Oxytocic And Tocolytics Flashcards
As the pregnancy gets closer to parturition, what hormonal shift happens?
Shifts from progesterone > estradiol dominance to estradiol > progesterone dominance
What effect does progesterone have on the pregnancy?
Causes hyperpolarization of myometrial cells (preventing contractions); decreases adrenergic receptors, inhibits oxytocin synthesis, inhibits estrogen receptor synthesis; promotes storage of prostaglandin synthesizing enzymes
What effect does progesterone have on the adrenergic of the uterus?
Decreases adrenergic receptors
Prior to parturition, what hormone inhibits synthesis of oxytocin receptors and estrogen receptors?
Progesterone
When closer to parturition and the hormones shift to estradiol > progesterone, what effect does this have on the uterus?
Promotes uterine contractility, increases oxytocin receptors, promotes cervical ripening, increases local prostaglandins release from the placenta (which cause myometrial contractions)
What effect do local prostaglandins released from the placenta have on the uterus?
Causes myometrial contractions
What prostaglandins predominate in reproduction?
PGF2 and PGE2
What is responsible for the mild Braxton Hicks contractions during pregnancy?
PGF2 and PGE2
What produces the prostaglandins important for contractions during parturition?
The placental unit
What is the function of oxytocin?
Induces smooth muscle contraction - important for myoepithelial cells in breast and myometrium in uterus
What do tocolytics do to the pregnancy?
Maintain pregnancy
What do oxcytocics do to pregnancy?
Promote labor
Where is oxytocin synthesized?
Paraventricular and supraoptic nuclei of the hypothalamus
What is neurophysin?
Oxytocin protein carrier protein
What kind of receptors are oxytocin receptors?
Gq - coupled to PLC
How is oxytocin administered?
Parenteral, sublingual, nasal; not orally
What is the drug of choice for labor induction?
Pitocin
What is Pitocin?
Synthetic oxytocin
What are contraindications of Pitocin?
Not intended as abortifacient; large baby; hypertonic uterine contractions; previous C sections
What prostaglandin contracts the uterus and produces hyperalgesia?
PGE2
What are the effects of PGE2 in regards to pregnancy/labor?
Contracts uterus; produces hyperalgesia; promotes softening of the cervix
PGER is coupled to what?
Gi
PGF2 causes what effects in regards to labor/pregnancy?
Causes uterine contractions
PGFR is coupled to what?
Gq - stimulates IP3
What effects do prostaglandins have on pregnancy/labor?
Induces local myometrial contractions; promotes cervical ripening prior to delivery
What effect do prostaglandins have on the cervix?
Ripening - softening, thinning, dilating
What is indomethacin?
NSAID - inhibits COX and therefore prostagladin synthesis
What is Indomethicin used for in pregnancy/labor?
Reduces uterine contractions and cervical ripening
What is dinoprostone?
Natural PGE
What is misoprostol?
Synthetic PGE
What is dinoprost?
PGF2 alpha
What is Carboprost?
PGF2 alpha used i.m.
What can misoprostol be used for?
Ripen (dilate) cervix for labor; abortifacient
What can carboprost be used for?
Used in any trimester as an abortifaceint or to induce labor
What can dinoprostone be used in treatment of?
Hydatidiform mole
What is ergonovine? What is its effect?
It is an ergot; causes contraction of the uterus
What is ergometrine? What does is do?
Ergot; causes contraction of uterus
What are ergots used for medically?
Control postpartum bleeding
What receptors do ergots work on?
Alpha adrenergic, dopaminergic, and 5-HT2 receptors
What is ergotamine? Use?
Ergot; used in migraines for its contraction of blood vessels
What can be used to control postpartum bleeding?
Ergots; oxytocics
What are tocolytics used for?
Suppress uterine smooth musc contration; suppress premature labor
Who is an optimum candidate for tocolytic therapy?
Women in early phase of acute preterm labor, when cervical dilation is not advanced
What is terbutaline?
Beta 2 agonist
What is nifedipine?
Calcium channel blocker (dihyropyridines)
What are the downstream effects of calcium binding calmodulin?
Activates MLCK, which phosphorylates myosin light chain, promoting contraction
What are the downstream effects of beta 2 agonists?
Gs - activates AC and increases cAMP; cAMP activates protein kinase A which inhibits MLCK (decreasing smooth muscle contraction)
During what week is terbutaline used in pregnancy?
After week 20
What effect does magnesium sulfate have on uterine contractions?
Inhibits them by competing with calcium; causes smooth muscle relaxation
What is atosiban?
Oxytocin receptor antagonist
What are the concerns with the use of atosiban?
Increased fetal mortality
What NSAID is used as a tocolytic? What is its mechanism?
Indomethacin; blocks cox and inhibits prostaglandin formation
What are the PGE agonists used as oxytocics?
Misoprostal and dinoprostone
What are the PGF2 alpha agonists used as oxytocics?
Dinoprost, carboprost
What beta 2 agonist is used as a tocolytic?
Terbutaline