antidepressants Flashcards
What are the key monoamine oxidase inhibitors? Do they inhibit type A or B?
Phenelzine – MAO-A and MAO-B
Tranylcypromine – MAO-A and MAO-B
Selegiline – MAO-B at low doses
What are the MAOIs used therapeutically for?
Atypical depression, treatment-resistant depression, treatment-resistant anxiety disorders (panic disorder and social anxiety disorder)
What are the major side effects of the MAOIs?
Orthostatic hypotension, weight gain, insomnia, sexual dysfunction and hepatoxocity (rare)
What are the signs of serotonin syndrome?
vomiting, diarrhea, sweating, hyperthermia, tachycardia, hypertension, tremor, myoclonus, rigidity, hyperreflexia. People can die from this.
What drugs should you avoid with MAOIs to avoid serotonin syndrome? To avoid a hypertensive crisis?
Serotonin syndrome: SSRIs, tryptophan, dextromethorphan, tramadol, meperidine
Hypertensive crisis: noradrenergic drugs (ephedrine, pseudoephedrine, phenylephrine, amphetamines), appetitie suppressants, TCAs, SNRIs, buproprion, and food that are high in tyramine (soy, aged cheese, red wine, beer, fava beans, smoked fish and liver).
What are the key tricyclic antidepressant drugs?
Amitriptyline, nortriptyline, imipramine, desipramine, clomipramine
What are the TCAs used therapeutically for?
Major depressive disorder, childhood enuresis (imipramine), anxiety disorders (GAD, panic, OCD), insomnia, neuropathic pain, migraines, fibromyalgia
What receptors do TCAs block?
Presynaptic reuptake of norepi and serotonin, muscarinic receptors, Na channels, histamine receptors, adrenergic alpha 1 receptors
What are the side effects of TCAs based on the receptors they block?
Muscarinic receptors in parasympathetic system – dry mouth, urinary hesitancy, constipation, tachycardia
Muscarinic receptors in the brain – memory impairment, drowsiness, delirium
Histamine receptors in the brain – drowsiness and weight gain
Na channels – heart block, ventricular tachycardia
Adrenergic alpha 1 receptors – orthostatic hypotension, priapism
Others – seizure
What antihypertensives do TCAs block?
Guanethidine, beta blockers and clonidine
What are the drugs that produce additive effects when combined with TCAs?
Antiarrhythmics (quinidine, amiodarone), QTc prolonging agents, anticholinergics, CNS depressants, sympathomimetics
What are the drugs that increase TCA levels?
Cimetidine, fluoxetine, thiazides, acetazolamide, ritonavir, antifungals
What are the drugs that decrease TCA levels?
Carbamazepine, rifampin, phenytoin, nicotine, barbiturates
What are the key selective serotonin reuptake inhibitor drugs?
Fluoxetine, sertraline, paroxetine, fluxovamine, citalopram, escitalopram
What are the therapeutic uses of SSRIs?
Major depressive disorder, anxiety disorders (GAD, OCD, PTSD, panic), premenstrual dysphoric disorder, bulimia
What are the side effects of SSRIs?
Abdominal cramps, diarrhea, nausea, akathisia/inner feeling of restlessness, extrapyramidal symptoms, sexual dysfunction, weight gain, excessive sweating, bradycardia, thoughts of suicide in young adults/adolescents
Which antidepressant is associated with a Discontinuation Syndrome? What are the symptoms of DS?
SSRIs, particularly paroxetine and fluvoxamine.
Symptoms are dysphoric mood, irritability, agitation, paresthesias, tinnitus, seizures
Which SSRI has the least drug-drug interactions?
citalopram and escitalopram
Which SSRI is not approved for depression? What is it used for instead?
Fluxovamine is not approved for depression but is used for OCD
Which SSRI has the longest-half life/requires the most infrequent dosing?
fluoxetine
What are the serotonin and norepinephrine reuptake inhibitors (SNRIs)? Which one acts like a SSRI at low doses?
Venlafaxine/desvenlafaxine – acts like an SSRI at low doses
Duloxetine – always acts like an SNRI
What are the therapeutic uses for duloxetine?
Pain in diabetic neuropathy, fibromyalgia, osteoarthritis and lower back pain
What is the mechanism of action of buproprion? What is it used for?
Mechanism – weak norepi and dopamine reuptake inhibitor, inhibitor of nicotine acetylcholine receptors
Used for major depressive disorder, seasonal affective disorder, smoking cessation and ADHD (off-label)
What is trazodone used for?
Sleep aid because it is very sedating
What are the side effects of trazodone?
Sedation (primary purpose, not side effect), orthostatic hypotension, priapism
What is the mechanism of action of mirtazapine? What is it used for?
Blocks many of the 5HT receptors except the 5HT1A receptors so all the serotonin is directed at the 5HT1A receptors which causes antidepressive and anxiolytic effects. It also is an adrenergic alpha-2 antagonist -> increased norepi release
