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Winter Exam #3 - Antidepressants, Antimanic Agents
n/a
39
Pharmacology
Graduate
01/30/2010

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Term
imipramine (Tofranil, Janimine)
Definition
TCA; protoype; block reuptake of NE and 5-HT (lesser); Brand: Tofranil, Janimine
Term
amitriptyline (Elavil)
Definition
TCA; block reuptake of NE and 5-HT (lesser); more sedation & anticholinergic activity; Brand: Elavil
Term
trazadone (Desyrel)
Definition
2nd generation antidepressant; inhibit reuptake of 5-HT but also block 5-HT2 receptors; lower anticholinergic & CV SEs; SEs: priapism, sexual dysfunction; VERY SEDATING! - dose at bed time; Brand: Desyrel
Term
nefazodone (Serzone)
Definition
2nd generation antidepressant; inhibit reuptake of 5-HT but also block 5-HT2 receptors; Brand: Serzone
Term
venlafaxine (Effexor), desvenlafaxine (Pristiq)
Definition
2nd generation antidepressants; inhibits DA, NE, & 5-HT reuptake; Tx: depression, generalized anxiety disorder (GAD); more rapid onset of action; fewer CV SEs but still can cause HPN, tachycardia; "Energizes" depressed individuals; one is active metabolite of drug; SEs: nausea, nervousness, anxiety, sweating, HTN, tachycardia, palpitations, sexual dysfunction; Brands: Effexor, Pristiq
Term
duloxetine (Cymbalta)
Definition
SNRI, 2nd generation antidepressant; newer drug that resembles venlafaxine; Brand: Cymbalta
Term
bupropion (Wellbutrin, Zyban)
Definition
2nd generation antidepressant; DA reuptake inhibitor; mild stimulant activity - "psychich energizer"; more likely to produce SEIZURES; used in tx of nicotine, cocaine, & amphetamine dependence; Brand: Wellbutrin, Zyban
Term
mirtazepine (Remeron)
Definition
2nd generation antidepressant; chemically different than SSRIs, TCAs; blocks presynaptic alpha-2 adrenergic receptors --> enhances release of NE & 5-HT, blocks some serotonin receptors; SEs: mild anticholinergic, hypotension, tachycardia; may be used to tx depression & anxiety disorders; Brand: Remeron
Term
fluoxetine (Prozac)
Definition
prototypical SSRI; selectively inhibits reuptake of 5-HT; Tx of depression, OCD, & GAD; SEs: MUCH less sedation, anticholinergic, & CV effects; Main SEs: HA, anxiety, tremor, agitation, nausea, sexual dysfunction; metabolized in liver; slowly eliminated, converted to several active metabolites, takes 4-5 weeks to get to SS & long times to be cleared; Brand: Prozac
Term
fluvoxamine (Luvox)
Definition
SSRI used mainly for Obsessive Compulsive Disorder (OCD)in US, tx for depression in foreign countries; selectively inhibits reuptake of 5-HT; Brand: Luvox
Term
sertraline (Zoloft)
Definition
SSRI; selectively inhibits reuptake of 5-HT; relatively slow elimination, several active metabolites formed, LESS potential for drug interactions; Brand: Zoloft
Term
paroxetine (Paxil)
Definition
SSRI; selectively inhibits reuptake of 5-HT; more rapidly metabolized, DOES NOT form active metabolites Brand: Paxil
Term
citalopram (Celexa), escitalopram (Lexapro)
Definition
newest SSRIs; selectively inhibits reuptake of 5-HT; Brands: Celexa, Lexapro; one is a racemic mixture of R & S-enantiomers, one is pure S-enantiomer
Term
atomoxetine (Strattera)
Definition
SNRI - selective norepinephrine reuptake inhibitor; used to tx ADHD in children & adults; SEs: suppression of appetite, decreased weight gain, increased BP, tachycardia, sexual dysfunction; Brand: Strattera
Term
phenelzine (Nardil)
Definition
MAO-I of both subtypes; third-line drugs for tx of depression; MoA: acute increases in synaptic levels of NE, 5-HT, & DA; chronic: decreased # & sensivitity of adrenergic & serotonergic receptors; Brand: Nardil
Term
tranylcypromine (Parnate)
Definition
MAO-I; third-line drugs for tx of depression; MoA: acute increases in synaptic levels of NE, 5-HT, & DA; chronic: decreased # & sensivitity of adrenergic & serotonergic receptors; Brand: Parnate
Term
selegiline (Emsam, Eldepryl)
Definition
selective MAO-B Inhibitor; tx of depression; Brand: Emsam (patch) - depression, Eldepryl (Oral tab) - Parkinson's dx
Term
lithium carbonate (Eskalith)
Definition
mood stabilizer; most effective drug for tx of manic depressive disorders; Effects: control of mood swings, most effective against manic phase but is effective against depressed phase; MoA: phospholipid theory; PK: excreted by kidney, enhanced reabsorption in Na-depleted pts, long half-life (20-24 hrs), 4-5 days to SS; Carefully monitor blood levels; Brand: Eskalith; Therapeutic Levels: 0.8 - 1.4 mEq/L, Severe toxicity levels: >2.0 mEq/L; Avoid in pts with pregnant pts, pts w/ renal dx, CV dx, or thyroid dx
Term
valproic acid analogs (Depakene/Depakote)
Definition
mood stabilizers; Brand: Depakene, Depakote
Term
carbamazepine (Tegretol)
Definition
mood stabilizer; Brand: Tegretol
Term
clonazepam (Klonopin)
Definition
mood stabilizer; Brand: Klonopin
Term
Depression
Definition
Characteristics: severe sadness, despair; Symptoms: anhedonia, anxiety, guilt, emotional liability, blunted affect, sleep disturbances, anorexia, fatigue, loss of energy
Term
Bipolar Disorder
Definition
cyclic swings in mood with periods of depression and mania; Manic phase: excessive energy, insomnia, increased activity, delusions, flight of thought & speech
Term
Tx of Depression
Definition
1) psychotherapy & emotional support; 2) Drugs effective in 70-80% of depressed people: a) DRUGS OF CHOICE --> SSRIs and 2nd generation antidepressants; b) 2nd line: TCAs; c) 3rd line: MAO-Is; d) benzodiazepines, especially alprazolam (Xanax); e) antipsychotics to control schizophrenic-like symptoms; 3) Electroshock therapy; 4) psychotherapy
Term
Tx of Manic Depressive Disorders
Definition
1) Lithium - reduces flucutations in mood swings, very effective; 2) antipsychotics - used in severe phases of mania; 3) antidepressants - helps some severely depressed pts but may trigger manic phase
Term
Pharmacological CNS Effects of Antidepressants - imipramine (Tofranil, Janimine) is prototype
Definition
sedation (paradoxical early in therapy, tolerance develops); antidepressant effect takes 2-4 wks to develop (NO immediate results); Useful for tx: other psychiatric problems - OCD, panic attacks, generalized anxiety disorder (GAD), & social phobias; DECREASED seizure threshold; Stimulation - tremor, restlessness, insomnia, irritability, seizures
Term
Tricylic Antidepressant Mechanism
Definition
inhibition of synaptic reuptake of NE & 5-HT (lesser); causes alteration in density & sensitivity of receptors for NT amines; may also act at muscarinic, other subtypes of serotonin, alpha-adrenergic, or dopaminergic receptors (DIRTY DRUGS)
Term
Anticholinergic Side Effects of Antidepressants - particularly imipramine
Definition
dry mouth, constipation, urine retention, loss of visual accomodation; WORST: TCAs (amitriptyline); LEAST: SSRIs
Term
Cardiovascular Side Effects of Antidepressants - imipramine
Definition
may be severe: postural hypotension, tachycardia, arrhythmias
Term
Side Effects & Toxicities with Antidepressants - imipramine
Definition
loss of visual accomodation, constipation, urine retention, dry mouth; tremor, agitation, anxiety, irritability, switch to manic phase, parkinsonism (rare), INCREASED risk of seizure, hypotension, tachycardia, arrhythmias, with gain, impotence or delay of organism, possible teratogenicity
Term
Acute Poisoning with TCAs
Definition
life-threatening emergency; CNS agitation --> grand mal seizures --> coma; extreme hypotension, tachycardia, arrhythmias --> total cardiovascular collapse; classic "anticholinergic" symptoms; Tx: symptomatically - sodium bicarbonate (preferred) --> reduces cardiotoxic effects; antiarrhythmics, beta-blockers, & CCBs may be useful; DO NOT use physostigmine
Term
Drug Interactions with TCAs or Antidepressants
Definition
anticholinergis; sedatives & alcohol; biogenic amines & adrenergic drugs (potentiation); MAO-I's --> Seratonin Syndrome (tremors, HTN, hyperpyrexia, seizures) --> 2-4 wks should elapse before switching to drug
Term
Pharmacological Effects of MAO-I's
Definition
Takes 2-4 wks to develop; antidepressant action; normalization of sleep patterns; CNS stimulation - tremors, insomnia, hallucinations, may cause switch to manic phase
Term
Side Effects & Toxicities of MAO-I's
Definition
orthostatic hypotension (normal doses); HYPERtension (overdoses or interaction with sympathomimetic [tyramine]); GI - nausea, constipation; CNS - HA, dizziness, vertigo; liver damage (HEPATOTOXICITY)
Term
Tyramine (Cheese) Toxicity
Definition
substrate found in aged foods & drinks (cheese, wine, beer, sausage, chocolate) that potentiates the sympathomimetic --> severe HTN, fever, & convulsions
Term
Acute Li Intoxication
Definition
GI - N/V, diarrhea; Neuromuscular - fatigue, weakness, fine tremor, ataxia, hyperirritability; Neurosensory - blurred vision, tinnitus; CNS - slurred speech, dizziness, confusion, restlessness, grand mal seizures, stupor, coma; CV - arrhythmias, hypotension, circulatory collapse
Term
Treatment of Lithium Intoxication
Definition
remove drug; support symptomatically - maintain fluids & electrolytes; Administer anticonvulsants, antiarrhythmics, & CV drugs as needed; INDUCE DIURESIS (mannitol); HEMODIALYSIS
Term
Drug interactions with Lithium
Definition
NSAIDs, diuretics --> increase levels; carbamazepine, antidepressants, antipsychotics, & methyldopa enhance neurotoxic effects; The Drug can enhance effects of antidepressants & other CNS drugs
Term
Other drugs used to treat Mania
Definition
carbamazepine (Tegretol), valproic acid (Depakene/Depakote), clonazepam (Klonopin)
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