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Over the Counter (OTC) Drugs
Clinical Pharmacology Seminar
Department of Pharmacology and Toxicology,
Faculty of Pharmacy
Vladimir Patras, PharmD, MBA
OTC – What is it?

“Over the Counter”

Non-prescription medicines
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Medicinal products marketed as drugs - regulatory
approval (marketing authorization) is needed, which is
issued on base of proof of safety and efficacy (legal or
regulatory meaning)
In broader sense all non-prescriptional medicines
including traditional herbal medicines or nutritional
supplements (pharmaceutical care meaning)
Need not to be dispenced by pharmacist, in some
countries sold also outside pharmacies
Directive 2001/83/EC
Medicinal products shall be subject to medicinal
prescription where they:
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Are likely to present danger, even when used
correctly
Are frequently and to very wide extent used
incorrectly
Contain substances which require further
investigation
Are to be administered parenterally
Non-prescription medicines when none of these
criteria apply
Criteria for OTC Designation


Low toxicity and low risk of serious adverse reactions
Not to mask any underlying condition or increase
resistance
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Correct self-assessment of the condition
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No known incorrect use
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Risk to public health limited in case of misuse

Drugs are usually approved as prescription only first
and just after they prove safety in clinical use they are
recategorized as OTC
Switching
Switching = Move from prescriptional category into OTC
Self-medication
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Treatment of common health problems with
medicines especially designed and labeled for
use without medical supervision and approved
as safe and effective for such use
Desire of people to take responsibility for their
own health and to reduce health expenditure
Importance of patient education,
pharmaceutical care
Move toward self-medication has support of
governments/regulatory agencies
Consumption - Slovakia
Packages Value in
sold (in
millions of
thousands) Sk
Analgesics
14044
219158
Vitamins
8091
286327
Cough and cold preparations
4179
136299
Antiinflamatory/antirheumatic products
4143
159788
Antithrombotic agents
3092
41998
Phytopharmaca
2725
87566
Nasal preparations
2716
106153
Mineral supplements
2534
149027
Vasoprotectives
2143
102485
Topical products for joint and muscle pain
1736
94591
Digestives and enzymes
1297
150105
ATC category
Consumption of OTC products in Slovakia by categories,
SIDC data, 2001
Gastric Acidity and Gastroesophageal
Reflux Disease
Antacids
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Buffering gastric acid > raising acidity
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Aluminium hydroxide - MAALOX
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Calcium carbonate - TUMS
H2 antagonists
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Decrease acid production
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Ranitidine – ZANTAC, RANISAN
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Famotidine – FAMOTIDIN, QUAMATEL
Exocrine Pancreatic Insufficiency
Takasidase
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Purified fungal (Aspergillus oryzae) enzymes
Digestion of oligosaccharides and
polysaccharides
ORENZYME
Purified animal pancreatin
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PANGROL, PANZYTRAT, KREON
Constipation
Lactulose
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Disaccharide that draw water into bowel – osmotic action
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DUPHALAC
Bisacodyl
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Acts by irritating of colon
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BISAKODYL-K, FENOLAX
Sodium picosulfate
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GUTTALAX, REGULAX
Diarrhea
Cloroxin, nifuroxazid
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Antibacterial effects - used in infectious diarrhea including traveler`s diarrhea
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ENDIARON
Loperamide
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μ opioid receptor agonist – decreasing smooth muscles motility
IMODIUM
Intestinal Adsorbents – bind toxins in gastrointestinal tract
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Diosmectite – SMECTA
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Activated carbon - CARBOCIT, CARBOSORB
Antimycotics (Antifungal Drugs)
Skin, nails, vaginal fungal infections
Nystatine
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Polyene antifungal used also in combinations
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FUNGICIDIN
Imidazoles
inhibition of ergosterol (component of fungal cell membrane) synthesis
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Clotrimazole – CANESTEN, CANDIBENE
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Ketoconazole – NIZORAL
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Others: Miconazole, Bifonazole, Oxiconazole
Allylamines
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Terbinafine - LAMISIL
Disinfection, Antiseptics and
Antibiotics
Wounds/skin disinfiction
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Benzalkonium – DETTOL
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Carbethopendecinium bromide – SEPTONEX (aer deo)
Antiseptics for oral use
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Amylmetacresol, dichlorbenzyl alcohol – STREPSILS, NEO-ANGIN
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Chlorhexidine – SEPTOFORT, DRILL
Antibiotics
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Fusafungine – the only OTC antibiotic
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Used as spray for treatment of nasal and throat infection
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BIOPAROX
Nasal Preparations (Decongestants)
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Applied in nasal spray/drops to relieve nasal
congestion in rhinitis
Vasoconstriction of blood vessels within the nasal
cavity
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Should not be taken longer than 3 days in a row
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Xylometazoline – OLYNTH
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Oxymetazoline – NASIVIN
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Tramazoline – MUCONASAL PLUS
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Nafazoline – SANORIN
Allergies
Anihistamines
H1 antagonists
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Often used to relieve allergic rhinitis (hay fever). Neither loratadine nor
cetirizine are causing sedation
Loratadine
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CLARITINE
Cetirizine
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ZODAC, ZYRTEC, CETIRIZINE-SANDOZ
Corticosteroids
Beclometazone
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OTC products as nasal spray
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BECLOMET NASAL AQUA
Vasoprotectives
Bioflavonoinds
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Troxerutin – CILKANOL, VENORUTON
Calcium dobesilate – DANIUM
Aescin
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Saponine isolated from the horse chesnut (Aesculus
hippocastanum)
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Induction of endothelial nitric oxide synthesis
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AESCIN, YELLON
Analgesics (painkillers) and
antipyretics
Major classes
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Paracetamol
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Salicylates
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Non-steroidal anti-inflammatory drugs
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Most drugs of this group has both anti-inflammmatory
and antipyretic effects through inhibition of
biosynthesis of prostaglandins
It is not recommended to use antypiretics in only
slightly elevated temperature
Paracetamol
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Most widely used analgesic in the world, lacks anti-inflammatory properties
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Mechanism of action is disputed – COX 3 inhibition in brain (?)
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Preferred antipyretic agent in children, no side effects in gastrointestinal
tract, is not contraindicated in pregnancy (ASA is preferred in first trimester)
Some studies suggested link between heavy paracetamol use in early
childhood and development of asthma. FDA issued Public Health Advisory
recommending use of cold and cough medicines in children under 2 years
only when necessary
Possible liver and kidney damage in case of other liver/kidney disease or
high doses
Combinations with caffeine, dimenhydrinate, phenylephrine,
pseudoephedrine, promethazine, guaifenesin, ascorbic acid
PANADOL, PANADOL EXTRA, PARALEN, COLDREX, COLDREX HOT
REM, ATARALGIN, VALETOL
Acetylsalicylic Acid (ASA)
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Most common salicylate is acetylsalicylic acid (ASA), others are
salycilamide, diflunisal
Irreversible cycloooxygenase (COX) inhibition > suppression of
production of prostaglandins and tromboxanes (inflammation
inhibitors)
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Common side effects are gastrointestinal bleeding, ulcers and tinnitus
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Not used in children due to risk of Reye`s syndrome
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May be used in first and second trimesters of pregnancy if benefit
outweighs risk
Often used in combinations with other drugs such as ascorbic acid,
caffeine, paracetamol, phenacetin
ASPIRIN, ASPIRIN-C, ASPIRIN PROTECT, ACYLPYRIN,
ACYLCOFFIN, ACIFEIN, ALKA-SELTZER, ACIFEIN
Non-Steroidal Anti-Inflammatory Drugs (NSAIDs)
Ibuprofen
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Indications include arthritis, dysmenorrhea, fever, migaine and other
conditions with involving inflammation. Investigational (clinical trials) use
include also Alzheimer and Parkinson diseases.
BRUFEN, NUROFEN, IBALGIN
Naproxen
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Pain in rheumatic conditions, marketed as relieve in pain of teeth
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ALEVE, NALGESIN S
Diclofenac
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Treatment of pain of various origin – most commonly in rheumatism. It is
possible to use antipyretic effects but other substances are preferred in fever
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Beside oral administration topical use is common
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VOLTAREN ACTIGO, VOLTAREN EMULGEL, VERAL, DICLOBENE
Joint, Connective Tissue and
Rheumatism OTC preparations
Other NSAIDs - Indometacin, Ketoprofen, Nimesulide (COX-2)
Combination of enzymes such as trypsin, bromelaine, papain has presumed
anti-inflammatory effect - WOBENZYME
Chondroitin sulfate, Glucosamine sulfate
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Often used in combination in treatment of osteoarthritis. They are
components of joint cartilage but have also anti-inflammatory effect
CONDROSULF
Antioedema local preparations - Heparin
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Glycosaminoglycan used in ointments/gels in oedemas and bruises.
Anticoagulant effects
LIOTON, HEPAROID
Cough Medicines
Pharmacotherapy depends on type of cough
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Productive – mucolytics
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Non-productive – antitussics
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Opioid
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Non-opioid
Mucolytics and antitusics shall not be used together
FDA issued public health statement promoting
cautious use of cough medicines in children under 4
years
Antitussics
Opioid
Dextromorphan
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Used in combinationS with other substances such as pseudoephedrine,
paracetamol
COLDREX NITE, PARALEN PLUS
Non-opioid
Butamirate
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Used as drops or sirup, most common cough suppresant
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STOPTUSSIN, TUSSIN, SINECOD
Diphenhydramine
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Antihystamine with antitussic (sedative, anticholinergic and antiemetic)
effects, drawsiness is common side effect
BENADRYL N
Mucolytic Agents
Guaifenesin
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ROBITUSSIN EXPECTORANS
Acetylcysteine
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Potent mucolytic agent, antioxidative effect
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SOLMUCOL
Ambroxol
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Common mucolytic used as sirup or tablets
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MUCOSOLVAN, AMBROBENE
Bromhexine
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Metabolizes to ambroxol
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BROMHEXIN, BRONCHOSAN
Contraception
Emergency (postcoital) contraception
Levonorgestrel in 1.5 mg dose
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Estimated effectiveness is 84 %
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ESCAPELLE
Local contraception – spremicides
Not efficient enough alone – should be complemented with other
form of contraception (barrier contraception)
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Nonoxynol – PATENTEX OVAL N
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Benzalkonium chloride – PHARMATEX
Psychoactive OTC preparations
Sedatives
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Guaifenesin – moderate sedative effect - GUAJACURAN
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Valerian, Humulus and Lemon balm extracts
Antidepressants
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St. John wort – multiple drug interaction through cytochrome P450 induction
Nootropics
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Pirecetam – NOOTROPIL, PIRACETAM, OIKAMID
Lecithin – phosphatidylcholine naturraly occuring in body with presumed
nootropic effects
Vitamin and Mineral Supplements
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Many preparations are on the market, some of them
are marketed as drugs others as nutritional
supplements
CENTRUM, GERIAVIT PHARMATON, REVALID
Many nutritional supplements are associated with
various health claims but efficacy is not required to be
demonstrated in order to gain marketing authorization
for nutritional supplements
Where to find information
Books
V. Foltán: Voľnopredajné lieky, 2002
Online Databases
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NobelPLUS – Slovak database of pharmaceutical products:
http://www.nobelplus.sk/
MedlinePlus – service of U.S. National Library of Medicine and National
Institute of Health: http://www.nlm.nih.gov/medlineplus/druginformation.html
Industry Associations
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Association of the European Self-Medication Industry: http://www.aesgp.be
Thank You For Your Attention !
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This presentation is published at
http://vpatras.blogspot.com