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35 Cards in this Set

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Fluoxetine
(floo-OXS-e-teen)
Trade name: Prozac
Drug Class: SSRI (1st generation)
Administration: PO
Clinical Indications: MDD (incl. kids), OCD (incl. kids), panic disorder +/- agoraphobia, bulimia, PMDD
Interactions:
-CYP2C9 & 2D6 substrate (converted to norfluoxetine) - combination of active fluoxetine and norfluoxetine = half-life of ~14 days
-Potent inhibitor of CYP2D6
Sertraline
(ser-TRA-leen)
Trade name: Zoloft
Drug Class: SSRI (1st generation)
Administration: PO
Clinical Indications: MDD, OCD (incl. kids), SAD, panic disorder +/- agoraphobia, PTSD, PMDD
Interactions: Dose-dependent CYP2D6 inhibition ("cleaner" SSRI)
Paroxetine
(pa-ROKS-e-teen)
Trade name: Paxil
Drug Class: SSRI (1st generation)
Administration: PO
Clinical Indications: MDD, OCD, SAD, GAD, panic disorder +/- agoraphobia, PTSD, PMDD
Interactions: Potent CYP2D6 inhibitor; Category D in pregnancy - high risk of major and CV malformations
Fluvoxamine
(floo-VOKS-a-meen)
Trade name: Luvox
Drug Class: SSRI (2nd generation)
Administration: PO
Clinical Indications: MINIMAL use due to multiple drug interactions
Citalopram
(sye-TAL-oh-pram)
Trade name: Celexa
Drug Class: SSRI (2nd generation)
Administration: PO
Clinical Indications: MDD
Interactions: Minimal inhibition of cytochrome enzymes
Escitalopram
(es-sye-TAL-oh-pram)
Trade name: Lexapro
Drug Class: SSRI (2nd generation)
Administration: PO
Clinical Indications: MDD, GAD
*S-enantiomer of citalopram*
Interactions: Minimal inhibition of cytochrome enzymes
SSRIs: Class Effect ADRs
1. Suicidal ideation & behavior (*esp in initiation of therapy or dosage changes*)
2. Serotonin Syndrome
3. Sexual SEs (ED, anorgasm (women), decreased libido)
4. Anorexia, then weight gain
5. Sedation, bruxism, SIADH (elderly)
6. Discontinuation Syndrome - TAPER
Serotonin Syndrome
Cause: Combination of SSRIs and MAOIs*, additional SSRIs, SNRIs, TCAs, St. John's Wort, buspirone, mirtazipine, trazadone
- possible with "triptans," INH, linezolid, DM, tramadol, Li, meperidine, selegiline

Sx:
Mild: increased HR, diaphoresis, mydriasis, tremor/shivering, hyperreflexia
Moderate: HTN, fever, hyperreflexia, clonus (ocular and LE>UE), AMS changes
Severe: Agitated delirium, severe HTN, marked tachycardia, rigidity, high fevers, possible seizures/CV shock
*uncontrolled hyperthermia can cause rhabdo, DIC & ARF

Tx:
1. D/C ALL serotenergic meds
2. Cooling measures
3. Benzodiazepines & cyproheptadine (antihistamine w/ serotonin antagonist properties)
4. Intubate if necessary
SSRIs and Pregnancy
MDD associated with intrauterine growth problems and low birth weight - must weigh risks.
Most SSRIs are category C (except Paroxetine - category D); may be related to development of persistent pulmonary HTN.
Venlafaxine
(VEN-la-faks-een)
Trade name: Effexor, Effexor XR
Drug Class: SNRI
Administration: PO
Clinical Indications: MDD, GAD, SAD, panic disorder +/- agoraphobia
Interactions: CYP2D6 & 3A4 substrate
Desvenlafaxine
Trade name: Pristiq
Drug Class: SNRI
Administration: PO
Clinical Indications: MDD, GAD, SAD, panic disorder +/- agoraphobia
Interactions: CYP3A4 substrate
Duloxetine
(doo-LOX-e-teen)
Trade name: Cymbalta
Drug Class: SNRI
Administration: PO
Clinical Indications: MDD, GAD, diabetic peripheral neuropathy pain, fibromyalgia
*may work in patients that didn't respond to or couldn't tolerate an SSRI*
Interactions: CYP2D6 substrate, moderate CYP2D6 inhibitor
SNRIs: Class Effect ADRs
1. Dose-dependent BP increase
2. Nausea, dizziness, insomnia, and constipation common
3. Discontinuation Syndrome: even after one missed dose, may be more severe than with SSRIs - TAPER
4. Serotonin Syndrome
5. May cause neonatal behavioral syndrome in 3rd trimester
*may have less sexual SEs than SSRIs*
Bupropion
(byoo-PROE-pee-on)
Trade name: Wellbutrin, Zyban
Drug Class: Structural analogue of amphetamines
Administration: PO
Clinical Indications: MDD, seasonal affective disorder ("prophylaxis"), smoking cessation (Zyban)
Interactions: Minimal cytochrome interaction, **seizure threshold-lowering drugs (antipsychotics, FQ, theophylline) - contraindicated in seizure patients**
ADRs: HA, anxiety/insomnia, possible seizures in anorexia/bulimia patients
*Minimal sexual dysfunction, sedation, and weight gain*
Trazadone
Administration: PO
Clinical Indications: MDD (esp with insomnia) *NOT 1st line*
Interactions:
- CYP3A4 substrate, moderate CYP2D6 inhibitor
- CNS depressants (because of sedation effect)
ADRs:
-SEDATION
-Postural hypotension
-Priapism
-Assoc. w/ cardiac dysrhythmias
-Hepatotoxicity (failure)*
Mirtazapine
(mir-TAZ-a-peen)
Trade name: Remeron, Remeron SolTab
MOA: increases NE and serotonin, potent H1 receptor antagonist (= sedation)
Clinical Indications: MDD (esp with insomnia or anorexia) *used more in older patients*
Interactions: Minimal cytochrome inhibition, *CNS depressants
ADRs: SEDATION (more sedation at lower doses), increased appetite/weight gain, dry mouth
Imipramine (im-IP-ra-meen) and Amitriptyline
Drug Class: TCAs (tertiary amines)
Administration: PO
MOA: thought to increase synaptic serotonin +/- NE concentrations in the CNS by blocking reuptake; additional receptor activity causes orthostasis, sedation and wt gain, anticholinergic effects
*Used LESS commonly due to ADRs*
Desipramine (des-IP-ra-meen), Nortriptyline (nor-TRIP-ti-leen)
Trade name: Desipramine - Norpramin; Nortriptyline - Pamelor
Drug Class: TCAs (secondary amines)
MOA: Similar to tertiary with less receptor activity = less severe ADRs
*Used MORE commonly because they are better tolerated*
Tricyclic Antidepressants (general)
Clinical Indications:
Labeled: MDD (pts intolerant or refractory to SSRI/SNRI), nocturnal enuresis in kids (imipramine)
Unlabeled: Neurogenic pain, migraine prophylaxis (amitriptyline)
*Do NOT use for sleep*
Interactions: CYP2D6 substrates, moderate CYP2D6 inhibitor; CNS depressants, anticholinergic agents (ex: Benedryl), QTc prolonging agents
Clinical Issues:
Initiation/Withdrawal:
-Need baseline EKG to check for cardiac conduction abnormalities (required for pts > 40)
-no abrupt withdrawal - TAPER
TCA ADRs
*ADRs more common with tertiary amines than secondary*
1. Overdose - respiratory suppression, cardiac arrhythmias, hypothermia, seizures, hallucinations, HTN for up to 5 days
-fatality usually due to QT prolongation
2. Orthostatic hypotension (common)
3. Sedation
4. Anticholinergic effects
5. Gynecomastia, libido changes, SIADH
*No known effects on pregnancy*
Isocarboxazid, Tranylcypromine, Phenelzine** (FEN-el-zeen)
Trade name: Phenelzine - Nardil
Drug Class: MAO-A inhibitors
MOA: Inhibits MAO-A, increasing concentrations of serotonin and NE
Administration: PO
Clinical Indications: Atypical MDD - usually issued by psychiatrist
Interactions:
-Sympathomimetics, CNS depressants, serotonergic drugs, ETOH, high tyramine foods (ex: "cheese-induced crisis")
MAO-A Inhibitors: Contraindications and ADRs
Contraindications: Comorbid disease (Uncontrolled HTN, CHF, pheochromocytoma)

ADRs:
1. Dizziness*
2. Xerostomia, nausea, HA common
3. Abrupt cessation can cause delirium, agitation, myoclonic jerks, insomnia
Selegiline
(se-LE-ji-leen)
Trade name: Emsam
Drug Class: MAO-B inhibitor
MOA: selective for MAO-B at low dose (=increased DA); nonselective at high concentrations
Administration: Transdermal (patch)
Clinical Indications: "Atypical" MDD - usually issued by psychiatrist
Interactions: Sympathomimetics, CNS depressants, sertonergic drugs
-Fewer diet interactions than MAO-A inhibitors (no diet restrictions with 6mg patch)
ADRs: Skin irritation from patch most common
Buspirone
(byoo-SPYE-rone)
Trade name: BuSpar
Administration: PO
Clinical Indications: GAD
Interactions: CYP3A4 substrate
ADRs: Dizziness, sedation common
Alprazolam
(al-PRAY-zoe-lam)
Trade name: Xanax, Xanax XR
Drug Class: Benzodiazepine
Administration: PO
Clinical Indications: GAD, panic disorder +/- agoraphobia (outpatient)
Interactions: CYP3A4 substrate, CNS depressants
Lorazepam
(lor-A-ze-pam)
Trade name: Ativan
Drug Class: Benzodiazepine
Administration: PO, IM, IV
Clinical Indications: Status epilepticus, ETOH withdrawal/"agitation" (SIWA protocol) - preferred use "in house"
Interactions: CNS depressants
Benzodiazepines (general)
MOA: Binds BZD receptors on postsynaptic GABA neuron --> hyperpolarization/stabilization (in GABA-A)
ADRs:
1. Dose-related sedation, dizziness, confusion, ataxia
2. Teratogenicity
3. Abuse potential (related to speed of onset)
4. Abrupt discontinuation = withdrawal sx (increased temp/BP/pulse/RR, delirium, tremulousness)
Lithium
Trade name: Lithium, Lithobid
Administration: PO
Clinical Indications: Bipolar disorder (mood stabilizer)
Interactions:
*Kidney doesn't differentiate between Li and Na*
Increase Li: thiazides, NSAIDs, ACEI
Decrease Li: K-sparing diuretics
Can increase or decrease Li: Loop diuretics, CCBs
*Narrow therapeutic window*
ADRs:
Most common: N/V/D, tremor (tx by lower dose or adding BB), weight gain, polyuria (nocturia)/polydipsia (from nephrogenic diabetes insipidus - ADH resistance)
Long-term: Potential for renal impairment (renal tubular acidosis > nephrotic syndrome), cardiac dysrhythmia, hypothyroidism > hyperthyroidism
Lithium and Pregnancy
1st trimester: Congenital cardiac abnormalities, *Ebstein's anomaly

3rd trimester: Nontoxic effects - shallow respiration, hypotonia, lethargy, cyanosis, DI, thyroid dysfunction
Chlorpromazine
(klor-PROE-ma-zeen)
Trade name: Thorazine
Drug Class: Phenothiazine
*Conventional" antipsychotic
Administration: PO, IM, IV*
MOA:
-antagonist at DA II receptors = EPS
-alpha receptors = orthostasis, depresses release of hypothalamic/hypophyseal hormones
-histaminic = sedation and wt gain
-muscarinic = anticholinergic effects
Clinical Indications: control of mania, schizophrenia, intractable hiccups
Interactions:
-CYP2D6 substrate AND inhibitor
-Anti-HTN agents, CNS depressants, QTc prolonging agents*
ADRs: EPS, postural hypotension, sedation, NMS, QTc prolongation*, increased prolactin
Haloperidol
(ha-loe-PER-i-dole)
Trade name: Haldol
Drug Class: Conventional antipsychotics (1st generation)
Administration: PO, IM, depot injection, IV*
MOA: Antagonist at postsynaptic mesolimbic DA receptors (= EPS); alpha receptors - orthostasis; histaminic - sedation and weight gain; muscarinic: anticholinergic effects
Clinical Indications:
Labeled: schizophrenia, Tourette's (tic/vocal utterance control)
Unlabeled: Psychosis, emergency sedation of severely agitated or delirious patients
Interactions: CYP2D6 and 3A4 substrate and moderate inhibitor; anti-HTN agents, CNS depressants, QTc prolonging agents
ADRs: EPS, postural hypotension, sedation, NMS, QTc prolongation*, increased prolactin
*Use EKG monitoring with IV Haldol*
*Large doses (PO/IM) or IV should not be used in patients with electrolyte imbalance, cardiac abnormalities, hypothyroidism, or taking other drugs that prolong QTc*
Clozapine
(KLOE-za-peen)
Trade name: Clozapine or Clozaril
Drug Class: "Atypical" (2nd generation) antipsychotic
Administration: PO, ODT
MOA: Antagonist at serotonin, DA4>DA2 receptors (= fewer EPS)
Clinical Indications: Refractory schizophrenia - typically prescribed by psychiatrist
*unlabeled use uncommon*
ADRs (specific to clozapine):
-Dose-dependent seizure risk
-Agranulocytosis (required to strictly monitor WBC count throughout duration of tx)
Aripiprazole
(ay-ri-PIP-ray-zole)
Trade name: Abilify
Drug Class: Atypical (2nd generation) antipsychotics
Administration: PO, IM
MOA: Partial agonist* at DA2 and serotonin 1A receptors; antagonist at sertonin 2 receptors
"Special" Clinical Indication: FDA approved to tx depression in addition to an SSRI
Olanzapine (oh-LAN-za-peen)
Risperidone (ris-PER-i-done)
Quetiapine (kwe-TYE-a-peen)
Ziprasidone (zi-PRAY-si-done)
Paliperidone
Drug Class: "Atypical" (2nd generation) antipsychotics
Administration: PO, IM
*Exceptions:
Quetiapine and Paliperidone: only PO
MOA: Potent serotoninergic >> DA2 receptor antagonist (may = EPS)
-alpha: orthostasis
-histaminic: sedation and wt gain
-muscarinic: anticholinergic effects
Clinical Indications: Schizophrenia, acute manic episodes (bipolar)
*unlabeled use uncommon*
Interactions: Less cytochrome interactions than conventional antipsychotics; anticholinergic agents, CNS depressants, anti-HTN agents, QTc prolonging agents
ADRs (class effect): Sedation, postural hypotension, prolactin elevation, *wt gain/dislipidemia/DM*, dose dependent EPS
Monitoring Parameters for Atypical Antipsychotics
-BMI
-Fasting lipid profile (prior to tx, at 3 mo, then annually)
-Fasting blood glucose (Hgb A1c): prior to tx, at 3 mo, then annually