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Pharmacology Test #6 > CNS Stimulants > Flashcards

CNS Stimulants Flashcards

1
Q

Classes of CNS stimulants

A
  1. Catecholamine releasers
  2. Catecholamine reuptake blockers
  3. Stimulant antidepressants
  4. Methylxanthines
  5. Nicotinic agents
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2
Q

Therapeutic uses of CNS sitmulants

A
  1. ADHD
  2. Narcolepsy
  3. Obesity
  4. Smoking cessation
  5. Alcohol use disorder? (varenicline)
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3
Q

Historical prototype of catecholamine releasers

A

D-ephedrine

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4
Q

Catecholamine releasers

A
  1. Amphetamine (Adderal)
  2. Methamphetamine (Desoxyn)
  3. Methylphenidate (Ritalin SR, Concerta, Metadate)
  4. Ephedrine
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5
Q

MOA of catecholamine releasers in CNS

A
  1. Binds to presynaptive membrane and induces release from vesicles
  2. Causes release of DA from vesicles into the intracellular space in terminal
  3. Blocks MAO, blocking degradation of DA and causing buildup inside cytoplasm in terminal
  4. Induces reverse transport through the DAT to “release” DA into EC space
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6
Q

Reuptake blockers

A
  1. Cocaine
  2. Modafinil (Provigil)
  3. Sibutramine (Meridia)
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7
Q

MOA of reuptake blockers

A

pure block of re-uptake, prolonging lifetime of catecholamine in the synapse and promoting its action on postsynaptic cell

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8
Q

Cocaine

A

abuse potential; short/intense action; NaV activity (locak anesthetic)

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9
Q

Modafinil (Provigil)

A

monoamine reuptake blocker; MOA unclear; less abuse potential than cocaine

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10
Q

What are bath salts?

A

Synthetic cathinones

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11
Q

Intoxication from synthetic cathinones

A

psychosis, hallucinations, agitation, tachycardia, hypertension, hyperthermia, and combative or violent behaviors

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12
Q

What is MDPV?

A

reuptake blocker for DAT and NET; 10-50X cocaine potency

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13
Q

Cathinones that are releasers have variable selectivity for

A

DAT, SERT, and NET

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14
Q

Stimulant antidepressants

A
  1. Atomoxetine (Strattera)

2. Bupropion (Zyban, Welbutrin)

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15
Q

Atomoxetine (Strattera)

A

Net activity; alternative to classical stimulants; refractory ADHD, ADD, and adult ADD

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16
Q

Bupropion (Zyban, Welbutrin)

A

Adjunct for depression/anxiety; smoking cessation; lowers seizure threshold

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17
Q

MOA of stimulant antidepressants

A

mixture of antidepressants properties (block NET or SERT) plus some mild CNS activating properties via block of DA reuptake

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18
Q

When are stimulant antidepressants used

A

used as alternative to classical stimulants, likely in situations refractory to first-line drugs

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19
Q

How is bupropion often used?

A

often used as an adjunct mood enhancer along with an SSRI, has NET and DAT blocking activity

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20
Q

Methylxanthines

A
  1. Caffeine
  2. Theophylline
  3. Theobromine
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21
Q

Caffeine

A

short-acting; diuretic; mild DA and NE stimulant

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22
Q

Theophylline

A

found in tea; bronchodilation, used in asthma

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23
Q

Where does caffeine act as an antagonist?

A

at adenosine receptors; in the brain the A2a receptor seems to be most important for the wakefullness-promoting properties of caffeine

24
Q

Describe A2a receptors

A

Gs-coupled and have high expression in the area of the brain called the striatum, involved in arousal and drug addiction

25
Q

What does specific knock out of A2a receptors in the striatum do?

A

eliminates the wakefullness property of caffeine

26
Q

Nicotine’s action in the DA system

A
  1. Stimulate AP firing

2. Stimulate DA release (direct and indirect)

27
Q

Nicotinic agents

A
  1. Nicotine
  2. Varenicline (Chantix)
  3. Bupropion (Zyban)
28
Q

Describe nicotinic acetylcholine receptors

A

acetylcholine-gated cation channels, where activation promotes cellular depolarization and NT release when receptors on presynaptic terminals are activated

29
Q

Brain or neuronal nicotinic receptors have the same secondary structure as

A

muscle receptors

30
Q

Brain nicotinic receptors have high affinity for

A

both nicotine and Ach

31
Q

Most brain nicotinic receptors are expressed

A

pre-synaptically (in axon terminals) or pre-terminally (on axons) where they regulate NT release

32
Q

Key area with regard to the medical pharmacology of nicotine addiction and nicotinic agents

A

dopamine pathway from the VTA to the striatum and cortex

33
Q

Essential for ligand binding to the nicotinic receptor binding site

A

nitrogens that are protonated at physiological pH

34
Q

The likely form of nicotine that binds to receptors

A

the charged or protonated form of nicotine

35
Q

Which enzyme is nicotine degraded by?

A

trick question - it has no enzyme that can degrade it like ACh does

36
Q

How does bupropion work as a smoking cessation aid?

A

It has nAChR antagonist activity at receptors in the DA system and it can block nicotine-stimulated action potential firing and ACh-activated nAChR currents

37
Q

Varenicline

A

partial agonist at most nAChRs; can directly activate receptors but can also interfere with full action of stronger agonists like nicotine

38
Q

May explain why varenicline has unwanted side effects

A

It also has activity at a3b4 nAChRs expressed in peripheral sites

39
Q

How does varenicline promote cessation of nicotine intake?

A

Blocks reinforcing action of nicotine and produces moderate DA release (alleviates craving)

40
Q

Abuse potential of catecholamine releasers

41
Q

Abuse potential of reuptake blockers

A

Cocaine > modafinil, silbutramine

42
Q

Abuse potential of stiulant antidepressants

43
Q

Abuse potential of methylxanthines

44
Q

Abuse potential of nicotine

45
Q

Toxicity of amphetamines

A

have CV side effects, can exacerbate HTN, HR can slow reflexively at moderate doses, but tachycardia happens in overdose situations, psycological symptoms includes psychosis

46
Q

Toxicity of cocaine

A

CV (MI, stroke, arrhythmias), CNS (seizure), respiratory depression

47
Q

Toxicity of Nicotinics

A

GI upset and CNS (odd dreams, suicide ideations, insomnia)

48
Q

ADHD

A

mainly children with poor attention: poor listening, cannot follow instructions, forgetful, poor academic performance, easily distracted, impossible to sit still, engage in quiet tasks, impulsive in thought or action, impatient

49
Q

Treatment of ADHD

A

amphetamine (Adderall) or methylphenidate (Ritalin)

50
Q

Adverse effects of ADHD

A

insomnia, abdominal pain, anorexia/weight loss (growth suppression in children)

51
Q

Narcolepsy

A

refreshing “sleep attacks” with cataplexy; REM sleep intrusions

52
Q

What is cataplexy

A

sudden loss of muscle tone (bilateral) often with intense emotional engagement

53
Q

Treatment of Narcolepsy

A
  1. TCAs and MAOIs
  2. Methylphenidate (Ritalin), amphetamine
  3. Modafinil (Provigil)
54
Q

Problems of using CNS stimulants to control obesity

A
  1. Weight can be re-gained after discontinuation
  2. Exacerbated HTN, problem in population who would take this for obesity
  3. Tolerance to anorexic effect
  4. Abuse and habituation
55
Q

CNS stimulants used for obesity treatment

A
  1. Amphetamine
  2. Benzphetamine
  3. Phentermine
56
Q

Treatment for nicotine addiction

A
  1. Varenicline (Chantix)
  2. Bupropion (Zyban) - puts people in a better mood
  3. Nicotine (patch, gum)

Pharmacology Test #6 (12 decks)

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