[UF PharmD] Top Dietary Supplements

Clinical Uses of [St. John's Wort]

Tx of mild --> moderate depressive disorders

Dose Range of [St. John's Wort]

900 - 1800 mg/day

Proposed Active Ingredients of [St. John's Wort]

Hypericin (naphthodianthrone)

Hyperforin (phloroglucinol)

Quercetin glycosides (isoquercitrin and hyperoside)

What active ingredient of St. John's Wort is responsible for affecting CYP3A4 and P-gp?

BONUS: Does this ingredient INDUCE or INHIBIT said enzymes?

HYPERFORIN can cause INDUCTION of both CYP3A4 and P-gp.

MAJOR Drug Interactions of [St. John's Wort]

CYP3A4 substrates & P-gp substrates

NOTE! Be aware of reduced effectiveness of contraceptives when interacting w/ St. John's Wort.

Clinical Uses of [Gingko]

Tx of cerebral insufficiency, central hypoxemia, dementia, tinnitus, vertigo, Alzheimer's disease, and arteriosclerotic conditions

*Primarily CNS effects

Dose Range of [Gingko]

120-240 mg/day

*certain doses can reach up to 720 mg/day

Proposed Active Ingredients of [Gingko]

Ginkgolides (cyclic diterpene lactones)

Bilobalides (cyclic diterpene lactones)

Biflavones

Quercetin derivatives

MAJOR Drug Interactions of [Gingko]

Anticoagulant Drugs

Ibuprofen

Warfarin

Clinical Uses of [Kava]

Tx of social anxiety disorders, phobias, postmenopausal, and generalized anxiety disorders

No significant muscle relaxant or impairing side effects or sedation

Dose Range of [Kava]

60-120 mg/day

OR

1.5-3 g dried root/day

Proposed Active Ingredients of [Kava]

Kavalactones

Kavain (anesthetic effect and smooth muscle relaxing effect)

MAJOR Drug Interactions of [Kava]

Alprazolam

Barbiturates

Benzodiazepines

Clinical Uses of [Valerian]

Sleeping aid + Mild anxiolytic

Dose Range of [Valerian]

270-900 mg/bedtime (aqueous)

OR

600 mg (hydroalcoholic)

Proposed Active Ingredients of [Valerian]

Valerenic acid (non volatile sesquiterpene)

Valerenal & valtrate (monoterpene)

Pinoresinol (lignan derivative)

*Valtrate degrades to baldrinal present in extracts

MAJOR Drug Interactions of [Valerian]

Alcohol

Alprazolam

Benzodiazepines

CNS Depressants

Clinical Uses of [Red Yeast Rice]

Effective in lowering cholesterol and LDL levels by 20-30%

Suppression of aortic atherosclerotic plaque formation

Dose Range of [Red Yeast Rice]

1.5-2.5 g/day

Proposed Active Ingredients of [Red Yeast Rice]

Monacolin K,

Ankaflavin

Monascin (polyketides)

What active ingredient of red yeast rice caused heavy FDA enforcement on its products?

Monacolin K

MAJOR Drug Interactions of [Red Yeast Rice]

Statin drugs (due to its synergistic effect w/ monacolin K in inhibiting HMG-CoA to lower cholesterol levels)

Clinical Uses of [Cinnamon]

Decrease blood glucose levels

Decrease platelet count

Increase hemoglobin concentrations

Increase wound healing

Potential antimicrobial/antiseptic effect

Dose Range of [Cinnamon]

80 mg/day (ethanolic)

0.5-1 g/day (aqueous)

Up to 6 g/day (ground cinnamon in divided doses)

Proposed Active Ingredients of [Cinnamon]

Essential oil (cinnamaldehyde, eugenol)

Oligomeric polyphenols (cinnamtannin B1)

MAJOR Drug Interactions of [Cinnamon]

NONE

Clinical Uses of [Fish Oil]

Hypertriglyceridemia

Cardiovascular disease

Hypertension

Psoriasis

Dose Range of [Fish Oil]

1-4 g/day

What standardized ratio is used to determine the dosing range for fish oil?

EPA:DHA ratio of 1.2-1.5 : 1

Fish oil formulations are preferred to be ________ coated?

Enteric

Proposed Active Ingredients of [Fish Oil]

Poly-unsaturated fatty acids (PUFAs)

Eicosapentaenoic acid (EPA)

Docosahexaenoic acid (DHA)

MAJOR Drug Interactions of [Fish Oil]

NONE

Clinical Uses of [Saw Palmetto]

Benign prostate hyperplasia (BPH)

Dose Range of [Saw Palmetto]

160-800 mg/day

Proposed Active Ingredients of [Saw Palmetto]

Fatty acids (linoleic, stearic, palmitic, and γ linolenic acid)

Triterpene sterol (β-sitosterol)

MAJOR Drug Interactions of [Saw Palmetto]

NONE

Clinical Uses of [Chastetree Berry]

Mastalgia and menstrual irregularities

Premenstrual syndrome

Secondary amenorrhea

Postmenopausal symptoms

Hyperprolactinemia

Dose Range of [Chastetree Berry]

1.6-4.2 mg/day (commercial extracts)

30-40 mg/day (dried fruit extract)

Proposed Active Ingredients of [Chastetree Berry]

Diterpenes

Aucubin and agnuside (iridoid glycosides)

Casticin (flavonoid)

MAJOR Drug Interactions of [Chastetree Berry]

NONE

Clinical Uses of [Black Cohosh]

Potentially hot flashes

Perimenopausal symptoms

Dose Range of [Black Cohosh]

40-80 mg/day

Proposed Active Ingredients of [Black Cohosh]

Cimicifugoside

Actein (triterpene glycosides)

Formononetin (isoflavone)

MAJOR Drug Interactions of [Black Cohosh]

NONE

What herbal supplements from this Quizlet do NOT have contraindications for pregnancy and lactation?

Cinnamon

**Fish oil could be included as well.. although this supplement has a higher degree of caution for use compared with cinnamon due to potential exposure to toxic metals (Hg and Cd).