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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
Ergot Alkaloids - MOA?
- Agonists and/or antagonists at 5-HT, dopamine & α-adrenergic receptors Produce strong uterine contractions: – Low doses – clonic contractions – High doses – tonic contractions
26
Ergonovine - Drug class?
Ergot Alkaloid
27
Methylergonovine - Drug class?
Ergot Alkaloid
28
Methylergonovine - uses?
↓ bleeding postpartum or after abortion | IM or IV
29
Ergonovine - uses?
↓ bleeding postpartum or after abortion | IM or IV
30
Ergonovine - AEs?
NVD, vasospasm, bowel ischemia
31
Methylergonovine - AEs?
NVD, vasospasm, bowel ischemia
32
Tocolytic Agents - what are they used for?
Objective is to inhibit premature labor (< 36 weeks) to permit further fetal development
33
What types of drugs may function as Tocolytic agents?
- β-2 agonists - MgSO4 & Calcium Entry Blockers (CEB) - COX-inhibitors (NSAIDS) - Atosiban – Oxytocin Receptor Antagonist - (Hydroprogesterone or Progesterone)
34
Via what molecular mechanisms do myometrium cells contract & relax?
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
Ritodrine - what is it?
- β-2 agonist, Tocolytic
36
Terbutaline - MOA?
β-2 agonist (Tocolytic) that should NOT be used in pregnant women more than 48-72 hrs
37
Albuterol - MOA?
β-2 agonist - Tocolytic that should NOT be used as a tocolytic
38
β-2 agonists - AEs?
``` – ↑ maternal & fetal HR – Arrhythmias – Hypokalemia – Maternal pulmonary edema – Myocardial ischemia – Skeletal muscle tremor – Hyperglycemia ```
39
Magnesium Sulfate (Mg2SO4) - MOA?
- ↓ Ca(2+) for contraction (causing relaxation) | Tocolytic agent that shouldn't actually be used as a tocolytic
40
Magnesium Sulfate (MgSO4) - AEs?
``` – Hypermagnesemia, Hypocalcemia – Flushing, nausea, vomiting – Headaches, visual disturbances – Muscle paralysis – Cardiac electrical disturbances – Pulmonary edema ``` - Use is discouraged!
41
Nifedipine - MOA?
Calcium-channel blocker | - yet another Tocolytic drug that is not approved in the USA
42
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.
Nifedipine
43
Nifedipine - AEs?
``` – Dizziness, lightheadedness, nervousness – Flushing, headache, nausea – Muscle cramps or tremors – Hypotension – ↓ fetal blood supply ```
44
NSAIDS - MOA as Tocolytics?
(COX-inhibitors) inhibit uterine contractions, prolonging gestation and/or slowing labor
45
Combination of _____ with other tocolytics provides enhanced tocolysis
NSAIDs
46
NSAID use as tocolytic agent - encouraged or discouraged?
Use is discouraged because of potential adverse effects on fetal development – closure of ductus arteriosus
47
Atosiban - MOA?
- Synthetic peptide analog of oxytocin - Oxytocin Receptor Antagonist - Specific for uterine smooth muscle -- (not a general smooth muscle relaxant) • Not available in US
48
Atosiban - used in USA as Tocolytic?
No, it's available in 30 countries but NOT the USA due to efficacy/safety concerns
49
Atosiban - AEs?
Nausea & vomiting, headache, dizziness, flushing, tachycardia, hypotension, hyperglycemia
50
a) What is the only FDA-approved Tocolytic drug that we learned about?
a) Hydroxyprogesterone
51
Hydroxyprogesterone - uses?
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
What is the benefit on infant mortality from Hydroxyprogesterone in a woman w/ a Hx of preterm births?
Hydroxyprogesterone causes reduced # of preterm births, but has NO EFFECT on infant mortality
53
Hydroxyprogesterone - MOA?
Progesterone (Tocolytic)
54
Hydroxyprogesterone - AEs?
Nausea & vomiting, headache, dizziness, flushing, tachycardia, hypotension, diarrhea, hyperglycemia, depression
55
Stress urinary incontinence - Cause?
- ↑ intra-abdominal pressure | - weakened pelvic muscles
56
Stress urinary incontinence - Tx?
``` ↑ sphinctor contraction – α1-adrenergic agonist (pseudoephedrine) – estrogens (?) – TCA (imipramine) – exercise, surgery, implants ```
57
What is Urge urinary incontinence?
Sudden involuntary bladder contraction – Bladder contracts at inappropriate volume – Also called detrusor instability, irritable bladder, spasmodic bladder, etc.
58
What is Stress urinary incontinence?
Involuntary loss of urine with physical activity (coughing, laughing, etc.) - Common in women – ↑ age, pregnancy - Cause:  intra-abdominal pressure weakened pelvic muscles
59
Urge urinary incontinence - Tx?
↓ detrusor instability – Muscarinic antagonists/ antispasmodics --- Oxybutynin, Tolterodine
60
AEs of antimuscarinics used for Urge Incontinence?
``` – Dry mouth – Blurred vision – Dizziness – Constipation – Urinary retention – Sedation ``` Many patients may not tolerate AE’s – use adult diapers
61
Urge incontinence drug available as SR & patch, which may ↓ peak plasma concentrations – reducing systemic AE’s
Oxybutynin
62
Newer agent used for Urge Incontinence claimed to be bladder selective (M3 receptors)? – less dry mouth
Tolterodine
63
Tolterodine - MOA?
M3-selective (supposedly) anticholinergic | - less AEs, like dry mouth
64
Tolterodine - uses?
Urge incontinence
65
Urinary Retention - Tx?
Relax sphincter, ↓ prostate size – α1-selective adrenergic antagonists – 5 α-reductase inhibitors – PDE5-inhibitor – Tadalafil (Cialis®)
66
Female Sexual Dysfunction - Tx?
- 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
Sildenafil - efficacy in female sexual dysfunction?
In clinical studies, Sildenafil had little or no efficacy in treating female sexual dysfunction. But “some patients do benefit”
68
OTC herbal massage oil that is claimed to increase desire and arousal?
Zestra
69
What drug? | Topical cream applied to the genitalia for sexual arousal – mixed results.
Alprostadil
70
_____ may increase sexual desire & arousal in females.
Bupropion

OSD_Repro (15 decks)

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