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91 Cards in this Set

  • Front
  • Back
Prostacyclins
PGE2
PGI2
Cream used to treat Osteoarthritis
Capsaicin cream
Mechanism of action of capsaicin cream
Desensitizes receptors
Aggressive therapy for Rheumatoid Arthritis
Methotrexate
Treatment of gout
Colchicine
2 Drugs to prevent gout
Allopurinol
Probenecid
Enzyme metabolizing Phospholipids to arachidonic acid
Phopholipase A2
Cyclooxygenases produce what two products?
1. Prostaglandins
2. Thromboxanes
PGE and PGI2 effect on blood pressure
Decrease BP
TXA2 effect on blood pressure
Increase BP
PGE and PGI2 effect on coronary vessels
Dilate coronary vessels
TXA2 effect on coronary vessels
Constricts coronary vessels
TXA2 effect on platelet aggregation
Stimulates platelet aggregation
PGI2 (prostacyclin) effect on platelet aggregation
Inhibits platelet aggregation
Drug used to maintain patency of patent ductus arteriosus
Alprostadil (PGE1)
To maintain maternal/fetal blood flow
PGE and PGI2 effects on renal vessels
Renal vasodilation
PGE and PGI2 effects on renin
Increase renin release
PGE and PGI2 effects on bronchioles
Dilation of bronchioles
TXA2 and PGF2alpha effects on bronchioles
Constricts bronchioles
PGE2 and PGI2 effect on gastric acid secretion
Inhibits gastric acid secretion
Protective of gut
PGE and PGI2 effect on mucous secretions in gut
Increased mucous secretions in gut
Misoprostol
PGE1 analog
Promote ulcer healing
Gastric protection
PGE2 effects on non pregnant uterus
Relax non-pregnant uterus
PGE2 effect on pregnant uterus
Contract pregnant uterus
PGF2alpha effect on nonpregnant uterus
Contracts non-pregnant uterus
PGF2alpha effect on pregnant uterus
Contracts pregnant uterus
PGF2alpha effect on corpus luteum
Lysis of corpus luteum
PGE2 and PGF2alpha main use in childbirth:
Control post-partum hemorrhage
Carboprost tromethamine
Drug for parturition
Dinoprostone
Induce labor by promoting ripening and dilation of cervix
PGE2
Central administration of PGs into hypothalamus induces what?
Fever
Improve harvesting and storage of platelets
PGG
PGI2
Epoprostenol
PGI2
Dilate pulmonary vessels
Alprostadil
Maintenance of PDA
PGE2
Zafirlukast
LTC4 and LTD4 actions blocked at cys-LT1 receptor
LT receptor antagonist
Treatment of asthma
Montelukast
LTC4 and LTD4 actions blocked at cys-LT1 receptor
LT receptor antagonist
Treatment of asthma
Activation of what receptor by Leukotrienes causes bronchoconstriction
cys-LT1 receptor
Which pathway of AA metabolism produces leukotrienes
Lipoxygenase pathway
Why no tolerance development with ASA?
Binding enzyme activity
NSAIDS block what enzymes?
COX1 and COX2
NSAIDS treat what part of the diseas?
Only the symptoms, not the underlying cause of disease
ASA is purified from what plant?
Willow bark
81 mg baby ASA administered for:
MI prophylaxis by reducing platelet aggregation
ASA must be avoided in which subset of women?
Pregnant in 3rd trimester
ASA can cause what disease in children/young adults?
Reyes Syndrome
Respiratory effect of toxic ASA
True metabolic acidosis
Directly depresses respiration causes increase in CO2
Displacement of bicarbonate
Decreased excretion of organic acids
Respiratory effect of therapeutic dose of ASA
Respiratory alkalosis
Directly stimulates respiration causes increased O2 consumption and CO2 production
Compensate with increased renal excretion of bicarbonate
APAP does/does not have anti-inflammatory actions
Does not have anti-inflammatory actions
APAP
Analgesic and Antipyretic
Overdose of APAP leads to
Fatal hepatic necrosis
Liver toxicity
Liver toxicity with APAP can occur in what conditions of glutathione?
Low glutathione
Produces free radical adduct that destroys hepatocytes
Treatment of APAP poisoning
N-acetylcysteine
Recycles glutathione
Cox2 is constitutive or inducible?
Inducible
Cox1 is constitutivce or inducible?
Constitutive
2 functions of Cox1
1. Electrolyte balance in kidney
2. Cytoprotection of gastric mucosa
Function of Cox2
Induced inflammation
Celecoxib
COX2 inhibitor
Sulfa containing (CI in Sulfa sensitive patients)
Side effect of COX2 inhibitors
Increased MI's
COX2 produces what in endothelial cells?
Prostacyclin (PGE2, PGI2)
Effects of prostacyclin induced by COX2 (2 effects)
1. Vasodilation
2. Block platelet aggregation
COX1 produces what in platelets
Thromboxanes (TXA2)
Effect of TXA2 induced by COX1 (2 effects)
1. Vasoconstriction
2. Platelet aggregation
Disease Modifying Antirheumatic Drugs (DMARDS): List 4
1. Azathioprine
2. Methotrexate
3. Leflunomide
4. Penicillamine
Mechanism of action of DMARDS
Anti-cancer drugs therefore suppress cellular proliferation
Serious side effect of DMARDS
Infection secondary to immunosuppression
DMARDS does/does not treat the underlying disease
Yes
Attenuate both inflammation and destructive process
DMARDS can/cannot be used continuously?
Must be stopped in 1-2 years (2-4 for MTX)
NSAIDS can/cannot be used continuously?
Can be used continuously b/c bind to enzymes
Biological modifiers are/are not disease modifying drugs
Yes they are disease modifying drugs
Infiximab
TNFalpha chimeric monoclonal antibody
Etanercept
Construct of TNFalpha receptor (False receptor)
Adalimumab
TNFalpha human monoclonal antibody
Anakinra
IL-1beta receptor antagonist
Abatacept
Costimulation modulator; fusion protein to CD4
Rituximab
Monoclonal antibody to CD20 on B cells
Major side effect of biological modifiers and DMARDS
Infection secondary to immunosuppression
Gold compounds used in treatment of what disease?
Rheumatoid arthritis
Auranofin
gold compound
Aurothioglucose
Gold compound
Gold sodium thiomalate
Gold compound
2 causes of Hyperuricemia
1. Increased Uric acid production
2. Decreased Uric acid excretion
Prostacyclins
PGE2
PGI2
Neurons in peripheral sensitization
Small diameter sensory neurons
Eicosanoids
Oxygenated C20 fatty acids that are metabolites of arachidonic acid (5,8,11,14 eicosatretraenoic acid)
Two major pathways in arachidonic acid breakdown
1. Cyclooxygenase
2. Lipoxygenase
Metabolic products of cyclooxygenase
Prostaglandins
Thromboxanes
Prostacyclin
Metabolic products of lipoxygenases
Leukotrienes
HPETEs
HETEs
Lipoxins
Phospholipid --> Arachidonic Acid (Enzyme?)
Phospholipase A2
ASA reversibly/irreversibly blocks COX enzyme?
Irreversibly blocks
Lipoxygenase found mostly where?
Central Nervous System
Eicosanoids are paracrine/autocrine/endocrine hormones?
Paracrine/Autocrine
Are not stored, but synthesized on demand in response to hormones, drugs, or stressors