Anti-Depressants, Anxiety, Bipolar Flashcards by Ashley Wong

Tricyclic Antidepressants- Available Drugs

Imipramine
AMITRYPTYLLINE
DOXEPIN
DESIPRAMINE (ACTIVE METABOLITE OF IMIPRAMINE)
NORYPTYLLINE
CLOMIPRAMINE

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Tricyclic Antidepressants- Mech of Action

block reuptake of serotonin and NE from nerve terminals

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Tricyclic Antidepressants- Adverse Effects/ contraindications

ANTI-HISTAMINE= SEDATING
ANTICHOLINERGIC EFFECTS
ANTI-ALPHA1 ADRENERGIC= ORTHOSTATIC HYPERTENSION
WEIGHT GAIN
SEXUAL DYSFUNCTION

CONTRAINDICATED IN ELDERLY

ADDITIVE EFFECT WHEN USED WITH OTHER CNS DEPRESSANTS

EASY TO OVERDOSE

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SSRIs- Available Drugs

FLUOXETINE (least 5-HT selective)
Sertraline
Paroxetine (highest 5-HT affinity)
Citalopram (most selective racemate)
Escitalopram (S+ isomer of Citalopram, more selective than citalopram)
Fluvoxamine

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SSRIs- Mech of Action

Selective, but not exclusive, blockade of 5-HT reuptake receptor

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SSRIs- Adverse Effects/ contraindications

SIDE EFFECTS BEFORE REACHING THERAPEUTICALLY EFFECTIVE DOSE
SEXUAL DYSFUNCTION
DISCONTINUATION SYNDROME (LESS COMMON W/ FLUOXETINE)

WITHDRAWAL SYMPTOMS IN NEWBORNS
INCREASED SUICIDAL THOUGHTS IN YOUNG PATIENTS

CAN BE LETHAL WHEN COMBINED W/ MAOIs

FLUOXETINE & FLUVOXAMINE INHIBIT MANY CYP ENZYMES= MANY DRUG INTERACTIONS

PAROXETINE= HEART DEFECTS IN PREGNANCY

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SNRIs- Available Drugs

Venlafaxine
Desvenlafaxine
Duloxetine

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SNRIs- Mech of Action

inhibit serotonin and NE reuptake

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SNRIs- Side Effects/ Contraindications

Fewer side effects than TCAs

Venlafaxine-
HYPERTENSION
SEXUAL DYSFUNCTION
nausea, anxiety, dizziness

Duloxetine-
SEXUAL DYSFUNCTION
elevated liver enzymes, dizziness

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Mixed Action/Atypical- Available Drugs

Mirtazapine
Vilazodone
Bupropion
Nefazodone

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Mirtazapine- Mech of Action

Alpha2 receptor antagonist, thus prevents synaptic feedback inhibition

Also blocks 5-HT2a/2c serotonin receptor and H1 histamine receptor (also blocking feedback inhibition)

Net result: increases activity of NE, 5-HT, and histamine

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Mirtazapine- Side Effects/Contraindications

HIGHLY SEDATING AT LOW DOSES
NO SEXUAL DYSFUNCTION
stimulatory at high doses
weight gain

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Vilazodone- Mech of Action

Blockade of 5-HT transporters

Partial agonist of 5-HT1A

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Vilazodone- Side Effects/Contraindications

NO SEXUAL DYSFUNCTION
diarrhea
nausea
vomiting
insomnia

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Bupropion- Mech of Action

may desensitize 5-HT1A and alpha-2 adrenergic receptor

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Bupropion- Side Effects/ Contraindications

NO SEXUAL DYSFUNCTION
NO ANTICHOLINERGIC OR ANTIADRENERGIC EFFECTS
WEIGHT LOSS
STIMULATORY EFFECTS
seizure risk at high doses

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Nefazodone- Mech of Action

5-HT reuptake inhibitor

5-HT2A receptor antagonist

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Nefazodone- Side Effects/Contraindications

NO SEXUAL DYSFUNCTION

NAME BRAND REMOVED FROM MARKET FOR LIVER TOXICITY, GENERIC STILL AVAILABLE

MAOIs- Available Drugs

Irreversible:
Phenelzine
Tranylcypromine
Selegeline

Reversible:
Meclobemide

MAOIs- Mech of Action

Inhibit MAO-A, MAO-B that metabolize monoamines and tyramine

MAOIs- Side Effects/ Contraindications

AGITATION
SLEEP DISTURBANCE
SEROTONIN SYNDROME
HYPERTENSIVE CRISIS

POTENTIALLY FETAL INTERACTIONS W/ DRUGS OR FOODS RICH IN TYRAMINE

SSRIs

Anti-Anxiety Drugs- Available Drugs

Buspirone

Benzodiazepines

Buspirone- Mech of Action

5-HT1A partial agonist

Benzodiazepines- Mech of Action

Bind BZ1 and BZ2 benzodiazepine receptors on the GABAa receptor complex= increases affinity of GABA for GABAa receptor= open chloride channel= hyperpolarization, inhibition

Benzodiazepines- Adverse Effects/Contraindications

SEDATION ANTEROGRADE AMNESIA REBOUND ANXIETY confusion, ataxia, physical dependence, tolerance

Lithium- Mech of Action

unknown effects on second messenger systems that mediate NT action inhibit enzymes involved in inositol recycling= depletion of PIP2 for IP3 and DAG increasing evidence for role of GSK-3 GOLD STANDARD FOR BIPOLAR DISORDER

Lithium- Side Effects/Contraindications

``` SLURRED SPEECH ATAXIA FINE TREMORS EXCESSIVE THIRST/URINATION RENAL TOXICITY INHIBITION OF THYROID HORMONE TOXICITY IN NEWBORNS edema ```

Anticonvulsants- Available Drugs

Valproic Acid Carbamazepine Lamotrigine

Valproic Acid- Mech of Action

Facilitate GABA synthesis and block its reuptake Influence GSK-3 Blocks sustained high frequency neuronal firing rates

Valproic Acid- Side Effects/ Contraindications

``` FINE TREMOR WEIGHT GAIN HEPATOTOXICITY TERATOGENIC BLOOD DYSCRASIAS nausea, vomiting, abdominal pain, heart burn, increased appetite, hair loss ```

Carbamazepine- Mech of Action

Reduce Na and K conductance Reduce release of NE and excitatory AA (glutamate) Adenosine receptor agonist (caffeine is the antagonist)

Carbamazepine- Side Effects/Contraindications

``` DERMATOLOGIC CONDITIONS ATAXIA SUICIDALITY NEURAL TUBE DEFECTS RARE BLOOD DYSCRASIAS FDA ALERT FOR STEVEN JOHNSON GI reactions rash ```

Lamotrigine- Side Effects/Contraindications

EFFECTIVE IN 2/3 OF PEOPLE THAT HAVEN'T RESPONDED TO OTHER DRUGS MORE ANTI-DEPRESSIVE THAN OTHER BIPOLAR DRUGS RELATIVELY BENIGN SIDE-EFFECTS TERATOGENIC- CLEFT LIP/PALATE dizziness, headache, double vision, blurred vision, unsteadiness, sleepiness, rash, vomiting; side effects increased w/ EtOH, may also cause Steven Johnson

Atypical Antipsychotics- Available Drugs

``` Risperidone Ziprasadone Olanzapine Quetiapine Aripipazole ```

Risperidone- Mech of Action

D2, 5-HT2, 5-HT7 receptor antagonist

Risperidone- Side Effects/Contraindications

DROWSINESS FATIGUE WEIGHT GAIN anxiety, low BP, muscle stiffness/pain side effects are common

Ziprasadone- Mech of Action

D2, 5-HT2, ALPHA1, H1 antagonist

Ziprasadone- Side Effects/Contraindications

SLEEPY TREMOR SHUFFLING upset stomach, constipation, dizzy, rash, restlessness

Quetiapine- Mech of Action

D2, D1, 5-HT2, 5HT1A, Alpha1, H1 Antagonist

Quetiapine- Side Effects/Contraindications

Common- SEDATION, dry mouth, constipation Less common: dizziness, upset stomach, abnormal liver tests, tardive dyskinesia Rare- LIFE THREATENING NEUROLIPTIC MALIGNANT SYNDROME (NMS)- AUTONOMIC INSTABILITY

Aripipazole- Mech of Action

partial agonist of D2 and 5-HT1a | 5-HT2 antagonist

Aripipazole- Side Effects/Contraindications

RARE: NEUROLEPTIC MALIGNANT SYNDROME (NMS)= HYPERPYREXIA, MUSCLE RIGIDITY, AUTONOMIC INSTABILITY no appreciable anticholinergic effects Common: akathesia, headach, tiredness, weakness, nausea, constipation, trouble sleeping, blurred vision CYP DRUG INTERACTIONS

Symbax (olanzapine + fluoxetine)- Side Effects/Contraindications

WEIGHT GAIN dizziness, drowsiness, diarrhea, dry mouth, constipation, increased appetite, trouble sleeping POSSIBLY FATAL INTERACTION WITH PIMOZIDE, SIBUTRAMINE, THIORIDAZINE, MAOIs