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Pain MedicationsWhat are pain medications (analgesics)? Pain relievers, also called analgesics or painkillers, are medicines that treat aches and pains. The goals of pain relievers are to reduce pain and suffering, enhance quality of life, and increase the ability to function. Analgesics are divided into two major categories: opioid and non-opioid medications. The latter category includes NSAIDs, as well as acetaminophen. They are used for short-term, acute pain like menstrual cramps, headaches, or minor sprains, as well as for severe pain of either an acute or chronic nature. Opioid analgesics are very powerful and are reserved for conditions where non-opioids do not provide the needed degree of pain relief. One major difference between NSAIDs and opioids is that the former have a "ceiling effect" - that is, continuous dose escalation does not provide concomitant increase in pain relief. Increasing the dose of an opioid may achieve relief, but this can lead to serious undesirable effects, especially if they are used for a long time. It is important to understand that analgesics don't treat the underlying cause of the pain. They provide only symptomatic relief. Opioid analgesics relieve pain by acting directly on the central nervous system. They act by depressing pain impulse transmission at the spinal cord level by interacting with opioid receptors. Opioids can cause drowsiness, dizziness, breathing problems, and physical or mental dependence. Although addiction is possible, it appears to be rare among people who take opioids for therapeutic purpose. Tramadol is a peculiar analgesic, introduced in the United States in 1995. It is much stronger than NSAIDs and is equal to lower-dose morphine. Its analgesic action combines opioid (weak activity at the µ-opioid receptor) and non-opioid (weak inhibition of noradrenaline and serotonin reuptake) effects. Tramadol APAP (Ultracet) is a combination of tramadol and acetaminophen. It offers enhanced efficacy, faster onset of action, and longer duration of action compared with either component alone. Butalbital with Acetaminophen and Caffeine (Fioricet) is used to relieve mild to moderate tension headaches and migraines for which it is usually very effective. Fioricet may cause you to become drowsy and less alert, although most people still are able to go to work and function on a normal basis after taking it. The downside of butalbital-containing preparations is that the long-term use can lead to rebound headaches. NSAIDs comprise a large class used to relieve pain and reduce inflammation. The most well-known NSAID is aspirin, or acetasalicylic acid, first synthesized in 1899. They act through blocking of enzymes necessary for the synthesis of prostaglandins -- hormone-like chemicals that promote inflammation, pain, and fever. The enzymes that produce prostaglandins are called cyclooxygenase (COX). There are two types of COX enzymes, COX-1 and COX-2. Both COX-1 and COX-2 produce prostaglandins that promote inflammation and pain. However, only COX-1 produces prostaglandins that protect the stomach and intestinal lining. NSAIDs vary in their potency, how they are eliminated from the body, and how strongly they inhibit COX-1. COX-2 inhibitors are NSAIDs that selectively block the COX-2 enzyme. Because they do not affect COX-1 enzyme, they are uniquely different from traditional NSAIDs which usually block both COX-1 and COX-2. They are less likely to cause ulcers than traditional NSAIDs, but have higher risk of cardiovascular problems. The only COX-2 inhibitor on the market is celecoxib (Celebrex). Two major potential risks of NSAIDs include stomach and kidney damage. By blocking the COX-1 enzyme and disrupting the production of prostaglandins in the stomach, NSAIDs can damage the stomach lining and cause ulcers. Some NSAIDs affect stomach prostaglandins less than others, and, therefore, have a lower risk of causing ulcers. NSAIDs can harm the kidneys as well by reducing the flow of blood to the kidneys and impairing their function. As all NSAIDs produce a blood-thinning effect, their use in conjunction with blood-thinning medications may be dangerous. Ibuprofen (Motrin) is the safest and cheapest of NSAIDs available in lower strengths as Advil and at higher strengths as a Motrin. Ibuprofen is used to reduce fever, relieve pain and inflammation associated with arthritis, headache, toothache, back pain, menstrual cramps, or minor injury. It appears to have the lowest risk of gastrointestinal side effects of all the traditional NSAIDs3. Naproxen (Naprosyn, Aleve) is an antipyretic and analgesic. Naproxen has a greater potential to increase blood pressure than other NSAIDs2. It appears to be risk-neutral with regard to cardiovascular side effects4. It is reasonably well tolerated in older people. Diclofenac (Voltaren) is one of the safest NSAIDs used to relieve mild to moderate pain and inflammation in ankylosing spondylitis, dysmenorrhea, rheumatoid arthritis, osteoarthritis. Ketorolac (Toradol) is a very strong pain reliever and is indicated for moderate to severe pain for short periods. Ketorolac has the distinction of being the only non-narcotic analgesic available in a parenteral formulation that can be used for the relief of acute pain. Triptans are indicated for the management of moderate to severe migraine headaches. About 60% of people who take triptan achieve pain relief within two hours. Although the exact cause of migraine is not understood, triptans are thought to shorten a migraine attack by constricting blood vessels and preventing the release of pro-inflammatory neuropeptides. There is some evidence that sumatriptan (Imitrex), almotriptan (Axert), eletriptan (Relpax), and zolmitriptan (Zomig) all have similar efficacy. Frovatriptan (Frova) is probably less effective. Some triptans (e.g. sumatriptan, zolmitriptan, rizatriptan, almotriptan and eletriptan) have rapid onset of effect and relieve migraine headaches quickly. Others (e.g. naratriptan, frovatriptan) work more slowly but have longer-lasting effects. A major drawback with the triptans is their potential to cause vasoconstrictive effects. All of the triptans cause similar mild coronary artery contraction5. References
Last updated: April, 2011 |
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