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Pharmacology > Adrenergic and Antiadrenergic Drugs > Flashcards

Adrenergic and Antiadrenergic Drugs Flashcards

1
Q

Adrenergic agonists

What drug has alpha > beta selectivity as an adrenoceptor agonist?

A

Norepinephrine

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2
Q

What drug has beta > alpha selectivity as an adrenoceptor agonist?

A

Adrenaline (epinephrine)

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3
Q

What drug is selective for alpha-1 and beta-1 adrenoceptor as an agonist?

A

Dopamine

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4
Q

What drug is a non-selective alpha adrenoceptor agonist?

A

Oxymetazoline

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5
Q

What drug is selective for alpha-1 adrenoceptors (agonist)?

A

Phenylephrine

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6
Q

What drug is selective for alpha-2 adrenoceptor agonists?

A

Brimodine

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7
Q

What drug is non-selective for beta-adrenoceptors (agonist)?

A

Isoprenaline

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8
Q

What drug is selective for beta-1 adrenoceptors (agonist)?

A

Dobutamine

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9
Q

What drug is selective for beta-2 adrenoceptors (agonist)?

A

Salbutamol, terbutaline

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10
Q

What drug is selective for beta-3 adrenoceptors (agonist)?

A

Mirabegon

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11
Q

Uses of norepinephrine? List some adverse effects

A
  1. Severe hypotension

Adverse effects – hypertension, tachycardia, (reflex) bradycardia, arrthymias, necrosis due to vasoconstriction at injection site

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12
Q

Uses of adrenaline?

A

Cardiac resuscitation (beta-agonist > alpha-agonists), anaphylactic shock

Vasoconstriction: local anaesthetics, slowing absorption of medication; blood-free field for minor surgery

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13
Q

Uses of dopamine

A

Cardiac resusciation, severe hypotension

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14
Q

Uses of oxymetazoline
What happens as a reflex?

A

Nasal decongestion due to vasoconstriction of blood vessels in visceral organs

There is rebound mucosal secretion

Reflex tachycardia due to increased systemic BP

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15
Q

Uses of phenylephrine

A

Hypotension, nasal decongestant (vasoconstriction of visceral and mucosal blood vessels) and reduction of mucosal secretion.

but this leads to rebound mucosal secretion

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16
Q

What are the uses of brimodine

A

Used to reduce IOP through vasoconstriction, treating glaucoma

17
Q

Why is brimodine used on the eyes?

A

Large amount of alpha-2 adrenoceptors on eye blood vessels; used to treat open/wide-angle glaucoma

18
Q

What is an additional effect of alpha-2 agonists?

A

They also act at pre-synaptic alpha-2 adrenoceptors, resulting in an indirect antiadrenergic effect (negative feedback loop to decrease NE bioavailability)

19
Q

What is the major concern with beta-agonists?

A

They are structurally similar and show dose-dependent selectivity; chance of cross-over arising in cardiac/lung adverse effects

20
Q

State the 3 ways indirect adrenoceptor agonists increase the availability of endogenous neurotransmitters in synapses.

A
  1. Inhibiting breakdown of catecholamines by MAOI [moclobemide]
  2. Blocking uptake 1 [TCA]
  3. Displacement of endogenous norepinephrine from vesicular storage, competitively inhibiting MAOI [Ephedrine and pseudoephedrine]
21
Q

State 3 indirect adrenoceptor agonists

A
  1. moclobemide (MAOI)
  2. TCAs (NE uptake blocker)
  3. Pseudoephedrine (displacement of endogenous NE)
22
Q

State two alpha-blockers and their selectivity

A
  1. Phenoxybenzamine (nonselective alpha-blocker)
  2. Prazosine (and other -ozines) are selective alpha-1 blockers
23
Q

State the selective beta-blockers.

A
  1. Bisoprolol
  2. Betaxolol
24
Q

State the non-selective beta blockers. Which of the three is applied to the eye to treat glaucoma, and why?

A
  1. Propranolol
  2. Sotalol
  3. Timolol, since it is less lipophilic with little anaesthetic-like actions allowing for blink reflex
25
Q

What should be taken caution of when prescribing beta-1 selective blockers?

A

Selectivity is highly dose-dependent and crossover may occur from beta-1 to beta-2 adrenoceptors, resulting in heart and lung adverse effects.

26
Q

Salivary gland secretion is controlled by which adrenoceptor subtype?

A

alpha-1

27
Q

Aqueous humour production is controlled by which adrenoceptor subtype?

A

beta-1

28
Q

Lens accommodation and pupil dilation is achieved by which adrenoceptor subtype?

A

alpha-1

29
Q

Glycogenolysis is achieved by which receptor subtype?

A

beta-2

30
Q

Vasoconstriction of blood vessels around visceral organs + vasodilation of vessels for skeletal muscles are achieved by which adrenoceptor subtypes?

A

alpha-1, beta-2

31
Q

State the two indirect methods of adrenergic antagonism.

A
  1. (alpha-2) agonists at presynaptic autoreceptors decrease release of NE into synaptic cleft
  2. Decreasing norepinephrine synthesis through methyldopa (false transmitter)
32
Q

State an alpha-2 agonist that can inhibit the bioavailability of endogenous catecholamines in synaptic clefts by acting at presynaptic autoreceptors

A

Dexmedetomidine (sedative); brimodine has alpha-2 agonist effects as well

33
Q

What are the main uses of norepinephrine and epinephrine?

A
  1. Increasing blood pressure (hypertension), which increases the force and rate of heart (beta-1 agonists) and vasoconstriction of blood vessels supplying visceral organs (a2-adrenoceptors)
  2. Treat hypotension
  3. Adrenaline is used in anaphylactic shock and cardiac resuscitation (stronger beta-1 agonist actions)
  4. Leads to blood-free environment for surgery and slows absorption of medicine at administration site
34
Q

The urinary, GI and iris sphincter muscles are all controlled by what receptor?

A

alpha-1 adrenergic receptors

35
Q

contraction of the iris sphincter results in? which receptor is involved?

A

dilation of the pupil - alpha1 (eyes are first organ from the brain so a1)

Pharmacology (2 decks)

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