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Pharma 2nd semester > A.29.Tricyclic, tetracyclic and unicyclic antidepressants. MAO-inhibitors. > Flashcards

A.29.Tricyclic, tetracyclic and unicyclic antidepressants. MAO-inhibitors. Flashcards

1
Q

what is the mechanism of MAO inhibitors

A

interfere with the metabolism of amines in nerve endings–> ↑ in the vesicular stores of NE and 5-HT

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2
Q

MAO-A is responsible for the metabolism of..?

A

NE, 5-HT, Tyramine

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3
Q

MAO-B is responsible for the metabolism of..?

A

DA, synthetic compounds

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4
Q

what is Moclobemide?

A

MAO-A selective inhibitor

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5
Q

what is Selegiline?

A

MAO-B selective inhibitor

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6
Q

what are Phenelzine and Tranylcypromine?

A

MAO non-selective inhibitors

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7
Q

how are MAO inhibitors given?

A

orally

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8
Q

how long does it take to achieve an antidepressant effect with MAO inhibitors

A

2-4 weeks

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9
Q

what type of inhibition do MAO-A inhibitors have?

A

reversible

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10
Q

what type of inhibition do MAO-B and non-selective inhibitors have?

A

irreversible

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11
Q

is Moclobemide an efficient antidepressant?

A

no

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12
Q

MAO inhibitors have a long or short T1/2?

A

long

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13
Q

when do we give Selegiline?

A

Parkinsonism (adjunct to levodopa)

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14
Q

what is the indication for Moclobemide?

A

major depressive disorders

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15
Q

indications for MAO non-selective inhibitors (Phenelzine)

A
  1. major depressive disorders (in patients unresponsive to any other newer agents- ‘atypical depression’)
  2. anxiety disorders
  3. phobic disorders
  4. hypochondriasis
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16
Q

adverse effects of MAO inhibitors

A

insomnia
hypotension
sexual dysfunction
CNS stimulation effects–> agitation, convulsions ,seizures
toxicity–> shock, hyperthermia, seizures

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17
Q

what drugs can cause a hypertensive crisis when given with MAO inhibitors?

A 
TCA'S 
indirect sympathomimetics
tyramine
𝝰₁-agonists 
levodopa
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18
Q

what are the symptoms of hypertensive crisis?

A

↑ BP
cardiac arrhythmias
hyperthermia

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19
Q

what are the symptoms of serotonin syndrome?

A 
muscle rigidity 
myoclonus 
hyperthermia 
CV instability
CNS stimulation
seizures
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20
Q

what drugs can cause serotonin syndrome when given with MAO inhibitors?

A

SSRI’S
TCA’S
meperidine

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21
Q

what is Tyramine?

A
  1. naturally occurring monoamine
  2. metabolized by MAO-A enzymes
  3. can be found in aged meat, cheese, and wine
  4. acts as a catecholamine-releasing agent (indirect sympathomimetic)
22
Q

what is the ‘Cheese effect’?

A

consumption of dietary tyramine +taking non-selective MAO inhibitor –> ↑ sympathetic stimulation –>hypertensive crisis

23
Q

what risk increases in the first 2 months of MAO inhibitors treatment?

A

suicide risk

24
Q

management of ‘cheese effect’

A

Phentolamine (non-selective 𝝰-antagonist)

25
Q

what is the most sedative TCA?

A

Amitriptyline

most anticholinergic effect

26
Q

name the Tricyclic antidepressants

A

CIA
Clomipramine
Imipramine
Amitriptyline

27
Q

how are TCA’s given?

A

orally

28
Q

what is the T1/2 of TCA’S?

A

8-36 hours

allows once-daily dosing

29
Q

what type of metabolism do TCA’s have?

A

hepatic P450 metabolism

30
Q

mechanism of action of TCA’s

A
  1. inhibit the reuptake transporters in the CNS (SERT, NET)

2. blocks muscarinic, 𝝰₁, H₁ receptors

31
Q

indications of TCA’s

A
  1. Major depressive disorders- not 1st line!
  2. Bipolar disorders
  3. acute panic attacks
  4. phobic disorders
  5. Enuresis (involuntary urination), nocturnal (imipramine)
  6. Migraine (Amitriptyline, Imipramine)
  7. Neuropathic pain disorders (diabetic neuropathy)
  8. ADHD
32
Q

Adverse effects of TCA’s

A
  1. CNS depression–> sedation, fatigue, confusion
  2. Atropine- like effects (M blockade) –> dry mouth, urinary retention, constipation, blurred vision
  3. orthostatic hypotension, ECG changes, arrhythmias (due to 𝝰₁ blockade)
  4. tremor, paraesthesia
  5. weight gain
33
Q

toxicities caused by Tricyclic antidepressants

A

‘the 3 C’s’
Coma
Convulsions
Cardiotoxicity

34
Q

how do we treat TCA’s toxicity?

A

NaHCO₃ to prevent arrhythmia

35
Q

what is Maprotiline?

A 
Tetracyclic antidepressant (TeCA)
has NET>>SERT inhibition
36
Q

what are the indications and side effects of Maprotiline?

A

same as TCA’s

37
Q

what drugs cause an additive CNS depression when used with TCA’s?

A

alcohols
barbiturates
benzodiazepines
opioids

38
Q

what happens when TCA’s are mixed with MAO inhibitors?

A

Hypertensive crisis
Serotonin syndrome
*also mixed with SSRI’s and meperidine

39
Q

what drugs reverse guanethidine’s action

A

TCA’s

they block its hypertensive action by blocking its transport into sympathetic nerve endings

40
Q

what is Mirtazapine?

A 
Tetracyclic antidepressant (TeCA)
𝝰₂ selective antagonist
41
Q

how is Mirtazapine and Bupropion given?

A

orally

42
Q

mechanism of action of Mirtazapine

A
  1. inhibitor of pre-synaptic 𝝰₂ receptors (inhibit sympathetic activity) –> ↑ amine release from nerve terminals
  2. 5-HT₂,5-HT₃, H₁ receptor inhibition
43
Q

side effects of Mirtazapine

A

weight gain
sedation (due to H₁ blockade)
anxiolytic effect
↓ libido

44
Q

what is Bupropion?

A

NDRI -NE DA reuptake inhibitor

45
Q

what are the indications for Bupropion?

A

Major depressive disorders

management of nicotine withdrawal

46
Q

mechanism of action of Bupropion?

A

inhibition of dopamine reuptake (DAT)

*may have CNS stimulant effect

47
Q

what type of metabolism does Bupropion have?

A

hepatic

48
Q

T1/2 of Bupropion is..

A

short

49
Q

is Bupropion a cytochrome P450 inhibitor?

A

yes

50
Q

side effects of Bupropion

A

dry mouth
sweating
seizures
insomnia (from stimulant effect)

NO SEXUAL DYSFUNCTION!
NO WEIGHT GAIN!

51
Q

CI of Bupropion

A

pre-existing seizure disorder

conditions that increase the risk of seizures (CNS tumors, CNS injury, bulimia)

Pharma 2nd semester (49 decks)

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