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W09 Pharmacology 2
Exam 2
263
Other
Professional
02/03/2009

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Term
CNS
Definition
The __NS consists of the brain and spinal cord and is the center of integration and control.
Term
PNS, 31 spinal, 12 cranial
Definition
The __NS is outside the brain and spinal cord and consists of __ spinal nerves and __ cranial nerves.
Term
PNS --> sensory and motor divisions
Definition
The PNS is divided into ___ and ___ divisions. It functions to recognize changes to the environment and moves muscles or secretes chemicals.
Term
Sensory --> afferent (arrive at the brain)
Definition
The Sensory division is also called the ___ division. It conducts impulses from receptors to the CNS and informs the CNS of the body interior/exterior and contains sensory nerve fibers.
Term
somatic = skin, muscles, joints; visceral = organs
Definition
Sensory nerve fibers can be ___ from skin, skeletal muscles or joints or ___ from organs w/in the ventral body cavity.
Term
efferent division (exits brain)
Definition
The motor division of the PNS is also called the ___ division. It conducts impulses from the CNS to effectors (muscles/glands) and contain motor nerve fibers.
Term
Somatic nervous system, division of PNS
Definition
___ nervous system is voluntary and conducts impulses from the CNS to skeletal muscles. It provides voluntary control over skeletal muscles.
Term
Autonomic nervous system, division of PNS
Definition
___ nervous system is involuntary and conducts impulses from the CNS to smooth muscle, cardiac muscle and glands. It regulates nerves to heart, digestive tract, reproductive tracts, salivary glands and some parts of the eye.
Term
sympathetic, parasympathetic
Definition
Autonomic nervous system can be divided into ___ (fight or flight) and ___ (rest and digest) nervous systems.
Term
Neurons
Definition
___ are the functional and structural unit of the nervous system. They are specialized to conduct information from one part of the body to the other.
Term
soma = cell body, dendrites = input, axon = conducting, axon terminal = output
Definition
___ is a neuron cell body. ___ is the input region and the __ is the conducting component. The __ ___ is the secretory/output region.
Term
Acetylcholine, norepinephrine, epinephrine and dopamine
Definition
Name the four neurotransmitters.
Term
acetylcholine
Definition
___ is released from cholinergic fibers.
Term
ACh
Definition
___ is the primary transmitter in all preganglionic efferent autonomic fibers and somatic motor fibers to skeletal muscle, all parasympathetic postganglionic and a few sympathetic postganglionic fibers.
Term
norepinephrine
Definition
___ is released from adrenergic fibers. It is the primary transmitter in most postganglionic sympathetic fibers.
Term
dopamine, epinephrine
Definition
___ is released by some peripheral sympathetic fibers. ___ is released from adrenal medullary cells along with NE.
Term
Cholinergic = nicotinic or muscarinic, adrenergic = alpha or beta
Definition
Cholinergic receptors can be either ___ or ___. Adrenergic receptors can be either ___ (1 and 2) or ___ (1 and 2).
Term
Somatic = motor
Definition
Somatic nervous system innervates/controls the (sensory/motor) function of the body.
Term
autonomic nervous system
Definition
The ___ nervous system is regulated by the brain stem and has two parts - parasympathetic and sympathetic.
Term
Parasympathetic: decrease HR, increase gastric emptying, bladder/bowel emptying, focusing eye, pupil constriction, bronchial smooth muscle constriction
Definition
Parasympathetic division of the autonomic nervous system results in the following: ___ in HR, ___ gastric secretion, emptying of bladder and bowel, focusing of eye for near vision, pupil (constriction/dilation) and bronchial smooth muscle (constriction/dilation).
Term
increase HR/CO/rate-force of contraction, vasoconstriction, blood flow to skin, sweat glands and making your hair stand up on end
Definition
Sympathetic division of the autonomic nervous system's main functions include: (increase/decrease) HR, CO, force/rate of contraction; vaso(dilation/constriction); blood flow to skin, sweat glands and piloerection.
Term
sympathetic (fight or flight)
Definition
___ division of the autonomic nervous system's main functions are increased HR and BP, shunt blood to skeletal muscle, bronchodilation, pupil dilation, mobilize stored energy
Term
Albuterol/ventalin = bronchodilation; epinephrine = vasoconstriction
Definition
Albuterol and ventalin (dilate/constrict) bronchi. Epinephrine (dilates/constricts) blood vessels.
Term
True!
Definition
T/F: All PREganglionic neurons release Ach.
Term
True!!
Definition
T/F: All PARASYMPATHETIC POSTganglionic neurons release ACh.
Term
True, baby!
Definition
T/F: Most SYMPATHETIC POSTganglionic release norepinephrine.
Term
False! They release ACh.
Definition
T/F: Sympathetic POSTganglionic that innervates sweat glands release norepinephrine.
Term
False! It releases norepinephrine and epinephrine, epinephrine being the dominant one.
Definition
T/F: The adrenal medulla releases norepinephrine only.
Term
True!!
Definition
T/F: All motor neurons to skeletal muscles release ACh.
Term
1. preganglionic neurons (autonomic); 2. postganglionic (parasympathetic) neurons; 3. Some postganglionic (sympathetic) neurons
Definition
Which three locations have ACh as the major neurotransmitter?
Term
ACh
Definition
___ is released from preganglionic fibers of parasympathetic and sympathetic, postganglionic fibers of parasympathetic, somatic efferents innervating skeletal muscle.
Term
Acetyl-Co-A synthesized in mitochondria, combines with choline to create ACh via action of choline acetyltransferase (ChAT)
Definition
Acetyl-Co-A is synthesized in the ____. It then combines with ___ to create ACh via catalytic action of ___ ____ enzyme.
Term
Ca2+
Definition
An increase in ___ interacts with the vescicle membrane proteins causing ACh vescicles to fuse to nerve terminal membrane.
Term
Botulinum toxin (Botox)
Definition
___ blocks acetylcholine release from nerve endings = no muscle contraction.
Term
metabolized by pseudocholinesterase, hydrolyzed by acetylcholinesterase (AChE)
Definition
ACh can diffuse away from the synapse and is metabolized by ____ or it can be hydrolyzed by ___ to choline and acetate.
Term
False! It is a very rapid process.
Definition
T/F: The half-life of ACh in the synapse is very long.
Term
pseudocholinesterase
Definition
___ is found in blood plasma, liver and many other tissues and can metabolize ACh.
Term
Muscarinic and nicotinic
Definition
What are the two subtypes of receptors for cholinergic receptors?
Term
Nicotinic receptors
Definition
___ receptors are located on postsynaptic membrane of autonomic ganglia on postganglionic neurons and postjunctionally in adrenal medulla and at NMJ of skeletal muscles.
Term
Inhibitors, physostigmine is reversible; malathion is irreversible
Definition
Physostigmine and malathion are acetylcholinesterase (inhibitors/activators).
Term
Physo = reversible, malathion = irreversible
Definition
Physostigmine is a(n) (reversible/irreversible) AChE inhibitor. Malathion is a(n) (reversible/irreversible) AChE inhibitor.
Term
False!! Everything is true except that they are also called INdirect cholinergic agonists.
Definition
T/F: AChE inhibitors are also referred to as direct cholinergic agonists because they increase the [ACh] in the synaptic cleft resulting in activation of cholinergic receptors (both nicotinic and muscarinic)
Term
Muscarinic = g-protein linked, nicotinic = ion channel
Definition
(Muscarinic/Nicotinic) = g-protein linked; (Muscarinic/Nicotinic) = ion channel
Term
Direct acting
Definition
(Direct/indirect) acting cholinergic agonists bind and activate muscarinic or nicotinic receptors. Examples are choline esters such as carbachol or bethanechol and plant alkaloids such as pilocarpine and nicotine.
Term
Indirect acting
Definition
(Direct/Indirect) acting cholinergic agonists inhibit AChE and increase [ACh] which stimulates cholinoreceptors. Examples are reversible ACHe inhibitors such as physostigmine and irreversible AChE inhibitors such as malathion and sarin.
Term
Choline esters... (all have "chol" in name)
Definition
Acetylcholine, carbachol and bethanechol are all ___ ___.
Term
True! (remember, all have "Chol" in name)
Definition
T/F: Choline esters are cholinomimetic and include Acetylcholine, carbachol and bethanechol.
Term
plant alkaloids (all have "ine" in name)
Definition
Muscarine, pilocarpine and nicotine are all ___ ___ that are direct-acting cholinergic agonists.
Term
Muscarine (MuscarINE - amINE)
Definition
___ is a quaternary amine that is less completely absorbed from the GI tract that tertiary amines, but still toxic when ingested. It is excreted by the kidneys and its excretion is enhanced by acidification of the urine.
Term
irreversible
Definition
Malathion and sarin are organophosphorus compounds that are (reversible/irreversible) indirect-acting cholinergic agonists.
Term
reversible
Definition
Donepezil and physostigmine are (reversible/irreversible) indirect-acting cholinergic agonists.
Term
reversible (all have "stigmine" in name)
Definition
Physostigmine, neostigmine and pyrisdostigmine are esters of carbamic acid and are (reversible/irreversible) indirect-acting cholinergic agonists.
Term
reversible
Definition
Donepezil and tacrine are centrally acting (reversible/irreversible) indirect-acting cholinergic agonists that can cross the BBB. They are used clinically for Alzheimer's disease.
Term
True!!
Definition
T/F: Pyrisdostigmine and Edrophonium do not cross the BBB.
Term
Physostigmine
Definition
___ is a reversible indirect acting cholinomimetic that can cross the BBB. It is used clinically as an eye ointment (miotic) and an antidote to atropine-like drugs.
Term
Neostigmine
Definition
___ is a reversible indirect-acting cholinergic agonist that cannot cross the BBB because it is more polar. It is used clinically post op to stimulate bladder and GI tract, as an antidote to tubocurarine and other competetive NM blockers and myasthenia gravis.
Term
False!! It stimulates cholinergic receptors therefore increases salivation, flushes skin and decreases BP.
Definition
T/F: Since neostigmine stimulates cholinergic receptors, some adverse effects include a decrease in salivation, pale skin and increase in BP.
Term
Covalently
Definition
Organophosphorus compounds irreversibly bind with AChE how?
Term
Irreversible such as organophosphorus compounds.
Definition
(Reversible/Irreversible) indirect-acting cholinergic agonists cause salivation, lacrimation, miosis, bronchoconstriction, bradycardia, intestinal cramps, urinary incontinence, muscle paralysis, seizures, respiratory depression and coma.
Term
Belladonna alkaloids
Definition
Atropine, scopolamine and hycoscyamine are all ____ ____ that dilate pupils
Term
Atropine-like drugs
Definition
____-like drugs interact with antihistamines and CNS depressants by causing dry mouth.
Term
dilators (...tropium in both)
Definition
Ipratropium and tiotropium are anticholinergic broncho(dilators/constrictors).
Term
oxybutynin
Definition
___ is an antispasmodic for the urinary tract used with other anticholinergics and CNS antidepressants.
Term
vagus nerve
Definition
SA and NA node is innervated by the ___ nerve. This nerve releases ACh and activates muscarinic receptors resulting in decrease in HR.
Term
nitric oxide
Definition
Activation of muscarinic receptors brings about the release of ___ ___ from endothelial cells which causes vasodilation and decreases peripheral vascular resistance.
Term
ACh is released from cholinergic nerve endings causing ciliary muscle constriction which relaxes the lens for near vision. Also causes the pupil to contract.
Definition
How do cholinergic receptors effect the eye?
Term
glaucoma and in ocular surgery
Definition
Carbachol, pilocarpine and physostigmine are used to treat ___ and in ___ surgery.
Term
Mydriasis
Definition
___ is dilation of the pupil caused by blocking muscarinic receptors by drugs such as atropine, cyclopentolate and tropicamide.
Term
mydriasis by blocking muscarinic receptors.
Definition
Atropine, cyclopentolate and tropicamide all cause ____.
Term
tropicamide
Definition
___ causes ciliary muscle spasm.
Term
True! Stimulating muscarinic = increase secretion. Blocking muscarinic = decrease secretion.
Definition
T/F: All glands are innervated by cholinergic nerves.
Term
atropine, gastric/sweat = atropine and scoplamine
Definition
___ inhibits secretion and relaxes smooth muscles of the bronchi to assist in intubation. Gastric acid and sweat production is also decreased by this drug.
Term
sialogogue, antisialogogue
Definition
___ increases saliva production by activating muscarinic receptors. Pilocarpine is an example. ___ decreases saliva production. Propantheline, atropine and scoplamine are examples.
Term
Parasympathetic
Definition
(Sympathetic/Parasympathetic) stimulation results in urination by contracting detrusor muscle, decreasing bladder capacity, relaxing trigone and urethra sphincter.
Term
Oxybutynin and tolterodine
Definition
___ and ___ are muscarinic antagonists used to treat urinary incontinence.
Term
True!
Definition
T/F: Salivary and gastric glands are strongly stimulated by parasympathetic. Pancreas and small intestinal glands are less affected.
Term
parasympathetic stimulation (muscarinic agonist)
Definition
___ stimulation increases motor activity of the gut involving depolarization of the smooth muscle cell membrane and increased calcium influx.
Term
GI Atony (carbachol, bethanechol "nature "chols")
Definition
___ ___ is when the gastrointestinal tract lacks muscular tone. Following surgery, you need to stimulate the parasympathetic nervous system to stimulate gastric and intestinal motility and increase lower esophaageal sphincter pressure.
Term
diphenoxylate and atropine
Definition
When you have diarrhea you need to decrease the motor activity of the gut using ___ and ____ to block muscarinic receptors.
Term
False!! Drugs like atropine relax GI muscles except sphincters and reduce intestinal motility, thereby increasing gastric emptying time and intestinal transit times
Definition
T/F: Drugs that act like atropine constrict the GI muscles except sphincters and increase intestinal motility.
Term
muscarinic
Definition
ACh released and activates ___ receptors causing bronchoconstriction.
Term
muscarinic
Definition
Atropine, ipratopium(atrovent), and tiotropium block ___ receptors causing bronchial relaxation.
Term
ipratropium
Definition
Combivent is made up of atrpine and ___.
Term
False! Vice versa
Definition
T/F: Atropine is more sedating than scopolamine.
Term
Atropine
Definition
___ causes mild stimulation followed by a slower and longer-lasting sedative effects, but at higher doses, patients experience delerium and hallucinations.
Term
>240/>100 hypertensive crisis
Definition
Hypertensive crisis = >___/>___
Term
trimethaphan or mecamylamine
Definition
___ and ___ selectively blocks nicotinic receptors at autonomic ganglia and rapidly decreases blood pressure. These drugs also cause xerostomia, blurred vision and urinary retention.
Term
neuromuscular blocking agents
Definition
____ ___ ___ block nicotinic receptors and cause muscle weakness and paralysis.
Term
nondepolarizing
Definition
___ (curariform drugs) include tubocurarine and pancuronium. Muscle relaxes without stimulation.
Term
depolarizing
Definition
____ neuromuscular blocking agents include succinylcholine. They stimulate muscle before relaxation.
Term
neuromuscular junction blockers
Definition
___ ___ blockers are adjuncts to surgical anesthesia to produce muscle relaxation and to facilitate intebation, adjunct to electroconvulsive therapy to prevent muscle tearing and diagnosis of myasthenia gravis.
Term
malignant hyperthermia
Definition
___ ___ is an increase in body temp leading to protein denaturation @ about 40 degrees C/108 degrees F
Term
pseudocholinesterase
Definition
Succinylcholine is metabolized in blood by ____.
Term
Bethanechol
Definition
____ in high doses may cause CNS stimulation, orthostatic hypotension, parasympathetic overstimulation, increased saliva or sweating, nausea, vomiting, or seizures.
Term
pilocarpine
Definition
____ stimulates muscarinic receptors and is clinically used to increase salivary flow. Its adverse effects include sweating, nausea, urinary frequency, and dizziness. Patients with uncontrolled asthma should not take this.
Term
norepinephrine
Definition
___ is synthesized from pehylalanine, tyrosine, DOPA, and DA.
Term
dopamine
Definition
____ is transported into vesicles and is then converted to norepinephrine.
Term
adrenal gland
Definition
In the ___ ___, norepinephrine is converted to epinephrine.
Term
Beta 1/2 post, alpha 1 post, alpa 2 pre
Definition
Beta 1/2 receptors are (pre/post) synaptic, alpha 1 is (pre/post) synaptic, alpha 2 is (pre/post) synaptic.
Term
COMT
Definition
Epinephrine is inactivated by ___ in the liver.
Term
epinephrine and isoproterenol
Definition
___ and ___ are direct-acting adrenergic agonists.
Term
amphetamines
Definition
___ promotes NE release and is an indirent-acting adrenergic agonist that lead to an increase in [NE].
Term
phenelzine and tranylcypromine
Definition
___ and ___ are indirect-acting adrenergic agonist and inhibit NE inactivation by inhibiting MAO.
Term
cocaine and tricyclic antidepressants
Definition
___ and ___ antidepressants such as imipramine, amitryptyline and doxepin are indirect-acting adrenergive agonists that inhibit NE reuptake leading to an increase in [NE].
Term
Epinephrine, norepinephrine
Definition
___ works with alpha 1/2 and beta 1/2 while ___ only works with alpha 1/2 and beta 1.
Term
norepinephrine, dopamine
Definition
___ works with alpha 1/2 and beta 1. ___ works with alpha 1, beta 1 and dopamine.
Term
norepinephrine
Definition
Adrenergic agonists mimic the action of ____ and are called sympathomimetics. They stimulate adrenergic receptors.
Term
Both false! Catcholamines are short acting and noncatecholamines are long acting.
Definition
T/F: Catecholamines are long-acting direct-acting adrenergic agonists. Noncatecholamines are short-acting direct-acting adrenergic agonists.
Term
catecholamines
Definition
Norepinephrine, epinephrine and dopamine are _____ along with isoproterenol and dobutamine.
Term
noncatecholamines
Definition
Ephedrine and phenylephrine are ______.
Term
catecholamines such as norepinephrine, epinephrine, dopamine, isoproterenol and dobutamine
Definition
____ have to be injected, have short duration of action, do not cross BBB, are rapidly inactivated by MAO/COMT enzymes and have a short shelf life.
Term
monoamine oxidase (MAO)
Definition
___ ___ enzyme is present in the liver, intestinal wall and presynaptic nerve endings.
Term
catechol-o-methyltransferase (COMT)
Definition
______ enzyme is present in the liver, intestinal wall and postsynaptic nerve endings.
Term
Oral
Definition
___ administration is ineffective so NE, dopamine and dobutamine requires slow infusion, subcutaneous or intramuscular.
Term
noncatecholamines such as ephedrine, phenylephrine and terbutaline
Definition
___ are metabolized slowly by MAO and not inactivated by COMT. They have longer half lives, can be given orally, and cross the BBB.
Term
Alpha 1
Definition
Alpha __ agonist receptor activation results in vasoconstriction.
Term
epinephrine
Definition
___ is used for hemostasis and an adjunct to local anesthesia. It is activates alpha 1 receptors.
Term
alpha 1
Definition
Adverse effects of ___ ___ agonist receptor activation include hypertension, necrosis and bradycardia.
Term
beta 1
Definition
___ ___ agonist receptors are activated by NE, epi, dopamine, isoproterenol, dobutamine and ephedrine.
Term
Beta 1
Definition
___ ___ agonist receptors are activated to treat cardiac arrest, heart failure, shock, AV heart block, tachycardia, dysrhythmias and angina.
Term
Beta 2
Definition
___ ___ agonist receptors affect the lungs and uterus. Epinephrine, isoproterenol, terbutaline, albuterol or ventalin are used to activate these receptors.
Term
beta 2
Definition
___ ___ agonist receptors are activated to treat asthma, hyperglycemia, tremors and to delay preterm labor.
Term
epinephrine
Definition
___ is administered in the event of anaphylactic shock to activate agonists beta 1, alpha 1 and beta 2.
Term
epinephrine
Definition
___ reacts with cocaine, tricyclic antidepressants, MAO inhibitors, general anesthetics and adrenergic blockers.
Term
nonselective, selective
Definition
____ alpha adrenergic blocking agenst block both alpha 1 and 2. ____ block only alpha 1.
Term
nonselective, selective
Definition
___ beta adrenergic blocking agents block beta 1 and 2. ___ block beta 1 only.
Term
False! Vice versa!
Definition
T/F: Phentolamine and phenoxybenzamine are selective alpha blockers. Prazosin and terazosin are nonselective alpha blockers.
Term
alpha 1
Definition
___ ___ adrenergic antagonist blocks on blood vessels as a local anesthesia reversal. It blocks in the eye and bladder also.
Term
alpha 2
Definition
___ ___ adrenergic antagonist has no clinical application.
Term
True!
Definition
T/F: Alpha adrenergic antagonists lower blood pressure via vasodilation.
Term
pheochromocytoma
Definition
___ is a catecholamine tumor in the adrenal medulla.
Term
raynaud's disease
Definition
___ ___ is a peripheral vascular disorder with vasospasm in toes and fingers.
Term
prazosin
Definition
___ is a competitive selective alpha 1 antagonist indicative in hypertension.
Term
beta, 1, 2
Definition
___ adrenergic antagonists are competitive blockers. (1/2) blockage of cardiac tissue results in decrease HR, force of contraction, velocity of impulse conduction via VA node. (1/2) antagonists have minimal clinical use because it blocks the lungs.
Term
Beta 1
Definition
___ ___ adrenergic antagonis is used to treat angina, hypertension, cardiac dysrhythmias and myocardial infarction.
Term
reserpine
Definition
___ depletes NE from nerve endings and has both peripheral and central effects. It is an indirect-acting antiadrenergic agent.
Term
Clonidine
Definition
____ is a centrally acting alpha 2 agonist that is used to treat hypertension. It reduces the firing of sympathetic nerves to blood vessels and heart, causes vasodilation, slows HR and decreases in cardiac output.
Term
reserpine
Definition
___ is a both centrally and peripherally acting adrenergic neuron blocking agent. It depletes NE from nerve endings and stops neurotransmission. "Shut down/restart computer"
Term
clonidine
Definition
____ is a centrally acting alpha 2 agonist used in hypertension. It affects alpha 2 receptors on PREsynaptic nerve terminal in brain stem.
Term
clonidine
Definition
___ reacts with alpha 2 receptors on the presynaptic nerve terminal in the brain stem causing vasodilation (decrease HR, BP, CO)
Term
clonidine
Definition
___ is a centrally acting alpha2 agonist that causes drowsiness and xerostomia.
Term
False!
Definition
T/F: It is ok to give a patient local anesthesia with epinephrine if you suspect that they have used cocaine in the last 24 hours.
Term
amphetamine
Definition
___-like drugs are used to treat ADHD.
Term
acute pain
Definition
(Acute/Chronic) pain deals with nociceptors when an excessive noxious stimulus gives rise to an intense and unpleasant sensation.
Term
chronic pain
Definition
___ pain is an aberration of normal physiologic pathways. It deals with hyperalgesia, allodynia and spontaneous pain spasms.
Term
hyperalgesia
Definition
___ is an increased amount of pain associated with a mild noxious stimulus.
Term
allodynia
Definition
___ is pain evoked by a non-noxious stimulus.
Term
analgesia, analgesics
Definition
___ relieve pain by inhibiting specific pain pathways. ____ are the pharmacological agents that inhibit specific pain pathways.
Term
A-delta, C fibers
Definition
Primary afferent neurons consist mainly of ___ fibers and ___ fibers.
Term
A delta fibers
Definition
___ fibers conduct intense, sharp, stinging pain. They are lightly myelinated and fast-acting.
Term
C fibers
Definition
___ fibers conduct dull, burning, aching pain and are unmyelinated and slow-acting.
Term
A delta, C fibers
Definition
___ fibers deal with pain localization and withdrawal reflexes. ___ fibers deal with autonomic reflexes, pain memory and discomfort.
Term
A beta
Definition
Peripheral ___ sensory fibers inhibit A delta and C fibers via the release of enkaphalins. This principle is used in acupuncture, TENS and rubbing an injury site.
Term
spinothalamic
Definition
___ neurons include A delta and C fibers.
Term
nociception
Definition
___ is the sensory detection, transduction and neural transmission of noxious/painful events.
Term
algogenic
Definition
___ are pain producing substances.
Term
algogenic substances
Definition
___ substances are generated at the injury site, stored in cells as precursors and are liberated during inflammatory response. Eg: Adenosine, adenosine triphosphate, serotonin, histamine, bradykinins, prostaglandins and neuroactive substances.
Term
1. histamine and bradykinins 2. Presence of inflammatory cells (PGE, leukotrienes, PAFs) 3. lymphocyte involvement (interleukins, TNF-alpha and tissue repair occurs)
Definition
Explain the three steps in the time-related process of inflammation.
Term
False! They're SAIDS!
Definition
T/F: Hydrocortisone and betamethason are NSAIDS.
Term
False! Acetaminophen is NOT an NSAID!
Definition
T/F: Acetaminophen is an NSAID along with ibuprofen and aspirin.
Term
Definition
Be able to understand the flow charts on the 3rd powerpoint of this exam.
Term
COX isoenzymes
Definition
Products of what are used to induce/mimic biological effects and their biological effects are inhibited by NSAIDs?
Term
PGE2alpha, PGF2alpha, PGD2alpha
Definition
___, ___, ___ are COX isoenzymes that we use to induce/mimic biological effects.
Term
PGE2 (cervidil, prepidil, and prostin E2)
Definition
___ is used to induce abortion in the 12th-20th week of pregnancy. It acts directly on the myometrium, stimulates uterine contractions and induces labor. It also is used for cervical ripening during labor.
Term
PGE1 analog (misoprostol)
Definition
___ is used to prevent gastric ulcers in susceptible patients taking NSAIDs. It enhances gastric mucosal defense mechanism and healing in acid-related disorders by increasing production of gastric mucus and increasing mucosal secretion of bicarbonate.
Term
Misoprostol
Definition
___ is a PGE1 analog that prevents gastric ulcers.
Term
TXA2
Definition
Tissue injury induces ___ to be produced/released from the platelets, which then promotes platelet aggregation and causes vasoconstriction.
Term
Thromboxanes
Definition
___ act on smooth muscle and platelet aggregation. TXA2 is an example and it stimulates platelet aggregation.
Term
TXA2
Definition
If a patient is taking NSAIDs then ___ production is inhibited leading to prolonged bleeding time.
Term
COX 1 inhibitors
Definition
ASA, APAP and naproxen are all NSAID COX___ inhibitors.
Term
COX 2
Definition
Celecoxib/celebrex is an NSAID COX __ inhibitor.
Term
COX 3
Definition
Acetaminophen (APAP) is a COX __ inhibitor.
Term
False! APAP works on central COX only, not peripheral
Definition
T/F: Acetaminophen has action on the peripheral COX as well as the brain.
Term
constitutive
Definition
COX1 (constitutive/inducible) deals with platelets' production of TXA2, the kidney's regulation of renal blood flow, maintains gastric mucosa's integrity and regulates vasomotor tone.
Term
Constitutive
Definition
COX 2 (constitutive/inducible) deals with the brain, renal medulla and reproductive tract.
Term
inducible
Definition
COX 2 (constitutive/inducible) deals with inflammation and pain by a number of inflammatory mediators.
Term
constitutive
Definition
COX3 (constitutive/inducible) deals with the CNS and is inhibited by APAP.
Term
COX1 inhibitors are rapidly absorbed via the STOMACH and the upper GI. Liquid formulation is absorbed FASTER than tablets. Absorption is primarily via the GASTRIC MUCOSA and is delayed by food. It CAN cross the placenta and is metabolized in the liver and excreted via the kidneys.
Definition
COX1 inhibitors are rapidly absorbed via the ___ and the upper GI. Liquid formulation is absorbed (faster/slower) than tablets. Absorption is primarily via the ___ ___ and is delayed by food. It (can/cannot) cross the placenta and is metabolized in the liver and excreted via the kidneys.
Term
1st false (it binds irreversibly), 2nd true
Definition
T/F: ASA reversibly binds. This is called acetylation.
Term
COX1 > COX2
Definition
ASA has selectivity for COX __ > COX __. It inhibits the production of cyclooxygenase products.
Term
True!!
Definition
T/F: Ibuprofen binds reversibly.
Term
aspirin
Definition
___ is a peripheral analgesic that inhibits the formation of eicosanoid mediators such as prostaglandins.
Term
aspirin
Definition
___ is effective in reducing mild to moderate pain and has antagonist actions of kinins.
Term
eicosanoid mediators
Definition
____ ____ are products of arachidonic acid.
Term
aspirin (ASA)
Definition
___ has anti-inflammatory, analgesic, antipyretic and antithrombotic effects.
Term
salicylates and NSAIDs including methyl salicylate and tartrazine
Definition
Aspirin has cross-sensitivity with all ____ and ____.
Term
aspirin (ASA)
Definition
____ inhibits thromoxane A2 formation, leading to prolonged bleeding time.
Term
aspirin (ASA)
Definition
___ decreases fetal PGE1 causing closure of the ductus resulting in decreased birth weight and increased mortality. It also increases the duration of labor and bleeding.
Term
ASA and NSAIDs
Definition
____ and ____s interact with antihypertensives such as ACE inhibitors, diuretics and non-selective beta blockers.
Term
captopril, enalapril and lisonopril (...pril)
Definition
___, ___ and ___ are angiotensin converting enzymes (ACE) inhibitors that interact with ASA and NSAIDs.
Term
furosemide and hydrochlorothiazide (...ide)
Definition
___ and ___ are diuretics that interact with ASA and NSAIDs.
Term
propanolol and pindolol (...olol)
Definition
___ and ___ are non-selective beta blockers that interact with ASA and NSAIDs.
Term
warfarin
Definition
___ is an anticoagulant that interacts with ASA and NSAIDs by increasing gastric bleeding, gastric damage and platelet function inhibition.
Term
ethanol
Definition
____ along with ASA and NSAIDs damage gastric mucosal barrier and one should separate their ingestion by 12 hours.
Term
acetaminophen
Definition
NSAIDs and ___ have shown to cause renal damage.
Term
...profen/oxen = propionic acid. ...acin/ac = acetic acid.
Definition
Ibuprofen, naproxen and ketoprofen are all ___ acid derivitives. Indomethacin, ketorolac and diclofenac are ___ acid derivatives.
Term
nasal polyps, asthma and chronic urticaria
Definition
___ ___, ___ and ___ ___ are allergic reactions to ASA.
Term
reye's syndrome
Definition
ASA in children <6months may cause ___ ___.
Term
Cox 1 (ASA and ibuprofen), Cox 2 (celecoxib)
Definition
COX-__ inhibitors interact with NSAIDs by prolonging bleeding time. COX-__ inhibitors have no affect on platelet aggregation.
Term
True!
Definition
T/F: In regards to gastric bleeding, ibuprofen < naproxen < aspirin
Term
leukopenia or thrombocytopenia
Definition
ASA/NSAIDs chronic use may cause soreness, irritation or ulceration of oral mucosa, ____ or ___.
Term
less GI effects, less bleeding effects
Definition
COX2 inhibitors differ from aspirin in that they have (more/less) GI adverse effects and (more/less) effect on bleeding time.
Term
celecoxib
Definition
____ is a COX2 inhibitor.
Term
3, APAP
Definition
COX__ inhibitors have less GI adverse effects, no effects on bleeding time, and no anti-inflammatory activity.
Term
acetaminophen (APAP)
Definition
___ is an equianalgesic to ASA, no effect on platelets, non-ulcerogenic, safe for children (no Reye's syndrome), no effects on peripheral COX isoenzymes, acts in CNS on COX3 isoenzyme.
Term
APAP
Definition
____'s oral pharmacokinetics are rapid and almost complete and is evenly distributed, crosses placenta and milk.
Term
APAP
Definition
___ is hepatotoxin and nephrotoxic as intermediate metabolites in phase I. Then goes through conjugation with glucuronic acid in phase II metabolism.
Term
4g, 4g, 3.2g
Definition
Max dose for APAP = ___grams. Max dose for ASA = ___ grams. max dose for ibuprofen = ___ grams.
Term
5% by CPY2E1 --> NAPQ1, inactivated by glutathione. 95% metabolized by conjugation
Definition
___% of APAP is metabolized by CYP2E1 to MAPQ1 which causes hepatic cell death, it is then inactivated by ___. ___% is metabolized by conjugation to inactive metabolites.
Term
ethanol
Definition
___ is also metabolized by CYP2E1 along with APAP, which induces CYP2E1 levels and also inhibits CYP2E1.
Term
pain relief
Definition
Codeine, oxycodone, hydrocodone, morphine, methadone and heroin all activate to give ___ ___.
Term
naloxone
Definition
___ pushes morphine off receptor to reverse its effects.
Term
enkephalins
Definition
___ are small peptides (5 amino acids). Have met- and leu- types which are endorphines found in spinal tap of 2nd trimester pregnancy.
Term
opioid peptides
Definition
___ peptides are also produced by many non-neuronal cells including endocrine and exocrine glands and cells of immune system. Also found in distinct areas in brain associated with nociception and play regulatory roles in many different systems.
Term
presynaptic nerve
Definition
Opioid receptors on the __synaptic nerve inhibit the opening of calcium channels resulting in inhibition of neurotransmitter release.
Term
postsynaptic nerve
Definition
Opioid receptors on the ___synaptic nerve open the potassium channels resulting in hyperpolarization of the postsynaptic membrane, inhibiting firing.
Term
opioid receptors
Definition
____ receptor activation produces analgesia, sedation, pupillary constriction and cradycardia.
Term
mu
Definition
Most analgesic opioids are __-receptor agonists.
Term
mu receptors
Definition
__ opioid receptors are mainly responsible for alagesic effects as well as respiratory depression, euphoria, sedation and dependence.
Term
activate (agonist to) both
Definition
Morphine, codeine and meperidine (activate/block) mu and (activate/block) kappa.
Term
blocks mu, activates kappa
Definition
Pentazocine (activate/block) mu and (activate/block) kappa.
Term
block both
Definition
naloxone and neltrexone (activate/block) mu and (activate/block) kappa.
Term
pure opioid agonists
Definition
Morphine, meperidine (demerol), codeine, oxycodone, and hydrocodone are (agonists/antagonists).
Term
pentazocine
Definition
___ is a partial opioid agonist.
Term
Naloxone and naltrexone
Definition
___ and ____ are pure opioid antagonists.
Term
pure agonists
Definition
(Pure/Partial) opioid (agonist/antagonist) are morphine like drugs that have a high affinity for mu receptors and lower affinity for delta and kappa receptors.
Term
strong agonists
Definition
Morphine and meperidine are (strong/weak) opioid agonists.
Term
pentazocine... antagonist at mu, agonist at kappa... it should not be used with morphine
Definition
___ is a mixed opioid agonist.
Term
weak agonists
Definition
Codeine, oxycodone and hydrocodone are (weak/strong) opioid (agonists/antagonists).
Term
naloxine (narcam)
Definition
____ is administered to reverse effects of opioids by blocking mu receptors.
Term
15, 8, 60
Definition
__mg codeine in tylenol 3. __mg codeine in tylenol 2. __mg in tylenol 1. __mg in tylenol 4.
Term
opioids
Definition
___ increase tone of GI smooth muscle leading to constipation.
Term
vomiting
Definition
emesis is ____. This is a side effect of opioids.
Term
morphine
Definition
___ is well absorbed orally with extensive 1st pass effect (90%). It does not cross the BBB easily. It is a strong opioid.
Term
codeine, CYP2D6
Definition
___ is a prodrug metabolized to morphine by CYP___.
Term
codeine
Definition
___ is excreted in the urine and bile via the enteroheptaic cycling. It is subjected to 1st pass effect and metabolized to morphine.
Term
tramadol HCl
Definition
___ ___ is a centrally acting analgesic that is not chemically related to opioids but acts on mu receptors. Its brand name is Ultram or Ultracet (w/APAP).
Term
tramadol HCl
Definition
___ ___ lowers seizure threshold of patients and may cause syncope.
Term
oxycodone
Definition
___ is 12x more potent than codeine.
Term
weak
Definition
Ibuprofen + (weak/strong) opioid is best mix for ibuprofen-narcotic combo.
Term
amitriptyline
Definition
___ is an tricyclic antidepressant analgesic adjuvant.
Term
carbamazepine
Definition
___ is an antiepileptic/anticonvulsant analgesic adjuvant.
Term
capsaicin... used as a topical analgesic in TMD
Definition
___ is an active substance in chili peppers responsible for their burning taste. It is a highly potent pain-producing substance which selectively stimulates nociceptive and temperature-sensitive nerve endings in tissues.
Term
capsaicin
Definition
___ causes the release/depletion of substance P from afferent neurons and spinal interneurons. It takes days to weeks to recover from effects.
Term
strong
Definition
Bupivacaine and etidocaine are (strong/weak) vasodilating local anesthetics.
Term
weak
Definition
mepivacaine and prilocaine are (strong/weak) vasodilating local anesthetics.
Term
alpha-1 acid glycoprotein
Definition
Once in blood, local anesthetics are reversibly bound to plasma proteins, principally _________ and to a lesser extent albumin and RBCs.
Term
esters
Definition
(Esters/Amides) such as benzocaine are absorbed in blood by pseudocholinersterase.
Term
amides
Definition
(Esters/Amides) such as lidocaine are metabolized primarily in the liver. When excreted by kidney they may have active metabolites.
Term
prilocaine, articaine
Definition
____ is metabolized outside the liver (extrahepatic). ___ is inactivated/metabolized in the liver and plasma by hydrolysis.
Term
esters
Definition
Pseudocholinesterases metabolize ___ in the blood often to para-aminobenzoic acid (PABA).
Term
amides such as prilocaine and articaine
Definition
___ local anesthetics cause methemoglobinemia where patient turns blue = medical emergency. The ability of hemoglobin to pick up/drop off O2 decreases.
Term
1. beta blockers, 2. H2-antihistamine
Definition
What are 2 drugs that lower hepatic blood flow?
Term
True!
Definition
T/F: Allergic reactions are extremely common and they exhibit cross-sensitivity between ALL esters.
Term
True! You can still be allergic to one amide, but it does not mean you are allergic to all like you would be with easters.
Definition
T/F: Amide allergic reactions are rare and there is no cross-sensitivity between them.
Term
methylene blue
Definition
What is the treatment of choice in methemoglobinemia?
Term
epinephrine
Definition
____ stimulates alpha 1/2 receptors causing vasoconstriction. It is a sympathomimetic.
Term
Blood --> liver (MAO and COMT)
Definition
Where and how is epinephrine metabolized?
Term
0.04 mg = 2 carpules
Definition
When used with non-selective beta blockers such as propanolol, epinephrine should not exceed ___mg.
Term
0.04 mg = 2 carpules
Definition
When used with tricyclic antidepressants such as amitripytline or doxepine, epinephrine should not exceed ___mg.
Term
0mg!! Treatment should be deferred!
Definition
When used with cocaine (w/in 24 hrs), epinephrine should not exceed ___mg.
Term
False! Only use with caution in corticosteroid-dependent asthmatics and contraindicated in patients with documented sulfite allergy.
Definition
T/F: Local anesthetics with epinephrine is contraindicated for all asthmatic patients.
Term
False! Only in LAs w/epi
Definition
T/F: Metabisulfite is a preservative found in local anesthetics without epinephrine.
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