Exam 2 Flashcards
(90 cards)
History of Cocaine
- Incas in Peru, chew on coca plant for strength/energy
- Cocaine = active drug in coca, extracted by lime
- Inca religious ceremonies, settler currency
- European interest in last half of 1800s
- 3 individuals
- Mariani - coca wine, other coca products
- Halsted - local anesthesia
- Freud - psychiatric uses, withdrawal - 1887-1914: 46 states had cocaine regulation laws, bc associated with undesirables “cocaine fiend”
- 1960s concern bc amphetamines harder to obtain, so use grew
- seemed to have few side effects–bulk amounts expensive–restricted access masked negative consequences
- associated with elite until 1985, wealth and fame (60-85)
- mid/late 80s dealers started selling crack–$5-10
- Len Bias 1986, thought died of crack, fr used powder
- Don Rogers
- Oct 1986: Reagan’s Crack Cocaine Awareness Month
- Congress passed Anti-Drug Abuse Act of 1986: 100:1 ratio
- 2010: Obama –> 18:1
Cocaine Forms
- Coca leaves mixed with organic solvent, such as kerosine or gasoline —> soaked and filtered to form coca paste
- absorbed slowly through mucous membranes, slow onset of effects, lower blood levels
- In SA, paste mixed with tobacco and smoked - Paste can be made into cocaine hydrochloride, a salt that mixes easily in water and is stable enough that heating can’t produce vapors for inhalation
- Either snort or shoot up- Snorting = most common route
- cocaine hydrochloride powder up nose to nasal mucosa; absorbed rapidly and reaches brain quickly
- Snorting = most common route
- Freebase: smokable cocaine/heroin
- Done by extracting it into volatile organic solvent, like ether
- Dangerous: combination of fire + fumes = explosive
- freebase declined in 80s, when crack discovered by mixing with household chems like baking soda+H2O - Cocaine can be taken by mouth, insufflation (blow/snort), injection, or inhalation
- intravenous > inhalation > oral > intranasal
Adulterated
- make something poorer in quality by adding another substance
- bc crack cocaine is very adulterated, actually more expensive than powder
Anti-Drug Abuse Act
1986
Reagan
100:1 ratio
add details
2010: Obama 18:1
US Sentencing Commission Study
(1) Penalties most impacted blacks (85% of convicted)
(2) Exaggerated relative harmfulness of crack
(3) Penalties sweep too broadly and most often applied to low-level offenders
(4) Quantity-based penalties overstated seriousness of crack offenses and failed to provide proportionality
Cocaine Chemical Structure
- Blocks the reuptake of DA, NE, and Serotonin…causing prolonged effect of these neurotransmitters in synapse
- Focus used to be on DA (blockage/destruction of DA neurons lessened animal self-admin rates of cocaine)
Cocaine Metabolism
- Metabolized by enzymes in the blood and liver
- Rapidly removed, with half-life of one hour
- Major metabolites: 8 hrs
- 3 days for complete elimination
Cocaine Beneficial Uses
Local anesthesia
- Still used in nasal, laryngeal, and esophageal surgeries bc absorbed so well into mucous membranes
Other claims
- overcome fatigue (celebs, athletes)
Cocaine Causes for Concern
- Acute toxicity
- Acute cocaine poisoning leads to profound CNS stimulation, progressing into convulsions, which can lead to respiratory and cardiac arrest
- Toxicity dependent on dosage size, adulteration
- Cocaethylene: (c+alc) more toxic than cocaine in mice, less potent in humans - Chronic toxicity
- In a binge (taken repeatedly and at increasingly high dosages) produces irritability, restlessness, paranoia
- Extreme cases: paranoid psychosis—lose touch with reality, auditory hallucinations
- Most recover after drug leaves system - Dependence Potential
- Majority do not become addicted
- Powerfully reinforcing drug (lab and animals will perform tasks to receive, big % of drug rehab causes)
- Withdrawal: anxiety, depression, craving, etc. - Reproductive Effects
- Increased risk of miscarriage and torn placenta
Chronic v. Acute Toxicity
- Acute: effects of single exposure or few in short period of time (24 hrs)
- Chronic: effects of repeated, long-term exposure
Supplies of Cocaine
- Price and purity by DEA indicators of supply
- Columbia, Bolivia, Peru
Cocaine Trends
1880s: first appeared, positive, benign substance
1890s: more use–>dangers became well known
1990s: society against it, laws to control it
Cocaine - Amphetamines
As cocaine use declines, amphetamine use increases
History of Amphetamines
- Chinese medicinal tea from herbs
- Active ingredient: ephedrine, used to dilate bronchial passages in asthma patients
- does so by stimulating sympathetic branch of autonomic nervous system
- also raises blood pressure
- in 1920s synthesized similar chemical: amphetamine, patented in 1932
- First use: ASTHMA replacement for ephedrine (potent dilator for nasal and bronchial passages, efficiently delivered through inhalation)
- Stay awake and study longer: students and truck drivers; Adderall
- Narcolepsy
- Appetite suppression
- Hyperactivity in children
Wartime: WWII used to improve soldier efficiency (Germans first)
Misuse in 60s: became widespread after WWII, legally manufactured oral preparation, realized that you could get similar cocaine effect if injected heroin + amph “speed”; widely available and cheap to use with heroin or alone. Not hard to get prescription
Most desired: methamphetamine (liquid or ampules for injection; used to be used to stimulate breathing in sleeping pill OD patients, sometimes injected to treat obesity
Use grew in 60s, by 70s restrictions were in place, associated with drug-abusing hippies
REACTIONS
- Rise in cocaine use
- Rise in illicit meth labs (meth called “cranks”)
- relative ease, synthesis difficult, so crank often very impure, many chemicals more toxic
1990s “smoking” crystal meth
- meth in more rural areas – Honolulu, midwest
- cocaine in cities
Adderall
mixture of amphetamine salts used to treat ADHD
Amphetamines Chemical Structure
- similar structure to catecholamine neurotransmitters, produces its effects bc recognized as catecholamine in CNS and PNS
- the methyl group allows to BBB more readily, increasing CNS potency
- increase activity of monoamine neurotransmitters by stimulating release
- DOPAMINE, norepinephrine, serotonin
- more potent releaser of norepinephrine (NE most likely causes euphoria)
Amphetamines Forms
intravenous, smoked, intranasal, oral
intravenous and smoked: 5-10 mins
intranasal: 5-20 mins
oral: 1.5 hrs
Amphetamines Metabolism
Half life: 5-12 hrs
Complete elimination: 2-3 days
Effect of high amphetamine dosage
Tachyphylaxis
- (rapid tolerance)
- produce effects by displacing/releasing neurotransmitters from their storage sites, monoamines may be depleted with large doses, resulting in reduced effect
Amphetamine Beneficial Uses
- Depression
- in 1950s were TOC for depression and fatigue; stigmatized in 60s, use decreased
- used for depression only in adjunctive therapy (used to assist primary treatment)
- ADV: antidepressant effects within 1-2 days
- potential for abuse, although little evidence in controlled trials - Weight Control
- 60s most common use was weight control
- reduce appetite and food intake (few weeks, short term) - Narcolepsy
- ADHD (Ritalin –> increases catecholamine activity in response to deficit)
- suppresses height and weight gain - Reduces shift-related disruptions
- reduce performance effects
- fatigue and sleep deprivation
Adjunctive Therapy
- Treatment used to assist primary treatment
- Amphetamines
Amphetamine Addiction
- Was not thought to produce “withdrawal” therefore soft
- Oral by prescription «_space;intravenous to get high
- Addiction depends on dose, route, and reason for use
Table 6.1
- Federal cocaine offenders
- powder:
- crack:
while % were roughly comparable in powder situations (usually mostly hispanic) there was HUGEly disproportionately high for black crack situations (always 80s/90s)
Cocaine Individuals
- Mariani - coca wine, other coca products
- Halsted - local anesthesia
- Freud - psychiatric uses, withdrawal
unintentional and intentional CODs (respiratory depression) 5. Meprobamate - patented in 1952, thought to be new CNS depressant - FDA approved in 1955 --> wide use - also produced same dependence 6. Methaqualone - wide search of better hypnotic (sleeping pill) - synthesized in India for sedative properties - Germany introduced it in 1962, changed status when 10-20% of people misusing and ODing - marketed in US in 1965, "ludes" "supors" qualades, by 1985 no longer available for prescription, now sched 1 7. Benzodiazepine - Librium marketed in 1960s as a more selective "antianxiety" that produced less drowsiness and OD - no dependency/OD, much safer than barbiturates - Replaced with Valium in 1970s - important difference in DOSE AND TIME COURSE OF DRUG TAKING (not chem class)