Pharmaceutical Chemistry 1 (Lecture)

RADIOPHARMACEUTICAL AND CONTRAST MEDIA – ANSWERS AND RATIONALE

1. ________ – Block pp 374

2. ________ – Remington pp 479
3. ________ – Remington pp 478
4. ________ – Gisvold’s pp 413
 As the ratio deviates significantly away from unity, atomic nuclei become ___________ and have a greater amount of
internal nuclear energy. Such unstable nuclei are ___________ and obtain stability by emitting energy in the form of
particulate and/or electromagnetic radiation that propagates through space or matter. (Gisvolds – 413)
 Two major types of isotopes are found in nature. ___________ isotopes maintain their elemental integrity, and do not
decompose to other isotopic or elemental forms. ___________ or __________ isotopes decompose or decay, by
emission of nuclear particles, into other isotopes of the same or different elements. The ___________is a characteristic
of a particular isotope and continues until a ___________ isotopic level is achieved. Since the transition from one
isotope to another involves nuclear transformation, the chemistry of radioactive isotopes differs from the chemistry of
stable isotopes by the additional aspects of nuclear reactions. Some unstable isotopes exist or pass through
___________ states. ___________ isotopes are characterized by slow rates of decay, allowing an accumulation of
the metastable form which often gives the appearance of a stable form of isotope. In reality, the metastable form is
decaying at a rate significantly slower than the parent isotope. (Block pp 375)
5. ________ – (Block pp 375)
 Not all radioactive isotopes are found naturally in elements. A large number of unstable isotopes are produced
synthetically. The production of radioactive isotopes usually involves the bombardment of atomic nuclei with high-
energy subatomic particles (neutrons or electrons) to produce _____________ nuclei of the same of different element.
6. ________ – Remington pp 479
 Radionuclides are used for medicine and pharmacy in two different ways: as (1) ____________________ or (2)
___________________.
 As SEALED READIATION SOURCES, their principal roles are in (1) therapy and (2) calibration of radiation
detection instrumentations. For THERAPY, the choice of the radionuclide for a give application is governed largely
by the properties of the radiation required for treatment; the type and energy of radiation and range in tissue are
prime considerations. For therapeutic applications, the radiations sources are either (1) EXTERNALLY BEAMED
INTO CANCEROUS TISSUES (_______________) OR (2) IMPLANTED IN THE FORM OF SEED, WIRES, OR
RIBBONS (OR OTHER PHYSICAL FORMS) WITHIN, OR IN PROXIMITY TO, CANCEROUS TISSUE FOR
SPECIFIED PERIODS OF TIME (________________). For these purposes the chemical properties or chemical form
of the radionuclide are relatively unimportant. Likewise for calibration purposes, the nature of the radiation emitted is
usually pertinent whereas the chemical properties are not.
7. ________ – Gisvold’s pp 413
 __________________ is radiation, that when interacting with matter, can cause changes in the atomic or nuclear
structure. PARTICULATE RADIATION includes ___________, ___________, ___________, and
___________particles. Particulate radiation is energy in the form of __________ with kinetic energy.
8. ________ – Gisvold’s pp 413
 Types of Ionizing radiation: (1) ___________________ and (2) ________________________.
 _______________ radiation is an electric and magnetic disturbance that is propagated through space at the speed of
light. It is unaffected by either an electrical or magnetic field because it has ______ charge. These properties are
shared by ___________, ___________, ___________, ___________, ___________, and ___________. The various
forms of electromagnetic radiation differ in their frequency and therefore, their energy. The difference between x-rays
and gamma rays is based on where they originate. ___________come from outside the nucleus via electron orbitals.
___________originate in the nucleus via nuclear transformation. X-rays and Gamma rays have properties resembling
both waves and particles and are often referred to as ___________.
9. ________ – Gisvold’s pp 413
10. ________ – Gisvold’s pp 413 (See#8)
11. ________ – Gisvold’s pp 413 (See#8)
12. ________ – Gisvold’s pp 413
 Radionuclides are ___________ nuclei that undergo processes called decay. A nucleus may undergo a single
transformation or several decays before finally reaching a stable configuration. Nuclear particles, either a proton or a
neutron, are called ___________. A species of an atom with a specified number of neutrons and protons in its nucleus
is called ___________ Nuclides with the same number of protons and a different number of neutrons are called
___________. Nuclides with the same number of neutrons and a different number of protons are called ___________.
Nuclides with same atomic mass are called ___________. Nuclides with the same number of protons and atomic mass
but at two energy levels are called ___________.
13. ________ – Shargel pp 1160
14. ________ – Shargel pp 1160
 The biological construct targets a physiological or pathological process of interest, allowing the localization of radiation
that, in turn, may be imaged or used to effect therapy. Most of these agents are used in diagnostic medical imaging;
however, they are also used in therapeutic applications, such as in the treatment of hyperthyroidism, thyroid cancer,
polycythemia vera, and in the alleviations of bone pain. (Shargel pp 1160)
 These agents may exist as a solid, liquid, gas, or pseudogas. The chemical and physical identity and form of a
radiopharmaceutical is very important because in each case, once administered, the radiopharmaceutical is intended
to target certain tissues, binding sites, and/or biochemical pathways. Depending on its specific physicochemical and
radiation properties, a radiopharmaceutical can be used for either diagnostic or therapeutic purposes, and in a few
cases for both. (Remington pp 479)
Pharmaceutical Chemistry 1 (Lecture)

 For diagnostic applications, a radiopharmaceutical should ______ be pharmacologically active. It is administered in

extremely small (tracer) quantities so that it does not alter the physiologic or pathologic process which is being
measured. The nature of the radiation emitted by a diagnostic radiopharmaceutical is important primarily for its ease of
detection. On the other hand, for the therapeutic radiopharmaceutical, the type and energy of the radiation as well as
its range in tissues are very important considerations. A radiopharmaceutical preparation designed for therapeutic
purposes must contain enough radioactivity to produce the intended tissue effects. (Remington pp 480)
15. ________ – Shargel pp 1160 (See#14)
16. ________ – Remington pp 480
 ________________ is defined as a phenomenon by which one nuclide is spontaneously transformed into another
nuclide with the emission of energy in the form of radiation. A nuclide that undergoes spontaneous nuclear reaction is
said to be radioactive. After one or more decay processes, a ___________ nucleus is formed.
17. ________ – Gisvold’s pp 414
 In a stable atom, the energy level is called the ___________ state. A unstable, high-energy nucleus or a stable
nucleus that is excited to a higher level by interaction with a high-speed particle can EMIT this EXCESS energy by
___________ to the GROUND STATE. If this decay process is delayed, the excited state may be referred to as a
METASTABLE (m) STATE. During ___________, certain particles or quantity of energy is released from the
NUCLEUS.
 ___________ are characterized by the notation (see below) where X is the symbol of the chemical element to which
the nuclide belongs, A represents the ___________ (Number of neutrons + the number
of protons), and Z represents the ___________(number of protons). The right side of
the element is reserve for the oxidation state (valence), and N represents the number of ___________. In most
medical references, various notations indicating the elements and mass number are used (e.g., I-131 or Iodine-131, or
131I)

18. ________ – See#17

19. ________ – Gisvold’s pp 414
 The nuclide at the beginning of the decay is referred to as the ___________. The nuclide produced by decay is
referred to as the ___________. Daughter nuclei may be stable or unstable. There are five types of radioactive decay
processes that are distinguished according to the nature of the primary radiation event. The type of decay that occurs
for a particular isotope generally depends on the balance of protons and neutrons in the nucleus.
20. ________ – Gisvold’s pp 414
 ______________________ (IT) is a decay process where the nucleus simply changes from a higher energy level to a
lower energy level by emitting ___________. Therefore, both _____________and _____________remain unchanged.
The daughter nucleus is the same chemical element as the original nucleus. The original nucleus, before the transition,
is said to be in a metastable (m) state. The predominant isotope used in nuclear medicine procedures, ___________,
has a half-life of 6 hrs. Tc-99m is considered a ___________ GAMMA EMITTER.
 _____________________ (EC). The nucleus captures an ___________ from the electron cloud of the atom (mainly
the K shell). This electron combines with a proton to produce a ___________. The excess energy form this
transformation can be liberated in the form of a gamma-ray and/or a ___________ (a highly energetic, chargeless
particle of extremely small mass). Therefore, ___________nuclear particles are emitted during this transformation.
 _____________________ (β+). An alternative decay process in a proton rich nucleus is the conversion of a
___________ to a ___________ with the subsequent ejection of an energetic ___________ and a ___________.
Positrons are considered ___________ and exist only for a very short periods of time. The positron loses its kinetic
energy, by interacting with surrounding atoms. The Positron ultimately combines with a free electron form one of the
surrounding atoms in an interaction in which the rest masses of both particles are converted to two gamma-rays of 511
keV emitted. This combination is called ______________ RADIATION. This characteristic decay process is utilized for
the specialized imaging technique called ____________________________ (PET).
 __________________ (β-). A neutron-rich nucleus decays by conversion of a ___________ to a ___________ with
subsequent emission of an energetic negatron and antineutrino (a highly, chargeless particle of extremely small mass)
with or without gamma-ray emission.
 _____________________ (He+2). A heavy, unstable nucleus may decay to a daughter nuclide and an ___________
particle consisting of two ___________ and two ___________, essentially the equivalent to a charged ___________
nucleus. If the particle has sufficient energy, it may escape the nucleus in an excited energy state with or without the
emission of excess energy in the form of gamma-ray.
21. ________ – See#20
22. ________ – See#20
23. ________ – Remington pp 480; Block pp 375 – 376
 __________________– which constitute alpha radiation, are compound particles consisting of TWO ___________ and
TWO ___________. It is identical with ___________ nucleus – that is, a HELIUM atom, less ___________ orbital
electrons. As an alpha particle loses energy, its velocity decreases. It then attracts electrons to its K- shell and
becomes and ordinary helium atom. The range of alpha particles in air is about 5cm; the range in tissue is less than
100um in tissue. It is by far the slowest and the heaviest of all the radioactive emissions. It has low penetrating power,
hence, useless for biological applications.
 This form of radiation is usually emitted only from element having atomic number greater than ___________. Isotopes
emitting alpha particles will decay to the element having a mass number of ___________ less and an atomic number
of ___________ less than the original isotope.
24. ________ – See#23
25. ________ – Remington pp 480
 ___________________ exists as two types because there are two kinds of electrons, the negative electron (or
___________), and the positive electron (or ___________). The positron is identical with the negatron in all aspects
Pharmaceutical Chemistry 1 (Lecture)

except for its charge of +1 instead of -1. The positron is also known as the ______________ of the electron. When
these electrons are emitted, they are called BETA PARTICLES. That is, the two particles β- and β+ are the same as e-
and e+, respectively, except for their origin. Beta particles may have the range of over 3m in air and up to about 1mm
in tissue, depending in the specific energy of the beta particles.
 Beta particles are ___________ and faster than alpha particles. Beta particles have more penetrating power than
alpha articles. The emissions of these particles DO NOT ALTER the ___________but ALTER the ___________. The
negative charge causes the beta particles to produce ionizations of molecules when they pass through various media.
 NEGATRONS are emitted when the __________________ ration exceeds stable limits leading to the transformation of
neutrons to protons with the expulsion of beta radiation.
 POSITRONS are emitted when the _________________ ratio is above stable limits causing the transformation of
protons into neutrons.
26. ________ - See #25
27. ________ – Remington pp 480; Block pp 377- 378
 ___________ PARTICLES is an electromagnetic wave. These are radiated as ___________ or QUANTA of energy.
They are often emitted as a result of ____________________, which is required when nuclei produced in nuclear
reactions are in an excited state rather than in the ground state. When excited, nucleons occupy high-energy quantum
levels. They tend to lose excess energy, returning to the ground quantum state by gamma ray emission. Gamma
radiation differs from X-rays, UV rays, visible light only in wavelength or frequencies.
 GAMMA RAYS are the _________ penetrating of all the emitted particles. Gamma-emitting radionuclides are
particularly useful for diagnostic radiopharmaceuticals.
 Gamma rays have NO ___________ and NO ___________ but they are of very high energy. They have ___________
ionizing power. NOTE: Emission of gamma rays is almost always accompanied by the emission of other forms of
radiation.