Extra Pharm Flashcards

1
Q

What factors are unique about neonatal devo pharmacokinetics?

A
  • Slower GI, but faster IM absorption
  • More body water than lipid in early life
  • Limited protein binding
  • Larger liver/body weight ratio (and brain/body weight)
  • Immature enzymes
  • Higher BBB permeability
  • Immature renal function
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2
Q

How can drug 1/2 lives vary in neonates/young children?

A
  • Half-lives are longer in the neonate than the young child or adult
  • Dose adjustment may be necessary on an ongoing basis: ex of Phenytoin pharmacokinetics changing as the neonate ages, even over a period of days
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3
Q

How should drugs be adjusted for neonates?

A
  • Based on weight or surface area ratio to adults
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4
Q

How does breast milk affect drug transfer to the infant?

A
  • Acidic pH and high fat content, so will concentrate bases and lipid-soluble drugs
  • Lower transfer of highly protein-bound drugs
  • Drugs with shorter half-lives preferred; dose immediately after feeding, allowing levels to decline
  • Most cautious in early post-partum -> alveolar cells in breast milk buds mature in response to prolactin, reducing drug transfer to milk
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5
Q

Breastfeeding: Chloral hydrate

A

Drowsiness if fed at peak concentrations

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6
Q

Breastfeeding: Chloramphenicol

A
  • Antimicrobial
  • Grey baby syndrome if given directly to infant: vomiting, grey skin, hypotension, CV collapse, etc.
  • Blood dyscrasias and bone marrow suppression if exposed via breast milk
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7
Q

Breastfeeding: Diazepam

A

Sedation; accumulation in neonates

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8
Q

Breastfeeding: Heroin

A

Can produce narcotic dependence

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9
Q

Breastfeeding: Iodine (labeled)

A

Thyroid suppression

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10
Q

Breastfeeding: Lithium

A

Avoid unless levels quantitated

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11
Q

Breastfeeding: Methadone

A

Withdrawal if drug interrupted

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12
Q

Breastfeeding: PTU

A

Thyroid suppressed

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13
Q

Oxytocin

A
  • Most common drug used to induce labor
  • Half-life 10-12 minutes; discontinuation of the drug an effective way to alleviate adverse effects (MC: uterine hyperstimulation)
  • Excessive doses can predispose to post-partum bleeding
    1. Can also cause hyponatremia due to anti-diuretic effect
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14
Q

Dinoprostone

A
  • PGE2: timed-release suppository left in place for 12 hours -> can be removed if hyperstimulation occurs
  • Cervical ripening
  • GI side effects and fever uncommon with vaginal administration
  • Can start Oxytocin 30-60 min after removal
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15
Q

Misoprostol

A
  • PGE1
  • Intravaginal tablets Q3-6 hrs
  • Oxytocin should NOT be given within 4 hours of last dose
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16
Q

Carboprost tromethamine

A
  • PGF-2-alpha
  • Oxytocic properties (labor induction), and can reduce post-partum bleeding
17
Q

Magnesium sulfate

A
  • Parenteral: anti-convulsant that depresses the CNS and blocks peripheral neuromuscular transmission
  • To treat hypomagnesemia
  • Prevent/control preeclampsia/eclampsia; contraindicated in women with Myasthenia Gravis
  • IV: immediate effect, lasting 30 minutes
    1. IM: onset in 1 hour, and lasts around 4 hours
  • Crosses placenta, and excreted into breast milk, but no reported problems
  • Renal excretion: Mg reabsorbed -> impaired renal function can lead to toxicity, characterized by flushing, nausea, blurry vision, headache, hypotension, and pulm edema
  • Orally: laxative effect
18
Q

Indomethacin

A
  • Non-selective COX INH: delays/prevents premature parturition
  • Loading dose, followed by more doses Q6hrs
  • Maternal side effects: related to GI tract (N/V, gastritis, reflux), platelet dysfunction
  • Fetal side effects: premature closure of ductus arteriosus, oligohydramnios
  • Seems to be safe and effective as a tocolytic when used for a short period of time
19
Q

Menotropin

A
  • From urine of post-menopausal women
  • Contains FSH, LH (IM injection) -> INFERTILITY TX
  • Recombinant FSH also used subq
20
Q

How does estrogen affect protein synthesis?

A
  • INC synthesis of several hepatic proteins: TBG, transcortin, SHBG, clotting factors
21
Q

Ethinyl estradiol

A
  • Synthetic estrogen -> ethinyl groups greatly reduce hepatic metabolism (can’t give native estrogens orally)
22
Q

Clomiphene/Fulvestrant

A
  • Ovulation induction for infertility in anovulatory women
  • Anti-estrogens (SERD’s)
  • Act on ER’s in the hypothalamus to block feedback INH of natural estrogens and stimulate release of GnRH, which stimulates pituitary to INC LH and FSH secretion, leading to ovulation
  • Can be used to treat PCOS
23
Q

Minipill

A
  • Low-dose progestin: blocks ovulation in 60-80% of cycles
  • Impairs sperm transport by thickening cervical mucus
  • DEC motility of ovules in oviduct, altering endo to impair implantation
  • Taken daily and continuously
  • Best for women who are breastfeeding or over 35 and smoke
  • May cause acne and weight gain
24
Q

How can combo pills be used to treat PCOS?

A
  • Used “off-label”
  • Reduced dysfunctional uterine bleeding, and dysmenorrhea
  • Menstrual regularity, INC hemoglobin
  • Raise SHBG, DEC androgens, so less hirsutism and acne
25
Who can't use the transdermal combo patch?
- Women \>90kg because too much adipose tissue
26
Depo-provera
- Progesterone only =\> usually medroxyprogesterone - _Injected every 3 months_ - Amenorrhea common, but irregular bleeding can occur - AE's: weight gain, headache, _DEC bone density_ - Discontinue after 2 years, unless no other alternative -\> _6-12 mo delayed fertility_
27
Copper IUD
- 10-15 years - Spermicidal -\> fertility quickly restored upon removal - FDA-approved for dysmenorrhea bc \< blood loss - AE's: copper may cause cramping
28
Mifepristone
- Blocks binding of progesterone to its receptor - FDA-approved for termination of pregnancy - Main side effect is abdominal cramping
29
Spironolactone
- Primarily used as an aldosterone antagonist for the tx of primary or secondary hyperaldosterism or as an antihypertensive (diuretic) - Competes for testosterone receptor - Used as a treatment for hirsuitism in women