An open label, single dose, phase I pilot study to determine the pharmacokinetic, safety and tolerability profiles of oxymorphone delivered from a transdermal oxymorphone patch

Exclusion Criteria20

• Evidence of clinically significant impairment/disorders.
• History of coronary disease, peripheral vascular disease, cerebrovascular accident, transient ischaemic attack, uncontrolled hypertension or signs/symptoms of ischaemic heart disease.
• Have a seated systolic blood pressure of < 90 mmHg or >160 mmHg and/or diastolic blood pressure of < 50 mmHg or >95 mmHg at Screening or Check-In.
• History of acute or severe bronchial asthma, diagnosed obstructive sleep apnoea, hypoxia, hypoxaemia, hybercarbia, or other obstructive airway disease or any condition that may increase the risk for respiratory depression.
• A resting (seated for at least five minutes) pulse rate at rest of < 45 BPM or > 100 BPM at Screening or Check-In.
• History of neurologic conditions such as seizures or convulsive disorders (including epilepsy), severe head injury or increased intracranial pressure.
• A calculated creatinine clearance of < 85 mL/minute.
• Have undergone surgery or received anaesthetic within 30 days of Day 1.
• Use of CNS depressants including: other opioids, sedative, anxiolytics, hypnotics, neuroleptics, phenothiazines, tranquillisers, skeletal muscle relaxants, sedating antihistamines or cimetidine within 30 days of Day 1.
• Use of macrolide antibiotics (e.g., Erythromycin), azole antifungal agents (e.g., Ketoconazole) or protease inhibitors (e.g., Ritanovir) within 30 days of Day 1.
• Use of any prescription medication during the 14 days prior to Day 1 and for duration of study, unless approved by both the PI and the Medical Monitor (in writing).
• Use of any OTC product, herbal product, diet aid, or hormone supplement, within 14 days prior to Day 1 and for duration of study.
• Known intolerance, allergy or hypersensitivity reactions to naltrexone, naloxone, oxymorphone, opioid analgesics, or any commercially available adhesives.
• Any history of a dermatological condition or recurrent generalised skin disorder within the last 5 years including psoriasis and eczema or any other skin condition.
• Any tattoos, bruises, scars or skin lesions on the area where the IP is to be applied which may interfere with study assessments.
• Positive screening test for HIV antibodies, Hepatitis B surface antigen or Hepatitis C antibody.
• Evidence or history of substance or alcohol abuse (drink more than 2 standard units of alcohol per day), including positive test results for drugs of abuse in the urine or a positive alcohol breath test at Screening or at Check-In.
• Unwilling or unable to abstain from recreational drug/substance use, alcohol, caffeine or other xanthine-containing products from Day -1 until discharge.
• Participants who are not willing to refrain from smoking 48 hours before Day –1 until discharge.
• Consumption of grapefruit, grapefruit juice or any products containing CYP3A4 inhibitors and inducers within 14 days of Day 1 and through to completion of the confinement period.