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Pharmacology - Block 3 - Part 2

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davidwurbel7's version from 2016-07-18 00:48

Antidepressant

Question Answer
Theory in which depression results from a deficiency in ammount or function of cortical and limbic Serotonin, Norepinephrine and to a lesser extent dopamineMono-Amine Hypothesis
Theory in which brain derived neurotropic factor (BDNF) is critical for regulation of neural plasticisty and neurogenesis. In depression there is loss of BDNF in hippocampusNeurotyophic Hypothesis
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Question Answer
Fluoxetine, Fluvoxamine, Sertraline, Paroxetine, Citalopram and Escitalopram are examples of this class of drugsSSRIs
Inhibit serotonin transporter (SERT). They block only serotonin (not NE) reuptake leading to elevated serotonin levelsSSRIs
Serotonin and NE reuptake inhibition with effects on multiple receptor system (H1, M, and alpha 1) and sodium conductanceTCA
Inhibit serotonin and norepinenephrine transporters only without any effect on other receptorsSNRIs
Blocks 5-HT 2 receptors but also are weak SERT inhibitors5-HT 2 Antagonists
Tetracyclic and unicyclic antidepressantsAtypical Antidepressants
Inhibits the action of mono-amine oxidaseMAO-Inhibitors
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Question Answer
Fluoxetine is metabolized to this active formNorfluoxetine
This class of drugs are CYP inhibitorsSSRIs
Seen in up to 40% of all patients and is a reason for non compliance with SSRIsSexual Dysfunction
This SSRI is associated with weight gainParoxetine
Venlafaxine, Desvenlafaxine, Duloxetine are examples of this class of drugSNRIs
Amitriptyline, Desipramine, Doxepin, Imipramine, Nortriptyline, trimipramine, clomipramine and protriptyline are examples of this class of drugTricyclic Antidepressants (TCA)
Class of antidepressant drug class that lack the potent antihistamine, adrenergic blocking, and antimuscarinic effectsSNRIs
Class of antidepressant drug class that has potent antihistamine, adrenergic blocking, and antimuscarinic effectsTricyclic Antidepressants (TCA)
Antidepressant drug that has more affinity to bind to SERT than it does to NETClomipramine
Clomipramine can be used along with any SSRIs to treat thisOCD
Side effects include serotonergic A/E (diarrhea, vomiting) and noradrenergic effects- increase BP and HR, and CNS activation, such as insomnia, anxiety, and agitationSNRIs
Side effects include Alpha-1 Blockade: orthostatic hypotension, sexual dysfunction, cardiac conduction delays (QT prolongation), Histamine Blockade: weight gain, sedation, Anti cholinergic: Dry mouth, Blurred vision, constipation, urinary hesitancy, Sexual Dysfunction, Lowers seizure threshold – seizures may occurTricyclic Antidepressants (TCA)
Signs of overdoses of this class of drug include coma, convulsions, cardiac arrhythmiasTricyclic Antidepressants (TCA)
Treatment for TCA overdoseIV Sodium Bicarbonate
Trazadone and Nefazodone are examples of this class of drug5-HT2 Antagonists
This drug causes the adverse effects of mainly sedation and priapismTrazodone
5-HT2 Antagonist that inhibits CYP3A4Nefazodone
Nefazodone inhibits this enzymeCYP3A4
Bupropion, Amoxapine, Maprotiline and Mirtazapine are examples of the class of drugAtypical Antidepressants
Mechanism of action of this drug is increased NE and DA activity. no effect on 5-HT (No sexual dysfunction). Used for smoking cessationBupropion
This drug is contraindicated in persons with epilepsy as it lowers the seizure thresholdBupropion
These drugs NET > SERT inhibitionAmoxapine and Maprotiline
Mechanism of action of this drug is antagonism of presynaptic alpha2 receptors, increase release of NE, 5-HT . Also an antagonist of 5-HT2 and 5-HT3 and is a potent H1 antagonist (sedation)Mirtazapine
This drug antagonism of presynaptic alpha 2 receptor and increases release of NE and5-HT. Also an antagonist of 5-HT2 and 5-HT3 and is a potent H1 antagonistMirtazapine
This drug adverse effects are sedation and weight gainMirtazapine
Phenelzine and Tranylcypromine are examples of this class of drugNonselective MAO Inhibitors
Selegiline is an example of this class of drugSelective MAO –B Inhibitors
Treatment for cheese reaction is thisPhentolamine
The co-administration of SSRIs and MAO-Is may lead to thisSerotonin Syndrome
Clinical findings include Hyperthermia, Mental Status Changes, seizures, muscular rigidity, tremor, myoclonus, hyperreflexia and increased muscle creatine kinaseSerotonin Syndrome
The treatment for Serotonin Syndrome is thisDantrolene and Diazepam
A 5-HT 2 antagonist that can be used to treat Serotonin Syndrome in conjunction with diazepam and dantroleneCyproheptadine
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SSRIs, SNRIs, 5-HT antagonists, preferred over TCAs because of better tolerability
Bipolar disorder(for depressive phase) SSRI /TCAs in combination with Lithium (for maniac phase)
Panic disorder- SSRIs, venlafaxine
Obsessive compulsive disorder- clomipramine, SSRI(especially fluvoxamine)
Enuresis (bedwetting)- Imipramine
Attention deficit hyperactivity disorder(ADHD)- TCAs and Atomoxetine
Patients who want to withdraw from nicotine dependence(to quit smoking)- Bupropion
Neuropathic pain and fibromyalgia- Duloxetine, TCA
GAD , panic attacks, social phobias, post-traumatic stress disorder, bulimia, and premenstrual dysphoric disorder- SSRI

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