Agents For Depression

Front 1

Amitriptyline

Back 1

Tricyclic antidepressants (TCAs)
5 HT selective
has strong anti-cholinergic, antihistamine (H1),
and a1-adrenergic antagonist effects. strongly sedating,

Front 2

Clomipramine

Back 2

(Anafranil; generic)Tricyclic antidepressants (TCAs)
5 HT selective

Front 3

Desipramine

Back 3

(Norpramin; generic)Tricyclic antidepressants (TCAs) NE selective

Front 4

Doxepin

Back 4

(generic only)Tricyclic antidepressants (TCAs) NE selective

Front 5

Imipramine

Back 5

(Tofranil; generic)Tricyclic antidepressants (TCAs) 5 HT selective

Front 6

Nortriptyline

Back 6

(Pamelor; generic)Tricyclic antidepressants (TCAs) NE selective

Front 7

Protriptyline

Back 7

(Vivactil; generic)Tricyclic antidepressants (TCAs) NE selective

Front 8

Trimipramine

Back 8

(Surmontil)Tricyclic antidepressants (TCAs)

Front 9

Phenelzine

Back 9

(Nardil; generic) Monamine Oxidase Inhibitors,irreversible inhibitors, non-selective

Front 10

Tranylcypromine

Back 10

(Parnate; generic) Monamine Oxidase Inhibitors Reversable inhibitor, non-selective

Front 11

Isocarboxazid

Back 11

(Marplan) Monamine Oxidase Inhibitors, irreversible inhibitors, non-selective

Front 12

Selegiline

Back 12

(Emsam patch: for depression; Carbex, Etdepryl, Zelapar for
Parkinson’s) Monamine Oxidase Inhibitors,irreversible inhibitors
selective for MAO-B at low doses beneficial in Parkinson’s
At higher concentrations, MAO-A is inhibited (needed for depression)
metabolites are amphetamine and metamphetamine!
NO Hepatotoxicity

Front 13

MAO-Is + Following May Result in Serotonin Syndrome:

Back 13

• TCAs, SSRIs, SNRIs, SARIs, NaSSAs, Vilazodone
• Triptans (Migraine)
• Ergots
• Opiates: Tramodol, Fentanyl, Meperidine, Dextromethorphan
• Linezolid (Zyvox, antibiotic with MAO-I activity)
• St. John’s Wort

Front 14

Fluoxetine

Back 14

(Prozac) SSRI bulimia, depression, OCD, Panic Disorder, PMDD
Weight loss

Front 15

Fluvoxamine

Back 15

(Luvox) SSRI OCD, SAD only

Front 16

Paroxetine

Back 16

(Paxil) SSRI depression, GAD, OCD, Panic Disorder, PTSD, PMDD, SAD
Weight gain

Front 17

Sertraline

Back 17

(Zoloft) SSRI depression, OCD, Panic Disorder, PTSD, PMDD, SAD

Front 18

Citalopram

Back 18

(Celexa) SSRI depression

Front 19

Escitalopram

Back 19

(Lexapro) SSRI depression, GAD

Front 20

SSRI Pharmacology

Back 20

blockade of serotonin reuptake without “baggage” of
TCAs (eg. anti-histamine, a1 block, antimuscarinic effects) or cardiac/BP effects
of SNRIs. Elevated serotonin levels result in elevated serotonergic
neurotransmission and receptor changes mentioned above. Adverse effects are
primarily due to 5-HT receptors.

Front 21

SSRI Adverse Effects

Back 21

CNS:
• Anxiety/nervousness• Agitation • Insomnia Sedation/hypersomnia (fluvoxamine primarily)• Headache
• Yawning
GI :• Nausea/Vomiting• Diarrhea
Sexual Effects:• Decreased libido • Impaired arousal
• Delayed/absent orgasm

• Bleeding disorders/anti-platelet activity

Front 22

Venlafaxine

Back 22

(Effexor XR; generic) (SNRIs) MDD, SAD, GAD, Panic

Front 23

Desvenlafaxine

Back 23

(Pristiq) (SNRIs) MDD only

Front 24

Duloxetine

Back 24

(Cymbalta) (SNRIs) MDD, Diabetic Neuropathy, fibromyalgia, GAD, Musculo-skeletal pain,
osteoarthritis.

Front 25

SNRI Pharmacology

Back 25

SNRIs have activity against SERT (serotonin transporter) and
NET (NE transporter), but not DAT (DA transporter). They differ from TCAs in that they don’t have (or have far fewer) anti-cholinergic, anti-histaminergic or anti-a1 adrenergic effects. Venlafaxine is converted to desvenlafaxine as its active metabolite. Ven/Des have more potent SERT than NET activity; Duloxetine is more balanced, but stronger SERT activity than NET.

Front 26

SNRI Adverse Effects

Back 26

• All SSRI effects +
o Cardiac Effects: dose-related hypertension (Ven IR worse than Ven ER),
tachyarrhythmias
o Other NE effects: excessive sweating, constipation, increased Pulse Rate
o Hepatotoxicity
o Hypercholesterolemia (Ven/Des primarily) and lipid changes
o CNS effects include: agitation, anxiety, insomnia

Front 27

Bupropion

Back 27

(Wellbutrin) “Norepinephrine & Dopamine Reuptake Inhibitor
(NDRI) MDD, SAD, nicotine withdrawal
much-reduced sexual
adverse effects compared to SSRIs and SNRIs.

Front 28

Bupropion Pharmacodynamic Interactions:

Back 28

• MAO-Is: additive adverse effects
• Agents that lower seizure thresholds: TCAs, anti-psychotics
• Benzodiazepine Withdrawal: lowers seizure threshold
• Anti-seizure medications

Front 29

Bupropion Adverse Effects:

Back 29

• Seizures (dose-related)
• Insomnia/nightmares
• Psychotic manifestations: delusions and hallucinations
• Anxiety/agitation
• Headache
• Tremor
• Nausea/vomiting
• Weight loss

Front 30

Nefazodone

Back 30

(generic only) Serotonin Antagonists/Reuptake Inhibitors (SARIs) MDD, Insomnia (off-label, but common use)5-HT2 receptor antagonists, and block reuptake of 5-HT (SERT) modest effects on NET some a1 adrenergic antagonist effects associated with fewer sexual side effects than SSRIs or
SNRIs.

Front 31

Trazodone

Back 31

(Oleptro; generic) Serotonin Antagonists/Reuptake Inhibitors (SARIs) MDD, Insomnia (off-label, but common use)5-HT2 receptor antagonists, and block reuptake of 5-HT (SERT) some a1 adrenergic antagonist effects
modest antihistamine
(H1) effects

Front 32

(SARIs) Pharmacokinetics:

Back 32

Both Nefazodone and Trazodone are
metabolized to mCPP, a potent and non-selective 5-HT receptor agonist (particularly
5-HT-1 and 2 series).

Front 33

(SARIs) Pharmacodynamic Interactions:

Back 33

• MAO-Inhibitors: Serotonin Syndrome
• Clonidine: may decrease anti-hypertensive effect
• CNS depressants: additive sedation
• Other 5-HT agents: Serotonin Syndrome

Front 34

(SARIs) Adverse Effects:

Back 34

• Sedation (trazodone > nefazodone)
• Orthostatic hypotension (traz > nef) Which receptor?
• Arrhythmias
• Dizziness • Nausea
• Abnormal vision (nef > traz)
• Sexual Dysfunction (traz > nef)
• Priapism (trazodone primarily)
• Hepatotoxicity ***(nef- black box)****

Front 35

Mirtazapine

Back 35

(Remeron; generic) Noradrenergic and Specific Serotonergic Antidepressants (NaSSAs) MDD Central (primarily) a2 adrenergic antagonist with little effect on
periphery; blocks “auto” and “hetero” receptors to elevate both NE and 5-HT in
brain synapses. Also blocks postsynaptic 5-HT receptors: particularly 2A, 2C and 3.

Front 36

Mirtazapine Pharmacodynamic Interactions:

Back 36

• MAO-Is
• Serotonin Agents
• Clonidine Why?

Front 37

Mirtazapine Adverse Effects/Precautions:

Back 37

• Sedation
• Weight Gain
• Agranulocytosis and Neutropenia (probably minor risk; watch for flu-like
symptoms)
• Elevated Liver enzymes (monitor)
• Elevated cholesterol and triglycerides (in some patients; monitor)

Front 38

Vilazodone

Back 38

(Viibryd) MDD Inhibitor of SERT and is a 5-HT1A partial agonist. 5-HT1A receptors
are found as “autoreceptors” on 5-HT neurons and also postsynaptically. Upon acute
administration, 5-HT1A autoreceptor activation results in decreased 5-HT release from
presynaptic nerves. Upon chronic treatment, these autoreceptors desensitize resulting
in increased 5-HT release and increased postsynaptic 5-HT1A receptor activation.

Front 39

Vilazodone Pharmacodynamic Interactions: Adverse Effects:

Back 39

• MAO-Is and other 5-HT enhancing agents: Serotonin Syndrome
• GI: N/V, diarrhea
• Sexual Dysfunction: not as prevalent as SSRIs
• Discontinuation/Withdrawal Symptoms
• Platelet dysfunction