Drug Therapies
"Pain is deeper than all thought; laughter is higher than all pain"
Elbert Hubbard
American’s are quick to look for a pill that brings relief when they find themselves in pain, and most doctors and pharmacists are most obliging when their patients request a pain medication. Indeed, there are some wonderful medications available to bring rapid relief to pain suffers, but the savvy consumer will use other therapies in combination with pain medication to remedy the cause of the discomfort. Pills do little to cure the source of the pain, but generally work to mask the symptom of pain.
Both acute and chronic pain is almost always a symptom of a disease process or injury, and is not a malady unto itself. Today there are a number of routes of administration to deliver pain medications to the body, and are available both over-the-counter (OTC) and by preblockedion. Most pain management experts agree that for optimal management of pain any kind medication should be taken before the pain reaches it peak for effective, continuous pain control. This means that medication should be taken on a regular schedule, or shortly after the pain is first noticed by the patient.
Over-the-Counter Medications
Milder forms of pain may be relieved by over-the-counter medications such as Tylenol (acetaminophen) or nonsteroidal anti-inflammatory drugs (NSAIDs). Both acetaminophen and NSAIDs relieve pain caused by muscle aches and stiffness, but only NSAIDs can also reduce inflammation (swelling and irritation). Topical pain relievers are also available, such as creams, lotions, patches, or sprays that are applied to the skin in order to relieve pain from sore muscles and arthritis.
Acetaminophen is used to treat mild-to-moderate pain and reduce fever. Acetaminophen provides relief from pain by elevating the amount of pain one can tolerate before experiencing the feeling of pain. The best-known brand of acetaminophen is Tylenol, but there are also many generic versions available.
Two drugs in the NSAID category, ibuprofen and naproxen, reduce fever. NSAIDs work by reducing the body's production of prostaglandin, an enzyme that sends pain messages to the brain. When these drugs are taken regularly, they build up in the blood to levels that fight pain caused by inflammation and swelling, and also provide general pain relief.
There are several different types of NSAIDs. These include:
- Aspirin (Bayer Aspirin, Ecotrin, Excedrin, St. Joseph's, and many others)
- Ibuprofen (Advil, Motrin, and others)
- Ketoprofen (Orudis)
- Naproxen (Aleve)
Recently, there has been a good deal of controversy associated with NSAID pain relievers because of their unwanted potential side effects. The FDA has pulled two preblockedion NSAIDS, Vioxx and Bextra, off the market and has required the makers of Celebrex to issue new warnings on its label. These drugs may be associated with an increased risk of serious cardiovascular events (heart attack and stroke) especially when they are used for long periods of time or in very high risk settings (immediately after heart surgery).
Preliminary results from a long-term clinical trial (up to three years) suggest that long term use of a non-preblockedion NSAID, naproxen (sold as Aleve, Naprosyn and other trade names and generic products), may be associated with an increased cardiovascular risk when compared to placebo treatment. [i]
Although over-the-counter pain relievers are not thought to be physically addictive, they do hold a small potential for fostering a psychological addiction in that some patients will not risk going a day without taking their OTC pain reliever for fear that their pain will return.
Non-Narcotic Preblockedion Medications for Pain Relief
Cox-2 Inhibitors: A new class of NSAIDs is gaining wide acceptance in its ability to reduce inflammation. Commonly called COX-2 inhibitors, these newer NSAIDS work by selectively blocking the formation of pain-causing inflammatory chemicals. COX-2 inhibitors appear to be easier on the stomach, mainly because they don't interrupt stomach enzymes like traditional NSAIDs. Celebrex is the most commonly prescribed COX-2 inhibitor.[ii] Be aware, however, that Vioxx and Bextra are also in this class of drugs and are no longer available, so Celebrex is the only one currently on the market.
Muscle Relaxants: If a patient is having muscle spasms, muscle relaxants may help relieve pain. They have only been shown to be marginally effective. Muscle relaxants also have a significant risk of drowsiness and depression. Long-term use is not suggested; only three to four days is typically recommended.
Anti-depressants: Back pain is a common symptom of depression and could be an indicator of its presence. Similarly back pain can lead to emotional distress and depression. It seems that the same chemical reactions in the nerve cells that trigger depression also control the pain pathways in the brain. Anti-depressants such as Elavil can relieve emotional stress associated with back pain.
Some types of anti-depressants make good sleeping medications. If the patient is having trouble sleeping due to back pain, the doctor may prescribe an anti-depressant to help return the patient to a normal sleep routine. Anti-depressants can have side effects such as drowsiness, loss of appetite, constipation, dry mouth, and fatigue.
Anticonvulsants: Tegretol is a seizure medication that can treat some kinds of pain. Specifically, neuralgic pain, which is seldom responsive to NSAIDS, Tylenol or codeine, does tend to respond well to Tegretol.
Narcotic Pain Medications
It is commonly known that if one aspirin works well, two will work even better. It is dangerous to apply this same logic to the ingestion of narcotic pain medications. Taking more than the maximum dose prescribed will not increase the pain relief, but may cause toxic side effects such as stomach ulcers, kidney damage, liver damage, chemical imbalance in the bloodstream, or death.
Strong opioid medications are slightly different in this regard, and this is fortunate for people who suffer from severe pain. With strong opioids, the dose depends on the amount of pain. These medications should not be mixed with acetaminophen or other non-opioid drugs when used to treat chronic pain. People with intense pain can take very high doses of opioids without getting side effects. Some people with intense pain get such high doses that the same dose would be fatal if taken by someone who was not suffering from pain. In the pain patient, that same high dose can control the pain and still allow the person to be wide awake enough to do his or her activities of daily living.
Opioids: Opioids are commonly prescribed because of their effective analgesic, or pain relieving, properties. Studies have shown that properly managed medical use of opioid analgesic compounds is safe and rarely causes addiction. Taken exactly as prescribed, opioids can be used to manage pain effectively.
Among the compounds that fall within this class—sometimes referred to as narcotics—are morphine, codeine, and related medications. Morphine is often used before or after surgery to alleviate severe pain. Codeine is used for milder pain. Other examples of opioids that can be prescribed to alleviate pain include oxycodone (OxyContin—an oral, controlled release form of the drug); propoxyphene (Darvon); hydrocodone (Vicodin); hydromorphone (Dilaudid); and meperidine (Demerol), which is used less often because of its side effects.
Opioids act by attaching to specific proteins called opioid receptors, which are found in the brain, spinal cord, and gastrointestinal tract. When these compounds attach to certain opioid receptors in the brain and spinal cord, they can effectively change the way a person experiences pain.
In addition, opioid medications can affect regions of the brain that mediate what we perceive as pleasure, resulting in the initial euphoria that many opioids produce. They can also produce drowsiness, cause constipation, and, depending upon the amount taken, depress breathing. Taking a large single dose could cause severe respiratory depression or death.
Opioids may interact with other medications and are only safe to use with other medications under a physician's supervision. Typically, they should not be used with substances such as alcohol, antihistamines, barbiturates, or benzodiazepines. Since these substances slow breathing, their combined effects could lead to life-threatening respiratory depression.
Long-term use also can lead to physical dependence—the body adapts to the presence of the substance and withdrawal symptoms occur if use is reduced abruptly. This can also include tolerance, which means that higher doses of a medication must be taken to obtain the same initial effects. Note that physical dependence is not the same as addiction—physical dependence can occur even with appropriate long-term use of opioid and other medications. Addiction, as noted earlier, is defined as compulsive, often uncontrollable drug use in spite of negative consequences.
Symptoms of withdrawal can include restlessness, muscle and bone pain, insomnia, diarrhea, vomiting, cold flashes with goose bumps, and involuntary leg movements.
Long-acting opioids: The best way to treat chronic, severe pain is by keeping it under control all the time. A long-acting opioid works to keep the pain under control over a protracted period of time, and a short-acting opioid is used to deal with those few times during the day when the pain breaks through. Morphine, for example, comes in a slow-release tablet that keeps pain under control most of the time, and a short-acting tablet or liquid for those times when pain breaks through.
Some opioids are not recommended for chronic pain. Demerol (meperidine), which is used often for acute pain after surgery, is a poor drug for chronic pain. It is not absorbed well when taken by mouth, and it causes dysphoria (feeling truly lousy) and seizures if used for more than a few days. Talwin (pentazocine) is also bad for chronic pain. It has a ceiling effect. There is a maximum dose after which raising the dose gives no further pain relief. It also causes withdrawal symptoms when given to someone who is also taking another opioid. The opioid/acetaminophen (Percocet, for example) or opioid/NSAID (Percodan, for example) combination drugs are fine for short-term use, but acetaminophen is poisonous to the kidneys and liver when used for a long time or in high doses.
Fentanyl: Fentanyl is a powerful synthetic opiate analgesic similar to, but more potent than morphine. It is typically used to treat patients with severe pain, or to manage pain after surgery. It is also sometimes used to treat people with chronic pain who are physically tolerant to opiates. It is a schedule II preblockedion drug.In its preblockedion form, fentanyl is known as Actiq, Duragesic, and Sublimaze. Like heroin, morphine, and other opioid drugs, fentanyl works by binding to the body's opiate receptors, highly concentrated in areas of the brain that control pain and emotions. When opiate drugs bind to these receptors, they can drive up dopamine levels in the brain's reward areas, producing a state of euphoria and relaxation. When prescribed by a physician, fentanyl is often administered via injection, transdermal patch, or in lozenge form.
Oxycodone: Oxycodone is a potent and potentially addictive opioid analgesic medication synthesized from thebaine. Its name is derived from codeine and their chemical structures are very similar. It is effective orally and is marketed in combination with aspirin (Percodan, Endodan, Roxiprin) or paracetamol/acetaminophen (Percocet, Endocet, Roxicet, Tylox) for the relief of pain. More recently, ibuprofen has been added to oxycodone (Combunox). It is also sold in a sustained-release form under the trade name OxyContin as well as generic equivalents, and instant-release forms Endone, OxyIR, OxyNorm, Percolone, OxyFAST, and Roxicodone. Due to its sustained-release mechanism, is effective for eight to twelve hours. In the United States, oxycodone is a Schedule II controlled substance both as a single agent and in combination products containing acetaminophen, ibuprofen or aspirin.
Oxycodone can be administered orally, intranasally, via IV, IM or Sub Q injection, or rectally. Oral oxycodone is the most efficient means of administration. Injecting oxycodone will result in a stronger effect and quicker onset.
Oxycodone is used in treatment of moderate to severe chronic pain. When used at recommended doses for relatively short periods (several weeks), it provides effective pain control with manageable side effects. Nausea, constipation, lightheadedness, rash or itchiness, dizziness, and emotional mood disorders are the most frequently reported side effects. Other side-effects can also include slightly decreased testosterone levels in men. Misuse or long-term medical use of the drug can cause temporary impotence as well as a significant prostate enlargement in men.
Tolerance and physical dependence occurs after several days to weeks of treatment, with larger doses being required to achieve the same degree of analgesia. According to the companies that manufacture the drug, psychological addiction as a result of medical use is uncommon. Despite this statement, there are several lawsuits underway brought by plaintiffs who claim to have developed addiction as a result of medical use.[iii]
Addiction to Narcotic Pain Medications
Individuals who become addicted to preblockedion medications can be treated. Options for effectively treating addiction to preblockedion opioids are drawn from research on treating heroin addiction. Some pharmacological examples of available treatments include:
- Methadone, a synthetic opioid that blocks the effects of heroin and other opioids, eliminates withdrawal symptoms and relieves craving. It has been used for over 30 years to successfully treat people addicted to opioids.
- Buprenorphine, another synthetic opioid, is a recent addition to the arsenal of medications for treating addiction to heroin and other opiates.
- Naltrexone is a long-acting opioid blocker often used with highly motivated individuals in treatment programs promoting complete abstinence. Naltrexone also is used to prevent relapse.
- Naloxone counteracts the effects of opioids and is used to treat overdoses.
It is noteworthy to mention that chronic pain patients who are prescribed narcotics are at risk of becoming victims of crime. Drug addicts who become aware that the pain patient is in possession of these powerful drugs may be willing to mug or rob the patient of their medication in order to get the “fix” that they need.
Trigger Point Injections
Trigger point injection (TPI) may be an option in treating pain for some patients. TPI is a procedure used to treat painful areas of muscle that contain trigger points, or knots of muscle that form when muscles do not relax. Many times, such knots can be felt under the skin. Trigger points may irritate the nerves around them and cause referred pain, or pain that is felt in another part of the body.
In the TPI procedure, a health care professional inserts a small needle into the patients trigger point. The injection contains a local anesthetic that sometimes includes a corticosteroid. With the injection, the trigger point is made inactive and the pain is alleviated. Usually, a brief course of treatment will result in sustained relief. Injections are given in a doctor's office and usually take just a few minutes. Several sites may be injected in one visit. If a patient has an allergy to a certain medication, a dry-needle technique (involving no medications) can be used.
TPI is used to treat many muscle groups, especially those in the arms, legs, lower back, and neck. In addition, TPI can be used to treat fibromyalgia and tension headaches. TPI also is used to alleviate myofascial pain syndrome (chronic pain involving tissue that surrounds muscles) that does not respond to other treatments.
Spinal Drug Delivery Systems
Pain relief through spinal drug delivery systems, also called intrathecal drug delivery systems, involves implanting a small pump that delivers medication directly to the spinal cord, where pain signals travel. In many cases, spinal drug delivery systems are used to treat people who have cancer pain or chronic pain.
Spinal drug delivery systems increase pain relief and comfort for people with severe pain with less medicine. In addition, the system can cause fewer side effects than oral medications because less medicine is required to control pain. People who have extreme pain can improve their quality of life and become more involved in daily activities with the help of the systems.
Nerve Blocks
Nerve blocks are used for pain treatment and management. There are several different types of nerve blocks that serve different purposes. Often a group of nerves, called a plexus or ganglion, that causes pain to a specific organ or body region can be blocked with the injection of medication into a specific area of the body. The injection of this nerve-numbing substance is called a nerve block.
Different kinds of nerve blocks are used for different purposes. Therapeutic nerve blocks are used to treat painful conditions. Such nerve blocks contain local anesthetic that can be used to control acute pain. Prognostic nerve blocks predict the outcomes of given treatments. For example, a nerve block may be performed to determine if more permanent treatments (such as surgery) to block the activity of a nerve would be successful in treating pain.
Side effects and risks involved with using nerve blocks include elevated blood sugars, rash, itching, weight gain, extra energy, soreness at injection site, bleeding, and in rare cases, death.
Patient-Controlled Analgesia (PCA)
Patient controlled analgesia (PCA) is a method of pain control that gives the patient the power to control their pain. In PCA, a computerized pump contains a syringe of pain medication as prescribed by a doctor, and is connected directly to a patient's intravenous (IV) line.
In some cases, the pump is set to deliver a small, constant flow of pain medication. Additional doses of medication can be self-administered as needed by the having the patient press a button. Other times, a patient can control when he or she receives pain medication and does not receive a constant flow.
Patients recovering from surgery often are equipped with PCA pumps. The machines also can be used by people coping with other kinds of pain. Children who are four to six years old may be able to use PCA with the help of a parent or nurse. Children who are as young as seven can independently use the PCA pump.
The pump can be used whenever the patient is feeling pain. However, patients should not press the button on the machine if they are feeling too sleepy. The more alert the patient is, the more likely he or she is to participate in a therapy program to aid and possibly shorten recovery. Once the acute pain from surgery is controlled, the patient will be switched to pills for pain relief. PCA pumps have built-in safety features. The total amount of analgesic (pain reliever) that the patient can self-administer is within a safe limit.
Study Questions
Answering the following questions is an optional activity. These questions are provided as a study aid to help you prepare to take the post test.
- Even though NSAIDS that are COX-2 Inhibitors are non-narcotic, they hold certain risks. What are the risks associated with this group of drugs?
- Name 3 types of drugs that are non-narcotics and are not NSAIDS, yet are used to treat pain as well as other conditions.
- What are the benefits to using opioids for relief of chronic pain?
- What are the risks involved in using opioids for relief of chronic pain?
- How are Trigger Point Injections and Nerve Blocks similar and how are they different?
