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PHARM 203 > 26: Stimulants and Psychotomimetics > Flashcards

26: Stimulants and Psychotomimetics Flashcards

1
Q

central effects of amphetamines and related compounds

A 
locomotor stimulation
euphoria and excitement
insomnia
increased stamina
anorexia
anxiety, irritability, panic, paranoia
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2
Q

amphetamines and related compounds release

A

dopamine and noradrenaline from nerve terminals

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3
Q

how do amphetamines release DA and NE

A
  1. competitive inhibitors of monoamine uptake transporters DAT and NET
  2. are taken up into neuronal storage vesicles by VMAT2 and displace endogenous monoamines from vesicle into cytoplasm
  3. cytoplasmic monoamines transported out of nerve terminals by DAT and NET working in reverse
  4. can inhibit MAO at high conc
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4
Q

DA and NA release caused by amphetamines cause

A

locomotor and rewarding effects

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5
Q

peripheral effects of amphetamines are generally

A

mainly sympathomimetic

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6
Q

specific peripheral effects of amphetamines

A

increase BP and HR

reduce GI motility

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7
Q

what happens when you stop amphetamines

A

deep sleep

lethargy, depression, anxiousness, hunger on wakening

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8
Q

dependence develops as

A

dose is increased

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9
Q

uncontrolled binges cause

A

high risk for acute toxicity

  • tachycardia
  • hypertension
  • hyperthermia
  • rhabdomyolysis
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10
Q

what is used for ADHD

A

dextroamphetamine

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11
Q

mephedrone is a

A

cathinone derivative

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12
Q

cathinone and cathine are active ingredients in

A

khat shrub

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13
Q

mephedrone, methedrone, and methylone are

A

cathinone derivatives that produce amphetamine like effects

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14
Q

mechanism of action for cathinone derivatives

A

increase EC levels of DA and 5HT by inhibiting their reuptake and enhancing release

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15
Q

methylphenidate is also called

A

ritalin

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16
Q

methylphenidate mechanism

A

inhibits NET and DAT transporters

inhibits SERT. but not as potent as NET and DAT

17
Q

modafinil is used for

A

narcolepsy

18
Q

mechanism of modafinil

A

blocks DAT and DA reuptake

19
Q

cocaine plant

A

south american coca shrub

20
Q

mechanism of cocaine

A

inhibits NET, DAT, and SERT

21
Q

cocaine resembles amphetamines but has less

A

stereotyped behaviour, delusions, paranoia, hallucinations

22
Q

excessive dose of cocaine causes

A

tremors, convulsions, respiratory and vasomotor depression- generally sympathetic

23
Q

2 main methylxantines

A

caffeine and theophylline

24
Q

methylxantine side effects

A

diuresis
stimulation of cardiac muscle
relaxes smooth muscle- bronchioles

25
Q

mechanism of action of methylxantines

A

antagonizes A2 receptors in brain

adenosine usually inhibits transmitter release from neurons in CNS

26
Q

methylxantines may also ___ PDEs and ____ cAMP

A

inhibit PDE
increase cAMP

explaisn stimulation of cardiac muscle and dilation of bronchial muscle

27
Q

diuretic effect of methylxantines likely due to

A

vasodilation of afferent glomerular arteriole = increased GFR

28
Q

psychomimetic drugs affect

A

thought, preception, and mood without causing psychomotor stimulation or depression

29
Q

2 classes of psychomimetic drugs

A
  1. acts of 5HT signalling

2. block NMDA receptor channel

30
Q

LSD

A

lysergic acid diethylamide

31
Q

LSD mech

A

agonist on 5HT2A receptors of the brain

32
Q

psilocybin mech

A

agonist on 5HT2A receptors on the brain

33
Q

MDMA mech

A

inhibits DA and NA reuptake + SERT

34
Q

inhibition of 5HT reuptake of MDMA is responsible for

A

psychomimetic effects

35
Q

inhibition of DA and NA reuptake with MDMA is responsible for

A

euphoria and rebound dysphoria

36
Q

mescaline is derived from

A

mexican cactus

37
Q

mescaline action

A

acts on 5HT signalline

38
Q

which 2 drugs block NMDA receptor channel

A

ketamine and phencyclidine

39
Q

PCP can cause psychotic episodes and

A

schizophrenic attacks

PHARM 203 (21 decks)

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