Unit 3 Pharm Guiding Questions Flashcards
What is the blood brain barrier?
refers to the unique structure and function of CNS capillaries, which act as a selective filter and protects the CNS by limiting the substances that enter the brain and spinal cord
What is the blood brain barrier’s role in clinical pharmacotherapeutics?
-nonpolar, lipid-soluble drugs are able to cross the barrier by passive diffusion
-polar and lipophobic compounds are usually unable to enter the brain but exceptions occur because of the presence of carrier-mediated transport systems
central neurotransmitters that have an excitation effect
-acetylcholine
-glutamate, aspartate
-substance P
-enkephalins
central neurotransmitters that have an inhibition effect
-norepinephrine
-dopamine
-serotonin
-GABA
-glycine
the majority of CNS drugs work by modifying synaptic transmission in some way.
list the sites at which drugs can alter transmission at a CNS synapse.
- action potential
- synthesis
- storage
- release
- reuptake
- degradation
- postsynaptic receptor
- presynaptic “autoreceptor”
- membrane
drugs that attempt to rectify CNS-related disorder do so by either ___ or ___ transmission at specific synapses.
increasing or decreasing
a drug that modifies synaptic transmutation must somehow alter the ___ of the neurotransmitter that is released from the presynaptic terminal or affect the ___ of postsynaptic receptors, or both.
quantity, stimulation
Why are barbiturates effective sedative hypnotics?
because of their specificity for neurons in the midbrain portion of the reticular formation as well as some limbic system structures
how to nonbenzodiazepine sedative hypnotics work?
they bind to the GABA receptors in the brain which causes GABA to bind more effectively thus increasing chloride conductance and the level of inhibition in the neuron. increased inhibition results in less arousal and promotion of sleep.
how do nonbenzodiazepines work?
they promote relaxation and sleep via depressing the CNS
pharmacokinetics of benzodiazepines and nonbenzodiazepine sedative hypnotics
usually highly lipid soluble
administered orally and absorbed easily from the GI tract
metabolized primarily by the liver
excretion occurs through the kidney after metabolism in the liver
pharmacokinetics of benzodiazepines and nonbenzodiazepine sedative hypnotics
usually highly lipid soluble
administered orally and absorbed easily from the GI tract
metabolized primarily by the liver
excretion occurs through the kidney after metabolism in the liver
what is the primary problem associated with sedative hypnotic use
residual effects that occur the day after (drowsiness and decreased motor performance)
define drug tolerance
the need to take more of a drug to exert the same effect
define drug dependence
the onset of withdrawal symptoms if drug administration is ceased