Pharm Reproductive Flashcards by Lori Shenep

Timing of drug exposure in utero is important; organogenesis occurs?

Weeks 3-9

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HCV first line tx?

acylovir (pro-Rx = valcyclovir - lower dose
Ae - neurotoxicity/ seizures
Nephrolithiasis (dose adjust w/ renal failure)
Resistance: requires thymidine kinase activation

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First line tx for syphillis?

Penicillin G

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Caused by release of spirochetes all at once in secondary syphilis hours after tx initiation

Jarisch-Herxhemier Rxn

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Macrolide given for Chlamydia; CYP3A4 interaction; in an infant can cause hypertrophic pyloric stenosis

Erythromycin

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4 classes of Rx to tx Chlamydia

Macrolides - Azithromycin or Erythromycin
Doxycyline - Tetracycline
Flouroquinolones - Levofloxacin or ofloxacin
B lactam - Amoxicillin

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3 class of Rx for Chanchroid

Similar to chlamydia except no tetracycline
Macrolides - Azithromycin or Erythromycin
Flouroquinolones -Ciprofloxacin
B lactam - Cetriaxone

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Rx regimen for Gonorrhea

Ceftriaxone or Cefixime (genital not oral)

and azithromycin & doxycycline(resistance)

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tx for trichomonas

Metronidazole (stops nucleic acid synthesis when reduced to ionized form) or Tinidazole
Has a disulfuram-like effect

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For ER+ metastatic BC w/ progression following anti-estrogen therapy
Contains a bulk substituent that prevents the dimerization leading to disruption of nuclear localization
Monthly IM, sustained levels

Selective Estrogen Receptor Down-regluator

Fulvestrant

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SERM
Estrogen antagonist in breast tissue and agonist in endometrial tissue
CYP2D6- suboptimal clinical effect in poor metabolizers  metabolized to enoxifen (more effective than tamoxifen),
5 years of tx
More effective for BRCA2 than BRCA1

Tamoxifen

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SERM
monthly IM injections
no endometrial agonism

Raloxifene

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SERM
2nd generation derived from Tamoxifen
No BBW in previous slides,
Prolongs QT (add. Moety that inhibits MTs)
Avoid w/ 3A4 inhibitors
Avoid w/ history of endometrial cancer/ hyperplasia, thromboembolic disease

Toremifene

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Current recommendation, after 5 years of tamoxifen, give add 5 years of aromatase inhibitors for post-menopausal woman
AE:
1- Increased arthralgia compared to SERMS
2- produce cataracts
4- more diarrhea than tamoxifen

**no good giving this Rx pre-menopausally because most of the estrogen comes from the ovary & giving this can stimulate GnRH release and drive estrogen up further
What are the non-steroidal AIs?
the steroidal?

Non-steroidal: Anastrozole, letrozole

steroidal (irreversible): exemestane

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mAb for HER2 extracellular domain

Cardiomyopathy, infusion rxns, respiratory insuffiency, hepatotoxicity

Trastuzumab

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HER2 EC domain linked to DM1 w/ BBW for HF, liver disease, ventricular dysfuncion

Ado-Trastuzumab

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mAb for HER2 dimerization domain

Pertuzumab

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TKI for HER1 and HER2; competes w/ ATP binding site
Liver Disease
interstitial lung disease, pneuomonitis, QT prolongation

Lapatanib

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Breast Cx tx
Less likely to be used; endocrine therapy
Only beneficial under limited circumstances
(will be seen less frequently)
Can be used if pre-menopausal at dx and wishes to keep option of childbearing open

Increases the pain arising from bone mets of cancer
(can cause a disease flair)

Goserelin

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mTOR inhibitor (central regulator of cellular proliferation, angiogenesis, cell metabolism)

Everolimus

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Tx for endometrial cx; binds to progestin receptors to decrease GnRH
Amenorrhea, edema, weakness, anorexia

Meroxyprogesterone

tx for endometrial cx

synthetic oral progestin, blocks LH, increases estrogen degedation; promotes mainentance of the endometrium

Megestrol

Bladder Cx
IVe instillation common
Mono & bi-funcional alkylating agent
Chemical cystitis, contact dermatitis, palmar, plantar erythema (poor hand hygiene) – contact w/ the void volume
Pulmonary infiltrates

Mitomycin

Bladder Cx
IVe (intravesicular instillation), can produce hemorrhagic cystitis
Polyfunctional alkylator w/ loss of aziridine (alkylator) moiety
Dysuria, urinary retention, hemorrhagic cystitis, renal dysfunction

Thiotipa

Prostate Cx GnRH agonists

Leuprolide Triptorelin Histrelin Goserelin

GnRH Antagonist

Degarelix | Hepatotoxic, QT prlongation

Androgen Receptor Blockers

Bicalutamide Enzalutamide Flutamide - more hepatotoxic Nilutamide - less hepatotoxic

Prostate Cx | Estrogen binding protein; inhibits MTs and causes ds breaks

Estramustine

Prostate Cx | Take the pt's APCs and modify them to attack the cx - then return to the prostatic acid phosphatase (PAP)

Sipuleucel

Inhibit 17 alpha hydroxylase to prevent production of DHEA and androstenedione increase aldosterone and cortisol

abiraterone

Anti-cholinergics for urinary incontinence | long acting available? - usually these are short acting selective

Oxybutynin - long-acting available | Tolterodine - long acting available

Anti-cholinergics for urinary incontience positively charged, cannot get across the blood brain barrier, so it is less likely to produce somnolence? non-selective quaternary amine no CYP metabolism

Trospium - + charge

Anti-cholinergics for urinary incontinence | highest oral avialability (VESicare)

Solifenacin - highest oral avia

Anti-cholinergics for urinary incontinence | M3 selective, poor bioavailability

Darifenacin

Used in pts response to anti-cholinerfics but who cannot tolerate the side effects

Botox

Tx urinary incontinence B3 agonist, increases bladder capacity by relaxing detrusser sm; decreased bioavailability with food, 3A4 >> 2D6 butylcholinesterase, UGT & alcohol dehydrogenase, ~10% as parental drug, ~50 hours Increases blood pressure, tachycardia

Miragebron

inhibits AChE; augments action of Ach at both muscarinic and nicotinic receptors; < 1 hour

Neostigmine [Prostigmin]

Prostaglandins - labor induction | 150 per insert, timed release, but can be removed from the vaginal fornix if uterine hyperstimulation occurs

Dinoprostone

Prostaglandins - labor induction | cheapest; oral; should not be used within 4 hours of OT due to risk of uterine rupture

Misoprostol, PGE1 (Cytotec)

most commonly used tocolytic Rx in the US;, which antagonizes calcium, at EC and IC levels – blocking membrane and intracellular channels which decreases myometrial contractility; neuroprotective agent (prevents cerebral palsy in infant) Monitor petallar reflexes & urine output/ Not used in women w/ myasthenia gravis, renal insufficiency  flushing, nausea, vomiting, blurry vision, headache, lethargy , HOTN, pulmonary edema Used to treat pre-eclampsia/ eclampsia; anti-convulsant

Magnesium sulfate

OT receptor antagonist (18 min half-life); only used in Europe not, FDA approved b/c increased deaths in infants exposed to Atosiban

Atosiban

2 common synthetic estrogens

Ethinyl estradoil | Mestranol

3 formulations of progesterone

Norethindrone Noregestrel Levonorgestrel

Injectable BC

Medroxyprogesterone

Progesterone implant

Etonogestrel

2 types of IUDs

Copper (kills sperm) progestin releasing (fertility is quickly restored after removal)

Morning after pill?

2 doses of levonorgestrel within 72 hours of intercourse

Termination of pregnancy:

Mifepristone (7 weeks) | Onapristone (anti-progeseterone)

Alpha receptors Lower - trigone, prostatic urethra, prostatic gland, penile urethra Upper - detrusser muscle

``` Lower = alpha 1a Upper = alpha 1d ```

Only alpha 1 blocker that requires titration

Prazosin

Alpha blockers for BPH - Common side effects? Advantage of selective alpha -1a blockers?

Common side effects? xerostomia, nausea, dizziness, insomnia No need for dose titration Retrograde ejaculation