2.4 - Adrenergic Drugs Flashcards by Sydney Denney

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

Catecholamines are adrenergic agonists
–> Noradrenaline, adrenaline, dopamine

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Adrenaline binds to which kind of adrenergic receptors?

Can bind to alpha and beta receptors

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NA can bind to which receptors?

Binds to alpha1/2, and only B1

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DA can bind to which receptors?

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

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What are some uses for adrenaline?

–> 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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What is a caution or adverse effect of administering adrenaline?

Arrythmias, HTN, Increased BGL.

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What class of drugs is phenylephrine?

A selective A1 adrenergic agonist

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What does an a1 agonist do?

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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What are some adverse effects of a1 agonists?

excessive increase in BP.

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What kind of drug is clonidine?

A selective a2 adrenergic agonist

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

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

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

A2 agonist –> antihypertensive

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

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

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

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

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

treatment of acute HF

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

Arrythmias, tachycardia.

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

Beta 2 agonist
–> Dilation of bronchi

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

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

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

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

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

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

What kind of drug is isoproterenol?

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

What is a displacer drug

A drug that causes stored NE to be released from vesicles

What kind of drugs are ephedrine and pseudoephrine?

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

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

Used to treat nasal congestion (A1 effect)

What kind of drug is amphetemine?

Displacement drug

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

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.

How do you treat toxicity via amphetamines?

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)

What are some ways to increase NE levels?

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

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

Alpha 1 antagonists --> Reduces vasoconstriction and peripheral resistance

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

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

What kind of drug is yohimbine?

Alpha 2 antagonist

What is the mechanism of action of yohimbine?

"Increases perfusion for certain tissues"

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

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

What kind of drugs are phentolamine and phenoxybenzamine?

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

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

Used to treat NA secreting tumour (pheochromocytoma)

What are some general uses for beta antagonists?

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

What does prophylaxis mean?

Disease prevention

What are some general adverse effects of beta antagonists?

Sedation, lethargy, erectile dysfunction, nightmares

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

Bradycardia, HF, hypotension

What are some adverse effects of a beta 2 blockade?

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

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

propranolol

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

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

What are the uses of beta 2 antagonists?

Not clinically useful.