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Antidepressant drugs Pharmacology - Coggle Diagram
Antidepressant drugs Pharmacology
1.Tricyclic antidepressants
Pharmacokinetics
CYP substrates: interactions with inducers and inhibitors ,Long half lives
Toxicities
α block, M block, sedation,weight gain,Overdose arrhymias,seizures
Clinical use
Major depression(backup), chronic pain, obsessive compulsive disorder(OCD)—clomipramine
Mechanism of Action
Block norepinephrine (NE) and 5-HT transporters
Drug
Amitriptyline,
clomipramine,
imipramine, etc
3.Serotonin-norepinephrine reuptake inhibitors (SNRIs)
Clinical use
Major depression, chronic
pain, fibromyalgia, menopausal symptoms
Pharmacokinetics
Half-lives: 10 + h
Mechanism of Action
Block NE and 5-HT transporters
Toxicities
Anticholinergic, sedation,
hypertension (venlafaxine)
Drug
Venlafaxine,
desvenlafaxine,
duloxetine
2.Selective serotonin reuptake inhibitors (SSRIs)
Clinical use
Major depression, anxiety disorders, OCD, PMDDPTSD, bulimia, etc
Pharmacokinetics
CYP 2D6 and 3A4 inhibition n (fluoxetine, paroxetine) 1A2 Fluvoxamine ,Half life +15 hr.
Mechanism of Action
Block 5-HT transporters
Toxicities
Sexual dysfunction
Drug
Citalopram,
fluoxetine,
paroxetine,
sertraline, etc
6. Monoamine oxidase inhibitors (MAOIs)
Pharmacokinetics
Hypertension with tyramine and sympathomimetics, serotonin syndrome with SSRIs,Very long half-lives.
Clinical use
Major depression unresponsive to other drugs
Mechanism of Action
Inhibit MAO-A and MAO-B
Toxicities
Hypotension, insomnia
Drug
Isocarboxazid,
phenelzine,
selegiline
5.Other heterocyclics
Clinical use
Major depression, smokoing cessation (bupropion),
sedation (mirtazepine)
Pharmacokinetics
Extensive hepatic
metabolism
CYP2D6 Inhibition (Bupropian)
Mechanism of Action
Mirtazepine blocks presynaptic α2 receptors
Toxicities
Lowers seizure threshold
(amoxapine, bupropion)
sedation and weight gain
(mirtazepine)
Drug
Amoxapine,
bupropion,
maprotiline,
mirtazepine
4. 5-HT2 antagonists
Clinical use
Major depression, hypnosis (trazodone)
Pharmacokinetics
Usually require bid dosing .CYP3A4 inhibition (nefasodone),
Short half-life.
Mechanism of Action
Block 5-HT2 receptors
Toxicities
Sedation-Modest α and H1 blockade (trazodone)
Drug
Trazodone
Nefazodone