mechanisms of action Flashcards
Prozac
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
Zoloft / Solotik
Sertraline (HL 26H)
SSRI
(Serotonin agonist)
50-200 mg/d
for PTSD, post MI, COPD
Paxil
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
Luvox / Faverin
Fluvoxamine (HL 17-22H)
SSRI
(Serotonin agonist)
OCD 100-300
most GI SE
Celexa
Citalopram (HL 33H)
SSRI
(Serotonin agonist)
20-40 mg/d
torsades de pointes / most GI SE
Lexapro / Escipharm
Escitalopram (HL 30H)
SSRI
(Serotonin agonist)
10-20 mg/d
Brintellix
Vortioxetine
SSRI
(Serotonin agonist at 5HT1A, and antagonist at 5HT3)
least sexual SE
Effexor
Venlafaxine
SNRI
(Serotonin and Norepinephrine agonist)
DC syndrome
Pristiq
Desvenlafaxine
SNRI
(Serotonin and Norepinephrine agonist)
Cymbalta
Duloxetine
SNRI
(Serotonin and Norepinephrine agonist + weak D Receptor inhibitor)
60 mg/d
for diabetic neuropathy and stress urinary incontinence
Wellbutrin / Bupran
Bupropion
NDRI
(Norepinephrine and Dopamine agonist)
Desyrel
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!)
Serzone
Nefazodone
Serotonin (SARI)
—> antagonist on 5HT2A, 5HT2C
—> agonist on (reuptake inhibitor) 5HT1A, 5HT2A, 5HT2C
blocks alpha 1 receptors
blocks H1 receptors
Remeron
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
Elavil / Tryptizole
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
Tofranil
Imipramine
TCA (1st gen, tertiary amine)
—> Serotonin and Norepinephrine agonist
—> Acetylcholine and Histamine antagonist
—> Na and Ca channel blockers
Anafranil
Clomipramine
TCA (1st gen, tertiary amine)
—> Serotonin and Norepinephrine agonist
—> Acetylcholine and Histamine antagonist
—> Na and Ca channel blockers
phobic and obsessional states / catalepsy
Sinequan
Doxepin
TCA (1st gen, tertiary amine)
—> Serotonin and Norepinephrine agonist
—> Acetylcholine and Histamine antagonist
—> Na and Ca channel blockers
Pamelor /Aventyl
Nortriptyline
TCA (2nd gen, secondary amine)
—> Serotonin and Norepinephrine agonist
—> Acetylcholine and Histamine antagonist
—> Na and Ca channel blockers
Norpramine
Desipramine
TCA (2nd gen, secondary amine)
—> Serotonin and Norepinephrine agonist
—> Acetylcholine and Histamine antagonist
—> Na and Ca channel blockers
Asendin
Amoxapine
Tetracyclic antidepressant (2nd gen, secondary amine)
—> Serotonin and Norepinephrine agonist
—> Acetylcholine and Histamine antagonist
—> Na and Ca channel blockers
Nardil
Phenelzine
MAOI
Inhibit MAO-A –> increases Serotonin and Norepinephrine
Inhibit MAO-B –> increases phenethylamine
Inhibit both –> increases Dopamine and tyramine
Parnate
Tranylcypromine
MAOI
Inhibit MAO-A –> increases Serotonin and Norepinephrine
Inhibit MAO-B –> increases phenethylamine
Inhibit both –> increases Dopamine and tyramine
Marplan
Isocarboxazid
MAOI
Inhibit MAO-A –> increases Serotonin and Norepinephrine
Inhibit MAO-B –> increases phenethylamine
Inhibit both –> increases Dopamine and tyramine
Thorazine
Chlorpromazine
Typical antipsychotic (1st gen)
Dopamine 2 antagonist
max: 1000mg
low potency
Mellaril
Thioridazine
Typical antipsychotic (1st gen)
Dopamine 2 antagonist
low potency
high risk of sudden death - discontinued
Loxitane
Loxapine
Typical antipsychotic (1st gen)
Dopamine 2 antagonist
mid potency
Navane
Thiothixene
Typical antipsychotic (1st gen)
Dopamine 2 antagonist
mid potency
Moban
Molindone
Typical antipsychotic (1st gen)
Dopamine 2 antagonist
mid potency
Trilafon
Perphenazine
Typical antipsychotic (1st gen)
Dopamine 2 antagonist
max: 24mg
mid potency
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
high potency
Prolixin
Fluphenazine
Typical antipsychotic (1st gen)
Dopamine 2 antagonist
- depot (modecate): test dose 12.5, depot max: 100mg Q2w
high potency
Stelazine
Trifluoperazine
Typical antipsychotic (1st gen)
Dopamine 2 antagonist
min:10-15mg /max:30mg
high potency
Orap
Pimozide
Typical antipsychotic (1st gen)
Dopamine 2 antagonist
high potency
High likelihood of QTc prologation
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
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
Risperdal / Respal
Risperidone (HL 20H)
Atypical antipsychotic
(D2 and 5HT2A receptor antagonists)
min: 2-4mg / max: 16mg, depot 50mg Q2w
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
max:750 schizophrenia, max:800 bipolar, used for bipolar depression
Zylanza / Zyprexa / Prexal / Olexa / Oprexa
Olanzapine (HL 30H)
Atypical antipsychotic
(D2 and 5HT2A receptor antagonists)
min:5-7.5mg / max:20mg
Geodon
Ziprasidone (HL 7H)
Atypical antipsychotic
(D2 and 5HT2A receptor antagonists)
min: 40-80mg /
Abilify / Aripal / Abizol / Zorta
Aripiprazole (HL 75H)
Atypical antipsychotic
- 5HT2A antagonist
- 5HT1A and D2 partial agonist
min: 10mg / max:30mg, depot max: 400mg Qm
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
Saphris
Asenapine
Atypical antipsychotic
(D2 and 5HT2A receptor antagonists)
min: 10mg / max: 20mg