1. Over the Counter (OTC) Drugs
Clinical Pharmacology Seminar
Department of Pharmacology and Toxicology,
Faculty of Pharmacy, Comenius University
Nov 2009
Vladimir Patras, PharmD, MBA
2. OTC
“Over the Counter”
Non-prescription medicines
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 dispensed by pharmacist, in some
countries sold also outside pharmacies
3. Directive 2001/83/EC
Medicinal products shall be subject to medicinal
prescription where they:
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
4. Criteria for OTC Designation
Low toxicity and low risk of serious adverse reactions
Not to mask any underlying condition or increase
resistance
Correct self-assessment of the condition
No known incorrect use
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
6. Self-medication
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
7. Consumption - Slovakia
ATC category 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
Consumption of OTC products in Slovakia by categories,
SIDC data, 2001
12. Antimycotics (Antifungal Drugs)
Skin, nails, vaginal fungal infections
Nystatine
Polyene antifungal used also in combinations
FUNGICIDIN
Imidazoles
inhibition of ergosterol (component of fungal cell membrane) synthesis
Clotrimazole – CANESTEN, CANDIBENE
Ketoconazole – NIZORAL
Others: Miconazole, Bifonazole, Oxiconazole
Allylamines
Terbinafine - LAMISIL
13. Disinfection, Antiseptics and
Antibiotics
Wounds/skin disinfiction
Benzalkonium – DETTOL
Carbethopendecinium bromide – SEPTONEX (aer deo)
Antiseptics for oral use
Amylmetacresol, dichlorbenzyl alcohol – STREPSILS, NEO-ANGIN
Chlorhexidine – SEPTOFORT, DRILL
Antibiotics
Fusafungine – the only OTC antibiotic
Used as spray for treatment of nasal and throat infection
BIOPAROX
14. Nasal Preparations (Decongestants)
Applied in nasal spray/drops to relieve nasal
congestion in rhinitis
Vasoconstriction of blood vessels within the nasal
cavity
Should not be taken longer than 3 days in a row
Xylometazoline – OLYNTH
Oxymetazoline – NASIVIN
Tramazoline – MUCONASAL PLUS
Nafazoline – SANORIN
15. Allergies
Anihistamines
H1 antagonists
Often used to relieve allergic rhinitis (hay fever). Neither loratadine nor
cetirizine are causing sedation
Loratadine
CLARITINE
Cetirizine
ZODAC, ZYRTEC, CETIRIZINE-SANDOZ
Corticosteroids
Beclometazone
OTC products as nasal spray
BECLOMET NASAL AQUA
17. Analgesics (painkillers) and
Antipyretics
Major classes
Paracetamol
Salicylates
Non-steroidal anti-inflammatory drugs
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
18. Paracetamol
Most widely used analgesic in the world, lacks anti-inflammatory properties
Mechanism of action is disputed – COX 3 inhibition in brain (?)
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
19. Acetylsalicylic Acid (ASA)
Most common salicylate is acetylsalicylic acid (ASA), others are
salycilamide, diflunisal
Irreversible cycloooxygenase (COX) inhibition > suppression of
production of prostaglandins and tromboxanes (inflammation
inhibitors)
Common side effects are gastrointestinal bleeding, ulcers and tinnitus
Not used in children due to risk of Reye`s syndrome
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
20. Non-Steroidal Anti-Inflammatory Drugs (NSAIDs)
Ibuprofen
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
Pain in rheumatic conditions, marketed as relieve in pain of teeth
ALEVE, NALGESIN S
Diclofenac
Treatment of pain of various origin – most commonly in rheumatism. It is
possible to use antipyretic effects but other substances are preferred in fever
Beside oral administration topical use is common
VOLTAREN ACTIGO, VOLTAREN EMULGEL, VERAL, DICLOBENE
21. 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
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
Glycosaminoglycan used in ointments/gels in oedemas and bruises.
Anticoagulant effects
LIOTON, HEPAROID
22. Cough Medicines
Pharmacotherapy depends on type of cough
Productive – mucolytics
Non-productive – antitussics
− Opioid
− 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
23. Antitussics
Opioid
Dextromorphan
Used in combinationS with other substances such as pseudoephedrine,
paracetamol
COLDREX NITE, PARALEN PLUS
Non-opioid
Butamirate
Used as drops or sirup, most common cough suppresant
STOPTUSSIN, TUSSIN, SINECOD
Diphenhydramine
Antihystamine with antitussic (sedative, anticholinergic and antiemetic)
effects, drawsiness is common side effect
BENADRYL N
24. Mucolytic Agents
Guaifenesin
ROBITUSSIN EXPECTORANS
Acetylcysteine
Potent mucolytic agent, antioxidative effect
SOLMUCOL
Ambroxol
Common mucolytic used as sirup or tablets
MUCOSOLVAN, AMBROBENE
Bromhexine
Metabolizes to ambroxol
BROMHEXIN, BRONCHOSAN
25. Contraception
Emergency (postcoital) contraception
Levonorgestrel in 1.5 mg dose
Estimated effectiveness is 84 %
ESCAPELLE
Local contraception – spremicides
Not efficient enough alone – should be complemented with other
form of contraception (barrier contraception)
Nonoxynol – PATENTEX OVAL N
Benzalkonium chloride – PHARMATEX
26. Psychoactive OTC Preparations
Sedatives
Guaifenesin – moderate sedative effect - GUAJACURAN
Valerian, Humulus and Lemon balm extracts
Antidepressants
St. John wort – multiple drug interaction through cytochrome P450 induction
Nootropics
Pirecetam – NOOTROPIL, PIRACETAM, OIKAMID
Lecithin – phosphatidylcholine naturraly occuring in body with presumed
nootropic effects
27. Vitamin and Mineral Supplements
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
28. Where to Find Information
Books
V. Foltán: Voľnopredajné lieky, 2002
Online Databases
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
Association of the European Self-Medication Industry: http://www.aesgp.be