Medicinal Chemistry of Antidepressants

A set of vocabulary flashcards covering key concepts from the medicinal chemistry of antidepressants.

Antidepressant

A class of drugs used to treat mood disorders such as depression.

Reuptake Inhibition

The process of blocking neurotransmitters from being reabsorbed into the presynaptic neuron, increasing their availability in the synaptic cleft.

SSRI

selective serotonin reuptake inhibitor - inhibits the reuptake of serotonin into the synaptic cleft (fluoxetine, citalopram, escitalopram, sertraline, paroxetine)

MAOi

Monoamine oxidase inhibitors - inhibit the monoamine oxidase enzyme, increasing levels of serotonin and norepinephrine (phenelzine, tranylcypromine, isocarboxazid)

TCA

Tricyclic antidepressants - inhibit reuptake norepinephrine and serotonin (imipramine, desipramine, amitriptyline)

SNRIs

Serotonin norepinephrine reuptake inhibitors - inhibit serotonin and norepinephrine reuptake (venlafaxine, desvenlafaxine, duloxetine, atomoxetine)

Tertiary Amine TCAs

Typically more selective for serotonin, more potent than secondary amines and are more likely to cause anticholinergic effects, sedation, and hypotension. Examples include amitriptyline and imipramine. They are called tertiary amines because they have three alkyl groups attached to the nitrogen atom. some alpha blocking activity and may cause cardiovascular side effects. Long half-life and have active metabolites

Secondary Amine TCAs

Typically more selective for norepinephrine. Less sedating than tertiary amine TCAs. Examples include desipramine and nortriptyline. Some alpha blocking activity which may lead to cardiovascular side effects. Long half-life and have active metabolites

Serotonin Reuptake Transporter (SERT)

The protein responsible for the reuptake of serotonin from the synapse.

Norepinephrine Reuptake Transporter (NET)

The protein responsible for the reuptake of norepinephrine from the synapse.

Active Metabolite

A metabolite that retains pharmacological activity, contributing to the effects of the parent drug.

Antimuscarinic Effects

Side effects related to the blockade of muscarinic acetylcholine receptors M1, causing symptoms like dry mouth, urinary retention, and constipation.

S-enantiomer

The specific active isomer of a chiral drug. It often exhibits distinct pharmacological properties compared to its R-enantiomer.

Catecholamines

A class of neurotransmitters that includes norepinephrine and dopamine.

Phase 2 Metabolism

Biochemical reactions that make drug metabolites more water-soluble for excretion.

Steric Factors

Spatial considerations in molecular interactions that influence drug binding and efficacy.

Pharmacophore

The part of a molecule responsible for its biological activity.

Enantiopure Drug

A formulation that contains only one enantiomer of a chiral compound.