Pharm: Sedative Hypnotics Flashcards
How do benzodiazepines distribute through the body and how are they metabolized?
- Widely distributed throughout body: CNS, placenta, breast-milk
- Hepatic metabolism (CYP3A4) and excretion via kidney
What are the benefits of using benzodiazepines for anxiety states?
- High therapeutic index; antagonist available for OD (flumazenil)
- Low-risk of drug-drug interactions
- Minimal effect of cardiovascular or autonomic function
Which benzodiazepine has the fastest rate of onset?
Diazepam
How does Diazepam differ from Alprazolam in terms of half-life, active metabolites and rate of onset?
- Diazepam: long half-life (>100 hr); has active metabolite; very fast onset
- Alprazolam: short half-life (12-15); no active metabolite; fast onset
Which benzodiazepine has a short half-life (5-14 hr), no active metabolite, and the slowest rate of onset?
Oxazepam
Which 2 benzodiazepines have the shortest half-lifes?
Triazolam and Midazolam
Which 4 benzodiazepines have the longest half-lives all >100 hr and all have active metabolites?
- Chlordiazepoxide
- Clorazepate
- Diazepam
- Flurazepam
List 5 benzodiazepines that are short to intermediate acting?
- Alprazolam
- Temazepam
- Triazolam
- Oxazepam
- Midazolam
What is the effect of barbituates on CYP450 enzymes?
Can induce CYP450 enzymes
What is the prototype ultra-short acting barbituate used in anesthesia?
Thiopental
What is the prototype short-acting barbituate that is used for insomnia?
Secobarbital
What is the prototype long-acting barbituate that is used for seizures?
Phenobarbital
What are 3 of the newer sedative hypnotics that are used as sleep aids?
- Eszopiclone (Lunesta)
- Zolpidem (Ambien)
- Zaleplon (Sonata)
Which newer sedative hypnotic has the advantage of coming in a biphasic release formulation for sustained sleep maintenance?
Zolpidem (Ambien)
Which newer sedative hypnotic has the longest half-life?
Eszopiclone (Lunesta)
What are 4 AE’s associated with the sedative drug, Ramelteon?
- Dizziness
- Somnolence
- Fatigue
- Endocrine changes –> ↓ testosterone and ↑ prolactin
What is Buspirone used for and what must you keep in mind when prescribing this drug?
- Approved for tx of generalized anxiety disorder
- Anxiolytic effects may take more than a week to become established (less effective in acute panic disorders)
What are CIs of Alprazolam?
acute narrow angle glaucoma
HS rxn
What is the Black Box Warning of Midazolam?
respiratory depression/arrest
use: pre-op sedation/anxioysis/amnesia
CIs of Diazepam
HS
pts under 6 y/o
MG
severe respiratory insufficiency
severe hepatic insufficiency
sleep apnea syndrome
acute narrow angle glaucoma
What benzo can aid in insomnia with difficulty falling asleep, frequent awakenings, and/or early morning awakenings?
flurazepam
What are the indications, and CIs of secobarbital?
indications - short term tx of insomnia
CIs - HS, hx of manifest or latent porphyria, marked impairment of liver function, respiratory disease with dyspnea or obstruction
What tx for insomnia due to difficulties with sleep initiation can also worsen depression or inc suicidal thinking?
zolpidem
