Pharm II exam 7 - Nitrates and Eicosanoids

What are eicosanoids?

lipid signaling molecules

What are 3 examples of eicosanoids?

arachidonic acid, eicosatetraenoic, docosahexaenoic acid

How is arachidonic acid freed from the cell membrane?

by the action of phospholipase A2.

What converts arachidonic acid into the leukotrienes?

the lipoxygenase pathway

What does the cyclooxygenase pathway convert arachidonic acid into?

prostacyclin, prostaglandins, and thomboxane

What is cyclooxygenase?

enzymes that converts arachidonic acid to Prostaglandins and prostacyclin

What are prostaglandins and prostacylin precursors to?

COX 1 and COX 2

Where is COX 2 usually found?

found primarily in inflammatory cells; play a major role in tissue injury such as inflammation

Where is thromboxane preferentially synthesized?

platelets

What is prostacyclin?

a vasodilator and an inhibitor of platelet aggregation.

What does low dose aspirin inhibit?

selectively inhibits platelet COX1 thereby reducing the production of TXA2

What are the vasoconstrictors?

TXA2, PGF2a

What class is epoprosternol?

PGI2

What is the MOA of epoprosternol?

PGI2, prostacyclin, that is synthesized in endothelial cells.

A patient presents with a pulmonary artery test on right side cath that is >25, what would you prescribe?

epoprostenol

What prescription is indicated to treat erectile dysfunction, prevention of ductus arteriosus closure?

alprostadil

What class of medication will stimulate renal COX2 activity and increase the synthesis of vasodilator prostaglandins?

loop diuretics

What is misoprostol?

PGE1 synthetic analog

What might be prescribed to a patient to prevent NSAID induced gastric ulcers?

misoprostol

What class is bimatoprost in?

synthetic analog of PGF2a

What is the MOA of bimatoprost when used as an eyedrop?

lowers intraocular pressure

What might you prescribe to a patient with open angle glaucoma or someone trying to grow eyelashes?

bimatoprost

What side effect would you warn a patient about when prescribing bimatoprost?

increased pigmentation about the eye

Does NSAIDs or ASA reduce the incidence of cancer?

NSAIDS, ASA does NOT lower the incidence

What are 3 examples of prostanoids?

prostaglandins, prostacyclin, and thromboxanes

What is the function of prostaglandins?

vasodilation, bronchodilation, smooth muscle contraction, inflammation

What is the function of thromboxanes?

platelet aggregation, vasoconstriction

What is endoperoxide?

general term for prostaglandin precursor such as PGG, PGH

What is carboprost tromethamine?

analog of PGF2a

What could you give IM to a control postpartum hemorrhage?

carboprost tromethamine

What is slow-reacting substance of anaphylaxis or SRS-A?

recognized as a mixture of leukotrienes

What substances are pro-inflammatory?

prostaglandins and leukotrienes

What class is montelukast in?

leukotriene receptor blocker

What class is zileuton in?

5-lipoxygenase inhibitor

What is endothelium-derived relaxing factor?

a mixture of nitric oxide and other vasodilator substances synthesized in the vascular endothelium

What is nitric oxide produced from?

L-arginine

T or F: Nitric oxide is stored in cells.

false

Acetylcholine, other muscarinic agonists, and bradykinin cause release of what?

endogenous nitric oxide

Nitric oxide is an important _________ vasodilator.

paracrine

3 multiple choice options

Nitric oxide has effects on cell adhesion that result in what?

reduced platelet aggregation

What is the clinical significance of nitric oxide with pulmonary hypertension?

Nitric oxide by inhalation improves cardiopulmonary function in adults and newborns with pulmonary HTN and acute respiratory distress syndrome

What might you prescribe parenterally to cause vasodilation to treat hypertensive emergency?

nitroprusside

what is released from nitroprusside spontaneously in the blood in the presence of oxygen?

nitric oxide

When might tolerance develop to nitrates?

if endogenous thiols are depleted

What is a side effect of nitroprusside?

accumulation of cyanide with prolonged use

What is the MOA of nitroglycerin?

metabolized to NO by mitochondrial aldehyde reductase

What would you prescribe to acutely relieve anginal chest pain to a patient?

nitroglycerin

What is the oral availability of nitrates?

10-20% due to first pass metabolism

Where must NTG be stored?

in a tightly sealed glass bottle because it is volatile

How long should you go between doses of nitrates?

8 hours

What is the primary direct results of NTG?

marked relaxation of veins with increased venous capacitance and decreased ventricular preload

What might you warn a patient as a side effect to nitrates?

throbbing headache

What is a contraindication to giving nitrates?

elevated intracranial pressure

What happens when you give nitrates or nitrites to a patient on PDE inhibitors such as sildenafil?

profound hypotension

How can you give nitrates?

buccal, sublingual, lingual spray, transdermal, oral, and intravenous.

What class is amyl nitrite in?

organic nitrite, vasodilator

What is the MOA of amyl nitrite?

a nitric oxide donor, vasodilator