NAPLEX Exam Study Material 2023: Overview of Common CYP Inhibitors and Inducers

True or False?

Enzyme inhibition is fast, effects are seen within a few days

True

True of False?

Enzyme inhibition is slow, effects are seen within a few weeks to months

False

Inhibitors Increase/Decrease

enzyme function

Decrease

Inhibitors Increase/Decrease

substrate metabolism

Decrease

Inhibitors Increase/Decrease

serum drug level

Increase,

less drug is being metabolized and excreted from the system

What clinical outcome occurs with CYP inhibition?

increased substrate

increased side effects

toxicity

Inhibitors Increase/Decrease

Prodrug level

Increase prodrug level

Inhibitors Increase/Decrease

Prodrug active form

Decrease active form

What clinical outcome does CYP Inhibitors have on Prodrugs?

decreased effectiveness because prodrug is not being converted to active form

Inducers Increase/Decrease

enzyme function

Increase function

Inducers Increase/Decrease

substrate metabolism

Increase metabolism

Inducers Increase/Decrease

drug serum level

decrease level

What is the clinical outcome of CYP induction?

increased metabolism

decreased drug

decreased clinical effect

Inducers Increase/Decrease

Prodrug level

Decrease level

Inducers Increase/Decrease

Prodrug active form

Increase

What clinical effect do CYP Inducers have on prodrugs?

Increased clinical effect because more prodrug is being converted to the active form

What is the acronym for common CYP inhibitors?

G*PACCCMAN

G*PACCCMAN is the acronym for

inhibitors or inducers?

CYP inhibitors

The G in G*PACCCMAN stands for?

Grapefruit

The P in G*PACCCMAN stands for?

Protease Inhibitors

ritonavir,

The first A in G*PACCCMAN stands for?

Azole antifungals

fluconazole, itraconazole, ketoconazole, posaconazole, voriconazole, isavuconazonium

The CCC in G*PACCCMAN stands for?

Cyclosporine

Cobicistat

Cimetidine

The M in G*PACCCMAN stands for?

Macrolides

clarithromycin, erythromycin

(not azithromycin)

which macrolide is NOT a common CYP inhibitor?

azithromycin

The second A in G*PACCCMAN stands for?

Amiodarone

(and dronedarone)

The N in G*PACCCMAN stands for?

Non-DHP CCB

diltiazem, verapamil

Grapefruit

CYP Inducer or Inhibitor?

Inhibitor

(G*PACCCMAN)

Ritonavir

CYP Inducer or Inhibitor?

Inhibitor

(Protease inhibitor G*PACCCMAN)

fluconazole

CYP Inducer or Inhibitor?

Inhibitor

(Azole antifungals G*PACCCMAN)

itraconazole

CYP Inducer or Inhibitor?

Inhibitor

(Azole antifungals G*PACCCMAN)

ketoconazole

CYP Inducer or Inhibitor?

Inhibitor

(Azole antifungals G*PACCCMAN)

posaconazole

CYP Inducer or Inhibitor?

Inhibitor

(Azole antifungals G*PACCCMAN)

voriconazole

CYP Inducer or Inhibitor?

Inhibitor

(Azole antifungals G*PACCCMAN)

isavuconazonium

CYP Inducer or Inhibitor?

Inhibitor

(Azole antifungals G*PACCCMAN)

Cyclosporine

CYP Inducer or Inhibitor?

Inhibitor

(G*PACCCMAN)

Cobicistat

CYP Inducer or Inhibitor?

Inhibitor

(G*PACCCMAN)

Cimetidine

CYP Inducer or Inhibitor?

Inhibitor

(G*PACCCMAN)

Clarithromycin

CYP Inducer or Inhibitor?

Inhibitor

(Macrolides G*PACCCMAN)

Erythromycin

CYP Inducer or Inhibitor?

Inhibitor

(Macrolides G*PACCCMAN)

Amiodarone

CYP Inducer or Inhibitor?

Inhibitor

(Amiodarone G*PACCCMAN)

dronedarone

CYP Inducer or Inhibitor?

Inhibitor

(Amiodarone G*PACCCMAN)

Diltiazem

CYP Inducer or Inhibitor?

Inhibitor

(Non-DHP CCBs G*PACCCMAN)

Verapamil

CYP Inducer or Inhibitor?

Inhibitor

(Non-DHP CCBs G*PACCCMAN)

What is the acronym for Common CYP Inducers?

PS PORCS

PS PORCS is the acronym for

Inducers or Inhibitors?

Inducers

The first P in PS PORCS stands for?

Phenytoin

The first S in PS PORCS stands for?

Smoking

The second P in PS PORCS stands for?

Phenobarbital

(Prodrug Primidone)

The O in PS PORCS stands for?

Oxcarbazepine

(and eslicarbazepine)

The R in PS PORCS stands for?

Rifampin

(and rifabutin, rifapentine)

The C in PS PORCS stands for?

Carbamazepine

(auto inducer)

The second S in PS PORCS stands for?

St. John's wort

Phenytoin

CYP Inducer or Inhibitor?

Inducer

(PS PORCS)

Smoking

CYP Inducer or Inhibitor?

Inducer

(PS PORCS)

Phenobarbital

CYP Inducer or Inhibitor?

Inducer

(PS PORCS)

Prodrug Primidone

CYP Inducer or Inhibitor?

Inducer

(PS PORCS)

Oxcarbazepine

CYP Inducer or Inhibitor?

Inducer

(PS PORCS)

eslicarbazepine

CYP Inducer or Inhibitor?

Inducer

(PS PORCS)

Rifampin

CYP Inducer or Inhibitor?

Inducer

(PS PORCS)

rifabutin

CYP Inducer or Inhibitor?

Inducer

(PS PORCS)

rifapentine

CYP Inducer or Inhibitor?

Inducer

(PS PORCS)

Carbamazepine

CYP Inducer or Inhibitor?

Inducer

(PS PORCS)

St. John's wort

CYP Inducer or Inhibitor?

Inducer

(PS PORCS)

True of False

Enzyme induction is fast, effects are seen within a few days

False

True of False?

Enzyme induction is slow, effects may not be seen for up to four weeks

True

When an inducer is stopped, how long does it take for inductions effects to disappear completely?

2-4 weeks