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DR.VISHNU.R.NAIR,
PHARM-D,
NATIONAL COLLEGE OF PHARMACY, KERALA.
Penicillins  come under the class of “Antibiotics”
Penicillins  bactericidal in nature, owing to their cell-
synthesis inhibition property  leads to death of susceptible
organism.
Penicillins  consist of both natural and semi-synthetic
penicillins
Penicillins show variety of drug-drug and drug-food
interactions
This presentation  aims at exploring the significant drug-
food interactions of penicillins with food.
 Absorption of Penicillin & Penicillin V(Phenoxymethyl penicillin)
Reduced significantly with food co-administration
 Thus  Penicillin V(the only oral formulation currently available)
Should be taken on an empty stomach(1 or 2 hours before meals)
Facilitates drug absorption!
Cronk GA, Wheatley WB, Fellers GF, Albright H (1960) The relationship of food intake to the absorption of potassium alpha-phenoxyethyl penicillin and potassium phenoxymethyl penicillin from the
gastrointestinal tract. Am J Med Sci 241:125–131
 Ampicillin if given with food  AUC reduces by 50%!
 According to some studies  ampicillin absorption was reduced, when given with:
a. High carbohydrate
b. High protein
c. High-fat meals
d. Sudanese diet(rich in wheat, flour and corn)
Welling PG, Huang H, Koch PA, Craig WA, Madsen PO (1977) Bioavailability of ampicillin and amoxicillin in fasted and nonfasted subjects. J Pharm Sci 66:549–552
Ali HM, Farouk AM (1980) The effect of sudanese diet on the bioavailability of ampicillin. Int J Pharm 6:301–306
Eshelman FN, Spyker DA (1978) Pharmacokinetics of amoxicillin and ampicillin: crossover study of the effect of food. Antimicrob Agents Chemother 14:539–543
 Interestingly  amoxicillin  if given in 25 ml of water  absorption is reduced,
as compared to 250 ml!
 Thus  amoxicillin is recommended to be taken with a full glass of water(250
ml)!
 Amoxicillin extended-release(ER) tablets  given to provide OD dosing of
amoxicillin for the treatment of tonsillitis &/ pharyngitis, secondary to
Streptococcus pyogenes.
 If ER tablet  given with food  rate of absorption is reduced, but extent is
unaffected
 Thus  ER tablets should be taken within 1 hour of finishing a meal.
Anonymous. MOXATAG (amoxicillin extended-release tablets) [package insert]. Germantown, MD; Middlebrook Pharmaceuticals, Inc. Revised December 2008. Available from:
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=a6c0e721-2021-4983- a305-49bdf8f135a9. Accessed 14 November 2019
 Combination of amoxicillin-clavulanate  if given with food  reduced GI ADRs
observed!
 According to the manufacturer
Amoxicillin tablets, powder and chewable tablets
May be given irrespective of meals.
Staniforth DH, Lillystone RJ, Jackson D (1982) Effect of food on the bioavailability and tolerance of clavulanic acid/amoxycillin combination. J Antimicrob Chemother 10:131–139
Anonymous. AUGMENTIN (amoxicillin/clavulanate potassium) [package insert]. Research Triangle Park, NC; Glaxo Smith Kline. Revised May 2002. Available from: https://www.
accessdata.fda.gov/drugsatfda_docs/label/2008/050575s037550597s044050725s025050726 s019lbl.pdf. Accessed 14 November 2019
 Combination of amoxicillin-clavulanate  if given with food  reduced GI ADRs
observed!
 According to the manufacturer
Amoxicillin tablets, powder and chewable tablets
May be given irrespective of meals.
Staniforth DH, Lillystone RJ, Jackson D (1982) Effect of food on the bioavailability and tolerance of clavulanic acid/amoxycillin combination. J Antimicrob Chemother 10:131–139
Anonymous. AUGMENTIN (amoxicillin/clavulanate potassium) [package insert]. Research Triangle Park, NC; Glaxo Smith Kline. Revised May 2002. Available from: https://www.
accessdata.fda.gov/drugsatfda_docs/label/2008/050575s037550597s044050725s025050726 s019lbl.pdf. Accessed 14 November 2019
Although prescribing information for dicloxacillin mentions that
Food in GIT reduces drug absorption of dicloxacillin
There are no substantial data's
 According to recommendations  dicloxacillin should be taken on an empty
stomach, atleast 1 hr before or 2 hours after a meal!
Anonymous. DYNAPEN (dicloxacillin) [package insert]. North Wales, PA; Teva Pharmaceuticals, Inc. Revised June 2016. Available from: https://www.drugs.com/pro/ dicloxacillin.html. Accessed 14
November 2019
CONCLUSION
PENICILLIN FORMULATION MANUFACTURER
RECOMMENDATIONS
Penicillin V Penicillin V, powder for oral
solution
• May be given with meals
• Plasma drug concentrations 
higher, when given on empty
stomach
Ampicillin Capsules Administer 30 minutes before / 2
hours after meals
Powder for oral suspension Administer 30 minutes before / 2
hours after meals
Amoxicillin Capsules, tablets, chewable
tablets
Can be given without regard to
meals
Extended-release tablets Should be taken within 1 hour of
finishing a meal.
PENICILLIN FORMULATION MANUFACTURER
RECOMMENDATIONS
Amoxicillin/clavulanate Tablets and chewable tablets Should be given at the start of
meals to minimize GI upset
Extended-release tablets • Should be taken at start of meal
 increases drug absorption 
reduces GI ADRs
• Never take drug with HIGH-
FAT MEALS(Clavulanate
absorption is reduced)
Powder for oral suspension Can be given, regardless of meals.
Dicloxacillin Capsules Should be taken on an empty
stomach(1 hour before meals or 2
hours after meals).
THANK YOU!!!

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Food drug interactions with penicillins: by RxVichuZ!

  • 2. Penicillins  come under the class of “Antibiotics” Penicillins  bactericidal in nature, owing to their cell- synthesis inhibition property  leads to death of susceptible organism. Penicillins  consist of both natural and semi-synthetic penicillins Penicillins show variety of drug-drug and drug-food interactions This presentation  aims at exploring the significant drug- food interactions of penicillins with food.
  • 3.  Absorption of Penicillin & Penicillin V(Phenoxymethyl penicillin) Reduced significantly with food co-administration  Thus  Penicillin V(the only oral formulation currently available) Should be taken on an empty stomach(1 or 2 hours before meals) Facilitates drug absorption! Cronk GA, Wheatley WB, Fellers GF, Albright H (1960) The relationship of food intake to the absorption of potassium alpha-phenoxyethyl penicillin and potassium phenoxymethyl penicillin from the gastrointestinal tract. Am J Med Sci 241:125–131
  • 4.  Ampicillin if given with food  AUC reduces by 50%!  According to some studies  ampicillin absorption was reduced, when given with: a. High carbohydrate b. High protein c. High-fat meals d. Sudanese diet(rich in wheat, flour and corn) Welling PG, Huang H, Koch PA, Craig WA, Madsen PO (1977) Bioavailability of ampicillin and amoxicillin in fasted and nonfasted subjects. J Pharm Sci 66:549–552 Ali HM, Farouk AM (1980) The effect of sudanese diet on the bioavailability of ampicillin. Int J Pharm 6:301–306 Eshelman FN, Spyker DA (1978) Pharmacokinetics of amoxicillin and ampicillin: crossover study of the effect of food. Antimicrob Agents Chemother 14:539–543
  • 5.  Interestingly  amoxicillin  if given in 25 ml of water  absorption is reduced, as compared to 250 ml!  Thus  amoxicillin is recommended to be taken with a full glass of water(250 ml)!  Amoxicillin extended-release(ER) tablets  given to provide OD dosing of amoxicillin for the treatment of tonsillitis &/ pharyngitis, secondary to Streptococcus pyogenes.  If ER tablet  given with food  rate of absorption is reduced, but extent is unaffected  Thus  ER tablets should be taken within 1 hour of finishing a meal. Anonymous. MOXATAG (amoxicillin extended-release tablets) [package insert]. Germantown, MD; Middlebrook Pharmaceuticals, Inc. Revised December 2008. Available from: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=a6c0e721-2021-4983- a305-49bdf8f135a9. Accessed 14 November 2019
  • 6.  Combination of amoxicillin-clavulanate  if given with food  reduced GI ADRs observed!  According to the manufacturer Amoxicillin tablets, powder and chewable tablets May be given irrespective of meals. Staniforth DH, Lillystone RJ, Jackson D (1982) Effect of food on the bioavailability and tolerance of clavulanic acid/amoxycillin combination. J Antimicrob Chemother 10:131–139 Anonymous. AUGMENTIN (amoxicillin/clavulanate potassium) [package insert]. Research Triangle Park, NC; Glaxo Smith Kline. Revised May 2002. Available from: https://www. accessdata.fda.gov/drugsatfda_docs/label/2008/050575s037550597s044050725s025050726 s019lbl.pdf. Accessed 14 November 2019
  • 7.  Combination of amoxicillin-clavulanate  if given with food  reduced GI ADRs observed!  According to the manufacturer Amoxicillin tablets, powder and chewable tablets May be given irrespective of meals. Staniforth DH, Lillystone RJ, Jackson D (1982) Effect of food on the bioavailability and tolerance of clavulanic acid/amoxycillin combination. J Antimicrob Chemother 10:131–139 Anonymous. AUGMENTIN (amoxicillin/clavulanate potassium) [package insert]. Research Triangle Park, NC; Glaxo Smith Kline. Revised May 2002. Available from: https://www. accessdata.fda.gov/drugsatfda_docs/label/2008/050575s037550597s044050725s025050726 s019lbl.pdf. Accessed 14 November 2019
  • 8. Although prescribing information for dicloxacillin mentions that Food in GIT reduces drug absorption of dicloxacillin There are no substantial data's  According to recommendations  dicloxacillin should be taken on an empty stomach, atleast 1 hr before or 2 hours after a meal! Anonymous. DYNAPEN (dicloxacillin) [package insert]. North Wales, PA; Teva Pharmaceuticals, Inc. Revised June 2016. Available from: https://www.drugs.com/pro/ dicloxacillin.html. Accessed 14 November 2019
  • 10. PENICILLIN FORMULATION MANUFACTURER RECOMMENDATIONS Penicillin V Penicillin V, powder for oral solution • May be given with meals • Plasma drug concentrations  higher, when given on empty stomach Ampicillin Capsules Administer 30 minutes before / 2 hours after meals Powder for oral suspension Administer 30 minutes before / 2 hours after meals Amoxicillin Capsules, tablets, chewable tablets Can be given without regard to meals Extended-release tablets Should be taken within 1 hour of finishing a meal.
  • 11. PENICILLIN FORMULATION MANUFACTURER RECOMMENDATIONS Amoxicillin/clavulanate Tablets and chewable tablets Should be given at the start of meals to minimize GI upset Extended-release tablets • Should be taken at start of meal  increases drug absorption  reduces GI ADRs • Never take drug with HIGH- FAT MEALS(Clavulanate absorption is reduced) Powder for oral suspension Can be given, regardless of meals. Dicloxacillin Capsules Should be taken on an empty stomach(1 hour before meals or 2 hours after meals).