Chapter 6 - Psychostimulants Flashcards

1
Q

What do sympathomimetics do?

A

increase sympathetic NS activity; inc motor activity; improve alertness; elevate mood
ex. amphetamine, methamphetamine; cocaine

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2
Q

medical vs non medical purposes of sympathomimetics

A

decongestant, ADHD, narcolepsy VS meth, crack, cocaine

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3
Q

First natural amphetamines were derived from ____ and was used as ____

A

Ephedra (ephedra sinica); cough suppressant (16th century China) and was a precursor for the illicit manufacture of methamphetamine

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4
Q

Amphetamine was developed by ____ and was used to ____

A

German chemists in 1887; inc BP (20s), treat adhd (30s) and in WWII

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5
Q

Two optical isomer forms of amphetamines

A

d-amphetamines and l-amphetamines; d is more potent

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6
Q

Racemic mixtures of amphetamines

A

contains both d- and l- isomers
ex. adderall contains 3:1 of d- to l-
-mostly used for narcolepsy and ADHD; less military use

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7
Q

Methamphetamine was developed by ____ and is mainly used ____

A

a JPN chemist in 1919; illicitly (notorious drug of abuse) but was recently approved by FDA as treatment for ADHD (Desoxyn)

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8
Q

Methylphenidate

A

relatively weaker psychostim; discovered in 1944 (Ritaline); prescribed to more than 2/3 US kids with ADHD

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9
Q

Cathinones

A

bath salts (new drugs, 90s); synthetic cathinone compounds

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10
Q

what is cocaine?

A

derived from Erythroxylon coca; salt/powder form is called cocaine hydrochloride
-crack cocaine is formed when hydrochloride is freed from base with baking soda

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11
Q

For therapeutic effects, psychostimulants are usually administered ____

A

orally (pills); however methylphenidate sometimes liquid and skin patch form

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12
Q

Why do users (for rewarding effects/illicit use) prefer intravenous injection/insufflation/inhalation?

A

these routes guarantee rapid absorption
inhalation: 1.4min
IV: 3.1min
Insufflation: 14.6min

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13
Q

The ____, the more likely is it for addiction to occur

A

quicker the route of administration

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14
Q

There are active metabolites for ___, ____, and ____

A

mathamphetamine, cathinone, and cocaine
-often have similar effects as original drug

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15
Q

____ use can also result in stronger active metabolites

A

polydrug
ex. cocaine and alcohol produces the metabolite cocaethylene which has greater rewarding properties than either drug alone

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16
Q

half lives of psychosimulants

A

methamphetamine = 11 hours
amphetamine = 10 hours
methylphenidate – 2.5 hours
cathinone = 1.5 hours
cocaine = 1 hour

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17
Q

amphetamine and methamphetamine increases DA levels in the synapse by 1. ____ and 2. ____

A
  1. reversing the direction of DA transporters found on the presynaptic cell
  2. displacing DA from synaptic vesicles which allows more DA to be released through the reversed transporters
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18
Q

pharmacodynamics of methylphenidate and cathinones

A

similar to amphetamine and methamphetamine; inc levels of monoamines DA, 5HT, NE; less efficacy than amphetamine

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19
Q

Does cocaine block dopamine reuptake?

A

yes (of all monoamines incl DA); incr the movement of DA into synaptic vesicles so that there is more DA stored for future release

20
Q

at a sufficiently high dose, cocaine can act as a ____ which explaines why it can act as a ____

A

Na+ channel; local anesthetic

21
Q

DA levels in the ____ are important for reinforcing the properties of ____

A

nucleus accumbens; psychostimulant drugs

22
Q

What is CART?

A

Cocaine- and Amphetamine- Regulated Transcript; a peptide NT produced with use of psychostimulants; synthesized and stored in mesolimbic and tuberinfundibular DA pathways

23
Q

BY ITSELF, CART ___ DA and acts as a ____

A

increases; psychostimulant

24
Q

When CART is given in combination with a psychostimulant, it ____

A

reduces the effect of a psychostimulant

25
Q

What system do psychostimulant drugs produce most of their effects on?

A

Sympathetic NS (vasoconstriction, pupil dilation, etc)
-can also act an an anorectic

26
Q

How do low doses of psychostimulants effect behaviour?

A

increases purposeful behaviour; effects are dependent on pre drug rates; incr low baseline behaviour activity BUT decr high rates of baseline behaviour activity (thats why it can treat ADHD)

27
Q

How do high doses of psychostimulants effect behaviour?

A

increases purposeless behaviour
-produces stereotypies in rats: repetitive grooming, head swaying, licking, etc
-produces punding in humans: repetitive teeth grinding, tapping, skin picking, nail biting

28
Q

Subjective effects of low doses

A

increased alertness, energy, well-being, enthusiasm; used to treat narcolepsy

29
Q

Subjective effects of high doses

A

produces a “rush” and euphoria (very rewarding effect) especially with rapid absorption

30
Q

Tolerance of drugs

A

more pronounced for reinforcing effects of the drug (less high); occurs more often with continuous drug use

31
Q

Sensitization to drugs

A

cravings may become more powerful as the incentive value of drug-related stimuli increases; increase in purposeless behaviours; associated with intermitted drug use

32
Q

Cardiovascular effects (adverse effects of psychostimulant use)

A

enhanced sympathetic NS activation, constricts blood vessels and increases HR
-hypertension, stroke, aortic rupture, heart attack

33
Q

Abnormal fetal development (adverse effects of psychostimulant use)

A

blood vessel constriction, blood flow to fetus is reduced, limited O2 and nutrient delivery

34
Q

Pulmonary dysfunction (adverse effects of psychostimulant use)

A

injury during inhalation; hemorrhaging; edema; tissue inflamation

35
Q

diseases associated with IV use (adverse effects of psychostimulant use)

A

HIV, HEP, TB

36
Q

Meth mouth (adverse effects of psychostimulant use)

A

toothy decay; caused by poor dental hygiene, damage to gums, decreased salivation

37
Q

psychostimulant-induced psychosis (adverse effects of psychostimulant use)

A

similar to schizophrenia (paranoia, delusions, agitation); tactile hallucinations (formication); sometimes visual hallucinations

38
Q

psychostimulant withdrawal

A

primarily occurs from psychological dependence rather than physical dependence
-psychostimulants produce incr in activity/enjoyment/euphoria, withdrawal can produce lethargy, lack of joy (anhedonia), and dysphoria

39
Q

Women may be more vulnerable to addiction because…

A

starting earlier in life; more likely to binge; develop dependence quicker; may be related to sex hormones or stress

40
Q

Disulfiram - Antabuse (treatments for psychostimulant addiction)

A

often used for treating alcoholism (inhibits aldehyde dehydrogenase); prevents DA conversion to NE (increases aversive effects)

41
Q

Modafil - Provigil (treatments for psychostimulant addiction)

A

substitution therapy (has mild psychostimulant effects); often used to treat narcolepsy

42
Q

Tricyclic antidepressants (treatments for psychostimulant addiction)

A

reduce cravings and depression

43
Q

Anticonvulsant drugs (treatments for psychostimulant addiction)

A

increases GABA; reduces conditioned responses to drugs; thought to block learned associations (weakens incentive salience)

44
Q

Psychostimulants as cognitive enhancers (college students)

A

college students have been used to improve memory, cognition, or concentration; illicit drug use since drug was not prescribed to them

45
Q

Psychostimulants elevate DA in ____ and could increase ____

A

prefrontal cortex; working memory
-psychostims enhance motivation for engaging in novel stimuli or experiences

46
Q

What is ADHD?

A

disorder characterized by attention deficits and/or hyperactivity and inability to control impulsive behaviours

47
Q

Psychostimulants treat ADHD through its ____

A

rate-dependent effects
-decrease high rates of baseline behavioural activity