PDA Block 2 Week 1 Flashcards

(53 cards)

1
Q

Etanercept

A
Cytokine	
interfers with TNF (fused to Fc fragment of IgG--> suicide inhibitor by binding TNF) (acute rxn, fever, sepsis)	
Autoimmune disease (Rheumatoid arthritis & Crohn's disease)
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2
Q

Infliximab

A

Cytokine

MAB against TNF Autoimmune disease (Rheumatoid arthritis & Crohn’s disease)

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3
Q

Zileuton

A

Leukotrienes
5-lipoxygenase inhibitor (inhibits synthesis of leukotrienes)
metabolism: CYP 1A1, 2C9, 3A4

propylactic treatment of mild asthma

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4
Q

Zafirlukast

A

Leukotrienes competitive leukotriene
Receptor antagonist: inhibit cys-LTs to increase vascular permeability; chemotaxis (LTB4); decrease bronchoconstriction

Metabolism: CYP 2C9

propylactic and chronic treatment of mild askthma

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5
Q

Steroid

A

glucocorticoids
binds cytoplasmic R–> transcription –> inhibit cytokines, phospholipase A2, COX2, and CAM

chronic inflammatory disease

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6
Q

dinoprostone

A

PGE2 analog
“1. Gel: promotes cervical ripening, relax cervical muscles (E4R)
2. suppository: pregnancy termination (EP1/3R)- uterine contraction”

GI related, fever, uterine rupture

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7
Q

carboprost

A

PGF2a analong
IM injection
1. termination of pregnancy at FP R
2. control post-partum hemorrhage

GI related, fever, uterine rupture

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8
Q

misoprostol

A

PGE1 analog
oral replacement therapy for prevention of ulcers cased by NSAIDS by suppressing gastric acid secretion & increase mucus

diarrhea, contraindicated in pregnancy

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9
Q

alprostadil

A

PGE1 analog
1. Intracavernous injection
increase cAMP–> relax smooth muscle in erectile dyfunction
2. IV: maintenance of patent ductus arteriosus (relaxation of muscle)

Adverse:

  1. priapism: prolonged erection
  2. apnea
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10
Q

epoprostenol

A

PGEI2 analog
IV: primary pulmonary HTN (cAMP mediated dilation of pulmonary vascular Smooth m.)

Nausea, vomiting, headache, flushing

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11
Q

bimatoprost

A

PGF2a analog

  1. Glaucoma (increase outflow of aqueous humor)
  2. eyelash hypotrichosis (increase length and number of eyelashes)

Adverse

  1. eye redness, itching
  2. excess unwanted hair growth, brown pigmentation, redness, itching”
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12
Q

Aldosterone

A
Steroid	
"adrenal insufficiency
allergic disease
inflammatory disease
cerebral edema"	

“dose is variable
single dose usually does not have harmful effect
used to treat symptoms

abrupt discontinuation may cause adrenal insufficiency” Contraindication: existing infection

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13
Q

Cortisol

A

Steroid
adrenal insufficiency, inflammation, immunosuppresant
1. dose is variable
2. single dose usually does not have harmful effect
3. used to treat symptoms
4. abrupt discontinuation may cause adrenal insufficiency

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14
Q

Dexamethasone

A

Steroid
adrenal insufficiency, inflammation, immunosuppresant
1. dose is variable
2. single dose usually does not have harmful effect
3. used to treat symptoms
4. abrupt discontinuation may cause adrenal insufficiency

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15
Q

Prednisolone

A

Steroid
adrenal insufficiency, inflammation, immunosuppresant
1. dose is variable
2. single dose usually does not have harmful effect
3. used to treat symptoms
4. abrupt discontinuation may cause adrenal

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16
Q

Fludrocortisone

A

Steroid
adrenal insufficiency, inflammation, immunosuppresant
1. dose is variable
2. single dose usually does not have harmful effect
3. used to treat symptoms
4. abrupt discontinuation may cause adrenal

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17
Q

Metyrapone

A

Steroid synthesis inhibitor

Blocks 11 Beta hydroxylation –> 11-desoxycortisol does not inhibit ACTH release via neg. feedback–> increase synthesis of 17 hydroxycorticoids (excreted)

Used as a diagnostic test for renal function

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18
Q

Mifepristone

A

competitive antagonist at progesterone and glucocorticoid R

Terminate pregnancy; treat Cushings

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19
Q

Spironolactone

A

competitive antagonist at mineralcorticoid R

Diuretic, treat HTN, cardiac hypertrophy and heart failure

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20
Q

Eplerenone

A

competitive antagonist at mineralcorticoid R

Diuretic, treat HTN, cardiac hypertrophy and heart failure

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21
Q

Drospirenone

A
  1. progesterone R agonist: suppress ovulation, hormone replacement therapy with estrogen
  2. mineralcorticoid R antagonist: diuretic
  3. androgen R antagonist
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22
Q

Prednisolone

A

corticosteroid

  1. cell traffic/accumulation decreased
  2. interferes with antigen processing, inhibits binding to Fc receptors

used in combination with other drugs to prevent transplant rejection and some autoimmune disease

contraindicated: existing infection

23
Q

Azathioprine

A

cytotoxic agent

Metabolized to 6-mercaptopurine–> inhibits De Novo and Salvage pathway

used to inhibit rejection of transplanted organs,

bone marrow depression, BI and hepatic toxicity

24
Q

Cyclophosphamide

A

cytotoxic agent

alkalating agent that results in cross-linking DNA to kill replicating and non -replicating cell

Used for treating autoimmune disease
NOT effective for graft rejection

bone marrow depression

25
Methotrexate
cytotoxic agent inhibitor of dihydrofolate reductase-inhibits purine synthesis (inhibits DNA synthesis) used to treat autoimmune disease hepatic toxicity
26
Mycophenolate Mofetil
cytotoxic agent "metabolized to mycophenolic acid inhibits IMP dehydrogenase --> inhibits de novo purine synthesis. No effect of salvage (selective for lymphocytes)--> inhibits lymphocyte proliferation and expression of cell surface adhesion molecules." "used with cyclosporine/ corticosteroids to prevent renal allograft rejection used to treat autoimmune disease" "use w/ caution: active GI disease, reduced renal function/infection side effects: infection,leukopenia, anemia do not use in pregnancy
27
Cyclosporine
cyclosporine-like binds to cellular receptor and inhibts ca dependent phosphatase (calcinurin)--> blocks NFAT for IL2 production--> blocks helper T cell function used to prevent transplant rejection nephrotoxicity
28
Tacrolimus
cyclosporine-like Binds FK binding protein--> inhibts ca dependent phosphatase (calcinurin)--> blocks NFAT for IL2 production--> blocks helper T cell function used to prevent transplant rejection less nephrotoxicity and hepatotoxicity than cyclosporine
29
Sirolimus
cyclosporine-like inhibits T cell acitivtion and proliferation. Binds FKBP12--> binds mTOR (kinase in cell cycle progression) used to prevent transplant rejection; coating of cardiac stents
30
Acetylsalicylic Acid/Aspirin
Irreversible inhibitor of COX by acetylation of serine group of COX "anti-inflammatory, antipyretic, analgesia Other effects NOT from COX: 1. uric acid excretion (low dose=block secretion of uric acid; high dose-increases secretion of uric acid) 2.CNS: BBB (delirium)- high dose 3. Respiration: increase RR" Fever, low intensity pain, inflammatory disorders, cancer, anti-platelet for CV
31
NSAID Adverse events
1. GI: gastric irritation--> gastric ulcers and bleeding (inhibits COX1) 2. Blood: increase bleeding time (inhibits COX1 in platelets) 3. Hypersensitivity: bronchoconstriction, edema(Leukotrienes from shunting) 4. Renal: decreased renal blood flow--> water/water rention (COX1 vasodilation) 5. pregnancy: decrease uterine contraction (inhibit PG for contractions) 6. Ductus Arteriosus: maintains patent DA 7. Salicylism: aspirin OD--> saturation of metabolic enzymes --> 0 order kinetics 8. Reye's syndrome: related to viral epidemics (seen in children)
32
Ibuprofen
reversible inhibitor of COX-1 and COX2 Half life is 2 hours "inflammatory disease, rheumatoid disorders, pain, fever, osteoarthritis, dysmenorrhea lysine injection to induce patent ductus arteriosus GI effects, hypersensitivity, kidney, blood, drug interactions
33
Naproxen
reversible inhibitor of COX-1 and COX2 Half life is 14 hours ankylosing sponylitis, osteoarthritis, rheumatoid disoder, pain, tendonitis, bursitis, dysmenorrhea, fever, acute gout GI effects, hypersensitivity, kidney, blood, drug interactions
34
Nabumetone
reversible inhibitor of COX-1 and COX2 (mostly COX2) Pro-drug: converted to active metabolite; long half life osteoarthritis, rheumatoid arthritis well tolerated, less GI effects
35
Indomethacin
reversible inhibitor of COX-1 and COX2 Half life is 3 hours; 90% bound to plasma protein "acute gout arthritis, acute bursitis/tendonitis, rhematoid arthritis, ankylosing spondylitis, closure of patent ductus arteriosus Not routinely used to treat pain/fever"
36
Ketorolac
reversible inhibitor of COX-1 and COX2 highly plasma protein bound oral/injection for short term management of moderate to severe acute pain requiring analgesia at opiod level
37
Piroxicam
reversible inhibitor of COX-1 and COX2 half life = 50 hours; 99% bound to plasma symptomatic treatment of acute and chronic rheumatoid arthritis and osteoarthritis GI toxicity
38
Sulfasalazine
inhibition of production of IL1, TNFa, LO pathway, NFkB inhibition oral drug "inhibit inflammatoyr response for local GI effect ulcerative colitis" Sulfa allergies
39
Celecoxib
reversible inhibitor of COX2 (binds to distinct hydrophilic side pocket region) metabolized by CYP2C9 symptoms of rheumatoid arthritis; primary dysmenorrhea; acute pain; "hypersensitivity increased risk of GI irritation, ulceration increased risl of adverse CV thrombotic events anemia (rare) contraindications: sulfonamide toxicity; CV risk factors; GI disease; do not use in patients after coronary heart disease; CYP2C9 deficiency"
40
Acetaminophen (tylenol)
inhibits COX1 and COX2 half life= 2 hours, little binding to plasma proteins; renal excretion. Metabolized by phase II enzymes. Minor metabolism by Phase I (CYP 2E1) analgesic, antipyretic. NOT anti-inflammatory OD:depleted glutathione--> toxicity (treat with N-acetylcysteine)-glutathione substitute
41
Diphenhydramine
H1 Blocker; 1st gen " Benadryl: allergies motion sickness sleeping tablet early stage parkinson's" "Sedation: anti-cholinergic, antihistamine paradoxal effect on children GI: nausea, vomiting"
42
Dimenhydrinate
H1 Blocker; 1st gen "Dramamine: motion sickness vestibular disturbance" "Sedation: anti-cholinergic, antihistamine paradoxal effect on children GI: nausea, vomiting"
43
Chlorpheniramine
H1 Blocker; 1st gen Chlor-trimenton: allergies "Sedation: anti-cholinergic, antihistamine paradoxal effect on children GI: nausea, vomiting"
44
Promethazine
H1 Blocker; 1st gen "motion sickness chemo induced nausea" "Sedation: anti-cholinergic, antihistamine paradoxal effect on children GI: nausea, vomiting"
45
Fexofenadine
H1 Blocker; 2nd gen Terfenadine metabolized to fexofenadine (3A4 & 2P6) Allegra: allergies CV effects: no longer prescribed in US
46
Loratadine
H1 Blocker; 2nd gen Loratadine metabolized to desloratadine Claritin: allergies
47
Desloratadine
H1 Blocker; 2nd gen Loratadine metabolized to desloratadine | Clarinex: allergies no cardiac toxicity
48
Cetirizine
H1 Blocker; 2nd gen active metabolite of hydroxyzine Zyrtec: allergies higher incidence of sedation than other 2nd gen
49
Cimetidine
H2 Blocker inhibits P450 enzymes--> prolongs half life of other drug substrates of p450 Tagamet: reduce symptoms of GERD long term use--> gynecomastia, impotence
50
Ranitidine
H2 Blocker inhibits P450 enzymes Zantac: reduce symptoms of GERD diarrhea, heaches, drowsiness
51
Famotidine
H2 Blocker Pepcid: reduce symptoms of GERD diarrhea, heaches, drowsiness
52
Cromolyn sodium
inhibit histamine release (stabilizes mast cell membranes and prevents release of histamines) inhaled used for preventive management of asthma, allergic rhinitis, conjuctivitis" safe/few side effects
53
Omalizumab
decrease amount of antigen specific IgE that normally binds and sensitizes mast cells (anti-antibody antibody) subQ allergic asthma life threatening anaphylaxis;