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Bey-OTC-copy_Layout 1 11-03-24 2:12 PM Page 1 BEYOND THEBASICS
Over-the-counter Drugs
What are over-the-counter drugs?
BEYOND BASICS
BEYOND BASIC
Over-the-counter drugs are medications sold directly to consumers through pharmacies, grocery andconvenience stores without a prescription. The availability of remedies is as ubiquitous as the conditions OVER-THE-COUNTER
for which consumers may seek assistance and are offered in the form of pharmaceutically producedand naturally occurring (herbal) products. Over-the-counter formulations available in Canada have been deemed safe for public use as directed by the manufacturer for the specific requirement of conditions identified; however, some of thesedrugs have abuse potential.
The most significant potential for abuse exists in medications containing the following drug classes:
• dissociative substances and sedatives:1
– dimenhydrinate: an antiemetic available in Gravol®. – diphenhydramine: available in antihistamine medications, such as Benadryl®, and sleep-aids, – dextromethorphan (DXM or DM): the active cough suppressant in most over-the-counter cough and cold remedies, such as Robitussin®, Vicks Nyquil®, Vicks Formula 44® and Coricidin®.
• stimulants:1
– ephedra, ephedrine and pseudoephedrine: nasal decongestants in products such as Robitussin®. While pseudoephedrine is not generally a drug of choice for recreational purposes, it does cause a
rapid heart rate, high blood pressure and an excitable, hyperactive feeling. This is a state that has
attracted use by some body builders to obtain a “pumped” feeling prior to competition. Other athletes
abuse this drug for its ability to enhance energy and aggression. People may also use pseudoephedrine
for its ephedra-like effects in an attempt to lose weight. Of significant concern is this drug’s use in the
manufacture of methamphetamine.2
Additional drug classes have the potential for abuse or dependence in terms of seeking a euphoricstate, attaining weight loss, obtaining a revved up feeling or managing pain. These are: dietary supplements and diet aids; stomach preparations; laxatives; steroids; analgesics, including acetaminophen,ibuprofen and acetylsalicylic acid (ASA); and herbal supplements.
Medical Use
the ease with which they can be obtained and therelatively low cost associated with purchasing them.
Over-the-counter medications are available for any number of symptoms a person may be The research suggests young people, primarily experiencing, including nausea and vomiting, teens, are most likely to abuse these easily cough, cold, allergies, insomnia, constipation, accessed drugs. This is supported by a proliferation diarrhea, mild pain and weight issues.
of websites targeting teens with the intent to provide information about which over-the-counter These medications are intended for relatively drugs (among others) will produce the best high, minor, self-limiting conditions that can be safely how much of the drug to take, cautions they should managed without a diagnosis by a doctor or other consider and how to do so without getting caught (identification of side effects they will need to hide).
Prevalence of Use 3,4
According to the U.S. government’s NationalInstitute on Drug Abuse website, a survey Data specific to use and abuse of over-the-counter conducted in 2008 of children in grades 8, 10 drugs is limited in Canada and in the United States; and 12 revealed that 3.6 % of 8th grade students, however, it is generally understood abuse of these 5.3% of 10th grade students and 5.5 % of 12th drugs is a growing concern. This is due, in part, to www.afm.mb.ca
Bey-OTC-copy_Layout 1 11-03-24 2:12 PM Page 2 grade students had used cough medicine containing Short-term Effects
DXM in the past year to get high.3
At recommended dosages, medications containing Other groups at risk of abusing over-the-counter dimenhydrinate and/or diphenhydramine or drugs, particularly dimenhydrinate, appear to be dextromethorphan may cause an individual to feel individuals with a history of a psychiatric disorders, drowsy, dizzy and experience blurred vision. At this such as schizophrenia, depression, substance level, concentration and motor coordination may abuse and personality disorders. A significant also be impaired. An individual may experience challenge is the difficulty in identifying the chronic side effects that include dry mouth, ringing consumption of dimenhydrinate because symptoms in the ears, tremors, excitation and nervousness.
of the dependence resemble the symptoms of An individual may also experience feelings of some psychiatric disorders.4
well-being, relaxation and euphoria.8
Pharmacokinetics
These same medications, when taken in excess of recommended dosages (generally a package Over-the-counter drugs are provided in a variety at a time by abusers), may manifest symptoms of of formulations, including liquids, tablets or gel sluggishness, paranoia, agitation, memory loss, capsules. To experience a “high,” an individual increased blood pressure and heart rate, and must generally consume excessive amounts of the difficulty swallowing or speaking.8
drug. For example, abusers of dimenhydrinate maytake as many as 16 tablets, equivalent to 800 mg Misuse may also result in dissociation and of dimenhydrinate, as this is understood to be hallucinations. Misuse of dextromethorphan creates the standard dose for a “high.” Dimenhydrinate both depressant and mildly hallucinogenic effects is a combination of diphenhydramine and the that have been reported as “plateaus.” Plateaus methylxanthine, 8-chlorotheophylline. Many range from mild stimulation with distorted visual researchers suggest diphenhydramine, the perceptions to complete dissociation from the antihistaminergic component of dimenhydrinate, user’s body at high doses.3,9
is responsible for the reinforcing effect of the drug.4
When an individual ingests dosages in excess of Diphenhydramine, readily absorbed through the 1250 mg (25 tablets) of dimenhydrinate on a single intestinal tract, is widely distributed throughout the occasion, confusion and violence can result.4
body and easily crosses the blood-brain barrier.5
Initially, short-term use of ephedra, ephedrine Dextromethorphan is rapidly absorbed from or pseudoephedrine will dilate the bronchial the gastrointestinal tract, where it enters the tubes, increase blood pressure and heart rate, bloodstream and crosses the blood-brain barrier.5
boost energy and suppress appetite. An individualmight also experience sleeplessness, restlessness, Ephedra alkaloids are well absorbed in the irritability, headache, nausea, vomiting and urinary intestine.6
disorders.10
Pharmacodynamics
Many of the over-the-counter preparations canhave significantly more serious side effects when Dimenhydrinate is an antiemetic associated with antagonism of the H1 histamine receptor.4
Diphenhydramine, the most likely active
Long-term Effects
component of dimenhydrinate, is a competitiveantagonist at the H1 histamine receptor in both Sleep aids containing diphenhydramine that the peripheral and central nervous systems (CNS).
are abused repeatedly can result in narcolepsy, or Antagonism of CNS H1 receptors account for its a disruption of regular sleep patterns.11 Daytime
sedative properties.4
drowsiness, psychomotor impairment and learningimpairment are known to occur with chronic At high doses, it has been suggested that dextromethorphan acts as a glutamate and NMDA
antagonist9 and affects similar sites in the brain
Excessive use of dimenhydrinate (Gravol® as ketamine and phencyclidine (PCP).3,5
specifically) over an extended period of time isknown to create problems for the user that The major alkaloids in ephedra, ephedrine include depression, confusion, loss of energy, and pseudoephedrine are non-selective sympath- vomiting, urine retention and difficulty thinking omimetic agents that stimulate both alpha- and and socializing.8 More recently, reports have
beta-receptors.6
emerged of dimenhydrinate abuse masquerading
as psychiatric disorders (primarily depression that
is often resistant to treatment) among adolescents.4
Extended use of ephedrine can lead to toleranceand dependence.
Bey-OTC-copy_Layout 1 11-03-24 2:12 PM Page 3 Toxic Effects
In Manitoba, certain formulations containing Class IIIdrugs must be physically located close to the Dimenhydrinate taken at extreme levels resulting pharmacist to ensure appropriate and considered in overdose can manifest as confusion, irrational supervision of the purchase of these formulations.15
behaviour, loss of muscle coordination, high feverand convulsions. As well, serious heart and Certain pharmacies in Manitoba have made the breathing issues may occur and can be followed decision to place specific products from Class III by coma. Children will generally experience these drugs behind the counter despite there not being symptoms at lower doses than an adult. Overdoses a requirement to do so. This may occur when the can be fatal.8
demographic profile of their customer base indicates potential for misuse of these products.
Dextromethorphan, when combined with decongestants (which is often the case in cold Other products are voluntarily placed behind the medications), has on rare occasions caused hypoxic counter to ensure closer monitoring of their use brain damage as a result of severe respiratory depression and a lack of oxygen to the brain.3
Risks & Other Harms
Dextromethorphan-based cough remedies containother ingredients (i.e. acetaminophen, Tylenol®) Abusers who inject the drug expose themselves that, if used excessively, can cause serious health to additional risks, including contracting human effects, including liver damage.12
immunodeficiency virus (HIV), hepatitis B and C
and other blood-borne viruses.8
Ephedrine, caffeine and phenylpropanolamine arejust some of the dangerous substances found in As is the case in any abuse of licit and illicit diet pills. All of these substances act as stimulants drugs, there are potential adverse consequences to the central nervous system and can have serious related to the law, a person’s financial situation, and potentially fatal side effects.13
family relationships, and generally putting oneselfat risk by participating in unsafe behaviours while Ephedrine’s toxic effects include hypertension under the influence of the drug.5
and tachyarrhythmias and potentially death. This medication is particularly dangerous when Pregnancy & Lactation 16
combined with heart drugs, such as digitalis,blood pressure medication, monoamine oxidase Cough medicines and decongestants: The vast (MAO) inhibitors and ergot-based migraine drugs.
majority of research relevant to over-the-counter Symptoms of overdose include severe sweating, drugs as they relate to pregnancy is in terms of enlarged pupils, spasms and increased body risk of malformations. Generally speaking, if temperature.10
women need to use a very specific medication totreat cold symptoms during pregnancy, there is no Tolerance and Dependence
significant evidence of harm to the fetus; however,any use of over-the counter medications should be Chronic use of dimenhydrinate can result in of limited use for a short duration of time.
tolerance and dependence. Tolerance will occur Consultation with a health care professional should within only a few days.8
precede use of any medication during pregnancy Chronic use of ephedrine can lead to tolerance and dependence.10
Use of any over-the-counter medication that is in Withdrawal
excess of the recommended dosage or is used foran extended period of time has the potential to Dimenhydrinate (Gravol®) users who have been cause difficulties and should be avoided without abusing the drug or using for an extended period the specific recommendation of a doctor or other of time will experience a range of withdrawal symptoms that include excitability, agitation,weakness, clumsiness, discomfort, poor appetite, Interventions
stomach cramps, nausea and hostility.4,8
When drug abuse involves over-the-counter Legal Issues
medications, health care professionals such asdoctors and pharmacists may be in an ideal position In Canada, over-the-counter drugs are regulated to provide information and referrals for treatment.
by Good Manufacturing Process (GMP) to ensure the overall quality and consistency of marketed management tool for all patients. A comprehensive drug products. Health Canada is in the process medical history puts physicians and other health of adopting a more extensive approach to care professionals in the best position to determine management of over-the-counter drugs that appropriate clinical interventions.1
include active pharmaceutical ingredients. Thisapproach will hold manufacturers accountable for specific drug formulations and the resulting
proprietary mixtures.14
Bey-OTC-copy_Layout 1 11-03-24 2:12 PM Page 4 A rigorous approach to determining a person’s Substance Use & Mental Health
relationship to all drug classes involves: • Substance use and mental health problems can • asking questions at the initial and subsequent often occur together. This is commonly referred appointments about prescription, over-the- counter, herbal and illicit drug use regardless of • Substance use may increase the risk of mental a presumption someone misusing drugs might • People with mental health problems are at higher • providing appropriate containers where risk of developing substance abuse problems: patients can dispose of unused medications, – Sometimes they use alcohol and other drugs both prescription and over-the-counter varieties.
in an attempt to relieve themselves from • referring patients who have drug misuse issues to appropriate programs.1
– For most people alcohol and other substance Treatment can involve detoxification, including rapid detoxification techniques, and traditional behaviour-oriented therapies, such as individualcounselling, group or family therapy, contingency Remember: A person’s experience with any drug
management and cognitive-behavioural therapies.2
can vary. Here are a few of the many things thatmay affect the experience: the amount and Any treatment strategy used with those abusing strength of the drug taken, the setting, a person’s over-the-counter drugs must take into account mood and expectations before taking the drug, the specific needs of the individual, as well as the gender, overall health, past experience with that particular substance being abused. This principle drug and whether more than one drug is being is the same for treatment of those who abuse both used at the same time. Using alcohol and other drugs at the same time can also be dangerous.
Sources
10. Drug Abuse Help website. Ephedra. Available at http://www.
drugabusehelp.com/drugs/ephedra/ 1. Lessenger, J. E. & Feinberg, S.D. Clinical Review – Abuse ofPrescription and Over-the-counter Medications doi: 10.3122/jabfm, 11. Teen Drug Abuse website. Over-the-counter Drug Abuse. Available at http://www.teendrugabuse.us/over_the_counter_drug_abuse.html 2. eMedtv. Abuse of Pseudophedrine, 2009. Available at http:// 12. Indiana University, Indiana Prevention Resource Centre website.
cold.emedtv.com/pseudoephedrine/abuse-of-pseudoephedrine.html DXM PowerPoint Presentation, 2005. Available at http://www.drugs.
indiana.edu/drug-info-dxm.html 3. National Institute on Drug Abuse. InfoFacts – Prescription and Over-the-counter Medications, 2009. Available at http://www.nida.nih.gov/ 13. National Center on Addiction and Substance Use at Columbia University (CASA). Formative Years: Pathways to Substance AbuseAmong Girls and Young Women Ages 8-22, New York, NY, 2003.
4. BC Mental Health and Addiction Services. For Your Inpharmation Available at http://www.casacolumbia.org/articlefiles/380-Formative_ Pharmacy Newsletter, 2003. Available at http://www.bcmhas.ca/NR/ rdonlyres/8BFC92AF-4023-4D5F-BF51-38DF2B13F531/12668/2003_Mar_Dimenhydrinate.pdf 14. Health Canada. Consultation on the Creation of a RegulatoryFramework for the Implementation of Good Manufacturing Practices 5. National Highway Traffic Safety Administration. Fact Sheet – for Active Pharmaceutical Ingredients (API), 2009. Available at Diphenhydramine and Fact Sheet – Dextromethorphan, 2004.
http://hc-sc.gc.ca/dhp-mps/consultation/compli-conform/ Available at http://www.nhtsa.dot.gov/Peopleinjury/research/ 15. National Association of Pharmacy Regulatory Authorities (NAPRA) 6. Memorial Sloan-Kettering Cancer Center. Ephedra, 2009. Available website. Supplemental Standards of Practice for Schedule II and III at http://www.mskcc.org/mskcc/html/69213.cfm Drugs, 2005. Available at http://napra.ca 7. Pharmacodynamic Basis of Herbal Medicine, 2nd Edition, Manuchair 16. Hospital for Sick Children, MOTHERRISK website. Treating the S. Ebadi, CRC Press, 2 edition (September 6, 2006), p. 313.
Common Cold During Pregnancy, 2008. Available at http://www.
8. Alberta Health Services. The ABCs – Over the Counter Drugs, 2007.
motherisk.org/prof/updatesDetail.jsp?content_id=881 Available at http://www.aadac.com/87_427.asp. The ABCs – Gravol,2007. Available at http://www.aadac.com/87_433.asp 9. Parents – The Anti Drug website. Dextromethorphan. Available athttp://www.theantidrug.com/drug-information/otc-prescription-drug-abuse/over-the-counter-drug-abuse/dextromethorphan.aspx The Addictions Foundation of Manitoba (AFM) offers a broad range of prevention and treatment services for alcohol, other drugs and gambling. These are designed to meet the needs of all Manitobans and include harm reduction and abstinence-based programs. For more information, contact your local AFM office or visit our website: www.afm.mb.ca. AFM Disclaimer: This information is not intended as a substitute for professional advice. Every effort
has been made to ensure that the information was accurate at the time of publication. Permission to reproduce is granted by AFM. If you wish to order
multiple copies of this or other topics in The Beyond the Basics Series,
please contact AFM Library at 204-944-6233 or library@afm.mb.ca.

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