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Pain Medications Guide

What are pain medications (analgesics)?

Pain relievers, also called analgesics, 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.

It is important to understand that analgesics don't treat the underlying cause of the pain.

Tramadol

Tramadol (Ultram) is one of the most potent non-narcotic analgesics, introduced in the United States in 1995, treating moderate to moderately severe pain. Tramadol is a stronger alternative to NSAIDs and an alternative to lower-dose morphine.

Tramadol’s dual mechanism of action distinguishes it from opioid analgesics such as morphine or codeine. The analgesic action combines opioid (weak activity at the µ-opioid receptor) and non-opioid (weak inhibition of noradrenaline and serotonin reuptake) effects.

These unique pharmacological properties may explain both the significantly low potential for abuse and dependence and the unique side effects profile.

The non-controlled status of tramadol as a regular prescription-only medication has proven to be of important benefit to millions of people who might otherwise suffer with inadequately treated pain.

Tramadol wirh APAP (Ultracet) is a combination of 37.5 mg of tramadol with 325 mg of acetaminophen. It offers an effective and well-tolerated alternative to anti-inflammatory drugs or other opioid/acetaminophen combinations.

The Tramadol/APAP combination has enhanced efficacy, faster onset of action, and longer duration of action compared with either component alone. These benefits are achieved with no increase in side effects.

Butalbital

Butalbital with Acetaminophen and Caffeine (Fioricet) is a strong pain reliever and sedative. It is used to relieve mild to moderate tension headaches and migraines for wich 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 the medication.

The downside of butalbital-containing preparations is that the long-term use can lead to rebound headaches.

Traditional NSAIDs

Nonsteroidal anti-inflammatory drugs ( NSAIDs) comprise a large class of medications used to relieve pain and reduce inflammation. The most well-known NSAID is aspirin, or acetasalicylic acid, first synthesized in 1899.

Two major potential risks of NSAIDs include stomach problems 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. They reduce the flow of blood to the kidneys and impair kidneys function.

As all NSAIDs produce a blood-thinning effect, their use in conjunction with blood-thinning drugs may be dangerous.

Because of the large number of available NSAIDs, it can be difficult to know which one is a better choice.

Ibuprofen (Motrin) is a popular NSAID available in lower strengths as an over-the-counter 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.

Ibuprofen is the safest and cheapest NSAIDs. It appears to have the lowest risk of gastrointestinal side effects of all the traditionsl NSAIDs3.

Naproxen (Naprosyn, Aleve) is a NSAID with antipyretic and analgesic properties. Naproxen is used to reduce pain and inflammation caused by arthritis, rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, tendinitis, or menstrual cramps.

Naproxen has a greater potential to increase blood pressure than other NSAIDs2. It appears to be risk-neutral with regard to cardiovascular side effects4.

The main benefit of naproxen is convenient two times per day dosing schedule. It also is reasonably well tolerated in older people.

Diclofenac (Voltaren) is a potent NSAID used to relieve mild to moderate pain and inflammation in ankylosing spondylitis, dysmenorrhea, rheumatoid arthritis, osteoarthritis. Diclofenac is one of the safest NSAIDs.

Meloxicam (Mobic) is an enolic acid derivative chemically related to piroxicam. Its advantage is relatively long half-life which permits once-day dosing regimen.

Ketorolac (Toradol) is a very strong pain reliever and is indicated for the treatment of 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.

Piroxicam (Feldene) has higher gastrointestinal toxicity than most other NSAIDs.

Triptans

Triptans are indicated for the treatment 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 contraction6.

Sumatriptan (Imitrex), the first triptan developed, is potent fast-acting medication. Many years of experience demonstrated sumatriptan to be highly effective and the standard for other triptans development.

Zolmitriptan (Zomig), the second triptan to be marketed, was developed with the goal of creating a medication which is more rapidly orally absorbed than sumatriptan.

Rizatriptan (Maxalt) has the most rapid onset of effect and may be more effective than other triptans5.

Naratriptan (Amerge) is a "gentle triptan". It is less likely than other triptans to relieve moderate to severe pain, but it is also appreciably less likely to cause side effects

References

  • 1. Tyndale RF, Droll KP, Sellers EM. Genetically deficient CYP2D6 metabolism provides protection against oral opiate dependence. Pharmacogenetics. 1997;7(5):375-379.
  • 2. Pope JE, Anderson JJ, Felson DT. Archives of Internal Medicine. 1993 Feb 22;153(4):477-84.
  • 3. Bjarnason I. Ibuprofen and gastrointestinal safety: a dose-duration-dependent phenomenon. J R Soc Med. 2007;100 Suppl 48:11-4.
  • 4. Kearney PM, Baigent C, Godwin J, Halls H, Emberson JR, Patrono C. Do selective cyclo-oxygenase-2 inhibitors and traditional non-steroidal anti-infalmmatory drugs increase the risk of atherothrombosis? Meta-analysis of randomized trials. BMJ. 2006; 332: 1302–8.
  • 5. Adelman JU, Lipton RB, Ferrari MD, Diener HC, McCarroll KA, Vandormael K, Lines CR. Comparison of rizatriptan and other triptans on stringent measures of efficacy. Neurology. 2001 Oct 23;57(8):1377-83.
  • 6. Tepper SJ, Rapoport AM. The triptans: a summary. CNS Drugs 1999 Nov; 12 (5): 403-17

Last updated: August, 2010

Interesting facts

  • Codeine is usually the first-line opioid for managing chronic non-malignant pain because it is the least potent opioid. However, up to 10% of white people lack the enzyme that converts codeine into its active metabolite morphine, so stronger opioids might be required. [1]
  • Fentanyl, synthetic narcotic analgesic, is the most potent narcotic in clinical use. Fentanyl is approximately 80 times more potent than morphine. Its potency is so great that the standard dose is in micrograms, not milligrams like most other narcotics.
  • Ohmefentanyl (OMF) is the most potent analgesic, 6000 to 10000 times stronger than morphine.