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NRO > CNS Stimulants > Flashcards

CNS Stimulants Flashcards

1
Q

List the amphetamines (3)

A

i) DL-amphetamine (Adderall, Speed)
ii) Dextroamphetamine (More potent D-isomer of amphetamine, Dexedrine)
iii) Methamphetamine (Crystal meth)

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2
Q

Amphetamines release monoamines, primarily __________and _________, from nerve terminals in the brain

A

norepinephrine, dopamine

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3
Q

i) NET =

A

norepinephrine transporter

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4
Q

ii) DAT =

A

dopamine active transporter

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5
Q

__________ Enter the sympathetic nerve ending and displace stored NE and DA
i) “Displacer” effect – NE and DA released

A

Amphetamines

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6
Q

_____________At high concentration – Inhibit monoamine oxidase (MAO)
[MAOs break down DA and NE]

A

Amphetamines

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7
Q

The main central effects of amphetamine-like drugs are

A

Locomotor stimulation, Euphoria and excitement, Especially intense with IV injection, Insomnia, Increased stamina, Anorexia

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8
Q

c) Amphetamine Peripheral sympathomimetic effects – rise in _____________, inhibition of ______________

A

blood pressure, gastrointestinal motility

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9
Q

Amphetamine stimulant effect lasts for a few hours, followed by ______ and ______

A

depression and anxiety

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10
Q

i) If amphetamines taken repeatedly over a few days
ii) Resembles an acute schizophrenic attack – hallucinations, paranoia and aggressive behavior
iii) Repetitive stereotyped behavior may develop

A

Amphetamine psychosis

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11
Q

develops rapidly to euphoric and anorexic effects of amphetamines, but more slowly to the other effects.

A

Tolerance

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12
Q

No clear-cut physical withdrawal syndrome

A

6) Amphetamines

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13
Q

a) Readily absorbed from the gastrointestinal tract
b) Can be snorted or injected
c) Smoked in crystal form (crystal meth)
d) Freely penetrate the blood–brain barrier
e) Mainly excreted unchanged in the urine
f) The plasma half-life of amphetamines varies from 5 to 30 hours, depending on urine flow

A

7) Amphetamines PharmacokinetiCs

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14
Q

a) Profound and sustained elevation of extracellular NE and DA
b) Inhibits the NET and DAT transporters
i) (Also inhibits SERT, but with much lower potency)
c) NOT a substrate for NET/DAT transporters –> does not enter the nerve terminals to facilitate NE and DA release
d) Orally active, absorbed from the intestine and colon

A

Methylphenidate (Ritalin)

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15
Q

Methylphenidate (Ritalin) Clinical use:

A

e) Clinical use: attention deficit/hyperactivity disorder (ADHD)

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16
Q

a) Increases extracellular DA levels in striatum and nucleus accumbens
i) Likely inhibits DA reuptake by binding to DAT
b) Other effects:
i) enhanced release of 5-HT, glutamate and histamine
ii) inhibition of GABA release
c) Well absorbed from the gut, metabolized in the liver and has a half-life of 10–14 h.

A

9) Modafinil

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17
Q

d) Used in treatment of narcolepsy
e) Promoted as a ‘wakefulness promoting agent’ rather than a classic amphetamine-like stimulant
f) Reported to ‘brighten mood’
g) Claimed to enhance cognitive performance
h) Effective treatment for ADHD in adults
i) No euphoria when administered by mouth

A

9) Modafinil

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18
Q

a) 3,4-methylenedioxymethamphetamine, or MDMA
b) Widely used as a party drug
c) Euphoria, loss of inhibitions, and energy surge that it induces
d) Stimulant + mild hallucinogenic effects

A

Psychotomimetic

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19
Q

e) ______________- affect thought, perception and mood

i) Thoughts and perceptions become distorted and dream-like, rather than being merely sharpened or dulled

A

Psychotomimetic

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20
Q

e) Psychotomimetic

f) Feelings of empathy and emotional closeness to others (empathogen)

A

10) MDMA (Ecstasy)

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21
Q

a) An amphetamine derivative
b) Inhibits monoamine transporters, principally the 5-HT transporter
c) Also releases 5-HT
d)  large increase in free 5-HT in certain brain regions
i) Similar changes occur in with DA and NE
e) Followed by monoamine depletion

A

11) MDMA Pharmacological Effects

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22
Q

j) Sudden illness and death can occur even after small doses of MDMA. This can be due to several factors:

A

Acute hyperthermia
Excess water intake and water retention
heart failure

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23
Q

d) The stimulant effects have not proved to be clinically useful
i) But have led it to becoming a widespread drug of abuse.

A

12) Cocaine

24
Q

Cocaine Pharmacological Effects

A

a) Binds to and inhibits the transporters NET, DAT and SERT
i) marked psychomotor stimulant effect
ii) enhances the peripheral effects of sympathetic nerve activity
b) Euphoria, chattiness, increased motor activity, magnification of pleasure
c) Users feel alert, energetic and physically strong and believe they have enhanced mental capabilities

25
Q

d) Effects similar to amphetamines

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

A

13) Cocaine Pharmacological Effects

26
Q

13) Cocaine Pharmacological Effects: e) Euphoric effects involve inhibition of both ___ and ____ reuptake

A

DA and 5-HT

27
Q

Cocaine peripheral sympathomimetic actions

A

tachycardia
vasoconstriction
increase in blood pressure

28
Q

g) Body temperature may increase, owing to the increased motor activity coupled with reduced heat loss.

A

13) Cocaine Pharmacological Effects

29
Q

h) Overdose:
i) tremors and convulsions
ii) respiratory and vasomotor depression

A

Cocaine

30
Q

c) No clear-cut withdrawal syndrome

i) Depression, dysphoria and fatigue may be experienced following the initial stimulant effect

A

Cocaine

31
Q

readily absorbed by many routes

b) Hydrochloride salt: nasal inhalation or IV
i) Intense and immediate euphoria with IV
ii) Nasal inhalation less dramatic
(1) Atrophy and necrosis of the nasal mucosa and septum.

A

Cocaine

32
Q

e) Rapidly metabolized in the liver

f) Occasionally used topically as a local anesthetic

A

Cocaine

33
Q

exposure during pregnancy – in utero impact

i) Brain size is significantly reduced
ii) Neurological and limb malformations are increased
iii) Incidence of ischemic, hemorrhagic brain lesions, and SIDS, also higher in cocaine-exposed babies

A

Cocaine

34
Q

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

A

Cocaine

35
Q

a) Tea, coffee and cocoa
b) Mild central stimulant effects
c) Main compounds caffeine and theophylline

A

17) Methylxanthines

36
Q

a) Methylxanthines have the following major pharmacological actions:

A

i) CNS stimulation
ii) Diuresis
iii) Stimulation of cardiac muscle
iv) Relaxation of smooth muscle, especially bronchial muscle

37
Q

i) inhibit phosphodiesterase

ii) Block PDE, increase intracellular cAMP  effects that mimic those of mediators that stimulate adenylyl cyclase

A

methylxanthines

38
Q

c) Antagonize many of the effects of adenosine, acting on both A1 and A2 adenosine receptors

A

methylxanthines

39
Q

d) The diuretic effect of methylxanthines probably results from vasodilatation of the afferent glomerular arteriole, causing an increased _________________

A

glomerular filtration rate

40
Q

19) Methylxanthines Clinical use

A

b) Effective respiratory stimulants in the treatment of apnea of prematurity
i) Developmental disorder caused by immaturity of central respiratory control
ii) Caffeine is preferred to theophylline because of its long half-life and safety
c) Theophylline is used mainly as a bronchodilator in treating severe asthmatic attacks.
d) Mutagenic activity in vitro, and large doses are teratogenic in animals

41
Q

CLINICAL USES OF CNS STIMULANTS: b) Attention deficit/hyperactivity disorder (ADHD):

A

i) Amphetamines
ii) Methylphenidate
iii) Modafinil

42
Q

20) CLINICAL USES OF CNS STIMULANTS: c) Narcolepsy

A

modafinil for the excessive sleepiness

43
Q

20) CLINICAL USES OF CNS STIMULANTS:d) Apnea of prematurity

A

xanthine alkaloids (under expert supervision in hospital) are effective; caffeine is preferred to theophylline

44
Q

rare, disabling sleep disturbance

i) Sudden, unpredictable sleep during day
ii) Nocturnal insomnia
iii) Often accompanied by cataplexy
(1) abrupt onset of paralysis of variable extent often triggered by emotion, sometimes with ‘frozen’ posture
iv) Amphetamine is helpful but not completely effective
v) Modafinil is also effective in reducing the need for sleep

A

e) Narcolepsy

45
Q

Catecholamine release, inhibition of catecholamine uptake

A

Amphetamines

46
Q

Dexamphetamine used for ADHD; narcolepsy; otherwise important as drugs of abuse

A

Amphetamines

47
Q

Inhibition of catecholamine uptake

A

Methylphenidate

48
Q

ADHD

A

Methylphenidate

49
Q

Unclear, likely inhibits DA uptake

A

Modafinil

50
Q

Reduce fatigue, enhance cognition

A

Modafinil

51
Q

Inhibition of catecholamine uptake; also a local anesthetic

A

Cocaine

52
Q

Occasionally for nasopharyngeal or opthalmic anesthesia; otherwise important drug of abuse

A

Cocaine

53
Q

Inhibition of phosphodiesterase, antagonism of adenosine A2 receptors

A

Methylxanthines

caffeine and theophylline

54
Q

Widely consumed in beverages, some clinical use unrelated to CNS stimulation (cardiac and bronchial actions)

A

Methylxanthines

caffeine and theophylline

55
Q

5-HT release and blocks reuptake

A

MDMA

56
Q

Nothing currently, potential in PTSD and depression; important as drug of abuse

A

MDMA

NRO (22 decks)

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