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PDA Block 2 > PDA Block 2 Week 1 > Flashcards

PDA Block 2 Week 1 Flashcards

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
Q

Methotrexate

A

cytotoxic agent

inhibitor of dihydrofolate reductase-inhibits purine synthesis (inhibits DNA synthesis)

used to treat autoimmune disease

hepatic toxicity

26
Q

Mycophenolate Mofetil

A

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
Q

Cyclosporine

A

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
Q

Tacrolimus

A

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
Q

Sirolimus

A

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
Q

Acetylsalicylic Acid/Aspirin

A

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
Q

NSAID Adverse events

A
  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
Q

Ibuprofen

A

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
Q

Naproxen

A

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
Q

Nabumetone

A

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
Q

Indomethacin

A

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
Q

Ketorolac

A

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
Q

Piroxicam

A

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
Q

Sulfasalazine

A

inhibition of production of IL1, TNFa, LO pathway, NFkB inhibition oral drug

“inhibit inflammatoyr response for local GI effect
ulcerative colitis”

Sulfa allergies

39
Q

Celecoxib

A

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
Q

Acetaminophen (tylenol)

A

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
Q

Diphenhydramine

A

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
Q

Dimenhydrinate

A

H1 Blocker; 1st gen “Dramamine: motion sickness
vestibular disturbance”
“Sedation: anti-cholinergic, antihistamine
paradoxal effect on children
GI: nausea, vomiting”

43
Q

Chlorpheniramine

A

H1 Blocker; 1st gen Chlor-trimenton: allergies “Sedation: anti-cholinergic, antihistamine
paradoxal effect on children
GI: nausea, vomiting”

44
Q

Promethazine

A

H1 Blocker; 1st gen “motion sickness
chemo induced nausea” “Sedation: anti-cholinergic, antihistamine
paradoxal effect on children
GI: nausea, vomiting”

45
Q

Fexofenadine

A

H1 Blocker; 2nd gen Terfenadine metabolized to fexofenadine (3A4 & 2P6)

Allegra: allergies

CV effects: no longer prescribed in US

46
Q

Loratadine

A

H1 Blocker; 2nd gen Loratadine metabolized to desloratadine Claritin: allergies

47
Q

Desloratadine

A

H1 Blocker; 2nd gen Loratadine metabolized to desloratadine

Clarinex: allergies no cardiac toxicity

48
Q

Cetirizine

A

H1 Blocker; 2nd gen

active metabolite of hydroxyzine Zyrtec: allergies

higher incidence of sedation than other 2nd gen

49
Q

Cimetidine

A

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
Q

Ranitidine

A

H2 Blocker
inhibits P450 enzymes
Zantac: reduce symptoms of GERD
diarrhea, heaches, drowsiness

51
Q

Famotidine

A

H2 Blocker
Pepcid: reduce symptoms of GERD
diarrhea, heaches, drowsiness

52
Q

Cromolyn sodium

A

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
Q

Omalizumab

A

decrease amount of antigen specific IgE that normally binds and sensitizes mast cells (anti-antibody antibody) subQ

allergic asthma

life threatening anaphylaxis;

PDA Block 2 (3 decks)

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