Block 3 PHARM Exam -- Intro to CNS Lecture
Terms
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- Properties of the brain capillary endothelium
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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
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PITUITARY
HYPOTHALAMUS
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
- L-DOPA
- Type of metabolism that clears CNS drugs
- Hepatic
- Route to administer POORLY diffusable CNS drugs
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Intrathecally
(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
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High abuse potential
NO medical use
(THC, heroin, opiates, LSD) - Schedule II Drugs
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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
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Low abuse liability
Do NOT require a prescription
BUT, dispensed by pharmacists - Location and function of serotonergic projections
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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
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CNS, gut
Agonists are anxiolytic - Serotonin Receptor IB/D
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Sensory nerve endings, meningeal vessels
Agonists are used for migraines - Serotonin Receptor IIA
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CNS
Agonists are hallucinogenic
Antagonists are anti-psychotic - Serotonin Receptor III
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ION CHANNEL
CNS, Gut
Agonists are powerful anti-emetics - Serotonin Receptor IV
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CNS, gut
Agonists are prokinetics
(Treat IBS and GI reflux) - Where is histamine synthesized
- Only in the hypothalamus
- Uses of H1-receptor ANTagonists
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Those that CROSS BBB --- sedatives
Those that do NOT CROSS BBB --- anti-allergics