Pharmacology Flashcards

1
Q

Describe the cyclical pattern of myometrial activity during labor

A

A switch in pattern of myometrial contractility between contractures (long-lasting, low-frequency) & contractions (frequent, high-intensity, high- frequency activity)

  • results in effacement & dilatation of the cervix
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2
Q

Parturition: Phase 1

- What occurs & how long does it take?

A
  • Uterine contractions of increasing strength and frequency
  • Cervix dilates

Time = Variable # of hours

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3
Q

Parturition: Phase 2

- What occurs & how long does it take?

A

Expulsion of fetus

Time = ~1 hour

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4
Q

Parturition: Phase 3

- What occurs & how long does it take?

A
  • Expulsion of placenta
  • Aftercontractions of uterus (reduces bleeding)

Time = ~ 10 min

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5
Q

Oxytocin:

- Where is it synthesized?

A

Posterior Pituitary, Ovary, Endometrium, & Placenta

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6
Q

Oxytocin:

- MOA?

A
  • Stimulates uterine smooth muscle

Near end of term (due to ↑ Estrogen):
- ↑ #’s of oxytocin receptors, Na+ channels, &
gap junctions

  • Stimulates myoepithelial cells → lactation
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7
Q

Oxytocin - effects are dependent on what? What effects does this have

A

Its effects are dependent on Estrogen.

  • Immature uterus is resistant to effects
  • ↑ Uterine sensitivity near term (~36 wks)
  • ↑ #’s of oxytocin receptors, Na+ channels, &
    gap junctions
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8
Q

Oxytocin - uses?

A
  • Induce labor (IV)
  • Augment labor – ONLY in abnormal labor (IV)
  • Contract uterus after labor - ↓ bleeding (IM)
  • Promote milk release – (intranasal)
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9
Q

What 3 things must be monitored during labor induction?

A
  • Fetal & maternal HR
  • Maternal BP
  • Frequency of contractions
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10
Q

Oxytocin - AEs?

A
  • Uterine hyper-stimulation (tetany)
  • Anti-diuretic actions
  • Vasodilation → hypotension, tachycardia
  • Trauma to mother = uterine rupture
  • Trauma to fetus = hypoxia
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11
Q

Dinoprostone - uses?

A

– “Cervical ripening” (softening, effacement & dilation of cervix – prep labor)
– Produce midtrimester abortion
– Vaginal gel or suppository

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12
Q

Dinoprostone - type of drug?

A

Prostaglandin (PGE2)

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13
Q

Carboprost - type of drug?

A

Prostaglandin (15-methyl PGF2)

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14
Q

Carbaprost - uses?

A

– Used to produce midtrimester abortion
– Used to ↓ postpartum bleeding

– Administered IM

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15
Q

In what types of situations are Prostaglandins contraindicated?

A

Cardiac, renal, pulmonary disease, prior uterine surgery, fetal distress, etc.

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16
Q

Prostaglandins - AEs?

A

– Nausea, vomiting, abdominal pain, diarrhea, fever & bronchoconstriction
– Hypotension, hypertension, syncope, dizziness & flushing.
– Fetal cardiac bradycardia

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17
Q

IM ___a___ & local administration of ___b___ may limit systemic AE’s

A

a) Carbaprost

b) Dinoprostone

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18
Q

Misoprostol - type of drug?

A

PGE1 analog

typically used to prevent NSAID-induced ulcers

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19
Q

Mifepristone - type of drug?

A

RU-486, a progestin receptor partial agonist

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20
Q

Misoprostol - uses?

A
  • Used 48 hr after Mifepristone to produce first trimester abortion
  • typically used to prevent NSAID ulcers
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21
Q

Mifepristone - uses?

A

Used in combo w/ Misoprostol to produce first trimester abortion

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22
Q

Misoprostol & Mifepristone - AEs?

A

Vomiting, diarrhea, abdominal & pelvic pain

  • Vaginal bleeding common!
  • Infection – sepsis.
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23
Q

Misoprostol & Mifepristone - off-label use?

A
  • Cervical ripening
  • Labor induction
  • Induce abortion in early pregnancy
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24
Q

Drug class derived from fungus that grows on rye, etc.?

A

Ergot Alkaloids

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25
Q

Ergot Alkaloids - MOA?

A
  • Agonists and/or antagonists at 5-HT, dopamine & α-adrenergic receptors

Produce strong uterine contractions:
– Low doses – clonic contractions
– High doses – tonic contractions

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26
Q

Ergonovine - Drug class?

A

Ergot Alkaloid

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27
Q

Methylergonovine - Drug class?

A

Ergot Alkaloid

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28
Q

Methylergonovine - uses?

A

↓ bleeding postpartum or after abortion

IM or IV

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29
Q

Ergonovine - uses?

A

↓ bleeding postpartum or after abortion

IM or IV

30
Q

Ergonovine - AEs?

A

NVD, vasospasm, bowel ischemia

31
Q

Methylergonovine - AEs?

A

NVD, vasospasm, bowel ischemia

32
Q

Tocolytic Agents - what are they used for?

A

Objective is to inhibit premature labor (< 36 weeks) to permit further fetal development

33
Q

What types of drugs may function as Tocolytic agents?

A
  • β-2 agonists
  • MgSO4 & Calcium Entry Blockers (CEB)
  • COX-inhibitors (NSAIDS)
  • Atosiban – Oxytocin Receptor Antagonist
  • (Hydroprogesterone or Progesterone)
34
Q

Via what molecular mechanisms do myometrium cells contract & relax?

A

Contraction:
- ↑ intracellular Ca(2+) via Ca2+/calmodulin-dependent activation of myosin light chain kinase (MLCK)

Relaxation:
- ↑ of cyclic nucleotides (cAMP & cGMP) and their activation of protein kinases, which cause phosphorylation/inactivation of MLCK

35
Q

Ritodrine - what is it?

A
  • β-2 agonist, Tocolytic
36
Q

Terbutaline - MOA?

A

β-2 agonist (Tocolytic) that should NOT be used in pregnant women more than 48-72 hrs

37
Q

Albuterol - MOA?

A

β-2 agonist

  • Tocolytic that should NOT be used as a tocolytic
38
Q

β-2 agonists - AEs?

A
– ↑ maternal & fetal HR
– Arrhythmias
– Hypokalemia
– Maternal pulmonary edema
– Myocardial ischemia
– Skeletal muscle tremor
– Hyperglycemia
39
Q

Magnesium Sulfate (Mg2SO4) - MOA?

A
  • ↓ Ca(2+) for contraction (causing relaxation)

Tocolytic agent that shouldn’t actually be used as a tocolytic

40
Q

Magnesium Sulfate (MgSO4) - AEs?

A
– Hypermagnesemia, Hypocalcemia
– Flushing, nausea, vomiting
– Headaches, visual disturbances
– Muscle paralysis
– Cardiac electrical disturbances
– Pulmonary edema
  • Use is discouraged!
41
Q

Nifedipine - MOA?

A

Calcium-channel blocker

- yet another Tocolytic drug that is not approved in the USA

42
Q

Name the Tocolytic agent that is as effective as ritodrine but has fewer maternal AE’s and lower neonatal morbidity. It is also not approved in the USA for use as a tocolytic.

A

Nifedipine

43
Q

Nifedipine - AEs?

A
– Dizziness, lightheadedness, nervousness
– Flushing, headache, nausea
– Muscle cramps or tremors
– Hypotension
– ↓ fetal blood supply
44
Q

NSAIDS - MOA as Tocolytics?

A

(COX-inhibitors) inhibit uterine contractions, prolonging gestation and/or slowing labor

45
Q

Combination of _____ with other tocolytics provides enhanced tocolysis

A

NSAIDs

46
Q

NSAID use as tocolytic agent - encouraged or discouraged?

A

Use is discouraged because of potential adverse effects on fetal development – closure of ductus arteriosus

47
Q

Atosiban - MOA?

A
  • Synthetic peptide analog of oxytocin
  • Oxytocin Receptor Antagonist
  • Specific for uterine smooth muscle – (not a general smooth muscle relaxant)

• Not available in US

48
Q

Atosiban - used in USA as Tocolytic?

A

No, it’s available in 30 countries but NOT the USA due to efficacy/safety concerns

49
Q

Atosiban - AEs?

A

Nausea & vomiting, headache, dizziness, flushing, tachycardia, hypotension, hyperglycemia

50
Q

a) What is the only FDA-approved Tocolytic drug that we learned about?

A

a) Hydroxyprogesterone

51
Q

Hydroxyprogesterone - uses?

A

to reduce the risk of preterm birth in women with a singleton pregnancy who have a history of singleton spontaneous preterm birth

  • Reduced # of preterm births, but no effect on infant mortality
52
Q

What is the benefit on infant mortality from Hydroxyprogesterone in a woman w/ a Hx of preterm births?

A

Hydroxyprogesterone causes reduced # of preterm births, but has NO EFFECT on infant mortality

53
Q

Hydroxyprogesterone - MOA?

A

Progesterone (Tocolytic)

54
Q

Hydroxyprogesterone - AEs?

A

Nausea & vomiting, headache, dizziness, flushing, tachycardia, hypotension, diarrhea, hyperglycemia, depression

55
Q

Stress urinary incontinence - Cause?

A
  • ↑ intra-abdominal pressure

- weakened pelvic muscles

56
Q

Stress urinary incontinence - Tx?

A
↑ sphinctor contraction
– α1-adrenergic agonist (pseudoephedrine)
– estrogens (?)
– TCA (imipramine)
– exercise, surgery, implants
57
Q

What is Urge urinary incontinence?

A

Sudden involuntary bladder contraction
– Bladder contracts at inappropriate volume
– Also called detrusor instability, irritable bladder, spasmodic bladder, etc.

58
Q

What is Stress urinary incontinence?

A

Involuntary loss of urine with physical activity (coughing, laughing, etc.)

  • Common in women – ↑ age, pregnancy
  • Cause:  intra-abdominal pressure
    weakened pelvic muscles
59
Q

Urge urinary incontinence - Tx?

A

↓ detrusor instability

– Muscarinic antagonists/ antispasmodics
— Oxybutynin, Tolterodine

60
Q

AEs of antimuscarinics used for Urge Incontinence?

A
– Dry mouth
– Blurred vision
– Dizziness
– Constipation
– Urinary retention
– Sedation

Many patients may not tolerate AE’s – use adult diapers

61
Q

Urge incontinence drug available as SR & patch, which may ↓ peak plasma concentrations – reducing systemic AE’s

A

Oxybutynin

62
Q

Newer agent used for Urge Incontinence claimed to be bladder selective (M3 receptors)?
– less dry mouth

A

Tolterodine

63
Q

Tolterodine - MOA?

A

M3-selective (supposedly) anticholinergic

- less AEs, like dry mouth

64
Q

Tolterodine - uses?

A

Urge incontinence

65
Q

Urinary Retention - Tx?

A

Relax sphincter, ↓ prostate size
– α1-selective adrenergic antagonists
– 5 α-reductase inhibitors
– PDE5-inhibitor – Tadalafil (Cialis®)

66
Q

Female Sexual Dysfunction - Tx?

A
  • Oral or vaginal estrogen used to treat vaginal atrophy, dryness & dyspareunia.
  • Low dose transdermal testosterone appears to improve lack of sexual desire and arousal, but was rejected by FDA because long-term safety is unknown
  • Bupropion may increase sexual desire & arousal
  • Sildenafil - not likely useful, but “some patients do benefit”
  • Topical alprostadil cream applied to the genitalia for sexual arousal – mixed results.
  • Zestra – an OTC herbal massage oil is claimed to increase desire and arousal in one manufacturer funded study
67
Q

Sildenafil - efficacy in female sexual dysfunction?

A

In clinical studies, Sildenafil had little or no efficacy in treating female sexual dysfunction.
But “some patients do benefit”

68
Q

OTC herbal massage oil that is claimed to increase desire and arousal?

A

Zestra

69
Q

What drug?

Topical cream applied to the genitalia for sexual arousal – mixed results.

A

Alprostadil

70
Q

_____ may increase sexual desire & arousal in females.

A

Bupropion