Sedative-Hypnotics

Question 1

What is the difference between sedation & hypnosis?

Answer 1

• Sedation : reduced anxiety & minimal CNS depression
• Hypnosis: envouragement & maintenance of sleep, CNS depression is more pronounced & does not refer to the trance-like state

Question 2

What is the dose-response relationship of Sedative-hypnotic drugs?

Answer 2

• As dose is increased, CNS effects also increase
• CNS effects can increase then maintain its effects at a constant point even if higher doses are given

Question 3

Why do Benzodiazepines have a greater margin of safety?

Answer 3

Even at higher doses, its CNS effects not necessarily progress further

Question 4

What is the relationship of sedation dose to assistance in respiration?

Answer 4

As u increased sedation dose, the need for assistance in respiration also increases because of the increase in level of sedation.

Question 5

What are the different levels of sedation?

Answer 5

• Minimal Sedation: Normal response to verbal stimulation, unaffected airway, CVS, & spontaneous ventilation
• Moderate sedation: Responsiveness is purposeful + responds to verbal & tactile stimulation, no intervention required for airway, adequatew spontaneous ventilation, maintained CVS
• Deep sedation: Responsiveness is purposeful ff repeated or painful stimulation, inervention for airway may be required, inadequate spontaneous ventilation, maintaned CVS
• General anesthesia: unarousable even w/ painful stimulus, airway intervention required, frequently inadequate spontaneous ventilation, CVS may be impaired

Question 6

Why is it important for px undergoing sedation to fast?

Answer 6

they are at risk for pulmonary aspiration

Question 7

What are the fasting recommendations for px undergoing sedation?

Answer 7

• Clear water (water, juice w/o pulp) = 2h
• Breast milk = 4h
• Infant formula, Nonhuman milk, Light meal (non fatty) = 6h
• Fried foods, fatty foods or meat = addtl fasting time like 8hr

Question 8

What are the diff Sedative Hypnotic Drugs?

Answer 8

Benzodiazepines, Barbiturates
Alchohol: ethanol, CHloral hydrate
New drugs: Bispirone (anxiolytic), Suvorexant (Hypnotic), Ramelteon & Tasimelteon (hypnotics)

Others: Clonidine (anti-HTN), antipsychotics, tricyclic depressants, antihistamines

Question 9

What is the distribution characteristic of Sedative-Hypnotic drugs?

Answer 9

• Lipid soluble = allow entry to CNS
• Rapid distribution= terminates CNS effects
• Can cross placenta
• Expressed in breast milk
• Benzodiazepines = extensive protein-binding

Question 10

What metabolized Sedative-Hypnotics in the liver?

Answer 10

P450 CYP3A4

Question 11

Out of all newer hypnotcs, which ones become active metabolites?

Answer 11

Ramelteon
Buspirone

Question 12

What is the difference betw Benzodiazpines & Barbiturates?

Answer 12

• Benzodiazepines: Enhances inhibitory effects of GABA
• Barbiturates: in lower doses, it enhances the inhibitory effects of GABA, in higher doses, it mimics GABA

Question 13

What are different drugs that have agonists in the GABA receptor?

Answer 13

Benzodiazepines
Zolpidem, Zaleplon, Eszopiclone bind with a1 subunit

Question 14

What drug has an antagonist benzodiazepine binding site ligand?

Answer 14

Flumazenil

Question 15

What drug has an antagonist benzodiazepine binding site ligand?

Answer 15

Flumazenil

Question 16

What are the organ level effects of sedation?

Answer 16

Euphoria = general feeling of well-being
Anterograde amnesia = cannot recall events happening during drug’s duration ofa ction

Question 17

What are other organ level effects of sedative-hypnotics?

Answer 17

Hypnosis
Anesthesia
Anticonvulsant effect
Muscle relaxation
Zolpidem, Zaleplon reflexes and internuncial transmission

Question 18

What is the MOA & 1/2 life of Flumazenil?

Answer 18

competitive antagonism at GABA receptor

0/7-1.3 hr

Question 19

What should you look out for when giving Flumazenil?

Answer 19

recurrenec of CNS depression abt an hr of giving Flumazenil

Question 20

What are the AEs of Flumazenil?

Answer 20

• agitation
• confusion
• dizziness
• nausea
• abstinence symptooms in dependent px

Question 21

What is a new anxiolytic that is for relief of anxiety w/ no marked sedation or euphoria?

Answer 21

Buspirone

Question 22

What are other important mechanisms of Buspirone?

Answer 22

does not potentiate CNS actions of other drugs

Question 23

What is the MOA of Buspirone?

Answer 23

partial agonist at 5-HT1A receptor

Question 24

What should u look out for when giving Buspirone?

Answer 24

• not for panic states, only for general anxiety states
• liver dysfunction can decrease clearance

Question 25

What drug interaction with Buspirone should be noted?

Answer 25

Buspirone + **Monoamine Oxidase inhibitors** -> **INC BP**

Question 26

What are the **purposes** of giving Sedative-Hypnotic drugs?

Answer 26

* relief of anxiety * insomnia * sedation & amnesia before and during medical and surgical procedures * tx of epilepsy and seizure states * component of balanced anesthesia (IV) * muscle relaxation in specific neuromuscular disorders * diagnostic aids for tx in psych

Question 27

What are clinical toxicology of sedative-hypnotic drugs?

Answer 27

* **CNS Depression**: severe toxicity * **HSN Reaction**: skin rashes * **Teratogenicity**: Dysmorphic characteristics * **Enhance Porphyrin Synthesis**: Barbiturates are C/I in px with acute intermitted porphyria, variegated porphyria

Question 28

What are the diff alterations in drug response?

Answer 28

* **Tolerance**: Cross-tolerance exists between diff sedative-hypnitics * **Physiologic dependence**: withdrawal symptoms, Cross-dependence is the ability of a substitute similar drug to suppress abstinence symptoms