Sedative-Hypnotics and Alcohol Flashcards
Anxiety is usually ___ to other disorders
Anxiety is usually secondary to other disorders
What is anxiety?
Feelings of fear, tension, apprehension, etc.
The best way to treat anxiety is often to…
Treat the underlying illness
What are sedative-hypnotics?
Benzodiazepines and barbiturates.
What are anxiolytic drugs?
Sedative drugs that help treat anxiety without impacting motor or mental function
What are hypnotics?
Drugs that produce drowsiness and induce sleep
What are benzodiazepines?
Drugs that bind to a separate site on GABAa receptors and increase the frequency of Cl-channel openings.
No matter how high the dose, benzodiazepines require ____ for their effects.
They only work in the presence of GABA
Give an example of a benzodiazepine
Diazepam (VALIUM)
How is diazepam broken down?
Phase I: Diazepam is oxidized by cytochrome P450
Its metabolites are active (they produce the same calming effects)
Phase II: Interaction with glucuronide makes it passable in urine
What is an example of a barbiturate?
Phenobarbital
What makes barbiturates different from benzodiazepines like Diazepam?
They have a smaller safety margin
Their metabolites are generally not active
At high doses, barbituates can directly activate GABAa receptors
Barbiturates can increase the expression of some cytochrome p450 enzymes which is…
dangerous because cytochrome p450 plays a big role in drug metabolism, it messes with the breakdown rates of other drugs.
Both benzodiazepines and barbiturates enhance Cl- conductance which…
Increases the inhibition of many neurons all throughout the brain
Benzodiazepines and barbiturates bind to ____ sites on GABAa receptors
different sites, meaning their effects can stack
Sedative hypnotics are used to treat…
Anxiety, insomnia, psychosis, epilepsy, alcohol withdrawl
Before surgery, sedative-hypnotics are given as part of the
anesthesia process
What are some of the adverse effects of sedative-hypnotics (benzos and barbiturates)
Dose-dependent CNS depression (ranging from impaired motor skills -> coma -> death) *CNS depression can combine with other drugs ex. alcohol
Withdrawal symptoms after prolonged use
Tolerance will develop
Extra toxic if liver function is impaired
How does THC regulate anxiety?
the endocannabinoid system regulates anxiety by dampening excitatory glutamate signals (THC decreases glutamate release)
How does marijuana become addictive?
Chronic marijuana use down-regulates receptors, leading to increased anxiety due to a lack of receptors available for the natural endocannabinoid system
Endocannabinoids work by ____ by activating CB1 receptors
inhibiting transmitter release by activating CB1 receptors
Marijuana contains compounds which…
activate CB1 receptors
Overall THC is responsible for reducing the release of both ____
Glutamate and GABA
What is ethanol?
Beer, wine, rum etc
What are the acute effects of ethanol?
DOSE DEPENDANT CNS depression
Decreased membrane excitability
Increased GABAa activation
Decreased NMDA activation
How does ethanol impact myocardial contractility?
Initially, it is increased, then it decreases.
What are the behavioral effects of ethanol?
Decreased anxiety, impaired judgement, slurred speech
What happens when a toxic dose of ethanol is taken?
CNS and respiratory depression
What are the chronic effects of ethanol use?
liver failure
pancreatitis and gastritis
malnutrition
How is 90% of ethanol metabolized?
In the liver
Major pathway: alcohol dehydrogenase
Minor pathway: cytochrome p450
How is the last 10% of ethanol metabolized?
Its excreted in the lungs and urine
Alcohol has a ___ clearance rate
constant clearance rate
How is ethanol different from methanol?
Methanol has the same CNS depression effects
When metabolized, methanol turns into formic acid -> builds up in retina -> blindness
How do you treat methanol poisoning?
With ethanol
Ethanol has a higher affinity for alcohol dehydrogenase so the formic acid levels won’t peak as high
