Hypothyroidism following gastric sleeve surgery resolved by ingesting crushed thyroxine tablets

Fain, Kristen; Rojas, Alexsandra P.; Peiris, Alan N.

doi:10.1080/08998280.2019.1669412

Cited by 7 publications

(8 citation statements)

References 10 publications

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“…71 Tablet crushing/capsule opening is meant to spare the process of dosage from disintegration and thus speeds up the dissolution of the drug dose. 96 However, in this study, tablet crushing did not affect the amount of dissolved loratadine in OAGB conditions (f 1 = 0.29), and while increased post-SG dissolution was evident (f 1 = 70.4), this increase was very modest (3.1 to 4.4%) and practically insignificant (Table 4). Apparently, tablet crushing may be beneficial in some cases, but it is important to realize that this is not a "magic" solution that guarantees overcoming solubility/dissolution complications.…”

Section: Discussioncontrasting

confidence: 56%

“…Also, if possible, oral liquid dosage forms should be used instead of solid dosage forms . Tablet crushing/capsule opening is meant to spare the process of dosage from disintegration and thus speeds up the dissolution of the drug dose . However, in this study, tablet crushing did not affect the amount of dissolved loratadine in OAGB conditions ( f 1 = 0.29), and while increased post-SG dissolution was evident ( f 1 = 70.4), this increase was very modest (3.1 to 4.4%) and practically insignificant (Table ).…”

Section: Discussionmentioning

confidence: 62%

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Antiallergic Treatment of Bariatric Patients: Potentially Hampered Solubility/Dissolution and Bioavailability of Loratadine, but Not Desloratadine, Post-Bariatric Surgery

et al. 2022

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Gastrointestinal anatomical/physiological changes after bariatric surgery influence variables affecting the fate of drugs after ingestion, and medication management of these patients requires a thorough and complex mechanistic analysis. The aim of this research was to study whether loratadine/desloratadine antiallergic treatment of bariatric patients is at risk of being ineffective due to impaired solubility/dissolution. The pH-dependent solubility of loratadine/desloratadine was studied in vitro, as well as ex vivo, in gastric content aspirated from patients before versus after bariatric surgery. Then, a biorelevant dissolution method was developed to simulate the gastric conditions after sleeve gastrectomy (SG) or one-anastomosis gastric bypass (OAGB), accounting for key variables (intragastric volume, pH, and contractility), and the dissolution of loratadine/desloratadine was studied pre- versus post-surgery. Dissolution was also studied after tablet crushing or syrup ingestion, as these actions are recommended after bariatric surgery. Finally, these experimental data were implemented in a newly developed physiologically based pharmacokinetic (PBPK) model to simulate loratadine/desloratadine PK profiles pre- versus post-surgery. For both drugs, pH-dependent solubility was demonstrated, with decreased solubility at higher pH; over the pH range 1–7, loratadine solubility decreased ∼2000-fold, and desloratadine decreased ∼120-fold. Ex vivo solubility in aspirated human gastric fluid pre- versus post-surgery was in good agreement with these in vitro results and revealed that while desloratadine solubility still allows complete dissolution post-surgery, loratadine solubility post-surgery is much lower than the threshold required for the complete dissolution of the drug dose. Indeed, severely hampered loratadine dissolution was revealed, dropping from 100% pre-surgery to only 3 and 1% post-SG and post-OAGB, respectively. Tablet crushing did not increase loratadine dissolution in any post-bariatric condition, nor did loratadine syrup in post-OAGB (pH 7) media, while in post-laparoscopic SG conditions (pH 5), the syrup provided partial improvement of up to 40% dissolution. Desloratadine exhibited quick and complete dissolution across all pre-/post-surgery conditions. PBPK simulations revealed pronounced impaired absorption of loratadine post-surgery, with 84–88% decreased C max, 28–36% decreased F a, and 24–31% decreased overall bioavailability, depending on the type of bariatric procedure. Desloratadine absorption remained unchanged post-surgery. We propose that desloratadine should be preferred over loratadine in bariatric patients, and as loratadine is an over-the-counter medication, antiallergic therapy after bariatric surgery requires special attention by patients and clinicians alike. This mechanistic approach that reveals potential post-surgery complexity, and at the same time provides adequate substitutions, may contribute to better pharmacotherapy and overall patient care after bariatric surgery.

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Section: Discussioncontrasting

confidence: 56%

Section: Discussionmentioning

confidence: 62%

Antiallergic Treatment of Bariatric Patients: Potentially Hampered Solubility/Dissolution and Bioavailability of Loratadine, but Not Desloratadine, Post-Bariatric Surgery

et al. 2022

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“…Pharmacokinetics of levothyroxine has been shown to play a role in other studies, including a case report describing a patient presenting with recurrent features of hypothyroidism following sleeve gastrectomy [ 6 ]. The TSH in this patient continued to rise, despite increasing the levothyroxine dose.…”

Section: Discussionmentioning

confidence: 99%

“…A retrospective study in 2017 stated that bariatric surgery reduces the requirement for thyroid replacement therapy in bariatric patients with concomitant hypothyroidism one year following surgery, with 13% of patients no longer requiring any thyroid replacement [ 5 ]. Conversely, a case report published in 2020 described the development of iatrogenic hypothyroidism following gastric sleeve surgery [ 6 ].…”

Section: Introductionmentioning

confidence: 99%

The Effect of Different Types of Bariatric Surgery on Levothyroxine Requirement in Hypothyroid Bariatric Patients

Dewantoro¹,

Davenport²,

Goh³

et al. 2022

Cureus

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BackgroundBariatric surgeries are carried out to improve a patient's quality of life, and to reduce respiratory, cardiac, endocrine, and metabolic complications encountered by those with high body mass index (BMI). A complication associated with high hypothyroidism is weight gain, which may lead to obesity. Here, we explore the effect of different bariatric procedures on thyroid function and levothyroxine dosage. MethodsThis is a retrospective review of 887 patients referred to a tertiary bariatric service between 2008 and 2020 and treated for hypothyroidism at the time of referral.The study identified 57 patients on thyroxine replacement. Of these, 22 underwent restrictive bariatric procedures, 16 underwent restrictive/malabsorptive procedures, and 19 did not undergo operative intervention.Comparisons were made among each group throughout the timeline of interest.

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“…antacids, calcium, iron), drugs (e.g. laxatives, sevelamer, proton pump inhibitors), or soya protein [24][25][26][27][28][29]. The solubility of LT4 increases as pH decreases [30].…”

Section: Malabsorption Of and Suboptimal Adherence To Levothyroxinementioning

confidence: 99%

Administration and Pharmacokinetics of Levothyroxine

Lipp

2021

70 Years of Levothyroxine

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Lifelong treatment with LT4, guided by levels of thyrotropin, is the mainstay of management of hypothyroidism. The bioavailability of LT4 is about 70% following an oral dose, with absorption occurring mainly in the ileum and jejunum. Maximum plasma concentrations of LT4 are achieved about 3 h after an oral dose in patients with hypothyroidism. The long terminal half-life of orally administered LT4, about 7.5 days, is consistent with once-daily dosing. Pregnancy, several medical conditions (especially) those affecting the gut, and a number of drugs, supplements, or foodstuffs can reduce the absorption and absolute bioavailability of LT4, or can alter the secretion of TSH, with detrimental consequences for longterm control of thyroid function. Poor adherence to LT4 therapy is also a common challenge. The introduction of novel formulations of LT4, with more precise delivery of the active ingredient and higher levels of bioequivalence with existing products will facilitate accurate titration of LT4 for patients with hypothyroidism.

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Hypothyroidism following gastric sleeve surgery resolved by ingesting crushed thyroxine tablets

Cited by 7 publications

References 10 publications

Antiallergic Treatment of Bariatric Patients: Potentially Hampered Solubility/Dissolution and Bioavailability of Loratadine, but Not Desloratadine, Post-Bariatric Surgery

Antiallergic Treatment of Bariatric Patients: Potentially Hampered Solubility/Dissolution and Bioavailability of Loratadine, but Not Desloratadine, Post-Bariatric Surgery

The Effect of Different Types of Bariatric Surgery on Levothyroxine Requirement in Hypothyroid Bariatric Patients

Administration and Pharmacokinetics of Levothyroxine

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