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Direct –Acting Cholinergic Agonists

- Stimulates and binds to the muscarinic receptors

Mechanism of action:
Mimics ACH, can cause pupil contraction, urinary retention, prevent constipation

Drugs:
1. acetylcholine
2. pilocarpine (Pilocar® )
3. bethanechol (Urecholine®)

Indirect –Acting Cholinergic Agonists

Mechanism of action:
inhibits acetylcholinesterase, increases ACH, used to treat myasthenia gravis, antidote for overdosed anticholinergics

Drugs:
1. neostigmine (Prostigmin®)

Anticholinergic

- Binds to cholinergic receptors

Mechanism of Action:
acts as a blocking drug; competitive antagonism

Drugs:
1. atropine
2. dicyclomine (Bentyl®)
3. Ipratropium Bromide

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U2-ANSPart1.ppxd
U2-ANSPart2.ppxd

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Muscarinic

- Located on cardiac, smooth muscle, glands, and the cell membrane of visceral organs
-Stimulated by ACH
-at parasympathetic postganglionic nerve endings

decreases heart rate, bronchoconstriction of the lungs, increases digestion and secretions in the GI tract, increases urination, and cause pupillary constriction in the iris

Nicotinic 1 (Nn):

- at ganglia of parasympathetic nerves and sympathetic nerves (synapse area)
- Stimulated by ACH

Nicotinic 2 (Nm):

- located on the cell membrane of skeletal muscles

- neuromuscular junction of skeletal muscle
- stimulated by ACH

When stimulated, muscle contracts

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Alpha-1

- found on glands, smooth muscles, eyes, most arteries and veins, and ureters
- stimulated by NE and EPI (catecholamines)

Causes vasoconstriction of arteries and veins (increases blood pressure), causes dilation of the pupils (mydriasis), causes smooth muscle contraction

Alpha-2

- parasympathetic response
- decreases the release of NE

Causes vasodilation of arteries and veins (decreases blood pressure), causes a decrease in the contraction of smooth muscles

Beta-1

- located on the heart <3
- stimulated by NE and EPI

Increased heart rate, conduction, and the force of contraction on the heart

Beta-2

- located on smooth muscle, lungs, uterus, skeletal muscle arteries, and coronary arteries
- stimulated by EPI

Causes bronchodilation in the lungs, vasodilation of the coronary and skeletal arteries, relaxes the uterus, and smooth muscle relaxation

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Acetylcholine (ACH)

released at ganglia and postganglionic nerve endings

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Acetylcholine (ACH)

- cholinergic

- released at ganglia from presynaptic nerve ending

Norepinephrine (NE)

- adrenergic

- released at postganglionic
- released by adrenal medulla and neurons

Epinephrine (EPI)

- adrenergic

- produced adrenal medulla

Dopamine (DA)

- precursor to NE

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Also known as the Visceral Nervous System

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(Cholenergic System)
"Rest & Digest"

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(Adrenergic System)
"Fight, Flight, Fright"

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Alpha-1 Adrenergic Agonists

- alpha-1 receptor acted on

Mechanism of action:
contraction of smooth muscle
vasoconstriction causes an increase in blood pressure, and a decongestant effect

Drugs:
1. ephedrine
2. phenylephrine (Neo-Synephrine®)

Adrenergic Agonists

- Acts on all receptors

Mechanism of action:
vasoconstriction causes an increase in blood pressure
Cardiac stimulant
Bronchodilator

Drugs:
1. epinephrine (Adrenalin®)

Alpha-1 Adrenergic Blocking Drugs

- Acts on Alpha-1 receptors and blocks them

Mechanism of action:
relaxes smooth muscle
vasodilation of blood vessels causes a decrease in blood pressure
relaxes the smooth muscle of ureters and increases urine flow

Drugs:
1. prazosin (Minipress®)
2. terazosin (Hytrin®)
3. doxazosin (Cardura®)

Beta-1 Adrenergic Agonists

- Acts on Beta-1 receptor

 Mechanism of action:
Low dose: stimulates d-1 receptors in kidneys causing vasodilation and increased renal blood flow
Moderate dose: stimulates beta 1 receptors and increases force of contraction and cardiac output
High dose: stimulates alpha-1 receptors and causes vasoconstriction increasing blood pressure

Drugs:
1. dobutamine

Beta-2 Adrenergic Agonist

- Acts on Beta-2 receptors

Mechanism of action:
bronchodilation
relaxes the smooth muscle in the uterus

Drugs:
1. albuterol (Proventil®, Ventolin®)
2. terbutaline (Brethine®)
3. formoterol (Foradil®)
4. salmeterol (Serevent®)

Beta-Adrenergic Blocking Drugs

Selective Beta-1 Blockers
- Blocks Beta-1 receptor

Mechanism of action:
decreases force of contraction, cardiac output, heart rate, conduction, and blood pressure

Drugs:
1. atenolol (Tenormin®)
2. metoprolol (Lopressor®)

Non-selective Beta Blockers
- Blocks Beta-1 and Beta-2 receptors

Mechanism of action:
decreases force of contraction, cardiac output, heart rate, conduction, and blood pressure
can cause bronchoconstriction

Drugs:
1. nadolol (Corgard®)
2. propanolol (Inderal®)
3. timolol (Blocadren®)