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14 Cards in this Set

  • Front
  • Back

Amphetamines

•Synthetic


•Parent compound of a family of synthetic psycho stimulants structurally related to dopamine


•Benzedrine is L-amphetamine


•Dexedrine is D-amphetamine

Amphetamines (70s Decline)

Gov forced companies to decrease production


•Amount of approved medical uses decreased


•Physicians and public became more educated about them


•More specific drug treatment for depression


Cocaine replaced amphetamine as the main recreational drug

Amphetamines (Compounds)

Least to most potent:


•L


•DL


•D


•Meth


•Crystal Meth

Amphetamines (Mode of Action)

•Indirect agonists of catecholaminergic systems


•Two actions


1. The molecules enter dopamine nerve terminals via uptake by dopamine transporters and cause vesicles to release DA


2. The dopamine transporters are then reversed, causing the DA to be transported out of the cell


•(In high doses: block MAO)

Nonamphetamine behavioral stimulants

•Methylphenidate (Ritalin)


•Pemoline (Cylert)


•Sibutramine (Meridia)


•Modafinil

Amphetamines (Uses)

•1932-1970s


•Current


ADHD (helps 75% of patients)


Narcolepsy (repeatedly falling asleep)


Short term weight reduction (tolerance increases in 4 weeks)

Amphetamines (Effects)

•Autonomic - sympathomimetic




•CNS – behaviorally reinforcing psychomotor stimulant




•High dose – paranoid psychosis

Amphetamines (Autonomic [Physical] Effects)

Sympathomimetics:


•Increase blood pressure


•Increase blood flow


•Relaxe bronchial muscle


•Increase rate of respiration


•Dilate pupils


•Enhance athletic performance


•Highly reinforcing through enhancement of the medial forebrain bundle

Amphetamines (CNS [psychological] Effects)

•Heighten alertness


•Reduce fatigue


•Feelings of exhilaration


•A generalized sense of well-being


•Increase confidence


•Sustained physical effort without rest


•Delay in sleep onset


•When stop taking: rebound sleep (sleep more)

Amphetamines (High Dose Effects)

•Stimulate mesolimbic dopamine pathway-> similar symptoms to schizophrenia


•Psychotic reactions


•Visual & auditory hallucinations


•Behavioral disorganization


•Development of a paranoid state with delusions of persecution

Amphetamines (Ice: Meth hydrochloride crystalline form)

•Smoked


•Easily made from commercially available material (sedated)


•Purity depended on the route of synthesis (20-90%)


•$700 investment = $225,000 street value


•1989, the #1 drug problem in Hawaii


•Originally manufactured in South Korea and Taiwan

Meth (Behavioral/Neural Effects)

•Meth causes damage to DA axons and terminals


•Main mechanism for the neurotoxicity is oxidative stress:


•Since meth causes DA to leak out of vesicles, DA is oxidized in the cytoplasm of the neuron. It loses an Electron and becomes a free radical that steals an electron from the lipid membrane, causing oxidative stress. This kills the axon ending.


•Ex chronic users have decreased DA in:


Basal ganglia (movement)


Frontal cortex (executive functioning)


Nucleus accumbens (reward)

Cocaine (History/Research)

•Comes from Coca in South America


•Albert Leimen – Created cocaine


•Use started in 1800s




•Freud 1


–Reduces hunger, sleep, fatigue


–Therapeutic uses: Stimulant, digestion, cachexia (wasting disease of CNS), alcohol/morphine addiction, asthma, aphrodisiac, local anesthetic


–Did not find tolerance, dependence, psychosis, and withdrawal symptoms




•Freud 2


–Should not be used for morphine addiction


–Misuse of cocaine is worse than misuse of morphine




•William Holsted – used cocaine as nerve block (regional anesthetic)

Drugs are stabilized as salts

•Bases and acids neutralize each other


•To a base, an acid is added, such as hydrochloric acid


•To an acid, a base is added, such as sodium hydroxide