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PHAR2002 > Adrenergic Agonists > Flashcards

Adrenergic Agonists Flashcards

1
Q

Catecholamines differ in

A
  1. Oral usability
  2. Duration of action
  3. CNS penetration
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2
Q

Catecholamines are composed of

A

Catechol and ethylamine group

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3
Q

3 types of Adrenergic agnoists

A

Direct, indirect, mixed acting

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4
Q

How does tyramine act as a indirect acting sympathomimetic?

A

Tyramine displaces NA from cytoplasmic pool (sympathomimetic) -> taken by uptake 1 (NE transporter) into terminal then into vesicle by VMAT in exchange for NA which is taken up by uptake1 in exchange for tyramine. (if not metabolised by MAO)

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5
Q

What are direct acting catecholamines?

A

Non-selective catecholamines -> NA + AD

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6
Q

What are Indirect Acting Sympathomimetics?

A

Drugs that cause NA release in the absence of nerve stimulation

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7
Q

a1 direct acting agonists and usage

A

Oxymetazoline, phenylephrine

-> eye drops + runny nose

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8
Q

Noradrenaline is ______ in the gut

A

inhibitory

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9
Q

What is adrenaline reversal?

A

Presence of an a antagonist causes vasoconstrictor action to be blocked unmasking b2 mediated vasodilator -> fall in bp

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10
Q

Why are adrenaline stimulating drugs used during cardiac arrest?

A

Increases HR without bp change - no vagal drive to heart

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11
Q

Why are adrenaline stimulating drugs used for asthma?

A

b2 selective agonist -> bronchodilaton

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12
Q

Which adrenaline stimulating drug is used for cardiac arrests?

A

Dobutamine, b1 agonist

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13
Q

Why are adrenaline stimulating drugs used to treat glaucoma?

A

Reduces rate of aqueous humour prod. through a2 on ciliary body + veins (absorption)

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14
Q

Which adrenaline stimulating drug is used to treat glaucoma?

A

Dipivefrine (prodrug)

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15
Q

What type of glaucoma are adrenaline stimulating drugs used on?

A

open-angle (filtration angle between iris and cornea) simple glaucoma (intra-ocular pressure above 21mmHg)

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16
Q

What other drug can be used to treat open angle simple glaucoma?

A

Brimonidine, a2 agonist

17
Q

What type of agonist is used during an anaphylactic shock? How is relief achieved?

A

Direct acting agonist, adrenaline. Counteracts laryngeal oedema, bronchospasm + hypotension (from histamine)
-> vasoconstriction through a1 reduces laryngeal oedema, b1 increase bp + bronchodilator (b2) Physiological antagonism

18
Q

Adrenaline is used for vaso____ alongside ____ to prolong _____

A

constriction, LA’s, anaesthesia

19
Q

Propranolol is more selective for

A

beta

20
Q

Phentolamine is very selective for

A

alpha

21
Q

Isoprenaline causes

A

vasodilation -> bp falls

-> tachycardia + direct b mediated force of contraction increases

22
Q

Isoprenaline is very selective for

A

beta

23
Q

Adrenaline is more potent on

A

beta than alpha

24
Q

Adrenaline acts in

A

the adrenal medulla

25
Q

Noradrenaline is more potent on

A

alpha than beta

26
Q

Noradrenaline acts on

A

Post-ganglionic sympathetic nerve terminals

27
Q

Isoprenaline causes smooth muscle to

A

relax

28
Q

Dopamine is dose dependant. Which receptors are affected at different doses?

A

Low- D receptors
Med: B1 receptors
High: a1 receptors
Med + high doses can cause acute severe heart failure and hypertensive shock

29
Q

Direct acting agonists are

A

selective

30
Q

a2 direct acting agonists and usage

A

Clonidine -> hypertension + ADHD

31
Q

B1 direct acting agonists and usage

A

Dobutamine for increase cardiac output

32
Q

B3 direct acting agonists and usage

A

Mirabegron -> overreactive bladder

33
Q

B2 direct acting agonists - short acting

A

Albuterol, terbutaline

34
Q

B2 direct acting agonists - long acting

A

Salmeterol, formotorol

35
Q

How do indirect acting agonists work?

A

Enhance NA + AD by inhibition of reuptake/breakdown

  • > block reuptake of NA/dopamine in reward system
  • > a1 + b1 -> increase BP + HR
36
Q

Ephedrine

A

Mixed action agonist -> not catechloamine

  • > direct binding, release of stored NA from pre-sympathetic terminals
  • vasoconstriction
  • bronchodilation
37
Q

Pseudoephedrine

A

Mixed action agonist:

  • > long duration
  • > vasoconstriction and broncho muscle relaxation
  • > nasal passages decrease mucus production

PHAR2002 (14 decks)

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