Pharmacokinetic Interactions of Metamizole (Dipyrone) in Healthy Subjects

• Status: Completed
• Trial end date: 2018-10-31
• Target enrollment: 0
• Participant gender: Male

Summary

Investigators conducted a single center, two-phased, open, controlled pharmacokinetic study to investigate the drug-drug interaction potential of metamizole. For this reason, healthy male volunteers were screened.

Enrolled participants were phenotyped on day 1 using the Basel Cocktail (phenotyping cocktail containing specific substrates for CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, CYP3A4). After, they received metamizole treatment for 8 days (3 grams per day). On the 8th day (day 9), they were phenotyped again with the Basel Cocktail and the respective phenotypes (d1 vs. d9) were compared.

• Phase: Phase 1
• Accepts Healthy Volunteers?: Accepts Healthy Volunteers

Details

• Lead Sponsor: University Hospital, Basel, Switzerland
• Treatments: Dipyrone

Criteria

Inclusion Criteria:

• Healthy subjects aged between 18 and 45 years (inclusive) at screening

• BMI between 18 and 28 kg/m2 (inclusive) and bodyweight at least 50 kg at screening

• systolic blood pressure: 100-140 mmHg, diastolic blood pressure: 60-90 mmHg and heart rate: 45-90 bpm (inclusive), measured on the leading arm, in the supine position at screening

• No clinically significant findings on the physical examination at screening

• Signed informed consent prior to any study-mandated procedure

• Hematology and clinical chemistry results not deviating from the normal range to clinically relevant extent at screening

• Ability to communicate well with the investigator to understand and comply with the requirements of the study

Exclusion Criteria:

• Smoking >5 cigarettes per day

• History or clinical evidence of alcoholism or drug abuse within the 3- year period prior to screening

• Loss of ≥250 ml of blood within 3 months prior to screening. Treatment with an investigational drug within 30 days prior to screening

• Previous systemic treatment with any prescribed or over the counter medication (including herbal medicines such as St John's Wort) within 2 weeks prior to the intended start of the study

• Inability to stop consumption inducing food products (e.g. grapefruit juice) 72 h before start of the study

• Excessive caffeine consumption (>8 cups of coffee/ 8l coca cola per day)

• Legal incapacity or limited legal capacity at screening

• Positive results from urine drug screen at screening

• History or clinical evidence of any disease (e.g. gastrointestinal disease: Morbus Crohn, Colitis Ulcerosa, anamnestic gastrointestinal bleeding) and/or existence of any surgical or medical condition, which might interfere with the absorption, distribution, metabolism or excretion of the study drugs, or which might increase the risk for toxicity

• Known hypersensitivity to Metamizole (Novalgin®) or excipients of the drug formulation

• Any circumstances or conditions, which, in the opinion of the investigator, may affect full participation in the study or compliance with the protocol.