Moclobemide


Generic Medicine Info
Indications and Dosage
Oral
Depression
Adult: Initially, 300 mg daily in 2 divided doses; based on patient’s clinical response, gradually increase up to 600 mg daily 1 week after initiating the therapy. To evaluate therapeutic effectiveness, continue for at least 4-6 weeks.

Oral
Social anxiety disorder
Adult: Initially, 300 mg daily; increase to 600 mg daily in 2 divided doses after 3 days. To evaluate therapeutic effectiveness, continue for 8-12 weeks.
Hepatic Impairment
Severe: Reduce to 1/2 or 1/3 of the recommended dose.
Administration
Should be taken with food. Take immediately after meals.
Contraindications
Acute confusional states and phaeochromocytoma. Children. Concomitant administration with drugs that are highly dependent on CYP enzymes for metabolism and clearance for which elevated plasma concentrations are associated with serious adverse effect, drugs that significantly increases the plasma concentration of moclobemide and drugs with serotonergic effect that may be potentiated by moclobemide.
Special Precautions
Patient with suicidal tendency, excitation or agitation, bipolar disorder, schizophrenia or schizophrenic symptom, thyrotoxicosis, cardiac impairment. Avoid abrupt withdrawal. Renal and hepatic impairment. Pregnancy and lactation.
Adverse Reactions
Significant: Serotonin syndrome.
Cardiac disorders: Angina, bradycardia, dyspnoea, extrasystoles, palpitations, tachycardia.
Ear and labyrinth disorders: Tinnitus.
Eye disorders: Blurred vision, photopsia, visual disturbance.
Gastrointestinal disorders: Abdominal pain, bloating, constipation, diarrhoea, dry mouth, dysgeusia dyspepsia, gastritis, heartburn, nausea, vomiting, gingivitis, stomatitis.
General disorders and admin site conditions: Asthenia, cold sensation, irritability, malaise.
Immune system disorders: Urticaria.
Investigations: Increased hepatic enzymes.
Musculoskeletal and connective tissue disorders: Musculoskeletal pain.
Nervous system disorders: Agitation, extrapyramidal symptoms, dizziness, headache, restlessness, paraesthesia.
Psychiatric disorders: Anxiety, confusion, delusion, disorientation, dysarthria, hallucination, insomnia, nervousness, sleep disturbances.
Renal and urinary disorders: Micturition disorders (e.g. dysuria, polyuria, tenesmus).
Reproductive system and breast disorders: Galactorrhoea, metrorrhagia, menorrhagia.
Respiratory, thoracic and mediastinal disorders: Dyspnoea.
Skin and subcutaneous tissue disorders: Rash, pruritus.
Vascular disorders: Hypotension, flushing, hot flushes.
MonitoringParameters
Monitor closely for suicidal thoughts or behaviour during early antidepressant therapy and period of dosage adjustment especially for those with history or suspected with suicidal ideation before initiation of therapy. Monitor blood pressure and liver function regularly.
Overdosage
Agitation, amnesia, convulsions, disorientation, drowsiness, hypertension, nausea, reduced reflexes, slurred speech and vomiting. Management: Supportive treatment. Gastric lavage, induce emesis, administration activated charcoal and correction of fluid imbalances may be considered.
Drug Interactions
Increases the effects of opiates (e.g. morphine, fentanyl, codeine, dextropropoxyphene). Increases the serum plasma concentration of non-selective monoamine reuptake inhibitors (e.g. trimipramine, maprotiline). Reduced renal clearance when concurrently administered with cimetidine. Concurrent use with proton pump inhibitors (e.g. omeprazole) leads to an increased serum plasma concentration of both the proton pump inhibitor and moclobemide.
Potentially Fatal: May increase the hypertensive effect of bupropion. Increased risk of serotonin syndrome with MAOIs (e.g. isocarboxazid, phenelzine, selegiline, tranylcypromine), SSRIs (e.g. escitalopram, fluoxetine, fluvoxamine, paroxetine, sertraline, vortioxetine), serotonin-norepinephrine reuptake inhibitors (e.g. venlafaxine, duloxetine, desvenlafaxine, milnacipran, sibutramine), TCAs (e.g. amitriptyline, amoxapine, clomipramine, desipramine, doxepin, imipramine, nortriptyline, trimipramine), sympathomimetic agents (e.g. amphetamine, ephedrine, pseudoephedrine, phenylpropanolamine), dextromethorphan, pethidine, linezolid and methylene blue. Increases the serum plasma concentration of thioridazine and serotonin receptor agonist (e.g. sumatriptan, zolmitriptan, almotriptan, naratriptan). Increases the risk of toxicity, serotonin syndrome and seizure with tramadol.
Food Interaction
May increase tyramine pressor effect when concurrently administered with large amounts of tyramine-rich food (e.g. certain cheeses, tofu, soybeans, fish, lima beans, coffee). Increased risk of serotonin syndrome with St. John’s wort.
Action
Description: Moclobemide, a short-acting benzamide derivative, reversibly and selectively inhibits the isoenzyme monoamine oxidase type A. This action decreases the metabolism (deamination) of the neurotransmitters serotonin, dopamine and norepinephrine thereby increasing extracellular concentration and availability of these neurotransmitters.
Onset: Depression: Within 1-2 weeks.
Pharmacokinetics:
Absorption: Readily and almost completely absorbed from the gastrointestinal tract. Bioavailability: Approx 55% (single dose); approx 90% (multiple doses). Time to peak plasma concentration: 0.5-3.5 hours.
Distribution: Widely distributed throughout the body. Enters breast milk (low concentration). Plasma protein binding: Approx 50%, mainly to albumin.
Metabolism: Largely metabolised in the liver via oxidative reaction and partly metabolised by CYP2C19 and CYP2D6.
Excretion: Via urine (95% as metabolites; <1% as unchanged drug). Elimination half-life: 2-4 hours.
Chemical Structure

Chemical Structure Image
Moclobemide

Source: National Center for Biotechnology Information (2020). PubChem Compound Summary for CID 4235, Moclobemide. Retrieved September 24, 2020 from https://pubchem.ncbi.nlm.nih.gov/compound/Moclobemide.

Storage
Store below 25°C
MIMS Class
ATC Classification
N06AG02 - moclobemide ; Belongs to the class of monoamine oxidase A inhibitors. Used in the management of depression.
References
Anon. Moclobemide. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 10/09/2020.

Apotex NZ Ltd. Apo-Moclobemide 150 mg and 300 mg Film-Coated Tablets data sheet 17 May 2017. Medsafe. http://www.medsafe.govt.nz/. Accessed 10/09/2020.

Buckingham R (ed). Moclobemide. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 10/09/2020.

Joint Formulary Committee. Moclobemide. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 10/09/2020.

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