A.31. Norepinephrine and serotonin receptor antagonist antidepressants. Agomelatine. Flashcards
what is Trazodone?
Serotonin antagonist antidepressant
mechanism of action of serotonin antagonist antidepressant ( Trazodone)
- Inhibition of post-synaptic 5-HT₂ᴀ in the CNS
- inhibition of serotonin reuptake (SERT)
- with chronic use–>desensitize pre-synaptic 5-HT₁ᴀ autoreceptors–> ↑ serotonin release
what are the indications for giving Trazodone?
major depressive disorders
insomnia (highly sedative) –> “Trazzzodone”
Adverse effects of Trazodone?
priapism orthostatic hypotension (moderate 𝝰₁ blockade)
what is the T1/2 of Trazodone?
short (requires administration 2-3 times a day)
what is Agomelatine
agonist MT₁ and MT₂ receptors in the suprachiasmatic nucleus (melatonin receptors)
what does Agomelatine do?
5-HT₂ and 5-HT₃ receptor inhibition
a side effect of Agomelatine
weight gain
what is Agomelatin used for?
major depressive disorders
what is Tianeptine?
atypical antidepressant
AMPA-R modulator
μ-opioid receptor
what is Tianeptine used for?
major depressive disorders
anxiety
what is Lithium?
ion, mood stabilizer
for bipolar disorder (manic-depressive disease)
What is the mechanism of lithium?
unknown
enters through Na channels–> accumulates intracellularly
important pharmacokinetic property in lithium
narrow therapeutic index
requires monitoring of plasma levels to establish a safe dosage regimen
what drugs ↑ plasma levels of lithium?
NSAID’s
ACE inhibitors
thiazide and loop diuretics (chronic use)
what substances ↓ plasma levels
caffeine, theophylline
increases renal clearance
clinical use of Lithium
- acute treatment of bipolar disorders
2. maintenance therapy - ↓ frequency of mood swings (‘mood stabilizer’)
what agents are usually required at the beginning of lithium treatment?
antipsychotics and/or benzodiazepines
*due to the slow onset of action of lithium
what drugs are used concomitantly during maintenance therapy
antidepressants
what are the adverse effects of lithium
flu-like symptoms
GI distress
Neurotoxicity: tremors, seizures
hypothyroidism and goiter (lithium is a deiodinase inhibitor)
nephrogenic diabetes insipidus (late, usually reversible)
what can Lithium cause if given in pregnancy?
Ebstein’s anomaly
CI in pregnancy
symptoms of acute lithium toxicity
vomiting
hyperreflexia
ataxia
seizures
how do we treat acute lithium toxicity?
discontinuation of the agent
hydration
consider hemodialysis
other drugs used in bipolar disorders
valproate
carbamazepine
(acute and maintenance therapy)
Olanzapine (acute treatment)
drugs that can be used during pregnancy with bipolar disorders
clonazepam
Gabapentin
