Neurobiology Final Module 1 Flashcards
What the drug does to the target (receptor)
drug action
impact drug action has on physiological and psychological functions
drug effect
the action of _____ is to block sodium channels which affect the release of glutamate
lamotrigine
what is the drug effect of lamotrigine
raise the seizure threshold and stabilize mood
this drug is given to reduce certain types of anxiety while also causing reduction in heart rate and blood pressure
propranolol
slow and can be impacted by first pass metaboliam
oral route
these types of drugs require an active transport pump
ionized
why do highly vascular areas such as heart, liver, kidney, and brain have high drug concentrations?
because capillaries are porous
area responsible for detecting and responding to toxins by inducing vomiting, do not have a BBB
chemical trigger zone (area postrema)
what is the most common depot binding site (silent receptor)
albumin
once in the bloodstream, drugs can be bound to other substances like protein or stored in other tissues as inactive substances making them _____ available to target receptors
less
sites that cause no appreciable effect causing drugs to be inactivated (when a drug is heavily protein bound)
drug depots (silent receptors)
most common metabolic process that takes place through the actions of the cytochrome P450 enzyme chains
biotransformation
the whole purpose of the CYP450 enzyme chain is to:
metabolize drugs/hormones
causes the enzyme to do its work of metabolizing its substrates
enzyme induction
used for mood stabilization, is a strong inducer of 3A4 which can lead to decreased levels of birth control when taken together
carbamazepine
a substrate of 3A4 therefore requiring higher doses d/t inducing its own metabolism
carbamazepine
cigarette smoking induces CYP450 1A2 which can lead to reduction in levels of substrate drugs such as _____ and _____
antidepressants, caffeine
causes substrates to be broken down more slowly
enzyme inhibition
an inhibitor of CYP450 2D6 and 3A4 which metabolizes aripiprazole therefore when taken together it will cause aripiprazole to be metabolized more slowly resulting in elevated levels in the bloodstream
fluoxetine
any substance that binds to a receptor is a _____
ligand
type of receptor in cell wall that alter membrane potential
ion coupled
type of receptor in cell wall that cause a prolonged response such as changes in enzyme activity
G protein
drugs that initial a cellular response, stimulate the normal response brought about by activating the receptor
receptor agonist
centrally acting alpha 2 agonist used for ADHD in children causing stimulation to decrease BP, HR, and vascular resistance while the increased alpha 2 stimulation in PFC leads to improved focus
guanfacine
chemicals that bind to the receptor but have no effect but also block the receptor from being stimulated
receptor antagonists
used for mood stabilization and seizure d/o, is a glutamate voltage sensitive sodium channel blocker
lamotrigine
an excitatory neurotransmitter that when blocked reduces excitatory stimulation
glutamate
sometimes referred to as modulators/stabilizers, their action depends on the amount of natural agonist available. If none available it will act as agonist if too much available it will act as an antagonist
partial agonist
atypical antipsychotic, partial agonist of D2 and D3 receptors. When levels too high it reduces leading to improvement of +symptoms. When too low it increases resulting in improved cognition, stable mood and reduces -symptoms
cariprazine
causes a response where antagonist block
inverse agonist
drugs that compete with an agonist by occupying a receptor but creating no response resulting in reduced agonist effects
competitive antagonists
competes with opiates for receptors occupying them and causing no response but resulting in a reduction of opiate effect
naloxone (competitive)
do not occupy the receptor but reduce the agonist effect in other ways
noncompetitive antagonists
occurs when 2 drugs interact to decrease the effect of both drugs on the target receptors (Adderall for ADHD increases HR and metoprolol lowers HR)
physiological antagonism
a patient is given an opiate for pain and a benzo for anxiety with a result of increased sedation
additive effect
2 drugs given together produce an effect greater than the sum of their individual effects
potentiation
when an agonist drug is used long term resulting in reduction of available receptors
down regulation
beta receptors stimulate _____
sympathetic responses
beta 1 receptors cause _____ HR
increased
beta 2 receptors cause
bronchodilation and increased glucose production
the extent of the effect produced by a given drug concentration, provides a measure of receptor activity
dose response curve
lowest dose that achieves an effect
threshold dose
amount of a drug required to achieve desired effect
potency
occurs when long-term used reduces the drug that is available to the receptor site such as when a drug induces its own metabolism in the CYP450 system
metabolic tolerance
results from changes in the function of nerve cell that occur in response to the presence of the drug
pharmacodynamic tolerance
the most studied gene mutations are those responsible for determining the function of specific _____
CYP450 enzymes
this gene determines whether folate metabolism occurs normally and mutations can cause a reduction in
methylenetetrahdrofolate reductase gene (MTHFR)
when folate is not metabolized in adequate amounts the monoamine levels are _____ leading to increased rates of ______
reduced, depression
mutation in histocompatibility complex HLA-B*1502 is common in _____ populations
Chinese
process by which neurons transmit signals out to other neurons
divergence
when there are normal spines but fewer of them such as in schizophrenia, intellectual function is normal, but the patient has _____ and _____ characteristic of the disorder
cognitive, negative symptoms
carry synaptic vesicles containing neurotransmitters
terminal buttons
_____ and _____ in the chemical environment can alter transcription factors leading to changes in protein production
prolonged stress, chronic changes
_____ and _____ open the gene to transcription factors which effectively turns the gene “on” so it is expressed
acetylation, demethylation
_____ and _____ turn gene “off” by denying access by transcription factors
deacetylation, methylation
Alzheimer’s disease is in part caused by a problem with _____ responsible for maintaining normal axoplasmic transport through neurofilaments and microtubules
protein tau
neurofibrillatory tangles occur when _____ of substance tau causes it to be malformed
hyperphosphorylation
_____ works by blocking voltage-gated Na+ channels which means an action potential cannot occur
lidocaine
the time it takes for a drug to unbind allows for longer refractory period and reduced rate of firing which decreases ______
seizure activity
_____ come from the ventral horn thoracic and lumbar regions. Axons are short and synapse with sympathetic ganglia
efferent sympathetic neurons
_____ release acetylcholine to the ganglia and postganglionic cells release NE to target tissues
preganglionic fibers
_____ located in either the brain or the ventral horn of the spinal cord at the sacrum. Their axons are long and synapse with ganglia close to target organs
efferent parasympathetic neurons
postganglionic fibers also release
acetylcholine
controls HR, BP, RR, digestion, coughing, and vomiting
medulla
_____ and _____ contain the reticular formation which is key to arousal, attention, sleep, muscle tone, and some cardiac and respiratory reflexes
pons, midbrain
a nuclei in the reticular formation that is a cluster or neurons releasing NE causing arousal, vigilance, and increased attention
locus coeruleus
amphetamines _____ the function of the locus coeruleus
enhance
dorsal and medial raphe nuclei are the course of neurons that release _____
serotonin
part of the visual system and controls pupil response
tectum
receives visual, auditory, and somatosensory stimuli, information about balance and body position, coordinates time, patterns and skeletal muscle contractions
cerebellum
innervates the striatum in the basal ganglia, a group of cells that produce DA for transmission
substantia nigra
_____ results from cell death in the substantia nigra
Parkinson’s disease
ventral tegmental area, limbic system (mesolimbic tract), frontal cortex, cingulate cortex, and entorhinal areas are key to development of:
Schizophrenia and Parkinson
established long term memory, spatial memory, and contextual memory, sensitive to changes in stress hormone levels and involved in the development of depression
hippocampus
4 classic neurotranmitters
amino acids
monoamines
acetylcholine
purines
small protein molecules that stimulate opiate receptors and play a role in drug abuse, take longer to produce and replace than classical neurotransmitters because they can only be produced in the cell body
neuropeptides
block serotonin removal by serotonin transporters
SSRIs
_____ blocks DA, NE, and serotonin transporters
cocaine
drug mimics the neurotransmitter at the receptor
agonist
receptor that works fast and is key to process that requires immediate response
ionotropic (ligand-gated channel)
slower than ionotropic and the postsynaptic response is slower and longer lasting result. Work by activation of G proteins stimulate or inhibit the opening of ion channels
Metabotropic receptors
one of the key functions of second messengers is activation of _____
protein kinases
inhibits phosphodiesterase which results in increased cGMP and the relaxation of smooth muscle around blood vessels
Viagra
a monoamine oxidase inhibitor that blocks function of monoamine oxidase which is responsible for the breakdown of 5-HT, DA, and NE
phenelzine
_____ are agonists for GABA receptors by enhancing the inhibitory effects of GABA
benzodiazepines
secretes cortisol, epinephrine and NE in response to stress
adrenal gland
secretes melatonin which helps regulate sleep/wake with 5-HT as a precursor for production
pineal gland
_____ is a common SE in schizophrenia bc of D2 receptors being blocked
hyperprolactinemia
percentage of D2 receptors that must be occupied for relief of schizophrenia symptoms
50
