Antidepressants and Anxiolytics Med Chem Flashcards
What is the most common mood disorder in adults?
Major depressive disorder
Criteria required for diagnosis of major depressive disorder
One or more depressive episodes without a history of manic, mixed or hypomanic episodes
Monoamine hypothesis
Deficiency or imbalances in the monoamine neurotransmitters (serotonin, norepinephrine, dopamine) causes depression
Based on the monoamine hypothesis, increasing which two neurotransmitters could alleviate depression?
Serotonin and norepinephrine
Drugs that selectively increase which neurotransmitter decrease depression?
Serotonin
Hypercholinergic hypothesis of depression
Hyperactivity of cholinergic system and excessive nicotinic receptor activity can lead to depression
Examples of antidepressants with nicotinic acetylcholine receptor inhibitory activity
Bupropion
Nicotinic transdermal patch
Which amino acid is a precursor for serotonin?
Tryptophan
Which enzyme is responsible for serotonin synthesis?
Tryptophan hydroxylase
Which amino acid is a precursor for norepinephrine?
Tyrosine
Which enzyme is responsible for norepinephrine synthesis?
Tyrosine hydroxylase
True or false: For all monoamines, the first synthetic step is rate limiting
True
Serotonin is transported into the vesicles via what?
Vesicular monoamine transporter (VMAT)
Reserpine binds irreversibly to what to inhibit packaging of DA, NE, EPI, and 5-HT into vesicles?
VMAT
What two compounds degrade serotonin?
Monoamine oxidase (MAO) and catechol-O-methyl-transferase (COMT)
MAO inhibitor MOA
Increase serotonin and norepinephrine available in the cytoplasm by blocking the deamination of monoamines via MAO
MAOi contrindications
Concomitant use of: sympathomimetic drugs, other MAOIs, L-DOPA, L-tryptophan, phenylalanine, bupropion, excessive coffee, chocolate intake, high tyramine containing foods, heart failure, general anesthesia, local anesthesia with vasoconstrictors, liver disease
What is the result of MAOi use with high levels of tyramine?
Hypertension