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Antidepressants

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alex0624's version from 2016-07-16 22:29

Section 1

Question Answer
Selective Serotonin Reuptake InhibitorsFluoxetine, fluvoxamine, sertraline, paroxetine, citalopram, escitalopram
Block only serotonine reuptake-Causing elevated serotonin levelsSSRIs
is metabolised to active norfluoxetine long elimination half life. Hence it has to be discontinued 4weeks or longer before an MAOI can be administered to reduce risk of serotonin syndromeFluoxetine
if not discontinued can cause Serotonine syndrome because of long half life metabolismFluoxetine
SSRIs that are CYP2D6 inhibitors"Fluoxetine" and paroxetine
SSRIs CYP3A4 inhibitorFluvoxamine
Drug interaction or co-action of Selective Serotonin reuptake inhibitor and MAO iinhibitor may causeSerotonine Syndrome
Major complain for non compliance with SSRIsSexual dysfunction
Weight gain as adverse effectParoxetine
SNRIs drugsVenlafaxine, duloxetine
TCAs drugsAmitriptiline, Desipramine, Doxepin, Imipramine, Nortriptyline, trimipramine, clomipramine, protriptyline
Main difference b/n SNRIs and TCAs?TCAs also acts as a potent antihistamine, Increase adrenergic blocking, and antimuscarinic. Increase Na conductance.
________ are prefered over the TCAs in treatment of MDD and pain syndromes because of their better tolerability.SNRIs(duloxetine, Venlaxafine)
TCA drug that have more affinity to bind to SERT than to NET--> contributing to a better tratment for OCDClomipramine
DOC for obsessive compulsive disorderClomipramine
serotonergic A/E (diarrhea, vomiting) and noradrenergic effects- increase BP and HR, and CNS activation, such as insomnia, anxiety, and agitationSNRIs
Alpha-1 Blockage: orthostatic hypotension, sexual dysfunction, cardiac conduction delays (QT prolongation); Histamine Blockade: weight gain, sedation; Anti cholinergic: Dry mouth, Blurred vision, constipation, urinary hesitancyTCA adverse effect
coma, convulsion, cardiac arrythmias are signs ofTCA toxicity
Increased NE and DA activity. no effect on 5-HT (No sexual dysfunction ). Used for smoking cessation and depression)Bupropion
more NET > SERT inhibitionAmoxapine, maprotiline
antagonism of presynaptic a2 R increase release of NE, 5-HT . Also an antagonist of 5-HT2 and 5-HT3 and is a potent H1 antagonist (sedation)bupropion
bupropion,mirtazapine, amoxapine, and maprotilineTetracyclins and unicyclic antidepressants
Lowers seizure threshold (contraindicated in epilepsy=can develop seizures early on). No sexual dysfunction (unlike SSRI)Bupropion(atypical drug-act on DA)
Adverse effects: Sedation and weight gainMirtazapine
Non selective MAO inhibitorsPhenelzine, Tranylcypromine
Selective MAO-B inhibitorsSelegiline
Act by inhibiting the MAO enzyme responsible for metabolism of the neurotransmitters (NT). Thus increases vesicular storage of NE and 5-HTMAO inhibitors
Cheese reaction Hypertensive Crisis from foods with highTyramine
Tyramine escapes metabolism in MAO inhibited patients , causes more release of NE leading to hypertensive crisisCheese reaction
DOC for cheese reactionPhentolamine
Results from combination of MAOI with SERT inhibitorsSerotonine syndrome
Adverse effects Hyperthermia, Mental Status Changes, seizures, muscular rigidity, tremor, myoclonus, hyperreflexia, Increased muscle creatine kinaseSerotonine syndrome
Drugs that cause Serotonin syndromeDrugs implicated include MAOIs, TCAs, SSRI, meperidine, MDMA ("ecstasy")
DOC or management for Serotonine syndromedantrolene, (muscle relaxant), Antiseizure drugs.
Major depressive disorderSSRIs, SNRIs, 5-HT antagonists, preferred over TCAs because of better tolerability
SSRI/TCABipolar disorder(for depressive phase)
SSRI in combination with litium for Maniac phase of bipolar disorder
Panic disorderVenlafaxine, SSRIs
Obsessive compulsive disorderClomipramine, SSRI(especially fluvoxamine)
Enuresis(bedwtting)Imipramine
ADHDTCA, Atomoxetine
Patients who want to withdraw from nicotine dependence(to quit smoking)Bupropion
Neuropathic pain and fibromyalgiaDuloxetine, TCA
Treatment for GAD , panic attacks, social phobias, post-traumatic stress disorder, bulimia, and premenstrual dysphoric disorderSSRI
Depression results from a deficiency in ammount or function of cortical and limbic Serotonin, Norepinephrine and dopamineMono-Amine Hypothesis
Brain derived neurotropic factor (BDNF) is critical for regulation of neural plasticisty and neurogenesis. In depression there is loss of BDNF in hippocampus Neurotrophic hypothesis:
Will affect VMAT and are not stored causing depletion of monoamines causing depression. Major side effect of reserpine is depression.Reserpine
serotonin and NE reuptake inhibition with effects on multiple receptor system and sodium conductanceTCA
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Section 2

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