Over-the-Counter (OTC)Drugs
Aka nonprescription drugs

u   Drugs with a relatively low risk of adverse reactions/toxicity if used according to directions & high margin of safety

u   Generally used to relieve symptoms of conditions that can be self-diagnosed

u   Many categories of OTCs, but we’ll stick with the psychoactive ones

Aspirin (acetylsalicylic acid)

u     most common "salicylate" analgesic

u    325-650mg (most do not need more)

u    1.  analgesic for mild to moderate pain

u    2.  anti-pyretic (anti-fever)

u    3.  anti-inflammatory

u    Also:  anticoagulant action (used to prevent heart attack or stroke due to clots);  has                anti-colon cancer, anti-skin cancer effects


Adverse Effects of Aspirin

u    Causes stomach irritation & bleeding

u    2% of population allergic to aspirin

u    Anticoagulant effect is undesirable before or after surgery, during pregnancy, if you are already already a “bleeder”or on anticoagulants

u    Can delay & prolong labor & increase bleeding

u    In those <16 yr with virus, flu or chicken pox,  increased risk of Reye's disease (serious liver & neurological disease)

Signs of Taking Too Much Aspirin (“salicylism: 

u   Tinnitus (ringing in ears)or impaired hearing, nausea & vomiting, thirst, rapid breathing, confusion

u   Lethal dose for average adult ~ 20g (60 tablets)

Drug Action of Aspirin

u    Decreases production of body chemicals known as the prostaglandins by inhibiting COX enzymes

u    Prostaglandins normally sensitize pain receptors, trigger inflammation & fever, are involved in clotting of blood, protect the cells of the stomach, increase uterine contractions in labor.

u    Inhibiting the production of prostaglandins can affect all of these functions

Newest Advance

u   Enzymes (COX) producing prostaglandins found in diff. forms in diff. parts of body

u   Discovery of selective COX2 inhibitors which relieve pain & inflammation with little effect on stomach or platelets:

l  Celebrex (celecoxib)

l  Vioxx (rofecoxib)

l  (These are prescription drugs)

Acetaminophen ("aspirin substitute or non-aspirin pain reliever")

u   325-650mg (same potency as aspirin)  Equal  analgesic  & antipyretic action

u   Not anti-inflammatory or anticoagulant

u   Less gastric distress & tinnitus, but more damaging to liver with heavy use

u   Can be used by those with aspirin allergy.

u   No risk of Reye’s syndrome in kids

Ibuprofen( e.g. Motrin, Advil)

u    Both OTC (200 mg) & prescription (higher doses); used every 4-6 hr

u    More potent than aspirin or acetominophen (take less)

u    More effective for certain conditions (inflammation, joint problems, sports injuries, dysmenorrhea, dental pain)             

u    Weaker anticoagulant effect than aspirin

Naproxen ( OTC Alleve;  Naprosyn or Anaprox)

u    Very similar to ibuprofen but somewhat different time course (can take twice a day)

u    Both naproxen & ibuprofen are similar enough to aspirin that they should not be used by those with aspirin allergy. 

u    Similar stomach irritation &  should be avoided by those with kidney disease.

u    200mg OTC, higher doses prescription

Naproxen’s Timecourse

u    Absorbed more slowly (peaks in 2-4 hrs) & stays longer (binds to proteins in the blood).

u    If taken regularly blood levels will be maintained taking just 2 doses a day. PDR states that pain relief lasts UP TO 7-8 hrs. 

u    FDA pushed 12 hr OTC dosing to limit risks (not just because naproxen sometimes has a longer action). 

u    Naproxen sodium is absorbed faster.

Ketoprofen (e.g. Orudis, Actron)

u   Same analgesic/anti-inflammatory family

u   More potent, but otherwise not different in its effects/risks

u   OTC dosage is 12.5 mg/4-6 hrs whereas prescription dose is 25-50 mg/6-8 hrs

Non-Steroidal Anti-Inflammatory Drugs (NSAIDS)

u   All of these except acetominophen relieve inflammation. There are additional prescription NSAIDS that tend to have greater risk of side effects.

u   The other group  of potent (& hence prescription) anti-inflammatory drugs for are steroids like prednisone

Cold Medications

u    Usually contain a “shotgun”* mix of ingredients to relieve symptoms:

l   decongestant

l   analgesic/antipyretic

l   antihistamine

l   anti-tussive (anti-cough)

l   some include alcohol

l   some include stimulants

l   Not everyone needs this fixed combination of ingredients!

u    More “individualized” preparations now available


u   Mild stimulants which constrict blood vessels in nose, sinuses, etc. to reduce stuffiness & runny nose

u   Examples:

l  phenylephrine

l  pseudoephedrine

l  phenylpropanolamine*

l  oxymetazoline

l  xylometazoline



u   Block the action of histamine, the body chemical which triggers allergy-type responses (itchy eyes, sneezing, hives)

u   Examples:

l  chlorpheniramine

l  brompheniramine

l  diphenhydramine

l  doxylamine

Other Uses

u   Antihistamines are also used as

l  anti-motion sickness drugs (like Dramamine)

l  cough suppressants (like Benedryl Cough Syrup)

l  OTC sleep aids (e.g.Bayer PM, Tylenol PM)

u   Not really effective for colds

Anti-tussives (cough-suppressants)

u   Decrease the cough reflex - good for when you have a tickly, nonproductive cough.

l  dextromethorphan

l  codeine

l  diphenhydramine (antihistamine)


u   Loosen/thin phlegm to make it easier to clear lungs with a productive cough

u   Example:

l  guaifenesin

Doesn’t make sense to combine cough suppressant with an expectorant