Term
| What are sedatives and hypnotics used for? |
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Definition
sedatives-to reduce anxiety
hypnotics-for sedation but at higher doses hypnosis. |
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Term
| Which class of drugs are used for acute anxiety and rapid relief. |
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Definition
Benzodiazepines.
NOTE: They cause tolerance. |
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Term
| What would you use for chronic anxiety? |
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Definition
| SSRIs, SNRIs or Buspirone. (slower onset drugs) |
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Term
| which class of drugs are prescribed for insomnia? |
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Definition
Benzos
try to promote good sleep habits and excercise first. |
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Term
| Why are barbiturates not given to pts for insomnia anymore? |
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Definition
| They have high abuse potential and are dangerous in overdose. |
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Term
| What are we trying to achieve when we give hypnotics? |
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Definition
Fairly rapid onset of sleep
Sufficient duration of sleep
Minimal hangover effects next day |
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Term
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Definition
| It is an antagonist of the GABA-A receptor and helps in benzo overdose. It is short acting-may need to readminister several times for overdose |
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Term
| What is the action of the Benxos, BZ-1 Receptor agonists and Barbiturates on its binding site? |
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Definition
They all bind to GABA-A receptor
Benzos-increase frequency Cl- channel opening
BZ1-R agonist enhance GABA actions w/o anesthetic anticonvulsant or muscle relaxant effects (enhance action by inhibiting breakdown of GABA)
Barbiturates: increase duration of Cl- channel opening at high doses they are GABA mimetic (act like GABA even when no GABA around) and they inhibit Glu AMPA receptors |
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Term
| Do Benzos and BZ-1 receptor have direct action on GABA receptors? |
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Definition
| No they enhance GABA activity so you need GABA to be around. |
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Term
| Describe the Pharmakokinetics of Barbiturates vs. benzodiazepines. |
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Definition
Benzos level off at a certain dose and takes a lot more drus to achieve CNS effect like coma. They are lethal when taken with other depressant like alcohol, codeine.
Barbiturates have a linear slope and they can lead to coma with overdose. Specially due to the GABA mimetic effect and anti Glu effect. |
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Term
| Barbituates and Benzos induce tolerance because they work right away. Why do these drugs have an abuse potential? |
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Definition
Physical tolerance-pt. can get rebound anxiety, insomnia, agitation. fatigue (withdrawal syndrome)
Psychological tolerance- euphoria, disinhibition, promtion of sleep. Pt. gets use to these effects.
Abrupt withdrawal can cause suicide need to withdraw slowly. may take yrs. Short half life drugs may develop withdrawal symptoms sooner so need to withdraw this slower than long half life drug like diazepams. |
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Term
| How does CNS depression manifest with sedative-hypnotics? |
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Definition
| drowsiness, motor incoordination, impaired cognition, disinhibition, sleep driving. |
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Term
| What are some additional adverse effects? |
|
Definition
Anterograde amnesia (dose dep.)
Hangover, paradoxical reactions like aggression and psychosis
Depression of resp and vasomotor centers of medulla. Cardiovascular problems, pulmonary disease or hypovolemic states increase risk.
Hypersensitivity |
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Term
| What is Midazolam used for? |
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Definition
| anticonvulsive therapy (very short acting) or preananesthesia |
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Term
When is Alprozolam used?
When is Chlordiazepoxide used?
Clonazepam?
Diazepam (Valium)?
Triazolam (Halcion)? |
|
Definition
Alprazolam s used for anxiety
Chlordiazepoxide is the prototype benzo used for management of withdrawal of alcohol abuse.
Clonazepam used as antiepyleptic in myoclonus type but cannot use it for chronic epilepsy is tolerance.
Diazepam used as antiepyleptic but anti-seizure effect is onnly 30 min bc it resdistributes from CNS to other parts of body since they are highly lipophyllic
Triazolam has sleep walking effects at high doses. Has a very short hal life. |
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Term
| Why would you not give Flurazepam to the elderly? |
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Definition
| Due to its long half life |
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Term
| What are some important pharmakokinetics of benzos? |
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Definition
Rapid onset, widely distributed Crss BBB, placenta, breast milk,
CYP3A4 inducer diazepam is CYP2C19 inducer as well.
Many of them have active metabolites, glucoronidation
Renal excretion of metabolites |
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Term
| Which drug is frequently given as a muscle relaxant? |
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Definition
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Term
| What are some important properties of BZ-1Receptor agonist? |
|
Definition
rapid onset, duration 6-8 hrs, hepatic metabolism, urine/fecal excretion
Binds GABA-A-alpha1 subunit enhances GABA effects
Shortens sleep latency and prolongs total sleep time.
Less intense withdrawal symptoms than benzos |
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Term
| Can BZ-1s be used as muscle relaxants, anesthesia or anticonvulsant? |
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Definition
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Term
| Which drug would you give for chronic insomnia? |
|
Definition
BZ-1 R agonist
Zalpolon, eszopiclone
Recommended with insomina where pt wakes up in the middle of the night. |
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Term
| Why are barbiturates particularly dangerous when taken with other drugs? |
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Definition
| They are strong inducers of many microsomal enzymes including UGT |
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Term
| What would you give to a patient with Hyperbilirubinemia? How ould the drug work? |
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Definition
| Barbiturates. Phenobarbital induces UGT1A1 which clears out the bilirubin |
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Term
| Which sedative is absolutely contraindicated in acute intermittent porphyria? |
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Definition
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Term
| Which drug is an M1, M2 receptor agonist and binds to suprachiasmic region of hypothalamus to regulate circadian rhythms? |
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Definition
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Term
| Which drug is similar to BZs but has a higher potential for abuse? |
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Definition
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Term
| Which drug is a H1 receptor antagonist with a half life of 9 hrs? |
|
Definition
Diphenhydramine
Do not give to elderly pts! Has anticholinergic effects causes drowsiness, half life is too long.
D |
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Term
| What would be a good sleeping agent for a patient who has never taken benzos? |
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Definition
Ramelteon b/c it does not produce withdrawal or tolerance and is quick acting.
If a pt has already taken benzos they won't like this drug. |
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