Effect of a Short-Term Oral Administration of Cimetidine and Ranitidine on the Basal and Thyrotropin-Releasing Hormone-Stimulated Serum Concentrations of Prolactin, Thyrotropin and Thyroid Hormones in Healthy Volunteers

Perret, G; Hugues, Jean‐Noël; Louchahi, M; Varoquaux, O; Modigliani, E

doi:10.1159/000138157

Cited by 15 publications

(8 citation statements)

References 17 publications

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“…There is also evidence that histamine may play a role in the regulation of hepatic metabolism of thyroid hormone (6). There is a slight but significant decrease in radioiodine uptake by the liver at 1 d after 131 I administration in both famotidine-(1.67-fold decrease) and promethazine-(1.41-fold decrease) treated rats.…”

Section: Discussionmentioning

confidence: 98%

“…Whole blood, which is an indicator of whole-body burden of radioiodine and an indirect indicator of bone marrow exposure, was also assayed. Radioiodine uptake by the liver was also measured because of data that support that hepatic metabolism of thyroid hormone may be regulated by H2 receptors (6). Although the bladder wall also receives a relatively high dose of exposure (from urinary excretion), urine activity was not assayed because of the volatile nature of 131 I in the urine and difficulty with an accurate collection in small rodents.…”

Section: Discussionmentioning

confidence: 99%

“…Histamine receptor levels in the brain may be sensitive to thyroid function in both the developing and the adult brain (5). H2 receptors may mediate thyroid-releasing hormoneinduced increases in thyroxine excretion and may regulate hepatic metabolism of thyroid hormone (6). Conversely, H2 blockers can decrease secretion of thyroid-stimulating hormone possibly through a pituitary effect (7).…”

mentioning

confidence: 99%

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Histamine Receptor 1 and 2 Antagonists Alter Biodistribution of Radioiodine

Edwards

Yakish

Wang

et al. 2015

J. Nucl. Med. Technol.

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Nuclear medicine technology assumes responsibility for examinationspecific patient preparation procedures. This requires a clear understanding of the possible effects of medications on the outcome of examinations. There is evidence that common over-the-counter drugs, histamine 1 (H1) and histamine 2 (H2) receptor blockers and proton pump inhibitors, may directly or indirectly affect thyroid function. The objective was to determine whether short-term use of these drugs alters biodistribution of radioiodine in a rat model. Methods: Rats received no drug (controls) or daily subcutaneous injections of H1 blocker (promethazine), H2 blocker (famotidine), or proton pump inhibitor (esomeprazole) commencing 1 d before a single intraperitoneal injection of 0.037 MBq (1 μCi) of 131 I (NaI) and continuing daily until euthanasia at either 1 d or 8 d after 131 I. Organ uptake of 131 I by control and drug-treated rats was compared by γ-well counting. Results: Promethazine significantly increased uptake of 131 I by the thyroid (drug-treated-to-control ratios) both at 1 d (1.32) and 8 d (1.52) after 131 I. Both famotidine and promethazine (respectively) significantly increased salivary gland uptake of 131 I (drug-treated-to-control ratios) at 1 d (1.37, 1.40) and 8 d (4.52, 5.57) after 131 I. Promethazine significantly increased gastric 131 I uptake (drug-treated-to-control ratios) at 1 d (1.47) and 8 d (1.46) after 131 I. Famotidine and promethazine (respectively) significantly decreased uptake of 131 I by the liver (drug-treated-to-control ratios) at 1 d (0.60, 0.71) after 131 I but resulted in a marked increase over control levels (11.21, 9.28) at 8 d. Blood levels of 131 I were not altered by drug treatment. Esomeprazole did not affect radioiodine distribution. Conclusion: H1 and H2 blockers alter the biodistribution of radioiodine in the rat. Although the findings remain to be confirmed in humans, these drugs could increase radiation exposure to nontarget tissues, particularly the stomach and salivary tissue, during 131 I therapy and consideration should be given toward avoiding the elective use of these drugs during radioiodine therapy.

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Section: Discussionmentioning

confidence: 98%

Section: Discussionmentioning

confidence: 99%

mentioning

confidence: 99%

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Histamine Receptor 1 and 2 Antagonists Alter Biodistribution of Radioiodine

Edwards

Yakish

Wang

et al. 2015

J. Nucl. Med. Technol.

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“…Before and after treatment a TRH test was performed as previously described (Perret et al, 1986). The treatments lasted 1 wk.…”

Section: Methodsmentioning

confidence: 99%

Effect of Nifedipine on Thyrotropin, Prolactin, and Thyroid Hormone Release in Man: A Placebo‐controlled Study

Valensi

Perret

Vassy

et al. 1989

Fundamemntal Clinical Pharma

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Nifedipine (10 mg tid) or placebo was administered in a randomized double-blind trial for 1 wk to 2 groups of 10 mildly hypertensive euthyroid patients. Hormonal concentrations (thyrotropin [TSH], prolactin [PRL], thyroxin, triiodothyronine, and reverse triiodothyronine) before and during a TRH test were assessed in the 2 groups before (D0) and after (D7) each treatment. Parameters of the TRH test were determined (peak values, area under the curve [AUC], release [Kr], and elimination [Ke] rate constants) and their D7:D0 ratios were compared in the 2 groups. The TSH (peak values and Kr) and PRL (peak values and AUC) responses to TRH were significantly decreased in the nifedipine group compared to the placebo group. Neither basal nor TRH-stimulated thyroid hormone levels were modified. These results confirm experimental data but seem to be clinically irrelevant.

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“…1989;Pasquali et al 1981;Perret et al 1986); a possible influence on thyroxine (T4) has been put forward (Pasquali et al 1981;Perret et al 1986). No clinical adverse effects on thyroid function have been reported to date.…”

Section: Other Endocrine Effectsmentioning

confidence: 99%

Side Effects of Ranitidine

et al. 1991

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Ranitidine was first marketed in 1981; since then many patients have been treated such that much experience has been accumulated on the safety of this histamine H2-receptor antagonist in the treatment of gastroduodenal disease. A wide array of ranitidine-associated side effects has been described, but infrequently. As so much information is now available, the aim of this review is to assess the weight of evidence for a causal link between ranitidine and the reported side effects. Overall, ranitidine is well tolerated. The incidence of general side effects at less than 2% is very similar to placebo. Headaches, tiredness, dizziness and mild gastrointestinal disturbance (e.g. diarrhoea, constipation and nausea) are among the most frequent complaints, but have very seldom resulted in stopping treatment. Cardiovascular side effects are extremely rare and unpredictable with the usual doses of oral ranitidine (at most 1 in 1 million patients). They mostly comprise sinusal bradycardia and atrioventricular blockade, especially after rapid intravenous administration, receding after cessation of the drug. Clinical studies, however, have not shown a significant pharmacological effect of ranitidine on the cardiovascular system via H2-receptors, even though individual sensitivities cannot be ruled out in a few isolated reports. Ranitidine is unlikely to be directly hepatotoxic: a transient change in liver function tests has been noted in only 1 in 100 to 1 in 1000 patients. Several cases of mixed hepatitis have been reported, but very few were fully documented. The incidence of ranitidine-associated acute hepatitis has been estimated to be less than 1 in 100,000 patients. Neuropsychiatric complications may be less common and clinically quite similar to those reported with cimetidine, i.e. confusion, disorientation, hallucinations, delirium. These side effects have occurred especially in critically ill and multiple-therapy patients, or patients with chronic renal or hepatic failure, so that the direct causal link with ranitidine treatment was often difficult to ascertain. Even though an H2-receptor-mediated effect is an attractive hypothesis (since similar complications were noted with other H2-receptor antagonists), other mechanisms have been suggested to play a role, e.g. cholinergic or histaminic effects. The overall incidence of neuropsychiatric complications is probably markedly less than 1%. White cell injury (i.e. agranulocytosis) appears to be the most frequent haematological complication, even though case reports are very few and poorly documented.(ABSTRACT TRUNCATED AT 400 WORDS)

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Effect of a Short-Term Oral Administration of Cimetidine and Ranitidine on the Basal and Thyrotropin-Releasing Hormone-Stimulated Serum Concentrations of Prolactin, Thyrotropin and Thyroid Hormones in Healthy Volunteers

Cited by 15 publications

References 17 publications

Histamine Receptor 1 and 2 Antagonists Alter Biodistribution of Radioiodine

Histamine Receptor 1 and 2 Antagonists Alter Biodistribution of Radioiodine

Effect of Nifedipine on Thyrotropin, Prolactin, and Thyroid Hormone Release in Man: A Placebo‐controlled Study

Side Effects of Ranitidine

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