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Pharmacology III > CNS Drug Mechanisms > Flashcards

CNS Drug Mechanisms Flashcards

1
Q

Binds GABA-A receptor → Prolonged Receptor Opening → Cl- influx → hyperpolarization → decreased neuron activity

A

Barbiturates

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2
Q

BZs or Barbs?

Effects can occur independent of GABA

A

Barbs

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3
Q

Binds GABA-A receptor → More Frequent Receptor Opening + Increased GABA Affinity → Cl- influx → hyperpolarization → decreased neuron activity

A

Benzodiazepines

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4
Q

Competitive antagonist at GABA receptor → reversal of BZ effects

Also binds site of “Z drugs”

A

Flumazenil/BZ Antagonists

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5
Q

Partial agonist at postsynaptic 5-HT1A Serotonin Receptor → Inhibition of cell signaling

Full agonist at presynaptic 5-HT1A Serotonin autoeceptor → decreased 5-HT release

A

Buspirone

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6
Q

What about Buspirone’s mechanism prevents its use for EtOH withdrawal?

A

GABA independent

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7
Q

How long does it take for buspirone’s mechanism to take full therapeutic effect? This means it is a bad choice for what type of anxiety?

A

2 weeks, not good for acute anxiety

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8
Q

Buspirone exerts effects outside of the GABA system, that means that it lacks what 3 properties?

A

sedation
muscle relaxant
anticonvulsant

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9
Q

Binds BZ1 GABA Receptor → Increased GABA-Mediated Inhibition → strong, rapid sedation

No anxiolytic, anticonvulsant, muscle relaxant properties

A

Zolpidem, Zaleplon, Eszopiclone

Z Drugs

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10
Q

Orexin Receptor Antagonist: orexin regulates sleep-wake cycle, promotes wakefulness

GABA Independent

A

Suvorexant

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11
Q

Melatonin Analogue → reset sleep-wake cycle → promotes sleepiness

GABA Independent

A

Ramelteon

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12
Q

H1 Receptor Antagonist → antihistamine properties

Also causes sedation, major ingredient in OTC insomnia meds

A

Deiphenhydramine

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13
Q

The Mechanism of EtOH is similar to which 2 drug classes?

A

BZs and Barbs

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14
Q

Receptor Downregulation → Tolerance

Inhibits Glutamate on NMDA Receptor → up-regulation of NMDA Receptor

Increases DA in mesolimbic pathway

A

EtOH

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15
Q

Opioid Receptor Antagonist → blocks reward pathway stimulation

(not acute)

A

Naltrexone

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16
Q

Structural analogue of GABA

Restores normal balance of GABA & Glutamate

A

Acamprosate

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17
Q

Inhibits aldehyde dehydrogenase → acetaldehyde build up → flushing, HA, Nausea, Confusion

A

Disulfiram

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18
Q

Spasmolytic

Response depends of alpha receptor subtype
Alpha 1: Sedative + Anticonvulsant
Alpha 2: Anxiolytic
Alpha 2/3/5: Muscle Relaxant

A

Diazepam

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19
Q

GABA-B Agonist → opening of K+ channels → Hyperpolarization → inhibition of presynaptic Ca2+ Channels → Decreased NT Release

Inhibitions AC and cAMP formation to reduce excitatory NTs

Spasolytic

A

Baclofen

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20
Q

Spasmolytic

Alpha 2 Receptor Agonist → Presynaptic and Postsynaptic inhibition of spinal cord synaptic activity → decreased spasticity

Inhibits pain transmission in dorsal horn

A

Tizanidine

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21
Q

Spasmolytic

Competitive Antagonist to SR RyR1 Channel → Inhibited Ca2+ release → impaired E-C Coupling → decreased spasm of skeletal muscle

A

Dantrolene

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22
Q

Brain stem sedative → decreased neuronal activity in spinal cord

Antimuscarinic Activity → sedation, confusion, hallucination

Acute spasm drug

A

Cyclobenzaprine

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23
Q

Brain stem sedative → decreased neuronal activity in spinal cord

Similar to barbiturates, caution recovering addicts

Acute Spasm Drug

A

Carisoprodol

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24
Q

Block GABA reuptake

A

Tiagabine

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25
Q

Irreversible inhibition of GABA Transaminase → decreased GABA metabolism

A

Vigabatrin

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26
Q

Binds Synaptic Vesicular Protein SV2A

A

Levetiracetam

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27
Q

Blockage of T-type Ca2+ channels (2)

A

Ethosuxamide, Valproate

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28
Q

Block sodium and calcium channels

A

Valproate

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29
Q

Carbamazepine MoA

A

Inhibition of Na+ Channels

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30
Q

Phenytoin MoA

A

Inhibition of Na+ Channels

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31
Q

Topiramate MoA

A

Inhibition of Na+ Channels

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32
Q

Lamotrigine MoA

A

Inhibition of Na+ Channels

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33
Q

Zonisamide MoA

A

Inhibition of Na+ Channels

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34
Q

GABA analogue…

A

Gabapentin

35
Q

GABA analogue┃Binds voltage-gated Ca2+ channels → inhibited excitatory NT release

A

pregabalin

36
Q

Selective 5HT reuptake inhibition → increased 5HT in cleft → downregulation of 5HT postsynaptic receptors

2-3 weeks for effects to begin

A

SSRIs

Fluoxetine
Paroxetine
Sertraline
Citalopram
Escitalopram
37
Q

Inhibits reuptake of NE & 5HT

More S/Es than SSRIs

A

SNRIs

Venlafaxine, Duloxetine

38
Q

Inhibit reuptake of NE & 5HT
(No euphoria, low abuse potential)
(2-4 weeks for effect)

Block alpha adrenergic, histamine, muscarinic receptors

A

TCAs

Amitriptyline (Elavil)┃Imipramine (Tofranil)┃Nortriptyline (Pamelor)┃Desipramine (Norpramin)

39
Q

General: Irreversible MAO inhibition → increased NE, DA, 5HT in cleft

A

MAOIs

Phenelzine (Nardil)┃Selegiline (Deprenyl)

40
Q

Inhibits DA < NE and 5HT

Combined w. SSRI

A

Bupropion

41
Q

Blocks presynaptic Alpha 2 Receptors → blocked inhibitory pathway → increased NE & 5HT

Eliminates SSRI S/Es (anxiety, insomnia, nausea, sexual dysfunction)

A

Mirtazapine (Remeron)

42
Q

Selective NE reuptake inhibitor

A

Atomoxetine

43
Q

5HT2A Antagonist

A

Trazodone

44
Q

Gi signal transduction → decreased cAMP → closing presynaptic voltage-gated Ca2+ channels → decreased NT release & neuron activity

A

Opioids

45
Q

Which opioid receptor?

opening of K+ channels → hyperpolarization → inhibited nerve transmission → decreased pain signaling

A

Mu receptor

46
Q

Stimulates all opioid receptors

Strong Agonist

Production of all opioid effects

A

Morphine

47
Q

Stronger than morphine, similar duration, same routes

Moderate to severe pain

No metabolite accumulation → use if renal dysfunction

No histamine release → less itching

A

hydromorphone (Dilaudid)

48
Q

Mu receptor agonist

Maintenance Tx for addicts

Long-term Pain Control

A

Methadone

49
Q

Mu agonist

Metabolite → Seizures

Anticholinergic Effects → Tachycardia, Pupil Dilation

A

Meperidine (Demerol)

metabolite = Normeperidine via CYP2D6

50
Q

Cough Suppressant

PO in combo with acetaminophen

Must be metabolized by CYP2D6 to be active

A

Codeine

51
Q

Kappa Agonist, Mu Partial Agonist

Used for Moderate Pain

A

Pentazocine/Naloxone

52
Q

Partial Mu agonist

Ceiling effect = not much euphoria → low abuse potential

Used for opioid addiction/withdrawal, combined with Naloxone

A

Buprenorphine (Suboxone)

53
Q

Mild-Moderate Pain

Weak Mu Agonist, Inhibits NE/5HT reuptake

A

Tramadol

54
Q

No analgesia, Cough Suppressant

Blocks NMDA Receptors, decreased 5HT reuptake

A

dextromethorphan

55
Q

Which DA pathway?

VTA → Limbic System

Emotion

A

Mesolimbic

56
Q

Which DA pathway?

VTA → Frontal Cortex

Cognition, emotion

A

Mesocortical

57
Q

Which DA pathway?

Substantia Nigra → Striatum

Motor Control

A

Nigrostriatal

58
Q

Which DA pathway?

Hypothalamus → Pituitary

Prolactin

A

Tuberoinfundibular

59
Q

block D2 Receptors and alpha adrenergic actions → alleviate positive sxs

requires 60% receptor occupancy

A

Chlorpromazine

classical antipsychotic

60
Q

Selective for D2, less anticholinergic activity → more EPS

alleviate positive sxs

requires 60% receptor occupancy

A

Fluphenazine

classical antipsychotic

61
Q

Potent D2, D1, 5HT and H1 receptor blocker→ alleviate positive sxs

A

Haloperidol

classic antipsychotic

62
Q

Blocks 5HT2A & D2 Receptors

No effect on DA transmission in nigrostriatal pathway

A

Risperidone

atypical antipsychotic

63
Q

Blocks 5HT2A & DA D2 Receptors

5HT1A agonist → Some antidepressant activity

A

Ziprasidone

atypical antipsychotic

64
Q

Which class has the below mechanism?

blockage of 5HT2A and DA D4 Receptors

A

Atypical Antipsychotics

65
Q

Blocks 5HT2A, D4, D2

Some anticholinergic activity

A

Olanzapine

atypical antipsychotic

66
Q

Partial agonist for D2 and 5HT1A; Antagonist for 5HT2A

Low DA tone: DA receptors Activated

High DA tone: DA receptors Blocked

Also blocks alpha1 and histamine receptors

A

Aripiprazole

atypical antipsychotic

67
Q

DA system stabilizer

A

Aripiprazole

atypical antipsychotic

68
Q

suppression of secondary messengers (IP3)

May increase ACh, NE, DA

Effective in 60% of patients

A

Lithium

mood stabilizer

69
Q

crosses BBB and is converted to DA by neurons, low bioavailability (1-3% makes it to CNS)

A

l-dopa

70
Q

inhibit Dopa-Decarboxylase + no BBB passage → Increased CNS bioavailability of l-dopa

Decreased peripheral conversion → decreased S/Es

Decreased peripheral conversion → decreased l-dopa dose

A

carbidopa

71
Q

Reduce Striatal Metabolism of DA

Doesn’t affect peripheral metabolism by MAO-A

A

MAO-B (CNS) Inhibitor

Selegiline, Rasagiline, safinaminde

72
Q

inhibits COMT in CNS and Periphery leading to increased DA

A

COMT Inhibitors

Tolcapone
Entacapone

73
Q

What is the mechanism of the below?

Bromocriptine
Ropinirole
Pramipexole
Apomophine

A

DA D2 Receptor Agonists

74
Q

Antiviral, may increase DA release/inhibit reuptake

Early/Mild PD

A

Amantadine

75
Q

inverse agonist/antagonist for 5-HT Receptors

doesn’t affect DA, Adrenergic, Cholinergic, Histamine Receptors

A

pimavanserin

76
Q

M receptor antagonists → restored DA/ACh balance in striatum

A

Anticholinergics: Benztropine, Trihexyphenidyl, benadryl

77
Q

increases ACh in nerve terminal

A

Cholinesterase Inhibitors: Donepezil, Rivastigmine, Galantamine

78
Q

Galantamine blocks AChE and what other channel?

A

Presynaptic ACh Autoreceptor

79
Q

NMDA Receptor Antagonist → reduced excitotoxic effects of glutamate and slows degeneration

A

memantine

80
Q

what drug class has the following mechanism, making them useful for…

Direct action at tissue inflammation

inhibition of dorsal horn excitatory NTs

thalamic action

A

opioids, pain

81
Q

stimulation of opioid _____ receptors causes increased postsynaptic IPSPs

A

Mu

82
Q

Stimulation of presynaptic ______ receptors by opioids causes decreased NT release

A

mu, delta, kappa

83
Q

opioids have _____ effect on GABA release which allows activation of the descending pain inhibition pathway

A

inhibitory GABA effect

Pharmacology III (15 decks)

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