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mechanisms of action Flashcards

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1
Q

Prozac

A

Fluoxetine (HL 4-6d)
SSRI
(Serotonin agonist)
note: the half life increases as you continue to use it because it inhibits its own metabolism on CYP2D6

bipolar and bulemia 20-60, MDD 20-80, OCD 40-80, PANIC 10-60

comorbid DM / causes the most anxiety and agitation at first

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2
Q

Zoloft / Solotik

A

Sertraline (HL 26H)
SSRI
(Serotonin agonist)

50-200 mg/d

for PTSD, post MI, COPD

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3
Q

Paxil

A

Paroxetine (HL 22H)
SSRI
(Serotonin agonist)

20-50 or 60, panic 10-60 / extended release min is 12.5-25

for PTSD, OCD, panic / DC syndrome / most antich&sedation SE

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4
Q

Luvox / Faverin

A

Fluvoxamine (HL 17-22H)
SSRI
(Serotonin agonist)

OCD 100-300

most GI SE

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5
Q

Celexa

A

Citalopram (HL 33H)
SSRI
(Serotonin agonist)

20-40 mg/d

torsades de pointes / most GI SE

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6
Q

Lexapro / Escipharm

A

Escitalopram (HL 30H)
SSRI
(Serotonin agonist)

10-20 mg/d

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7
Q

Brintellix

A

Vortioxetine
SSRI
(Serotonin agonist at 5HT1A, and antagonist at 5HT3)

least sexual SE

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8
Q

Effexor

A

Venlafaxine
SNRI
(Serotonin and Norepinephrine agonist)

DC syndrome

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9
Q

Pristiq

A

Desvenlafaxine
SNRI
(Serotonin and Norepinephrine agonist)

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10
Q

Cymbalta

A

Duloxetine
SNRI
(Serotonin and Norepinephrine agonist + weak D Receptor inhibitor)

60 mg/d

for diabetic neuropathy and stress urinary incontinence

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11
Q

Wellbutrin / Bupran

A

Bupropion
NDRI
(Norepinephrine and Dopamine agonist)

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12
Q

Desyrel

A

Trazodone
Serotonin (SARI)
—> antagonist on 5HT2A, 5HT2C
—> agonist on (reuptake inhibitor) 5HT1A, 5HT2A, 5HT2C
blocks alpha 1 receptor
blocks H1 receptor

most common drug to cause priapism (Trazobone!)

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13
Q

Serzone

A

Nefazodone
Serotonin (SARI)
—> antagonist on 5HT2A, 5HT2C
—> agonist on (reuptake inhibitor) 5HT1A, 5HT2A, 5HT2C
blocks alpha 1 receptors
blocks H1 receptors

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14
Q

Remeron

A

Mirtazapine (NaSSa)
Serotonin antagonist (5HT2, 5HT3)
Norepinephrine antagonist (a1, a2)
H1 antagonist
Acetylcholine (Muscarinic) antagonist

all mechanisms enhance sleep except alpha 2, post MI, COPD

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15
Q

Elavil / Tryptizole

A

Amitriptyline
TCA (1st gen, tertiary amine)
—> Serotonin and Norepinephrine agonist (reuptake inhibitor)
—> Acetylcholine and Histamine antagonist
—> Na and Ca channel blockers

neuropathic pain / most dangerous in overdose

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16
Q

Tofranil

A

Imipramine
TCA (1st gen, tertiary amine)
—> Serotonin and Norepinephrine agonist
—> Acetylcholine and Histamine antagonist
—> Na and Ca channel blockers

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17
Q

Anafranil

A

Clomipramine
TCA (1st gen, tertiary amine)
—> Serotonin and Norepinephrine agonist
—> Acetylcholine and Histamine antagonist
—> Na and Ca channel blockers

phobic and obsessional states / catalepsy

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18
Q

Sinequan

A

Doxepin
TCA (1st gen, tertiary amine)
—> Serotonin and Norepinephrine agonist
—> Acetylcholine and Histamine antagonist
—> Na and Ca channel blockers

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19
Q

Pamelor /Aventyl

A

Nortriptyline
TCA (2nd gen, secondary amine)
—> Serotonin and Norepinephrine agonist
—> Acetylcholine and Histamine antagonist
—> Na and Ca channel blockers

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20
Q

Norpramine

A

Desipramine
TCA (2nd gen, secondary amine)
—> Serotonin and Norepinephrine agonist
—> Acetylcholine and Histamine antagonist
—> Na and Ca channel blockers

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21
Q

Asendin

A

Amoxapine
Tetracyclic antidepressant (2nd gen, secondary amine)
—> Serotonin and Norepinephrine agonist
—> Acetylcholine and Histamine antagonist
—> Na and Ca channel blockers

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22
Q

Nardil

A

Phenelzine
MAOI
Inhibit MAO-A –> increases Serotonin and Norepinephrine
Inhibit MAO-B –> increases phenethylamine
Inhibit both –> increases Dopamine and tyramine

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23
Q

Parnate

A

Tranylcypromine
MAOI
Inhibit MAO-A –> increases Serotonin and Norepinephrine
Inhibit MAO-B –> increases phenethylamine
Inhibit both –> increases Dopamine and tyramine

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24
Q

Marplan

A

Isocarboxazid
MAOI
Inhibit MAO-A –> increases Serotonin and Norepinephrine
Inhibit MAO-B –> increases phenethylamine
Inhibit both –> increases Dopamine and tyramine

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25
Thorazine
Chlorpromazine Typical antipsychotic (1st gen) Dopamine 2 antagonist | max: 1000mg ## Footnote low potency
26
Mellaril
Thioridazine Typical antipsychotic (1st gen) Dopamine 2 antagonist ## Footnote low potency high risk of sudden death - discontinued
27
Loxitane
Loxapine Typical antipsychotic (1st gen) Dopamine 2 antagonist ## Footnote mid potency
28
Navane
Thiothixene Typical antipsychotic (1st gen) Dopamine 2 antagonist ## Footnote mid potency
29
Moban
Molindone Typical antipsychotic (1st gen) Dopamine 2 antagonist ## Footnote mid potency
30
Trilafon
Perphenazine Typical antipsychotic (1st gen) Dopamine 2 antagonist | max: 24mg ## Footnote mid potency
31
Haldol
Haloperidol Typical antipsychotic (1st gen) Dopamine 2 antagonist - depot injection: haloperidol decanoate (test dose 25mg), depot max:300mg Qm | min: 2-4mg / max:20mg ## Footnote high potency
32
Prolixin
Fluphenazine Typical antipsychotic (1st gen) Dopamine 2 antagonist - depot (modecate): test dose 12.5, depot max: 100mg Q2w ## Footnote high potency
33
Stelazine
Trifluoperazine Typical antipsychotic (1st gen) Dopamine 2 antagonist | min:10-15mg /max:30mg ## Footnote high potency
34
Orap
Pimozide Typical antipsychotic (1st gen) Dopamine 2 antagonist ## Footnote high potency High likelihood of QTc prologation
35
Clopixol
Zuclopenthixol Atypical antipsychotic (D2 and 5HT2A receptor antagonists) Clopixol depot = Zuclopenthixol decanoate (long-term treatment of schizophrenia), test dose 100mg, depot max:600mg Qw Clopixol acuphase = Zuclopenthixol acetate (management of severe aggression not responsive to other medications) | oral max:150mg
36
Clozaril / Leponex
Clozapine (HL 12H) Atypical antipsychotic - D4 > D2 antagonist - 5HT2A antagonist and 5TH1A partial agonist - M1, M2, M3, M5 antagonist - H antagonist - alpha 1 antagonist | min:25mg / max:900mg
37
Risperdal / Respal
Risperidone (HL 20H) Atypical antipsychotic (D2 and 5HT2A receptor antagonists) | min: 2-4mg / max: 16mg, depot 50mg Q2w
38
Asero / Quzal / Seroquel / Quetra
Quetiapine (HL 6H) Atypical antipsychotic (D2 and 5HT2A receptor antagonists) | 25-100 sleep/100-200 mood/200-600 mood stabilizer, bipolar/> 600 psychos ## Footnote max:750 schizophrenia, max:800 bipolar, used for bipolar depression
39
Zylanza / Zyprexa / Prexal / Olexa / Oprexa
Olanzapine (HL 30H) Atypical antipsychotic (D2 and 5HT2A receptor antagonists) | min:5-7.5mg / max:20mg
40
Geodon
Ziprasidone (HL 7H) Atypical antipsychotic (D2 and 5HT2A receptor antagonists) | min: 40-80mg /
41
Abilify / Aripal / Abizol / Zorta
Aripiprazole (HL 75H) Atypical antipsychotic - 5HT2A antagonist - 5HT1A and D2 partial agonist | min: 10mg / max:30mg, depot max: 400mg Qm
42
Invega / Invega sustenna / Trivecta
Paliperidone (HL 20H) Atypical antipsychotic (D2 and 5HT2A receptor antagonists) - invega sustenna (paliperidone depot Q1month): max 150mg - invega travecta (paliperidone depot Q3months): max 525mg | oral - min:3mg / max:12mg
43
Saphris
Asenapine Atypical antipsychotic (D2 and 5HT2A receptor antagonists) | min: 10mg / max: 20mg
44
Fanapt
Iloperidone Atypical antipsychotic (D2 and 5HT2A receptor antagonists) | min: 4-8mg /
45
Latuda
Lurasidone Atypical antipsychotic - D2 and 5HT2A receptor antagonists - 5HT1A partial agonist - 5HT7, alpha 2a, alpha 2c antagonist | min: 40mg / max: 160mg
46
Reagila / Vrayler
Cariprazine Atypical antipsychotic (D2 and 5HT2A receptor antagonists) | min: 1.5mg / max: 6mg
47
Moclobemide
MAOI Inhibit MAO-A --> increases Serotonin and Norepinephrine Inhibit MAO-B --> increases phenethylamine Inhibit both --> increases Dopamine and tyramine
48
Selegiline
MAOI Inhibit MAO-A --> increases Serotonin and Norepinephrine Inhibit MAO-B --> increases phenethylamine Inhibit both --> increases Dopamine and tyramine
49
Tegretol
Carbamazepine Anticonvulsants (mood stabilizer) Na channel stabilizer ## Footnote CI in bone marrow depression and to + MAOI, TEN, SJS, decrease lamotrigine
50
Depakote / Depakine / Cronoval
Valproic acid Anticonvulsants (mood stabilizer) - GABA modulator - Na channel inhibitor - NMDA antagonist ## Footnote liver damage and teratogenic, increases lamotrigine
51
Pravia
Sodium valproate + Valproic acid Anticonvulsant (mood stabilizer) - GABA modulator - Na channel inhibitor - NMDA antagonist
52
Lamictal
Lamotrigine Anticonvulsant (mood stabilizer) - GABA modulator - Na channel stabilizer - NMDA modulator ## Footnote prevention of bipolar depression, SJS
53
Trileptal
Oxcarbazepine Anticonvulsant (mood stabilizer) Na channel stabilizer
54
Neurontin / Gabatrex
Gabapentin Anticonvulsant (mood stabilizer) binds to alpha-2-delta subunit of Ca channel blocking it --> decreases glutamate and substance P ## Footnote analogue of GABA
55
Lyrica
Pregabalin Anticonvulsant (mood stabilizer) binds to alpha-2-delta subunit of Ca channel blocking it --> decreases glutamate and substance P ## Footnote analohue of GABA (strong)
56
Topamax
Topimarate Anticonvulsant (mood stabilizer) - GABA modulator - Na channel inhibitor - NMDA antagonist ## Footnote decreases lamotrigine
57
Keppra
Levetiracetam Anticonvulsant (inhibits presynaptic calcium channels)
58
Valium
Diazepam Benzodiazepine enhance GABA by non-specific positive allosteric modulation of GABA-A receptors = by increasing the frequency of Cl channel opening ## Footnote long acting >20h (20-100)
59
Rivotril / Klonopin
Clonazepam Benzodiazepine enhance GABA by non-specific positive allosteric modulation of GABA-A receptors = by increasing the frequency of Cl channel opening ## Footnote long acting >20h (18-50)
60
Xanax
Alprazolam Benzodiazepine enhance GABA by non-specific positive allosteric modulation of GABA-A receptors = by increasing the frequency of Cl channel opening ## Footnote intermediate acting 6-20h (10-15)
61
Lorans / Ativan
Lorazepam Benzodiazepine enhance GABA by non-specific positive allosteric modulation of GABA-A receptors = by increasing the frequency of Cl channel opening ## Footnote intermediate acting 6-20h (10-20)
62
Serax
Oxazepam Benzodiazepine enhance GABA by non-specific positive allosteric modulation of GABA-A receptors = by increasing the frequency of Cl channel opening ## Footnote intermediate acting 6-20h (6-10)
63
Restoril
Temazepam Benzodiazepine enhance GABA by non-specific positive allosteric modulation of GABA-A receptors = by increasing the frequency of Cl channel opening ## Footnote intermediate acting 6-20h (8-22)
64
Versed
Midazolam Benzodiazepine enhance GABA by non-specific positive allosteric modulation of GABA-A receptors = by increasing the frequency of Cl channel opening ## Footnote short acting <6h
65
Lofexidine
alpha 2 agonist used to relieve opioid withdrawal
66
Moclobemide
MAOI Reversible Inhibitor of MAO-A --> increases Serotonin and Norepinephrine
67
Selegline
MAOI At higher doses, it inhibits MAO-A --> increases serotonin and norepinephrine Welective irreversable Inhibitor of MAO-B --> increases phenethylamine Inhibit both --> increases dopamine and tyramine
68
Fluanxol
Flupentixol Atypical antipsychotic (D2 and 5HT2A receptor antagonists) | depot max: 400mg Qw, test dose 20mg
69
Phenytoin
Anticonvulsants (mood stabilizer) Na channel stabilizer
70
Zopiclone
Non-BZD hypnotic (Z-drugs) enhance GABA by non-specific positive allosteric modulation of GABA-A receptors ## Footnote 5-6h
71
Eszopiclone
Non-BZD hypnotic (Z-drugs) enhance GABA by non-specific positive allosteric modulation of GABA-A receptors
72
Zaleplon
Non-BZD hypnotic (Z-drugs) enhance GABA by non-specific positive allosteric modulation of GABA-A receptors ## Footnote 2h
73
Stilnox
Zolpidem Non-BZD hypnotic (Z-drugs) enhance GABA by non-specific positive allosteric modulation of GABA-A receptors ## Footnote 2h
74
Benadryl
Diphenhydramine Non-BZD hypnotic - H antagonist - Ach antagonist
75
Rozerem
Ramelteon Non-BZD hypnotic melatonin MT1, MT2 agonist
76
Buspar
Buspirone Non-BZD anxiolytic 5TH1A partial agonist
77
Atarax
Hydroxyzine Non-BZD anxiolytic H antagonist
78
Butalbitol / phenobarbital / amobarbital / pentobarbital
Bartbiturates Non-BZD anxiolytics facilitate GABA-A action by increasing the duration of Cl channel opening
79
GHB (gamma-hydroxybutyrate)
General anesthetic enhances GABA-B action
80
Baclofen
enhance GABA-B action ## Footnote used as muscle relaxant and for cramps
81
Provigil
Modafinil Psychostimulant Dopamine agonist
82
Strattera / Axepta
Atomoxetine psychostimulant norepinephrine agonist
83
Guanfacine
Psychostimulant alpha-2a agonist
84
Clonidine
Psychostimulant alpha-2a agonist
85
Ritalin / Concerta
Methylphenidate Psychostimulant Dopamine and NE agonist
86
Adderall
Mixed amphetamine salts Psychostimulant Dopamine and NE agonist
87
Aricept
Donepezil cognitive enhancer (Ach agonist = AchE inhibitor)
88
Razadyne
Galantamine cognitive enhancer - Ach agonist = AchE inhibitor - allosteric modulation of nicotinic Ach R
89
Exelon
Rivastigmine cognitive enhancer (Ach agonist = AchE inhibitor)
90
Tacrine
cognitive enhancer Ach agonist = ''butyryl cholinesterase inhibitor''
91
Namenda
Memantine cognitive enhancer - NMDA antagonist (non-competitive) - 5HT3 receptor antagonist
92
Ketamine
cognitive enhancer NMDA antagonist (non-competitive)
93
Acamprosate
cognitive enhancer - NMDA antagonist - positive allosteric modulation of GABA-A receptor
94
Buprenorphine
mu opioid receptor partial agonist
95
Naloxone
pure opioid antagonist (mu, delta, kappa) ## Footnote short acting
96
Naltrexone
pure opioid antagonist (mu, delta, kappa) ## Footnote long acting
97
Champix
Verenicline nicotinic receptor partial agonsit (high affinity for alpha-4 and beta-2 nicotinic receptor) ## Footnote smoking cessation, 12w then additional 12w, exacerbate psych ds
98
Disulfiram
binds irreversably to aldehyde dehydrogenase and causes acetaldehyde to accomulate from alcohol
99
Viagra
Sildenafil cGMP specific phosphodiesterase type 5 inhibitor --> blocks the breakdown oF cGMP --< prolongs its effect = prolongs the erection
100
Agomelatine
Atypical antidepressant - 5HT2C receptor agonist - MT1, MT2 receptor agonist
101
Flumazenil
BZD antidote selective GABA-A antagonist (competitive antagonist or reverse the binding of bzd or hypnotics) - negates the seadtive effect of bzd within 1-2min for 20-50min then sadation may return and you'd need to repeat
102
Lithium
Mood stabilizer mechanism of action unknown therapeutic dose 0.4-1 (toxicity 1.5)
103
Cocaine
Blocks dopamine transporte DAT, serotonin transporter SERT, norepinephrine transporter NET increaseing the levels of D, SE, NE. - at higher concentrations, it blocks Na and cardiac Ikr (rapid delayed rectifier channel)
104
Amphetamine
Reverses the action of DAT, SERT, NET by: - binds to transporters and is taken up to the presynaptic axon terminal - once inside --> it inhibits VMAT2 and disrupts the electrochemical gradient that's important for its function --> increasing D, SE, NE in cytosol - it also inhibits MAO --> inhibiting the metabolism and increasing the levels of D, SE, NE - stimulates the intracellular receptor TAAR1 --> reversal of DAT | vesicular monoamine transporter 2
105
Hallucinogens | LSD, psilocybin, DMT, mescaline
binds to and activates 5HT2A receptor in the cortex
106
Caffeine
Xanthines Adenosine (NT) receptor antagonsit
107
Vigabatrin
Irreversable inhibitor of GABA transaminase, increases GABA
108
Dustonex
Cabergoline used to treat high prolactin and ovulation problems 0.5mg PO 1/2 apill in 2days per week

Drug Names (1 decks)

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