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Pharmacology > 6- Drugs For Inflammatory And Related Disorders > Flashcards

6- Drugs For Inflammatory And Related Disorders Flashcards

1
Q

H1 activation leads to ?

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

H2 activation leads to ?

A

Increase gastric acid secretion —> increase gastrointestinal ulcer
Positive inotropism

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3
Q

H1 antagonists ?

A 
Diphenhydramine 
Promethazine 
Chlorpheniramine 
Meclizine 
Cetirizine 
Loratadine 
Fexofenadine
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4
Q

H2 antagonists ? Uses ?

A

Cimetidine
Ranitidine
Famotidine

PUD
GERD
Zollinger Ellison syndrome

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5
Q

Side effects of cimetidine ?

A

Major inhibitor of P450 isoforms

Decrease androgens —> gynecomastia and decrease libido

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6
Q

Antacids ?

A

Al(OH)3
Mg(OH)2
CaCo3

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7
Q

Drugs for nausea and vomiting?

A

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

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8
Q

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

A

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

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

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9
Q

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

A

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

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10
Q

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

A

Found in area postrema , peripheral sensory and enteric nerves

Ondansetron : decrease emesis in chemotherapy , radiation and postoperatively

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11
Q

Ergotamine mechanism of action ? Use ?

A

Partial agonist at both alpha and 5HT2 receptors

Acute migraine attacks

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12
Q

Ergonovine mechanism of action ? Use ?

A

Uterine smooth muscle contraction

IM injection after placental delivery

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13
Q

Prophylaxis against migraine headache?

A

Propranolol
Topiramate
Valproic acid

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14
Q

COX 1 and COX 2 site of expression ?

A

COX 1 : in most tissues including platelets and stomach

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

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15
Q

PGE1 drugs ? Uses ?

A

Misoprostol : ttt of NSAID-induced ulcers

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

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16
Q

PGE2 drug ? Uses ?

A

Dinoprostone : for cervical ripening and as abortifacient

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17
Q

PGF2 alpha drugs ? Uses ?

A

Carboprost : abortifacient

Latanoprost : ttt of glaucoma

18
Q

PGI2 drug ? Uses ?

A

Epoprostenol : in pulmonary hypertension

19
Q

PGE2 and PGF2 drugs ?

A

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

20
Q

Effect of Aspirin on Uric acid elimination ?

A

Low to moderate doses : decrease tubular secretion —> hyperuricemia

High doses : decrease tubular reabsorption—> uricosuria

21
Q

Salicylism symptoms ?

A

Tinnitus
Vertigo
Decrease hearing

22
Q

Renal affection doesnot occur with which type of NSAIDS?

A

Sulindac

23
Q

Side effects of Indomethacin ?

A

Thrombocytopenia

Agranulocytosis

24
Q

Side effects of Sulindac ?

A

Stevens-Johnson syndrome

Hematotoxicity

25
Q

Primary difference between Celecoxib and NSAIDS?

A

Less git toxicity

Less antiplatelet action

26
Q

There is cross hypersensitivity between Celecoxib and ?

A

Sulfonamides

27
Q

Ttt of acetaminophen induced hepatotoxicity ?

A

N-acetylcysteine preferably within the first 12 hours

28
Q

Hydroxychloroquine MOA In treating RA ? SE ?

A

Stabilizes lysosomes and decrease chemotaxis

GI distress
Visual dysfunction ( cinchonism )
Hemolysis in G6PD

29
Q

Methotrexate MOA in treating RA ? SE ?

A

Cytotoxic to lymphocytes

Hematotoxicity
Hepatotoxicity

30
Q

MOA of Leflunomide ?

A

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

31
Q

Etanercept MOA ?

A

Binds TNF ( a recombinant form of TNF receptor )

32
Q

Infliximab MOA ?

A

Monoclonal antibody to TNF

33
Q

Anakinar MOA ?

A

IL-1 receptor antagonist

34
Q

Colchicine MOA ?

A

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

35
Q

Allopurinol MOA ?

A

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

36
Q

MOA of pegloticase ?

A

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

37
Q

Probenecid MOA ?

A

Inhibits proximal tubular reabsorption of urate

38
Q

Drug for prevention of tumor lysis syndrome ? MOA ?

A

Rasburicase

A recombinant urate oxidase enzyme

39
Q

MOA of glucocorticoids?

A

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
40
Q

How theophylline cause bronchodiltation ?

A

Inhibition of PDE —> ⬆️cAMP

Antagonism of adenosine

41
Q

Cromolyn and Nedocromil MOA ?

A

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

42
Q

Inhalation glucocorticoids?

A

Budesonide

Flunisolide

Pharmacology (9 decks)

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