Sedative Hypnotics - I

Question 1

What are the 4 therapeutic effects of Benzodiazepines?

Answer 1

1. Anti-convulsants
2. Muscle relaxants
3. Anti-anxiety
4. Sedative / hypnotic

Question 2

Describe catalepsy.

Answer 2

Rigidity of the limbs

Question 3

Define sedative.

Answer 3

An agent with the ability to calm or reduce anxiety with mild depression of the cerebral cortex.

Question 4

Define tranquilizer.

Answer 4

An agent that reduces anxiety without the loss of consciousness, where the hypothalamus and reticular formation function are depressed.

Question 5

Fill in the missing steps of the sequence of signal tranduction events: Benzodiazepines bind to GABA-A receptors –> Conformational change in the receptor –> __1__ –> Membrane hyperpolarization –> __2__

Answer 5

1. GABA mediated Cl- influx increased

2. Neuronal firing decreased

Question 6

____ determines the rate of entry across the blood-brain-barrier.

Answer 6

Lipid solubility

Question 7

List all ways Benzodiazepines can be administered.

Answer 7

Orally, IV, IM

Question 8

True or False: Benzodiazepines induce CYP-450.

Answer 8

FALSE: Benzodiazepines do NOT induce CYP-450.

Question 9

True or False: Benzodiazepines, like Barbiturates, are likely to cause respiratory depression, coma, and death.

Answer 9

FALSE: the occurrence is rare with Benzodiazepines

Question 10

Which of the following causes irritation on IM injection: Diazepam or Midazolam?

Answer 10

Diazepam

Question 11

Which of the following has these therapeutic uses, Diazepam or Midazolam: anticonvulsant, tranquilizer, and muscle relaxant?

Answer 11

BOTH

Question 12

Which of the following is more potent: Diazepam or Midazolam?

Answer 12

Midazolam

Question 13

At what pH is Midazolam water soluble?

Answer 13

pH less than 4

Question 14

At a higher pH, Midazolam is lipid soluble. How will this affect the drug crossing the blood-brain-barrier?

Answer 14

More easily crosses

Question 15

What is Flumazenil used for?

Answer 15

To counteract respiratory depression associated with intravenously administered Diazepam

Question 16

List all the ways by which Flumazenil can be administered.

Answer 16

Only IV

Question 17

Describe Flumazenil’s rate of onset and duration of action.

Answer 17

Rapid onset & short duration

Question 18

What are the 2 major uses of Barbiturates?

Answer 18

1. Anesthesia

2. Seizure management

Question 19

What is the mechanism of action of Barbiturates?

Answer 19

Potentiate the actions of GABA by prolonging the duration of chloride channel openings, while also inhibiting the release of acetylcholine, NE, and glutamate.

Question 20

What is the NET RESULT of Barbiturates?

Answer 20

Decreased neuronal excitability

Question 21

Which of the following can act in the absence of GABA: Benzodiazepines or Barbiturates?

Answer 21

Barbiturates

Question 22

In comparison to Benzodiazepines, Barbiturates have a ____ toxicity and ____ margin of safety.

Answer 22

In comparison to Benzodiazepines, Barbiturates have a GREATER toxicity and LOWER margin of safety.

Question 23

True or False: Barbiturates are associated with the “ceiling effect”.

Answer 23

FALSE - no “ceiling effect”

Question 24

What are the unwanted effects associated with Barbiturates?

Answer 24

Respiratory depression, coma, and death at higher doses

Question 25

True or False: Barbiturates are inducers of cytochrome P-450.

Answer 25

TRUE

Question 26

Which species metabolizes barbiturates more quickly, cats or ruminants?

Answer 26

Ruminants (sheep and goats)

Question 27

Which of the following is long acting and which is short acting: Phenobarbital, Pentobarbital?

Answer 27

Long-acting = Phenobarbital

Short-acting = Pentobarbital