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[PHARM] Uterine Stimulants & Relaxants

Total questions: 22

Worksheet time: 12mins

Name
Class
Date
1.

Uterine Stimulants

• 9-amino acid peptide synthesized in hypothalamus and secreted by posterior pituitary gland

• Important in parturition

• Stimulates both frequency and force of uterine contractions

• Milk letdown

a)

Oxytocin

b)

Ergot alkaloids

c)

Prostaglandin derivatives

2.

Uterine Stimulants

• Not effective orally

• IV: for initiation and augmentation of labor

• IM: control of postpartum bleeding

• Nasal spray: for impaired milk ejection

a)

Oxytocin

b)

Ergot alkaloids

c)

Prostaglandin derivatives

3.

Uterine Stimulants

• Given only when cervix is soft and dilated

• 3rd stage of labor

• Control post-partum bleeding

• Effect is dependent on the presence of estrogen

a)

Oxytocin

b)

Ergot alkaloids

c)

Prostaglandin derivatives

4.

Uterine Stimulants

• __________ uterus is resistant to oxytocin

a)

Mature

b)

Immature

5.

Uterine Stimulants

Adverse Effects

• Uterine rupture

• Water intoxication (at high concentrations)

• Fetal death

• Maternal death from hypertension

a)

Oxytocin

b)

Ergot alkaloids

c)

Prostaglandin derivatives

6.

Uterine Stimulants

Contraindications to oxytocin use

a)

Fetal distress

b)

Prematurity

c)

Abnormal presentation

d)

Cephalopelvic disproportion

7.

Uterine Stimulants

• Produced by Claviceps purpurea fungus

• Induce tetanic contraction (without relaxation)

• Causes contraction of uterus as a whole including fundus and cervix (this tends to compress the fetus rather than expel)

• Given parenterally and orally

• Onset of action: 5-15 minutes

• Duration: up to 3 hours

a)

Oxytocin

b)

Ergot alkaloids

c)

Prostaglandin derivatives

8.

Uterine Stimulants

Ergot alkaloids

• More selective than other ergot alkaloids in affecting the uterus

a)

Ergometrine

b)

Ergonovine

9.

Uterine Stimulants

• Should never be given before delivery; given at the time of delivery of placenta


Adverse Effects

• GI upset: nausea, vomiting, diarrhea

• Leg cramps

• Difficulty in breathing

• Overdose: St. Anthony’s Fire → Prolonged vasospasm (pain and gangrene of limbs)

a)

Oxytocin

b)

Ergot alkaloids

c)

Prostaglandin derivatives

10.

Uterine Stimulants

Contraindications to use of ergot alkaloids

a)

Coronary heart disease

b)

Hypertension

c)

Anemia

d)

Myocardial infarction

11.

Uterine Stimulants

Prostaglandin Derivatives

• Brand name: Prostin E2

• Synthetic preparation of PGE2 (synthetic according to Katzung, but “naturally occurring” according to slides)

• Administered vaginally for oxytocic use

• Stimulates contraction throughout pregnancy and softens cervix by affecting collagenase

• Approved in USA for abortion in 2nd trimester (12 to 20 weeks), for missed abortion, for benign H. mole, and for ripening of cervix to induce labor near or at term

a)

Dinoprostone

b)

Carboprost

c)

Misoprostol

12.

Uterine Stimulants

Prostaglandin Derivatives

• Brand name: Hemabate

• PGF2a analogue

• Single 250 mcg IM

• Used to induce 2nd trimester abortions and to control postpartum hemorrhage that is not responding to conventional management

a)

Dinoprostone

b)

Carboprost

c)

Misoprostol

13.

Uterine Stimulants

Prostaglandin Derivatives

• Brand name: Cytotec

• PGE1 synthetic analogue (PGE1 according to Katzung and other sources, but “PGE2” in lecture slides)

• Cervical ripening agent

• For treatment of peptic ulcer disease (acts as cytoprotectant; hence, “Cytotec”)

a)

Dinoprostone

b)

Carboprost

c)

Misoprostol

14.

Uterine Stimulants

Adverse Effects

• GI disturbances

• Transient fever

• Headache

• Decreased diastolic BP

• Retained placental fragments


Precautions

• Asthma

• Hyper/hypotension

• DM

• Cervicitis

a)

Oxytocin

b)

Ergot alkaloids

c)

Prostaglandin derivatives

15.

Uterine Relaxants

• Peptide analogue of oxytocin

• Very short half-life (15 minutes)

• Oxytocin receptor antagonist

• Tocolytic

• Approved for use as a treatment of preterm labor

• Used to inhibit uncomplicated premature labor between 24 and 33 weeks of gestation

a)

Atosiban

b)

Terbutaline & Ritodrine (B-agonists)

c)

Magnesium sulfate

d)

Prostaglandin Synthetase Inhibitors

16.

Uterine Relaxants

Adverse Effects

• Nausea and vomiting

• Headache and dizziness

• Tachycardia and hypertension

• Hyperglycemia

a)

Atosiban

b)

Terbutaline & Ritodrine (B-agonists)

c)

Magnesium sulfate

d)

Prostaglandin Synthetase Inhibitors

17.

Uterine Relaxants

• Selective B2 agonist

• Binding to beta receptors activates adenylyl cyclase increasing cAMP & decreasing Ca

• Tocolytic

• Smooth muscle relaxant

• Effective at 20-36 weeks

a)

Atosiban

b)

Terbutaline & Ritodrine (B-agonists)

c)

Magnesium sulfate

d)

Prostaglandin Synthetase Inhibitors

18.

Uterine Relaxants

Adverse Effects

• Tremors

• Tachycardia at high dose

• Hypotension

• Hyperglycemia

• Hypokalemia

a)

Atosiban

b)

Terbutaline & Ritodrine (B-agonists)

c)

Magnesium sulfate

d)

Prostaglandin Synthetase Inhibitors

19.

Uterine Relaxants

• Selective B2 agonist

• Interferes with calcium uptake by myometrial cells

• Effective inhibitor of uterine contraction

• Prevents convulsion in preeclampsia

• Preferred over beta agonists in patients with heart disease, DM, hypertension, and hyperthyroidism

a)

Atosiban

b)

Terbutaline & Ritodrine (B-agonists)

c)

Magnesium sulfate

d)

Prostaglandin Synthetase Inhibitors

20.

Uterine Relaxants

Adverse Effects

• Nausea, vomiting

• Hot flushes

• Nystagmus


Toxicity

• Respiratory depression

• Cardiac arrest

• Loss of patellar reflexes


*Close monitoring is required

a)

Atosiban

b)

Terbutaline & Ritodrine (B-agonists)

c)

Magnesium sulfate

d)

Prostaglandin Synthetase Inhibitors

21.

Uterine Relaxants

• Selective B2 agonist

• Cyclooxygenase inhibitors (NSAIDs especially Indomethacin)

• Delays preterm labor

• Used in gestation prior to 34 weeks

a)

Atosiban

b)

Terbutaline & Ritodrine (B-agonists)

c)

Magnesium sulfate

d)

Prostaglandin Synthetase Inhibitors

22.

Uterine Relaxants

Adverse Effects

• Premature closure of ductus arteriosus

• Increased risk of pulmonary hypertension

• Oligohydramnios

• IVH

a)

Atosiban

b)

Terbutaline & Ritodrine (B-agonists)

c)

Magnesium sulfate

d)

Prostaglandin Synthetase Inhibitors