OTC Options:
Pain, Pain Go Away
by Ruth Papazian
       Used to be, aspirin and other salicylates were the only
medications available for nonprescription relief of minor ailments-
-from headaches and fever to muscle strain and minor arthritis.
Today, consumers looking for temporary relief from such garden-
variety ills have their pick of what can be a bewildering array of
"regular," "extra-strength," and "maximum pain relief" tablets,
caplets and gel caps on the drugstore shelf.
       Though this cornucopia can seem confusing, the products' pain-
relieving ingredients fall into just four categories: aspirin (and
other salicylates), acetaminophen, ibuprofen, and naproxen sodium.
For the most part, these over-the-counter (OTC) analgesic
ingredients are equally effective. However, some may be more
effective for certain types of ailments, and some people may prefer
one type to another because of their varying side effects. "Knowing
the pros and cons of each type of pain reliever will allow you to
choose among them," says William T. Beaver, M.D., professor of
pharmacology and anesthesia at Georgetown University School of
Medicine in Washington, D.C.

Old Faithful
       Americans have been reaching for aspirin for almost 100 years
as an all-purpose pain reliever (see "Aspirin: A New Look at an Old
Drug" in the January-February 1994 FDA Consumer). Aspirin (or
acetylsalicylic acid) works in part by suppressing the production
of prostaglandins, hormone-like substances that have wide-ranging
roles throughout the body, such as stimulating uterine
contractions, regulating body temperature and blood vessel
constriction, and helping blood clotting. "Regular" strength
aspirin contains 325 milligrams (mg) per tablet; "extra" or
"maximum" strength, 500 mg per tablet. The usual adult (defined as
12 years and older) dosage is one to two 325-mg aspirin tablets
every four hours.
       Some manufacturers add caffeine to aspirin. "There is no
evidence that caffeine relieves pain, but it can enhance the
effects of aspirin, possibly by lifting a person's mood," says
Michael Weintraub, M.D., director of FDA's Office of OTC Drug
Evaluation. Since a two-tablet dose provides roughly the same
amount of caffeine as a cup of coffee, you can get the same effect
by taking two plain aspirin with coffee.
       To minimize the stomach irritation aspirin can cause, some
brands are "buffered" with calcium carbonate, magnesium oxide, and
other antacids or coated so the pills don't dissolve until they
reach the small intestine. Buffered formulas may offset aspirin's
directly irritating effects on the stomach lining. They may be
useful for people who get heartburn or stomach pain when they take
aspirin, as well as for those with arthritis, who need to take as
much as 4,000 mg every day.
       Aspirin also causes gastrointestinal (GI) upset indirectly (by
inhibiting production of a prostaglandin that protects the stomach
lining by stimulating mucus production); buffering does nothing to
offset this effect.
       The downside of coated aspirin products is that they may  take
up to twice as long to provide pain relief as plain aspirin,
according to Weintraub. Last September, an FDA advisory panel
recommended that labels on products containing aspirin warn that
heavy drinkers are especially vulnerable to developing GI bleeding.
       Aspirin should not be taken by people who have:
fl      ulcers, because it can worsen symptoms
fl      asthma, because it can trigger an attack in some asthmatics
fl      uncontrolled high blood pressure, because of an increased risk
of one type of stroke
fl      liver or kidney disease, because it may worsen these
conditions
fl      bleeding disorders or who are taking anticoagulant medication,
because it may cause bleeding.
       Continual high dosages of aspirin can cause hearing loss or
tinnitis--a persistent ringing in the ears.
       FDA requires products containing aspirin and other salicylates
to carry a label warning that children and teenagers should not use
the medicine for chickenpox or flu symptoms because of its
association with Reye syndrome, a rare disorder that may cause
seizures, brain damage, and death.
       The label also alerts pregnant women that use of aspirin in
the last trimester may increase the risk of stillbirth and of
maternal and fetal bleeding during delivery.

One Aspirin Alternative
       Twenty years ago, FDA approved acetaminophen (Tylenol, and
other brands and generics) in dosages of 325 mg and 500 mg for OTC
use. "Nobody knows exactly how acetaminophen works, but one theory
is that it acts on nerve endings to suppress pain," says Weintraub.
Acetaminophen is as effective as aspirin in relieving mild-to-
moderate pain and in reducing fever, but less so when it comes to
soft tissue injuries, such as muscle strains and sprains, he adds.
The usual adult dosage is two 325-mg tablets every four hours.
       Acetaminophen-based products to ease menstrual cramps often
contain other ingredients, such as pamabrom (a diuretic) or
pyrilamine maleate (an antihistamine used for its sedative
effects). "While these ingredients are safe, they have not been
proven effective against uterine cramps, although they may relieve
other symptoms associated with menstrual pain," says Weintraub.
       Though acetaminophen is no better or faster at pain relief
than aspirin, the drug is gentler on the stomach and reduces fever
without the risk of Reye syndrome. However, even at moderate doses,
acetaminophen can cause liver damage in heavy drinkers. At press
time, FDA was planning to require a warning about this on the
labels of OTC products containing the drug.

From Rx to OTC
       Like aspirin, ibuprofen and naproxen sodium inhibit
prostaglandin production. However, they are more potent pain
relievers, especially for menstrual cramps, toothaches, minor
arthritis, and injuries accompanied by inflammation, such as
tendinitis. FDA approved ibuprofen for OTC marketing in 1984 at a
dosage level of 200 mg  every 4 to 6 hours, and naproxen sodium in
1994 at a dosage level of 200 mg every 8 to 12 hours.
       "Ibuprofen and naproxen sodium were converted to OTC status
after their manufacturers did the necessary studies to show that
these pain relievers were effective at OTC dosages, which are lower
than prescription dosages," explains Weintraub. The lowest dosage
strength for prescription-strength ibuprofen (Motrin and others) is
300 mg per tablet, and 275 mg per tablet for the prescription
version of naproxen sodium (Anaprox, for example). "In addition,
the pharmaceutical companies had to show that these drugs were safe
for use by a larger, more varied group of people [than would have
received them by prescription only] and that the drugs were safe to
use without medical supervision, as is the case with all
nonprescription drugs."
       Taken at the recommended adult dosage, OTC ibuprofen (Advil
and others) and naproxen sodium (Aleve) are somewhat gentler on the
stomach than aspirin. However, people who have ulcers or who get GI
upset when taking aspirin should avoid both. In addition,
asthmatics and people who are allergic to aspirin should avoid
ibuprofen and naproxen sodium. An FDA advisory panel has
recommended labeling on ibuprofen products like that recommended
for aspirin, warning heavy drinkers about increased risk of gastric
bleeding and impaired liver function (products with naproxen sodium
labels already include this information).
       Although ibuprofen and naproxen sodium interfere with blood
clotting much less than aspirin does, they should not be used by
people who have bleeding disorders or who are taking
anticoagulants. Children under 12 should not be given either drug,
except under a doctor's supervision, and people over 65 are advised
to take no more than one naproxen sodium tablet every 12 hours.
       Choosing an OTC pain reliever involves balancing effectiveness
for a particular ailment with side effects. Often this is a very
individual choice, based in part on your health history and how the
drug affects you. Regardless of which type of OTC pain reliever you
choose, remember that it is intended to be used on a short-term
basis, unless directed by a doctor, cautions Weintraub. The warning
labels on these products include limitations on duration of use to
ensure that chronic or serious illnesses are not masked. Typically,
labels advise against taking the product for more than 10 days to
relieve pain (for children, the upper limit is five days), or more
than three days to reduce fever. If symptoms worsen, pain persists,
or there is redness or swelling, medical attention should be
sought.

Ruth Papazian is a writer in New York City.