2. Oral Sedation Flashcards
What chemical propertie of drugs affects absorption properties
- lipid solubility (because absorption is the drugs ability to traverse membranes which are composed of lipids)
- Molecular weight (the smaller the better the absorption)
- Degree of ionization (uncharged crosses membrane)
- Drug release characteristics (i.e some drugs are sustained release)
What must a drug taken orally penetrate in order to be absorbed into the blood
gastrointestinal epithelium
T/F Sedatives must cross the blood brain barrier
t
sWhat are the patient specific factors that influence drug absorption
- Surface area for absorption
- Gastric and duodenal pH (pH and dissociation constant of the drug (or pKa) should be similar)
- Gastric emptying time
- Bile salt pool size (some drugs require bile salts for breakdown)
- Bacterial colonization
- Presence/extent of underlying disease
A person with gastric reflux has (faster/slower) gastric emptying
slower
What structure allows bile salts to enter the duodenum
ampulla of vader
Why is slow gastric emptying a disadvantage for drug absorption
the drug is inactivated when sitting in a pool of stomach acid
Most common causes of delayed gastric emptying
- Peptic ulcers
- DM
- Anticholinergics
- GERD
Define bioavailability
Fraction of drug dose reaching systemic circulation following administration
T/F Bioavailability is only influenced by the drug properties not the person
f both
What are the influences of bioavailability
- Drug formulation
- Particle size
- Solubility
- Degree of absorption from GI tract
- Rapid metabolism during “first pass” through the liver with considerable degree of biotransformation
T/F You can titrate a drug into effect with drugs given both IV and orally
f- just IV
What are the different transport mechanisms of drugs
- Passive diffusion
- Ion pair transport
- Pinocytosis
- Receptor mediated
Define passive diffusion
Movement of molecules from high to low conc.
- Nonpolar lipid soluble compounds diffuse more readily
- Small molecule diffuse more readily than large
Describe ion pair transport
Anions combine with cations to form neutral molecules to diffuse via passive diffusion
Describe pinocytosis
engulfment by cell membrane/internalization
Describe receptor mediated transport
- receptor control ion channels- ligand or voltage gated channels
- Receptors coupled to G proteins (2nd messangers)
What factors influence drug distribution
- Lipid solubility
- Degree of ionization
- Tissue perfusion (someone with atherosclerosis will not get as well sedated because they can’t distribute the drug as well
- Biochemical composition of tissues
Binding of plasma protein to drugs is (reversible/irreversible)
reversible
T/F certain disease states may result in reduced production of plasma proteins
t