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Apomorphine

Apomorphine is a type of aporphine having activity as a non-selective dopamine agonist which activates both D?-like and, to an order of magnitude lesser extent, D?-like receptors. More

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Description

Apomorphine is a type of aporphine having activity as a non-selective dopamine agonist which activates both D?-like and, to an order of magnitude lesser extent, D?-like receptors.

Generic Name

Apomorphine

Chemical names

Apomorphine, Apokyn, Apomorphin, Uprima, L-Apomorphine

Brand names

Zyprima

IUPAC name

(9R)-10-methyl-10-azatetracyclo[7.7.1.0²,?.0¹³,¹?]heptadeca-1(16),2(7),3,5,13(17),14-hexaene-3,4-diol

Pharmacokinetics

  • Absorption: Well absorbed-100% bioavailability after subcutaneous administration
  • Distribution: ~50%-albumin
  • Metabolism: Hepatic
  • Excretion: Urine

Actions

Apomorphine is a type of dopaminergic agonist, in higher doses it is a highly effective emetic. Drugs containing this substance are sometimes used in the treatment of erectile dysfunction or Parkinson's disease. 

Dosage/Dosage form

Initial dose is 2 mg (0.2ml) 3 times a day.

Therapeutic uses

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

Adverse effects/Side effects

Nausea and vomiting; transient sedation; dyskinesia; dizziness; yawning; drowsiness; postural hypotension; CNS stimulation; pharyngitis; increased salivation and perspiration; neuropsychiatric disturbances; eosinophilia; rhinitis; cough; flushing; taste disturbance; vaso vagal syndrome. 

Interaction

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

Contraindications

  • Patients who have an 'on' response to levodopa marked by severe dyskinesia; hypotonia; or psychiatric effects.
  • Respiratory or CNS depression, dementia, neuropsychiatric problems, recent MI, severe heart failure, severe unstable angina, pregnancy, hypotension, breast-feeding. 
  • Combination treatment with other drugs for erectile dysfunction.
  • Hypersensitivity to opioids

Storage

Store at 25°C.

Information

Molecular weight

267.3224

Molecular formula

C17H17NO2

CAS number

58-00-4

Precautions

  • Before starting apomorphine to treat parkinsonism disease, domperidone should be given for at least 2 days before the treatment.
  • Patients with anatomical penile deformity. 
  • Debilitated or elderly patients