Thursday, February 19, 2009

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somatostatin analogs



111-In Octreotide


the somatostatin neuro is a small cyclic peptide present in neurons and endocrine cells particularly in the brain, in peripheral neurons in the endocrine pancreas and gastrointestinal tract. The native somatostatin has a half-life very short (1-3 min.) And have therefore been developed with a therapeutic purpose, its synthetic analogues:

  • L ' Octreotide acetate is available corresponds to one of the similar molecule 111In-[DTPA Dphe ] Octreotide ( Octreoscan ). This molecule binds specifically to somatostatin receptors particular affinity with the subtypes 2 and 5.
I somatostatin receptors have been identified in numerous source neuro endocrine cells and their presence with varying degrees of density has also been documented in some non-neuronal cells and endocrine . For these reasons could be visualized by octreotide scintigraphy tumors that originate from cell lines expressing receptors for somatostatin . The main indication for the execution of a 111In-[DTPA Dphe ] is represented by neuro endocrine tumors that show a high density of somatostatin receptors and can be easily viewed by scintigraphy. The examination is indicated for the location of the primary tumor and metastases may be present to diagnose recurrent disease or its progression, to monitor the effect of surgery, radiation, or of chemotherapy to predict response to therapy as a prognostic factor for selecting patients for radioiodine therapy with an analogue of somatostatin labeled a beta-emitting radionuclide such as' Yttrium -90.

Since the density of somatostatin receptors in neuroendocrine tumors is highly variable, the sensitivity of the technique in different isoptipi is very diverse. It may also be reduced if concomitant therapy with octreotide acetate. in the case of neuroendocrine tumor scintigraphy with 111In-[DTPA Dphe ] octreotide not a question of choice except in determining the concentration of somatostatin receptors present in the tissue. The molecule of 111In-[DTPA Dphe ] octreotide is rapidly cleared from the circulation, and in fact only 10 min . after administration, only 35% of is injected into the circulation, a figure that at 20 min . down to '1%. Elimination is mainly via the kidneys with approximately 50% of injected activity was recovered in urine after 6 hours and 85% after 24 hours of injection. Elimination is through the hepatobiliary system. Somatostatin receptors are expressed in many cells of different organs that appear normal during a 111In-[DTPA Dphe ] octreotide :

  • liver, spleen, pituitary, thyroid and kidney
Even after adrenal stimulation can be viewed dimly. Other organs appear at different times as a result of the process of elimination of tracer:

  • gallbladder intestinno , renal pelvis, ureter and bladder.

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Radiopharmaceuticals and perfusion of "cellularity"



99mTc-Sestamibi
---> (esakìs-2-methoxy-isobutyl isonitrile)
99mTc-tetrofosmin ---> (6,9-bis (ethoxyethyl) - 3)

lipophilic cationic radiopharmaceuticals are capable of creating complex with technetium in reduced state. As the 201Tl hano a predominantly intracellular distribution. LEDU chemical characteristics of these molecules are alal basis of the mechanism of accumulation at the cellular level:

The
  • lipopfilicità that helps overcome
  • the cell membrane that allows the positive polarity of the molecule inside the cell phone intreppolamento through transmembrane electronegative potential, the more electronegative potential of mitochondria within the cytoplasm compared to explain the preferential accumulation of 99mTc-Sestamibi and 99mTc-tetrofosmin in the mitochondria.
areas of accumulation of these molecules depends on the regional blood flow, the intensity of the ATP-dependent metabolism and the degree of cellularity. the normal distribution of 99mTc-Sestamibi and 99mTc-tetrofosmin is at the level of the glands, thyroid, myocardium , liver, gallbladder, small intestine, colon, kidney, bladder, choroid plexus, skeletal muscle.

Tuesday, February 17, 2009

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Radiopharmaceuticals II and perfusion of "cellularity"

Thallium 201 chloride (201Tl)

The 201 Tl, radioactive isotope of thallium (Tl 81, atomic weight 204) per decade electron capture by issuing three types of X-rays with half-life of 73 hours and is a cation with chemical properties similar to those of k +. In fact, such as K +, has a predominantly intracellular distribution and its transport within the cytoplasm requires the presence of cell membrane integrity. The mechanisms of intracellular transport are different, some of which are probably not yet clear:
  • pump sodium-potassium ATP dependent
  • system cotransport of potassium / sodium / chloride
  • transport through the channels Ca + + dependent
for these reasons, the 201Tl, tends to accumulate in tissues with high cellularity and cell viability, E 'is negligible in the hyperaccumulator load of necrotic tissue and low level of inflammatory and connective tissue. Other factors which positively affect the accumulation of 201Tl in a tissue is blood flow (its distribution in the context of a body is directly proportional to regional blood flow), the increased vascular permeability and cell membrane.
The heart, liver, spleen, muscles, thyroid, salivary glands and kidneys are normal sites of accumulation of 201Tl. The 201Tl is currently being used since the 70s to study myocardial perfusion in the assessment of ischemic heart disease. With regard to its use in cancer early studies have been performed for the differential diagnosis of thyroid nodules. Later it was used in the diagnosis of various cancers, including those of the parathyroid glands and brain. The disadvantages of 201Tl
reside primarily in the physical characteristics of this radionuclide:
  • long half-life involving high dosimetry and the consequent need to use the amount of dose contained causing a signal with low photon flux.
  • 72Kev the low energy emission is due to a low resolution image

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Radiopharmaceuticals for the study of the skeleton

study Skeleton

since 1972 have been introduced phosphates and diphosphates Perla Studio 's bone imaging. Phosphate compounds (pyrophosphate, metilendifosfonato, idrossimetilendifosfonato), 99mTc-labeled radiopharmaceuticals are the most commonly used today to perform a scintigraphic study of the skeleton. The uptake of these radiopharmaceuticals by bone by bone occurs through mechanisms not yet fully understood. Through an initial chemo-absorbed on the surface of crystals of calcium idrossipatite newly formed. The deposition then essentially reflects the extent of osteoblastic phenomena, in fact, skeletal scintigraphy is a young person growing sites show net uptake in physiological bone growth. A skeletal maturation occurred in the scintigraphic images stand out on the basis of a diffuse and homogeneous uptake linked to the normal replacement mineral that constantly affects the whole skeleton, the mineral districts with the most intense parts. Thanks to rapid renal excretion, phosphates have a high ratio bone tissue / soft 2-3 hours after injection. 50-60% of the injected dose is localized to bone, and the remainder is excreted by the kidneys. The uptake of phosphate by bone is related to a high number of factors, contingency plans are important blood supply and the extent of bone tournover. Essential condition for the radiopharmaceutical to settle on a certain segment of bone is, in fact, that this bone segment receives an adequate blood supply. In fact, in cases of vascular necrosis, such as the femoral head, the scan here shows a lack of uptake in the early stages after the occurrence of disease (1-2 weeks). Only belatedly, started the phenomena of reparative bone remodeling, the edesima area previously "cold" shows uptake of rafiofarmaco. On the contrary phenomena are iperafflusso blood scintigraphically marked with an increased uptake of radiopharmaceutical.

Monday, February 9, 2009

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Quality Control Calibrator Dose II




CRC-35R "Radioisotopes dose calibrator Owner's manual" - Capintec Inc.




Press TEST to enter the menu and choose the procedure DAILY to begin the test day. This procedure consists of the following controls:

    Size
  1. Fund - Background
  2. Test System - System Test
  3. Test Accuracy - Accuracy test
  4. Test Constance - Constancy Test

1. Size of the Fund - Background

  • This procedure determines the value of the environmental fund that is automatically subtracted for each measurement. It 'so important during the implementation of the measure there are no radioactive corgenti in the cockpit or in the vicinity.
  • Press BEGIN and await the outcome of the measure Please Wait
  • if at the end of the measure shows:
  • OK : take notadel value of the fund and prepare the F3 key
  • HIGH : nnotadel take the fund's value and repeat the measurement by pressing a button
  • TOO HIGH: press F3
  • Pay attention to the presence of radioactive sources in the vicinity and repeat the measurement. Where the value of the fund does not fall within normal range, notify the Health Physics


2. TEST SYSTEM - System test

  • E 'important that during the implementation of the measure there are no radioactive sources in or near the cockpit.
  • Press BEGIN and await the outcome of the measure PLEASE WAIT
  • Record the voltage measured: VOLTS: V
  • of its deviation from the nominal value: DEVIATION:%
  • and the outcome of the test: OK - FAIL
  • Prepare the ENTER key



3. TEST ACCURACY - Accuracy test

    Lower in the cockpit
  • the low-activity source calibration (133Ba content in shielding BLACK and serial number: s8107015 or other) and press F4
  • Record the value of assets measured ACCURACY mCi
  • its rated deviation: DEVIATION%
  • press the button to save the current data F3
If the message appeared ERROR write down the message and notify the Health Physics.



4. TEST CONSISTENCY - Constancy Test

  • Lower in the cockpit of the calibration source 133Ba and press F4
  • Record the value of assets measured CONSTANCY: mCi
  • Of his departure from value DEVIATION:%
  • Press SAVE or F3 to save the current data
  • Press DONE or F1 to exit test
  • Press F1 key to end the controls
  • Select Radionuclide measurement used in the ordinary course