Pharm: Sedative and Hypnotic Drugs Flashcards
Which drugs are the Benzodiazepines?
-Am
Alprazolam
Clonazepam
Diazepam
Lorazepam
Midazolam
Temazepam
What drugs are the Non-Benzo BZ1 agonits?
Esxopiclone
What drugs are the Benzo antagonists?
Flumazenil
Which drugs are the barbiturates?
-tal
Pentobarbital
phenobarbital
thiopental
which drug is in a misc. category?
buspirone
Which drug is a melatonin agonist?
ramelteon
which drug is a dual orexin receptor antagonist?
suvorexant
which drug is an antihistamine?
doxepin
What are the main clinical uses of sedative-hypnotics?
relief of anxiety
insomnia
what is the most prescribed benzo?
Alprazolam
also-clonazepam, lorazepam, diazepam, temazepam
What is the MOA for benzos?
Work on GABA A receptor to increase frequency of Cl- channel opening
causes a local hyperpolarization, meaning cell is less likely to fire
What is the most common side effect of benzos?
drowsiness
elderly are more susceptible while alcoholics and barbiturate abusers are more resistant
What are paradox reactions as caused by benzos?
excitement leading to nightmares, hyperactivity, insomnia, agitation, rage, etc.
occur occasionally in elderly or young
Benzos can alter sleep patterns in which way?
may cause changes in stages, but is quickly adapted to
Day-time hangover
Rebound insomnia after abrupt d/c
Can dependence to benzos develop?
tolerance and psychological dependence-yes
physiologic dependence-less likely
Which class schedule are benzos?
Schedule IV
relatively safe compared to barbiturates
What are some signs of benzo abuse?
confusion, depression, impaired judgment, decreased inhibitions, “act drunk”
altered vision, sedation, drowsiness
Diazepam is a substrate of which CYP?
CYP3A4
What is the main concern of combining benzos and opioids?
may result in profound sedation, respiratory depression, coma and death
What condition has been associated with IV Midazolam?
respiratory depression and arrest, espcially when used for sedation in non-critical care settings
What is the MOA of Zolpidem?
Does it carry anxiolytic effects?
Is it safe in pregnancy?
Why is it used?
Forms?
similar to benzo’s MOA
Nope
Yep!
Sleep/insomnia
IR, siblingua tablets, oral spray to initiate sleep
ER tablet for maintenance or onset sleep difficulties
What are some concerns associated with Zolpidem?
complex sleep behaviors like sleepwalking, sleep-driving?!?!, and engaging in other activities while not fully awake
can result in death
can include making/eating food, phone calls, having sex, etc.
What is the main concern of flumazenil?
this is an antagonist at benzoe sites on the GABA A receptor and is associated with Seizures especially in people who have been on long-term sedation or were treated with TCAs
What drug class are classic inducers of CYP3A4?
Barbiturates
What is the initial treatment for GAD?
then what?
CBT
SSRIs
Buspirone
Pregabalin
Benzos
What are the best treatments for specific phobias?
exposure therapy
CBT
benzos
What is the best treatment for separation anxiety?
CBT +/- SSRI
How should benzos be tapered?
decrease by 25-50% every 1-2 weeks over a period of 6-10wks
longer duration of use means higher liklihood of symptoms
can replace a short acting benzo for a long acting benzo, as short acting ones have a higher dropout rate and worse rebound anxiety
what is the effect of Flumazenil?
blocks the actions of benzos and Zolpidem, but not other sedatives (like ETOH, barbiturates, etc)
What is unique about the properties of Midazolam?
It is given IV or IM and is water soluble but highly lipid soluble in vivo
