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P-GP Common substrates:
Anticoagulants: ______, ______
CV drugs: ___, ___, _____
Immunosuppressants: ____, ______
Others: _____
Anticoagulants: rivaroxaban, apixaban
CV drugs: diltiazem, verapamil, digoxin
Immunosuppressants: cyclosporine, tacrolimus
Others: colchicine
P-GP Common Inducers: (decrease concentration)
similar to CYP3A4
Anti-epileptics: ___, ____, ________
Other: ____, _______
Anti-epileptics: Carbamazepine, phenobarbital, phenytoin
Other: rifampin, st john’s wort
P-GP Common Inhibitors: (increase concentration)
similar to CYP3A4
CV drugs: ___, ____, ________
HIV drugs: _____, _____
Immunosuppressants: ____, _______
CV drugs: verapamil, diltiazem, amiodarone
HIV drugs: ritonavir, cobicistat
Immunosuppressants: cyclosporine
CYP3A4 substrates
Analgesics: ____, _____, ____, _____
Anticoagulants: _____, ____, _____
CV drugs: ___, ____, ____, ____
Immunosuppressants: ____, ____, ____
Statins: ____, _____, _____
HIV drugs: ___, ____, _____
PDE-5 inhibitors: sildenafil, tadalafil, vardenafil, avanafil
Analgesics: fentanyl, methadone, hydrocodone, oxycodone
Anticoagulants: s-warfarin, rivaroxaban, apixaban
CV drugs: amiodarone, diltiazem, verapamil, digoxin
Immunosuppressants: cyclosporine, tacrolimus, sirolimus
Statins: atorvastatin, lovastatin, simvastatin
HIV drugs: cobicistat, ritonavir, NNRTIs
PDE-5 inhibitors: sildenafil, tadalafil, vardenafil, avanafil
CYP3A4 inducer
___, ____, ___, _____
____
____
____
Carbamazepine, oxcarbazepine, phenobarbital, phenytoin
Rifampin
Smoking
St John wort
CYP3A4 inhibitor
MADVAP + (Cyclosporine)
Macrolides, azoles, diltiazem, verapamil, amiodarone, protease inhibitors (and cobicistat and ritonavir)
CYP2C9 substrate
S-Warfarin
CYP2C9 inducer (same as CYP3A4)
Carbamazepine, phenobarbital, phenytoin, st john wort, smoking
CYP2C9 inhibitor
BAMIF
Bactrim, amiodarone, metronidazole, itraconazole (and other azoles), FQs
CYP2C19 PPIs
esomeprazole, omeprazole
CYP2D6 SUBSTRATES
___, ____, ____
CYP2D6 INHIBITORS
____, ____, ___, ___
meperidine, tramadol, codeine
Amiodarone, duloxetine, paroxetine, fluoxetine
CYP1A2 SUBSTRATES
___, ____
CYP1A2 INHIBITORS INDUCERS (same as CYP2C9, CYP3A4)
CYP1A2 INHIBITORS
____, ____
theophyline, warfarin
ciprofloxacin, fluvoxamine
Opioids with serotonergic activity (contraindicated within 14 days of MAO-I)
___, ____, ____, ____ (there is a risk with any but particularly these)
meperidine, fentanyl, methadone, tramadol, codeine
MAO inhibitors
Antidepressants: _____, _____, _____
Selective MAO-Is: _____, _____
Others: _____, _____
Antidepressants: isocarboxazid, phenelzine, tranylcypromine
Selective MAO-Is: selegeline, rasagiline
Others: linezolid, methylene blue
Serotonin syndrome can cause altered mental status such as ___ and ____ as well as neuromuscular excitation like ___ and ____. Avoid using serotonergic drugs together, but if used the doses should be within recommended ranges. A washout period is ____ weeks or ____ weeks for drugs with a longer duration of action such as _____.
agitation and delirium ; rigidity and seizures ; 2 weeks ; 5 weeks ; fluoxetine
Amiodarone ______ CYP____ which would usually ____ warfarin. If using warfarin 1st and adding amiodarone _______.
inhibits CYP3A4 ; metabolize ; reduce warfarin dose by 30-50%
Amiodarone inhibits ____. Digoxin is a substrate of it, and inhibition of this means that drugs will not be pumped back into the stomach for excretion. More circulation, more toxicity. If using digoxin first and adding amiodarone then _____.
P-GP ; reduce digoxin 50%
Which statins are contraindicated with strong CYP3A4 inhibitors?
Simvastatin and lovastatin
Valproate ____ ____ of lamotrigine. When initiating lamotrigine use the starter kit with ___ ___
reduces metabolism (increase risk for SJS/TENS) ; lower dose
Many ASM and ____ are metabolized by CYP enzymes. Inducers such as ____ will reduce levels. (IT is an autoinducer)
contraceptives ; carbamazepine
QT prolongation
Antiarrhythmics
Anti-infectives: FMT, ___ (except ___), antimalarials (_____)
Anti-depressants: ____, _____, _____, mirtazapine, trazodone, venlafaxine
Anti-emetics: ___, ____, promethazine
To avoid QT prolongation (especially in the elderly) do not exceed citalopram doses of ___ (or ____ if >65). Do not exceed escitalopram doses of ___ (or ____ if >65). Do not use ____ inpatient.
40 mg (20 mg) ; 20 mg (10 mg) ; droperidol
CNS depression: Several ER formulations act like short-acting ones when taken with ____. This increases rate of mortality.
alcohol
Cisplatin is basically GUARANTEED kidney damage. If available use ___to protect kidneys.
amifostine
PDE-5s + NITRATES: _____
PDE-5s + CYPCA4 inhibitor: ____ staring dose
PDE-5s + Alpha-1 blocker: start with ____ ____ aka _____ _____.
contraindicated
half
low dose ; half starting-dose