Origins of Present-Day Medications


Understanding the medications you're taking is important. Why? Preventing an accidental overdose is one good reason. Another is avoiding a mixture of the wrong medications. This is something you can't leave entirely to your doctor or pharmacist.


Although they are vigilant, they see hundreds of people every week and although they are trained and responsible for avoiding mistakes, that's not going to do you much good when you're in a coma or the grave.


Doctors don't like to be questioned. The majority do not like to be brought articles from the Internet.


Pharmacists are much more open. They also have all your records in front of them and can tell you if an interaction is possible. Several have helped us personally avoid potential mistakes.


Whether people like to be questioned or not shouldn't figure into your questioning them. It's your life and you're responsible for protecting it, but frankly good doctors are hard to find and aggravating them isn't a good idea.


So let's learn something about medications.


Present-Day Medications Derived From Opium


By the time pain medications reach us, the opium in them has been cut so drastically that calling them opiates nearly refers only to their origin.


Often a mixture of pain medicines, such as a primary and a breakthrough, are used, sometimes in combination with a muscle relaxer and antidepressant since depression and chronic pain go hand-in-hand.


Many chronic pain patients who have lived strong "normal" lives until chronic pain hits are embarrassed to find themselves depressed and refuse to admit it, seeing it as something they should be able to overcome themselves. This is like saying a diabetic should be able to control their disease without diet or insulin. There is no more shame in seeing a therapist and taking antidepressants than in taking insulin for diabetes.


Depression is an illness, often caused by a chemical imbalance in the body. Just as you would not ask your body to magically produce a medication to take care of the pain, don't ask it to do so for depression. We discuss this further under Chronic Pain and Depression.


Each medication acts differently on each patient. If one does not work for you, do not despair. Your doctor will work with you to find one or a conbination that does. If you have an allergic reaction -- rash, trouble breathing, vomiting, contact your physician or hospital immediately or call 911. It's always better to be safe than sorry.




"Breakthrough" - a secondary medication used when the primary medication isn't enough to take care of the pain.


"Synthetic" - a man-made medication developed to have the same effects as an opiate-based one.


"Titrate" - to increase or decrease the dosage of a medication.


The use of synthetic opiates cuts back on addiction and many side effects, but may be addictive themselves. Check with your doctor.


The amount of actual opium in medications is controlled today in a way it never was in the past. Most likely you are getting a derivative of opium (see History of Opium and Morphine).


Prescriptions are carefully mixed and controlled. Overdoses under a doctor's care are rare. Physicians today are knowledgeable about the amount of medication to prescribe to alleviate pain.


However you may experience an unforeseen reaction to a medication. This is why it is so important you immediately report it or seek help.


Seldom is pain completely controlled by oral medications. Patients are made "comfortable." Most must still deal with a certain amount of pain, and most gladly live with a level 5 on the famous scale of "1 to 10" (with 10 being the worst pain you've ever experienced in your entire life) if they can get away from the 7 to 10 level that keeps them awake days and nights, pacing the floor if they can pace, or bundled into crying bits of humanity from the hideous pain they otherwise live in.




The pharmacological effects of opiates result from the fact that these substances are a bit (like a key) like the natural endorphins in the body and in antidepressants. Normally released by the brain, further released during exercise and pleasant stimuli, they thus directly stimulate the endorphin receptors.


Because the opiates were known about earlier than the endorphins, these are usually called opiate receptors. Researchers can trace these receptors in the brain by injecting radioactive opiates and then by monitoring where the radioactivity collects in the brain. This appears to be in very specific areas in the brain.


The first concentration of opiate receptors is formed by a nerve cell system which plays an important role in transmitting pain stimuli. A brief digression regarding pain is required here.


Acute Pain


If someone unexpectedly pricks herself, for instance on an improperly stored needle in the sewing box, she will experience acute pain -- sudden and sharp -- retract the injured finger (and bleeding or not, put it in her mouth) before any pain is felt.


This is due to an emergency telegraph from the finger to the spinal cord where another message is immediately transmitted back to the arm muscles (comparable to the knee jerk reflex). At the same time, a message from the spinal cord is transmitted to the cortex of the cerebrum, which results in the first experience of pain.


Until then, there are only signals aimed at a direct reaction to end the painful stimuli. If that were to be the end of it, there is every chance that the person would put her hand into the sewing box just as carelessly on a second occasion. In order to prevent this, and to introduce a moment of learning, stimuli are sent (slowly) from the spinal cord to the part of the brainstem where the opiate receptors are located.


Analgesic Effect


This area is responsible for alarming a threatening aspect of pain and it is exactly this effect which is remedied so effectively by the administration of opiates. The feeling itself does not disappear so much as lose its threatening character. It is this which lends the opiates their pain-killing (analgesic) effect.


The most striking quality of this pain-killing effect of opiates is that it has virtually no effect whatever on the other sensory perceptions, consciousness or motor functions.


All other substances with a pain-killing effect, such as laughing gas, alcohol, ether and barbiturates have, in an effective dose, a definite effect on consciousness, motor coordination, the intellect and emotional control. The drowsiness which can be caused by opiates is experienced only at high dosage.


Opiates Inhibit Receptors


A concentration of opiate receptors is located in the respiratory center. These cells serve as a kind of metronome, that apparatus countless people have standing on their pianos to keep the beat. This respiratory metronome regulates the breath in a similar way, with fast or slow settings according to requirements, but ensuring in-and-out breaths take place regularly.


Opiates also have an inhibiting effect on these cells: both the frequency and the depth of breathing is reduced under the influence of opiates. In the case of an overdose, respiration can come to a complete halt.


Through shortage of oxygen, the heart muscles can no longer beat and as a result, brain cells die, and death occurs. Besides this, opiates inhibit sensitivity to the impulse to cough. Codeine in particular is used in many cough remedies, but even heroin is used for this purpose in England.


The Digestive System


The third concentration is in the vomiting center, which, stimulated by the stomach (by contaminated food for instance), normally causes the stomach muscles to contract, resulting in vomiting. These cells are stimulated into activity by opiates. Opiate use causes nausea and vomiting.


However, tolerance for this effect is built up very quickly, although some users continue to vomit after each 'shot' for years. This effect is strongest with the opiate apomorphine, which is used medically specifically for this purpose.


The effect of opiates on the digestive system, which also contains large numbers of opiate receptors, has been known about for the longest period of time. Long before opiates were used as painkillers, opium was used for diarrhea: opiates inhibit intestinal peristalsis. For this reason, most heroin addicts are constipated.


The Endocrinal System


Opiates also affect the endocrinal system. By influencing the hypothalamus, the part of the brain linked to the conductor of the hormonal orchestra, body temperature is slightly lowered, although it goes up with chronic use of high doses.


Opiates lower the amounts of cortisol and testosterone in the blood, although these effects disappear again with chronic use as the body becomes tolerant to the medication.


Opiates influence the pupils: they contract (miosis). This is an extremely reliable signal of opiate use. When suffocation occurs (as a result of respiratory inhibition) in the case of an overdose, the pupils dilate (mydriasis).


In the usual therapeutic dosage, morphine widens the veins in the skin, often giving the face, throat and upper part of the chest a flushed appearance and a warm sensation. This happens as morphine releases histamine. This is also the reason for itching and perspiration often seen in opiate users.


Opiates Cause Euphoria


The effects mentioned so far do not explain the mood changes which occur with opiate use, and even less, the phenomenon of addiction. These are dependent on the influence of opiates on the largest cell complex which is strewn with opiate receptors: the limbic system and the nucleus acumens.


In this way, opiates cause euphoria, but lessen negative stimuli such as pain and distress, leading to emotional indifference often combined with inhibition of the sexual functions. The effect is comparable to that on pain: the signal is not removed, but the emotions linked to it are.


Build Up of Tolerance


Chronic use of all opiates leads to a tolerance. Many of these symptoms disappear. Unfortunately it also leads to a strong physical dependence. The relative severity of the abstinence syndrome is in general related to the duration of efficacy, leading to the paradoxical situation in which the abstinence syndrome of heroin, although occurring extremely quickly, is nonetheless less extreme than that of methadone.


The individual must also be factored in and this is perhaps the most mysterious element of all. Many patients in chronic pain, along with their doctors, claim that the pain absorbs the medications and there is no addiction. This seems to be borne out by the reaction different people have to medications. While there may be an initial "high" when starting a new medication, just as often there is not and either way, it usually goes away and the person functions normally. The pain does seem to absorb the medication.


No Withdrawal Symptoms?


One patient was put through detox by a doctor who definitely qualified as a quack. He thought she had been abusing her medications and he could not believe that she had no physical reaction to the sudden withdrawal of them. No tremors or other physical reactions he expected from an "addict." Only a return of the pain.


Chronic pain patients can take quantities of pain medications that would knock a normal person out without any change in their behavior at all other than a relief from pain. They feel no differently emotionally or mentally after taking their pain medication.


Thus automatically labeling pain patients drug addicts is obviously a misnomer. The medications may be addictive, but many patients do not become or display addictive behavior. They simply need pain relief.


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