Shared Flashcard Set

Details

Lecture#70: Pharm of Sedatives and Hypnotics
Nervous System Part III
28
Medical
Professional
03/01/2011

Additional Medical Flashcards

 


 

Cards

Term
What are sedatives and hypnotics used for?
Definition
sedatives-to reduce anxiety
hypnotics-for sedation but at higher doses hypnosis.
Term
Which class of drugs are used for acute anxiety and rapid relief.
Definition
Benzodiazepines.
NOTE: They cause tolerance.
Term
What would you use for chronic anxiety?
Definition
SSRIs, SNRIs or Buspirone. (slower onset drugs)
Term
which class of drugs are prescribed for insomnia?
Definition
Benzos
try to promote good sleep habits and excercise first.
Term
Why are barbiturates not given to pts for insomnia anymore?
Definition
They have high abuse potential and are dangerous in overdose.
Term
What are we trying to achieve when we give hypnotics?
Definition
Fairly rapid onset of sleep
Sufficient duration of sleep
Minimal hangover effects next day
Term
What is Flumazenil?
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
Term
What is the action of the Benxos, BZ-1 Receptor agonists and Barbiturates on its binding site?
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
Term
Do Benzos and BZ-1 receptor have direct action on GABA receptors?
Definition
No they enhance GABA activity so you need GABA to be around.
Term
Describe the Pharmakokinetics of Barbiturates vs. benzodiazepines.
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.
Term
Barbituates and Benzos induce tolerance because they work right away. Why do these drugs have an abuse potential?
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.
Term
How does CNS depression manifest with sedative-hypnotics?
Definition
drowsiness, motor incoordination, impaired cognition, disinhibition, sleep driving.
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
Term
What is Midazolam used for?
Definition
anticonvulsive therapy (very short acting) or preananesthesia
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.
Term
Why would you not give Flurazepam to the elderly?
Definition
Due to its long half life
Term
What are some important pharmakokinetics of benzos?
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
Term
Which drug is frequently given as a muscle relaxant?
Definition
Diazepam
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
Term
Can BZ-1s be used as muscle relaxants, anesthesia or anticonvulsant?
Definition
No
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.
Term
Why are barbiturates particularly dangerous when taken with other drugs?
Definition
They are strong inducers of many microsomal enzymes including UGT
Term
What would you give to a patient with Hyperbilirubinemia? How ould the drug work?
Definition
Barbiturates. Phenobarbital induces UGT1A1 which clears out the bilirubin
Term
Which sedative is absolutely contraindicated in acute intermittent porphyria?
Definition
Barbiturates
Term
Which drug is an M1, M2 receptor agonist and binds to suprachiasmic region of hypothalamus to regulate circadian rhythms?
Definition
Ramelteon (Rozerem)
Term
Which drug is similar to BZs but has a higher potential for abuse?
Definition
Meprobamate
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
Term
What would be a good sleeping agent for a patient who has never taken benzos?
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.
Supporting users have an ad free experience!