Chapter 11 Flashcards
______ can overcome some of the difficulties associated with oral administration
drug formulation
true or False: drugs normally taken as tablets or capsules
True
A ______ gelatinous envelope enclosing the active substance
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
______ 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
sustained release
a tablet is usually a compressed preparation that contains:
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
What are the 3 types of drug delivery discussed?
Approaches to prevent degradation and/or target disease
Antibody-drug conjugates
Synthetic-polymer drug conjugates
_____ is the use of prodrugs and the use of water-soluble macromolecules to aid drug reaching target
Approaches to prevent degradation and/or target disease
_____ are anti
cancer agents linked to antibodies that are stable in body but released when the antibody binds to tumour cell
Antibody-drug conjugates
____ are polyethylene glycol (PEG), polyglutamate, N-(2-hydroxypropyl)-methacrylamide (HPMA)
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
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)
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
_____ 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
liposomes
______ 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
Liposomes
______ is first in its class of drugs using nanoparticle albumin bound (nab) technology
Abraxane, protein bound paclitaxel
______ 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.
Formulation
_____ – initial concentration following IV administration
_____ – peak plasma concentration after extravascular administration
Cinitial
Cmax
______ – time to reach Cmax
____ – elimination half life
______– area under the curve
Tmax
T1/2
AUC
_______ – volume of plasma cleared of the drug per unit time
_______ – apparent volume in which a drug is distributed
______ – systemically available fraction of a drug
Clearance (CL)
Volume of distribution (Vd)
Bioavailability (f)
_____ 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 _____
ADME
Absorption/administration
Distribution
Metabolism
Excretion
_____determines the compound’s bioavailability
absorption
majority of small-molecule drug metabolism is carried out in the liver by _____
redox enzymes
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)
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)
_____ is the administration method with the fewest variables
Intravenous (IV) bolus
True or False: rate of elimination is directly proportional to Cp
True
