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PubMed1980

Ipodate and 8-anilino-1-naphthalene sulfonic acid block receptor binding of T3 in rat liver.

We have determined that 8-anilino-1-naphthalene sulfonic acid (ANS) and ipodate are effective inhibitor in vitro of 125I-T3 binding to rat hepatic nuclei receptors. Both of these agents are estimated to have a Kd for the T3 receptor of about 1--2 x 10(-4) M. Indirect preliminary studies suggest that ANS is a non-competitive inhibitor and ipodate is a competitive inhibitor of T3 binding. Compounds such as tyropanoate and diatrizoate and iodide had no effect on T3 receptor binding. Further in vivo studies with ipodate suggested that T3 receptor binding inhibition also occurred when ipodate was given intravenously to rats.

Anilino Naphthalenesulfonates↗
PubMed1989

Comparison of the effects of amiodarone and ipodate on the rat heart.

Chronic treatment of rats with amiodarone has been shown to produce hypothyroid-like effects such as a reduction in body and heart weight and increased synthesis of the low ATPase V3-cardiac isomyosin (Bagchi, Brown, Schneider and Banerjee 1987). In this report, we have tested the hypothesis that amiodarone causes these effects through the inhibition of intracellular production of triiodothyronine (T3) from thyroxine (T4) by comparing the effects of amiodarone with those of ipodate, a potent inhibitor of T4 to T3 conversion. Separate groups of rats were given dietary ipodate and amiodarone respectively for six weeks. Both agents increased serum T4 and T4/T3 ratios, a finding consistent with the inhibition of peripheral T4 to T3 conversion. However, ipodate failed to produce hypothyroid-like effects on body weight, heart weight and isomyosin transitions similar to those found in the amiodarone group. These data indicate that the hypothyroid-like effects of amiodarone on the rat heart are not due to the inhibition of intracellular generation of T3 from T4.

Amiodarone↗
PubMed1995

Use of sodium ipodate in management of hyperthyroidism in subacute thyroiditis.

Five hyperthyroid patients (two men and three women) with typical features of subacute thyroiditis were treated with sodium ipodate (Oragrafin; 0.5 g, orally daily or every other day) for 15-60 days; the treatment was stopped when both serum T4 and T3 levels were normal. All patients studied demonstrated a prompt normalization of serum T3, improvement in clinical symptoms of hyperthyroidism, and/or weight gain. We observed no side-effects of treatment with sodium ipodate. Our data suggest that sodium ipodate is a safe and effective agent for management of hyperthyroidism in subacute thyroiditis.

Adult↗
PubMed1984

Propylthiouracil, ipodate, dexamethasone and periods of fasting induce different variations in serum rT3 in dogs.

Fasting or administration of propylthiouracil (PTU), ipodate, or dexamethasone are all known to induce a pattern of low serum triiodothyronine (T3) concentrations and high serum reverse T3 (rT3) concentrations in humans. In the present study it was found that this is not a universal phenomenon. In normal dogs exposed to fasting or these various pharmacologic agents, the serum T3 level was always depressed as in humans. However, different variations in serum rT3 levels were observed. Fasting and PTU administration were accompanied by slight decreases in the serum rT3 concentration. A single dose of ipodate did not alter serum rT3 levels, but serum thyroxine (T4) levels increased by more than 50%. Dexamethasone induced a considerable increase in serum rT3 levels, while serum T4 levels were unaltered. The results suggest that the high serum rT3 level nearly always seen in "the low T3 syndrome" in humans is merely a coincidental character of the human species, and that it has little importance for in vivo homeostasis.

Animals↗
PubMed1980

Fractionated dose cholecystography: a comparison between iopanoic acid and sodium ipodate.

Two randomised groups of 100 subjects each, undergoing oral cholecystography, were given either a 6 g fractionated dose of iopanoic acid (Telepaque) or sodium ipodate (Biloptin) to determine the relative merits of this dose schedule. Exclusions to the study were pregnancy and iodine sensitivity. Calculi or abnormal gallbladder opacification were present in 45% of subjects. Both agents were equally effective in demonstrating abnormalities, although bile duct visualisation was better using iopanoic acid (P less than 0.05). Of 46 subjects with abnormal cholecystograms subsequently undergoing surgery, all had the diagnosis confirmed. Side effects occurred in 63% of all subjects, being twice as common in those taking iopanoic acid (P less than 0.01). Sodium ipodate in a large fractionated dose is favoured because of the lower occurrence of side effects without loss of diagnostic accuracy.

Cholecystography↗
PubMed1985

Comparative effects of sodium ipodate and iodide on serum thyroid hormone concentrations in patients with Graves' disease.

Patients with thyrotoxic Graves' disease were treated daily for 10 d with 1 g sodium ipodate, an iodine rich X-ray contrast agent which impairs outer ring (5'-) deiodination of T4 to T3, or with 12 drops of a saturated solution of potassium iodide (SSKI). T4, T3 and reverse T3 (rT3) concentrations were measured before, during, and 5 and 10 d after the administration of each drug. SSKI therapy induced a decrease in the serum T4 concentration from 14.7 +/- 1.3 microgram/dl (mean +/- SE) to a nadir of 7.9 +/- 0.9 on days 9 and 10 of therapy, all values reaching the normal range by day 9; a decrease in the serum T3 concentration from 402 +/- 43 ng/dl to a nadir of 143 +/- 20 on day 10, remaining elevated in all patients until day 5 and decreasing into the normal range in all except one patient on days 9 and 10; and no change in the serum rT3 concentration. Serum T4 and T3 concentrations returned to baseline values 10 d after withdrawal of SSKI. In contrast sodium ipodate therapy induced only a modest decrease in the serum T4 concentration from 15.1 +/- 0.7 micrograms/dl to a nadir on day 9 of 11.3 +/- 1.0 and serum T4 remained above the normal range in most patients until day 8; a striking and rapid decrease (within 12 h) in ther serum T3 concentration from 340 +/- 36 ng/dl to mean values ranging from 79 to 85 during the last 5 d of therapy, with most values below the normal range during the last 3 d; and a marked increase in the serum rT3 concentration from 111 +/- 15 ng/dl to a peak value of 376 +/- 59 on day 5.(ABSTRACT TRUNCATED AT 250 WORDS)

Adult↗
PubMed1978

Changes in circulating iodothyronines in euthyroid and hyperthyroid subjects given ipodate (Oragrafin), an agent for oral cholecystography.

A dose (3 g) of sodium ipodate used routinely in oral cholecystography caused a fall in serum 3,5,3'-triiodothyronine and a rise in serum 3,3',5'-triiodothyronine in three patients taking thyroxine (T4), four euthyroid subjects,and four hyperthyroid patients. Serum T4 fell in patients with hperthyroidism, whereas it rose in the other two groups. Sodium ipodate appears to alter peripheral T4 metabolism and, in addition, produces thyroid-inhibiting effects in hyperthyroidism.

Graves Disease↗
PubMed1980

The reliability of cholecystography with calcium ipodate augmentation.

Sixty-one patients who underwent augmentation cholecystography with calcium ipodate (Oragrafin calcium granules) were reviewed. Sixty-four per cent (39/61) of nonvisualizing or poorly visualizing cholecystograms were converted to well-visualizing studies, of which 26 per cent (10/39) involved cholethiasis. In 55 per cent of the cholecystograms (12/22) that remained nonvisualizing or poorly visualizing, patients were found to have gallstones. The remaining cases of poor or nonvisualizing cholecytograms were associated with abnormal liver function, cholecystitis, and pancreatitis. If the gallbladder is nonvisualized with a calcium ipodate augmentation technique it is reliable evidence of gallbladder disease, and is likely cholelithiasis when extrinsic factors affecting contrast absorption or liver function are excluded.

Cholecystography↗
PubMed1991

Therapy of Graves' disease with sodium ipodate is associated with a high recurrence rate of hyperthyroidism.

To evaluate the long-term efficacy of sodium ipodate (IPO) in the treatment of hyperthyroid Graves' disease, we studied 12 consecutive patients with Graves' hyperthyroidism treated only with 500 mg IPO po daily for several weeks to 22 months. Serum thyroid hormone concentrations markedly decreased and serum free T3 values normalized in all patients within 7 days of therapy. Five patients (42%, Group 1) were euthyroid after 6 weeks of IPO treatment and remained so until IPO was discontinued after 22 months. Recurrence of hyperthyroidism after drug withdrawal occurred in only one of these Group 1 patients, who was promptly responsive to a second course of IPO. In contrast, seven of 12 patients (58%, Group 2) relapsed with recurrent hyperthyroidism between 14 and 42 days of IPO therapy. After IPO was withdrawn, these Group 2 patients were treated with methimazole (20-30 mg/day, initial dose), but the therapeutic response was poor and delayed. Two patients were still hyperthyroid after 6 months of methimazole treatment. Elevated serum FT3 concentrations were observed in the Group 2 patients at 21 days following the early normalization of serum FT3 concentrations. No changes in serum thyroglobulin and thyroid microsomal and TSH-receptor autoantibody titers were observed in either groups during IPO therapy. In conclusion, the results of the present study demonstrate that IPO rapidly restores euthyroidism, but its prolonged administration is associated with a high rate of relapse of hyperthyroidism and a poor response to subsequent methimazole treatment and that long-term IPO administration does not affect humoral markers of thyroid autoimmunity.

Adolescent↗
PubMedDate not supplied

Sodium ipodate increases triiodothyronine action in vivo.

Sodium ipodate (IPO) has been shown to bind nuclear T3 receptors (NT3R) in vitro, but previous studies have conflicted in regard to demonstration of this interaction in vivo. We sought evidence for IPO-NT3R binding in vivo by giving large doses of IPO to thyroidectomized (TDX) rats replaced with low doses of T3. We predicted that IPO-NT3R binding would inhibit T3 induced increases in mitochondrial alpha glycerophosphate dehydrogenase activity (alpha-GPDH) in kidney, heart and liver. Three groups of ten euthyroid rats each received 13 daily injections of vehicle, or 6 or 12 mg/100 g body weight of IPO, respectively. Both doses of IPO resulted in decreases in serum T3 and increases in serum TSH. Liver and kidney alpha-GPDH, however, were decreased only in the group receiving 6 mg IPO. In addition, three groups of 30 TDX rats were implanted with osmotic minipumps that contained T3 in the following concentrations: 33, 69 and 96 ng/ul. Ten rats in each group received 13 daily injections of vehicle, or IPO (vide supra). The alpha-GPDH responses were complex in that there was significant interaction between T3 and IPO effects in the kidney (AxB F ratio 5.13, p less than 0.001) and liver (AxB F ratio 2.85, p less than 0.05). The major finding, however, was that alpha-GPDH was not significantly reduced by IPO in any T3 replaced group. Rather, in all three organs, alpha GPDH was significantly increased above that produced by T3 alone by at least one combination of IPO and T3. Changes in serum TSH also suggested that IPO could enhance T3 effects. We conclude that IPO-NT3R binding is not a prominent mechanism via which the drug attenuates T3 effects in vivo. The data suggest that IPO may enhance T3 effects at the cellular level and that this enhancement may not be reflected by routinely monitored serum TSH. The latter observation may have clinical importance.

Analysis of Variance↗
PubMed1978

Comparative study of iocetamic acid and calcium ipodate in the visualisation of the gallbladder and common bile duct.

Iocetamic acid (Cholebrin) and calcium ipodate (Solubiloptin) were randomly allocated to two groups of 50 patients. Each patient completed a detailed questionnaire for side effects. There was no significant difference between the contrast media in their ability to opacify the gallbladder. Cholebrin was superior to Solubiloptin in opacifying the common bile duct in the presence of abnormal liver function, but there was no difference when liver function was normal. Palpitations were significantly higher with Solubiloptin (P = 0.01) but the incidences of other side effects showed no significant differences. Unabsorbed contrast residues were noted in similar frequency with both media. A high incidence of chronic cholecystitis was found in patients with non-opacified gallbladders and in those with gallstones.

Arrhythmias, Cardiac↗
PubMed1997

Sodium ipodate (oragrafin) in the preoperative preparation of Graves' hyperthyroidism.

Fourteen Graves' hyperthyroid patients who had been prepared for surgery with sodium ipodate (SI) 500 mg orally twice daily for 3 days were retrospectively studied. SI was administered in combination with propylthiouracil (10 cases) and beta blockers (all cases), which had been previously initiated. Free serum thyroxine (T4) and total triiodothyronine (T3) concentrations were measured before and after SI therapy on the morning of surgery. SI treatment significantly reduced total T3 concentration from 445.9 to 193.4 ng/dL (P < 0.0001) and free T4 concentration from 3.874 to 2.800 ng/dL (P = 0.0003). Preoperatively, only one patient had persistent tachycardia, and intraoperatively this same patient required beta blockers. Blood loss was unremarkable or reduced (average blood loss, 121 mL). On clinical examination glands were firm with normal or somewhat decreased vascularity. On histologic study all glands demonstrated changes consistent with treated Graves' disease. Preoperative treatment with SI appears to be a safe and efficacious method of preparing hyperthyroid patients for surgery.

Adrenergic beta-Antagonists↗
PubMed1983

Effect of the combination of dexamethasone and sodium ipodate on serum thyroid hormones in Graves' disease.

To investigate the effect of the combination of dexamethasone (Dex) and sodium ipodate (SI) on hyperthyroidism, we studied 24 patients with typical Graves' disease, divided into four groups of six persons each. Three groups (Study I) were studied acutely (24 h) to determine the effects of Dex (5 mg every 12 h intramuscularly), SI (one oral dose of 3 g) and both drugs at the same doses, upon T4, T3, and rT3 at 0900 h before therapy was started and 24 h later. The group on Dex and that on SI had a similar T3 decrement of 25.9 +/- 4.0% and 35.8 +/- 5.0%, respectively, (P less than 0.05), whereas the effect of both drugs combined was greater (64.2 +/- 3.6%; P less than 0.01, Dex, and P less than 0.01, SI, respectively). The increment of rT3 was markedly greater in those patients on SI than in those on Dex (561.3 +/- 149.2% and 58.9 +/- 11%, respectively, P less than 0.025). A fourth group (Study II) was studied for seven days while receiving both Dex (1 mg orally three times per day) and SI (500 mg orally three times per day). Both T4 (from 18.8 +/- 1.1 to 13.1 +/- 1.1 micrograms/dl, P less than 0.02) and T3 (from 593 +/- 41 to 136.3 +/- 12.7 ng/dl, P less than 0.001) decreased at day 8. The initial brisk increment of rT3 at 24 h (808 +/- 149%, P less than 0.005) then diminished concomitantly with the fall of its precursor, T4.(ABSTRACT TRUNCATED AT 250 WORDS)

Adolescent↗
PubMed1989

Sodium ipodate in the preparation of Graves' hyperthyroid patients for thyroidectomy.

Sodium ipodate (SI) is an oral cholecystographic agent that also affects thyroid hormone metabolism. It inhibits the peripheral T4 to T3 conversion and the thyroidal hormone release. We investigated the safety and efficacy of SI (500 mg daily during 5 days) in the preparation for subtotal thyroidectomy of 7 Graves' hyperthyroid patients in whom treatment with thionamides was unsuccessful due to allergy or noncompliance. Plasma T3 levels (mean +/- SD) decreased from 4.90 +/- 1.80 nmol/l on day 0 to 1.70 +/- 0.30 nmol/l on day 4 of treatment. Thyroidectomy performed on day 5 of treatment was uneventful. In comparison with 14 Graves' hyperthyroid patients who underwent thyroidectomy during the same period after conventional preparation with thionamides and potassium iodide, the therapeutic outcome 1 year postoperatively was similar in both groups. However, in the mildly hypothyroid patients prepared with SI, the plasma thyroid-stimulating hormone level was transiently higher 3 and 6 months postoperatively. It is concluded (1) that SI is a safe and efficacious drug in the preparation of Graves' hyperthyroid patients for thyroidectomy; (2) the therapeutic outcome 12 months postoperatively is similar in SI and in conventionally prepared Graves' hyperthyroid patients, and (3) postoperative mild or subclinical hypothyroidism is more pronounced in SI than in conventionally prepared patients.

Adult↗
PubMed1979

Clinical comparison of locetamic acid (cholebrine) and ipodate sodium (Orgrafin).

Locetamic acid (Cholebrine) and ipodate sodium (Oragrafin) were compared in a double blind study of 503 patients. The radiographs were evaluated for contrast density, visualization of common duct, gallstones, residual in the intestinal tract, and side effects. Cholebrine demonstrated better opacification, fewer repeat examinations, slightly greater common duct opacification, and more frequent visualization of gallstones. Oragrafin had less residue. Side effects were minimal with both contrast agents.

Administration, Oral↗