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14-September-2008 18:02:35 - Analgesic Redirected from Analgesia Painkiller redirects here. For other uses, see Painkiller disambiguation. An analgesic colloquially known as a painkiller is any member of the diverse group of drugs used to relieve pain achieve analgesia. The word analgesic derives from Greek an- without and -algia pain. Analgesic drugs act in various ways on the peripheral and central nervous systems; they include paracetamol acetaminophen, the non-steroidal anti-inflammatory drugs NSAIDs such as the salicylates, narcotic drugs such as morphine, synthetic drugs with narcotic properties such as tramadol, and various others. In choosing analgesia, the severity and response to other medication determines the choice of agent; the WHO pain ladder, originally developed in cancer-related pain, is widely applied to find suitable drugs in a stepwise manner.1 The choice of analgesia is also determined by the type of pain: for neuropathic pain, traditional analgesia is less effective, and there is often benefit from classes of drugs that are not normally considered analgesics, such as tricyclic antidepressants and anticonvulsants.2 Contents 1 The major classes 1.1 Paracetamol and NSAIDs 1.2 COX-2 inhibitors 1.3 Opiates and morphinomimetics 1.4 Specific agents 2 Specific forms and uses 2.1 Combinations 2.2 Topical or systemic 2.3 Psychotropic agents 2.4 Atypical and/or adjuvant analgesics 3 Addiction 4 See also 5 References 6 External links The major classes Paracetamol and NSAIDs Main article: Non-steroidal anti-inflammatory drug The exact mechanism of action of paracetamol/acetaminophen is uncertain, but it appears to be acting centrally. Aspirin and the other NSAIDs inhibit cyclooxygenase, leading to a decrease in prostaglandin production; this reduces pain and also inflammation in contrast to paracetamol and the opioids.citation needed Paracetamol has few side effects and is regarded as very safe, although excessive doses lead to Analgesic Abuse Nephropathy AAN which is commonly caused by cumulative lifetime use of large amounts ≥ 2 kg ref. Merck Manual and hepatotoxicity liver damage. NSAIDs predispose to peptic ulcers, renal failure, allergic reactions, and occasionally hearing loss, and they can increase the risk of hemorrhage by affecting platelet function.citation needed The use of certain NSAIDs in children under 16 suffering from viral illness may contribute to Reye's syndrome. COX-2 inhibitors Main article: COX-2 inhibitor These drugs have been derived from NSAIDs. The cyclooxygenase enzyme inhibited by NSAIDs was discovered to have at least 2 different versions: COX1 and COX2. Research suggested that most of the adverse effects of NSAIDs were mediated by blocking the COX1 constitutive enzyme, with the analgesic effects being mediated by the COX2 inducible enzyme. The COX2 inhibitors were thus developed to inhibit only the COX2 enzyme traditional NSAIDs block both versions in general. These drugs such as rofecoxib and celecoxib are equally effective analgesics when compared with NSAIDs, but cause less gastrointestinal hemorrhage in particular. However, post-launch data indicated increased risk of cardiac and cerebrovascular events with these drugs due to an increased likelihood of clotting in the blood due to a decrease in the production of protoglandin around the platelets causing less clotting factor to be released, and rofecoxib was subsequently withdrawn from the market. The role for this class of drug is debated. Opiates and morphinomimetics Main articles: Opioid and Opiate Morphine, the archetypal opioid, and various other substances e.g. codeine, oxycodone, hydrocodone, diamorphine, pethidine all exert a similar influence on the cerebral opioid receptor system. Tramadol and buprenorphine are thought to be partial agonists of the opioid receptors. Dosing of all opioids may be limited by opioid toxicity confusion, respiratory depression, myoclonic jerks and pinpoint pupils, but there is no dose ceiling in patients who tolerate this. Opioids, while very effective analgesics, may have some unpleasant side-effects. Up to 1 in 3 patients starting morphine may experience nausea and vomiting generally relieved by a short course of antiemetics. Pruritus itching may require switching to a different opioid. Constipation occurs in almost all patients on opioids, and laxatives lactulose, macrogol-containing or co-danthramer are typically co-prescribed. When used appropriately, opioids and similar narcotic analgesics are otherwise safe and effective, however risks such as addiction and the body becoming used to the drug tolerance can occur. The effect of tolerance means that drug dosing may have to be increased if it is for a chronic disease this is where the no ceiling limit of the drug comes into play. However what must be remembered is although there is no upper limit there is a still a toxic dose even if the body has become used to lower doses. Specific agents In patients with chronic or neuropathic pain, various other substances may have analgesic properties. Tricyclic antidepressants, especially amitriptyline, have been shown to improve pain in what appears to be a central manner. The exact mechanism of carbamazepine, gabapentin and pregabalin is similarly unclear, but these anticonvulsants are used to treat neuropathic pain with modest success. Specific forms and uses Combinations Analgesics are frequently used in combination, such as the paracetamol and codeine preparations found in many non-prescription pain relievers. They can also be found in combination with vasoconstrictor drugs such as pseudoephedrine for sinus-related preparations, or with antihistamine drugs for allergy sufferers. The use of paracetamol, as well as aspirin, ibuprofen, naproxen, and other NSAIDS concurrently with weak to mid-range opiates up to about the hydrocodone level has been shown to have beneficial synergistic effects by combatting pain at multiple sites of action-NSAIDs reduce inflammation which, in some cases, is the cause of the pain itself while opiates dull the perception of pain-thus, in cases of mild to moderate pain caused in part by inflammation, it is generally recommended that the two be prescribed together.3 Topical or systemic Topical analgesia is generally recommended to avoid systemic side-effects. Painful joints, for example, may be treated with an ibuprofen- or diclofenac-containing gel; capsaicin also is used topically. Lidocaine, an anesthetic, and steroids may be injected into painful joints for longer-term pain relief. Lidocaine is also used for painful mouth sores and to numb areas for dental work and minor medical procedures. Psychotropic agents Tetrahydrocannabinol THC and some other cannabinoids, either from the Cannabis sativa plant or synthetic, have analgesic properties, although the use of cannabis derivatives is illegal in many countries. Other psychotropic analgesic agents include ketamine an NMDA receptor antagonist, clonidine and other α2-adrenoreceptor agonists, and mexiletine and other local anaesthetic analogues. Atypical and/or adjuvant analgesics Orphenadrine, cyclobenzaprine, scopolamine, atropine, gabapentin, first-generation antidepressants and other drugs possessing anticholinergic and/or antispasmodic properties are used in many cases along with analgesics to potentiate centrally acting analgesics such as opioids when used against pain especially of neuropathic origin and to modulate the effects of many other types of analgesics by action in the parasympathetic nervous system. Dextromethorphan has been noted to slow the development of tolerance to opioids and exert additional analgesia by acting upon the NMDA receptors; some analgesics such as methadone and ketobemidone and perhaps piritramide have intrinsic NMDA action. Strong liquor has been used in the past as an agent for dulling pain, due to the CNS depressant effects of ethyl alcohol, most notably during the Civil War. However, the ability of alcohol to kill pain is said to be inferior to virtually all analgesics used today e.g. morphine, codeine. As such, the idea of alcohol for analgesia is generally regarded as being as primitive as the practice in virtually all industrialized countries today. The use of adjuvant analgesics is an important and growing part of the pain-control field and new discoveries are made practically every year. Many of these drugs combat the side effects of opioid analgesics, an added bonus. For example, antihistamines including orphenadrine combat the release of histamine caused by many opioids, methylphenidate, caffeine, ephedrine, dextroamphetamine, and cocaine work against heavy sedation and may elevate mood in distressed patients as do the antidepressants. A well-accepted benefit of THC to chronic pain patients on opioids is its superior anti-nauseant action. Some think it would make more sense to use the synthetic THC capsule trade name Marinol, which is administered orally. However, in patients suffering from nausea, the swallowing of the capsule itself may provoke vomiting. Likewise, the use of medicinal cannabis remains a debated issue. Addiction This article's section called Addiction does not cite any references or sources. July 2008 In the United States in recent years, there has been a wave of new addictions to prescription narcotics such as oxycodone such as OxyContin, or with acetaminophen, as Percocet and hydrocodone commonly prescribed with acetaminophen, as in Vicodin, Lortab etc. when available in pure formulations as opposed to combined with other medications as in Percocet which contains both oxycodone and acetaminophen/paracetamol. See also Pain management Patient-controlled analgesia Co-proxamol References ^ Anonymous 1990. Cancer pain relief and palliative care; report of a WHO expert committee, World Health Organization Technical Report Series, 804 in English. Geneva, Switzerland: World Health Organization, 1-75. ISBN 924120804X. ^ Dworkin RH, Backonja M, Rowbotham MC, et al 2003. Advances in neuropathic pain: diagnosis, mechanisms, and treatment recommendations. Arch. Neurol. 60 11: 1524-34. doi:10.1001/archneur.60.11.1524. PMID 14623723. ^ Mehlisch DR 2002. The efficacy of combination analgesic therapy in relieving dental pain. J Am Dent Assoc 133 7: 861-71. doi:10.1001/archneur.60.11.1524. PMID 12148679. External links Bandolier pain site Oxford pain group v d e Analgesic products N02A, N02B Opioids See also: Opioids template Opium alkaloids thereof Codeine · Morphine · Opium · Laudanum · Paregoric Semi-synthetic opium derivatives Acetyldihydrocodeine · Benzylmorphine · Desomorphine · Dihydrocodeine · Dihydromorphine · Ethylmorphine · Diamorphine · Hydrocodone · Hydromorphinol · Hydromorphone · Nicocodeine · Nicodicodeine · Nicomorphine · Oxycodone · Oxymorphone · Thebacon Synthetic opioids Alphaprodine · Anileridine · Buprenorphine · Butorphanol · Dextromoramide · Dextropropoxyphene · Dezocine · Fentanyl · Ketobemidone · Levorphanol · Methadone · Meptazinol · Nalbuphine · Pentazocine · Propoxyphene · Propiram · Pethidine · Phenazocine · Piminodine · Piritramide · Tapentadol · Tilidine · Tramadol Pyrazolones Ampyrone/Aminophenazone · Metamizole · Phenazone Cannabinoids Ajulemic acid · AM404 · Cannabidiol · Cannabis · Nabilone · Tetrahydrocannabinol Anilides Paracetamol acetaminophen · Phenacetin · Propacetamol Non-ateroidal anti-inflammatories See also: NSAIDs template Propionic acid class Fenoprofen · Flurbiprofen · Ibuprofen · Ketoprofen · Naproxen · Oxaprozin Oxicam class Meloxicam · Piroxicam Acetic acid class Diclofenac · Indometacin · Ketorolac · Nabumetone · Sulindac · Tolmetin COX-2 inhibitors Celecoxib · Rofecoxib Anthranilic acid fenamate class Meclofenamate · Mefenamic acid Salicylates Aspirin Acetylsalicylic acid · Benorylate · Diflunisal · Ethenzamide · Magnesium salicylate · Salicin · Salicylamide · Salsalate · Trisalate Atypical, adjunct miscellaneous Bicifadine · Clonidine · Cyclobenzaprine · Duloxetine · Flupirtine · Gabapentin · Glafenine · Nefopam · Orphenadrine · Tebanicline · Trazodone · Ziconotide v d e Major drug groups Gastrointestinal tract/metabolism A stomach acid Antacids, H2 antagonists, Proton pump inhibitors Antiemetics Laxatives Antidiarrhoeals/Antipropulsives Anti-obesity drugs Anti-diabetics Vitamins Dietary minerals Blood and blood forming organs B Antithrombotics Anticoagulants, Antiplatelets, Thrombolytics Antihemorrhagics Cardiovascular system C cardiac therapy/antianginals Cardiac glycosides, Antiarrhythmics, Cardiac stimulant Antihypertensives Diuretics Vasodilators Beta blockers renin-angiotensin system ACE inhibitors, Angiotensin II receptor antagonists, Renin inhibitors Antihyperlipidemics Skin D Emollients Cicatrizant Antipruritics Reproductive system G Hormonal contraception Fertility agents SERMs Sex hormones Endocrine system H Corticosteroids Sex hormones Thyroid hormones Antithyroid agent Infections and infestations J, P Antibiotics Antivirals Vaccines Antifungals Antiparasitic Antiprotozoals, Anthelmintics Malignant and immune disease L Anticancer agents Immunostimulators Immunosuppressants Muscles, bones, and joints M Anabolic steroids Anti-inflammatories NSAID Antirheumatics Corticosteroids Muscle relaxants Brain and nervous system N Anesthetics General, Local Analgesics Anticonvulsants Mood stabilizers Psycholeptic Anxiolytics, Antipsychotics, Hypnotics/Sedatives Psychoanaleptic Antidepressants, Stimulants/Psychostimulants Respiratory system R Bronchodilators Decongestants H1 antagonists Other ATC V Antidotes Contrast media Radiopharmaceuticals Dressing Retrieved from http://en..org/wiki/Analgesic Categories: Analgesics | PainHidden categories: All articles with statements | Articles with statements since February 2007 | Articles lacking sources from July 2008 | All articles lacking sources Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages Türkçe العربية Català Česky Dansk Deutsch Español Français Bahasa Indonesia Italiano עברית Bahasa Melayu Nederlands 日本語 Polski Português Română Simple English SlovenÄ?ina SlovenÅ¡Ä?ina СрпÑ?ки / Srpski Suomi Svenska தமிழà¯? ไทย Türkçe УкраїнÑ?ька اردو 䏿–‡ This page was last modified on 29 August 2008, at 08:3
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