Prostaglandins-COMP Flashcards
Prostaglandins act as
Local hormones.
Prostaglandins are synthesized in the body form the essentials fatty acids
Arachidonic acid
Dihydrolinoleic acid
Eicosapentaenoic acid
Arachidonic acid is a component of _________is released by
Cell membrane ; Action of phospholipase C and phospholipase A2
Phospholipase enzymes are inhibited by
Corticosteroids
Phospholipase A2 leads to
Arachidonic acid
Arachidonic Acid gives rise to 2 pathways
Cyclooxygenase and Lipooxygenase
Pathway of clyclooxygenase lead to
Endoperoxides leading to Thromboxane synthethase and prostacyclin synthethase, leading to thromboxane and prostacyclin
Pathway of Lipooxygenase lead to
5-Hydroxy-Arachidonic Acid –> Leukotrienes
Mechanism of Action of Prostaglandins
Stimulate synthesis of cyclic Adenosine monophosphate (cAMP) by activation of adenylate cyclase
cAMP activates protein A to express it effect, including decreased free intracellular concentration of calcium which leads to
Vascular relaxation
Act as filter fro many of the prostaglandins
Lungs
Half time of Thromboxane A2
30 seconds
Half time of Prostacyclin
3 minutes
Under strict regulation of prostacyclins
Normal platelet function and hemostasis
Regulated by prostaglandins
Renal blood flow
Prostaglandins maintain or increase
mucosal blood flow and help increase secretion mucus and bicarb in the stomach
What is the principal Cyclooxygenase product of arachidonic acid in platelet?
Thromboxane
Act as an intense stimulus for platelet aggregation and vasoconstriction
Thromboxane
Low doses of ASA
IRREVERSIBLY inhibits Thromboxane
NSAIDS
Reversible inhibited by NSAIDS
The most potent endogenous inhibitor of platelet aggregation and is a potent vasodilator
Prostacyclin
Doses needed to inhibit both thromboxane and prostacyclin production
Large doses of ASA
What is important in maintaining platelet activity and coagulation?
A normal Thromboxane to prostacyclin ratio
What can lead to decrease blood flow leading to possible ischemia or infarction of vital organs?
Increase thromboxane
Decrease prostacyclin
What can lead to Bleeding disorders?
Decrease Thromboxane
increase prostacyclin
What is the major site of prostaglandin synthesis?
The lungs
Can lead to bronchial asthma
Thromboxane and prostacyclin
Leukotrienes vs histamine
Leukotrienes have thousand times more potent bronchial smooth muscle vasoconstriction activity than histamine
ASA can lead to an increase in
production of leukotrienes
Intrarenal release of prostaglandins lead to
Modulate renal blood flow and GFR
Inhibition of cyclooxygenase with NSAID
can interfere with normal renal prostaglandin protective mechanisms and accentuate catecholamine induced renal vasoconstriction
Used for primary pulmonary HTN
Epoprosterenol (flolan)
Illoprost
Derivative of prostacyclin
Uniprost
Derivative of prostacyclin
Treatment (inhaler) of Pulmonary HTN
Illoprost
Administered SC by portable pump
Uniprost
Epoprosteronol also known as
Prostacyclin and PGI2, strong vasodilator
MOA epoprosterenol
A potent endogenous inhibitor of platelet aggregation
Epoprosterenol Steady state levels are reached in
15 mins with continuous infusion
Half life Epoprosterenol
2.7 - 6 minutes
Epoprosterenol usually initiated at
2ng/kg/min
Never do this with EPOPROSTERENOL
Never interrupt infusion
Monitoring parameters for Isoproterenol
Improvement in pulmonary function
PA pressures
PVR
HR and decrease in dyspnea
Use for temporary maintenance of ductus arteriosus in neonates with ductul dependant CHD until surgery
ALPROSTADIL
Newest medication may see with PUMP
Label: REMODULIN (treprostinil)
Controlled hypotension achieved with a continuous dose of
Alprostadil
Alprostadil dose for controlled hypotension
0.1ng/kg/min to maintain CBF
Used to treat ED
Alprostadil
Alprostadil
Vasodilation and inhibition of platelet aggregation
Administration by IV prevents premature closure of the ductus arteriosus until surgery can be performed
Alprostadil
Side effects of Alprostadil
Depression of ventilation Bronchoconstriction Flushing Bradycardia Hyperthermia
Use to promote cervical ripening prior to labor induction
Dinoprostone (cervidil)
Used to terminate pregnancy in weeks
12 through 28 weeks evacuate the uterus in cases of missed abortion, intrauterine fetal death
Produces physiologic uterine contractions
Dinopros
Warning for Dinoprost
Bronchospasm in asthmatics
Seizures
N/V
Termination of pregnancy and treatment of refractory PP uterine bleeding
Carboprost
Carboprost dose of
250cmg IM repeat at 1 1/2 to 3 1/2 interval
Caution for carboprost
History of asthma , hypotension or HTN, renal or hepatic , DM , seizures
Side effects of Carboprost
Vomiting, diarrhea, hyperthermia
Used to prevent NSAID induces gastric ulcers
Misoprostol , cytotec
Inhibits secretion of gastric acid by parietal cells
Misoprostol cytotec
Misoprostol replaces the
Protective prostaglandins consumed by NSAIDs
Side effects of Misoprostol
Diarrhea, abd pain
Thomboxane on SVR
Increase
Thomboxane on Airway Resistance
Increase
Thomboxane on Platelet aggregation
Increase
Prostacyclin and Epoprosterenol on SVR
Decrease
Prostacyclin and Epoprosterenol on airway resistance
Increase
Prostacyclin and Epoprosterenol on Platelet aggregation
Decrease
Illoprost on airway resistance
Decrease
The only prostacyclin reduces AIRWAY RESISTANCE
ILLOPROST
Illoprost platelet aggregation
Decrease
Increase Uterine Muscle tone
Alprostadil
Dinoprost
Dinoprostone
Decrease platelet aggregation
Prostacyclin (epoprosterenol)
Illoprost
Alprostadil
Dinoprost
Increase or decrease SVR