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Tocolytic drugs have what general effect?
Relax the uterus
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Indomethacin (Indocin) is what type of drug?
Cyclooxygenase inhibitor that prevents uterine contraction
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What is Indomethacin (Indocin) used for
Used off label to prevent premature labor/uterine contractions
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What is the MOA for Indomethacin (Indocin)?
- Inhibits cyclooxygenase:
- Blocks synthesis of prostaglandins (PGE1, PGE2, PGF2α)
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What are the Contraindications of Indomethacin (Indocin)?
Bbleeding disorders, G.I. ulcers and renal impairment
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What are the Maternal side effects of Indomethacin (Indocin)?
Nausea, heartburn, gastritis, increased postpartum bleeding
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What are the Fetal side effects of Indomethacin (Indocin)?
- Constriction of the ductus arteriosus causing pulmonary HTN
- Renal insufficiency
- Deficiency of amniotic fluid
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How is Indomethacin (Indocin) usually administered?
Given orally to delay labor
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What type of drug is Nifedipine?
CCB that relaxes the uterus
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What is Nifedipine (Procardia) used for?
Treats premature labor
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What is the Mechanism of tocolytic action of Nifedipine (Procardia)?
Blocks calcium influx through L-type voltage-gated calcium channels to inhibit uterine contraction
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What are the Contraindications for Nifedipine (Procardia)?
Hypotension (B/c lowers BP) and Heart failure
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What are the Maternal side effects of Nifedipine (Procardia)?
Flushing, HA, dizziness, nausea, tachycardia
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What are the Fetal side effects of Nifedipine (Procardia)?
Little information available in humans
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How is Nifedipine (Procardia) administered?
Given orally
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Does Nifedipine (Procardia) cause issues with the Ductus arteriosus in the fetus/infant?
No
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What type of drug is Terbinafine?
β2 adrenergic receptor agonist that relaxes the uterus
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What is the Mechanism of uterine relaxation for Terbinafine?
- Increases cAMP
- Ativates protein kinase A (PKA)
- Cause dephosphorylation of myosin light chains
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What are the Contraindications for Terbinafine?
- Tachycardia and tachycardia sensitive disease
- Caution in Arrythmias
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What are the Maternal side effects of Terbinafine?
- Tachycardia, palpitations, hypotension, hyperglycemia, tremor
- Tachyphylaxis.
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What are the Fetal side effects of Terbinafine?
Tachycardia, neonatal hypoglycemia, hypotension
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What is Terbinafine used for?
Use discouraged because of adverse CV effects
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What is Magnesium Sulfate approved to treat?
Seizures in preeclampsia
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How is Terbinafine administered?
SQ or IV infusion for < 72 hours
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What is Magnesium Sulfate used off label for?
Premature labor/ Relax the uterus
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What is the Mechanism of action for Magnesium Sulfate?
- Competes with calcium at voltage-gated calcium channels
- Causes hyperpolarization
- Inhibits myosin light-chain kinase
- Inhibits acetylcholine release
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What are the Contraindications for Magnesium Sulfate?
- Cardiac dysfunction
- Renal dysfunction
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What are the maternal side effects for Magnesium Sulfate?
Flushing, diaphoresis, palpitations, depressed reflexes, respiratory depression, impaired cardiac conduction
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What are the fetal side effects for Magnesium Sulfate?
Muscle weakness and neonatal bone abnormalities ( b/c interacts with Ca)
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Atosiban (Antocin) has what MOA?
- Oxytocin receptor antagonist
- Atosiban has what major issue for use?
- Not available in the US
- Commonly used outside the U.S. for premature labor
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What are the Maternal side effects of Atosiban (Antocin)?
Transient headache and nausea, allergic reactions
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What are the Fetal side effects of Atosiban (Antocin)?
- Few reported
- May increase mortality when used early in pregnancy
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What type of molecule is Atosiban?
Peptide
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How is Atosiban (Antocin) administerd?
Given by IV infusion
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Hydroxyprogesterone (Makena) is approved for the treatment of what?
To prevent preterm labor
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At what point, is Hydroxyprogesterone (Makena) not usedful for preterm labor?
Once labor has begun
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What type of molecule is Hydroxyprogesterone (Makena) ?
A progestin
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What is the mechanism of tocolytic action of Hydroxyprogesterone (Makena)?
- Relaxes smooth muscle
- Prevents the formation of connexin-43 gap junctions
- Maintains inhibitory progesterone/estrogen ratio
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What are the maternal side effects of Hydroxyprogesterone (Makena)?
- Contraindicated with breast, cervical, uterine, liver cancer (Causes abnormal cell growth)
- Thromboembolic disease (can cause clotting)
- Causes fluid retention, edema, hyperglycemia and depression
- May cause itching, rash at the injection site, nausea
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What are the fetal side effects of Hydroxyprogesterone (Makena)?
No major adverse effects known at this time.
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How is Hydroxyprogesterone (Makena) administered?
IM x1 weekly
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