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35 Cards in this Set
- Front
- Back
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 |
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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) |
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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 |
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Fluvoxamine
(floo-VOKS-a-meen) |
Trade name: Luvox
Drug Class: SSRI (2nd generation) Administration: PO Clinical Indications: MINIMAL use due to multiple drug interactions |
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Citalopram
(sye-TAL-oh-pram) |
Trade name: Celexa
Drug Class: SSRI (2nd generation) Administration: PO Clinical Indications: MDD Interactions: Minimal inhibition of cytochrome enzymes |
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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 |
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SSRIs: Class Effect ADRs
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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 |
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Serotonin Syndrome
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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 |
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SSRIs and Pregnancy
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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. |
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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 |
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Desvenlafaxine
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Trade name: Pristiq
Drug Class: SNRI Administration: PO Clinical Indications: MDD, GAD, SAD, panic disorder +/- agoraphobia Interactions: CYP3A4 substrate |
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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 |
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SNRIs: Class Effect ADRs
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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* |
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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* |
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Trazadone
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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)* |
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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 |
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Imipramine (im-IP-ra-meen) and Amitriptyline
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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* |
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Desipramine (des-IP-ra-meen), Nortriptyline (nor-TRIP-ti-leen)
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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* |
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Tricyclic Antidepressants (general)
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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 |
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TCA ADRs
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*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* |
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Isocarboxazid, Tranylcypromine, Phenelzine** (FEN-el-zeen)
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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") |
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MAO-A Inhibitors: Contraindications and ADRs
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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 |
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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 |
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Buspirone
(byoo-SPYE-rone) |
Trade name: BuSpar
Administration: PO Clinical Indications: GAD Interactions: CYP3A4 substrate ADRs: Dizziness, sedation common |
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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 |
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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 |
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Benzodiazepines (general)
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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) |
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Lithium
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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 |
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Lithium and Pregnancy
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1st trimester: Congenital cardiac abnormalities, *Ebstein's anomaly
3rd trimester: Nontoxic effects - shallow respiration, hypotonia, lethargy, cyanosis, DI, thyroid dysfunction |
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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 |
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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* |
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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) |
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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 |
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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 |
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Monitoring Parameters for Atypical Antipsychotics
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-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 |