Antidepressants & Mood Stabilizers Flashcards
Impramine Amytriptyline Despiramine Nortriptyline Doxepin Clomiphene Amoxapine
MOA AND USES
MOA: Tricyclic Antidepressant
useful for major depression, chronic pain, OCD
impramine: bed-wetting
desipramine: least anticholinergic
Clomipramine: OCD
Amitrytyline: neuropathic pain, migraine
Amoxapine: some d2 blockade
Impramine Amytriptyline Despiramine Nortriptyline Doxepin Clomiphene Amoxapine
TOXICITY
Antimuscarinic: mydriasis, cycloplegia, urinary retention, sedation.
Alpha-1 block: hypotension, orthostasis
Histamine 1 block: sedation, weight gain
Overdose: coma, convulsion, cardiotoxicity. Sodium bicarbonate attaches to sodium channel to decrease CV effects
CYP drug interactions
CYP2D6 polymorphism associated with slow metabolism of TCAs
Serotonin Syndrome
Bupropion MOA, Usefulness and Toxicity
MOA: reuptake inhibition of DA & NE. noncompetitive antagonist at nicotinic receptor (smoking cessation)
Verenicline: partial nicotinic receptor agonist (erratic behavior, suicide). not related to bupropion mechanism
Uses: Major depression & smoking cessation
Toxicity: Lower seizure threshold, caution in bulimic pts. No sexual dysfunction. Little M, H1 effects.
Mirtazapine MOA, Usefulness & Toxicity
MOA: Alpha 2 block, increased NE and 5-HT release. opposite clonidine mechanism.
Uses: major depression sedation.
Weight gain, sedation
Duloxetine
Venlafaxine
Desvenlafaxine
Milnacipran
MOA, USES, & TOXICITY
MOA: 5-HT-NE reuptake inhibitors SNRI
Uses: Major depression, chronic pain, fibromyalgia, neuropathic pain
Toxicity: Mechanism like tricyclics. no blockade of h1, alpha 1, M
Fluoxetine Fluvoxamine Citalopram Paroxetine Sertraline Escitalopram
MOA & USES & TOXICITY
MOA: SSRI; takes 4 weeks for full effect
Uses: major depression, anxiety, panic, OCD, post-traumatic stress disorder, premenstrual dysphoric disorder, bulimia, social phobias
Toxicity: insomnia, headache, nausea, vomiting, bleeding abnormalities (platelets), impotence (tx with PDE5 inhibior), Serotonin Syndrome, Drug interactions (mostly with fluoxetine CYP450 2D6; sertraline, citalopram, and escitalopram)
Trazodone
Nafazodone
USES, MOA, TOXICITY
MOA: serotonin reuptake inhibitor and blocker (SARI); also alpha1 and h1 block.
USES: major depression, sedation, sleep aid
Toxicity: alpha1 block (priapism), h1 block (sedation), increased levels of trazadone with inhibitors of CYP3a4, nefedazone (hepatotoxic)
Phenelzine
Tranylcypromine
Isocarboxazid
MOA, USE, & Toxicity
MOA: MAOI-a, selegiline (MAOI-b, DA) treatment for PD.
uses: refractory depression
Tox: HTN with tyramine-containing foods or sympathomimetics (cold medicine), tyramine foods: aged cheese and meats, red wine, chocolate, avocado. Serotonin Syndrome (SSRIs, TCAs, meperidine, dextromethorphan, triptans, linezolid, St. John’s Wort)
Lithium MOA, Use, & Tox
MOA: blocks NE adenylyl cyclase signaling
Use: bipolar disorder
Tox: sodium loss promotes lithium reabsorption (toxicity with diuretics), NSAIDs, ACEI facilitate lithium reabsorption in PCT, Amiloride enhances Li+ secretion, narrow therapeutic index (1.5meq vs. 2 meq), tremors (tx. beta blocker), leukocytosis, polyuria, polydipsia (loss of ADH response), amiloride benefit here, hypothyroidism, abstain anomaly (use lamatrogine in pregnancy.)
Valproate MOA, Use, Tox
MOA: broad-spectrum: blocks Na+ channels and T-type Ca+ channels, decrease glutamate at NMDA receptors, increases GABA at receptor action, increases GABA synthesis, blocks degradation of GABA.
Use: Use: tonic-clonic and partial seizures, absence, migraine prophylaxis, alternative to lithium in bipolar mania
Use: Use: tonic-clonic and partial seizures, trigeminal neuralgia, bipolar dx.
Carbamazepine MOA, Use, Tox
MOA: blocks sodium channels, blocks NE reuptake
Use: Use: tonic-clonic and partial seizures, trigeminal neuralgia, bipolar dx.
Tox: drowsiness, ataxia, diplopia, SIADH (water intox), aplastic anemia, teratogen (NTD), Stevens-Johnson Syndrome (HLA allele in ethnic pop.), inducer of CYP3A4
Lamatrogine MOA, Use Tox
MOA: potentiates GABA, blocks voltage-gated sodium channels, glutamate blockade.
Use: partial tonic-clonic and absence seizures, manic phase of bipolar disorder, lennox-gastaut syndrome
Tox: black box warning, Stevens-johnson syndrome= rash, CNS effects
Atypical Antipsychotics
5-HT»_space;>D2; D3 & D4 block
increase DA release to relieve neg symptoms (positive too) of psychosis.
few extrapyramidal effects (EPS), hyperprolactinemia
all prolong QT interval–aripiprazole, olanzapine, quetiapine, risperidone, ziprasidone, all approved for mania
Risperidone MOA, Use, & Tox
5HT»»D2; D3 & D4 block
Tox: hypotension from alpha1 blockade, increase prolactin, hyperlipidemia, hyperglycemia
Olanzapine MOA, Use & Tox
Blockade of 5-HT2A > H1>D4>D2>alpha1>D1
Use: approved in combo with fluoxetine for mania
Tox: less ANS effects. Fewer extrapyramidal effects (EPS) weight gain, sedation.
