inject for a heroin-like high. Oxycontin is a brand of oxycodone.
Opana abuse can be deadly because it is more potent, per milligram, than Oxycontin, and users who are not familiar with how strong it is may be vulnerable to overdosing.
Opana, known by such street names as "stop signs," "the O bomb," and "new blues," is crushed and either snorted or injected. Crushing defeats the pill's "extended release" design, releasing the drug all at once.
"This Opana pill has really kicked us in the rear," said Indiana State Police Sergeant Jerry Goodin. "We've never seen an addiction like this."
Oxycontin's new pills make it harder to crush them into a powder as they instead become gummy and cannot be readily snorted or injected. This drove abusers to switch to Opana or to generic, immediate-release forms of oxycodone, according to John Burke, president of the National Association of Drug Diversion Investigators. Drug abuse experts have also found an increase in heroin use.
Endo Pharmaceuticals, which produces Opana, announced in December that it would reformulate Opana. The new pill is being manufactured now.
The new formulation makes it difficult to crush and it turns viscous or "gooey" if an abuser tries to add liquid to it, said company spokesman Kevin Wiggins. When used properly, Opana is indicated for chronic low back and osteoarthritis pain, and cancer pain.
But the old form of Opana is still available, and pharmacy and home robberies are on the rise as addicts search for a way to get their fix, according to police.
"We're pretty much consumed by it," Shane McHenry, a detective with the Dearborn County Sheriff's Department in southern Indiana, said of Opana. He said users who cannot afford Opana sometimes travel to Cincinnati to get heroin, which is cheaper in smaller amounts.
Fort Wayne, Indiana reported about 11 pharmacy robberies related to Opana since Endo announced the reformulation, according to Fort Wayne police spokeswoman Raquel Foster. The thief would hand the pharmacist a note, as in a bank robbery, threatening harm if Opana was not delivered.
MANY SOURCES
The Opana problem has been reported by abuse experts around the country. In Florida, for example, the number of oxymorphone-related deaths rose to 493 in 2010, an increase of 109 percent from the previous year, according to Jim Hall, director of a drug abuse center at Nova Southeastern University in Florida.
Some users and dealers get painkillers from so-called "pill mills" -- storefront pain clinics that sell drugs for cash up front, often to out of-state buyers who take them for resale.
But the other way users get pills is from their doctors, or by buying from seniors looking to supplement a fixed income. One Opana pill brings up to $90 on the street depending on dosage, so it is tempting to sell, said Scott County Sheriff Dan McClain.
A woman in her late 70s was arrested in Austin, Indiana for exchanging pills for work around her house, McClain said.
"Most of what I see is people with a prescription from their doctors and they need the money," said Austin, Indiana Police Detective Lonnie Noble. He said the appetite for Opana is "more aggressive" than it was for Oxycontin.
Nashville, Tennessee Detective Michael Donaldson, who also has seen an increase in Opana abuse, said many small towns have "dirty doctors" willing to give out unneeded prescriptions.
Scott County is one of the poorest areas in Indiana, with a median household income of $39,588 in 2010. It was a hot spot for oxycodone retail distribution in 2010, with 48.79 per capita dosage units -- the highest in the state, according to Lori Croasdell, a coordinator for CEASe of Scott County, a drug abuse prevention group.
A northern section of Austin in Scott County showed signs of poverty and neglect. Run-down trailers and houses with broken windows and peeling paint were mixed in among well-kept homes and tidy gardens.
McClain said the drugs cause a vicious cycle of poverty, since abusers cannot hold a job. "Most of them sleep until noon, get up, and try to find a way to get another pill," said McClain.
One reason for the rise in prescription pill abuse is that Americans feel they can fix any problem - pain, depression, anxiety, hopelessness - with a pill, according to Shane Avery, a Scott County doctor. And some doctors, who may mean well but fear being sued for undertreating pain, give out pills better suited for cancer patients to soothe a backache, Avery said.
"The people who abuse prescription medications know how to doctor shop," said Collins, the Scott County coroner.
(Reporting By Mary Wisniewski; Additional reporting by Tim Ghianni in Nashville, Tennesee; Editing by Greg McCune and Tim Dobbyn)
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This prescription medication is a narcotic and meant for treating moderate to severe pain. It’s the generic name for medications including Opana, Opana ER and Numorphan HCI.
Oxymorphone is said to act similar to morphine. Opana ER is the extended release version and used to treat moderate to severe, around-the-clock pain. Oxymorphone works by attaching to receptors in the brain and nervous system to block pain. One of the most important things to know about oxymorphone and other potent narcotic analgesics is that they can be habit-forming. It is also considered a drug of abuse and can lead to problems including the development of tolerance, physical and psychological addiction, abuse, overdose, withdrawal symptoms and the need for medical detox. Oxymorphone is not for everyone so you should check the product’s instructions on use before taking it. It can interact with other medications and medical conditions. It’s essential to take oxymorphone only as prescribed. Taking it more often than prescribed or recommended or in higher doses could lead to dependence or overdose. Important Safety Information : When Taking Oxymorphone This opiate medication should be taken cautiously. Because it can cause drowsiness, dizziness and light headed feelings, it should not be taken with alcohol, other narcotics and certain other meds . The combination of oxymorphone and other substances could heighten side effects. The elderly may be more sensitive to side effects and the effectiveness of oxymorphone has not been established in children under 18. The drug may cause harm to a fetus so pregnant women should talk to their doctors and weigh the benefits and risks. Misuse or abuse of the drug can lead to serious side effects including:
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