Autonomic Nervous System Flashcards
List of receptors
Nicotinic, alpha, beta, dopamine, muscarinic
Cholinergic effect
DUMBELLS Diarrhea Urination Miosis Bradycardia Emesis Lacrimation Salivation Sweating
Inhibits transporters (uptake of choline into the vesicles)
Hemicholiniums
Inhibits transporter (uptake of acetylcholine)
Vesamicol
Causes release of ACh (exocytosis)
Spider venom (alpha-latrotoxin)
Blocks release of ACh (exocytosis)
Botulinum toxin
Wrinkle tx
Botulinum toxin
Other term for botulinum toxin
Botox
Found in canned goods
Clostridium botulinum
Enzyme for hydrolysis of ACh
Acetylcholinesterase
T/F: choline has no more pharmacologic action
T
Precursor amino acid in synthesis of dopa, adrenaline
Tyrosine
Enzyme tyrosine-> dopa
Tyrosine hydroxylase
DOPA means
Dihydroxyphenylalanine
Enzyme: DOPA to dopamine
DOPA decarboxylase
Inhibits tyroxine hydroxylase
Metyrosine
Inhibits DoPA decarboxylase
Carbidopa
Enzyme: dopamine to norepi
Dopamine beta-hydroxylase
Responsible for degradation of dopamine
Reserpine
Enzyme: noradre to adrenaline
Phenylethanolamine n-methyltransferase
Used for diagnosis of too much catecholamines
Urine matabolites: vanillylmandelic acid, metanephrine, normetanephrine
Inhibits reuptake of catecholamines
Cocaine, TCA
Promotes release of cathecolamines from presynapse
Amphetamine, methamphetamine, ephedrine, tyramine, pseudoephedrine
Inhibits release of cathecolamines
Guanethidine, bretylium
Ion that Causes release of NE
Calcium
Alpha 1 receptors
Blood vessels (vasoconstriction), pili erector muscles(contrac), pupils (mydriasis), sphincters GIT/GUT(closed)
Alpha 2
Presynaptic (modulates NE, decrease cathecolamine release), postsynaptic( relax smooth muscles, vasoconstric)
Beta 1
Heart increase rate, kidney (renin release)
Beta 2
Bronchus (dilation), skeletal muscles (contract), uterus (relax), pancrease (insulin release), metabolism ( glucogenesis)
Beta 3
Adipose tissue (lipolysis)
Dopamine 1
Blood vessels of renal, mesenteric, coronary (vasodilation therfore increase blood flow in kidney)
Dopamine 2
Cns
Types of adrenergic agonist
Catecholamines and noncatecholamines
Catecholamines with __ groups, __ metabolism, __ polarity
Catechol or 3,4-dihydroxybenzene group, COMT AND MAO metabolism, polar therefore difficult to penetrate CNS
Non-catecholamine, __ metabolism, __ polarity
Decrease metab therefore longer half life, increase lipid solubility therefore non polar
DOC: bronchospasm
Epinephrine
DOC: anaphylactic rxn
Epinephrine
1st line cardiac stimulant
Epinephrine
1st line anaphylaxis
Epi
1st line local vasoconstriction
Epi
1st line glaucoma
Epi
Beta 1 and 2 agonist
Isoproterenol
Tocolytics
Ritodrine, terbutaline, isoxsuprine
Partial beta 1 agonist
Penalterol
AE: orthostatic hypotension
Clonidine, methyldopa, guanabenz, guanfacine
Drug thAt causes false + in coombs text
Methyldopa
Causes withdrawal rebound hypertension
Clonidine
Alpha 1 agonist
Phenylephrine, phenylpropanolamine, pseudoephidrine, methoxamine
Hypotension during surgery involving halothane anesthetics
Methoxamine
Usually combined with local anesthetics during hypotensive emergencies
Phenylephrine
Alpha 2 agonist
Clonidine, methyldopa, guanabenz, guanfacine, apraclonidine, brimonidine
For paroxysmal atrial tachycardia
Phenylephrine, methoxamine
T/F methyldopa is a prodrug
True
Alpha 1 and 2 agonist
Oxymetazoline, xylometazoline
Short acting beta 2 agonist
Albuterol, terbutaline, metaproterenol, pirbuterol
Alpha 2 agonist with nasal decongestant effect
Clonidine
Alpha 2 agonist used in adhd
Clonidine, guanfacine
Alpha 2 agonist for glaucoma
Apraclonidine, brimonidine
Drug under dopamine 1 selective
Fenoldopam
Doc for acute asthma
Epinephrine
Doc for chronic asthma
Beta 2 agonist
Long acting beta agonist
Salmeterol, formoterol, bambuteril
T/F indirect acting sympathomimetics are non catecholamines
T
Can cause HTN in patients taking MAOI
Tyramine
Indirect acting sympathomimetics
Tyramine, amphetamine, metamphetamine, phenmetrazine, methylphenidate, pemoline, phentermine, modafinil
Phenmetrazine
Adhd
Methylphenidate
Adhd
Pemoline
Adhd
Phentermine
Adhd
Modafinil
Narcolepsy
Alkaloid from ma huang
Ephedrine
Mixed acting sympathomimetic
Ephedrine, metaraminol
Used in shock patients when infusion of norepi and dopa is not possible
Metaraminol
List of neurotransmitters
Ach, NE, Epi, Dopamine
Alpha 1 blockers
Prazosin, doxazosin, terzosin, trimazosin, alfuzosin
For BPH
Alpha 1 blockers
First dose syncope
Alpha 1 blockers
Indole alkaoid drug alpha 2 antagonist
Yohimbe
For persistent neonatal pulmonary HTN
Tolazoline
For impotence (penile injection)
Yohimbe
For vasospasm in raynaud’s syndrome
Phenoxybenzamine, phentolamine
For HTN due to pheochromocytoma
Phenoxybenzamine (irreversible), phentolamine(reversible)
CI of propronolol
Asthma and copd, due to bronchoconstriction
More potent than propranolol
Nadolol, one dose per day
For Life threatening vtach
Sotalol
Maintenance of sinus rhthym in patients with atrial fibrillation
Sotalol
Beta 1 and 2 blocker with action potential prolonging action
Sotalol
Beta 1 blockers
Bisoprolol, betaxolol, esmolol, atenolol, acebutolol, alprenolol, metoprolol, nebivolol, celiprolol
For HTN with impaired pulmonary function
Beta 1 blockers
For diabetic HTN px with insulin or oral hypoglycemic agents
Beta 1 blockers
Beta blockers with intrinsic sympathomimetic activity (with bronchodilatory effects), with min carbs disturbance, with moderate bradycardia
Pindolol. Penbutolol, acebutalol. Carteolol,
Beta blockers with membrane stabilizing activity (can act as local anesthetic effects)
Pindolol, propranolol, betaxolol, labetalol, metoprolol, acebutolol
Mixed alpha, beta blocking effects
Labetalol, carvedilol, medroxalol, bucindolol
Alkaloid from rauwolfia serpentina
Reserpine
Indirect acting adrenergic blockers
Guanethidine, reserpine
__ bond of acetyl derivative and choline, hydrolyzed by: ___
Ester bond, cholinesterase
Prototype of beta blockers
Propranolol
Increase cardiac output with little change in the heart rate
Dobutamine
Choline esters, mixed M and Nicotinic
Acetylcholine, carbachol, methacoline (weak)
Choline ester, muscarinic only
Betanechol, metacholine
Muscle that causes miosis
Papillary constrictor muscles
Muscle that accomodates focus for near vision, facilitating outflow of aqueous humor to schlemn cannal
Ciliary muscles
Prototype cholinomimetics
Acetylcholine
Most potent cholinergic agonist
Acetylcholine
Indication of bethanechol
Bladder (urination,), bowel (diarrhea)
For increase intestianl motility after surgery
Bethanecol
T/F acetylcholine has limited therapeutic use
T bcoz rapid hydrolysis
For open angle glaucoma resistant to pilocarpine
Carbachol
For diagnosis of asthma
Methacholine (provocholine = provoke testing) possible cause ng bronchoconstriction
Alkaloid direct acting muscarinic
Pilocarpine, muscarine
Alkaloid directing acting nicotinic only
Nicotine, lobeline, varenicline
Alkaloid direct acting mixed muscarinic and nicotinic
Arecoline
Alakoid from pilocarpus sp.
Pilocarpine
Can cross bbb cholinomimetic
Pilocarpine
Pilocarpine dosage form
Open angle, use gel time release
Closed angle, use drops
Doc for glaucoma cholinomimetic
Pilocarpine
Alkaloid from amanita muscaria
Muscarine
Where to find muscarine
Inocybe, clitocybe, omphalatus
The only irreversible indirect acting chlonergic agonist
Organophosphate
Thiophosphate prodrugs
Malathion, parathion
Active metabolites of malathion, parathion
Malaoxon, paraoxon
Nerve gases
Tabun, sarin, soman
Chemical warfare
Tabun, sarin, soman
Drugs under organophosphates
Isofluorophate, echothiophate, malathion, parathion, tabun, sarin, soman
Cholinergic crisis
Organophosphate toxicity
Antidote for organophosphate toxicity
Pralidoxime chloride (2-PAM), atropine
Moa of organophosphate
Bind to AChE forming covalent phosphorus bond (phosphorylated enzyme)
Aging - breaking of oxygen-phosphorus bond, forming strenghtened phosphorus enzyme bond.
AChE enzyme reactivator
Pralidoxime chloride
Cholinesterase regenerator drug
Pralidoxime chloride
Physiological antagonist for cholinergic syndrome
Atropine
Drugs under carbamates
Physostigmine (eserine), neostigmine, pyridostigmine(mestinon), carbyl, propoxur, aldicarb
Alkaloid from physotigma venenosum
Physostigmine
Used in tensilon test, dosage, observation
Esdrophonium, initial dose (2mg), if no rxn after 45sec additional 8mg
Onservation: i,prove,emt im muscle strength that last for 5 mins.
+: movement of muscle (MG)
-: further weakening of muscle
Test in diagnosis of myasthenia gravis
Tensilon test
Short acting indirect cholinomimetics
Edrophonium
Intermediate to long indirect cholinomimetics
Neostigmine, pyridostigmine, physostigmine, ambemonium, demecarium
Very long acting indirect cholinomimetics
Organophosphates, echothiophate
Centrally acting indirect cholinomimetics
Donepezil (benzylpiperidine), tacrine (acridine), rivastigmine (carbamate), galantamine (phenanthrene)
Other name for atropine
Hyoscyamine
Prototype muscarinic antagonist
Atropine
Used to treat acute mushroom poisoning
Atropine
Muscarinic antagonist
Atropine, scopolamine, homatropine, cyclopentolate, tropicamide, ipratoprium bromide, pirenzepine, benztropine, trihexyphenidyl, oxybutynin, dicyclomine, propantheline
Other drugs that have anticholinergic effects
Antihistamine, antipsychotica, TCA, opiods
Other name for scopolamine
Hyoscine
The only M1 blocker
Pirenzepine, telenzepine
Prevents motion sickness trandermal
Scopolamine
Blocks short term memory
Scopolamine
Used to produce sedation amnesia used in obstetrics with morphine
Scopolamine
Competitive non depolarizing blockers neuromuscular (nicotinic)
Curare derivatives ( vecuronium, atracurium, pancuronium, tubocurarine, mivacurium, rocuronium, pipecuronium, doxacurium)
Prototype neuromuscular blocker
Tubocurarine
Adjunct to anesthesia providing muscle relaxant
Vecuronium
Order of paralysis
Eyes, face, fingers
Limbs, neck, trunk
Intercostal and diaphragm
No histamine release curare but with vagolytic effect
Pancuronium
Prevents fasciculations associated with succinylcholine
Tubocurarine
Adjunct to anesthesia
Pipecuronium, doxacurium
Drug interactions of neuromuscular blockers
Cholinesterase inhibitors
Halogenated hydrocarbon anesthetics
Aminoglycosides antibiotics
Ca channel blockers
Competitive depolarazing neuromuscular blocker
Succinylcholine
Useful when rapid endotracheal intubation is required during induction of anesthesia
Succinylcholine
AE of succinylcholine
Malignant hyperthermia
Tx for malignant hyperthermia
Dantrolene
Alice in wonderland
Mad as a hatter - hallucinations, delirium
Blind as a bat - mydriasis and cyclopegia (blurring of vision)
Dry as a bone - decrease secretions
Red as a beet - tachycardia, vasodilation, flushing
Hot as a hare - fever, hyperthermia
Moa of dantrolene
Block calcium release
Ganglionic blockers
Nicotine, hexamethonium, mecamylamine, trimethaphan
Was introduced clinically as the first drug effective for mngt of hyptertension
Hexamethonium
For smoking cessation theraphy
Nicotine
Nicotine moa
Low dose, sympa (increase bp)
High dose, para (decrease bp)
Tx of HTN caused by pulmonary edema or dissecting aortic aneurysm
Trimethaphan