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44 Cards in this Set
- Front
- Back
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phase Ii metabolism
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Consists of conjunction reactions (addition of a chemical group): makes substances more water soluble
Usually completes the process begun in Phase I |
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Most common route; not active in neonates
Requires UDP-glucuronyl transferase (UDPGT) |
glucoronidation
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inducers of glucoronidation
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Limonene-containing foods:
• Citrus peel, dill weed oil, caraway oil Fish oils Cigarette smoking Birth control pills Many other drugs |
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detoxed via glucoronidation
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Many drugs & xenobiotics are detoxed via this route, including:
• Acetaminophen, nicotine, morphine, codeine, benzodiazepines • Androgens, estrogens, glucocorticoids, mineralcorticoids • Bile acids & bilirubin • Oganophosphates (insecticides), epoxides (carcinogens) |
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inhibit glucoronidation
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Aspirin
Probenecid (anti-gout medicine) |
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gilbert's disease is difficulty with
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glucoronidation, bilirubin builds up, limonene to treat
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sulfation detoxes
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Detoxifcatinon of many drugs & endogenous compounds such as:
• Estrogens: E1, E2, E3 & metabolites • Coumarin, acetominophen |
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sulfation inducers
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Brassicas
• Cabbage, broccoli, etc. Cysteine Methionine Taurine |
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sulfation inhibitors
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NSAID’s
Molybdenum deficiency Norepinephrine |
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Requires glutathione
Tripeptide of cysteine, glutamic acid and glycine A potent antioxidant |
glutathione conjugation
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glutathione conjugation detoxes
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Important route for elimination of various carcinogens
• N-acetylcysteine (NAC), glycine, methionine increase levels of glutathione |
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glutathione conjugation inducers
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Brassicas
• Cabbage, broccoli, etc. Cysteine Methionine Taurine Selenium Zinc Vitamin B12 |
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glutathione conjugation inhibitors
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Required nutrient deficiencies
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Primary detox for endogenous neurotransmitters (epi, norepi,
dopamine, histamine); also steroid hormones & heavy metal detox Role of methyltransferases |
methylation
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methylation inducers
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Lipotropic nutrients
• Choline, methionine • Betaine (beets) • Folic acid, vitamin B12 S-adenosyl methionine (SAMe) |
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methylation inhibitors
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Folic acid or vitamin B12 deficiency
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3 most important factors for renal clearance
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glomerular filtration, proximal tubule secretion, distal tubule reabsorption
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Free drug (unbound to albumin) passes through capillary slits into Bowman’s space as part of the glomerular filtrate
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glomerular filtration
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Drugs that weren’t excreted in the glomerulus pass via capillaries that surround the proximal tubule, where they may be
actively transported into the tubule |
proximal tubule secretion
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The concentration of drugs increases towards to distal tubule
Nonpolar drugs may be reabsorbed; changing the pH in the urine may create more of the ionized form of the drug, which won’t be reabsorbed Compounds that have been made polar via Phase I and II reactions cannot be reabsorbed, and thus pass through the kidney and out via the urine |
distal tubule secretion
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3 absorption interactions
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binding, acidity, GI motility
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Herbs and drugs may bind to one another in the intestines, leading to
absorption issues |
binding
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Most drugs need an acidic stomach environment to be absorbable
pH determines ionization of the drug Some drugs and/or herbs change the pH of the stomach, which may lead to decreased stomach acid and poor breakdown/absorption of drugs/herbs |
absorption
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Drugs/herbs may affect GI motility and affect absorption of other
compounds |
motility
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drugs/herbs that have binding effect
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Cholestyramine
• Colestipol • Sucralfate • E jiao, Lu jiao jiao, Bie jia jiao, etc. |
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acidity effect
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• Cimetidine (Tagamet)
• Famotidine (Pepcid) •Nizatidine (Axid) • Ranitidine (Zantac) •Omeprazole (Prilosec) • Mu li, Long gu, etc. may act as antacids |
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motility effect
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Increase motility
(Thus decrease time available for absorption) • Metoclopramide (Reglan) • Cisapride (Propulsid) Decrease motility (Increase time available for absorption) • Haloperidol (Haldol) |
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A highly protein-bound drug may be unbound from albumin due to
competition from another drug or herb, leading to high levels of free drug in the blood |
protein binding - distribution interactions
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warfarin has a protein binding interaction wtih
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Highly protein-bound drug
Interactions between warfarin &other compounds may either increase or decrease INR, and have been reported with: • Aspirin, ibuprofen • Vitamin K, leafy greens, Vitamin E • Green tea • Fish oils • Gingko (Gingko biloba) • American ginseng (Panax quinquefolius) • St. John’s Wort (Hypericum perfoliatum) • Garlic |
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metabolism interactions
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Herbs may induce or inhibit either phase I or phase II reactions,
leading to longer or shorter half-lives when taken with certain medications |
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drug inducers of liver metabolism
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Phenytoin (Dilantin)
• Carbamazepine (Tegretol) • Phenobarbitals • Rifampin |
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inhibitors of liver metabolism
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Cimetidine (Tagamet)
• Erythromycin • Ethanol • Fluconazole (Diflucan) • Itraconazole (Sporonox) • Ketoconazole (Nizoral) |
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herbal inhibitors of phase I
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Wu wei zi/Schizandra
• Jue ming zi/Cassia seed • Tian hua fen/Trichosanthus root • Others? |
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elimination interactions
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Kidney disease may inhibit proper elimination of herbs/drugs
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kidney damaging drugs
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Amphotericin B, gentimicin, tobramicin,
methotrexate |
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pharmacodynamic herb-drug interactions
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Refers to the fluctuation in bioavailability of ingested substances as a result of synergistic or antagonistic interactions
between herb-drug molecules • More difficult to predict that pharmacokinetic interactions • Important just to monitor the signs/symptoms of your patient |
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additive/synergistic efffects
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Occurs when 2 molecules of similar properties
show an additive or increased clinical effects when given together |
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Herbs with sympathomimic effects may interfere with
antihypertensive and antiseizure drugs |
Ma Huang
• Zhi shi • Fu zi |
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herbs with psychotropic effects
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may interact
with psychiatric medications such as SSRI’s, atypical antidepressants, MAO-inhibitors, tricyclic antidepressants, and benzodiazepines • Ginkgo • Ren shen • St. John’s wort |
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Herbs with diuretic effects and diuretic drugs may have additive or
synergistic effects • May induce hypotensive episodes/syncope |
• Fu ling
• Zhu ling • Che qian zi • Ze xi |
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Herbs with anticoagulant effects (blood-activing, blood-stasis
removing herbs) may interfere with anticoagulant medication (Warfarin/Coumadin) to prolong bleeding time |
Dan shen
• Dang gui • Chuan xiong • Tao ren • Hong hua • Shui zhi |
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Herbs with anti-diabetic properties may interfere with anti-diabetic
drugs by enhancing hypoglycemic effects |
Zhi mu & Shi gao
• Xuan shen & Cang zhu • Shan yao & Huang qi |
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Occurs when 2 molecules of similar properties show lessened or no clinical effect when given together
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antagonistic effects
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Adverse Effects in Pregnancy/Teratogenic Herbs
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Prohibited herbs
Potent and very toxic: prohibited during pregnancy • Ba Dou, Qian Niu Zi • Da Ji • Ban Mao • Shang Lu • She Xiang • San Leng, E Zhu • Shui Zhi, Meng Chong Herbs used with caution during pregnancy • Tao Ren • Hong Hua • Da Huang • Zhi Shi • Fu Zi • Gan Jiang • Rou Gui |
