reboxetine (Vestra, Edronax, Prolift, Integrex, Norebox)

Indications

treatment of depression

Contraindications

• concurrent use of MAO inhibitor
  • separate by a 2 week washout

Dosage

• 4 mg PO BID
• in the elderly, start 2 mg BID
• maximum: 12 mg/day

Reduce dose by 50% with renal or hepatic dysfunction

Pharmacokinetics

• metabolized by cyt P450 3A4
• inhibits cyt P450 3A4 & cyt P450 2D6

elimination via liver

elimination via kidney

Adverse effects

• dry mouth
• constipation
• insomnia
• sweating
• vertigo
• urinary hesitancy or retention
• impotence
• sinus tachycardia (> 100/min) > 20% (no other EKG abnormalities)

• drug adverse effects of antidepressants
• drug adverse effects of psychotropic agents

Drug interactions

• reduce reboxetine dose when administered concurrently with inhibitors of cyt P450 3A4
• MAO inhibitors

• drug interaction(s) of benzodiazepines with antidepressants
• drug interaction(s) of antidepressants with benzodiazepines
• drug interaction(s) of NSAIDs with antidepressants

Laboratory

• reboxetine in serum/plasma

Mechanism of action

• inhibition of norepinephrine reuptake (transporter)

More general terms

• atypical antidepressant

Additional terms

• Na+ dependent noradrenaline transporter; norepinephrine transporter; NET; solute carrier family 6 member 2 (SLC6A2, NAT1, NET1, SLC6A5)

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=65856
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5311403
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=127150