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pharmaceutics > Quiz 6 > Flashcards

Quiz 6 Flashcards

1
Q

non-target drug delivery

A

most conventional dosage form - eventually reaches the site of action by distribution and passive diffusion

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2
Q

targeted therapies

A

reach the right site at the right dose at the right time for the correct duration - pick out the cancer cells

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3
Q

how targeted therapy is different from chemotherapy

A

uses drugs, targets the cancers specific genes, proteins, or the tissue environment that contributes to cancer growth and survival. takes advantage of the difference between normal cells and cancer cells. sometimes they are used alone, but most often used in combination therapy

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4
Q

targeted therapy can work to

A

block or turn off chemical signals that trigger growth and division
change proteins inside the cancer cells
stop making new blood vessels that provide nutrition
trigger your immune system to attack cancer cells
carry toxins to the cancer cells to kill specific cells

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5
Q

targeted therapy strategies (4)

A
  1. monoclonal antibodies
  2. antibody directed enzyme prodrug therapy (ADEPT)
  3. immunotherapy (cellular immunotherapy, virotherapy/oncolytic virus therapy, MAbs)
  4. gene therapy
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6
Q

delivery carrier strategies

A
  1. vectors
  2. liposomes
  3. nanoparticles
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7
Q

monoclonal antibodies

A

the formation of a monoclonal antibody (mAb) is one of the most powerful techniques for incorporating a drug into a site-specific system- mABs are highly specific and recognize only one antigenic determinant or receptor site

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8
Q

naked mab

A

add nothing to mAB - trastuzumab - cause other tcells/bcells to get rid of what is attached - targets the extracellular domain of the HER2 protein

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9
Q

conjugated MABs

A

circulates until it finds its target antigen, once bound- releases a toxic agent. thus, less damage to normal cells

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10
Q

radiolabeled MAbs

A

goes to the side of action and kills, antibody against CD20, antigen on >20% B-cell lymphomas, target B cells if they have CD20 on their surface, non-hodgkins lymphoma, targets only what you want to kill

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11
Q

Ibritumomab tiuxetan

A

radiolabeled mAbs

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12
Q

trastuzumab

A

naked mab

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13
Q

chemolabeled MAbs ADC

A

antibody drug conjugates (ADC), mAb to CD30 attached to chemo drug MMAE, antigen on lymphocytes, hodgkin lymphoma - has a linker that is a synthetic protease-cleavable linker that covalently attaches MMAE to the CD30 directed antibody and releases the agent in the cell -MMAE binds to tubulin disrupting the microtubule network and arresting the cell cycle resulting in apoptosis of the cancer cell

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14
Q

drawbacks to chemolabeled MAbs

A
  1. off target toxicity- takes up normal cell if there is not a toxic cells (bistandard effect- once cell dies leads to kill of other cells nearby)
  2. mAb: linker needs enzymatic reaction, sometimes linker is weak and breaks out early causing cytotoxicity
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15
Q

antibody directed enzyme prodrug therapy

A

mab used to target the side, the enzyme breaks down the prodrug, works around the timor not in the tumor

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16
Q

bystander effect of ADEPT

A

capability to kill the surrounding non-dividing/non-expressing tumor cells and it amplifies the drug effect

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17
Q

good ADEPT canidates

A

small molecules with ability to diffuse inot the tumor tissue

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18
Q

targeted immunotherapy

A

non-specific immunotherapy and specific immunotherapy (cancer vaccines and virotherapy)
T-cell transfer therapy (CAR-T-Cells), immune checkpoint inhibitors (mAbs)

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19
Q

provenge

A

cancer vaccine, cellular immunotherapy

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20
Q

virotherapy

A

designed to replicate tumors (not normal tissue) and initiate an immune response to target cancer cells that have metastasized

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21
Q

CAR T-cells - cellular immunotherapy

A

engineers patients immune cells (T-cells) to treat their cancer
blood is drawn from patients and T-cells separated
viral vector gene coding for a specific antigen is inserted into the T-cells to produce receptors on their service called chimeric antigen receptors (CARs), speciic to a protein on tumor cells, Eg of antigen: Car T cell therapy furthest along in development target an antigen found on B cells called CD19

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22
Q

keytruda (pembrolizumab)

A

mAb targets PDL-1

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23
Q

gene therapy

A

fixing a defective gene in the cell by insertion of a functional gene or group of genes - gene control protein expressed, used to treat, cure or prevent disease by changing the expression of a person’s genes or providing a missing protein via delivery of the gene for that protein - effective in getting the right genes into the accurate cells

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24
Q

sucessful gene therapy requires two main components

A
  1. therapeutic gene

2. gene deliver system

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25
Q

why has gene therapy not been very successful

A

delivery vehicle to target genes to desired cells, internalized and reaches nucleus, not enough expression of the delivered gene

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26
Q

delivery carrier strategies - vectors

A

carrier- a transfection vector - delivers the therapeutic gene to a patients target cells
vectors used on viral and non-viral

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27
Q

viral vectors

A

carry a modified or foreign gene, most efficient method for gene transfer, infect target cell and transfer the therapeutic gene using their natural biological mechanism, primary requirement is that virus must be unable to replicate and have no lytic (ability to rupture a cell) activity

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28
Q

examples of viral vectors

A

retroviruses, adeno-associated virus, parvoviruses, herpesviruses, poxviruses

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29
Q

non-viral vectors- Why and what are they made of ?

A

naked DNA, because viral vectors cause toxicity, immune and inflammatory responses, gene control and tissue targeting (other approaches use liposome complexes and polymer DNA carriers)

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30
Q

liposomes

A
  • alter the pharmacokinetic profile of drugs
  • reduce off-target toxicity
  • improve the therapeutic index

usually liposomes cannot release drug without interacting with cells

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31
Q

liposome interactions occur in several ways

A
  1. endocytosis
  2. adsorption
  3. fusion
  4. lipid exchange
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32
Q

doxil

A

liposomal doxorubicin
PEGylated liposome carrier loaded with cytotoxic anticancer drug doxorubicin
diffuses across blood vessels into normal tissues and tumors, retained within the blood pool except at sites of increased vascular permeability such as the liver, spleen and tumors - half life 100x longer than free doxorubicin
cardiotoxic risk is 7x lower than free drug

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33
Q

nanoparticles

A

improve deliver, therapeutic efficacy, patient outcome
Stealth-like features : evade the immune system • Protective layers : prevent the degradation of biologics (e.g. proteins, DNA) • Targeting moieties : improve specificity and tumor accumulation • Membrane-permeation moieties : improve cell uptake • Imaging agents : assess delivery and dosing • Endosome escape mechanisms : longer half-life • Target-dependent assembly or disassembly : control drug release • Microenvironment sensors. eg: pH, proteases : trigger drug release and cellular uptake • Intracellular targeting moieties : direct drugs to specific intracellular compartments

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34
Q

each new functionality elevates

A

complexity, cost, regulatory barriers

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35
Q

tumor biomarkers

A

are antigens and help target -

1. folate receptor 2. EGFR 3. HER2

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36
Q

nuclear medicine

A

branch of medicine that utilizes radioisotopes/ radionuclides and radiation in diagnosis and treatment of disease

37
Q

radioactivity

A

radiation emitted as a result of spontaneous decay of unstable nuclei of atoms. break down/decay of unstable isotope - undergoes changes until stable state is reached - consists of alpha, beta, positron emission, gamma rays (PET< SPECT (, therapeutic (zevalin)

38
Q

decay rate vs half life of radioisotopes

A

differ in rate of decay but definite time required for half of original atoms to decay

39
Q

alpha particles

A

fast moving helium atoms - have high energy - due to their large mass they are stopped by just a few inches of air or a piece of paper

40
Q

beta

A

fast moving electrons are ejected from nuclei, since electrons are much lighter than alpha particles, they are able to penetrate further, penetrate several feet of air or several millimeters of tissue or plastic

41
Q

positrons are

A

counter parts to B particles

42
Q

gamma

A

these are photons, except much higher energy, more than x rays, energy depends on the stability of nuclei that emits them. they pass through most materials, depending on their energy, they can be stopped by a thin piece of aluminum foil or they can penetrate several inches of lead

43
Q

frequently used radionuclides/isotopes

A

Technetium -99m, indium 111, selenium 75, flourine 18, iodine 123, FDG, xenon gas

44
Q

tc-99m

A

m - metastable
used in 80% diagnostic procedures, half life 6 hours, biological half life is shorter due to rapid renal cl, shorter biological half-life will clear excess drug from the body quicker providing better images
decay: gamma emission has no beta emission which minimizes patient exposure

45
Q

technitium tc-99m

A

made in a molybdenum (Mo-99) generator, t 1/2 = 200000 years decays by beta emission

46
Q

Tc-99m sestamibi injection (cardiolite) indications

A

myocardial perfusion, breast cancer, parathyroid

47
Q

Tc-99m sestamibi injection (cardiolite) MOA

A
  • Diffuses into myocardium amount of drug taken up is proportional to amount of blood flow in tissues
  • Ischemic areas of myocardium can be visualized and occluded vessel leading to ischemic area can be determined
48
Q

Tc-99m sestamibi injection (cardiolite) administration procedure

A

Initial dose: 14-17 mCi Tc-99m sestamibi IV, Initial imaging: Begin 1 hr after initial dose administration

49
Q

Tc-99m sestamibi injection (cardiolite) stress test

A

walk on treadmill

50
Q

fluorodeoxyglucose (FDG)

A

Fluorine-18 (F-18)
Decay: positron emission
t1/2: 110 mins (very short half-life)
Produced by bombardment of O-18 with protons
Used to detect cancers or tumors that cannot be visualized with MRI

51
Q

fluorodeoxyglucose (FDG) F-18 indications

A

Cancer diagnosis – staging evaluation of
treatment response
Brain activity in seizure patients
Diagnosis of Alzheimer’s disease

52
Q

fluorodeoxyglucose (FDG) F-18 MOA

A

Structure similar to glucose attached to
positro9n emitting F18 isotope
Imaging parallel to tissue uptake of glucose
Eg: cancer cells have high metabolic
requirements, so higher levels of glucose
uptake. FDG concentrates in tumors

53
Q

fluorodeoxyglucose (FDG) F-18 admin procedure

A

Administration procedure
Initial dose: 14-16 mCi FDG I.V.
Allow patient to rest while drug distributes
Limit physical activity to reduce muscle uptake
If specifically imaging the brian, keep patient in a
dark room
Imaging begins 1 hr after dose administration

54
Q

fume hood

A 
ISO Class 5
• Laminar vertical airflow
• Sides, back, and bottom
are covered in 3⁄4” thick
lead
• Dose calibrators are lead-
lined, 2” thick
L-block is a 3/4 lead shield which provides protection while compounding
55
Q

hot cell

A

Shielded nuclear radiation containment chamber
Used to protect individuals from radioactive
isotopes by providing a safe containment box in
which they can control and manipulate the
equipment required.
Used for handling high energy radiopharmaceuticals
like FDG

56
Q

geiger meuller survey meter and pigs

A

• Pigs are used to transport
doses
• Usually made of tungsten
or lead

57
Q

compounding kits

A

Kits are sterile ingredients made for specific
radiopharmaceutical preparations
Kits include: buffers, antioxidants, ligand, and reductant
The kit is mixed with the radioactive isotope to produce the
required product
Commercially available
Preferred in this environment, since they are “closed”
systems
Preparations can be made “in-house”, if needed, but the
process is complicated

58
Q

radiation dosimetry

A 
Important devices used to measure exposure over
a certain period of time
 Types of dosimeters:
 Ring
 Badge
 Pen
59
Q

radioactive decay - first order reaction

A

N = N0e-λt
N = number of atoms remaining at elapsed time t,
N0 = number of atoms originally present
� = decay constant for time (also disintegration or transformation)
Decay constant units– reciprocal seconds, minutes, hours, etc…

Half life (t1/2) = 0.693/λ

60
Q

units for radioactivity

A

Curie (Ci)
That quantity of radioisotope in which 37 billion (3.7*1010) atoms disintegrate per second
Becquerel (Bq) – SI
1 disintegration per second, most common is multiples of this unit KBq, MBq, GBq
Doses currently expressed in both Bq as well as Ci (most common system in Cardinal
Health in nuclear pharmacy is still Ci).

61
Q

Authorized User:

A

practitioner of the healing arts who is identified as an authorized user
on a license issued by the State Board of Health that authorizes the medical use of
radioactive material, hazards, and the applicable regulations of the U.S. Nuclear
Regulatory Commission.

62
Q

Radiopharmaceutical:

A

Any substance defined as a drug which exhibits spontaneous
disintegration of unstable nuclei with the emission of nuclear particles or photons and
includes any such drug which is intended to be made radioactive.

63
Q

Radiopharmaceutical Quality Assurance:

A

the performance of appropriate chemical,
biological and physical tests on radio-pharmaceuticals, and the interpretation of the
resulting data to determine their suitability for use in humans and animals, including internal test assessment authentication of product history and the keeping of proper records.

64
Q

transdermal for PEDs

A

variable in younger children. teens are more viable because it has matured

65
Q

parenteral dosage

A

drugs admin continuously via the IV route in small children typically require a syringe pump, the dose volume in very young patient is likely to be small yet each requires that there be sufficient volume to permit admin of the correct dose per hour.

66
Q

pediatric population age

A

birth-18

67
Q

geriatric population age

A

65 and older

68
Q

pediatric absorption

A

Neutral gastric pH for first 2 weeks of life
Gastric pH slowly decreases to adult levels by 2 years of age
Neonates and infants can have variable GI motility and absorption
Infants and children have thinner, more hydrated skin
Neonates have scares musculature

69
Q

pediatric distribution

A

Infants have increased volume of distribution of water-soluble drugs
Neonates have increased BBB permeability
Infants less than 6 months old have decreased albumin

70
Q

pediatric metabolism

A

Ability to metabolize develops at varying rates

Some enzymes are not fully viable until 4 years of age

71
Q

pediatric excretion

A

Renal function is highly variable, approaching full capacity between 6 months and 3 years of age

72
Q

geriatric absorption

A

Increased gastric pH
Decreased GI motility, intestinal blood flow, and absorptive area
Thinner, less hydrated skin
Less musculature

73
Q

geriatric distribution

A

Increased volume of fat distribution for fat-soluble drugs

Decreased albumin

74
Q

geriatric metabolism

A

Decreased hepatic blood flow and metabolic capacity

75
Q

why are pediatric patients therapeutic orphans

A

Children are the population most often excluded from medication dosing guidelines as only 20% of all medications have FDA-approved pediatric indications.
FDA approval requires testing on children, which brings major ethical dilemmas with it.

76
Q

when considering dosage for a pediatric patient you need to examine

A
  1. ability of the patient to use the dosage form

2. patient acceptance of the dosage form

77
Q

solid dosage form drawback -peds

A

locks you into a specific dose - most childeren can’t swallow tablets or capsules until age 6,

78
Q

when are chewables good

A

appropriate for children eating solid food, especially if it reduces dose volume and unpleasant taste

79
Q

orally disintegrating tablets

A

useful for school-age children

80
Q

liquid dosage forms- peds

A

more freedom to individualize dose, addresses problem with inability to swallow pills

81
Q

problems with excipients in liquid dosage forms with children

A
  1. elixirs are not suitable for the smallest patients due to adverse effects
  2. ethanol: CNS depressant, confusion, GI upset
  3. propylene glycol: hypotension arrhythmia, hemolysis
82
Q

suspensions - peds

A

compounded suspensions should follow primary literature guidelines, suspensions are preferred to solutions because of masking of unpleasant taste - also challenge to patient acceptance due to texture

83
Q

how does ADEPT work

A

utilizes mAb that target cancer cells to carry a pro-drug activating enzyme, patient is given prodrug via IV infusion, when the prodrug encounters the enzyme on the mAb that are bound to the receptors on the cancer cells, the prodrug is activated to its cytotoxic form

84
Q

acetris (bentruximab vedotin)

A

chemolabeled mAb

85
Q

immune checkpoint mAb

A

Immune checkpoint mAbs target antigens on tumor cells that tell the T-cell that they are normal cells. The mAbs block the inhibition of T-cells so that they will recognize and kill the cancer cells.
Now being combined with other immunotherapies to amplify the effects.

86
Q

BSA

A

square root (((pt wt in kg)(pt ht in cm)/ 3600))

87
Q

childs dose BSA

A

(childs BSA) (adult dose) / 1.73 m2

88
Q

ideal body weight male

A

IBWm = 50 kg + 2.3 kg for each inch of height over 5 feet

89
Q

ideal body weight female

A

IBWf = 45 kg + 2.3 kg for each inch of height over 5 feet

pharmaceutics (8 decks)

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