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MOHD 4: Exam 5 Drugs > L93 - Antidepressants, Stimulants and Bipolar Drugs > Flashcards

L93 - Antidepressants, Stimulants and Bipolar Drugs Flashcards

1
Q

What class of drugs are:

  1. Amitriptyline (Elavil)
  2. Amoxapine (Asendin)
  3. Imipramine (Tofranil)
  4. Nortriptyline (Pamelor
A

Tricyclics (TCAs)

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2
Q

TCA:

  1. Use?
  2. Similar efficacy? Yes or no
A
  1. Used to treat severe major depression

2. Yes: all have similar therapeutic efficacy

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3
Q

TCA Mechanism

A

Block Serotonin and NE reuptake

Off target effects: Also block muscarinic, adrenergic and histamine receptors, which underlies a number of side effects

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4
Q

TCA pharmacokinetics

  1. oral? yes or no
  2. absorption? where?
  3. Therapeutic effect time?
  4. Lipid solubility? into CNS?
  5. Half life?
  6. Binding to plasma proteins? %?
  7. Metabolism?
  8. Elimination?
A
  1. Yes Orally active
  2. Readily absorbed, primarily in the small intestine
  3. Therapeutic effect requires >2 weeks
  4. Highly lipid soluble, readily penetrate into the CNS
  5. Long half-life (10-40 hrs)
  6. High binding to plasma proteins (90-95%); 7. Metabolized by hepatic microsomal enzymes
  7. Eliminated primarily via the kidneys
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5
Q

TCA Side effects

A

Off target effects can determine side effects
Antimuscarinic effects; **Cardiovascular; Orthostatic hypotension; Sedation; Metabolic-endocrine; Neurologic; Psychiatric

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6
Q 
What class of drugs are these?
Citalopram (Celexa)
Escitalopram (Lexapro)
Fluoxetine (Proxac)
Sertraline (Zoloft)
A

SSRIs (serotonin-reuptake inhibitors)

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7
Q

SSRI

  1. use?
  2. Similar efficacy? Yes or no
A
  1. most widely prescribed antidepressant

2. Yes: similar therapeutic efficacy

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8
Q

SSRI mechanism

A

Block Serotonin reuptake only

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9
Q

SSRI drug interactions

A 
Primarily fluoxetine
Block several liver P450 enzymes - CYP2D6, CYP1A2 and CYP3A4; TCAs antidepressants
Neuroleptic drugs (haloperidol)
Some antiarrhythmic drugs
Some b-adrenergic antagonists
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10
Q

SSRI pharmacokinetics

  1. oral? Yes or no
  2. absorption? where?
  3. Therapeutic effect time?
  4. Half life?
  5. Binding to plasma proteins? %?
  6. Metabolism?
  7. Elimination?
A
  1. Yes Orally active
  2. Readily absorbed, primarily in the small intestine
  3. Therapeutic effect requires >2 weeks
  4. Long half-life (1-3 days); Fluoxetine is demethylated to the active metabolite norfluoxetine (half-life time up to 30 days);
  5. High binding to plasma proteins (70-90%);
  6. high first-pass hepatic metabolism; Block several liver P450 enzymes (potential for drug interactions)
  7. Eliminated primarily via the kidneys
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11
Q

SSRI Side effects

  1. early onset
  2. late onset
A
  1. Early Onset, Transient (Nausea, Anxiety, Sleep disturbance/insomnia)
  2. Late Onset (Anorexia, Sexual dysfunction, Induction of mania in patients with bipolar disorder - common SE of anti-dep)
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12
Q

What class of drugs are these?
Duloxetine (Cymbalta)
Venlafaxine (Effexor)

A

SNRIs (serotonin-norepinephrine reuptake inhibitors)

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13
Q

SNRI use?

A

treat depressed patients refractory to SSRIs

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14
Q

SNRI mechanism?

A

Selectively inhibit reuptake of 5-HT and NE

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15
Q

Which SNRI is only 27% bound to plasma proteins?

A

Venlafaxine

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16
Q

Which SNRI is 97% bound to plasma proteins?

A

Duloxetine

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17
Q

CYP2D6 liver enzyme metabolizes which SNRI?

A

venlafaxine and duloxetine

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18
Q

CYP1A2 liver enzyme metabolizes which SNRI?

A

duloxetine

19
Q

Contraindicated in patients with hepatic insufficiency

A

duloxetine

20
Q

Which class of drugs are these?
Bupropion (Wellbutrin)
Mirtazapine (Remeron)
Nefazodone (Serzone)

A

Atypicals

21
Q

What class of drugs are these?
Phenelzine (Nardil)
Selegiline (Emsam)
Tranylcypromine (Parnate)

A

MAO inhibitors

22
Q 
What class of drugs are these?
Lithium
Carbamazepine (Tegretol)
Olanzapine (Zyprexa)
Risperidone (Risperdal)
Valproic acid (Depakene)
A

Bipolar treatment

23
Q 
What class of drugs are these?
 Amphetamine (Adderall)
 Atomoxetine (Strattera)
 Dextro-amphetamine (Dexedrine)
 Methylphenidate (Ritalin)
 Modafinil (Provigil)
A

stimulants

24
Q

inhibits dopamine reuptake; is useful for treating rapid-cycling bipolar disorder (>3-4 cycles of mania)

A

Bupropion (Wellbutrin®)

25
Q

inhibits the reuptake of serotonin and blocks the 5-HT2 receptors
Antipsychotic drug and antidepressant

A

Nefazodone (Serzone®)

26
Q

increases NE and serotonin release by blocking a2 receptors

A

Mirtazapine (Remeron®)

27
Q

T/F: atypicals have more side effects than TCAs?

A

False: fewer anticholinergic effects and no significant cardiotoxic effects
Common side-effects: headache, nausea, tinnitus, insomnia and nervousness

28
Q

Third-line drugs for depression in patients who do not respond to SSRIs and TCAs (atypical depression) and work by increasing presynaptic concentration of NT

A

MAOIs

29
Q

Use of ______ is limited due to severe and often unpredictable side effects.
What are the SE?

A

MAOIs
CNS effects; Cardiovascular: orthostatic hypotension, tachycardia;
Drug interaction: when combined with SSRIs may lead a potentially fatal condition, serotonin syndrome, which includes cognitive (delirium, coma), autonomic (hypertension, and tachycardia) and somatic (hyperthermia, hyperreflexia, tremor) effects;

30
Q
  1. MAO-A deaminates which 3 NT?

2. MAO-B deaminates which NT?

A
  1. MAO-A deaminates NE, 5-HT and dopamine (DA)

2. MAO-B deaminates DA

31
Q

Tyramine (cheese, chicken, liver, beer, red wine) is metabolized by MAO. In the presence of MAO inhibitors, elevated tyramine will cause the release of large amounts of _________________ leading to headache, tachycardia, hypertension, seizures and potentially, stroke - “cheese effect”
Restrictions in diet?

A
  1. catecholamines

2. yes: patients taking MAOIs need to be educated to avoid tyramine-containing foods

32
Q

Pharmacokinetics of MAOIs:

  1. Orally active?
  2. Transdermal patch for ____________?
  3. Therapeutic effect requires __ weeks;
  4. Eliminated primarily via the ____
  5. Block MAO (irreversibly/reversibly), which means that the loss of MAO activity persists long after the drugs are metabolized and eliminated
  6. No new MAO enzymes must be synthesized for MAO activity to return to normal (several weeks)
A
  1. Yes
  2. Selegiline
  3. 2-4 weeks
  4. kidneys
  5. irreversibly
  6. False
33
Q

Drug of choice for maintenance treatment of bipolar illness

A

Lithium

34
Q

prophylactic drug significantly decreases the frequency of both manic and depressive attacks in about 70% of patients

A

Lithium

35
Q

fluoxetine combined with olanzapine

A

Antidepressants

36
Q

risperidone, olanzapine and quetiapine

A

Antipsychotics

37
Q

valproic acid, carbamazepine and lamotrigine

A

Anticonvulsants

38
Q

Lithium: Pharmacokinetics:

  1. 2 ways lithium is available:
  2. Administration?
  3. Rapidly absorbed from the ____
  4. insoluble or soluble ion?
  5. Peak plasma level is reached in __hrs;
  6. Half-life?
  7. Elimination?
  8. How does reduced kidney function affect lithium?
A
  1. carbonate and citrate salts
  2. oral
  3. GI tract
  4. Soluble (no binding to plasma proteins)
  5. 2-4 hours
  6. 20-24 hrs
  7. kidneys
  8. is associated with greater lithium toxicity
39
Q

Inc release of DA and NE into VMAT; inhibits MAO

Drug for ADHD and narcolepsy; potential for addiction; SE (CNS, cardiovascular, GI)

A

Amphetamines

40
Q

Drug for ADHD treatment. NE reuptake inhibitor (not a psychostimulant and non-habit forming)

A

Atomoxetine

41
Q 
Inc release of DA and NE into VMAT; inhibits MAO. 
psychomotor stimulant (combats fatigue); prevents narcolepsy, children with ADHD; oral administration, is completely absorbed from GI tract, metabolized by the liver and excreted in the urine; smoking or via IV by abusers
A

Dextro-amphetamine

42
Q

Inc release of DA and NE into VMAT; inhibits MAO
prevents narcolepsy; children with attention deficit hyperactivity disorder (ADHD); oral administration, good absorption from GI tract, high concentration in the brain; its de-esterified product, ritalinic acid is excreted in the urine

A

Methylphenidate

43
Q

Prevent narcolepsy and shift work disorder. MOA unclear, but likely involves NE and DA systems. Fewer psychoactive and euphoric effects as well as effects on mood and thinking.

A

Modafinil

44
Q

tx binge eating disorder

A

lisdexamfetamine

MOHD 4: Exam 5 Drugs (7 decks)

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