Pain Relievers (Analgesics) and Fever Reducers (Antipyretics)
Pain is the most common reason for people to seek medical advice, and medicines for pain are the most frequently purchased over-the-counter (OTC) medications. Fever is one of the most common reasons for people to seek medical advice for their children, and one in five emergency room visits for children is due to fever. Since OTC medicines that are effective in treating pain also are effective at reducing fever, they will be considered together.
What classifications of pain are there?
Pain can be classified as acute, chronic non-malignant, or chronic malignant. Headaches, the most common cause of pain, can be considered a separate class of pain.
Acute pain usually is due to mechanical or thermal (usually heat) injuries. Examples of mechanical injuries include soreness of muscles due to overuse or strain (and sometimes to viral infections), tears of the ligaments, broken bones, bruises, and cuts. These types of acute pain usually respond well to OTC medications for pain. Muscle soreness also may respond well to heat and massage.
Chronic non-malignant pain is a type of pain associated with progressive, debilitating diseases such as arthritis . OTC medications for pain usually are effective for this type of pain. However, because of the chronic nature of the pain, their use often leads to excessive use of the medications and frequent side effects. The pain of arthritis also may respond well to heat.
Chronic malignant pain is pain associated with advanced, progressive diseases (often fatal) such as cancer , multiple sclerosis , AIDS, and terminal kidney disease. OTC medications for pain may be useful for the management of chronic malignant pain. However, stronger prescription medications usually are necessary.
What types of headaches are there?
Headaches--most common reason that analgesic medications are taken-- can be classified into three types: muscle contraction, migraine or vascular, and sinus.
A muscle contraction headache , the most common type, results from the continuous tightening of the muscles in the upper back, neck, or scalp. This type of headache often is described as a tight, pressing, or throbbing sensation of the head. It can be brought on by emotional stress and anxiety ("tension headaches"). Acute muscle contraction headaches generally respond well to OTC analgesics, but chronic muscle contraction headaches often require physical therapy or relaxation techniques.
Migraine or vascular headaches are due to dilation (expansion) of blood vessels in the head. Although many patients use the expression "migraine" to describe any particularly painful headache, many of these are actually muscle contraction headaches. OTC medications for pain may be quite effective for treating migraine headaches. However, prescription medications that are specifically formulated for treating or preventing migraines often are necessary.
A sinus headache is caused by an infection or blockage of one or more sinuses in the head. The pain often is limited to the area around the eyes or the forehead where the major sinuses are located. The pain may occur upon awakening, and may decrease in intensity after the person has been standing or sitting up for a while. In addition to analgesics, OTC decongestants can be effective by helping to drain the sinus.
What is a fever and what is it's causes?
Most fevers are transient (lasting only a few hours or a few days) and are not dangerous, but they may cause a great deal of discomfort. A rectal temperature of greater than 101.8 degrees F (38.8 degrees C), an oral temperature of more than 100 degrees F (37.8 degrees C), or an armpit temperature of greater than 99 degrees F (37.2 degrees C) is considered abnormal. Fevers usually are due to infections, either viral or bacterial, but they also can be due to cancers, injury to tissue (for example, heart attacks), hyperthyroidism , other illnesses in which there is inflammation, and dehydration . Additionally, over 40 different drugs have been reported to cause "drug fever."
Harmful effects of fever (for example, dehydration, changes in consciousness, seizures, or coma) are most likely to occur at temperatures above 106 degrees. Lower fevers are dangerous in persons with heart disease, since fever increases the work of the heart because the pumping of blood must increase. Seizures occur in 2 to 4% of all children between the ages of 6 months and 5 years (usually before age 3) with high fevers though these seizures generally last no more than 15 minutes. Children who experience febrile seizures have a higher risk of developing epilepsy later in life.
What are the different classes of pain relievers and fever reducers?
The three classes of OTC analgesic/antipyretic medications are: - Salicylates: aspirin (also called acetylsalicylic acid or ASA), choline salicylate, magnesium salicylate, and sodium salicylate;
- Acetaminophen ; and
- Nonsteroidal anti-inflammatory drugs (NSAIDs): ibuprofen , naproxen sodium, and ketoprofen . (Aspirin is also an NSAID, but it is considered separately from the other NSAIDs because it has some unique properties.) Each of these drugs is discussed in detail below.
In most circumstances, these medications all have very similar analgesic (pain- relieving) and antipyretic (fever-lowering) abilities. Their onset of action (the interval from the time of ingestion to the start of pain relief) also are similar. Naproxen sodium may have a somewhat longer duration of pain relief (analgesia) than the other NSAIDs or aspirin. At high doses, salicylates and NSAIDs suppress inflammation and are, therefore, particularly useful in treating inflammatory diseases such as arthritis. Acetaminophen does not have anti-inflammatory actions.
Many OTC analgesics are available in combination with other drugs. There is some evidence that caffeine and antihistamines enhance the effects of analgesics. Thus, caffeine increases the pain-relieving effects of aspirin and ibuprofen, and the antihistamines orphenadrine and phenyltoloxamine enhance the pain- relieving effects of acetaminophen. Combinations of decongestants with analgesics are logical only when nasal or sinus congestion are present, for example, for sinus headaches.
Aspirin
Formulations of aspirin: Aspirin can damage the lining of the stomach and duodenum, thereby causing abdominal pain , bleeding, and/or ulcers. As a result, 1 in 5 persons who take aspirin in a dose of 2.5 grams per day or more develops ulcers and about 1 in 6 will lose enough blood from gastrointestinal bleeding to develop anemia . In an attempt to reduce the potential for these complications, some aspirin-containing tablets have been coated with a special coating that prevents the tablet from dissolving until it is past the stomach and duodenum. These "enteric-coated" aspirin products may reduce the frequency of abdominal pain, but not the bleeding or ulcers. Moreover, the onset of pain relief is delayed with enteric-coated aspirin because it takes more time for the tablets to dissolve. Other attempts to prevent complications have included aspirin-containing products that release the aspirin slowly over time (e.g., Zorprin; Measurin; Verin). Like enteric-coated products, these products are not ideal when prompt relief of pain is needed. They also do not prevent ulcers or bleeding. Buffered (e.g. Bufferin) and effervescent (e.g. Alka-Seltzer) aspirin products are absorbed more quickly from the stomach and intestine than aspirin, but they do not act more rapidly than regular aspirin and do not reduce the risk of bleeding or ulcers. Furthermore, effervescent aspirin products contain large amounts of sodium (salt) and should be avoided in persons with high blood pressure , heart failure, or certain kidney diseases.
Side Effects: Aspirin prevents platelets from sticking together and forming blood clots. On the one hand, this effect can be used beneficially, for example, to prevent the blood clots that cause heart attacks or strokes. On the other hand, by preventing blood clots, aspirin can have the detrimental effect of promoting bleeding. Therefore, aspirin should not be used by people who have diseases that cause bleeding (e.g., hemophilia, severe liver disease) or diseases in which bleeding may occur as a complication (e.g., stomach ulcers). Moreover, since the effect of aspirin on platelets lasts for several days, people should not take aspirin for seven days before surgical or dental procedures because of the increased risk of bleeding after the procedures. In patients at risk for bleeding, acetaminophen can be an excellent alternative to aspirin since acetaminophen does not have an effect on platelets, blood clots, or bleeding. Like aspirin, other NSAIDs affect platelets, but the duration of the effect is less than with aspirin. Two aspirin-related, salicylate-containing products ( salsalate and choline magnesium trisalicylate) have no effect on the platelets, but they are available only by prescription.
Although many people claim to be "allergic" to aspirin, most describe their "allergy" as abdominal pain or heartburn. These common side effects are not allergies, but rather reflect the irritating effects of aspirin on the lining of the stomach. True allergy to aspirin occurs in fewer than 1 out every 100 persons. True allergy may include hives , itching, swelling, or difficulty breathing. Allergy to aspirin is more common in persons with asthma , allergic rhinitis, or nasal polyps. In such persons, the risk of an allergic reaction to aspirin may be as high as 1 to 3 persons out of every 10. People with true aspirin allergy also may be allergic to other compounds. One such compound is tartrazine, or yellow dye #5. This dye is used in many medicines, foods (such as soft drinks), and candy or desserts. In addition, people with an allergy to aspirin often are allergic to other NSAIDs, such as ibuprofen.
Pregnancy/Lactation: Regular aspirin consumption during pregnancy has been associated with side effects in the pregnant mother, including bleeding and complications during labor. It is unclear if aspirin taken in the first two trimesters poses a risk to the fetus. However, when taken during the third trimester, aspirin may increase the risk of bleeding in the newborn. Although very little aspirin is secreted into milk, most authorities recommend that nursing mothers avoid using aspirin.
Viral infections in children: Because aspirin causes Reye's syndrome (a potentially fatal liver disease that occurs almost exclusively in persons under the age of 15 years), aspirin should not be given to children when a viral infection is suspected.
Drug Interactions: High doses of aspirin can increase the activity of valproic acid (Depakene; Depakote), an effect which can cause drowsiness or behavioral changes. High doses of aspirin also can enhance the effect of some sugar-lowering medications used in diabetes, e.g. glyburide (Diabeta), glipizide (Glucotrol), and tolbutamide (Orinase), which can possibly lead to hypoglycemia (low blood sugar). The effects of probenecid (Benemid) are reversed by aspirin. Aspirin can increase the toxicity of methotrexate and the risk of bleeding with warfarin (Coumadin).
Salicylates other than Aspirin
There are three other OTC salicylates; choline salicylate, magnesium salicylate, and sodium salicylate. The advantage of these drugs over aspirin is their shorter effect on the platelets that promote bleeding.
Choline salicylate (Arthropan) is available as a liquid. It is absorbed more quickly, but its onset of action is no different than that of aspirin. Some people find choline salicylate fishy. Fortunately, it can be mixed with juice or soda prior to ingestion. It is less effective at reducing fevers in children than either aspirin or acetaminophen.
Magnesium salicylate (Arthriten; Backache) is as effective as aspirin at reducing pain. Patients with chronic kidney disease should avoid magnesium salicylate, since the magnesium may accumulate in their bodies.
Sodium salicylate (Scot-Tussin Original) and aspirin are equally effective in the long-term treatment of rheumatoid arthritis , but sodium salicylate is less effective at reducing pain or fever.
Acetaminophen
Formulations: Acetaminophen comes in various oral formulations, including different types (elixirs or syrups) and flavors of liquids, capsules, tablets, caplets, and suppositories. The capsules contain tasteless granules that can be emptied onto a teaspoon containing a small amount of drink or soft food, and can then be swallowed. However, the granules should not be mixed in a glass of liquid since the granules will stick to glass itself. The amount of acetaminophen that is absorbed from rectal suppositories is about half that of the oral formulations.
Side Effects: Acetaminophen generally is safe to use, and few people develop side effects. In high doses, however, it can cause liver damage and doses of 4000mg (4 grams) per day should not be exceeded.
Pregnancy/Lactation: Acetaminophen has no known harmful effects on the mother, fetus, or infant and, therefore, can be used safely during pregnancy and during lactation.
Drug Interactions: It has been reported that patients with HIV- related diseases (e.g., AIDS) who take AZT ( zidovudine ; Retrovir) and acetaminophen are at an increased risk of developing suppression of their bone marrow. Such patients develop lower white and red blood cell and platelet counts and, therefore, are more susceptible to infection, anemia, and bleeding.
Nonsteroidal Anti-inflammatory Drugs (NSAIDS)
There are three OTC NSAIDs--ibuprofen, naproxen sodium, and ketoprofen. All have pain relieving (analgesic), fever reducing (antipyretic), and anti-inflammatory properties. Additionally, NSAIDs are more effective than aspirin or acetaminophen for cramps associated with the menstrual cycle (dysmenorrhea).
Formulations: Ibuprofen is available in tablets as well as in a pediatric suspension. Naproxen sodium is available in tablets. Ketoprofen is available as tablets and caplets.
Pregnancy/Lactation: NSAIDs are safe for use during the first or second trimesters of pregnancy, but should not be taken during the third trimester, since they can prolong labor and delay birth, increase bleeding in the mother following birth, and can cause cardiac (heart) and vascular (blood vessels) complications in the newborn. Ibuprofen and naproxen sodium also are safe for use by nursing mothers. Due to insufficient data, ketoprofen is not recommended for use by nursing mothers.
Side effects: The most frequent side effect of NSAIDs is damage to the lining of the stomach and duodenum that can lead to abdominal pain, nausea, and loss of appetite. NSAIDs also can cause ulcers and bleeding from the stomach and duodenum, but less frequently and less severely than occurs with aspirin use. NSAIDs, like aspirin, affect platelets and can inhibit the formation of blood clots, and, therefore, they should be discontinued at least 24 hours before surgery or dental procedures. Because alcohol intensifies the effect of NSAIDs on bleeding, alcohol should not be taken with NSAIDs. NSAIDs also can cause kidney damage, particularly in the elderly or patients with high blood pressure, diabetes, atherosclerosis, or who take diuretic medications ("water pills"). Patients who are allergic to aspirin should not take NSAIDs since they are likely to be allergic to NSAIDs as well. NSAIDs may cause fluid retention in persons with congestive heart failure , and, therefore should not be used in this setting.
Drug interactions: Ibuprofen may increase blood levels of digoxin (Lanoxin); however, it is unclear whether this interaction is important enough to recommend that patients taking digoxin not take ibuprofen.
NSAIDs reduce the blood pressure-lowering effects of certain high blood pressure (antihypertensive) medications, including: thiazide diuretics such as hydrochlorothiazide (Dyazide, Maxzide); beta-blockers such as propranolol or atenolol (Inderal, Tenormin), and metoprolol (Lopressor); angiotensin receptor antagonists such as enalapril (Vasotec), lisinopril (Zestril; Prinivil), benazepril (Lotensin), quinapril (Accupril), ramipril (Altace), and captopril (Capoten); and some medications that act on the brain, such as clonidine (Catapres).
NSAIDs can increase the levels of lithium in the blood, which can result in lithium-related side effects.
NSAIDs can also increase the levels of methotrexate in the blood and have been reported to result in methotrexate-related side effects.
What about overdoses of pain relievers and fever reducers?
The American Association of Poison Control Centers reported that of all overdoses of OTC products, 66% involved acetaminophen, 19% involved ibuprofen, and 15% involved aspirin. Aspirin overdose can occur with as little as 150 mg/kg (10,000mg or 10 grams in the average sized male) as a single dose, or 90 mg/kg per day for at least two consecutive days. Symptoms of toxicity due to aspirin may include tiredness, ringing in the ears, rapid breathing, seizures, vomiting, bleeding, and coma. Large doses of acetaminophen rarely cause serious problems in children. In adults, as little as 10 grams can damage the liver and the kidneys. Overdoses of ibuprofen rarely produce important problems. Nausea, vomiting, stomach pain, tiredness, and dizziness are the most common symptoms of large doses of ibuprofen. Rarely, coma may occur.
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