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Drug Interactions between benzgalantamine and itraconazole

This report displays the potential drug interactions for the following 2 drugs:

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Interactions between your drugs

Moderate

itraconazole benzgalantamine

Applies to: itraconazole and benzgalantamine

MONITOR: Coadministration with potent inhibitors of CYP450 2D6 and/or 3A4 may increase the plasma concentrations of galantamine, which is also an active metabolite of benzgalantamine. Up to 75% of galantamine is eliminated via metabolism and in vitro studies have identified CYP450 2D6 and 3A4 as the major isoenzymes involved. The systemic exposure (AUC) of galantamine (4 mg, 8 mg, or 12 mg twice daily) increased by 40%, 45%, and 48%, respectively, when administered to healthy volunteers (n=16) also receiving the strong CYP450 2D6 inhibitor paroxetine. Similarly, the strong CYP450 3A4 inhibitor ketoconazole (200 mg twice daily) increased the AUC of galantamine (4 mg twice daily) by 30% when given concurrently to study subjects (n=16). An increase in the AUC of galantamine can increase the risk of acetylcholinesterase inhibitor-related adverse effects. One potential side effect of galantamine is bradycardia, which may increase the risk of QT prolongation. If the inhibitor being coadministered is also associated with QT prolongation (e.g., adagrasib, ceritinib, fluoxetine, ketoconazole, levoketoconazole, mifepristone), the risk of experiencing this adverse effect may be further increased.

MANAGEMENT: Caution and closer monitoring of the pharmacologic response to galantamine and its prodrug benzgalantamine is advised whenever a potent CYP450 2D6 and/or 3A4 inhibitor is added to or withdrawn from therapy. Some authorities suggest considering a reduction in the galantamine dose for patients on concurrent potent CYP450 2D6 and/or 3A4 inhibitors. Patients should be monitored more closely for acetylcholinesterase inhibitor related adverse effects including vagotonic effects on the heart rate (e.g., bradycardia, which may increase the risk of QT prolongation, and heart block), neurologic side effects (e.g., seizure activity), respiratory distress, bladder outflow obstruction, dizziness or syncope, nausea, vomiting and diarrhea. These effects may be more severe when the coadministered inhibitor shares a similar adverse effect profile with galantamine.

References (7)
  1. (2024) "Product Information. Galantamine Hydrobromide ER (galantamine)." Aurobindo Pharma USA Inc
  2. (2024) "Product Information. Galantamine Hydrobromide (galantamine)." Aurobindo Pharma USA Inc
  3. (2022) "Product Information. Gaalin (galantamine)." Auro Pharma Inc
  4. (2023) "Product Information. Galzemic (galantamine)." Zentiva Pharma UK Ltd
  5. (2023) "Product Information. Galantyl (galantamine)." Viatris UK Healthcare Ltd
  6. (2020) "Product Information. Auro-Galantamine ER (galantamine)." Auro Pharma Inc
  7. (2024) "Product Information. Zunveyl (benzgalantamine)." Alpha Cognition, Inc., SUPPL-1

Drug and food interactions

Moderate

itraconazole food

Applies to: itraconazole

ADJUST DOSING INTERVAL: Food increases the absorption of itraconazole capsules but decreases the absorption of itraconazole oral solution. Cola beverages may increase the bioavailability of itraconazole capsules. Itraconazole capsules require an acidic gastric pH for adequate dissolution and subsequent absorption. Cola beverages help lower gastric pH and improve absorption.

GENERALLY AVOID: Grapefruit juice may impair the absorption of itraconazole capsules, resulting in decreased antifungal effects. In a small, randomized, crossover study, the administration of itraconazole capsules with double-strength grapefruit juice (compared to water) was associated with significantly decreased (43%) plasma concentrations of itraconazole and its pharmacologically active hydroxy metabolite, as well as delayed times to reach peak concentrations of both. The exact mechanism of interaction is unknown but may involve reduced absorption of itraconazole secondary to enhanced activity of intestinal P-glycoprotein drug efflux pumps and delayed gastric emptying induced by certain compounds present in grapefruits. Another study reported no pharmacokinetic changes with single-strength grapefruit juice. Whether or not these observations apply to itraconazole oral solution is unknown.

MANAGEMENT: The manufacturer recommends that the capsules be taken immediately after a full meal and the solution be taken on an empty stomach to ensure maximal absorption. Cola beverages may help increase the bioavailability of itraconazole capsules, particularly in patients with hypochlorhydria or those treated concomitantly with gastric acid suppressants. Until more information is available, it may be advisable to avoid the consumption of grapefruits and grapefruit juice during itraconazole therapy.

References (10)
  1. Van Peer A, Woestenborghs R, Heykants J, et al. (1989) "The effects of food and dose on the oral systemic availability of itraconazole in healthy subjects." Eur J Clin Pharmacol, 36, p. 423-6
  2. Wishart JM (1987) "The influence of food on the pharmacokinetics of itraconazole in patients with superficial fungal infection." J Am Acad Dermatol, 17, p. 220-3
  3. (2002) "Product Information. Sporanox (itraconazole)." Janssen Pharmaceuticals
  4. Barone JA, Koh JG, Bierman RH, Colaizzi JL, Swanson KA, Gaffar MC, Moskovitz BL, Mechlinski W, Van de Velde V (1993) "Food interaction and steady-state pharmacokinetics of itraconazole capsules in healthy male volunteers." Antimicrob Agents Chemother, 37, p. 778-84
  5. Zimmermann T, Yeates RA, Albrecht M, Laufen H, Wildfeuer A (1994) "Influence of concomitant food intake on the gastrointestinal absorption of fluconazole and itraconazole in japanese subjects." Int J Clin Pharmacol Res, 14, p. 87-93
  6. (2022) "Product Information. Sporanox (itraconazole)." Janssen Pharmaceuticals
  7. Kawakami M, Suzuki K, Ishizuka T, Hidaka T, Matsuki Y, Nakamura H (1998) "Effect of grapefruit juice on pharmacokinetics of itraconazole in healthy subjects." Int J Clin Pharmacol Ther, 36, p. 306-8
  8. Barone JA, Moskotitz BL, Guarnieri J, Hassell AE, Colaizzi JL, Bierman RH, Jessen L (1998) "Food interaction and steady-state pharmacokinetics of itraconazole oral solution in healthy volunteers." Pharmacotherapy, 18, p. 295-301
  9. Penzak SR, Gubbins PO, Gurley BJ, Wang PL, Saccente M (1999) "Grapefruit juice decreases the systemic availability of itraconazole capsules in healthy volunteers." Ther Drug Monit, 21, p. 304-9
  10. Katz HI (1999) "Drug interactions of the newer oral antifungal agents." Br J Dermatol, 141, p. 26-32

Therapeutic duplication warnings

No warnings were found for your selected drugs.

Therapeutic duplication warnings are only returned when drugs within the same group exceed the recommended therapeutic duplication maximum.

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Drug Interaction Classification

These classifications are only a guideline. The relevance of a particular drug interaction to a specific individual is difficult to determine. Always consult your healthcare provider before starting or stopping any medication.
Major Highly clinically significant. Avoid combinations; the risk of the interaction outweighs the benefit.
Moderate Moderately clinically significant. Usually avoid combinations; use it only under special circumstances.
Minor Minimally clinically significant. Minimize risk; assess risk and consider an alternative drug, take steps to circumvent the interaction risk and/or institute a monitoring plan.
Unknown No interaction information available.

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