•  Celebrex (Celecoxib) •  Drug Information Center •  Pain Relievers and Intestinal Disorders •  Quiz: Do You Know Your Pain Relievers?

If you often suffer from pain that’s too tough for a simple aspirin, you may need stronger relief. Prescription pain medicines may be the only real option for easing severe pain, including the pain caused by cancer, arthritis, or serious injuries. Unfortunately, both doctors and patients often have misconceptions about prescription pain relievers. Learning about prescription medications for pain can be an important first step toward getting your pain under control. Keep in mind, every medication has risks and benefits, and what works for one person may not be a good choice for another.

You may know this drug as Tylenol, but acetaminophen is also available by prescription, usually in combination with opioid drugs like hydrocodone (Vicodin) and oxycodone (Percocet). Doctors consider acetaminophen to be safe in doses up to 2,000 to 3,000 milligrams (mg) per day for most people, and it is often the first-line pain medication that they recommend, especially to people who may have problems with anti-inflammatory medicines like ibuprofen. Acetaminophen is effective against many types of pain and gentler on the stomach than anti-inflammatory drugs.

The main concern with acetaminophen is that in large doses the drug may stress or damage the liver, measured by elevated liver enzymes. Damage can begin even in healthy adults taking as little as 4,000 mg a day after as few as four days, according to a recent study. Acetaminophen overdose is now the leading cause of acute liver failure in the US, and cases are on the rise. About half of acetaminophen overdoses are accidental overdoses (most of the rest are suicide attempts).

A recent study in the journal Hepatology found that 63 percent of patients who overdosed accidentally had been using prescription drugs that combined acetaminophen and an opioid drug, and 38 percent had been using two drugs that contained acetaminophen. (A large number of OTC formulas contain acetaminophen, including pain relievers like Excedrin, multi-symptom remedies like TheraFlu, sinus medicines like Sinutab and Sudafed Cold and Sinus, and combination pain and sleep aids like Anacin PM and Midol PM.)

People who take acetaminophen regularly should not drink alcohol and should check all their prescription and over-the-counter drugs to see if they contain any additional acetaminophen in them. (It may also be listed as APAP.) Although current labeling still allows 4,000 mg/day, some experts feel a lower maximum of 2,000 or 3,000 mg/day may be safer for some patients, such as the elderly, who may have decreased kidney or liver function. Those with liver or kidney disease need to be extra careful, and should check with their doctors before taking any acetaminophen, even in over-the-counter medications.

Painkillers known as nonsteroidal anti-inflammatory drugs (NSAIDs) include the old standby, aspirin. For common pain like muscle cramps, menstrual cramps, headache, back pain, arthritis, and related conditions, NSAIDs are usually very effective in reducing both pain and inflammation. When over-the-counter options don't provide enough relief, prescription NSAIDs are usually the next option that doctors try.

These medications work by blocking certain enzymes called COX-1 and COX-2 involved in inflammation (the immune response to injury or irritation). Examples of NSAIDs include ibuprofen (Advil, Motrin), naproxen (Aleve, Naprosyn), diclofenac (Cataflam, Voltaren), indomethacin (Indocin), and ketoprofen (Orudis). Ibuprofen and naproxen are available over-the-counter at lower doses than prescription versions.

Although still controversial, certain prescription NSAIDs may increase the risk of heart attack. A 2005 UK study in the British Medical Journal found that people who had been prescribed NSAIDs during the previous three months were more likely to have a heart attack than people who hadn't used prescription NSAIDs in the last three years. This was true of all NSAIDs they looked at, and included a 24 percent greater risk for current use of ibuprofen, 27 percent for naproxen (Aleve), and 55 percent for diclofenac (Cataflam).

NSAIDs can also cause gastritis or bleeding ulcers in the stomach. Other common side effects of prescription NSAIDs include stomach pain, heartburn, dizziness, headaches, gas, diarrhea, constipation, fatigue, and dry mouth. NSAIDs can make chronic kidney problems worse, so if you have kidney problems your doctor will be monitoring you closely with regular tests. People who have to take the drugs for more than a week or two at a time should thoroughly discuss the risks with their doctors.

Celecoxib (Celebrex) is an NSAID that belongs to a class of drugs called COX-2 inhibitors. These drugs were heralded as a major breakthrough when they first appeared on the market in 1998 because they work in a more targeted way than traditional NSAIDs, selectively blocking the COX-2 enzyme. As COX-1 is involved in many "housekeeping" functions in the body, including producing protective stomach mucus, this makes the targeted drugs less likely to cause ulcers, in theory. But there’s some controversy about whether they really do prevent ulcers, and they have another downside: They may increase the risk of heart disease or stroke, at least as much as other prescription NSAIDs. In fact, the Food and Drug Administration ordered labeling changes for all NSAIDs, including Celebrex, to include a boxed warning of the potential for increased risk of cardiovascular problems and life-threatening gastrointestinal bleeding associated with the drug's use.

A 2006 study published in the Journal of the Royal Society of Medicine, a British journal, concluded that patients taking celecoxib more than doubled the risk of heart attacks. A similar medication -- rofecoxib (Vioxx) -- was pulled off the market in 2004 after studies found that an unexpectedly large number of patients developed heart trouble. Again, patients taking celecoxib for prolonged periods should talk to their doctor about the potential risks.

Two hundred years after the discovery of morphine, this drug and others like it continue to play a major role in pain relief. Morphine and codeine are opiates, found naturally in opium poppies. Newer synthetic drugs such as oxycodone (Oxycontin), hydrocodone (Vicodin), and fentanyl (Duragesic) all belong to a class of medications called opioids because they are related to the opiate drugs. These drugs all work by blocking pain messages in the brain, and are commonly prescribed to treat chronic pain caused by cancer, damaged nerves, and inflammatory diseases such as rheumatoid arthritis.

Short-acting formulas are often combined with acetaminophen, so make sure you check the label if you are already taking it in another medication; according to the American Liver Foundation, the total dosage of acetaminophen should not exceed 3,000 mg/day for any prolonged period of time. People with liver or kidney problems, or who drink regularly, should also check with their doctor before using acetaminophen.

Although they are highly effective for many types of pain, opioids are also controversial. When taken inappropriately, the drugs can be highly addictive: Heroin is derived from morphine, and oxycodone addiction is a growing problem. People who legitimately need pain relief may be reluctant to take opioids out of a fear of addiction, and doctors may be reluctant to prescribe the medications for fear of patients getting patients hooked.

Much of the fear is unfounded. According to a joint statement from the American Academy of Pain Medicine and the American Pain Society, opioids rarely cause addiction when taken as directed for pain relief. For example, a study published in the New England Journal of Medicine of 12,000 patients treated with opioids found only four cases of addiction in people who didn’t already have a history of drug abuse.

Over time, the body can become used to opioids, and a patient may need gradually increasing doses to get the same level of relief. This phenomenon, called tolerance or dependence, is not the same as an addiction, and it’s not a major cause for alarm. The American Academy of Pain Medicine and the American Pain Society assert that tolerance shouldn’t be a barrier to long-term treatment with opioids. When necessary, doctors can simply adjust the dosage to meet the patient’s changing needs. The organizations also note that tolerance may not be as common as once thought: In many cases, people need increasing amounts of pain relief simply because their condition is becoming gradually more painful. However, at high doses there are more side effects.

Addiction isn’t the only possible risk when taking opioids. Constipation is almost inevitable with long-term treatment. A doctor may prescribe stool softeners or laxatives along with opioids to avoid this unpleasant complication, especially if you are taking opioids daily. Other common side effects include dry mouth, nausea, vomiting, and itching. If you haven't taken these drugs before, you and your family will be asked to watch carefully for extreme drowsiness or dizziness, confusion, bluish or clammy skin, dramatic slowdowns in breathing or heart rate, and other signs of extreme sensitivity and overdose.

Opioids come in several different forms. A controlled release drug that spreads the medication throughout the day will bring more consistent relief than a quick-acting drug that works all at once. Controlled release drugs are available in pills (such as CR oxycodone) or patches (such as transdermal fentanyl). Fentanyl patches have been linked to accidental fatal overdoses and should be used with extreme caution. Cancer patients or patients in hospice who have trouble swallowing, among others, may also be given liquid morphine.

Lidocaine, prilocaine, and similar medications have prevented many tears from being shed in doctors' and dentists' offices. Anesthetic drugs numb nerve endings and are often applied to skin to take the sting out of shots. They are also used to relieve itchy skin and numb toothaches and mouth sores. Recently doctors have found new uses for these medications. A patch that slowly releases lidocaine is now a common treatment for pain that comes from nerve damage, including pain associated with shingles. Lidocaine can also be injected to relieve chronic pain stemming from injured nerves, such as in carpal tunnel syndrome.

If your pain has not responded to other treatments, your doctor may consider prescribing something different. Drugs developed to treat depression and epilepsy are now widely used off-label (often in combination with other medications) to treat certain types of chronic pain because they alter spinal cord and brain chemistry. (Off-label use refers to the legal practice of prescribing drugs for a purpose outside the scope of the drug's Food and Drug Administration-approved label.) They are most helpful in treating neuropathic conditions, in which someone feels chronic pain from nerves that have been damaged during tissue injury. In these conditions, the nervous system often keeps sensing pain even when there is no current injury; they include phantom limb pain (in which an amputee feels pain in a missing limb), diabetic neuropathy, multiple sclerosis, and Parkinson's disease. Physicians may prescribe antidepressants and antiepileptics for certain non-neuropathic pain syndromes such as fibromyalgia and low back pain.

Commonly used drugs include tricyclic antidepressants such as desipramine (Norpramin) and amitriptyline (Elavil), and antiepileptic drugs such as carbamazepine (Tegretol) and pregabalin (Lyrica). Keep in mind that antidepressants such as desipramine and amitriptyline carry black box warnings from the FDA for increased risk of suicidal behavior. If you and your doctor decide to use a drug for an off label use, your doctor will want to monitor you closely and may try several different drugs or combinations before finding something that works for you. As always, please be sure to tell your doctor about all medications and supplements you are taking, whether OTC or prescription, because of many possible drug interactions, especially with antidepressants.

-- Deepi Brar is the multimedia editor for Consumer Health Interactive. Chris Woolston, MS, is a contributing editor to Consumer Health Interactive. A former staff writer for Hippocrates magazine, he has written for Health, WebMD, and other journals. He is also the co-author of Generation Extra Large: Rescuing Our Children from the Epidemic of Obesity (Perseus paperback, 2006).

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First published December 7, 2006
Last updated May 12, 2008
Copyright © 2006 Consumer Health Interactive

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