Reboxetine

Oral
Major depressive disorder

Initially, 2 mg bid, may be increased based on patient tolerability.

Initially, 2 mg bid, may be increased based on patient tolerability.

May be taken with or without food.

Concurrent use with or within 2 weeks of stopping MAOIs, including linezolid and methylene blue.

Patient with history of seizure disorder, bipolar disorder, history of suicide-related events or previously exhibiting suicidal ideation, cerebrovascular conditions, hypertension, CV disease (e.g. recent history of MI, unstable heart disease, heart failure), hyperthyroidism, history of urinary retention or prostatic hypertrophy, increased intraocular pressure or at risk of acute narrow-angle glaucoma; predisposition to hypotension (e.g. dehydration, hypovolaemia). Not recommended in patients with narrow-angle glaucoma. Avoid abrupt withdrawal. Renal and hepatic impairment. Elderly. Pregnancy and lactation.

Significant: Suicidal thoughts and behaviour, worsening of depression, shift to mania or hypomania, orthostatic hypotension, mydriasis, increased blood pressure, tachycardia, urinary retention, withdrawal syndrome. Rarely, seizures.
Cardiac disorders: Palpitations.
Ear and labyrinth disorders: Vertigo.
Eye disorders: Accommodation disorder.
Gastrointestinal disorders: Dysgeusia, nausea, vomiting, dry mouth, constipation.
General disorders and administration site conditions: Chills.
Metabolism and nutrition disorders: Decreased appetite.
Nervous system disorders: Akathisia, paraesthesia, headache, dizziness.
Psychiatric disorders: Agitation, anxiety, insomnia.
Renal and urinary disorders: Dysuria, sensation of incomplete emptying of bladder, UTI.
Reproductive system and breast disorders: Erectile dysfunction, ejaculatory pain or delay.
Skin and subcutaneous tissue disorders: Rash, hyperhidrosis.
Vascular disorders: Hypertension, vasodilatation.

This drug may impair judgment or motor skills, if affected, do not drive or operate machinery.

Monitor renal and hepatic function. Closely monitor for signs and symptoms of clinical worsening, suicidal ideation or unusual behavioural changes especially at the start of therapy or during dose adjustments.

Symptoms: Anxiety, postural hypotension, and hypertension. Management: Symptomatic and supportive treatment. Ensure adequate airway, oxygenation, and ventilation. May administer activated charcoal. Monitor cardiac function and vital signs.

May increase plasma concentration with potent CYP3A4 inhibitors (e.g. ketoconazole, nefazodone, erythromycin, fluvoxamine). May decrease serum levels with CYP3A4 inducers (e.g. phenobarbital, carbamazepine, phenytoin, rifampicin). May increase blood pressure with ergot derivatives. May exacerbate orthostatic hypotensive effect with antihypertensive agents. May cause hypokalaemia with K-depleting diuretics.
Potentially Fatal: Increased risk of tyramine-like effect with MAOIs, including linezolid and methylene blue.

Delayed the rate but not the extent of absorption with food. May decrease serum levels with St. John’s wort.

Description: Reboxetine is a selective and potent inhibitor of norepinephrine reuptake and a weak inhibitor of serotonin reuptake. It does not affect dopamine uptake and has no significant affinity for adrenergic (α₁, α₂, β) and muscarinic receptors.
Pharmacokinetics:
Absorption: Well absorbed from the gastrointestinal tract. Delayed the rate but not the extent of absorption with food. Bioavailability: ≥60%. Time to peak plasma concentration: Approx 2 hours.
Distribution: Distributed into total body water. Enters breast milk (small amount). Plasma protein binding: 97%, mainly α₁-acid glycoprotein; 92% (in elderly).
Metabolism: Metabolised primarily in the liver via dealkylation, hydroxylation and oxidation then glucuronide or sulfate conjugation by CYP3A4 isoenzyme.
Excretion: Mainly via urine (78%, 10% as unchanged drug). Elimination half-life: 12-13 hours.

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 127150, Reboxetine mesylate. https://pubchem.ncbi.nlm.nih.gov/compound/Reboxetine-mesylate. Accessed June 24, 2021.

Store below 25°C.

Antidepressants

N06AX18 - reboxetine ; Belongs to the class of other antidepressants.

Anon. Reboxetine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 30/04/2021.

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Edronax 4 mg Tablets (S&M Medical Limited). MHRA. https://products.mhra.gov.uk. Accessed 30/04/2021.

Joint Formulary Committee. Reboxetine. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 30/04/2021.

Pfizer New Zealand Limited. Edronax 2 mg, 4 mg Tablet data sheet 26 February 2019. Medsafe. http://www.medsafe.govt.nz. Accessed 30/04/2021.

Reboxetine 4 mg Tablets (Pfizer Limited). MHRA. https://products.mhra.gov.uk. Accessed 30/04/2021.