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Thursday, September 23, 2010

4.(4-5) Pain? Recreational Drugs?

Physician's Notebooks 4  http://physiciansnotebook.blogspot.com - See Homepage

Two Chapters - Pain (& Pleasure) and Drugs for Recreation (For marijuana, opioids, LSD, et al, scroll down to Chapter 5) Update: 11 September 2021. (Note the high interest as expressed by the relatively high number of clicker-on hits.)

Chapter 4. Pain
The following column has main topics as they appear.
Types of Pain
Medication for Pain
Pain Management 
Endorphin Pleasure
End Note:  Principles of Anti-pain Medication

Once you convince yourself a pain is harmless to your health and life, it tends to become tolerable and may even disappear. And a pain that excites your fear of deadly diagnoses even if it does not limit your movement will torment you and may become chronic even when minor. That is the psychological overlay of pain; it is a top-down nervous system effect; the raw pain is a bottom-up effect, the bottom being the pain stimulus and the top is from the cerebral cortex that dials up or down the raw emotional response making it stronger or weaker depending on its threat to your survival and its limitation on your life. An example is the soldier in combat being shot by a bullet in the leg and not feeling its pain  because it means a non lethal relief from combat while, on the other hand the same soldier if he got the bullet in same spot in non-combat would feel it badly.
  Types of Pain (Not Inclusive but Typical Pains I've Experienced)
   A sharp electric shock-like pain that runs down the back or extremity and is worsened by cough or sneeze is an irritated spinal root. If you must see an M.D. for such pain, arrange a consultation with a neurologist in a University-HMO (Health Maintenance Org in U.S.A. or large hospital outpatient). Often in case of shooting pain down the back and into back of leg (sciatica) the cause is obvious (accident, too heavy lifting). It is worsened by starting movements (I call it "Tin Man" effect from the Wizard of Oz scene where the tin man needs to be oiled after a long lack of oiling and it takes time for the oil to loosen him up enough to move.)
  Sore or irritated feeling around certain joints – one or other shoulder, wrist, especially wing bone (scapula) may indicate important internal organ disease. Such pain in left shoulder or left wrist ought to lead to a heart check up. With one-sided hip pain, think Collapsed lumbar vertebra from osteoporosis or Osteoarthritis of hip. If a woman, think of a pelvic organ problem.
   Pain coming from a blocked tube in abdomen has as its most characteristic quality its wavelike pattern, building up to peak and letting-up over a minute with pain-sharp free interval. The pain lasts as long as it takes the tube to get rid of its blockage, usually a small kidney stone that dislodged into the ureter. One type is renal colic; it is one-sided, each spasm starts in upper rear flank and rapidly goes around side of abdomen down into groin and lets up and new spasm builds up after painless minute. The type from intestinal colic occurs in the hour after eating. It goes from above downward and from your right to left, following the intestine contents passage. It is caused by movement of bowel contents and ends in a good bowel movement but, briefly, it can be rather severe. If intestinal cramp is too painful, or has nausea and vomiting, get to hospital emergency; it may be surgical abdomen.
  Pain from cancer is usually dull and continuous; it has emotional overlay as warning of dying.
   Two types of similar feeling pain with great differences in implication can be felt in the toes and usually symmetrical (right and left equal). It is a sore pain worsened by banging the toes. It can be due to neuropathy (from damaged nerve or spinal root irritation) or ischemia (from poor circulation of blood into lower extremities). Ischemic pain is not good news because it presages skin ulcers, loss of toes and the like. Ischemic pain is worsened by activity.  Neuropathic pain is due to hyperpathia, an excessive reaction to pain stimulus because of pressures on the nerves; it does not have a poor prognosis and stays stable in older persons with vertebrae collapse. I`ve tolerated it for the last 2 years.
Medication for Pain
  Medication for muscle, joint, bone and soft tissue pains should start with headache-dose (300-325mg) acetaminophen or aspirin (but note not to use aspirin if at high risk for bleeding or peptic ulcer), and with severe pain the secret of success is starting the max dose (500 mg acetaminophen aka Tylenol, and limit each to max 2 a day, timed conveniently). But keep in mind before blindly medicating a pain to reasonably determine the cause. And avoid the other NSAIDs; stick to acetaminophen but, if you want to try a NSAID, ibuprofen max dose 800 mg is best because of highest safety profile.


   Warning!  Avoid places that advertise Interventional Pain Management. These are usually non medically controlled, commercial "clinics" with a hired staff of doctors or osteopaths who will write "scrip" for narcotics or popular mind-bender medication or, even worse, will subject patients to invasive procedures like corticosteroid injections or even nerve ablation surgery.
Endorphin Pleasure
   A note about pain's opposite: pleasure. The word "endorphin" is used for chemical substances that cause pleasure and also for a type pleasure typically noted by first user of opioids. Endorphin pleasure may result from a good eating and one should note what foods and circumstance caused the feeling. It is more generalized, felt just beneath skin, at times described as a bubbling-up pleasure centered in navel,  breast nipples, and joint surfaces like knees and elbows. Warmth enhances the endorphin effect. (Sunlight on abdomen) For example, even in late April with the outside temperature moderate (23 degrees C or 70F) in Tokyo and no need for indoor heating, I notice my endorphin pleasure from a dose of opioid enhanced by direct sunlight heat. Light in eyes seems to enhance painful effects and oppose endorphin effects. A darkened, warm room is the best room condition for enhancing body pleasure and opposing pain. (This, despite the observation, that direct sunlight can enhance endorphin feeling)

End Note:  Principles of Anti-pain Medication
Anti-pain medication either reverses the cause of the pain (e.g., anti-inflammatory reverses inflammation, anti-spasm reverses the spasm) or is just general against pain (like opioids). The most useful pain medications are the anti-inflammatories. These divide into 2 types: cortico-steroids and Non-Steroid Anti-Inflammatory Drugs (NSAIDs). The cortico-steroids are used to reverse severe inflammation but they do not do anything quickly against the acute pain that came from the inflammation. On the other hand the NSAIDs are both anti-inflammatory and anti-pain and rapid acting (within minutes) and effective against the already existing pain of the inflammation. 
The NSAIDs are aspirin, acetaminophen and the standard NSAIDs. Aspirin and acetaminophen are not usually called NSAIDs although practically they are.        

The NSAIDs work best for pains from connective tissues like muscles, bones and other soft tissues that are damaged or irritated. When the pains come from muscles or bones they can be debilitating. In these cases an NSAID can be virtually life saving in terms of living a normal life. Aspirin has a special good and bad point. Its good: it affects the blood platelet aggregation in a way that weakens internal blood clots. But it also may cause hemorrhage in at risk persons and it may irritate the linings of the stomach and intestines. For a person who is taking aspirin already to prevent blood clot, the aspirin may be used in higher dose against pains. For persons who cannot use aspirin, the next choice is acetaminophen. And in its daily max 500 mg dose, it is safe, but persons who are at risk for liver disease (alcoholics) should avoid taking more than two a day 
Opioids are a general anti-pain medication which are not good against inflammation pain but useful against cancer pains. They work centrally. Medically they are safe but in countries where they have been criminalized, or too strictly regulated their use may create an addiction. The best NSAID is ibuprofen which as single dose is max up to 850 mg for most severe head, joint and bone/muscle pains.
Opioids should not be used (as they often are) in a combination pill with anti-inflammatories. If you are going to use 2 or more types of medication, each one should be sequenced (i.e., first take the anti-inflammatory and then an hour later the other type. Other pain medications fall into the category of anesthesia, analgesia, and anti-depression (general term “neuropathic”) medications that work against pain. Then there are special migraine headache medications. These have only specialized use under supervision of a physician.
End of Chapter

Chapter 5. Drug for Intellectual Work and for Recreation: Marijuana, Opioids, LSD & pschedelics, and other drugs of abuse.
Contents of the chapter in descending order.
Marijuana
Stimulants: Cocaine, the Amphets and  Methylphenidate (Ritalin)
LSD and other Hallucinogens aka Psychedelics
Club Drugs
Inhalants
Sedatives, Hypnotics, Anxiolitics, Tranquilizers
OPIOIDS  
Withdrawal 
Availability 
Opioid Addiction 
Pentazocine (P, trade name in USA, Talwin) 
The Stretch Effect 
Conditioning by Taste
Codeine 
OxyContin (OxyC) Slow Release 
Reason for Using Opioids 
fictional treatment of my morphine experiences  
Other Drugs or Behaviors of Abuse

Marijuana:  What are its positive features that cause it to be the most popular recreational drug?  Here a psychiatrist who interviewed pot-smokers details a cannabis "trip."  First users, 10 to 30 minutes after lighting up a "joint" start by noting a vague anxiety, like something evil will happen. (Best to have an experienced person there to reassure.) But within a few minutes (In repeated users, too.) that changes into euphoria, elation, exhilaration, a lightness of the body. One may laugh, talk a lot, and think what one is saying is witty or brilliant, but for others it is not. One gets hungry for munchies. Eyes get bloodshot. If a pot smoker is tested while on his trip, his immediate memory is poor and his thinking incoherent. By 2 hours after lighting up one gets drowsy, sleeps, and awakens feeling fine and with memory of what had happened to him during the trip.
This description though considered accurate comes from former days when marijuana was only smoked and when its potency was less than today.
   What is marijuana?  It comes from a hemp plant, Cannabis sativa that originated in Asia and was "discovered" (for Europeans) by Napoleon`s troops as the Egyptian recreational drug hashish  (a more powerful form) in the early 1800s. Later it spread to the Americas and was popularized by the US 1930s jazz musicians and go from there to 2021 when marijuana use is common and it is being legalized.
   What is the essence of marijuana, how is it prepared and how does it work?   A chemical, THC, is the psychoactive ingredient (like Morphine is the psychoactive ingredient of opium).  The potency of a marijuana dose (whether it be smoked, taken by vaporization or swallowed as a cookie, pill or capsule) is the percent of THC in the product.  The marijuana we are using in USA comes from the female plant. It is most strongly found in the resin (waxy secretion of plant) that covers the flowering tops and upper leaves of the plants. The concentration of THC has increased much over the years. Initially it ranged from 0.5 to 5%. but today in 2021 it is estimated to be at 7 to 14%. Originally in the US, marijuana was smoked as a "joint" like a cigarette.  But, today, some users take it by vaporization (Use of a vaporizer like you use for nose but in this case you inhale the vapor into the lungs). Smokers and vaporizer users typically inhale the smoke or vapor deeply and hold their breath to maximize the absorption of THC by the lungs. Also marijuana is being eaten as cookies or swallowed as capsules or pills, appropriately dosed. (Oral cannabis, as in baked goods, requires 2X to 3X as much as smoked cannabis for same effects.)  When marijuana is smoked or taken by vapor, it is absorbed into the blood within minutes, giving a rapid effect. Peak levels of THC are reached at 10 minutes and by 1 hour after taking your dose the levels have declined to 5 to 10% of initial dose levels.  When swallowed it takes 1 to 3 hours to enter the blood (To speed absorption, do it on an empty stomach) and so you have a delayed, lesser but more prolonged effect. Most heavy users in USA smoke up to 5 joints a day. (But most users are not heavy users.) But the interesting thing is that rather few users become chronic.  Most enter into it as teenager or age 20s, use it for a few years and then go off or use it intermittently.  So the addictive risk is low. The phenomena of tolerance (more you use, less it works) and withdrawal are less than with opioids.
   How is it working?  A natural cannabis chemical, anandamide (from the Sanskrit word, ananda, which translates as "bliss") , has been discovered in the human body and found to be most important in the lessening of anxiety in one`s natural state. THC mimics it.
   What are other good effects of marijuana?  It stimulates the release of dopamine, the neurotransmitter that is important in mediating pleasures and in muscle movement disorders. So it has been suggested as part of treatment for Parkinsonism. It lowers intra-ocular pressure and so is good against glaucoma.  It stimulates appetite and so is being used against various causes of anorexia and nausea (like terminal cancer).
   What bad points?  Various studies have associated marijuana use with schizophrenia and other psychoses but it is guessed that the drug-use is not causative but rather brings on the tendency for psychosis. (Also only in heavy, chronic users) In any case pre-psychotic personalities should not use it.  An important study from New Zealand that followed groups of marijuana users and non-users for 20 years individually found that persistent heavy marijuana users showed an average IQ decline (from pre-use level as adolescent to age 38) of 8 points of IQ.  And a 15-year follow up of 50,465 Swedish men reported that those who used M by 18 years of age were 2.4 times more likely to develop schizophrenia.  Related to this, childhood development has been found to be disturbed by teenage use of marijuana. (So parents beware!)
   Abrupt stopping of M by adolescents is reported to result in a withdrawal syndrome of insomnia, irritability, restlessness, drug craving, depressed mood, and nervousness followed by anxiety, tremors, nausea, muscle twitches, increased sweating, muscle aches and general malaise.  Typically, the syndrome begins 24 hours after last use, peaks at 2 to 4 days, and diminishes after 2 weeks.
   And, finally, marijuana should not be used within 24 hours of driving a car or operating a large machine.
Base on these results I do not advise recreational use of marijuana.

Stimulants: Cocaine, the Amphets and  Methylphenidate (Ritalin)
Cocaine is strongest with euphoria, and was popular in the drug culture. But its causing high blood pressure and the risk of acute myocardial infarct or brain stroke; the danger, expense and inconvenience of obtaining illegal, contaminated and denatured product; and cocaine’s effect to cause violent, irrational behavior – all are too high to pay for an effect you could get from a cup of strong caffeine coffee. The Amphets (&Methamphetamine) have replaced it because they are easy to synthesize in illegal home labs and therefore cheap; but they have the same problem.    MethylPhenidate (Ritalin) and the related Concerta and Adderall are used in attention-deficit hyperactivity disorder (ADHD) of children. Fashion models use it to stop appetite in order to lose weight and smoke-stoppers use it. Also, it is taken in order to up the IQ or other test score. As an adrenaline-like drug, its psychic effect is to focus the mind for task at hand, and to strengthen motivation and energy. I used MP in 2.5 mg dose up to twice a day. At high dose, MP produces toxic psychosis or hyper-manic state. Its most frequent early sign of overdose is hyper-talk. What I noted (For self experiment see in Section 4.3 Medication.) at 2.5 mg dose is that MP gave a few hours of high energy, like strong coffee. But I no longer use it, because the risk of blowing out artery in brain from sudden high blood pressure is not worth the caffeine-like effect.
Club Drugs are euphoriants that are undetectable in drinks and so are used in clubs on women for date rape. They include MDMA, GHB, Rohynpol and ketamine.

LSD and other Hallucinogens aka Psychedelics are natural and synthetic substances that produce hallucinations, loss of contact with reality, and an experience of expanded and heightened consciousness. Here we deal with class of drug that puts its user's mind out of control. The street purpose to take it is to experience a good, mind-expanding “trip.” As one who values controlled cognition above all else, I have no desire for psychedelic. Its danger is to make or worsen psychosis in borderline personality. I favor controlled experiments by scientists, and exploring possible uses in psychoanalysis, creative insight and in terminal disease. But note the use of LSD in an unauthorized experiment on Harvard undergraduates that included the later unibomber, Ted Kaczynski, and may have produced a localized psychosis causing him to psychotically act out his free-flowing anger by his unibombing. 
The following will detail specific Hallucinogens.
LSD (lysergic acid diethylamide) is the most famous because it discovery by Albert Hoffman in 1938. (He had no idea he was working on the most powerful  hallucinogen until he inadvertently tasted it and went on the first LSD trip.).  LSD happens to be very easy and inexpensive to make but it languished in obscurity until Timothy Leary at Harvard in the early 1960s realized its potential as a mind-expanding drug. From 1965 to 1969 there was the first peak of use mainly among the literati and cultured types who found it seemed to increase creativity and solve mental problems.  In fact much useful research was done on it then.  But its bad points soon became evident: a tendency to produce psychotic behavior like believing you could walk on air and ending up falling from high place, and like frightening hallucinations on the so-called "bad trips" and like a so-called "crystallized" type that left chronic users apathetic, lethargic and good for nothing. So the drug fell into relative disuse although most street persons had access to it cheaply. The minimal active dose is 25 micrograms (very tiny) usually distributed as "blotter acid" on soaked and dried blotter squares that are mouthed.  Each sheet contains as many as a few hundred squares; one square containing 30 to 75 micrograms of LSD is the usual chewed dose Action onsets within the hour, it peaks at 2 to 4, and lasts 8 to 12 hours. Users initially (1st hour) may note tremors, fast heart, sweating, blurring of vision and wide eye dilation (opposite of opioids which make pinpoint pupil). Sudden deaths have been reported. Following come the changes in consciousness: perceptions like colors become unusually brilliant and intense, music more emotionally profound, and smells & tastes heightened. Users claim to recover lost childhood or infant memories, and get feelings of religious and philosophic insight that have been described as a mystical ecstasy.  But there are also the unpredictable bad trips when psychotic behavior puts a user and friends in danger.
    Today LSD has been much replaced by other hallucinogens, starting with Phencyclidine (PCP; angel dust)  & ketamine, and MDMA (ecstasy, a methamphetamine with hallucinogenic action). There are also a number of natural hallucinogens that have cultural origins: Mescaline consumed as peyote “buttons” from the small blue-green cacti, Lophophora williamsii and L. diffusa; certain Morning Glory seeds (I. violacea, T. corymbosa from American tropics that are taken as a soup of the boiled seeds).  Psilocybin from Psilocybus genus mushrooms, large mushrooms P. cubensis (gold caps, can be easily grown at home and are advertised for that) and P. semilanceata (liberty cap) grows on lawns in Pacific NW.  The dried mushroom is eaten directly for LSD effects. And other plant sources. (Here is a vignette: A 22-y-o student with no prior psychiatric history presented to hospital with inappropriate mood and bizarre thinking. Nine days before, she had eaten 1 or 2 psilocybin mushrooms.  Immediately following the eating she began to giggle, became euphoric and developed auditory hallucinations and belief in her ability to broadcast her thoughts to the media (Typical schizophrenic!). Two days after the first eating of the mushrooms she repeated it, and then continued to exhibit psychotic symptom to the day she came to hospital. She claimed to hear voices telling her she could be president and reported hearing "lambs crying", and continued to giggle inappropriately.  She was treated with an anti-psychotic and lithium and her symptoms abated after 5 days and she has been normal since.)
   On the good side psilocybin has been reported to be helpful in reducing morbid anxiety about death and dying.  And many persons with the experience maintain that a single experience with LSD has given them creative capacity, new psychological insight, relief from neurotic or psychosomatic symptoms, or a desirable change in personality (which is the ideal of psychoanalysis). Clearly more research is needed, especially on dose and repeated usage effects.
The treatment of a bad trip is for an experienced therapist or a friend to “talk the tripper down” with words of reassurance and comfort often taking up to an hour. Trips may last for hours to almost a day and sometimes the experience returns as a flashback, usually unpleasant.

Club Drugs are euphoriants that basically depress the CNS.  They are tasteless and odorless and so lend themselves to being slipped into a woman’s drink for date rape. They include the previously mentioned MDMA (Ecstasy), GHB (gamma hydroxybutyric acid), Rohynpol (a benzodiazepine), and ketamine, a former anesthetic. Such use is outlawed and will get one who is caught using it a jail sentence.

Inhalants used & abused for recreation are 1) solvents for glues and adhesives, 2) propellants (e.g., for aerosol paint or hair sprays, and shaving cream), 3) thinners (e.g., for paints and correction fluids, and 4) fluids (e.g., gasoline, propane).  Not included are anything you smoke (e.g., marijuana, tobacco) although they are also abused, and dangerous inhalants that do you not make for a long, halth life and should never be started or stopped forthwith. (I went cold turkey with tobacco and it was easy. I just used my own cognitive method, i.e., thinking of me dead in bed after a gasping last 10 years on an oxygen mask and canister.
  Inhalants are mainly used by kids and the homeless because easy to get and almost cost nothing.  They’re sometimes combine with plastic bags over the head ( way to suicide). They give periods of euphoria but have terrible side effects on all the vital organs.  If you catch your kid using one, stop him or her by force majeur if you can.

Sedatives, Hypnotics, Anxiolitics, Tranquilizers:  Today, the benzodiazepines (Any med ending in -pine, -p(h)am. or -ium is a benzo) top the list among barbiturates (any med ending in -al) and bromides and other psychoactives that are used for tranquilizing effect. All can be used as sleeping pills. My experience is that phenobarbital is too slow and long acting to have good sedative effect. For sleep, seconal (reds) or pentobarbital (Yellow jackets) are best (standard single pill or cap lowest dose).  I am finding the popular flurazepam (dalmane) 15 mg useless as tranquilizer, and see my comments on it under sleep medicine. Valium and Librium (You must titrate their dose best for yourself.) and Ativan (Lorazepam) is seen by my patients to be the most useful.  Again, lowest dose pill or cap) Also note that the benzodiazepines are infamous causes of poor memory, especially worsening anomia (difficulty recalling a popular name) in older persons.
Other Drugs or Behaviors of Abuse like Caffeine, Tobacco or Gambling are well dealt with in the latest, 12th Ed. Of Kaplan and Sadock’s Synopsis of Psychiatry (2021).

OPIOIDS

Opium has been used medically for thousands of years. It comes from the poppy flower. Its fruit is small berry-size and -shape with edible seed at center. Small incisions in the immature fruit allow collecting and drying of white juice, which clots and turns black. Raw material is formed into lump, cake or brick that may be powdered.
Raw opium may be brewed as drink or smoked in pipe. Early medicinal forms are laudanum (alcoholic tincture of opium) and paregoric (tincture of opium spiced with camphor) for diarrhea.
   Morphine is the active chemical in opium into which other opiates are converted in the body, and it was isolated as chemical in 1806, followed by the closely structured codeine and heroin.
   Opiate is natural opium derivative and includes morphine, codeine, heroin, hydrocodone, oxycodone.“Opioid” now dominates the language. Originally, it meant synthetic drug that gave morphine effect. Now, it is any drug that shows a morphine effect and includes natural opiate and synthetic.

  Warning Note. Because of the great controversy that has surrounded the use of opioids, there is a tremendous amount of prejudice against their use especially in the United States and even in Japan. I am writing the below with the attitude of a scientist who is both a physician and someone who has used (and still using) opioids on myself since 1995 and is using opioids successfully now at age 88.  I ask you to keep an open mind and not necessarily to believe the received opinion in the U.S.A against the use of opioids. 

Effect: Data come from my experiences with injecting self with morphine or with pentazocine (Talwin in U.S.A.; and Sosegon in Japan). I also used oral pentacozine (now sosegon), di-hydrocodone (same as hydrocodone, oxycodone [Perco-dan & -set]) and codeine. I find small differences among them in effect, withdrawal and tolerance. A point ignored in books is the importance of dose. Morphine is famous for its sleep. (Named for God of dreams) But this comes from observation of  a high, 10 mg, dose when a patient is worn out by pain.  At start of use, before I became, as I now am, highly tolerant, self-injecting 3-mg, I noted within 2 minutes an alerting effect with high motivation to read, and it lasted an hour. Much data describing opioid effect comes from the reports of heroin addicts who overdose and are unreliable. And mention of morphine to alleviate pain emphasizes the importance of physical state in perception of effect. If one receives an opioid when wearied by pain, it is natural to fall asleep. But if one takes the same dose in non-sleep-deprived, healthy state it does not cause unpleasant sleepiness.
   Opioid tolerance is the gradually lessening effect for same dose and time schedule. Thus, for the main effect of endorphin pleasure and accompanying good feeling, a just-starting drug-user will notice the most effect and a long-time user the least. It depends on dose, and body chemistry of the user. In my many-year use of pentacozine at a daily 15 to 25 mg dose level it took 5 years before the pleasure effect was lost due to tolerance. This tolerance involved all pleasure effects and left me mainly with an anti-paranoid loss of anxiety and happy mentation but without the pleasure effects initially felt.
   As a new user without any tolerance effect, 2 minutes after injecting self with morphine 3 mg, or pentazocine 15 mg, or drinking hydrocodone 2.5 mg on empty stomach, in rested state, I noted relief of anxieties (the usual back-of-mind, disturbing worries most of us have). And I noted energy and a desire to do chores. At this dose the opioid is good for reading, movie watching, or quiet thinking. Endorphin pleasure starts on same time schedule. First felt in knees, ankles or wrists, then abdomen, chest, neck and head; the deep to skin pleasure is best for 20 to 30 minutes after the dose. With continued use, tolerance develops and a similar dose gives little deep pleasure although it continues to relieve anxieties.
   Another effect is that opioids give good patience to bear boredom by increasing the pleasure in solitary thinking. And, also, sought-after repose. Tolerance to this effect does not develop. Mucous membranes lose their sensitivity to stretch and irritability; therefore the irritable bladders of prostate sufferers may bw relieved. For a pentazocine injection, the various effects may satisfactorily continue at lesser intensity for an hour.
   Concerning repose and sleep, an opioid is not very effective except too high dose. One may experience pleasant lie-down twilight state.
   Constipation is well known. Codeine is most, it gives a mushy, poorly formed stool; oxycodone close second. I find pentazocine causes no constipation. (If constipation is severe, digital finger removal of stool from rectum is easy.)
   User of opioid will find losing weight or keeping slim easy. Opioids do not lower appetite; rather a dose makes you feel so satisfied that you find it easy to pass up eating. But if you are motivated to eat, it increases the pleasure of eating. Also, opioids can stimulate eating in clinically depressed persons as part of their anti-depression effect.
   Sexual: Common belief states that opioids may cause impotence and decreased sexual desire. This comes from street heroin addict who takes other drugs and overdoses. My experience at moderate dose is that opioid improves orgasm pleasure and does not affect lust or erection.
   User may notice itching of especially forehead. It did not bother me. Also a tendency for runny nose.
  Withdrawal:  Its description is affected by observations in heroin addicts and varies from the worst – “cold turkey” with shaking, kicks, goose-bump, screaming and shouting, body ache; to the least - a mild achy, depressed state. Withdrawal is dose related. Also, it shows cross tolerance, i.e., as long as one opioid continues to be taken, withdrawal from another will be mild or will not occur. This is the basis of the methadone treatment.
Withdrawing, I experience several-day muscle-ache worse in bed, and a longer abulia (lack of motivation). Most users are unknowingly self treating for depression, anxiety, or paranoia and when they stop medication the pre-treatment neurotic symptom returns. Withdrawal severity is related to daily dose. On hydrocodone, I found weaning down to daily 5 mg (2.5 mg in double daily session) eliminated my withdrawal muscle-ache and made psychological withdrawal mild, allowing caffeine to give motivation energy.
Availability:  In U.S.A., heroin is illegal and possession gets jail. Only a licensed and registered Medical Doctor with Drug Enforcement Administration (DEA) certificate can obtain and order morphine. And the doctor is under pressure to dispense or order morphine and similar opioid only for severe pain or as part of anesthesia. And must account for use in record, accessible to DEA.
   At lesser control are pentazocine, hydrocodone and under least control, codeine, which can be obtained and dispensed by licensed, certified M.D directly or by Rx (Doctor prescription) and may even be available OTC (no Rx) in cough syrups. If prescribing is excessive, records must be produced and explanation given. Easiest oral med from pharmacy via Rx with DEA number is codeine, hydrocodone and its like (Vicodin, Lortab, OxyContin). Relatively low level check is kept on the Rx drugs but every pharmacy checks a prescribing physician’s current DEA, license status and signature via computer before filling Rx.
   Opioid Addiction:  The key to addiction is difficult availability. Good analogy is to imagine if tomorrow the most popular anti-depression drug Prozac is declared illegal while other anti-depression drugs only are allowed under rigid limitation? We would create a new class of addict and criminal by removing a family of needed drugs.
   Criminalization of opioids and other drugs has consistently failed. In a nation with a more intelligent population than the U.S.A., like Switzerland or the Netherlands, opioids are legal and low cost by doctor Rx. Legalization of opioids would end gangster mob participation, markedly reduce political bribery corruption and lower all the medical complications presently seen with drug use. It would result in increased tax moneys, better social health and an improved society. I speak and write with authority as a physician with 30+ years of multiple opioid use and now at age 88 going strong and long, not despite using opioids but because I was lucky enough to obtain a legal, low-cost supply and used the drugs according to my and my treating physician’s medical knowledge. Nonetheless, although what I write is positive for my use of opioids it should be read in the context of my being a physician in Japan where opioids by prescription are not criminalized and are relatively easier to get than in the United States. I advise against using opioids in a place like the USA where it is criminalized and very hard to get legally because you will be creating a destructive addiction on yourself. (Even in a country like Japan which has a relatively relaxed attitude towards use of opioids; still, there is a strong prejudice against their use so that the situation is not so very different for the Japanese as the average American.)

Pentacozine (Sosegon in Japan) with which I have a many-year experience, has pleasing effect at low to moderate subcutaneous injection (not IV) dose (to 15 mg) but at higher dose produces dysphoria (bad feeling). This reduces effects of overdose and  limits addiction. Can be taken orally or injected, but its pill in U.S. has been mixed with a receptor-blocker naloxone hydrochloride (TALWIN NX contains in tablet, 50 mg equivalent pentazocine base and 0.5 mg equivalent naloxone base). Purpose of the mix is to prevent drug abuser from using crushed tablet powder to get injection high. Naloxone guarantees bad injection effect for opioid addict and no opioid effect for injection user. When taken as tablet by mouth, naloxone is said to be rapidly deactivated in stomach allowing pentazocine to have the usual oral mixed-opioid mu-/kappa-antagonist receptor effect. Another Talwin product is compounded with aspirin (TALWIN COMPOUND) or acetaminophen (TALCEN) neither of which is mixed with naloxone. In Japan, pentacozine is available as 25 mg Sosegon pill..
   Pentazocine is imperfectly absorbed by intestine, especially if mixed with food so that standard 25 mg swallowed tablet is equivalent to 15 mg IM injection dose. But note my use of sublingual (under tongue).
   Injection Pentazocine in U.S. is produced as TALWIN Injection 10 ml multiple dose vial, 30 mg P base per ml. It is a Schedule IV drug according to DEA regulation, which means it can only be obtained by state licensed, DEA certified physician.
   Pentazocine is advised as painkiller and potency is 30 to 60 mg injection equivalent to 10 mg morphine. In the mid to late 1990's I experimented by injecting myself  with pentazocine up to 15 mg on max schedule of once every 24 hr. My frequency use varied from once a day for months to none in recent years. For injection I used either the Japanese pentazocine product PENTAGIN, which came as single injection ampoule at 15 mg, 0.5 ml injection or the U.S. TALWIN Injection, using 15 mg, 0.5 ml injection, allowing me 20 injections per 10 ml vial.
   Injection is SubCutaneous; into fat between skin and underlying muscle of arm, abdomen, buttock or front thigh using insulin type syringe with small diameter #29 short needle.
   My minimum rules were: Frequency never more than once a day and max dose 15 mg.
   I used the injected pentazocine for approx 1-hour session where I read, studied, wrote and watched movie for review. I did not use for pain.
   Concerning effect of pentazocine or other opioid I have used, keep in mind it is an effect of a particular dose and under particular circumstance not comparable to street drug user overdosing or patient in pain. The difference I note is due to mode of administration – injected versus oral. Both injected morphine and pentazocine have more rapid onset and more powerful peak effect compared to similar oral doses. Both show similar tolerance with continuance.

   Oral Use of Pentazocine: Since 2002, I started using 25 mg tablet of Pentagin (Now, in Japan, named,  Sosegon) cut in half (12.5 mg dose) or on 4-hr schedule to make my life efficient and happy after age 70. It replaced injected pentacozine and other opioid and was sufficient for my need with no constipating or other side effect. In 2006 I started cutting the pill in quarters and using the quarter-pill 6 mg dose. I note after years of use and a stable level of tolerance that the 6 to 12 mg under-the-tongue dose within 5 minutes relieves impatience and anxiety and allows a pleasant 30 minutes of thinking and rest. Time that passed boringly starts to pass more pleasantly with good thoughts shortly after I put the 6 mg dose under my tongue. Most recently I was hospitalized for an orthopedic problem and had to limit to one 25 mg a day and had no problem with withdrawal symptom. In hospital I found it useful against the boredom of enforced bed rest. Using the 25 mg pentacozine pill taken under the tongue until dissolved (5-minute interval) at maximum every 6 (more recently as I became more tolerant, every 4) hours gives the most efficient one-pill use for a long-term opioid-tolerant  such as I.  Each time one takes the pill one will experience at least 1 hour anxiety-free, paranoia-free, with good thinking that continues at lower level in the few hours after.  I did not find it useful for pain although it may relieve chronic pains; I take it for peace of mind and anxiety-free relaxation with good thinking. It may be used several times a day depending on stresses and mental state of each 24-hour period. In my old age and especially during my recent time in hospital bed it has been a good drug against boredom. I still find the 1/2 cut pill (c. 12.5 mg) useful for use when traveling or if low supply. Recently, I had a person who never took the drug before put a quarter of a 25 mg pentagin (sosegon) in her mouth. She immediately strongly complained of the very bitter taste and needed a couple of glasses of water to even partly clear the taste. And at 30 minutes she still noted the moderately bitter taste and no other effect. Her increased taste acuity is probably due to her youth versus my age but her lack of response to medication effect shows the importance of individual variation. First, test a drug effect on yourself using minimal dose; do not trust book descriptions.
The present Rx for Sosegon (pentacozine) in Japan may be renewed and repeated not more frequently than 84 pills total at single doses of two 25-mg tablets, three times a day, every 14 days.  For codeine, not more frequently than 90 powder packs total as single dose 20-mg powder pack, 3 times a day every 30 days.
The Stretch Effect: Several minutes after taking a dose of pentazocine, if I stretch arms above head tautly, I get pleasure directly in the stretched muscles. A sign of good endorphin effect from an opioid dose.  But keep in mind the affect of tolerance. In my case, many years.

Conditioning by Taste:  especially with sosegon but also with other opioids, I have found that the bitter taste of the quartered pill under the tongue if used all the time, conditions me to get a good reaction to the opioid. It is like Pavlov's conditioning. Initially, the unconditioned stimulus is the sosegon's chemistry that reacts with the body to cause pleasure but quickly it gets linked with the bitter taste of the sosegon so that if one did an experiment and just took a quartered pill that looks like sosegon and has a bitter taste, one should get the reaction to sosegon that I get from the chemistry but not as potent as the real McCoy.

Codeine: aka Codeine phosphate: recently I started getting prescription access to Codeine in packets of 20 mg. (In USA, the 60 mg pill dose is standard for pain, often mixed with acetaminophen or aspirin.) It is easy to get in Japan and inexpensive. Physicians are limited to Rx’ing one Rx, a 20-mg packet 3 times a day for 30 days before renewal.  I experimented and I found it is a study-helper and a passing-boring-time assist, and for giving a general body good feeling and loss of usual anxieties. A good thing about Codeine is that one can use it "surgically", i.e., in a very exact fashion (20, 40, 60 mg) for short periods like 30 minutes to an hour, that does not have strong sleepy or other bad side effect. I found that the ideal dose-use of Codeine is to sprinkle it under the tongue and dissolving it with water.  I find max continuous dosage is 1 packet every 2 or 3 hours.  It may cause constipation. 
Oral opioids abused ignorantly are Percocet, which is oxycodone with acetaminophen (APAP); it comes as – oxycodone 5 mg/APAP 325 mg, oxycodone 7.5 mg/APAP 500 mg, and oxycodone 10 mg/APAP 650 mg.  Also comes as Percodan, which is oxycodone 4.8315 mg with aspirin 325 mg per pill. Oxycodone also comes in 7% alcoholic elixir or syrup (with guafenesin, e.g., Hycodan and other opioid cough syrup). The fluid vehicle leaves no choice but to swallow. Keep aware that many oral opioid pills have either an adult aspirin or APAP (acetaminophen; doses see above). It is not wise to take an aspirin or an APAP in the same pill with an opioid as is commonly done because it is too easy to chronically overdose on the aspirin or the acetaminophen. If you take one or the other for pain or other reason, take as a separate aspirin or acetaminophen pill and keep the opioid as single-drug pill.

OxyContin (OxyC) Slow Release
Approved by the FDA in 1995, OxyC had risen to top sales by 2018. It comes in pill doses 80 and 160 mg and is free of Aspirin and APAP in its most popular pill. The opioid is oxycodone. Addicts crush it and make injections and overdose orally by taking too much or by absorbing it by mouth. The 80 mg dose is too high for new user to get safe recreational effect. If you prefer OxC, use a pill cutter and experiment with fractional doses of the 80 mg pill, starting with the ¼ (20 mg or one quarter pill) dose. For highest efficiency and economy, try mouth absorption rather than swallowing the pill. (Under tongue or chewing) Do not inject it. You may note on the prescription-insert a warning against such mouth-absorption use because with 80 to 160 mg pill it could lead to overdose, especially in non-tolerant new opioid user. But that is due to the company making pills with excessive milligram dosage for mouth absorption and can be prevented by cutting the pill in fractions.
   As of mid 2012, an oxyContin pill or capsule was designed so that if a user tries to crush it up in order to snort or use for injection it will turn into a jelly-goo. I have no experience with it so not sure if this affects cutting the pill into halves or quarters.

Reason for Using Opioids:
I have dealt with opioid used for study or anti-depressive or anti-anxiety or, in appropriate dose, mild stimulant.  Its use as preventive of suicide or other death fears or stage fright is based on observing its powerful anti-depression effect. A person with a deadly diagnosis of cancer or other mortal illness, by using opioid as I advise, should benefit by the enjoyable intervals --- relief of anxiety, depression, pain (add an aspirin or an acetaminophen and caffeine) or paranoia during the dose interval --- as his or her life is ending. Especially in old age, opioids could be a blessing against existential boredom.
   Anyone who uses opioid in U.S. or where it has been criminalized or made difficult to obtain has the problem of creating an addiction due to difficulty in obtaining. Unless one has a secure source through a cooperative physician, it is best not to depend on opioids in such places (Like the U.S.A.).

For fictional treatment of my morphine experiences click the below hyperlinked chapters from http://adventuresofkimi.blogspot.com, the Slim Novels 2 and 12 and read separately. Specific chapters to click on and read are below.

  • 4. (24-25) Opium Sanity
  • 4.(26-27) House of Mamka/Opium Wisdom
  • 12.(0-1) Slim Novel 12 Intro and Chapter 1
  • 12.8 The Problem Getting Morphine
  • 12.(11-13) Ali Explains - A Walk on the Wild Side
  • 12.(21-22) Bronx Wilderness with Pizza and Spaghet...
  • 12.23 Morphine Moment - Forest Primeval
  • 12.24: A Walk on the Wilderness Side
  • 12.29 Morphine in a Meadow
  • 12.33 Dear Miss - Could You Help Me to Die?
  • 12.34. Suicide Should be Painless
  • 12.36 Helping Dan Die - The Morphine Effect
  • 12.37 Ali's Alone Day
  • 12.39 Dan's Alone Day - Life at the End of Its Te...


  • End of Chapter. To read on next, now, click 4.6a Coffee ----Secrets of Caffeine.















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