EXAM #3: SEDATIVES Flashcards Preview

Pharmacology > EXAM #3: SEDATIVES > Flashcards

Flashcards in EXAM #3: SEDATIVES Deck (38):
1

What is the definition of CNS depression?

Decreased neuronal excitability

2

What are CNS depressants generally used to treat?

1) Anxiety states
2) Sleep disorders

3

List the categories of selective CNS depressants.

Benzodiazepines
Barbiturates
Ethanol

4

List the categories of non-selective/ general CNS depressants.

Antihistamines
Opoid analgesics

5

What is the effect of sedative anxiolytics?

Exertion of a calming effect and relief of anxiety

6

What is the effect of hyponotics?

Production of drowsiness

7

What are the graded dose-dependent effects of the sedative hypnotics?

1) Sedation
2) Sleep
3) Anesthesia
4) Coma
5) Respiratory depression/ death

8

What is a linear slope sedative-hypnotic? Non-linear? Which is safer?

Linear= higher dose leads to increased dose-dependent effects

Non-linear= plateau in dose-dependent effects*

*****Non-linear are SAFER*****

9

What are the indications for sedative-hypnotics (6)?

1) Anxiety
2) Insomnia
3) Amnesia
4) Seizures
5) Ethanol withdrawal
6) Muscle relaxation

10

What suffix is associated with the benzodiazepines?

- "zepam"
- "zolam"

11

What are the three main pathways of benzodiazepine metabolism?

1) Inactive water-soluble glucuronides
2) Weakly active short-lived metabolites
3) Long-lived and active metabolites

12

What benzodiazepines undergo metabolism to inactive water-soluble glucuronides? What is the half-life/ duration of action?

Lorazepam
Oxazepam

*****Short acting*****

13

What benzodiazepines undergo metabolism to weakly active, short-lived metabolites? What is the half-life/ duration of action?

Alprazolam
Triazolam

*****Intermediate-acting*****

14

What role does age play in the metabolism of benzodiazepines?

Hepatic processing SLOWS in the elderly and INCREASES the half-life

15

What is the general mechanism of action of the benzodiazepines?

- Bind GABA-A ion channel (Cl-) at specific binding site increasing opening of GABA channels
- Increased Cl- enters the neuron and is INHIBITORY/ causes HYPERPOLARZIATION

16

What is Alpha-1 GABA agonism associated with?

Sedation
Anti-seizure
Anterograde amnesia

17

What is Alpha 2,3,5 GABA agonism associated with?

Anxiolysis

18

What are the adverse effects of the benzodiazepines?

1) Respiratory depressant
2) Anterograde amnesia
3) Tolerance
4) Dependence
5) Withdrawal

19

What increases the adverse effects of benzodiazepines?

Use with other CNS depressant

20

What drug is strongly associated with anterograde amnesia and is used as a date-rape drug?

Flunitrazepam i.e. Rohypnol/ roofies

21

What drugs when combined with benzodiazepines will cause additive CNS depression?

Ethanol
Opoids
Anti-consulsants
Phenothiazine
Anti-histamines
Tricyclic antidepressants

22

What is the common name for flumazenil? Why is this drug important?

Romazicon

****Can reverse the adverse effects of benzodiazepine overdose*****

23

What is the mechanism of action of Flumazenil?

Competitive inhibitor of benzodiazepines

24

What are the "z-drug" benzodiazepine related drugs?

Newer sedative agents used to treat insomnia

25

What is the mechanism of action of z-drugs?

Agonism of benzodiazepine receptors on GABA-A receptors

26

What are the clinical uses for Barbiturates?

1) Anesthesia
2) Sedative/hypnotic
3) Anticonvulsant
4) Medically induced coma

27

What is the important clinical difference between benzodiazepines and barbiturates?

Barbiturates follow a linear slope and are much less safe

28

What is the mechanism of action of barbiturates? How does this differ from the benzodiazepines?

Barbiturates= increased the duration GABA channel opening

****Benzodiazepines increase the frequency of GABA channel opening****

29

What is the mechanism of action of Ramelteon?

Melatonin receptor agonist

30

What is the clinical use of Ramelteon?

Insomnia-- especially for people that have difficulty falling asleep

31

What is the mechanism of action of Buspirone?

Partial agonist of 5-HT1a receptors (autoreceptors)
- Decreases 5-HT release
- Decreases neuronal excitability

32

What is unique about Buspirone?

NON-SEDATING anxiolytic (long-term/ maintenance)
- Less psychomotor impairment
- Does NOT affect driving skills

33

Where are 5-HT1a receptors located?

Located on the pre-synaptic terminal and INHIBIT release of the NT from the pre-synaptic membrane

34

What is classification 5-HT1a receptors?

Autoreceptors

35

What Beta-Blocker is used to treat anxiety?

Propranolol

36

What facets of anxiety is propranolol treating?

Somatic manifestations of anxiety

37

What antihistamines have a mild sedative effect?

Hydroxyzine
Diphenhydramine

38

What is the oldest ad most commonly used anxiolytic?

Ethanol

Decks in Pharmacology Class (64):