Stimulants Chapter 10 Major Stimulants All major stimulants increase alertness, excitation, and euphoria; thus, these drugs are referred to as “uppers.” Schedule I (“designer” amphetamines)
Download ReportTranscript Stimulants Chapter 10 Major Stimulants All major stimulants increase alertness, excitation, and euphoria; thus, these drugs are referred to as “uppers.” Schedule I (“designer” amphetamines)
Stimulants Chapter 10 Major Stimulants All major stimulants increase alertness, excitation, and euphoria; thus, these drugs are referred to as “uppers.” Schedule I (“designer” amphetamines) Schedule II (amphetamine, cocaine, methylphenicate – Ritalin : See next Slide.. Methylphenidate (Ritalin) “Why is this medication prescribed? Methylphenidate is used as part of a treatment program to control symptoms of attention deficit hyperactivity disorder (ADHD; more difficulty focusing, controlling actions, and remaining still or quiet than other people who are the same age) in adults and children. Methylphenidate (Ritalin, Ritalin SR, Methylin, Methylin ER) is also used to treat narcolepsy (a sleep disorder that causes excessive daytime sleepiness and sudden attacks of sleep). Methylphenidate is in a class of medications called central nervous system (CNS) stimulants. It works by changing the amounts of certain natural substances in the brain.” Source - http://www.ncbi.nlm.nih.gov/pubmedhealth/PMH0000606/ Amphetamines Cause dependence due to their euphoric properties and ability to mask fatigue. Can be legally prescribed by physicians for appetite control in weight loss programs, narcolepsy, and hyperactivity disorders. Abuse occurs in people who acquire their drugs by both legitimate and illicit ways. History of Amphetamines First synthesized in 1887 by German Pharmacologist L. Edeleano, and at that time the stimulant effects were unnoticed. In 1927, Gordon Alles gave a firsthand account of its effects. Reduced fatigue Increased alertness Caused a sense of confident euphoria In 1932, Benzedrine inhalers (bennies) became available as a nonprescription medication (nasal congestion). History of Amphetamines (continued) The Benzedrine inhalers became widely abused for their stimulant action. 1971, all potent amphetamine-like compounds in nasal inhalers were withdrawn from the market. Widely used in World War II to counteract fatigue. Other users: Korean War soldiers, truck drivers, homemakers, high achievers under pressure (as performance-enhancers). History of Amphetamines (continued) In the early period of amphetamine use, medical professionals recommended amphetamine as a cure for a range of ailments— alcohol hangover, narcolepsy, depression, weight reduction, hyperactivity in children, and vomiting associated with pregnancy. The use of amphetamine grew rapidly because it was inexpensive, readily available, had long lasting effects, and because professionals purported that amphetamine did not pose an addiction risk In 1971, all potent amphetamine-like compounds in nasal inhalers were withdrawn from the market. At the height of the epidemic (1967) some 31 million persons in the U.S. were written prescriptions for anorexiants (diet pills) alone. Amphetamine Terminology Street amphetamine: bennies, black beauties, copilots, eye-openers, lid poppers, pep pills, speed, uppers, wake-ups, and white crosses. Street dextroamphetamine: dexies Street methamphetamine: chalk, chris, crank, cristy, crystal, crystal meth, go, gofast, meth, speed, and zip Concentrated methamphetamine hydrochloride: ice, crystal, and glass (article on crystal meth) Amphetamine Terminology (continued) Combinations: Amphetamines and barbiturates: goofballs Methamphetamine and heroin: speedballs Use and users: Speed run: increasing doses of injectable methamphetamine taken over several days or weeks Speeders or speed freaks: serial speed users; methamphetamine users who inject their drugs intravenously Source - http://www.cesar.umd.edu/cesar/drugs/amphetamines.asp How Amphetamines Work (see Mechanisms in hyperlink) Synthetic chemical similar to the natural neurotransmitters such as norepinephrine, dopamine, and epinephrine Increase the release and block the metabolism of these catecholamine substances, and serotonin, in the brain and peripheral nerves associated with the sympathetic nervous system. Thus, amphetamines control both arousal and mood. Because amphetamines cause the release of catecholamines they are classified as a sympathomimetic drugs. How Amphetamines Work (continued) Amphetamines can cause “Fight-or-flight” effect, a response to crisis Alertness Continual “high” can promote Anxiety, severe apprehension, or panic Potent effects on dopamine (pleasure) in the reward center of the brain “Whole-body Orgasms” Behavioral stereotypy: see next slide.. Behavioral stereotypy Meaningless repetition of a single activity produced by the user that has been reported with heavy amphetamine users. An amphetamine user will get “hung up”, caught in a repetitious activity for hours. They may take items apart (clocks, radios) and carefully categorize the parts, sit in a tub all day, persistently sing a not, repeat phrases of music, or repeatedly clean the same object for long periods of time. (see also “Punding” here) Approved Uses of Amphetamines • Narcolepsy • Attention Deficit Hyperactivity Disorder (ADHD) • Weight reduction (controls appetite center in hypothalamus) Short Term /Adverse Effects of Amphetamines Abuse and Addiction High body temperature, Cardiovascular system failure, Hostility or paranoia, Irregular or increased heart rate/heart beat, Increased diastolic/systolic blood pressure, Increased activity/talkativeness, Euphoria, Heightened sense of well-being, Decreased fatigue/drowsiness Short Term /Adverse Effects of Amphetamines (continued) Decreased appetite, Dry mouth, Dilated pupils, Increased respiration, Heightened alertness/energy, Nausea, Headache, Palpitations, Unrealistic feelings of cleverness, great competence, and power Current Misuse of Amphetamines Decline in abuse in the late 1980s and early 1990s. In 1993 the declines were replaced by an increasein the number of persons abusing amphetamines. Currently, 3–6% annual use of methamphetamine by adolescents in the United States. Due to the ease of production, methamphetamine can be made in makeshift labs using cookbook-style recipes. Toxic chemicals in such labs pose a threat to residents, neighbors, law enforcement officials, and the environment. Current Misuse (continued) Illegal labs that synthesize methamphetamine use decongestant ingredients from common OTC cold medicines. (ephedrine, pseudoephedrine = Precursor chemicals) Role of the Comprehensive Methamphetamine Control Act 2008 in reducing illegal manufacturing of methamphetamine. Illicit neighborhood labs have been replaced by small local “shake and bake” and large Mexican drug cartel operations for methamphetamine supplies. Current Misuse (continued) Patterns of High-Dose Use Amphetamines can be taken: (The initial effect is the “rush” and the period that follows 4-16 hours is the “high”) Orally Intravenously (speed freak) Smoked (ice) - Methamphetamine hydrochloride is processed to produce a potent, a smoked form of methamphetamine known as “glass” or “ice”. This substance is called “ice” because it resembles rock candy or a chip of ice. Meth Ice How is ice used? Ice is used by placing the substance in a glass pipe, heating it, and inhaling the resulting vapors. The vapors enter the bloodstream directly through the lungs and are rapidly transported to the brain. When ice is heated, its solid crystals turn to liquid. When it cools, ice reverts to its solid state and is therefore reusable. Since ice is odorless, it can easily be used in public without being detected. In addition to its use for recreational purposes, ice is often used in the workplace to increase alertness. Some users smoke ice for days at a time and then “crash” in a deep sleep lasting 24 hours or more. Source: http://www.methamphetamineaddiction.com/methamphetamine_ice.html Summary of the Effects of Amphetamines (p 315) High Dose Users The amphetamine addict tries to maintain the “high” as long as possible leading to extended mental and physical hyperactivity. This “run” can persist for 3-15 days (tweaking) The “Tweaker” can be hyperpyrexic , irritable and paranoid because they have not slept for days, and thus may act out violently. To control the side effects, Tweakers often use depressants – typically barbituates or alcohol High Dose Users Continued abuse (high doses) often leads to: Considerable Skin weight loss lesions Oral damage (meth mouth – see p. 316) Liver disease Hypertensive disorders Stroke / MI Kidney damage Seizures Small Towns, Big Problems: The Female Methamphetamine Epidemic High Dose Users Withdrawal (high dose users) often leads to: Depression (suicidal behavior) Lethargy Muscle pains Abnormal Sleep Patterns There is evidence that long term abuse among adolescents or adults may damage both long term dopamine and serotonin neurotransmitter systems of the brain. This may result in persistent episodes of psychosis, long term memory, motor impairment, and cognitive deficits. Amphetamines Amphetamine combinations Speedballs - a term commonly referring to the intravenous use of heroin or morphine and cocaine together in the same syringe. Designer drugs Methylenedioxymethamphetamine (MDMA, Ecstasy; most popular of the designer amphetamines) – see later slide.. Methylenedioxyamphetamine (MDA) A special amphetamine Methylphenidate (Ritalin) Amphetamines Treatment of Amphetamine Abuse Methamphetamine addiction is the principal problem with these drugs. Addiction causes long-term brain damage and is difficult, but not impossible, to treat. Requires long-term treatment to deal with compromised decision-making, memory deficits, increased impulsivity and lack of emotion control. No FDA-approved medications/treatment is principally behavioral management. Treatment typically requires more than one year of intense intervention consisting of drug abstinence, cognitive, emotional, and motivational rehabilitation. MDMA (Ecstasy) • A designer amphetamine that continues to be popular with young people. • It enhances sensory input and is referred to as an entactogen (a combination of psychedelic and stimulant effects) and it releases both serotonin and dopamine. • While dependence can occur, it tends to be unusual. • Withdrawal includes depression and sleep disruption that can last for days. Performance Enhancers • These are stimulants used to embellish physical/mental endurance and enhance performance. • Often used by college, and even high school, students to help academically. • The drugs used can be illegal amphetamines or related prescription stimulants that are used to treat ADHD, like Ritalin. • As with other potent stimulants, use of these drugs can be very dangerous and cause dependence. Cocaine Cocaine abuse continues to be a major drug concern in the United States. From 1978 to 1987, the United States experienced the largest cocaine epidemic in history. As recently as the early 1980s cocaine was not believed to cause dependency. Cocaine is known to be highly addictive. In 2010, approximately 2.4% of high school seniors used cocaine. © Corbis History of Cocaine The first cocaine era (2500 BC) South American Indians (see p 302) Erythroxylon coca shrub The second cocaine era (began 19th century) Vin Mariani (Angelo Mariani’s Wine) – p.324 Coca-Cola ( see history) Sigmund Freud - “magical drug” The third cocaine era (began 1980s) Celebrities Decreased in price to $10 a “fix” with large suppliers Current Trends in Cocaine and Crack Use by High School Seniors Source: Johnston, L D., P. M. O’Malley, J. G. Bachman, and J. E. Schulenberg. Monitoring the Future. “Long-Term Trends in Annual Prevalence of Use of Various Drugs in Grade 12 (Table 16).” Ann Arbor, MI: University of Michigan, 2010. Available at: http://monitoringthefuture.org/data/10data/pr10t16.pdf. Accessed March 4, 2011. Cocaine Administration Form of administration important in determining intensity of cocaine’s effects, its abuse liability, and likelihood of toxicity. Orally: Chewing of the coca leaf Inhaled: Into the nasal passages (“snorting”) Injected: Intravenously Smoked: Freebasing, crack © Medioimages/age fotostock Pharmacological Effects of Cocaine Enhanced activity of the catecholamine and serotonin transmitters Blocks the reuptake of these substances following their release from neurons The summation of cocaine’s effects on dopamine, noradrenaline, adrenaline, and serotonin is to cause CNS stimulation Cardiovascular system Increased sympathetic drive – increased hear rate and vasoconstriction Local anesthetic effect Main Stages of Cocaine Withdrawal (see Table 10-3 p. 333) 1. 2. 3. Crash: Initial abstinence phase consisting of depression, agitation, suicidal thoughts, and fatigue Withdrawal: Including mood swings, craving, anhedonia, and obsession with drug seeking Extinction: Normal pleasure returns, mood swings, cues trigger craving Treatment of Cocaine Dependence Is highly individualistic and has variable success. Most cocaine users use other drugs as well, such as alcohol. Principal treatment strategies include inpatient and outpatient programs. Drug therapy is often used to relieve cocaine craving and mood problems. (levodopa, bromocriptine) both assist in dopamine transmission Psychological counseling, support, and a highly motivated patient are essential. Cocaine and Pregnancy Cocaine babies; not clear the effect of cocaine on the fetus. Some possibilities are: Microencephaly Reduced birth weight Increased irritability Subtle learning and cognitive defects Minor Stimulants Caffeine is the most frequently consumed stimulant in the world. It is classified as a xanthine (methylxanthine) It is found in a number of beverages Also found in some OTC medicines and chocolate In the U.S., the average daily intake of caffeine is equivalent to 2-3 cups of coffee a day. © AbleStock Caffeine Content of Beverages and Chocolate Physiological Effects of Xanthines CNS effects Enhances alertness, causes arousal, diminishes fatigue Adverse CNS effects Insomnia, increase in tension, anxiety, and initiation of muscle twitches Over 500 milligrams: panic sensations, chills, nausea, clumsiness Extremely high doses (5 to 10 grams): seizures, respiratory failure, and death Physiological Effects of Xanthines (continued) Cardiovascular effects Low doses: Heart activity increases, decreases, or does nothing High doses: Rate of contraction of the heart increases, minor vasodilation in most of the body, cerebral blood vessels are vasoconstricted Respiratory system effect Can cause air passages to open and facilitate breathing Physiological Effects of Xanthines (continued) Caffeine intoxication Caffeinism (about 10% of consumers) Restlessness, nervousness, excitement, insomnia, flushed face, diuresis, muscle twitching, rambling thoughts and speech, stomach complaints Caffeine dependence © Christa DeRidder/ShutterStock, Inc Physiological Effects of Xanthines (continued) © Christa DeRidder/ShutterStock, Inc Other Stimulants (Table 10.6, p.341) OTC sympathomimetics included in cold, allergic and diet aid medications OTC Sympathmimetics can pose emergencies and be deadly (See Here and Now, p. 341and 342) Herbal stimulants: often contain ephedrine, ephedra, ma huang, or guarana Other Stimulants - Diet Pills Are Russian Roulette for Athletes End of Presentation