food-drug interactions by professor: kamal el din hussein el tahir and dr.: dana m. bakheet...
TRANSCRIPT
Food-Drug Interactions
By
Professor: Kamal El din Hussein EL Tahir
and
Dr.: Dana M. Bakheet
Department of Pharmacology,
College of Pharmacy, KSU, Riyadh.
IntroductionIntroduction
Drugs are chemicals that are used Drugs are chemicals that are used for treatment of diseases. Their actions for treatment of diseases. Their actions
can be increased or decreased by the can be increased or decreased by the concurrent intake of other drugs or food. concurrent intake of other drugs or food. Such interaction may lead to : Such interaction may lead to :
a) An Increase or loss of the drug effect a) An Increase or loss of the drug effect
or or b) An increase in the drug’s Toxicityb) An increase in the drug’s Toxicity . .
Interactions with Foods
Interactions of Foods with Drugs can occur at different sites: a) In the stomach (By or pH) Affect the stability of the
drugs, e.g
Proteins , milk, gelatin …etc
can buffer the stomach Acidity
b) In the Intesine: b) In the Intesine: ( i ) Delay, Decrease or Increase of ( i ) Delay, Decrease or Increase of Absorption that occurs via diffusion or Absorption that occurs via diffusion or Trans porters ( Influx or Efflux types) Trans porters ( Influx or Efflux types) Influx transporters increase Influx transporters increase absorption absorption e.g Organic Anion Polypeptides e.g Organic Anion Polypeptides Efflux Transporters increase secretion Efflux Transporters increase secretion from intestinal cell into intestinal from intestinal cell into intestinal lumen e.g p-glycoprotein lumen e.g p-glycoprotein
)i i ( Increase or Decrease of Metabolism via cytochrome P 450: CYP3A4
)iii ( Adsorption of the Drug e.g pectins
)iv ( Complex formation: e.g Ca with Tetracyclines or penicillamine
((cc ) )LiverLiver increase or decrease of metabolism via Enzymes increase or decrease of metabolism via Enzymes
inhibition or stimulationinhibition or stimulation..
((dd ) )KidneyKidney : :increase or decrease of Excretion via increase increase or decrease of Excretion via increase or decrease in urinary pHor decrease in urinary pH
((ff ) )Drug ActionDrug Action : : Increase or decrease of the Beneficial ActionsIncrease or decrease of the Beneficial Actions
Increase or decrease of the side effect & ToxicityIncrease or decrease of the side effect & ToxicityPredisposition to Drug - ResistancePredisposition to Drug - Resistance
Examples of Food-Drugs Interactions 1 -Citrus Fruits:
)a (Grape Fruit Juice : Active Constituents
1 -5 - Geranyl oxy furocoumarin ) 0.3 - 6µg/ml juice (
2 -Naringenin (flavonoid) (0.7mg/ml).3 -Bergamottin (25ng/ml).
Effects on Drugs
1 (Bioavailability and t½ (Duration)
2 )Peak Blood-level concentration
in Beneficial and Toxic Actions .
)i (Drugs that are Enhanced
β – Blockers : Celiprolol, Talinolol
Antimalarials : Halofantrine; Quinine
Calcium channel Blockers :
Verapamil; Nifedipine
Felodipine; Nimodipine
Nitrendipine; Nisoldipine
Benzodiazepines: midazolam ; TriazolamAntiarrhy thmics :
Quinidine; Amiodarone Disopyramide; Propafenone
Hypolipoproteinemics: Lovastatin; Simvastatin
AtrovastafinPenile vasodilators:
Sildenafil; Tadalafil; Vardenafil
Anti – Cancer / Immuno-suppressant : Cyclosporin
Antibiotics: Clarithromycin
Anti HIV : Saquinavir
Oral Hypoglycemics Repaglinide
) ii (Drugs that are Inhibited by Grape Fruit Juice
Anticancers: Etoposide
Angiotensin II Receptor Blocker Losartan
Antiplatelets Clopidogrel
Mechanisms of Action:
)1 (Inhibition of Intestinal and Hepatic CYP450 3A4
"irreversible ”
)2 (of Transporter P-glycoprotein
Dose 250 ml of juice
Problems of Grape JuiceIncrease in Toxicity of Some Drugs
)1(Enhancement of Verapamil – induced Suppression of A – V Conduction
)2 (in Toxicity of Anti – arrhythmics
Amiodarone ; Quinidine Propafenone;
Disopyramide ; )3 (in Toxicity (Cardiac) of Carvedilol
)4 (in Ergotamine – induced gangrene
(5) in Hypotensive effects of Vasodilators
(6) in Halofantrine – induced
Prolongation of Q – T interval
(7) in Lovastatin – induced rhabodmyolysis
) 2 ( Orange Juice Consitiuents:
Dihydrobergamottin Vitamin C
Action :a) Inhibition of Bioavailability of Fexofenadine and Celiprolol Mechamism:
Of Influx Transporters Organic Anion Polypeptides
b) Decrease in Duration of Action of e.g chloroquine Mechanism: Acidification of urine increase in Excretion .
3 )Tangeretin of Citrus Fruits Action: Blocking of Breast Anticancer Effect of Tamoxifen Mechanism: Reduction in Natural Killer T – Lymphocytes (CD8+).
4 )Citrus Flavonoids Kaempferol; Quercetin
Naringenin Action:decrease of Metabolism of 17β – Oestradiol
5 )Citrus aurantium fruit and Citrus grandis pericarp
Constituents: Flavonoids Action: increase in cyclosporin bioavailability &
Increase in maximum peak Blood level Mechanism: Enhancement of Absorption Inhibition of Intestinal metabolism .
Effect of other foods or Drugs
Food Drug Effect 1) Fatty meals Carbamazepine Increase in Bioavailability
Praziquantel, Daiazepam, Phenytoin, Lovastatin
Theophylline Delay of Absorption
Cefaclor // // Indinavir // // Isosorbide mono-nitrate Delay of Absorption
due to delay in Gastric
emptying Ethambutol Decrease in Absorption Rapamy cin Delay of Absorption Metri fonate Delay of Absorption
2) Vitamin A Isotretinoin Increase in Absorption
Food Drug Effect
3( Coca – Cola Phenytoin Absorption Pepsi – Cola Antihypertensives Effect
4( Honey Carbamazepine Absorption 5( Milk Ciprofloxacin
6( Yoghourt Warfarin in Action 7( Garlic and Antiplatelets onion Hypoglycemics in Action
Antihypertesives Anticoagulants
8( Peanut and Antiplatelets sesame oil Anti hypertensives in Action
EffectDrug Food 9) Dietary fibre 9) Dietary fibre Digoxin Decrease in Absorption Digoxin Decrease in Absorption BranBran
10) Cheese 10) Cheese Tranylcypromine Increase in Action Tranylcypromine Increase in Action )Tyramine) )MAO – A lnhibitors) Severe Fever & )Tyramine) )MAO – A lnhibitors) Severe Fever & 11) Soyabean Sause11) Soyabean Sause Convulsions & Convulsions &
HypertensionHypertension
12) Foods Fortified12) Foods Fortified with iron and Ca with iron and Ca 22+ Tetracyclines+ Tetracyclines
PenicillaminePenicillamine in in AbsorptionAbsorption
FoodFood DrugDrug EffectEffect
13) Foods 13) Foods Omeprazole Omeprazole in in ActionAction
)Full stomach) )Full stomach) lansoprazole lansoprazole Itraconazloe Itraconazloe in Bioavailability in Bioavailability
14) Cran berry 14) Cran berry Warfarin Warfarin in Bleeding in Bleeding Juice Juice
15) Vitamin C15) Vitamin C Basic drugs Basic drugs e.g Pseudoephedrine Excretione.g Pseudoephedrine Excretion Tetracyclines Tetracyclines Absorption Absorption
16) Millet 16) Millet Carbimazole Carbimazole in in Action Action
17) Tea and coffee 17) Tea and coffee Analgesics in Action Analgesics in Action ) in PGI2)) in PGI2)
Haloperidol Haloperidol in Action in Action )in )in
metabolism)metabolism) Iron Iron in in
Absorption Absorption β- Blockersβ- Blockers in in
Action Action HydralazineHydralazine in Action in Action
18) Dates 18) Dates Anti-hyperlipedemics in Action Anti-hyperlipedemics in Action
19) Banana19) Banana Cimetidine Cimetidine Ranitidine Ranitidine in in
Action Action
Food Drug Food Drug InteractionInteractionLicoriceLicorice
Organic nitrate actionOrganic nitrate action
Corticosteroids Corticosteroids Retention in NaRetention in Na++
+H+H22OO
FludrocortisoneFludrocortisone
Capsicum Antihypertensive in Capsicum Antihypertensive in actionaction
Cola nut Analgesics in actionCola nut Analgesics in action
Ginger Antiplatelets in Ginger Antiplatelets in BleedingBleeding
Curcum NSAIDs in activityCurcum NSAIDs in activity
KK++ Containing ACEIs Containing ACEIs
Foods AngiotensinFoods Angiotensin
Blockers in Blockers in HyperkalemiaHyperkalemia
CyclosporineCyclosporine
KK++ Sparing Diuretics Sparing Diuretics
Other Diuretics in side Other Diuretics in side effectseffects
Tea Alkaloids e.g. in activityTea Alkaloids e.g. in activity AtropineAtropine
a) High Sodium diet Lia) High Sodium diet Li++ ExcretionExcretion
b) Alfaalfa and Ginger Anticoagulants in b) Alfaalfa and Ginger Anticoagulants in BleedingBleeding
c) Fenugreek Lovastatin in action c) Fenugreek Lovastatin in action ((Antihyperlipedemic effectAntihyperlipedemic effect))
Effect of Drugs on Foods
Drug FoodFood EffectEffect
1) Acarbose 1) Acarbose Sucrose Sucrose Absorption of Absorption of glucose glucose
and and fructosefructose
2) Fluoxetine 2) Fluoxetine Sucrose Sucrose Absorption AbsorptionLeucine Leucine in Absorption in Absorption
) Transporters)) Transporters)3) Metformin 3) Metformin Vitamins Vitamins
glucose of Absorption glucose of Absorption
4) Oral Contraceptive Vitamin B6 4) Oral Contraceptive Vitamin B6 in Excretion in Excretion
5) Tetracyclines 5) Tetracyclines Ca2+ Ca2+ and and and of Absorption and of Absorption Penicillamine Penicillamine Iron Iron