EXAM #3: CNS STIMULANTS Flashcards

1
Q

What endogenous molecule are most CNS stimulants chemically similar to?

A

NE

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2
Q

What will CNS stimulants increase?

A

1) Alterness
2) Productivity/ motivation
3) Arousal
4) Euphoria
5) Nervousness and anxiety

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3
Q

What will CNS stimulants decrease?

A

Requirements for:

1) Sleep
2) Food intake

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4
Q

What can overdose on CNS stimulants lead to?

A
  • Convulsions

- Death

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5
Q

What is an Analeptic?

A

Respiratory stimulants used to reverse drug-induced CNS depression (esp. post-op)

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6
Q

What is the hallmark analeptic?

A

Doxapram

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7
Q

What is the clinical utility of Doxapram?

A

This is a stimulant used to counteract anesthesia induced respiratory depression

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8
Q

What is the MOA of doxapram?

A

Binds to carotid artery chemoreceptors/ medullary respiratory centers

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9
Q

What is the common MOA of the non-doxapram analeptics?

A

GABA-A antagonists

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10
Q

What is a methylxanthine?

A

Xanthine derivative CNS/ respiratory stimulant

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11
Q

List the Methylxanthines.

A

Caffeine

Theophylline

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12
Q

What is the primary clinical indication for caffeine?

A

Apnea of prematurity

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13
Q

What is the clinical indication for Theophylline?

A

COPD/Asthma

*Drug has bronchodilator properties

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14
Q

List the Sympathomimetic Amide stimulants.

A

Amphetamine analogs:

  • Methamphetamine
  • Dexamphetamine
  • Methylphenidate

Cocaine
Modafinil
Atomoxetine

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15
Q

How are the amide psychomotor stimulants metabolized?

A

1) Monamine oxidase

2) Liver p450

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16
Q

What classes of drugs will have adverse drug-drug interactions with the psychomotor stimulants?

A

MAOI

SSRI

17
Q

What is the duration of action of many psychomotor stimulants? What are the clinical implications?

A
  • Short duration

- Multiple dosing or extended release formulas

18
Q

What is the clinical indication for Modafinil?

A

Narcolepsy/ sleep disorders

19
Q

What drug is primarily used to treat ADHD?

A

Methylphenidate (Ritalin)

20
Q

What drug was historically used for weight loss?

A

Amphetamine

21
Q

How is the drug Orlistat used clinically?

A

Weight loss

22
Q

What is the MOA of Orlistat?

A

Lipase inhibitor that decreases GI fat absorption

23
Q

What are the three approved clinical uses for amphetamine?

A

1) Narcolepsy
2) ADHD
3) Short-term weight loss

24
Q

What risk potential does cocaine have? Why?

A

Level 5 i.e. highest b/c it stimulates VTA reward pathway

25
Q

What is the MOA of cocaine?

A

Inhibits DAT i.e. prevents DA reuptake

26
Q

What is the MOA of amphetamine?

A

1) Taken up into pre-synaptic vesicle by DAT (prevent DA reuptake)
2) Binds/ inhibits VMAT to cause DA release

27
Q

Aside from DAT, what other transporters do cocaine and amphetamine have effects on?

A

SERT

NET

28
Q

What are the common CNS related side effects of the psychomotor stimulants?

A
Euphoria 
Dysphoria 
Insomnia 
Irritability 
Tremor 
Headache 
Anorexia
29
Q

What are the cardiovascular related side effects of the psychomotor stimulants?

A

MI

CVA

30
Q

What percentage of ADHD patients are the predominant hyperactive/impulse subtype?

A

10%

31
Q

What percentage of ADHD patients are the predominant inattentive subtype?

A

30-40%

32
Q

What percentage of ADHD patients are the combined subtype?

A

50-60%

33
Q

What are the symptoms of ADHD that are common in children with the disorder?

A

1) Motor hyperactivity
2) Aggressive
3) Low frustration tolerance
4) Impulsive

34
Q

Why are psychomotor stimulants given in ADHD?

A

Dopamine Deficit Hypothesis of ADHD–esp. in the PFC

35
Q

What drugs are used to treat ADHD?

A

Methylphenidate
Amphetamine salts
- Addreall/ Adderall XR
Dextroamphetamine

36
Q

What are the non-stimulant drugs that are given for ADHD?

A

1) Atomoxetine (NE-reuptake blockade)
2) Clonidine (alpha-2 agonist–>increase blood flow to PFC)
3) Modafinil (Activates histamine)
Antidepressants
- TCA
- MAOI
- Bupropion

37
Q

Can Modafinil be used in children? Why or why not?

A

NO–Rash?

38
Q

What are the major side effects of ADHD treatment?

A
  • Decreased appetite/ weight loss

- Insomnia