Tablet levothyroxine (L-T4) malabsorption induced by proton pump inhibitor: a problem that was solved by switching to L-T4 in soft gel capsule
Abstract
Objective To report a patient in whom the impaired absorption of tablet levothyroxine (L-T4) due to a proton pump inhibitor (PPI) use was corrected by switching the patient to the soft gel capsule.Methods A woman with Hashimoto's thyroiditis-associated hypothyroidism (serum thyroid-stimulating hormone [TSH] 6.8-9.6 mU/L) had been treated with tablet L-T4 (100 μg/day). Because she used to take pantoprazole just before L-T4 in the morning, TSH failed to normalize (4.4-6.5 mU/L). Thus, the daily dose had been progressively increased to 125 and 150 μg/day, with serum TSH levels of 2.4 and 0.6 mU/L, respectively.Results While maintaining pantoprazole, we switched the tablet L-T4 (150 g/day) to a soft gel capsule (125 μg/day; Tirosint® capsule, IBSA, Lugano, Switzerland) and after 2 months, to 100 μg/day. Serum TSH was lower than under the equivalent regimens with the tablet: 0.5 versus 2.4 mU/L (125 μg/day) and 2.4 versus 4.4 to 6.5 mU/L (100 μg/day). Upon switching back to the tablet (100 μg/day), serum TSH increased to 3.2 and 4.7 mU/L and then dropped to 2.7-3.0 mU/L when the dose was increased to 125 μg/day. We also acutely evaluated the intestinal absorption of L-T4 by administering 600 μg LT4 as a tablet or soft gel capsule while maintaining pantoprazole. Pharmacokinetic indices showed better and faster absorption for the soft gel capsule versus tablet (area under the curve [AUC]0-4h = 16,240 vs. 10,960 nmol/L x 4 hours, maximum absorption [Cmax] = 108 vs. 73 nmol/L, and time of maximum absorption [Tmax] = 120 minutes vs. 180 minutes).Conclusion Confirming in vitro studies conducted by other authors, the soft gel capsule L-T4 is negligibly affected by changes in gastric pH compared to tablet L-T4.
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An absorption study showed better absorption of LT4 from the gel capsule.
“An absorption study showed better absorption of the LT4 from the gel capsule (114).”
From Guidelines for the Treatment of Hypothyroidism: Prepared by the American Thyroid Association Task Force on Thyroid Hormone Replacement (2014) · cites this paper as [114]
A case report describes a patient taking a PPI whose serum TSH was higher during treatment with LT4 tablets than with the same dose given as a gel capsule.
“A case report describes a patient taking a PPI whose serum TSH was higher during treatment with LT4 tablets than with the same dose given as a gel capsule.”
From Guidelines for the Treatment of Hypothyroidism: Prepared by the American Thyroid Association Task Force on Thyroid Hormone Replacement (2014) · cites this paper as [114]
Malabsorption due to calcium supplements, PPIs, breakfast, H. pylori infection, and gastroparesis was eradicated after switching from tablets to capsules.
“Malabsorption due to calcium supplements (99), PPIs (226), breakfast (206), H. pylori infection (227), and gastroparesis (202) was eradicated after switching from tablets to capsules.”
From Levothyroxine: conventional and novel drug delivery formulations. (2023) · cites this paper as [226]
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- Authors
- Vita, R., & Benvenga, S.
- Affiliations
- University of Messina (IT)
- Corresponding author
- Vita, Roberto
- Venue
- Endocrine Practice
- Publisher
- Elsevier BV
- Published
- 2014-03
- Volume
- 20
- Issue
- 3
- Pages
- e38-e41
- ISSN
- 1530-891X (ISSN-L)
- OpenAlex
- W2013324388
- Cited by
- 60
- References
- 14
- Citations by year
- 2025: 1 · 2024: 4 · 2023: 2 · 2022: 7 · 2021: 6 · 2020: 3 · 2019: 6 · 2018: 4 · 2017: 7 · 2016: 8 · 2015: 7 · 2014: 4 · 2013: 1
- FWCI
- 5.24
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Endocrine Practice (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Thyroid Disorders and Treatments
- Health Sciences › Medicine › Surgery › Thyroid and Parathyroid Surgery
- Health Sciences › Medicine › Gastroenterology › Gastroesophageal reflux and treatments
- Keywords
- levothyroxine, drug malabsorption, proton pump inhibitors, pantoprazole, tablet formulation, Hashimoto's thyroiditis, hypothyroidism, thyroid-stimulating hormone, pharmacokinetics, drug-drug interactions, antacids, dose adjustment, TSH normalization, antithyroid drugs
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