module 3 Flashcards
Gaba signalling
Causes gaba inhibition by binding to and selectiveky opening chloride channels.
why does GABA cause CNS depression and how
when GABA binds to and opens the chloride channel, chloride ions flow into the post synaptic neuron. the influx of chloride ions makes it harder for the post synaptic neuron to transmit incoming messages to other neurons, therefore depressing CNS neuronal signalling
benzodiazepines mechanisms of action
activation of benzodiazepines receptor increases the frequency of the opening of the chloride channel
benzos have _______ on rem sleep
minimal suppression
benzos have a _____ therapeutic index
high
antidote for benzodiazepines
flumazenil , a benzo receptor antagonist
mechanism of action barbiturates
increases duration of the opening of the chloride channel
difference between barbiturates and benzodiazepine
benzodiazepines increase frequency of chloride channel opening while barbiturates increase duration of opening. benzodiazepines have a higher therapeutic index while barbiturates have a low therapeutic index, and the withdrawal can cause death. benzos have an antidote flumazenil while barbiturates do not. benzos minimally suppress rem sleep but barbiturates suppress rem sleep.
short term effects of barbiturate use
in large doses, they can depress the cardiovascular system slowing the heart and lowering blood pressure. may cause dizziness and mild impairment of motor coordination
barbiturates potential for misuse and sud
potential for misuse greater or equal to alcohol pleasurable effects give significant degree of reinforcement. inherent harmfulness very high due to risk of death from respiratory depression or withdrawal
cross tolerance can develop with other sedatives
barbiturates are ______ while benzodiazepines are________
anti epileptic, anti anxiety
buspirone
an anxiolytic that does not act on the gaba receptor, but on the serotonin receptor. used in general anxiety states, does not have additive effects with other sedative hypnotic drugs
which affects sleep less, zopiclone or benzodiazepine
zopiclone
______ does not appear to be a problem for the clinical use of benzodiazepines however can develop to the _______ effects and impairment of coordination the anxiolytic effects or euphoric effects
tolerance, sedative
4 effects of sedative hypnotics on the cns depending on the dose
anti- anxiety, sedation, hypnosis, general anesthesia
____ of alcohol is absorbed in the stomach , ____ is absorbed in the upper small intestine
20%, 80%
short term effects of opioids
analgesia
suppression of cough centre
respiratory depression
miosis
decreased intestinal motility
endocrine effects
sedation and hypnosis
irregular heart rate, low body temperature and sweating
classes of opioids
endogenous opioids (excercise)
natural opioids ( opium poppy)
semi synthetic opioids (oxycodone)
synthetic opioids (fentanyl)
therapeutic use for opioids
treatment of diarrhea
relief of severe pain
cough suppression
opioids made in the body that bind to opioid receptors
endogenous opioids
opioids not made in the human body but derived from the opium poppy plant
natural opioids morphine and codeine
slightly altered versions of morphine that are chemically changed to obtain different pharmacological properties
semi synthetic opioids
hydromorphone
diacetyl morphine
brand name heroine
diacetylmorphine
opioids not serviced from morphine by chemically synthesized to bind to the opioid receptor
synthetic opioids such as fentantyl and loperamide and methadone
opioid receptors
MU, KAPPA, DELTA
where are MU opioid receptors found
all structures of the brain and spinal cord
what are KAPPA receptors responsible for
analgesia dysphoria and miosis
receptors involved in analgesia at the level of spinal cord and brain and may module emotional response to opioids
DELTA receptors
opioids reduce the emotional reaction to pain through :
the modulation of the limbic system
how to opioids prevent pain signals
by reducing neurotransmitter release from presynapic neurons and reducing the effect on post synaptic neurons
opioid misuse potential
large risk for misuse as they have very powerful euphoric effects
opioid antagonist
naloxone
what receptor does thc bind to
CB1 receptors in brain and spinal cord
cannabis mechanism of action
anandamide is an endogenous ligand for CB receptors involved in learning and memory processes. the CB1 receptor when activated by anandamide or THC inhibits the release of excitatory neurotransmitters. explaining the reduction in cognitive function and CNS depressant effects seen with THC
where are CB1 and CB2 receptors found
CB1 Receptors are found in the brain and spinal cord and CB2 are found on lymphocytes and are thought to be responsible for immunosuppressive properties of THC
thc is highly ____ soluble
lipid
half life of THC
30 hours
short term cannabis use effects
cns effects drowsiness impaired motor coordination increased appetite euphoria
cardiovascular increases heart rate increased blood flow to extremities
pots
gi tract increased appetite mouth dry
reduced sex drive and testosterone levels
disruption of ovarian cycle
long term effects of cannabis
high doses short term memory loss lack of concentration loss in ability in abstract thinking emotional flatness
changes in blood pressure
respiratory issues like copd
decreased sperm count
reduced fsh and lh
