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32 Cards in this Set

  • Front
  • Back

MOA of epinephrine?

Epinephrine is a direct acting sympathomimetic drug.



It mimics the actions of sympathetic neurotransmitters by activating adrenoreceptor.

Therapeutic use of epinephrine? (4)

1. Reduction of regional blood flow (surgery, local anesthesia)


2. Cardiac arrest


3. Bronchial asthma


4. Anaphylactic shock (bronchospasm, mucous membrane congestion, angioedema, severe hypotension)

Effect of epinephrine on CNS? (2)

1. Mydriasis (pupil dilation)


2. Doesn't cross BBB, but fear, anxiety, restlessness, tremors and headache are indirect effect.

Effect of epinephrine on cardiovascular system? (3)

1. Vasoconstriction


2. Increased inotropy and chronotropy


3. Vasodilate skeletal muscle blood vessels (may increase systolic BP but also decrease diastolic)

Effect of epinephrine on respiratory system?

Bronchodilation (relaxation of bronchial smooth muscles)

Effect of epinephrine on GI?

Decreased motility and secretion

Effect of epinephrine on urinary system?

Decreased voiding pressure

Effect of epinephrine on glands?

Increased sweating and pallor

Function of a1 adrenergic receptor subtype? (2)

1. Increase IP3 to release Ca2+


2. Increase DAG to activate protein kinase C



*Main role is excitation

Function of a2 adrenergic receptor subtype?

Inhibition of adenylyl cyclase



*Main role is inhibition

Function of B receptor subtypes?

Increase cAMP for increased contraction



B1 - Heart


B2 - Bronchial smooth muscles


B3 - Adipose tissue, muscles

Where are dopamine receptors found?

Kidneys

Function of D1 receptor subtypes?

Increase adenylyl cyclase (like a1)

Function of D2, D3, and D4 receptor subtypes?

Inhibition of adenylyl cyclase, open potassium channel, decrease calcium influx


(like a2)

Where are a1 receptors located?

Vascular smooth muscle (Contraction)


Pupillary dilator muscle (Contraction - pupil dilates)


Prostate (Contracts)


Bladder sphincter (Contracts)


Heart (Positive inotropy)


Pilomotor muscle (Erects hair)

Where are a2 receptors located? (3)
Vascular smooth muscles (contraction)
GI smooth muscles (relax; indirect)
Fat cells (inhibits lipolysis)

*Inhibits nerve endings at adrenergic and cholinergic sites

Where are B1 receptors located?

Heart (increase inotropy and chronotropy)

Where are B2 receptors located? (2)
Respiratory (relax)
Vascular smooth muscles (relaxation/ dilate)
Uterus (relax)
Skeletal muscles ( uptake K+)
Where are B3 receptors located? (2)
Fat cells (lipolysis)
Bladder (relaxation)
Heart (negative inotropy)

Where are D1 receptors located?

Smooth muscles (dilates renal vessels)

MOA of dopamine?

Dopamine is a selective adrenergic agonist.



It is a precursor of norepinephrine and activates D1 and D2 receptors.



It also activates b1 receptors in the heart due to similar structure to adrenaline.

1. MOA and 2. Therapeutic uses of dobutamine?

1. Dobutamine is an adrenergic agonist. It is a catecholamine that is selective for B1 receptors, but also activates a1.



2. Hypotensive emergency to preserve cerebral and coronary blood flow.

What does the fox say?

Ring-ding-ding-ding-dingeringeding

1. MOA and 2. Therapeutic use of phenylephrine?

1. Phenylephrine is an a-receptor agonist.



2. Mydriasis, decongestant, and raises blood pressure.

1. MOA and 2. Therapeutic use of xylometazoline/ oxymetazoline?

1. Both are a-receptor agonist.



2. Topical decongestant. May also cause hypotension due to significant affinity for a2 receptors (inhibition)

How does a2 selective agonists affect blood pressure?

Causes BP to decrease by decreasing sympathetic output.



Done through decreasing chronotropy and inotropy (B1) and decreasing vascular tone (a1).

1. MOA and 2. Therapeutic use of clonidine?
1. a2 selective agonist 2. Antihypertensive, alcohol and nicotine withdrawal, analgesic
Side effects of clonidine?

1. Dry mouth (decreased sympathetic tone) 2. Constipation (block release of acetylcholine)

1. MOA and 2. Therapeutic use of isoproterenol?
1. Is a B agonist 2. Positive inotropy and chronotropy, increase cardiac output, potent vasodilator (B1)
1. MOA and 2. Therapeutic use of salbutamol?

1. B2 selectic agonist 2. Treatment of asthma (dilates bronchial smooth muscles)

1. MOA and 2. Therapeutic use of myrabegron?
1. B3 selective agonist 2. Treatment of overactive bladder (relaxes bladder detrusor muscles) 3. Also possible antiobesity drug (increase lipolysis)

Side effects of myrabegron?

1. Hypertension and tachycardia 2. Inhibits CYP2D6 (drug interactions)