2.4 - Adrenergic Drugs Flashcards

1
Q

What is a catecholamine? give some examples of some endogenous catecholamine.

A

Catecholamines are adrenergic agonists
–> Noradrenaline, adrenaline, dopamine

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2
Q

Adrenaline binds to which kind of adrenergic receptors?

A

Can bind to alpha and beta receptors

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3
Q

NA can bind to which receptors?

A

Binds to alpha1/2, and only B1

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4
Q

DA can bind to which receptors?

A

DA receptors as well as B1/2, and only a1.

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5
Q

What are some uses for adrenaline?

A

–> Treatment of anaphylactic shock (combats bronchoconstriction, vasodilation and leakiness and edema)
–> Cardiac arrest (not MI)
–> Controlling superficial bleedings
–> Limit diffusion of medications injected into tissues (such as local anesthetics) by causing local vasoconstriction.

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6
Q

What is a caution or adverse effect of administering adrenaline?

A

Arrythmias, HTN, Increased BGL.

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7
Q

What class of drugs is phenylephrine?

A

A selective A1 adrenergic agonist

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8
Q

What does an a1 agonist do?

A

Vasoconstriction (Increase BP), among other A1 things
–> Control superficial bleeding
–> Reduce congestion (via vasoconstriction of BVs in sinuses)
–> Mydriasis
–> Treat hypotensive emergencies

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9
Q

What are some adverse effects of a1 agonists?

A

excessive increase in BP.

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10
Q

What kind of drug is clonidine?

A

A selective a2 adrenergic agonist

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11
Q

How does an a2 agonist (such as clonidine) work?

A

Presynaptic negative feedback results in decreased NA release, causing decreased sympathetic effects (specifically less vasoconstriction)

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12
Q

What is the use of clonidine (an a2 agonist)?

A

A2 agonist –> antihypertensive

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13
Q

What is an adverse effect of alpha 2 agonist like clonidine?

A

Less sympathetic effects for A1/B1 (not so much for B2, noradrenaline does not effect them).
–> Hypotension, dry mouth, sedation

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14
Q

What kind of drug is dobutamine? what does it do?

A

A beta 1 agonist
–> Increase heart rate and force of contraction

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15
Q

Why would you give someone a beta 1 agonist like dobutamine?

A

treatment of acute HF

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16
Q

What are some adverse effects of Beta 1 agonists like dobutamine?

A

Arrythmias, tachycardia.

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17
Q

What kind of drug is salbutamol? What does it do?

A

Beta 2 agonist
–> Dilation of bronchi

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18
Q

What are the uses and adverse effects of a beta 2 agonist such as salbutamol?

A

Relieves asthma caused by bronchospasm
Adverse effects including palpitations, tremor, and hyperglycemia.

19
Q

What kind of drug is mirabegron? What are its effects?

A

A beta 3 adrenergic agonist
–> Relaxation of bladder’s detrusor muscle

20
Q

What is the use for a beta 3 agonist such as mirabegron?

A

Used to treat urinary urgency/incontinence
Adverse effects include tachycardia and increased blood pressure (notice b1 effects)

21
Q

What kind of drug is isoproterenol?

A

A non-specific beta adrenergic agonist (specificities about whether it binds to beta 3 is currently unknown)

22
Q

What is a displacer drug

A

A drug that causes stored NE to be released from vesicles

23
Q

What kind of drugs are ephedrine and pseudoephrine?

A

Displacement drugs (indirect sympathomimetics)
–> Can also act as agonists (mixed acting)

24
Q

What are the uses of ephedrine and pseudoephedrine (Mixed acting (agonist + displacement)?

A

Used to treat nasal congestion (A1 effect)

25
Q

What kind of drug is amphetemine?

A

Displacement drug

26
Q

What are the uses of amphetamines? What are their adverse effects?

A

Used for CNS stimulation (improved concentration, mood), treatment of ADHD, decreased appetite (for weight loss)
Adverse effects include insomnia, irritability, psychosis, anorexia, tachycardia, dependance and tolerance.

27
Q

How do you treat toxicity via amphetamines?

A

Acidification of urine
–> Amphetamine is a weak base, so encouraging its elimination requires it to be in its BH+ form.

Urine can be acidified by making the plasma more acidic (with ammonium chloride)

28
Q

What are some ways to increase NE levels?

A

Displacers
–> Amphetamines, ephedrine, pseudophedrine
Inhibit reuptake
–> Cocaine, tricyclic antidepressant
Inhibit NE breakdown
–> Pargyline

29
Q

What drug class are prazosine, terazosin, and doxazosin? What are the mechanism of action?

A

Alpha 1 antagonists
–> Reduces vasoconstriction and peripheral resistance

30
Q

What are the uses for alpha 1 antagonists such as prazosin, terazosin, and doxazosin? What are some adverse effects?

A

Used to treat HTN.
Adverse effects include orthostatic hypotension (with reflex tachycardia or palpitations)

31
Q

What kind of drug is yohimbine?

A

Alpha 2 antagonist

32
Q

What is the mechanism of action of yohimbine?

A

“Increases perfusion for certain tissues”

33
Q

What are the uses for an alpha 2 antagonist like yohimbine? What is its adverse effects?

A

Used for erectile dysfunction and “fat burning” (prof says this is unsubstantiated)
Adverse effects include tachycardia, HTN, and hypoglycemia.

34
Q

What kind of drugs are phentolamine and phenoxybenzamine?

A

Non-specific alpha antagonist
–> Phentolamine is reversible
–> Phenoxybenzamine is irreversible

35
Q

What are the uses of non-specific alpha antagonists such as phentolamine and phenoxybenzamine?

A

Used to treat NA secreting tumour (pheochromocytoma)

36
Q

What are some general uses for beta antagonists?

A

Treatment of angina, HTN, HF, post MI, arrythmias, stage frights, anxiety, migraine prophylaxis

37
Q

What does prophylaxis mean?

A

Disease prevention

38
Q

What are some general adverse effects of beta antagonists?

A

Sedation, lethargy, erectile dysfunction, nightmares

39
Q

What are some adverse effects of an unwanted beta 1 blockade?

A

Bradycardia, HF, hypotension

40
Q

What are some adverse effects of a beta 2 blockade?

A

Bronchoconstriction, inhibition of hepatic gluconeogenesis, inhibition of symptoms of hypoglycemia, and inhibition of lipolysis.

41
Q

What is an example of a non-specific beta antagonist?

A

propranolol

42
Q

What are the actions of beta 1 antagonists such as metoprolol, bisoprolol, and atenolol?

A

Decreased heart rate and cardiac contractility and decreased secretion of renin (and therefore, activation of the renin-angiotensin-aldosterone system) - resulting in decreased vasoconstriction and blood volume.
Treats HTN, angina, arrythmias

43
Q

What are the uses of beta 2 antagonists?

A

Not clinically useful.