*  H  e l p     f o r     A  d d i c t s   L  i v i n g   O  p i o i d - d e p e n d e n t   *

---

     An Online Opioid Addiction Information & Recovery Resource:

                  ~ For Those Suffering From Opioid Addiction And/Or  For The Loved Ones Of Those Who Are ~

................................

.

---

opiate /opi·ate/ (o´pee-it)
1. a drug that contains opium or derivatives of opium.
e.g. Opium, Codeine, Morphine
.................................
opioid /opi·oid/ (o´pee-oid)
1. Opioids are a class of drugs that include both natural and synthetic substances.
.................................
*The natural opioids (referred to as opiates) include opium and morphine.
.................................
Heroin, the most abused opioid, is synthesized from opium.
.................................
Other synthetics:
(man-made) and commonly
prescribed for pain, such as cough suppressants, or as anti-diarrhea agents, include:
-hydrocodone (Lortab,Vicodin)
-oxycodone (OxyContin)
-meperidine (Demerol)
-fentanyl (Sublimaze)
-hydromorphone (Dilaudid)
-Methadone (Dolophine) 
       and
-propoxyphene (Darvon,Darvocet)
*Many others as well not listed

---

What Its Like To Be :  addicted.

---

For many years we as a society have assumed that those who become addicted
to drugs or alcohol do so out of character weakness and or moral depravity. While choices and judgment make up a part of why some people become addicted,  it does not account for all people. Many people are treated with prescription painkillers for legitimate pain only to discover they have exchanged a pain problem for an addiction.

Once addiction sets in certain behaviors quickly develop to sustain the need for
more and more drugs to get the same effect, and ultimately just to stop the agony of withdrawal symptoms. The rest of the world sees these behaviors of survival as cunning, devious, ugly, covert, and very dangerous and destructive.

Opiate addiction is a brain disease characterized by increased tolerance leading to more and more substance needed to achieve the same effect. Also, there is a continued use of the substance despite negative consequences, which is baffling to the non-drug user.

The opioid-addicted individual experiences unpredictable mood swings, exhibits manipulative behaviors, lying, inability to keep appointments, neglecting important relationships and responsibilities. Often bills go unpaid in favor of buying drugs, which leads to utilities being turned off, families being angry and frustrated and even bankruptcy.

Addiction to opioids is a cycle of highs and lows. The highs begin with feelings of extreme euphoria and comfort unlike any feeling that can be obtained naturally. In the beginning the lows are just a return to normal. This is why heroin and other opioids are often called a trap; it appears to have no down side, when someone takes the opioids they feel euphoric and content and do not suffer any negative side effects.

However, this does not last for long.  Soon they notice the level of euphoria is not as great as it was the first few times and they start to feel less than normal without the drug. This condition escalates and eventually life becomes so unbearable without the opioid; they take it whenever possible. The feelings of euphoria have diminished over time. Now the opioid only causes feelings of "normalcy" and no longer euphoria.

The process has completely reversed itself,  before they felt normal without the drug now they only feel normal with it. But it doesn’t end there. As time goes on they need more and more to feel normal and to prevent withdrawal.  Eventually a depression starts to take over even while taking the drugs, no matter how much they take, signs of depression are still there. They are just medicating themselves to lower the depression. To stop using would mean being overwhelmed with depression and feelings of despair not to mention the extreme physical effects of withdrawal.

This is why it is so hard to quit. They are trying to do the hardest thing they have ever done in their lives, while feeling worse then they ever had. The pain is BOTH mental and physical. It’s very difficult to discuss feelings and review painful circumstances that led to addiction while fighting depression, the intense physical withdrawal symptoms, and cravings.

Only 5% report remaining drug free after quitting "cold turkey". The other 95% need some kind of treatment. Buprenorphine and Methadone are both treatments that can eliminate these symptoms of withdrawal and allow an addicted person to address the root problem without the distraction of withdrawal.

The root problem (the reason for drug use in the first place) must be addressed if they are to remain abstinent.

How then does addiction to opiates happen in the first place?. It may occur as a result of treatment for chronic pain, peer pressure, self medication for an undiagnosed psychiatric disorder or post traumatic stress disorder such as rape, incest, abortion, poor judgment, the loss of someone very important such as a child, parent, or spouse. There may be an unknown genetic predisposition to addiction. One thing for certain is that opiate addiction is unintentional.

The important thing to note is that it can happen to anyone.

The emotional attraction can begin almost instantly upon using opioids. Many young people think they are safe because they aren’t using heroin or putting a needle in their arm. They use prescription painkillers, which they believe,  are safe because they are pharmaceutical. "If they are FDA approved, they must be safe." This just is not the case. Misusing these pharmaceuticals can be just as deadly as heroin. Furthermore, buying Oxycontin, Vicodin, Percocet, etc., on the street is very expensive. Soon it becomes cheaper to maintain an expensive addiction by switching to heroin, which is about 5-10 times cheaper on the street.

Why is it so difficult to stop?

Once addicted, the patient continually seeks to prevent the withdrawal symptoms, others seek the euphoria they felt in the beginning – before they developed a tolerance – but they are never able to achieve it again. Some overdose and die trying. Others are self medicating by constantly taking the opioid only to prevent the withdrawal symptoms.

Some will do almost anything to prevent withdrawal. The symptoms of withdrawal are described by thousands of patients as "The flu times 100." The symptoms include prolonged nausea, vomiting, diarrhea, chills, sweats, painful goose bumps, anxiety, uncontrolled leg movement, dilated pupils, irritability, depression, insomnia for several days on end, anger, stomach pain, cramps, muscle and joint pain, tremors, nasal congestion, tearing eyes, and feeling like they are going to die. Some patients have reported that they keep toughing it out but after two weeks or more they just can’t fight the depression any longer, and just need an escape from quitting. They know that just a pill or a little white powder will take away the agony, and they feel compelled to do it.

Denial is such an imposing part of the illness that it is difficult, even impossible to
get through to the addicted person with what the rest of us know to be simple common sense. The addicted person is aware they have a problem; they deny that
they have lost control of it. The only time they think about the gravity of their problem is when they are nearing withdrawal. At that time their focus narrows to
just getting the substance to prevent the withdrawal. Once they take the substance, they feel they have no problem, or it just doesn’t seem that bad anymore. This cycle doesn’t leave much time for a rational review of one’s life.

Often it is said someone must hit rock bottom before they ready to stop and seek help. A devastating shock is often what it takes before someone ascends from the cloud of denial. Research has shown hitting "rock bottom" is not entirely necessary. Patients can benefit from treatment at any time. Patients incarcerated and forced into treatment unwillingly have still benefited.

What is consistent is the sooner treatment begins, the better the chances & outcome  of surviving this addiction.                                                                                                                                                                                                                                                                                                            source: www.suboxone.com

---

Could you be suffering from opioid dependence  —  addiction to opioid painkillers, such as:  OxyContin®, Vicodin®, Percocet®, or Actiq®,* or to Heroin?

 *Have you experienced 3 or more of these over a  12-month period?

• Needing to take more of the drug to get the same effect—or getting a lesser  effect from the same amount of drug?


• Experiencing withdrawal symptoms when not using opioids, or taking other drugs  to help relieve withdrawal symptoms ?
• Persistently wanting to quit, or are you trying to  but unsuccessful to quit?


• Spending a lot of time and effort
  to obtain, use, and recover from taking opioids ?


• Working less, missing work, or,
  if unemployed, and you aren't seriously looking for a job ?


• Spending less time seeing friends
  who don’t use opioids; skipping
  social and/or recreational activities ?


• Continuing to use opioids despite it's negative and harmful consequences?

*If You Answered YES to at least 3 of the above quesstions, I urge you to Please seek help  ASAP.

The longer you continue = the more you will use =  the Harder it becomes to stop. 

 If you do need help with opioid addiction or dependence,
help is available.

If you need any help in locating or finding out whats offered in your area please email me at: KDtha1@aol.com

   What are Opiates and Opioids ?

Opiates are drugs derived from opium. At one time "opioids" referred to synthetic opiates only (drugs created to emulate opium, however different chemically). Now the term Opioid  is used for the entire family of opiates including natural, synthetic and semi-synthetic.

Medical professionals use the word opioid  to refer to most opioids, and opiate for a specific non-synthetic opioid; however, many only use  “opioid”. Consistent with the newest definition, this website uses “opioid” to refer to all opioids and opiates.
 
An opioid is any agent that binds to opioid receptors (protein molecules located on the membranes of some nerve cells) found principally in the central nervous system and gastrointestinal tract, and elicits a response.

There are Four Broad Classes of Opioids:                         

    1. Endogenous Opioid, naturally produced in the body, Endorphins.

    2. Opium Alkaloids, are produced directly from the opium poppy, such as                       Morphine and Codeine.
   
    3. Semi-Synthetic Opioids, are man-made but similar chemically to opium          such as Heroin, Oxycodone, and Buprenorphine.

    4. Fully-Synthetic Opioids, these have structures that are chemically unrelated  to the opium alkaloids and made to mimic the action of a natural opiate alkaloid, an example would be Methadone and  Fentanyl.


Examples of some of the most common opioids that are prescription painkillers are:  Morphine, Methadone, Buprenorphine (Suboxone), Hydrocodone, Oxycodone, and Oxymorphone (Opana).

Heroin is also an opioid and is illegal.  

Opioid drugs sold under brand names include: OxyContin® , Percocet® ,
Vicodin® , Percodan® , Tylox®  and Demerol®  among others. 

Opioids attach to receptors in the brain.  Normally these opioids are the endogenous variety created naturally in the body. Once attached, they send signals to the brain of the “opioid effect” which blocks pain, slows breathing, and has a general calming and anti-depressing effect. The body cannot produce enough natural opioids to stop severe or chronic pain nor can it produce enough  to cause an overdose.

To understand the appeal of opioids it is necessary to understand the effects. At low to moderate doses the “High” from opioids is not intoxication or impairing (as with alcohol). It does not feel like alcohol or marijuana, or  hallucinogens. It instead provide feelings of intense joy and comfort, more so than can be obtained naturally. It is similar to feelings of great achievement or accomplishment, or success of a lifetime goal, rather than an impairment.

Most likely, you wouldn't even notice or be able to tell by appearance if someone was under the influence of these substances, which is another attractive quality to users.



                                                

HBO Documentary Series presents:
  Opiate Addiction: 
Understanding Replacement Therapy
( Click Arrow Below to Watch Video )

---

---

International Journal of Methods in Psychiatric Research
Int. J. Methods Psychiatr. Res. 17(S1): S39–S44 (2008)
Copyright © 2008 John Wiley & Sons, Ltd
Factors Influencing the Course of Opiate Addiction
N. SCHERBAUM, M. SPECKA
Department of Addictive Behaviour and Addiction Medicine/Addiction Research Group at the Department of Psychiatry and Psychotherapy, Rhine State Hospital Essen, University Duisburg-Essen, Essen, Germany

(To Read Document) 
CLICK ON  Download File  BELOW

---

factors_opiate_abuse.pdf
File Size:	145 kb
File Type:	pdf

Download File

---

---

'Why Opioid Dependence Is a Disease'
------------------------------------------------------------------------------------

Opioid dependence is a
chronic brain disease caused by complex, long-term, changes in the structure and functioning of the brain. The significant changes to brain "circuitry" common to opioid dependence have led physicians to classify it as a disease that interferes with normal brain functioning.

Most brain diseases are linked to a distinct behavioral symptom—for example, Alzheimer's disease is linked to memory loss, schizophrenia is linked to mood changes, and opioid dependence is linked to compulsive opioid use.

While a portion of opioid-dependent patients may have elected to misuse opioids at some point, this does not mean their condition is not the result of disease. Consider the following:

   #1. Many chronic diseases either begin or are made worse by (or both) patients' choices—for example, decisions about diet and exercise directly contribute to such common illnesses as high blood pressure, heart disease, and diabetes.
 
   #2. Regardless of whether patients' opioid use may have begun willingly, once opioid dependence takes hold, drug use is no longer voluntary.
 
   #3. Although opioid dependence is preceded by repeated use of higher and higher doses of opioids, opioid use is actually only one of several factors that causes this disease—opioid use will not "become" opioid dependence all by itself.
 
Compulsive drug use
Opioid cravings and opioid withdrawal are both very powerful drivers of drug seeking and use. However, only opioid cravings are tied to compulsive drug seeking and use. Furthermore, the intensity of cravings can drive compulsive opioid use even though a person is not physically dependent on opioids and is not experiencing any withdrawal symptoms.

Cravings also seem to be one of the last symptoms of opioid dependence to go away completely. This persistence is most likely a reflection of the time needed for the brain to heal itself and restore some degree of pre-disease normalcy. Opioid cravings can occur months and even years after a patient's last opioid use. Their suddenness and intensity can put patients' at risk for relapse.

Why Opioid Dependence Affects Behavior
In addition to the reward circuit, the brain has other ways to help ensure its survival. For instance, in response to a threat, survival is always the brain's No.1 priority. In a crisis, certain sections of the brain "take over." This is the origin of the "fight versus flight" response as well as the drives for sex and food, among other things.

The behavioral changes seen with opioid dependence may be explained by the result of a combination of different influences.
One of these factors may be the brain's "belief" that opioids are
related to survival. Another point to take into account is that, by the time a person develops opioid dependence, his or her brain can no longer function normally without opioids.

Under these circumstances, the motivation to obtain opioids comes from 3 places:

• Physical pain and discomfort caused by withdrawal symptoms
• Increasing anxiety due to powerful, unsatisfied opioid cravings
• Stress resulting from the brain's fear that the current lack of opioids presents a threat to its survival
  

Regarding this last point, even though, logically, a person may know that opioids are not essential for life, as long as those parts of the brain in charge of survival behavior still believe opioids are necessary, they may override "higher reasoning." Furthermore, to an opioid-dependent brain, not having enough opioids to satisfy cravings or suppress withdrawal is comparable to not having enough food to satisfy hunger.

The need to obtain opioids can become more important than that person's safety because opioid-dependence can impair the mechanism by which information from certain areas of the brain—namely, those involved with judgment and caution—is received. The brain responds by taking whatever steps are necessary to see that its opioid "hunger" is met, which usually means pursuing opioids with all the drive of a basic instinct.


Source: www.suboxone.com

---

       ENDORPHINS & OPIATES:          Effects On The Human Brain

In 1972, brain researchers from Johns Hopkins University made a puzzling discovery that  would illuminate scientists' understanding of addiction.

They found that the human brain's neurons had specific receptor sites for opiate drugs: opium, heroin, codeine and morphine.

But then there was the  obvious question:
   
Why would nature put in our brains a receptor for a plant?

After all, humans beings didn't evolve over millions of years eating opium or shooting heroin. The scientists reasoned there must be some other function for these receptors sites. They soon figured out that the active ingredient in all these opiates - morphine - had a chemical structure similar to endorphins, a class of chemicals present in the
brain . Endorphins are feel-good chemicals naturally-manufactured in the brain when the body experiences pain or stress. They are called the natural opiates of the body.

Endorphins flood the space between nerve cells and usually inhibit neurons from firing, thus creating an analgesic effect. On a lower level they can excite neurons as well. When endorphins do their work, the organism feels good, high, or euphoric, and feels relief from pain [analgesia]. Logically, endorphin levels go up when a person exercises, goes into labor, or is stressed out. Although they seem to be triggered by stress, endorphins can do more than relieve pain, they actually make us feel good.

Like an evil twin, the morphine molecule locks onto the endorphin-receptor sites on nerve endings in the brain and begins the succession of events that leads to euphoria or analgesia.

This imposter is more powerful than the body's own endorphins because the organism can actually control how much of the feel-good chemical hits the brain. Since we are all pleasure-seeking organisms, the motivation to self-administer such a drug is easy to understand.

The drawback, of course, is addiction.     
                                                                                                                       source: pbs.com

---

Obama Administration's
National Drug Control Policy (ONDCP)

Prescription drug abuse is the Nation’s fastest-growing drug problem. While there has been a marked decrease in the use of some illegal drugs like cocaine, data from the National Survey on Drug Use and Health (NSDUH) show that nearly one-third of people aged 12 and over who used drugs for the first time in 2009 began by using a prescription drug non-medically. The same survey found that over 70 percent of people who abused prescription pain relievers got them from friends or relatives, while approximately 5 percent got them from a drug dealer or from the Internet. Additionally, the latest Monitoring the Future study—the Nation’s largest survey of drug use among young people—showed that prescription drugs are the second most abused category of drugs after marijuana. In our military, illicit drug use increased from 5 percent to 12 percent among active duty service members over a three-year period from 2005 to 2008, primarily attributed to prescription drug abuse.
  Although a number of classes of prescription drugs are currently being abused, this action plan primarily focuses on the growing and often deadly problem of prescription opioid abuse. The number of prescriptions filled for opioid pain relievers—some of the most powerful medications available—has increased dramatically in recent years. From 1997 to 2007, the milligram per person use of prescription opioids in the U.S. increased from 74 milligrams to 369 milligrams, an increase of 402 percent. In 2000, retail pharmacies dispensed 174 million prescriptions for opioids; by 2009, 257 million prescriptions were dispensed, an increase of 48 percent. Further, opiate overdoses, once almost always due to heroin use, are now increasingly due to abuse of prescription painkillers.
 These data offer a compelling description of the extent to which the prescription drug abuse problem in America has grown over the last decade, and should serve to highlight the critical role parents, patients, healthcare providers, and manufacturers play in preventing prescription drug abuse.
  These realities demand action, but any policy response must be approached thoughtfully, while acknowledging budgetary constraints at the state and Federal levels. The potent medications science has developed have great potential for relieving suffering, as well as great potential for abuse. There are many examples: acute medical pain treatment and humane hospice care for cancer patients would be impossible without prescription opioids; benzodiazepines are the bridge for many people with serious anxiety disorders to begin the process of overcom- ing their fears; and stimulants have a range of valuable uses across medical fields. Accordingly, any policy in this area must strike a balance between our desireto minimize abuse of prescription drugs and the need to ensure access for their legitimate use. Further, expanding effective drug abuse treatment is critical to reducing prescription drug abuse, as only a small fraction of drug users are currently undergoing treatment.
 This Prescription Drug Abuse Prevention Plan expands upon the Administration’s National Drug Control Strategy and includes action in four major areas to reduce prescription drug abuse: education, monitoring, proper disposal, and enforcement.
   1.) Education is critical for the public and for healthcare providers to increase awareness about the dangers of prescription drug abuse, and about ways to appropriately dispense, store, and dispose of controlled substance medications.
   2.) Enhancement and increased utilization of prescription drug monitoring programs will help to identify “doctor shoppers” and detect therapeutic duplication and drug-drug interactions.
   3.) The development of consumer-friendly and environmentally responsible prescription drug disposal programs may help to limit the diversion of drugs, as most non-medical users appear to be getting the drugs from family and friends.
   4.) It is important to provide law enforcement agencies with support and the tools they need to expand their efforts to shut down “pill mills” and to stop “doctor shoppers” who contribute to prescription drug trafficking.

                           To Read The Official II-Page Document
                           DOWNLOAD FILE Below (PDF FORMAT)

---

Epidemic: Americas RX Abuse Crisis 2011.pdf
File Size:	313 kb
File Type:	pdf

Download File

---

---

---

questions? concerns?
confused?

If You Have Any Questions Contact Me Below

---

---

~A REAL-LIFE LOOK AT AMERICA'S #1 GROWING EPIDEMIC:
PRESCRIPTION DRUG ABUSE~

---

ad⋅dic⋅tion

*ARE YOU ADDICTED TO RX PAINKILLERS AND/OR HEROIN?
*
*HAS IT BEEN YEARS AND YOU ARE T I R E D  OF THIS NIGHTMARE? 
*
*TRIED TO STOP BUT SCARED OF BEING SICK?
*
*DO YOU WORK/SCHOOL AND IN-PATIENT IS OUT THE QUESTION?
*
*DO YOU DREAM OF BEING 'NORMAL' AGAIN?
* 
HELP IS OUT THERE - YOU ARE NOT ALONE.

---

~ Timeline Of Opioid-Addicts: Same Problem, Different Faces ~

The C h a n g i n g  F a c e of 
Opioid Addiction

*The size and composition of the U.S. opioid-addicted population
began to change in the early 20th century with the arrival of waves of European immigrants. Most users of opioids were young men in their 20s: down-and-outs of recent-immigrant European stock who were crowded into tenements and ghettos and became addicted during adolescence or early adulthood. They often resorted to illegal means to obtain their opioids. 
 
*The initial treatment response in the early 20th century involved prescribing short-acting opioids. By the 1920s, morphine was prescribed or dispensed in treatment programs. 
 
*Addictive use of opium, cocaine, and heroin, along with drug-related crime, especially in urban communities, increasingly concerned social, religious, and political leaders. Negative attitudes toward, and discrimination against, new immigrants probably influenced views of addiction. Society‘s response was to turn from rudimentary forms of treatment to law enforcement. 
 
*Another major change in the U.S. opioid-addicted population occurred after World War II. As many European immigrants moved from crowded cities, Hispanics and African Americans moved into areas with opioid use problems, and the more susceptible people in these groups acquired the disorder. 
 
*The post-World War II shift in the composition of opioid-addicted groups coincided with hardening attitudes toward these groups. 
 
*By the 1980s, an estimated 500,000 Americans used illicit opioids (mainly heroin). Although this number represented a 66-percent increase over the estimated number of late 19th-century Americans with opioid addiction, the per capita rate was much less than in the late 19th century because the population had more than doubled. Nevertheless, addiction became not only a major medical problem but also an explosive social issue. 
 
*By the late 1990s, 898,000 people in the United States used heroin, and the number seeking treatment was approximately 200,000 (almost double the number during the 1980s).

*Year 2000, The abuse of prescription opioids was a growing concern.
Treatment admission rates for addiction to opioid analgesics more than doubled between 1992 and 2001, and emergency room visits related to opioid analgesic
abuse increased 117 percent between 1994 and 2001.
 
. . . To Be Continued. . .

---

---

DRAMATIZATION OF METHADONE KICKIN ADDICTION'S ASS

Any QuEsTiOnS???

---

tolerance, addiction & pain.
by K. Trout

Originally Published at Opioids.com
archived by erowid September 2001

"Millions of people suffer needlessly from agonizing pain because physicians have been reluctant to use ‘high-risk' opioids"
Crain & Shen 2000

"The first thing they told us in medical school is that no one has ever died from pain but plenty of physicians have had theircareers destroyed trying to help people who are in pain."
Comment from an emergency room physician requesting anonymity (2001)

  A major problem faced by narcotics users and ed by narcotics users and abusers is the well-known development of tolerance when an opiate is given repeatedly over a period of time. This is directly responsible for a number of the problems associated with narcotic use and abuse since increasing tolerance requires that steadily larger doses be used to achieve the same effects or degree of pain relief.

This also underlies much of the crime associated with street addiction as the cost of maintaining a habit also escalates along with the dosage, often leading addicts to turn to drug dealing, prostitution or criminal activities to enable them to afford their daily dose.

Many experienced junkies, especially if heroin users, address this problem by taking regular breaks from their drug of choice, allowing their tolerance to diminish and their effective dosage to also be decreased. Due to the unpredictable quality of unregulated black-market street drugs this can actually be potentially dangerous if they then acquire material of greater potency than they were expecting. (Junkies who relapse after recovery face a similar risk when they return to use.)

Some users employ materials like cimetidine (Tagamet) [R.A.H. 2000] to retard drug metabolism and thereby maximize their effectiveness. [An interesting but unrelated point worthy of further investigation is the report of Peterson et al. 1983 indicating that use of cimetidine one hour before and after administration of large amounts of cocaine to rodents prevented hepatic toxicity and liver damage. Pellinen et al. 1994 also reported a prevention of "metabolism-related hepatotoxicity" by use of Cytochrome P450 3A inhibitors.]

Other users recommend grapefruit juice (Anonymous 2000) to interfere with the metabolism of the opiates by the liver and small intestinal Cytochrome P450 enzyme CYP3A and thus attempt to maximize their per dose effects, blood concentration and duration. While this has been reported by many users to be effective at maximizing per dose results this does not affect the development of tolerance.

Presently many questions remain, as there is also been some conjecture made that administration of grapefruit juice might interfere with the conversion of codeine to morphine due to its lesser inhibition of some CYP subfamilies. This does not seem to be the case; Caraco et al. 1996 reported (in animals) that if codeine was coadministered with selective inhibitors of CYP3A4 this could result in increased morphine production and enhanced effects due to "shunting into the CYP2D6 pathway" (as CYP2D6 would NOT be affected).

It is worth noting that I can thus far locate NOTHING in the *scientific* literature specifically supporting the use of grapefruit juice to increase the general effectiveness of opiates or even that CYP3A is responsible for the metabolism of heroin. Although, it is certainly reasonable to assume that CYP3A is responsible for its metabolism since it is proven as such for other opioids such as codeine (Caraco et al. 1996) and fentanyl (Feierman & Lasker 1996)

Reports of successful application, circulating orally among users (Anonymous 2000 & 2001) and posted on web-based bulletin boards, are common enough that this should be investigated further.

It is important to keep in mind that grapefruit juice can also prove problematic due to the elevated levels of bioavailable drug, requiring a reduction of the dosage. Sometimes it can even be dangerous if certain other drugs are being used. The combination of grapefruit juice with some specific pharmaceuticals has produced many serious problems and even some deaths. (Ameer & Weintraub 1997; Dresser et al. 2000)

Another practice reportedly employed by some narcotic users is combining hydroxyzine with opiates to potentiate their effects. This is said to produce a rough doubling of intensity with the addition of unwanted side effects like a dry mouth. [Anonymous 2000] It appears to have no effect on the development of tolerance.

An interesting approach is the combination of opiates with the opiate antagonists naloxone or naltrexone in miniscule amounts. The combination of less than 0.001% of what would be a normal dose of the antagonist with an opiate allows a far greater response ("at least 50%") to the opiate which in turn permits a much lower effective dose to be used. It is also said to prevent respiratory depression, tolerance and addiction. This approach has apparently been patented (Crain & Shen 1996) and is being commercially developed by Pain Therapeutics. [R.A.H. 2000; Crain & Shen 2000]

Another interesting comment was made by Karl Jansen (2001) concerning the administration of small oral doses of ketamine being found to be of use in chronic pain clinic for "greatly reducing" the development of tolerance (via blockade of NMDA receptors).

However, many people are unaware that both enhanced effectiveness of narcotic analgesics AND prevention or reversal of tolerance is readily achievable through the oral use of up to 200-250 mg of Proglumide [(DL)-4-Benzamido-N,N-dipropylglutaramic acid]. [See Ott 1999; Watkins et al. 1984]

The work of Watkins suggests there may be a therapeutic dosage window with diminished results above it but more detailed work to define this is apparently lacking.

Rather than simply augment the action of the opiates, proglumide actually interferes with the anti-opioid activity of the neuropeptide CCK.

The chronic administration of opiates, or spinal cord and other CNS injuries, elevates the level of Cholecystokinin (CCK) that is present. Such elevated levels exert an antagonistic effect on opioid activity resulting in significantly diminished analgesic effects. (Watkins et al. 1984; Xu et al. 1993 & 1994)

It is this rise in CCK levels that directly leads to the condition known as drug tolerance and the corresponding increase in its anti-opioid activity that requires the opiate user to use increasingly larger amounts to achieve the same effects.

This anti-opiate effect can be prevented or even reversed through the administration of CCK inhibitors such as proglumide. (Watkins et al. 1984)

Besides just interfering with the adverse action of CCK on opiate activity, proglumide is also known to augment the analgesic effect of opiates. Often this can provide a higher quality of analgesia for those patients who suffer from an incomplete response to pain medications.

Watkins & coworkers reported that proglumide reversed morphine tolerance and also:
 1) hastened the onset of analgesia
 2) increased the peak levels
 3) prolonged the duration.

They suggested that not simply did this indicate that effective narcotic doses could be decreased but it also indicated that proglumide might be able to enhance the effects of other procedures, such as acupuncture, which involve endogenous opiates. (Watkins et al. 1984)

Proglumide is a nonselective CCK inhibitor that was formerly employed as an anti-ulcer medication (Hahne et al. 1981). It shows NO analgesic effects of its own.

Although proglumide is now considered to be an obsolete pharmaceutical due to changes in our understandings of ulcer etiology, it has already seen extensive pharmacological and toxicological testing proving its safety and has been approved for use in humans.

It has largely fallen into disuse but is still available in bulk via chemical houses or as a pharmaceutical in Europe and Africa sold under the trade name Milid and Milide.

Other CCK inhibitors show similar properties (Idänpään-Heikkilä et al. 1997; Xu et al. 1993). However, beyond simply having seen previous use in humans, proglumide is both inexpensive and nontoxic. (Ott 1999)

Proglumide is not some sort of magic bullet for completely eliminating the risk of tolerance development and addiction as its effects are only effective for a limited duration before tolerance to IT begins to develop. (After 8 days its effectiveness begins to wane) The work of Kellstein & Mayer 1990 suggests that successful therapeutic/maintenance applications will probably require its discontinuation for a week after each week of use. More work is needed to better define the precise parameters of its effective use for this purpose.

Despite this, proglumide has already demonstrated itself to be of value both in pain management and as an adjunct to maintaining a narcotic addiction within a larger program of harm reduction (Anonymous 2000; Ott 1999).

What is fascinating is how few drug educators, drug treatment facilities or even drug users are aware of this despite it being readily available information for nearly 20 years.

If development of tolerance and the high price of a sustained addiction are truly as serious of a problem as we all agree that they are, one can only wonder how it is that, despite the tools existing to remove or at least reduce this problem, there seems to be no interest or research except on a limited scale related to specific small areas of chronic pain management and understanding.

The current misguided approach of substituting methadone is commonly reported to actually cause MORE perceptual and thinking problems than the opiates it replaces PLUS methadone is known to cause physical damage to internal organs that are not encountered with opiate use itself.

Harm reduction approaches would benefit greatly by using proglumide as a cornerstone and making it readily available to both narcotic users and abusers.

Those who will most certainly object include organized crime and drug dealers who enjoy the obscene profits reaped from escalating drug tolerances, and possibly also the so-called "drug educators" that sadly often seem to be the ones most in need of some factual education.

There are many problems associated with opiate use and abuse. While the majority of these are legal in origin, the most sensible approach would be to ameliorate [or mitigate] those that aren't.

Increased analgesic effectiveness and prevention of tolerance are two obvious areas where harm reduction is readily possible TODAY. Both sufferers of chronic pain and narcotic addicts stand to benefit from having their needs met and their health risks simultaneously decreased.

As this is first and foremost a health problem, the current approach of harm maximization is both counterproductive and unacceptable. To a rationale or caring mind it might even be perceived of as unethical and amoral.

Not only do sufferers of chronic pain and narcotic addicts stand to benefit from such harm reduction approaches but, by decreasing drug-associated crimes, a significant area of the true "drug problem" can be directly addressed, thereby benefiting society as a whole.

---

F.D.A. to Place New Limits On Prescriptions of Narcotics

---

Text:  COPYRIGHT 2009
 The New York Times Company
Pg.158.54582 (Feb 10, 2009): p(L). (684 words)
 
 Many doctors may lose their ability to prescribe 24 popular narcotics as part of a new effort to reduce the deaths and injuries that result from these medicines' inappropriate use, federal drug officials announced Monday.
  A new control program will result in further restrictions on the prescribing, dispensing and distribution of extended-release opioids like OxyContin, fentanyl patches, methadone tablets and some morphine tablets.
   These products are classified as Schedule II narcotics and already are restricted according to rules jointly administered by the Food and Drug Administration and the Drug Enforcement Agency. But the current restrictions have failed to ''fully meet the goals we want to achieve,'' said Dr. John K. Jenkins, director of the F.D.A.'s new drug center.
  ''What we're talking about is putting in place a program to try to ensure that physicians prescribing these products are properly trained in their safe use, and that only those physicians are prescribing those products,'' Dr. Jenkins said in a news conference on Monday. ''This is going to be a massive program.''
Hundreds of patients die and thousands are injured every year in the United States because they were inappropriately prescribed drugs like OxyContin or Duragesic or they took the medicines when they should not have or in ways that made the drugs dangerous. The agency has issued increasingly urgent warnings about the risks, but the toll has only worsened in recent years.
   The blame for this is shared among doctors who prescribe poorly, patients who pay little attention to instructions or get access to the medicines inappropriately, and companies that have marketed their products illegally.
    The F.D.A. this year will hold meetings with manufacturers, patient and consumer advocates, and the public to ask for advice on how to carry out the new control program, officials announced. The first meeting will be on March 3, and no immediate changes in access to the drugs is planned.
   The 24 medicines under review had 21 million prescriptions written for them in 2007, to 3.7 million patients, Dr. Jenkins said. They are extremely effective in reducing pain, which many medical studies suggest is widely undertreated in patients suffering serious illness. (A complete list of the drugs is at fda.gov/cder.)
   But many doctors prescribe the drugs far too cavalierly, Dr. Jenkins said. The F.D.A. has received reports of patients' being prescribed such medicines to treat something as simple as a sprained ankle, he said. In such patients, the medicines can be dangerous.
   Part of the problem is marketing. Several reports, for instance, have suggested that Purdue Pharma, the maker of OxyContin, helped fuel widespread abuse of the drug by aggressively promoting it to general practitioners not skilled in either pain treatment or in recognizing drug abuse.
   The company has denied such a connection, but a holding company connected with Purdue and three top Purdue executives pleaded guilty last year to criminal charges that the company had misled doctors and patients by claiming for five years that OxyContin was less prone to abuse because it was a long-acting narcotic.
   Doctors are also to blame. A common reason for disciplinary actions at state medical boards is the use of narcotics in patients who show clear signs of addiction or for whom the drugs are obviously inappropriate.
   The F.D.A. generally avoids interfering with the practice of medicine because doctor behavior is governed by state medical boards. Instead, the agency usually tries to provide doctors with the best and most current information, and then allows them to decide how to use it.
   Most of the drugs withdrawn over the last 20 years, however, were taken off the market because doctors continued to use the medicines in ways that the F.D.A. warned against.
   For decades, the agency's armory in these battles held only a popgun and a cannon -- the popgun being the issuance of widely ignored warnings; the cannon being its ability to force a medicine's withdrawal. But a law passed in 2007 gave the agency a new, intermediate weapon -- Risk Evaluation and Mitigation Strategies. Known as REMS, these programs allow the agency to place strong restrictions on the distribution of certain drugs.

source:

---

---

---

---

Who woulda ever known
that  "Normal'  would end up being
the
'Ultimate' High...
I  guess  s o m e t i m e s ,
in order to T R U L Y
appreciate what we have;
We Must First Suffer Thru,
and
Be   D e v a s t a t e d  By
the Loss Of It.  
                                                KD Slattery

---

Disclaimer:  The contents of OpioidAddiction.weebly.com/HALO inc. are for general informational purposes only and are not intended to substitute for professional or medical evaluation,  diagnosis, treatment, or advice. Users of this site are encouraged to contact your professional healthcare provider for medical assistance regarding addictive disorders, general health problems, mental health problems, and any & all health-related questions.