ANS drugs Flashcards by Eric Sun

Where parts of spinal cord do symp and parasymp originate?

Symp—>thoracolumbar

Parasymp—>cranial sacral part

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All ANS start with ___ neurotransmitter and the synapse at ___ receptor?

ACh/nicotinic receptor

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Where do you find Nm receptor?

Skeletal muscle

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What are the 2 exceptions for symp that do not use epi or norepi?

Sweat gland (ACh)
Adrenal medulla--->recieve ACh--->produce epi

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D1 receptor stimulation at the kidney causes?

Renal vasodilation

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TPR or CO has a greater influence on BP?

TPR

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Which 3 receptors control constriction or dilation of the blood vessels?

Alpha 1—>vasoconstrict
Beta 2—>vasodilate
M3—>vasodilate via NO

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What if you give alpha 1 agonist with M antagonist?

Increase BP without reflex bradycardia

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What if you give beta 2 agonist and a beta 1 antagonist?

Decrease BP without reflex tachycardia

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What kind of drug block both reflex tachy and bradycardia?

Nn blocker—>hexamthonium/mecamylamine

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What are the 2 receptor that cause brady or tachycardia?

Beta 1—>tachy

M2—>brady

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What are parasymp/symp affect on the eye?

Parasymp—>sphincter (M)—>miosis
Parasymp—>ciliary muscle (M)—>accommodate to near sight
Symp—>radial muscle (alpha 1)—->mydriasis

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How do you cause cycloplegia (paralysis of accommodation)?

anti M

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How is ACh produced?

Choline uptake—>choline + acetyl CoA—(choline acetyl transferase)—>ACh

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Which drug block the uptake of choline?

Hemicholinium

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AChE inhibitor can only work on ___ organs?

innervated

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Where are M1/2/3 located?

M1—>CNS
M2—>heart
M3—>peripheral

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M stimulation at LES cause constriction or relaxation?

Constriction

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Which M3 receptor is not innervated in your body?

M3 on blood vessel that does vasodilation through NO

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Anti M would produce what kind of affect for M3 on blood vessel?

It would inhibit M3 on blood vessel but it would do nothing to the blood vessel since M3 is not innervated (thus no agonist to compete with)

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M agonist and AChE inhibitor usually produce the same affect except for one place?

M3 on blood vessel—>AChE inhibitor has no effect there

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What organs are only innervated by symp?

Sweat gland/blood vessels

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AChE inhibitor activate both symp and parasymp, but why does it look like it’s mainly parasymp?

Parasymp is the dominate force

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What are the 4 M agonist drugs?

Bethanechol/methocholine/cevimeline/pilocarpine

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Which AChE inhibitor can cross the BBB?

Physostigmine (3rd ammine)

Neuromuscular blockade and myasthenia gravis have what in common?

They both work on Nm receptor

What's the rationale behind treating Alzheimer's with AChE inhibitor?

Alzheimer's--->lost of cholinergic nerve in Meynert's nucleus

Emesis is mediated by which M receptor?

Why is organophosphate fatal?

Permanent depolarization of diaphragm--->inhibiting breathing

Why do we need to be careful on using antimuscarinic on elderly pt?

Precipitate elderly pt for glaucoma

What are some other group of drugs that are antimuscarinic?

1st generation antihistamine/TCA/low potency typical antipsychotic/quinidine/amantadine (antiparkingson)/meperidine (opioid)

List some antimuscarinic drugs

"trop" and "scop" | Atropine/Tropicamide/Ipratropium/Tiotropium/Scopolamine/

What is Oxybutynin used for?

Antimuscarinic--->urge incontinence

If a pt who is on pyridostigmine for myathenia gravis also takes atropine for side effect, would it interfere with pyridostigmine?

No--->Myathenia gravis has antibodies against Nm receptor--->atropine is M antagonist so it does not affect Nm

How is norepi produced?

Tyrosine---(tyrosine hydroxylase)--->dopa--->[dopamine--->norepi] Last step takes place in storage vesicle

What are the rate limiting step for ACh and norepi production?

Uptake of choline/tyrosine hydroxylase

How is norepi being taken out of the synaptic cleft once released?

COMT degrade norepi/norepi reuptake

What does MAO-A do?

It degrades norepi when norepi is reuptaken into the presynaptic neuron

What are the mechanism of amphetamine/TCA/cocaine

Amphetamine--->promote releasing of NE | TCA/cocaine--->prevent reuptake of NE

What do AMPT/clonidine/alpha methyldopa/reserpine/guanethidine do?

They all decrease NE release AMPT--->tyrosine hydroxylase inhibitor Clonidine/alpha methyldopa--->alpha 2 agonist Reserpine--->destroy storage vesicle Guanethidine--->replace NE in the vesicle (release wrong things)

Where do alpha 1 receptor found in your body?

Radial muscle of the eye/blood vessels/bladder (stimulate--->contract--->urinary retention)/kidney (decrease renin release)

Where do alpha 2 receptor found in your body and what happens if you stimulate them?

Presynaptic nerve terminal/platelets (aggregation)/pancreas (decrease insulin secretion)

Stimulate what receptor cause increase renin release?

Beta 1

What are the effect of increase cAMP on skeletal and smooth muscle?

Skeletal muscle--->contract | Smooth muscle--->relax

What is special about beta 2 receptors and where are they found?

``` They are mostly not innervated (thus activated by epi) Blood vessel (vasodilate)/uterus (relax)/branchioles (dilation)/skeletal muscle (contract) ```

What would happen to skeletal muscle if you take too much beta 2 agonist for asthma?

Muscle tremor (skeletal muscle has beta 2)

What are the metabolic affects of beta 2 receptor?

If stimulated--->increase glycogenolysis--->increase blood glucose increase insulin secretion

What happens when you stimulate D1 receptor?

Increase renal perfusion--->increase GFR and Na secretion

What is dose dependent character of dopamine?

Low dose stimulate D1--->medium dose beta 1--->high dose alpha 1

What is fenoldopam used for?

D1 agonist for severe HTN

Between beta and alpha receptor, which one would be activated first in terms of doses?

Beta (low)--->alpha (high)

Which drug is a alpha 1 agonist? what does it used for?

Phenylephrine | Nasal decongestant/eye exam (dilate pupil)

Stimulation of what receptor increase pulse pressure?

Beta 1 (decrease diastolic pressure)

What are the nonselective beta agonist/beta 1 agonist/beta 2 agonist?

``` Nonselective--->isoproterenol (iso=same) Beta 1--->dobutamine--->HF Beta 2: bronchodilator Albuterol Terbutaline--->also used to relax uterus during labor (prevent preterm labor) ```

What receptors do NE work on? what is its affect on the heart?

Alpha 1/alpha 2/beta 1 only (Beta 2 is not innervated) | Increase HR but then decrease (due to reflex bradycardia responding to increase BP caused by alpha 1)

What receptors do epi work on?

Alpha1/2 beta1/2

What are the affect of low and high dose epi?

Low dose--->same as isoproterenol (only beta1/2) | High dose--->same as norepi (mainly alpha1/beta1)

How to distinguish between norepi and high dose epi?

Give alpha 1 blocker Norepi--->BP goes back to normal Epi--->BP goes below normal because of beta 2 affect

Which one (epi or norepi) is used for anaphylaxis shock?

Epi

What does tyramine (cheese and wine) do?

Degraded by MAO-A | If taken MAOi--->tyramine increase NE release like amphetamine--->HTN crisis

What do MAO-A/B metabolize and where are they found?

MAO-A--->metabolize NE/5-HT/tyramine (found Anywhere) | MAO-B--->dopamine (Brain)

Indirect adreoceptor agnoist (e.g. amphetamine/cocaine) can only work on what kind of tissue?

Innervated

Why is reflex tachycardia worse with nonselective alpha blocker?

Blocking alpha 2 as well--->block an inhibitor--->increase NE activity--->worsen reflex tachycardia

What are the 2 non selective alpha blockers and which one is the competitive and which one is the noncompetitive inhibitor? and what are they used for?

Phentolamine--->competitive Phenoxybenzamine--->noncompetitive (longer name) They are used for pheochromocytoma

What are the alpha 1 blockers and what do they do?

"zosin" --->HTN and BPH | Tamsulosin--->alpha 1a receptor blocker--->BPH only

What is the alpha 2 blocker?

Mirtazapine--->antidepressant

What are some affects of beta 2 blockade?

Bronchospasm/decrease aqueous humor production/decrease glucose/increase LDLs and TGs (prevent breakdown)

How to distinguish beta 1 or non selective beta blockers?

start with A-M--->beta 1 blocker only | N-Z--->non selective

What are 2 beta blockers that are also partial agonists?

Acebutolol and pindolol/they do not increase LDL and TG

What should we be cautious about pt who is on chronic beta blocker?

Don't abruptly stop the beta blocker

What can you give with beta blocker overdose?

Glucagon (increase cAMP to oppose beta blocker)

What are selective and nonselective beta blocker most commonly used for?

Selective-->HTN/angina/anti arrhythmia | Nonselective--->glaucoma/migraine prevention/thryotoxicosis/performance anxiety/essential tremor

What is special about carvedilol and labetalol?

Nonselective beta blocker and alpha 1 blocker | Treat HTN and CHF

What is sotalol?

Nonselective beta block + K+ channel blocker (class III anti arrhythmia)