3 Phases Of Drug When Drug Taken By Mouth Like Tablet Or Capsule:
PHARMACEUTIC PHASE
PHARMACOKINETIC PHASE
PHARMACODYNAMIC PHASE
is the first phase of drug action
pharmaceutic phase
____ and ____ are used in drug preparation to allow the drug to take on a particular size and shape and to enhance drug dissolution.
Excipient fillers and inert substances
is the breakdown of a tablet into smaller particles
Disintegration
is the dissolving of the smaller particles in the GI fluid before absorption
Dissolution
What are the two pharmaceutic phases?
Disintegration and Dissolution
Drugs in ____ form are more rapidly available for GI absorption
liquid
drugs are both disintegrated and absorbed faster in acidic fluids with a pH of
1 or 2
drug absorption is generally ____ for those drugs absorbed primarily in the stomach
slower
resist disintegration in the gastric acid of the stomach
Enteric-coated drugs
_____ and _____ should not be crushed
Enteric-coated tablets or capsules and sustained-release (beaded) capsules
True or False: Food in the GI tract may interfere with the dissolution of certain drugs.
TRUE
What are the 4 processes of pharmacokinetic?
Absorption
Distribution
Metabolism/Biotransformation
Excretion/Elimination
the movement of drug particles from the GI tract to body fluids by passive absorption, active absorption, or pinocytosis
Absorption
What are the mechanisms of absorption?
Passive absorption
Active absorption
Pinocytosis
Type of mechanism of absorption: occurs mostly by diffusion (movement
from higher concentration to lower concentration)
Passive absorption
Type of mechanism of absorption: requires a carrier such as an enzyme or protein to move the drug against a concentration gradient. Energy is required for active absorption.
Active absorption
Type of mechanism of absorption:
is a process by which cells carry a drug across their membrane by engulfing the drug particles
Pinocytosis
Factors Affecting Drug Absorption
pH partitioning absorption
blood flow
surface area
lipid solubility
The process in which the drug passes to the liver first
first-pass effect, or hepatic first pass
It is the percentage of the administered drug dose that reaches the systemic circulation.
Bioavailability
The percentage of bioavailability for the oral route is?
always less than 100%
The percentage of bioavailability for the IV route is?
100%
Oral drugs that have a high first-pass hepatic metabolism may have a bioavailability of?
only 20% to 40%
Factors that alter bioavailability include:
drug form
route of administration
GI mucosa and motility
food and other drugs
changes in liver metabolism caused by liver dysfunction or inadequate hepatic blood flow
increases the bioavailability of the drug and can cause an increase in drug concentration
rapid absorption
can limit the bioavailability of the drug, thus causing a decrease in drug serum concentration
Slow absorption
is the process by which the drug becomes available to body fluids and body tissues
Distribution
Drug distribution is influenced by:
1. blood flow
2. the drug’s affinity to the tissue
3. the protein-binding effect
Volume of drug distribution (Vd) is dependent on ___ and its _____
drug dose and its concentration in the body
As drugs are distributed in the plasma, many are bound to varying degrees (percentages) with protein (primarily albumin)
Protein-binding effect
The portion of the drug that is bound is ___
inactive
the portion of the drug that remains unbound is ___.
free or active drug
Only ___ drugs (drugs not bound to protein) are active and can
cause a pharmacologic response.
free
As the free drug in the circulation decreases, more bound drug is
released from the protein to ____
to maintain the balance of free drug
True or False:
Abscesses, exudates, body glands, and tumors does not hinder drug distribution
FALSE
Abscesses, exudates, body glands, and tumors hinder drug distribution
is a semipermeable membrane in the central nervous system (CNS) that protects the brain from foreign substances
blood-brain barrier (BBB)
True or False:
Highly lipid-soluble drugs are able to cross the blood-brain barrier
True
True or False:
Drugs that are not bound to proteins and are not lipid soluble are able to cross the BBB
False
Drugs that are not bound to proteins and are not lipid soluble
are not able to cross the BBB
True or False:
During pregnancy, both lipid-soluble and lipid-insoluble drugs are able
to cross the placental barrier.