Sedative and Hypnotic Drugs Flashcards
Amphetamine, Methylphenidate, and methamphetamine are stimulants that are what schedule drug class? What does that mean?
Schedule 2
- medical use
- high potential for abuse/dependanve
- require written presecription
- no refills allowed
Phentobarbital and secobarbital are what schedule drug schedule? What does that mean?
Schedule 2
- medical use
- high potential for abuse/dependanve
- require written presecription
- no refills allowed
Alprazolam, Clonazepam, midazolam, Diazepam, and Lorazepam are what drug scedule? What does that mean>
Schedule 4
What is the most prescribed benzodiazepine?
alprazolam (xanax)
Clonazepam(long half life), Alprazolam, Lorazepam, and triazolam are high or low potent Benzos?
Higher
CALT –> It is highly potent and dangerous to join cult
Chorldiazepoxide, diazepam, temazepam(short half life) are high or low potent Benzos?
Low
Flunitrazepam is also known as what?
date rape drug, not prescribed sold on the streets
What drug class facilitates GABA interaction with the GABAa receptors to increase the frequency of the Cl- channel opening in response to GABA but does not have GABA-mimetic effects?
Benzodiazepines - causes local hyperpolarization, meaning cell is less likely to fire
What anti anxiety med is useful to only treat sx of acute, transient stress?
Benzodiazepines
75% show improvement, 35% show marked improvement; 25% have no response
• best used in combination with psychotherapy
What IV benzo can cause respiratory depression and apnea?
midazolam
– >in healthy adults, little effect on either cardiac output or
blood pressure with therapeutic doses
–> large doses cause clinically insignificant decreases in blood pressure and cardiac output
Are the cardiovascular effects of what drug?
Benzodiazepines
phase I reactions (CYP3A4) and then glucuronidation (phase II) are the metabolism for most drugs in what class?
Benzodiazepines
Elderly are particularly susceptible to side effects while alcoholics and barbiturate drug abusers are resistant to what drug?
Benzodiazepines
Paradoxic reactions, such as excitement leading to nightmares, hyperactivity, insomnia, irritability, agitation, and/or rage/hostility, occur occasionally in the elderly and young occur with what drug?
Benzodiazepines
• benzodiazepines change normal sleep patterns… gain stage II sleep at the expense of stages I, III, IV and REM sleep
What is MOA of Diazepam, alprazolam, temazepam, midazolam?
-binds to specific GABA-A receptor subunits at central nervous system (CNS) neuronal synapses facilitating GABA- mediated chloride ion channel opening frequency
• enhances membrane hyperpolarization
Dose- dependent depressant effects on the CNS including: • sedation • relief of anxiety • amnesia • hypnosis • anesthesia • coma can be caused by what drug?
- Diazepam (valium)
- Alprazolam (xanax)
- Temazepam (restoril)
- Midazolam (Versed)- also causes respiratory depression
Opioids + Benzos can cause what?
sedation, respiratory depression, coma, and death
- alcohol withdrawal syndrome:
- anxiety, acute/severe:
- management of anxiety disorders
- muscle spasm, spasticity, and/or rigidity:
- spasticity caused by upper motor neuron disorders:
- seizures, acute, active: adjunct intermittent if seizures are refractory, atypical for patient, etc.
- status epilepticus:
Are indications for what drug?
Diazepam
How is diazepam administered?
- Oral or injectable
- metabolized by CYP3A4
- half like of 60-72 hours
- caution with kidney or liver problems
What is temazepam used for?
Insomnia
What is triazolam (halcyon) used for?
Insomnia, also can cause amnesia (used as a murder defense)
Zolpidiem, Eszopiclone, and zaleplon are what?
non-benzodiazepine agonists
-eszopiclone was the first approved for long term use because no tolerance or dependance
What drug binds selectively to BZ1 receptors, a subgroup of GABA-A receptors, acting like benzodiazepines to enhance membrane hyperpolarization?
Zolpidem (Ambien)
What drug has rapid onset of hypnosis with few amnestic effects or day-after psychomotor depression or somnolence
-BUT NO anxiolytic, anesthetic, anticonvulsant, muscle relaxing, respiratory, or cardiovascular effects?
zolpidem (Ambien)
What is the use of zolpidem (Ambien)?
Insomnia
Can zolpidem (ambien) be used in pregnancy?
yes
What drug is an antagonist at benzodiazepine-binding sites on the GABA-
A receptor?
Flumazenil
What drug is used for management of benzodiazepine overdose and reversal of benzodiazepine- induced sedation during surgical procedures
Flumazenil –> reverses Benzes in 1-2 minutes
What drug blocks actions of benzodiazepines and zolpidem
Flumazenil
• does not block other sedative- hypnotic drugs like barbiturates, alcohol, ramelteon, suvorexant
What is a long-acting barbiturate (t1/2 = 10 hr) used to control tonic-clonic seizures?
Phenobarbital
What barbiturate is used for headache pain and has a half life of 35 hours?
butablbital
What is MOA of barbiturates?
– binds to the GABAA receptor, increases the DURATION of GABA-gated channel openings
–↑ chloride influx, ↑ hyperpolarization, ↓ number of action potentials (= CNS depression)
DIFFERENCES FROM BENZOS
– at higher doses, barbiturates also lead directly to Cl- channel opening in absence of GABA
– also inhibit a subset of excitatory glutamate receptors
• these latter 2 actions are not shared by benzodiazepines and may help explain why
barbiturates have a much lower margin of safety
What drugs can easily cross the placenta and cause respiratory depression in the fetus?
Barbiturates
Barbiturates are classic inducers of what?
CYP3A4
- undergo hepatic metabolism and excretion via kidney
-high risks for dependence and development of drug tolerance
– cause respiratory depression, do not use if compromised
respiration
– cause sneezing, cough, laryngospasm, hiccough
– confusion, somnolence, impaired psychomotor performance
– unusual behavioral reactions can occur, but rarely:
• attitudinal depression
• manic behavior, anxiety, hostility, rage…
– possible severe consequences if combined with other CNS depressants (e.g., alcohol)
are adverse side effects of what?
Barbiturates
What is MOA of Buspirone?
A nonbenzodiazepine anxiolytic
• mechanism uncertain: partial agonist at 5- HT receptors, but interactions with other receptor
What nonbenzodiazepine anxiolytic is used in generalized anxiety states
- useful to augment partial response to antidepressant
- lacks tolerance, dependence, and withdrawal
Buspirone
- insomnia
- agitation
- nausea
- alsoriskof
- tachycardia
- paresthesias
- gastrointestinal distress
- Interactions: CYP3A 4 inducers and inhibitors
Are side effects for what drug?
Buspirone
has interactions with CYP3A 4 inducers and inhibitors
- does not cause sedation, hypnotic, euphoric, anticonvulsant, or muscle relaxant effects of benzodiazepines
- does not augment sedation of alcohol or other CNS depressants
- little effect on cognitive or psychomotor function
What drug activates MT1 and
MT2 receptors in suprachiasmatic nuclei in the CNS?
Ramelteon
What are the effects of Ramelteon?
-rapid onset of sleep
with minimal rebound insomnia or withdrawal symptoms
- used from sleep disorders, esp falling asleep
- no abuse, withdrawal, or dependency risk but doesn’t work well
What enzyme does ramelteon activate?
CYP1A2
What drug blocks binding of orexins, neuropeptides that promote wakefulness?
Suvorexant
What are the clinical applications of suvorexant?
sleep disorders, especially those characterize d by difficulty in falling asleep
What drug antagonizes H1 receptors and inhibits reuptake of NE and 5-HT?
Doxepin
What are the applications of doxepin?
• insomnia, sleep
maintenance only
• treatment- resistant
major unipolar depressive disorder (requires ~ 2wks of treatment)
- causes sefation
Black box warning of all antidepressants related to increased suicidal ideation
possible anticholinergic effects (opposite of SLUDGE) and CNS depression impairing ability to operate machinery, etc are toxicities of what?
Doxepin
What drug class causes sedation but does not relieve anxiety?
antihistamines
