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ADR Exam 3

Terms in this set (129)

small MW drugs less than ___daltons can cross the placenta
less than 500 daltons
drugs greater than 1000 daltons are
insulin, heparin
there are more plasma protein bounds drugs on which side mother or baby
baby- drugs like warfarin will distribute more to fetal side
are weak acids or bases more likely to cross placenta
weak bases are more likely to cross the placenta because the fetal pH is more acidic
do lipophilic drugs readily cross the placenta
yes, opioids and antibiotics
drugs for diabetes in pregnancy
insulin, metformin, glyburide

PO agents lack long term safety
glyburide- risk of neonatal hypoglycemia
when do you start aspirin therapy for preeclampsia
60-150mg/day
start 2nd trimester to birth

ONLY if there's a preeclampsia risk (diabetes??)
drugs to use for hypertension in pregnancy
lifestyle management, labetalol, nifedipine, methyldopa, diltiazem, clonidine, prazosin
drugs to avoid in hypertension in pregnancy
ace, arb, renin inhibitors, mineralocorticoid receptor antagonists, atenolol
drugs to use in hyperlipidemia in pregnancy
omega 3 fatty acids
drugs not recommended to use in hyperlipidemia in pregnancy? avoid?
not recomm- niacin and fibrates
avoid- statins
drugs to use in hyperthyroidism in pregnancy? 1st trim? 2/3 trim?
Avoid?
1st trim- propylthiouracil (risk of hepatotox if used later on)

2/3 trim- methimazole

AVOID IODONE

complications: fetal death, low birth weight, intrauterine growth restriction, preeclampsia
ok meds to use for migraines and pain and nausea in pregnancy
sumatriptan, APAP, ibuprofen

nausea- promethazine, prochlorperazine, metoclopramide
meds to avoid for pain in pregnancy

nausea meds to avoid in preg
ergotamine, NSAIDs, aspirin, meloxicam (especially in 3rd trimester)

nausea- ondansetron- crosses into fetal tissue
migraine prophylaxis in pregnancy
propranolol

alternatives: TCAs ami and nortyptiline
complications od depression with pregnancy
premature birth, low birth weight, miscarriage, fetal growth restriction
drugs that can be used in depression in pregnancy
CBT, SSRIs, TCAs
what drugs to avoid for depression in pregnancy
paroxetine-- causes heart defects. can be used if benefit has been shown
drugs that can be used in bipolar disorder in pregnancy
lamotrigine-
drugs to avoid in bipolar disorder in pregnancy
lithium, valproic acid, and carbamazepine

lithium- congenital cardiac malformations, hypoglycemia, premature delivery
VPA- neural tube defects, craniofacial and CV abnormalities, fetal growth restriction, cognitive impariemtn
carbamazepine- facial dyspmorhpism, fingernail hypoplasia
drugs to use in asymptomatic bacteria/UTI in pregnancy
beta lactams- PCN and cephalosporins
drugs to limit in UTI in pregnancy
NTF- limit in 1st trimester, AVOID 38-42 weeks
Bactrim- avoid in 1st trim
drugs to treat VTE during pregnancy
LMWH > UFH
treat for >= 3 months
through pregnancy then 6 weeks after delivery for >= 3 months
for prosthetic heart valve in pregnancy
LMWH BID, UFH BID, low dose aspirin
drugs to avoid in VTE in pregnancy
warfarin, DOACs
drugs to use in cold/cough/rhinitis in pregnancy
intranasal corticosteroids- budesonide, beclomethasone
intranasal cromolyn
1st gen antihistamines
drugs to avoid during cold/cough/rhinitis in pregnancy
alcohol containing formulations (robitussin, dimetapp, nyquil)
-PO decongestant 1st trimester
-hydroxyzine

use of guaifenesin and dextromethorphan are OB specific
drugs to use in constipation in pregnancy
Moderate physical activity
Increased dietary fiber/fluid intake
Fiber supplementation
Stool softener
Psyllium, methylcellulose, polycarbophil
Osmotic or stimulant laxatives
drugs to avoid in constipation in pregnancy
magnesium and sodium salts-- electrolyte imbalance
mineral oil and castor oil
1st line GERD and pregnancy
lifestyle and dietary modifications
2nd line GERD and pregnancy
aluminum, calcium or mag containing antacids

Tums (calc carb) crosses placenta and increases intestinal absorption. avoid excessive use
3rd line GERD and pregnancy
H2RAs
avoid with GERD and pregnancy
Na bicarb, Mg trisilicate
PPIs-major birth defects
what should pregnant women do lifestyle modifications
avoid alcohol, smoking cessation, weight loss if obsessive, do not eat raw meat/seafood-(toxoplasmosis, salmonella), deli meat, smoked seafood, soft cheese(listeria), fish with mercury
additional drugs to avoid pregnancy
dronendatone, fluorouracil, temazepam, isotretinoin, mifeprostone, misoprostol, methotrexate, finasteride, dutasteride, hormone products
antibiotics that interact with Birth control
rifampin, PCNs, TCs
reduced ethinyl estradiol levels
what anticonvulsants interact with birth control
phenobarbital, CBZ, PHT - increase estrogen and progestin metal

LTG- reduced LTG efficacy
drospirenone(in some BC) with what increases potassium and interacts with oral contraceptives
ace/arb, aldosterone antagonists --inc potassium
who should be on progestin only pills or DMPA
breastfeeding, smoking and age >= 35, CI in CVA, VTE, some cancers, uncontrolled HTN, migraines with aura
estrogens and progestins are C/I with what
history of breast cancer, VTE, recent CVA, liver dx

consider: SSRIs(paroxetine) or SNRIs (venlafaxine)
if patient is on tamoxifen and paroxetine what is the issue
paroxetine goes through 2d6 and it inhibits tamoxifen metabolism to the active metabolite-- recommend and alternative
raloxifene cant be used with what?
cholestyramine
it interacts with warfarin because it is highly protein bound, monitor INR more closely
what two things interact with osteoporosis drugs?
calcium carb and vitamin D
osteoporosis patients on calcium carb interact with what by reducing calcium absorption
PPIs fiber laxatives, empty stomach
osteoporosis patients on what drugs reduce absorption of other drugs
iron, TCs, FQs, biphosphonates, thyroid supplements
osteoporosis patients on vitamin D with what drugs affects vitamin D metabolism
rifampin, PHT< barbiturates, VPA, CBZ
osteoporosis patients on vit D with what drugs reduce vit D absorption
cholestyramine, colestipol, orlistat
how do you administer bisphosphonates
separate all other meds by 30 mints, take with water only
azathioprine adverse effects
GI toxicity, myelosuppresion, hepatotoxicity, infections, malignancies, pancreatitis, alopecia
azathioprine interacts with what two drugs?what is the effect?
allopurinol and febuxostat inhibit the metabolism of mercaptopurine to inactive metabolite

increased antimetabolite effect, increased toxicity
what should you do to the azathioprine dose if patient is on allopurinol or febuxostat
reduce dose of azathiorpine by 25-33% and or allopurinol

monitor for BMS

could change to colchicine
what effect does ribavirin (used for Hep C) do to azathioprine
inhibitors metabolism of azathioprine-- increased toxicity esp myelosuppression

discontinue azathioprine during ribavirin course, reduce dose, monitor for BMS
adverse effects of CI and mTOR inhibitors
HTN, HLD, DM, GI, infection, malignancy, nephrotoxicity
what are the calcineurin inhibitors
cyclosporine, tacrolimus
what are the mTOR kinase inhibitors
sirolimus, everolimus
effect of inducers of 3A4 and or PgP with calcineurin or mTOR inducers
enhances metabolism of immunosupp and
CsA inhibits metabolism of interacting drugs

effect- dec serum drug levels and efficacy, CsA increased serum drug levels of interacting drugs

cyclosporine may inhibit and increase toxicity of inducer

need to reduce dose of calicin/mTOR inhibitor
effect of inducers of 3A4 and or PgP with calcineurin or mTOR inhibitors
inhibit metabolism of immunosupp and increase serum drug levels and toxicity

use alternative agent, empirically decrease dose
antimicrobials that inhibit 3a and or PgP with calcineurin or mTOR inhibitors
macrocodes, azoles, FQs, quinupristin

inhibitors metabolism of immunosuppressants, increase toxicity and drug levels

may see significant changes in short courses of antibiotics
adverse effects of mycophenolate
severe GI toxicity, HA, leukopenia, thrombocytopenia

drug monitoring available but not routinely used
what is the mycophenolate metabolism
mofetil (MMF) --> hydrolysis in liver to mycophenolic acid(MPA-active metabolite) --> glucoronidation in liver to mycophenolic acid glucoronide(MPAG- Inactive metabolite) --> recycled to liver via enterohepatic recirculation

Cellcept- inactive prodrug can be converted back to MPA
what's the diff between MMF and MMA
MMF- mycophenolate mofetil- cellcept

MMA- mycophenolic acid- myfortic
antibiotics interacting with mycophenolate and their effect
Amoxicillin/clav, cipro, flagyl

reduce plasma conc of MPA, dec serum drug levels and efficacy, increased risk of GVHD(?)

consider increasing dose of mycophenolate
what interaction to binding agents have with mycophenolate
binds mycophenolate metabolites in the GI tract and interefere with enterohepatic circulation-- dec serum drug levels and efficacy

use statins instead, separate antacids
what interactions do gastric antisecretories have with mycophenolate (h2ras and PPIs)
increased gastric pH decreases dissolution of mycophenolate, dec absorption and serum concentration of mycophenolate

consider enteric coated mycoplasma (myfortic) instead of cellcept

Dosing switch is not equivalent
disease interactions with calcineurin inhibitors and mTOR inhib
hypertension, hyperlipidemia, diabetes, kidney disease, grapefruit

nephrotox?
herbal supplements interactions with calcineurin inhibitors and mTOR inhib
boldo- reduce immunosupp conc
echinacea- may result reduced efficacy of immunosupp
st johns wort- may reduce efficacy of immunosupp by acting as an enzyme inducer
zinc- may reduced efficacy of immunosupp by acting as immunostimulant
methotrexate(at cancer doses) and amoxicillin/piperacillin interaction
inhibits tubular secretion of MTX --> MTX toxicity, BMS, GI tox
mycophenolate with amoxicillin interaction
inhibits enterohepatic recirculation--> reduced serum level of MPA
WARFARIN interaction with dicloxacillin and nafcillin
2c9 induction, reduced INR

MAJOR INTERACTION- may take one to two weeks for INR to update
what cephalosporins are affected by increasing gastric pH with gastric alkalinizers
cefditoren, cefpodoxime, and cefuroxime

decrease serum levels and efficacy
valproic acid interacts with what antibiotic
carbapenems --> dec enterohepatic circulation and reduced VPA concentrations and reduced seizure control
macrolide general interactions
3a4 substrates and inhibitors(Clarithromycin and eryth >azith)
pGp inhibitors
QTc prolongation and tornados when used with other QT prolonging agents
macrolide interaction with DOACs
3a4 and pgp inhibition --- increased concentration of anticoagulants and risk of bleeding
digoxin and macrolide interaction
pgp inhibition
2-4 fold increase in digoxin concentrations
immunosuppressant interaction with macrolides-
3a4 and pgp inhibition
increase conc of immunosupp --> toxicity
what FQ is a 3a4 inhibitor
cipro
fluoroquinolone general interactions
3a4 inhbitor
qtc prolongation
bi and trivalent cations
corticosteroids and FQ interactions
additive toxicity and inhibit metabolism of steroids (cipro) increased risk of tendon rupture
oral contraceptives and tetracyclines
enzyme induction--> menstrual irregularities --> unintended pregnancy
bactrim is what CYP substrate and inhibitor
2c9
trimethoprim acts as a
potassium sparing diuretic
warfarin and bactrim interaction
increased INR
sulfonylureas, nateglinide, rosiglitazone and bactrim interaction
hypoglycemia from 2c9 inhibition
mtx and bactrim interaction
inhibits renal tubular secretions --> mtx toxicity
phenytoin and smx interaction
2c9 inhibition and pht toxicity
procainamide and trimethoprim interaction
procainamide toxicity inhibits renal tubular secretion
QT prolongation
dofetilide and trimethoprim
competes for cationic tubular secretion -- dofetilide toxicity (QT)
zidovudine and trimethoprim
inhibits of glucoronidation and causes zidovudine toxicity (anemia)
drugs with additive toxicity to trimethoprim
Drospirenone, heparins, non-selective beta-blockers, NSAIDs, COX-2 inhibitors, cyclosporine, tacrolimus, succinylcholine, pentamidine, K-containing salt substitutes
-ace/arbs/K sparing diuretics
flagyl interaction with warfarin
2c9 inhibition, increased INR
flagyl interaction sulfonylurea, nateglinide, and rosiglitazone
flagyl and 2c9 inhibition- hypoglycemia
mycophenolate and flagyl interaction
inhibits enterohepatic recirculation --> reduced serum level of MPA
phenytoin and flagyl
2c9 inhibition and phenytoin toxicity
what TCAs interact with linezolid
clomipramine and imipramine

use an alternative such as amitriptyline, doxepin, despiramine

or use alternative antibiotic such as tedizolide, vanc, or telavancin
indirect sympathomimetics interaction with linezolid (Amphetamines
Cocaine
Dopamine
Ephedrine
Pseudoephedrine
Methylphenidate
Phentermine
Phenylephrine)
effect: modest increase in pressor response

use an alternative antibiotic (tedizolid, vanc, and telavancin)

monitor for hypertension, fever, seizures, and arrhythmias
azoles with 3a4 inhibition
itraconazole, ketoconazole, posaconazole > fluconazole
gastric antisecretories (H2RA and PPIs)
same for antacids
decreased absorption of azoles antifungals due to requirement of gastric acidity for absorption

use alternative (flu or vori)
use alternative dosage form (itra solution and posaconazole DR tablet are not affected)
administer with coke/pepsi
consider inc azole dose
warfarin with azole interaction
increased INR
sulfonylureas, nateglinide, and rosiglitazone and azole interaction
2c9 inhibition, hypoglycemia
phenytoin and flagyl interaction
2c9 inhibition, phenytoin toxicity
know that anti tubercular interact with lots of stuff
Isoniazid
Inhibits 2C19 and 3A4

Rifampin
Induces 1A2, 2B6, 2C8, 2C9, 2C19, 3A4, p-gp

Rifabutin
Substrate and inducer of 3A4

Bedaquiline
Substrate of 2C8, 2C19, and 3A4
anti TB drugs interact with what
DOACs, acetaminophen, and all the sulfonylureas?, CBZ, clopidogrel, phenytoin

lots of things no way of memorizing all
rifabutin and bedaquiline interactions with what 3a4 inhibiting antidepressants
decreased metabolism of rifabutin/bedaquiline so increased serum levels and toxicity
rifabutin toxicity
uveitis, rash, BMS, heptotoxicity
bedaquiline toxicity
hepatotoxic, QTc prolongation
alternative antimicrobials that are 3a4 inhibitors such as macrocodes, azoles, fq's, quinupristin
Fluconazole = weaker inhibitor than ketoconazole, itraconazole
Azithromycin = weaker inhibitor than erythromycin, clarithromycin
Ciprofloxacin = stronger inhibitor than other FQs
skipped al the random rifabutin and bedaquilines
ya
anti parasitic drugs
Chloroquine
2C8, 2D6 substrate
2D6 inhibitor

Hydroxychloroquine
2D6 inhibitor

Quinidine
3A4, p-gp, OCT substrate
2D6, p-gp, OCT inhibitor
QTc prolongation
anti parasitic drugs interactions
interact with thioridazine, DOACs and digoxin
antimicrobials with pgp activity inhibitors and inducers
P-gp Inhibitors:
Macrolides
Azole antifungals (itraconazole, ketoconazole, posaconazole)
Quinidine

P-gp Inducers:
Rifampin
antimicrobials with QT prolongation
Macrolides
Fluoroquinolones
Quinidine
zidovudine interaction with enzyme inducers
enhances glucoronidation of zidovudine and dec serum levels and efficacy and may lead to resistant viral strains
what are some glucoronidation inhibitors and what interaction do they have with zidovudine
probenecid, trimethoprim, VPA

dec hepatic metabolite and renal elim of zidovudine and inc serum levels and toxicity

consider alternative to zidovudine like satvudine
dec zidovudine dose
use alt glucoronidation inhibitor
which NNRTI on empty stomach
efavirenz
which NNRTI with high fat meal
rilpivirine
class wide protease inhibitor effects
hyperglycemia, hyperlipidemia
PIs sometimes need
food
PI with high fat meal
saquinavir
NNRTIs or PIs with enzyme inducers
enhance metabolism of ARV and dec drug efficacy --> resistance
NNRTIs and PIs interaction with antimicrobials that inhibit 3a4 (Macrolides
Azole antifungals
Fluoroquinolones
Quinupristin)
dec metabolism, inc serum levels, inc side effects

Fluconazole = weaker inhibitor than ketoconazole, itraconazole
Azithromycin = weaker inhibitor than erythromycin, clarithromycin
Ciprofloxacin = stronger inhibitor than other FQs
NNRTIs and PIs interact with which 3a4 inhibiting antidepressants
with fluvoxamine and nefazodone

dec metabolism --> increased serum levels, inc side effects

Sertraline, citalopram, escitalopram, venlafaxine, paroxetine less likely to inhibit 3A4
Fluoxetine is a weaker inhibitor than fluvoxamine
NNRTIs and PIs and gastric antisecretory agents H2RAs and PPIs
decreased absorption of antivirals --> resistance (Specific agents: atazanavir, fosamprenavir, indinavir, nelfinavir, rilpivirine)

Use an alternative antiretroviral
Amprenavir, darunavir, lopinavir, ritonavir, saquinavir are minimally affected by gastric pH
statins and NNRTIs and PIs
atorva, lova, and simva

inhibitors dec metab -->increase side effects

inducers-->enhance metabolism and dec efficacy

Use alternative agent (e.g. pravastatin, rosuvastatin)
INSTIs class wide side effects
GI disturbances, transaminitis, CPK elevation, myalgia

relatively well tolerated
which INSTI with food
elvitegravir
INSTIS and 1A1 enzyme inducers (Efavirenz
Etravirine
Rifampin
St John's wort
Tipranavir
)
increased metab of INSTIs --> decrease serum levels of ARVs by 50% --> resistance
INSTIs need to be separated by what by a few hours?
Antacids
Ca supplements
Mg supplements
Iron
Sucralfate

Give INSTI 2 hours before or 6 hours after binding agent
raltegravir interacts with what herbal product
gingko--modestly increases raltegravir plasma conc
saquinavir interacts with what herbal product
garlic- reduces saquinavir concentrations substantially
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