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Pharm 3 > Antidepressants > Flashcards

Antidepressants Flashcards

1
Q

Biogenic Amine Theory of Depression

A

Depression results from deficiency in one of the NT’s (norepinephrine (NE), dopamine, and serotonin (5HT)) in specific parts of the brain.

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2
Q

3 Reasons for deficiency of NT’s (Biogenic Amine Theory of Depression)

A

1) Monoamine oxidase (MAO) may break them down to be recycled or restored in the neuron
2) Rapid fire of neurons may lead to their depletion
3) The number or sensitivity of postsynaptic receptors have been down-regulated

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3
Q

3 Ways Antidepressant drugs work to counteract deficient NT’s

A

1) inhibit the effects of MAO, leading to increased NE or 5HT in the synaptic cleft.
2) block reuptake by the releasing nerve= increased NT levels in the synaptic cleft.
3) regulate receptor sites and the breakdown of NT’s =accumulation of NT in the synaptic cleft.

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4
Q

3 Antidepressant Drug Classifications

A 
Tricyclic antidepressants (TCAs)
MAO inhibitors (MAOIs)
Selective serotonin reuptake inhibitors (SSRIs)
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5
Q 
Tricyclic Antidepressants (TCA's) Actions
*also Anti-cholinergic
A

Reduce the reuptake of 5HT and NE into nervesbes
TCA’s in general may best suited for Depression with symptoms of anxiety and sleep disturbance. *Enuresis in kids 6+. Chronic Pain.
Clomipramine Tx OCD.

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6
Q 
Tricyclic Antidepressants (TCA's) Indications
*No specific indications except with PEDS.  The choice of which drug comes down to side effects vs. effectiveness.
A

Relief of symptoms of depression
Used for patients with sleep disorders
Treatment of enuresis
Chronic pain

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7
Q

Tricyclic Antidepressants (TCA’s) Pharmacokinetics

A

Absorbed from the GI tract
Peak in 2 to 4 hours
Bound to plasma proteins and lipid soluble
Metabolized in the liver and excreted in the urine
T½ 8 to 46 hours

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8
Q

Tricyclic Antidepressants (TCA’s) Contraindications and Cautions

A

Known allergy, recent MI, myelography, pregnancy, and lactation
Cautions: CV disease, angle closure glaucoma, urinary retention, and manic depression
SUICIDEALITY in Kids/Adolescent

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9
Q

Tricyclic Antidepressants (TCA’s) Adverse reactions

A

Sedation, sleep disturbances, fatigue, hallucinations, ataxia, dry mouth, constipation, nausea, and vomiting Anticholinergic side effects

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10
Q

Tricyclic Antidepressants (TCA’s) DD Interactions

A

MAOIs, cimetidine, fluoxetine, ranitidine, and oral anticoagulants. sympathomimetic drugs: clonidine=risk for HTN, and Arrhythmia

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11
Q

TCA’s for PEDS patients

A

Caution: Unpredictable Rx. Monitor for Suicidal Ideation. Clomipramine, Imipramine, Nortriptyline, and Trimipramine have established PEDS Dosage

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12
Q

TCA Antidepressant Name ending

A

“amine” “tyline” “apine” Be Careful…many other drugs have similar, even in the other classifications. Also Doxepin does not fit name ending.

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13
Q

Prototype Drug Imipramine Indications

A

Tx depression; enuresis in children older than 6 years, off-label consideration— control of chronic pain.

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14
Q

Prototype Drug Imipramine Actions

A

Inhibits presynaptic reuptake of norepinephrine and serotonin; anticholinergic at central nervous system and peripheral receptors; sedating.

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15
Q

Prototype Drug Imipramine Pharmacokinetics

A

Route: Oral O=Varies D=2–4 h

T1/2: 8 to 16 hours, metabolized in the liver, excretion in the urine.

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16
Q

Prototype Drug Imipramine Adverse Effects

A

Sedation, anticholinergic effects, confusion, anxiety, orthostatic hypotension, dry mouth, constipation, urinary retention, rash, bone marrow depression.

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17
Q

Monoamine Oxidase Inhibitors (MAOIs) Action

A

Irreversibly inhibit MAOs, allowing norepinephrine, serotonin, and dopamine to accumulate in the synaptic cleft

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18
Q

Monoamine Oxidase Inhibitors (MAOIs) Indication

A

Treatment of patients with depression who are unresponsive to or unable to take other safer antidepression agents

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19
Q

Monoamine Oxidase Inhibitors (MAOIs) Pharmacokinetics

A

Absorbed from the GI tract
Peak in 2 to 3 hours
Metabolized in the liver and excreted in the urine
Cross placenta and enter breast milk

20
Q

Monoamine Oxidase Inhibitors (MAOIs) Contraindications

A

Known allergy, pheochromocytoma, CV disease (remember your “fight or flight” response with increased NE), headaches, and renal or hepatic impairment. Caution: Psychiatric-could cause switch to manic. Seizure disorders and hyperthyroidism.

21
Q

Monoamine Oxidase Inhibitors (MAOIs) Adverse reactions

A

Dizziness, excitement, nervousness, mania, hyperreflexia, tremors, confusion, insomnia, agitation, liver toxicity, nausea, vomiting, diarrhea or constipation, anorexia, weight gain, dry mouth, and abdominal pain

22
Q

Monoamine Oxidase Inhibitors (MAOIs)

DD interactions

A

Other antidepressants: hypertensive crisis and coma with TCAs and serotonin syndrome with SSRIs
Methyldopa: sympathomimetic effects increase
Insulin or oral antidiabetic agents: additive hypoglycemia

23
Q

Monoamine Oxidase Inhibitors (MAOIs) Food Interactions

A

Tyramine or pressor amines: increase blood pressure-Pts must follow strict diet, most may not be able to comply

24
Q

MAOI’s and Children

A

Avoid: Risk of Food Interactions and Severe AE’s.

25
Q

Hight Tyramine foods-Food interactions with MAOI’S

A

aged cheeses, aged meats, Brewer’s yeast, Fava Beans, red wines, smoked/pickled foods.

26
Q

Prototype Drug Phenelzine Indications:

A

Tx of patients with depression who are unresponsive to other antidepressive therapy or in whom other antidepressive therapy is contraindicated.

27
Q

Prototype Drug Phenelzine Actions:

A

Irreversibly inhibits monoamine oxidase, allowing norepinephrine, serotonin, and dopamine to accumulate in the synaptic cleft; this accumulation is thought to be responsible for the clinical effects.

28
Q

Prototype Drug Phenelzine Pharmacokinetics:

A

Route: Oral O= Slow. D= 48–96 h

T1/2: Unknown; metabolized in the liver, excreted in urine.

29
Q

Prototype Drug Phenelzine Adverse Effects:

A

Dizziness, vertigo, headache, overactivity, hyperrefl exia, tremors, mania, weakness, drowsiness, fatigue, sweating, orthostatic hypotension, constipation, diarrhea, dry mouth, edema, anorexia, potential for hypertensive crisis.

30
Q

Selective Serotonin Reuptake Inhibitors (SSRIs)

A
  • newest antidepressant drugs
  • Specifically block the reuptake of 5HT, with little to no known effect on NE
  • Fewer Side effects than with TCAs and MAOIs
31
Q

SSRIs Action

A

Inhibit CNS neuronal reuptake of serotonin with little effect on norepinephrine and little affinity for cholinergic, histaminic, or alpha-adrenergic sites

32
Q

SSRIs Indications

A

Depression, OCD, panic attacks, bulimia, PMDD, posttraumatic stress disorders, social phobias, and social anxiety disorders

33
Q

SSRIs Pharmacokinetics

A

Absorbed from the GI tract
Metabolized in the liver
Associated with congenital abnormalities

34
Q

SSRIs Contraindications

A

Known allergy, lactation and impaired renal or hepatic function
Strict Caution in pregnancy

35
Q

SSRIs Adverse reactions

A

Headache, drowsiness, dizziness, insomnia, anxiety, tremor, and agitation

36
Q

SSRIs Drug-to-drug interactions

A

MAOIs

TCAs increase therapeutic and toxic effect

37
Q

SSRIs Withdrawal

A
  • after long term may need tapered off slowly over a period of months to a year d/t severe withdrawal symptoms
  • Can occur when dose is decreased or stopped and begins depending on the half life of the SSRI (fluoxetine has a half life of 3-5 days note change from Karch text, others are shorter)
  • Symptoms can include “brain zaps”, “brain shocks,” “brain shivers”, dizziness, sweating, nausea, insomnia, tremor, confusion, nightmares, and vertigo
38
Q

Serotonin Syndrome

A
  • Dangerous high levels of serotonin –occurs when two meds are given together that increase serotonin
  • Most likely to occur when you first start or increase the medicine
39
Q

Serotonin Syndrome Symptoms

A

within minutes to hours. include:
Agitation or restlessness, diarrhea, tachycardia, hallucinations, increased body temperature, loss of coordination, nausea, overactive reflexes, rapid changes in blood pressure, vomiting

40
Q

Serotonin Syndrome Tx

A
  • Benzodiazepines such as diazepam (Valium) or lorazepam (Ativan) to decrease agitation, seizure-like movements, and muscle stiffness
  • Cyproheptadine (Periactin), a drug that blocks serotonin production (this is an antihistamine)
  • Fluids by IV
  • Withdrawal of medicines that caused the syndrome
41
Q

Tx of Life Threatening Serotonin Syndrome

A

medicines that keep your muscles still (paralyze them) and a temporary breathing tube and breathing machine will be needed to prevent further muscle damage.

42
Q

Prototype Drug Fluoxetine Indications:

A

Treatment of depression, obsessive– compulsive disorders, bulimia, premenstrual dysphoric disorder, panic disorders; off-label uses include chronic pain, alcoholism, neuropathies, obesity.
*Widely used to tx depression in adolescents. Off label usage for kids as young as 6 months.

43
Q

Prototype Drug Fluoxetine Actions:

A

Inhibits central nervous system neuronal reuptake of serotonin, with little effect on norepinephrine and little affinity for cholinergic, histaminic, or alpha-adrenergic sites.

44
Q

Prototype Drug Fluoxetine Pharmacokinetics:

A

Route: Oral O=Slow Peak=6–8 h

T1/2: 2 to 4 weeks; metabolized in the liver, excreted in urine and feces.

45
Q

Prototype Drug Fluoxetine Adverse Effects:

A

HA, nervousness, insomnia, drowsiness, anxiety, tremor, dizziness, sweating, rash, GI= N,V,D,Dry mouth. anorexia, sexual dysfunction, upper respiratory infections, weight loss, fever.

46
Q

SSRI’s and Children

A

Fluvoxamine and Sertraline have PEDS Dosage Guides for Tx of OCD. Fluvoxamine widely used t

Pharm 3 (7 decks)

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