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Prostaglandin synthesis
-Prostaglandin modulate some components of:
-_______
-_______temperature
-_______ temperature
-platelet aggregation (formation of _______)
-prostaglandins come from _______ Acid which is liberated from cells in response to _______, _______, _______, _______ & other stimuli.
Prostaglandin synthesis
- -Prostaglandin modulate some components of:
- -inflammation
- -body temperature
- -pain temperature
- -platelet aggregation (formation of platelet plugs)
- -prostaglandins come from Arachidonic Acid which is liberated from cells in response to physical, chemical, hormonal,bacteria & other stimuli.
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Prostaglandin Synthesis
-Prostaglandin is the result of conversion from ________ acid by the enzyme ________ (COX)
-In order for prostaglandin to be made ________ acid must be metabolized through ________ (an enzyme)
-There are two forms of cyclooxygenase (COX)
-1. COX I- which is found in ________ cells
-2. COX II- which is found in ________ cells
-There are a variety of prostaglandins implicated in the _______ associated with inflammation. However, the key ones are PGE1 & PGE 2
Prostaglandin Synthesis
- -Prostaglandin is the result of conversion from Arachidonic acid by the enzyme cyclooxygenase (COX)
- -In order for prostaglandin to be made arachidonic acid must be metabolized through cyclooxygenase (an enzyme)
- -There are two forms of cyclooxygenase (COX)
- -1. COX I- which is found in non-inflamed cells
- -2. COX II- which is found in inflamed cells
- -There are a variety of prostaglandins implicated in the pain associated with inflammation. However, the key ones are PGE1 & PGE 2
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Prostaglandins
-Prostaglandins are needed for normal cell _____
-Current NSAIDS inhibit COX __ as much as or more than they inhibit COX __
-When NSAIDS inhibit _____ cells the stores of prostaglandins are _____ and normal cell function is _____
-The action of NSAIDS accounts for numerous _____ effect of the drugs.
Prostaglandins
- -Prostaglandins are needed for normal cell functions
- -Current NSAIDS inhibit COX I as much as or more than they inhibit COX II
- -When NSAIDS inhibit non-inflammatory cells the stores of prostaglandins are depleted and normal cell function is disrupted.
- -The action of NSAIDS accounts for numerous adverse effect of the drugs.
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NSAIDS
-1. ________
-Prototype: ________
-Variety of________ uses
-used for ________ to ________ pain
-Interferes with prostaglandin synthesis by irreversibly inhibiting ________
-Causes bleeding by interfering with ________ cascade.
NSAIDS
- -1. Salicylates
- -Prototype: Aspirin
- -Variety of therapeutic uses
- -used for mild to moderate pain -Interferes with prostaglandin synthesis by irreversibly inhibiting COX
- -Causes bleeding by interfering with coagulation cascade.
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Salicylates
-Contraindicated in children with ___ illness including chicken pox (___) or flu-like illness due to association with ___ Syndrome.
Salicylates
-Contraindicated in children with viral illness including chicken pox (varicella) or flu-like illness due to association with Reye's Syndrome.
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Salicylates
-Adverse Effects
-A. Salicylism: Mild _______ toxicity seen either in long term use of high dose _______ therapy
-B. Salicylate Poisoning:
- ______-threatening
-no _______
-syrup of _______
-Treatment includes gastric _______
-activated _______
-S &S: High _______ and _______
Salicylates
- -Adverse Effects
- -A. Salicylism: Mild aspirin toxicity seen either in long term use of high dose aspirin therapy -
- B. Salicylate Poisoning:
- -Life-threatening
- -no antidote-syrup of ipecac
- -Treatment includes gastric lavage
- -activated charcoal
- -S &S: High fever and coma
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NSAIDS CONTINUED
-2. _______ Synthetase Inhibitors (PSI)
-Prototype: _______
-Sub group of NSAIDS
-PSI'S are group by _______ synthesis
-Chronic use can --> _______, _______ & ___ bleed.
-Contraindicated in those with a history of _______ disease
-Used with caution in _______, _______ or _______ disease.
NSAIDS CONTINUED
- -2. Prostaglandin Synthetase Inhibitors (PSI)
- -Prototype: Ibuprophen
- -Sub group of NSAIDS
- -PSI'S are group by chemical synthesis
- -Chronic use can --> gastritis, ulceration & GI bleed.
- -Contraindicated in those with a history of GI disease
- -Used with caution in hematopoetic, hepatic or renal disease.
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Disease Modifying Antirheumatoid Drugs
-Used when _______ are not tolerated or a ineffective.
-Called _______ because they can arrest the progression of rheumatoid arthritis & induce _______ in some patients.
-Also known as Slow Acting Antirheumatic Drugs (SAARDS) because of the _______ in achieving a response.
Disease Modifying Antirheumatoid Drugs
- -Used when PSI'S are not tolerated or a ineffective.-Called DEMARDS because they can arrest the progression of rheumatoid arthritis & induce remission in some patients.
- -Also known as Slow Acting Antirheumatic Drugs (SAARDS) because of the delay in achieving a response.
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DMARDS
-most common DMARDS are gold salts _________ (an antineoplastic used for a variety of _________ disorders)
-The major disadvantages induce:
-______ onset of action
-______ in achieving a therapeutic response
-potential for serious _______ & even _____ reactions
-prototype : ________ (_______ - gold salt)
DMARDS
- -most common DMARDS are gold salts methotrexate (an antineoplastic used for a variety of malignant disorders)
- -The major disadvantages induce:
- -slow onset of action
- -delay in achieving a therapeutic response
- -potential for serious adverse & even fatal reactions
- -prototype : auranofin (Ridaura - gold salt)
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Gold Salt Theory
-Adminstration of gold salts is called ________
-________ contains 29% gold
-mechanism of actions is ________
-chrysotherapy can produce serious,______ reactions
-most serious effect is lethal ____ ____ suppression
-most common effect is ________
-gold can deposit in the ________ -> skin pigment changes ________ to ________ coloration
-can cause ________ syndrome.
Gold Salt Theory
- -Adminstration of gold salts is called chrysotherapy
- -Auranofin contains 29% gold
- -mechanism of actions is unknown
- -chrysotherapy can produce serious, toxic reactions
- -most serious effect is lethal bone marrow suppression
- -most common effect is diarrhea
- -gold can deposit in the tissue -> skin pigment changes grey to blue coloration
- -can cause nephrotic syndrome.
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Anti-gout
-gout is aka the rich man's disease because it is associated with a diet high in _______ (_______ cream, _______ meats)
-prototype: _______
-used to treat gout since 1763
-Colchicine_______ leukocyte phagocytosis which inhibit further _______ deposits
-Contraindicated in patients with severe_______ , _______or _______ disease due to risk of cumulative toxicity
-most adverse effect is ____
-S&S that must be reported immediately include:
-fever, chills, sore throat, difficulty _______ & muscle _______ (drug cause _______)
Anti-gout
- -gout is aka the rich man's disease because it is associated with a diet high in purines (whipped cream, organ meats)
- -prototype: Colchicine-used to treat gout since 1763
- -Colchicine opposed leukocyte phagocytosis which inhibit further urate deposits
- -Contraindicated in patients with severe heart , liver or kidney disease due to risk of cumulative toxicity
- -most adverse effect is GI
- -S&S that must be reported immediately include:
- -fever, chills, sore throat, difficulty breathing & muscle weakness (drug cause myoneuropathy)
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Uricosurics
-prototype: _______ (_______)
-Used in _______ gout
-keeps the uric acid level _______ saturation to prevent the formation of uric _______
-must not be used during _______ attacks since it can _______ the anti- inflammatory response
-contraindicated in patients with uric acid _______ and bone marrow _______
-should not be used in ______ impairment
-probenecid reduce renal failure secretion of many drugs -> _______ -> toxicites
Uricosurics
- -prototype: probenecid (Benmid)
- -Used in chronic gout
- -keeps the uric acid level below saturation to prevent the formation of uric crystals
- -must not be used during acute attacks since it can prolong the anti- inflammatory response
- -contraindicated in patients with uric acid stones and bone marrow depression
- -should not be used in renal impairment
- -probenecid reduce renal failure secretion of many drugs -> accumulation -> toxicites
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