21. RADIO PHARMACEUTICALS

Introduction to Radio Pharmaceuticals

Radio pharmaceuticals are special pharmaceutical preparations that contain radioactive isotopes. They can be in the form of solutions, capsules, or injections and are primarily used for diagnostic imaging and therapeutic purposes.

In India, most radio-pharmaceuticals are developed and supplied by the Bhabha Atomic Research Centre (BARC), Mumbai, to approved hospitals and laboratories. Each preparation is named according to its radioactive component, for example, sodium-radio-iodide injection or sodium-iodide I-131 capsules. BARC produces more than 40 different radioactive preparations, kits, and generators.


Important Radio-Pharmaceutical Preparations

ProductRadionuclideShelf LifeHalf-LifeApplication
Ammonium bromide injectionBr-8236 hrs36 hrsMeasurement of extracellular water
Calcium chloride solutionCa-45180 days160 daysStudy of calcium metabolism
Chromic chloride injectionCr-5190 days27.7 daysProtein loss and absorption studies
Colloidal gold injectionAu-19865 hrs56 hrsTreatment of cancer and RES studies
Cyanocobalamin preparationCo-57 / Co-5860 / 270 days71 daysDiagnosis of pernicious anemia
Ferric chloride solutionFe-59120 days44.6 daysStudy of iron metabolism
Indium chlorideIn-113m / Sn-1138 hrs / 99.5 minDiagnosis of placental and cardiac diseases
Potassium chloride injectionK-4212.5 hrs12.5 hrsPotassium exchange studies
Rubidium chloride injectionRb-8645 days18.6 daysDetermination of myocardial blood flow
Sodium chloride injectionNa-2415 hrs15 hrsSodium exchange studies
Sodium iodide capsulesI-13130 days8.06 daysThyroid function study
Sodium orthophosphate solutionP-3230 days14.3 daysTreatment of polycythemia
Sodium sulphate solutionS-35180 days87.4 daysExtracellular fluid volume measurement
Sodium pertechnetateTc-99m24 hrs6.02 hrsVarious diagnostic applications

Designing Radio Pharmaceuticals

The design of radio-pharmaceuticals focuses on choosing compounds that selectively accumulate in target organs or tissues. The goal is to ensure that adding the radioactive isotope does not alter the chemical or biological behavior of the molecule.

Similar to Structure-Activity Relationship (SAR) in drug development, the Structure-Distribution Relationship (SDR) helps predict how the compound will distribute in the body. The main objective is to optimize delivery to the target site before testing in animals or humans.


Technetium-99m (Tc-99m) Radio Pharmaceuticals

Technetium-99m (Tc-99m) is the most widely used radionuclide in diagnostic medicine, present in about 75% of all radio-pharmaceuticals. It has excellent imaging characteristics:

  • Half-life of 6 hours (ideal for short diagnostic procedures)
  • Emits a 140 keV gamma photon suitable for imaging
  • Forms stable complexes with various ligands due to flexible chemistry

Tc-99m compounds are used to study organs such as the heart, brain, lungs, liver, kidneys, and bones.


Sodium Iodide I-131 (Solution and Capsules)

Form: Clear, colorless solution (pH 7.5–9.0) for oral or IV administration. Capsules are made by evaporating the radioactive solution onto inert fillers.

Uses:

  • Diagnosis of thyroid structure and function
  • Treatment of thyroid cancer, hyperthyroidism, and hypothyroidism
  • Evaluation of thyroid-related cardiac conditions

Half-life: 8.08 days

It is prepared with minimal impurities and carefully processed for stability and safety.


Safe Storage and Handling of Radioactive Materials

  • Store radioactive materials in restricted, shielded areas using lead or thick glass.
  • Monitor radiation levels regularly in both storage and working areas.
  • Use protective equipment such as gloves, tongs, and lab coats.
  • Follow national safety regulations for handling, disposal, and personnel monitoring.
  • Avoid eating, drinking, or smoking in handling areas.
  • Waste should be stored securely until radiation decays to safe levels.

Pharmaceutical Applications of Radioactive Substances

Radioactive isotopes have been used in medicine since the early 20th century. Radium was the first radionuclide used medically (1901–1946). Today, more than 50 radionuclides are available for diagnosis, therapy, and calibration.

In diagnostics, radio-pharmaceuticals act as tracers — pharmacologically inactive compounds that help image specific organs or biological processes. Therapeutic isotopes, on the other hand, deliver controlled doses of radiation to treat diseases such as cancer.

Common Applications Include:

  • Gold-198: Used for treating malignant effusions and carcinomas.
  • Cobalt-57 / 58: Used in vitamin B12 labeling for diagnosing anemia.
  • Sodium Iodide I-131: Used for thyroid disorder diagnosis and treatment.
  • Ferric Citrate: Used in hematological studies.
  • Calcium Isotopes: Used for studying bone metabolism.
  • Strontium-90: Used for superficial carcinoma treatment.
  • Deuterium and Tritium: Used to measure total body water content.

In addition, strong gamma radiation sources like Cobalt-60 and Cesium-137 are used for sterilizing pharmaceutical products and surgical instruments.

Detailed Notes:

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