Apomorphine was previously licensed in the UK for erectile dysfunction (ED) under the brand name Uprima, offering a sublingual treatment that worked through a unique central nervous system mechanism. Unlike phosphodiesterase-5 (PDE5) inhibitors such as sildenafil, apomorphine stimulated dopamine receptors in the brain to trigger erectile responses. However, the European marketing authorisation was withdrawn in 2006 due to limited efficacy compared to PDE5 inhibitors and concerns about side effects including nausea and syncope. Apomorphine is no longer licensed or recommended for ED treatment in the UK. Men experiencing erectile dysfunction should consult their GP to discuss currently licensed alternatives recommended by NICE guidance.
Summary: Apomorphine worked for erectile dysfunction by stimulating dopamine receptors in the hypothalamus, triggering neural signals that promoted nitric oxide release and increased penile blood flow, but it is no longer licensed in the UK.
- Apomorphine is a dopamine receptor agonist that acted centrally in the brain, unlike PDE5 inhibitors which work peripherally in penile tissue.
- The sublingual formulation allowed rapid absorption with onset of action within 15–20 minutes, requiring sexual stimulation to be effective.
- European marketing authorisation was withdrawn in 2006 due to limited efficacy compared to PDE5 inhibitors and concerns about nausea and syncope.
- Common side effects included nausea, dizziness, hypotension, and syncope, particularly with postural changes after administration.
- NICE guidance recommends PDE5 inhibitors as first-line pharmacological treatment for erectile dysfunction, not apomorphine.
- Men experiencing erectile dysfunction should consult their GP for currently licensed, evidence-based treatments appropriate to their individual circumstances.
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What Is Apomorphine and How Does It Work?
Apomorphine is a dopamine receptor agonist that was previously licensed in the UK for the treatment of erectile dysfunction (ED) under the brand name Uprima. It represented a novel approach to ED management, offering a sublingual formulation that acted centrally rather than peripherally like phosphodiesterase-5 (PDE5) inhibitors such as sildenafil.
The mechanism of action differs fundamentally from other ED treatments. Apomorphine works by stimulating dopamine D1 and D2 receptors in the hypothalamus, specifically within the paraventricular nucleus. This central nervous system stimulation triggers a cascade of neural signals that travel down the spinal cord to the sacral parasympathetic nuclei, ultimately promoting the release of nitric oxide in the corpus cavernosum of the penis. This nitric oxide release causes smooth muscle relaxation and increased blood flow, facilitating an erection in response to sexual stimulation. Sexual stimulation is required for the medication to be effective.
Unlike PDE5 inhibitors that work peripherally by preventing the breakdown of cyclic guanosine monophosphate (cGMP) in penile tissue, apomorphine's central action means it requires intact neural pathways between the brain and the erectile tissue. The sublingual route of administration allows rapid absorption through the oral mucosa, with onset of action typically within 15–20 minutes.
It is important to note that apomorphine for ED is no longer licensed in the UK. The European marketing authorisation for Uprima was withdrawn in 2006 due to limited efficacy compared to PDE5 inhibitors and concerns about side effects, particularly nausea and syncope. Whilst apomorphine remains available for other indications such as Parkinson's disease, it is not licensed or recommended for erectile dysfunction treatment in the UK.
Effectiveness and Clinical Evidence for Apomorphine
Clinical trials evaluating apomorphine for erectile dysfunction demonstrated modest efficacy compared to placebo, though results were generally less impressive than those achieved with PDE5 inhibitors. In randomised controlled trials, apomorphine at doses of 2–3 mg showed statistically significant improvements in erectile function compared to placebo, though the magnitude of benefit was smaller than that observed with sildenafil or other PDE5 inhibitors.
The International Index of Erectile Function (IIEF) scores showed improvements across multiple domains, including erectile function, intercourse satisfaction, and overall satisfaction. Studies suggested that apomorphine was most effective in men with mild to moderate ED of psychogenic or mixed aetiology, whilst those with severe organic ED, particularly vascular or neurogenic causes, showed limited response.
A significant limitation identified in clinical practice was the high discontinuation rate, with many patients stopping treatment due to inadequate efficacy or troublesome side effects. Post-marketing surveillance data suggested that real-world effectiveness was lower than that observed in controlled trials, contributing to the eventual withdrawal of the product from the European market.
Current NICE guidance does not include apomorphine in recommendations for ED management. NICE Clinical Knowledge Summaries recommend PDE5 inhibitors as first-line pharmacological treatment for erectile dysfunction, alongside assessment and management of underlying cardiovascular risk factors, diabetes, and hormonal status.
Dosage, Administration and What to Expect
When apomorphine was available for ED treatment, it was supplied as sublingual tablets in 2 mg and 3 mg strengths. The recommended starting dose was typically 2 mg, taken sublingually (placed under the tongue to dissolve) approximately 10–20 minutes before anticipated sexual activity. The tablet was designed to dissolve rapidly without water, allowing absorption directly through the oral mucosa into the bloodstream.
Administration technique was important for optimal absorption. Patients were advised to:
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Place the tablet under the tongue and allow it to dissolve completely without chewing or swallowing
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Avoid eating or drinking immediately before or during tablet dissolution
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Be aware of the risk of dizziness or fainting, particularly when standing up; lie down if feeling dizzy
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Take no more than one dose in 24 hours
If the 2 mg dose proved ineffective after several attempts, the dose could be increased to 3 mg under medical supervision. However, higher doses were associated with increased side effects, particularly nausea and hypotension.
What to expect: Men using apomorphine typically experienced onset of action within 15–20 minutes, though this required sexual stimulation to be effective—the medication did not produce automatic erections. The duration of action was relatively short, approximately 1–2 hours.
Patients were advised that several attempts might be necessary to determine effectiveness, as response could vary between occasions. The medication was contraindicated in men with severe cardiovascular disease, severe hepatic or renal impairment, recent myocardial infarction or stroke, unstable angina, and conditions predisposing to priapism. Caution was required in men taking antihypertensive medications due to the risk of additive blood pressure lowering effects.
Given that apomorphine is no longer available for ED in the UK, men experiencing erectile dysfunction should consult their GP to discuss currently licensed alternatives such as PDE5 inhibitors or other evidence-based treatments recommended by NICE.
Side Effects and Safety Considerations
Apomorphine's side effect profile was a significant factor in its limited clinical success and eventual market withdrawal. The most common adverse effects were related to its dopaminergic activity and included nausea (reported in a substantial proportion of users), dizziness, headache, and sweating. These effects were generally dose-dependent, occurring more frequently with the 3 mg dose.
Cardiovascular concerns were particularly important. Apomorphine could cause hypotension and syncope (fainting), especially when patients stood up quickly after administration—a phenomenon known as postural or orthostatic hypotension. This risk necessitated the recommendation that men be cautious with postural changes and lie down if feeling dizzy. Cases of syncope occurred in clinical trials and post-marketing use.
Other reported side effects included:
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Yawning (a characteristic dopaminergic effect)
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Somnolence or drowsiness
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Taste disturbances
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Oral discomfort or irritation at the sublingual site
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Rhinitis
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Rarely, priapism (prolonged, painful erection)
Contraindications included severe hepatic or renal impairment, recent myocardial infarction or stroke, unstable angina, severe cardiovascular disease, and conditions predisposing to priapism. Unlike PDE5 inhibitors, apomorphine was not contraindicated with nitrates, though caution was required due to the potential for hypotension.
Drug interactions required careful consideration, particularly with antihypertensive medications and alcohol (which could exacerbate hypotension), and other dopaminergic agents. Patients were advised to avoid driving or operating machinery if experiencing dizziness or drowsiness.
Important safety advice: If you experience an erection lasting more than 4 hours (priapism), seek urgent medical attention at an emergency department. If you experience severe dizziness, fainting, chest pain, or other concerning symptoms, seek immediate medical advice. If you suspect a side effect from any medication, you can report it via the MHRA Yellow Card scheme at yellowcard.mhra.gov.uk.
For men currently experiencing erectile dysfunction, it is essential to consult a GP or specialist rather than seeking apomorphine, as it is no longer licensed for this indication in the UK. Modern ED management follows NICE guidelines, which recommend PDE5 inhibitors as first-line treatment, with alternative options including intracavernosal injections, vacuum erection devices, or psychological interventions depending on the underlying cause. Any man experiencing ED should seek medical assessment to identify treatable underlying conditions such as cardiovascular disease, diabetes, or hormonal imbalances, and to receive evidence-based treatment appropriate to their individual circumstances.
Frequently Asked Questions
Is apomorphine still available for erectile dysfunction in the UK?
No, apomorphine is no longer licensed for erectile dysfunction in the UK. The European marketing authorisation for Uprima was withdrawn in 2006 due to limited efficacy compared to PDE5 inhibitors and concerns about side effects.
How did apomorphine differ from Viagra for treating erectile dysfunction?
Apomorphine worked centrally by stimulating dopamine receptors in the brain, whilst Viagra (sildenafil) works peripherally by preventing the breakdown of cGMP in penile tissue. Apomorphine had a faster onset (15–20 minutes) but demonstrated lower efficacy in clinical trials.
What are the current recommended treatments for erectile dysfunction in the UK?
NICE guidance recommends PDE5 inhibitors such as sildenafil as first-line pharmacological treatment for erectile dysfunction. Alternative options include intracavernosal injections, vacuum erection devices, or psychological interventions, depending on the underlying cause and individual circumstances.
The health-related content published on this site is based on credible scientific sources and is periodically reviewed to ensure accuracy and relevance. Although we aim to reflect the most current medical knowledge, the material is meant for general education and awareness only.
The information on this site is not a substitute for professional medical advice. For any health concerns, please speak with a qualified medical professional. By using this information, you acknowledge responsibility for any decisions made and understand we are not liable for any consequences that may result.
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