Sunne? Palermo Psych 321 Test 2 · Stimulants and Depressants Exam Cocaine and the Amphetamines 1. WHERE DOES COCAINE COME FROM? HOW IS IT MADE? · Cocaine is made from the coca plant which contains the alkaloid cocaine, grows mainly on the slopes of the Andes Mountains in South America. · The cocaine refinement technique is a 4-5 step process: (1) Soak the leaves in an alkali and water (2) add gasoline, kerosene, or acetone, (3) discard the waste leaves and add acid, (4) mix in lime and ammonia, and (5) separate the cocaine hydrochloride from the paste. 2. TRACE THE USE OF COCAINE OVER TIME. ü The Incas usually chewed usually chewed the leaf for the juice; they grew if for personal profit, to generate government taxed, and to enable the Incas to work more efficiently at high altitudes. In 1859 Albert Niemann isolated cocaine from the other from the other chemicals in the coca leaf. This powerful alkaloid, cocaine hydrochloride was 200 times more powerful by weight than the coca leaf, setting the stage for the widespread use and abuse of the dru g . Beginning in the late 1860s cocaine wines became popular. Suddenly in the 1880s and 1890s patent medicines laced with cocaine, opium, morphine, heroin, Cannabis and alcohol became the rage. In the late 1800s the prolonged use of cocaine and other prescr i ption medications created a large group of dependent users and addicts, the majority being women. The invention of the hypodermic needle in 1853 had a more immediate effect on the use of morphine than on cocaine. The early 1900s gave rise to a popular new form of cocaine: snorting the powder into the nostrils. 3. DEFINE ? STIMULANT PSYCHOSIS, FORMICATION ü Stimulant Psychosis: i s a psychotic disorder that appears in some people who abuse stimulant drugs. ü Formication: A cocaine- or methamphetamine- induced sensation that makes users think that bugs are crawling under their skin 4. WHAT IS THE DIFFERENCE BETWEEEN THE POWDER AND ROCK FORM OF COCAINE? WHY IS THE ROCK FORM CONSIDERED TO BE MORE ADDICTIVE? 5. HOW WERE THE AMPHETAMINES DEVELOPED? ü Amphetamines were firs t synthesized in 1897 by a German chemist. The explicit purpose to find psychoactive drugs. At first no therapeutic use til the 1920s with nasal inhalers called crack pipes. First inhaler was straight Benzedrine. Served as an appetite depressant for overw e ight people. 6. CAN THE SUBJECTIVE EFFECTS OF COCAINE AND AMPHETAMINES BE DISCRIMINTED? 7. DESCRIBE THE MECHANISM OF ACTION OF STIMULANTS? 8. WHY DOES DEPRESSION FOLLOW COCAINE AND AMPHETAMINE USE? ü Cocaine prevents the reabsorption of these neurotransmitters, increasing their concentration in the synapse & intensifying the effects. Because cocaine is metabolized so quickly, the initial euphoria disappears as suddenly as they appeared. So the crash a f ter using cocaine can be intensely depressing. 9. DESCRIBE THE ADMINISTRATION, ABSORPTION, METABOLISM AND ELIMINATION OF STIMULANTS. ü Metabolism- Because cocaine is metabolized very quickly, effects dissipate faster than with amphetamines and amphetamine cong eners. Cocaine is metabolized to ecgonine methyl ester, benzoylecgonine, and if alcohol is present, cocaethylene. ü Administration ? i. Chewing the leaf ? The Incas usually chewed the leaf for the juice, adding some lime or ash to increase absorption by the mucosal tissue in the cheeks and gums which takes 3 ? 5 minutes ii. Drinking cocaine ?Beginning in the late 1860s cocaine wines became popular. Angelo Mariani concocted Vin Mariani and promoted its use through the first celebrity endorsements that the f irst cocaine epidemic began. It takes 15 to 30 minutes to reach the brain iii. Injecting cocaine- The hypodermic needle was invented in1853. Injecting cocaine intravenously results in an intense rush within 30 sec and gives the highest blood cocaine level iv. Snorting cocaine- This method gets the drug to the nasal mucosa and into the brain in 3-5 minutes . The drug constricts the capillaries that absorb the drug, so the more that is snorted, the slower the absorption. v. Smoking cocaine- Mid 1970s street chemists converted cocaine hydrochloride to freebase cocaine. This process lowered the vaporization point to 98 degrees C and made the drug smokable. Mid 1980s an easier method of making freebase cocaine was developed, setting the stage for cocaine epidem i c. This new form of smokable cocaine called ?crack? ü Mucosal & contact absorption - Cocaine can be absorbed through mucosal tissue in the rectum and the vagina and act as a topical anesthetic. When absorbed through the lungs, cocaine reaches the brain in onl y 5 to 8 seconds. ü Elimination- 10. DESCRIBE THE LOW DOSE EFFECTS OF STIMULANTS ü Low moderate doses: 15-16mg ü 10-20 mg normal substance in a line ü 1-2 lines would be considered a low moderate dose ü Enhances sexual desire, delays ejaculation ü They are sympathomimetic meaning they mimic nervous system: heart rate increases, blood pressure, sweating, pupils dilate, has anorectic affects, appetite suppressant. ü Mimics a flight or fight response ü Male gear doesn?t work/ females lack of interest but no lack in performance 11. WHAT ARE THE THERAPUTIC USES OF COCAINE AND AMPTHETAMINES ü Cocaine is the only naturally occurring topical anesthetic with powerful vasoconstriction effects, cocaine is used in aerosol from to numb the nasal passages when inserting breathing tubes in a patient, to numb the eye or throat during surgery, and to deaden the pain of chronic sores. ü Amphetamines are used to treat attention-deficit/hyperactivity disorder, narcolepsy, and occasionally weight control. 12. DESCRIBE THE HIGH DOSE EFFECTS OF STIMULANTS ü Often people die ü Cocaine over time can cause stimulant psychosis ü Mos t common symptom is paranoid delusions = Delusions is when you believe something that is not real ü Allusions = when you have a feeling and you are thinking it is so ü Hallucinations tactile is rank bugs 13. DOSE STIMULANT USE INVOLVE TOLERANCE? IS SO, WHAT TYPES? ü There is tolerance to the reinforcing effect but no the lethal effects 14. WHAT IS KINDLING? ü Also called inverse tolerance, when continuous use changes brain chemistry to the point that the same dose suddenly starts causing a more intense reaction. The user be comes sensitive to the drug?s effects as use continues. 15. IS THERE A WITHDRAWAL SYNDROME ASSOCIATED WITH STIMULANT USE? IS SO, DESCRIBE IT. ü If a person binges- they binge & recover for a long time. ü Cravings ? their insides will tighten up, if they get coca ine that feeling or craving will go away. i. A big trigger for relapse ü Chronic Phases of Withdrawal i. Phase 1: Crash ~ 1 day ? week, person is recovering from last binge. ii. Phase 2: For the next 10 weeks ? more depression & craving becomes more pronounced iii. Phase 3: Extinction: lifelong, recovery craving will continue to occur, at first when people give up the drug, the craving will become more generalized. 1. A stimulate cue will stimulate the craving (driving past a specific neighborhood where they once scored dope) 2. Money is an automatic trigger NICOTINE 1. WHERE DOES NICOTINE COME FROM? GROWN? DISTRUBUTED? ü Tobacco originally grown in Central and South America was brought to the rest of the world by Christopher Columbus and other explores and seamen. ü Tobacco was venerated as a plant of the gods and used in spiritual and health rituals in ancient Mesoamerica. ü The major growing areas are Virginia, North Carolina, and South Carolina ü Louisiana was once the biggest cash crop for tobacco 2. WHAT ARE THE FORMS OF NICOTINE? ü Cigarettes, cigars, pipes, and chewing tobacco ü Powder snuff (dry snuff) is a fine powder that is most often sniffed into the nose or rubbed on the gums. ü Loose-leaf chewing tobacco, larger sections of leaf are stuffed into the mouth and chewed to all allow the nicotine-laden juice to be absorbed. ü Moist snuff is finely chopped tobacco that is stuck in the mouth next to the gums, where the nicotine is absorbed in the capillaries. 3. HOW WAS THE POPULARITY OF SMOKING WAXED AND WANED OVER TIME? WHEN DID IT PEAK? WHY? ü Improved cigarette-manufacturing technology, a milder type of tobacco, lower prices, increased and more-skillful advertising, and more aggressive marketing techniques led to the increase in popularity of tobacco. In 1963 prevalence of sm oking peaked but by 1964 smoking overall had dropped. Smoking has declined in popularity. 4. HOW HAVE THE TOBACCO COMPANIES CHANGED THEIR BUSINESS PRACTICES OVER TIME? ü Recognizing the decline in American sales over the past 30 years, tobacco companies have t ried to increase sales overseas. In the US just a handful of companies control the tobacco market. Because of ever increasing cost of a pack of cigarettes, in the 1980s many manufactures came out with generic brands that were cheaper. The big manufacturin g companies have also lowered the prices of name brands. In the early 1970s the US tobacco industry voluntarily agreed to a partial advertising ban rather than face a total ban or a requirement to surrender $1 for every $3 spent on advertising that the gov e rnment would use to create antismoking advertisements, 5. WHO USES TOBACCO THE MOST? 6. HOW IS NICOTINE DELIVERED? ü Nicotine is the crucial ingredient in tobacco in terms of cardiovascular and psychoactive effects. The average cigarette contains 10mg of nicotine but delivers only 1 to 3mg of that to the lungs when burned and inhaled. Chain smokers might get up to 6mg in their lungs. One chew of tobacco will deliver 4.5 mg of nicotine and one pinch of snuff has about 3.6 mg. 7. DESCRIBE THE MECHANISM OF ACTIO N OF NICOTINE? ü The effects of nicotine are the main reason for the widespread use of tobacco. Nicotine, a central nervous system stimulant, disrupts the balance of neurotransmitters. Nicotine mimics acetylcholine by slotting into nicotinic acetylcholine re ceptor sites, so those cholinergic effects are exhausted. The release of dopamine makes a smoker feel satisfied and calm, so a cigarette both stimulates and tranquilizes. 8. DESCRIBE ANY TOLERANCE ASSOCIATED WITH NICOTINE USE. ü Physiological adaptation to the initial effects of nicotine develops quite rapidly. A few hours of smoking are sufficient for the body to begin learning how to handle these new toxins, probably through neural adaptation. Once smokers adapt to the initial effects of tobacco, they find a level of smoking that they can maintain over time, so the tolerance does not continue to build as it does with amphetamines or benzodiazepines. 9. DESCRIBE THE WITHDRAWAL SYNDROME FROM NICOTINE. ü Withdrawal from a 1/pack or 2/p ack a day habit ager prolonged use can cause headaches, nervousness, fatigue, hunger, sever irritability, poor concentration, depression, increased appetite, sleep disturbances, and intense nicotine craving. When a smoker stops using tobacco, the activity of acetylcholine is greatly exaggerated by all these extra activated receptors, making the user restless, irritable, and discontent. The smoker comes to depend on smoking to stay normal. 10. DESCRIBE THE ACUTE EFFECTS OF NICOTINE USE? ü Feelings of dizziness and high. A calming feeling, a sense of relaxation and well being. 11. ARE THERE ANY CHRONIC EFFECTS OF NICOTINE USE? ü Pages 141-143 CAFFEINE 1. WHAT ARE THE METHYLXANTHINES AND WHERE DO THEY OCCUR? ü Methylxanthines are related to . These drugs provide mild to moderate relaxation of muscles in the airway to decrease bronchospasm. Essentially, they work as long-acting bronchodilators. These medi cations may have a mild anti-inflammatory effect . 2. DESCRIBE THE HISTORY OF METHYLXANTHINE USE. ü Tea is the most widely consumed beverage in the world besides water. It was thought to be present in China as early as 2700 B.C. A tea ceremony became an important ritual in Japanese homes and castles. Its purpose is to enter a mental state in which ones t rue self can be discovered. Primary exporters of tea ? India, China, and Sri Lanka. Coffee was first cultivated in Ethiopia. The drink was so stimulating that many cultures banned it as an intoxicating drug. Coffee and tea were great sources of revenue. I n the US each coffee drinker consumes about 20lbs of coffee per year. Cocoa from the roasted and ground beans of the cacao tree was first used in the New World by Mayan and later Aztec royalty not only as an unsweetened drink or as a spice but also as a fo o d, a stimulant, and even a currency. There is a small amount in chocolate but theobromine also has stimulatory effects. Caffeinated soft drinks from the African kola tree but mostly they use caffeine extracted from the process of decaffeinating coffee. En e rgy drinks contain taurine, ginseng, guarana, glucose or glucuronolactone, B-complex vitamins, minerals, and carbohydrates to provide a quick energy boost. 3. DESCRIBE THE PREVALENCE OF CAFFEINE USE. ü Caffeine is not only the most popular stimulant in the wor ld but also the world?s most popular mood altering and habit forming drug. Caffeine is found in coffee, tea, chocolate, soft drinks, energy drinks, 60 different plants, and hundreds of over the counter and prescription medications. In America 85% of the p o pulation consumes substantial amounts of caffeine every day. 4. DESCRIBE THE ADMINISTRATION, ABSORPTION, DISTRIBUTION, METBAOLISM, AND ELIMINATION OF CAFFEINE. 5. WHAT IS THE MECHANISM OF ACTION OF THE METHYXANTHINES? 6. WHAT IS THE EVIDENCE FOR TOLERANCE AND WITHDRAWAL FOR CAFFEINE? ü Tolerance to the effects of caffeine does occur, although there is a wide variation among the ways different ppl react to several cups of coffee or tea. Continuous caffeine use increases the number of adenosine recept or sites, so it takes more caffeine to block them; this is one of the main mechanisms for the development of tolerance. Withdrawal symptoms do occur after cessation of long-term high dose use and can occur after levels of use as low as 100mg per day, whic h is one strong cup of coffee or 2 colas. The most prominent withdrawal symptom is a throbbing headache that is worsened by exercise but of course relieved by a cup of coffee. Other symptoms include ? sleepiness, fatigue, lethargy, depression, decreased al e rtness, sleep problems, irritability, and even flulike symptoms. 7. WHAT ARE THE ACUTE EFFECTS OF METHYXANTHINES/CAFFEINE? ü Caffeine constricts blood vessels in the brain, making it valuable as a treatment for headaches, especially migraine headaches. Caffein e is most widely known and used as a mild stimulant. In low doses (100 to 200 mg) caffeine can increase alertness, dissipate drowsiness or fatigue. The stimulation is caused by caffeine?s inhibiting effect on adenosine, a neuromodulator that normally depr e sses mood, induces sleep, and causes low blood pressure. When caffeine blocks adenosine, the result is wakefulness, raised mood, high blood pressure, fast heart rate, and vasoconstriction. 8. WHAT ARE THE CHRONIC EFFECTS OF METHYXANTHINES/CAFFEINE? ü At doses of more than 350 mg per day, again depending on the user?s susceptibility and tolerance, anxiety insomnia, gastric irritation, high blood pressure, nervousness, and flushed face can occur. At doses about 1000 mg taken over a short period of time, increase d heart rate, palpitations, muscle twitching, rambling thoughts, jumbled speech, and even convulsions. Caffeine is lethal at about 10 grams ( 100 cups of coffee). Coronary heart disease, ischemic heart disease, heart attacks, intestinal ulcers, diabetes, a n d some liver problems. Opiates 1. Where does opium originate? · The poppy plant 2. Describe the history of opiate use including the development of morphine and heroin. · The ancient Sumerians and Egyptians listed opium as a cure for all illnesses, a pleasure inducing substance, and a poison. · Greek writings told of the gods use of opiu m for mystical or mythical purposes i. Jason : used it to sedate monsters ii. Demeter : took opium to sleep and forget the death of her daughter iii. Hippocrates : prescribed it for sleep, diarrhea, pain, female ills, and epidemics. 3. Describe the pharmaco kinetics and pharmacodynamics of opiates. · Pharmacokinetics (absorption, distribution, elimination) i. Orally ii. Smoking iii. Injection iv. Snorting v. (Need to check answer) 4. What is Naloxone and for what is used? · Its an opioid antagonists · To block and reverse the life-threatening effects of too much drug · Used to counter the effects of opioid drug overdose 5. Are there tolerance and withdrawal syndromes associated with opiate use? If so, describe. · Tolerance: No syndromes i. Occurs when the body tries to neutralize the opiate drug, it may?. 1. Speed up the metabolism 2. Desensitize the nerve cells 3. Excrete the drug more rapidly 4. Alter the brain and body chemistry ii. The body?s adjustment requires the user to increase dosa ge if the same effects are desired iii. B /c tolerance occurs rapidly with opioids user might need 20 times as much drug in as little as 10 days iv. There is almost no limit to the development of opioid tolerance · Withdrawal: Yes Syndrome i. Precipitated a bstinence syndrome ii. (Need to check answer) 6. What are the medical uses of opiates ? · Pain control · Pleasure · Cough suppression · Diarrhea control 7. What are the acute (short-term) effects of heroin use? · Appear after a single dose in a few short hours · Euphoria ?Rush?, impaired night vision · Dry mouth , slow walk, constricted pupils, droopy eyelids , vomiting · Warm flushing of the skin , Slowed and slurred speech , constipation 8. What kinds of diseases do the chronic use of heroin cause? · Hepatitis C i. 50-90% of all needle-using heroin addicts carry it · Liver Diseases i. Once infected with Hepatitis C, 20-40% will develop liver disease · Liver Cancer i. And 4 -16% will develop liver cancer · HIV i. 74-94 % are heroin addicts that are HIV positive ii. Worldwide 40 million people are HIV/AIDS positive · Endocarditis i. An infection of heart valves · Cotton Fever i. Caused by endotoxins ii. Resulting in fever, chills, tremors, aches, and pains · Necrotizing Fasciitis ?flesh eating disease? i. Worst infection ii. Destroys fascia and subcutaneous tissue 9. What is the prevalence estimate of heroin users worldwide? · 5-10 million 10. What are some of the side effects of using Opiates? · Insensitivity to pain · Lowered blood pressure · Lowered pulse and respiration rate · Confusion 11. What is one of the most abused muscle relaxants? · Soma (guessed from experience, not sure of this answer) 12. What was the major development in 1853 that fa cilitated the use of opiates ? · Was the hypodermic needle, IV instead of SUB-Q · By Dr. Alexander Wood · Found that intravenous use could inject high concentrations of the drug directly into the bloodstream through the veins · IV=15-30 seconds for an injected opiate to affect the CNS · SUB-Q: delayed 5-8 minutes 13. Why do cities in the Southwest US have such a large heroin problem? · Because the US major supplier of heroin is Mexico (8 metric tons) 14. What is morphing? · Pg 178 15. What is Fentanyl? · ( Sublimaze ) · Most p owerful of the opioids · Used intravenously during and after surgery for sever pain · Available in a skin patch to give steady pain relief for patients with intractable pain · It is diverted from pills, liquid, patch · Street name ?china white? extremely p otent Depressants 1. Describe the history of depressants. How were they discovered/developed? Ho w have they been used in the US · ? 2. Describe the pharmacokinetics of barbiturates · Long-Acting Barbiturates o Last 12-24 hours o Used as day time sedatives o Used to control epileptic seizures o Metabolized by the liver into inactive compounds before the effects wane, metabolites are excreted through the kidneys into the urine · Intermediate-Acting o Long-acting sedatives o Last 6- 12 hours · Short-Acting o 3 to 6 hours o Induce sleep · Very Short-Acting o Used for anesthesia o Cause immediate unconsciousness o Inactivated o IV: proceed directly to the brain to produce anesthesia and unconsciousness. 3. What is the mechanism of action for barbiturates? · GABA, acting as a brake on inhibitions, anxiety, and restlessness. 4. What are the medical uses of barbiturates? · Seizer disorder · Sleep aid · Tension relief 5. What are the dangers of barbiturate use? · Withdrawal symptoms resulting from heavy tissue dependence are very dangerous and can result in seizures within 12 hours to one week from the last dose. 6. Are there tolerance and withdrawal effects for barbiturat e use? · Tolerance i. Most dramatic is dispositional tolerance 1. Results from the conversion of liver cells to more-efficient cells that metabolize or destroy barbiturates more quickly ii. Pharmacodynamics tolerance 1. Causes affected nerve cells and tissues to become less sensitive. · Withdrawal i. Within 6 to 8 hours after stopping use of short-acting barbiturates users will begin to experience withdrawal symptoms 1. Anxiety, agitation, loss of appetite, increased he art rate, etc. ii. Symptoms tend to peak on 2 nd or 3 rd day iii. Withdrawal symptoms resulting from heavy tissue dependence are very dangerous and can result in seizures within 12 hours to one week from the last dose. 7. Describe the non-barbiturate sedativ es · 8. What are benzodiazepines and how are they related to the barbiturates? · Benzodiazepines i. Most widely used sedative- hypnotics in US ii. Developed as an alternative to barbiturates iii. Should be used short term and for specific conditions 9. In general, what effects do depressants exert at what doses? 10. Describe the pharmacokinetics and pharmacodynamics of benzodiazepines 11. What are the therapeutic uses of benzodiazepines · Short term treatment for anxiety and panic disorder · Control anxie ty in surgical patients · Treat sleep · Control skeletal muscular spasms · Elevate seizer threshold · Control acute alcohol withdrawal symptoms 12. Is there tolerance and withdrawal effects associated WITH CHRONIC USE OF BENZODIAPINES? 13. What is BuSpar? · Buspirone · A sedative- hypnotic medication · Used as an anxiolytic or anti-anxiety medication · But is also used in combination with SSR antidepressant medications to treat depression · Has high affinity for serotonin receptors · Low affinity for dopamine receptors in the brain · Has no direct effects on GABA · Lacks the ability to produce abuse, addiction, or withdrawal symptoms · Good to use for patients who suffer from addiction 14. Describe synergism and why is it a problem? · An exaggerated effect that occurs when two or more drugs are used at the same time. · One reason why this effect occurs is because the liver or body s busy metabolizing one drug while the other slips through unchanged. · The problem is exaggerated respirator depression, it causes more blackouts or loss of memory · Causes about 19,000 deaths per year and 275,000 are treated with ED 15. What is ?mothers little helper?? 16. Each year, how many people die in the US from bad re actions to prescription drugs? Are many suffer injury from prescribed drugs? Inhalants 1. Describe the class of inhalants. What do they have in common? a. Volatile Solvents and Aerosols i. Synthesized from petroleum and combined with other chemicals b. Volatile Nitrates i. Blood vessel dilators for heart problems c. Anesthetics i. Block pain or induce unconsciousness during surgery 2. Who is most likely to be an inhalant abuser? 3. What inhalants are the least dangerous? Most Dangeous
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