Pharm Reproductive Flashcards
Timing of drug exposure in utero is important; organogenesis occurs?
Weeks 3-9
HCV first line tx?
acylovir (pro-Rx = valcyclovir - lower dose
Ae - neurotoxicity/ seizures
Nephrolithiasis (dose adjust w/ renal failure)
Resistance: requires thymidine kinase activation
First line tx for syphillis?
Penicillin G
Caused by release of spirochetes all at once in secondary syphilis hours after tx initiation
Jarisch-Herxhemier Rxn
Macrolide given for Chlamydia; CYP3A4 interaction; in an infant can cause hypertrophic pyloric stenosis
Erythromycin
4 classes of Rx to tx Chlamydia
Macrolides - Azithromycin or Erythromycin
Doxycyline - Tetracycline
Flouroquinolones - Levofloxacin or ofloxacin
B lactam - Amoxicillin
3 class of Rx for Chanchroid
Similar to chlamydia except no tetracycline
Macrolides - Azithromycin or Erythromycin
Flouroquinolones -Ciprofloxacin
B lactam - Cetriaxone
Rx regimen for Gonorrhea
Ceftriaxone or Cefixime (genital not oral)
and azithromycin & doxycycline(resistance)
tx for trichomonas
Metronidazole (stops nucleic acid synthesis when reduced to ionized form) or Tinidazole
Has a disulfuram-like effect
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
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
SERM
monthly IM injections
no endometrial agonism
Raloxifene
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
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
mAb for HER2 extracellular domain
Cardiomyopathy, infusion rxns, respiratory insuffiency, hepatotoxicity
Trastuzumab
HER2 EC domain linked to DM1 w/ BBW for HF, liver disease, ventricular dysfuncion
Ado-Trastuzumab
mAb for HER2 dimerization domain
Pertuzumab
TKI for HER1 and HER2; competes w/ ATP binding site
Liver Disease
interstitial lung disease, pneuomonitis, QT prolongation
Lapatanib
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
mTOR inhibitor (central regulator of cellular proliferation, angiogenesis, cell metabolism)
Everolimus