Opioids Part V

By Frank G. Vice, DVM, BS Pharm

OpioidsThroughout history, opium has been both a blessing and a curse, with its greatest blessing gained from its ability to manage pain.  However, its curse is realized through its abusive and addictive properties which can result in toxicities and death. The need to manage pain poses a unique challenge and until other pain management methods are developed, studied and implemented into therapy, prescription opioid use is essential for pain relief and the patient’s over-all quality of life. Constant opioid use for chronic pain management will cause patients to develop a tolerance. As opioid tolerance develops, individuals look for products to deliver more opioid support for their physical needs and euphoric desires. Current Center of Disease Control (CDC) guidelines, along with some additional state laws, are discouraging chronic prescription opioid use. These new guidelines are encouraging the medical profession to offer alternative therapies for pain management. As more restrictive opioid guidelines are implemented, dependent people seek stronger opioid alternatives, ultimately turning to illegal heroin, fentanyl or carfentanil. This cycle of need, tolerance and abuse has become a public health disaster. The Drug Enforcement Agency (DEA) regards heroin as a schedule Cl medication, with no approved human medical use, with fentanyl scheduled as a Cll medication having a very closely monitored human medical use, mostly in hospitals. The dangers posed by carfentanil, a DEA scheduled Cll synthetic opioid, surround its use as a very potent tranquilizer for large wild animals.  These opioid alternatives are illegally manufactured outside the United States and sold illegally to illegal drug suppliers who eventually flood the small towns and cities all across the country and throughout the world. Many times, opioid abusers don’t know or don’t realize these more potent synthetic opioids are in a heroin mixture.  When either one of these products is mixed with heroin, abusers may experience a more intensified euphoric response which will entice an experienced abuser to inject even higher doses. The anticipated euphoria will actually end up being an overdose, which is a common result among drug users. Yet the desire to experience chemical induced brain stimulating pleasure is greater than the fear of death.

The overwhelming desire for dependent patients to use opiates can partially be explained by the drugs’ action on the brain. Opiates work by attaching and stimulating opiate receptors located throughout the body and especially concentrated in clustered areas of the brain. These brain receptors are designed to respond to opiates by reducing pain perception and maintaining analgesia. In addition, opiates also stimulate emotional activity in the reward centers of the brain. When administered intravenously, opiates move from the bloodstream into the brain, nearly instantly attaching to the receptors with rapid activity, stimulating the release of brain chemicals called neurotransmitters. As this rush of neurotransmitters is released, the patient relaxes, experiencing a rapid euphoria of pleasure described as wonderful bliss or a sense of contentment. All the while, the brain is functioning to record this stimulated pleasure as an uncontrollable memory creating an uncontrollable desire. This unforgettable experience of pleasure will progress to drug dependence and tolerance. However, along with the brief euphoric stimulation, the abuser will experience multiple adverse effects, which occur during periods of drug withdrawal. During the withdrawal period patients may experience drug craving, sweating, mood swings, irritability, agitation, depression, nausea, vomiting, confusion, constipation, drowsiness, sedation, physical dependency, respiratory depression, respiratory failure, unconsciousness, coma, and death.

The abusive impact of illegal opioids expanded to a national epidemic during 2017, with cities across this country reporting multiple overdoses. Although it is true that opioid tablets can result in respiratory failure and death, investigators don’t see the frequency or rapid respiratory depression as often as intravenous use. Experts suggest that the increased overdose problem has extended beyond prescription opioids and is now directly related to the illegally manufactured opioids like carfenatnil and fentanyl. The potency of fentanyl is estimated to be 50 to 100 times greater than morphine, which is the reference opioid standard. When these drugs are mixed with heroin and injected into the bloodstream, an immediate rapid respiratory depression develops. Even in medically approved surgical procedures, fentanyl is used with comprehensive attention and care by medically trained personnel. This is in stark contrast to the rapid unregulated injections used by untrained abusers rushing to satisfy the next euphoric experience. Dependent abusers have no medical training, they simply add the mixture in a syringe and place the needle into any available blood vessel, and with one push of the plunger, release a toxic juice flowing into the blood and throughout the body, flooding the central nervous system (CNS) with enough drug to anesthetize an elephant.

The brainstem and medulla are areas in the CNS responsible for respiration. As an involuntary system, it is designed to maintain an adequate oxygen and carbon dioxide balance throughout the body. Potent opioids rapidly attach to receptors located in the brain, inducing respiratory depression, a life threatening condition resulting in death unless reversed. Depressive respiratory activity due to an opiate overdose can be blocked by using an antagonist or blocking agent called naloxone (Narcan). Kentucky is legally allowing naloxone to be used in all suspected opiate overdoses due to its life saving ability. Naloxone’s availability has even be extended to veterinary use when needed to reverse intentional or unintentional narcotic overdoses in dogs.

Even though heroin is readily available and usually inexpensive, the overall cost of abuse is enormous. Expense consideration should be focused on the health of the addicted users, their families, the community and state at-large, along with the resources devoted to the addicted population. The overwhelming expense is the death loss of thousands of young lives and the potential that each life represented. Treatment efforts for this health care crisis cannot be accomplished by the dependent patient alone, since drug abusers are stuck in a web of confusion with limited options. Many opioid dependent patients gain most of their confidence and drug independence from focused rehabilitation programs designed to guide individuals though the maze of abuse recovery. These community based treatment assistance options are exhausted from working with increasing patient loads, limited funds, and under staffing. Many times, the long waiting lists leave the abuser with no choice. It has been suggested that private funded treatment options are too expensive for most patients unless they have personal economic resources available. Even though treatment options are limited, opioid abusers should not be expected to withdraw through a “Cold Turkey” method. This type of opiate withdrawal affects the dependent patient both physically and psychologically, possibly beyond what most people can tolerate, ultimately driving the abusers into another drug abuse cycle ending in death.

Recently, Public Television (KET) invested extensive time and resources exploring the drug abuse problem in Kentucky. This TV program addressed the abuse epidemic and provided information regarding drug abuse treatment options. Their featured program titled “Inside Opioid Addiction”, brought together experts, policy makers and medical professionals from across the country, collectively reviewing multiple approaches for a very complex problem.

The telecast indicated Kentucky is maintaining a proactive position, which began as early as 2004, with the formation of the office of Drug Control Policy. This Policy office has a goal to coordinate all substance abuse related problems, with the intent to make Kentucky the model for management of the opioid epidemic. Their plan is to join forces with law enforcement and educational resources, along with prevention and treatment programs, with each group understanding the entire problem. Part of the proposed treatment plan involves delivery of needle exchange programs which would at least reduce the spread of hepatitis C and HIV, along with other blood borne diseases. In addition, there will be an increase in the availability of the opiate antagonist, naloxone, which is needed to reverse the effects of most opiates, including heroin. Opioid detoxification and withdrawal management programs might include the synthetic opioid methadone. It offers control of withdrawal symptoms but no euphoria, since withdrawal is a major obstacle facing opioid dependent patients. Additional products used to help control opioid dependency include Suboxone and Vivitrol. The use of these drugs will depend on multiple talented people, all focused on a solution. It goes without further comment that opioid abuse is a very complicated issue, requiring some of the best minds available to resolve an age old problem. Complete treatment information is beyond the scope of this article, however, additional information can be obtained through the Kentucky office of Drug Control Policy.

The author wishes to thank the following educational resources for their literary contributions: Public Television (KET); “Inside Opioid Addiction”, Christopher Stock Pharm D August 2016, “The Rx Consultant” “Opioid Prescriptions” Christopher Stock Pharm D, October 2015, “The Rx Consultant” “Opioid overdose and Naloxone Rescue Kits” US Pharmacist “March 2017 Managing pain in the Opioid tolerant Patients” Kentucky Cabinet for Health and Family Services.Ky.gov

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