CNS Depressants and Stimulants

Question 1

Target for many anxiolytics and sedative-hypnotics

Answer 1

GABA A receptor

Question 2

Drugs that act on the GABA A receptor

Answer 2

Benzodiazepines
Triazolobenzodiazepines
Nonbenzodiazepines (Z-Drugs)

Question 3

Ramelteon (Rozerem)

Answer 3

Melotonin receptor agonist

Readjusts the circadian rhythm

Question 4

Barbiturates

Answer 4

Bind to allosteric site of GABA A receptor

Have been replaced by benzodiazepines, which are safer

Question 5

Potency of alcohols

Answer 5

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

Question 6

System that antipsychotics act on

Answer 6

Dopamine system: dopamine D2 receptor

Question 7

Phenothiazines

Answer 7

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

Question 8

Benzazepines

Answer 8

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

Question 9

Fluorobutyrophenones

Answer 9

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

Question 10

Lithium salts

Answer 10

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

Question 11

Analeptics

Answer 11

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

Question 12

Methylxanthines

Answer 12

Caffeine, theophylline, theobromine

CNS-stimulant activity: inhibition of adenosine A1 and A2A receptors

Question 13

Most potent of methylxanthines

Answer 13

Caffeine (most lipophilic)

Question 14

Central sympathomimetic agents

Answer 14

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

Question 15

How to increase CNS activity of central sympathomimetics

Answer 15

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

Question 16

Tricyclic antidepressants: methyl vs. dimethyl substitution to amino group

Answer 16

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

Question 17

Classes of hallucinogens

Answer 17

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