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DRUG-FOOD & HERBAL

INTERACTIONS
HASHMI FURQAN
• FOOD can increase, decrease or not affect the
absorption of drugs
• Food may influence bioavailability of drugs
from modified-release dosage form
For example: opening of capsule of enteric coated
Omeprazole beads & giving it in a acidic food
such as orange juice  eases administration of
the drug maintaining the enteric coating until the
drug reaches the basic pH of the duodenum
• Complexation & Adsorption affecting the extent of absorption
For example: Quinolones & di- or tri-valent containing elements
• Food can be metabolized by the same hepatic enzymes
causing enzyme induction or inhibition  toxic or subtherapeutic
levels
For example: grapefruit inhibits CYP3A4  increased level of substrate
drugs such as Midazolam. Nimodipine, Nifedipine, Lovastatin, CBZ,
Verapamil
• Food can pharmacodynamically antagonize the effects of some
drugs 
For example: Spinach & broccoli provide dietary source of vitamin-K 
antagonizes the effect of warfarin
garlic can cause additive antiplatelet effect in combination with
warfarin, heparin & low mol. wt. heparin (LMWH)  increased risk
of bleeding
Foods can contain pharmacologically
active compounds  Interact with drugs
meant to inhibit endogenous compounds
For Example: MAOIs prevent normal
metabolism of catecholamines.
Also inhibit the metabolism of tyramine from
tyramine-containing foods such as red
wine & cheese (increased levels of
tyramine cause hypertensive crisis)
Affect of food on drug bioavailability

Reduced or Increased No effect


Delayed
NSAIDs Naproxen, Griseofulvin Theophylline
naproxen sodium, Metoprolol
aspirin, Phytoin
acetoaminophen
Proproxyphene Metronidazole
Antibiotics
Dicumarol
Tetracyclin &
penicillins Morphine

Ethanol
HERBAL-DRUG INTERACTIONS

• Herbal preparations contain combinations


of herbs or a single herb

• Some herbal preparations represent a


single herb containing a variety of
alkaloids or constituents that may exhibit a
variety of pharmacological activities
Some herbs contain a No. of different pharmacologically active
constituents
For example: St John’s wort  6 different constituents i.e. Hyperforin,
Biapigenin, Hypericin, Quericitin, Chlorogenic acid, &
Pseudohypericin
• Each constituent has its own action, metabolism, binding &
pharmacological action
• Predominant effect or interaction depends on the relative potency of
each constituent
The constituents of St john wort have inhibitory effects on CYP450
isozymes 3A4, 2C9, 1A2, 2D6 & 2D9
It appears overall to be an inducer of CYP3A4

Many herbal drugs interact at the same transport, metabolism &


receptor sites as traditional prescription drugs
• Traditional Chinese medicines may
contain combination of herbs

• Some products have been found to


contain some unlisted legend drugs

• Some herbals may contain some


contaminants such as heavy metals
• Pharmacodynamic or pharmacokinetic interactions
• Drugs with narrow therapeutic window are at greater risk for drug-herbal
interactions

For example  important herbal-drug interaction occurs in patients taking


warfarin

• Coenzyme Q10 has a chemical structure related to vitamin K. combination


of CoQ10 and warfarin antagonizes warfarin’s effects  inadequate
anticoagulation

• Ginger and garlic also increase bleeding in pts taking warfarin by directly
inhibiting platelets & causing increased risk of bleeding

• Wheat grass contains high levels of vit-K which directly antagonize the
warfarin  inadequate anticoagulation
Potency of herbal product
Potency of herbal product is influenced by a
variety of factors
• The stage of growth during which herb
was harvested
• Drying time
• Solvents used for the extraction of herbs
• Shelf life & storage conditions of the
herbal extract

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