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26 Cards in this Set
- Front
- Back
Uterine Stimulants (Oxytocics)
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Oxytocin
Ergonovine and Methylergonovine Dinoprostone and Carboprost Tromethamine |
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Oxytocin - General info
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- Peptide hormone of post. pituitary that elicits milk ejection in lactating women
- Can be used to induce uterine contractions and maintain labor - During second half of pregnancy, uterine SM inc expression of oxytocin receptors and become sensitive to action of endogenous oxytocin - Pharmacologic conc of oxytocin powerfully stimulate uterine contraction |
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Oxytocin - MOA
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Oxytocin --> Gprotein receptor --> (i) activation of phospholipase C, (ii) activation of voltage-gated calcium channels
also Oxytocin --> increases local PG synthesis --> further stimulation of uterine contractions |
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Oxytocin - Clinical Uses
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- induction of labor (DOC!!)
- augmentation of dysfunctional labor (prolonged latent phase of cervical dilation; arrest of dilation or descent) - postpartum hemorrhage - oxytocin challenge test - induction of abortion |
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Oxytocin - Pharmacokinetics
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IV infusion - for labor induction
IM injection - control of postpartum bleeding Nasal spray - promote milk ejection |
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Oxytocin - Adverse Effects
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- excessive stimulation of uterine contractions --> fetal distress, placental abruption, uterine rupture
- high conc of oxytocin --> activate vasopressin receptors --> excessive fluid retention, or water intoxication leading to hypontaremia, heart failure, seizures, and death - bolus injections of oxytocin can cause hypotension (to avoid this, oxytocin is admin IV as dilute solutions at a controlled rate) |
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Oxytocin - Contraindications
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- fetal distress
- prematurity - abnormal fetal presentation - cephalopelvic disproportion |
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Ergonovine and Methlyergonovine - General information
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- partial agonists for alpha-adrenergic receptors and some serotonin receptors
- sensitivity of the uterus to the stimulant effects of ergot alkaloids increases dramatically during pregnancy - in small doses can evoke rhythmic contraction and relaxation of the uterus - at higher conc induce powerful and prolonged contractions |
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Ergonovine and Methylergonovine - Clinical uses
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Ergonovine and methylergonovine are given IM as second line agents (behind oxytocin) for postpartum hemorrhage
**Ergot derivatives should ONLY be used for control of LATE uterine bleeding and should NEVER be given before delivery |
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Ergonovine and Methylergonovine - Adverse effects
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- HTN, headache, possible seizures
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Ergonovine and Methylergonovine - Contraindications
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- Angina pectoris, MI, PREGNANCY, history of CVA, TIA, or HTN
- Can be found in breast milk so neither should be admin longer than necessary --> can lead to ergot poisoning (ergotism) including gangrene in the nursing infant |
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Dinoprostone and Carboprost Tromethamine - General info
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Dinoprostone = PGE2
Carboprost tromethamine = synthetic analogue of PGF2-alpha - PG's are more effective stimulants of uterine contraction thru the second trimester than is oxytocin - Inhibition of PG synthesis with a NSAID can increase the length of gestation, prolong spontaneous labor, or interrupt premature labor |
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Carboprost Tromethamine - Clinical uses
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- induction of abortion in 2nd trimetster
- control of postpartum hemorrhage due to uterine atony (3rd line behind oxytocin and ergonovine) |
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Dinoprostone - Clinical uses
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- induction of abortion in 2nd trimester
- evacuation of uterine contents (missed abortion) - mgmt of benigh hydatidiform mole - ripening of cervix for inductino of labor in pts at or near term |
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Dinoprostone and Carboprost Tromethamine - PK
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Carboprost tromethamine = IM
Dinoprostone = vaginal insert, vaginal suppository, cervical gel |
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Uterine Relaxants (Tocolytics)
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- Beta-2-adrenoreceptor agonists (ex: Terbutaline)
- Magnesium sulfate - Indomethacin - Nifedipine - Atosiban |
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Beta-2-adrenoreceptor agonists - General info
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- can arrest preterm labor for at least 48-72 hrs
- even though most commonly used in US, not always effective in treating preterm labor |
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Beta-2-adrenoreceptor agonists - MOA
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agonist --> B-2-adrenoreceptor on myometrium --> adenylyl cyclase --> cAMP --> 2 things happen:
(i) - decreased intracellular Ca --> reduced effect of Ca on muscle contraction (ii) - protein kinase A --> phosphorylates smooth-muscle myosin light chain kinase (SmMLCK) --> lower affinity of SmMLCK for Ca-calmodulin complex --> no phosphorylation of myosin by SmMLCK --> muscle relaxes |
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Beta-2-adrenoreceptor agonists - Adverse effects
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- palpitations, tremor, nausea, vomiting, nervousness, anxiety, chest pain, SOB, hyperglycemia, hypokalemia, hypotension
- serious = pulm edema, cardiac insuff., arrhythmias, MI, maternal death |
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Terbutaline
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- mgmt of premature labor (not FDA-approved for it though)
- specific B2-adrenoreceptor agonist - can decrease frequency, intensity, and duration of uterine contractions - prevents premature labor esp more than 20wks into gestation and have no indication of ruptured fetal membranes or in whom labor is not far advanced - should be given initially in hospital setting - given orally or subcutaneously or IV |
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Magnesium sulfate - MOA
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- Uncouples excitation-contraction in myometrial cells thru inhibition of cell action potentials
- Decreases Ca uptake by competing for its binding sites, activating adenylyl cyclase, and stimulating Ca uptake by the sarcoplasmic reticulum |
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Magnesium sulfate - Clinical use
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- Preferred over B-adrenergic agents in pts with heart disease, diabetes, HTN, or hyperthyroidism
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Magnesium sulfate - AE
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- Toxicity = life-threatening (in increasing doses):
- loss of patellar reflexes - resp. depression - resp. paralysis --> arrest - cardiac arrest |
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Indomethacin
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- an NSAID (acts as an inhibitor to PG synthesis) used to delay preterm labor
- given orally or rectally - AE = premature closure of fetal PDA (bc of the fetus's ability to inhibit PG synthesis) [more sensitive beyond 32 wks] |
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Nifedipine
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- Ca channel blocker
- acts by impairing entry of Ca into myometrial cells via voltage-dep Ca channels (so inhibits contractility) - given orally |
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Atosiban
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- competitive antagonist at oxytocin receptors
- decreases and stops uterine contractions - not available in US |