B. 6- indirect sympathomimetics Flashcards

1
Q

classify the indirect-acting sympathomimetics

A
  1. release inducing agents
  2. reuptake inhibitors
  3. MAO inhibitors
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2
Q

function of the release inducing agents

A

displace stored catecholamines from nerve endings (monoamines releasers)

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3
Q

examples of release inducing agents

A

amphetamine
methylphenidate
tyramine
Ephedrine

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4
Q

examples of reuptake inhibitors

A

cocaine
TCA- tricyclic antidepressants
atomoxetine
modafinil

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5
Q

examples of MAO inhibitors

A

moclobemide
selegiline
tranylcypromine

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6
Q

function of reuptake inhibitors (Modafinil)

A

increase the activity of neurotransmitters in the synapse by inhibiting their reuptake into the presynaptic nerve terminal

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7
Q

function of MAO inhibitors (Selegiline)

A

inhibit the metabolism of catecholamines by MAO

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8
Q

what is the “cheese effect”?

A

acute attack of hypertension caused by the interaction of MAO inhibitors and eating cheese which contains tyramine.

*the MAO Inhibitor results in ↑ bioavailability of tyramine, usually limited by rapid metabolism by MAO-A in the gut and liver

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9
Q

which drug has both direct and indirect sympathomimetic effects?

A

ephedrine

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10
Q

indications for amphetamine (5)

A

ADHD
Central nervous system disorders (narcolepsy)
Psychostimulant (due to release of DA, NE, 5-HT)
Appetite suppression
drug of abuse (high addiction liability)

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11
Q

SE of amphetamine

A

seizures
aggression
insomnia
hypertension

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12
Q

indications for methylphenidate

A

ADHD

narcolepsy

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13
Q

where is tyramine found?

A

in fermented foods (red wine, cheese)

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14
Q

when will we give tyramine?

A

there is no clinical use

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15
Q

indications of Ephedrine

A

appetite suppressant
decongestant (nose drops)
hypotension associated with anesthesia

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16
Q

which indirect-acting sympathomimetics inhibit both NET and DAT?

A

cocaine and Modafinil

17
Q

what is cocaine used for?

A
it's a drug of abuse
local anesthetic +vasoconstrictor 
phentolamine antidote (?)
18
Q

`what is Atomoxetine used for ?

A

ADHD

19
Q

What is modafinil used for ?

A

improve wakefulness in narcolepsy

20
Q

which MAO inhibitor is irreversible?

A

Tranylcypromine

21
Q

which MAO inhibitor is used for Parkinson’s disease?

A

selegiline

22
Q

which MAO inhibitors are used as antidepressants?

A

moclobemide

Tranylcypromine

23
Q

please list the 𝝰 agonists (non-catecholamines)

A
Phenylephrine 
oxymetazoline
clonidine
Rilmenidine
methyldopa 
Brimonidine 
Tizanidine
24
Q

which drugs are imidazole derivatives (agonists for both I₂ and 𝝰₂ receptors)

A

clonidine
Rilmenidine
moxonidine
oxymetazoline (is a local 𝝰₁-agonist and systemic 𝝰₂-agonist)

25
Q

which 𝝰 agonist is phenylephrine?

A

𝝰₁ agonist

26
Q

how is oxymetazoline given?

A

topically

27
Q

what is oxymetazoline?

A

decongestant

28
Q

what are the SE of oxymetazoline?

A

hypotension if given systemically (𝝰₂ effect)

29
Q

indications for phenylephrine (3)

A

ophthalmologic use -mydriatic agent (without blocking accommodation)
Decongestant
hypotension (↑ BP)

30
Q

SE of phenylephrine

A

reflex bradycardia
hypertension
stroke
MI

31
Q

which 𝝰₂ agonist drugs are antihypertensive drugs?

A

clonidine
Rilmenidine
methyldopa

32
Q

which 𝝰₂ agonist drug is for glaucoma?

A

brimonidine (↓ aqueous humor production)

33
Q

what is tizanidine?

A

centrally acting muscle relaxant

34
Q

which 𝝰₂ agonist drugs cause drug-induced lupus?

A

clonidine

methyldopa

35
Q

which 𝝰₂ agonist drugs have a milder SE compared to clonidine?

A

moxonidine

rilmenidine

36
Q

indications for clonidine

A

antihypertensive (↓ sympathetic activity)
ADHD
Tourettes’s syndrome
alcohol/ opiates withdrawal syndrome

37
Q

SE of clonidine

A

sedation, dry mouth, severe rebound hypertension if suddenly stopped, drug-induced lupus