2. Sedative and Hypnotic Drugs Flashcards
Sedative-Hypnotic drugs have three categories including Benzodiazepines, barbiturates and miscellaneous agents. Benzodiazepines have short acting (triazolam), long acting (flurazepam) and intermediate acting such as?
Alprazolam
Barbiturates have an ultra-short action such as thiopental, short acting such a secobarbital, and what is the long acting barbiturate? (Note: misc drugs are busprione, eszopiclone, zaleplon, and zolpidem)
Phenobarbital (he likes dis one)
Sedative drugs are CNS depressants, moderates and calms the patient, fast acting, is anxiolytic and causes sedation. Hypnotic drugs produce drowsiness and facilitates the onset and maintenance of sleep, they involve more pronounced depression of?
CNS (which can be acheived by many drugs by increasing dosage)
barbiturates and benzodiazepines have the same effect as lower doses, but as doses increase the effects do as well. At the max dosage, benzos can only cause anesthesia, what can barbiturates cause?
Increasing dosage of barbiturates can lead to medullary depression, coma and at even higher doses- DEATH
Clinically, sedative hypontic drugs are used for relief of anxiety, insomnia, sedation before procedures, epilepsy, seizures, control ETOH and other withdrawal states, muscle relaxation, and as diagnostic aids or for tx in?
Psychiatry (my strange addiction type shit)
What acts on GABAa receptors to cause sedation, hypnotic effects, muscle relaxation, anxiolytic and anticonvulsant effects?
Benzodiazepines
What acts on GABAa receptors to cause a wide spectrum of effects, such as mild sedation to anesthesia?
Barbiturates
Benzos are widely used and distributed through the body including CNS, placenta and breast milk, they are metabolized by CYP3A4 and elimination ranges from 2-100 hours, there is a risk of dependence and tolerance and the MOA is what?
Bind to GABAa receptor and enhances GABAs effects leading to increase chloride influx, hyperpolarization, decreasing number of action potentials = CNS depression
Benzos are used to treat anxiety, including alprazolam, diazepam, clonazepam, lorazepam. Advantages include that there is a high therapeutic index (flumazenil is used for overdose), low risk of drug drug interaction and minimal effect on?
Cardiovascular or autonomic function
Disadvantages of benzos used for anxiety states include a risk of dependence, depression of CNS when combined with other drugs, especially ETOH… Newer antidepressants are sometimes preferred such as?
SSRIs
What drug has a 1/2 life of >100, active metabolites, and has a very fast rate of onset after administration?
Diazepam
What drug has a 1/2 life of 5-14, no active metabolites, and has a slow rate of onset after administration?
Oxazepam
What drug has a 1/2 life of 10-20hrs, no active metabolites, and has an intermediate rate of onset after administration?
Lorazepam
What drug has a 1/2 life of 12-15, no active metabolites, and has a fast rate of onset after administration?
Alprazolam
What drug has a 1/2 life of 20-50hrs, no active metabolites, and has an intermediate of onset after administration?
Clonazepam
The following drugs are considered what type? alprazolam oxazepam temazepam midazolam triazolam
Short to intermediate acting benzodiazepines
The following drugs are considered what type?
diazepam
lorazepam
clonazepam
Intermediate to long acting benzodiazepines