Anxiety and Sleep Pharm Flashcards
How would you classify if a patient is suffering from acute anxiety/panic disorder or generalized anxiety disorder?
General Anxiety Disorder
- At least 1 month duration, constant worry about self and others, not correlated with any specific symptoms that indicate panic disorder.
What are physical symptoms of anxiety?
Increased Sympathetic Stimulation
- Sweating, Tachy, Palpitations
- Dry Mouth
- Frequent Urination
- Jitteriness and inability to relax
What receptor is most important in Benzo binding and functionality?
GABA-A Receptor
How do Benzodiazepines affect GABA receptor function?
Benzodiazepines – bind to an allosteric binding site, which causes increased frequency/chance of opening of the GABA channel for the SAME amount of GABA
- sensitizes the channel to GABA
How do Barbiturates differ in function compared to Benzodiazepines?
- Barbiturates bind to a different allosteric site inducing the channel to state open LONGER per stimulation per GABA molecule.
What should you give a patient if you suspect they have overdosed on Benzodiazepines?
Flumazenil – Benzo Receptor Antagonist
How does the GABA receptor typically function when activated by GABA?
- Opens allowing in Cl- hyperpolarizing the membrane making it more difficult to depolarize the membrane
What drug that is used for general anxiety syndrome, but does not involve the GABA receptor, while its a partial agonist of the 5-HT1A receptor (inhibiting adenylate cyclase) opening K+ channels.
Buspirone
What Benzodiazepines are primarily used for hypontic agents?
- Flurazepam
- Triazolam
(Lorazepam too, but not generally just for sleep)
What Benzodiazepam hypnotic agent is long acting agent?
-Flurazepam
What Benzodiazepam hypnotic agent is rapid acting with a very short half life primarily used to help fall asleep, not stay asleep?
Triazolam
- Alpha-Hydroxy-Triazolam active metabolite
How does Lorezepam and Flurazepam affect sleep, other than helping the patient sleep?
- Decreases Sleep Latency
- Increases Stage 1 / 2 Sleep, decreases Stage 3/4 Sleep
- Decreases REM sleep
What happens when there is abrupt withdrawl of sleep aids (Lorazepam) for sleep?
- REM Rebound
- Rebound Insomnia
- Deep Sleep Rebound
What are some adverse site effects of taking Hypnotic agents for sleep?
- Daytime Sedation
- Ataxia at night, increased risk of falls
- Rebound Insomnia
- Tolerance / Dependence
- Increased Death Rate
What hypnotic drugs have minimal effect on REM Sleep and preserve normal Stage 3-4 Sleep?
Zolpidem
Zaleplon
How do the Non-benzodiazepine hypnotic agents work, compared to Lorezapam?
Trick Question!
– Both Bind the BDZ receptor of the GABA receptor, just Zolpidem/Zaleplon are not structurally related.
If you see a patient in the ED who consumed an entire bottle of Zolpidem intending on suicide, what can be given immediately to limited effects?
- Flumazenil
BDZ Receptor Antagonist
What hypontic agent affects Melatonin receptors and is primarily used to help patients who have difficulty falling asleep?
- Ramelteon
Melatonin MT1/MT2 Receptor Agonist
Which hypnotic agent acts in the same way as Zolpidem, but is thought to have limited likelihood of dependence and withdrawal?
Eszopiclone
What is the fast acting Barbiturate?
Secobarbital
How do Barbiturates illicit their effects?
They are lipid soluble, rapidly absorbed, that distribute to the brain quickly causing their effects, but terminated by redistribution.
If a GABA channel increases the amount of time the channel is open per activation, what might be the drug the patient is taking?
Phenobarbital
Secobarbital
What are the most concerning and worrisome side effects of Barbiturates?
- General CNS Depression w/ Respiratory Depression
- Cytochrome Induction changing metabolism
- Physical Dependence
- CV Effects in high doses
- Exacerbate Acute Porphyria (increased delta-aminolevulinic acid synthase)
What is the difference between Benzodiazepines and Barbiturates in regards to CNS Depression?
Barbiturates have a dose dependent action of CNS Depression and include Respiratory Depression
What drug has a very pungent taste that does not effect sleep stages as Benzos or Barbiturates?
Chloral Hydrate
What hypnotic drug antagonizes the Orexin Receptor (inhibits wakefulness usually stimulated by orexin)?
Suvorexant
What agents are most commonly used for muscle spasticity and relaxation?
- Diazepam
- Baclofen
What agent acts at the GABA-B receptor preventing release of excitatory transmitters (Glu) in the spinal cord?
Baclofen
How does diazepam work in the spinal cord to promote relaxation?
- Promotes GABA-induced presynaptic inhibition in spinal cord
What is the agent that agonizes Alpha-2 receptor in the spinal cord inhibiting presynaptic-post synaptic inhibition?
Tizanidine
- drowsiness, hypotension, dry mouth, and inhibits CYP1A2
How is Buspirone different from Benzodiazepines?
- Less Sedating
- No Cross Tolerance
- Takes several weeks to illicit a response in the patient
What might be a good pharmaceutical agent for occasional performance anxiety?
Beta-Blockers
What is the best way to stop treatment with Benzodiazepines?
- Gradual Dose Reduction
- Switch to longer acting Drugs
Does either Diazepam or Lorazepam cause a faster action?
Diazepam – more lipid soluble
Which has an active metabolite Lorazepam or Diazepam?
Diazepam – Oxazepam it is converted to for action
- rapid redistribution after single dose
Which is more lipophilic Lorazepam or Diazepam?
Diazepam – faster absorption
What is a unique characteristic with IV Lorazepam administration?
- Retrograde Amnesia
What is key in differing Benzodiazepines from other CNS Depressants?
Does not effect the Respiratory Drive or CV, however is additive with other depressants that do such as:
- Ethanol
- Barbiturates
- Antihistamines
What should be given an Alcoholic when they are attempting to stop drinking and need to manage withdraw symptoms?
Chlordiazepoxide
- prevents seizures and withdraw symptoms in alcholics
What Benzodiazepine can be used to treat an ACUTE manic episode?
- Clonazepam
What is Alprazolam usually used for?
Fast Acting Effects
- Panic Disorder, etc
