Autonomic Pharmacology Flashcards
Bradycardia
Decreased Heart Contractility
Receptor, Para/Sympathetic
M2, Parasympathetic
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
No effect on skin, skeletal vessels, sweat glands, liver, fat cells and kidney
Parasympathetic nervous System
Smooth muscle contraction
(Mydriasis, vasoconstriction, GIT/bladder sphicter contraction, Uteral contraction, Ejaculation)
Sweating
Glycogenolysis (with Beta2)
Receptor, Para/Sympathetic
Alpha1, Sympathetic
GIT wall relaxation (With Beta2)
Receptor, Para/Sympathetic
Alpha2, Sympathetic
Tachycardia
Increased heart contractility
Increased renin
Receptor, Para/Sympathetic
Beta1, Sympathetic
Smooth muscle relaxation
(Skeletal vasodilation, Bronchiodilation, GIT/bladder wall relaxation, Uteral relaxation)
Glycogenolysis (With Alpha1)
Receptor, Para/Sympathetic
Beta2, Sympathetic
No effect on GIT secretion
Sympathetic Nervous System
Enzyme for synthesis of Ach from Acetyl CoA and Choline
Choline Acetyltransferase
Inhibitor of Ach synthesis
Inhibits Choline Acetyltransferase
Hemicholinium
Hear Very Brief Noise, AChooo
Inhibitor of Ach storage in vesicles
Vesamicol
Hear Very Brief Noise, AChooo
Inhibitor of Ach release into synaptic cleft
Botulinum toxin
Hear Very Brief Noise, AChooo
Inhibitor of Ach degradation/metabolism by acetylcholinesterase
Class? Drugs?
Indirect-acting cholinomimetics
(Neostigmine, Carbamates, Orgnophosphates)
Hear Very Brief Noise, AChooo
Degrades Ach into choline and acetate
Acetylcholinesterase
Drug for bowel and bladder atony
Drug, class
Betanechol, direct acting cholinomimetic
Drug that increases aqueous humor outflow and
increases salivation, acts on M3
Drug, class
Pilocarpine, direct acting cholinomimetic
Drug for glaucoma, sjogren syndrome, sicca syndrome
SE: miosis, BOV from cyclospasm
Drug, class
Pilocarpine, direct acting cholinomimetic
Triad of:
Xerostomia (dry mouth)
Xerophthalmia (dry eyes)
Rheumatoid arthritis
Sjogren Syndrome
Xerostomia (dry mouth)
Xerophthalmia (dry eyes)
Sicca Syndrome (milder Sjogren)
Drug for smoking cessation
Acts on Nicotinic receptors
Varenicline (Nicotine)
Direct Acting Cholinomimetic
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
Toxicity of which receptor presents as: Fasciculations Paralysis Convulsions followed by CNS depression Ganglionic stimulation
Nicotinic
MOA of indirect acting cholinomimetics
Bind to cholinesterase, inhibiting effects on Ach, causing increased Ach effects in sites of Ach release
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
Increase in GIT secretion (with M3)
Receptor, Para/Sympathetic
M1, Parasympathetic
