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247 Cards in this Set
- Front
- Back
Antacids, chelating agents, alkylating agents are specific or non-specific drug targets?
|
non-specific
|
|
The occupational theory of drug action assumes that overall pharmacodynamic effect of drug is proportional to how much drug binds to receptor. True or False?
|
True
|
|
E max does not necessarily equal B max or the occupancy max? Why is this?
|
There are spare receptors and also amplification of the signal
|
|
Does a lower Kd mean that the drug has a higher or lower affinity for the receptor?
|
higher
|
|
What is the best indication of drug potency?
|
EC50
|
|
Do more potent drugs tend to be more or less safe?
|
More safe because takes less of the drug to lead to an effect
|
|
Is the drug with the lower EC50 more or less potent?
|
more potent- need less concentration of drug to generate effect compared to another drug with higher EC50
|
|
How do you tell what drug has more efficacy?
|
the drug that has the most maximal response is most efficous
|
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The modified occupation theory is E/Emax is proportional but not equal to B/Bmax. True or False?
|
True
|
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An antagonist is an agonist with ___ efficacy
|
zero
|
|
Does competitive antagonists increase or decrease potency? efficacy?
|
decrease potency
can still have same efficiacy at high concentrations, cause still have maximal effect |
|
A noncompetitive antagonist will have an increase or decrease in efficacy?
|
decrease, will never reach the same Vmax as control sample
|
|
Competitive antagonists lowers ____ while non-competitive antagonists lowers ____
|
potency
efficacy |
|
Will a partial agonist produce a bigger or lower response if used with a full agonist?
|
lower response because the partial agonist can displace the full agonist and hence produce a lower than expected response compared to the full agonist
|
|
For a noncompetitive antagonist is the ED50 the same or changed from the drug alone?
|
same, therefore same potency but does lead to less efficacy because less maximal response
|
|
Does the inverse agonist hold the drug in the active or non-active state?
|
non-active resting state
|
|
How does one calculate the therapeutic index?
|
LD50/ED50
|
|
Is a high therapeutic index mean a safer or less safer drug?
|
safer drug
|
|
Does Warfarin or Penicillin have a higher therapeutic index?
|
penicillin
|
|
For a molecule to qualify as a ___ it must meet 3 criteria: 1) In a given sample, there are a finite number of receptors (saturation of binding and effect) 2) Ligand binding is specific and can be competed off by a ligand of the same or similar structure 3) Binding kinetics are consistent with biological effect
|
receptor
|
|
Steroid receptors are what type of receptors?
|
nuclear hormone receptors
|
|
What type of receptors have the most rapid response?
|
ion channels
|
|
Nicotinic receptors are of what type?
Muscarinic receptors are of what type |
ion channels
G-protein coupled |
|
Type III receptor classes are transmembrane and are of what receptor class?
|
G-protein
|
|
With a Type I receptor the amino group is on the ___ of the membrane, whereas the carboxylic group is on the ____ of the membrane
|
outside
inside |
|
Which receptors also act as transcription factors?
|
nuclear hormone receptors
have a slow mechanism of action that can take hours, but have long lasting effects (hours to days) |
|
The activation of receptor tyrosine kinase will activate the Ras cascade and eventually lead to the translocation of ____ into the nucleus, where there will be stimulation of transcription factors and DNA expression
|
ERK
|
|
How can receptors be inactivated?
|
internalized via endocytosis after being clathrin coated
can be targeted to lysosome and be degraded |
|
WIth G-protein coupled receptors, which is the active state and which is the inactive state?
|
the active state is when the receptor is bound to GTP
|
|
Gt1 is present in photons and increases the production of what?
|
cGMP phosophodiesterase
|
|
cAMP can bind to PK___
|
PKA which has 2 catalytic subunits and 2 regulatory subunits
|
|
Gq activates PLC which cleaves PIP2 to PIP3 and DAG. DAG activates PKC, whereas IP3 leads to the release of calcium from intracellular stores, activating ____
|
calmodulin
|
|
What molecule regulates receptor desensitization?
|
beta arrestin
|
|
In ____ desensitization, the response to ligand b is unimpaired, whereas impaired for a
|
homologous
|
|
Atropine is part of what family of receptor drugs?
|
Muscarinic cholinergic receptors
|
|
Adrenergic receptors are ligand gated or GPCRs?
|
GPCRs
|
|
The parasympathetic nervous system is mediated by what type of response?
|
cholinergic
|
|
Parasympathetic ganglions release acetylcholine onto ____ receptors
|
muscarinic
|
|
Sympathetic ganglions release norepinephrine onto _____ receptors,
|
adrenergic (alpha/beta receptors)
|
|
The adrenal medulla is supplied by the ____ nervous system but is stimulated by acetylcholine, whereby it will secrete epinephrine
|
sympathetic
|
|
A ____ acting drug is a molecule that physically binds to the target for its effect
|
direct
|
|
Choline acetyltransferase generates what product?
|
acetylcholine
|
|
Acetylcholine is broken down into what two products by acetylcholinesterase?
|
choline + acetic acid
|
|
What is an irreversible inhibitor of AchE, causing increased cholinomimetic effects?
|
organophosphates
|
|
What is the main muscarinic antagonist?
|
atropine
|
|
Carbachole and pilocarpine are cholinergic agonists that are ____ acting
|
direct
|
|
What drug blocks the uptake of choline into the pre-synaptic nerve terminal?
|
hemicholinium
|
|
What is a reversible antagonist of Acetylcholine esterase?
|
Neostigmine, used to treat myasthenia gravis
|
|
Physostigmine's effect on acetylcholine receptor is _____. This effect is mediated through the inhibition of cholinesterase, which causes an increase in the local concentration of acetylcholine. The net effect is _____ on acetylcholine receptor. Physostigmine is an antidote for _____ overdose
|
indirect
agonistic atropine |
|
Dopamine beta hydroxylase converts ____ to ____
|
dopamine to norepinephrine
|
|
COMT is responsible for the reuptake of ___. Cocaine works by blocking reuptake leading to stimulus
|
norepinephrine
|
|
Pentolamine is a competitive inhibitor of ___ receptors
|
alpha 1
|
|
Propranolol is a ____ blocker
|
beta
|
|
Amphetamine, tyramine, and ephedrine increase ____ release
|
norepinephrine
|
|
Isoproterenol and albuterol are ____ agonists
|
Beta receptor
|
|
Bretylium is an anti-arrthymic drug that blocks the release of ____
|
norepinephrine
|
|
Reserpine blocks the release of vesicles containing ____
|
norepinephrine
|
|
Metyrosine is used to treat what disease of the adrenal medulla?
|
pheochromocytoma
|
|
What drug does alpha receptors have the most affinity to? beta receptors?
|
norepinephrine
isoproterenol |
|
Alpha 1 agonists signal through G___
Alpha 2 agonists signal through G___ Beta agonists signal through ____ |
Gq
Gi Gs |
|
alpha 2 receptors cause ____ aggregation
|
platelet
|
|
alpha 1 receptors causes smooth muscle ____
|
vasoconstriction
|
|
beta 3 receptors increase ____
|
lipolysis
|
|
beta 1 receptors have effects on what tissue predominantly?
|
heart
|
|
bronchodilation is mediated by what type of beta receptors?
|
beta 2 receptors
|
|
Dobutamine, a beta agonist has higher affinity for beta1 or beta 2 receptors?
|
beta 1
|
|
Albuterol, terbutaline, metaproterenol, and ritodrine are beta agonists that have a higher affinity for what beta receptor?
|
beta 2 receptor
|
|
Fenoldopam is a ___ agonist
|
dopamine
|
|
Isoproterenol has equal affinity for both b1 and b2 receptors?
|
Yes
|
|
Phenylephrine and methoxamine are ___ agonists
|
alpha1
|
|
Phenoxybenzamine is a alpha1 ____ and is the drug of choice to treat _____
|
antagonist
pheochromocytoma |
|
Selective a1 blockers include prazosin, doxazosin, terazosin and tasulosiin. True or False?
|
True
|
|
Labetalol and carvedilol are mixed antagonists that block both alpha and beta receptors. True or False?
|
True
|
|
Are alpha antagonists used to drop hypertension?
|
Yes, antagonizes vasoconstriction, causing a drop in blood pressure
|
|
Atenolol is ___ antagonistic
|
beta1
it is a beta blocker |
|
Is Metoprolol a selective beta antagonist? Is nadolol?
|
Metoprolol = B1 selective
Nadolol = not beta1 selective A-M = B1 selective |
|
In the periphery D1 dopamine receptor medates renal vaso____ and increased myocardial contractility
|
renal vasodilation
|
|
D1 and 5 signal through G__
D 2,3,4 signal through G__ |
Gs
Gi |
|
Dopamine at ____ doses will decrease bp, but increase cardiac output. At ___ doses it will further increase cardiac output by increasing myocardial contractility
|
low
higher |
|
What are the two major subtypes of cholinergic receptors?
|
nicotinic and muscarinic receptors
|
|
Actions mediated by nicotinic cholinergic receptors include 1. stimulation of all autonomic ganglia (Nn) 2. stimulation of voluntary muscle (Nm) 3) secretion of ____ from the adrenal medulla (Nn)
|
epinephrine
|
|
When a nicotinic receptor is depolarized, the receptor is bound by ligand and locks the receptor open. True or False?
|
True
|
|
Are M2 receptors of the stimulatory or inhibitory type?
|
inhibitory
|
|
M1 receptors are stimulatory or inhibitory?
|
stimulatory Gq
|
|
The M2 receptor is associated with the ___ nerve. It slows the heart and increases ____ conductance
|
vagus
potassium |
|
What are the effects of muscarinic acetylocholine receptors on the GI system?
|
Increases GI motility
|
|
What is the effect of activating muscarinic acetylcholine receptors in the lungs?
|
bronchospasm, as activation leads to contraction of visceral smooth muscle
|
|
M___ receptors target the glands in the body and cause increased or decreased secretions?
|
M3
increased |
|
On the endothelium what is the effect of cholinergic muscarinic receptor activation?
|
dilation via nitric oxide
|
|
Do indirect agonists for cholinergic muscarinic receptors work on blood vessels?
|
No because there is no innervation of the parasympathetic system
|
|
_____ is a muscarinic antagonist, blocks M2 receptor, increases heart rate
|
atropine
|
|
Defecation, Urination, Miosis, Bradycardia, Emesis, lacrimation, and salivation are clinical manifestations of excessive _____ effects
|
cholinergic
|
|
Dry as bone, red as a beet, mad as hatter is used to describe the effects of _____ antagonists
|
muscarinic
|
|
Mydriasis can be caused by what two action? One stimulatory, one inhibitory?
|
inhibit muscarinic receptors
stimulate a1 receptors |
|
Increased renin release is stimulated by the activity of ___ receptors at the level of the kidney
|
B1
|
|
in arterioles and veins is parasympahetic or sympathetic tone predominant
|
sympathetic
|
|
In the heart what is the predominant tone? If there is a ganglionic blockade will it lead to bradycardia or tachycardia?
|
parasympathetic
tachycardia |
|
With the administration of norepinephrine, there will be increased total peripheral resistance and increased blood pressure due to ____1 effects. There will be increased heart rate, increased stroke volume, and increased cardiac output due to ____1 effects. There can also be a potential for reflex ____.
|
alpha
beta bradycardia |
|
With increasing doses of epinephrine, the effects of ___ receptors predominate more
|
alpha
|
|
Acetylcholine causes a ___ in BP due to vaso____. A larger dose of Ach produces ____cardia
|
fall
vasodliation bradycardia |
|
Why is it that under the influence of atropine, with a dose of acetylcholine you will cause a rise in BP and tachycardia?
|
with atropine you have blocked all parasympathetic stimulation and now the acetylcholine is stimulation the sympathetic ganglia only
|
|
nitric oxide activates ___ cyclase
inhibitor of ____ lead to sustained levels of cGMP that maintains smooth muscle relaxation |
guanyly cyclase
PDE |
|
Beta agonists and theophylline lead to bronchodilation or bronchoconstrication?
|
bronchodilation
|
|
What is the mechanism of action of theophylline and what does it do?
|
theophylline blocks PDE, leading to increased levels of cAMP and increases bronchodilation.
Theophylline also blocks adenosine (this increases bronchoconstriction) |
|
Beta 2 receptors are ___s coupled
|
Gs
|
|
Can muscarinic antagonists such as atropine relieve bronchospasms?
|
Yes
decrease the bronchoconstriction of M3 receptors |
|
with COPD use inhaled _____ antagonist to increase respiratory patency
|
muscarinic
|
|
sympathetic neurons control the dilator muscle (radial muscle of iris) via alpha1--> constricts and dilates the pupil leading to ____
|
mydriasis
|
|
____sympathetic systems control the ciliary muscle and sphincter muscle via cholinergic input
|
parasympathetic
|
|
Infusion of atropine will cause the ciliary muscle to contract or relax?
|
relax
loss of accomodation (cycloplegia) |
|
Contraction of the ciliary muscle will lead to a bulge in the lens which will allow you to accommodate for ___ vision
|
near
|
|
Cholinergic effects will increase or decrease the outflow of the aqueous humor?
|
increase
|
|
What is the two pronged approach to treating glaucoma?
|
Give a beta blocker to stop the production of aqueous humor
Give a muscarinic agonist to increase the outflow of aqueous humor |
|
Ganglionic blockade does not prevent HR changes elicited by beta __ and M__ agonists but will prevent reflex changes in HR elicited by vasconstriction (alpha ___) and vasodilation (beta ____)
|
beta 1 and M2
alpha 1 and beta 2 |
|
Hexamathonium and trimetaphan are what type of blockers?
|
ganglionic blockers
|
|
Pilocarpine a ____ agonist is used to treat glaucoma
|
muscarinic
increases outflow of vitreous humor |
|
edrophonium, physostigmine, neostigmine, pyridostigmine and isoflurophate are what type of drugs?
|
inhibit acetylcholinesterases
|
|
2PAM is an antidote to poisoning via which anti-cholinesterase?
|
organophosphates, which bind irreversibily
|
|
Do alpha 1 agonists increase or decrease TPR? Do beta 2 agonists increase or decrease TPR?
|
increase for alpha1, decrease for beta 2
|
|
Treatment with alpha 1 agonists will lead to reflex ____
|
bradycardia due to M2 receptors, to cancel reflex bradycardia use muscarinic antagonist
|
|
Treatment with beta 2 agonists will lead to reflex _____ due to B1 receptors being activated
|
tachycardia
|
|
Can a beta 1 antagonist stop reflex tachycardia?
|
Yes
|
|
The radial muscle is stimulated by ___ agonists whereas the sphincter muscle is stimulated by ____ agonists
|
alpha 1
muscarinic |
|
Contraction of the sphincter muscle will do what to the pupil?
|
cause it to shrink (miosis)
|
|
If contraction of the radial muscle occurs, what will happen to the pupil?
|
it will become dilated: mydriasis
|
|
Ciliary muscles which are important for accommodation have only parasympathetic innervation. Therefore only ___ drugs affect accomodation
|
muscarinic
|
|
Muscarinic stimulation leads to accommodation to near or far vision?
|
near
|
|
What are the effects of muscarinic receptors on the blood vessel endothelium?
|
dilation
|
|
Can muscarinic agonists such as pilocarpine be used to treat glaucoma?
|
Yes
|
|
Physostigmine is an antidote for ____ overdose
|
atropine
|
|
Does muscarinic effects lead to bronchoconstriction or bronchodilation?
|
bronchoconstriction
|
|
What is the chronic toxicity of AchE inhibtiors?
|
Peripheral neuropathy causing muscle weakness and sensory loss
|
|
Cardiotoxicity, convulsions, and coma can result from overdose of muscarinic antagonists. True or False?
|
True
|
|
Decreased secretions, hyperthermia, tachycardia, and constipation can result from the usage of _____ antagonists
|
muscarinic, such as atropine
|
|
Ipratropium can be used in treatment of asthma and COPD. It is a ____ antagonist
|
muscarinic
|
|
Scopolamine is used to treat ____
|
motion sickness, causes sedation and short term memory block, anterograde amnesia
|
|
Block of the ANS would lead to what effects in the heart?
|
Tachycardia that is fixed
|
|
Will alpha 1 receptor stimulation lead to urinary retention or urine being expelled?
|
urinary retention
|
|
Do alpha 2 receptors increase or decrease platelet aggregation?
|
increase
|
|
Do beta 1 receptors have positive or negative chronotrophy?
|
positive, they increase the HR
|
|
Can Beta 2 receptors be activated by norepinephrine?
|
no, thus NE can never lower BP, can never vasodilate
|
|
D1 receptors cause vasodilation in the kidney. True or False?
|
True
|
|
Is there a change in pulse pressure with alpha 1 agonists? alpha 2 agonists?
|
no for alpha 1 agonists
yes for alpha 2 agonists |
|
Can alpha 2 agonists be used to treat hypertension?
|
Yes
|
|
Carbonic anhydrase inhibitors exert their effects on the proximal tubule and inhibit the reabsorption of ____
|
sodium bicarbonate
|
|
Edema and hypertension can be treated with diuretic therapy. True or False
|
True
|
|
Loop diuretics exert their effects by inhibiting the sodium, potassium, chloride symporter. Where is the site of action of loop diuretics?
|
ascending loop of henle
|
|
Where is the side of action of thiazides? What is their mechanism of action
|
distal convoluted tubule, inhibit sodium chloride symporter
|
|
acetazolamide is what type of drug?
|
carbonic anhydrase inhibitor
|
|
Metabolic ___ can be a side effect of inhibition of carbonic anhydrase
|
acidosis
|
|
Acute mountain sickness can be treated with what diuretic?
|
carbonic anhydrase inhibitor such acetazolamide
|
|
Sodium absorption in the collecting tubule is regulated by ____
|
aldosterone
|
|
Drugs that inhibit sodium reabsorption in the collecting tubule also inhibit ____ secretion
|
potassium, site of action of potassium sparing diuretics
|
|
Water permeability in the collecting tubule is regulated by ____ hormone
|
anti-diuretic
|
|
Is the diuretic effect of carbonic anhydrase inhibitors strong or mild?
|
mild because the tubular fluid may be compenseated partially by increased sodium chloride reabsorption in later segments of the tubule
|
|
Is carbonic anhydrase inhibitors such as acetazolamide indicated to treat metabolic alkalosis, glaucoma, and cystinuria?
|
yes
|
|
Can renal stones be a side effect of the use of carbonic anhydrase inhibitors as diuretics?
|
Yes
|
|
Allergic reaction to sulfonamides can occur with use of carbonic anhydrase inhibitors. True or False?
|
True
|
|
What is the main osmotic diuretic? Where is their main site of action
|
mannitol, loop of henle and proximal tubule where the membrane is most permeable to water
|
|
A major side effect of this drug is expansion of extracellular fluid volume may result in hyponatremia causing central nervous system symptoms such as nausea, headache, and vomiting. In patients with CHF, expansion of extracellular volume may produce pulmonary edema
|
osmotic diuretices such as mannitol
|
|
This diuretic can be used to treat hemoglobinuria and myoglobinuria and also rhabdomyolysis (which can be a side effect of statin use)
|
osmotic diuretic such as mannitol
|
|
There are two major classes of loop diuretics. There are the ____ derivatives suchas furosemide, bumetanide and torsemide and the non_____ loop diuretics such as ethacrynic acid
|
sulfonamide
|
|
Which diuretics are called high ceiling diuretics?
|
Loop diuretics
|
|
Besides sodium, potassium, and chloride, what other ions are inhibited from reabsorption by loop diuretics?
|
calcium and magnesium
|
|
Loop diuretics have a direct effect on vasculature including ___ in renal blood flow and ____ in systemic venous capacitance
|
increase
|
|
What can be used in the treatment of hypertension when patients do not respond to thiazide diuretics and anti-hypertensive drugs?
|
loop diuretics
|
|
Can loop diuretics be used in anion overdose such as the ingestion of bromide, fluoride, and iodide?
|
Yes, negative charges follow the positive charges to the lumen where they are excreted
|
|
Can loop diuretic use lead to hyperkalemia or hypokalemia?
|
hypokalemia
|
|
Ototoxicity is a major toxicity of what class of diuretics?
|
loop diuretics
|
|
Are thiazides sulfonamide derivatives? Where do they exert their action (in what part of the tubule?)
|
Yes they are sulfonamide derivatives and they work in the distal convoluted tubule
|
|
Thiazides enhance ___ reabsorption, as opposed to loop diuretics that inhibit this ions reabsorption
|
calcium
|
|
Hypercalcemia can be a major side effect of what class of diuretics?
|
thiazides
|
|
Why are thiazides effective in treating nephrolithiasis?
|
because thiazides allow for calcium reabsorption which leads to less calcium in the tubules and therefore you are less likely to form calcium stones
|
|
Are hyperglycemia and hyperlipidemia seen with thiazide use?
|
Yes, because insulin is released via ATP dependent opening of potassium channels, lack of potassium caused by thiazides could lead to decrease release of insulin from the beta cell
|
|
Can use of thiazides lead to allergic reaction?
|
Yes because thiazides are sulfonamide derivatives
|
|
Indapamide, metolazone, hydrochlorothiazide and chlothiadone are all what type of drugs?
|
thiazides, therefore are diuretics
|
|
What are sodium channel inhibitors that are potassium sparing diuretics?
|
amiloride and triamterene
|
|
Inhibition of the sodium channel with triamterene causes decreased secretion of what two ions?
|
potassium and hydrogen
|
|
Liddle's Syndrome can be treated with what potassium sparing diuretic?
|
amiloride, aldosterone levels are low in Liddle's Syndrome
|
|
___ is used to treat lithium induced nephrogenic diabetes insipidus by blocking Li transport into tubular epithelial cells
|
Amiloride
|
|
___ inhibits sodium channel in airway epithelial cells, and is used to improve mucociliary clearance in patients with cystic fibrosis
|
amiloride
|
|
Triamterene may reduce glucose tolerance, and induce intersitital nephritis and renal stone. True or false?
|
True
|
|
____ is the only available aldosterone antagonist in the US
|
Spironolactone
|
|
___ are used in combination with loop diuretics and thiazides in treatment of edema and hypertension. ____ enhances sodium excretion and reduces potassium wasting
|
Spironolactone
|
|
____ is the diuretic of choice for patients with hepatic cirrhosis
|
Spironolactone
|
|
Hyperkalemia and metabolic acidosis can occur in patients on potassium sparing diuretics. True or False?
|
True
|
|
Due to its steroid structure this type of diuretic can cause gynecomastia, impotence, and hirsutism
|
spironolactone
|
|
What common antihypertensive do african americans have poor sensitvity to?
|
beta blockers
|
|
Hydrochlorothiazide is a diuretic that _____ blood sugar, calcium, uric acid, and cholesterol and ______ serum potassium
|
increases
decreases |
|
beta blockers can cause ____cardia
|
bradycardia
|
|
What drug which causes a blockade of the adrenergic response to hypoglycemia (tachycardia, nervousness) may leave ____ wihtout the usual warning sign foa decrease in blood sgugar
|
diabetics, loop dirutics
|
|
What are the three classes of anti-thrombotic agents?
|
anti-coagulants, fibriolytic agents, and anti-platelet agents
|
|
The endogenous anti-Thrombin III inhibits what coagulation factor?
|
10A
|
|
Thrombin is a very strong ___ activator
|
platelet
|
|
Factor IIa is also known as ___
|
thrombin
|
|
In the stabilization phase of thrombus formation there is platelet aggregation and fibrin formation. True or False
|
True
|
|
The key product in the coagulation cascade is ____ which activates platelets to aggregate and porduces insoluable fibrin
|
thrombin
|
|
Do platelets synthesize tissue factor?
|
Yes
|
|
In veins are there white or red thrombi? What about in arteries?
|
veins= red thrombi due to entrapped RBCS, in arteries there are white thrombi
|
|
What is the difference between direct and indirect antithrombinagents?
|
indirect inhibitors need the help of anti-thrombin III, direct inhibitors can directly inhibit thrombin without anti-thrombin III
|
|
Are fondaparinux, idraparinux, and heparin direct or indirect thrombin inhibitors?
|
indirect
|
|
Is warfarin given via IV or orally?
|
orally
|
|
Direct thrombin inhibitsors include hirudin, bivalirudin, and argatroban. True or False?
|
True
|
|
Heparin activates what compound?
|
anti-thrombin III
|
|
The ____ part of heparin binds to anti-thrombin
|
pentasaccharide
|
|
Heparin is monitored by PT or PTT?
|
PTT
|
|
Heparin is metabolized by the ___
|
liver
|
|
Protamine sulfate is an antidote for the side effects of what drug?
|
heparin
|
|
minor side effects of this drug include allergy, alopecia, and osteoporosis. Major side effects include HIT
|
heparin
|
|
Do patients with venous thromboembolism or acute coronary snydrome require a higher dosage of heparin?
|
thromboembolism
|
|
Enoxaprin and Dalteparin are names for what type of drug?
|
low molecular weight heparin
|
|
Compared to just heparin, does Enoxaparin and Dalteparin (LMWH) have higher or lower risk of HIT and osteoporosis?
|
lower
|
|
LMWH has more anti-F___ activity than standard heparin
|
factor 10a
|
|
Does fondaparinux and idraparinux have any anti-thrombin activity?
|
No, only factor 10a activity
|
|
Can hirudin, bivalirudin, and argatroban be used for treatment of patients with HIT?
|
yes, they are direct thrombin inhibitors
|
|
Warfarin is an orally available ____ antagonist
|
Vitamin K
|
|
What coagulation factors depend on Vitamin K?
|
Factor 2, 7, 9, 10
|
|
Does foot increase or decrease the rate of absorption of warfarin?
|
decrease
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In plasma most of warfarin is bound to ___, but only the free form is active. Drugs that compete with warfarin binding to ____ are dangerous because a transient increase of ree warfarin increases chances of hemorrhage
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albumin
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Is the PT or PTT used to monitor Warfarin?
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PT, INR should be below 3.0
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Rivaroxaban is an orally available ___ inhibitor
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Factor 10a
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Dabigatran is an orally available ___ inhibitor
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thrombin
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Plasminogen is converted by the enzyme ___ to plasmin leading to breakdown of fibrin clot
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tPA
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Should plasminogen activator inhibitor or alpha2-antiplasmin be used in situations of hemorrhage?
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Yes because they inhibit the breakdown of fibrin closts and therefore would be good to use if a person is bleeding out
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Tissue type plasminogen activator (tPA) is a serine protease that is synthesized by ____ cells
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endothelial
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Alteplase, tenecteplase, and reteplase are all variants of what enzyme that is a fibrinolytic agent?
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tissue plasminogen activator
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Urokinase is synthesized by the ____ and excreted in the urine
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kidney
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Usually in the plasma, pro-urokinase forms a complex with an inhibitor. However in the presence of ____, there is dissociation of the inhibitor
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fibrin
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THis is a protein that is produced by beta-hemolytic strep and forms a complex with plasminogen altering its conformation and exposing its active site
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streptokinase
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Is streptokinase a fibrin specific plasminogen activator?
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No
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Anistreplace (Apsac) is the anisoylated plasminogen streptokinase activator complex. True or False?
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True
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E-aminocaproic acid is an antidote for overdoses of plasminogen activator and is found in _____
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toothpaste
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Plavix and Toclopidine are ADP receptor (P2Y12) antagonsts. True or False?
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True
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What anti-platelet agent is a cyclo-oxygenase inhibitor?
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aspirin
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What is an agent that increases cAMP levels and is an anti-platelet agent?
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Dipyridamole
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Abciximab, Eptifibatide and Tirofiban are ____ antagonists
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GPIIb, IIIa
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What is the main side effect of usage of aspirin?
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GI bleeding
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some patients when treated with ____, see no difference, can be due to defective CYP450 2C19 enzyme
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clopidogrel (Plavix)
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Complications of these two anti-platelet drugs include nausea, dyspepsia, diarrhea, hemorrhage, severe neutropenia, and anemia
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Clopidogrel and Ticlopidine
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Dipyridamole inhibits cAMP phosphodiesterases and increases platelet cAMP. Does this activate or inhibit platelet action?
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Inhibits platelet function by sequesting calcium into its platelet storage sites
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Dipyridamole is used in combination with ____ to prevent thromboembolism in patients with artificial heart valves
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warfarin
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Are abciximab, eptifibatide, or tirofiban available orally? What types of side effects do they cause?
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Not oral, cause bleeding, thrombocytopenia
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Aspirin impairs platelets aggregation, enhancing rsponse of Warfarin. yes or no?
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Yes
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Phenobarbital induces drug metabolism system, decreasing the response of Warfarin. yes or no?
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yes
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Phenylbutazone compete with Warfarin binding to albumin, increasing the response to Warfarin. yes or no?
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yes
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LMWH inhibits factor 10a better than thrombin, less inhibition of platelets than standard heparin. True or Fals?
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True
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Which anti-thrombotic agent can be injected subcutaneously?
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Low molecular weight heparin
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