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Block 3 PHARM Exam -- Intro to CNS Lecture


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Properties of the brain capillary endothelium
Does NOT support vesicular transport
Histamine, 5-HT and NE do NOT increase its permeability
Has NO contractile protein
(CNS drugs must cross TWO lipid membranes)
Type of epithelium in choroid plexus
Ciliated Cuboidal
Major areas WITHOUT the BBB
Pineal gland, Median Eminence, Area Postrema
Olfactory, Endings of perip. nerves (viral), sensory ganglia
Dura, part of optic nerve
CNS-active drug that is NOT lipid soluble
Type of metabolism that clears CNS drugs
Route to administer POORLY diffusable CNS drugs
(Remember, NO diffusion barrier between CSF and ECF)
Pharmacokinetic Tolerance
Decrease in drug efficacy results from increase in disposition
Pharmacodynamic Tolerance
Decrease in drug efficacy results from decrease in responsiveness
Schedule I Drugs
High abuse potential
NO medical use
(THC, heroin, opiates, LSD)
Schedule II Drugs
Prescribed by physicians only
High potential for abuse and dependence
(Cocaine, morphine, codeine, phenobarbital)
Schedule III Drugs
High psych. dependence and/or moderate phys. dependence
Schedule V Drugs
Low abuse liability
Do NOT require a prescription
BUT, dispensed by pharmacists
Location and function of serotonergic projections
LIMBIC SYSTEM to regulate mood
HYPOTHALAMUS to regulate appetite and hormone production
DORSAL HORN to regulate pain
BRAINSTEM to regulate breathing
(Control respiration after birth)
(Control airway diameter later in life)
Serotonin Receptor IA
CNS, gut
Agonists are anxiolytic
Serotonin Receptor IB/D
Sensory nerve endings, meningeal vessels
Agonists are used for migraines
Serotonin Receptor IIA
Agonists are hallucinogenic
Antagonists are anti-psychotic
Serotonin Receptor III
CNS, Gut
Agonists are powerful anti-emetics
Serotonin Receptor IV
CNS, gut
Agonists are prokinetics
(Treat IBS and GI reflux)
Where is histamine synthesized
Only in the hypothalamus
Uses of H1-receptor ANTagonists
Those that CROSS BBB --- sedatives
Those that do NOT CROSS BBB --- anti-allergics

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