Over the Counter OTC Drugs Clinical Pharmacology Seminar

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Over the Counter (OTC) Drugs Clinical Pharmacology Seminar Department of Pharmacology and Toxicology, Faculty

Over the Counter (OTC) Drugs Clinical Pharmacology Seminar Department of Pharmacology and Toxicology, Faculty of Pharmacy Vladimir Patras, Pharm. D, MBA

OTC – What is it? “Over the Counter” Non-prescription medicines Medicinal products marketed as

OTC – What is it? “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 dispenced by pharmacist, in some countries sold also outside pharmacies

Directive 2001/83/EC Medicinal products shall be subject to medicinal prescription where they: Are likely

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

Criteria for OTC Designation Low toxicity and low risk of serious adverse reactions Not

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

Switching = Move from prescriptional category into OTC

Switching = Move from prescriptional category into OTC

Self-medication Treatment of common health problems with medicines especially designed and labeled for use

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

Consumption - Slovakia Consumption of OTC products in Slovakia by categories, SIDC data, 2001

Consumption - Slovakia Consumption of OTC products in Slovakia by categories, SIDC data, 2001

Gastric Acidity and Gastroesophageal Reflux Disease Antacids Buffering gastric acid > raising acidity Aluminium

Gastric Acidity and Gastroesophageal Reflux Disease Antacids Buffering gastric acid > raising acidity Aluminium hydroxide - MAALOX Calcium carbonate - TUMS H 2 antagonists Decrease acid production Ranitidine – ZANTAC, RANISAN Famotidine – FAMOTIDIN, QUAMATEL

Exocrine Pancreatic Insufficiency Takasidase Purified fungal (Aspergillus oryzae) enzymes Digestion of oligosaccharides and polysaccharides

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

Constipation Lactulose Disaccharide that draw water into bowel – osmotic action DUPHALAC Bisacodyl Acts

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

Diarrhea Cloroxin, nifuroxazid Antibacterial effects - used in infectious diarrhea including traveler`s diarrhea ENDIARON

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

Antimycotics (Antifungal Drugs) Skin, nails, vaginal fungal infections Nystatine Polyene antifungal used also in

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

Disinfection, Antiseptics and Antibiotics Wounds/skin disinfiction Benzalkonium – DETTOL Carbethopendecinium bromide – SEPTONEX (aer

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

Nasal Preparations (Decongestants) Applied in nasal spray/drops to relieve nasal congestion in rhinitis Vasoconstriction

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

Allergies Anihistamines H 1 antagonists Often used to relieve allergic rhinitis (hay fever). Neither

Allergies Anihistamines H 1 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

Vasoprotectives Bioflavonoinds Troxerutin – CILKANOL, VENORUTON Calcium dobesilate – DANIUM Aescin Saponine isolated from

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

Analgesics (painkillers) and antipyretics Major classes Paracetamol Salicylates Non-steroidal anti-inflammatory drugs Most drugs of

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

Paracetamol Most widely used analgesic in the world, lacks anti-inflammatory properties Mechanism of action

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 HOT REM, ATARALGIN, VALETOL

Acetylsalicylic Acid (ASA) Most common salicylate is acetylsalicylic acid (ASA), others are salycilamide, diflunisal

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

Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) Ibuprofen Indications include arthritis, dysmenorrhea, fever, migaine and other conditions

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

Joint, Connective Tissue and Rheumatism OTC preparations Other NSAIDs - Indometacin, Ketoprofen, Nimesulide (COX-2)

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

Cough Medicines Pharmacotherapy depends on type of cough Productive – mucolytics Non-productive – antitussics

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

Antitussics Opioid Dextromorphan Used in combination. S with other substances such as pseudoephedrine, paracetamol

Antitussics Opioid Dextromorphan Used in combination. S with other substances such as pseudoephedrine, paracetamol COLDREX NITE, PARALEN PLUS Non-opioid Butamirate Used as drops or sirup, most common cough suppresant STOPTUSSIN, SINECOD Diphenhydramine Antihystamine with antitussic (sedative, anticholinergic and antiemetic) effects, drawsiness is common side effect BENADRYL N

Mucolytic Agents Guaifenesin ROBITUSSIN EXPECTORANS Acetylcysteine Potent mucolytic agent, antioxidative effect SOLMUCOL Ambroxol Common

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

Contraception Emergency (postcoital) contraception Levonorgestrel in 1. 5 mg dose Estimated effectiveness is 84

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

Psychoactive OTC preparations Sedatives Guaifenesin – moderate sedative effect - GUAJACURAN Valerian, Humulus and

Psychoactive OTC preparations Sedatives Guaifenesin – moderate sedative effect - GUAJACURAN Valerian, Humulus and Lemon balm extracts Antidepressants St. John wort – multiple drug interaction through cytochrome P 450 induction Nootropics Pirecetam – NOOTROPIL, PIRACETAM, OIKAMID Lecithin – phosphatidylcholine naturraly occuring in body with presumed nootropic effects

Vitamin and Mineral Supplements Many preparations are on the market, some of them are

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

Where to find information Books V. Foltán: Voľnopredajné lieky, 2002 Online Databases Nobel. PLUS

Where to find information Books V. Foltán: Voľnopredajné lieky, 2002 Online Databases Nobel. PLUS – Slovak database of pharmaceutical products: http: //www. nobelplus. sk/ Medline. Plus – 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

Thank You For Your Attention ! This presentation is published at http: //vpatras. blogspot.

Thank You For Your Attention ! This presentation is published at http: //vpatras. blogspot. com