mechanisms of action Flashcards

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
Q

Thorazine

A

Chlorpromazine
Typical antipsychotic (1st gen)
Dopamine 2 antagonist

max: 1000mg

low potency

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26
Q

Mellaril

A

Thioridazine
Typical antipsychotic (1st gen)
Dopamine 2 antagonist

low potency
high risk of sudden death - discontinued

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27
Q

Loxitane

A

Loxapine
Typical antipsychotic (1st gen)
Dopamine 2 antagonist

mid potency

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28
Q

Navane

A

Thiothixene
Typical antipsychotic (1st gen)
Dopamine 2 antagonist

mid potency

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29
Q

Moban

A

Molindone
Typical antipsychotic (1st gen)
Dopamine 2 antagonist

mid potency

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30
Q

Trilafon

A

Perphenazine
Typical antipsychotic (1st gen)
Dopamine 2 antagonist

max: 24mg

mid potency

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31
Q

Haldol

A

Haloperidol
Typical antipsychotic (1st gen)
Dopamine 2 antagonist
- depot injection: haloperidol decanoate (test dose 25mg), depot max:300mg Qm

min: 2-4mg / max:20mg

high potency

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32
Q

Prolixin

A

Fluphenazine
Typical antipsychotic (1st gen)
Dopamine 2 antagonist
- depot (modecate): test dose 12.5, depot max: 100mg Q2w

high potency

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33
Q

Stelazine

A

Trifluoperazine
Typical antipsychotic (1st gen)
Dopamine 2 antagonist

min:10-15mg /max:30mg

high potency

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34
Q

Orap

A

Pimozide
Typical antipsychotic (1st gen)
Dopamine 2 antagonist

high potency
High likelihood of QTc prologation

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35
Q

Clopixol

A

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

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36
Q

Clozaril / Leponex

A

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

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37
Q

Risperdal / Respal

A

Risperidone (HL 20H)
Atypical antipsychotic
(D2 and 5HT2A receptor antagonists)

min: 2-4mg / max: 16mg, depot 50mg Q2w

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38
Q

Asero / Quzal / Seroquel / Quetra

A

Quetiapine (HL 6H)
Atypical antipsychotic
(D2 and 5HT2A receptor antagonists)

25-100 sleep/100-200 mood/200-600 mood stabilizer, bipolar/> 600 psychos

max:750 schizophrenia, max:800 bipolar, used for bipolar depression

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39
Q

Zylanza / Zyprexa / Prexal / Olexa / Oprexa

A

Olanzapine (HL 30H)
Atypical antipsychotic
(D2 and 5HT2A receptor antagonists)

min:5-7.5mg / max:20mg

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40
Q

Geodon

A

Ziprasidone (HL 7H)
Atypical antipsychotic
(D2 and 5HT2A receptor antagonists)

min: 40-80mg /

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41
Q

Abilify / Aripal / Abizol / Zorta

A

Aripiprazole (HL 75H)
Atypical antipsychotic
- 5HT2A antagonist
- 5HT1A and D2 partial agonist

min: 10mg / max:30mg, depot max: 400mg Qm

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42
Q

Invega / Invega sustenna / Trivecta

A

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

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43
Q

Saphris

A

Asenapine
Atypical antipsychotic
(D2 and 5HT2A receptor antagonists)

min: 10mg / max: 20mg

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44
Q

Fanapt

A

Iloperidone
Atypical antipsychotic
(D2 and 5HT2A receptor antagonists)

min: 4-8mg /

45
Q

Latuda

A

Lurasidone
Atypical antipsychotic
- D2 and 5HT2A receptor antagonists
- 5HT1A partial agonist
- 5HT7, alpha 2a, alpha 2c antagonist

min: 40mg / max: 160mg

46
Q

Reagila / Vrayler

A

Cariprazine
Atypical antipsychotic
(D2 and 5HT2A receptor antagonists)

min: 1.5mg / max: 6mg

47
Q

Moclobemide

A

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

48
Q

Selegiline

A

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

49
Q

Tegretol

A

Carbamazepine
Anticonvulsants (mood stabilizer)
Na channel stabilizer

CI in bone marrow depression and to + MAOI, TEN, SJS, decrease lamotrigine

50
Q

Depakote / Depakine / Cronoval

A

Valproic acid
Anticonvulsants (mood stabilizer)
- GABA modulator
- Na channel inhibitor
- NMDA antagonist

liver damage and teratogenic, increases lamotrigine

51
Q

Pravia

A

Sodium valproate + Valproic acid
Anticonvulsant (mood stabilizer)
- GABA modulator
- Na channel inhibitor
- NMDA antagonist

52
Q

Lamictal

A

Lamotrigine
Anticonvulsant (mood stabilizer)
- GABA modulator
- Na channel stabilizer
- NMDA modulator

prevention of bipolar depression, SJS

53
Q

Trileptal

A

Oxcarbazepine
Anticonvulsant (mood stabilizer)
Na channel stabilizer

54
Q

Neurontin / Gabatrex

A

Gabapentin
Anticonvulsant (mood stabilizer)
binds to alpha-2-delta subunit of Ca channel blocking it –> decreases glutamate and substance P

analogue of GABA

55
Q

Lyrica

A

Pregabalin
Anticonvulsant (mood stabilizer)
binds to alpha-2-delta subunit of Ca channel blocking it –> decreases glutamate and substance P

analohue of GABA (strong)

56
Q

Topamax

A

Topimarate
Anticonvulsant (mood stabilizer)
- GABA modulator
- Na channel inhibitor
- NMDA antagonist

decreases lamotrigine

57
Q

Keppra

A

Levetiracetam
Anticonvulsant
(inhibits presynaptic calcium channels)

58
Q

Valium

A

Diazepam
Benzodiazepine
enhance GABA by non-specific positive allosteric modulation of GABA-A receptors = by increasing the frequency of Cl channel opening

long acting >20h (20-100)

59
Q

Rivotril / Klonopin

A

Clonazepam
Benzodiazepine
enhance GABA by non-specific positive allosteric modulation of GABA-A receptors = by increasing the frequency of Cl channel opening

long acting >20h (18-50)

60
Q

Xanax

A

Alprazolam
Benzodiazepine
enhance GABA by non-specific positive allosteric modulation of GABA-A receptors = by increasing the frequency of Cl channel opening

intermediate acting 6-20h (10-15)

61
Q

Lorans / Ativan

A

Lorazepam
Benzodiazepine
enhance GABA by non-specific positive allosteric modulation of GABA-A receptors = by increasing the frequency of Cl channel opening

intermediate acting 6-20h (10-20)

62
Q

Serax

A

Oxazepam
Benzodiazepine
enhance GABA by non-specific positive allosteric modulation of GABA-A receptors = by increasing the frequency of Cl channel opening

intermediate acting 6-20h (6-10)

63
Q

Restoril

A

Temazepam
Benzodiazepine
enhance GABA by non-specific positive allosteric modulation of GABA-A receptors = by increasing the frequency of Cl channel opening

intermediate acting 6-20h (8-22)

64
Q

Versed

A

Midazolam
Benzodiazepine
enhance GABA by non-specific positive allosteric modulation of GABA-A receptors = by increasing the frequency of Cl channel opening

short acting <6h

65
Q

Lofexidine

A

alpha 2 agonist
used to relieve opioid withdrawal

66
Q

Moclobemide

A

MAOI
Reversible Inhibitor of MAO-A –> increases Serotonin and Norepinephrine

67
Q

Selegline

A

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
Q

Fluanxol

A

Flupentixol
Atypical antipsychotic
(D2 and 5HT2A receptor antagonists)

depot max: 400mg Qw, test dose 20mg

69
Q

Phenytoin

A

Anticonvulsants (mood stabilizer)
Na channel stabilizer

70
Q

Zopiclone

A

Non-BZD hypnotic
(Z-drugs)
enhance GABA by non-specific positive allosteric modulation of GABA-A receptors

5-6h

71
Q

Eszopiclone

A

Non-BZD hypnotic
(Z-drugs)
enhance GABA by non-specific positive allosteric modulation of GABA-A receptors

72
Q

Zaleplon

A

Non-BZD hypnotic
(Z-drugs)
enhance GABA by non-specific positive allosteric modulation of GABA-A receptors

2h

73
Q

Stilnox

A

Zolpidem
Non-BZD hypnotic
(Z-drugs)
enhance GABA by non-specific positive allosteric modulation of GABA-A receptors

2h

74
Q

Benadryl

A

Diphenhydramine
Non-BZD hypnotic
- H antagonist
- Ach antagonist

75
Q

Rozerem

A

Ramelteon
Non-BZD hypnotic
melatonin MT1, MT2 agonist

76
Q

Buspar

A

Buspirone
Non-BZD anxiolytic
5TH1A partial agonist

77
Q

Atarax

A

Hydroxyzine
Non-BZD anxiolytic
H antagonist

78
Q

Butalbitol / phenobarbital / amobarbital / pentobarbital

A

Bartbiturates
Non-BZD anxiolytics
facilitate GABA-A action by increasing the duration of Cl channel opening

79
Q

GHB (gamma-hydroxybutyrate)

A

General anesthetic
enhances GABA-B action

80
Q

Baclofen

A

enhance GABA-B action

used as muscle relaxant and for cramps

81
Q

Provigil

A

Modafinil
Psychostimulant
Dopamine agonist

82
Q

Strattera / Axepta

A

Atomoxetine
psychostimulant
norepinephrine agonist

83
Q

Guanfacine

A

Psychostimulant
alpha-2a agonist

84
Q

Clonidine

A

Psychostimulant
alpha-2a agonist

85
Q

Ritalin / Concerta

A

Methylphenidate
Psychostimulant
Dopamine and NE agonist

86
Q

Adderall

A

Mixed amphetamine salts
Psychostimulant
Dopamine and NE agonist

87
Q

Aricept

A

Donepezil
cognitive enhancer
(Ach agonist = AchE inhibitor)

88
Q

Razadyne

A

Galantamine
cognitive enhancer
- Ach agonist = AchE inhibitor
- allosteric modulation of nicotinic Ach R

89
Q

Exelon

A

Rivastigmine
cognitive enhancer
(Ach agonist = AchE inhibitor)

90
Q

Tacrine

A

cognitive enhancer
Ach agonist = ‘‘butyryl cholinesterase inhibitor’’

91
Q

Namenda

A

Memantine
cognitive enhancer
- NMDA antagonist (non-competitive)
- 5HT3 receptor antagonist

92
Q

Ketamine

A

cognitive enhancer
NMDA antagonist (non-competitive)

93
Q

Acamprosate

A

cognitive enhancer
- NMDA antagonist
- positive allosteric modulation of GABA-A receptor

94
Q

Buprenorphine

A

mu opioid receptor partial agonist

95
Q

Naloxone

A

pure opioid antagonist (mu, delta, kappa)

short acting

96
Q

Naltrexone

A

pure opioid antagonist (mu, delta, kappa)

long acting

97
Q

Champix

A

Verenicline
nicotinic receptor partial agonsit
(high affinity for alpha-4 and beta-2 nicotinic receptor)

smoking cessation, 12w then additional 12w, exacerbate psych ds

98
Q

Disulfiram

A

binds irreversably to aldehyde dehydrogenase and causes acetaldehyde to accomulate from alcohol

99
Q

Viagra

A

Sildenafil
cGMP specific phosphodiesterase type 5 inhibitor –> blocks the breakdown oF cGMP –< prolongs its effect = prolongs the erection

100
Q

Agomelatine

A

Atypical antidepressant
- 5HT2C receptor agonist
- MT1, MT2 receptor agonist

101
Q

Flumazenil

A

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
Q

Lithium

A

Mood stabilizer
mechanism of action unknown
therapeutic dose 0.4-1 (toxicity 1.5)

103
Q

Cocaine

A

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
Q

Amphetamine

A

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
Q

Hallucinogens

LSD, psilocybin, DMT, mescaline

A

binds to and activates 5HT2A receptor in the cortex

106
Q

Caffeine

A

Xanthines
Adenosine (NT) receptor antagonsit

107
Q

Vigabatrin

A

Irreversable inhibitor of GABA transaminase, increases GABA

108
Q

Dustonex

A

Cabergoline
used to treat high prolactin and ovulation problems
0.5mg PO 1/2 apill in 2days per week