Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0030193 (pain)
 261,466 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

A patient with disseminated osseous metastases due to breast cancer reported multifocal pain. Because of persisting pain after a first cycle of chemotherapy, 1,295 MBq Re-186 HEDP was administered intravenously. Excellent pain relief was observed. Subsequently, the patient received further combined chemotherapy and Re-186 HEDP therapy and remained pain free. Tc-99m MDP bone imaging showed a significant regression of osseous metastases. It may be speculated that the combination of Re-186 HEDP and chemotherapy results in significantly increased palliation of metastatic bone disease.
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PMID:Remission of bone metastases after combined chemotherapy and radionuclide therapy with Re-186 HEDP. 971 80

99mTc-HEDP is widely used as a bone imaging agent and its Re analog [186Re]Re-HEDP is now well established as a therapeutic radiopharmaceutical for palliation of pain due to bone metastases. In the present paper, we report the work carried out for the preparation of stable 186Re-HEDP which retains RC purity up to 5 days when stored at 4 degrees C. 186Re was prepared by irradiation of natural Re metal at a flux of 3 x 10(13) neutrons/cm2/s for seven days and processed after a cooling period of four days. The specific activity of 186Re formed was approximately 35 mCi/mg. A complex with RC purity > 98% could be prepared by varying the reaction conditions. By carefully optimizing the reaction and storage conditions, a complex which was stable for over 4 days could be synthesized. Bio-distribution studies carried out in rats revealed approximately 30% bone uptake of 186Re-HEDP at 3 h postinjection which remained almost constant for 48 h, at which time there was negligible activity in other organs.
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PMID:Preparation, stability studies and pharmacological behavior of [186Re]Re-HEDP. 1037 21

Rhenium-186 (tin)-labeled hydroxyethylidene diphosphonate (186Re-labeled HEDP) was evaluated in 27 men with progressive androgen-independent prostate cancer and bone metastases. Administered activities ranged from 1251 to 4336 MBq (33.8-117.2 mCi). The primary objectives were to assess tumor targeting, normal organ dosimetry, and safety. Antitumor effects were assessed by posttherapy changes in prostate-specific antigen and, when present, palliation of pain. Whole-body kinetics, blood and kidney clearance, skeletal dose, marrow dose, and urinary excretion of the isotope were assessed. Targeting of skeletal disease was observed over the period of quantification (4-168 h). Radiation doses to whole body, bladder, and kidney were well tolerated. The dose-limiting toxicity was myelosuppression (grade III) at 4107 MBq (111 mCi) and grade II at 296 MBq (80 mCi). Probe clearance (whole body) and urinary excretion measurements were highly correlated. Of the six patients treated at the highest dosage schedules (three at 1510 MBq/m2 and three at 1665 MBq/m2), three showed a posttherapy decline in prostate-specific antigen of 50% or more. The declines were not sustained. The determination of total activity retained at 24 h, as well as an estimate of marrow dose, correlated with the amount of myelosuppression observed. These results suggest that a single 24-h measurement of retained activity would allow individualized dosing and an improved therapeutic index relative to fixed dosing schema. Repetitive dosing is required to increase palliation.
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PMID:Rhenium-186-labeled hydroxyethylidene diphosphonate dosimetry and dosing guidelines for the palliation of skeletal metastases from androgen-independent prostate cancer. 1038 13

A 78-year-old patient with prostate cancer and osseous metastases had a pain symptomatic. In the Urology he was treated with antiandrogenes. The outcome of the bone scintigraphy showed a super bone scan with normalization after antiandrogene-therapy which seemed to be a sign of remission, before he showed a progressive form with multiple osseous metastases. Pain could not be treated with non steroidal antiphlogistics and opiates, so the indication for treatment with Rhenium-186-HEDP was given in this case.
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PMID:[Bone scintigraphy and rhenium radioisotope management in the course of metastatic prostatic cancer]. 1059 71

We evaluated the effectiveness of Re-186-HEDP in 25 patients with painful metastatic bone disease. Twenty-five patients with known prostatic (n = 19), non-small-cell lung cancer (n = 1) and breast cancer (n = 5) and multiple confirmed skeletal metastases were studied. All were taking analgesics daily (nonsteroidal antiinflammatory drugs/opiates). Re-186-HEDP (mean 35.2 mCi) was administered and patients were monitored for at least 50 days. In five patients, a repeat dose was administered 9 to 10 weeks later. The evaluation of the analgesic effect was based on a "pain diary" and by recording the use of analgesics. In 80% (20 of 25) of the patients, the effect was significant palliation, moderate in 3 patients (12%), and insignificant in 2 (8%). No significant myelotoxicity was observed. Transient pain flare was recorded in 8 of 25 patients. These results indicate that Re-186-HEDP can offer pain palliation in patients with painful bone metastases without being complicated by significant myelotoxicity.
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PMID:Preliminary results of the use of Re-186-HEDP for palliation of pain in patients with metastatic bone disease. 1068 86

Pain palliation with bone-seeking radiopharmaceuticals is an effective and cost-effective management tool in patients with advanced cancer metastatic to bone. Strontium-89 ((89)Sr) (Metastron) and samarium-153 ((153)Sm) EDTMP (Lexidronam) are licensed for use in patients in the United States. Patients with a positive bone scan using technetium 99m methylene diphosphonate ((99m)Tc MDP) are eligible for treatment, and indications and contraindications for use are now well defined. The evidence in the literature now suggests that the radiopharmaceuticals can significantly reduce pain and analgesic requirements, can improve quality of life, can reduce lifetime radiotherapy requirements and management costs, and may slow the progression of painful metastatic lesions. Retreatment is safe and effective. Rhenium-186 ((186)Re) HEDP and Tin-117m diethylenetriaminepenta-acetic acid (DTPA) are in phase II/III trials to evaluate efficacy and compare efficacy with the licensed agents. Phosphorus-32 ((32)P) has been reassessed in two trials evaluating efficacy in comparison with (89)Sr and safety. Toxicity is reversible myelosuppression, which may be significant, and the treatments should not be given to patients with suspected disseminated intravascular coagulation.
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PMID:Use of radionuclides for the palliation of bone metastases. 1072 99

Rhenium-188 hydroxyethylidene diphosphonate (Re-188 HEDP) is a new radiopharmaceutical for treatment of metastatic bone pain. Re-188 is a generator-produced radionuclide emitting high energy beta and gamma rays and having a relative short physical half-life makes it of especially interesting for therapeutic purpose. Seven patients (pts) with multiple painful bone metastases were treated with Re-188 HEDP. Five pts with prostate cancer and 2 pts with breast cancer received a fixed activity of 3000 MBq of Re-188 HEDP intravenously in two steps. Complete blood counts were determined, blood chemistry examinations and urine-analysis were performed before and 1, 2, 3, 4, 6, 8, 12 weeks following the treatment. A visual analogue score, a verbal rating scale, the Spitzer index and the Karnofsky score were used to assess pain and performance status. Three hours after Re-188 HEDP administration at 1 m from the anterior mid-trunk of the pts gamma and at the patient body surface beta-radiation dose measurements were made, together with urine radioactivity measurements. Three pts become pain-free, 2 pts exhibited partial pain improvement and 1 patient gave no response to the Re-188 HEDP therapy. In 1 patient due to central nervous system metastasis the modification of the pain intensity could not be evaluated. Three pts displayed a flare reaction within 1 week after the treatment. Transient decreases in platelet and white blood cell counts were observed. There were no significant changes in the liver and renal functions. Radiation dose rate values of 6.3 +/- 1.0 microSv/h for gamma, and of 183 +/- 40 s-1 for beta-radiation were found. 25-32% of the administered dose was eliminated via the urinary tract in the first three hours. The preliminary data suggests that Re-188 HEDP is an effective radiopharmaceutical in treatment for metastatic bone pain. An administered activity of 3000 MBq can bring about a pain reduction without causing any clinically significant bone marrow toxicity.
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PMID:[Clinical experience with rhenium-188 HEDP therapy for metastatic bone pain]. 1084 24

To compare the effects of sodium fluoride and etidronate in severe postmenopausal osteoporosis, we conducted a 3 year, prospective, trial in 118 postmenopausal osteoporotic women with at least one vertebral fracture, who were randomly assigned to receive sodium fluoride (25 mg twice daily, as enteric-coated tablets) plus calcium (1000 mg/day) or intermittent etidronate (400 mg/day for 14 days) followed by calcium (1000 mg/day for 76 days). Lateral spine X-ray films and dual-energy X-ray absorptiometry (DXA) measurements of the lumbar spine and proximal femur were performed at enrollment and yearly. Nonvertebral fractures were recorded every 6 months. Thirty-one women in the fluoride group and 47 in the etidronate group completed the trial. At 36 months, the mean change from baseline of the lumbar bone density in the fluoride group was 8.5 +/- 2.04% (p = 0.001) and in the etidronate group was of 3.6 +/- 0. 84% (p < 0.001). The changes in the fluoride group were significantly higher than in the etidronate group (p = 0.01). Both groups showed nonsignificant changes in femoral neck bone density. There was no significant difference between groups in the cumulative proportion of women with new vertebral fractures, with an incidence in the fluoride group of 16% vs. 17% in the etidronate group. However, the number of new vertebral fractures was significantly lower in the fluoride group (6 fractures) than in the etidronate group (19 fractures) (p = 0.05). The number of patients with nonvertebral fractures was similar in both groups. A high incidence of side effects, mainly gastrointestinal symptoms and lower extremity pain syndrome, was observed in the fluoride group. Etidronate was well tolerated. We conclude that, in women with severe osteoporosis, although sodium fluoride is more favorable than cyclical etidronate for increasing lumbar bone mass, no differences were observed in the incidence of fractures.
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PMID:Cyclical etidronate versus sodium fluoride in established postmenopausal osteoporosis: a randomized 3 year trial. 1086 19

A 59-year-old man with prostate cancer and pain from multiple bone metastases was treated with 1,424 MBq (38.5 mCi) rhenium-186 hydroxyethylidene diphosphonate (Re-186 HEDP). In addition, he had nonsteroidal antiandrogen, progestagen, and an analog-luteinizing hormone. Neither chemotherapy nor external-beam radiotherapy was administered. Bisphosponate therapy was stopped 4 weeks before the administration of Re-186 HEDP. The Tc-99m HMDP whole-body scan obtained 6 weeks after therapy showed the same results as before therapy. However, 1 year after therapy, a significant reduction of the mass of the metastases was visible on bone scan. The bone scan index decreased from 34 before therapy to 10 after 1 year. The patient described significant pain relief and stopped his analgesic intake 3 weeks after therapy.
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PMID:Significant reduction of the mass of bone metastasis 1 year after rhenium-186 HEDP pain palliation therapy. 1107 88

Etidronate and medronate have been labelled with technetium-99m (99mTc-HEDP, 99mTc-MDP) for bone scanning and, with rhenium-188 (188Re-HEDP) to palliate the pain resulting from bone metastases. The objective of this study was to label alendronate, ABP, a new bisphosphonate, with SnF2-reduced-188Re. The reagents for the 5 mg ABP kit were SnF2, KReO4 and gentisic acid at acid pH. The chemical, spectroscopic and microscopic characteristics, quality control, rat bone uptake of [188Re]Re-ABP and similarities with 99mTc-ABP are presented. We conclude that this is a promising new radiopharmaceutical for bone metastases pain palliation.
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PMID:Labelling of Re-ABP with 188Re for bone pain palliation. 1121 78


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