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68 Cards in this Set
- Front
- Back
synaptic location of parasympathetic preganglionic neuron
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ganglia near organ innervated
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synaptic location of sympathetic preganglionic neuron
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ganglia located near spinal cord
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neurotransmitter for parasympathetic preganglionic and postganglionic neuron
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ACh for both
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neurotransmitter for sympathetic preganglionic and postganglionic neuron
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ACh for preganglionic and NE for postganglionic
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M1 receptor
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neural
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M2 receptor
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cardiac
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M3 receptor
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glandular
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Two types of nicotinic receptor?
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ganglionic and NMJ
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For cholinergic agonist, describe change in airway resistance, GI function, pupil function
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increase airway resistance
increase GI motility pupils will contract (miosis) |
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How is ACh synthesized?
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acetyl CoA + choline, w/ choline acetyltransferase as enzyme
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benthenacol
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- directly acting muscarinic agonist
- stimulate atonic bladder - not degraded by AChE |
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carbachol
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- directly acting muscarinic agonist
- can be used to treat glaucoma... but is rarely used - resistant to AChE |
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pilocarpine
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- directly acting muscarinic agonist
- drug of choice to treat glaucoma (esp emergency) - resistant to AChE |
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physostigmine
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- reversible cholinesterase inhibitor
- used to treat atony of GI and bladder |
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neostigmine
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- reversible cholinesterase inhibitor
- treat symptomatic myasthania gravis |
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pyridostigmine
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- reversible cholinesterase inhibitor
- treat chronic myasthania gravis - duration of action is longer than neostigmine |
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edrophonium
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- reversible cholinesterase inhibitor
- diagnosis of myasthania gravis - short duration of action |
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isofluorate
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- irreversible cholinesterase inhibitor
- can be used for open-angle glaucoma (echotiophate is used instead) |
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pralidoxine
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- aka 2-PAM
- used to reactivate AChE that has been inhibited by isofluorate - cannot penetrate CNS |
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atropine
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- given iv
- to treat bradycardia after MI |
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tropacamide
cyclopentolate |
- to dilate pupil
- tropacamide short acting - cyclopentolate long acting - muscarinic antagonist |
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scopolamine
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- prevent motion sickness
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benztropine
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- parkinson's
- muscarinic antagonist |
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ipratropium
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- inhibit bronchoconstriction
- treat asthma - muscarinic antagonist |
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dicyclomine
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- irritable bowel syndrome
- colonic diverticular disease -muscarinic antagonist |
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pirenzepine
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- peptic ulcer disease
- muscarinic antagonist |
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nicotine
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- low conc - ganglionic stimulation
- high conc - ganglionic blockade - both sympathetic and parasympathetic are stimulated |
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hexamethonium
trimethaphan trbucurarine |
- block all autonomic ganglia and enteric ganglia
- hypotension, loss of cardiovascular reflexes, inhibition of secretions, GI paralysis, impaired micturition - clinically obsolete except trimethaphan |
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substances that block choline uptake
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hemicholinium
triethylcholine |
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substances that block ACh release
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aminoglycoside antibiotics
botulinum toxin |
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drugs used to cause paralysis during anaesthesia
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turbocurarine
gallamine pancuronium atracurium succinylcholine |
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curare
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- non-depolarizing competitive blocker
- in low conc, combines with nAChR and prevents binding of ACh - in high conc, blocks ion channels |
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succinylcholine
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- depolarizing blocker
- binds to nAChR, acts like ACh and depolarizes muscle - not destroyed by AChE - causes flaccid paralysis - adverse effects: hyperthermia, apnea |
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B1 receptors are found on.... (3)
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heart
kidney fat cells |
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B2 receptors are found on.. (3)
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BRONCHIAL tree
ciliary muscle detrusor muscle |
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a1 receptors are found on...
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ARTERIES
uterus ureter/trigone/spincter SMOOTH MUSCLE secretion/glands ..everything basically |
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a2 receptors are found on
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GI
bronchial tree insulin from pancreas |
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What is the rate limiting step in the synthesis of norepinephrine?
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tyrosine -> DOPA
w/ tyrosine hydroxylase |
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COMT metabolizes norepinephrine and epinephrine into what products?
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norepinephrine -> normetanephrine
epinephrine -> metanephrine |
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Which receptors does epinephrine act on?
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ALL adrenergic receptors (a1, a2, b1, b2)
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In terms of skeletal muscle dilatation, how do epinephrine, norepinephrine, and isoproterenol differ?
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Epi and Iso dilate skeletal muscle vessals, NE does not
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Which receptors does isoproterenol act on, and what is its major effect?
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- b1 and b2
- major cardiac effect (increases HR, decreases peripheral resistance) - used for emergency heart situations |
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Why is dopamine the choice drug for shock?
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- has an effect on heart function (b1)
- also causes renal and messenteric vasodilation b/c of D1 and D2... this increases kidney blood flow, glomerular filtration rate and Na+ diuresis which the other drugs do not do |
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What are the differences between cathecholamines and noncatecholamines?
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- C are rapidly metabolized by COMT/MAO, NC are not
- C have poor CNS penetration b/c they are polar... NC are more lipid soluble therefore can penetrate CNS - NC have longer duration of action |
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What are the major uses for epinephrine?
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- acute asthma attack (bronchodilation, b2)
- anaphylactic shock - glaucoma (applied topically to reduce intra-ocular pressure.. decreased production of aqueous humor) - anaesthetic |
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What receptor does dobutamine act on and what is its therapeutic use?
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b1, used to increase CO in congestive heart failure
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What receptor does phenylephrine act on and what is its use?
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- a1 agonist
- used as nasal decongestant (vasoconstrictor) |
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methoxamine receptor and use
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- a1 agonist
- used to raise blood pressure during surgery (also raises TPR) |
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How does clonidine lower blood pressure in essential hypertension?
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- a2 receptor
- dimishes sympathetic outflow from medulla, which decreases CO, TPR and HR |
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albuterol
pirbuterol terbutaline salmeterol |
- b2 bronchodilators
- duration of action varies |
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amphetamine
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- indirect acting agonist
- peripheral action via release of stored catecholamines.. - can increase BP and stimulate heart |
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tyramine
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- enters nerve terminal and displaces stored NE.. can increase BP
- not a useful clinical drug - found in ripe cheese and wine |
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phentolamine
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- direct acting antagonist (a)
- causes postural hyptension - reflex cardiac stim. and tachycardia; blocks a2 receptors on cardiac sympathetic nerves |
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phenoxybenzamine
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- noncompetitive, irreversible alpha antagonist
- not useful in maintaining lower BP in hypertension - used in pheochromocytoma removal |
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prazosin
terazosin tamsulosin |
- alpha 1 blockers (competitive)
- treat hypertension - "first-dose" exaggerated hypotensive effect |
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propranolol
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- nonspecific beta blocker (competitive)
- decreases HR, BP, CO - bronchostriction - increased Na+ retention and plasma volume can lead to compesatory increase in BP - used to treat glaucome, hypertension, migraine, hyperthyroidism, angina, MI patient to prevent second heart attack |
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What receptor(s) does propanolol affect?
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b1 and b2. .nonspecific beta blocker
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Why might propanolol lead to a compensatory increase in blood pressure?
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b/c decreased blood pressure and renal perfusion leads to Na+ retention and plasma volume
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What are the therapeutic uses for propanolol?
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- glaucoma (decrease secretion of aqueous humor)
- migraine - hyperthyroidism - angina - MI patient |
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timolol and nadolol
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nonspecific b1 and b2 blockers
more potent than propanolol timolol useful for glaucoma |
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atenolol
acebutolol pindolol |
b1 specific blocker
lower blood pressure in hypertension (esp diabetic) acebutolol and pindolol are partial agonists |
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carvedilol
labetalol |
alpha and beta blockers
reduce blood pressure carvedilol benefits heart failure patients labetalol for black hypertensives |
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reserpine
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- affects transport of catecholamines from cytoplasm to storage vehicles
- therefore MAO metabolizes cytoplasmic NE - gradual decline in blood pressure |
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guanethidine
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- blocks release of stored NE
- gradual decline of BP and HR - rarely used |
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cocaine
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blocks Na-K-APTase which is needed for NE uptake
NE accumulate in synaptic cleft, duration of NE action increased |
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amitriptyline
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tricyclic antidepressant
prevent uptake of NE and serotonin |
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phenelzine
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MAO inhibitor
similar to normal substrate of MAO; binds covalently to MAO and inactivates it |
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ephedrine
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mixed action adrenergic agonist
- induce release of NE from presynaptic terminals and activate post synaptic adrenergic receptors - not metabolized by MAO or COMT - raises BP, bronchodilator - penetrates CNS |