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1.12 Principles of Pharmacology
By Dr. Backes
37
Pharmacology
Professional
01/12/2012

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Cards

Term
What are the mechanisms of drug transport?
Definition
passive diffusion, filtration/bulk flow, carrier-mediated transport, endocytosis, (ion-pair transport)
Term
What is bulk flow?
Definition
the mechanism for transfer of drugs across capillary membranes
Term
What is kp?
Definition
[] in oil/ [] in water
Term
What is the pka?
Definition
pH at which the product equals the reactant
Term
How is a drug ultimately unbound to its receptor in receptor mediated endocytosis?
Definition
acidification of the vesicle from 7 to 5
Term
Name examples of parenteral administration.
Definition
IV, IM, subq, inhalation, through skin
Term
Irritating solutions are best given by what route?
Definition
IV
Term
What affects the rate of absorption of an IM injection?
Definition
surface area of capillaries and solubility of the drug in the interstitial fluid
Term
How can you slow down absorption rate of IM injection?
Definition
administration with oil
Term
How are subq injections abosorped?
Definition
filtration or bulk flow
Term
Which has a faster abosrption IM or subq?
Definition
IM
Term
How can you decrease the absorption of Subq drug?
Definition
suspend in oil or implant a solid pellet
Term
What are the advantages of enteral administration?
Definition
safe, covenient, economical
Term
How are drugs absorbed in the mouth?
Definition
mouth has a small surface area and a pH of 6. Can diffuse passively: sublingual (NTG) or buccal (chewing tobacco)
Term
How can the stomach absorb drugs?
Definition
passive diffusion; pH of 1-2, more rapid transfer of acid than base (ion trapping)
Term
What is the primary site for absorption of most orally administered drugs?
Definition
small intestine
Term
How does the small intestine abosrb drugs?
Definition
pH of 5-8; large surface area. usually by passive diffusion also facilitated diffusion, active transport, endocytosis and filtration
Term
Why does the large intestine absorb less than the small intestine?
Definition
smaller surface area and solid nature of contents
Term
What are the advantages of rectal administration/
Definition
drugs that cause gastric irritation, after GI surgery, uncooperative patients, 50% avoids first pass effect
Term
What else is in a tablet besides the drug?
Definition
fillers, disintegraters, binders, lubricants
Term
What are the pros and cons of administering a drug through the lung?
Definition
large surface area and lots of blood flow but cumbersome administration b/c particles need to be the right size
Term
By what method does the lung absorb drugs?
Definition
passive diffusion mostly but some active transport
Term
Why do you cover nicotine patches in saran wrap?
Definition
induce moisture to get drug in acqueous solution to enhance absorption
Term
What factors influence drug distribution?
Definition
regional blood flow, capillary permeability, rate of transfer into tissues, binding to plasma proteins, accumulation into tissues
Term
WHy should digoxin not be taken with a drug that affects intestinal motility?
Definition
because it is absorbed very slowly
Term
What tissues will see IV administered drugs first?
Definition
highly vascularized ones like the brain and the liver (esp seen if the drug is lipid soluble and transfered rapidly
Term
How is thiopental so fast acting and breif?
Definition
because inital high concentrations are lipid soluble and diffuse into the brain and other highly perfused areas. As the drug diffuses it reaches lower concentrations in teh brain and no longer has an affect
Term
Where in the body is capillary permeability increased?
Definition
glomerulus and liver sinusoids
Term
What accounts for the delayed onset and prolonged effects of warfarin?
Definition
binding to plasma proteins
Term
What are the three types of plasma proteins?
Definition
albumin, lipoproteins, and alpha1-acid glycoprotein
Term
How does albumin bind drugs?
Definition
has one to 2 high affinity sites for acids. weaker binding of lipid soluble drugs and weak bases
Term
How do lipoproteins bind drugs?
Definition
bind lipid soluble drugs and amoutn of drug absorption depends on lipid content of lipoproteins
Term
What kinds of drugs does alpha1-acid glycoprotein bind?
Definition
basic drugs; levels are inducible by trauma, injury or stress; 1/2 life of 5.5 days
Term
What causes a drug to accumulate in tissues?
Definition
ion trapping, binding to intracellular components (e.g. iodine in thyroid), partitioning into lipid
Term
How does the blood brain barrier prevent substances from entering the CNS?
Definition
glial cells and endothelial cells form tight jxns. Stops only drugs that are water soluble, NOT lipid soluble. Altered by inflammation
Term
How does placental barrier prevent substances from crossing the placenta?
Definition
smaller fenestra but still allows diffusion of very small particles
Term
Where else in the body is a barrier similar to the BBB?
Definition
testicles
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