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immunology louie
sickle cell, woster
46
Pharmacology
Graduate
11/14/2009

Additional Pharmacology Flashcards

 


 

Cards

Term
Deferoxamine (Desferal)
Definition

iron chelating agent

1-2g SQ over 10-12hrs daily

Term
Deferasirox (exjade)
Definition

iron chelating agent

20mg/kg/daily

Term
acetylsalicylic acid (aspirin)
Definition

- acetlyation of the cyclooxygenase active site

-acts on the hypothalmus

- anti-inflammatory

- low degree of analgesia

- uricosuric, only in high doses

- metabolized by N-deacylation to salicylic acid

Term
Salicylic acid
Definition

- active metabolite of aspirin

- metabolized by glycine conjugation to salicyluric acid

- metabolized by p-hydroxylation to gentisic acid

Term
sodium salicylate
Definition
- unstable
Term
methyl salicylate
Definition

- found in oil of wintergreen

-toxic when taken internally

- mainly used in topical preparations like Ben-Gay

Term
phenyl salicylate
Definition

- a salol (covalently bonded combination of 2 drugs)

- cleaved in the GI tract to salicylic acid and phenol

Term
flufenisal
Definition

- salicylate class with a nuclear substitution

- twice as potent as aspirin

- less GI toxicity

Term
Diflunisal (Dolobid)
Definition

- salicylate class with a nuclear substitution

- 3 times more potent than aspirin

Term
aniline
Definition

- antipyretic effects

- causes methemoglobinemia, which may result in cyanosis and death

Term
p-aminophenolacetaminophen
Definition

analgesic

antipyretic

not an anti-inflammatory drug

Term
glutathione
Definition

- reacts with the epoxide

- protects the liver from the arylation intermediate

Term
acetaminophen
Definition

- becomes particularly toxic in an acute overdose

- metabolized by N-deacetylation and glucuronidation

Term
Arylating intermediate
Definition

- a metabolite of acetaminophen that occurs when the normal pathway is staturated

- reacts rapidly with GSH, causing a complete depletion of glutathione

results in dramatic hepatotoxicity

Term
acetylcysteine
Definition
- reacts with arylating intermediate and protects the liver until GSH can be resynthesized.
Term
phenacetin
Definition

- ethyl ether derivative of acetaminophen

- more toxic

- immediately O-dealkylated to acetaminophen

- no longer marketed

Term
phenetsal
Definition

- a salol

- metabolized to acetaminophen and salicylic acid

Term
antipyrene
Definition

- pyrazolinone

- antipyretic and analgesic

- can cause sedation

Term
derivatives of pyrazole
Definition

- pyrazoline: one of the double bonds is saturated

- pyrazolidine: both are saturated

Term
aminopyrene
Definition

- more potent than antipyrene

- can cause agranulocytosis

- removed from the market

Term
phenylbutazone
Definition

- anti-inflammatory

- quite toxic

- pka near 4.5

- causes blood dyscrasias, no longer marketed

Term
oxyphenbutazone
Definition

-active metabolite of phenylbutazone

- very toxic, off market

Term
sulfinpyrazone
Definition

- strong electron leaving group

- pKa 2.8

- less anti-inflammatory agent, used as an uricosuric in the treatment of gout

Term
fenamates
Definition
- N-arylanthranilic acid derivatives
Term
flufenamic acid (Arlef)
Definition

- trifluoromethyl group in the 3 position

- NSAID, no analgesia

Term
Mefanamic acid (Ponstel)
Definition

- methyl groups on the 2 and 3 position

- many side effects

- lower potency

Term
meclofenamic acid (mecolmen)
Definition

2nd position: Cl

3rd position: CH3

6th position: Cl

- 150 x more potent than aspirin

- the halogens prevent the free rotation of the rings, making it a better fit for the receptor.

Term
Indomethacin (Indocin)
Definition

- potent NSAID

- carboxyl moiety is termed alpha

- pka 4.5

Term
sulindac (clinoril)
Definition

- arylacetic acid

- pKa 4.7

- a indene isostere: double bond replaces nitrogen in the indole ring

- remains in cis position, which is optimal for receptor activity

- metabolite sulfide form is also active

Term
Tolmetin sodium (Tolectin)
Definition

NSAID equal to ibuprofen

- lower risk of GI upset

Term
Ibuprofen
Definition

- arylpropionic acid

- alpha methyl group, giving it stereochemistry

- S isomer is active

- R isomer is inactive

Term
Naprosyn
Definition
S isomer
Term
Anaprox
Definition
R isomer
Term
diclofenac
Definition

- contains arylalkanoic acid and anthranilic acid classes

- NSAID

Term
Nabumetone (relafen)
Definition

- drug contains no acidic fuctional groups

- converted by oxidation to the arylacetic acid 6MNA

- causes less GI erosion

- long half life

Term
Etodolac (Lodine)
Definition

- pyranocarboxylic acid

- NSAID

Term
ketorolac (Toradol)
Definition
NSAID
Term
Oxaprozin (Daypro)
Definition
NSAID
Term
Piroxicam (Feldene)
Definition

- oxicam

long half life

- enolic hydroxyl group, pha 4.3

- arthritis treatment

Term
celecoxib (Celebrex)
Definition
- COX 2 inhibitor
Term
Rofecoxic (Vioxx)
Definition
- selective COX 2 inhibitor
Term
DMARDs
Definition

- disease modifying agents for rheumatoid diseases

- alter factors pertaining the etiology of disease rather than alleviaing disease- induced inflammation

Term
Misoprostol (Cytotec)
Definition

- mimics the action of prostaglandins PGE1

- protects the stomach from damage caused by chronic use of NSAIDs

Term
colchicine
Definition

- used in acute attacks in gout

- 1mg q2hrs until pain subsides

Term
probenecid (Benemid)
Definition

- increases the renal secretion of uric acid

- it also inhibits the renal excretion of penicillin, increasing its half life

Term
allopurinol (zyloprim)
Definition

- competitive inhibitor of xanthine oxidase

- its converted to alloxanthine which also inhibits the enzyme

- inhibits the metabolism of 6-mercaptopurine (cancer drug)

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