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Apomorphine information from DrugsUpdate  

See Available Brands of Apomorphine in India

P - Caution when used during pregnancy
L - Caution when used during lactation

Apomorphine is a non-selective dopamine agonist which activates both D1-like and D2-like receptors, with some preference for the latter subtypes.

Pharmacodynamics

Apomorphine is a morphine derivative with structural similarities to dopamine. It is a dopamine D1- and D2-receptor agonist.

Pharmacokinetics

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.

Apomorphine Indications / Apomorphine Uses

In Erectile dysfunction and in Refractory motor fluctuations in Parkinson's disease.

Apomorphine Adverse Reactions / Apomorphine Side Effects

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.

Special 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.

Other Drug Interactions

Antipsychotics, CNS dopamine inhibitors, antihypertensives, organic nitrates, entacapone and memantine.

Dosage

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.

Over Dosage: Overdosage may result in persistent vomiting, respiratory depression, bradycardia, hypotension and coma; death may occur in severe cases.

List of Contraindications

Apomorphine and Pregnancy

Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Apomorphine and Lactation

Caution when used during Lactation.

Apomorphine and Other 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.

Storage

Subcutaneous: Store at 25°C. Sublingual: Store at 25°C

Apomorphine brands in India:

Zyprima

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