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

5. Switching
Switching = Move from prescriptional category into 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

8. Gastric Acidity and Gastroesophageal
Reflux Disease
Antacids

Buffering gastric acid > raising acidity

Aluminium hydroxide - MAALOX

Calcium carbonate - TUMS
H2 antagonists

Decrease acid production

Ranitidine – ZANTAC, RANISAN

Famotidine – FAMOTIDIN, QUAMATEL

9. Exocrine Pancreatic Insufficiency
Takasidase

Purified fungal (Aspergillus oryzae) enzymes

Digestion of oligosaccharides and
polysaccharides

ORENZYME
Purified animal pancreatin

PANGROL, PANZYTRAT, KREON

10. Constipation
Lactulose

Disaccharide that draw water into bowel – osmotic action

DUPHALAC
Bisacodyl

Acts by irritating of colon

BISAKODYL-K, FENOLAX
Sodium picosulfate

GUTTALAX, REGULAX

11. Diarrhea
Cloroxin, nifuroxazid

Antibacterial effects - used in infectious diarrhea including traveler`s diarrhea

ENDIARON
Loperamide

μ opioid receptor agonist – decreasing smooth muscles motility

IMODIUM
Intestinal Adsorbents – bind toxins in gastrointestinal tract

Diosmectite – SMECTA

Activated carbon - CARBOCIT, CARBOSORB

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

16. Vasoprotectives
Bioflavonoinds

Troxerutin – CILKANOL, VENORUTON
Calcium dobesilate – DANIUM
Aescin

Saponine isolated from the horse chesnut (Aesculus
hippocastanum)

Induction of endothelial nitric oxide synthesis

AESCIN, YELLON

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

29. Thank You For Your Attention !