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163 Cards in this Set

  • Front
  • Back
Phytomedicines
A medicinal product containing as active ingredients only plants, parts of plants or plant materials, or combinations thereof, whether in the crude or processed state
Rational phytotherapy
Therapeutic system of science-based medicine

Cure

Dose-effect relationships usually apply: a larger dose will usually have a more powerful effect

Clinical and pharmacological evidence of efficacy is AVAILABLE
Traditional phytotherapy
A therapeutic system derived from the traditional use of plants

"support, improvement, alleviation..."

Dose-effect relationships usually apply: a larger dose will usually have a more powerful effect

Clinical and pharmacological evidence of efficacy is usually LACKING
Homeopathy
A therapeutic system with its own concepts, not scientifically based

"Cure, support, alleviation, improvement..."

The strength of the effect increases with increasing dilution (so-called "dynamisation")

Scanty clinical and pharmacological evidence of efficacy
Principles of homeopathy
A system of medicine based on the principle of "like cures like"

Uses the smallest dose possible to produce a response
Basis of homeopathy treatment
Homeopathy works with the body's response to illness and remedies are prescribed according to the symptoms

One remedy can be used to treat several ailments

One ailment may need to be treated with different remedies in different patients
Homeopathy: preparation of remedies
1. whole plant is macerated in alcohol = mother tincture

2. if insoluble, it is finely ground and pulverized in similar proportions with powdered lactose (milk sugar)

3. 1 mL added to 9mL or 99mL of solution results in 1X or 1C potency

4. Shake vigorously in between dilutions

5. standard dilutions: 6X-30X but products of 30C or more are marketed

X = 10-fold, C = 100-fold
Limit to the Dilution in Remedy preparation
Limit = 6.023 x 10^23 which equals homeopathic concentrations of 12C or 24X (1 part in 10^24)
Cort.
full name (Latin) = cortex
full name (English) = bark
Fol.
Full name (Latin) = folium, folia
Full name (English) = leaf, leaves
Frct.
Full name (Latin) = fructus
Full name (English) = fruits
Pericarp.
Full name (Latin) = pericarpium
Full name (English) = peel
Rad.
Full name (Latin) = radix
Full name (English) = root
Rhiz.
Full name (Latin) = rhizome
Full name (English) = rhizome
Sem.
Full name (Latin) = semen
Full name (English) = seed
Flor.
Full name (Latin) = flores
Full name (English) = flowers
Components of scientific name
Genus species (in italics)
St. John's Wort
Hypericum perforatum
Cranberries
Vaccinium macrocarpon
Most important chemical found in grapefruit juice that contributes to drug-drug interactions
6',7'-dihydroxybergamottin
Marker substances
chemically defined constituents of herbal drugs of interest for control purposes only (may be independent of whether they have any therapeutic activity or not)

when constituents responsible for therapeutic activity unknown, assays of other determinants required (appropriateness of marker substance should be justified)
Standardization
Defined as all measures during manufacturing process and quality control to yield reproducibility

this includes adjusting herbal drug or derived preparation to a defined content of a constituent or a group of substances with known therapeutic activity (ex = add excipients, mix herbal drugs or derived preparations)
Control of Starting Materials (plants)
1. controlled wild collection

2. controlled post collection

3. controlled transport and storage

4. propagation for cultivation

5. cultivation

6. processing
Parameters influencing extract composition: herb material
extractive concentration, water content, drug particle size, powder fraction
Parameters influencing extract composition: manufacturing procedure
extraction mode, extraction time, extraction pressure, batch size
Parameters influencing extract composition: solvent effects
solvent type, modifier concentration, solvent amount, flow-through rate
Parameters influencing extract composition: manufacturing plant
filling amount, filling height (density), static pressure
Coffee
Coffea arabica
Dietary Substance Health Education Act (DSHEA)
herbs are "dietary supplements." not drugs
DSHEA Ramifications
1. food safety division of the FDA regulates these products, not the drug division

2. no safety or efficacy tests required, but manufacturer is responsible for safety

3. no adverse event reporting to FDA necessary

4. no treatment claims, but "structure-function" claims are acceptable

5. to halt sales or distribution, FDA must prove that the product is "unsafe"
2007 FDA Good Manufacturing Practice (GMP) requirements for dietary supplements
GMP ensures that all dietary supplements are manufactured consistently with respect to identity, purity, strength, and composition

Requirements include:
1. design and construction of physical maintenance plants
2. proper manufacturing operations
3. quality-control procedures
4. testing final products
5. handling customer complaints
USP Certification Program
1. totally voluntary
2. certify ingredients
3. certify quantity of ingredients
4. will disintegrate or dissolve effectively to release nutrients for absorption into your body
5. product screened for harmful contaminants such as pesticides, bacteria, and heavy metals
6. product is manufactured using safe, sanitary and well-controlled procedures
Selecting herbal supplements
1. look for standardized herbal supplements

2. buy only single herb products

3. beware of claims that sound too good to be true

4. be extremely cautious about herbal supplements manufactured outside the US (except most European manufacturers)
Saw palmetto
Serenoa repens

part used: berries

unique compound: steroids = beta-sitosterol, campesterol, stigmasterol
Saw palmetto uses
1. benefit the urinary tract

2. relieve strain from painful bladder problems

3. tone the bladder by improving urinary flow

4. for treatment of BPH symptoms
Saw palmetto MOA
BPH probably involves 5-alpha-dihydrotestosterone (DHT)

ACTS TO INHIBIT 5-alpha-reductase
Isoforms of 5-alpha-reductase
1. 5-alpha-reductase - 1 (liver, non-genital skin, brain)

2. 5-alpha-reductase - 2 (liver, urogenital tract)
Potency of DHT
DHT (dihydrotestosterone) is 10 times more potent than testosterone!
Saw palmetto conclusions
Saw palmetto provides mild to moderate improvement in urinary symptoms, flow measures

Relative to finasteride, improvements in urinary symptoms and flow measure are comparable, but fewer side effects and lower cost with saw palmetto
Saw palmetto drug interactions
1. Androgenic drugs: therapy may decrease the effectiveness of therapeutic androgens

2. Anti-androgenic drugs: additive effects may occur with anti-androgen drugs such as finasteride

3. Anticoagulants, anti-platelets, NSAIDs: not confirmed so far
Saw palmetto dose
1-2 grams of ground, dried, or whole berries daily

**teas prepared from saw palmetto berries are potentially ineffective because the purported active constituents are water insoluble**

extract: 320 mg daily in one dose or two divided doses (160mg BID) = recommended by German expert panel, the Commission E

DER (drug extract ratio): 9-12:1
DER (drug extract ratio)
the ratio of herbal substance to the herbal preparation

one of the most important criteria to approve the therapeutic equivalence of different herbal preparations

increased DER = hard to extract compound!!
Pygeum (extract of bark of an evergreen tree found in Africa)
Pygeum africana

part used: bark extract

products should be standardized to contain 14% triterpenes and 0.5% docosanol
Pygeum MOA
possible MOA: pygeum might inhibit growth factors

NO special safety concerns
Pygeum Dose
75-200 mg standardized lipophilic extract (14% tripterpenes, 0.5% n-docosanol) per day has been used

some research suggests daily or BID dosing is equally effective
Pygeum adverse effects
general: Pygeum has been well tolerated in most studies, with adverse effects similar to placebo

GI: some people may experience abdominal discomfort, including diarrhea, constipation, stomach pain, or nausea
Pumpkin
Cucurbita pepo, Cucurbita moschata (2 different plants)

Active part: seeds (whole or crushed), seed extract oil, tablets, tea
Pumpkin use
BPH

Proposed dose: 480mg per day (pumpkin seed extract) in 3 divided doses in combo with saw palmetto and other herbs
Pumpkin adverse effects
electrolyte imbalance (from mild diuretic actions)

drug interactions: diuretics (potentiation of fluid loss and electrolyte imbalance)
Stinging nettle
Urtica dioica

Parts of plant used: root

Hairs that cover the plant contain acetylcholine, histamine, serotonin, leukotrienes
Stinging Nettle other uses
adjuvant in the symptomatic treatment of arthritis, arthroses, and/or rheumatic conditions

also used as a diuretic, in inflammatory complaints of the lower urinary tract

BPH
Stinging nettle precaution/side effects
Use with caution in patients taking anti-inflammatory agents

Use with caution in patients with hyponatremia as nettle has a synergistic diuretic effect
Cranberry
Vaccinium macrocarpon

For prevention and treatment of UTI (diuretic, antiseptic, urinary deodorizer)

**rich in anthocyanins --> antioxidant, anti-inflammatory
Cranberry MOA and dose
MOA thought previously to be urine acidification, now MOA through adhesion inhibitors

Need about 8-16 oz (240-480 mL) of pure juice (NOT DRINK OR COCKTAIL)
Cranberry tablets caution
Dietary supplementation with cranberry concentrate tablets may increase the risk of nephrolithiasis (calcium oxalate increased)
Cranberry possible drug interaction
cranberry-warfarin
Cranberry dose
>8 oz/day of JUICE

(caution in diabetics due to sugar content)
Bearberry
Arctostaphylos uva-ursi

part of plant used: leaves (as diuretic, astringent, antiseptic, and treatment for UTIs)
Bearberry key compounds
ARBUTIN is the active ingredient in bearberry present in fairly high amounts (up to 10%)

HYDROXYQUINONE is a very powerful anti-microbial agent and seems to be responsible for bearberry's ability to treat UTIs
Bearberry Medicinal Use
UTIs including cystitis, nephritis, urethritis, yeast infection, early stage of genital herpes
Bearberry Side Effects
nausea, vomiting (due to high tannin content)
Bearberry Dose
cold water infusions of the dried leaf (3g per day) correspond to 400-800 mg arbutin per day
Bearberry duration
until complete disappearance of symptoms, maximum of 12 weeks
Bearberry drug interactions
corticosteroids: may potentiate the effects of prednisolone and dexamethasone

diuretic drugs: may increase urine flow

NSAIDs: may increase the anti-inflammatory activity of indomethacin
Chasteberry
Vitex agnus

Part used: dried, ripe berries
Chasteberry indication
menstrual irregularities including dysmenorrhea, secondary amenorrhea, oligomenorrhea, and polymenorrhea

symptoms of menopause

PMS

treating female infertility, increasing lactation, and treating fibrocystic breasts
Chasteberry key compounds
vitexilactone, casticin (may also be used for standardization), rotundifuran, agnuside (usual standardized ingredient)
Standardization of chasteberry
many extracts are standardized to contain 0.5% agnuside or 0.6% aucubin (may be standardized to casticin content)
Chasteberry MOA
works similar to dopamine molecule by acting at dopamine receptor to block conversion of ATP to cAMP and therefore INHIBITING prolactin secretion
Chasteberry Dose
single dose each morning before breakfast throughout cycle

extract: 30-40mg/day

powdered berries: 3 x per day at 500mg/dose (total 1500mg/day)

0.15-0.2mL daily of tincture (1:5 g/mL)

long-term use acceptable within recommended therapeutic range
Chasteberry Contraindications
DO NOT take with dopamine receptor antagonist/agonist

Avoid using in women undergoing in vitro fertilization

use during pregnancy and lactation should be avoided
Black cohosh
Cimifuga racemosa

Part used: root
Black cohosh use
premenstrual complaints and dysmenorrhea as well as neurovegetative conditions related to menopause
Black cohosh key compounds
deoxyactein, caffeic acid, salicylic acid, formononetin
Black cohosh standardization
based on content of triterpenes, calculated as 27-deoxyactein

1mg of 27-deoxyactein per 20mg tablet
Black cohosh MOA
have selective estrogen receptor modulating (SERM) effects

(estrogenic and anti-estrogenic effects)
Estrogen receptors/locations
ER-alpha: uterus, breast, ovary, testis, kidney, and adrenal gland

ER-beta: brain, prostate, lung, bladder, intestine, bone
SERMs
designed to act in specific ways at each of the estrogen receptor sites in different tissues

SERMs preferentially bind to ER-beta, potentially activating cardioprotective and bone-stabilizing metabolic processes

SERMs down-regulate activity of ER-alpha, found in breast and uterus, and may help prevent cancer in these tissues
Traditional Black cohosh dose
40-200mg dried rhizome daily in divided doses
Modern/recommended black cohosh dose
ethanol extract: equivalent to 40mg of dried rhizome/root/day

Remifemin: standardized extract where each 20mg tablet contains 1 mg triterpene glycosides, 40mg/day (2 tabs per day)
Black cohosh adverse reactions
might cause liver disease
Black cohosh contraindications and warnings
contraindicated in pregnancy

anti-HTN medications

allergy to aspirin

in patients with known estrogen sensitive conditions

interactions: atorvastatin
Soybeans
Glycine max

observations of Asian populations: generally a diet higher in soy than America (but must start eating soy at a young age for protective effect)
Beneficial components of soy
fatty acids:

mainly unsaturated fat
minimal saturated fat
plant source of omega-3 fatty acid, linoleic acid
Omega ratio
omega-6 to omega-3 ratio should be 2:1

omega-6 family: thrombotic, inflammatory

omega-3 family: less thrombotic, less inflammatory
Plant derived estrogens (phytoestrogens)
soy or red clover--> soy (ISP) or clover isolate --> isoflavone concentrate --> genistein, daidzein, glycitin (all have weak estrogenic effects)
Phytoestrogens in human health
cancer preventative
post-menopausal supplement
prevention of osteoporosis
cardiovascular health
Soy dose
soy protein 20-60 grams providing 34-76 mg of isoflavones daily

concentrated soy isoflavone extracts providing 35-120 mg of isoflavones daily

osteoporosis: 80-90mg, in 40 grams of soy protein
Red clover
Trifolium pratense

part used: flowering top
Red clover key compounds
isoflavones

coumestrol (similar in structure to warfarin, increase bleeding risk)
Red clover use
orally, red clover is used for menopausal symptoms and hot flashes (evidence is poor)
Red clover dose
menopausal symptoms: 40, 80, or 160mg of red clover isoflavones/day

HRT: 40-80mg of red clover isoflavones/day

cholesterol: 28.5, 57, or 85.5mg of red clover isoflavones/day

osteoporosis: 40mg of red clover isoflavones/day
Dong quai
Angelica sinensis

part used: root
Dong quai use
dysmenorrhea, PMS, and menopausal symptoms

(no phytoestrogens, coumarin derivatives)
Dong quai dose
4.5 grams of powdered dong quai has been used daily

interactions: warfarin
Wild yam
Disocorea species

part used: all parts grown underground
Wild yam uses
menopausal complaints

osteoporosis

precursor for commercial chemical synthesis of human steroidal hormomes
Wild yam active ingredient
diosgenin --> progesterone

NOTE: this conversion happens synthetically but NOT in the body

some products are spiked with progesterone!!
Wild yam effectiveness
applied topically appears to be no better than placebo for reliving vasomotor symptoms

dosage: not known
interactions: not known
adverse effects: vomiting
Garlic
Allium sativum

part used: bulb

(all garlic for commercial use is cultivated)
Modern use of garlic
anti-HTN

antimicrobial

fibrinolytic

**anti-atherogenic

antithrombotic

**lipid-lowering
RLS of synthesis of cholesterol
conversion of HMG-CoA to mevalonic acid through HMG-CoA reductase
Garlic key compounds
Alliin: chemically stable, odorless, little physiological activity

Allicin: chemically unstable, typical garlic odor, physiologically active (RELEASED BY CRUSHING THE GARLIC)
Garlic odor...why does your breath and skin stink after eating garlic?
The sulfur molecules that are created when garlic is smashed or chewed are absorbed into the bloodstream and lungs and escape through exhaled air and perspiration
Garlic MOA
inhibit HMG-CoA reductase (primary)

inhibit squalene epoxidase (in conversion of squalene to lanosterol)
Garlic product formulation
product needs to be enteric coated to be effective!!
Aged garlic-A potent antioxidant
extracts of fresh garlic that are aged over a prolonged period to produce aged garlic extract (AGE) that contains antioxidant phytochemicals that prevent oxidant damage
Formation of free radicals
UV light
ionizing radiation
smoking
air pollution
inflammation
metabolism
AGE MOA
AGE exerts antioxidant action by scavenging reactive oxygen species (ROS)

It protects DNA against free radical-mediated damage and mutations
Garlic clinical considerations
side effects: odor and GI upset

active component allicin is odiferous; reduced in many products to decrease odor
Garlic dose
tablets or capsules: 600-900mg (10mg allicin) daily

odorless formulations other than enteric-coated may be less effective!!

fresh garlic: 2-5g/day (5-20 cloves)

must be taken for 6 weeks - 2 months for maximal effect
Garlic drug interactions
Norvir (ritonavir): cases of GI toxic effects

Fortovase/Invirase (saquinavir): combination results in decreased effectiveness of saquinavir

warfarin: prolongs the time for blood to clot, increased risk for bleeding
Red yeast rice
Monascus purpureus
Red yeast rice key compounds
major compound: monacolin K = mevinolin (similar in structure to statin)
Red yeast rice MOA
inhibits the action of HMG-CoA reductase
Red yeast rice dose
traditional: 6-9 grams/day
recommended: 1.2 grams/day
Red yeast rice contraindications
patients who are hypersensitive or allergic to rice or yeast
Red yeast rice drug interactions
cholesterol-lowering medications = additive effects

grapefruit juice - HMG-CoA reductase inhibition
Red yeast rice side effects
only mild effects have been reported: heartburn, flatulence, dizziness
Oats
Avena sativa

part used: seeds or oat bran (milled)
Oat uses (orally)
hypercholesterolemia

diabetes

lowering uric acid levels
Oat uses (topically)
seborrhea

dry and itchy skin
Oat key compound
beta-glucans --> in the bran of grasses
Oats MOA
(beta-glucan)

1. binds with bile acids in the gut and increasing fecal bile acid excretion

2. decreases cholesterol absorption

3. increases the viscosity of food
Oats dose
for hypercholesterinaemia:

56-150 grams of whole oat products such as oatmeal containing 3.6-10 grams of beta-glucan
Oats and FDA regulation
health claim: product may reduce the risk of heart disease if they contain at least 750mg of soluble fiber per serving

approximately 3 grams soluble fiber taken daily
Artichoke
Cynara scolymus

part used: leaves of the STEM
Artichoke key compounds
Caffeoylquinic acids

Flavonoids (eg luteolin-7-O-glycoside)

Sesquiterpene lactones

luteolin (most prominent), chlorogenic acid, cynarin
Artichoke therapeutic indications
adjuvant to a low fat diet in the treatment of mild to moderate hyperlipidemia
Artichoke dose
320-640mg artichoke leaf extract three times daily
Artichoke MOA
indirect inhibition of HMG-CoA reductase
Artichoke side effects
mild GI disturbances, allergic reactions (in individuals sensitive to Asteracease/Compositae family plant)

also allergic contact dermatitis
Artichoke safety
interactions with other medications: none

overdose: no toxic effects reported

duration of treatment: no restriction

GRAS
Hawthorn
Crataegus species
(C. monogyna, C. laevigata)

part used: leaves and flowers
Hawthorn key compounds
Flavonoids (vitexin-4'-rhamnoside, rutin, quercetin, hyperoside)

flowers and leaves: high in flavonoids, fruits contain lowest amount
Hawthorn standardization
range from 0.6-1.5% flavonoids, typically calculated as hyperoside
Hawthorn key compound
Proanthocyanidins

OPCs = oligomeric proanthocyandins
Hawthorn therapeutic indications
preparations based on hydroalcoholic extracts: declining cardiac performance (NYHA class I or II)

herbal teas and other preparations: nervous heart complaints, support of cardiac and circulatory function
Hawthorn side effects
GI complaints
vertigo
headache
sleeplessness
in general, very well tolerated
Hawthorn special warning
Self-medication is inappropriate among patients with heart failure!!
Hawthorn MOA
increasing force of contraction and lengthening refractory period

increasing coronary blood flow and cardiac output, and reducing oxygen consumption

cardiotrophic properties: increased membrane permeability for calcium, and phosphodiesterase inhibition (intracellular cAMP increased)

increased cAMP = increased coronary blood flow, vasodilation, and positive inotropic effects
Hawthorn dose
160-900mg extract per day in 2-3 divided doses

powdered drug: 2-5 grams daily

tincture: 20 drops 2-3x day

herbal teas: 1-1.5 grams of drug as an infusion
Hawthorn duration of treatment
Should be used for 4-8 weeks to determine benefit
Hawthorn interactions
conventional CV drug therapy

not reported
Hawthorn safety
safe, when used short term

pregnancy and lactation: avoid using

overdose: NO toxic effects reported
Fish oil
omega-3 EPA and DHA
EPA
eicosapentaenoic acid (primarily from fish)
DHA
docosahexaenoic acid (primarily from fish)
ALA
alpha-linolenic (primarily from flax)
1 gram fish oil = ?
150 mg EPA/DHA
1 gram flax seed oil = ?
19.6 mg EPA/DHA
Desired omega-6 to omega-3 ratio
2:1
Goal omega-3 EPA/DHA consumption
500-650 mg per day
EPA/DHA dose
eat two 4 oz. servings of fatty fish per week:

providing 3500 mg EPA + DHA per week OR 496 mg of EPA + DHA per day
Fish oil safety concerns
contamination with toxins (mercury)
EPA/DHA benefits
heart health
brain development
brain function
asthma
visual acuity
immune function
arthritis
skin and hair health
Horse chestnut
Aesculus hippocastanum
Horse chestnut key compounds
terpenoid compounds:

escin (also aescin) = complex mixture of various, chemically similar triterpene glycosides **major prominent compound

fatty acids

coumarin derivatives (aesculin)
Horse chestnut standardization
horse chestnut seed extract (HCSE)

16-20% triterpene glycosides calculated as aescin
Horse chestnut therapeutic applications
treatment of chronic venous insufficiency, treatment of inflammatory conditions, skin care products, treatment of hemorrhoids
Phases of compression therapy
Phase I: reduction of edema and/or ulcer healing, achieved by applying non-elastic compression

Phase II: maintenance of compression, elastic compression
Horse chestnut dose
drug or hydroalcoholic extracts = 300 to 900 mg of a 16% extract

2 or 3 x daily

**in all cases, patient must continue physician-prescribed treatments including the use of supportive elastic stockings
Horse chestnut safety profile
FDA status: unsafe herb

toxicity: attributed to the glycoside aesculin (dilation of pupils, diarrhea, vomiting, paralysis)

interactions: none reported
theoretically: anticoagulants