NCMA 216: PRELIM Flashcards
In PHARMACOKINETIC PHASE, when drug is taken by mouth, it undergoes 3 phases. What are these phases?
- Pharmaceutical/dissolution
- Pharmacokinetics
- Pharmacodynamics
In PHARMACEUTIC PHASE, _________ is the breakdown into smaller parts
Disintegration
In PHARMACEUTIC PHASE, ________ is the further breakdown into smaller parts in GIT-absorption; dissolve into liquid
Dissolution
PHARMACEUTIC PHASE
TABLET → DISINTEGRATION →
DISSOLUTION
the 1st phase of drug action.
DISSOLUTION
___________ is the time it takes the drug to disintegrate and dissolve to become available for the body to absorb it
Rate of dissolution
are not 100% drug.
Tablets
- excipients
Eillers and inert substances
Allow drugs to take on particular size and shape and to enhance drug dissolution.
EXCIPIENTS
Tablet Excipients Formula
Tablet Excipients = Tablets - Drug substance(s)
are the acidity of the stomach
Gastric ph
Normal gastric pH
1.5-3.5
Young/elderly acidity ph
above 3.5
liquids more absorbed than solid, already in solution, rapidly available for GI absorption
Form of drug ( LIQUID VS. SOLID) -
resist disintegration in gastric acid
Enteric coated drugs
Disintegration occurs only in
alkaline environment (intestine)
interfere with dissolution & absorption, enhance absorption of other drugs, may be protectants of gastric mucosa
Presence of food
Process of drug movement throughout the body that is necessary to achieve drug
action.
PHARMACOKINETICS
A drug taken orally is dissolved in the _________ and absorbed in the _________
STOMACH, SMALL INTESTINE
Passive diffusion across cell membrane
By ____________ through
the spaces between cells
By ___________ of small drug
containing membrane vesicles
through cells, or by the action of drug transporter proteins
Paracellular Transport
Endocytosis
4 Process
● Absorption
● Distribution
● Metabolism: biotransformation
● Excretion: elimination
Physiological factors controlling the rate and reliability of drug absorption:
Blood flow to absorbing
site
Total surface area for
absorption
Time of arrival and
contact time at
absorption site
Physico-chemical factors controlling the rate and reliability of drug absorption:
solubility
Chemical stability
Lipid to water partition
coefficient
Degree of ionization
Movement of drug particles from GIT to body fluids involve 3 processes:
- Passive transport
- Pinocytosis
- Active Transport
drugs move across the cell membrane from an area of higher concentration to one of lower concentration.
Diffusion
passive transport - requires a carrier such as enzyme or protein to move the drug against a concentration gradient. This
does not require energy.
Facilitated diffusion
is the process by which cells carry a
drug across their membrane by
engulfing the drug particles in a
vesicle.
Pinocytosis
requires energy to facilitate the
transport of drug molecules against a concentration gradient, which usually occurs at specific sites in the small intestine
Active Transport
process by which drug becomes available to body fluids and tissues.
and is the movement of the drug from the circulation to body tissues.
DISTRIBUTION
Factors affecting drug distribution
● Size of the organ
● Blood flow
● Solubility
or biotransformation is the process by which the body chemically changes drugs into a form that can be excreted
DRUG METABOLISM
Drug given orally may be metabolized by the liver before they reach the systemic
circulation
FIRST PASS METABOLISM