CNS Depressants and Stimulants Flashcards Preview

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Flashcards in CNS Depressants and Stimulants Deck (17):
1

Target for many anxiolytics and sedative-hypnotics

GABA A receptor

2

Drugs that act on the GABA A receptor

Benzodiazepines
Triazolobenzodiazepines
Nonbenzodiazepines (Z-Drugs)

3

Ramelteon (Rozerem)

Melotonin receptor agonist
Readjusts the circadian rhythm

4

Barbiturates

Bind to allosteric site of GABA A receptor
Have been replaced by benzodiazepines, which are safer

5

Potency of alcohols

Tertiary > secondary > primary
Increases with additional C's (up to 8 total)
Increases with halogenation of short chain molecules
Increases with carbamylation

6

System that antipsychotics act on

Dopamine system: dopamine D2 receptor

7

Phenothiazines

Tricyclic system (6-6-6 system: "Satan drugs")
Traditional antipsychotics (Thorazine, etc.)

8

Benzazepines

Similar in structure to phenothiazines (6-7-6 ring system instead of 6-6-6 ring system)
Less severe side effects than phenothiazines: high serotonin 2A receptor affinity in addition to dopamine D2 receptor

9

Fluorobutyrophenones

Highly potent antipsychotics (Haloperidol, etc.)
D2 and D3 receptor agonists
Some have significant side effects

10

Lithium salts

Antimanic agents
Mechanism of action isn't completely known
Do know that they resemble and take the place of K+, Mg+2, and Ca+2 ions, but can't maintain membrane potential in the same way as Na+ does

11

Analeptics

Convulsants (potent and non-selective CNS stimulants), respiratory stimulants, or narcolepsy treatments

12

Methylxanthines

Caffeine, theophylline, theobromine
CNS-stimulant activity: inhibition of adenosine A1 and A2A receptors

13

Most potent of methylxanthines

Caffeine (most lipophilic)

14

Central sympathomimetic agents

CNS stimulating and anorexiant effects
Resemble norepinephrine
Beta-phenethylamine moiety gives activity

15

How to increase CNS activity of central sympathomimetics

Branch on carbon atom adjacent to amino nitrogen (beta-phenethylamine has no activity, but amphetamine does)
N-methylate (amphetamine -> methamphetamine)

16

Tricyclic antidepressants: methyl vs. dimethyl substitution to amino group

Methyl: stimulatory, greater NE reuptake inhibition, less Ach blocking effects
Dimethyl: sedative, greater 5HT reuptake inhibition, more Ach blocking effects

17

Classes of hallucinogens

Indolethylamines (psilocin)
2-phenylethylamines (mescaline)
Both indoletylamine and phenylethylamine (LSD)