Pharm Exam #1

Two major sides of the autonomic nervous system

Parasympathetic and Sympathetic

Parasympathetic

- Main transmitter

Acetylcholine (ACh)

Sympathetic

- Main transmitter

Mostly norepinephrine

Parasympathetic

-Drug family

Cholinergic

Sympathetic

- Drug family

Adrenergic

Parasympathetic

- Heart

Heart rate goes down

Sympathetic

- Heart

Heart Rate goes up/contractility

Parasympathetic

- Pupils

Constrict

Sympathetic

- Pupils

Dilate

Parasympathetic

- lungs

bronchoconstriction

Sympathetic

- Lungs

bronchodilation

Parasympathetic

- GI

increased peristalsis

Sympathetic

- GI

Decreases digestion

Parasympathetic

- Bladder

contracts bladder

- Urinate

Sympathetic

- Bladder

relaxes bladder

- Retains urine

Agonist

Activates/stimulates a receptor

Antagonist/blocker

Prevents the receptor from being activated

Cholinergic agonist

Turns parasympathetic ON

Cholinergic blocker

Turns parasympathetic OFF

Adrenergic agonist

Turns sympathetic ON

Adrenergic blocker

Turns sympathetic OFF

a1 = squeeze

so this causes...

vasoconstriction

and pupil dilation

a2 = sympathetic OFF switch

Stimulating a2 receptors in the CNS decreases sympathetic output

Associate phenylephrine with...

a1

associate clonidine with...

a2

Clonidine stimulates what

inhibitory a2 receptors in the brainstem ---> decreasing sympathetic outflow to the heart and vessels

B1 = 1 heart

- Increased heart rate

- Increased contractility

- Increased conduction

Main drug of B1

Dobutamine

B2 = 2 lungs

- Stimulation

Bronchodilation

Main B2 drug

Albuterol

B3 = bladder

- Stimulation

Relaxes the detrusor, helping an overactive bladder

Main B3 drug

Mirabegron

Cholinergic agonists increase...

Cholinergic/ACh activity

Parasympathetic causes

- Miosis

- Salivation

- Bronchoconstriction

- Decrease HR

- Increase GI activity

- Increase urination

Parasympathetic

SLUDGE

- S

Salivation

Parasympathetic

SLUDGE

- L

Lacrimation

Parasympathetic

SLUDGE

- U

Urination

Parasympathetic

SLUDGE

- D

Diarrhea

Parasympathetic

SLUDGE

- G

GI cramping

Parasympathetic

SLUDGE

- E

Emesis

Pilocarpine

Direct muscarinic agonist

Pilocarpine for

- Chronic glaucoma and xerostomia (dry mouth)

Causes miosis, which improves aqueous humor drainage and decreases intraocular pressure

Direct muscarinic agonist is...

A type of medication that mimics the neurotransmitter acetylcholine by binding directly to and activating muscarinic acetylcholine receptors

Bethanechol: Direct muscarinic agonist

Big thing...

Bladder empties

How does Bethanechol empty the bladder

Contracting the detrusor and relaxes the urinary sphincter

So Bethanechol leads to what...

Increased urination

What could Bethanechol be used for?

Post-op/Postpartum bladder hypoactivity

Bethanechol also increases what...

GI activity

- Think...

BETH = bathroom

Pyridostigmine

It inhibits acetylcholinesterase

acetylcholinesterase

a fast-acting enzyme that breaks down the neurotransmitter acetylcholine into choline and acetate to stop nerve signals

ACh --> acetylcholinesterase destroys ACh

Pyridostigmine blocks that enzyme

Pyridostigmine --> Acetylcholinesterase ↓ → ACh ↑

Therefore it is...

- Indirect cholinergic agonist

myasthenia gravis

Antibodies damaging ACh receptors, producing muscle weakness

More ACh available...

Improves skeletal muscle activation

Donepezil

Acetylcholinesterase inhibitor → ↑ ACh

- But it acts in the brain

Main use of Donepezil

Alzheimer's disease

Alzheimer's involves degeneration of cholinergic nerves and decreased brain ACh

Donepezil increases available ACh

DONEpezil --> Alzeheimer's

- Does not cure Alzheimer's

- Goal is to improve.support cognitive symptoms

Malathion and Sarin are...

Irreversible cholinesterase inhibitors

Malathion

Pesticide

Sarin

Nerve agent

Malathion and Sarin prevent...

ACh breakdown

Since Malathion and Sarin prevents ACh breakdown...

There is a MASSIVE ACh accumulation

The result of Malathion and Sarin

SLUDGE + bronchoconstriction + bradycardia + muscle problems

High exposure of Malathion and Sarin...

ACh ↑↑↑

→ nicotinic receptors overstimulated

→ desensitization

→ muscle weakness

→ flaccid paralysis

→ respiratory collapse.

Treatment of massive ACh accumulation (malathion and sarin)

Atropine + Pralidoxime

Atropine

Blocks excessive muscarinic stimulation

Pralidoxime

Reactivates acetychlolinesterase if administered early enough; your blocker slides

Varenicline - Chantix

It is a partical nicotinic agonist which is used for..

- Smoking cessation

Varenicline - Chantix

- Smoking cessation

It mildly activates nicotine receptors while preventing nicotine from producing its larger rewarding effect

Think... (Varenciline)

Varenicline partially pretends to be nicotine

Cholinergic agonist adverse effects

You get a wet, slow patient

Diarrhea

Nausea/vomiting

Salivation

Urinary urgency

Bronchoconstriction

Secretions

Bradycardia

Hypotension

Miosis

Be cautious with adverse effects about Cholinergic...

Asthma

Bradycardia

GI obstruction

Cholinergic blockers

Block muscarinic parasympathetic activity

Cholinergic blockers

- DRY patient

Dry mouth

Constipation

Urinary retention

Tachycardia

Dilated pupils

Blurred vision

Decreased sweating

Classic saying for Cholinergic blockers

Can't see, can't pee, can't spit, can't shit

Atropine

- Muscarinic blocker

Blocks parasympathetic slowing of the heart

Atropine leads too..

Increased heart rate

Which then is used for... bradycardia duh

Scopolamine

- Antimuscarinic

Has strong CNS effects

MAIN USE...

Motion sickness

- Usually think scopolamine patch

Scopolamine acts on...

Vestibular/balance system to prevent nausea and comiting

Scopolamine

- Think

Scopolamine -> sea sickness

Oxybutynin

Opposite of bethanechol

Oxybutynin blocks...

Bladder contraction -> don't pee as much

Oxybutynin is used for

Overactive bladder / urinary incontinence

Oxybutynin blocks detrusor contraction increasing...

Bladder cpacity and reducing leakage

Oxybutynin =

Peeing too much -> helps you hold it

Tiotropium

Antimuscarinic in the lungs

Tiotropium

- Blocking parasympathetic bronchoconstriction causes

Bronchodilation

Tiotropium used primarily for

COPD and asthma

- Decreases respiratory secretions

Think... Tiotropium --->

Lungs open

Benztropine

Antimuscarinic acting in the CNS

Benztropine used as an...

Adjunct for Parkinson's disease, particularly:

- Tremor

- Rigidity

- Drooling

Neuromuscular blockers

These are under cholinergic blockers but they're different from atropine/scopolamine/etc.

Neuromuscular blockers affect...

Nicotinic receptors at the neuromuscular junction

Neuromuscular blockers

- Main outcome

Skeletal muscle paralysis

A neuromuscular blocker does not mean...

The patient can't experience pain or awareness

Neuromuscular blockers

- Drugs

- Vecuronium

- Succinylcholine

They work differently

Vecuronium

Non-depolarizing neuromuscular blocker

Think... Vecuronium...

BLOCKS the receptor

Vecuronium blocks the receptor

ACh cannot activate the nicotinic receptor

- Muscle can't contract

- Paralysis