DEMYSTIFYING OTC DRUGS - Eric M. Mazur, MD, MACP
Allergies and Colds
Clinical Indication Symptoms treated Drug class/mechanism of action Generic Drug Name Common brand names Dosage/tablet Comments
Colds/URIs Runny nose, red and itchy eyes 1st generation antihistamines diphenhydramine Benadryl 25-50 mg As a class, very sedating.  Use early In the course of a cold to prevent sinus complications.  All are comparable in efficacy although sedative effect may vary.  Tolerance to sedative effect may occur after several days among some people.  Causes dry mouth.  May exacerabate glaucoma and urinary retention caused by an enlarged prostate.
chlorpheniramine Chlor-Trimeton 4 mg Commonly used in many cold and allergy combinations
brompheniramine 1-2 mg Antihistamine used in many Dimetapp preparations.
triprolidine 2.5 mg Original antihistamine used in Actifed
doxylamine 6.25-25 mg Very sedating; comparable in sedation to diphenhydramine.  Also, a very effective antihistamine.  Often used to create a "PM" or night version of a name brand cold medicine.
Nasal Congestion sympathomimetics (like adrenalin) pseudoephedrine Sudafed 15-30 mg Sympathomimetics are marketed as "non-drowsy decongestants" or "day" medicines.  Pseudoephedrine is very effective at treating nasal congestion.  May raise blood pressure, cause rapid heart rhythms and exacerbate heart disease.  A similar decongestive agent, pheylpropanolamine, was removed from the market because of an association with brain hemorrhages.  Pseudoephedirine is now sold only from "behind the counter" in pharmacies because it was being used illegally to manufacture methamphetamine.  It has been replaced in most current OTC combinations by phenylephrine, a much less effective decongestant.
phenylephrine Neo-synephrine 10-20 mg,   nasal spray Available in tablets and nasal spray. Taken by mouth, much less effective and shorter acting than pseudoephedrine. Many brand names use the abbreviation "PE" to indicate phenylephrine as the decongestant.   For nasal spray caveat, see Afrin below.
oxymetazoline Afrin nasal spray Very effective over the short term.  Use for no more than 3 continuous days.  Severe rebound nasal congestion can occur after prolonged use (i.e. several days).
Cough cough suppressant dextromethorphan 10-30 mg Very marginal clinical efficacy in treating cough.  Recreational abuse potential at high doses.  Should not be used for chronic cough.
codeine 5-15 mg Available OTC as Robitussin AC in 4 oz. quantities containing codeine and guaifenesin.  Similar marginal efficacy in treating cough as dextromethorphan.
expectorants guaifenesin 200-400 mg Supposed to help thin the mucus to facilitate clearance. Used as the base for almost all OTC cough syrups.   True clinical efficacy in ameliorating cough has not been established.
Notes: *OTC cold medications typically include a 1st generation antihistamine, a decongestant, and a cough suppressant and/or expectorant and sometimes also a pain and fever reducer.
*"Day" and "Non-sedating" medications eliminate the 1st generation antihistamine and thus don't treat the runny nose from a cold at all.
*Newer, non-sedating antihistamines (see below) are NOT effective at treating the runny nose from a cold.
*It is not clear that any OTC medication is effective at treating the cough associated with a cold or the flu.
Acute pain, inflammation and fever Pain, inflammation and fever NSAIDs (Non-steroidal anti-inflammatory drugs) aspirin 325-650 mg Aspirin is a remarkable drug.  In addition to it's effects on pain fever and inflammation, aspirin inhibits blood clotting and thus reduces cardiovascular events, i.e. heart attacks and strokes in higher risk individuals.  Regular aspirin also helps prevent colon polyps and colon cancer.  GI and bleeding side effects are seen and can limit its use.  Aspirin should never be used in children or teenagers with influenza or chicken pox as it may cause a serious/fatal illness, i.e. Reye's Syndrome.
ibuprofen Advil, Motrin 200-400 mg Ibuprofen and naproxen are excellent NSAIDs. However, particularly in older individuals (>60 yo) regular use, even at OTC doses, can cause internal bleeding and kidney failure. Extended therapy with ibuprofen and naproxen should be avoided in the elderly. Ibuprofen and naproxen have also been linked to an increased risk of heart attacks and also interfere with medications for high blood pressure.
naproxen Aleve, Naprosyn 250-500 mg Efficacy is comparable to ibuprofen but dosing is half as frequent and thus is more convenient.
Only pain and fever, not inflammation analgesic and antipyretic acetominophen Tylenol 650-1000 mg Active ingredient in over 600 medicines so be aware of duplicate dosing.  Does not cause stomach upset and has no effect on blood clotting.  However, inadvertent, dangerous overdosage is "easy".  At doses of over 4000 mg per day (or eight extra strength tablets), fatal liver failure can occur. Do not take if you have liver disease or drink more than 3 alcoholic beverages daily.  1000 mg dosing offers only marginally better effacacy and much higher risk than the safer 650 mg/dose.  The FDA is now discouraging products with the extra-strength dosing.  Not considered effective in reducing inflammation.
Notes: *Combining acetominophen with either ibuprofen or naproxen at recommended OTC dosages may provide superior, synergistic pain relief.
*Taking a daily OTC PPI (omeprazole, lansoprazole, esomeprazole) along with ibuprofen or naproxen may significantly reduce GI upset and risk of internal bleeding.
Allergies and allegic rhinitis Runny nose, itchy eyes, red eyes, sneezing, nasal congestion 1st generation antihistamines see above ("Colds")
Non-sedating (2nd generation) antihistamines fexofenadine Allegra 60, 180 mg No sedation, even at higher than recommended doses.  This class is most effective at treating allergic rhinitis and conjunctivitis.  2nd generation antihistamines have no effect on cold symptoms.  Do not cause the dry mouth so typical of 1st generation antihistamines.
cetirizine Zyrtec 5-10 mg Some sedation possible at recommended doses.
loratadine Claritin, Alavert 10 mg Some sedation at higher than recommended doses.  Slower onset of action and perhaps lower efficacy than fexofenadine and certirizine.
Nasal congestion sympathomimetics see above ("Colds")
corticosteroid nasal sprays triamcinolone Nasacort nasal spray Nasal corticosteroid sprays have recently been released on the OTC market.  They are highly effective without rebound.  They do not act acutely since the antinflammatory effect takes a few to several days.  Ideally, should be started several days before allergy exposure and used once to twice daily.  Corticosteroids inhibit many of the inflammatory pathways stimulated by allergies, not just one.  Meaningful amounts of drug are not absorbed internally but nasal mucosal atrophy, nose bleeds, and susceptibility to yeast infections can occur with prolonged use.  Nasocort is the least expensive corticosteroid nasal spray @ $10 for 120 sprays. No generics of any of the corticosteroid nasal sprays are available (but stay tuned).
fluticasone Flonase nasal spray Recently released.  Unpleasant "taste" discourages some users of fluticasone vs. triamcinolone.  Intermediate cost @ $20 for 120 sprays
budesonide Rhinocort nasal spray Recently released.  Highest cost @ $38 for 60 sprays.  May be the most potent.
mast cell stabilizer cromolyn sodium NasalCrom nasal spray Prevents release of inflammatory substances from mast cells.   Used 3-6 times daily and may take up to 4 weeks to have effect.  No immediate effect on imflammation.