Cocaine HistoryEarly Legal Controls on CocainForms of CocaineContemporary Legal ControlsFederal Cocaine Offenders (by race)Mechanism of ActionAbsorption and Onset of EffectsCocaine EliminationBeneficial UsesConcernsAcute ToxicityChronic ToxicityDependence PotentialReproductive EffectsSupplies of Illicit CocaineCurrent Patterns of UseAmphetamines HistoryThe Return of MethamphetamineAmphetamine PharmacologyAbsorption and EliminationBeneficial UsesConcernsAcute ToxicityChronic ToxicityDependence PotentialStimulants - Stimulants are substances that can keep a person going mentally and physically- Restricted stimulants: Examples: cocaine and amphetamine- Readily available stimulants: Examples: caffeine and nicotineCocaine History- Coca a bush that grows in the Andes and produces cocaine Harvested for thousands of years and actively cultivated for over 800 years- The coca leaf was an important part of Inca culture Used in religious ceremonies and as currency - Some natives of the Andes still chew coca leaves to reduce fatigue and increase productivity- Cocaine was in use in Europe by the 19th century- Coca wine Developed by Angelo Mariani  Used coca leaf extract in many other products includinglozenges and tea - Cocaine was also used in the United States in early versionsof Coca-Cola and in many patent medicines- Cocaine was isolated from the plant before 1860 Processing 500 kilograms of coca leaves yields 1 kilogramof cocaine - Early psychiatric uses: Sigmund Freud studied use of cocaine as a treatment for depression and morphine dependence Later opposed use of the drug after nursing a friend through cocaine psychosisEarly Legal Controls on Cocain- Press and politicians made unsubstantiated claims about cocaine use among southern blacks:  Widespread use Associated with increased violent crime- 46 states passed laws to regulate cocaine between 1887 and 1914- Negative publicity about cocaine influenced the passage of the 1914 Harrison ActForms of Cocaine- Coca paste Crude extract created during the manufacture of cocaine In South America, often mixed with tobacco and smoked - Cocaine hydrochloride  Most common form of pure cocaine Stable water-soluble salt Often insufflated - Freebase Extraction of the cocaine base with a solvent (ether) Can be heated and the vapors inhaled- Crack cocaine Lumps of cocaine base prepared by mixing cocaine with water and baking soda Can be heated and the vapors inhaledContemporary Legal Controls- Cocaine use increased in the late-1960s- Prior to 1985, the major form of the drug available was cocaine hydrochloride Most often insufflated Usually sold in bulk amounts that were relatively expensive Cocaine use was associated with status, wealth, and fame- By the mid-1980s, crack became available Relatively inexpensive ($5 to $10 a hit) Smoked cocaine use was associated with poor, black Americans- Media and politicians focused on crack use among urban black Americans Associated with violence and dependency- Anti-Drug Abuse Acts of 1986 and 1988 Penalties for sale of crack cocaine significantly more severe compared with powder cocaine Tougher penalties for first-time users of crack- U.S. Sentencing Commission concerns about policy: Penalties’ severity disproportionately impacted blacks Exaggerated relative harmfulness of crackFederal Cocaine Offenders (by race)Mechanism of Action- Cocaine’s mechanism of action is complex- Cocaine blocks reuptake of dopamine, serotonin, and norepinephrine - GABA and glutamate have also been implicatedAbsorption and Onset of Effects- Chewing or sucking coca leaves Slow absorption and onset of effects- Insufflation “Snorting” Absorbed through nasal mucous membranes Rapid absorption and onset of effects- Intravenous injection Rapid and brief effects- Smoked Rapid and brief effectsCocaine Elimination- Cocaine is metabolized by enzymes in the blood and liver- Half-life of about one hour- Major metabolites have a half-life of eight hours These are detected by urine drug screensBeneficial Uses- Local anesthesia: Used medically since 1884 Early applications were eye surgery and dentistry- Synthesized drugs with few CNS effects have largely replaced cocaine Cocaine remains in use for surgery in the nasal, laryngeal, and esophageal regionsConcernsAcute Toxicity - No evidence that occasional use of small amounts is detrimental to health- Potential toxicity increases with larger doses Profound CNS stimulationo which can lead to respiratory or cardiac arrest- Illicit cocaine is often adulterated Adulterants may be more toxic than the drugChronic Toxicity- Binge use Drug is taken repeatedly and at increasingly high doses- Risks of binge use Increasing irritability, restlessness, paranoia Can result in paranoid psychosis Most seem to recover once the drug leaves the systemDependence Potential- Cocaine dependence occurs in some users Animal and human studies have shown that cocaine is a powerfully reinforcing drug Example: Animals will readily self-administer the drug by lever-pressing - After binge use, some people experience withdrawal symptoms Cocaine craving, irritability, anxiety, depressed mood, increased appetite, fatigue Reproductive Effects- “Crack Baby” phenomenon Media reports overstated the expected long-term effects of cocaine exposure Recent studies indicate no consistent associations between cocaine exposure and several developmental measures- Cocaine use during pregnancy  Increased risk of miscarriage and torn placentaSupplies of Illicit Cocaine- Readily available in all major U.S. cities- Price and purity have remained stable for the past decade- Most illicit cocaine in the U.S. comes from: Peru, Bolivia, and ColumbiaCurrent Patterns of Use- NSDUH and MTF surveys indicate: Less than 2 percent of adults currently use cocaine (2010 data) Down from a peak of 7 to 9 percent in the 1980s - In general, usage rates of cocaine and amphetamine tend to cycle in opposition to each other When cocaine use decreases, amphetamine use may increaseAmphetamines History- The Chinese used a medicinal tea made from ma huang (Ephedra)- Active ingredient is ephedrine Stimulates the sympathetic branch of the autonomic nervous systemo Sympathomimetic drug Used to treat asthma- Amphetamine  Synthesized chemical similar to ephedrine Patented in 1932- Early