Mechanism of Action and Pharmacokinetics
Apomorphine acts as a centrally acting emetic. Its primary pharmacological target is the $D_2$ receptors of the chemoreceptor trigger zone (CTZ) of the vomiting center, exerting a direct stimulating effect upon them.
From a pharmacokinetic perspective, the drug is characterized by rapid penetration into the CNS. With standard subcutaneous administration, the latent period is very short: a pronounced emetic reflex occurs within just 5–10 minutes.
Elimination occurs in two stages: hepatic metabolism followed by renal excretion of the resulting metabolites.
Indications
In modern clinical practice, centrally acting emetics are rarely used; however, Apomorphini hydrochloridum has two specific clinical niches:
- Acute Poisoning. Used for the emergency and rapid removal of poisons from the stomach. This is particularly relevant when traditional gastric lavage via a nasogastric tube is technically impossible or hindered for any reason.
- Treatment of Chronic Alcoholism. In addiction medicine, the drug is used in aversion therapy. The principle relies on establishing a strong conditioned negative reflex to alcohol: the patient is given alcohol while under the influence of apomorphine, associating the taste and smell of alcohol with severe vomiting.
Contraindications
The act of vomiting is a severe physical stressor accompanied by a sharp increase in intrathoracic and intra-abdominal pressure, as well as significant muscular contraction. Consequently, apomorphine has several strict contraindications:
- Severe heart disease (due to the risk of acute decompensation secondary to hemodynamic stress).
- Active forms of tuberculosis and pulmonary hemorrhage (increased intrathoracic pressure can provoke or worsen profuse bleeding).
- Peptic ulcer disease of the stomach and duodenum (intense antiperistaltic contractions create a risk of ulcer perforation or gastrointestinal bleeding).
- Organic CNS lesions.
Formulations and Administration
The drug is available as a 1% solution in 1 mL ampoules. It is administered exclusively subcutaneously.
Adult Dosing:
- Average therapeutic dose: 2–3 mg (0.002–0.003 g).
- Maximum single dose (MSD): 5 mg (0.005 g).
- Maximum daily dose (MDD): 10 mg (0.01 g).