Autonomic Pharmacology Flashcards by Tin Hernandez

Bradycardia
Decreased Heart Contractility

Receptor, Para/Sympathetic

M2, Parasympathetic

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Increase in GIT secretion (with M3)

Receptor, Para/Sympathetic

M1, Parasympathetic

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Miosis
Bronchial constriction
GIT wall contraction
GIT sphincter relaxation
Increased GIT Secretion (with M1)
Bladder wall contraction
Bladder sphincter relaxation
Uteral contraction
Erection

Receptor, Para/Sympathetic

M3, Parasympathetic

Lahat ng nakakahiyang mangyari in public
Sikip sa mata, di makahinga
For digestion, urination, erection

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No effect on skin, skeletal vessels, sweat glands, liver, fat cells and kidney

Parasympathetic nervous System

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Smooth muscle contraction
(Mydriasis, vasoconstriction, GIT/bladder sphicter contraction, Uteral contraction, Ejaculation)
Sweating
Glycogenolysis (with Beta2)

Receptor, Para/Sympathetic

Alpha1, Sympathetic

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GIT wall relaxation (With Beta2)

Receptor, Para/Sympathetic

Alpha2, Sympathetic

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Tachycardia
Increased heart contractility
Increased renin

Receptor, Para/Sympathetic

Beta1, Sympathetic

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Smooth muscle relaxation
(Skeletal vasodilation, Bronchiodilation, GIT/bladder wall relaxation, Uteral relaxation)
Glycogenolysis (With Alpha1)

Receptor, Para/Sympathetic

Beta2, Sympathetic

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No effect on GIT secretion

Sympathetic Nervous System

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Enzyme for synthesis of Ach from Acetyl CoA and Choline

Choline Acetyltransferase

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Inhibitor of Ach synthesis

Inhibits Choline Acetyltransferase

Hemicholinium

Hear Very Brief Noise, AChooo

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Inhibitor of Ach storage in vesicles

Vesamicol

Hear Very Brief Noise, AChooo

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Inhibitor of Ach release into synaptic cleft

Botulinum toxin

Hear Very Brief Noise, AChooo

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Inhibitor of Ach degradation/metabolism by acetylcholinesterase

Class? Drugs?

Indirect-acting cholinomimetics
(Neostigmine, Carbamates, Orgnophosphates)

Hear Very Brief Noise, AChooo

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Degrades Ach into choline and acetate

Acetylcholinesterase

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Drug for bowel and bladder atony

Drug, class

Betanechol, direct acting cholinomimetic

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Drug that increases aqueous humor outflow and
increases salivation, acts on M3

Drug, class

Pilocarpine, direct acting cholinomimetic

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Drug for glaucoma, sjogren syndrome, sicca syndrome
SE: miosis, BOV from cyclospasm

Drug, class

Pilocarpine, direct acting cholinomimetic

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Triad of:
Xerostomia (dry mouth)
Xerophthalmia (dry eyes)
Rheumatoid arthritis

Sjogren Syndrome

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Xerostomia (dry mouth)

Xerophthalmia (dry eyes)

Sicca Syndrome (milder Sjogren)

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Drug for smoking cessation

Acts on Nicotinic receptors

Varenicline (Nicotine)

Direct Acting Cholinomimetic

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Toxicity of which receptor presents as:
CNS stimulation
Miosis (constriction), Cycloplegia (loss of accomodation)
Bronchoconstriction
Excessive GIT smooth muscle activity
Increased secretory activity
Vasodilation

Muscarinic

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Toxicity of which receptor presents as:
Fasciculations
Paralysis
Convulsions followed by CNS depression
Ganglionic stimulation

Nicotinic

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MOA of indirect acting cholinomimetics

Bind to cholinesterase, inhibiting effects on Ach, causing increased Ach effects in sites of Ach release

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Drug for Myasthenia Gravis diagnosis Can differentiate Cholinergic from Myasthenic Crisis Very short acting

Edrophonium | Indirect acting cholinomimetic

Tx for Myasthenia gravis Reversal of nondepolarizing blockade Muscarinic effects are blocked by Atropine

Neostigmine | Indirect acting cholinomimetic

Indirect acting cholinomimetic used as tx for glaucoma

Physostigmine

Which receptors are destroyed in Myasthenia gravis?

Nicotinic Ach receptors

In Myasthenia Gravis: Worsening of sx due to UNDER medication Improved muscle strength with Edrophonium

Myasthenic crisis

In Myasthenia Gravis: Worsening of sx due to OVER medication Weakens muscle strength with Edrophonium

Cholinergic crisis

Drug for Alzheimer's

Rivastigmine Indirect acting cholinomimetic (Donezepil, Galantamine, Tacrine)

Signs and Sx of Organophosphate Poisoning | DUMBBELSS

``` Diarrhea Urination Miosis Bronchospasm Bradycardia Excitation Lacrimation Sweating Salivation ```

Prototype non-selective muscarinic blocker Tertiary amide, readily crosses membrane barriers Tx for Organophosphate poisoning SE: Tachycardia, Mydriasis, Cycloplegia, Skin flushing, delirium, hallucinations

Atropine Muscarinic Antagonist (Homatropine, Cyclopentolate, Tropicamide)

Antidote for Organophosphate poisoning

Atropine | Adjunct: Pralidoxime - to regenerate AchE Give within 6-8 hours

Muscarinic Antagonist Restores neurotransmitter balance in the basal ganglia Drug for Parkinson's Reduces tremors>bradykinesia/rigidity

Benztropine Biperiden Trihexyphenidyl TRI to PARK a BENZ, BIP(beep) here

Drug for asthma Prevents vagal-stimulated bronchoconstriction Most common side effect is dry mouth Preferred in pxs with COPD and heart disease

Ipratropium Tiotropium Muscarinic Antagonist Decreased tachycardia and arrhythmia

Muscarinic antagonist Drug given as transdermal patch for motion sickness Antagonizes histamine and serotonin

Scopolamine

``` HOT as a hare DRY as a bone RED as a beet BLIND as a bat MAD as a hatter ```

``` Atropine Toxicity Hyperthermia Decreased secretions Cutaneous vasodilation (flush) Blurred vision CNS toxicity ```

Muscarinic Blockers are contraindicated in:

Infants: cannot thermoregulate Hyperthermia: decreased sweating Acute angle closure glaucoma BPH

Competitive nicotinic antagonist First successful agents for hypertension but obsolete SE: postural hypotension

Hexamethonium | Trimethapan

Depolarizing neuromuscular blocker

Succinylcholine Naka-DEPOsit sa toilet = SUCCess Depolarizing = Succinylcholine

Nondepolarizing Neuromuscular blocker

Tubocurarine Pancuronium Atracurium Vecuronium "CURa/i/o"

Primary neurotransmitter at post ganglionic sympathetic synapses

Norepinephrine

Dopa/NE on renal BV: VasoDILATES: VasoCONSTRICTS:

Dopa | NE

Inhibits NE synthesis by hydroxylation of tyrosine by Tyrosine Hydroxylase

Metyrosine

Inhibits NE storage in vesicles

Reserpine

Inhibits NE release

Guanethidine

Promotes NE release

Amphetamines | Tyramine

Inhibits diffusion and reuptake of NE in the synaptic cleft

Cocaine | TCAs

Inhibits metabolism of NE by MAO and COMT

MAOIs and COMT inhibitors

2nd messenger of Alpha 1

IP3, DAG (increase)

2nd messenger of Alpha 2

cAMP (decrease)

2nd messenger of Beta 1, 2, and 3

cAMP (increase)

2nd messenger of Dopa 1

cAMP (increase)

Piloerection Adrenoreceptor?

Alpha 1

Platelet aggregation Inh lipolysis Inh insulin release Adrenoreceptor?

Alpha 2

``` Relaxes airway Stim glycogenolysis Stim insulin release Causes tremors Also stimulates rate and force of heart ``` Adrenoreceptor?

Beta2 (Lungs) You have 1 heart, 2 lungs

Stim rate and force of heart Stim JG cells to release renin Adrenoreceptor?

Beta 1 (heart) You have 1 heart, 2 lungs

Stimulates lipolysis Adrenoreceptor?

Beta 3

Dilates renal and other splanchnic vessels Adrenoreceptor?

Dopa 1

Inhibits adenylyl cyclase in nerve terminals (2nd messenger)

Dopa 2