Posts Tagged ‘New Opioids’

A New Drug on the Scene: Isotonitazene

As if fentanyl and its derivatives weren’t killing enough people, we another opioid to worry about. It’s isotonitazene, sometimes called “Iso” or “Nitazene” for short. it’s related to etonitazene and has similar drug effect profile.

This drug, which is not approved for medical use anywhere in the world, is a synthetic opioid with high potency. It has been identified in drug seizure analyses by the DEA on a regular basis since 2019. In 2020, the DEA issued a temporary order to schedule isotonitazene and its isomers as Schedule I controlled substances, with all the civil and criminal sanctions carried by this designation.

This drug has a high potential for addiction and causes respiratory depression in a dose-related fashion. Some reports suggest this drug may be worse at causing respiratory depression than other opioids, making it more dangerous. Its effects can be reversed by naloxone, though some sources say it might take a higher dose.

Since this drug is sold illicitly, buyers get it through unregulated sources, so the purity varies widely and inconsistently, adding to the danger of this drug.

A recent article by the Washington Post goes into more detail about how the drug and its analogues have been found in the District of Columbia’s drug supply:

This article says that according to experts, isotonitazene analogues are more potent than fentanyl. Deaths from analogues, mostly protonitazene, have occurred in Tennessee, Texas, New Jersey, and Iowa, among other states. Overdose deaths have also been seen in Europe and British Columbia, Canada.

There have been some reports of overdosed patients presenting to the Emergency Department with respiratory arrest, which is a common mechanism of death with opioids, but also with no heartbeat. With other opioids, respiratory depression or arrest is often accompanied by slow heart rhythm ( )

This all sounds pretty bad. Several doctors in my state have seen patients who mentioned this drug among the types of opioids they are using, so I plan to start asking patients about it.  I don’t know of any drug test available commercially to detect this drug, further complicating treatment.

Out of curiosity, I Googled the drug and how to buy it, leading to a depressing array of purchase options. One website based in China offers this drug for $450 for 10 grams, or $9000 for a kilogram. Of course, they offer a selection of other controlled substances to consumers. Who knows what would be shipped if anyone bought off this website – if anything at all. And it would be illegal, and subject to schedule 1 drug penalties if discovered, lest any of my readers feel tempted to purchase off the internet.

Some news articles say the drug dealers buy isotonitazene in bulk to add to whatever illicit opioid they are selling, to make it go farther. This practice led to series of deaths in some states.

In the Sept-Oct 2021 issue of the Journal of Addiction Medicine, Shover et al published an article titled, “Emerging Characteristics of Isotonitazene-involved Overdose Deaths: A Case Control Study,” in which they compared characteristics of 40 isotonitazene deaths with overdose deaths from other opioids. They found deaths from isotonitazene more often involved other drugs and were also more often found in combination with a designer benzodiazepine called flualprazolam.

 I suspect some dealer somewhere added this second drug to a bulk supply of isotonitazene, which was then sold on the street. This emphasizes the problem of knowing what a drug bought illicitly actually contains. Potent opioids, when taken with sedatives like benzos, are known to cause overdose deaths in the unsuspecting buyer.

So what do we do about Iso? I plan to ask new patients about their use of it, or if they’ve even heard of it. We need a cheap commercially available test for the drug to get better information about the extent of the problem. And we need to educate and warn patients and providers about the drug’s presence.

And keep giving out lots of naloxone kits.

New Opioids

I’ve blogged about states that have passed new laws addressing the prescribing of opioids, but the manufacturers of prescription opioids medications also have made changes to help reduce the potential for medication misuse. Of course, opioids will never be misuse-proof, but at least it’s a little harder to misuse some of the newer ones.

Oxecta is a new immediate-release brand of the drug oxycodone. It’s formulated so that it breaks into chunks when crushed, instead of a powder. When it’s mixed with water, it forms a gel so that it can’t be injected. This pill contains sodium laurel sulfate, a substance that irritates the nose if snorted.

Lazanda is a new delivery form of a very potent opioid, fentanyl. This brand is designed to be used as a nasal spray, which I would expect to be very addictive. The preparation itself has no anti-abuse features, but in order to distribute, dispense, prescribe, or be prescribed this medication, parties have to sign an agreement and be enrolled with the drug company. This extra scrutiny is hoped to deter diversion by distributor, pharmacy, doctor, or patient. Physicians must take a training program specific for this brand, and be enrolled with the drug company as a prescriber, or pharmacies can’t dispense to the patient.

Patients also need to complete a patient-prescriber agreement. Many people (like me) think doctors aren’t likely to jump through these extra hoops to prescribe this particular brand, when other brands of the same medication are already on the market, though not in the form of nasal spray.

Remoxy, another brand of oxycodone, hasn’t yet been FDA approved. Supposedly, it’s resistant to injection or snorting, and also has been formulated to be resistant to alcohol extraction.

Drug companies are now required by the FDA to have plans to evaluate and mitigate the risks associated with the opioid drugs they manufacture, particularly if they make sustained release or long-acting opioid preparations. This cooperation by drug manufacturers is a necessary part of turning the tide of opioid addiction in this country.

Last year, Purdue Pharma re-formulated OxyContin, making it more difficult to crush to snort or inject.  I noticed a sudden drop-off in patients entering treatment for pain pill addiction who said OxyContin was their drug of choice. During the years 2002 through 2007, nearly all of the opioid addicts I admitted to treatment said OxyContin was their preferred drug. It became obvious that the re-formulation made a big difference.

Addicts can and will still abuse these medications orally to get high, but the new formulations really do reduce abuse by making pills less likely to be snorted or injected.