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191 Cards in this Set

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  • Back
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What is the major neurotransmitter of the parasympathetic autonomic nervous system
Acetylcholine
Where are four places where nicotinic receptors are located
Postsynaptic neurons in ganglia of both the parasympathetic nervous systems and sympathetic nervous systems
Neuromuscular junction
Central nervous system
Adrenal medulla
Where are three places where muscarinic receptors are located
Organs innervated by the PNS
Thermoregulatory sweat glands innervated by the SNS
CNS (cortex, hippocampus)
What drug inhibits transport of choline from the extracellular fluid into the cytoplasm of a cholinergic neuron
Hemicholinium
What enzyme catalyzes the reaction between choline and acetyl CoA to form Ach
Choline acetyltransferase (CAT)
The neuronal release of Ach into the synapse is inhibited by what toxin
Botulinum toxin
What organism produces botulinum toxin
Clostridium botulinum (anaerobic, spore-forming, gram positive rod)
The venom of what spider results in the release of stored Ach into the synapse
Black widow
What enzyme degrades Ach
Acetylcholinesterase (AchE)
What are the breakdown products of Ach
Choline and acetate
Where is AchE located
Synaptic cleft
What is muscarine
Alkaloid compound found in various poisonous mushrooms
Where is the M1 muscarinic receptor found in the body
Neurons
Gastric parietal cells
None
Where is the M2 muscarinic receptor found in the body
Neurons
Cardiac cells
Smooth muscle
None
Where is the M3 muscarinic receptor found in the body (7)
Neurons
Smooth muscle
Exocrine glands
Lungs
GI tract
Eye
Bladder
None
Where is the M4 muscarinic receptor found in the body
Neurons
Where is the M5 muscarinic receptor found in the body
Neurons
Name the type of G protein that M1 is coupled to
Gq coupled
Name the type of G protein that M2 is coupled to
Gi coupled
Name the type of G protein that M3 is coupled to
Gq coupled
Does the PNS innervate the vasculature
No (however there are muscarinic receptors located on the vasculature)
How can Ach lower blood pressure
Ach binds to Ach receptors in the vasculature leading to increased synthesis of NO via second messenger pathways
NO is also known as what
Endothelial-derived relaxation factor (EDRF)
What amino acid is a precursor to NO synthesis
Arginine
None
Does AchE have a high affinity for Ach
Yes
Does Ach increase or decrease blood pressure
Decreases
Does Ach increase or decrease heart rate
Decreases
Does Ach increase or decrease salivation
Increases
Dose Ach increase or decrease lacrimation
Increases
Does Ach increase or decrease sweating
Increases
Does Ach increase or decrease GI secretions
Increases
Does Ach increase or decrease GI motility
Increases
Does Ach increase or decrease Miosis (constriction of pupil)
Increases
Does Ach increase or decrease bladder detrusor muscle tone
Increase (this lead to increased urination)
Does Ach increase or decrease Bronchodilation
Decrease
What does Ach do to the ciliary muscle of the eye
Increased contraction which leads to increased accommodation
How does Ach cause miosis
Increased contraction of the circular muscle in the iris
Does bethanechol have muscarinic activity
Yes (agonist)
Does AchE have a high affinity for bethanecol
No (zero affinity)
Does bethanechol have nicotinic activity
No
What is bethanechol used for
Neurogenic bladder (nonobstructive urinary retention)
Does carbachol have muscarinic activity
Yes (agonist)
Does carbachol have nicotinic activity
Yes (agonist)
Does AchE have a high affinity for carbachol
No (zero affinity)
What is carbachol used for
Miotic agent to reduce intraocular pressure (IOP)
Does pilocarpine have muscarinic activity
Yes (agonist)
Does pilocarpine have nicotinic activity
No
Does AchE have a high affinity for pilocarpine
No (zero affinity)
What is pilocarpine used for
Mitotic drug of choice to lower IOP in emergency settings of narrow-angle and open-angle glaucoma
Can pilocarpine cross the blood-brain barrier (BBB)
Yes (tertiary amine)
Give examples of reversible AchE inhibitors
Neostigmine
Pyridostigmine
Physostigmine
Edrophonium
Rivastigmine, Donepezil, Galantamine, Tacrine
None
What are donepezil, galantamine, rivastigmine, and tacrine used for
Alzheimer’s disease
What two AchE inhibitors are quaternary ammonium compounds and therefore cannot cross the BBB
Neostigmine
Pyridostigmine
None
What short-acting AchE inhibitor is used to diagnose myasthenia gravis and is also used to differentiate myasthenic from cholinergic crisis
Edrophonium
Which reversible AchE inhibitor is used as an antidote in atropine overdose
Physostigmine (tertiary amine therefore crosses BBB to enter CNS)
Give examples of irreversible AchE inhibitors
Sarin
Malathion
Parathion
Echothiphate
Isoflurophate
None
Which irreversible AchE inhibitor is used as nerve gas
Sarin
Which two AchE inhibitors are used as insecticides
Malathion
Parathion
None
What is another name for the irreversible AchE inhibitors
Organophosphates
How do organophosphates irreversibly inhibit AchE
Phosphate group covalently binds to serine hydroxyl group in the active site of AchE thereby rendering the enzyme permanently inactive
What is used to counteract the muscarinic and CNS effects during organophosphate poisoning
Atropine (protects muscarinic receptors, via competitive inhibition, from the increased levels of Ach thereby preventing overstimulation)
What agent is used to reactivate inhibited AchE during organophosphate poisoning
Pralidoxime (2-PAM)
True or False? The effectiveness of 2-PAM in counteracting organophosphate poisoning is not time dependent
False, 2-PAM must be given before the “aging” process of the organophosphate-AchE complex is complete
What are the signs and symptoms of organophosphate poisoning
Miosis
Diarrhea
Urination
Bradycardia
Sweating
Lacrimation
Salivation
Bronchoconstriction
Peripheral nerve demyelination
None
Does atropine block nicotinic receptors, muscarinic receptors, or both
Muscarinic receptors
What are the pharmacologic actions of atropine
Mydriasis
Cycloplegia
Tachycardia
Sedation
Urinary retention
Constipation
Dry mouth
Dry eyes
Decreased sweating
Hallucination
Sedation
Hyperthermia
Delirium
Blurred vision
Coma (high doses)
None
What class of drugs can be used to counteract atropine overdose
AchE inhibitors
Name three drug classes, other than atropine, that may cause antimuscarinic adverse effects
Sedating/ first generation antihistamines (diphenhydramine)
Tricyclic antidepressants (TCAs)
Phenothizines
None
Low dose (<0.5 to 1 mg) atropine does what to heart rate
Decreases heart rate (unknown paradoxical vagalmimetic effect)
High dose(>0.5 to 1 mg) atropine does what to heart rate
Increases heart rate (parasympatholytic effect)
What is the half life of atropine
4 hours
Name four belladonna alkaloids
Belladonna
Atropine
Scopolamine
Hyoscyamine
None
What is belladonna
Perennial atropine-based plant; also known as “nightshade”
How does scopolamine differ from atropine (3)
Longer duration of action
More potent CNS effects
Able to block short-term memory
None
What is the main therapeutic indication of scopolamine
Motion sickness
Giving drugs with anticholinergic activity can precipitate an emergent situation in what type of patients
Patients with narrow-angle glaucoma
What are the signs and symptoms of acute angle closure glaucoma
General distress
Pain
Headache
Red eye
Photophobia
Increased IOP
Visual changes
Malaise
Nausea
Vomiting
None
What two anticholinergic agents are quaternary ammonium compounds used for the treatment of asthma and COPD
Ipratropium
Tiotropium
None
How often is tiotropium dosed
Once daily (longer half-life vs. ipratropium)
Does ipratropium affect airway secretions
No (unlike atropine)
None
Name three ganglionic blocking agents
Hexamethonium
Mecamylamine
Trimethaphan
None
What are ganglionic blocking agents primarily used for
Lowering blood pressure
Blocking autonomic nervous system reflexes
None
Will trimethaphan block a reflex bradycardia after a vasoconstricting agent is given
Yes
Will trimethaphan block a directly induced bradycardia by a muscarinic agonist
No
Neuromuscular blocking agents can be grouped into what two general categories
Depolarizing and nondepolarizing
Do neuromuscular blockers (NMBs) work at muscarinic or nicotinic receptors
Nicotinic (NMJ has nicotinic receptors)
How many subunits is the nicotinic receptor made of
Five
Which subunit of the nicotinic receptor does Ach bind to
Alpha subunit (nicotinic receptors have two alpha subunits)
Binding of Ach to the nicotinic receptor at the NMJ is required to open which type of ion channel
Sodium channel
What is the most commonly used NMB
Succinylcholine (depolarizing NMB)
How does succinylcholine work at the NMJ
Behaves as a cholinergic agonist that remains bound to the Ach receptor for a prolonged period
What happens during phase I of succinylcholine activity at the NMJ
Receptors become depolarized and transient fasciculations are observed
None
What happens during phase II of succinylcholine activity at the NMJ
Receptor becomes resistant to depolarization and a flaccid paralysis ensues
What are the main uses of succinylcholine
Endotracheal intubation
Adjunct during electroconvulsive shock therapy
None
Is succinylcholine short or long acting
Short acting (duration 4-8 minutes) because of rapid hydrolysis by cholinesterase
Where is the enzyme (cholinesterase) that metabolizes succinylcholine found
Plasma
What are the adverse effects of succinylcholine
Malignant hyperthermia
Apnea
Hypertension
Hyperkalemia
None
What are the signs and symptoms of malignant hyperthermia
Sudden onset of hyperthermia
Tachycardia
Tachypnea
Sweating
Cyanosis
Muscle rigidity
None
How is malignant hyperthermia treated
Rapid cooling of patient
Dantrolene
None
What is the mechanism of action of dantrolene
Inhibits calcium release from the sarcoplasmic reticulum of muscle cells thereby relaxing muscle tone and reducing heat production
Succinylcholine may have a prolonged half-life in what type of patients
Patients with a genetic deficiency or altered form of plasma cholinesterase
What is the mechanism of action of nondepolarizing NMBs
Competitive antagonists of Ach at the NMJ
Which drug is the prototype of the nondepolarizing NMBs
Tubocurarine
What antidote is used in tubocurarine overdose
AchE inhibitor (increases Ach concentration which competes with tubocurarine at the NMJ)
List in order, from first to last, the muscles that are paralyzed by nondepolarizing NMBs
Small muscles of the face and eye; fingers; limbs, neck, trunk; intercostals; diaphragm
Which antimicrobial class of drugs may act in synergy with nondepolarizing NMBs by inhibiting release of Ach from nerve endings by competing with calcium ions, thereby increasing neuromuscular blockade
Aminoglycosides (most likely to occur with high doses; patients with hypocalcemia, hypomagnesemia, or neuromuscular disorders)
None
Give examples of nondepolarizing NMBs
Tubocurarine
Atracurium
Rocuronium
Mivacurium, Vecuronium, Pancuronium, Pipercuronium
None
What is the only nondepolarizing NMB that does not require dosage reduction in patients with renal failure
Atracurium
What nondepolarizing NMB has the most rapid onset of action
Rocuronium
In what situations are nondepolarizing NMBs used
Adjunct to general anesthesia to facilitate endotracheal intubation and to relax skeletal muscles during surgery
Facilitate mechanical ventilation in ICU patients
None
What are the two major neurotransmitters of the SNS
Epinephrine; norepinephrine
What amino acid is the precursor to dopamine, norepinephrine, and epinephrine
Tyrosine
None
What are the steps, in order, to the synthesis of epinephrine starting from tyrosine
Tyrosine converted into DOPA by tyrosine hydroxylase (rate limiting step);
DOPA is converted into dopamine by DOPA decarboxylase;
Dopamine is converted into norepinephrine by dopamine β-hydroxylase;
Norepinephrine is converted into epinephrine by methylation in the adrenal medulla
None
What is the mechanism of action of fuanethidine and bretylium
Inhibits the release of norepinephrine into the synapse
What two enzymes metabolize norepinephrine
Monoamine oxidase (MAO); catechol-O-methyltransferase (COMT)
What is the mechanism of action of reserpine
Inhibits the transport of norepinephrine from the neuronal cytoplasm into the synaptic vesicles
What are the common side effects of reserpine
Depression
Sedation
None
What breakdown products of norepinephrine are excreted in the urine and can be measured to help diagnose pheochromocytoma
Vanillylmandelic acid (VMA)
Metanephrine
Normetanephrine
None
How does cocaine increase norepinephrine levels in the synaptic cleft
Inhibits reuptake of neurotransmitter back into the presynaptic neuron
What are the two major classes of adrenergic receptors
α-receptors; β-receptors
None
What drug can inhibit tyrosine hydroxylase
Methyl-p-tyrosine; feedback inhibition by norepinephrine
What neurotransmitters are metabolized by MAO type A
Norepinephrine
Serotonin
Tyramine
None
What neurotransmitters does MAO type B metabolize
Dopamine
How do amphetamine, ephedrine, and tyramine increase norepinephrine levels
Act as indirect sympathomimetic agents by displacing norepinephrine from the mobile storage pool (drug enters presynaptic nerve terminal and displaces stored norepinephrine)
None
Where are α2-receptors found
Presynaptic neurons
Pancreatic β cells
None
What happens when α2-receptors are activated
Inhibits the release of norepinephrine from synaptic vesicles
None
Give examples of α2-receptor agonists
Clonidine
Dexmedetomidine
α-methyldopa; guanabenz; guanfacine;
None
What are the therapeutic indications (7) of clonidine
Hypertension
Severe pain
Heroin withdrawal
Nicotine withdrawal
Ethanol dependence
Clozapine-induced sialorrhea
Prevention of migraines
None
What is dexmedetomidine used for
Sedation of intubated and mechanically ventilated patients
With drugs that activate both α and β-receptors, which receptors are generally activated first (which receptors are more sensitive)
β-receptors
None
Activation of what receptor type in the eye will lead to contraction of the radial muscle and subsequently lead to mydriasis
α1-receptor
None
Name the G-protein associated with α1 receptors
Gq
None
Name the G-protein associated with α2 receptors
Gi
None
Name the G-protein associated with β1, β2, and D1 receptors
Gs
None
Name the major effects mediated by α1 receptors (7)
Mydriasis
Vasoconstriction
Increased blood pressure
Increased glycogenolysis
Decreased renin release
Decreased urination
Ejaculation
None
Name the major effects mediated by α2 receptors (3)
Inhibition of norepinephrine release
Inhibition of insulin release
Platelet aggregation
None
Name the major effects mediated by β1 receptors (4)
Increased heart rate
Increased conduction velocity
Increased force of heart contraction
Increased renin release
None
Name the major effects mediated by β2 receptors (5)
Vasodilation
Bronchodilation
Increased insulin secretion
Increased glycogenolysis
Relaxation of uterine smooth muscle
None
Name the major effects mediated by peripheral D1 receptors (4)
Vasodilation of coronary, renal, and mesenteric vasculature
Increased GFR
Increased renal blood flow
Increased sodium excretion
None
α2-receptor activation in the pancreas will cause insulin secretion to increase or decrease
Decrease
β2-receptor activation in the pancreas will cause insulin secretion to increase or decrease
Increase
None
Which receptor type does epinephrine preferentially bind to at low doses
β-receptors (vasodilation in vasculature)
None
Which receptor type does epinephrine preferentially bind to at high doses
α-receptors (vasoconstriction in vasculature)
None
What is the drug of choice in patients with type 1 hypersensitivity reactions
Epinephrine
Why is epinephrine often given in combination with local anesthetics
Epinephrine causes a vasoconstriction thereby inhibiting the local anesthetics redistribution away from its site of action (increases the duration of local anesthesis)
None
What is the concentration of epinephrine when given in combination with local anesthetics
1:100,000
State whether peripheral vascular resistance increases or decreases with low dose epinephrine
Decreases
State whether systolic blood pressure increases or decreases with low dose epinephrine
Increases
State whether diastolic blood pressure increases or decreases with low dose epinephrine
Decreases
State whether pulse pressure increases or decreases with low dose epinephrine
Increases
What receptors are activated by isoproterenol
β1=β2
None
What receptors are activated by dopamine
D>β>α
None
What receptors are activated by dobutamine
β1>β2
None
What receptors are activated by phenylephrine
α1>α2
None
What receptors are activated by methoxamine
α1>α2
None
Does norepinephrine activate β2 receptors
No
None
Activation of dopamine receptors will cause what type of response in the mesenteric and renal vasculature
Vasodilation
What is dopamine metabolized to
Homovanillic acid (HVA)
What is dobutamine used for
Increases cardiac output in congestive heart failure without affecting RBF (unlike dopamine)
Tyramine is a breakdown product of which amino acid
Tyrosine
Where is tyramine found
Cheeses (aged)
Alcoholic beverages
Fish
Chocolates
Red wines
Processed meats (fermented, aged, and pickled foods)
None
What enzyme is responsible for the breakdown of tyramine
MAO type A
What can potentially happen if a patient on a MAOI consumes large amounts of fermented cheese
Hypertensive crisis
What are phenylephrine and pseudoephedrine used to treat
Nasal congestion
None
What are mixed action adrenergic agonists
Substances that release stored norepinephrine from nerve terminals
Directly stimulate α and β receptors
None
What are some examples of mixed action adrenergic agonists
Ephedrine
Metaraminol
None
Which drug is a nonselective, competitive antagonist at both α1 and α2 receptors
Phentolamine
None
Which drug is a nonselective, irreversible antagonist at both α1 and α2 receptors
Phenoxybenzamine
None
What are phentolamine and phenoxybenzamine mainly used for
Pheochromocytoma
None
What is the mechanism of action of prazosin
Selective α1 antagonist
None
What are prazosin, terazosin, and doxazosin used to treat
Benign prostatic hypertrophy
Hypertension
None
What is alfuzosin used to treat
BPH
This drug is a selective α1A receptor antagonist, used in the treatment of BPH, and has less cardiovascular side effects vs. traditional α1 antagonists
Tamsulosin
None
What advantage do selective α1 antagonists have over nonselective α antagonists
Less reflex tachycardia
None
What CNS prejunctional α2 receptor antagonist is used to treat postural hypotension and impotence
Yohimbine
None
What CNS prejunctional α2 receptor antagonist is used to treat depression
Mirtazapine
None
Give examples (6) of β1 selective antagonists
Acebutolol
Atenolol
Bisoprolol
Betaxolol
Exmolol
Metoprolol
None
Give examples (4) of nonselective β antagonists
Propranolol (angina pectoris)
Pindolol (ISA)
Sotalol (anti-arrythmic)
Timolol
Nadolol
None
Give two examples of mixed α2/β antagonists
Carvedilol
Labetalol
None
What is the name of a β antagonist that also blocks potassium channels and is used as an antiarrhythmic
Sotalol
None
Which two β antagonists have intrinsic sympathomimetic activity (ISA)
Acebutolol
Pindolol
None
What is ISA
Drugs act as partial agonists and only work when there is increased sympathetic drive such as with exercise
This results in less bradycardia and less effects on lipid metabolism
None
What happens to exercise tolerance in patients being treated with β-blockers
Decreased exercise tolerance
None
What are the main therapeutic indications (6) of β-blockers
Angina
Arrhythmias
Hypertension
CHF (not all β-blockers)
Thyrotoxicosis
Glaucoma (ophthalmic formulations)
None
What are some noncardiovascular uses of propranolol
Migraine prophylaxis
Performance anxiety (stage fright)
None
β-blockers can inhibit the majority of effects caused by thyrotoxicosis except for what sign
Diaphoresis
None
β-blockers can inhibit the majority of effects caused by hypoglycemia except for what sign
Diaphoresis
None
What does propranolol do to serum triglycerides
Increases serum triglycerides
What does propranolol do to serum LDL
Increases serum LDL
Why does propranolol cause vivid dreams
Crosses the BBB
Why should β-blockers be tapered down instead of abruptly discontinued
Chronic therapy leads to upregulation of β-receptors; therefore, abrupt discontinuation may lead to life-threatening cardiovascular rebound effects (tachycardia; hypertension; arrhythmias; death)
None