Over the Counter Drugs (OTC)

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

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 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

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

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

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

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 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 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 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

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

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 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 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

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

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.

Naproxen

•       Pain in rheumatic conditions, marketed as relieve in pain of teeth

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

Joint, Connective Tissue and Rheumatism OTC preparations

Other NSAIDs - Indometacin, Ketoprofen, Nimesulide(COX-2)‏

Combination of enzymes such as trypsin, bromelaine, papainhas 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

–      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 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

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 %

•       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 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

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

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