Pain Medications

Pain is an unpleasant sensation. Pain can be sharp or dull, burning or numbing, minor or major, acute or chronic. It can be a minor inconvenience or completely disabling.

Both the area of the injury and how the brain deals with signals from the area of pain affect the sensation. Generally, medications try either to stop the transmission of pain from the site of injury or to affect the brain directly.

The tolerance of pain varies greatly from one person to another and the effects of pain medications are different for different people. For this reason, one medication may not be right for everyone with the same injury. For example, an over-the-counter medication for an ankle sprain may be adequate for some, while others will need a more powerful prescription pain reliever. The right pain medication depends on the person experiencing the pain, not on the condition that is causing the pain.

The most common nonsteroidal anti-inflammatory drug (NSAID) for pain is ibuprofen. Three NSAIDs are available without a prescription in drug and grocery stores:

Naproxen

• Aleve

Ibuprofen

• Advil
• Children's Advil
• Children's Motrin
• Excedrin IB
• Midol 200
• Motrin IB
• Nuprin
• Pamprin IB

Aspirin

• Anacin
• Ascriptin
• Aspergum
• Bayer Aspirin
• Bayer Buffered Aspirin
• Bayer Low Adult Strength
• Bufferin
• Ecotrin
• Empirin
• St Joseph Adult Chewable Aspirin

Essentially, aspirin and ibuprofen are short-acting, while the effects of naproxen last longer. This difference means sometimes it takes three to four doses of naproxen before an effect is noted. Because of this difference, it may be better to use ibuprofen for more immediate relief from pain and to use naproxen for long-lasting relief.

Many NSAID medications are available only with a prescription. These include:

• fenoprofen (Nalfon)
• flurbiprofen (Ansaid)
• ketoprofen (Oruvail)
• oxaprozin (Daypro)
• diclofenac sodium (Voltaren, Voltaren-XR, Cataflam)
• etodolac (Lodine)
• indomethacin (Indocin, Indocin-SR)
• ketorolac (Toradol)
• sulindac (Clinoril)
• tolmetin (Tolectin)
• meclofenamate (Meclomen)
• mefenamic acid (Ponstel)
• nabumetone (Relafen)
• piroxicam (Feldene)

This class of drugs is one of the most marketed types of medications by drug companies. No clear evidence exists that the prescribed medicines that cost more are any better than those that cost less.

Different NSAIDs also are marketed as being better for certain conditions. An example is indomethacin (Indocin) as a recommended treatment for gout. There is no proof this is true, but some evidence shows that different families of NSAIDs may have a selective effect on a person-to-person basis.

The main side effect of these types of medicines is that they can cause bleeding and irritation in the stomach. This bleeding usually occurs after long-term use but can also occur with short-term use. Long-term use can also affect the kidneys, (for these reasons, acetaminophen is probably safer for long-term use, although taking too much acetaminophen can cause liver damage).

NSAIDs have both a pain-relieving and inflammation-stopping effect. Generally, the pain-relieving effect does not increase with higher doses; thus, 400 mg of Motrin has just as much pain relief as 800 mg of Motrin. A person is more likely to suffer a significant stomach problem with the higher dose.

Consult a doctor if a person taking NSAIDs experiences pain in the stomach, has black stools, or has blood in the stool.

• Long-term use of NSAIDs can cause bleeding in the stomach. In response to this, the drug industry has produced a class of NSAIDs, the COX-2 Inhibitor.
• Presently, only celecoxib (Celebrex) remains on the market. Valdecoxib (Bextra) and rofecoxib (Vioxx) were voluntarily withdrawn from the market because of an increased risk of heart attack, stroke, and severe skin toxicity (see below).
• Because these medications have been on the market for only a short time, the long-term side effects are just beginning to be understood. These medications have not been proven to be stronger than ibuprofen, acetaminophen, or naproxen. It is also unclear whether these medications cause less significant stomach problems.
• People older than 75 years are at more risk of significant stomach problems, such as ulcers, from NSAIDs, especially if they have had previous ulcers. Elderly individuals also typically have higher risk factors for heart attack and stroke.
• Alert: On September 30, 2004, Merck & Co, Inc, announced a voluntary withdrawal of the COX-2 inhibitor, rofecoxib (Vioxx), from the US and worldwide market because of its association with an increased rate of cardiovascular events (including heart attacks and strokes) compared to that of placebo. A major US Food and Drug Administration (FDA) study of rofecoxib found an apparent 3-fold increase in the risk of sudden cardiac death or heart attack among patients who had taken higher doses of the drug compared to the risk of patients who had not recently received similar medication. The report showed that even patients taking the standard starting dose of 12.5 mg or 25 mg of rofecoxib had a 50% greater chance of heart attack or sudden cardiac death than patients on any dose of celecoxib (Celebrex). The large-scale study was conducted after analyzing the medical records of 1.4 million people insured by Kaiser Permanente in Oakland, Calif, between 1999-2001.
• Alert: On April 7, 2005, valdecoxib (Bextra, by Pfizer, Inc) was voluntarily withdrawn from the US market, pending further discussion with the FDA. The association of valdecoxib with potentially life-threatening risks, including myocardial infarction, stroke, and serious skin reactions, initiated an investigation to determine whether the benefits of the drug outweighed the risks. The serious skin reactions are most likely to occur in the first two weeks of treatment, but they can occur at any time during therapy. Other COX-2 inhibitors and traditional NSAIDs (for example, naproxen [Aleve, Naprosyn], ibuprofen [Motrin]) also have a risk for these rare, serious skin reactions, but the reported rate of the reaction appears to be greater for valdecoxib. Data regarding risks in individuals who take valdecoxib following heart bypass surgery showed an increased risk of heart attack, stroke, deep vein thrombosis (blood clots in the leg), and pulmonary embolism (blood clots in the lungs).
• Celecoxib (Celebrex) remains on the market and appears to have the same cardiac risk profile as does ibuprofen.

Acetaminophen is just as effective as NSAIDs for noninflammatory types of pain if used in proper doses. Acetaminophen has few side effects and does not interact with other medications in any significant way. The only people who should avoid it are those with chronic liver problems. Even in this group, a day or two of use is probably safe; consult your doctor. It is available in a variety of brand names.

For adults, the dose of acetaminophen is up to a gram (two extra strength [500 mg] or three regular strength [325 mg]) every four hours. Do not take more than four doses per day. Acetaminophen is contained in many over-the-counter products (such as cold or sinus medication), and if these products are taken in addition to acetaminophen, it is possible to take overall doses that are higher than the recommended maximum dose. When taking pain medication or combinations of pain medicine, check whether they contain acetaminophen to assure that more of the recommended dose is not taken mistakenly.

For stronger pain relief, acetaminophen is combined with narcotic type drugs. These drugs can be obtained only with a prescription.

For moderately severe pain, a doctor may prescribe a combination pill with acetaminophen and a narcotic.

• Acetaminophen with codeine (Tylenol with Codeine, Capital and Codeine, Phenaphen with Codeine)
• Acetaminophen with hydrocodone (Vicodin, Anexsia, Anodynos-DHC, Bancap HC, Co-Gesic, Dolacet, Lortab, Margesic H, Medipain 5, Norcet, Stagesic, T-Gesic, Zydone)
• Acetaminophen with oxycodone (Percocet, Roxicet, Endocet, Roxilox, Tylox)

It is difficult to evaluate the relative strength of different medications because all medications affect people differently.

• Tylenol with codeine is no stronger than an adequate dose of ibuprofen. It also has unpleasant side effects such as nausea, vomiting, constipation, and feeling disoriented. Codeine must be converted by the body to morphine to be effective. Some people lack the enzyme necessary to do the conversion. In these people, codeine is not effective.
• Vicodin is probably twice as strong as acetaminophen or any NSAID and has few side effects. However, use can lead to dependency and it is increasingly being abused, so its use should be limited (less than a week), except under the management of your doctor or a pain management specialist. The potential for narcotic addiction exists in certain people.
• Percocet is probably stronger than Vicodin and is very similar in its safety and side effect profiles. The main side effect of both is constipation.

An effective way to take these medications for short-term pain resulting from something such as an injury or kidney stone is to take a regular dose of an NSAID such as ibuprofen and then take a Percocet or Vicodin as needed.

For severe pain, prescription narcotics are available.

• In high doses, they can affect breathing. In some cases, narcotics can lead to death if the person stops breathing. Medications taken by mouth are less likely to affect breathing.
• A doctor must supervise the adjustment of the dosage.

Narcotics, like all pain medications, can be used for both acute and chronic pain.

• Acute pain is pain which expected to occur after some event, such as an injury or surgery and that goes away after healing.
• Chronic pain is pain which persists after the expected healing time or is due to the underlying disease.

Narcotics are also divided into categories, called Schedules, by the government. Hydrocodone compounds, such as Vicodin, originally Schedule III, are now Schedule II  with many other narcotics. For the patient, a major difference is that a physician can call or fax in a Schedule III prescription to the pharmacy, whereas a Schedule II medication requires a tamper proof prescription that the patient must deliver directly to the pharmacy.

Narcotics can be classified as either immediate release, with an effect lasting several hours, or sustained release, with effects lasting anywhere from eight hours to three days. Physicians use the sustained release forms primarily for chronic pain, where there is a continual need for pain relief. The intent is that by providing constant relief, the person suffering from chronic pain can focus on living their life (maintaining function) rather than constantly worrying about taking the next pill. In this way, physicians hope to minimize the occurrence of addiction.

Immediate release medications are used in the acute pain setting and the chronic pain setting to treat breakthrough pain, or short-lived (up to about an hour) pain that occurs because of increased activity or sometimes for no reason at all. There are many commonly prescribed immediate release medications, including preparations of morphine, oxycodone, hydromorphone,  meperidine, oxymorphone and fentanyl. Most of these medications are pills. Fentanyl comes in two preparations, Actiq and Fentora, which allow it to be absorbed into the blood stream through the lining of the mouth or the skin. Actiq and Fentora have the advantage of fast onset and have been approved by the FDA for cancer breakthrough pain.

The following are five commonly prescribed sustained release narcotic medications:

• morphine (MS Contin, Avinza, Kadain, Oramorph)
• oxycodone (OxyContin, Roxicodone, M-oxy, ETH-Oxydose, Oxyfast, OxylR)
• fentanyl (Duragesic, Fentanyl Patch)
• oxymorphone (Opana)
• methadone (Methadose)

Meperidine (Demerol) is not a very effective oral pain medication and should not be used as such. With all opioids, the major side effects are sedation, nausea, and constipation. Anyone taking narcotics should treat possible constipation, by maintaining a high fluid intake, a high fiber diet, and using stool softeners.

The purpose of prescribing opioids for chronic pain is to allow someone who is in pain to function more normally. If someone is too sedated from the opioids to function, then the medications being prescribed should be re-evaluated or possibly a pump should be used to deliver the medications into the intrathecal space (into the cerebrospinal fluid that surrounds the brain and spinal cord).

Most people using chronic opioid therapy do drive. Consult the prescribing physician before taking pain medication and driving, operating heavy machinery, or performing any job that may put the patient or others in danger. If someone taking opioids is involved in a traffic accident, they can be charged with driving under the influence.

Another sustained release nonnarcotic pain medication is tramadol (Ultram ER). It has been placed in Schedule IV by the FDA, because there is significant abuse potential with this drug. While it is a less strong analgesic than the other "scheduled" narcotics, it is very useful in some chronic pain patients who do not require stronger analgesics and also in patients who have a history of substance abuse whose physicians wish to avoid scheduled medications.

A major concern with the prescribing of opioids is to ensure that they are used to treat pain and not abused for the euphoric effect that some people get when they take them. The Federal government demands that physicians who prescribe opioids do so for a legitimate medical purpose and they do not prescribe for either abuse or diversion. Every State Medical Board expands upon these prescribing requirements. For example, physicians should do a physical exam on every patient for whom medication is prescribed, making the Internet prescribing of these medications illegal. These issues are of particular concern in that the largest area of growth in drug abuse is the use of prescription medications rather than street drugs.

Many patients are concerned about addiction. Addiction is a confusing word, in that it has two meanings: physical addiction and psychological addiction.

Physical addition means that the body is used to having the narcotics on board. Abruptly stopping the medication can lead to withdrawal symptoms such as:

• flu-like symptoms,
• nausea,
• vomiting,
• diarrhea,
• bone aches,
• feeling like you are "crawling out of your skin,"
• goose bumps,
• chills,
• tremor, and
• difficulty sleeping.

These symptoms are all medical concerns and should be treated medically. Do not stop taking opioids unless under the direction of a physician.

Psychological addiction refers to craving for the narcotics, where the focal point of one's life is getting the opioids. Some people's brains are hardwired to crave narcotics. This drive is difficult to control and requires specific medical treatment. Patients suffering from psychological addiction are not good candidates for narcotic therapy to treat pain.

According to the National Institute on Drug Abuse, more than 90 Americans die every day from an overdose of an opioid, including prescription pain relievers, heroin and synthetic opioids such as Fentanyl. 

In 2015, more than 33,000 Americans died from an opioid overdose. This is now considered a national crisis affecting public health as well as having an economic and social impact. The CDC (Centers for Disease Control and Prevention) estimates that opioid misuse alone costs $78.5 billion a year. 

Abuse Statistics for Patients Prescribed Prescription Opioids

• About 21-29% of patients prescribed opioids for chronic pain misuse them
• About 8-12% develop an opioid disorder
• About 5% of patients that misuse prescription opioids transition to heroin

Other problems associated with the Opioid Crisis include neonatal abstinence syndrome among babies born to mothers misusing prescription opioids, and the spread of Hepatitis C and HIV due to injection drug use.

In addition to Tylenol with codeine and oral Demerol, certain other pain medications probably should be avoided for several different reasons.

Some medications just do not work very well, while others have significant side effects that, at times, can be dangerous. Often, less expensive medications are just as effective as expensive medications.

• pentazocine (Talwin) has very little pain-relieving effect and is strongly associated with dependency. It is of little value as a pain medication.
• propoxyphene (Darvon, Darvocet) likewise has no significant pain-relieving benefit compared to other options. In 2010 the FDA removed propoxyphene and its derivatives from the US market.