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Neuro Week 7 > CNS Stimulants > Flashcards

CNS Stimulants Flashcards

1
Q

amphetamines mechanism

A

Release monoamines, primarily NE and DO from nerve terminals in brain

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2
Q

amphetamines are substrates for

A

neuronal monoamine uptake transporters NET and DA (not SERT)

–> competitive inhibition of DA and NE reuptake

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3
Q

amphetamines mechanism once in nerve terminal

A

enter sympathetic nerve ending and displace stored NE and DE from vesicles –> cytoplasm
– release NE and DA out of DAT and NET in reverse

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4
Q

Effects of amphetamines

A

locomotor stimulation, euphoria and excitement, insomnia, increased stamina (mental and physical fatigue reduced), anorexia ( food intake returns to normal with continued administration)

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5
Q

AE amphetamines

A

Anxiety, irritability, restlessness
high dose- panic, paranoia
psychotic symptoms, anxiety, depression, cognitive impairment

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6
Q

peripheral effects amphetamines

A

sympathomimetic - rise in BP, inhibit GI motility

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7
Q

Locomotor and rewarding effects of amphetamines driven by

A

DA release
inhibited by destruction of DA containing nucleus accumben
inhibited by D2 receptor antagonists

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8
Q

amphetamine psychosis

A

acute schizophrenic attack - hallucinations, paranoia, aggressive behavior
repetitive stereotyped behavior

antipsychotics = effective tx

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9
Q

when amphetamine drug stopped

A

period of deep sleep
upon waking, feel lethargic, depressed, anxious, hungry

result of DA and NE depletion? recovery?

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10
Q

amphetamines tolerance

A

devleops rapidly to euphoric and anorexic effects, but slowly to other

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11
Q

amph dependence

A

strong psychological: insistent memory of euphoria
no clear-cut physical withdrawal syndrome
increase dose –> then uncontrolled binges –> high risk of acute toxicity

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12
Q

PK amph

A 
GI absorb
snorted or injected
smoked in crystal form
freely penetrate BBB
mainly excrete in urine (unchanged)
5-30 hrs, depending on urine flow and pH
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13
Q

methylphenidate name

A

ritalin (amph like)

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14
Q

ritalin mechanism

A

elevation of ec NE and DA

inhibits NET and DAT transporters (not a substrate of transporters - does not enter nerve terminal)

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15
Q

PK ritalin

A

orally active, absorbed in intestine and colon
presystemic metabolism - only 20% enter systemic
slow absorption
half life 2-4 hrs

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16
Q

clinical use ritalin

A

ADHD

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17
Q

modafinil mechanism

A

increase Ec DA levels in striatum and nucleus accumbens

likely inhibits DA reuptake by binding DAT

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18
Q

other effects madafinil

A

enhanced release of 5-HT, glutamate, histamine

inhibition of GABA release

19
Q

PK modafinil

A

gut absorb, metabolized in liver, half life 10-14 hrs

20
Q

uses modafinil

A

ADHD (adults, kids get rash), narcolepsy
shift work sleep disorder
excessive daytime sleepiness from sleep apnea

“wakefulness promoting agent”, enhance cognitive performance,

21
Q

MDMA

A

ecstasy

3,4-methylenedioxymethamphetamine, or MDMA

22
Q

MDMA effects

A

euphoria, loss of inhibitions, energy surge
stimulant + mild hallucinogenic effects
psychomimetic -affect thought, perception and mood (dream like)

23
Q

Potential use of MDMA

A

feelings of empathy and emotional closeness to others (empathogen) – useful in PTSD? depression?

24
Q

MDMA mechanism

A

inhibits monoamine transporters, principally the 5-HT transporter
Also releases 5-HT –> large increase in free 5-HT in certain brain regions (psychotomimetic)
similar changes occur in DA and NE (initial euphoria and later rebound dysphoria)
Followed by period of monoamine depletion

25
Q

AE MDMA

A

sudden illness and death can occur even after small doses of MDMA
acute hyperthermia –> damage to skeletal muscle and consequent renal failure

excess water intake and water retention (MDMA –> release ADH)

heart failure in undiagnosed heart conditions

26
Q

after effects mdma

A

depression, anxiety, irritability, increased aggression

evidence of long-term deleterious effects on memory and cognitive function in heavy mdma users

27
Q

cocaine mechanism

A

binds to and inhibits transporters NET, DAT, SERT (reuptake)

28
Q

cocaine effects

A

euphoria, chattiness, increased motor activity, magnification of pleasure

29
Q

cocaine vs amphetamines

A

Effects similar to amphetamines

less tendency to produce stereotyped behavior, delusions, hallucinations and paranoia

30
Q

peripheral sympathomimetic actions cocaine

A

tachycardia
vasoconstriction
increase in blood pressure
body temperature may increase –> motor activity coupled with reduced heat loss

31
Q

overdose cocaine

A

tremors and convulsions

respiratory and vasomotor depression

32
Q

cocaine dependence

A

strong psych dependence - crave euphoria and stimulatory effects
inc. dose, binges

33
Q

tolerance cocaine

A

debatable

34
Q

withdrawal cocaine

A

no clear-cut withdrawal syndrome

depression, dysphoria, fatigue

35
Q

PK

A 
readily absorbed many routes
nasal inhalation 
crack cocaine - smoked
~30 min affect
metabolized in liver
used as local anesthetic
36
Q

AE cocaine

A

Serious cardiovascular events
Cardiac dysrhythmias
Aortic dissection
Myocardial or cerebral infarction or hemorrhage
Progressive myocardial damage can lead to heart failure, even in the absence of a history of acute cardiac effects
Dependence

37
Q

cocaine in utero

A

brain size reduce, neuro and limb malformations increased, incidence of ischemic/hemorrhagic brain lesions and SIDS

38
Q

methylxanthines

A

tea, coffee, cocoa
mild central stimulant effects

caffeine and theophylline

39
Q

methylxanthines effects

A

CNS stimulation
Diuresis
stimulation of cardiac muscle
relaxation of smooth muscle, bronchial muscle

40
Q

MX effects on cardiac and smooth muscle resembe

A

beta-adrenoceptor stimulation
inhibit phosphodiesterase –> increase intracellular cAMP –> effects that mimic mediators that stimulate Adenylyl cyclase

41
Q

stimulant mech MX

A

antagonize many effects of adenosine - acting on both A1 and A2 adenosine receptors (A2 more important)

42
Q

diuretic mech mx

A

The diuretic effect probably results from vasodilatation of the afferent glomerular arteriole, causing an increased glomerular filtration rate.

43
Q

clinical uses MX

A

aspirin
ergotamine in migraine
alertness
respiratory stimulants in treatment of apnea in premature babies
theophylline - bronchodilator in asthma attacks

Neuro Week 7 (6 decks)

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