OTC Drugs,
Herbal Remedies
and
Other Stuff
Chapter 14
Lecture Outline
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OTC Drugs
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Herbal Remedies
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Antihistamines
Decongestants
Cough medicine
Analgesics
St. John’s Wort
Ephedra
Ginkgo Biloba
Ginseng
Other Supplements and Prescription Drugs
ADHD Treatments

Primarily treated with stimulants
– Ritalin (Methylphenidate)
– Concerta (a longer acting form of Ritalin)
– Adderal (amphetamine salts)
– Strattera (atomoxetine) - SNRI
Antihistamines
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Used to treat allergies as well as dermatological
conditions
 All block H1 (Histamine) receptor
– Histamine is an excitatory NT and mediates part of the
generalized immune response.
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Drowsy vs. Non-drowsy
– Based on whether it crosses BBB
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Benadryl (Diphenhydramine) – Crosses
Chlorpheniramine (Chlor-Trimeton) - Crosses
Allegra (Fexofenadine) – Doesn’t Cross
Claritin (Loratadine) – Doesn’t Cross
Zyrtec (Citirizine) – Doesn’t cross
Clemastine (Tavist) - Crosses
H2 receptor antagonists are Pepcid, Tagamet, Axid …
Anti-ulcer and Antacid drugs
Decongestants
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Dilate bronchial passages by constricting blood
vessels in respiratory system
– Mediated by NE (Agonist)
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Pseudoephedrine most common
 Ephedrine once common
 Activate SNS, but cross BBB weakly
 Names
– Sudafed
– Actifed
– Dimetapp
Analgesics
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Non-Steroidal Anti-Inflammatory (NSAIDS)
 Inhibit Prostaglandins and Proinflammatory
Cytokines through inhibition of COX enzymes
 Names
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Acetylsalycillic Acid (Aspirin) – COX 1 & 2
Acetaminophen (Tylenol) – COX3
Motrin (Ibuprofen) – Cox 1 & 2
Alleve 1 & 2
Naprosin 1 & 2
Vioxx (Rofecoxib) 2
Celebrex (Relecoxib) 2
Not good to inhibit COX 1 = kidney and stomach
problems
OTC Sleep Aids
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For temporary relief of insomnia
 Vast majority contain antihistamines
– Benedryl
 Tylenol PM
 Unisom geltabs
 Sominex
– Doxylamine
 Unisom sleep tabs
Herbal Remedies

Derived from natural sources
 Not currently regulated by FDA
 Purity and potency are large issues
– Extraction of active ingredient can be a
problem
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Currently popular
 Have been around forever
St John’s Wort
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Grows as an invasive weed
 Hypericum
 For mood disorder (We think this is what it does)
– Agonist of catecholamines
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SSRI
Increases DA and GABA
Effective if one gets enough (mounting evidence is
good)
 Speeds up metabolism of birth control pills and
antivirals
 Induces photosensitivity
Ginseng
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Extract from plant
 Thought to induce a number of actions
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Anti-fatigue
Antioxidant
Lower cholesterol
Stimulant?
Headaches, insomnia, anxiety, breast soreness or
tenderness, skin rashes, asthma attacks, increased
blood pressure, diarrhea, euphoria, nervousness,
skin eruptions, heart palpitations, or postmenopausal uterine bleeding
Ginkgo Biloba
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Increases blood flow to brain
Thought to increase memory and cognitive ability
Inhibits Platelet Activating Factor and induces
vasodilation
Few side effects. GI distress. Possibly some
problems with >2 years use
Effective for people with problems; may not have
much effect for “normals”
Ephedra
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Ephedra, Ephedrine, Ma Huang
– Derived from plant source
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NE agonist. Stimulates NE release and acts on
receptors
 Typical sympathomimetic response
– Increase – HR, BP, Respiration, Glycogenesis and
Lypolysis
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Does not cross BBB very well, so little CNS effect
 Used for bronchial dilation, as well as weight loss
and narcolepsy in the past
 Stroke and arrhythmia
Kava
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Plant native to South Pacific
 Used much like alcohol
 GABA agonist
 Associated with liver failure
The Moral
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Look up the active ingredient
– What is it?
– What does it do?
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Be aware of drug interactions
– Antagonism
– Synergism
– Intolerance
– Allergy