CNS Stimulants

Question 1

CNS stimulus - main characteristics:

Answer 1

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

Question 2

Name the analeptic and respiratory stimulant drug?

Answer 2

Doxapram

Question 3

Doxapram

• what type of drug?
• does what to body?
• MOA?

Answer 3

• 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

Question 4

methylxanthine- list drugs?

Answer 4

caffeine

theophylline

Question 5

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

Answer 5

doxapram

Question 6

general effects of methylxanthines?

Answer 6

• -mild CNS and respiratory stimulants

* *-bronchodilators - for asthma

Question 7

caffeine

• what type of drug?
• *-primary treatment for?
• some effects?

Answer 7

• methylxanthine - CNS stimulant
• **-tx for apnea of premature infants or breathing cessation in premature infants
• fighs off drowsiness/restores alertness

Question 8

Theophylline

• what type of drug?
• *-Use?

Answer 8

• methylxanthine - CNS stimulant

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

Question 9

Name the sympathomimetic amide drugs? (psychomotor stimulants)

Answer 9

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

Question 10

What is MOA for atomoxetine?

Answer 10

NE reuptake inh

Question 11

Name the stimulant drugs used to treat ADHD?

Answer 11

• methylphenidate
• amphetamine salts
• dextroamphetamine

Question 12

Name the non-stimulant drugs used to treat ADHD?

Answer 12

• atomoxetine
• clonidine
• modafinil
• Antidepressants (TCAs, MAOIs, bupropion)

Question 13

metabolism of CNS stimulants

• what enzyme?
• where?
• anything interesting about metabolites?

Answer 13

• uses MAO_A and MAO_B
• liver degredation
• many precursor drugs metabolized into active drugs

Question 14

What drugs should you not give with CNS stimulants?

Answer 14

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

Question 15

How are most CNS stimulants excreted?

Answer 15

urine

Question 16

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

Answer 16

duration time is short

requires multiple doses or extended release formulas

Question 17

Analeptic stimulant drugs - MOA?

Answer 17

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

Question 18

Methylxanthine drugs - MOA?

Answer 18

• inh of CNS suppressnat

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

Question 19

Amphetamine drugs -MOA?

Answer 19

• 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

Question 20

cocaine - MOA?

Answer 20

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

Question 21

Atomoxetine drugs -MOA?

Answer 21

• enhancement of excitatory transmission

- selective NE transport blockade

Question 22

**Whcih drug used for narcolepsy and sleep disorders?

Answer 22

**modafinil

Question 23

Which drug used for ADHD?

Answer 23

methylphenidate

Question 24

**Drug used to treat obesity?

Answer 24

**orlistat

Question 25

Why are CNS stimulants used in obesity?

Answer 25

anorexia side effect- suppressed appetites (anorexiants)

Question 26

Orlistat MOA?

Answer 26

lipase inh = dec GI fat absorption results in GI effects- steatorrhea, fecal incontinence, flatulence

Question 27

3 legal uses of amphetamine:

Answer 27

- narcolepsy - ADHD - short-term weight loss

Question 28

What "schedule" controlled substance is amphetamine?

Answer 28

schedule II

Question 29

What "schedule" controlled substance is cocaine?

Answer 29

schedule II

Question 30

What area of the brain does the cocaine effect?

Answer 30

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

Question 31

***PSychomotor stimulants: CNS side effects

Answer 31

``` euphoria dysphoria insomnia iritability tremor headache loss of appetitie ```

Question 32

**Psychomotor stimulants: Cardiovascular side effects:

Answer 32

- MI | - cerebrovascular accident (CVA) =stroke

Question 33

**Psychomotor stimulants: Endocrine/metabolic side effects?

Answer 33

anorexia | severe weight loss

Question 34

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

Answer 34

atomoxetine

Question 35

Uncommon side effect for modanafil?

Answer 35

skin rash | stevens-johnson syndrome

Question 36

Which drugs impairs liver function?

Answer 36

atomoxetine

Question 37

Long term safety of psychomotor stimulants?

Answer 37

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

Question 38

two diagnostic/symptoms for ADHD?

Answer 38

Present for at least 6 months 1) inattention 2) impulsivity/hyperactivity

Question 39

3 types of ADHD diagnoses:

Answer 39

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

Question 40

**shift in symptoms for kids to adults:

Answer 40

kids: - motoric hyperactivity - aggressiveness - low frustration tolerance - impulsiveness ``` adults: -shifts activities -easily bored -impatient restlessness ```

Question 41

Pathophys of ADHD - which brain lobe is affected?

Answer 41

-frontal lobe dysfunction (executive function area)

Question 42

What is the dopamine deficit hypothesis of ADHD?

Answer 42

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

Question 43

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

Answer 43

- methylphenidate (MAIN) - amphetamine salts - dextroamphetamine

Question 44

Second line drugs to treat ADHD?

Answer 44

- atomoxetine - no abuse potential - clonidine - modafinil - antidepressants (TCAs, MAOI, bupropion)

Question 45

**Drug approved for narcolepsy?

Answer 45

modafinil - not to be used in children also can use methylphenidate (ADHD drug)

Question 46

Atomoxetine - used for? - mechanism?

Answer 46

- second line ADHD | - selective NE re-uptake block

Question 47

Clonidine - used for? - MOA?

Answer 47

- second line ADHD | - alpha2 agonist = inc blood flow to prefrontal cortex

Question 48

Modafinil - used for? - mechanism?

Answer 48

- 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

Question 49

side effects of ADHD treatment?

Answer 49

decreased appetite WL insomnia