Monday, June 6, 2011

Opioid Analgesics : prolonged use

Widely believed that prolonged use of opioid analgesics for relief of chronic pain often leads to abuse of drugs and drug addiction. Society and the media focus attention on the problem of medical drug due to the fact that doctors are increasingly prescribing narcotic drugs. His view on this issue poses the chief editor of Pain Treatment Topics Stewart B. Master Medicine Levitt (Stewart B. Leavitt). After analyzing a set of clinical studies and scientific articles on the subject specialist in pain argues that the danger of drug abuse patients is not as great as it seems at first glance. In the review he cites some of these studies.
drugs

Opiates (opium alkaloids), such as morphine, and their synthetic counterparts. Today considered to be the only drug which removes a very strong or chronic pain. Different opioid analgesics act in the body through different types of opioid receptors, in most cases through the m-receptors.
DA Fishbayn (DA Fishbain) from the University of Miami (Miller School of Medicine at the University of Miami) in Florida in 2008 summarized 24 studies. Of 2507 patients who were receiving treatment of opioid analgesics for relief of chronic pain noncancerous origin, symptoms of abuse of drugs and drug abuse occurred in 3.27%. It was found that the primary addiction was formed only 0.19% of patients and others have already had in the past experience of drug use.
Srinivaza Raja (Srinivasa Raja) of Johns Hopkins University (Johns Hopkins University School of Medicine) in May 2008 at the annual meeting of the American Society for the Study of the effects of pain (American Pain Society) said that the overall proportion of patients who manifest dependence on opiates, generally less than 3%.
M. Noble (M. Noble) and co-workers from the Research Institute of Emergency (ECRI) reviewed 115 clinical trials prolonged use of opioid analgesics and chose the 17 most deserving of trust. Patients with chronic pain noncancerous origin, from mild to severe, taking opioids for at least six months. Abused drugs, only three of 685 (0.4%) patients, and symptoms of drug dependence have only one of 2,042 (0.05%) patients. True, this is not specified whether these historically low rates to all patients or only to those who have no experience of drug use.

Sunday, June 5, 2011

Opioid analgesics : remain the main group of drugs used to treat severe pain.

Due to its high efficiency compared with other pain medication opioid analgesics are most often used for severe pain of traumatic, vascular origin in patients with malignant tumors, as well as in the postoperative period (AP Golikov, 1994; RN Lebedeva, 1994 , AN Osipov, 1994).
Identify several subtypes of opioid receptors on the basis of different interactions with a specific subtype of opioid receptor, opioid analgesics are divided into 4 groups.
Full agonists mediate the analgesic effect by binding to opioid receptors. These include: fentanyl, alfentanil, sufentanil, remifentanil, morphine, pritramid, mepiridin, promedol, prosidol, codeine, omnopon, tramadol. Total (net) agonists by binding to opioid receptors mainly cause their activation, which leads to the development of the maximum analgesic effect. Partial agonists (buprenorphine) is weaker than activate opioid receptors. Agonist-antagonists bind preferentially to one type of opioid and block opioid receptors in the other. Representatives of this group are pentazocine, butorphanol and albufin. Full antagonist naloxone upon binding to opioid receptors blocks them, eliminating the effects of agonists (M. Ya Avrutsky, 1997).
In Russian clinical practice in neonatal intensive care unit, ambulance traditionally used narcotic analgesics: morphine, promedol, omnopon. However, they can depress respiration, motility of the gastrointestinal (GI) tract, vomiting, addiction and dependence. In Britain and Germany in this regard over the past decade have found a wider application of opioid analgesics having mixed type of action, agonist-antagonists: piritramid, buprenorphine, pentazocine, pethidine, nalbuphine. The most frequent adverse events seen with narcotic analgesics, is observed in almost half of patients with sedation. Other side of manifestation, which as nausea and vomiting, sweating, hot flashes, GB, hallucinations and dizziness occur, according to different authors, with a frequency not exceeding 5% for each drug.
One of the most serious problems encountered in the application of drugs is the occurrence of this addiction. Well-known researcher of pain problems JJ Bonica (1986) urges medical personnel are not afraid to prescribe narcotic analgesics primarily to those patients whom they are vitally important: in acute pain (traumatic, post-operative) and chronic pain in incurable oncology patients.
Necessary to clearly distinguish the medical aspects of the use of analgesics on the social problems caused by the use of drugs in the home. Physical dependence in patients to a greater extent the true form of opiates (morphine and its analogues), whereas opioids are related to the group of agonist-antagonist, to a much lesser extent, provoke physical dependence.

Opioid analgesics : treatment

For the treatment of severe pain, reduce its sensory and emotional components are the major opioid analgesics. Opioids may be administered in traumatic and postoperative pain, chronic cancer pain and, in certain circumstances, for the treatment of severe chronic non-cancer pain.
Opioid analgesics interact with one or more subtypes of opioid receptors, ie m, d and k, at supraspinal, spinal and peripheral levels, causing analgesia, and many other effects. Opioids act by presynaptic inhibition of production of neurotransmitters C-fiber endings, postsynaptic suppression of evoked activity in nociceptive path or remove the remaining parts of the regulation of inhibition of nociceptive impulses. Supraspinal action of opioids is characterized by a strengthening of the descending inhibition of spinal transmission of nociceptive conduction. Opioid analgesics can be full agonists of specific opioid receptors, namely the m-receptor mixed agonist-antagonists have opposite effects on certain receptor subtype or partial m-agonist. Opioids are capable of causing physical and psychological dependence, and are the subject of illegal trade. They are therefore subject to control, assuming the legal responsibility of doctors and pharmacists. Safe use requires knowledge of available drugs, appropriate indications for use, dosage forms and routes of administration, as well as possible side effects and methods of prevention and treatment.
Opioid analgesic used for treatment of chronic pain should be well tolerated, does not cause severe sedation and suppress vital functions, allow the combined treatment and is slowly excreted from the body. The important point is the systematic use of opioids with the purpose of achieving the most effective drug concentration in the blood. Of great importance is compliance with a clear time schedule of drug administration (in hours). Opioids to treat chronic pain is not desirable to appoint injections. If the patient is not vomiting, the effectiveness of analgesics for oral administration is not following injection. Injection not only complicate the overall supervision, but also reinforce the "sick role", adding to the possibility of manipulation in relationships.

Saturday, June 4, 2011

Opioid Analgesics : the problem of rational use of opioid analgesics there is worldwide.

The problem of rational use of analgesics, and especially potent opioid analgesics, there is worldwide. The use of morphine - one of the oldest painkillers - and its analogs has always been and continues to cause some doctors caution. "However, these drugs remain today the basic therapeutic agents in the treatment of severe pain in cancer patients, and their application - an integral part of palliative care that will improve the quality of life" - said Professor George A. Novikov, president of the All-Russian Public Movement for Quality Medicine Life, "opening the symposium," Opioids in the treatment of chronic cancer pain: what's new? ", which took place in the XI All-Russian Congress of cancer in November 2007

The symposium was opened by the report of Professor Nadezhda Osipova, Honored Scientist, Head of the Department of Anesthesiology and Intensive Care MNIOI them. PA Herzen, devoted to the organizational aspects of the availability of opioid analgesics for patients with chronic pain. Nadezhda offered to split the problem into three components: legislative and regulatory issues, providing patients with modern medical opioid drugs, and improve education of medical applications of opiate and pharmacy staff in the use of narcotic analgesics. The country has registered and is included in the federal lists for privileged categories of citizens of a number of opioid drugs in prolonged non-invasive forms, such as transdermal therapeutic system and long-acting tablet. Unfortunately, in many cases it is rather formal. The sad statistics show that up to now in most regions of Russia antipain help cancer patients is poor: patients get basically inject drugs, often in inadequate analgesia for day number. Although according to the recommendations of the World Health Organization (WHO) in the treatment of chronic pain should be preferred noninvasive prolonged form, and the use of short-acting injectable drugs deemed inhumane and totally unacceptable.

Opioid analgesics : main method of treatment chronic pain syndromes in modern medicine.

The main method of treatment of acute and chronic pain syndromes in modern medicine is a systemic pharmacotherapy. The latter may be achieved by different ways of introducing the painkiller in the body (taking by mouth, rectally, sublingually, transdermally, by injection), but in any case, drug sucking, gets into the systemic circulation, and then to the place of his actions (as opposed to of regional method of introducing an analgesic, such as perineural, epidural).
For the treatment of pain of low intensity according to WHO recommendations using different non-opioid analgesics, and pain at moderate and high intensity - opioid analgesics. Non-opioid analgesia funds have predominantly peripheral action at the source of pain, have a small analgesic potential and therefore only suitable for removing mild pain. Opioids are centrally acting analgesics, implemented via an endogenous opioid system of the body at the level of the spinal cord and brain by inhibiting the ascending flow of pain impulses. They differ from each other analgesic potential and the ability to arrest the moderate or severe pain. Thanks to good analgesic properties of opioids are widely used in various fields of medicine dealing with the intense pain - particularly in oncology and surgery.
Agonist properties (sigma) receptor has ketamine, wherein a moderate analgesic effect and the whole complex of activating side effects (tachycardia, hypertension, psychomotor agitation).
Opioid antagonist naloxone, all groups is quickly neutralize their effects, including analgesia.
Existing opioid analgesics differ not only in the interaction with specific opioid receptors, but also the characteristics of binding to them in strength and duration. The higher the affinity of opioid receptor, the stronger analgesia, a longer relationship with the receptor, the analgesia is longer.
The choice of opioid for the treatment of pain of moderate or high intensity
An important consequence of the above analysis of mechanism of action of opioids is a common position on a leading role in opioid pain therapy analgesics belonging to the class of opioid agonists, since the preparations of all other groups have some kind of restriction (the effect of a ceiling analgesic dose, antagonism toward the most potent analgesics morphine group, the undesirable side properties). This provision is particularly important when treating chronic pain, to get the best result of anesthesia and to avoid possible failures.
Range of existing opioid agonists is quite broad and includes, as noted above, analgesics of different potencies, ability to manage moderate to severe pain, and indications for treatment of such pain exist in different areas of medicine.
When shown the appointment of opioid analgesics for pain relief and how to select an opioid? To do this, first of all must be guided by certain general rules.
- Testimony to the appointment of an opioid arise when non-opioid analgesics treatment does not resolve the pain, ie pain greater than the degree of the weak. In the treatment of chronic pain in cancer patients should be preferred opioid agonists.
- When determining the intensity of pain should be guided by a simple verbal scale ratings of pain (SHVO): 0 - no pain, 1 point - mild, 2 points - moderate, 3 points - severe, 4 points - the most severe pain. For the treatment of pain of moderate or high intensity in Russia Health Ministry guidelines recommend: tramadol, prosidol to moderate pain, buprenorphine for severe pain and morphine or fentanyl (including transdermal form) for the most severe pain.
- The right to use of opioid analgesics related to drugs, doctors are committed to working with drugs (most often in the oncology and surgical facilities).
- Opioids - nenarkotiki, ranked by potent drugs (tramadol, butorphanol, nalbuphine) can be written on the prescription form for the potent means of any doctor in consultation with the head of the department, if necessary relieve the patient's pain, does not eliminate non-opioid analgesics (articular, neurogenic, and other non-cancer pain). Among the opioid agonist-only drug nenarkotikom is tramadol.