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Mixin' It up - Alcohol and Legal Drugs Peter A. Kreckel, RPh. Assistant Professor of Pharmacology St. Francis University Physician Assistant Sciences • Tim Mizak • Nick Wytiaz Student Pharmacists University of Pittsburgh School of Pharmacy What is Alcohol? • Alcohol (ethyl alcohol or ethanol) is a central nervous system depressant – Rapidly absorbed from the stomach & small intestine into the bloodstream – Metabolized in the liver by enzymes – Intensity of effect on the body is directly related to the amount consumed Centers for Disease Control & Prevention: Summary Health Statistics for U.S. Adults: National Health Interview Survey, 2008. \http://www.cdc.gov/alcohol/faqs.htm#1 Alcohol Use in the U.S. • 50% of adults are regular drinkers (at least 12 drinks in the past year) - Incidence in the Northeast: 54% • 14% of adults are infrequent drinkers (1-11 drinks in the past year) Centers for Disease Control & Prevention: Summary Health Statistics for U.S. Adults: National Health Interview Survey, 2008. http://www.cdc.gov/fastats/alcohol.htm What is a Standard Drink? • Equal to 13.7 grams of pure alcohol http://myhealth.ucsd.edu/library/healthguide/en-us/images/media/medical/hw/alcohol.jpg Levels and Patterns of Drinking • Heavy drinking – For women, more than 1 drink per day on average. – For men, more than 2 drinks per day on average. • Binge drinking – For women, 4 or more drinks during a single occasion. – For men, 5 or more drinks during a single occasion. • Excessive drinking includes heavy drinking, binge drinking or both. Under Age Drinking • The 2007 Youth Risk Behavior Survey found that among high school students, during the past 30 days: – 45% drank some amount of alcohol – 26% binge drank – 11% drove after drinking alcohol – 29% rode with a driver who had been drinking alcohol Alcohol and Sex “Tequila Makes Her Clothes Fall Off” by Joe Nichols • 60% of college women who are infected with STDs, including genital herpes and AIDS, report being under the influence of alcohol at the time they had intercourse with the infected person. • As many as 70% of college students admit to having engaged in sexual activity primarily as a result of being under the influence of alcohol, or to having sex they wouldn't have had if they had been sober. • 90% of all campus rapes occur when alcohol has been used by either the assailant or the victim. Recommended Consumption • The National Institute on Alcohol Abuse and Alcoholism recommends: – Men <65: no more than 14 drinks per week, no more than 4 drinks per sitting – Women<65: no more than 7 drinks per week – Women & men > 65: no more than 7 drinks per week, no more than 3 drinks per sitting University of Michigan Comprehensive Cancer Center website: http://www.cancer.med.umich.edu Just a reminder… PURCHASE, CONSUMPTION, POSSESSION OR TRANSPORTATION OF LIQUOR OR MALT OR BREWED BEVERAGES BY A MINOR Section 6308 of the Pennsylvania Crimes Code (Title 18) • A person commits a summary offense if he/she, being less than 21 years of age, attempts to purchase, purchases, consumes, possesses or knowingly and intentionally transports any liquor or malt or brewed beverages And if you get caught…. Penalty 1 st Offense 2 nd Offense Subsequent Offenses Fine 0-$300 0-$500 0-$500 Jail 0-90 days 0-90 days 0-90 days License Suspension 90 days 1 year 2 years Why Do People React Differently to Alcohol? • Reactions to alcohol are dependent on numerous factors, including: – – – – – – – Age Gender Race or ethnicity Physical condition (weight, fitness level, etc) Amount of food consumed before drinking How quickly the alcohol was consumed Family history of alcohol problems – Use of drugs or prescription medications Centers for Disease Control & Prevention: Summary Health Statistics for U.S. Adults: National Health Interview Survey, 2008. \http://www.cdc.gov/alcohol/faqs.htm#1 Alcohol-Related Drug Interactions • 2 Types: – Pharmacokinetic- alcohol alters the metabolism or excretion of the drug or vice versa – Pharmacodynamic- additive effects of alcohol and drugs • Alcohol is metabolized in the liver by aldehyde dehydrogenase and cytochrome P450 2E1 (CYP2E1) – Infrequent drinkers: CYP2E1 metabolizes a small fraction – Chronic drinkers: have increased CYP2E1 activity (up to 10x) • Important to take into account an individual’s alcohol use patterns when looking at drug interactions Analgesics: Aspirin, NSAIDS (Advil®, Aleve®, etc.) • risk of GI hemorrhage: both aspirin and alcohol damage GI lining • Avoid alcohol/NSAIDS within 8-10 hours of heavy drinking. • Acetaminophen (Tylenol®) • Alcohol causes in Tylenol’s toxic metabolites. See liver failure. Opioids: Morphine, Methadone, Percocet®, Oxycontin®, Vicodin®, Lortab® • Both narcotics and alcohol are CNS depressants • Will see excessive CNS depression (additive effect) • Alcohol can cause dissolution of some tablets/capsules and cause absorption leading to fatal doses Sedatives/Hypnotics: • Barbiturates: see CNS depression • may absorption, AND block metabolism of barbiturates • Benzodiazepines (Valium®, Ativan®, Xanax®): alcohol may aggression • may absorption, AND block metabolism of benzodiazepines • Ambien®: depressant effects • may see risk of sleep driving Others: • Antihistamines (Chlor-Trimeton®, Benadryl®): drowsiness • Claritin® is ok • Antibiotics- Keflex®, Bactrim-DS®, Flagyl® and Tindamax®: may cause Disulfram reaction • Antipsychotics (Seroquel®, Abilify®, Geodon®): Impaired psychomotor performance • Avoid alcohol use beyond 1 or 2 drinks Treatment of AlcoholismAntabuse® • Mechanism: blocks acetaldehyde dehydrogenase – Acetaldehyde increases up to 10-fold causing: flushing, throbbing headache, respiratory difficulty, nausea, copious vomiting, sweating, thirst, chest pains, palpitations, hypotension, tachycardia, syncope • Avoid alcohol in all forms • Clinically, it reduces drinking days, but does not enhance abstinence • Compliance is THE major factor determining efficacy of disulfiram • BEST CHOICE: for a person who needs emergency help to stop drinking NOW. Treatment of Alcohol AbuseRevia® • Naltrexone (Revia®) • Mechanism: Blocks opioid receptors to reduce the pleasurable effects from alcohol. Increases abstinence days, reduces heavy drinking days and improves overall outcome. • BEST CHOICE: Abstinence from alcohol is NOT required for therapy. Helps for patients with high levels of cravings, especially in risky drinking situations. Treatment of AlcoholismCampral® • • Acamprosate (Campral®) Mechanism: reduces the anxiety & other unpleasant effects of alcohol withdrawal, balances the GABA and Glutamate neurotransmitters in the brain. • BEST CHOICE: for patients with significant liver pathology. Patients with SEVERE alcohol withdrawal symptoms. Patients able to initiate abstinence, but have difficulty in maintaining newly regained abstinence. The 12 Steps of AA: 1-4 1. We admitted we were powerless over alcohol-that our lives had become unmanageable. 2. Came to believe that a Power greater than ourselves could restore us to sanity. 3. Made a decision to turn our will and our lives over to the care of God as we understood Him. 4. Made a searching and fearless moral inventory of ourselves. A.A. World Services, Inc. The 12 Steps of AA: 5-8 5. Admitted to God, to ourselves, and to another human being the exact nature of our wrongs. 6. Were entirely ready to have God remove all these defects of character. 7. Humbly asked Him to remove our shortcomings. 8. Made a list of all persons we had harmed, and became willing to make amends to them. A.A. World Services, Inc. The 12 Steps of AA: 9-12 9. Made direct amends to such people wherever possible, except when to do so would injure them or others. 10. Continued to take personal inventory and when we were wrong promptly admitted it. 11. Sought through prayer and meditation to improve our conscious contact with God, as we understood Him, praying only for knowledge of His will for us and the power to carry that out. 12. Having had a spiritual awakening as the result of these Steps, we tried to carry this message to alcoholics, and to practice these principles in all our affairs. A.A. World Services, Inc. Dextromethorphan ABUSE • Dextromethorphan, the d-isomer of the opiate agonist levorphanol, is metabolized by the cytochrome P450 2D6 enzyme system in the liver. This metabolite, dextrorphan, has a high affinity for the excitatory amino acid receptor, the N-methyl-D-aspartate (NMDA) receptor, producing a “high.” • Symptoms following ingestion of high doses (five to ten times the normal therapeutic dose) include euphoria, an altered sense of time, paranoia, and disorientation. In addition, tactile, visual, and auditory hallucinations may occur. • The effects seen with dextromethorphan abuse are similar to those seen after phencyclidine (PCP) use, another agent which blocks NMDA receptors. EFFECTS of DXM abuse • • • • • • • • • Increased perceptual awareness Altered time perception Feelings of “floating” or dissociation of the body Visual disturbances Tactile, auditory, visual hallucinations Paranoia Disorientation and lack of coordination Slurred speech Impaired judgment and mental performance Sources for Dextromethorphan • Robitussin DM 10mg DXM + 100mg guaifenesin/ 5cc (“Roboshake”) • Delsym 30mg 30mg DXM/ 5cc (“Agent orange) (check out Urban Dictionary) • Coricidin HBP Cough and Cold: 30mg DXM + chlorpheniramine 4mg (Skittles) Dosage of DXM for ABUSE Plateau Dose (mg) Behavior effects Robitussin Delsym Coricidin DM HBP 1st 100200 200400 300600 Mild stimulation 50100ml 100200ml 150300ml 1734ml 3468ml 50100 3-7 tabs 7-14 5001500 Dissociative sedation 250750ml 83250 17-50 2nd 3rd 4th Euphoria hallucinations Distorted visual perception. Loss of coordination 10-20 DXM OVERDOSE • If ingested over 7.5mg DXM/kg should be referred to Emergency Dept • Can also overdose on antihistamines, decongestants if included in products • Serotonin syndrome if also taking: SSRI, Zyvox, tramadol: – Hyperthermia – Muscle rigidity – Myoclonus (clonic muscle twitching) – Changes in mental status and vital signs Blizzard • Concentrated Bath salts (Ivory Snow Salts) • Produces a “meth like high” when ingestedeither by eating, smoking or injecting • Causes anxiety, hallucinations & paranoia • Doesn’t show up (for now) on drug tests • Preliminary testing indicates that the active ingredients in many brands contain MDPV (3,4methylenedioxypyrovalerone) and/or mephedrone. Blizzard- MDPV source: drugs-forum.com • MDPV, 3,4-methylenedioxypyrovalerone, is an alkaloid in the pyrrolidine and ketone chemical classes. • Pharmacologically, it functions as a dopaminenorepinephrine reuptake inhibitor (NDRI) with stimulatory effects on the central nervous system and cardiovascular system. • It was first synthesized by Boehringer Ingelheim and patented in 1969, but was never marketed. MDPV appeared as a recreational drug in 2005. • Can blunt effect of increased heart rate with Propranolol • Dosage: MDPV can be taken orally, sublingually, rectally, intravenously, intramuscularly, insufflated, and inhaled. Oral doses for most users start at about 3-5 mg