Anti-Virals & Antibiotics Flashcards
Acyclovir MOA
Competitively inhibits viral DNA polymerase; competes w/ deoxyguanosine triphosphate for incorporation into viral DNA
Acyclovir Tox
Neurotoxicity including seizures; Hydrate pt well to avoid crystalline nephropathy or neurotox
Acyclovir PK
Little metabolism; renal elim; dose adj in renal dysfxn or failure may occur
Interesting fact about acyclovir and oral dose levels
*Oral bioavailability DECREASES with INCREASING dose; Req TK activity
Famciclovir MOA
Competitively inhibits viral DNA polymerase; competes w/ deoxyguanosine triphosphate for incorporation into viral DNA
Famciclovir Tox
No significant issues; Hydrate pt
Famciclovir PK
Little metabolism; renal elim; dose adj in renal dysfxn or failure may occur
Benzathine Pen G MOA
Bactericidal Beta-Lactam: binds PBPs causing cell lysis
Benzathine Pen G Tox
Poor penetration of CSF (not good tx for neurosyphilis); HSR or skin rxns may be problematic; Jarisch-Herxheimer Rxn (do NOT D/C penicillin)
Benzathine Pen G PK
Rapidly eliminated via renal tubular excretion (delayed in renal dysfxn)
Benzathine Pen G Admin
IM admin produces a drug depot that liberates drug over 2 week period
Use of procaine Pen G
Congenital Syphilis
Azithromycin MOA
Binds 50S ribosomal subunit; Bacteriostatic
Azithromycin Tox
GI upset, vaginitis
Azithromycin PK
Little metabolism; most elim in stool; long half-life; extensive tissue uptake & slow release
Doxycycline MOA
Binds 30S ribosomal subunit; Bacteriostatic
Doxycycline Tox
GI upset; hepatic damage in high dose esp in pregnancy; photosensitivity w/ sunlight or tanning bed
Doxycycline PK
Little metabolism; most elim in stool; long half-life; extensive tissue uptake & slow release
Doxycycline Pregnancy Cat
D
Levofloxacin/Ofloxacin MOA
Inhibits DNA gyrase (topo II) in Gram-negative; Inhibits topo IV in Gram-positive; Bactericidal (both)
Levofloxacin/Ofloxacin Tox
Taste disturbance; GI upset; 2 BBW
Levofloxacin/Ofloxacin BBW
BBW=increased risk of tendonitis & rupture; BBW=exacerbation of muscle weakness-avoid in Myasthenia Gravis
Levofloxacin/Ofloxacin PK
Little metabolism; most elim in urine; medium half-life (prolonged in renal dysfxn)
Fluoroquinolones pregnancy cat
Cat C
Ceftriaxone MOA
Bactericidal Beta-Lactam: binds PBPs causing cell lysis
Ceftriaxone PK
Medium half-life; widely distributed; elim in urine primarily via GF
Metronidazole MOA
Unionized drug taken up by anaerobic organisms & cells where it is reduced to its active form which disrupts DNA’s helical structure; Amebecidal, bactericidal, & trichomonacidal
Metronidazole Tox
GI upset; candidiasis; disulfram-like effect (avoid alcohol for 24 hours after completing therapy); secondary malignancies maybe
Metronidazole PK
Medium half-life; widely distributed; extensive hepatic metabolism w/ elim primarily in urine & stool; Inhibits CYP2C9
Metronidazole in pregnancy
Avoid in pregnancy & breastfeeding
Metronidazole interesting fact
*Discoloration of urine upon elimination
Clindamycin MOA
Binds 50S ribosomal subunit to inhibit protein synthesis; Bacteriostatic
Clindamycin Tox
Systemic- GI upset; Local Vag- vaginal erythema, vulvovaginal pruritis, vaginal discharge, vaginal swelling, vaginal bleeding, vaginal pain
Clindamycin PK
Short half-life; extensive metabolism w/ elim of products in urine & stool; 30% of vaginally instilled drug becomes systematized
Clindamycin in breast feeding
Excreted in breast milk- no issues but caution
Clindamycin in pregnancy
Intravag use only in 1st trimester due to AE of low birth wt, pre-term, PPROM, & neonatal infxns
Butoconazole MOA
Blocks ergosterol synthesis through interacting w/ 14-alpha-demethylase, a CYP necessary for conversion of lanosterol to ergosterol
Butoconazole Tox
Oil-based products can weaken latex condoms or diaphragms
Butoconazole PK
Limited systemic absorption; peak serum levels in 12-24 hrs; residual fungicidal activity in vagina for several days; systemic drug ext metabolized & recovered in stool
Butoconazole in pregnancy
Avoid in 1st trimester; High systemic doses produce abdominal wall defects & cleft palate in fetus + maternal stress
Cervarix MOA
Bivalent: 16 + 18 - L1 protein
Cervarix Tox
Injection site irritation & pain may occur
Gardasil MOA
Quadrivalent: 6, 11, 16, 18 - L1 protein
Gardasil Tox
Injection site irritation & pain may occur