Mechanism of action and pharmacokinetics
Apomorphine acts as a centrally acting emetic. Its main pharmacological target is the $D_2$ receptors of the vomiting center trigger zone. The drug exerts a direct stimulating effect on them.
In terms of pharmacokinetics, the drug is characterized by rapid penetration into the CNS. With standard subcutaneous administration, the latency period is very short: a pronounced vomiting reflex occurs within just 5–10 minutes.
Elimination of the drug from the body proceeds in two stages: first, metabolism occurs in the liver, after which the resulting metabolites are excreted by the kidneys.
Indications for use
In modern clinical practice, emetics are used quite rarely; however, Apomorphini hydrochloridum has two strict niches for prescription:
- Acute poisoning. The drug is used for the emergency and rapid removal of poison from the stomach. This is especially relevant in situations where traditional gastric lavage via a tube is technically impossible or difficult for any reason.
- Treatment of chronic alcoholism. In narcology, the drug is used as part of conditioned reflex therapy. The essence of the method is to develop a persistent negative conditioned reflex to alcohol: the patient is given alcohol against the background of apomorphine action, which associates the taste and smell of alcohol with agonizing vomiting.
Contraindications
The act of vomiting is a heavy physical load on the body, accompanied by a sharp increase in intrathoracic and intra-abdominal pressure, as well as tension in the muscular framework. In this regard, apomorphine has a number of strict contraindications:
- Severe heart disease (due to the risk of acute decompensation against the background of hemodynamic stress).
- Open forms of tuberculosis and pulmonary hemorrhage (increased intrathoracic pressure can trigger or intensify profuse bleeding).
- Peptic ulcer disease of the stomach and duodenum (intense antiperistaltic contractions pose a threat of ulcer perforation or gastrointestinal bleeding).
- Organic CNS lesions.
Formulations and prescription guidelines
The drug is available as a 1% solution in 1 ml ampoules. It is administered exclusively subcutaneously.
Dosage for adults:
- Average therapeutic dose: 0.002–0.003 g.
- Maximum single dose (MSD): 0.005 g.
- Maximum daily dose (MDD): 0.01 g.
Sample prescription for apomorphine:
Rp.: Sol. Apomorphini hydrochloridi 1% - 1 ml D.t.d. N. 5 in ampull. S. Subcutaneously 0.5 ml to induce vomiting.
Briefly: answers to topical questions
In poisoning with which substances is the use of apomorphine strictly contraindicated or ineffective?
The use of apomorphine is absolutely contraindicated in oral poisoning with corrosive substances — strong acids or alkalis. This is due to the risk of repeated chemical burns to the mucous membranes of the esophagus and respiratory tract during the return passage of the toxin.
APOMORPHINE: Alkaloid Subcutaneously — MOmentary Vomiting Reflex And No poisons.
Class and exam questions
Why is apomorphine administered specifically subcutaneously?
Upon subcutaneous administration, the drug penetrates the CNS as quickly as possible and stimulates $D_2$ receptors. This ensures a short latency period — vomiting occurs within 5–10 minutes.
Is apomorphine a painkiller?
No. Despite being a semisynthetic derivative of morphine, it lacks analgesic activity. Its main effect is emetic.
Why is the drug contraindicated in peptic ulcer disease?
Intense vomiting movements sharply increase pressure in the stomach and cause muscle spasm. This can trigger ulcer perforation or gastrointestinal bleeding.
How is apomorphine eliminated from the body?
Elimination occurs in two stages: first, the drug undergoes metabolism in the liver, and then its metabolites are excreted by the kidneys.
What else to study on this topic
- Topography and physiology of the vomiting center and trigger zone.
- The role of $D_2$ receptors in the central nervous system.
- Antiemetics (dopamine receptor antagonists: metoclopramide, domperidone).
- Principles of emergency care for acute oral poisoning.
- Mechanisms of conditioned reflex therapy in addiction treatment.
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