Antidepressants Flashcards
What are the MAOs MOA, uses, AE, and DI?
MOA: inactivates excess NE, dopamine, and serotonin that may leak out of synaptic vesicles when neuron is at rest
- Phenelzine: irreversibly bind MAO-A/B
- Isocarboxazid: irreversibly bind MAO-A/B
- Tranylcypromine: irreversibly bind MAO-A/B
- Selegiline: MAO-B inhibitor and MAO-A at high doses
Uses: tx of depression when unresponsive to other antidepressants; Selegiline Tx early Parkinson’s disease (transdermal)
AE: drowsiness, insomnia, N, orthostatic hypotension, weight gain, muscle pain sexual dysfunction
DI: serotonin syndrome, cheese reaction (pseudoephedrine and phenylpropanolamine)
How can you manage Serotonin Syndrome and Cheese Reaction?
- Serotonin Syndrome: Benzodiazepine (sedation) and Cyproheptadine (serotonin antagonist)
- Cheese Reaction: Phentolamine or Prazosin to manage tyramine-induced HTN
What are the TCAs MOA, AE, and what is used to Tx overdose?
MOA: block SERT and NET
- Amitriptyline
- Nortriptyline
- Clomipramine
- Desipramine
- Imipramine
AE: block alpha-andrenergic, muscarinic, histamine, and cardiac fast sodium channels
OD: Sodium Bicarbonate to reverse conduction block
SSRI MOA, uses, AE?
MOA: inhibit SERT with little other activity
- Citalopram
- Escitalopram
- Fluvoxamine
- Fluoxetine
- Paroxetine
- Sertraline
Uses: DOC depression; OCD, PD, GAD, PTSD, SAD, Premenstrual Dysphoric Disorder, Bulemia, Premature ejaculation
AE: N/D, GI upset; less of the TCAs AE; overdose can cause seizure
SNRIs MOA, uses?
MOA: block SERT and NET without other effects of TCAs
- Venlafaxine: potent inhibitor 5HT uptake, inhibits NE uptake at high doses, weak inhibitor of dopamine uptake
- Duloxetine
Uses: Tx depression when SSRIs are ineffective
NDRIs MOA, uses?
MOA: inhibits NE and dopamine uptake and increase release
- Bupropion
Uses: not associated with sexual dysfunction because it is not serotonergic and smoking cessation; overdose and cause seizures
SARIs MOA, uses?
MOA: weak inhibitors of SERT and NET and also 5HT2 antagonist
- Nefazodone: no longer prescribed bc of hepatotoxicity
- Trazodone: also blocks alpha1 and H1 so extremly sedating and used as a hypnotic
NASSA MOA, uses
MOA: antagonist of central presynaptic alpha2 receptors > enhance release of NE and 5HT; antagonist at 5HT2/3 receptors; H1 antagonist
- Mirtazapine
Uses: may be useful if insomnia or agitation is prominent
What is Antidepressant Discontinuation Syndrome, symptoms, drugs most likely to cause it?
- abrupt discontinuation of antidepressants causing symptoms:
- Anxiety/irritability/tearfulness, dizziness, HA, lethargy, flu-like symptoms, electic-shock sensation, insomnia, N/V/D
- By discontinuation of SSRI/SNRI specifically Paroxetine and Venlafaxine because of short half life
Which classes of antidepressants can be used for chronic pain?
- TCAs and SNRIs mainly for neuropathic pain because block NE and 5-HT
Lithium MOA, Uses, AE?
MOA: uncompetitive inhibitor of inositol polyphosphatase and monophosphatase to block regeneration of inositol
Uses: prophylactically in treating manic-depressive pts and in tx of manic episodes
AE: tremor/sedation/ataxia/aphasia, seizure, weight gain, hypothyroidism, nephrogenic diabetes insipidus, edema, dermatitis, alopecia, leukocytosis; category D
How are the adverse effects of tremor and nephrogenic diabetes insipidus from Lithium treated?
- Tremor: Propranolol or Atenolol
- Nephrogenic Diabetes Insipidus: Amiloride (Thiazides and NSAIDs)
What should be regularly monitored when taking Lithium and what drugs reduce its renal clearance?
- Monitor: Serum lithium concentrations, Thyroid function, Renal function
- Reduce renal clearance: Thiazide, NSAIDs, ACE inhibitors, ARBs