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Dr. Arnold
Pharmacology
Page 1 of 7
Specific Drug categories
I. Introduction [S1]: Special Drug Classes: Over-the-Counter (OTC) and Dermatologic Drugs
II. Study Objectives [S2]
a. Understand why some drugs require a prescription and some do not
b. Describe the trend toward self-medication and some conditions which are amendable to self-medication
c. Know some of the common drugs found in over-the-counter medications
d. Know the common types of drugs applied to the skin
e. Understand some common issues to consider in geriatric drug dosing
f. Understand some common issues to consider in pediatric drug dosing
III. Rx & OTC Medications [S3]
a. Difference between prescription and OTC. What is the difference between a prescription and an OTC drug?
b. Prescriptions require prescription and OTC does not.
c. Prescription (Rx) medications are available only by authorization from a licensed health professional, such as a
physician
d. Over-the-Counter (OTC) medications are available on request and do not require approval by a health
professional
IV. Rx & OTC Medications [S4]
a. Prior to 1951 there were no prescription drugs. Most things were available without a prescription. Drugs were not
regulated very well. Because of some things that occurred: some deaths, this class of legend drugs or
prescription drugs was created.
b. Since that time patients have viewed prescription drugs as potent, effective, and dangerous and used OTC as not
that dangerous. That’s not necessarily always the case. A lot of interactions can occur. Some drugs you may
want to prescribe may have reactions with OTC drugs.
c. In general, the public views OTC medications a minimally effective and safe and Rx drugs as more potent and
dangerous
d. Is this the case?
IV. Not Necessarily [S5]
a. Drug-drug interactions (Rx or OTC) (aspirin and warfarin). Example Warfarin: Warfarin is a highly protein bound
drug. Aspirin is as well. If your patients start taking Aspirin OTC, it could displace that Warfarin and the patient
would get a greater effect of that drug.
b. Drug-lifestyle interactions (antihistamines and alcohol)
c. Drug-disease state interactions (oral decongestants and hypertension) Example: decongestants can precipitate
bad hypertensive crisis.
d. Inappropriate usage of certain OTC medications in susceptible patient populations (i.e. salicylates in peds)
Example: Pediatric patient with fever of unknown etiology- shouldn’t treat w/ aspirin.
e. Potential for abuse (i.e. laxatives, decongestants, antihistamines, sleep aids, antacids)
V. “Switching” Policy of FDA [S6]
a. Despite the fact that these drugs can be dangerous, the FDA has been trying to switch more and more
prescription drugs to OTC status.
b. The FDA is attempting to make drugs more available to the general public by switching some frequently used and
safe Rx medications to OTC status
o This has lead to the recent movement of several drugs such as ranitidine (zantac), naproxen sodium
(aleve), and more recently loratadine (claritin) and omeprazole (prilosec).
c. Really need to keep abreast of what drugs our patients have access to OTC.
VI. How does the FDA decide? [S7]
a. How do they decide what will prescription and what will be OTC?
b. For the most part, it all comes down to the labeling
VII. The New Drug Facts Label [S8]
a. Required on most OTCs manufactured after 2002
b. Should make it easier for patients to safely select the most appropriate medication
c. A prescription drug is one that you, as a prescriber, need to provide directions to your patient so they can use it
safely and effectively.
d. If a drug can be labeled appropriately, if a patient can go to the drug store, look at directions, look at
interactions, and can make the decision if they should use it safely and effectively, in the FDA’s eyes, it can be
OTC.
e. In order to facilitate the switch of more drugs to a non-prescription or OTC status, the FDA recently implemented
new drug facts label. This is pretty similar to the Food Facts Label that came out in the 1990’s. The hope is that
this new label will make it easier for patients to safely use the more appropriate medication.
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Dr. Arnold
Pharmacology
Page 2 of 7
VIII. The New Drug Facts Label [S9]
a. Uses more plain language (i.e. “uses” instead of “indications”)
b. Has new features such as large type, bullets, line spacing and other features to improve readability.
IX. Drug Facts [S10]
a. This is an example of a Drug Facts Label.
b. Drug Facts: On outer package and on container whenever possible.
c. Active Ingredients: What the product is and what it is intended for. Tells the classification of that drug. In this
case Chloraphinaramine, which is an anti-histamine.
d. Uses: What problems or symptoms the medicine will help.
X. Drug Facts [S11]
a. Warnings: Absolute contraindications, interactions with other foods or drugs, side effects, when to consult a
doctor or pharmacist What you can see is this is a crystal structure of a class I and a class II, so we know
exactly what the thing looks like.
b. Directions: Directions for use. The most important part. Should be easy to understand by the patient.
c. Additional information (i.e. storage, potentially problematic ingredients)
d. Inactive ingredients
XI. The Trend for Self-Medication I [S12]
c. Currently, the U.S. spends over $15 billion on OTC medications
d. More than 100,000 different OTC products are available on the market.
e. A lot of the same drugs are in these products, so there are not 100,000 different drugs, but they use a lot of the
same drugs in a lot of different products.
f. The biggest categories are analgesics, cough/cold preps, and antacids.
XII. The Trend for Self-Medication [S13]
a. OTC expenditures comprise 60% of the annual drug purchases in the U.S.
o About 50% of drug usage is OTC drugs.
XIII. What makes a condition amenable to self-medication? [S14]
a. Few factors we need to remember and understand.
b. A condition is self-limiting and recognizable by the patient. In other words, we usually take OTC drugs for
congestion, headache, and those sorts of things. We probably won’t take an OTC for hypertension or
hyperlipidemia. The patient doesn’t readily observe these diseases.
c. OTC medications are simply used to treat symptoms. Sudafed will help alleviate the symptoms of a cold. You
can’t take an OTC to get rid of a bacterial infection.
d. We need to make sure what we’re treating is not a symptom of some underlying, more serious problem
XIV.
When might self-medication NOT be appropriate? [S15]
a. Symptoms are too severe to be endured without definitive treatment and diagnosis
b. Symptoms persist.
c. Alarm signs (i.e. blood in stool, difficulty in breathing or swallowing) If these symptoms are experienced, an OTC
should not be taken. The patient should go see a health-care professional.
d. Symptoms are minor, but have persisted and do not appear to be the result of some easily identified cause
XV. When might self-medication NOT be appropriate? [S16]
a. If patients have pain that is of unknown origin, it would not be advisable to send them to CVS to get an OTC. This
may be something the patients can’t take care of themselves.
XVI.
OTC Sales by Category [S17]
a. A list of major categories of OTC drugs.
b. Highlighted three of the top categories in terms of sales.
c. A lot of the patients that come to see you may take products from at least one of these categories.
XVII. Analgesics/antipyretics[S18]
a. These are non-steroidal anti-inflammatory (NSAIDs) that are out there on the market that patients can get
without a prescription.
 Aspirin/salicylates
 Ibuprofen
 Ketoprofen
 Naproxen sodium
 Acetaminophen- Not really an NSAID
XVIII. Salicylates [S19-21]
a. Aspirin (acetylsalicyclic acid)
b. Uses: mild-to-moderate pain, reduce inflammation and fever, and anti-platelet (antithrombotic; 80mg Aspirin that
some take)
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Dr. Arnold
Pharmacology
Page 3 of 7
c. MOA: Inhibits prostaglandin synthesis, acts on the hypothalamus heat-regulating center to reduce fever, block
prostaglandin synthetase action, which prevents formation of the platelet-aggregating substance thromboxane
A2.
d. Aspirin prime example
e. Hypersensitivity occurs in 0.5% of patients but can result in severe bronchoconstriction
f. Contraindicated in patients with bleeding disorders or peptic ulcers and should not be given to children and
teenagers with viral infections due to the possibility of Reye’s Syndrome (i.e. fatty liver degeneration followed by
encephalopathy)
g. Can have hypersensitivity to these; can be very severe (ER visit)
h. Avoid if have bleeding disorders, especially aspirin
i. GI disturbances occur in up to 40% of patients (quite high) but are decreased by using enteric-coated products,
with food, or antacids
j. CNS disturbances can occur such as convulsions, confusion, and tinnitus (important in geriatric patients)
k. Caution in the last trimester of pregnancy due to potential bleeding problems
l. Interactions with anticoagulants and potentiate adverse GI effects of NSAIDs and alcohol
m. CNS disturbances are important in elderly; they are particularly susceptible
XIX.
Non-steroidal Anti-Inflammatories (NSAIDs) [S22-24]
a. Ibuprofen (advil), naproxen sodium (aleve), ketoprofen (orudis)
b. Naproxen and ketoprofen- use for osteoarthritis/chronic situations
c. Ibuprofen for acute pain (mild to moderate; good for minor procedures); less GI disturbances than aspirin
d. Contraindicated in patients with bleeding disorders or peptic ulcers
e. Caution in the last trimester of pregnancy
f. GI disturbances in up to 20% of patients but ibuprofen is generally preferred to aspirin
g. Interactions with anticoagulants, can potentiate hypoglycemics, and potentiate adverse GI effects of NSAIDs
and alcohol
h. Patients should be careful to not use one NSAID with another one
XX. Acetaminophen (Tylenol) [S25-26]
a. Uses: mild-to-moderate pain, anti-pyretic
b. Minimal anti-inflammation so be careful when using in patients who have significant swelling
c. MOA: Inhibits the synthesis of prostaglandins in the CNS and peripherally blocks pain impulse generation:
produces antipyresis from inhibition of hypothalmic heat-regulating center.
d. IMPORTANT: Tylenol is not the best choice if pt will have inflammation; good for slight pain and fever
e. Routinely used in patients who are sensitive to the GI disturbances caused by salicylates and NSAIDs
f. Generally safe but exercise caution in alcoholic patients, hepatic disease, or viral hepatitis
g. Good if sensitive to NSAIDs
h. No more than 4g of Tylenol/day (2g for alcoholics) because can facilitate hepatic toxicities
i. A LOT OF NARCOTIC ANALGESICS have at least one of these components in them: For example,
(Percoset (contains oxycodone and acetaminophen), Percodan (oxycodone and aspirin), Vicoprofen
(hydrocodone and ibuprofen), etc.) HAVE AT LEAST ONE OF THESE COMPONENTS (Tylenol, ibuprofen,
etc.) IN THEM!!!
j. Need to tell pt. to stop Tylenol, etc. use if they are taking narcotic analgesics (e.g. Percoset) because
they may quickly approach or surpass the 4g limit.
k. Be careful what OTC drugs you recommend.
XXI.
Cough/Cold vs. Antihistamines [S27]
a. Cough/cold
i. Guaifenesin
ii. Dextromethorphan
iii. Codeine
iv. Oxymetazoline
v. Pseudoephedrine
vi. Phenylephrine
b. Antihistamines
i. Chlorpheniramine
ii. Brompheniramine
iii. Clemastine
iv. Diphenhydramine
v. Doxylamine
vi. Loratidine
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Dr. Arnold
Pharmacology
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XXII. Decongestants [S28-29]
a. Phenylephrine (Sudafed PE), pseudoephedrine (Sudafed), oxymetazoline (Afrin; topical nasal spray)
b. Uses: nasal ventilation and drainage of congestion
c. Available as topical preparations, nasal sprays, and oral formulations
d. Rebound congestion can be a significant problem especially in patients who use the topical formulations
e. Systemic effects should as nervousness, and increased heart rate can be pronounced with oral agents
f. Oral decongestants should be avoided in patients with problems such as heart disease, hypertension,
hyperthyroidism
g. As a class, can cause significant rebound congestion- occurs at higher doses and extended usage
h. People can get addicted to these; especially with the topical ones because they don’t have the some of the
nervousness and systemic effects of oral drugs like pseudoephedrine and phenylephrine
XXIII. Pseudoephedrine OTC restrictions [S30]
a. Use pseudoephedrine to make methwhy it’s behind counter
i.
Can only obtain 6 grams in 30 days
XXIV. Expectorants [S31]
a. Cough and cold preparations.
b. Guaifenesin (Robitussin)
c. MOA: Stimulates respiratory tract secretions
d. Uses: decreases viscosity of mucus; increase the fluidity of mucus so it can be coughed out
e. Some clinicians believe an equivalent action can be obtained by pushing fluids (i.e. 8-10 glasses of water/day)
f. Works well with productive cough
XXV. Antitussives [S32]
a. Codeine, dextromethorphan (Delsym)- both relatively easy to get; codeine is OTC in some states even though it
is a narcotic (not OTC in AL, is in GA)
b. Uses: cough suppressants (i.e. nonproductive cough)
c. ADRs: (codeine) drowsiness, lightheadness, nausea, vomiting, respiratory depression (dextromethorphan)
drowsiness, GI upset, nausea
d. Antitussives prevent cough; Robitussin DM combines antitussive with an expectorant (helps remove phlegm
when coughing)- seemingly contradictory
XXVI. Antihistamines [S33-34]
a. Older generation agents can cause extreme sedation-newer agents (i.e. loratadine and Zyrtec) are non-sedating
b. Uses: allergic rhinitis (anything histamine driven) somewhat controversial in the common cold
c. Older agents cause a lot of sedation; newer ones cause much less sedation
d. Common cold is not very histamine driven- therefore antihistamines are not as useful with common cold
e. MOA: Inhibits histamine-1 receptors
f. ADRs: anticholinergic effects (dry mouth, blurred vision, difficulty in urination, constipation), nausea/vomiting,
CNS activation possible in children
XXVII. Antacids [S35-36]
a. Ranitidine
Magnesium hydroxide
b. Famotidine
Magnesium/aluminum
c. Cimetidine
Aluminum hydroxide
d. Nizatidine
Calcium carbonate
e. Omeprazole
Sodium bicarbonate
f. Sodium bicarbonate (Alka-seltzer), Calcium carbonate (Tums), Aluminum hydroxide (Amphojel), Magnesium
hydroxide (Milk of magnesia), Magnesium-aluminum combos (Maalox, Mylanta)
g. Uses: mild-to-moderate heartburn, onset within 5-15 minutes but short duration
h. Category has grown rapidly- OTC; neutralize acid
i. A lot of electrolytes in these, so careful when have renal dysfunction/failure
XXVIII. Antacids [S37]
a. Contraindications
i. Renal failure (due to electrolyte content)-use cautiously in patients with renal dysfunction or renal failure
ii. Too many antacids can affect absorption of other drugs, so be careful of this!
b. Drug Interactions
i. Absorption- can decrease the absorption of several drugs
ii. Antibiotics- if patient is taking antacids, may have to adjust the antibiotic dosage
XXIX. H2 Antagonists [S38]
a. Now OTC and have sold quite well as OTC
b. Antagonize mechanisms that decrease the activity of the proton pump in the stomach
c. Have very few drug interactions (important)
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Dr. Arnold
Pharmacology
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d. Cimetidine (Tagamet HB)
i. Has interactions with a ton of drugs and almost interacts with every drug out there
ii. When taking patient medical history, if patient is taking Tagament, you may want to investigate more to
make sure the drug you plan to give doesn’t interact with Tagament
e. Ranitidine (Zantac 75)
i. Has no drug interactions
XXX. Proton Pump Inhibitors [S39]
a. Omeprazole (Prilosec OTC)
i. Antacid family
b. Proton pump inhibitor and shuts of the pump at the source
c. Inhibits more gastric acid secretion than average dose H2 antagonists
i. Omeprazole is more effective as an antacid than the H2 antagonist
ii. H2 antagonist are one mechanism that contributes to proton pump inhibitor
XXXI. Conclusions [S40]
a. The drug interaction of OTC in combination with narcotic drugs- this is what he wants us to take away from
the lecture
i. Must get a full medical history if you are planning on prescribing drugs
ii. Ask about OTC products – you may be surprised what your patient is actually taking!!
iii. The interactions can be very serious, so we must be very careful
XXXII. Skin Anatomy Figure [S41]
a. Considerations of dermatologic drugs
b. Skin is largest organ of the body- protects us from noxious insults of the external environment. The skin has two
layers:
i. Epidermis- top part is made of stratum corneum- layer of dead cells, tough outer layer and things typically
can’t penetrate
ii. Dermis
XXXIII. Routes through the Stratum Corneum Figure [S42]
a. Put together as a brick like structure
b. Excludes penetration of drugs; in order to get through must go through intercellular spaces or transcellularly
through the cell spaces- this is difficult for drugs to do
XXXIV. Major Goals of Topical (Skin) Delivery [S43]
a. Ointments, creams, topical emulsions, etc.
b. Topical Therapy – delivery of therapeutic concentration of drug to a local site of action
i. Ex. if you have a rash- you must deliver the drug to the rash, in order to have the anti-inflammatory effects
at that spot
ii. Delivery of drug to the top of the skin
c. Not to be confused with transdermal (Patch) drug delivery
i. Patch that is put so the drug is delivered for systemic effects
XXXV. Topical Drugs for Local Application [S44]
a. Antibacterials
b. Antifungals
c. Corticosteroids
d. Local anesthetics- for local (topical) effects
e. …compared to…
f. Transdermal (patch) deliveryi. Drugs can be: antihypertensive, contraceptives, hormone replacement therapy
ii. Lots of different classes of drugs, found in patches, that can have systemic effects
g. Summary (the main thing)
i. Transdermal- drugs (can be potent) used for systemic effect
ii. Topical- local delivery
XXXVI. Drug Use in Geriatric Patients [S45]
a. More than 12% of the American population is over 65 years of age (about 34 million people)
i. The US as a population is getting older- so for the bulk of our careers, we will be treating will be geriatric
patients
b. Most geriatric patients are medicated; 3 out of every 4 elderly people are taking prescription medications
c. About 50% of all drug usage in the U.S. is in our elderly population
d. Adverse drug reactions in geriatric patients are 2-3 times greater than that seen in younger adult
patients (important)
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Dr. Arnold
Pharmacology
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XXXVII. Factors (Reasons) Contributing to Adverse Drug Reactions in Geriatric Patients [S46]
a. Poly-pharmacy
i. Probably the main reason
ii. Patients taking a lot of medications
iii. Defined as 5 or more prescription medications taken at one time; increased chance of drug interactions
b. Increased chance for disease state interactions
i. Because elderly patients are generally more sick (general rule)
c. Pharmacokinetic and pharmacodynamic parameters change as we get older
i. Due to physiological changes in the body
d. Poor adherence
i. Another reason why we have adverse drug effects in geriatric patients
ii. So if I have to remember to take a combination of 15 drugs four or five times day, I probably won’t
remember to take all of the drugs or I will take too many doses
XXXVIII.
Table 36.1 [S47]
a. As we get older, certain things happen that alter pharmacokinetic and pharmacodynamic dynamics (reason #3
on previous slide)
b. Table listings: wants us to be familiar with when we are considering our geriatric patients
c. GI motility is decreased in older patients
i. Medications that are time released may be altered because they are not going through the GI tract at the
rate that we expect
ii. Typically doesn’t affect the extent of absorption
iii. Affects how fast the drug is absorbed-we may not get the affect as fast as we think we should
d. Decline in kidney and liver function in older patients
i. Drugs rely on kidney and liver to get out of the body
ii. Diminished clearance of drugs
e. Serum albumin decreases as we age
i. Drugs that are highly plasma protein bound not as much albumin to bind to
ii. Leads to an increase free drug concentrations
iii. NSAIDs are highly plasma bound and can lead to enhanced concentration of the drugs floating around in
the body and an enhanced chance of toxicity that is secondary to those drugs
f. Our lean muscles begin to atrophy as we age
i. Muscle begins to distribute to fat because the ratio of body fat is higher to muscle
ii. Body water decreases- so the water soluble drugs do not distribute as well into to extra cellular fluid; can
lead to decrease volume of distribution
iii. Decrease distribution to the body as we should
g. Increased response to benzodiazepine (Valium, Xanax) and opiod analgesics
i. Act in CNS
ii. Have greater effect in elderly population- must be taken into consideration
XXXIX. General Principles for Drug Therapy in Geriatric Patients [S48]
a. Start with lowest most effective dose
b. Due to reduced renal and hepatic function
i. Drug clearance will probably be diminished and we need to take that into consideration, when talking about
total dose or interval
c. The fewest number of drugs should always be used to treat elderly patients
i. Because they are most likely taking a lot of drugs to begin with
d. Geriatric patients can have atypical presentations of adverse drug reactions, may manifest as CNS changes
i. CNS changes: dementia, hallucinations, etc.
XL. Drug Use in Pediatric Patients [S49]
a. Children are not “little adults”
i. This is important to remember
ii. When dosing a pediatric patient, you don’t give a fractional dose of the dose that you would give to a
normal adult because pediatric patients have differences in pharmacokinetics, pharmacodynamics, drug
clearance (this is true for geriatric patients too)
b. In contrast to adults and geriatric patients, pharmacokinetic and pharmacodynamics parameters rapidly align to
adult
i. The hepatic pharmacokinetics & pharmacodynamics and renal functions are similar to adults when they are
around 2 years old; liver and kidney begin to work well as well as it is going to at age 2
c. Still need to give slower doses because we are dosing smaller people
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Pharmacology
Page 7 of 7
XLI.
Pediatric Age Group Terminology Tbl. 1 [S50]
a. Heterogeneous (large range) population of patients
XLII.
Pharmacokinetic Considerations in Pediatric Patients [S51, 53]
a. Gastrointestinal transit time
i. gastric pH and gastric emptying
ii. smallest patients (less than 6 mo old) GI transit time is prolonged
1. similar to geriatrics
2. prolonged gastric emptying time- more absorption of some drugs because drug is staying around
longer
b. Percutaneous absorption
i. Absorption through the skin is increased in our smallest patients because their skin is thinner
ii. Well hydrated- hydration promotes drug penetration
c. Intramuscular absorption
i. Variable
ii. Muscle mass is smaller as a ratio to the body in small patients
d. Distribution
i. Protein binding, size of body compartments
e. Metabolism & Elimination
i. Drug elimination can be delayed because of renal and hepatic functions (in pediatrics)
ii. Rise to adults levels rapidly but takes a couple of years
XLIII. Table 2 Comparison of Body Composition [S52]
a. As we age, our body fluid decreases through childhood up to adulthood
b. Fat content- fat as a percent of the body can be quite different depending on the age of the child
i. Fat soluble drugs can distribute differently in a child than in an adult
c. Can see different drug distribution in premature infants than in an adult- we most monitor closely
XLIV. General Principles for Drug Therapy in Pediatric Patients [S54]
a. Most drugs that are out in the market, were never tested in pediatric populations (imp)
i. When drug comes out, there is little information about dosing the drug in pediatric patients
ii. Recently the FDA is trying to get drug manufacturers to test drugs in pediatric patients but is difficult to do
b. Adult doses cannot be extrapolated to children
i. Really tricky and takes a lot of time, research, and experience
c. Pediatric drug dosages can be obtained from pediatric references
i. Have doses for all of the drugs (can be found in particular handbooks)
ii. Great reference to have if you must dose pediatric patients
d. Adverse drugs reactions in pediatric patients are not inconsequential; smaller dose in a pediatric patient
doesn’t mean that we don’t have to worry about drug toxicities because of the smaller dose
e. Drug toxicities are a lot more serious in smaller patients because they don’t eliminate the drug as fast
(important)
A: H2 antagonist most drugs are really benign except Tagament; Tagament can block the metabolism of many
other drugs
[End 50:45]