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59 Cards in this Set

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Arachidonic acid is released or mobilized from cell membranes phospholipids by: (3)

1. Phospholipase A2


2. Phospholipase C


3. Diglyceride lipase

What are isoprostanes?



What are their functions?

Prostaglandin stereoisomers.



They can bind to prostaglandin receptors as a potent vasoconstrict and may contribute to inflammation.

How are isoprostanes synthesized?

Formed by perioxidation of arachidonate by free radicals while part of cell membrane.



COX (cyclooxygenases) not needed.

How does COX -1 and COX-2 differ, in terms of how they are expressed.

COX 1 - expressed all the time, in all cells



COX 2 - expression is inducible

Which enzymes synthesize prostaglandins?

COX (cyclooxygenase)

What group of drugs blocks COX? (giggle giggle)

Non-steroidal anti-inflammatory drugs (NSAIDs)

The precursor for prostaglandins and thromboxanes:

PGH2

T/F: Most cells make several types of prostanoids.

False.



Most cells make one or two dominant ones.

T/F: Specific isomerases and synthases required for each type of prostaglandin.

True.

Label A, B, and C.

Label A, B, and C.

A - Phospholipase A2, Phospholipase C and Diglyceride


B - Lipoxygenase


C - Cyclooxygenase

Which receptors do PGE2 act on? (4)

EP1


EP2


EP3


EP4

Effects of EP1? (4)

1. Mediate stress response


2. Inflammatory thermal hyperalgesia (e.g. sunburn)


3. Activate GI smooth muscle


4. Protect against NSAID ulcers (stomach)

Effect of EP2? (3)

1. Facilitate pain transmission (spinal cord)


2. Join inflammation


3. Fertility and uterine contraction

Effects of EP3? (6)

1. Fever generation


2. Angiogenesis (inflammation and cancer)


3. Activate GI smooth muscles


4. Inhibit gastric secretions


5. Protect against NSAID induced ulcers (intestines)


6. Mediates pain associated from viruses

Effects of EP4? (6)

1. Increase bone turnover
2. Vasodilatation
3. Sensitize nociceptors & neurons
4. Pro-inflammatory in joint

5. Anti-inflammatory in duodenum
6. Promotes mucus secretion in stomach

Which receptors do PGD2 act on?

DP (1, 2)

Effect of DP (1,2)? (3)

1. Bronchoconstriction


2. Inhibits platelet aggregation


3. Promotes sleep

Which receptor does PGI2 act on?

IP

Effects of IP? (7)

1. Vasodilation


2. Bronchodilation


3. Inhibit platelet aggregation


4. Angiogenesis (cancer)


5. Increase renal H2O and Na clearance


6. Uterine relaxation


7. Sensitize nocireceptors

Which receptors does PGF2a act on?

FP (A, B)

Effects of FP (A,B)? (5)

1. Vasoconstriction


2. Activate GI smooth muscles


3. Bronchoconstrictor


4. Uterine contraction


5. Regulate IOP

Which receptor does TXA2 act on?

TP (A,B)

What did sushi A say to sushi B?

WASABI!!

Effects of TP(A,B)? (7)

1. Potent vasoconstrictor


2. Potent bronchoconstrictor


3. Mitogen (smooth muscle)


4. Promotes platelet aggregation


5. Angiogenesis (cancer)


6. Decrease renal function


7. Uterine contraction

Which prostaglandins (and receptors) protect against NSAID ulcers? (2)

1. PGE2 - EP1 - Stomach


2. PGE2 - EP3 - Intestines


Which prostaglandins (and receptors) regulate vasodilation and constriction? (4)

1. PGE2 - EP4 - Vasodilation


2. PGF2a - FP (A,B) - Vasoconstrict


3. PGI2 - IP - Vasodilate


4. TXA2 - TP(A,B) - Potent vasoconstrictor

Which prostaglandins (and receptors) cause bronchoconstriction? (3)

1. PGD2 - DP(1,2)


2. PGF2a - FP(A,B)


3. TXA2 - TP(A,B)

What is the function of corticosteroids? (2)
1. Blocks synthesis pathways for PG and LT
2. Blocks phospholipase A2

How do NSAIDs act as analgesics?

Blocks synthesis of PGE2 in periphery and CNS.

How do NSAIDs treat dysmenorrhea?

Blocks synthesis of PGE2 and PGF2, which cause contractions.

How do NSAIDs treat patent ductus arteroisis?

Blocks PGE2 synthesis. PGE2 keeps fetal ductus arteriosus open.

How are prostaglandins metabolized?

They are oxidized by prostaglandin 15-OH dehydrogenase, and also undergo hydrate to inactive metabolites. Inactive metabolites are excreted in urine.

1. MOA and 2. therapeutic use of Alprostadil?

1. Is a prostaglandin agonist - PGE2 analogue (also know as PGE1)



2. Is a vasodilator, for treatment of ED (intracavernosal injection; secondary option) and ductus arteosus patent in neonates awaiting cardiac surgery.

Adverse effects of Alprostadil?

Penile pain, common in IC injections (NO REALLY.)

What is Bruce Lee's favourite drink?

wa-TAAAAAA!

1. MOA and 2. therapeutic use of Dinoprostone?

1. MOA and 2. therapeutic use of Dinoprostone?

1. EP receptor agonist (PGE1 derivative). Promotes uterine contraction and cervical ripening.



2. Used at end of term for child birth or abortion (1/2 trimester)

Adverse effects of Dinoprostone?

Adverse effects of Dinoprostone?

Abdominal discomfort and diarrhea.

1. MOA and 2. Therapeutic use of misoprostol?

1. MOA and 2. Therapeutic use of misoprostol?

1. EP receptor agonist (PGE1 derivative). Is cytoprotective at low doses (GI), and inhibits gastric secretion at high dose.



2. Prevents NSAID-induced ulcers and causes early abortions.

Adverse effects of misoprostol?

Adverse effects of misoprostol?

Abdominal pain, diarrhea

Which prostaglandins (and receptors) regulate platelet aggregation? (3)

1. PGD2 - DP (1,2) - Inhibits


2. PGI2 - IP - Inhibits


3. TXA2 - TP (A,B) - Promotes

What effect would a selective agonist at the EP2 receptor have if administered in a joint?

Inflammation

1. MOA and 2. Therapeutic use of Lubiprostone?

1. Is a metabolite of PGE1. It is metabolized in the GI with very little absorption. It activates voltage-dependent chloride channels on the apical membrane of intestinal epithelial cells. This causes secretion of fluid into the intestines.



2. Treatment of chronic constipation.

Adverse effects of Lubiprostone?

Vomiting, nausea, abdominal cramping

1. MOA and 2. Therapeutic use of Latanoprost?

1. A PGF2 derivative.



2. Used topically for lower IOP in glaucoma.

1. MOA and 2. Therapeutic use of Prostacyclin (Epoprostenol)?

1. Is a PGI2 analogue, made mainly in vascular endothelium. Is a powerful vasodilator and inhibits platelet aggregation. Used for vascular homeostasis.



2. Used for pulmonary hypertension and porto-pulmonary hypertension (secondary to liver disease).

Therapeutic use of TXA2-receptor antagonists and synthesis inhibitors?

Originally developed for cardiovascular indications, but no clinical use is established.

1. MOA and 2. Therapeutic use for Acetylsalicylic acid (ASA)?

1. Blocks off synthesis of TXA4 for the life of the platelet, therefore decreasing platelet aggregation.



2. Is an anticoagulant and used for secondary prevention of myocardial infarction.

Adverse events of ASA?

GI ulceration


Inhibition of PGE2

Which enzyme converts arachidonic acid to leukotrienes?

Lipoxygenases (LOX)

Which cells are 5-lipoxygenase found in?

Inflammatory cells:


- polymorphonuclear leukocytes (PMN)


- basophils


- mast cells


- eosinophiles


- macrophages

What are the primary products of 5-LOX?

LTB4. This can be converted into lipoxins LX4A, LXB4, and other leukotrienes.

Which receptor does LTB4 act on?

BT1,2

What are the effects of receptor BT1,2? (2)

1. Chemoattractant


2. Activates inflammatory cells

What do you get when you cross a stream and a brook?

Wet feet!

Which receptor do LTC4, D4, E4 act on?

CystLT1,2

Effect of receptor CystLT1,2 (aka cysteinyl-leukotrienes)? (2)

1. Chemoattractant (eosinophil)


2. Potent bronchoconstrictor (induces bronchial inflammation)

1. MOA and 2. Therapeutic use of Zileuton?

1. Zileuton is a 5-lipoxygenase inhibitor.



2. Used for asthma.

Adverse effects of Zileuton?

Elevated liver enzymes, indigestion, abdominal pain, nausea.



Metabolized by cytochrome P450, may alter metabolism of drugs such as warfarin, theophylline, and propanolol.

1. MOA and 2. Therapeutic use of Montelukast?

1. Competitive antagonist at CystLT1 receptor.



2. Used for asthma, allergic rhinitis.



*Unknown if this receptor is relevant for treating asthma.