PHARM 1 Flashcards

1
Q

What does larger vs smaller volume of distribution mean

A

smaller– usually stays in blood larger- usually stays in fat/tissues (lipid soluble)

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2
Q

Drugs that have diff effects on women

A

CV drugs (higher risk of torsades/ prolonged QT) Zolpedim (ambien) (lower clearance and vol distr) Digoxin- may incr mortality ACEI- incr cough in women Ethanol- higher BAC

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3
Q

What does preganancy do to clearance and Vd

A

INcreases vd from incr fat (so less in blood) and increases clearance

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4
Q

What does preg do to levels of seizure drugs?

A

Incr vd decr it in blood, and so does incr in clearance, thus will be less effective and there will be more seizures

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5
Q

What are some teratogens in the first trimester>

A

Warfarin, Phenytoin, Valproate also thalidomide, lithium, DES (usu not taken in preg)

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6
Q

What can Warfarin, Phenytoin, and Valproate do as teratogens?

A

warfarin- facial and CNS abnorm, skeletal dysplasia Phenytoin- craniofacial, limb effects, growth def Valproate- spina bifida

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7
Q

What are some teratogens of second or third trimester?

A

Warfarin again, heparin, ACEI, tetracyclines, aminoglycosides

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8
Q

SxE of later trimester drugs Heparin Warfarin ACEI Tetracycline Aminoglycosides

A

hep- osteoporosis in mothers warfarin- fetal brain bleed ACeI- oligahydramnios, fetal renal failure and abonormal skull ossif Tetras- stains on teeth aminoglyco- ototox, renal tox (rev)

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9
Q

What are some breast milk sxe drugs?

A

Phenobarbital (seizure), naldixic acid/sulfonamide/nitrofurantoin(UTIs), lithium, alc ABX

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10
Q

Sxe in breast milk of Phenobarbital Nalidixic acid/nitrofurantoin/Sulfonamide Lithium Ethanol

A

Pheno- for seizures, but can sedate baby nalidixic/nitros/sulfon- hemolysis risk in G6PDH def kids LIthium- hypothermia, hypotonia, cyanosis (for bipolar) Ethanol- slow met in infants due to them having lower alc dehydrogenase

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11
Q

Category A-X drugs

A

A- not harmful B-safe if CLINICAL NEED C- safe ONLY if potential benefits outweigh risks D- evidence of risk to fetus X- do not use

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12
Q

How does clearance differ in baby, and what is an example of a drug that is affected by the differing HEPATIC clearance?

A

-infants have lower hep and renal clearance of drugs, lower gfr -example if Chloramphenicol which is excreted in bile: infants have lower glucoronyl transferase so this prolongs the half life in serum, causing Gray baby syndrome (cardiovascular collapse and death) -kids also have incr Vd (incr fat?)

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13
Q

Drug affected (in infants) by differing renal clearance?

A

Gentamicin, an aminoglycoside– levels are increased causing hearing loss

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14
Q

How should you change dosing in kids based on differing Vd and renal clearance?

A

increase loading dose due to Vd increase, and then increase dosing INTERVALS (time in between doses) due to incr in renal clearance (eg in aminoglycosides like gentamycin to avoid ototox)

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15
Q

What can Sulfonamides and Ceftriaxone do to babies and why?

A

They can cause kernicterus! (brain injury due to accum of bili) This is due to the fact that albumin normally binds free bili, but some drugs like cef and sulf can displace this bind-up causing serum unconj bili to accum

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16
Q

Tetracycline indications in infants?

A

stains teeth AND inhibits bone growth! -DO NOT GIVE in preganancy or under 8!

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17
Q

quinolones (fluoros like -floxacins) indications in infants?

A

can damage tendons and growing cartilage, dont give to ANY kids under 18!

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18
Q

Why might drugs affect geriatrics more strongly (what reasons)?

A

taking more meds, usu women, slower gastric emptying eg on antacids etc, reduced body water so decr Vd of water soluble drugs (need less!) and incr body fat so incr Vd of lipid sol drugs (need more!), renal blood flow and filtration decrease, and so does creat due to loss of muscle mass (unreliable indicator of renal fxn in elderly), decr hepatic blood flow (inhib met), elev in half life can accum to toxic levels

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19
Q

What do combined oral contraceptives contain/generally do?

A

They have combined estrogen which inhbits rel of FSH from ant pit, decr breakthrough bleeding, incr number of progestin receptors and progestin–thickens cervical mucus so sperm blocked, may inhib LH surge

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20
Q

Adverse effect of combined oral contraceptive on uterus?

A

polyp formation (in breast, suppresses lactation)

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21
Q

Contraindications of combined oral contraceptives?

A

THROMBO events (bc can coag), estro-dep neoplasm (obv), p450 drugs reduce efficacy

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22
Q

Serious side effects that are more rare in COCs

A

DVT, MI/stroke from hypercoagulability (smoking increases this risk, dont use prior to surg)

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23
Q

Timing of combined oral contraceptives?

A

must be taken at same time every day, can cause breakthrough bleeding, can cause the usual weight gain headache etc

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24
Q

What pop is progestin only contraceptives useful for>

A

women who cant take estro or are breastfeeding (unlike COC it doesnt reduce breast milk prod), have migraines, have heavy periods causing anemia, or smokers

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25
Q

Timing of POPs?

A

same time every day! bc it thickens and then thins cerv mucus throughout day

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26
Q

Depo medroxyprogesterone?

A

high dose progestin injxn that is able to prevent ovulation in all patients from decreasing freq of GnRH pulses from hypothal (preventing LH spike)

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27
Q

Sxe of progestin only contraceptives

A

breakthrough bleeding, and headache, usual etc -the lower gnrh can decr estro causing osteoporosis -Ca2+ depletion so should only be used for 2 yr max -decr HDL incr LDL, higher likelihood for ectopic preg if occurs

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28
Q

CxI of progestin only contraceptives?

A

undiagnosed vaginal bleeding, liver disease, BC, p450 -doesnt prevent ovarian cysts as well as COC, very careful timing (may need backup)

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29
Q

Advantages of POP over COC?

A

fewer sxe than extro, okay for DVT/emoblism/HTN/obesity/DM, safe during lactation, safe for sickle cell, easily reversible bc ovulation starts again after discontinuation

30
Q

Non oral contraceptive examples?

A

transdermal patch, ipmlanon (in skin), vaginal nuva ring, injxn like depo, IUD (copper or levon)

31
Q

Transdermal patch

A

ethinyl estradiol-norelgestromin -similar to coc, but higher sxe bc more estro plasma, -CxI smoking, preg, estro cancer, hep etc (similar to coc)

32
Q

Implanon

A

thin plastic under skin, Progestin only! -sxe irreg bleeding, cxi same as pop, 3 yr

33
Q

Vaginal nuva ring

A

similar to coc, incr incidence of vaginitis and vag secr, adv is lower doses of hormones so avoids daily fluctuations seen with pills

34
Q

IUD

A

-either copper releasing, or levonorgestrel releasing (mirena) copper toxic to sperm, thickens cerv, sxe cramping and abd bleeding, cxi is anatomical abnormalities and active pelvic infxn, and copper allergy -adv: opper effective for 10 yr, levo for 5, cheap

35
Q

What are the 3 main types of EC?

A

oral hormonal pills (COC or POP) copper iud mifepristone

36
Q

oral pill EC (emergency contraception)? what may make it less effective? which type is best?

A

-inhibits ov preg etc before implantation, etc etc -should take within 72 hr, less effective if vomit or diarr or if 2nd dose missed -POP better with fewer side effects (PLAN B)

37
Q

CxI of oral pill EC?

A

preg, BC/endomet cancer, thrombo, liver dis -usual sxe

38
Q

What is plan B

A

progestin only oral EC (levonorgestrel)

39
Q

Copper IUD EC

A

effective within 120 hr, prev implantation by changing lining of uterus, etc

40
Q

Mifepristone EC MOA, Cxi

A

synthetic steroid that competitively inhibits progesterone receptors and anti-glucocorticoid, abortifacient bc can be fatal to fetus if given after conception, but can also be used as EC if taken after intercourse but before ovulation CxI: contrind with ectopic preg /mass, IUD, adr failure, long term corticosteroid tx, anticoag tx/hemmor disorders, porphyries, after 63 days gestation, after ovlulation as EC

41
Q

Which EC is most effective?

A

copper IUD, then plan b, then coc (not always effective), the sooner taken, the better

42
Q

Estrogens/ gonadotropins/ GnRH agonist drugs?

A

Estradiol, DES, Leuprolide

43
Q

Antiestrogens/SERM drugs?

A

Clomiphene, tamoxifen, raloxifene

44
Q

Progestin drugs?

A

Medroxyprogesterone (depo-provera), norethindrone mini pill, and levonorgestrel

45
Q

Androgen drugs?

A

Test, Fluoxymesterone, and Danezol

46
Q

Anti-androgens/ anti-progestins

A

Mifeprisone, Dutasteride and finesteride

47
Q

Estradiol/ mestranol uses

A

act on estro receptor -used in hypogonadism, dysmenorrhea, contraceptive and morning after pill, endometriosis, postmenopause HRT

48
Q

estradiol and mestranol SxE and CxI?

A

SxE endometrial carc/BC, MI/stroke, dementia CxI preg, genital bleeding, BC, thrombo, smoking

49
Q

DES use

A

same MOA as estradiol, used for prostate carc, previously used to prevent premature death

50
Q

DES SxE

A

Clear cell adenocarcinoma in daughter

51
Q

Leuprolide MOA and use

A

GnRH agnosit pulsatile (continuous) dose, causes antag effects lowering estro levels -use in endometriosis (growing outside uterus), uterine fibroids -use with weak acting estrogen like estriol to offset menopause sx

52
Q

Clomiphene MOA and use

A

-inhib estro R at hypothal and blocks feedback inhib to decr GnRH -use: infertility, induces ovulation

53
Q

Clomiphene sxe

A

ovarian hyperstim causing cysts, hot flashes, nervousness, nausea etc

54
Q

Tamoxifen MOA and use

A

partial agonist, inhib estro by binding to receptor and preventing estro sensitive tumors, use in ER(+) BC

55
Q

Sxe Tamox

A

Uterine cancer and thromboembolism

56
Q

Raloxifene MOA and Use

A

Antag, prevents post menopause osteoporosis, prevent BC

57
Q

sxe of raloxifene

A

Thrombembolic events

58
Q

Progesterone MOA and use

A

similar to estro, contraceptive via negative feedback on GnRH release so no LH surge so no ovulation -use as contraceptive, control of uterine bleeding, endomet, dysmen

59
Q

sxe progesterone

A

weight gain, thrombo etc

60
Q

Medroxyprogesterone (depo-provera) use and moa

A

inhib GnRH rel to inhib follicle maturation and ovulation -use for contraceptive, injxn

61
Q

Depo sxe?

A

bone loss

62
Q

Mini pill norethindrone moa and uses

A

thickens cervical mucus, progestin oral contraceptive

63
Q

Testosterone MOA and uses

A

binds androgen receptors, cannot be given orally due to hepatic inactivation from first pass effect -use in hypogonadism

64
Q

side effects of test

A

increased LDL and decr HDL, aggr/psychosis, hep, cholestatic jaundice, closure of epiphyses, priapism and decr sperm count, masc of women

65
Q

Danazol (in pharmwiki only) MOA and use

A

synth test analog, partial agonist to a bunch of receptors, suppr pit-ovarian axis -used for fibrocystic breast dis, endometriosis, hereditary angioedema

66
Q

danezol sxe and cxi

A

thromboemb, androgenic effects, intracranial htn cxi: breast feeding, preg

67
Q

Fluoxymesterone MOA and use

A

similar to test but more potent, use in mammary cancer in postmen women, hypogonadism in men

68
Q

Mifepristone MOA and use?

A

progesterone R antag (and clucocorticoid R antag to tx cushings) -use: termination of intrauterine preg in first 49 days gestation, hyperglycemia of cushings

69
Q

mifepristone sxe

A

fetal infxn, prologned vaginal bleeding

70
Q

Dutasteride and finasteride moa and uses

A

Inhibits 5-a reductase preventing test from being conv to active DHT, duta inhibits both I and II and fina inhibs type 2 only, takes months -both are for BPH!, fina is for baldness

71
Q

dutasteride and finasteride sxe and cxi

A

sxe: importence, decr libido, gynecomastia -cxi: preg, cant donate blood for 6 months