Anti-depressants 2 Flashcards
SNRIs do NOT have affect upon
Alpha-1 adrenergic, cholinergic, dopaminergic, or histaminergic receptors
(less side effects, but unique side effects)
Unique side effects of SNRI
Pseudocholinergic effects by stimulating NE or receptors in the SNS
(decrease parasympathetic tone)
Duloxetine inhibits _____ (enzyme)
CYP2D6
SNRI adverse effects (class effects) (5)
- Nausea, dizziness, diaphoresis
- Blood pressure increase
- Headaches
- Sexual dysfunction
- Hyponatremia
In addition to treating depression Duloxetine also treats _____(4)
- Generalized anxiety disorder
- Diabetic peripheral neuropathic pain
- Fibromyalgia
- Chronic musculoskeletal pain
In addition to treating depression, Milnacipran also treats ______
Fibromyalgia
Venlafaxine side effects
sexual dysfunction
(Most likely SNRI to cause this)
Two types of Tricyclic antidepressants
Tertiary or secondary amines
(tertiary has the methyl group)
Tertiary amines effects (2)
- Highly anticholinergic
- Strong serotonin and norepinephrine reuptake inhibitor
(if this becomes too much, try the secondary Amine TCA)
Secondary amine effects (3)
- less anticholinergic
- More potent
- More selective norepinephrine reuptake inhibitor
Tricyclic antidepressant MOA
Serotonin and norepinephrine reuptake inhibitor
TCAs block: (4)
- Blockade of muscarinic M1, H1, alpha-adrenergic 1 receptors
- fast Na Channel in cardiac cells
(they bind to everyhing!)
Which Tri cyclic antidepressants have the best overall tolerability (2)?
- Notriptlyin
- Desipramine
All cyclic antidepressants are potentially _____ toxic
cardio
________ may treat childhood enuresis (bed-wetting)
Imipramine
What are the three C’s of Tri cyclic antidepressants poisoning
- Convulsion
- Cardiac arrest
- Coma
Two types of monoamine oxidase inhibitors
- Hydrazine
- Non hydrazine
Monoamine oxidase is responsible for _____(2)
Breakdown of Serotonin and norepinephrine
The blockade of monoamine oxidase a in the gastrointestinal tract is responsible for the ______ reaction associated w/MOAIs
“cheese reaction” = hypertensive crisis
(A patient taking MOAIs and just foods containing the sympathomimetics tyramine)
MOAIs are metabolized by ______ (process).
acetylation
MOAIs can also be effective in treating ______.
resistant depression
MOAIs have potent ____ effects
hypotensive (leading to dizziness)→risk in treating elderly
(also causes urinary hesitancy, headache and myoclonic jerks)
What is the only antidepressant that is available in a patch?
MAOIs
(Also available sublingually)
Indication of nefazodone
depression
Nefazodone MOA
Antagonize and down regulates postsynaptic serotonin 5-HT2A
Trazodone pharmacokinetics
The table is by CYPT3A4
Trazodone adverse effects
- priapism
- sedation
(dizziness, dry mouth, nausea)
Vilazodone MOA
- Serotonin reuptake inhibitor
- Partial Agonist of 5-HT1A receptor
(side effects: diarrhea, sexual dysfunction)
Vilazodone is metabolized by
CYP3A4
Vilazodone adverse effects
sexual dysfunction
(diarrhea, N/V)
Vortioxetine indications (2)
- Treatment for major depression
- Cognitive dysfunction associated with depression
(metabolized by CYP2D6)
Ketamine MOA
NMDA noncompetitve antagonist → releases BDNF
Ketamine indication
Suicide prevention (when the patient is on the brink; must be given at the doctor’s office); not for regular depression tx
(rapid effect)
Brexanolone indication
Postpartum depression → due to the drop in alopregnenalone
(effect lasts for 30 days, no dissociateive symptoms or risk of abuse)
Brexanalone
- Sedation / somnolence
- Dry mouth
- Loss of consciousness
Duloxetine should be prescribed with caution to patients with the following conditions (4).
- Severe kidney impairment
- Hepatic impairment
- Angle closure glaucoma
- Alcohol abuse
Levomilnacipran side effects
- Not recommended for patients with kidney disease
- Caution with angle closure glaucoma, hypertension or cardiovascular conditions
(at low dose blocks reuptake of NE 2xs more potently than 5-HT)
Milnacipran should be avoided in patients with the following conditions
- End stage kidney disease
- Angle closure glaucoma
- Chronic liver disease
- Alcohol abuse
Venlafaxine should be avoided in patients with the following conditions
- angle closure glaucoma
- patients at risk for bleeding (anticoagulants)
TCA Metabolism & elimination occurs largely in the liver by which enzymes (4)?
- 1A2
- 1C19
- 2D6
- 3A4
Many of the TCA metabolites have _____a ctivity. Desipramine is the active (demethylated) metabolite of _____, and nortriptyline is the active (demethylated) metabolite of ______.
- antidepressant
- imipramine
- amitriptyline
Trazadone use other than antidepressant:
- dyspepsia
- hypnotic
Nefazodone adverse effects is mainly ________.
Acute liver failure
Patients receiving the drug should be monitored for signs and symptoms of liver failure (nausea, abdominal pain, jaundice, impaired synthetic function, coagulopathy, and delirium)
TCA: adverse effects (5)
- Prolonged QT interval
- Tremor
- Bone fracture
- Neuroleptic malignant syndrome (amoxapine)
- Tardive dyskinesia (amoxapine)
Tricyclic antidepressant poisoning: treatment of hypotension
Isotonic crystalloid (vasopressor if necessary, i.e. neosynephrine or norepinephrine are preferred)
Tricyclic antidepressant poisoning: treatment of conduction disturbances
- Challenge with intravenous sodium bicarbonate
- If QRS Narrows, begin continuous infusion (150 mEq of sodium bicarbonate in 1 liter of D5W to run at 250 mL/hour in adults or twice the maintenance fluid rate in children)
Tricyclic antidepressant poisoning: treatment of gastrointestinal issues
Administer activated charcoal if patient presents within 2 hours of ingestion (1 g/kg. maximum dose 50 g)
Tricyclic antidepressant poisoning: treatment of seizures
Benzodiazepine
(do not treat with phenytoin)
Tranylcypromine predominantly an irreversible inhibitor of _____, but also irreversibly inhibits ____to a degree; It also appears to block reuptake of ______ (2).
- MAO A
- MAO B
- erotonin and catecholamines
Tranylcypromine: drug interactions (2)
- interact with sympathomimetics → hypertensive crisis
- interact with serotonin syndrome medications → serotonin syndrome
Phenelzine irreversibly inhibits _____(2).
- MAO A
- MAO B
Phenelzine side effects (3)
- Weight gain
- Sedation
- Sexual dysfunction
(rarely hepatotoxicity, all MAO-Is cause sexual dysfunction, except for selegiline)
All MAO-Is cause sexual dysfunction, except for ______.
Selegiline
Selegiline mechanism of action
Selective MAO B inhibitor; non-selective at higher doses
EMSAM is FDSA approved for use in the treatment of depression. Also available in ______
sublingual forms that bypass both gut and liver metabolism
(this is a form of selegeline; which also comes as a transdermal patch)
