Autonomic Pharmacology Flashcards
Spinal roots of origin for SANS
Thoracolumbar - thoracic ( T1-T12) and lumbar (L1-L5) segments of the spinal cord
Part of ANS consist of myenteric plexus and submucous plexus
Enteric nervous system (ENS)
Myenteric plexus - Auerbach plexus
Submucous plexus - Meissner plexus
Spinal roots of origin for PANS
Crariosacral - CN III, VII, IX and X and sacral segment of spinal cord (S3 and S4)
Ganglia for SANs are located at?
Paravertebral chains lie along the spinal cord
Location of ganglia for PANS
Located in the organ innervated
Has shorter preganglionic fiber and a longer postganglionic fiber
SANS - Sympathetic ANS
Shorter postganglionic fiber and longer preganglionic fiber
Parasympathetic ANS
Receptor causes Mydriasis? And miosis?
Mydriasis - a1 receptor of Sympathetic ANS
Miosis - M3 receptor of Parasympathetic ANS
Primary transmitter in all autonomic ganglia and parasympathetic postganglionic neurons synapses
Acethylcholine
Enzyme that synthesized ACh from acetyl-CoA and choline
Choline acetyltransferase (CHAT)
Choline transport is inhibited by what?
Hemicholinium
Vesamicol inhibit what enzyme that actively transport ACh into vesicles
Vesicle-associated transporter (VAT)
Calcium triggers interaction among SNARE proteins thus releasing ACh is prevented by what toxin?
Botulinum toxin
Indirect-acting Cholinomimetics inhibits what enzyme thus preventing degradation of ACh into choline and acetate
Acetylcholinesterase
Direct-acting, muscarinic drug used for post-surgery or spinal cord injury bladder/bowel atony
Betanechol-M3 receptor activator
Direct-acting, muscarinic, for glaucoma, Sjogren syndrome and Sicca syndrome
Pilocarpine - M3 receptor increasing aqueous humor outflow
Sjogren syndrome triad?
A. Xerostomia
B. Xerophthalmia
C. Rheumatoid arthritis
Varenicline is used for smoking cessation belongs to what type of drug classification?
Nicotine - direct-acting cholinomimetics, nicotinics
Cyclospasm, miosis, bronchoconstriction are present in what drug toxicity?
Muscarinic toxicity
Toxicity results to blockade of neuromuscular end plate depolarization leading to fasciculations and paralysis
Nicotinic toxicity
Group of drugs that bind to cholinesterase and amplify acetylcholine effects wherever ACh is released
Indirect-Acting Cholinomimetics
Drug used for differentiation between cholinergic and myasthenic crisis in Myasthenia gravis
Edrophonium - short-acting upon IV administration
Diagnosis for MG: Tensilon test
Used for MG, Ogilvie syndrome and reversal of nondepolarizing neuromuscular blockade
Neostigmine
Myasthenia gravis is an autoimmune destruction of what receptors? Resulting to fluctuating muscle, weakness, ocular symptoms and proximal muscle weakness
Nicotinic ACh receptors
Aside from infection and stress, Myasthenic crisis results from?
Undermedication - symptoms improved with Edrophonium
Cholinergic crisis results from excessive activation of cholinoreceptors due to?
Overmedication- Edrophonium weakens muscle strength
Indirect-acting cholinomimetic drug used for Alzheimer’s disease
Rivastigmine - SIMD: Donepezil, Tacrine
Signs and symptoms of organophosphate poisoning
DUMBBELSS-diarrhea, urination, miosis, bronchospasm, bradycardia, excitation, lacrimation, sweating and salivation
First choice antidote for organophosphate poisoning
Atropine - completely blocks all muscarinic receptors
Chemical antagonist, antidote for organophosphate poisoning and nerve gas poisoning, must be administered 6-8hrs before bond with cholinesterase
Pralidoxime
Prototype nonselective muscarinic blocker, a tertiary amine that crosses membrane barriers; SIMD: Homatropine, Cyclopentolate and Tropicamide
Atropine - also for mydriatic, cycloplegic
Non-selective muscarinic blocker used for Parkinson’s disease
Benztropine, Biperiden, and Trihexyphenidyl - reduces tremors more than bradykinesia
Cholinergic-muscarinic antagonist used for Asthma and COPD
Ipratropium - prevents vagal-stimulated bronchoconstriction, less likely cause tachycardia and cardiac arrhythmias
Cholinergic-muscarinic antagonist used for motion sickness, antagonizes histamine and serotonin
Scopolamine - applied as transdermal patch
What drug toxicity results to fever, flush, tachycardia, arrhythmias, CNS toxicity
Atropine toxicity
First successful agents for hypertension but were abandoned due to its severe adverse effect on ganglion blockade
Ganglionic blockers
Cholinergic-nicotinic antagonist used for hypertension and hypertensive emergencies
Hexamethonium - se: postural hypotension
Primary transmitter at the sympathetic postganglionic neuron-effector cell synapse in most tissues except for eccrine sweat glands and vasodilator sympathetic fibers in skeletal muscles
Norepinephrine
Hydroxylation of tyrosine to DOPA is inhibited by?
Metyrosine -inhibits tyrosine hydroxylase enzyme
Vesicular transport of NE and DOpamine to vesicles is inhibited by?
Reserpine (stage 2: storage)
Guanethidine inhibits release of NE during step 3 but promoted by _____ and _____
Amphetamine and Tyramine
Reuptake of NE via NET and DAT in synaptic cleft is inhibited by?
Cocaine and TCAs
Norepinephrine is metabolized by MAO and COMT into?
Metanephrines and VMA
Symphatomimetic, direct-acting, non-selective used for cardiac arrest, anaphylaxis,
Epinephrine - actions on a1, B1, and B2 receptors
Norepinephrine - sympathomimetic, direct-acting, non-selective is used as last resort for what type of shock?
Cardiogenic shock - also for neurogenic shock
Sympathomimetic, non-selective, direct-acting drug that activates alpha, beta and D1 receptors
Dopamine - used for shock, and heart failure
1-5mcg/kg/min dose of Dopamine causes vasodilation in the splanchnic and renal vascular beds via what receptors?
D1 receptors - increased renal blood flow and urine output
At what dose of Dopamine causes vasoconstriction and increased blood pressure via alpha receptors?
High dose (>15mcg/kg/min)
At what dose of Dopamine that activates the B1 receptors resulting to increase renal blood flow, heart rate, cardiac contractility and cardiac output?
Medium dose at 5-15 mcg/kg/min
Sympathomimetic, beta-nonselective drug used for asthma
Isoproterenol
Sympathomimetic, a1 selective drug, used for decongestant with a side effect of having rebound nasal congestion
Phenylephrine - causes mydriasis without cycloplegia
Drug that decreases central sympathetic outflow used for hypertension, cancer pain and opioid withdrawal
Clonidine - sympathomimetic, a2 selective
Drug used for rebound hypertension
Phentolamine
Sympathomimetic drug, a2-selective, used for pre-eclampsia
Methlydopa. - SE: hemolytic anemia
Apraclonidine, a2-selective drug used for glaucoma by what mechanism?
Activates a2-receptor : decreasing secretions of aqueous humor
Sympathomimetic, B1-selective drug for acute heart failure and cardiogenic shock. Also used in cardiac stress testing
Dobutamine
Drug of choice for acute asthma attacks, used also as tocolysis for preterm labor (terbutaline/ritodrine)
Albuterol/Salbutamol - may precipitate arrhythmias in patient with concurrent COPD and heart disease
If B1and D1 agonists is for acute heart failure/septic shock then ____ is for hemostasis, decongestion and spinal shock
a1 agonist
B2 agonist is for bronchospasm/premature labor then _____ is for hypertension and glaucoma
a2 agonist
Alpha-nonselective antagonist used for Pheochromocytoma (pre-surgical). Effects last for several days
Phenoxybenzamine - SE: orthostatic hypotension
Alpha-nonselective used as antidote to a1 agonist overdose, rebound hypertension, and pre-surgical pheochromocytoma
Phentolamine
a1 selective antagonist for benign prostatic hyperplasia, hypertension
Prazosin - Tamsulosin (most selective for prostatic smooth muscle)
Beta-nonselective antagonist for angina prophylaxis, hypertension, migraine and hyperthyroidism
Propranolol
Nonselective beta blocker that has combined a and B blockade maybe used for pheochromocytoma
Carvedilol and Labetalol
Nonselective beta blocker that has Intrinsic Sympathomimetic Activity
Acebutolol and Pindolol - ISA = advantage in treating patient with asthma because it less likely cause bronchospasm
Beta blockers that are useful for glaucoma since it has less effect on protective reflexes and less risk for corneal ulceration
Timolol and Betaxolol
Beta-blocker that has
A. Longest half-life
B. Shortest half-life
A. Nadolol - NasaDOLO = longest half life
B. Esmolol - ESMOL (small) = shortest half life
Autonomic drugs used for Glaucoma except:
Mannitol, Timolol, Apraclonidine, Epinephrine
Mannitol used for Glaucoma but it is not an autonomic drug, it is an osmotic agent