Showing posts sorted by date for query Fentanyl. Sort by relevance Show all posts
Showing posts sorted by date for query Fentanyl. Sort by relevance Show all posts

Tuesday, November 9, 2021

FDA Approves Zimhi (naloxone hydrochloride) Injection for the Treatment of Opioid Overdose

In continuation of my update on naloxone hydrochlorideAdamis Pharmaceuticals Corporation (Nasdaq: ADMP) announced   the U.S. Food and Drug Administration (FDA)   approval of  Adamis’ Zimhi™ (naloxone HCL Injection, USP) 5 mg/0.5 mL product. Zimhi is a high-dose naloxone injection product FDA-approved for use in the treatment of opioid overdose.


Naloxone is an opioid antagonist and is generally considered the drug of choice for immediate administration for opioid overdose. It works by blocking or reversing the effects of the opioid, including extreme drowsiness, slowed breathing, or loss of consciousness. Common opioids include morphine, heroin, tramadol, oxycodone, hydrocodone and fentanyl.

According to statistics published by the Centers for Disease Control and Prevention (CDC), drug overdoses resulted in approximately 96,779 deaths in the United States during the 12-month period ending March 2021, which was a 29% increase over the prior 12-month period. Drug overdoses are now the leading cause of death for Americans under age 50, with more powerful synthetic opioids, like fentanyl and its analogues, responsible for the largest number of those deaths.

Dr. Jeffrey Galinkin, an anesthesiologist, and former member of the FDA Advisory Committee for Anesthetics, Analgesics and Addiction Products, commented, “I am pleased to see this much needed high dose naloxone product will become part of the treatment tool kit as a countermeasure to the continued surge in fentanyl related deaths. The higher intramuscular doses of naloxone in Zimhi should result in more rapid and higher levels of naloxone in the systemic circulation, which in turn, should result in more successful resuscitations.”

Dr. Dennis J. Carlo, President and CEO of Adamis, stated, “We are very excited by this approval and are working with our commercial partner, US WorldMeds, to make this much-needed, lifesaving product readily available to the market. Zimhi provides the highest systemic levels of naloxone compared to any of the nasal or intramuscular products currently available.”

P. Breckinridge Jones, Sr., CEO of US WorldMeds, added, “We are pleased with the approval and now look forward to commercially marketing Zimhi in the United States. US WorldMeds has a proven track-record of successfully commercializing pharmaceutical products and have a First-in-Class and only FDA-approved product, LUCEMYRA® (lofexidine), for the treatment of withdrawal symptoms associated with abrupt opioid discontinuation. We are confident we can leverage our existing commercial infrastructure and presence in the opioid dependence market to speed the uptake of Zimhi and combat the growing opioid crisis. We are preparing for the full commercial launch of ZIMHI which is planned for the first quarter of 2022.”\

Thursday, June 20, 2019

FDA Approves First Generic Naloxone Nasal Spray Against Opioid Overdose


In continuation of my update on naloxone 


   Naloxone.svg



The first generic naloxone nasal spray to treat opioid overdose has received approval from the U.S. Food and Drug Administration.
Teva Pharmaceuticals' lifesaving product is also the first generic naloxone nasal spray approved for use by people without medical training. There was already a brand-name spray (Narcan) for emergency use by untrained people, such as family members and bystanders.
The need is urgent. On average, more than 130 Americans die every day from overdoses of opioids -- including prescription painkillers such as fentanyl, oxycodone (OxyContin), hydrocodone (Vicodin) and morphine, as well as illegal drugs such as heroin or drugs sold as heroin, the FDA said.
"In the wake of the opioid crisis, a number of efforts are underway to make this emergency overdose reversal treatment more readily available and more accessible," said Dr. Douglas Throckmorton, deputy center director for regulatory programs in the FDA's Center for Drug Evaluation and Research.
"In addition to this approval of the first generic naloxone nasal spray, moving forward we will prioritize our review of generic drug applications for naloxone," he added.
When someone overdoses on opioids, breathing may become shallow or stop completely, leading to death if no one intervenes. If administered quickly, naloxone can counter the effects within minutes.
Throckmorton said in an agency news release that the FDA is also helping drugmakers pursue approval of an over-the-counter naloxone product, and "exploring other ways to increase availability of naloxone products intended for use in the community."
The FDA is also considering whether naloxone should be routinely prescribed along with all or some opioid prescriptions in order to reduce the risk of overdose.
"Altogether, these efforts have the potential to put a vital tool for combating opioid overdose in the hands of those who need it most -- friends and families of opioid users, as well as first responders and community-based organizations," Throckmorton said.
Nearly 400,000 people in the United States died of opioid overdoses between 1999 and 2017, according to the U.S. Centers for Disease Control and Prevention.
"We're committed to working with other federal, state and local officials, as well as health care providers, patients and communities across the country to combat the staggering human and economic toll created by opioid abuse and addiction," Throckmorton said in the news release.
 Ref : https://en.wikipedia.org/wiki/Naloxone



Monday, February 13, 2017

Painkiller That Killed Prince Part of Dangerous Wave of New Synthetic Drugs

In continuation of my update fentanyl
The recent overdose death of rock legend Prince has brought renewed focus on the dangers posed by synthetic opioids -- laboratory-created narcotics tweaked by chemists to produce potentially lethal highs while skirting U.S. drug laws.
Fentanyl2DCSD.svg 
Prince Rogers Nelson, 57, died April 21 from an overdose of fentanyl, a drug often used to quell pain in cancer patients when traditional opioids prove ineffective.
Despite its legitimate medical uses, fentanyl has acquired a growing reputation as a dangerous street drug thanks to at least a dozen synthetic variants now available to users, according to the U.S. Drug Enforcement Administration (DEA).
And fentanyl is only one of numerous synthetic opioids and designer drugs now flooding the illicit drug market in the United States, DEA acting chief Chuck Rosenberg warned during a U.S. Senate hearing last week.
"We are trying to keep up with a picture that changes almost every day," Rosenberg testified. "We've identified something like 400 new psychoactive substances over the last four or five years."
Another synthetic opioid, U-47700, has been connected to at least 50 deaths nationwide, but is so new to the black market that the DEA has not yet moved to control it, according to the Associated Press.
U-47700 fixedstructure.svg U-47700
Synthetic narcotics are dangerous because their potency can far outstrip traditional opioids. For example, fentanyl is 25 to 40 times more potent than heroin, and 50 to 100 times more potent than morphine, said Dr. Mitra Ahadpour. She is a medical officer with the Center for Substance Abuse Treatment in the U.S. Substance Abuse and Mental Health Services Administration.
Rosenberg testified that "fentanyl is so dangerous we've had to instruct our agents that if they touch it or inhale it accidentally, they can die."
Several states reported sharp increases in overdose deaths caused by fentanyl and its analogs in 2014, a health advisory from the U.S. Centers for Disease Control and Prevention noted. Ohio reported 514 fentanyl-related deaths in 2014 compared to 92 in 2013, while Maryland had 185 fentanyl deaths in 2014 compared to 58 the year before.
Ahadpour explained that "if someone is not opioid-tolerant, and uses either pharmaceutical or illicit fentanyl, you have a very high increased chance of respiratory depression and dying. Their breathing slows down, it goes to shallow breathing, and then they stop breathing."
There's wide variation in the potency of these synthetic drugs, and often they are cut with other illicit drugs, Ahadpour added. A user might buy heroin not knowing that it has been cut with fentanyl to increase its potency.
Eleanor Artigiani, deputy director of policy and governmental affairs with the University of Maryland's Center for Substance Abuse Research, said, "They may think they're getting heroin, or they're just buying a Xanax pill off the street, when it's actually one of these other substances."
Artigiani added, "From what I've been hearing recently, sometimes even the people selling these drugs don't know exactly what's in them either. It's like Russian roulette, because you don't really know what you're getting or what effect it's going to have on you."
Toxicology tests concluded that Prince died from a fentanyl overdose, although the medical examiner's report did not say whether the fentanyl was prescription or an illicit analog, CNN reported.
Designer drugs are typically based on medications that have been around for decades, Artigiani said.
Fentanyl was first created in Belgium in the late 1950s, the DEA says, while U-47700 was developed in the 1970s by the pharmaceutical company Upjohn as a potential alternative for morphine.
Black market drug makers come across the formula for a drug, and then tweak the molecule slightly so that it has the same effect on people but isn't technically the same substance, Artigiani explained.
"There's a journal article or a patent document or something that gets produced," she said. "Illicit chemists find it and reproduce it or tweak the molecules to look for other kinds of things that aren't illegal, that haven't been scheduled yet."
Other synthetic opioids on the streets include substances with names like W-18, AH-7921 and MT-45, according to Congressional testimony provided by James Hall, an epidemiologist with the Center for Applied Research on Substance Use and Health Disparities at Nova Southeastern University in Miami.
Illicit drug manufacturers also produce other categories of designer drugs besides synthetic opioids, Hall said, including synthetic versions of cannabinoids, stimulants and hallucinogens.
Nearly all synthetic opioids and other designer drugs are manufactured in China, U.S. National Drug Control Policy Director Michael Botticelli testified before the Senate.
The designer drugs enter the United States either through the mail or across the Mexican or Canadian border, he said, and often are sold at head shops and other retail stores.
State and federal lawmakers are reviewing legislation designed to improve response against new synthetic narcotics, Botticelli said, and the United States is leading discussions with international partners to improve the global response to these drugs.
But right now, law enforcement often is several steps behind the traffickers because U.S. laws aren't flexible enough to quickly outlaw emerging drug analogs, Rosenberg told Congress.
"I almost feel each time I sign an administrative control regulation that I'm simply telling the bad guys, 'Not this one any more. Move over here.' And that's what they do," Rosenberg said. "For every one substance we've controlled, legislatively or administratively, there are 11 more out there that are uncontrolled."

Monday, March 31, 2014

New drug multiplies analgesic effect of opioids without increasing constipation


Systemic (subcutaneous) or local (intraplantar) treatment of wild-type mice with the selective σ1 antagonists BD-1063 [1-[2-(3,4-dichlorophenyl)ethyl]-4-methylpiperazine dihydrochloride] or S1RA [4-[2-[[5-methyl-1-(2-naphthalenyl)1H-pyrazol-3-yl]oxy]ethyl] morpholine hydrochloride] potentiated μ-opioid antinociception; these effects were fully reversed by the σ1agonist PRE-084 [2-(4-morpholinethyl)1-phenylcyclohexanecarboxylate) hydrochloride], showing the selectivity of the pharmacological approach. The μ-opioid antinociception potentiated by σ1 inhibition (by σ1-receptor knockout orσ1-pharmacological antagonism) was more sensitive to the peripherally restricted opioid antagonist naloxone methiodide than opioid antinociception under normal conditions, indicating a key role for peripheral opioid receptors in the enhanced antinociception. Direct interaction between the opioid drugs and σ1 receptor cannot account for our results, since the former lacked affinity for σ1 receptors (labeled with [3H](+)-pentazocine). A peripheral role for σ1 receptors was also supported by their higher density (Western blot results) in peripheral nervous tissue (dorsal root ganglia) than in several central areas involved in opioid antinociception (dorsal spinal cord, basolateral amygdala, periaqueductal gray, and rostroventral medulla). In contrast to its effects on nociception, σ1-receptor inhibition did not alter fentanyl- or loperamide-induced constipation, a peripherally mediated nonanalgesic opioid effect. Therefore, σ1-receptor inhibition may be used as a systemic or local adjuvant to enhance peripheral μ-opioid analgesia without affecting opioid-induced constipation.

Ref : http://jpet.aspetjournals.org/content/348/1/32.abstract?sid=60aaa64d-fb66-459c-aded-4e971ab39aac


New drug multiplies analgesic effect of opioids without increasing constipation

Thursday, March 11, 2010

Positive phase III efficacy clinical trial for Fentanyl sublingual spray .....

INSYS Therapeutics, Inc. announced positive results from the pivotal phase III efficacy  trial for patients utilizing the Fentanyl Sublingual Spray (SL Spray) technology to treat breakthrough cancer pain.  The company claims that all primary and secondary endpoints were achieved in the study, and the drug is the first product to ever show statistically significant pain relief when measuring the summary of pain intensity difference at five minutes (SPID(5)) in a phase III breakthrough cancer pain trial using Fentanyl.

Dr. Richard Rauck, a principal investigator in the Phase III study observed,  the sublingual spray demonstrated very rapid, effective pain relief. Patients began to experience meaningful pain relief within five minutes. This observation was supported by the clinical research findings.  As claimed by the researchers, to date, no other transmucosal Fentanyl  (see the general structure) product has produced pain relief this quickly. This  finding is supported with continued pain relief at all subsequent time intervals. 

Hope this easy-to-use oral spray that can produce effective, potent and very rapid pain relief will be a tremendous advantage for the  patients who experience moderate to severe cancer breakthrough pain.....

Ref : http://www.insysrx.com/news.htm