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Summary PHARMACOKINETICS PHARM WEEK 1 NOTES - WEEK 1.
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PHARMACOKINETICS PHARM WEEK 1 NOTES - WEEK 1.
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PHARMACOKINETICS PHARM WEEK 1 NOTES - WEEKPHARMACOKINETICS PHARM
WEEK 1 NOTES - WEEK 1
(what the body does to the drug as it moves through the system) Four major
pharmacokinetic processes:
o Drug absorption o
Drug distribution o
Drug metabolism o
Drug excretion
• Vocabulary terms: o Excretion o Extended release
o First-pass effect o
Formulation
o Generic
o Ghost capsules of pills
o Half-life T1/2 o
Induction o Inhaled
formulations o
Inhibition o Lipophilic
o Loading dose o
Metabolite
o Minimum effective
concentration (MEC)
PHARM WEEK 1 NOTES - WEEK 1 |
, PHARM WEEK 1 NOTES - WEEK 1
o P450 enzyme system
o Parenteral
• Vocabulary terms – occur as drug moves through body:
o Peak level of drug o
Per os (PO) o
Pharmacokinetics o
Pharmacogenetics o P
glycoprotein
o Placental drug transfer
o Plateau o Prodrug
o Protein binding o
Reconstitution o Renal
dosing o Scored o
Suppository o
Sustained-release o
Synergistic o
Therapeutic range o
Topically
o Transdermal o Trough
level of drug
Passage of drugs
across membranes o
Drugs must pass
PHARM WEEK 1 NOTES - WEEK 1 |
, PHARMACOKINETICS PHARM WEEK 1 NOTES - WEEK
through membranes in
order to reach their
targets o Three ways
to cross a cell
membrane
Cannels and pores (small ions)
Transport systems (P-glycoprotein)
• P-glycoprotein is a protein that transports drugs across cell membranes
• Some drugs inhibit or activate CYP450 and P-glycoprotein
Direct penetration (must be lipid soluble or lipophilic) (MOST COMMON!)
• Factors that affect drug absorption o Rate of dissolution
o Bioavailability of the drug (IMPORTANT)
Example: Alendronate which is a bisphosphonate for
osteoporosis
Known to have a low bioavailability which is why patients
must take with a full glass of water and wait 30min-1hr before they take
anything else. The availability of the drug to be absorbed is extremely limited.
o Surface area
o Blood flow
o Lipid solubility o pH partitioning
• Routes of Administration o Oral per os PO
• Tablets, capsules, liquids, enteric coasted, sustained release
• Absorption is variable with PO
PHARM WEEK 1 NOTES - WEEK 1 |
, PHARM WEEK 1 NOTES - WEEK 1
• Acid in stomach enzymes and the liver and inactivate PO drugs o
When patients take acid reducers, it can impact the absorption of the
drugs
Scored tablets
• Ease in splitting the dose, half of the dose is contained on each side of
the tablet
• Half of the dose is not assured if the tablet cut in half is not scored
Slow release (SR)
• Some ER, SR, CR can be cut in half
• Others have a rapid release and extended release portion and should
not be chewed
• Example: Hydrocodone controlled release (OxyContin)
• Chewing the tablets can lead to overdose
Ghost Capsule
• Slow release that occurs through little micro pores in the capsule
• Capsule comes out unchanged in the stool
• Examples: Quetiapine XL, Trazadone, Oxycodone, Paliperidone
(Invega) Sublingual (SL)
• Example: Nitroglycerin (can be given topically, SL, or IV because it
is destroyed in the “first pas” through the liver)
• Nitro has a large first pass effect, so you have to give it parenterally
(non-orally) and sublingual is considered parenterally because it is
absorbed from the mucous membranes directly into the bloodstream
PHARM WEEK 1 NOTES - WEEK 1 |
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