Download Bruyere/Primrose Units - R. Halil, August 2015

The ABCs of OTCs
Over the Counter Products
ROLAND HALIL ,
BSC(HON), BSC.PHARM, ACPR, PHARMD
B R U Y E R E A C A D E M I C FA M I LY H E A LT H T E A M
D E PA R T M E N T O F FA M I LY M E D I C I N E , U O T TAWA
[email protected]
AU G 2 0 1 5
Objectives
1. Simplify the understanding of OTCs
2. Dispel myths of brand competition
3. Discuss basic pharmacological ingredients
common to most products
4. Rationalize the choice of therapy when
considering OTC products
5. Identify factors that may alter management by
the primary provider
Table of Contents
 Antihistamines
 Analgesics
 Cough & Cold
 Emergency Contraception
 Anti-fungals & Anti-parasitics
 Vitamins and Minerals
 Antacids
 Laxatives
 Herbals & Natural Products (Briefly!)
Choosing Therapy
 Rational prescribing
 When evidence for
requires a process.
 Consider (in order):
efficacy is strong:
1.
2.
3.
4.
Efficacy
Toxicity
Cost
Convenience
o
Balance population-based
efficacy with individual
potential toxicities.
 When evidence for
efficacy is weak:
First, Do No Harm
 (ie. Toxicity outweighs
Efficacy)

OTCs
 Large variety of OTC products
 Many brand extensions
 But, most OTCs have…
 The same ingredients mixed in many combos
 Poor evidence for efficacy or good evidence of limited efficacy
 Important safety precautions


An incorrect presumption of safety
Are monetized versions of ‘home remedies’
 Focus on the Risk/Benefit of these limited ingredients
 Choice of therapeutics will be informed by understanding their
pharmacology
 Identify at-risk populations
Antihistamines
Antihistamines - Allergies
1st generation
2nd generation
More sedating
Less-sedating
Less specific for H1 rec
More specific for H1 rec

Anticholinergic etc.
Shorter acting (8hrs)
More potent:
 Diphenhydramine
(Benadryl®)
 Chlorpheniramine (ChlorTripolon®)
 Doxylamine
Longer acting (24hrs)
But less potent
 (Des)-Loratadine (Claritin®,
Aerius®)
 Cetirizine (Reactine®)
 Fexofenadine (Allegra®)
Marketed as non-sedating!
Antihistamines - Bottom Line
First Generation
 Efficacy
Equivalent
 More potent vs 2nd gen

Second Generation
 Efficacy
Equivalent
 Less potent vs 1st gen

 Toxicity
 Equivalent
 Toxicity
 Equivalent
 Cost
 Generics cheaper
 Cost
 Generics much cheaper
 Convenience
 Equivalent amongst 1st
generation
 Q8h dosing
 Convenience
 Equivalent amongst 2nd
generation
 Q24h dosing
Cough & Cold
Flu & Sinus
Cough & Cold
Flu & Sinus
 Everything is some combination of:
 Antihistamine
 Diphenhydramine, chlorpheniramine, doxylamine
 Analgesic / Antipyretic
 Acetaminophen, ibuprofen, ASA
 Decongestant
 Phenylephrine, pseudephedrine
 Anti-tussive
 Dextromethorphan, codeine
 Expectorant
 guaifenesin
Cough & Cold
Flu & Sinus
 There is no evidence for benefit, only symptomatic
relief!
 There is certainly risk of harm!



Products pulled for kids < 2 y.o.
Will be relabelled for use > 6 y.o.
Plenty of risks for adults too…
 Take Home: Only use if really needed and non-pharms
are ineffective for relief
Analgesics / Anti-pyretics
 Acetaminophen or NSAIDs (ASA, Ibuprofen)
 Efficacy
– no difference (in analgesia, nor anti-pyresis)
 Toxicity: _______________________
 Cost – no difference (cheap & generic)
 Convenience: no difference (all q4h)
Pierce CA et al. Efficacy and safety of ibuprofen and acetaminophen in children and adults: a meta-analysis and qualitative review. Ann
Pharmacother. 2010 Mar;44(3):489-506. PMID: 20150507
Analgesics / Anti-pyretics
 Acetaminophen or NSAIDs (ASA, Ibuprofen)

Toxicity: (generally well tolerated)
 Acetaminophen: Risk in overdose: hepatotoxicity
 Especially with combo products!
 Ibuprofen & ASA (as well as Naproxen and topical Diclofenac)
 1) Risk of acute renal failure (ARF)
• Avoid in renal disease, or with ACEinh, ARBs, diuretics
 2)
Risk of GI bleed
• Avoid with anti-thrombotics, or history of bleeding
 3)
Risk of hypertension
• Avoid in HTN, vasculopaths etc
Decongestants
Phenylephrine & Pseudoephedrine
 1) Efficacy – equivalent
 Relief of nasal congestion via
vasoconstriction
 2) Toxicity:
 Sympathomimetic
Amphetamine derivatives!
 Insomnia, tachycardia,
hypertension, palpitations ,
anxiety, agitation, etc.
 Avoid in vasculopaths ,
insomniacs, anxious patients,
hyperthyroidism, etc!

 .
 3) Cost – equivalent
 4) Convenience – equivalent
 Counteracts sedation of
antihistamines

Also added to “Daytime”
formulations

No sinus pressure? No
decongestant.


Won’t dry a runny nose
Topical Decongestants:
naphazoline, oxymetazoline

Rebound congestion with
“prolonged” use (> 3-5 days)
Anti-Tussives & Expectorants
 Dextromethorphan (DM syrup) & codeine:
 Codeine is a better anti-tussive vs DM


Risk of sedation, CNS effects



But, it’s kept behind the counter. (Schedule 2)
Constipation with codeine, abuse potential
DM cheaper than Codeine preps
Equivalent dosing frequency
 Guaifenasin: expectorant, not anti-tussive
 No better than adequate hydration
 Likely more benefit from sticky syrup on throat
Cough & Cold; Sinus & Flu
 Combination products:
 Eg. DM + guaifenasin + decongestant
 Lack of flexibility
 Not always logical (anti-tussive + expectorant?)
 Herbals/Natural Products: (Lozenges)
 Little evidence to support use
 Stimulate saliva secretion – throat soothing
 Echinacea: requires large doses, avoid in autoimmune
diseases
 Vitamin C (>1g/day) decreases cold sx duration by ½ day
 Zinc lozenges must be used q2h at onset of cold but poor
taste/tolerability
Cough & Cold – Take Home
 Symptomatic relief only
 Risk of toxicity
 Especially combinations of combination products! (acetaminophen
overdose)
 Buy individual ingredients based on need
 Avoid combination products with unnecessary ingredients
 Antihistamines for runny nose or eyes
 Analgesics for pain or fever
 Anti-tussive for cough
 Avoid decongestants!
 Try home remedies first
Emergency Contraception
Emergency Contraception

Birth control used after intercourse &
before implantation

It is not an abortifacient
 Multiple options

IUD insertion


Within 5-7 days of unprotected intercourse
Hormone tablets

Now available Over the Counter
OTC Emergency Contraception

Emergency Contraception Pills (ECPs)


1.
2.
aka “morning after” pill
Actually, within 72 hrs
Combined Regimen (YUZPE):
–
Levonorgestrel 500ug + Ethinyl Estradiol (EE)
100ug Q12H x 2
–
Eg: Ovral - 2 tab Q12H x 2 doses
Progestin Only:


Plan B® - Levonorgestrel 750ug
2 tabs stat
 N.B.
Less effective if > 75kg & ineffective if > 80kg
Proportion of Pregnancies Prevented by
Levonorgestrel vs. Yuzpe, by Timing of Treatment
100%
Levonorgestrel
Yuzpe
95%
80%
85%
77%
60%
58%
40%
36%
20%
0%
31%
<24
25-48
49-62
Timing of Treatment (hours)
N.B. Treatment is more effective the sooner it begins!
Task Force on Postovulatory Methods of Fertility Regulation.
Lancet. 1998;352:428-433.
Yuzpe Regimen: OC Formulations
Brand Name
Pills/Dose
g EE/
Dose
mg
levonorgestrel/
Dose
Ovral
Alesse
Levlite
Nordette
Levlen
Levora
Lo/Ovral
Triphasil
Tri-Levlen
Trivora
2 white
5 pink
5 pink
4 light orange
4 light orange
4 white
4 white
4 yellow
4 yellow
4 pink
100
100
100
120
120
120
120
120
120
120
0.50
0.50
0.50
0.60
0.60
0.60
0.60
0.50
0.50
0.50
Adapted from ACOG Practice Bulletin. Int J Gynecol Obstet. 2002;78:191-198.
OTC Emergency Contraception
 ECP Safety:
 No absolute contraindications except known pregnancy (ineffective)
 If strong contraindications to estrogen (VTE, breast cancer):

Use Plan B
 ECP Side effects:
 Nausea / Vomiting: Yuzpe (50%), Plan B (20%)
 Bloating, cramping, breast tenderness
 Spotting (normal!)
 Early / late menses
Emergency Contraception – cont’d
 Missed pills:
 If >1 hour w/ emesis  do not repeat dose
 If <1 hour w/ emesis  repeat dose with antiemetic
 Second dose late:
 < 3 hours late – take as usual
 > 3 hours late – take ASAP then take a 3rd dose 12 hours later
Moot
point now with Plan B – 2 tabs stat only
Plan B - Take Home
 Efficacy
 More effective vs Yuzpe method
 Toxicity
 Fewer side effects vs Yuzpe method
 Cost
 ~ $35-$40 is generally affordable to most
 Convenience
 New Dosing – 2 doses stat – improved compliance
 New OTC status – but sometimes still kept behind the counter to
minimize theft
Anti-Fungals
Fungal Infections - Tinea Pedis
 Superficial infections of the skin or nails
 Trichophyton rubrum, T. mentagrophytes & Epidermophyton
floccosum etc.
 Acute symptoms
 Wet
 Smelly
 Small blisters that ooze (due to secondary bacterial infection)
 Chronic symptoms
 Dry
 Itchy
 Scaly skin
Fungal Infections - Tinea Pedis
 Pharmacological Options:
 Acute:
antifungal + antibiotic (for Gram[-] infection)
 Chronic: antifungal agents
Butenafine
 fungicidal,
HCl 1% (Dr. Scholl’s®)
90% effective, QD
Clotrimazole 1% (Canesten®),
Tolnaftate (Tinactin®)
 fungistatic
Miconazole (Micatin®),
and weak antibiotic/anti-inflammatory
properties, 70-80% effective, cream, BID
 Monitoring for resolution:
 Acute - within 1 week,
 Chronic - within 6 weeks
Anti-fungals - Take Home
 Fungus – “slow to grow; slow to go”.
 Efficacy – about the same
 Toxicity – about the same
 Cost – about the same
 Therefore, compliance and patience are important!
Any
cream will do
(Compliance
is more important than published
rates of eradication)
Fungal Infections
- Vaginitis
Fungal Infections - Vaginitis
 Imidazole antifungal agents
 70-90% effective
 1,
3, 7-day treatments available
 Multi-day vs one day treatments
Equivalent efficacy, but multi-day is
better tolerated
(lower toxicity)
Miconazole (Monistat®)
 Clotrimazole (Canesten®)
 Tioconazole (Gynecure®)
 Terconazole (Terazol®)


Old school: Boric acid 600mg capsules intravaginally qd - bid
x 14 days
Lice - Pediculosis
Pediculosis
 For body lice:
 Hot water wash or dry clean clothes; Unwashables sealed in plastic for 10
days; Vaseline for eyelashes
 For head & pubic lice:

Treat all contacts, and re-treat in 1 week
Permethrin 1%
 (Nix Cream Rinse®, Kwellada-P Cream Rinse®)
 apply to towel dried hair, leave on for 10 min,
 best ovicidal activity (96-100% with retreatment)
 Pyrethrins with piperonyl butoxide
 (Pronto Lice Control System®, R&C Shampoo/Conditioner®)
 apply to dry hair
 White vinegar (Step 2®) apply before lice treatment, soak hair then wrap
in towel for 30-60min
 Lindane (PMS Lindane®, Hexit Shampoo®)
 not first line due to toxicities, (pesticide!)
 apply to dry hair for 4 min

Pinworms
 Infection of the colon by Enterobius vermicularis
 Common in school-age kids (2-5 y.o.)
 Pharm Options: treat all members of the household, retreat in 14
days


Pyrantel pamoate (Combantrin®) – single dose - 11mg/kg suspension, up to
max 1g/day, avoid in pregnancy
Pyrivinium pamoate (Vanquin®) – single dose - 5mg/kg susp up to max
350mg/day, stains teeth/feces red, preferred in symptomatic pregnant
women
 Non-Pharms:
 Wash hands/nails before meals and after use of washroom, regular cleaning
of linens/clothes
 Change night clothes & linens at start of each treatment
 Discourage nail biting/finger sucking
Vitamins & Minerals
Vitamins & Minerals – Take Home
 All multi-vitamins are created equal
 Choose individual vitamins & minerals based on specific
needs / deficiencies
 Beware common interactions

Eg. Calcium & Iron
Ca2+
(or Fe, Mg2+, Al3+) plus:
 Antibiotics
(Fluoroquinolones, Tetracyclines)
 Levothyroxine
Vitamins – Water soluble
 Vit B1 (thiamine) – 50-100mg qd - alcoholics
 Vit B2 (riboflavin) – 400mg qd for migraine
prophylaxis
 Vit B3 (niacin) – 1000mg for raising HDL (no benefit)
 Vit B6 (pyridoxine) – 25-100 mg - prevention of INH
toxicity
 Vit B9 (folate) – 0.4 – 5 mg - prevention of neural
tube defects, data for women and men now
 Vit B12 (cyanocobalamin) – 1-2000 mcg for
pernicious anemia (PO daily or IM monthly)
 Vit C – Iron absorption
Vitamins – Fat soluble
 Fat soluble vitamins (A, E, D, K)
 Low fat diets, malnutrition, alcoholism


20g of dietary fat required daily to ensure adequate levels of fat soluble
vitamins
Vit D – Osteoporosis
& Cancer prevention
Women
on high-dose vitamin D supplementation
(1100IU/day) had a lower risk of all cancers vs.
placebo


(Lappe et al. Am J Clin Nutr (2007):85;1586-1891)
Vit K – 500mcg qd - reduction in INR variability

(Kamali, F. et al. Blood. 2007 Mar 15;109(6):2419-23.)
Minerals
 Calcium:
 Osteoporosis: >1000mg/day
 Iron (Fe):
 Pregnancy: increase Fe needs in 2nd/3rd trimesters
(RDA = 27mg/day)
 Fe-deficiency anemia - Treatment: 150-200mg ele
Fe/day; Prophylaxis: 60-100mg ele Fe/day
Fe
Gluconate 300mg
= 35mg ele Fe;
Fe Sulfate 300mg = 65mg ele Fe;
Fe Fumarate 300mg
= 100mg ele Fe
Anti-acids
Anti-acids
Buffers
Mechanism of Action: Raise gastric pH
 Duration: 0.5 - 3 hours
 N.B. Drug interactions – antibiotics, levothyroxine
 Advantages: fast action, easy availability

Anti-acids - Buffers
 Calcium carbonate (TUMS®, Rolaids®)
Most potent; chew 1-3 tabs prn
 Side effects: Constipation

 Sodium bicarb (Alka-Seltzer®)
Side effects: flatulence, belching.
 Contraindicated in CHF, edema, renal dysfunction

 Mg/Al hydroxide (Gelusil®, Maalox liquid®)
Chew 2-4 tabs QID between meals and at hs
 Contraindicated in CKD, ARF

 Alginic Acid (Gaviscon®):

MOA: Forms a foam layer on top of gastric contents to protect
esophageal mucosa (in combo with traditional buffers)

2-4 tsps QID pc or at hs to max 16 tsps/day
Anti-acids
•
H2 Receptor Antagonists (Zantac® / Pepcid®):




Effective in treatment/prevention of mild-moderate GERD
MOA: Competitively inhibit H2 receptors on parietal cells decreasing
gastric acid secretion
Onset: 30-90min, Duration: 9 hours
Ranitidine (Zantac®) – 75mg to 150mg BID


N.B. 150mg tab was Rx strength!
Famotidine (Pepcid AC®) – 10-20mg BID

N.B. 20mg tab – Rx strength!
Anti-acids – Take Home
 Step-up therapy vs Step-down therapy
Step-up: start with simple buffers, step-up to H2RAs; consider Rx
PPI’s if not effective or chronic use.
 Step-down: start with H2RA – get immediate relief, then trial
lowest effective dose, or step down to buffer antacids

 Always obtain PMHx – assess for contraindications!
 Calcium carbonate – safest bet
 Ensure no drug interactions with cations
 (Al3+, Mg2+, Ca2+, Fe)
 Refer chronic users – risk of malignancy
Laxatives
Laxatives
 Emollients/Lubricants: “All mush, no push”
 Allow water and fat to penetrate fecal mass
 Docusate sodium (Colace®, Soflax®)
 Mineral oil (Lansoyl®)
Not recommended in children <1 year, bedridden pts, GERD  aspiration
risk (lipoid pneumonitis)
 Not recommended for long-term use (risk of fat soluble vitamin malabsorption)


?trial vegetable oil
 Bulk-Forming Agents: Psyllium (Metamucil®)
 Most effect prevention method
 Water absorption causes distention
 Take with plenty of water, else more constipation!
Laxatives
 Osmotics:
 Draws water into colon; acidification, irritation, stretch stimulation

Eg. Lactulose, sodium phosphate (Fleet®), Magnesium hydroxide/citrate
(Milk of Magnesia®), glycerin, PEG
 Stimulants:
 Stimulate peristalsis in GI mucosa
 Preferred in narcotic-induced constipation

Eg. Senna (Senekot®), Bisacodyl (Dulcolax®), Castor Oil
Constipation
Comparison of Agents
 Pharmacological Rankings

Stimulant > osmotics > bulk > stool softeners
 Onset/Duration
 Lubricants > osmotics > stimulants > bulk = stool softeners
 Side Effects
 Stimulants > lubricants > osmotics = bulk > stool softeners
 Cost (least to most)

Bulk < stool softeners < osmotics = stimulants = lubricants
 Convenience
 Bulk > stool softeners = osmotics = stimulants = lubricants
See: http://www.clinicalgeriatrics.com/article/7346
Laxatives – Take Home
 Ensure no obstruction
 Choose simplest laxative for job at hand
 Psyllium – for prevention / maintenance
 Stimulants or Osmotics – for narcotic-induced constipation
 Emollients for hard, painful stool
Herbals & Natural Products
 Lots of them! – ask your pharmacist!
 Efficacy
 Less well researched
 Lower requirements for license to sell, but claims of efficacy
are more restricted
 Toxicity
 Lower quality control requirements
 Risk of drug interactions
 Cost – Billions spent per year
 Convenience – no Rx needed. More “natural”.
Summary
 This is not an exhaustive list
 Recommend discussion with the pharmacist, even if the
product is OTC

Even a 5 minute discussion can reveal a lot!
 Most product benefits are marketing
 Any agent within a class will do.
 Avoid combination products. Target therapy with
individual ingredients
References
 Patient Self-Care, First Edition. Canadian Pharmacists’
Association, 2002. Ottawa, Canada