Antidepressants And Stimulants

Front 1

amitriptyline (Elavil)

Back 1

tricyclic antidepressant (TCA).

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amoxapine (Asendin)

Back 2

tricyclic antidepressant (TCA).

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imipramine (Tofranil)

Back 3

tricyclic antidepressant (TCA).

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nortriptyline (Pamelor)

Back 4

tricyclic antidepressant (TCA).

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citalopram (Celexa)

Back 5

seretonin-reuptake inhibitor.

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escitalopram (Lexapro)

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seretonin-reuptake inhibitor.

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fluoxetine (Prozac)

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seretonin-reuptake inhibitor. Demethylated to active metabolite norfluoxetine (half-life time up to 30 days) cardiac toxicity

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sertaraline (Zoloft)

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seretonin-reuptake inhibitor.

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buproprion (Wellbutrin)

Back 9

atypical antidepressant. Inhibits dopamine reuptake; useful for Tx in rapid cycling bipolar disorder

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mirtazapine (Remeron)

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atypical antidepressant. Inhibits reuptake of serotonin and norepinephrine

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nefazodone (Serzone)

Back 11

atypical antidepressant. Inhibits reuptake of serotonin and blocks 5-HT2 receptors

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venlafaxine (Effexor)

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atypical antidepressant. Increases NE and serotonin release by blocking alpha-2 receptors

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phenelzine (Nardil)

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MAO inhibitor - both A and B

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selegiline (Emsam)

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MAO inhibitor - mostly type B, only type A at high concentrations. Transdermal patch

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tranylcypromine (Parnate)

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MAO inhibitor - both A and B

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lithium

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bipolar Tx. Oral administration. No plasma protein binding. 1/2 life 20-24 hrs. eliminated by kidneys. LOW therapeutic index.

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carbamazepine (Tegretrol)

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bipolar Tx. Anticonvulsant

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olanzapine (Zyprexa)

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bipolar Tx. Antipsychotic. Combined with fluoxetine as antidepressant bipolar tx

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risperidone (Risperdal)

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bipolar Tx. Antipsychotic

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valproic acid (Depakene)

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bipolar Tx. Anticonvulsant

Front 21

amphetamine (Adderall)

Back 21

stimulant. Used in Tx of ADHD, narcolepsy. Abuse potential

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atomoxetine (Strattera)

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stimulant. Used in Tx of ADHD. Blocks NE reuptake. Not a psychostimulant; not habit forming and not a controlled substance

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dextro-amphetamine (Dexedrine)

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stimulant. Psychomotor stimulant (combats fatigue). Tx of ADHD and narcolepsy. Oral administration, absorbed in GI, metabolized in liver, excreted in urine, smoking or via IV by abusers

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methylphenidate (Ritalin, Concerta)

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stimulant. Tx of ADHD and narcolepsy. Increases dopamine transmission in brain. Oral administration, absorped from GI, high concentration in brain. De-esterified product - ritalinic acid excreted in the urine

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modafinil (Provigil)

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stimulant. Tx of narcolepsy. Increases DA and NE availability in brain. Not an amphetamine.

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tricyclic antidepressants (TCAs)

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the most effective drugs for patients who are severly depressed; nonspecific blocker of monoamine reuptake; also block muscarinic, adrenergic, and histamine receptors (side effects).

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selective serotonin reuptake inhibitors (SSRIs)

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drugs of choice for moderately depressed pts. Commonly used to treat severely depressed pts; selectively inhibits serotonin reuptake. fewer side effects than TCAs (not cardiotoxic) - safer

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atypical antidepressants

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considered newer, safer, have different mechanism than TCAs or SSRIs

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monoamine oxidase inhibitors (MAOIs)

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the first effective antidepressant used clinically - now use limited due to numerous severe and often unpredictable side effects. 3rd line if pt doesn't respond to SSRIs and TCAs. Irreversible inhibition of MAO (which deaminates NE, serotonin, DA)

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TCAs pharmokinetics (administration, time before effect, half life, metabolism

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Orally active. Absorbed in s.intestine. Therapeutic effect requires >2weeks. Highly lipid soluble, readily penetrate CNS. long 1/2 life (5-40hrs). high binding to plasma proteins. metabolized by hepatic microsomal enzymes, eliminated by kidneys.

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TCAs dose limiting side effect

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cardiovascular - overstimulation - tachy. Slowing of A-V conductance

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SSRI pharmacokinetics

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orally active. Absorbed in s.intestine. High first-pass effect. Therapeutic effect requires >2weeks. Long half life (1-3days) high binding ot plasma proteins, block several liver P450 enzymes, eliminated via kidneys

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MAOIs pharmacokinetics

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orally active. Effect takes 2-4 weeks. Eliminated via kidneys. Ierreversible loss of MAO, means activity lasts after drug is eliminated. New MAO must be made

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MAO side effects

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hallucinations, agitation, hyperreflexia, convulsions, orthostatic hypotension, constipation, SEROTONIN SYNDROME, Tyramine metabolized by MAO (found in some foods)

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lithium side effects

Back 35

will substitute for Na - disrupt electrical activity of mm, neurons; CNS (tremors, mental confusion, convulsions, coma) arrhythmias, decreased thyroid fxn, polydipsia, polyuria, induced diabetes insipidus (suppress vasopressin by working on its G-protein coupled receptor). teratogenic effects. drug interactions with thiazide diuretics and NSAIDS

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methamphetamine

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no clinical use. Psychomotor stimulant. Enhanced DA release in nuc. Accumbens. Abused widely. Cheap, easy to make

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amphetamine side effects

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CNS: euphoria, anxiety, vertigo, insomnia, confusion, paranois, psychoses, suicidal/homicidal impulses. CV: arrhythmias, hypertension. GI: nausea diarrhea. Potential for addiction!