moclobemide

Absorption: 98% absorbed following oral administration, but undergoes first-pass hepatic metabolism, resulting in 90% bioavailability.

Distribution: Unknown.

Metabolism/Excretion: Extensively metabolized (partially by CYP2C19 and CYP2D6); very small amounts are pharmacologically active; <1% excreted unchanged in urine.

Half-Life: 1.5 hr (↑ with dose).

Time/Action Profile ⬆ ⬇

ROUTE	ONSET	PEAK	DURATION
PO	days–several wk (antidepressant effect)	0.5–3.5 hr (plasma concentrations)	24 hr (MAO-A inhibition)

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
Acute confusional states;
Concurrent use of tricyclic antidepressants;
Concurrent use of SSRIs or other MAO inhibitors;

Use Cautiously in:

History of suicide attempt or ideation;
History of thyrotoxicosis or pheochromocytoma (possible risk of hypertensive reaction);
Renal impairment;
Severe hepatic impairment (↓ dose);
OB: Safety and effectiveness not established in pregnancy;
Lactation: Safety and effectiveness not established in breastfeeding;
Pedi: Safety and effectiveness not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

CV: hypotension

Neuro: agitation, insomnia, restlessness, SUICIDAL THOUGHTS/BEHAVIORS, tremor

Interactions ⬆ ⬇

Drug-drug:

Selegiline greatly ↑ sensitivity to tyramine; concurrent use contraindicated.
Tricyclic antidepressants may result in severe adverse reactions; concurrent use contraindicated.
Should not be used with SSRIs or other MAO inhibitors; when making a switch, allow 4–5 half-lives of previous drug; for fluoxetine, wait ≥5 wk.
May ↑ levels of and risk of QT prolongation with thioridazine; avoid concurrent use.
Excessive alcohol should be avoided.
Cimetidine may ↑ levels and risk of toxicity; ↓ moclobemide dose by 50%.
Because of the potential for interactions with anesthetics, especially local anesthetics containing epinephrine, moclobemide should be discontinued ≥2 days before procedures.
Concurrent use with opioids should be avoided; dosage adjustments may be necessary.
Sympathomimetics, including ephedrine and amphetamines, may ↑ BP; avoid concurrent use.
Dextromethorphan may ↑ risk of vertigo, tremor, nausea, and vomiting; avoid concurrent use.
Antihypertensives may ↑ risk of hypotension.

Drug-Food:

Ingestion of large amounts of tyramine-containing foods, including some cheeses and Marmite yeast extract, may result in hypertension and arrhythmias.

Route/Dosage ⬆ ⬇

PO (Adults ): 150 mg twice daily initially; may ↑ gradually after one wk, as needed/tolerated (max = 600 mg/day).

Hepatic Impairment

PO (Adults ): Severe hepatic impairment or concurrent use of cimetidine: ↓daily dose to ⅓–½ of standard dose.

Availability ⬆ ⬇

Tablets: 100 mg; 150 mg; 300 mg

Assessment ⬆ ⬇

Monitor BP and HR before and frequently during therapy. Report significant changes promptly.
Monitor mood changes. Assess for suicidal tendencies, especially during early therapy. Restrict amount of drug available to patient.
Monitor intake and output and daily weight. Assess for peripheral edema and urinary retention.

Lab Test Considerations:

Monitor liver and kidney function periodically during treatment.
- Monitor serum glucose closely in patients with diabetes; hypoglycemia may occur.

Toxicity and Overdose:

Concurrent ingestion of tyramine-rich foods and many medications may result in a life-threatening hypertensive crisis. Signs/symptoms of hypertensive crisis include chest pain, tachycardia, severe headache, nausea and vomiting, photosensitivity, and enlarged pupils. Treatment includes IV phentolamine.
- Symptoms of overdose include anxiety, irritability, tachycardia, hypertension or hypotension, respiratory distress, dizziness, drowsiness, hallucinations, confusion, seizures, fever, and diaphoresis. Treatment includes induction of vomiting or gastric lavage and supportive therapy as symptoms arise.

Implementation ⬆ ⬇

PO: Administer after meals.DNC: Swallow tablet whole. Do not crush, break, or chew. Dose may be adjusted gradually during the 1st wk of therapy.

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication to patient. Advise patient to read Patient Information before starting therapy. Advise to take as directed. Take missed doses if remembered unless almost time for next dose; do not double doses. Do not discontinue abruptly; withdrawal symptoms (nausea, vomiting, malaise, nightmares, agitation, psychosis, seizures) may occur.
Advise patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care provider before taking other medications.
Advise patient to avoid alcohol, CNS depressants, OTC drugs, and foods or beverages containing tyramine (see Food Sources for Specific Nutrients) during and for ≥2 wk after therapy has been discontinued; they may precipitate a hypertensive crisis. Contact health care provider immediately if symptoms of hypertensive crisis develop.
Advise patient to notify health care provider if neck stiffness, changes in vision, diarrhea, constipation, rapid/pounding heartbeat, sudden and severe headache, stiff neck, confusion, disorientation, slurred speech, behavioral changes, or seizures occur.
Advise patient, family, and caregivers to notify health care provider if thoughts about suicide or dying, attempts to commit suicide, new or worse depression, new or worse anxiety, feeling very agitated or restless, panic attacks, trouble sleeping, new or worse irritability, acting aggressive, being angry or violent, acting on dangerous impulses, an extreme ↑ in activity and talking, or other unusual changes in behavior or mood occur.
Advise patient to carry identification describing medication regimen.
Rep: Advise women of reproductive potential to notify health care provider if pregnancy is planned or suspected or if breastfeeding.

section name header

Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇