Prostaglandins Flashcards

1
Q

What has been identified as the main prostaglandin that causes redness, swelling, & pain?

A

PGE2

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2
Q

What is the treatment for open angle glaucoma and eyelash hypertrichosis?

A

Latanoprost

- darkens and elongates eyelashes

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3
Q

COX1 vs COX2 which are always present in the blood?

A

COX1 are always present - help maintain gastric lining

COX2 are induced & just appear

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4
Q

What is COX2 important for?

A

Synthesizing the prostaglandin mediators of PAIN, INFLAMMATION, & FEVER.

  • almost all COX2 inhibitors have been taken off the market d/t cardiovascular risk
  • except Celecoxib (Celebrex)
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5
Q

True or False: Aspirin and NSAIDs both inhibit COX enzymes.

A

True

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6
Q

Is Aspirin competitive or non-competitive inhibitor of platelet function?

A

Aspirin is a non-competitive inhibitor = irreversible inhibitor of platelet function = the effects lasts for the lifetime of the platelet (8-12 days)

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7
Q

Are NSAIDs competitive or non-competitive antagonists of COX1 & COX2?

A

NSAIDs are competitive antagonists

- their effect only lasts as long as the drug’s time to elimination

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8
Q

True or False: Naproxen & ibuprofen are selective COX inhibitors.

A

False: NON-selective

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9
Q

Relative contraindications for Ketorolac: (4)

A

Ketorolac (Toradol) is an NSAID

  1. Asthma
  2. Renal dysfunction
  3. GI dysfunction
  4. Bleeding disorders
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10
Q

What is the dose of IM Ketorolac for patients older than 65 yo, renal impairment, & or less than 50 kg

A

Just give one dose of 30 mg IM

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11
Q

What is the IV dose of Ketorolac for patients younger than 65 yo?

What about over 65 yo, < 50 kg

A

< 65 you = 30 mg dose

> 65 yo & < 50 kg = 15 mg

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12
Q

What is the maximal dose of Ketorolac?

A

If giving a multiple dose treatment of IV or SubQ & pts > 65 = 30 mg q 6 hrs

NEVER exceed 120 mg per day

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13
Q

True or False: Aspirin is a selective inhibitor of COX1

A

False: Aspirin (NSAID & anti-platelet) inhibits COX1 & COX2

BUT favors COX1

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14
Q

What medication is also known as an arachidonic inhibitor?

A

Aspirin

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15
Q

Which NSAID should you take on a full stomach to reduce stomach irritation?

A

Aspirin

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16
Q

True or False: Ibuprofen inhibits both COX1 & COX2

A

True.

Similar inflammatory response as aspirin

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17
Q

Which COX does Acetaminophen inhibit?

A

Inhibits COX3.

Not a complete COX1 or COX2 inhibitor but somewhere in between because it is not a good inflammation reducer.

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18
Q

Cleecoxib (Celebrex) inhibits which COX?

A

COX2 specific inhibitor

- good anti-inflammatory, analgesic, & antipyretic

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19
Q

When is Celecoxib (Celebrex) most commonly used?

A

Used for RA

  • good anti-inflammatory, analgesic, antipyretic
  • reduce prostaglandins in synovial fluid
  • increases platelet aggregation (clotting) so increases myocardial infarction & stroke
20
Q

What is the most commonly prescribed Adenosine diphosphate receptor inhibitor?

A

Clopidrogel (Plavix)

21
Q

Plavix works by binding ___________ to inhibit the expression of GPIIb/IIIa on the surface of the platelet thus inhibiting platelet adhesion & aggregation.

A

Non-competitive & irreversible antagonist.

22
Q

What is the goal of adenosine diphosphate receptor inhibitors?

A

To inhibit thromboembolism

23
Q

GPIIb/IIIa inhibitor abcixmab (ReoPro) has a half-life of ?

A

24-48 hrs
- longest acting
(Aggrastat) Tirofiban = 20-40 min
(Integralin) eptifibatide = 20-40 min

24
Q

Vitamin K antagonists inhibit synthesis of Vit K dependent clotting factors including:

A

II, VII, IX, & X

25
Q

How are Vit K antagonists metabolized?

A

CYP 450

26
Q

Vit K antagonists onset & half life?

A

Warfarin competes with Vit K for binding sites

  • Onset 72-96 hrs (requires heparin bridging)
  • Half-life 36-42 hrs
27
Q

What factors are inhibited by heparin?

Are they intrinsic or extrinsic?

A

Thrombin IIa and factor Xa by binding to AT (anti-thrombin), IX, XI, XII
- influences both intrinsic & common pathways

28
Q

Which test are used to monitor Heparin?

A

aPTT & ACT

29
Q

What is the reversal for Heparin?

A

Protamine

30
Q

What is the main complication of Heparin?

A

Thrombocytopenia

31
Q

What is a low molecular weight Heparin and what does it inhibit?

A

(LMWH) Lovenox

- Fractionated form of heparin w/ more specific inhibition of Xa

32
Q

What is the most important anticoagulant in the blood?

A

Antithrombin (AT)

- formally known as antithrombin III

33
Q

Antithrombin (AT) inhibits thrombin activity and disrupts clot formation via:

A

Binds factors II and X most strongly

- with less strength to factors IX, XI, XII

34
Q

How can you increase the inhibitory effect of antithrombin

A

The inhibitory effect of antithrombin is increased 1,000 fold by heparin

35
Q

Protamine comes from salmon sperm there fore what should you do before giving?

A

Give a test dose to check for anaphylaxis (usually 10 mg)

36
Q

How should you administer Protamine?

A

Slowly administer over 10-15 minutes to avoid hypotension

37
Q

What are the complications related to Protamine administration? (5)

A
  1. Too rapid of administration (histamine release)
  2. Overdose
  3. Repeated doses
  4. Repeated administration
  5. Current or previous use of protamine
38
Q

Indirect Factor Xa antagonists

A

(Arixtra) Fondaparinux - free factor Xa binds w/ AT

39
Q

How soon should you discontinue your indirect factor Xa antagonist?

A

Discontinue for elective minor surgery 48 hours ahead of time & longer before major surgeries (eye, spine, brain, or renal disease)

40
Q

What are the 3 Direct Factor Xa antagonists and when should you D/c them ?

A

(Xarelto) Rivaroxaban, (Eliquis) Apixaban, (Savaysa) Edoxaban

  • D/c 24 hrs in advance, 48 hrs ahead of major surgery (eye, spine, brain, or renal disease)
41
Q

What are the 2 Antifibrinolytics and which is more potent?

A

Amicar & TXA

- TxA is 5x’s more potent than Amicar

42
Q

What is the dose for TxA

A

Trauma dose 10-15 mg/kg followed by 1-5 mg/hr infusion

43
Q

What are considered competitive antagonists at the parietal H2 receptors, used to suppress gastric acid secretion?

A

H2 Blockers or Histamine antagonist

  • Famotidine (Pepcid, Zantac)
  • Cimetidine (Tagamet)
  • Nizatidine (Axid AR)
44
Q

What does histamine do after released?

A

It boosts blood flow to the area of the body where the allergen is, it will cause inflammation & let other chemicals in

45
Q

Which histamines cross the BBB?

A

H1 antagonist

  • cause drowsiness
  • helps with motion sickness