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Skeletal Muscle > Rheumatoid and Osteoarthritis Test 1 Med Chem > Flashcards

Rheumatoid and Osteoarthritis Test 1 Med Chem Flashcards

1
Q

What are prostanoids and leukotrienes synthesized from?

A. Protein

B. Arachidonic Acid

C. Free Fatty Acids

D. Triglycerides

A

B

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2
Q

What is another name for Arachidonic acid?

A. Eicosatetraeonic Acid

B. Ecothiosulfate

C. Lipotechoic Acid

D. Linoleic Acid

A

A

Eicosa= means 20 as in 20 carbons

Tetra= means 4 as in a double bond at position 4

Aen= means double bonds

EicosaTetraAenoic Acid.

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3
Q

Based on the picture provided what enzyme is responsible for liberating Arachidonic acid from the membrane phospholipid?

A. CYP3A4

B. Phospholipase A2

C. Acetylcholinesterase

D. Linoleicesterase

A

B

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4
Q

What source(s) can the body recieve Arachidonic acid from?

A. Dietary Arachidonic Acid

B. Synthesized from Linoleic Acid

C. A and B

D. None of the above

A

C

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5
Q

Which of these drug classes can inhibit Phospholipase A2 ?

A. NSAIDs

B. DMARDs

C. Corticosteroids

D. Immunosuppressants

A

C

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6
Q

What are the three enzymes that can metabolize Arachidonic Acid into products that the body will utilize? (Select All)

A. COX-1, COX-2

B. CYP450

C. Methyl-Transferases

D. LOX

A

A, B, D

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7
Q

When Arachidonic Acid is metabolized by COX-type enzymes Prostanoids will be produced. Which of the following are prostanoids? (Select All)

A. Prostacyclin

B. HETEs

C. Thromboxane

D. EETs

E. Leukotrienes

F. Prostaglandins

A

A, C, F

HETEs are made from LOX enzymes

EETs are made from CYP450 enzymes

Leukotrienes are made from LOX enzymes

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8
Q

Based on the image provided which of the structures represents Linolenic Acid?

A. 1

B. 2

A

B. 2

Omega-3 means on the omega carbon (the last carbon to the far right, the carbon furthest away from the carbonyl group) you count 3 carbons from the right and you land at 3. There is where you will find the first double bond. On the Omega-6 structure the 6th carbon from the last has the double bond and represents structure 1.

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9
Q

When COX enzymes metabolize Arachidonic acid it will produce prostanoids such as thromboxanes (TxA2). What is the function of thromboxane?

A. Anti-aggregation (hypotensive vasculature)

B. Protection of Stomach Lining

C. Pro-Aggregation (platelets)

A

C

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10
Q

When COX enzymes metabolize Arachidonic acid it will create Prostanoids such as PGE2. What is the function of PGE2?

A. Protection of Stomach Lining

B. Pro-Aggregation (Platelets)

C. Anti-Aggregation (Hypotensive vasculature)

A

A

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11
Q

When COX enzymes metabolize Arachidonic acid it produces prostanoids such as PGI2. What is the function of PGI2?

A. Pro-Aggregation (platelets)

B. Anti-Aggregation (Hypotensive vasculature)

C. Protection of Stomach Lining

A

B

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12
Q

What statements are true regarding COX-1 enzymes? (Select All)

A. It is a constituative enzyme (Expressed at all times)

B. Produces Prostacyclins from Arachidonic Acid

C. Expressed in mucosal lining and platelets

D. Produces Thromboxanes and Prostaglandins from Arachidonic Acid

E. It is an inducible enzyme that is expressed in response to inflammatory mediators

A

A, C, D

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13
Q

Which of the following statements are true regarding the COX-2 enzymes?

A. Inducible in response to inflammatory mediators

B. Expressed in vascular endothelial cells

C. Produces Thromboxanes from Arachidonic Acid

D. The enzyme is expressed constituitively (Always expressed)

E. Produces Prostacyclins (PGI2) which dilate vasculature

F. Produces Prostaglandins from Arachidonic Acid

A

A, B, E, F

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14
Q

The blue channels circled on both COX-1 (top-left) and COX-2 (bottom-right) enzymes are known as _____.

A. Hydrophobic Channel

B. Hydrophilic Channel

C. Lipid Channel

D. Enzyme Channel

A

A

It is known as a hydrophobic channel because all of the amino acids in that location have hydrophobic side-chains

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15
Q

What are the three amino acids located in these hydrophobic channels?

A. Valine

B. Tryptophan

C. Arginine

D. Aspartic Acid

E. Tyrosine

A

A, B, E

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16
Q

Based on the structures of the COX-1 and COX-2 enzymes the _____ portion in Arachidonic Acid will bind to the hydrophobic channel. The ____ portion of the Arachidonic Acid will bind to the Arginine group (on the left of the enzyme).

A. 20-carbon chain, carboxylic acid

B. carboxylic acid, 20-carbon chain

A

A

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17
Q

When comparing the strcutrures of the COX enzymes they differ in their allosteric pocket. COX 1 has a ____ amino acid in it’s allosteric pocket and COX-2 has a ___ enzyme in its allosteric pocket. How do these different amino acids affect the accessibility of the allosteric pocket for each enzyme?

A. Isoleucine (Ile), Valine (Val)

B. Valine (Val), Isoleucine (Ile)

A

A

The allosteric pocket in COX-1 will be closed since the isoleucine completely blocks it off. The allosteric pocket in COX-2 will be open since Valine is a very small amino acid in comparison to Isoleucine.

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18
Q

Which of the following statements regarding Acetaminophen are true?

A. The medication acts centrally

B. Also known as Paracetamol

C. Weakly acidic and insoluble in water

D. Can be formulated in solution with Propylene Glycol

E. All of the above

A

E

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19
Q

T/F Acetaminophen is one of the first medications used in the treatment of osteoarthritis for its analgesic properties.

A

T

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20
Q

The enzymes that normally metabolize Acetaminophen are (Blue**) and (**Green).

A. Glucuronidation, Sulfation

B. Sulfation, Glucuronidation

C. Methylation, Sulfation

D. Glucuronidaiton, Methylation

A

A

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21
Q

When medications have this particular p-Quinone or p-Benzoquinone in their structure what can be said about the medication?

A. Nothing notable

B. Pro-Antiinflammatory properites

C. This group causes Oxidative Damage

D. This group is unable to be metabolized by the body

A

C

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22
Q

Glucuronidation is the major pathway if acetaminophen in ____ and Sulfation is the major pathway of acetaminophen metabolism in _____.

A. Adults, Adults

B. Adults, Children

C. Children, Children

D. Children, Adults

A

B

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23
Q

The following picture shows the Minor metabolic pathway of Acetaminophen. What is the enzyme responsible for this metabolism?

A. GLUT

B. CYP3A4

C. CYP2E1

D. SULT

E. Both B and C

A

E

It is metabolized by both 3A4 and 2E1 but MORE by 2E1

24
Q

What is the name of the metabolite formed when Acetaminophen is metabolized by the CYP2E1 and 3A4 enzymes?

A. Paracetamol

B. NAPQI

C. Glutathione

E. Acetylcysteine

A

B

25
Q

When NAPQI is created it can undergo metabolism in order to remove it safely from the body. What enzyme is responsible for this?

A. GLUT

B. SULT

C. NAC

D. Glutathione (GSH)

A

D

26
Q

The portion of this reaction shown in green takes place when someone has overdosed on Acetaminophen and large amounts of NAPQI have been produced. What antidote for APAP toxicity is being illustrated here?

A. GSH

B. Esterase

C. N-Acetylcysteine (NAC)

D. Cholestyramine

A

C

27
Q

In the metabolic pathway illustrated in red, NAPQI is being metabolized by ____ and creating a metabolite that is hepatotoxic.

A. Glutathione metabolites

B. Hepatic Proteins (Sulfhydril, SH)

C. Renal Proteins

D. Hepatic Lipases

A

B

28
Q

What will happen when NAPQI is metabolized by Hepatic Proteins (SH) instead of GSH?

A. Hepato toxicity

B. Hepatic necrosis

C. Renal Failure

D. All of the above

A

D

29
Q

The amino acid ____ in glutathione is responsible for it’s ability to bind to APAP. The specific funcitonal goup in the amino acid that is is responsible for this is ___.

A. Valine, Sulfhydryl (SH)

B. Cysteine, Sulfhydryl (SH)

C. Cysteine, Carboxylic (COOH)

D. Methionine, Sulfhydryl (SH)

A

B

30
Q

How does taking acetaminophen with alochol cause an increased chance of hepatic necrosis?

A

Alcohol induces the expression of CYP2E1 which is responsible for converting APAP to NAPQI. Increased amouts of NAPQI will cause your GSH reserves to be depleted. As a result NAPQI will undergo more metabolism by the hepatic SH proteins and cause hepatotoxicity. This is true even at lower doses of APAP.

31
Q

What is the Black Boxed Warning for Acetaminophen?

A

Risk of Medication errors and hepatotoxicity

32
Q

Which of the following statements is true regading APAP drug interactions?

A Taking Isoniazid with APAP can increase risk of Hepatotoxicity

B. Will intensify the effects of anticoagulants such as warfarin

C. Food will decrease serum concentration by half but will not affect the efficacy.

D. Pregnancy category C and is the preferred analgesic during pregnancy and breast feeding

E. All of the above

A

E

33
Q

What is the mechanism of action of NONSELECTIVE NSAIDs?

A. Inhibits COX-1

B. Inhibits COX-2

C. Inhibits LOX

D. Inhibits both COX-1 and COX-2

A

D

34
Q

What is the mechanism of action of SELECTIVE NSAIDs?

A. Inhibitor of COX-1

B. Inhibitor of COX-2

C. Inhibitor of LOX

D. Inhibitor of COX-1 and COX-2

A

B

35
Q

Answer the following question from the picture provided

A

A

36
Q

Why is COX-2 a better anti-inflammatory target than COX-1

A

In theory its supposed to be better because COX-2 is inducible by inflammation so by inhibiting COX-2 you will decrease the prostaglandins made by that enzyme. Prostaglandins from COX-2 produce Pain and Fever and affect renal function so in theory it should be more effective than inhibiting COX-1.

37
Q

Which of these medications is a Salicylate? (Select All)

A. Acetylsalicylic Acid

B. Salicylate Salts

C. Celecoxib

D. Salsalate

E. Diflunisal

A

A, B, D, E

38
Q

Which of the following NSAIDs is an Aryl and Heteroarylacetic Acid derivative?

A. Indomethacin

B. Celecoxib

C. Etodolac

D. Peroxicam

E. Diclofenac

A

A, C, E

39
Q

Which of these medications is an Aryl and Heteroarylpropionic acid derivative?

A. Ibuprofen

B. Naproxen

C. Salicylate salts

D. Diclofenac

E. Ketoprofen

A

A, B, E

40
Q

Which of these NSAIDs is an Oxicam derivative?

A. Diclofenac

B. Salicylate Salts

C. Etodolac

D. Meloxicam

E. Ibuprfen

F. Piroxicam

A

D, F

41
Q

Which of these medications is Coxib derivative?

A. Ibuprofen

B. Piroxicam

C. Celecoxib

D. Meloxicam

E. Indomethacin

A

C

42
Q

What is the black box warning for NSAIDs? (select all)

A. Nephrotoxicity

B. Cardiovascular Risk

C. Renal impairment

D. GI Risk

A

B, D

43
Q

What is the “Primary Insult”to the GI tract from NSAIDs?

A. Indirect damage to the stomach lining by inhibiting COX-1 enzymes and stopping the gastroprotective effects of PGE2

B. Direct damage to the stomach lining by the acidc structure of the NSAID

C. Direct damage to the stomach liningby inhibiting COX-1 enzymes and stopping the gastroprotective effects of PGE2

D. Indirect damage tot he stomach lining by the acidic structure of the NSAID.

A

B

44
Q

What is the “Secondary Insult” to the GI tract caused by NSAIDs?

A. Indirect damage to the stomach lining by inhibiting COX-1 and stopping the gastro-protective prostaglandin PGE2

B. Direct damage to the stomach lining by inhibiting COX-1 and stopping the gastro-protective prostaglandin PGE2

C. Indirect damage to the stomach lining by the acidic structure of the NSAID.

D. Direct damage to the stomach lining by the acidic structure of the NSAID

A

A

45
Q

The picture depicts a chonine salicylate on the left and an Acetylsalicylic Acid on the right. Which of the following statements are true regarding the comparison of these two figures?

A. Choline Salicylate is an acetylated-salicylate

B. Acetylsalicylic Acid is an acetylated salicylate

C. Acetylsalicylic Acid is a non-acetylated salicylate

D. Choline Salicylate is a non-acetylated salicylate

A

B, D

46
Q

Which of these statements is true when comparing choline salicylate and methylsalicylate? (Select All)

A. Choline salicylate is an non acetylated salicylate while methyl salicylate is acetylated

B. Methyl salicylate is a non-acetylated salicylate with a methyl group attached to it (methylated)

C. Methyl salicylate is an acetylated salicylate while choline salicylate is a non-acetylated salicylate.

D. Methylsalicylate and choline salicylate are both non-acetylated salicylates

A

B, D

47
Q

What is the mechanism of action of Aspirin?

A. Reversible inhibition of COX-1 enzymes only

B. Irreversible inhibition of COX-2 enzymes only

C. Irreversible inhibition of COX-1 and COX-2 enzymes

D. Reversible inhibition of COX-1 and COX-2 enzymes

A

C

48
Q

Which of the following statements is NOT true?

A. It covalently acetylates Ser 530 of COX-1 and Ser 516 of COX-2

B. At low doses COX-1 is more selectively inhibited and blocks the synthesis of thromboxane (TxA2)

C. At higher doses COX-2 is blocked and cardioprotection benefits are lowered.

D. Aspirin is cardioprotective at lower dosages rather than at higher dosages

E. Aspirin is cardioprotective at higher dosages rather than at lower dosages

A

E

49
Q

T/F Other NSAIDs given before administering Aspirin will decrease the cardioprotective properites of Aspirin.

A

T

50
Q

T/F Giving Aspirin with varicella and/or influenza vaccines increases risk of Reye’s Syndrome.

A

T

51
Q

Salicylate allergy/sensitivity reactions consist of 3 main reactions known as the Salicylate Triad. What are the 3 types of reactions? (select all)

A. Hepatotoxicity

B. Uticaria

C. Nephrotoxicity

D. Bronchospasms

E. Rhinitis

A

B, D, E

This is more common with Aspirin than with other NSAIDs

52
Q

Which of the following is not a general PK properties of NSAIDs?

A. Excellent oral absorption (BA: 90-100%)

B. Highly bound to plasma protein due to acidic nature

C. Extensively metabolized (bioactivated or deactivated)

D. Elimination will vary from patient to patient and between different NSAIDs

E. Elimination is constant among the NSAIDs

A

E

53
Q

The body consists of numerous plasma proteins Acidic and Neutral drugs bind to ___. Basic drugs will bind to ___.

A. Albumin, Alpha-1-acid glycoprotein

B. Alpha-1-acid glycoprotein, Albumin

A

A

54
Q

When albumin is saturated what do acidic and neutral drugs bind to?

A. Alpha-1-acid glycoprotein

B. Lipoproteins

C. Random Transport Proteins (RTPs)

D. Basic proteins

A

B

55
Q

T/F Ethanol will increase risk of GI bleeding when taking with NSAIDs

A

T

56
Q

When giving an NSAID to a patient who is currently taking an anticoagulant the effects of the anticoagulant and antiplatelet will___ and the risk of bleeding will ___.

A. Decrease, Decrease

B. Decrease, Increase

C. Increase, increase

D. Increase, Decrease

A

C

57
Q
A

Skeletal Muscle (7 decks)

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