Chapter 11

Question 1

______ can overcome some of the difficulties associated with oral administration

Answer 1

drug formulation

Question 2

true or False: drugs normally taken as tablets or capsules

Answer 2

True

Question 3

A ______ gelatinous envelope enclosing the active substance

Answer 3

capsule

capsules can be designed to remain intact for some hours after ingestion in order to delay absorption

may also contain a mixture of slow- and fast-release particles to produce rapid and sustained absorption in the same dose

Question 4

______ tablets are are designed with an osmotically active core, surrounded by an impermeable membrane with a pore in it allowing the drug to percolate out from the tablet at a constant rate as the tablet moves through the digestive tract

Answer 4

sustained release

Question 5

a tablet is usually a compressed preparation that contains:

Answer 5

5-10% of the drug (active substance); 80% of fillers, disintegrants, lubricants, glidants and binders; 10% of compounds which ensure easy disintegration, disaggregation and dissolution of the tablet in the stomach or the intestine

Question 6

What are the 3 types of drug delivery discussed?

Answer 6

Approaches to prevent degradation and/or target disease

Antibody-drug conjugates

Synthetic-polymer drug conjugates

Question 7

_____ is the use of prodrugs and the use of water-soluble macromolecules to aid drug reaching target

Answer 7

Approaches to prevent degradation and/or target disease

Question 8

_____ are anti

cancer agents linked to antibodies that are stable in body but released when the antibody binds to tumour cell

Answer 8

Antibody-drug conjugates

Question 9

____ are polyethylene glycol (PEG), polyglutamate, N-(2-hydroxypropyl)-methacrylamide (HPMA)

Answer 9

Synthetic-polymer drug conjugates

Pegaptanib consists of an oligonucleotide drug linked to PEG and is used to treat neovascular (wet) age-related macular degeneration (AMD) in the eye

Question 10

Ionic interactions between the drug and the _____ result in folding and assembly of the protein polymer to form a protein–drug complex, which results in the drug being released at a slow and constant rate (protein is then degraded)

Answer 10

protein-based polymer

., the cationic drugs Leu-enkephalin (an endogenous opioid peptide neurotransmitter) or naltrexone (which reverses the effects of opioids and is used primarily in the management of alcohol dependence and opioid dependence) could be delivered using proteins with anionic carboxylate groups

Question 11

_____ are a physical method of protecting drugs from metabolic enzymes in the bloodstream and allowing a steady slow release of the drug is to encapsulate the drug within small vesicles

Answer 11

liposomes

Question 12

______ can be surface functionalized to endow stealth through PEGylation and to promote receptor-mediated endocytosis by using targeting ligands such as antibodies, peptides, proteins, carbohydrates, and various other small molecules

Answer 12

Liposomes

Question 13

______ is first in its class of drugs using nanoparticle albumin bound (nab) technology

Answer 13

Abraxane, protein bound paclitaxel

Question 14

______ refers to the method by which drugs are prepared for administration, whether by solution, pill, capsule, liposome or microsphere. Suitable formulations can protect drugs from particular pharmacokinetic problems.

Answer 14

Formulation

Question 15

_____ – initial concentration following IV administration

_____ – peak plasma concentration after extravascular administration

Answer 15

Cinitial

Cmax

Question 16

______ – time to reach Cmax

____ – elimination half life

______– area under the curve

Answer 16

Tmax

T1/2

AUC

Question 17

_______ – volume of plasma cleared of the drug per unit time

_______ – apparent volume in which a drug is distributed

______ – systemically available fraction of a drug

Answer 17

Clearance (CL)

Volume of distribution (Vd)

Bioavailability (f)

Question 18

_____ is a compound must usually enter into the bloodstream before being taken up by the target cells

_____ is a compound needs to reach its effector site, most often via the bloodstream, and then distribute into muscle and organs

_____ is a compounds begin to break down when they enter the body

_____ is a compounds and their metabolites need to be removed from the body via _____

Answer 18

ADME

Absorption/administration
Distribution
Metabolism
Excretion

Question 19

_____determines the compound’s bioavailability

Answer 19

absorption

Question 20

majority of small-molecule drug metabolism is carried out in the liver by _____

Answer 20

redox enzymes

Question 21

What are the three main sites where drug excretion occurs
kidney is the most important site, products are excreted as urine
biliary excretion initiates in the liver and the products pass through the gut and are excreted eventually as faeces
excretion through the lungs (e.g., anaesthetic gases)

Answer 21

kidney is the most important site, products are excreted as urine

biliary excretion initiates in the liver and the products pass through the gut and are excreted eventually as faeces

excretion through the lungs (e.g., anaesthetic gases)

Question 22

_____ is the administration method with the fewest variables

Answer 22

Intravenous (IV) bolus

Question 23

True or False: rate of elimination is directly proportional to Cp

Answer 23

True