Soft Tissue Pain Clinic

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The Alternatives
 Medication for Pain

Just because it isn’t prescribed by a doctor doesn’t mean that it is safe.

 

Just because you can buy many medicines without a prescription doesn't mean they're entirely safe. Over-the-counter drugs can kill you. It is very important that you always read the labels of over-the-counter medications. Make sure that you take into consideration combined doses when combining drugs.


Over-the-counter medications come in two main types:

  • analgesics/antipyretics 
  • Nonsteroidal Antiinflammatory Drugs (NSAIDs)  

 

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Analgesics/Antipyretics


Tylenol
(Acetaminophen)

Consider medications containing the active ingredient, paracetomol (also known as acetaminophen)Acetaminophen, commonly referred to as the brand name Tylenol (used by more than 200 million Americans a year), is not as safe as we all might think.  Acetaminophen can be highly toxic. The use of Tylenol instead of aspirin to treat fevers in infants has greatly reduced the occurrence of Reye's syndrome, an often fatal form of liver failure.  Ironically, however, taking too much Tylenol (an overdose) can also cause liver failure.  At Parkland Memorial Hospital (where President Kennedy died) in Dallas, acetaminophen is for example the #1 cause of acute liver failure.  The drug accounts for 100,000 calls to poison control centers, 56,000 emergency room visits, 26,000 hospitalizations, and 450 deaths annually.  Back to the top

 

Unsafe At Any Dose?

The FDA approved acetaminophen in 1951. The fact that an accidental overdose of acetaminophen can result in liver toxicity, liver failure, and even death has been known for some time.


Consumers may not be aware that acetaminophen
is an ingredient in nearly 200 medications both overthecounter (such as Excedrin, Midol, NyQuil, and Sudafed) and prescription (such as Vicodin), as well as many over-the-counter combination products, so they may unknowingly exceed the recommended maximum dose if they take more than one acetaminophen product without knowing that both contain acetaminophen. Most cases of liver damage occur in people who have taken at least 10-15 grams—more than twice the recommended dose. Many of the emergency room visits and deaths linked to acetaminophen poisoning are due to accidental or intentional overdoses (for example, suicide attempts). People who use over-the-counter medications should read labels carefully and look for the ingredient acetaminophen in analgesics, preparations for headaches, cold and allergy medications, sleep aids, preparations for osteoarthritis, and other products.

 

In addition some people are more susceptible to acetaminophen toxicity and can experience liver damage even at the recommended dose. A study by the U.S. Food and Drug Administration (FDA) showed that about 20% of people with acetaminophen-related liver toxicity had taken less than the recommended daily amount.

For other people, a dangerous dose is not much higher than the recommended dose—that is, the “window” between a therapeutic dose and a toxic dose is smaller for acetaminophen than it is for many other drugs.

 

Some experts also believe that taking acetaminophen for several days in a row may cause a dangerous build-up of the drug in the body. In 2006, the American Liver Foundation stated that acetaminophen should not be taken for more than 3 consecutive days, and then only sporadically.  Back to the top

 

Drug Class & Mechanism:

Acetaminophen belongs to a class of drugs called analgesics (pain relievers) and antipyretics (fever reducers). The exact mechanism of action of acetaminophen is not known.

 

Mode of action is not completely understood, but is thought to act in the brain. It has very weak effects on the COX-1 and COX-2 systems (see NSAIDs below), and therefore it has minimal peripheral anti-inflammatory actions, and does not cause gastric ulceration. Recent research suggests that it may work through a newly discovered COX-3 enzyme system.

 

Acetaminophen relieves pain by elevating the pain threshold, that is, by requiring a greater amount of pain to develop before a person feels it. It reduces fever through its action on the heat-regulating center of the brain. Specifically, it tells the center to lower the body's temperature when the temperature is elevated.   Back to the top

 

How Acetaminophen Harms the Liver ( i.e. the technical explaination )

Like many drugs, acetaminophen is metabolized by the liver. If the normal processing pathway is overwhelmed by a high dose, a different pathway known as the cytochrome P450 enzyme system kicks in. When this happens, a toxic metabolic byproduct called NAPQI is produced that can kill liver cells. Alcohol and

many other drugs also use the cytochrome P450 processing system, and the risk of a “bottleneck” is greater if the liver has to deal with both acetaminophen and these other substances at the same time. Acetaminophen poisoning has three stages. During the first 12- 24 hours after taking the drug, a person may experience nausea and vomiting. During the second phase, from 24-48 hours, the person usually feels better. After 48-72 hours, however, liver enzyme (ALT and AST) levels start to rise, indicating liver injury.  Back to the top

 

Potential Problems

Taking acetaminophen on an empty stomach causes a condition called acetaminophen toxicity. That alone kills 100 people every year. Toxicity occurs when your body cannot process the drug quickly enough. Acetaminophen, in itself, is a deadly poison to the human body. However, a healthy liver produces enzymes to counteract the poison. This is what gives us the analgesic effect that we all know and love from the drug. When someone is not receiving proper nutrition, the liver slows down on how quickly it can produce those enzymes. In turn, that leaves us with the poison in our systems.

 

Alcohol consumption is another key factor in potential liver damage from the drug. Individuals regularly consuming excess amounts of alcohol can develop liver toxicity at lower levels of acetaminophen intake. This, too, has been known for some time. It is not recommended that you take any NSAID (non steroid anti inflammatory drug) like acetaminophen if you consume more than three alcoholic drinks per day. Aspirin, ibuprofen, and naproxen sodium (Aleve) are all counted in that category, That means no more popping a handful of Tylenol to alleviate that hangover. Patients with liver and kidney disease should also exercise caution in taking acetaminophen.

 

Patients with overdoses of acetaminophen should seek emergency care immediately. Early treatment can prevent liver damage or death. The signs and symptoms of liver toxicity may not become apparent for 2-3 days after a toxic overdose.  Back to the top

 

The following tips can help prevent acetaminophen related liver toxicity:

• Do not take more than the recommended dose of 4 grams

within a 24-hour period (for example, 12 regular strength or 8

extra strength Tylenol tablets)

• Do not take the full day’s dose at one time; space it out over

the course of the day

• Do not take acetaminophen for more than 10 days in a row

• Avoid drinking alcohol; this is important for people with

hepatitis whether or not they use acetaminophen

• People who do consume 2-3 alcoholic drinks per day

should not take more than half the usual recommended dose

of acetaminophen (2 grams within 24 hours)

• People with advanced liver fibrosis or cirrhosis should avoid

acetaminophen

• Write down how much acetaminophen you take, and when,

if you have trouble remembering

• Check the labels of all medications; small doses of

acetaminophen in combination remedies can add up to big

trouble.

 

 

Web Reference:

Tylenol Toxicity

http://www.medicinenet.com/script/main/art.asp?articlekey=629

 

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Nonsteroidal Antiinflammatory Drugs (NSAIDs)

 

What are NSAIDs and how do they work?

Prostaglandins are a family of chemicals that are produced by the cells of the body and have several important functions. They promote inflammation, pain, and fever; support the blood clotting function of platelets; and protect the lining of the stomach from the damaging effects of acid.

Prostaglandins are produced within the body's cells by the enzyme cyclooxygenase (COX). There are two COX enzymes, COX-1 and COX-2. Both enzymes produce prostaglandins that promote inflammation, pain, and fever. However, only COX-1 produces prostaglandins that support platelets and protect the stomach. Nonsteroidal antiinflammatory drugs (NSAIDs) block the COX enzymes and reduce prostaglandins throughout the body. As a consequence, ongoing inflammation, pain, and fever are reduced. Since the prostaglandins that protect the stomach and support platelets and blood clotting also are reduced, NSAIDs can cause ulcers in the stomach and promote bleeding. Although NSAIDs have a similar mechanism of action, individuals who do not respond to one NSAID may respond to another.  Back to the top

 

For what conditions are NSAIDs used?

NSAIDs are used primarily to treat inflammation, mild to moderate pain, and fever. NSAIDs also are included in many cold and allergy preparations. Specific uses include the treatment of headaches, arthritis, sports injuries, and menstrual cramps. Aspirin (also an NSAID) is used to inhibit the clotting of blood and prevent strokes and heart attacks in individuals at high risk. Aspirin is a unique NSAID, not only because of its many uses, but because it is the only NSAID that inhibits the clotting of blood for a prolonged period (4 to 7 days). Most NSAIDs inhibit the clotting of blood for only a few hours. This prolonged effect of aspirin makes it an ideal drug for preventing blood clots that cause heart attacks and strokes.  Back to the top

 

What are the side effects of NSAIDs?

NSAIDs are associated with several side effects. The frequency of side effects varies among NSAIDs. The most common side effects are nausea, vomiting, diarrhea, constipation, decreased appetite, rash, dizziness, headache, and drowsiness. NSAIDs may also cause fluid retention, leading to edema. The most serious side effects are kidney failure, liver failure, gastric ulceration and bleeding, kidney impairment in the susceptible and elderly, increased bleeding risk due to an anti-platelet effect, poor asthma control in susceptible asthmatics, and potential drug interactions with other drugs.

Nonsteroidal antiinflammatory drugs also may increase blood pressure in patients with hypertension (high blood pressure) and therefore antagonize the action of drugs that are used to treat hypertension.  Back to the top

 

What NSAIDS are approved in the United States?

The complete list of approved NSAIDs is very long. The following list contains only NSAIDs that are commonly used:

aspirin

celecoxib (Celebrex)

diclofenac (Voltaren)

diflunisal (Dolobid)

etodolac (Lodine)

ibuprofen (Motrin)

indomethacin (Indocin)

ketoprofen (Orudis)

ketorolac (Toradol)

nabumetone (Relafen)

naproxen (Aleve, Naprosyn)

oxaprozin (Daypro)

piroxicam (Feldene)

salsalate (Amigesic)

sulindac (Clinoril)

tolmetin (Tolectin)


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Ibuprofen

 

Consider medications containing the active ingredient, Ibuprofen. Ibuprofen is commonly referred to as the brand name Advil, Motrin,or Nuprin. Ibuprofen is a nonsteroidal anti-inflammatory drug (NSAID), which relieves pain and swelling (inflammation). It is used to treat headaches, muscle aches, backaches, dental pain, menstrual cramps, arthritis, or athletic injuries. This medication is also used to reduce fever and to relieve minor aches and pain due to the common cold or flu.  Back to the top

 

Mode of action

NSAIDs produce a range of effects in the body by inhibiting the enzyme cyclo-oxygenase (COX). COX is the main enzyme which converts arachidonic acid to prostaglandins, thromboxane and prostacyclins. Decreasing prostaglandins helps to reduce pain, swelling, and fever. It is found in many central and peripheral tissues in the body, and this explains why NSAIDs have such a wide range of effects. The known effects of these drugs are:

  • analgesia - acting on peripheral tissues, the dorsal horn of the spinal cord, and the brain
  • anti-inflammatory - via the prostaglandin effect
  • anti-pyretic - temperature control in the brain
  • gastric ulceration - impaired gastric lining protection
  • anti-platelet - anti-thromboxane effect prevents platelets sticking together with increased bleeding tendency
  • renal impairment - altered kidney blood flow control worse with dehydration
  • increased wheezing in susceptible asthmatics increasing the muscle tone in the bronchi of the lungs   Back to the top


Side Effects:

Upset stomach, nausea, vomiting, heartburn, headache, diarrhea, constipation, drowsiness, and dizziness may occur. Side effects include increased bleeding risk due to an anti-platelet effect, poor asthma control in susceptible asthmatics, and potential drug interactions with other drugs.  Ibuprofen may infrequently cause serious (rarely fatal) bleeding from the stomach or intestines (increased risk with daily use of alcohol and tobacco), kidney impairment in the susceptible and elderly, also Ibuprofen may rarely cause serious (possibly fatal) liver disease.  Caution is advised when using this drug in the elderly because they may be more sensitive to the side effects of the drug, especially stomach bleeding and kidney effects.


It is not recommended for use during the last 3 months of pregnancy due to the potential for fetal harm and interference with normal labor/delivery.  Back to the top

 

Web Reference:

http://www.painclinic.org/aboutpain-medicationtypes.htm

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Aleve


Side Effects

Aleve is the brand name of the generic drug naproxen that is manufactured by Bayer. First sold by prescription in 1976, Aleve was later approved for over-the-counter sales in 1994. Since then, there has been no knowledge of significant Aleve side effects, but on December 20, 2004, the National Institutes of Health (NIH) announced it was suspending the use of Aleve from its study after finding patients taking the drug when compared to those taking a placebo have about a 50 percent greater chance of suffering strokes or heart attacks.

The Aleve side effects were considered great enough by the investigators that they could not continue to administer the drug until resolving questions. Aleve was the only medication used in the study, but the FDA says the warning pertains to all drugs that contain naproxen as the active ingredient. While some doctors are skeptical that significant Aleve side effects exist considering the drug has been on the market for decades, Dr. Gregg C. Fonarow, professor of cardiovascular medicine at UCLA noted these medicines were originally studied in the short term for treatment of pain, and their cardiovascular effects were never really well scrutinizedNow theyre being used in higher doses longer term, and were seeing they indeed can increase the risk for myocardial infarction and strokes.

The trial is suspended until more information is gathered since no one knows for sure why the Aleve side effects developed, or if the Aleve side effects are an indicator that all NSAIDs carry cardiovascular risks. NSAIDs, or nonsteroidal anti-inflammatory drugs, are the class of drug Aleve and other naproxen drugs belong to. Because heart attacks normally develop from a blood clot that forms in the blood vessels that supply these organs, the NSAIDs may increase the likelihood of developing such a blood clot, which researchers are trying to better understand the link.   Back to the top

In addition to the evidence that increased cardiovascular Aleve side effects were present, research investigators also suspended the use of Celebrex from the study after a separate federal study on cancer prevention found a strong indicator of heart risk among high dose Celebrex patients.

Celebrex belongs to the same class of NSAID drugs as Aleve, but more specifically to a subset of NSAIDs called Cox-2 inhibitors. The FDA warning that Aleve side effects may include increased heart risks has been made at an especially controversial time for both the drug industry and the federal drug agency regulating it. At the close of September 2004, Vioxx, another Cox-2 inhibitor, was recalled from the market in the largest prescription drug recall of all time.

The focus after the Vioxx recall soon expanded to questioning the safety of all Cox-2 drugs when shortly after, the FDA warned increased drug warnings were being placed on Bextra labels, a Cox-2 inhibitor as well. The Celebrex announcement made December 17, 2004 put further scrutiny and criticism on drug safety. If cardiovascular Aleve side effects do exist, the heart attack and stroke risks seen in Cox-2 drugs could possibly include all drugs in the NSAID class of drugs.

The FDA advised doctors at the time of the Celebrex warning to seek alternative treatment methods for patients, but the agency stopped short of issuing a similar warning about the possible Aleve side effects. Officials did warn patients to consult with their doctors and to carefully follow drug instructions and avoid taking Aleve for more than 10 days.

 

Web Reference:

http://www.adrugrecall.com/naproxen/aleve_effects.html


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