Pharm Ii - Anti-Depressant

Front 1

amitriptyline (Elavil)

Back 1

Anti-depressant - TCA

Front 2

bupropion (Wellbutrin, Zyban)

Back 2

Anti-depressant - monocyclic
Treatment of nicotine dependence

buproprion makes it so we don't NEeD Another smoke (NE/DA reuptake inhibitor)

Front 3

citalopram (Celexa)

Back 3

SRI:
Anti-depressant
Anti-anxiety

If the Taliban took some Citalopram, maybe they would stop suicide bombing (anti-depressant)

"A Flock of SERTified SIRens SITs (cit) and blocks CYPrus" - fluoxetine, fluvoxamine, sertraline, and citalopram are SRIs; inhibit CYPs

Front 4

desipramine (Norpramin)

Back 4

Anti-depressant - TCA

Front 5

fluoxetine (Prozac)

Back 5

SRI:
Antidepressant
Anti-anxiety

"A Flock of SERTified SIRens SITs (cit) and blocks CYPrus" - fluoxetine, fluvoxamine, sertraline, and citalopram are SRIs; inhibit CYPs

Front 6

fluvoxamine (Luvox)

Back 6

SRI:
Anti-depressant
Anti-anxiety

"A Flock of SERTified SIRens SITs (cit) and blocks CYPrus" - fluoxetine, fluvoxamine, sertraline, and citalopram are SRIs; inhibit CYPs

people who are anxious about the flu should get a fluvox (vax).

Front 7

imipramine (Tofranil)

Back 7

Anti-depressant - TCA

I'm-a-pray'in I feel better.

Front 8

lithium

Back 8

Anti-manic drug

Front 9

moclobemide (Aurorex)

Back 9

Anti-depressant - reversible inhibitor of MAO-A

Don't MOCk Mao (moclobemide is an MAOI)

Front 10

nefazodone (Serzone)

Back 10

Anti-depressant
Serontonin 2A receptor antagonist + SRI


1. Potent antagonist at 5-HT2 post-synaptic receptors.
2. Inhibits pre-synaptic reuptake of serotonin.
3. Minimal inhibition of norepinephrine uptake.
4. Blocks alpha-1 receptors peripherally.
5. No effects on muscarinic, or histaminic receptors.

Front 11

nortriptyline (Pamelor)

Back 11

Anti-depressant - TCA

"No trip" "don't break that hip": this one has the least orthostatic hypotension of the TCA's. Drug of choice for elderly pop.

NortriptyLINE makes you feel FINE (pain management)
with NORtryptyline, you will feel neither depressed NOR in pain.

Front 12

paroxetine (Paxil)

Back 12

SRI:
Anti-depressant
Anti-anxiety

if I were on parole, I'd be anxious all of the time. I'd want to take paroxetine.

Front 13

phenelzine (Nardil)

Back 13

Anti-depressant - Hydrazine derivative
Irreversible inhibitor of MAO

The Phenelzine limozine drives around the body picking up all of the MAOs.
Phenel is FINAL (irreversible inhibition)

Front 14

selegiline (Deprenyl)

Back 14

Anti-depressant - Selective inhibitor of MAO-B

"Seleg"-tively inhibits MAO-B (good for Parkinson's)

Front 15

sertraline (Zoloft)

Back 15

SRI:
Anti-depressant
Anti-anxiety

"A Flock of SERTified SIRens SITs (cit) and blocks CYPrus" - fluoxetine, fluvoxamine, sertraline, and citalopram are SRIs; inhibit CYPs

Sertraline at your Service! I'm here to make you feel less depressed or less anxious!

Front 16

tranylcypromine (Parnate)

Back 16

Anti-depressant - Nonhydrazine derivative. Slow reversible inhibitor of MAO

It takes a long time for trannies to transition. This drug's MAO inhibition is slowly reversible.

Front 17

venlafaxine (Effexor)

Back 17

Anti-depressant - Serotonin/Norepinephrine Reuptake Inhibitor

VenLAFazine makes you laf at Stupid, Noisy, Ridiculous Idiots (SNRI).

Potency is greater for inhibition of serotonin than norepinephrine. The side effect profile is very similar to SRIs since its most potent effect is on serotonin.

Front 18

Systems targeted by anti-depressants

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Major pathways of neurohormonal transmission are serotonergic, adrenergic and cholinergic.

Front 19

Monoamine oxidase inhibitors (MAOIs)

Back 19

phenelzine
tranylcypromine
isocarboxazid
selegeline

General MAO MOnoCLOnally (moclobemide) SELEcted (selegiline) a TRANnY/transvestite (tranylcypromine) for his PHriend (phenelzine)

Front 20

Serotonin reuptake inhibitors (SRIs)

Back 20

citalopram
fluoxetine
fluvoxamine
sertraline
paroxetine

SERTainly (sertraline) it's a PARadOX (paroxetine) if you can FLUV (fluvoxamine) but can't FLUOX (fluoxetine) in the CITAaaayyy (citalopram)

Front 21

Norepinephrine/dopamine reuptake inhibitors (NDRIs)

Back 21

bupropion

Front 22

Serotonin/norepinephrine reuptake inhibitors (SNRIs)

Back 22

venlafaxine

Front 23

Serotonin type 2A receptor (5 –HT2A) antagonists and reuptake inhibitors

Back 23

nefazodone

Front 24

Serotonin/norepinephrine reuptake inhibitors, antihistamines, anticholinergic, alpha-1 blockers

Back 24

tricyclic antidepressants

Front 25

5-HT1A receptors (pre-synaptic)

Back 25

Presynaptic on cell bodies in midbrain raphe, control firing rate of serotonergic neurons (autoreceptors). Stimulation of these autoreceptors by serotonin decreases neuronal firing, therefore, providing negative feed back.

Front 26

5-HT1D receptor (pre-synaptic)

Back 26

Presynaptic axon terminal also controls serotonin release from presynaptic part of cleft. If this receptor is stimulated it also reduces the release of 5HT from the nerve terminal.

Front 27

5-HT1A receptors (post-synaptic)

Back 27

5-HT1A receptor (postsynaptic) controls firing rate of serotonin system. These receptors may be involved in anxiety; depression; aggression; panic attack; obsessive-compulsive behavior.

Front 28

5HT2A (postsynaptic)

Back 28

when stimulated by 5-HT release from presynaptic terminal causes increased firing of post synaptic cell. Stimulation responsible for depression; anxiety; psychosis; hallucinations; sleep disorders (insomnia), and decreased sexual function.

Front 29

5HT2C (postsynaptic)

Back 29

involved in anxiety; aggression; depression; sensory information; nociception; appetite stimulation; weight gain.

Front 30

5HT3 receptor (postsynaptic)

Back 30

In brain (area postrema) and in gut. SRIs cause nausea and diarrhea through the stimulatory effect of serotonin on these receptors. Specific 5HT3 blockers are used to treat nausea and vomiting by blocking these receptors at both central and peripheral locations

Front 31

Dopamine deficiency

Back 31

Decreased ability to experience pleasure, decreased motivation, apathy, decreased attention, cognitive slowing.

Front 32

Norepinephrine deficiency

Back 32

Depression, lethargy, decreased alertness

Front 33

Serotonergic side effects

Back 33

-Sexual dysfunction
-GI upset
-Sleep disturbance
-Suppression of dopamine neurotransmission, which may result in:
•Decreased ability to experience pleasure
•Apathy and decreased motivation
•Decreased attention
•Cognitive slowing

Front 34

Noradrenergic side effects

Back 34

-Tremor
-Tachycardia

Front 35

Dopaminergic side effects

Back 35

-Psychomotor activation
-Aggravation of psychosis

Front 36

Tricyclic antidepressants

Back 36

Sertonin/Norepinephrine Reuptake inhibitirs (SNRIs)

imipramine
desipramine
amitriptyline
nortriptyline

I'm (Imipramine) neither Desperate (Desipramine) Nor (Nortriptylene) Am-I-Tryppin (Amitriptyline) on my tricycle (tricyclics)

Front 37

TCA side effects on other receptor systems

Back 37

a. Antagonism of central and peripheral α1-adrenergic receptors.
c. Anticholinergic effect (central and peripheral)
The drugs block muscarinic receptors. Amitriptyline has pronounced anticholinergic activity while desipramine has relatively weak anticholinergic effects.
d. H1 receptor block.
e. 5HT2 receptor block (amitriptyline).

Front 38

Metabolism of TCAs

Back 38

Amitriptyline and imipramine are metabolized by CYP3A4
Their metabolites, desipramine and nortriptyline are metabolized by CYP2D6

Front 39

TCA side effects

Back 39

Side effects of ALL tricyclics: "OH, TCA'S!" Orthostatic Hypotension, Tachycardia, Confusion/Cardiac arrhythmias, Anti-cholinergic, Sedation

-Peripheral anticholinergic effects
-Acute confusional state
-Orthostatic hypotension
-Cardiac: slows heart, should not be given patients with a previous MI
-Sedation

Front 40

MAO inhibition

Back 40

1. CNS
Excessive central nervous system stimulation, including insomnia, agitation, irritability, ataxia, and seizures.
2. Peripheral vascular effects
Orthostatic hypotension, dizziness. It is uncertain if this is related to MAO inhibition.
3. Anticholinergic action
Urinary retention, constipation, dry mouth, blurred vision.

Front 41

DDI of MAOI

Back 41

Prolongation of the half-lives of drugs that must undergo oxidative deamination in the liver which is inhibited by MAOIs. MAOIs may potentiate the effect of alcohol, sedative-hypnotics and analgesics. Severe reactions may occur if patients taking MAOIs are given meperidine (see lecture on Strong Analgesics). Patients on MAOIs should never be given meperidine, but may be given other narcotics for analgesia.

Front 42

Side effects of SRIs

Back 42

The most frequently occurring significant side effect of the SRIs is difficulty reaching orgasm or delayed ejaculation.
Also causes nausea and vomiting (GI disturbances), nervousness/ restlessness/anxiety, and sleep disruption.

"CHIEFS" CNS (anxiety, restlessness), Headache, Insomnia, Enteric (nausea), Fat, Sex
Also, can think of the SRI side effects as S's (for serotonin):
-Stomach: GI (nausea, vomiting)
-Sex: delayed orgasm
-Sleep disruption
-Shaky: nervousness/anxiety
-Softness: weight gain (mild)
-Severe headache

Front 43

bupropion

Metabolism

Back 43

Metabolized by CYP2D6 and also partially inhibits the enzyme.
Tricyclic antidepressants, Antiarrhythmics, haloperidol, propranolol, codeine, and many other drugs are metabolized by 2D6.

Front 44

DDI of SRI:
CYP2D6

Back 44

Inhibition by paroxetine, fluoxetine, sertraline
CYP2D6 metabolizes anti-arrhythmics, haloperidol, propranolol, codeine

Front 45

DDI of SRI:
CYP3A4

Back 45

Inhibition by norfluoxetine which it metabolizes

Front 46

DDI of SRI:
CYP1A2

Back 46

Inhibited by fluvoxamine which it metabolizes

Front 47

bupropion

Side effects

Back 47

Headache/migraine, insomnia, anxiety, irritability, weight loss, anticholinergic effects. Seizures (dose dependent). Infrequent changes in sexual function

Front 48

venlafaxine (Effexor)

Side effects

Back 48

-Drowsiness
-Dose related hypertension

Front 49

Nefazodone (Serzone)

Metabolism

Back 49

-Large first pass liver metabolism
-Liver metabolism by CYP3A4 to active metabolites (hydroxynefazodone, trazoledine). The drug also inhibits this enzyme. (DDI with calcium channel blockers, clozapine, triazolam)

Front 50

Nefazodone (Serzone)

Adverse effects

Back 50

-Rarely, causes lived damage, but got pulled from the market for it
-Drowsiness
-infrequent, changes in sexual function

Front 51

Lithium

Metabolism

Back 51

-Readily absorbed from the GI tract, eliminated in the urine
-Anything which impacts renal excretion (primarily proximal tubule) will effect lithium levels: dehydration, sodium loss, diuretics, and NSAIDS may increase lithium levels; aminophylline, osmotic diuretics, acetazolamide can decrease lithium levels by increasing renal excretion.

Front 52

Lithium

Adverse effects

Back 52

-Diarrhea, nausea, tremor, sedation.
-Toxic effects: GI effects, seizures, ataxia, coma.
-A small number of patients may develop thyroid dysfunction, with a goiter; however, hypothyroidism is uncommon.
-Polydipsia and polyuria occur in many patients. Small number develop chronic inflammatory change in the kidney.

"CHASTER" (as in, more chaste, since you're no longer manic): Coma, Hypothyroid, Ataxia, Seizures/Sedation, Tremor, Enteric (nausea/vomiting), Renal (polydipsia/polyuria)

Front 53

Side effects of all MAOIs

Back 53

"NightCAP" No drinking, or evening dose of Demerol (?); CNS, Anticholinergic, Peripheral vasodilation