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Pharma Recall - Pharmacology > Ch 13 - Drugs Used To Treat Depression And Mania - DONE > Flashcards

Ch 13 - Drugs Used To Treat Depression And Mania - DONE Flashcards

1
Q

What is depression?

A

An affective syndrome characterized by intense sadness, general loss of interest in the everyday aspects of life, insomnia, changes in the appetite, and loss of self-esteem

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2
Q

What does the biogenic anine theory of depression propose?

A

The depression is due to a deficiency of norepinephrine, serotonin, and dopamine in the synapses of the CNS.

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3
Q

List the major categories of antidepressants:

A
  • Tricyclics
  • Selective serotonin reuptake inhibitors (SSRIs)
  • Monamine oxidase inhibitors (MAOIs)
  • Heterocyclics (atypical antidepressants)
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4
Q

Which agents are cincidered first-line treatment for depression?

A
  • SSRIs

- Heterocyclics (Tetracyclic antidepressants and tricyclics antidepressants are in this group)

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5
Q

Give examples of tricyclics antidepressants:

Tertiary Amine Tricyclics

A
  • Amitriptyline
  • imipramine
  • Doxepin
  • Clomipramine
  • Trimipramine
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6
Q

Give examples of tricyclics antidepressants:

Secondary Amine Tricyclics

A
  • Amoxapine
  • Maprotiline
  • Protriptyline
  • Desipramine
  • Nortriptyline
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7
Q

What are the physiological differences between tertiary amine and secondary amine tricyclics?

A

The secondary amine tricyclics in general are less likely to cause sedation, hypotention, and anticholimergic effects.
- However they are more likely to induce psychosis.

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8
Q

What is the mechanizm of action of all tricyclics?

A
  • These drugs are thought to increase levels of norepinephrine and serotonin in the synaptic cleft by blocking reuptake.
  • They also block histamine, cholinergic, and alpha-adrenerhic receptors, which accounts for a large proportion of their side effects.
  • Tricyclics are also thought to cause a down-regulation of monoamine receptors; this may account for some of the therapeutic benefit
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9
Q

Does these drugs elevate the mood in normal individuals?

Tricyclics

A

No. These drugs are nor CNS stimulants

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10
Q

What are the clinical indications for tricyclics?

A
  • mood disorders (depression mainly)
  • panic disorders
  • generalized anxiety disorders
  • PTSD
  • OCD
  • pain disorders
  • enuresis in children cuases contraction of the internal sphincter of the bladder
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11
Q

Which tricyclic is used for OCD?

A

Clomipramine

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12
Q

What tricyclic is used for enuresis in children?

A

Imipramine

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13
Q

How are the tricyclics administered

A

They are all well absorbed orally and penetrate to the CNS easily

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14
Q

How are the tricyclics metabolized?

A

They undergo significant first-pass metabolism in the liver; they are conjugate with glucuronic acid and excreted through the kidney

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15
Q

Which of the tricyclics are the most efficiacious?

A

All are equally efficacious

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16
Q

When should a physician expect to see a change in the patients mood?

A

2-8 weeks

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17
Q

What are the signs and symptoms of tricyclic toxcicity of tricyclics?

A
  • Anticholinergic side effect
  • Autonomic effect
  • ECG changes
  • Lowering the seizure treshold
  • Wight gain
  • Sedation due to histamine blockade

The three C’s: Cholinergic blockade, Cardiac arrythmias, Convulsion.

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18
Q

Can tricyclics and MAOIs be given together for added benefit?

A

No! This combination can lead to severe covulsion and coma

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19
Q

SSRIs =

A

Selective serotonin reuptake inhibitors

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20
Q

Give some examples of SSRIs:

A
  • Fluoxetine
  • Sertraline
  • Paroxetine
  • Fluvoxamine
  • Citalopram
  • Escitalopram
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21
Q

What is the mechanism of action of SSRIs?

A

Inhibition of serotonin reuptake without significant effects of norepinephrine, muscarinic, histaminic, or alpha-adrenergic receptors.

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22
Q

Which one of the SSRIs are the most effective?

A

No drug has been shown to be superior in all patients. The åatients reaction to the drug is different.

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23
Q

When is the tricyclics indicated?

A

Clinical depression is the primary reason for prescribing these drugs.
- They are also used to treat OCD (fluvoxamine) and anxiety

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24
Q

How are the SSRIs administered?

A

Orally

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25
Q

How are the SSRIs metabolized?

A

By the cytochrome P-450 system.
- Fluoxetine and paroxetine are potent P-450 inhibitors. Therefore plasma levels of other coadministered drugs that are metabolized through the P-450 system may rise to the dangerous leves

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26
Q

Describe the side effect of SSRIs exprience:

A
  • Nausea
  • Diarrhea
  • Nervousness
  • Sleep disturbances
  • Dizziness
  • Sexual dysfunction
27
Q

When are the SSRIs CI:

A
  • when in combination with MAOIs, because it may cause “serotonin syndrome”, characterized by hyperthermia, muscle rigidity, myoclonus, and rapid changes in the mental status.
28
Q

What is monoamine oxidase?

A

MAO is a mitochondrial enzyme that is involved in the metabolism of catecholamine neurotransmitters

29
Q

Where are the highest concentration of monoamine oxidase?

A
  • liver
  • GI tract
  • CNS
30
Q

Name four MAOIs:

Monoamine oxidase inhibitor

A
  1. Tranylcypromine
  2. Phenelzine
  3. Isocarboxazid
  4. Selegiline
31
Q

Describe the mechanism of action of MAOIs (MAO-A)

A

Within the neuron, MAO-A is responsible for the inactivation of any serotonin or norepinephrine that may leak out of presynaptic storage vesicles.

When MAO-A is blocked, these neurotransmitters accumulate in the vesicles and are released into the synapse.

32
Q

Describe the mechanism of MAOIs (MAO-B):

A

MAO-B is responsible for the metabolism of dopamine and works in similar manner.

In general, the MAOIs except for Selegiline -which is a specific inhibitor of MAO-B- are nonspecific inhibitors of MAO.

33
Q

What are the MAOIs indicate for?

A
  • Treatment of atypical depression (with phobia or psychotic features).
  • Other classes of antidepressants are more frequently used today because they have fewer toxic effects.
34
Q

Describe the pharmacological properties pf MAOIs:

A
  • they are well absorbed orally
  • they are metabolized by acetylation in the liver
  • they require 2-4 weeks of treatment to reach a steady-state plasma level
35
Q

What are the adverse effects of MAOIs?

A
  • hypertensive crisis if the patient dont avoid eating food containing tyramine wich is normally inactivated by MAO
    • hypertensive crisis can also occure when MAOIs are administrated with meperidine.
  • orthostatic hypotention
  • agitation, seizure
  • dry mouth, blurred vision
  • weight gain
36
Q

When are MAOIs CI:

A

They should not be coadministered with SSRIs or beta-agonists

37
Q

Wht is a heterocyclic antidepressant?

A
  • they vary in organic structure, site of action, and in their mechanism of action
  • =atypical antidepressants
  • they are divided into second- and third generation drugs
38
Q

Give examples of two second-generation heterocyclic antidepressants:

A
  • Trazodone

- Bupropion

39
Q

What is Trazodone?

A

An antidepressant similar in structure to the Benzodiazepine Alprazolam, but more specific to the inhibition of serotonin reuptake.

40
Q

When is Trazodone indicated?

A
  • depression

- effective for improving sleep

41
Q

Where is Trazodone metabolized?

A

In the liver (excreted by the kidneys)

42
Q

Trazodone AE:

A
  • Sedation
  • Orthostatic hypertention
  • Nausea
  • Headache and dizziness
  • Agitation
  • Rarely priapism
43
Q

What is the mechanism of action of Bupropion?

A

This is not clearly known, but it is thought to work through dopaminnergic and noradrenerig systems.

44
Q

What are the indications for bupropion?

A
  • clinical depression

- smoking cessation

45
Q

What toxci ities are associated with bupropion?

A
  • headache
  • nausea
  • dry mouth
  • tachycardia
  • restlessness
46
Q

What is the advantage of using bupropion?

A

There are no side effects related to sexual dysfunction, such as those that occure with SSRIs

47
Q

Which drugs are considered to be third-generation heterocyclics?

A
  • venlafaxine
  • nefazodone
  • mirtazapine
48
Q

How do the third-generation heterocyclics work?

Venlafaxine

A

Venlafaxine and nefazodone block the reuptake of both serotonin and norepinephrine.

49
Q

How do the third-generation heterocyclics work?

Mirtazapine

A

Mirtazapine: a potent inhibitor of presynatic alpa2 adrenoreceptors, which are involved in feedback mechanism. This results in an increase of amine release from nerve endings.

Mirtazapine also antagonizes seretogenic 5HT2 and 5HT3 receptors

50
Q

What are the side effects of Venlafaxine?

A
  • nausea
  • anxiety
  • sustained increase in BP
  • headache
51
Q

What are the side effects of Nefazodone?

A
  • dry mouth
  • nausea
  • sedation
  • liver impairment
52
Q

What are the side effects of Mirzadapine?

A
  • sedation

- weight gian and increased serum cholesterol

53
Q

What is mania?

A

Elevated mood with grandios ideas, expansiveness, pressured speech, flight of ideas, decreased sleep, and increased activity

54
Q

In what cinditions is mania seen?

A

Affective disorders such as bipolar disorder

55
Q

Give some examples of antimanic agents:

A
  • lithium (drug of choice)

- anticonvulsants (valproic acid and carbamazepine)

56
Q

What is Lithium?

A

a light alkali metal available in carbonate, a slow-release, and controlled-release forms

57
Q

How does lithium work?

A

The mechanism is unclear; it is thought to block the enzyme inositol-1-phosphate, which affects neurotransmitters

58
Q

What is lithium´s major indication?

A

Lithium is primarily used in bipolar diorders- both manic and depressive episodes respond

59
Q

Describe some other uses of Lithium:

A

Lithium can be used as an adjuvant with other antidepressants to treat major depression with antipsychotics to treat Schizofrenia

60
Q

What are the pharmacokinetic properties of Lithium?

A

Lithium is well absorbed orally and is excreted in the urine.

61
Q

When is lithium CI?

A

pregnancy- it is teratogenic

62
Q

Lithium AE:

A
  • acute intoxication
  • nephrogenic diapetes insipidus
  • weight gain, vomiting, abdominal cramps, and diarrhea
  • distrubances in the thyroid function
  • depression of the T wave on ECG
  • leukocytosis
63
Q

Acute intoxication:

lithium

A
  • severe tremor
  • ataxia
  • seizures
  • confusion
  • coma
64
Q

What substances affect lithium plasma levels?

A
  • excessive intake of sodium lowers lithium levels

- thiazide diuretics increase the lithium plasma level

Pharma Recall - Pharmacology (14 decks)

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