Radiopharmaceuticals

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Susan F. Slovin - One of the best experts on this subject based on the ideXlab platform.

  • Metabolism and pharmacokinetics of radium-223 in prostate cancer.
    Expert Opinion on Drug Metabolism & Toxicology, 2015
    Co-Authors: Oladapo Yeku, Susan F. Slovin
    Abstract:

    Introduction: Prostate cancer metastatic to bone is a cause of significant morbidity and mortality. Bone pain and other skeletal events negatively impact the quality of life in patients who might otherwise be functioning well. As such, there has been intense interest in the development of strategies and pharmaceuticals to address this problem.Areas covered: The authors reviewed the current literature for articles relevant to metastatic prostate cancer, clinical Radiopharmaceuticals, castrate-resistant prostate cancer and development of Radium-223. The authors have referenced primary literature, clinical trials and relevant review articles that summarize the history, development and current utilization of Radiopharmaceuticals for management of bone metastases from prostate cancer.Expert opinion: Radium-223 is the first radiopharmaceutical with an overall survival benefit approved for the treatment of patients with castration-resistant prostate cancer, symptomatic bone metastasis and no known visceral metas...

Charles B. Sampson - One of the best experts on this subject based on the ideXlab platform.

  • Adverse Reactions and Drug Interactions with Radiopharmaceuticals
    Drug Safety, 1993
    Co-Authors: Charles B. Sampson
    Abstract:

    Adverse reactions to Radiopharmaceuticals are comparatively few in number. Various estimates quote an incident rate of 1 to 6 reactions per 100 000 injections. Other figures quoted are 1 in 800 for the bone-seeking radiopharmaceutical methylene diphosphonate, and 1 in 400 for the lung visualisation agent macroaggregated albumin. The very low numbers of reported adverse effects probably reflect the tiny amounts of material which are used in the formulation of Radiopharmaceuticals. Adverse reactions to Radiopharmaceuticals are usually mild and transient and require little or no medical treatment. A few reactions involve respiratory or circulatory collapse or loss of consciousness. Several fatalities have been reported with the liver scanning agent ^99mTc (technetium 99m)-albumin colloid. Clinical manifestations may be categorised under the headings of vasomotor effects i.e. faintness, pallor, diaphoresis or hypotension, and anaphylactoid effects such as nausea, dermographism, wheezing, bronchospasm, erythema and pruritus. The most prominent group of Radiopharmaceuticals that have been reported to produce adverse events are the diphosphonates, which are used for scanning the skeleton. Typical diphosphonate reactions include erythema (especially over the extremities), nausea, vomiting and malaise. The onset of reaction is usually 2 to 3 hours after injection. The second group of Radiopharmaceuticals which give rise to adverse events are the colloids, which are used for liver and spleen scintigraphy. Typical colloid reactions include pallor, nausea, flush and pulse changes. Adverse events may also occur as a result of the patient’s medication interfering with the disposition of the radiopharmaceutical. Although not usually hazardous or dangerous, such events may be so pronounced that a marked deviation in the expected pharmacokinetics may occur. Drug interactions can be conveniently categorised under the headings of unusual handling of the radiopharmaceutical because of pharmacological action, genuine in vivo interaction between the medication and radiopharmaceutical, drug-induced disease and interaction between the radiopharmaceutical and catheters or syringes. The most serious drug interactions are those where the patient is taking cortisone or cytotoxic agents prior to tumour scintigraphy. Other important effects occur in patients undergoing bone scanning who are receiving iron preparations. Nifedipine has been reported to produce quite severe problems in scanning, including difficulties in the radiolabelling of red cells (for cardiac scintigraphy), and other effects where the drug appears to prevent the transport of bone-seeking materials into the skeleton. Many drugs alter hormonal status and these effects may produce marked deviations from the expected biodistribution. Diethylstilbestrol (stilboestrol), digitalis, gonadotrophins, phenothiazines and cimetidine all increase estrogen levels in high doses. In such instances gynaecomastia can occur, and it has been found that there is increased localisation of the cardiac imaging agent ^99mTc-pyrophosphate and the tumour localisation agent ^67Ga (gallium 67)-citrate in gynaecomastic breasts. Many therapeutic drugs can cause or aggravate disease, and the disease itself may produce an unexpected biodistribution of radiopharmaceutical. An example is liver toxicity as a result of ingestion of large amounts of paracetamol (acetaminophen), aspirin, cytotoxic drugs, tetracycline and halothane. Liver disease would show up on the scintigram as a ‘cold’ area. For both adverse reactions and drug interactions there is, at present, considerable underreporting. It is essential to report all adverse events, no matter how trivial, in order to make a proper assessment of the size of the problem and to improve diagnostic accuracy.

  • Adverse reactions and drug interactions with Radiopharmaceuticals.
    Drug safety, 1993
    Co-Authors: Charles B. Sampson
    Abstract:

    Adverse reactions to Radiopharmaceuticals are comparatively few in number. Various estimates quote an incident rate of 1 to 6 reactions per 100 000 injections. Other figures quoted are 1 in 800 for the bone-seeking radiopharmaceutical methylene diphosphonate, and 1 in 400 for the lung visualisation agent macroaggregated albumin. The very low numbers of reported adverse effects probably reflect the tiny amounts of material which are used in the formulation of Radiopharmaceuticals.

Seyed Jalal Hosseinimehr - One of the best experts on this subject based on the ideXlab platform.

  • Fundamental concepts of Radiopharmaceuticals quality controls
    Pharmaceutical and Biomedical Research, 2019
    Co-Authors: Sajjad Molavipordanjani, Seyed Jalal Hosseinimehr
    Abstract:

    Quality control (QC) procedures should always be performed following radiopharmaceutical preparation and prior to patient administration. The main aim of QC is to ensure optimal radiopharmaceutical product properties except for some short half-life tracers such as some positron emission tomography (PET) imaging probs. by dispensing a radiopharmaceutical of the highest quality the risk of having to repeat a nuclear medicine study due to poorly performing Radiopharmaceuticals will be reduced. The existence of radiochemical impurity or impurities in radiopharmaceutical cause unnecessary radiation burden to the patient or undesirable high background without adding to the diagnostic information or improving treatment. Therefore, Radiopharmaceuticals quality control is crucial and involves two different aspects including pharmaceutical parameters (such as sterility, bacterial endotoxins/ pyrogens, bioaffinity and biodistribution studies) and radioactive parameters (such as radionuclide and radiochemical purity) and chemical impurity which will be focused on here.

  • Basic and practical concepts of radiopharmaceutical purification methods.
    Drug Discovery Today, 2018
    Co-Authors: Sajjad Molavipordanjani, Vladimir Tolmachev, Seyed Jalal Hosseinimehr
    Abstract:

    : The presence of radiochemical impurities in a radiopharmaceutical contributes to an unnecessary radiation burden for the patients or to an undesirable high radioactivity background, which reduces the imaging contrast or therapeutic efficacy. Therefore, if the radiolabeling process results in unsatisfactory radiochemical purity, a purification step is unavoidable. A successful purification process requires a profound knowledge about the Radiopharmaceuticals of interest ranging from structural features to susceptibility to different conditions. Most radiopharmaceutical purification methods are based on solid-phase extraction (SPE), high-performance liquid chromatography (HPLC), size exclusion chromatography (SEC), ion-exchange chromatography (IEC), and liquid-liquid extraction (LLE). Here, we discuss the basic and applied concepts of these purifications methods as well as their advantages and limitations.

Oladapo Yeku - One of the best experts on this subject based on the ideXlab platform.

  • Metabolism and pharmacokinetics of radium-223 in prostate cancer.
    Expert Opinion on Drug Metabolism & Toxicology, 2015
    Co-Authors: Oladapo Yeku, Susan F. Slovin
    Abstract:

    Introduction: Prostate cancer metastatic to bone is a cause of significant morbidity and mortality. Bone pain and other skeletal events negatively impact the quality of life in patients who might otherwise be functioning well. As such, there has been intense interest in the development of strategies and pharmaceuticals to address this problem.Areas covered: The authors reviewed the current literature for articles relevant to metastatic prostate cancer, clinical Radiopharmaceuticals, castrate-resistant prostate cancer and development of Radium-223. The authors have referenced primary literature, clinical trials and relevant review articles that summarize the history, development and current utilization of Radiopharmaceuticals for management of bone metastases from prostate cancer.Expert opinion: Radium-223 is the first radiopharmaceutical with an overall survival benefit approved for the treatment of patients with castration-resistant prostate cancer, symptomatic bone metastasis and no known visceral metas...

Manish Dixit - One of the best experts on this subject based on the ideXlab platform.