Pharmacology Exam I part 3
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Substances that affect drug metabolism
grapefruit juice -CYP 3A4 inhibitor, St John's wort, other herbal products, isosafrole, safrole: CYPA1, CYPA2 INHIBITOR (found in perfrume and root beer)
Phase II metabolism
considered anabolic, phase I metabolism is combined with another component to make it inactive, generally more water soluble and predictable than phase I reactions
Phase II turns lipid soluble drugs into
water soluble drugs
Blood-brain barrier and placenta
only very lipid soluble drugs can pass
What age group metabolize poorly?
old people and very young people
Another word for elimination?
receptors, enzymes, transporters, ion channels
3 types of receptors
ligand-gated ion channels, g-protein coupled receptors, and nuclear receptors
ligand-gated ion channels
time scale is in milliseconds (takes effect very fast) occurs in membrane bound (doesn't cross)
G-protein coupled receptors
occur in seconds (found in heart)
ligand has to cross cell membrane (ex. in oestregen receptors); causes gene transcription because the ligand changes DNA (ex. birth control takes a while to work)
Why does it take G-protein receptors a bit longer?
G-protein membranes have seven membrane-spanning a-helices
Monamine transporters are important in the
central nervous system
Peripheral nervous system 2 divisions
somatic (involuntary movement) and visceral
2 subdivisions of visceral
parasympathetic and sympathetic
Neurotransmitters for parasympathetic system
Neurotransmitters for sympathetic system
Norepinephrine and epinephrine
Increasing Norepinephrine does what to heart rate?
increase heart rate
Decreasing Norepinephrine does what to heart rate?
decreases heart rate
G-protein linked receptors; 5 subtypes (depend on location) m1=neuronal,m2=cardiac,m3=glandular smooth muscle, m4/m5=CNS;Agonist=AcH; Antagonist=atropine and scopolamine
AcH in the heart does what to heart rate and force of contration
decreases both heart rate and force of contraction
norepinephrine is not used in muscarinic receptors
becuase the half life is short and would be broken down before a physological response appears
"pilocarpine: used for glaucoma, increases intraocular pressure which activates constrictor muscle to promote fluid drainage.
- 1)inhibit secretions (salivary, lacrimal bronchial)
- 2) increase heart rate (tacliycardio)
- 3) dilate pupil
- 4) increase GI motility
- 5) relax smooth muscle
- 6) increase GI activity
skeletal muscle (only place where these receptors are used), nicotinic antagonists, skeletal muscle relaxants, non-depolarizing blockers (bind to receptor and prevent AcH from binding)
There is no depolarization in nicotinic antagonists, true or false?
true. (ex. atracurium and tubocurarine)
bind and depolarize membrane (produce effects) and can't repolarize, these compounds stay bound to receptor for a long time, nothing you can do to reverse effects of these. (ex. succinylcholine)
Acetylcholinesterarse (in depolarizing blockers)
breaks down AcH and then the choline is taken back up
block AcHesterase and increase AcH at receptors
Reversible AcHesterase (inhibit)
- have short duration
- Example 1
- neostigmine for the condition of myastehnia graris (autoimmune disease that breaks down muscle and causes fatigue) increases AcH levels at skeletal muscle receptors)
- Example 2
- aricept (donepezil) reversible AcHesterase inhibitor used for alzheimers
Irreversible inhibitors provide how many hours of AcH?
about 20-24 hours
mAcH (muscarinic), smooth, when used as antidote the effects of AcH inhibitors will be reversed
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