Valentovic - Herbal Products Flashcards
Herbal Agents that became drugs
Drug Natural Agent Clinical Purpose
Aspirin ____________ _____________
Digitalis ____________ _____________
Morphine . ____________ . ______________
Placlitaxel . _____________ ______________
Eribuline ____________ ______________
True or False: Herbal products are included in government regulation by the US Food, Drug and Cosmetic Act.
False - excluded!!
No standard for efficacy, safety, validation!
Fact: Herbals…
- cannot claim for cure or treatment of disease
- CAN SAY they improve, support, promotes, etc…
Fact: Complexity of Herbal Preps
- Herbs are not uniform in nature
- Active ingredient varies with climate, soil and fertilization
- Herbs contain a complex of ingredients
- Herb product activity dependent on family of compounds
- Multiple components may have synergistic effect
What herb?
- marketed for Cardiovascular action
- lowering cholesterol
- preventing heart attack
- contains allin converted to allicin by allinase in plant and GI tract
- crushing releases ____________ (found in garlic capsules, chopped garlic and cold extracted garlic in vegetable oil)
- heat volatilizes thiosulfinate compound and diallyl sulfides releasing in to air
Garlic
Allinase
Effects of what Herb?
- lowers cholesterol (6-12%) –> comparable to Cholestyramine
- 900 mg/day powder or 1 clove
- HMG CoA reductase inhibitor*
- *-inhibits Platelet aggregation** –> similar to Ibuprofen (reversible inhibitor)
- ingredients: ajoene (allicin metabolism) and diallyl trisulfiide
- inhibit platelet COX**
- reduces platelet TXA2 generation**
Garlic
When utilizing high doses (4 cloves/day) Garlic herbal supplements, it is important to be cautious of using in combination with __________ drugs.
Chopped garlic in oil needs to be stored in refrigerator. Why?
antiplatelet drugs
Clostridium infection
What herbal supplement?
- marketed to improve vasculature (decrease leg fatigue and pain)
- -> Varicose Veins (Venostat)
-Activity attributed to Saponins
Good Herb: Escin - decreases capillary edema/pain
Bad Herb: Aesculin - adverse effects, similar to Warfarin, potential for bleeding; anti-coagulant
Horse Chestnut
Horse Chestnut
Good Herb: __________ (standardized to 16.7%)
- reduces leg pain (4x) and swelling (p<0.05)
- decreases vascular permeability of venous capillaries
Bad Herb: __________
- anticoagulant
- similar to hydroxycoumarin (Warfarin)
- bleeding gums, nose, etc.
Escin
Aesculin
What are contraindications for Horse Chestnut?
1.
2.
3.
- Anticoagulants (Warfarin), NSAIDS –> increased bleeding
- Pregnancy (Category X)
- Breast Feeding
What herbal supplement?
- sharpens mental focus
- improves cerebral circulation
- improves peripheral circulation (perfusion of capillaries)
- standardized for ginkgo flavonglycosides (active ingredients: quercetin, kaempferol, isorhamnetine)
Ginko
Effects of ________
Cardiovascular: improves blood flow in skin (brain?)
CNS
-Kaempferol
-anti-oxidant reduces free radical damage, may slow aging and improve
mental focus
-improves utilization of ATP and glucose in brain
-slows cancer cells in Ovarian cancer
-Kaempferol & Apigenin: inhibitors of MAO-A and MAO-B
Ginki
What is the major adverse effect of Ginko?
Bleeding (bleeding times can double)
Adverse Effects of what Herb?
-Major adverse effect is bleeding (Bleeding times can double)
-Drug Interactions with increased risk of bleeding*****
◦ Inhibits platelet activating factor
◦ Aspirin, NSAIDs (inhibit platelet function)
◦ Warfarin and heparin
◦ Platelet IIb/IIIa receptor antagonists (Clopidogrel)
-Lethal Ingestion of ginko seeds (contain ginkotoxin) results in seizures and death –> neurotoxin
◦ ginkotoxin (4’-O-Methylpyridoxine) - antimetabolite
◦ Anti-vitamin B6 interferes with amino acid metabolism
Ginko
What Herbal Supplement?
- Improving Mood (Depression)
- Sleep Disorders
- Weight Loss
- Standardized for Hypericin and Hyperforin (active components)
St. John’s Wort
What Herb?
-mediated by multiple mechanisms d/t neurotransmitters are altered
- Serotonin re-uptake inhibitor –> mood benefit
- dependent on Hyperforin
- MAO inhibition
- Hypericin and Hyperforin
- SSRI > MAO inhibitor
- Activation of GABA
- inhibited by Flumazenil (given for BZD overdose)
St. John’s Wort
Fact: St. John’s Wort
- *Alcohol Extract is best for anti-depressant action**
- minimum of 3% hyperforin and/or .3% hypericin (FYI)
Effective for Mild Depression ONLY
Side Effects of what herb?
-Side effects
◦ Headache and loss of appetite
-Should not be taken with
◦ MAO inhibitors
◦ Selective serotonin re-uptake inhibitors (SSRIs)
-Induces P450 isozyme Cyp 3A4********
◦ May need to increase dose of oral contraceptives, theophylline, warfarin
St. John’s Wort
What Herbal supplement?
for INSOMIA
Active ingredients: Valerenic Acid, Valtrate, Glutamine
- binds to GABA-A receptor (similar to BZD)
- GABA opens the Cl- channel, hyperpolization and decreased neuronal activity
Major Side Effect: Sedation
Valerian
What Herbal Supplement?
- Capsules, tablets, tea alcohol extracts
- lessens symptoms of colds, flu and infections
- stimulates phagocytosis and chemotaxis
- alcohol extract better than water extract
- action on the immune system
- Arabinogalactan releases IL-1 and TNFa
- Heteroxylan stimulates PMN phagocytosis
Echinacea
True or False: Echinacea prevents colds.
FALSE!! Does NOT prevent colds, but people say they felt better during colds (less congestion, lethargy and cough)
Side Effects of what Herb?
- avoid use if allergic to plants in the daisy or ragweed family
- avoid use with IMMUNOSUPPRESSANTS (Azathioprine, Corticosteroids, Cyclosporine)
Echinacea
What Herbal supplement?
- improve health of prostate
- diuretic effect
- active component in berries
- inhibitor of 5alpha-reductase
- inhibits conversion of testosterone –> dihydrotestosterone (active test molecule in the body)
-may block the translocation of the cytosol androgen receptor when bound to DHT in to the nucleus
Saw Palmetto
What drug is used in comparison to Saw Palmetto?
Finasteride (5alpha-reductase inhibitor)
Fact.
What Herbal Supplement?
- anti-oxidant, anti-aging, anti-cancer, adaptogen
- most active ingredients: Ginsenosides
- *-Cardiovascular**
- Lipid lowering and increases HDL (red)
- Panax ginseng inhibits platelet aggregation (preventing MI)
-Stimulate nitric oxide production (vasodilators = improved blood flow)
- *-Adaptogen**
- reduces cortisol and neurotransmitters during stress
Ginseng
What herbal supplement?
-Anti-cancer
◦ Lower incidence of stomach and colon cancer with use
◦ Inhibits tumor growth, stimulates apoptosis of cancer cells
-Immune system
◦ Improves chemotaxis of PMNs
◦ Stimulates interferon production
-Endocrine
◦ Improves glycemic control in diabetics
- Promotes glycogen storage (glucose –> glycogen storage)
- 10% improvement in blood glucose
Ginseng
Fact: Ginseng Adverse Effects
- *-Nervousness, Insomia**
- avoid use with caffeine
- *-Ginseng Abuse Syndrome**
- insomnia, nervous, excitable
What Herbal Supplement?
- used for sedation*** and relaxation as an alternate to alcohol
- originated in the South Pacific
- interaction with GABA receptors
SIDE EFFECTS: Hepatic Toxicity (FDA BLACK BOX WARNING)****
sedation - do NOT mix with alcohol, BZD
Yellow pigmentatio to skin (eyelids) and nails
Kava
What is the Herbal Supplement?
- *-migrane relief
- arthritis pain**
- leaves contain sesquiterpene lactones
- active component: parthenolide
- inhibits phospholipase A2 (rate limiting step in release of Arachadonic acid from membrane phospholipids)
- lower PGs
- lower leukotriene production
- inhibits platelet serotonin release
- part of the initiation phase of migrane
- alternate to drug therapy, not more effective for prevention
Feverfew
Adverse effects of what herb?
- Joint pain, muscle aches, insomnia when abruptly stopped
- Causes uterine contraction DO NOT use in pregnancy****
- Menstrual irregularities and heavier blood flow
Feverfew
Herbs Products to Avoid Prior to Surgery:
_________: inhibits platelet aggregation (ajoene and diallyl trisulfide)
_________: aesculin similar to Warfarin
_________: increases bleeding times
_________: induces P450 metabolism affecting drugs taken administered during surgery
_________: affecting phospholipase and metabolism; lipoxygenase pathway helps with chemotaxis and infection; inhibitor of CYP2C9
Garlic
Horse Chestnut
Ginko Biloba
St. John’s Wort
Feverfew
2 Herbs to Avoid when taking MAO Inhibitors or Serotonin Re-uptake Inhibitors?
St. John’s Wort
Valerian
2 Herbs to Avoid with Alcohol, increased additive sedation?
- Valerian
- Kava
Which of the following herbal agents could increase the clearance of indinavir, an HIV protease?
A. Echinacea
B. Feverfew
C. Garlic
D. St. John’s Wort
E. Saw Palmetto
St. John’s Wort, a CYP450 inducer
Which ingredient in horse chestnut is responsible for reducing leg pain?
A. Ajoene
B. Aesculin
C. Escin
D. Heteroxylan
E. Parthenolide
A. Ajoene (antiplatelet agent in garlic)
B. Aesculin (coumarin like agent in horse chestnut)
C. Escin
D. Heteroxylan (stimulates phagocytosis-echinacea)
E. Parthenolide (feverfew inhibitor of platelet serotonin release)
