6- Drugs For Inflammatory And Related Disorders

Question 1

H1 activation leads to ?

Answer 1

1- vasodilatation 
2- increased capillary permeability 
3- bronchoconstriction 
4- increased pain and pruritus 
5- decrease AV nodal conduction

Question 2

H2 activation leads to ?

Answer 2

Increase gastric acid secretion —> increase gastrointestinal ulcer
Positive inotropism

Question 3

H1 antagonists ?

Answer 3

Diphenhydramine 
Promethazine 
Chlorpheniramine 
Meclizine 
Cetirizine 
Loratadine 
Fexofenadine

Question 4

H2 antagonists ? Uses ?

Answer 4

Cimetidine
Ranitidine
Famotidine

PUD
GERD
Zollinger Ellison syndrome

Question 5

Side effects of cimetidine ?

Answer 5

Major inhibitor of P450 isoforms

Decrease androgens —> gynecomastia and decrease libido

Question 6

Antacids ?

Answer 6

Al(OH)3
Mg(OH)2
CaCo3

Question 7

Drugs for nausea and vomiting?

Answer 7

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

Question 8

5HT1 actions ? Drugs acting on it and their use ?

Answer 8

Found in CNS ( inhibitory ) and smooth muscles ( excitatory )

Buspirone : partial 5HT1a agonist , anxiolytic
Sumatriptan : 5HT1d agonist , decrease migraine pain

Question 9

5HT2 receptor actions ? Drugs acting on it and their use ?

Answer 9

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

Question 10

5HT3 receptor site ? Drugs acts on it and their use ?

Answer 10

Found in area postrema , peripheral sensory and enteric nerves

Ondansetron : decrease emesis in chemotherapy , radiation and postoperatively

Question 11

Ergotamine mechanism of action ? Use ?

Answer 11

Partial agonist at both alpha and 5HT2 receptors

Acute migraine attacks

Question 12

Ergonovine mechanism of action ? Use ?

Answer 12

Uterine smooth muscle contraction

IM injection after placental delivery

Question 13

Prophylaxis against migraine headache?

Answer 13

Propranolol
Topiramate
Valproic acid

Question 14

COX 1 and COX 2 site of expression ?

Answer 14

COX 1 : in most tissues including platelets and stomach

COX 2 : in brain and kidney and at sites of inflammation

Question 15

PGE1 drugs ? Uses ?

Answer 15

Misoprostol : ttt of NSAID-induced ulcers

Alprostadil : maintains patency of ductus arteriosus, causes vasodilatation and is used in male impotence

Question 16

PGE2 drug ? Uses ?

Answer 16

Dinoprostone : for cervical ripening and as abortifacient

Question 17

PGF2 alpha drugs ? Uses ?

Answer 17

Carboprost : abortifacient

Latanoprost : ttt of glaucoma

Question 18

PGI2 drug ? Uses ?

Answer 18

Epoprostenol : in pulmonary hypertension

Question 19

PGE2 and PGF2 drugs ?

Answer 19

Therapeutic effects of NSAIDs may be due to inhibition of their synthesis

Question 20

Effect of Aspirin on Uric acid elimination ?

Answer 20

Low to moderate doses : decrease tubular secretion —> hyperuricemia

High doses : decrease tubular reabsorption—> uricosuria

Question 21

Salicylism symptoms ?

Answer 21

Tinnitus
Vertigo
Decrease hearing

Question 22

Renal affection doesnot occur with which type of NSAIDS?

Answer 22

Sulindac

Question 23

Side effects of Indomethacin ?

Answer 23

Thrombocytopenia

Agranulocytosis

Question 24

Side effects of Sulindac ?

Answer 24

Stevens-Johnson syndrome

Hematotoxicity

Question 25

Primary difference between Celecoxib and NSAIDS?

Answer 25

Less git toxicity | Less antiplatelet action

Question 26

There is cross hypersensitivity between Celecoxib and ?

Answer 26

Sulfonamides

Question 27

Ttt of acetaminophen induced hepatotoxicity ?

Answer 27

N-acetylcysteine preferably within the first 12 hours

Question 28

Hydroxychloroquine MOA In treating RA ? SE ?

Answer 28

Stabilizes lysosomes and decrease chemotaxis GI distress Visual dysfunction ( cinchonism ) Hemolysis in G6PD

Question 29

Methotrexate MOA in treating RA ? SE ?

Answer 29

Cytotoxic to lymphocytes Hematotoxicity Hepatotoxicity

Question 30

MOA of Leflunomide ?

Answer 30

Inhibits dihydro-orotic acid dehydrogenase —> decrease UMP —> decrease ribonucleotides —> arrests lymphocytes in G1

Question 31

Etanercept MOA ?

Answer 31

Binds TNF ( a recombinant form of TNF receptor )

Question 32

Infliximab MOA ?

Answer 32

Monoclonal antibody to TNF

Question 33

Anakinar MOA ?

Answer 33

IL-1 receptor antagonist

Question 34

Colchicine MOA ?

Answer 34

Binds to tubulin —> decrease microtubular polymerization Decrease LTB4 Decrease leukocyte and granulocyte migration

Question 35

Allopurinol MOA ?

Answer 35

Inhibit xanthine oxidase —> decrease purine metabolism —> decrease uric acid

Question 36

MOA of pegloticase ?

Answer 36

Recombinant urate-oxidase enzyme for refractory gout , metabolizes uric acid to allantoin —> decrease uric acid

Question 37

Probenecid MOA ?

Answer 37

Inhibits proximal tubular reabsorption of urate

Question 38

Drug for prevention of tumor lysis syndrome ? MOA ?

Answer 38

Rasburicase A recombinant urate oxidase enzyme

Question 39

MOA of glucocorticoids?

Answer 39

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 ```

Question 40

How theophylline cause bronchodiltation ?

Answer 40

Inhibition of PDE —> ⬆️cAMP | Antagonism of adenosine

Question 41

Cromolyn and Nedocromil MOA ?

Answer 41

Prevent degranulation of pulmonary mast cells and ⬇️ release of histamine , PAF and LTC4 from inflammatory cells

Question 42

Inhalation glucocorticoids?

Answer 42

Budesonide | Flunisolide