CYPs Flashcards

1
Q

NSAIDs

A

CYP2C9

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2
Q

Tacrolimus

A

Immunosuppressant used in transplantation; low bioavailability (due to CYP3A4 and 3A5 metabolism); low TI

CYP3A5 polymorphism => pharmacokinetic variation

  • no activity (most whites) => receive standard dose
  • extensive activity (most blacks) => 1.5-2x standard dose
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3
Q

Codeine

A

prodrug activated by CYP2D6 to form morphine

CYP2D6 polymorphism => pharmacokinetic variation

  • poor metabolizers (7% whites) => reduced analgesia
  • ultrarapid metabolizers => adverse effects of morphine OD
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4
Q

Clopidogrel (Plavix)

A

CYP2C19

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5
Q

Diazepam (and other “-azepam” benzos)

A

CYP2C19

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6
Q

Midalozam (and other “-azolam” benzos)

A

CYP3A4

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7
Q

Ethanol

A

CYP2E1

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8
Q

Proton pump inhibitors (“-prazoles”)

A

CYP2C19

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9
Q

CNS drugs (SSRIs like fluoxetine)

A

CYP2D6

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10
Q

CYPs affected by echinacea

A

CYP3A4 induced

CYP1A2 inhibited

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11
Q

Thiopurine

A

Prodrug that requires conversion to thioguanine for anticancer activity; inactivated by TPMT for excretion

TPMT polymorphism => pharmacokinetic variation
- poor metabolizers (rare) => increased risk of bone marror suppression

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12
Q

Metoprolol

A

CYP2D6

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13
Q

Warfarin

A

Anticoagulation activity via inhibition of vitamin K synthesis (VKORC1); inactivated by CYP2C9

CYP2C9 variation => pharmacokinetic variation
- *2 and *3 alleles are reduced function => reduced dose

VKORC1 variation => pharmacodynamic variation
- haplotype A => reduced dose

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14
Q

CYPs inhibited by furanocoumarins

A

CYP3A4

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15
Q

Clopidogrel

A

prodrug activated via two CYP2C19 oxidation steps to form active anti-platelet drug

CYP2C19 polymorphism => pharmacokinetic variation
- reduced function *2 and *3 => less antiplatelet effect and increased risk of thrombosis/MI/stroke

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16
Q

EGFR inhibitors

A

EGFR = hyperactive RTK in non-small cell lung cancer; inhibition = anti-cancer

ECFR mutations => pharmacodynamic variation

  • activating EGFR mutation => RTK inhibitor sensitivity
  • secondary EGFR resistance mutation => decreased inhibitor sensitivity
17
Q

Opioids

A

CYP2D6

18
Q

CYPs induced by gingko

A

CYP2C19

CYP2C9

19
Q

CYPs induced by St. John’s wort

A

CYP3A4
CYP2C19
CYP2C9
CYP2E1

20
Q

Acetaminophen

A

CYP2E1