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Pharm Exam 2 drugs/terms
317
Pharmacology
Graduate
09/15/2011

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Term
neurotransmitter of preganglionic autonomic neurons
Definition
ACh
Term
Receptor type present in all postganglionic neurons
Definition
nicotinic cholinergic (N) receptors
Term
neurotransmitter of parasypmathetic post-ganglionic nerves
Definition
ACh
Term
Basic type of receptor on parasympathetic target organs
Definition
muscarinic (M) cholinergic receptors (M1-5)
Term
Neurotransmitter of sympathetic post-ganglionic nerves
Definition
norepinepherine (NE)
Term
basic type of receptor on sympathetic target organs
Definition
adrenergic receptors (alpha and beta)
Term
this is organized for local regulation of innervated target organs
Definition
parasympathetic division of ANS
Term
This is organized for coordinated activation of all innervated target organs
Definition
Sympathetic division of ANS
Term
------- cells in adrenal medulla release -----when stimulated by ------
Definition
Chromaffin cells, epinepherine, ACh from the sympathetic divison
Term
Three methods of neurotransmitter metabolism
Definition
uptake, degredation, diffusion
Term
Main method of ACh metabolism
Definition
degradation by the enzyme acetylcholinesterase
Term
Three types of catecholamines used in signalling
Definition
epinepherine, norepinepherine, dopamine
Term
Main method of catecholamine inactivation
Definition
re-uptake into pre-synaptic neuron
Term
What is the basic method by which nicotinic cholinergic receptors work?
Definition
They are a ionotropic ligand-gated cation channel, so they allow for flow of ions (i.e. sodium)
Term
How many Muscarinic cholinergic receptors are we aware of?
Definition
M1-M5
Term
How many adrenergic alpha receptors are we aware of?
Definition
2--a1 and a2
Term
How many adrenergic beta receptors are we aware of?
Definition
3---B1, B2, (B3--not as important)
Term
Name the subunits of G-protein receptors
Definition
alpha, beta, gamma
Term
What type of nucleotides do G-protein receptors bind?
Definition
Guanosine nucleotides (GTP and GDP)
Term
Which subunit of G-protein receptors is most important in determining what its effect will be?
Definition
the alpha subunit
Term
cAMP (cyclic adenosine monophosphate) is increased/decreased by Gas
Definition
increased
Term
cAMP (cyclic adenosine monophosphate) is increased/decreased by Gai
Definition
decreased
Term
DAG (diacylglycerol) is increased/decreased by Gaq/11?
Definition
increased
Term
IP3 (inositol triphosphate) is increased/decreased by Gaq/11?
Definition
increased
Term
After dissociation from Gby, Ga subunits perform this function
Definition
increase or decrease quantity of second messenger molecules (cAMP, DAG, IP3)
Term
After dissociation from Ga, Gby subunits perform the following actions
Definition
increase or decrease quantity of secondary messengers, modulate the function of ion channels
Term
Muscarinic cholinergeic receptors (G-protein receptors) use the following Ga subunit types
Definition
Gaq/11 (M1, 3, 5)
Gai (M2,4)
Gby
Term
adrenergic alpha receptors use the following type of G-protein subunits
Definition
Gaq/11 (alpha 1)
Gai (alpha 2)
Term
Adrenergic beta receptors use the following type of G-protein subunit
Definition
Gas
Term
cAMP performs this action in the cell
Definition
activates protein kinase A (PKA)
Term
DAG performs this function in the cell
Definition
Activates protein kinase C (PKC)
Term
IP3 performs this function in the cell
Definition
activates protein kinase C (PKC)
Term
What is the basic function of presynaptic receptors?
Definition
Negative feedback to limit NT release
Term
What is an autoreceptor?
Definition
a presynaptic receptor that is activated by the same NT that neuron is releasing (self-feedback)
Term
What is a heteroreceptor?
Definition
a presynaptic receptor that is activated by a different NT than that neuron produces (allows "cross-talk")
Term
What type of Ga subunit is present in presynaptic receptors (both cholinergic and adrenergic), and what is its function?
Definition
Gai, decreases cAMP, decreases NT release
Term
What does NANC transmission stand for?
Definition
Non-adrenergic, non-cholingergic transmission (use different NT or NT-like substance)
Term
Where does NANC transmission occur?
Definition
smooth muscle innervated by ANS
Term
What are the primary effects of NANC transmission?
Definition
Inhibition
Term
What type of receptors are present in NANC purinergic neurotransmission?
Definition
adenosine receptors and ATP receptors
Term
This is an endothelium-derived relaxation factor that is a type of NANC transmission
Definition
Nitric oxide
Term
Effect of increased sympathetic tone in the heart?
Definition
increased heart rate, increased conduction velocity, increased contraction, increased automaticity
Term
Type of cholinergic muscarinic receptor present in heart?
Definition
M2
Term
Effect of increased parasympathetic tone in heart?
Definition
decreased heart rate, decreased conduction, decreased contraction
Term
type of adrenergic receptor present in the heart?
Definition
B1
Term
Effect of sypmathetic NS on blood vessels?
Definition
Constriction of some, dilation of others. overall directs flow to skeletal muscle
Term
Effect of parasympathetic NS on blood vessels?
Definition
Doesn't really innervate blood vessels, but does effect endothelial production of NO
Term
Effect of sympathetic NS on lungs? Receptor used?
Definition
bronchodilation. Adrenergic B2
Term
Effect of parasympathetic NS on lungs? Receptor used?
Definition
bronchoconstriction, increased secretion. M3 and M2
Term
Effect of sympathetic NS on GI system.
Definition
decreases activity
Term
Effect of parasympathetic NS on GI activity? receptors used?
Definition
increase activity. M3 and M2
Term
Effect of sympathetic NS on urinary bladder?
Definition
inhibit voiding
Term
effect of parasympathetic NS on urinary bladder? Receptors used?
Definition
Promote voiding. M3
Term
Effect of sympathetic NS on eye? receptors used?
Definition
Enhance vision. (dialate pupil, mydriasis, increase aqueous humor). a1 and B2
Term
Effect of parasympathetic NS on eye? receptors used?
Definition
limit vision (pin-point pupil, miosis, lacrimal gland secretion). M3 and M2
Term
Effect of sympathetic NS on salivary glands?
Definition
decrease secretion
Term
effect of parasympathetic NS on salivary glands? receptors used?
Definition
increase secretion. M3 and M2
Term
Effect of both sympathetic and parasympathetic on autonomic nerve endings?
Definition
decrease release of NT through negative feedback (autoreceptors and heteroreceptors)
Term
true or false: drugs can potentially target any component of autonomic transmission (NT synthesis,transport, release, receptors, breakdown/uptake)
Definition
true
Term
What, in general, do cholinergic agonists do?
Definition
mimic/enhance the effect of the parasympathetic system
Term
What is the effect of a cholinergic agonist on the heart?
Definition
decreased cardiac output (bradycardia, decreased conduction, decreased contractility)
Term
Effect of cholinergic agonists on lungs
Definition
causes bronchoconstriction and increased secretions
Term
Effect of cholinergic agonists on blood vessels?
Definition
increase production of NO by endothelial cells, smooth muscle relaxation and dilation
Term
Effect of cholinergic agonists on the GI
Definition
increased motility, secretions
Term
Effect of cholinergic agonists on the urinary bladder
Definition
promotes urination
Term
Effect of cholinergic agonists on the eye
Definition
miosis, lacrimation, loss of far vision
Term
What is the main muscarinic receptor on the heart?
Definition
M2
Term
What is the main muscarinic receptor on the bladder?
Definition
M3
Term
What is the acronym for the general effects of cholinergic agonists?
Definition
SLUDGE
Term
What does SLUDGE stand for?
Definition
salivation, lacrimation, urination, defecation, GI symptoms, emesis
Term
What is the acronym for EXCESSIVE cholinergic stimulation?
Definition
DUMBELS
Term
What does DUMBELS stand for?
Definition
Diarrhea/diaphoresis, urination, miosis, bronchorrhea/bronchospasm/bradycardia, emesis, lacrimation, salivation
Term
What is an direct acting muscarinic agonist?
Definition
a compound that directly stimulates the muscarinic receptor
Term
What is an indirect acting muscarinic agonist?
Definition
a compound that increases the muscarinic receptor activity by inhibiting acetylcholinesterase
Term
When the term "cholinergic" is used, does it generally refer to muscarinic or nicotinic receptors?
Definition
muscarinic
Term
This is an endogenous cholinergic rarely used clinically.
Definition
ACh
Term
What are the two direct acting cholinergic groups?
Definition
Cholinomimetic alkaloids and synthetic choline esters
Term
What are cholinomimetic alkaloids?
Definition
naturally occurring chemical compounds containing basic nitrogen atoms
Term
Classification and use of Bethanechol
Definition
a choline ester sympathetic agonist that stimulates muscarinic receptors (some M3 selectivity)
basic function: promotes urinary voiding
Term
What is Muscarine
Definition
a cholinomimetic alkaloid that stimulates muscarine receptors. contributes to mushroom poisoning. See general DUMBELS signs
Term
Classification and use of Pilocarpine
Definition
a cholinomimetic alkaloid sympathetic agonist used to induce pupil constriction and decrease intraocular pressure during glaucoma
Term
General function of AChE inhibitors
Definition
are indirect cholingergic agonists. prevent hydrolysis of ACh by acetylcholinesterase and cause accumulation of ACh at sites of release
Term
What, generally, would be affected by AChE inhibitors
Definition
Everywhere that uses the NT ACh. autonomic effector organs and ganglia, skeletal muscle, cholinergic synapses in the CNS
Term
What would be the effect of AChE inhibitors on autonomic ganglia?
Definition
Stimulation, and then depression (via nicotinic receptors)
Term
What would be the effect of AChE inhibitors on the CNS?
Definition
Stimulation, and then depression
Term
What are the three general types of AChE inhibitors?
Definition
Non-covelant inhibitors,
"reversible" covalent inhibitors,
"irreversible" covalent inhibitors
Term
What are two important AChE "reversible" covalent inhibitor drugs?
Definition
physostigmine and neostigmine
Term
Name some clinical uses of "reversible" covalent AChE inhibitors.
Definition
smoothe muscle atony, glaucoma, reversal of neuromuscular blocking agents, myasthenia gravis, counter CNS anticholinergic intoxication (physostigmine)
Term
This is a reversible AChE inhibitor that crosses the blood brain barrier
Definition
physostigmine
Term
What drug would you use to counter CNS symptoms of anticholinergic intoxication?
Definition
physostigmine
Term
This cholinergic agonist is used to empty the urinary bladder
Definition
bethanachol
Term
this cholingergic agonist is used to induce miosis in the eye
Definition
pilocarpine
Term
This is used to reverse NMJ blockade.
Definition
AChE inhibitors
Term
This drug is used to stimulate visceral smooth muscle
Definition
neostigmine
Term
This drug is used to counter anticholinergic toxicity
Definition
physostigmine
Term
What drug category do organophosphates fall under?
Definition
Irreversible covelant AChE inhibitors
Term
Name 3 varieties of irreversible covalent AChE inhibitors
Definition
organophophates, insecticides, and nerve gasses
Term
Poisoning with this class of compounds cause many symptoms attributable to excess muscarinic stimulation
Definition
organophosphates
Term
What do you use to treat organophosphate toxicity?
Definition
cholinesterase "reactivators." (pralidoxime, 2-PAM) or anticholinergics
Term
What receptor type do cholinergic antagonists act at?
Definition
muscarinic receptors (little effect at nicotinic)
Term
True or false: most cholinergic antagonists competitively block stimulation of muscarinic receptors by ACh
Definition
TRUE
Term
Name the two groups of cholinergic antagonists
Definition
natural anticholinergic alkaloids

semi-synthetic and synthetic alkaloid derivatives
Term
Name the two main natural anticholinergic alkaloids
Definition
atropine and scopolamine
Term
Name the 4 most common semisynthetic/synthetic cholinergic antagonists
Definition
tropicamide, ipratropium, glycopyrrolate, propantheline
Term
Effects of cholinergic antagonists on the heart
Definition
increased cardiac output (tachycardia, increased conduction, etc)
Term
Effects of cholinergic antagonists on vasculature
Definition
little effect, no innervation by Parasympathetic
Term
effects of cholinergic antagonists on lungs
Definition
bronchdilation, decreased secretions
Term
effects of cholinergic antagonists on GI
Definition
decreased motility, decreased secretion, (dry mouth)
Term
effects of cholinergic antagonists on urinary bladder
Definition
decreased urination
Term
effects of cholinergic antagonists on the eye
Definition
decreased lacrimation, mydriasis, cycloplegtia
Term
general effects of cholinergic antagonists
Definition
anti-SLUDGE, DUMBELS
Term
True/False: Salivary glands are generally insensitive to cholingergic antagonists
Definition
false, salivary glands are one of the most sensitive organs to anticholinergics
Term
True or false: the effect of anticholinergics depend on the amount of parasympathetic tone present in the first place
Definition
True..the greater the amount of parasympathetic tone the larger an effect a anticholinergic drug will have
Term
Classification and action of atropine
Definition
a cholinergic antagonist (natural alkaloid) that competitively inhibits binding and stimulation of M receptors by ACh. Enters the CNS.
Term
What are the primary concerns with the use of atropine
Definition
tachyarrhythmia, prolonged GI stasis, urine retention
Term
What is atropine used for?
Definition
a adjunct during general anesthesia to decrease salivary and airway secretions. Also to releive symptoms of AChE poisoning
Term
How might atropine cause increased salivation?
Definition
although the action is supposed to decrease salivation, when it somehow ends up in the mouth it will increase it (due to being very bitter).
Term
Classification and action of scopolamine
Definition
cholinergic antagonist (natural alkaloid). Enters CNS. Low dose=slight sedation. High dose=excitement. similar to atropine but usually not the drug of choice
Term
Classification and action of glycopyrrolate
Definition
a synthetic cholinergic antagonist. similar to atropine but is quaternary so few CNS effects. Used as adjunct to general anesthesia (cecreases salivary and airway secretions)
Term
Classification and use of tropicamide
Definition
synthetic cholinergic antagonist. used in the eye to produce mydriasis and cycloplegia. Shorter duration of action than atropine
Term
Classification and use of Ipratropium
Definition
Cholinergic antagonist. Use to decrease bronchoconstriction and airway secretions. Quaternary, restrict distribution by using as an inhalant. Used for animals in chronic respiratory distress.
Term
Classification and use of Propantheline
Definition
Cholinergic antagonist. used to promote urine retention. decreased detrusor contraction and increased trigone and sphincter contraction.
Term
2 cholinergic antagonists used to decrease secretions
Definition
atropine, glycopyrrolate
Term
chlolinergic antagonist used to prevent bradycardia
Definition
glycopyrrolate
Term
cholinergic antagonist used to promote bronchodialation
Definition
ipratropium
Term
cholinergic antagonist used to induce mydriasis and cycloplegia
Definition
tropicamide
Term
Cholinergic antagonist used to promote urine retention
Definition
propantheline
Term
Function of ganglionic blockers
Definition
decrease autonomic regulation of target organs (both sympathetic and parasympathetic)
Term
What is the affect of administering nicotine?
Definition
initial stimulation of nicotinic receptors (increased ANS activity), then inhibition of nicotinic receptors (decreased ANS activity)
Term
How do synthetic competitive ganglionic blockers compare with nicotine?
Definition
they cause inhibition without the initial stimulation. Blocks all ANS activity
Term
Why aren't ganglionic blockers commonly used clinically?
Definition
Since they are decreasing all the the ANS, the effects are widespread and difficult to predict.
Term
What is the basic function of NMJ blocking agents?
Definition
to relax skeletal muscle with no sedative effects.
Term
Why would we use NMJ blockers as an adjunct to normal anesthesia?
Definition
to prevent movement during surgery
Term
How do the nicotinic structures of neuronal synapses and NMJ's differ?
Definition
Neuronal contain only alpha and beta subunits, NMJ contain alpha, beta, delta, and epsilon. this means that they can be targeted via differential pharmacology.
Term
Why are spare receptors problematic when using NMJ blockers?
Definition
must block more receptors than expected, and have lost safety factor of important muscles (diaphragm)
Term
How do competitive NMJ blockers work?
Definition
They block motor end plate depolarization, causing a flaccid paralysis
Term
This is a long-acting competitive NMJ blocker
Definition
Pancuronium
Term
This is an intermediate-length acting competitive NMJ blocker
Definition
atracurium
Term
This is a short acting competitive NMJ blocker
Definition
Mivacurium
Term
This NMJ-blocking drug has a long duration of action, renally eliminated, and blocks muscarinic receptors (tachycardia)
Definition
Pancuronium
Term
This NMJ blocker has an intermediate duration of action, and the half-life is not increased with renal disease. It also promotes histamine release.
Definition
atracurium
Term
What can cause increased half-life of atracurium?
Definition
hypothermia and acidosis (degeneration is temperature and pH dependent)
Term
This NMJ blocker has a short duration of action and is rapidly hydrolysed by plasma enzymes. It also promotes histamine release.
Definition
Mivacurium
Term
What 2 competitive NMJ blockers promote histamine release?
Definition
Atracurium and Mivacurium
Term
What can you do to reverse the effects of competitive NMJ blockers?
Definition
Give AChE inhibitors to increase concentration of ACh to outcompete the antagonist.
Term
How do depolarizing NMJ blockers work?
Definition
Cause prolonged motor end plate depolarization by stimulation of nicotinic receptors. initial fasciculation followed by relaxation
Term
What is the only depolarizing NMJ used clinically?
Definition
succinylcholine
Term
Is succinylcholine pharmacologically reversible?
Definition
No. Although it is 2 ACh molecules linked together, it is resistant to AChE, and is a non-competitive antagonist
Term
Explain what is happening during early (phase 1) depolarizing NMJ blocker use
Definition
the drug causes persistant stimulation of the nicotinic receptors (muscle fasiciculations) until they are incapable of transmitting further impulses
Term
What are the potential side effects of succinylcholine use?
Definition
Histamine release and hyperkalemia (release of K from skeletal muscles)
Term
How do you monitor effectivness of a NMJ blockade?
Definition
Stimulate peripheral nerves (train of four)
Term
Problem with using NMJ blockers during anesthesia
Definition
Normal ways of monitoring patient (reflexes, muscle tone) are lost.
Term
What are the biggest dangers of using NMJ blockers during anesthesia?
Definition
Respiratory paralysis and malignant hyperthermia
Term
These antagonize ACh at NMJ nicotinic receptors
Definition
competitive NMJ blockers
Term
These mimic ACh at the NMJ, are non-reversible, and cause fasiculations followed by flaccid paralysis
Definition
non-competitive depolarizing NMJ blockers (aka succinylcholine)
Term
What are sympathomimetics?
Definition
drugs that mimic the effect of endogenous sympathetic catecholamine neurotransmitters. AKA adrenergic agonists
Term
Name three endogenous catecholamines.
Definition
Epinepherine, norepinepherine, dopamine
Term
What are the pre-junctional actions (a2 receptors) of adrenergic agonists?
Definition
decrease NT release, decrease sympathetic outflow, CNS depression
Term
What set of drugs induce a general catabolic state?
Definition
adrenergic agonists
Term
Direct acting adrenergic antagonists work on what specific part of signal transduction?
Definition
Receptor interaction
Term
What drugs work as direct acting agonists?
Definition
The endogenous catecholamines: dopamine, norepinepherine, epinepherine
Term
name an indirect acting adrenergic agonist.
Definition
amphetamine
Term
Name a mixed acting adrenergic agonist
Definition
phenylpropanolamine
Term
Classification and action of epinepherine.
Definition
a direct acting adrenergic agonist

potent a and b agonist

most important for cardiovascular effects (increase rate, conduction, contraction). Also affects arterial blood flow.
Term
What receptor does epinepherine act on in the heart?
Definition
B1 receptor
Term
What receptor does epinepherine work on in the central arteries? What does it do?
Definition
a1 receptors. stimulate smooth muscle, vasoconstriction.
Term
What receptor does epinepherine work on in arteries supplying skeletal muscle?
Definition
B2 receptor. inhibits smooth muscle, vasodilation
Term
What is the effect of a low dose of epinepherine on blood pressure?
Definition
decreases bp slightly due to B2 dominance
Term
What is the effect of a large dose of epinepherine on blood pressure?
Definition
increases blood pressure due to A1 receptors causing vasoconstriction
Term
Would a large dose of epinepherine increase/decrease flow to the renal artery
Definition
Decrease. stimulation of A1 receptors causes constriction on central arteries
Term
What is the effect of epinepherine on the lungs?
Definition
Strong bronchodialator through B2 receptor
Term
What is the general metabolic effects of epinepherine?
Definition
Increased glucose and free fatty acids
Term
What are the effects of epinepherine on the eye?
Definition
mydriasis (pupil dilation) and relaxation of the ciliary muscle (for distance vision)
Term
Name 4 clinical uses of epinepherine
Definition
relief of hypersensitivity rxns (cardio support and bronchodilation (B1 and B2)), restoring cardiac rhythm, topical hemostatic agent (constrict vessels,a1) adjunct with local anesthetics (limit spread, a1)
Term
Possible side effects of epinepherine?
Definition
cardiac arrhythmias, hypertension, cerebral hemorrhage, restlessness
Term
This is the major NT released by post-ganglionic sympathetic nerves
Definition
norepinepherine
Term
What is the main difference in using epinepherine vs norepinepherine?
Definition
Epinepherine is much more potent on B2 receptors. Norepinepherine will not cause bronchodilation
Term
What is the effect of norepinepherine on blood pressure?
Definition
intense vasoconstriction causes increase in blood pressure (no B2 effect for dialation of peripheral vessels)
Term
Why does the HR tend to slow when using norepinepherine?
Definition
norepinepherine causes such an increase in BP that the vagal reflex is triggered, slowing heart rate.
Term
What is the effect on cardiac output when using norepinepherine?
Definition
Doesn't change much. Have increased BP but decreased rate.
Term
What is the main clinical use of norepinepherine?
Definition
to maintain BP during a cardiovascular crisis (shock)
Term
This adrenergic agonist has a positive inotropic effect
Definition
dopamine
Term
This adrenergic agonist is used in low doses, has a short half-life
Definition
dopamine
Term
What is the effect of low-dose dopamine on kidneys?
Definition
increases blood flow and sodium excretion
Term
This drug is used to treat congestive heart failure with compromised renal function.
Definition
dopamine (low dose only, high dose decreases blood flow to kidneys)
Term
Name a clinically-used, non-selective B adrenergic agonist
Definition
dobutamine
Term
What receptor does dobutamine work best on?
Definition
B1 (explain to me how this is a non-selective agonist????)
Term
What are the most important effects of dobutamine?
Definition
effect on the heart through stimulation of B1 receptors. increased contractility but not heart rate or blood pressure.
Term
What are selective B2 agonists used for clinically?
Definition
bronchodilation
Term
What are the benefits of using a selective B2 agonist as a bronchodilator?
Definition
Fewer cardiovascular effects (no stimulation of B2 receptors)
Term
Are synthetic B2 agonists short acting or long acting?
Definition
Many are resistant to metabolism and have a long duration of action.
Term
What selective B2 adrenergic agonist is most commonly used for bronchospasms?
Definition
Albuterol
Term
What selective B2 adrenergic agonist is most commonly used for recurrent airway obstruction?
Definition
Clenbuterol
Term
What is the problem with long-term administration of B2 adrenergic agonists?
Definition
B receptor down-regulation can occur, leading to loss of efficacy. Can minimize with proper dose and dosing schedule
Term
What is the benefit of B2 adrenergic agonists in livestock?
Definition
partition energy towards muscle mass.
Term
What is the primary effect of an A1 adrenergic agonist?
Definition
vasoconstriction and increased blood pressure
Term
Classification and use of Phenylephrine
Definition
A selective A1 adrenergic agonist. used as a decongestant and vasopressor
Term
What is the main function of selective A2 adrenergic agonists?
Definition
pre-synaptic inhibition of sympathetic neurons and decreased sympathetic outflow from the brain. Causes sedation, analgesia
Term
Classification and use of (Dex)medetomaidine
Definition
a selective A2 adrenergic agonist. Used as an adjunct in sedation/anesthesia. inhibits sympathetic outflow.
Term
What is the main selective adrenergic agonist used for vasoconstriction? (classification and name)
Definition
phenylephrine, a selective A1 adrenergic agonist
Term
What is the main adrenergic agonist used as a sedative?
Definition
(dex)(medetomidine, a selective A2 adrenergic agonist. decreases sympathetic outflow
Term
These 3 adrenergic drugs cause vasoconstriction
Definition
EPI, NE and phenylephrine
Term
This adrenergic drug causes presynaptic inhibition
Definition
medetomidine
Term
These 4 adrenergic drugs increase heart rate and contractile force.
Definition
Epi, NE, dopamine, dobutamine
Term
These three adrenergic drugs cause bronchodilation
Definition
Epi, albuterol, clenbuterol
Term
What is another term for adrenergic antagonists?
Definition
sympatholytics
Term
What is the main pharmaceutical function of adrenergic antagonists?
Definition
block the effect of endogenous sympathetic catecholamine neurotransmitters
Term
What does the effect of sympatholytics depend on?
Definition
the sympathetic tone (high have more effect)
Term
What is the action of a direct-acting competitive adrenergic antagonist?
Definition
reversibly blocks the stimulation of A and B receptors by endogenous NT's
Term
What classification do most adrenergic agonists fall under?
Definition
direct acting competitive antagonists
Term
What is the action of a non-competitive adrenergic antagonist?
Definition
irreversibly blocks A1 and A2 receptors
Term
What is an example of a direct acting non-competitive adrenergic antagonist?
Definition
phenoxybenzamine
Term
What is a direct acting competitive antagonist that reversibly blocks A1 and A2 receptors?
Definition
phentolamine
Term
Clinical use of both phenoxybenzamine and phentolamine?
Definition
both are non-selective A antagonists. used to reduce urethral sphincter tone to manage urethral blockages
Term
Effect of A1 adrenergic antagonists
Definition
block stimulation of arterial smooth muscle. cause fall in blood pressure from decreased total peripheral resistance.
Term
Classification and use of Prazosin
Definition
a selective A1 antagonist. used to relax both arterial and venous smooth muscle. Decrease in total peripheral resistance and venous return. Used in hypertension and congestive heart failure.
Term
Function of selective A2 adrenergic antagonists
Definition
prevent central and pre-synaptic inhibition. increase sympathetic flow.
Term
Classification and use of Atipamezole
Definition
a selective A2 adrenergic antagonist. prevents pre-synaptic and central sympathetic inhibition. used to reverse sedative and analgesic effects of medetomidine (a A2 agonist)
Term
Why is atipamezole an excellent drug to counteract medetomidine?
Definition
There is little chance of a relapse into sedation because the half-life of atipamezole is 2x that of medetomidine
Term
This is a A1 adrenergic antagonist used for vasodilation
Definition
prazosin
Term
This is a A2 adrenergic antagonist used to reverse medetomidine
Definition
atipamezole
Term
This is a non-selective competitive A adrenergic angatonist (reversible)
Definition
phentolamine
Term
This is a non-selective non-competitive A adrenergic antagonist (irreversible)
Definition
phenoxybenzamine
Term
Effect of using a B1 adrenergic antagonist
Definition
block sympathetic innervation of the heart. Decreased heart rate and contractility
Term
True or false: B1 adrenergic antagonists decrease blood pressure.
Definition
True. Because they decrease cardiac output and BP=CO x PR, BP is decreased
Term
What dangerous side effect can excessive sympathetic innervation cause regarding the heart?
Definition
cardiac arrhythmias. Use a B1 adrenergic antagonist to decrease innervation.
Term
What is the primary effect of B2 adrenergic antagonists?
Definition
cause bronchoconstriction. (blocking sympathetic input to bronchiolar SM)
Term
What is the major clinical limitation of non-selective B antagonists?
Definition
Will effect the heart (usual goal) but will also cause bronchoconstiction
Term
This is a prototypical B antagonist with equal affinity for both B1 and B2 receptors
Definition
Propranolol
Term
Classification and use of Propranolol
Definition
a non-selective B adrenergic antagonist that is used for a antiarrhythmia. limited use because of effect on lungs (bronchoconstriction)
Term
A nonselective B adrenergic antagonist used for glaucoma
Definition
timolol
Term
Classification and use of timolol
Definition
A non-selective B adrenergic antagonist used to decrease aqueous humor production during glaucoma (ocular application)
Term
Why is it safer to use a selective B1 antagonist than a non-selective B antagonist?
Definition
Can effect B1 receptors in heart without affecting SM in lungs
Term
This selective B1 antagonist is used to decrease heart rate and counteract anticholinergic tachycardia
Definition
Atenolol
Term
Classification and use of atenolol
Definition
a selective B1 adrenergic antagonist used to decrease heart rate and counteract anticholinertgic tachycardia
Term
Name this drug. Adrenergic agonist, endogenous, stimulates A1, B1, B2
Definition
epinepherine
Term
Name this drug: Adrenergic agonist, endogenous, stimulates A1 and B1
Definition
norpinephrine
Term
name this drug: Adrenergic agonist, endogenous, stimulates D1 and B1 (little bit of A1)
Definition
dopamine
Term
Name this drug: a adrenergic agonist, selective for B1
Definition
dobutamine
Term
Name these 2 drugs: adrenergic agonists selective for B2
Definition
albuterol and clenbuterol
Term
Name this drug: an adrenergic agonist selective for A1
Definition
phenylephrine
Term
Name this drug: a adrenergic agonist selective for A2
Definition
medetomidine
Term
Name this drug: a adrenergic antagonist, non-competitive, blocks A1 and A2
Definition
phenoxybenzamine
Term
Name this drug: a adrenergic antagonist, competitive, blocks A1 and A2
Definition
phentolamine
Term
Name this drug: a adrenergic antagonist specific for A1
Definition
prazosin
Term
name this drug: a adrenergic antagonist specific for A2
Definition
atipamezole
Term
Name this drug: a adrenergic antagonist, non-selective B, systemic use
Definition
propranolol
Term
Name this drug: adrenergic antagonist, non-selective B, ocular use
Definition
timolol
Term
Name this drug: adrenergic antagonist, selective for B1
Definition
atenolol
Term
In case of shock, which branch of the ANS needs to be stimulated?
Definition
Symptathetic. Increase cardiac output, increase peripheral resistance, increase blood pressure.
Term
Why might Ne be preferred over EPI in shock associated with vasodilation?
Definition
NE can achieve a greater BP increase than Epi....and something about arrhymmias.....not sure.
Term
Primary therapy for anaphylactic shock?
Definition
epinephrine
Term
Elevated intraocular pressure in the absence of signs of concurrent ocular disease
Definition
primary glaucoma
Term
eleveated intraocular pressure associated with concurrent ocular disease
Definition
secondary glaucoma
Term
What breed tends to have open angle glaucoma?
Definition
beagles
Term
usual cause of primary glaucoma
Definition
narrow angle results in obstruction of aqueous outflow
Term
These 2 drugs are often used in combination to treat emergency glaucoma
Definition
timolol (beta antagonist, decrease aqueous humor production) and pilocarpine (cholinergic agonist, miotic agent than can open closed angle)
Term
The heart works ........ and in a ........manner
Definition
sequentially, synchronized
Term
The spread of electrical excitation in the heart is both ...... and ......
Definition
rapid and organized.
Term
Where does cardiac electrical activity originate?
Definition
in the SA node (sinoatrial)
Term
Describe the spread of electrial excitation through the heart
Definition
starts in the SA node, spreads rapidly through atria, moves slowly through AV node, spreads rapidly through ventricles via the His-Purkinje system
Term
How does electrical current spread from one cardiac cell to another?
Definition
via gap junctions
Term
Why do the action potential waveforms in the ventricles and the SA node appear different?
Definition
different populations of ion channels
Term
What is the resting trans-membrane electrical gradient of a cardiac cell?
Definition
-90mV
Term
What are the three major ions associated with cardiac cell electrical activity?
Definition
Sodium, Potassium, Calcium
Term
What is the point to which an ion will drive the cell membrane potential if it is allowed to move freely in or out of the cell?
Definition
reversal potential (the point at which that ion is in equilibrium across the membrane)
Term
The reversal potential of which ion determines resting membrane potential?
Definition
Potassium (only ion channels that are open at this point)
Term
The resting membrane potential of sodium is +50 mV. Why is this important?
Definition
Sodium will attempt to drive the membrane potential up to +50 mV when it can move freely into the cell
Term
How are sodium channels in cardiac cells activated?
Definition
by depolarization
Term
What are the 3 functional states of ion channels?
Definition
closed, open, and inactivated
Term
What is the threshold for activation of voltage gated sodium channels?
Definition
-60 mV (resting potential is -90 mV)
Term
True or false: the entire cell must reach -60 mV to activate threshold
Definition
False: a change along the membrane is sufficient
Term
Explain phase 0 of the ventricular action potential.
Definition
Depolarization. Na+ channels open and sodium floods into the cell.
Term
Explain phase 2 of the ventricular action potential
Definition
Ca++ enters the cell. initiation of contraction. K+ begins to exit the cell.
Term
Explain phase 3 of the ventricular action potential
Definition
K+ still exiting the cell. repolarization.
Term
In comparison to sodium channels, are calcium channels slower or faster?
Definition
Much slower. They open and inactivate more slowly than sodium channels. allow for substantial calcium influx to trigger and sustain contraction.
Term
Why doesn't the inward movement of calcium in phase 2 cause an rise in a cell's positive charge?
Definition
Because K+ is moving out of the cell at the same time, keeping it relatively balanced.
Term
Which node is usually the pacemaker?
Definition
the SA node
Term
What outside forces cause depolarization of the SA node?
Definition
trick question---spontaneous depolarization
Term
What ions are important in SA node action potentials?
Definition
Calcium and potassium (no sodium channels)
Term
Why don't SA node cells need a phase 2 (plateau)??
Definition
They are not contracting.
Term
What ion is important for depolarization of pacemaker cells?
Definition
calcium
Term
What channels do pacemaker cells use to depolarize?
Definition
slow opening voltage gated calcium channels (threshold=-40 mV)
Term
What does phase 3 consist of in SA nodal cells?
Definition
repolarization through K+ channels (same as ventricular)
Term
What is phase 4 of pacemaker action potential?
Definition
a continuous slow depolarization (funny current)
Term
How is the "funny" current activated in pacemaker cells?
Definition
by hyperpolarization (such as in phase 0 of action potential). slowly depolarize towards threshold.
Term
Influx of what ion trigger contraction in cardiac muscle cells?
Definition
calcium
Term
How does the influx of calcium induce contraction in cardiac cells?
Definition
calcium-induced calcium release.
Term
What are 2 ways calcium is removed from the cytoplasm to stop cardiac contraction?
Definition
pumped back into the SR by Ca++ ATPase

shunted out of cell by Na+/Ca++ exchanger
Term
What ion triggers contraction of cardiac muscle?
Definition
Calcium
Term
What is an electrocardiograph?
Definition
electrical activity of the heart recorded through the skin
Term
What does the P wave in an electrocardiograph signify?
Definition
atrial depolarization
Term
What does the QRS complex in an electrocardiograph signify?
Definition
ventricular depolarization
Term
What does the QRS complex in an electrocardiograph signify?
Definition
ventricular depolarization
Term
What does the T wave signify in an electrocardiograph?
Definition
ventricular repolarization
Term
What is an arrythmia?
Definition
a problem with the electrial activity of the heart. Can result from disorders of impulse formation, conduction, or both.
Term
A change in the normal pace maker or the developement of a new ectopic pacemaker would be a disorder of......
Definition
impulse formation
Term
True or false: a ectopic pacemaker is always in the ventricles.
Definition
False, it can form anywhere in the heart.
Term
Why is the SA node typically the pacemaker?
Definition
it has the highest depolarization frequency
Term
Name two situations in which a new pacemaker might become dominant.
Definition
The firing of the SA node slows abnormally, or there is an abnormal acceleration of the ectopic pacemaker.
Term
True or false: ectopic pacemaker activity will usually cause abnormal depolarization.
Definition
true
Term
Give an example of how disorders of impulse conduction can cause bradycardia.
Definition
AV nodal block, conduction not getting through normally to ventricles, slows ventricular contraction rate.
Term
Give an example of how a disorder of impulse conduction can cause tachycardia
Definition
A reenterent circuit can be self-perpetuating and become a pacemaker, cause abnormal impulse conduction and contraction.
Term
What are the realistic goals of antiarrhythmic drugs?
Definition
to minimize cardiac pump dysfunction and prevent less serious arrhythmias from becoming more serious
Term
What is the problem with all anti-arrhythmic drugs?
Definition
they can all induce arrthymias.
Term
under traditional classification of antiarrhythmic drugs, what is the function of Class 1?
Definition
sodium channel blockers.
Term
Class 1 antiarrhythmic drugs
(sodium channel blockers) have 3 sub categories. What are they? (name and function)
Definition
Class 1A:moderate conduction slowing, prolongs refractory period
Class 1B: little conduction slowing, shortens refractory period
Class 1C: profound conduction slowing, little change in refractory period
Term
do sodium channel blockers have any effect on the SA node?
Definition
no, the SA node has no sodium channels
Term
What is the effective refractory period?
Definition
The time before a cell can fire a subsequent action potential (is related to action potential duration)
Term
Name a Class 1A antiarrhythmic drug
Definition
procainamide
Term
What is the effect of procainamide on heart cells?
Definition
A class 1A antiarrhythmic, procainamide slows conduction velocity and prolongs the refractory period.
Term
What situation would procainamide be useful in relieving?
Definition
reentrant supraventricular tachycardia....slows conduction velocity and breaks the cycle.
Term
Explain how the class 1B drug lidocaine will effect cardiac cells
Definition
lidocaine binds to inactivated sodium channels (including "late" sodium channels, which shortens the refractory period) and keeps them in the in activated state. With fewer active sodium channels, automaticity decreases, and eccentric pacemakers can be slowed down.
Term
What type of cells does lidocaine tend to affect?
Definition
damaged depolarized cardiac cells (why good for treating ectopic pacemaker
Term
Name a Class 1C antiarrhymatic
Definition
flecainide
Term
What is the clinical use of flecainide
Definition
for use in emergency situations to decrease conduction velocity (ventricular fibrillation)
Term
In the traditional classification of antiarrhythmic drugs, what do Class II drugs do?
Definition
they are Beta Blockers
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