Non-opioid analgesics

Non-opioid analgesics


Nonsteroidal anti-inflammatory drugs (NSAIDs). Traditional recommendations of WHO (1996) provide for the application of NSAIDs among one of the three so-called essential (model) as the most studied drugs - aspirin, ibuprofen, indomethacin.
Aspirin and indomethacin are analgesics with anti-inflammatory component of the action, they also expressed significant adverse properties (irritation and erozirovanie gastric mucosa, etc.). Do not exceed the daily doses of aspirin and indomethacin, 4 g 200 mg due to an increase risk of adverse events. Ibuprofen (maximum daily dose 1.2 g) has a less pronounced gastrotoksicheskoe action than aspirin and indomethacin. Each of these traditional analgesics inferior to its main properties (analgesic and anti-inflammatory), the latest generation of NSAIDs, such as diklofenaki, ketoprofen, lornoxicam. These drugs are available in different dosage forms, their analgesic dose for systemic use (oral, rectal, parenteral) are for diclofenac 150-200 mg / day, ketoprofen, 200-300 mg / day, lornoksikama 16-24 mg / day.
If acute pain is effective NSAID ketorolac, but it should not be prescribed for long-term therapy HBS.
Selective blockers of COX-2 (meloxicam - up to 15 mg / day nimesulide - up to 200 mg / day, celecoxib - up to 400 mg / kg oral forms), is slightly inferior to the efficiency of the best non-selective NSAIDs, have an advantage over the latter due to less pronounced gastrotoksicheskomu action, but may contribute to increased blood pressure, fluid retention, allergic reactions are possible. Widespread use of drugs of the COX-2 is constrained by their high cost.
Metamizol sodium has a good analgesic effect comparable to the action of NSAID is different from the last weakly pronounced anti-inflammatory effect. The drug is widely used in Russia and in many other countries thanks to the effectiveness of the various types of pain, and low cost. In many Western countries metamizol excluded from clinical use because of possible fatal gematotoksicheski responses during prolonged therapy (agranulocytosis). However, serious complications, including fatalities are known and the application of NSAIDs (perforated ulcer of the stomach, gastric bleeding, renal failure, anaphylactic shock) and paracetamol (hepatic failure, anaphylaxis). Waiver of clinical application metamizol at this stage should be regarded as premature, since it extends the non-opioide treatment of acute and chronic pain, especially when contraindications to NSAIDs (gastric ulcer and duodenal ulcer, the risk of bleeding) and paracetamol (abnormal liver function).
Side effects may occur analgin allergic reactions varying degrees of severity, depression of blood (granulocytopenia, especially during prolonged therapy significant dose), renal dysfunction (especially in dehydrated patients). The drug has good solubility and biodostupnostyo is presented in the form of tablets for oral and injectable solutions in ampules for intramuscular and intravenous administration. The presence of high-speed injection forms determines the application of Analgin and drug based on it in conjunction with inflammatory components - baralgina - in surgery, urology, trauma and other fields of medicine associated with pain syndromes and invasive interventions. Dose analgin prolonged intake should not exceed: single - 1 g daily - 2 g. The short-term (several days) treatment of acute pain (postoperative pain, renal, hepatic colic), in the absence of contraindications and good tolerability in doses analgin injection can be: single 1-1,5 g daily up to 4 g (for baralgina respectively 2-3 ml and 8 ml). Contraindications to such therapy are the lack of information about the status of hemogram, the presence of the patient's neutropenia, dehydration, kidney failure, asthma, pregnancy. Analgin treatment should be carried out against the backdrop of an adequate fluid intake by mouth, or (in hospital) intravenous infusion. Long-term therapy HBS metamizol need periodic monitoring of blood counts (CBC monthly). There is also a wide range of multicomponent analgesic preparations containing metamizol, who should appoint the light of the rules for using metamizol. Should not be prescribed to the patient co-administration of NSAIDs and metamizol at risk of concomitant nephrotoxic action.
Paracetamol has analgesic effects without significant local anti-inflammatory component, as it has a central mechanism of action (in particular, inhibits the production of GHGs at a level of spinal structures CNS). Paracetamol is one of the non-opioid analgesics recommended by WHO for the treatment of cancer HBS, and is widely used as an OTC drug for various other kinds of pain. As an analgesic, it is slightly inferior to NSAIDs and metamizol, but can be used in conjunction with one of them with the best result. A single dose of paracetamol is 0,5-1 grams daily should not exceed 4 g. In large doses, hepatotoxic drug. It is contraindicated in liver dysfunction. With prolonged use should perform monthly biochemical monitoring the functional state of the liver.
Opioids starts from 2 nd grade (moderate pain). The optimal analgesic at this level is non-narcotic opioid average strength of tramadol in one of the non-invasive forms. Most shows appointment retard tablets 100, 150 or 200 mg, with long-acting (10-12 h), after a preliminary dose titration by the appointment caps a short action. Can be used as a capsule (50 mg), suppositories (100 mg) and injections (50 mg in 1 ml), duration of which is 5-6 hours daily dosage of tramadol in cancer patients can reach 600 mg and the duration of effective therapy is few months. The drug has no harmful side effects are well tolerated by most patients. At the beginning of therapy may cause transient drowsiness, nausea and sometimes vomiting. May require the appointment of antiemetics within 1-2 weeks of therapy tramadol, after which the side effects stopped.
Fentanyl Transdermal (dyurogezik) - the most potent opioid analgesic, first created as a system for transdermal administration in a different range of doses: 25, 50, 75 and 100 mg / h. It is now widely used as an alternative opioid in the treatment of HBS of high intensity. TTC Dyurogezik is virtually universal dosage form (patch from the depot of fentanyl, to be applied to the skin with minimal scalp) and can be used in any patients, including those unable to take tablets by mouth. The analgesic effect dyurogezika powerful and lasting than the oral form of morphine prolonged action. The duration of analgesia with application to skin patches with fentanyl is 72 hours, ie change the patch is 1 every 3 days. Incurable cancer patients with severe HBS estimate dyurogezik as the most effective and convenient way of pain therapy. Dyurogezik can cause the same side effects that are inherent to morphine. The most dangerous of these is respiratory depression. When a patient has difficulty breathing plaster must be removed and after normalization of breathing using the patch with a dose of fentanyl by one notch below.
Powerful opioid pain treatment 4-th stage of incurable patient continues much as required to alleviate their suffering.
The most rational list of opioid analgesics for the treatment of HBS in cancer patients include the following drugs in non-invasive as possible retard: tramadol - pill-retard (capsules, suppositories, injections), prosidol - tablets cheek, buprenorphine - sublingual tablets, morphine sulphate - retard tablets (MST, etc.), transdermal fentanyl dyurogezik.
The sequential use of these opioids with the growth of HBS an optimal clinical result, such a treatment regimen is most expedient economically. In various specific situations is acceptable and other options. With the ineffectiveness of the maximum doses of opioids, 2-nd stage of tramadol, codeine, prosidola can be assigned to small doses of morphine sulphate (20-30 mg / day) or dyurogezik 25 mg / day.
Along with the best of opioids, discussed earlier, in certain situations, for example, in the absence of these drugs and their poor tolerability, can be applied to other opioid analgesics.
HBS in the treatment of moderate to strong possibility of opioid agonist-antagonists: butorphanol, nalbuphine, with similar analgesic potential to prosidolu. It should however consider their antagonistic relationship with opioids 2-nd (tramadol, codeine), third (buprenorphine) and 4-th (morphine, dyurogezik) stages of therapy and possible destabilization of the therapeutic effect, if necessary, replace the opioid one group to another.