Pharmacology Flashcards

1
Q

Tx for HSV

A

acyclovir, vala-, and fam- = not curative, can decr. symptoms

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2
Q

MOA for acyclovir and vala-

A

inhibit viral DNA polymerase action (preferentially over host DNA polym.) by inserting into the growing chain and preventing further elongation.

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3
Q

how is acyclovir spec for virally infected cells?

A

dependant upon viral thymidine kinase for the first of three phosphorylations needed to be active drug.
has 100xs greater affinity for the viral polymerase than the hosts

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4
Q

MOA for famciclovir

A

metabolized to penciclovir,competitive inhib of viral DNA polymerase, does not cause chain termination (ACV does)

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5
Q

why does ACV have two dosing regimens?

A

the higher the does of ACV the less its bioavailability, so if you want to increase the dose, you have to give less but more frequently.

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6
Q

Mechanism of resistance to ACV, vala-, fam-

A

mutation of viral thymidine kinase (70%), or mut of viral DNA polymerase so that it won’t take up the modified bases.

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7
Q

AE of ACV and vala-

A

access the CNS- neurotoxicity, limited solubility so can precip. in kidneys and cause nephropathy

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8
Q

AE for famciclovir

A

really none, maybe headache. why isn’t this used then? more expensive and not as well studied as ACV

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9
Q

Tx for syphillis

A

PCN (the benzathine formulation = IM producing a extended release over 2 weeks)

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10
Q

AE for PCN

A

hypersens is biggest problem - if pt must be treated, then desensitize and give anyway.
renally excreted - caution in renal problems

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11
Q

jarisch-herxheimer rxn

A

70-90% of pts w/ 2 syph treated w/ PCN = chills, fever, HA, myalgias and arthralgias, cut. lesions become more brilliant. prob due to rel of spirochete antg. and do not discont. PCN tx.

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12
Q

tx for chlamydia

A

azithro or doxy (can sub erythro, levofloxacin, ofloxacin)

* assume co-infection w/ GC and give ceftriaxone as well until proven otherwise

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13
Q

contraindications for doxycycline in Ct tx, AE

A

pregnancy, replace w/ amoxicillan, photosens, hepatic damage in high doses

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14
Q

MOA of azithro, erythro (macrolides)

A

inhib the 50s ribosomal subunit, bacteriostatic

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15
Q

MOA of doxy (tetracycline)

A

binds the 30s ribo. subunit, bacteriostatic

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16
Q

MOA of -floxacins

A

flouroquinolones, inhibit DNA gyrase (topo II), bacteriocidal
levo= gram neg
oflo= gram pos (topo IV)
cipro= both pos and neg

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17
Q

AE of -floxacins

A

BBW for incr. risk of tendonitis and rupture and musc weakness
Preg cat C - animal studies show damage, not recomm.

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18
Q

Erythromycin AE

A

CYP inhibitor and P-gp

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19
Q

ceftriaxone, cefixime MOA

A

3rd gen cephalosporin, bacteriocidal beta lactam- causes cell lysis thru cell wall disruption.

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20
Q

tx for GC

A

ceftriaxone (IM) or cefixime PLUS Azithro or doxy

  • the others are oral.
  • azithro and doxy are incl. for coverage of Ct which is presumed present until proven otherwise, also helps reduce devlmpt of resistance in GC
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21
Q

tx for trichomoniasis

A

metronidazole or tinidazole

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22
Q

MOA for metronidazole, tinidazole

A

bacterio- ameb- and trichomonacidal, reduced to active form inside the cell and disrupts DNA helix

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23
Q

AE for metro and tinidazole

A

preg. cat B, not recomm during 1st trimester or breastfeeding, may predispose to malignancy

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24
Q

BV tx

A

metronidazole (or tinid), or clindamycin

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25
Q

MOA and AE for Clindamycin

A

binds 50s ribo subunit (similar to macrolide but is a lincosamide), bacteriostatic,
AE= C. diff is classically assoc. with this, not recommended for vaginal use after the 1st trimester in pregnancy can cause complications

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26
Q

tx for candidiasis

A

Azoles, OTC or prescription

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27
Q

MOA for conazoles

A

block ergosterol synthesis through inhib the cyp enzyme necc for converting it to this necc membrane component

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28
Q

AE for conazoles

A
  • avoid in 1st trimester - birth defects
  • can weaken latex condoms - unintended prey
  • fluconazole - potent cyp 2C9 inhibitor
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29
Q

What is the antigenic component of the HPV vaccine?

A

recombinant L1 protein ( a capsid protein) - the only component of the virus found in the vaccine so it is incapable of causing any dz

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30
Q

diff btwn gardisil an cervarix vaccine

A

Gardisil - covers HPV 6, 11, 16, 18
Cervavix - 16 and 18 only
*$300 not covered by insurance, three shots
recommended for m and f < 26 y/o

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31
Q

tx for genital warts

A
  • 90% caused by HPV 6,11
  • don’t elim. infectivitiy but can reduce
  • Imiquimod (immune resp modifier)
  • Podofilox - box MT in keratinocytes
  • Sinecatchins - antioxidant green tea extract
32
Q

three types of estrogen

A

estradiol E2
estrone E1
estriol E3

33
Q

which is the weakest estrogen and also made by the placenta

A

Estriol E3, also made by conv. of 2 and 3 in the liver and adipose

34
Q

what enzyme converts androstenedione and T into estrone and E2

A

aromatase

35
Q

what effect does administr. of E2 have on Sex Hormone Binding Globulin

A

it increases its transcription, thus the amount of free estrogen and androgens goes down.

36
Q

what molecule binds Progesterone in the blood

A

transcortin, same as cortisol

37
Q

where is E Recp. B located primarily? ERa?

A

prostate gland and ovary, female reprod. tract = ovary, uterus, vagina

38
Q

Effect of E’s on lipid

A

incr. HDL and decr. LDL

39
Q

Effects of E on bone

A

decr. # and activity of osteoclasts, hastens bone maturation and closure of epiphyseal plates of long bones

40
Q

Effects of E on liver

A

incr. synth. of TBG, transcortin, SHBG, and clotting factors (hypercoagulable)

41
Q

Effects of E on sexual devlpmt

A

stim breast tiss ( and tumors) as well as the dvlpmt of the endometrium during the proliferative phase. increases libido

42
Q

action of P on carb/lipid metab

A

enhances storage and transfer into tissues - thus it incr. insulin and incr glycogen synth. it also decr HDL and incr LDL while stimulating LPL so that the tissues can take up more lipid

43
Q

effects of P during pregnancy

A

released initially by the rescued corpus luteum and then by the placenta itself. maintains the decidua of the uterus, inhibits uterine contraction, alveolobular dvlmpt of the breast but inhibits lactation, thickens cervical mucous

44
Q

SERMs

A

selective E Receptor Modulators. tamoxifen, raloxifene, torimifene
-selective b/c they have estrogenic effects in tiss. where it is beneficial (bone, brain, liver), but block its effect in the breast or endometrium (useful for those cancers)

45
Q

clomiphene, fulvestrant

A

true anti estrogens, pure antagonist in all tissues. –b/c it blocks the feedback of ER on the hypothalmus it stimulates the release of GnRH and thus LH/FSH and thus stimulates ovulation, incr. E levels

46
Q

anastrozole, letrozole

A

aromatase inhibitors. used for breast CA after SERM failure

47
Q

estrogens incr risk of ________ in women, esp those who _________

A

clots (DVT, stroke, PE), smoke

48
Q

synthetic E for use in BC

A

ethinyl estradiol, mestranol

49
Q

synthetic progestin for BC

A

norethindrone, norgestrel, levonorgestrel

50
Q

side effects of E/P BC

A

incr. risk of thromboembolic events (E), GI disturbance (both), changes in lipid levels (P), breast enlgmt (E), acne and weight gain (P)

51
Q

non-contraceptive uses of BC, benefits

A

regular cycles, decr. acne, incr hgb, reduce risk of ovarian and endometrial CA

52
Q

drugs that reduce effectiveness of BC

A

antibiotics (PCNs, Tetracyclines), Rifampin (CYP inducer), Anticonvulsants, St. Johns wort

53
Q

emergency contraception

A

lg dose of progestins (levonorgestrel), 50-80% effective if taken w/in 24-72 hrs of intercourse, prevents ovulation, no effect on implantation

54
Q

mifepristone

A

antiprogestin, RU 486, for termination of pregnancy 49 days or less, blocks binding of P to recp.

55
Q

side effects of T administration to men

A

feminization bc conv to E2, suppr. of LH/FSH leads to decr. testis size, decr spermatogenesis, decr. endog T, decr. HDL and incr LDL

56
Q

5-a-reductase inhibitors

A

finasteride, dutasteride. antag of the enzyme that conv. T to DHT (the more active form). Used for BPH, male patt. baldness
- teratogenic to male fetuses (no contact w/ pregnant F) no blood donation

57
Q

spironolactone

A

aldo antag for 1/2 hyperaldosteronism but also competes w/ T recp.

58
Q

what antimycotic has effects on the cyp p450 enzymes and thus inhibs T synthesis (and other steroid hormones)

A

ketoconazole - antitestosterone effects are a side effect of antifungal tx. not useful as primary tx

59
Q

what role does the parasymp. NS play in urination?

A

ps nn. stim M3 recp on the bladder and stim contraction of (detrusor) sm. musc and bladder emptying

60
Q

Role of sympathetic NS in urination

A

sympathetics act on B3 recp in the bladder and inhibit detrusor musc contraction Also act on a1 recp causing contraction of the urethra.

61
Q

Role of somatic NS in urination

A

the somatic (voluntary) NS controls the external urethral sphincter thru pudendal N action on Nicotinic recp (+)

62
Q

AE of anticholinergics

A

dry mouth, tachycardia, constipation, urinary retention, sedation, slowed cognition, mydriasis

63
Q

which of the antichol. has the most selectivity for M3 as opposed to the rest which are non-selective

A

darifenacin

64
Q

Which of the antichol. has almost no CYP metabolism as opposed to the rest?

A

trospium

65
Q

which two antichol. have ER formulations to make up for their otherwise extremely short 1/2 lives?

A

oxybutynin, tolterodine

66
Q

which antichol. drug is metablized to another form and not detectable in systemic circ?

A

fesoterodine

67
Q

contraindications of antichol.

A
  • angle closure or narrow-angle glaucoma
  • urinary or gastric obstruction
  • need for mental alertness
  • alzheimers type dementia (already a cholinergic defect)
68
Q

in which type of pt does botox tx for bladder dysfunction work best?

A

recomm. for those unresp. to antimuscarinics, but only worked in 60% of those pts, as opposed to 86% of pts for whom the antimuscarinics merely had too many side effects but were otherwise effective.

69
Q

what do sympathomimetics do for bladder control?

A

they activate the B3 recp causing relaxation of the detrusor muscle and they also activate the a1 recp causing contraction of the urethral sm musc.

70
Q

mirabegron, pseudoephedrine, ephedra, Ma-Huang

A

sympathomimetics for urinary incontinence

71
Q

AE of sympmim

A

epi like effects, incr BP, HR, anxiety, insomnia, interact w/ MAOIs.

72
Q

methionine

A

creates ammonia-free urine (odorless) by acidifying urine pH.

73
Q

which of the sympmim is less orally available than the others?

A

mirabegron, b/c has substancial CYP metabolism and is decr. by food also. Has a much longer 1/2 life than the others though.

74
Q

two drugs used to tx urinary retention - strenghten cholinergic mediated detrussor musc contraction

A

neostigmine - inhib AChE
bethanechol - muscarinic agonist
both have short duration of action (adminst often)
and poor oral bioavailability

75
Q

AE of the urinary retention drugs

A

syncope, diarrhea, stomach cramps, AV block, bradys, cardiac arrest, hypoTN, dizziness

76
Q

what effects do opiates have on the urinary system?

A

can cause urinary retention by inhibiting PS outflow from the spinal cord (s1-3) and hence detrussor activation