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Pharmacology III > CNS Drug Mechanisms > Flashcards

CNS Drug Mechanisms Flashcards

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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
Irreversible inhibition of GABA Transaminase → decreased GABA metabolism
Vigabatrin
26
Binds Synaptic Vesicular Protein SV2A
Levetiracetam
27
Blockage of T-type Ca2+ channels (2)
Ethosuxamide, Valproate
28
Block sodium and calcium channels
Valproate
29
Carbamazepine MoA
Inhibition of Na+ Channels
30
Phenytoin MoA
Inhibition of Na+ Channels
31
Topiramate MoA
Inhibition of Na+ Channels
32
Lamotrigine MoA
Inhibition of Na+ Channels
33
Zonisamide MoA
Inhibition of Na+ Channels
34
GABA analogue...
Gabapentin
35
GABA analogue┃Binds voltage-gated Ca2+ channels → inhibited excitatory NT release
pregabalin
36
Selective 5HT reuptake inhibition → increased 5HT in cleft → downregulation of 5HT postsynaptic receptors 2-3 weeks for effects to begin
SSRIs ``` Fluoxetine Paroxetine Sertraline Citalopram Escitalopram ```
37
Inhibits reuptake of NE & 5HT More S/Es than SSRIs
SNRIs | Venlafaxine, Duloxetine
38
Inhibit reuptake of NE & 5HT (No euphoria, low abuse potential) (2-4 weeks for effect) Block alpha adrenergic, histamine, muscarinic receptors
TCAs Amitriptyline (Elavil)┃Imipramine (Tofranil)┃Nortriptyline (Pamelor)┃Desipramine (Norpramin)
39
General: Irreversible MAO inhibition → increased NE, DA, 5HT in cleft
MAOIs Phenelzine (Nardil)┃Selegiline (Deprenyl)
40
Inhibits DA < NE and 5HT Combined w. SSRI
Bupropion
41
Blocks presynaptic Alpha 2 Receptors → blocked inhibitory pathway → increased NE & 5HT Eliminates SSRI S/Es (anxiety, insomnia, nausea, sexual dysfunction)
Mirtazapine (Remeron)
42
Selective NE reuptake inhibitor
Atomoxetine
43
5HT2A Antagonist
Trazodone
44
Gi signal transduction → decreased cAMP → closing presynaptic voltage-gated Ca2+ channels → decreased NT release & neuron activity
Opioids
45
Which opioid receptor? opening of K+ channels → hyperpolarization → inhibited nerve transmission → decreased pain signaling
Mu receptor
46
Stimulates all opioid receptors Strong Agonist Production of all opioid effects
Morphine
47
Stronger than morphine, similar duration, same routes Moderate to severe pain No metabolite accumulation → use if renal dysfunction No histamine release → less itching
hydromorphone (Dilaudid)
48
Mu receptor agonist Maintenance Tx for addicts Long-term Pain Control
Methadone
49
Mu agonist Metabolite → Seizures Anticholinergic Effects → Tachycardia, Pupil Dilation
Meperidine (Demerol) | metabolite = Normeperidine via CYP2D6
50
Cough Suppressant PO in combo with acetaminophen Must be metabolized by CYP2D6 to be active
Codeine
51
Kappa Agonist, Mu Partial Agonist Used for Moderate Pain
Pentazocine/Naloxone
52
Partial Mu agonist Ceiling effect = not much euphoria → low abuse potential Used for opioid addiction/withdrawal, combined with Naloxone
Buprenorphine (Suboxone)
53
Mild-Moderate Pain Weak Mu Agonist, Inhibits NE/5HT reuptake
Tramadol
54
No analgesia, Cough Suppressant Blocks NMDA Receptors, decreased 5HT reuptake
dextromethorphan
55
Which DA pathway? VTA → Limbic System Emotion
Mesolimbic
56
Which DA pathway? VTA → Frontal Cortex Cognition, emotion
Mesocortical
57
Which DA pathway? Substantia Nigra → Striatum Motor Control
Nigrostriatal
58
Which DA pathway? Hypothalamus → Pituitary Prolactin
Tuberoinfundibular
59
block D2 Receptors and alpha adrenergic actions → alleviate positive sxs requires 60% receptor occupancy
Chlorpromazine | classical antipsychotic
60
Selective for D2, less anticholinergic activity → more EPS alleviate positive sxs requires 60% receptor occupancy
Fluphenazine | classical antipsychotic
61
Potent D2, D1, 5HT and H1 receptor blocker→ alleviate positive sxs
Haloperidol | classic antipsychotic
62
Blocks 5HT2A & D2 Receptors No effect on DA transmission in nigrostriatal pathway
Risperidone | atypical antipsychotic
63
Blocks 5HT2A & DA D2 Receptors 5HT1A agonist → Some antidepressant activity
Ziprasidone | atypical antipsychotic
64
Which class has the below mechanism? blockage of 5HT2A and DA D4 Receptors
Atypical Antipsychotics
65
Blocks 5HT2A, D4, D2 | Some anticholinergic activity
Olanzapine | atypical antipsychotic
66
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
Aripiprazole | atypical antipsychotic
67
DA system stabilizer
Aripiprazole | atypical antipsychotic
68
suppression of secondary messengers (IP3) May increase ACh, NE, DA Effective in 60% of patients
Lithium | mood stabilizer
69
crosses BBB and is converted to DA by neurons, low bioavailability (1-3% makes it to CNS)
l-dopa
70
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
carbidopa
71
Reduce Striatal Metabolism of DA Doesn’t affect peripheral metabolism by MAO-A
MAO-B (CNS) Inhibitor | Selegiline, Rasagiline, safinaminde
72
inhibits COMT in CNS and Periphery leading to increased DA
COMT Inhibitors Tolcapone Entacapone
73
What is the mechanism of the below? Bromocriptine Ropinirole Pramipexole Apomophine
DA D2 Receptor Agonists
74
Antiviral, may increase DA release/inhibit reuptake Early/Mild PD
Amantadine
75
inverse agonist/antagonist for 5-HT Receptors doesn’t affect DA, Adrenergic, Cholinergic, Histamine Receptors
pimavanserin
76
M receptor antagonists → restored DA/ACh balance in striatum
Anticholinergics: Benztropine, Trihexyphenidyl, benadryl
77
increases ACh in nerve terminal
Cholinesterase Inhibitors: Donepezil, Rivastigmine, Galantamine
78
Galantamine blocks AChE and what other channel?
Presynaptic ACh Autoreceptor
79
NMDA Receptor Antagonist → reduced excitotoxic effects of glutamate and slows degeneration
memantine
80
what drug class has the following mechanism, making them useful for... Direct action at tissue inflammation inhibition of dorsal horn excitatory NTs thalamic action
opioids, pain
81
stimulation of opioid _____ receptors causes increased postsynaptic IPSPs
Mu
82
Stimulation of presynaptic ______ receptors by opioids causes decreased NT release
mu, delta, kappa
83
opioids have _____ effect on GABA release which allows activation of the descending pain inhibition pathway
inhibitory GABA effect

Pharmacology III (15 decks)

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