Drug Absorption Flashcards
The effect of any given dose of drug on the Cp of that drug will depend on the ______ and _____ of drug from the site of administration to the blood.
rate (time to peak); extent (bioavailability) of transfer
When would the rectal route be chosen?
when pt is vomiting, uncon, post-surgery, GI irritation, or uncooperative
What is the bioavailability of subcutaneous administration?
very high- almost that of IV
Knowledge of _____ allows for dosage adjustments when the drug is given by different routes of administration.
drug bioavailability
What is the bioavailability of IV administration?
100%
If the inhaled particle size is < 0.5 μM, the drug is _____, leading to _____.
exhaled, no effect
The topical route is a localized application via _____ for treating local conditions.
skin or mucous membranes
A generic drug formulation is said to be bioequivalent to a brand name drug formulation if the ____ and _____ of absorption are similar to the brand name.
rate and extent
Drugs with a _____ are typically administered via IV.
narrow therapeutic index
What are the 2 most important factors to consider when choosing a route of administration?
1) bioavailability 2) relative rates of onset
What is the bioavailability of IM administration?
very high- almost that of IV
The transdermal route of administration is for ______.
systemic use
Why is the rate of absorption so fast in the inhaled route?
large surface area and blood flow in pulmonary tissue
What is the equation for F?
F = AUC (route) / AUC (IV)
How rapid is the onset of action of the oral route?
slow
Why are IV and inhaled drugs so addicting?
because their rate of action is so fast
How is the lipid solubility estimated?
oil:water partition coefficient
What is the bioavailability of the buccal/sublingual route?
high
What administration type has the second slowest time to peak?
subcutanous
The effect of any given dose of drug on the plasma concentration of that drug (Cp) will depend on the rate (time to peak) and extent (bioavailability) of transfer of drug from _______.
the site of administration to the blood
Name 2 routes for local effects.
1) inhalation (if targeting the lungs) 2) topical
In the _____ route, approximately 50% of dose will bypass the liver, thus first pass metabolism is less than for the oral route.
rectal
In the rectal route, approximately ____% of dose will bypass the liver, thus first pass metabolism is ____ than for the oral route.
50; less
What administration type has the slowest time to peak?
oral
Where is the concentration gradient created?
at the site of administration
What is the pKa of a sulfate group?
1
What is the onset speed of rectal administration?
slow
Sublingual/buccal drugs are typically _____ and _____.
lipid soluble; potent
Which route is the most hazardous?
IV
After absorption from oral mucosa, venous drainage from the mouth is to the ______, protecting the drug from rapid hepatic first-pass metabolism (faster onset of action).
superior vena cava
Because of the extremely large surface area of the intestine relative to the stomach, the rate of absorption of a drug from the intestine will be ______ than that from the stomach.
greater
After absorption from oral mucosa, venous drainage from the mouth is to the superior vena cava, protecting the drug from rapid _______ (faster onset of action).
hepatic first-pass metabolism
If the inhaled particle size is 1-5 μM, the drug is ______, leading to ______.
deposited in small airways; a therapeutic effect
How can the rate of absorption via the oral route be changed?
increase by using liquids or rapidly disintegrating tablets; decrease with enteric coated tablets or sustained release
Name 4 factors that affect drug membrane passage.
1) molecular size 2) lipid solubility 3) degree of ionization 4) concentration gradient
What is the rate of onset of the buccal/sublingual route?
within minutes