Apomorphine

Indications
 Sublingual
Erectile dysfunction
Adult: As hydrochloride: 2 mg/dose, approx 20 min before sexual activity, subsequent doses may be increased to 3 mg if necessary with a min of 8 hr between doses.
Max Dosage: 2 mg in severe renal impairment.
Renal impairment: Max dose for erectile dysfunction in severe impairment: 2 mg sublingually.
Subcutaneous
Refractory motor fluctuations in Parkinson's disease
Adult: Test dose: 1 mg followed by a 2nd dose of 2 mg 30 minutes later if needed. Subsequent increments can be made at intervals of at least 40 minutes to determine the lowest effective dose. Once the effective dose is determined, it is given at the 1st signs of an "off" period. Usual dose range: 3-30 mg daily in divided doses. For patients requiring >10 inj/day: may consider continuous SC infusion at 1 mg/hr. May increase in steps of 0.5 mg/hr at intervals of at least 4 hr up to a max rate of 4 mg/hr. Should only be given during waking hr and change infusion site every 12 hr. Intermittent bolus inj may be required to supplement the infusion. Max dose: 100 mg/day and 10 mg/dose.
Renal impairment: Mild-moderate impairment: initial doses should be reduced.
Contraindications
 Respiratory or CNS depression, neuropsychiatric problems, dementia, recent MI, severe unstable angina, severe heart failure, hypotension, pregnancy, breast-feeding. Hypersensitivity to opioids; patients who have an 'on' response to levodopa marked by severe dyskinesia; hypotonia; or psychiatric effects. Combination treatment with other drugs for erectile dysfunction.
Warnings / Precautions
 Debilitated or elderly patients; those with history of postural hypotension; pulmonary, CV or endocrine disease; renal or hepatic impairment, uncontrolled hypertension; patients with anatomical penile deformity. Patients receiving apomorphine and levodopa should be screened for haemolytic anaemia. Domperidone should be given for at least 2 days before starting treatment of parkinsonism with apomorphine.
Adverse Reactions
 Nausea and vomiting; dyskinesia; dizziness; yawning; drowsiness; transient sedation; postural hypotension; neuropsychiatric disturbances; CNS stimulation; increased salivation and perspiration; eosinophilia; rhinitis; pharyngitis; cough; flushing; taste disturbance; vasovagal syndrome. Less frequently syncope, stomatitis and mouth ulcers.
Overdose Reactions
 Overdosage may result in persistent vomiting, respiratory depression, bradycardia, hypotension and coma; death may occur in severe cases.
Drug Interactions
 Antipsychotics, CNS dopamine inhibitors, antihypertensives, organic nitrates, entacapone and memantine.
See Below for More apomorphine Drug Interactions
Mechanism of Actions
 Apomorphine is a morphine derivative with structural similarities to dopamine. It is a dopamine D1- and D2-receptor agonist.
Absorption: SC admin: Well absorbed. Oral: Extensive 1st-pass effect.
Distribution: About 90% bound to plasma proteins, mainly to albumin.
Metabolism: Extensively hepatic metabolism, mainly by conjugation with glucuronic acid or sulfate; also demethylated to form norapomorphine.
Excretion: Most of a dose is excreted in urine, largely as metabolites.
Storage Conditions
 Subcutaneous: Store at 25°C. Sublingual: Store at 25°C.
ATC Classification
 G04BE07 - apomorphine ; Belongs to the class of drugs used in erectile dysfunction.
N04BC07 - apomorphine ; Belongs to the class of dopamine agonist. Used in the management of Parkinson's disease.
Storage
 Subcutaneous: Store at 25°C. Sublingual: Store at 25°C.
Available As
  • Apomorphine 2 mg
  • Apomorphine 3 mg

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