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76 Cards in this Set

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Which drug is like tacrolimus but does not inhibit calcineurin?
What is the target of Sirolimus?
mTOR -> ultimately inhibits p70S6 kinase, thus inhibiting gene transcription
What is another name for FK506?

(FK506 is just such a tacky name)
What transcription factor does calcineurin activate?
Describe the activation of NFAT
dephosphorylation by calcineurin
What 2 drugs in inhibit calcineurin?
What is the cyclosporin binding protein?
What is the tacrolimus binding protein?
What mouse monoclonal antibody block CD3?

Muro -> mouse
monab -> monoclonal antibody
Which drug blocks IL-2R?
What does daclizumab do?
humanized monoclonal antibody against IL-2R
What are the side effects of cyclosporin? (4)
Renal dysfunction -> gout, HTN
Gigival hyperplasia
Which drug inhibits IMPDH?

(The fungus phenol)
Which drug blocks lymphocyte proliferation by interfering with de novo synthesis of GTP?

(The fungus phenol)
What does mycophenolate do?
Inhibits IMP-DH -> inhibits GTP synthesis -> inhibits lymphocyte proliferation
What is azathioprine?
Pro-drug for mercaptopurine -> immunosuppressant

Prior to the discovery of cyclosporine, this was a frequently used drug in the prevention of organ rejection.
Which drug is a prodrug for 6-mercaptopurine?
What are the two BROAD (seriously, very broad) ways that MTX is an immunosuppressant?
1) Inhibits DNA replication and proliferation.

2) Inhibits migration.
Which drug is an RA drug that is an inhibitor of pyrimidine sythesis?
LEFLUNOMIDE -> Inhibitor of DH-orotate DH -> inhibits pyrimidine synthesis -> inhibits RNA and DNA production
How does leflunomide work?
Inhibitor of DH-orotate DH -> inhibits pyrimidine synthesis -> inhibits RNA and DNA production
Which drug is a prodrug of mercaptopurine?
What does azathiprine do for RA?
Converted to mercaptopurine -> Hypoxanthine analogue -> purine antimetabolite -> blocks cellular proliferation
Which RA drug is a gold compound?
What is auranofin?
A gold compound used for the treatment of RA.
What are the side effects of auranofin? (3)
Hematologic disturbances


GI upset
What is OH-chloroquine used for?
Adjunctive treatment for RA, alongside NSAIDS.
What is the major toxicity associated with OH-chloroquine?
Retinal toxicity
What are the side-effects of leflunomide?
Virtually none (unusual)

Recall that this is a suppressor of pyrimidine synthesis.
What is the main drawback of leflunomide?
Expensive. Poor RA patients may want to take a different route.

There is a wealthy Frenchman with RA named le'Flu. He can afford this treatment for RA, but you, being a poor med student cannot.
What is the primary cytokine associated with RA?
How long does Anakinra take to work?
1-3 months

Which is roughly the same length as most of the recent Star Wars movies. Screw Anakin, that guy sucks.
What is anakinra?
recombinant IL-1ra
What is the name of recombinant IL-1ra?

(In Star Wars 1--as in IL-One--we learned about Anakin. In pharmacology, however, we learned about IL-1ra. Put them together and you have Anakin-RA)
What is etanercept?
Fusion protein of soluble TNF-R and Fc
What is the name of the fusion protein of soluble TNF-R and Fc?
How is Remicade different from Humira?
Remicade=humanized chimera

Humira=actual human antibody
What are the 2 anti-inflammatory drugs used in gout?

How does colchicine work?
disrupts microtubules in inflammatory cells
Is colchicine used on a long-term basis?
No, colchicine has major side effects -> only used during acute attack or to prevent acute attack (eg, with the administration of allopurinol or probenicid)
What are the two ways to lower uric acid concentration?
Increase excretion (probenecid)

Decrease production (allopurinol)
What are two major adverse events associated with probenecid use?
1) Acute gouty attack

2) Urate deposition -> Renal dysfunction
How does probenecid work?
Blocks active reabsorption of uric acid in the proximal tubule
Which drug blocks active reabsorption of uric acid in the proximal tubule?
Where in the nephron does probenecid work?
proximal tubule
What actions can be taken to prevent urate crystal preciptation in the urinary tract when probenecid is being administered?
1) Lots of fluids

2) Alkalinize the urine (acetazolamide)
Describe the exact mechanism of allopurinol.


ALLOXANTHINE inhibits XANTHINE OXIDASE, the same enzyme that created it.
A patient is metabolizing 6-mercaptopurine too quickly. What can be done to slow this catabolism?
Low dose allopurinol -> inhibits the xanthine oxidase that is catabolizing the mercaptopurinol
Which purine metabolites become increased in response to allopurinol administration?
Xanthine oxidase inhibition -> increased levels of xanthine and hypoxanthine.

These purines are MUCH more soluble than uric acid and are easily excreted by the kidneys.
What is the main side effect of allopurinol, other than precipitating a gouty attack?
A rash... ?
Which glucocorticoid is short-acting?
hydrocortisone (AKA cortisol)
Which glucocorticoids are intermediate-acting? (3)


Which glucocorticoids are long-acting? (2)

Which drug is an aldosterone analogue?

(You're losing FLUids with all those salts. Do you need hyDROCORTISONE? No, of course not. You need FLU-DROCORTISONE.)
How does aldosterone promote sodium reabsorption in the nephron? (2)
1) Promotes synthesis of sodium channels

2) Promotes synthesis of Na/K ATPase
What are the two main ways that adrenal cortical steroid synthesis can be inhibited? (Name all three drugs.)
Inhibit conversion of cholesterol to pregnenolone (eg, aminoglutethimide)

Inhibit p450 (eg, myterapone or ketoconazole)
What drug inhibits conversion of cholesterol to pregnenolone?

What two drugs inhibit p450?

(My terrible corn-pone memory never lets me remember myterapone.)
What is mifepristone better known as?
RU-486, the abortion pill.
What 2 pharmacological activities does mifepristone have?
GC-R antagonist
Progesterone antagonist
Does myterapone inhibit the production of sex steroids?
No, only GC's and MC's
Does ketoconazole inhibit the production of sex steroids?
No, only GC's and MC's
What is the main steroid used in the treatment of asthma?
What is the main side effect of beclomethasone?
oral candidiasis
What is the mechanism of cromolyn sodium?
Activates K+ channel -> cell hyperpolarization -> inability of mast cell to degranulate
What is the mode of delivery of cromolyn sodium? Why?
Aerosol -> significant first pass metabolism when taken orally
Asthma associated with what time of day is salmeterol especially helpful with?
Nighttime asthma

(Ipratropium is also good for nighttime asthma)
What is the one main side effect of albuterol?
sympathomimetic -> cardiac side effects
Describe the pharmacology of albuterol.
Beta-2 agonist

(Beta-1 is on the heart, so it's not that one)
Describe the pharmacology of ipratropium.
Which muscarinic receptor does ipratropium bind to?
Which asthma drug is especially good for asthma that has been induced by cold air or other irritants?
Describe the pharmacology of theophylline.
A3-Adenosine receptor ANTAGONIST -> blocks mast cell activation
Why does the blockade of adenosine receptors by theophylline improve the symptoms of asthma?
Adenosine triggers mast cell degranulation, so theophylline inhibits mast cell degranulation.
Which adenosine receptor does theophylline bind?
Which leukotriene receptor does montelukast block?
4! (LTD4)
Which drug is helpful in the treatment of aspirin-induced asthma?