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Pharm Exam 3 > CNS Stimulants > Flashcards

CNS Stimulants Flashcards

1
Q

CNS stimulus - main characteristics:

A

1) increase
- alertness/awareness
- productivity and motivation
- arousal, locomotion, HR, BP
- euphoria
- nervousness and anxiety
2) decrease requirement for sleep and food
3) overdose = convulsions and death

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2
Q

Name the analeptic and respiratory stimulant drug?

A

Doxapram

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3
Q

Doxapram

  • what type of drug?
  • does what to body?
  • MOA?
A
  • analeptic & Resp stimulant drug
  • *-respiratory stimulant used to counteract postanasthetic respiratory depression
  • binds to carotid chemoreceptors and medullary respiratory centers to increase tidal volume and respiratory rate
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4
Q

methylxanthine- list drugs?

A

caffeine

theophylline

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5
Q

Taking patient off a ventillator give what drug to help with breathing?

A

doxapram

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6
Q

general effects of methylxanthines?

A
  • -mild CNS and respiratory stimulants

* *-bronchodilators - for asthma

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7
Q

caffeine

  • what type of drug?
  • *-primary treatment for?
  • some effects?
A
  • methylxanthine - CNS stimulant
  • **-tx for apnea of premature infants or breathing cessation in premature infants
  • fighs off drowsiness/restores alertness
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8
Q

Theophylline

  • what type of drug?
  • *-Use?
A
  • methylxanthine - CNS stimulant

* *-used for COPD, asthma, and apnea of prematurity

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9
Q

Name the sympathomimetic amide drugs? (psychomotor stimulants)

A

1) amphetamine & derivatives
a) methamphetamine
b) dexamphetamine
c) methylphenidate
2) cocaine
3) modafinil
4) atomoxetine (NE reuptake inh)

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10
Q

What is MOA for atomoxetine?

A

NE reuptake inh

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11
Q

Name the stimulant drugs used to treat ADHD?

A
  • methylphenidate
  • amphetamine salts
  • dextroamphetamine
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12
Q

Name the non-stimulant drugs used to treat ADHD?

A
  • atomoxetine
  • clonidine
  • modafinil
  • Antidepressants (TCAs, MAOIs, bupropion)
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13
Q

metabolism of CNS stimulants

  • what enzyme?
  • where?
  • anything interesting about metabolites?
A
  • uses MAO_A and MAO_B
  • liver degredation
  • many precursor drugs metabolized into active drugs
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14
Q

What drugs should you not give with CNS stimulants?

A

(antidepressants) MAOIs and SSRI = results in increased levels monoamines

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15
Q

How are most CNS stimulants excreted?

A

urine

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16
Q

How long does effect of CNS stimulants last? What is dosing like?

A

duration time is short

requires multiple doses or extended release formulas

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17
Q

Analeptic stimulant drugs - MOA?

A
  • depression of inhibitory neurotransmission (DISINHIBITION)
  • GABA_A and glycine antagonists (dec Cl influx = hyperpolarization)
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18
Q

Methylxanthine drugs - MOA?

A
  • inh of CNS suppressnat

- reduce adenosine activity (CNS suppressany-neuroprotective) by A1 receptor antagonism

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19
Q

Amphetamine drugs -MOA?

A
  • COMPETITIVELY INH DAT AND INC SYNAPTIC DA
  • INTERFERE WITH VESICULAR MONOAMINE TRANSPORTER (VMAT) = VESICLES ARE DEPLETED AND SYNAPTIC DA INCREASES
  • enhancement of excitatory transmission
  • stimulate pre synaptic release from storage vesicles (DA,NE)=inc synaptic catecholamine levels
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20
Q

cocaine - MOA?

A

INH DOPAMINE TRANSPORTER (DAT) AND INC SYNAPTIC DA

  • enhancement of excitatory transmission
  • inh of monoamine uptake via blockade of DA, NE and 5-HT transporters (DAT,NET,SERT)=affect reward circuitry similar to amphetamines
21
Q

Atomoxetine drugs -MOA?

A
  • enhancement of excitatory transmission

- selective NE transport blockade

22
Q

**Whcih drug used for narcolepsy and sleep disorders?

A

**modafinil

23
Q

Which drug used for ADHD?

A

methylphenidate

24
Q

**Drug used to treat obesity?

A

**orlistat

25
Q

Why are CNS stimulants used in obesity?

A

anorexia side effect- suppressed appetites (anorexiants)

26
Q

Orlistat MOA?

A

lipase inh = dec GI fat absorption

results in GI effects- steatorrhea, fecal incontinence, flatulence

27
Q

3 legal uses of amphetamine:

A
  • narcolepsy
  • ADHD
  • short-term weight loss
28
Q

What “schedule” controlled substance is amphetamine?

A

schedule II

29
Q

What “schedule” controlled substance is cocaine?

A

schedule II

30
Q

What area of the brain does the cocaine effect?

A

Ventral tegmental area (VTA) –> reward circuitry of the brain (HOME OF DA NEURONS)

31
Q

***PSychomotor stimulants: CNS side effects

A 
euphoria
dysphoria
insomnia
iritability
tremor
headache
loss of appetitie
32
Q

**Psychomotor stimulants: Cardiovascular side effects:

A
  • MI

- cerebrovascular accident (CVA) =stroke

33
Q

**Psychomotor stimulants: Endocrine/metabolic side effects?

A

anorexia

severe weight loss

34
Q

***Which drug has an uncommon side effect of inc suicide risk esp in children?

A

atomoxetine

35
Q

Uncommon side effect for modanafil?

A

skin rash

stevens-johnson syndrome

36
Q

Which drugs impairs liver function?

A

atomoxetine

37
Q

Long term safety of psychomotor stimulants?

A
  • some effect of growth in males
  • sometimes get more tics in susceptible patients (tourettes or other)
  • cardiovascular-sometimes inc BP and HR
38
Q

two diagnostic/symptoms for ADHD?

A

Present for at least 6 months

1) inattention
2) impulsivity/hyperactivity

39
Q

3 types of ADHD diagnoses:

A

1) ADHD predominantly hyperactive
2) ADHD predominantly inattentive
3) ADHD combined type

40
Q

**shift in symptoms for kids to adults:

A

kids:

  • motoric hyperactivity
  • aggressiveness
  • low frustration tolerance
  • impulsiveness
adults:
-shifts activities
-easily bored
-impatient
restlessness
41
Q

Pathophys of ADHD - which brain lobe is affected?

A

-frontal lobe dysfunction (executive function area)

42
Q

What is the dopamine deficit hypothesis of ADHD?

A

Mutliple possibilities! environ/genetic/neurochem/CNS insults…

  • dorsal lateral prefrontal cortex (PFC) lacks DA
  • the PFC projects to anterior cingulate cortex = integration of inattentiveness and regulation of emotions
43
Q

**ADHD CNS Stimulant drugs? **Which is main?

A
  • methylphenidate (MAIN)
  • amphetamine salts
  • dextroamphetamine
44
Q

Second line drugs to treat ADHD?

A
  • atomoxetine - no abuse potential
  • clonidine
  • modafinil
  • antidepressants (TCAs, MAOI, bupropion)
45
Q

**Drug approved for narcolepsy?

A

modafinil - not to be used in children

also can use methylphenidate (ADHD drug)

46
Q

Atomoxetine

  • used for?
  • mechanism?
A
  • second line ADHD

- selective NE re-uptake block

47
Q

Clonidine

  • used for?
  • MOA?
A
  • second line ADHD

- alpha2 agonist = inc blood flow to prefrontal cortex

48
Q

Modafinil

  • used for?
  • mechanism?
A
  • second line ADHD (not in children - bc of skin rash/Stevens johnson syndrome)
  • sleep disorders (narcolepsy)

-activates histamine neurons in tuberomammillary nucleus (TMN) of hypothalamus

49
Q

side effects of ADHD treatment?

A

decreased appetite
WL
insomnia

Pharm Exam 3 (11 decks)

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