6- Drugs For Inflammatory And Related Disorders Flashcards
H1 activation leads to ?
1- vasodilatation 2- increased capillary permeability 3- bronchoconstriction 4- increased pain and pruritus 5- decrease AV nodal conduction
H2 activation leads to ?
Increase gastric acid secretion —> increase gastrointestinal ulcer
Positive inotropism
H1 antagonists ?
Diphenhydramine Promethazine Chlorpheniramine Meclizine Cetirizine Loratadine Fexofenadine
H2 antagonists ? Uses ?
Cimetidine
Ranitidine
Famotidine
PUD
GERD
Zollinger Ellison syndrome
Side effects of cimetidine ?
Major inhibitor of P450 isoforms
Decrease androgens —> gynecomastia and decrease libido
Antacids ?
Al(OH)3
Mg(OH)2
CaCo3
Drugs for nausea and vomiting?
1- 5HT3 antagonists : Ondansetron , Granisetrone
2- DA antagonists : prochlorpromazine , metoclopramide
3- H1 antagonists : diphenhydramine, Meclizine, Promethazine
4- Muscarinic antagonists : Scopolamine
5- Cannabinoids : dronabinol
6- NK1-receptor antagonist : aprepitant
5HT1 actions ? Drugs acting on it and their use ?
Found in CNS ( inhibitory ) and smooth muscles ( excitatory )
Buspirone : partial 5HT1a agonist , anxiolytic
Sumatriptan : 5HT1d agonist , decrease migraine pain
5HT2 receptor actions ? Drugs acting on it and their use ?
Found in CNS ( excitatory )
Found in periphery ( vasodilatation, contraction of git and bronchial and uterine smooth muscle , platelet aggregation )
Olanzapine : 5HT2a antagonist in the CNS , used in psychosis
Cyproheptadine : 5HT2 antagonist , used in carcinoid syndrome and gastrointestinal tumors and postgastrectomy and anorexia nervosa
Has marked H1-blocking action so used in seasonal allergies
5HT3 receptor site ? Drugs acts on it and their use ?
Found in area postrema , peripheral sensory and enteric nerves
Ondansetron : decrease emesis in chemotherapy , radiation and postoperatively
Ergotamine mechanism of action ? Use ?
Partial agonist at both alpha and 5HT2 receptors
Acute migraine attacks
Ergonovine mechanism of action ? Use ?
Uterine smooth muscle contraction
IM injection after placental delivery
Prophylaxis against migraine headache?
Propranolol
Topiramate
Valproic acid
COX 1 and COX 2 site of expression ?
COX 1 : in most tissues including platelets and stomach
COX 2 : in brain and kidney and at sites of inflammation
PGE1 drugs ? Uses ?
Misoprostol : ttt of NSAID-induced ulcers
Alprostadil : maintains patency of ductus arteriosus, causes vasodilatation and is used in male impotence
PGE2 drug ? Uses ?
Dinoprostone : for cervical ripening and as abortifacient
PGF2 alpha drugs ? Uses ?
Carboprost : abortifacient
Latanoprost : ttt of glaucoma
PGI2 drug ? Uses ?
Epoprostenol : in pulmonary hypertension
PGE2 and PGF2 drugs ?
Therapeutic effects of NSAIDs may be due to inhibition of their synthesis
Effect of Aspirin on Uric acid elimination ?
Low to moderate doses : decrease tubular secretion —> hyperuricemia
High doses : decrease tubular reabsorption—> uricosuria
Salicylism symptoms ?
Tinnitus
Vertigo
Decrease hearing
Renal affection doesnot occur with which type of NSAIDS?
Sulindac
Side effects of Indomethacin ?
Thrombocytopenia
Agranulocytosis
Side effects of Sulindac ?
Stevens-Johnson syndrome
Hematotoxicity
Primary difference between Celecoxib and NSAIDS?
Less git toxicity
Less antiplatelet action
There is cross hypersensitivity between Celecoxib and ?
Sulfonamides
Ttt of acetaminophen induced hepatotoxicity ?
N-acetylcysteine preferably within the first 12 hours
Hydroxychloroquine MOA In treating RA ? SE ?
Stabilizes lysosomes and decrease chemotaxis
GI distress
Visual dysfunction ( cinchonism )
Hemolysis in G6PD
Methotrexate MOA in treating RA ? SE ?
Cytotoxic to lymphocytes
Hematotoxicity
Hepatotoxicity
MOA of Leflunomide ?
Inhibits dihydro-orotic acid dehydrogenase —> decrease UMP —> decrease ribonucleotides —> arrests lymphocytes in G1
Etanercept MOA ?
Binds TNF ( a recombinant form of TNF receptor )
Infliximab MOA ?
Monoclonal antibody to TNF
Anakinar MOA ?
IL-1 receptor antagonist
Colchicine MOA ?
Binds to tubulin —> decrease microtubular polymerization
Decrease LTB4
Decrease leukocyte and granulocyte migration
Allopurinol MOA ?
Inhibit xanthine oxidase —> decrease purine metabolism —> decrease uric acid
MOA of pegloticase ?
Recombinant urate-oxidase enzyme for refractory gout , metabolizes uric acid to allantoin —> decrease uric acid
Probenecid MOA ?
Inhibits proximal tubular reabsorption of urate
Drug for prevention of tumor lysis syndrome ? MOA ?
Rasburicase
A recombinant urate oxidase enzyme
MOA of glucocorticoids?
Cellular :
1- ⬇️ leucocyte migration
2- ⬆️ lysosomal membrane stability —> ⬇️ phagocytosis
3- ⬇️ capillary permeability
Biochemical actions : 1- inhibit PLA2 —> ⬇️ PGs and ⬇️ LTs 2- ⬇️ expression of COX2 3- ⬇️ platelet activating factor 4- ⬇️ interleukins
How theophylline cause bronchodiltation ?
Inhibition of PDE —> ⬆️cAMP
Antagonism of adenosine
Cromolyn and Nedocromil MOA ?
Prevent degranulation of pulmonary mast cells and ⬇️ release of histamine , PAF and LTC4 from inflammatory cells
Inhalation glucocorticoids?
Budesonide
Flunisolide
