Adverse Effects, Drug Interactions, and Special Populations
Module 7 — Chapter 17: Antidepressant Drugs
Discontinuation Syndrome — FINISH Mnemonic and Risk by Agent
- F — Flu-like symptoms: myalgia, fatigue, sweating, chills
- I — Insomnia: vivid dreams, nightmares, disrupted sleep
- N — Nausea (and vomiting)
- I — Imbalance: dizziness, gait unsteadiness
- S — Sensory disturbances: "brain zaps" — electric-shock sensations from the head (pathognomonic)
- H — Hyperarousal: anxiety, agitation, irritability
- Highest: Paroxetine (shortest half-life, no active metabolite, anticholinergic rebound) and venlafaxine immediate-release (very short half-life)
- Intermediate: Sertraline, citalopram, escitalopram, duloxetine
- Lowest: Fluoxetine — norfluoxetine active metabolite provides inherent self-tapering over weeks
- Brain zaps distinguish discontinuation syndrome from relapse; relapse does not produce sensory disturbances
High-Yield Cytochrome P450 Drug Interactions
| Antidepressant |
Enzyme Inhibited |
High-Risk Victim Drug |
Clinical Consequence |
| Fluoxetine, Paroxetine |
Cytochrome P450 2D6 (potent) |
Tamoxifen |
Reduced endoxifen (active metabolite) → reduced breast cancer efficacy — use alternative selective serotonin reuptake inhibitor |
| Fluoxetine, Paroxetine |
Cytochrome P450 2D6 (potent) |
Tricyclic antidepressants, antipsychotics, codeine |
Elevated levels → toxicity risk (tricyclic antidepressants); reduced analgesia (codeine) |
| Fluvoxamine |
Cytochrome P450 1A2 (potent) |
Clozapine, olanzapine, theophylline |
3-fold or more increase in clozapine levels → seizures, cardiotoxicity; theophylline toxicity |
| Fluvoxamine, Fluoxetine, Paroxetine |
Cytochrome P450 2C9 |
Warfarin (S-enantiomer) |
Elevated international normalized ratio — check within 2 weeks of starting or changing dose |
| St. John's Wort |
Cytochrome P450 3A4 inducer + weak serotonin reuptake transporter inhibition |
Prescription antidepressants |
Reduces antidepressant levels + additive serotonergic risk — avoid combination |
Special Populations — Prescribing Principles
- Untreated depression carries its own fetal risks — weigh against medication risk
- Preferred: sertraline and escitalopram (most safety data, lowest placental transfer)
- Avoid paroxetine when possible (cardiovascular malformation signal)
- Neonatal adaptation syndrome in ~30% of third-trimester-exposed neonates — transient, resolves in 2 weeks
- Black-box warning for suicidality applies regardless of pregnancy
- Key measure: relative infant dose (infant weight-adjusted dose as percent of maternal dose)
- Sertraline: lowest relative infant dose — preferred first choice
- Paroxetine: also low relative infant dose — acceptable
- Fluoxetine: higher relative infant dose plus long neonatal half-life (norfluoxetine) — avoid when alternatives exist
- Individualize based on maternal illness severity and infant age
- Start at half adult dose; titrate slowly
- Avoid tertiary tricyclic antidepressants (Beers Criteria) — anticholinergic burden, fall risk
- Preferred: escitalopram or sertraline
- Citalopram maximum 20 mg per day in patients over 60 (QTc risk)
- Monitor sodium at baseline and 4 weeks (syndrome of inappropriate antidiuretic hormone secretion risk several-fold higher)
- Check orthostatic blood pressure — alpha-1 blockade causes falls
Serotonin Syndrome versus Neuroleptic Malignant Syndrome
Serotonin syndrome: rapid onset (hours), clonus and hyperreflexia, serotonergic drug combination, treat with cyproheptadine and benzodiazepines. Neuroleptic malignant syndrome: slow onset (24 to 72 hours or more), lead-pipe rigidity and bradyreflexia, dopamine antagonist precipitant, treat with bromocriptine and dantrolene. Clonus is the key distinguishing finding.