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PCEUT 510 > #3 Herb-Drug Interactions > Flashcards

#3 Herb-Drug Interactions Flashcards

1
Q

3 biggest categories of dietary supplements used

A
  1. Sports enhancement (steroids, ephedrine alkaloids)
  2. WT loss (silmutramine, ephedrine alkaloids)
  3. Sexual enhancement (PDE, inhibitors)
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2
Q

Ecstasy enzyme effects

A

Its metabolite is a VERY POTENT MDI INHIBITOR of 2D6

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3
Q

Ecstasy + dextromethorphan

A

Ecstasy (metabolite) = Very STRONG inhibitor
Dextromethorphan = 2D6 substrate
INCREASES [dextromethorphan] AUC 14-fold

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4
Q

Garlic active component

A

Allin

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5
Q

Garlic uses (2)

A
  1. hypercholesterolemia

2. Boost Immune System

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6
Q

Garlic enzyme effects

A

Studies show inconsistent results!

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7
Q

Garlic oil + midazolam

A

Showed no effect

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8
Q

Garlic + saquinavir (3A4 substrate)

A

DECREASED [saquinavir]

= suggests that garlic is INDUCER of 3A4

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9
Q

Garlic + docetaxel (3A4 substrate)

A

INCREASED [docetaxel]

= suggests that garlic is INHIBITOR of 3A4

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10
Q

Gingko biloba active components

A

Flavonoids

Terpenes

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11
Q

Gingko biloba use (1)

A

memory improvement

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12
Q

Gingko biloba enzyme effects

A

Weak INDUCER:

3A4, 2C9, 2C19….though not totally clear

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13
Q

Gingko biloba + tolbutamide DDI

A

Tolbutamide + 2C9 substrate Gingko = 2C9 inducer

DECREASED [tolbutamide]

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14
Q

Gingko biloba + midazolam DDI

A

Studies show inconsistent results

One study showed INCREASED [MDZ]
another showed DECREASED [MDZ]

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15
Q

Gingko biloba + omeprazole DDI

A

DECREASED [omeprazole] d/t gingko’s INDUCTION of both 2C19 and 3A4

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16
Q

Goldenseal active components

A

NTE 2% hydrastine, 2.5% berberine

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17
Q

Goldenseal uses (2)

A
  1. Enhance immune system

2. Stimulate digestion

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18
Q

Goldenseal Enzyme effects

Hint: Stop killing the seals! There’s only 2,634 seals left in the world

A

INHIBITS:
2D6
3A4

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19
Q

Goldenseal + debrisoquine DDI

A

Debrisoquine = 2D6 SUBSTRATE
Goldenseal = 2D6 INHIBITOR
=
INCREASED [debrisoquine]

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20
Q

Goldenseal + Midazolam DDI

A 
MDZ = 3A4 SUBSTRATE 
Goldenseal = 3A4 INHIBITOR

=
INCREASED [midazolam]

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21
Q

Green tea active component

A

Catechins

22
Q

Green tea enzyme effects (2)

A
  1. INHIBITS 1A2 (minor pathway for APAP)

2. INHIBITS OATP1A2

23
Q

Green tea + Folic acid DDI

A

DECREASED folate AUC

Suggests that green tea has some effect on uptake transporters….but could also be some “unstirred water layer osmolality” thing….

24
Q

Green tea + nadolol DDI

A

Nadolol = taken up by OATP1A2 (aka substrate)
Caused DECREASE AUC of nadolol

Suggest that green tea inhibits uptake transporter OATP1A2, however this transporter is not expressed in the GI…

25
Q

Green tea + drugs with low GI permeability (proposed mechanism)

A

Green tea affects GI osmolality and fluid volume = affects absorption of these drugs

26
Q

SJW effects on enzymes

A

INDUCES
3A4
Pgp

27
Q

Milk thistle effects on enzyme

A

no consistent PK interactions

28
Q

Saw palmetto effects on enzyme

A

no consistent PK interactions

29
Q

Valerian effects on enzymes

A

no consistent PK interactions

30
Q

Turmeric effects on enzymes

Hint: same as goldenseal

A

In VITRO INHIBITS 2D6

In VIVO maybe INHIBITS 2D6 & 3A4

31
Q

T/F:

The biggest SAFETY issue for herbal products and dietary supplements is accidental contamination

A

FALSE

The biggest SAFETY issue DELIBERATE contamination with DRUGS

32
Q

Ecstasy is a [TIME/CONCENTRATION] dependent inhibitor of 2D6

A

TIME

33
Q

Ecstasy is an INHIBITOR of this enzyme

A

2D6

34
Q

T/F:

Ecstasy is a mechanism based INHIBITOR of 2D6

A

TRUE

35
Q

[MEN/WOMEN/NEITHER] were more affected by ecstasy’s 2D6 INHIBITION

A

WOMEN

36
Q 
Garlic has been shown to have what effect on 3A4? 
A. Induce
B. Inhibit 
C. NO effect 
D. all of the above
A

D. all of the above
Inhibit = docetaxel
Induce = saquinavir
NO effect = midazolam/ritonavir

So garlic can both induce and inhibit 3A4.
The effects are modes and variable and the data is unclear

37
Q

This is the purported active ingredient of garlic

A

allicin

38
Q

Garlic was shown to have a noticeable effect on [Ritonavir/Midazolam/BOTH/neither]

A

NEITHER

39
Q

These supplements inhibit platelet aggregation according to the multiple reports of bleeding disorders

A

Garlic
Ginkgo
Asian ginseng (Panax)

40
Q

Ginkgo induces this enzyme

A

2C9

41
Q

What was the effect of Ginkgo with Tolbutamide?

A

Ginkgo INDUCED tolbutamide CL through 2C9 induction, 29% DECREASE IN AUC

42
Q

Ginkgo [inhibits/induces/either] 3A4

A

EITHER

43
Q

What was the effect of Ginkgo with MDZ?

A

Ginkgo INHIBITED MDZ CL through 3A4 = 24.6% INCREASE IN AUC

However later is was shown to INDUCE 3A4

44
Q

Ginkgo [inhibits/induces/either] 2C19 (omeprazole)?

A

INDUCES

Weak 3A4 & 2C19 induction seems to be the most consistent Ginkgo effect

45
Q

Goldenseal [inhibits/induces] 2D6

A

INHIBITS

46
Q

Goldenseal [inhibits/induces] 3A4

A

INDUCES

47
Q

Green tea extract lowered levels of this nutrient

A

Folic acid

48
Q

Caffeine INHIBITS _______ and interferes with the metabolism of this OTC?

A

1A2

APAP

49
Q

How does green tea effect Nadolol?

A

DECREASED

Concentration by 85%

50
Q

Why does green tea decrease nadolol concentrations?

A

Absorption of LOW permeability drugs depends on the drug concentration gradient, which is in turn influenced by GI fluid volume and osmolality and slows drug absorption

51
Q

Whether or not this supplement affected caffeine levels depended on the brand used

A

Echinacea

PCEUT 510 (12 decks)

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