PG 405
NAPLEX
Nonprescription (OTC)
Medications
Major categories of products to
review

Most important








PG 405
antacids , antidiarrheals
cough and cold remedies
diabetes products
dietary supplements
internal analgesics
laxatives
motion sickness
vitamins

Less Important

diet aids
eye solutions
external antiseptics
hemmorhoidal preps
mouthwashes
nutritional supplements

sunscreens





Strategies for reviewing

Be realistic – impossible to know all OTC
products and their ingredients

Concentrate on the types of ingredients in
each category
 cough suppressants – what’s available?
Strategies for reviewing

Learn only the major (best-selling) OTC
products and their ingredients and dosing
 Walk your shelves

Recognize the major problems (interactions,
key warnings/precautions) with each
ingredient

Be alert for Rx-to-OTC switches
Antacids

A pH range of between 3 and 4 should be maintained
during antacid therapy
 approximately 98% of all stomach acid is neutralized
but the gastric enzymes are still active for digestion

Antacids evaluated with USP “Acid Neutralizing
Capacity Test”
 based on the mEq of HCl consumed by the antacid
while still maintaining a pH of 3.5
PG 406
Major Ingredients of Antacids
Ingredient
Advantages
Disadvantages
Aluminum hydroxide
(Amphojel)
may cause constipation
decreased absorption
of phosphates
Magnesium
hydroxide
(MOM)
may cause diarrhea
accumulation of
magnesium ion in blood
– avoid if renal failure
Aluminum and
magnesium combo
(Maalox, Mylanta)
PG 406
Fewer side effects
than plain Al or Mg
may still cause
metabolic alkalosis and
magnesium
accumulation in renal
failure
Major Ingredients of Antacids
Ingredient
Calcium carbonate
(Tums, Alka-mints)
Advantages
Disadvantages
source of calcium
for osteoporosis
prevention
may cause
hypercalcemia and
kidney stones
Sodium bicarbonate
(alka-seltzer, Soda
Mint, ie)
Plus=simethacone
PG 406
High pH may cause acid
rebound
High sodium levels –
CHF/HTN
From the Pharmacist’s Letter 2008
You'll soon see a new formulation of Renagel called
Renvela. The original Renagel is the hydrochloride salt of
sevelamer... Renvela is a carbonate salt.
Both work equally well to bind phosphates in the gut...and
will cost about the same.
The carbonate salt is an acid buffer...the hydrochloride is
not. Therefore Renvela might help reduce the risk of
acidosis.
Keep in mind that Renagel will still be available for now.
Watch for potential mix-ups with Renagel and
Renvela...the names are very similar and the dosing is the
same.
General Comments on Antacids

Gavison and Algicon are intended for the
treatment GERD (lower neutralizing capacity)

Separate administration of Rx meds and antacids
by 2 hrs.
 iron, levodopa, quinolones, tetracyclines
 ketoconazole – needs lower pH for absorption

Can cause decrease activity of anticoagulants,
digoxin, phenothiazines, tetracylines as well
PG 407
Which of the following agents is NOT an
effective treatment for peptic ulcer
disease?
a. nizatidine
b. calcium carbonate
c. cetirizine
d. omeprazole
e. pantoprazole
Which of the following agents is NOT an
effective treatment for peptic ulcer
disease?
a. nizatidine (Axid)
b. calcium carbonate (Tums)
c. cetirizine (Zyrtec)
d. omeprazole (Prilosec)
e. pantoprazole (Protonix)
OTC H2-Antagonists & PPI

Cimetidine (Tagamet), famotidine (Pepcid),
ranitidine (Zantac), nizatidine (Axid) all have OTC
status
 dosing – half of RX dose
 interactions with cimetidine are significant
 Pepcid Complete – famotidine + calcium
carbonate + magnesium hydroxide
• provides rapid relief (CaCO3 and MgOH) plus
sustained acid suppression

Omeprazole (Prilosec OTC)

PG 407
20 mg daily before a meal for 14 days
Laxatives
Drugs known to cause
constipation











Antacids (calcium and aluminum)
Anticholinergics
Anticonvulsants
Antidepressants (TCAs)
Beta-blockers
Calcium Channel Blockers (verapamil)
Diuretics
Iron
Opiates (stimulant laxative is a must)
Clonidine
Methyldopa
PG 409
Laxatives

Classified into 5 categories





bulk-forming
emollient
lubricants
saline
stimulants

Categories have advantages/disadvantages.

Recognize abuse potential w/all laxatives
PG 407
Bulk Forming

Good initial choice; mild action





products swell and provide bulk for stool
formation
onset is 12-24 hrs., must take full glass of H2O
psyllium - Metamucil, Citracel, Fibercon
cellusoses
calcium polycarbophil
• Mitrolan and Equilactin
• can be used for constipation or diarrhea
• used in the treatment of IBS
PG 410
Emollients (stool softeners)

Used in patients w/severe HTN and
cardiovascular disease, post-hemorrhoidal
surgery
 act as a surfactant to soften stool
 Limits straining
 docusate (Colace) most common
• available in combination with a stimulant
• docusate + senna (Peri-colace)
• docusate + danthron (Doxidan)
PG 408
Lubricants

Sometimes used in elderly patients



also can act to soften stools
mineral oil most commonly used
disadvantage:
• impairs absorption of fat-soluble vitamins (A,D,E,K)
• aspiration risk in debilitated elderly – pneumonia
• avoid in pregnant women or patients on warfarin
PG 408
Saline Laxatives

Used for acute bowel evacuation


acts by osmotic pressure to increase water in
intestines/colon
Examples:
• magnesium sulfate/citrate (Epsom salts) – avoid in
renal impairment
• Phosphate salts (Fleets Phospho-soda) – have high
sodium levels
• Lactulose (Chronulose) – also used in hepatic failure
• Sorbitol

PG 409
rapid onset of action – don’t go far from home
Stimulants

Used alone or combination with other categories




stimulates GI motility
glycerin suppositories – dual action of stimulant and
lubricant
Senna (Senokot, Ex-Lax)
bisacodyl (Dulcolax)
• acts on colon, action in 6-10 hours when given PO, 15-60
min rectally
• enteric coated to prevent stomach irritation (avoid with
milk and antacids)

PG 409
castor oil – too strong, not recommended
Cold and Allergy Products

Classes of Agents to Know


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


Antihistamines
Decongestants
Antitussives
Expectorants
Analgesics / Antipyretics
Very many brand names, very few ingredients
 See top selling list on page 412
• NyQuil, Robitussin, Dimetap, Claritin, Sudafed,
PG 410
Antihistamines

Block H-1 receptors, decrease smooth muscle
response to histamine

Active Ingredients







brompheniramine – Dimetapp, Dimetane
chlorpheniramine – Chlor-Trimeton
clemastine – Tavist (D w / pseudoephedrine)
diphenhydramine – Benadryl
Loratadine – Claritin & Alavert
Cetirizine - Zyrtec
Counseling Points
• may cause drowsiness, CNS stimulation in children
• anticholingeric effects (dry mouth, tachycardia, urinary retention) can
be problematic in elderly patients, BPH
• narrow angle glaucoma
PG 410
Decongestants

Stimulate alpha-adrenergic receptors, causing
vasoconstriction of blood vessels

Active Ingredients


phenylephrine – Neo-Synephrine drops/spray
oxymetazoline or Xylometazoline – Afrin spray
• caution patients on overuse and secondary rebound congestion – do not use
for more than 3-5 consecutive days



pseudoephedrine – Sudefed, given po, 30-60mg q6h ; available
in numerous combinations
Use with caution in patients with HTN
Cromolyn nasal spray – mast cell stabilizer for nasal allergies and
allergic rhinitis – few side effects
PG 411
Antitussives / Expectorants

Antitussives - suppress cough reflex in the medullary cough
center
 dextromethorphan most common
 codeine limited by control drug laws
• may cause some drowsiness


Delsym has dextromethorphan alone - longer acting formulation
Expectorants
 thin mucous secretions in bronchioles
 guaifenesin is only one available
• counsel patients to consume large amounts of water

Robitussin +/- DM, Benylin, Mucinex
Trade Names: Robitussin DM, Naldecon, Dimetapp, PediaCare, Vicks, Triaminic, Benylin
PG 411
Analgesics

Background on pain


highly subjective, individualized symptom
numerous potential causes
•
•
•
•

organic pain – pathologic disturbance
psychogenic pain – emotional disturbance
somatic pain – from musculoskeletal system or skin
visceral pain – from organs, especially the stomach
Internal analgesics most effective for:
• Headache, neuralgia, myalgia, arthralgia, RA

Available agents

PG 413
APAP, ASA, ibuprofen, naproxen, ketoprofen
Analgesics (cont.)

Aspirin (ASA)


Available as 81mg, 325mg, EC, 81-325mg for CVD, 325-650mg
TID for pain, high dose for inflammation, RA
avoid use in young children (Reye Syndrome)
• Acquired encephalopathy in young children (infantcy-19 years)

Acetaminophen (APAP)




325mg, 500mg (extra strength), 650mg (max 4grms/day)
no anti-inflammatory
liver damage w/high dose, long-term, avoid alcohol, warfarin
interaction
Non-steroidal Anti-inflammatory Agents (NSAIDs)
PG 415

ibuprofen 200mg, naproxen 220mg, ketoprofen 12.5mg

avoid if GI disorders, frail elderly, kidney disease
External Analgesics

Used to treat local pain, itching from insect bites, burns,
muscle soreness
Anesthetics
 benzocaine 5% - 20% and lidocaine 2%
Anti-inflammatory
 hydrocortisone 0.5 – 1%, diphenhydramine 1-2%
Counterirritants
 methyl salicylate (Ben gay), menthol, camphor, eucalyptus
 capsaicin (inhibits substance P) – postherpetic neuralgia; use
continously, wash hands thoroughly, do not cover
PG 415
OTCs Continued

Sleep Aid Products


diphenydramine – note: Tylenol PM
Doxylamine (Unisom and in Nyquil)
•
•
•
•

be aware of many other products with antihistamines
do not use for long term; caution side effects
Not intended for kids <12
Not to be taken with alcohol
Sunscreen Agents



Sun Protection Factor = exposure time with skin protection
exposure time without
SPF of 15 should protect “all day” although reapplication is
recommended if swimming, sweating, ect.
Para-aminobenziod acid (PABA)
• 5% usual level
• Most common
PG 416
A patient who is experiencing a runny nose,
sneezing, headache and watery eyes should be
counseled to take which of the following OTC
agents?
I. diphenhydramine
II. acetaminophen
III. pseudoephedrine
a. I only
b. III only
c. I and II only
d. II and III only
e. I, II, and III
A patient who is experiencing a runny nose,
sneezing, headache and watery eyes should be
counseled to take which of the following OTC
agents?
I. diphenhydramine
II. acetaminophen
III. pseudoephedrine
a. I only
b. III only
c. I and II only
d. II and III only
e. I, II, and III
Antidiarrheals

Causes of diarrhea


Consultation w/ MD


microbes, drugs, IBS, colitis, foods
Duration >2 days , children <3y/o, fever or blood in stool
Agents



Adsorbants (water and toxins) – Kaopectate, pepto-bismol,
(bismuth)
Bulking agents – calcium polycarbophil (Fibercon, Fiberall)
Antiperistaltic agents – loperamide (Immodium 2mg)
• 2mg tabs, 1mg/5ml (Regimen – 4mg immediately, then 2mg until
loose bowel movement)


PG 417
Reestablish normal flora – lactobacillus acidophilus
(Lactinex) “reseed” the bowel, supress pathogenic
organisms---KEEP REFRIGERATED
Rehydrating solutions – Pedialyte, Infalyte
OTC Agents (cont.)

Calcium Supplements






Important for women to supplement, esp. post-menopausal or
those taking drugs for osteoporosis
Rec. doses: < age 50: 1000mg/day > 50: 1200-1500mg/d
Calcium carbonate (Oscal, Caltrate) taken with food, requires acidic
environment for absorption in stomach
Calcium citrate (Citracal) taken w/ or w/o, better absorbed in elderly
patients who have reduced stomach acid secretion
DON’T FORGET VIT D
Head Lice Products (parasites)


Permethrin (Nix) – caution if allergy to chrysanthemums
Pyrethrins (A-200, Rid, Pronto) – avoid if allergic to ragweed
•
•
•
•
PG 423
Wash hair without conditioner
Leave on hair 10 minutes
May repeat in 1 week
Must comb out nits
Premenstrual Syndrome Products




PG 425
Analgesics – Reduce synthesis of prostaglandins
Antihistamines – Pyrilamine - acts on smooth
muscles and reduce production of prolactin
Diuretic – Reduce bloating
 Ammonium Chloride, caffeine, pamabrom
Combination Products
 Aqua Ban, Midol, Midol PMS, Pamprin, Sunril
PG 427
NAPLEX
Dietary Supplements
Dietary Supplements - Definitions

Complimentary and Alternative Medicine



Dietary Supplements



Any product intended for ingestion as a supplement to the
diet
Includes herbal supplements, vitamins, minerals
Herbal Supplements

PG 426
Medicine practices not considered conventional
Includes herbal therapy, chiropractic, acupuncture,
homeopathy, biofeedback
Plant derived dietary supplements reported to have
medicinal and pharmacological effects
Regulatory Process

Industry began to take off in late-1980s


FDA began scrutinizing companies in early ’90s



herbal product use expanded, health concerns arose
consumers and the industry demanded the right to take and sell
these “dietary supplements”
wrote letters to Congress to campaign against regulations
FDA gave in and passed DSHEA of 1994
 Dietary Health and Education Act
Dietary Supplement Health and
Education Act of 1994

Categorized herbals, vitamins, protein bars, shakes as
“dietary supplements”
 manufacturers are not required to demonstrate safety, purity
or efficacy of supplements
 labeling must include FDA statement:
• Statement not evaluated by FDA, not intended to
diagnose, treat, cure or prevent disease
 products cannot have specific claims on labels
• use phrases like “helps boost, support, enhance…”

FDA can pull products if suspected unsafe
 Ephedra and Ma Huang - 2004
PG 426
DSHEA of 1994 - Limitations

Safety is reactive, not proactive; limited safety information
available

Available studies are small and poorly designed; a wide
variety of products are not available in the US

There are no standards for manufacturing practices;
labeled amounts and ingredients may be inaccurate

The FDA is considering imposing a requirement for good
manufacturing practices (GMPs) for all dietary
supplements.
PG 426
The Top 20 Dietary
Supplements



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


PG 426
Glucosamine/Chondroitin
Echinacea
Ginkgo biloba
Ginseng
Saw palmetto
Fish oil
St John’s Wort
Garlic
Melatonin
Coenzyme Q10










Cranberry
Feverfew
Ginger
Milk thistle
Soy isoflavones
Black cohosh
Valerian
Hawthorn
SAM-e
MSM
Glucosamine

Not an herbal; glycoprotein derived from marine
exoskeletons or synthetically


active compounds: glucosamine itself;(HCL or SO4)
Proposed Uses



PG 426
treatment of osteoarthritis; used in combination w/
chondroitin
mechanism of action
• Glucosamine stimulates metabolism of chondrocytes
in articular cartilage; preventing cartilage
breakdown and potential regrowth
• Chondroitin believed to serve as substrate for
production of joint matrix substances (minimally
absorbed)
dosing
• 500mg TID, (w/200-400mg of chondroitin)
Glucosamine/Chondroitin - Safety


Few common or serious ADRs reported
• GI, n/v, HA, drowsiness, similar to placebo
Interactions
 antidiabetic drugs - decreased effect
• anticoagulants w/chondroitin
 Caution in DM, HTN, Hyperlipidemia

PG 428
Caution in shellfish allergy
Glucosamine/Chondroitin - Efficacy

Osteoarthritis


Widely studied w/most trials demonstrating benefits
• shown to reduce pain and joint stiffness
• studied against low-moderate dose NSAIDs
• pain benefits modest but significant
Reginster et al. - effect on disease progression
• 106 pts. w/knee OA treated for 3 years with
1500mg/day vs. 106 pts. on placebo
• endpoints: radiographic changes, joint-narrowing
• results: -0.06mm tx. vs. –0.31mm placebo, also
symptom improvements
Reginster JY et al. Lancet 2001; 357: 251-56
PG 428
Glucosamine/Chondroitin - Efficacy

Some important counseling points




May confer benefits unlike other OA treatments

PG 426
requires 4-6 weeks of tx. for benefits to be seen
not for PRN use, must continually use
the sulfate salt is recommended, also some controversy on
combo w/chondroitin
cost is an issue, should insurance pay for it?
Echinacea

Extracts of E. purpurea and E. angustifolia
active compounds: several active constituents
Proposed Uses
 treating and preventing the common cold and URIs
• immunostimulant for treatment of infections
 mechanism of action
• some direct antiviral activity, stimulates lymphocyte
activity, increases phagocytosis, also antifungal
activity
 dosing
• 300mg TID for 7-14 days, must start at first sign of
sxs.
• 6-9ml of E. purpurea juice daily


PG 429
Echinacea- Safety

Adverse Effects


Drug Interactions
 Immunosuppressants
• may interfere w/therapy
 May inhibit CYP450 enzymes (CYP3A4)

PG 427
allergic reactions, rash fever, n/v
• a number of case reports of allergic reactions
avoid in pts. w/ autoimmune disorders
Echinacea – Efficacy

Prevention of colds/flu – benefits unclear

Grimm et al. Prevention w/ E.purpurea juice
•
•
•
•

109 pts. w/>3 colds in prev. year
4ml juice or placebo BID x 8 weeks
infx. rate: 65% vs. 74% (tx. vs. placebo)
no statistical benefit vs. placebo
Turner et al. Prevention of experimental colds
• No statistical difference in infection or illness rates vs. placebo, but
trend toward benefit w/Echinacea
Grimm et al. Am J Med 1999;106:259-60
Turner et al. Antimicrob Agents Chemother 2000;44:1708-9
PG 427
Echinacea – Efficacy

Treatment of cold and flu

Overall data suggests modest reductions in
duration and severity of symptoms
• studies varied in preparations used
• All initiated therapy at first sign of symptoms
• improvements seen on subjective symptoms severity and
duration questionnaires
• reduction in duration of approx. 1-2 days
Barrett et al. J Fam Pract 1999;48:628-35
PG 427
Gingko Biloba


PG 429
Extract derived from leaves of tree
 active compounds: flavonoids, terpenoids
Proposed Uses
 conditions assoc. w/cerebral vascular insufficiency
• Alzheimer’s dementia, memory loss, vertigo, tinnitus
• Others: intermittent claudication, motion sickness
 mechanism of action
• antioxidant activity, decrease blood viscosity
(inhibits platelet activation factor (PAF)), improve
circulatory flow
 dosing
• 120-240mg of leaf extract day/divided doses
Gingko Biloba - Safety

Adverse Effects
 Few common or serious ADRs documented
• mild GI upset, constip. Dizziness, HA
• high doses: diarrhea, restlessness, bleeding?

Drug Interactions**
 Anticoagulants, antiplatelet agents
• inhibits platelet activation factor (PAF)

May inhibit CYP450 enzymes
• inhibits 1A2, 2D6; induce or inhibit 3A4

PG 427
Caution in diabetes patients, epileptics
Gingko Biloba – Efficacy

Dementia: Alzheimer’s or vascular

meta-analysis in 1998: 50 studies identified, only 4 met
criteria ( 212 pts. total, 3-6 mos. in duration)
• fairly consistent improvements in cognitive function shown
(ADAS-Cog.)
• may delay progression

Memory Improvement


some improvements in short-term memory and cognition in
adults w/o dementia
Vertigo, Claudication
• few positive studies
Oken et al. Arch Neurol. 1998;55:1409-1415
PG 427
Ginseng

Extract from plant root; three types (American,
Asian** (Panax), Siberian)


Proposed Uses (panax ginseng)



PG 429
active compounds: ginsenosides
adaptogen (increases resistance to stress), improve immune
function, general tonic to improve energy
mechanism of action
• wide range of possible effects, stimulate immune
cells, affect adrenal gland secretion, increase
cortisol levels, many others
dosing
• 200mg – 600mg/day in capsule form, also in tea form
Ginseng - Safety

Rare but potentially serious ADRs reported
• short term < 3 mos., insomnia, edema, HTN
tachycardia
• Steven-Johnson syndrome
• avoid long-term use as may increase ADRs

Interactions





PG 429
anticoagulants (warfarin, ASA); bleeding risk
antidiabetic drugs; increased effect
immunosuppresants; reduced effect
may inhibit CYP2D6
caution in DM, cardiac dz., insomnia
Ginseng - Efficacy

Meta-analysis by Vogler et al.


PG 428
16 trials met inclusion criteria
• most were poor in quality
• numerous indications studied (energy/exercise
capacity, mood, immune function, memory)
• few beneficial effects seen vs. placebo
Probably not the “energy pill” people want it to be
• in low-doses, probably won’t hurt or help (placebo
effect)
Saw Palmetto

Extract of fruit from native American tree


active compounds: multiple fatty acid compounds
Proposed Uses


treatment of symptoms of benign prostatic hypertrophy,
prostate CA, alopecia?
mechanism of action
• appears to competitively inhibit 5-alpha reductase,
preventing conversion of testosterone to
dihydrotestosterone, leading to shrinking of prostate
– think finasteride (Proscar), dutasteride (Avodart)

PG 428
• also has anti-inflammatory process
dosing
• 160mg bid of extract containing 80-90% fatty acids
Saw Palmetto - Safety

Few common or serious ADRs reported
• dizziness, n/v/d
• sexual dysfunction (meta-analysis findings)
– 0.7% placebo
– 1.1% saw palmetto
– 4.9% finasteride

Drug Interactions

few noted
• additive effect or ADRs w/finasteride?
• hormone therapy

PG 428
does not affect PSA levels
Saw Palmetto - Efficacy

Benign Prostatic Hypertrophy

PG 430
Overall data suggests benefits
• multiple studies up to 48 wks have shown significant
improvement in urinary symptoms (nocturia, urine
flow)
• does not appear to affect prostate size
• symptomatic effects seem comparable to finasteride,
less than alpha-blockers
– not studied head-to-head w/alpha-blockers
Fish Oil

Derived from fatty fish (salmon, sardine, trout)

EPA and DHA are essential fatty acids

Rx prescription – Omacor change to Lovaza

Proposed uses: heart disease, hypertriglyceridemia

Mechanism of action: competes with arachidonic acid in
the COX and lipoxygenase pathways

Dosing: 1 g qd (CHD); 2-4 g/d for TGs
PG 430
Fish Oil - Safety

Most common
 Fishy aftertaste, GI intolerance, loose stools,
belching (dose-related)
 Allergies to fish protein not fish oil

Drug interactions
 Anticoagulants
 Antiplatelets
• Increase bleeding risk
• Does not appear to affect INR
PG 431
Fish Oil - Efficacy

Prevention of CHD
 Retrospective and prospective studies suggest benefits,
especially in high-risk patients

Hypertriglyceridemia
 Studies suggest 25-30% reductions in triglycerides with use of
higher doses
 Small increase in LDL and HDL also seen

Flaxseed Oil - Also point out that the omega-3s in flaxseed and
some nuts are different than the ones in fish. They contain alphalinolenic acid (ALA) which is the precursor of EPA and DHA. But the
amount of EPA and DHA the body converts from ALA is minimal.
Diets high in these foods MIGHT help decrease heart disease...but
NOT triglycerides.
PG 431
St. John’s Wort (SJW)


PG 431
Extract from buds, leaves & flowers of hypericum
perforatum
 active compounds: hypericin, hyperforin
Proposed Uses
 treatment of mild to moderate depression
 mechanism of action
• hypericin inhibits COMT & MAO, hyperforin
modulates effects of serotonin, inhibits reuptake of
various neurotransmitters
 dosing
• 300mg TID of extract standardized to 0.3% hypericin
content; other doses studies
St. John’s Wort - Safety


PG 431
Some adverse effects reported
• gastrointestinal, dry mouth, restlessness / insomnia
more common
• also vivid dreams, agitation, mania, dizziness, skin
rash, photosensitivity reported
• ADR profile similar to TCAs, fewer cardiac effects
• unsafe at high doses
Drug Interactions
 all antidepressants, triptans;
 Induces CYP450; reduce levels of cyclosporine, HIV meds,
OCs, CBZ, warfarin
 Caution in bipolar, schizophrenia, Alzheimer's
St. John’s Wort - Efficacy

Mild to Mod. Depression
• widely studied in Europe
• most evidence suggests as effective as low dose TCAs,
possibly as effective as SSRIs
• recent study reported no benefit; however pts. had more
severe depression
• depression in NOT like the common cold ; self-tx. not safe
in my mind
PG 431
Garlic :

Tasty spice used heavily in Italian cuisine
active compounds: alliin, allicin
Proposed Uses
 hyperlipidemia, hypertension, prevention of atherosclerosis
 mechanism of action
• may act as an HMG-CoA reductase inhibitor, may
vasodilate and relax smooth muscle, release NO
• may also reduce oxidation of LDL, inhibit platelet
function
 dosing
• 600mg – 1200mg in divided doses for HTN,
hyperlipidemia
– 4-6 cloves of wholes garlic/day
• most trials used garlic powder extract (1.3% alliin)


PG 431
“Cholesterol’s natural enemy”?
Garlic - Safety

Safe w/the exception of social side-effects
• GI, heartburn, n/v, BAD BREATH

Drug Interactions

antidiabetic medications
• risk of hypoglycemia

anticoagulants (warfarin, ASA)
• can increase INR and bleeding risk

induces CYP3A4
• cyclosporine, saquinivir, OCs
PG 430
Garlic - Efficacy

Hyperlipidemia


Meta-analysis by Stevinson et. al in 2002
– 13 of 39 trials met inclusion criteria
– 796 pts., 8-24 wks, 900mg/day most common
– overall reduction of 16mg/dl in TC (6% dec.)
– small, non-significant changes in LDL, HDL
• long-term clinical CV benefits unknown
Hypertension

7.7 mmHg reduction in SBP after 4 weeks
Stevinson et. al. Ann Intern Med 2000;133:420-9
Silagy CA et al. J Hypertens 1994;12:463-8
PG 432
Melatonin




Not an herbal; hormone that control circadian rhythm
and sleep-wake cycle
Proposed use: treatment of insomnia, jet lag
Mechanism of action: stimulates binding of GABA in
the CNS; leading to neuroinhibitory effects
Dosing:
 Insomnia: doses range from 0.3-5 mg hs
 Jet lag: 0.5-5 mg on day of arrival and
continued for 2-5 days
PG 432
Melatonin - Safety

Appears safe for short-term use (<2 mo)

ADRs
 Fatigue, drowsiness, anxiety, dizziness
 Avoid driving within 4-5 hours

Drug interactions
 Medications with CNS depressant effects
 May increasae BP and impair blood sugar control
 Potential antiplatelet effects
PG 432
Melatonin - Efficacy

Insomnia
 Results are mixed; may improve sleep
quality, especially in elderly subjects;
may not increase sleep duration

Jet lag
 May reduce symptoms of jet lag when
dosed appropriately; efficacy results
mixed
PG 432
Which of the following herbal products
does not have the potential to interact
with anticoagulant / antiplatelet agents?
a. gingko biloba
b. ginseng
c. garlic
d. saw palmetto
e. feverfew
Which of the following herbal products
does not have the potential to interact
with anticoagulant / antiplatelet agents?
a. gingko biloba
b. ginseng
c. garlic
d. saw palmetto
e. feverfew
Coenzyme Q10

Also not an herbal; substance found in all cells


Proposed Uses



PG 433
active compounds: a.k.a. ubiquinone
Treatment of congestive heart failure, angina, HTN
mechanism of action
• found in higher concentrations in cells of heart, liver,
lungs; has powerful antioxidant activity
• also serves as a co-factor for ATP in oxidative resp.,
appears to be beneficial in condition assoc. w/low
levels of CoQ10 (CHF)
dosing
• 100mg /day in divided doses (50mg BID)
Coenzyme Q10 - Safety

Few common or serious ADRs reported


very rare GI adverse effects noted
Drug Interactions





PG 433
warfarin; reduced effect due to similarity to vit. K;
antineoplastics; may protect tumor cells
synergistic effects w/ anti-HTNs
Statins lower CoQ10 levels; clinical signif. not known
caution; LFTS, HTN
Coenzyme Q10 - Efficacy

Treatment of congestive heart failure
 conflicting data
• a number of trials have shown benefits in QOL,
symptoms, hosp. Rates (poor design)
• Khatta et al. – more severe disease (class III,IV)
– no benefit seen in EF or exercise tolerance in 55
pts. treated for 6 months
• possibly consider in mild/moderate CHF in pts.
already on optimal Rx therapy

Angina, Hypertension
• Minimal benefits seen
Tran MT et al. Pharmacotherapy 2001;21:797-806
Khatta M et al. Ann Intern Med 2000;132:636-640
PG 431
Resources

Facts and Comparison: Review of Natural Products


good general info., poor on dosing
PDR for Herbal Medicines
• Hard to find unless you know plant names

German Commission E Monographs


monographs are not referenced, lack substance
Natural Medicine Comprehensive Database



THE BEST, updated, referenced, thorough
Costly ($132.00, book plus 1 year online)
www. naturaldatabase.com
When taken orally, all of the following drugs
may cause discoloration of soft-contact
lenses EXCEPT:
a. rifampin
b. ferrous gluconate
c. tetracycline
d. phenazopyridine
e. estrogens
When taken orally, all of the following drugs
may cause discoloration of soft-contact
lenses EXCEPT:
a. rifampin
b. ferrous gluconate
c. tetracycline
d. phenazopyridine
e. estrogens
Oxymetazoline acts as a nasal decongestant
by:
a. Causing a local anesthetic action
b. Blocking at the synaptic ganglia
c. Constricting blood vessels by alphaadrenergic stimulation
d. Dilating blood vessels by beta-adrenergic
stimulation
e. Blocking muscarinic receptors
Oxymetazoline acts as a nasal decongestant
by:
a. Causing a local anesthetic action
b. Blocking at the synaptic ganglia
c. Constricting blood vessels by alphaadrenergic stimulation
d. Dilating blood vessels by beta-adrenergic
stimulation
e. Blocking muscarinic receptors
Ingredients in Mylanta include:
I. Aluminum hydroxide
II. Magnesium hydroxide
III. Calcium carbonate
a. I only
b. III only
c. I and II only
d. II and III only
e. I, II, and III
Ingredients in Mylanta include:
I. Aluminum hydroxide
II. Magnesium hydroxide
III. Calcium carbonate
a. I only
b. III only
c. I and II only
d. II and III only
e. I, II, and III
A pharmacist should caution a patient purchasing
the dietary supplement glucosamine plus
chondroitin if he/she is allergic to which of the
following:
I. Bisulfites
II. Eggs
III. Shellfish
a. I only
b. III only
c. I and II only
d. II and III only
e. I, II, and III
A pharmacist should caution a patient purchasing
the dietary supplement glucosamine plus
chondroitin if he/she is allergic to which of the
following:
I. Bisulfites
II. Eggs
III. Shellfish
a. I only
b. III only
c. I and II only
d. II and III only
e. I, II, and III
Concurrent administration of antacids will
increase the plasma level of:
I. levodopa
II. ciprofloxacin
III. warfarin
a. I only
b. III only
c. I and II only
d. II and III only
e. I, II, and III
Concurrent administration of antacids will
increase the plasma level of:
I. levodopa
II. ciprofloxacin
III. warfarin
a. I only
b. III only
c. I and II only
d. II and III only
e. I, II, and III
Which of the following is an/are active
ingredient(s) in Children’s Dimetapp ND?
a. brompheniramine
b. brompheniramine and pseudoephedrine
c. loratadine
d. phenylephrine
e. pseudoephedrine
Which of the following is an/are active
ingredient(s) in Children’s Dimetapp ND?
a. brompheniramine
b. brompheniramine and pseudoephedrine
c. loratadine
d. phenylephrine
e. pseudoephedrine
THANKS!!!!!