A Pharmacokinetic Study to Evaluate the Effect of Antacids on Raltegravir (MK-0518) in HIV-Infected Participants (MK-0518-247)
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Purpose
This study will evaluate: (1) the effect of co-administration of single doses of calcium carbonate antacid and magnesium/aluminum hydroxide antacid on the steady-state plasma pharmacokinetic profile of raltegravir in human immunodeficiency virus (HIV)-infected participants; and (2) the effect of staggered dosing of a single dose of a magnesium/aluminum hydroxide antacid 2 hours before and 2 hours after administration of raltegravir on the steady-state plasma pharmacokinetic profile of raltegravir in the same participants.
The study will determine whether (1) the C12hrs of steady-state raltegravir after co-administration of single doses of calcium carbonate antacid is decreased to a clinically meaningful degree compared with C12hrs after administration of raltegravir alone; and whether (2) the C12hrs of steady-state raltegravir after co-administration of a single dose of magnesium/aluminum hydroxide antacid is decreased to a clinically meaningful degree compared with the C12hrs after administration of raltegravir alone.
| Condition | Intervention | Phase |
|---|---|---|
|
HIV Infections |
Drug: Raltegravir Drug: TUMS® + Raltegravir Drug: MAALOX® + Raltegravir Drug: MAALOX® Before Raltegravir Drug: MAALOX® After Raltegravir |
Phase 1 |
| Study Type: | Interventional |
| Study Design: | Allocation: Randomized Endpoint Classification: Pharmacokinetics Study Intervention Model: Crossover Assignment Masking: Open Label Primary Purpose: Treatment |
| Official Title: | A Study to Evaluate the Effect of Metal Cation-Containing Antacids on Raltegravir Pharmacokinetics in HIV-Infected Subjects on a Stable Raltegravir-Containing Regimen |
- Plasma concentration (C 12hrs) of raltegravir [ Time Frame: 12 hours postdose ] [ Designated as safety issue: No ]
- Area under the plasma concentration-time curve (AUC 0-12hrs) of raltegravir [ Time Frame: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 12 hours post-dose ] [ Designated as safety issue: No ]
- Maximum plasma concentration (Cmax) of raltegravir after co-administration of a single dose of antacid [ Time Frame: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 12 hours post-dose ] [ Designated as safety issue: No ]
- Time to maximum plasma concentration (Tmax) of raltegravir after co-administration of a single dose of antacid [ Time Frame: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 12 hours post-dose ] [ Designated as safety issue: No ]
- Number of participants with any clinical or laboratory adverse event [ Time Frame: Start of study drug administration to 12 hours post dose ] [ Designated as safety issue: Yes ]
| Enrollment: | 27 |
| Study Start Date: | June 2012 |
| Study Completion Date: | October 2012 |
| Primary Completion Date: | October 2012 (Final data collection date for primary outcome measure) |
| Arms | Assigned Interventions |
|---|---|
|
Experimental: Sequence 1
Raltegravir, TUMS® + Raltegravir, MAALOX® + Raltegravir, MAALOX® Before Raltegravir, MAALOX® After Raltegravir
|
Drug: Raltegravir
Raltegravir 400 mg Throughout the study, participants will continue to take raltegravir every 12 hours along with their other HIV medications. There will be a minimum of 2 days between treatment periods to permit raltegravir to re-establish steady state concentrations. On the day of co-dosing and intensive PK sampling, raltegravir will be dosed in the morning in a fasted state in all periods. Other Names:
Drug: TUMS® + Raltegravir
3 tablets TUMS® Ultra Strength (US) 1000 mg + 400 mg raltegravir Throughout the study, participants will continue to take raltegravir every 12 hours along with their other HIV medications. There will be a minimum of 2 days between treatment periods to permit raltegravir to re-establish steady state concentrations. On the day of co-dosing and intensive PK sampling, raltegravir will be dosed in the morning in a fasted state in all periods. 20 mL MAALOX® Maximum Strength (MS) + 400 mg raltegravir Throughout the study, participants will continue to take raltegravir every 12 hours along with their other HIV medications. There will be a minimum of 2 days between treatment periods to permit raltegravir to re-establish steady state concentrations. On the day of co-dosing and intensive PK sampling, raltegravir will be dosed in the morning in a fasted state in all periods. 20 mL MAALOX® MS 2 hours prior to 400 mg raltegravir Throughout the study, participants will continue to take raltegravir every 12 hours along with their other HIV medications. There will be a minimum of 2 days between treatment periods to permit raltegravir to re-establish steady state concentrations. On the day of co-dosing and intensive PK sampling, raltegravir will be dosed in the morning in a fasted state in all periods. 20 mL MAALOX® MS 2 hours following 400 mg raltegravir Throughout the study, participants will continue to take raltegravir every 12 hours along with their other HIV medications. There will be a minimum of 2 days between treatment periods to permit raltegravir to re-establish steady state concentrations. On the day of co-dosing and intensive PK sampling, raltegravir will be dosed in the morning in a fasted state in all periods. |
|
Experimental: Sequence 2
TUMS® + Raltegravir, MAALOX® + Raltegravir, Raltegravir, MAALOX® Before Raltegravir, MAALOX® After Raltegravir
|
Drug: Raltegravir
Raltegravir 400 mg Throughout the study, participants will continue to take raltegravir every 12 hours along with their other HIV medications. There will be a minimum of 2 days between treatment periods to permit raltegravir to re-establish steady state concentrations. On the day of co-dosing and intensive PK sampling, raltegravir will be dosed in the morning in a fasted state in all periods. Other Names:
Drug: TUMS® + Raltegravir
3 tablets TUMS® Ultra Strength (US) 1000 mg + 400 mg raltegravir Throughout the study, participants will continue to take raltegravir every 12 hours along with their other HIV medications. There will be a minimum of 2 days between treatment periods to permit raltegravir to re-establish steady state concentrations. On the day of co-dosing and intensive PK sampling, raltegravir will be dosed in the morning in a fasted state in all periods. 20 mL MAALOX® Maximum Strength (MS) + 400 mg raltegravir Throughout the study, participants will continue to take raltegravir every 12 hours along with their other HIV medications. There will be a minimum of 2 days between treatment periods to permit raltegravir to re-establish steady state concentrations. On the day of co-dosing and intensive PK sampling, raltegravir will be dosed in the morning in a fasted state in all periods. 20 mL MAALOX® MS 2 hours prior to 400 mg raltegravir Throughout the study, participants will continue to take raltegravir every 12 hours along with their other HIV medications. There will be a minimum of 2 days between treatment periods to permit raltegravir to re-establish steady state concentrations. On the day of co-dosing and intensive PK sampling, raltegravir will be dosed in the morning in a fasted state in all periods. 20 mL MAALOX® MS 2 hours following 400 mg raltegravir Throughout the study, participants will continue to take raltegravir every 12 hours along with their other HIV medications. There will be a minimum of 2 days between treatment periods to permit raltegravir to re-establish steady state concentrations. On the day of co-dosing and intensive PK sampling, raltegravir will be dosed in the morning in a fasted state in all periods. |
|
Experimental: Sequence 3
MAALOX® + Raltegravir, Raltegravir, TUMS® + Raltegravir, MAALOX® Before Raltegravir, MAALOX® After Raltegravir
|
Drug: Raltegravir
Raltegravir 400 mg Throughout the study, participants will continue to take raltegravir every 12 hours along with their other HIV medications. There will be a minimum of 2 days between treatment periods to permit raltegravir to re-establish steady state concentrations. On the day of co-dosing and intensive PK sampling, raltegravir will be dosed in the morning in a fasted state in all periods. Other Names:
Drug: TUMS® + Raltegravir
3 tablets TUMS® Ultra Strength (US) 1000 mg + 400 mg raltegravir Throughout the study, participants will continue to take raltegravir every 12 hours along with their other HIV medications. There will be a minimum of 2 days between treatment periods to permit raltegravir to re-establish steady state concentrations. On the day of co-dosing and intensive PK sampling, raltegravir will be dosed in the morning in a fasted state in all periods. 20 mL MAALOX® Maximum Strength (MS) + 400 mg raltegravir Throughout the study, participants will continue to take raltegravir every 12 hours along with their other HIV medications. There will be a minimum of 2 days between treatment periods to permit raltegravir to re-establish steady state concentrations. On the day of co-dosing and intensive PK sampling, raltegravir will be dosed in the morning in a fasted state in all periods. 20 mL MAALOX® MS 2 hours prior to 400 mg raltegravir Throughout the study, participants will continue to take raltegravir every 12 hours along with their other HIV medications. There will be a minimum of 2 days between treatment periods to permit raltegravir to re-establish steady state concentrations. On the day of co-dosing and intensive PK sampling, raltegravir will be dosed in the morning in a fasted state in all periods. 20 mL MAALOX® MS 2 hours following 400 mg raltegravir Throughout the study, participants will continue to take raltegravir every 12 hours along with their other HIV medications. There will be a minimum of 2 days between treatment periods to permit raltegravir to re-establish steady state concentrations. On the day of co-dosing and intensive PK sampling, raltegravir will be dosed in the morning in a fasted state in all periods. |
|
Experimental: Sequence 4
Raltegravir, MAALOX® + Raltegravir, TUMS® + Raltegravir, MAALOX® After Raltegravir, MAALOX® Before Raltegravir
|
Drug: Raltegravir
Raltegravir 400 mg Throughout the study, participants will continue to take raltegravir every 12 hours along with their other HIV medications. There will be a minimum of 2 days between treatment periods to permit raltegravir to re-establish steady state concentrations. On the day of co-dosing and intensive PK sampling, raltegravir will be dosed in the morning in a fasted state in all periods. Other Names:
Drug: TUMS® + Raltegravir
3 tablets TUMS® Ultra Strength (US) 1000 mg + 400 mg raltegravir Throughout the study, participants will continue to take raltegravir every 12 hours along with their other HIV medications. There will be a minimum of 2 days between treatment periods to permit raltegravir to re-establish steady state concentrations. On the day of co-dosing and intensive PK sampling, raltegravir will be dosed in the morning in a fasted state in all periods. 20 mL MAALOX® Maximum Strength (MS) + 400 mg raltegravir Throughout the study, participants will continue to take raltegravir every 12 hours along with their other HIV medications. There will be a minimum of 2 days between treatment periods to permit raltegravir to re-establish steady state concentrations. On the day of co-dosing and intensive PK sampling, raltegravir will be dosed in the morning in a fasted state in all periods. 20 mL MAALOX® MS 2 hours prior to 400 mg raltegravir Throughout the study, participants will continue to take raltegravir every 12 hours along with their other HIV medications. There will be a minimum of 2 days between treatment periods to permit raltegravir to re-establish steady state concentrations. On the day of co-dosing and intensive PK sampling, raltegravir will be dosed in the morning in a fasted state in all periods. 20 mL MAALOX® MS 2 hours following 400 mg raltegravir Throughout the study, participants will continue to take raltegravir every 12 hours along with their other HIV medications. There will be a minimum of 2 days between treatment periods to permit raltegravir to re-establish steady state concentrations. On the day of co-dosing and intensive PK sampling, raltegravir will be dosed in the morning in a fasted state in all periods. |
|
Experimental: Sequence 5
TUMS® + Raltegravir, Raltegravir, MAALOX® + Raltegravir, MAALOX® After Raltegravir, MAALOX® Before Raltegravir
|
Drug: Raltegravir
Raltegravir 400 mg Throughout the study, participants will continue to take raltegravir every 12 hours along with their other HIV medications. There will be a minimum of 2 days between treatment periods to permit raltegravir to re-establish steady state concentrations. On the day of co-dosing and intensive PK sampling, raltegravir will be dosed in the morning in a fasted state in all periods. Other Names:
Drug: TUMS® + Raltegravir
3 tablets TUMS® Ultra Strength (US) 1000 mg + 400 mg raltegravir Throughout the study, participants will continue to take raltegravir every 12 hours along with their other HIV medications. There will be a minimum of 2 days between treatment periods to permit raltegravir to re-establish steady state concentrations. On the day of co-dosing and intensive PK sampling, raltegravir will be dosed in the morning in a fasted state in all periods. 20 mL MAALOX® Maximum Strength (MS) + 400 mg raltegravir Throughout the study, participants will continue to take raltegravir every 12 hours along with their other HIV medications. There will be a minimum of 2 days between treatment periods to permit raltegravir to re-establish steady state concentrations. On the day of co-dosing and intensive PK sampling, raltegravir will be dosed in the morning in a fasted state in all periods. 20 mL MAALOX® MS 2 hours prior to 400 mg raltegravir Throughout the study, participants will continue to take raltegravir every 12 hours along with their other HIV medications. There will be a minimum of 2 days between treatment periods to permit raltegravir to re-establish steady state concentrations. On the day of co-dosing and intensive PK sampling, raltegravir will be dosed in the morning in a fasted state in all periods. 20 mL MAALOX® MS 2 hours following 400 mg raltegravir Throughout the study, participants will continue to take raltegravir every 12 hours along with their other HIV medications. There will be a minimum of 2 days between treatment periods to permit raltegravir to re-establish steady state concentrations. On the day of co-dosing and intensive PK sampling, raltegravir will be dosed in the morning in a fasted state in all periods. |
|
Experimental: Sequence 6
MAALOX® + Raltegravir, TUMS® + Raltegravir, Raltegravir, MAALOX® After Raltegravir, MAALOX® Before Raltegravir
|
Drug: Raltegravir
Raltegravir 400 mg Throughout the study, participants will continue to take raltegravir every 12 hours along with their other HIV medications. There will be a minimum of 2 days between treatment periods to permit raltegravir to re-establish steady state concentrations. On the day of co-dosing and intensive PK sampling, raltegravir will be dosed in the morning in a fasted state in all periods. Other Names:
Drug: TUMS® + Raltegravir
3 tablets TUMS® Ultra Strength (US) 1000 mg + 400 mg raltegravir Throughout the study, participants will continue to take raltegravir every 12 hours along with their other HIV medications. There will be a minimum of 2 days between treatment periods to permit raltegravir to re-establish steady state concentrations. On the day of co-dosing and intensive PK sampling, raltegravir will be dosed in the morning in a fasted state in all periods. 20 mL MAALOX® Maximum Strength (MS) + 400 mg raltegravir Throughout the study, participants will continue to take raltegravir every 12 hours along with their other HIV medications. There will be a minimum of 2 days between treatment periods to permit raltegravir to re-establish steady state concentrations. On the day of co-dosing and intensive PK sampling, raltegravir will be dosed in the morning in a fasted state in all periods. 20 mL MAALOX® MS 2 hours prior to 400 mg raltegravir Throughout the study, participants will continue to take raltegravir every 12 hours along with their other HIV medications. There will be a minimum of 2 days between treatment periods to permit raltegravir to re-establish steady state concentrations. On the day of co-dosing and intensive PK sampling, raltegravir will be dosed in the morning in a fasted state in all periods. 20 mL MAALOX® MS 2 hours following 400 mg raltegravir Throughout the study, participants will continue to take raltegravir every 12 hours along with their other HIV medications. There will be a minimum of 2 days between treatment periods to permit raltegravir to re-establish steady state concentrations. On the day of co-dosing and intensive PK sampling, raltegravir will be dosed in the morning in a fasted state in all periods. |
Eligibility| Ages Eligible for Study: | 18 Years and older |
| Genders Eligible for Study: | Both |
| Accepts Healthy Volunteers: | No |
Inclusion Criteria:
- HIV-infected male or female, 18 or more years of age, on a stable raltegravir dose (400 mg every 12 hours [q12h]) as part of a stable anti-retroviral regimen (ARV) for at least 1 month and will maintain current ARV therapy throughout the study
- Body Mass Index (BMI) ≤32 kg/m^2
- Good general health
- Can be a current smoker and/or user of nicotine or nicotine-containing products, but use of nicotine-containing products will not be permitted during the stay at the clinical research site
Exclusion Criteria:
- History of gastric bypass surgery
- Pregnant or nursing
- Mentally or legally incapacitated, has significant emotional problems, or has a history of a clinically significant psychiatric disorder; participants who have had situational depression may be enrolled at the discretion of the investigator.
- History of stroke, chronic seizures, or major neurological disorder
- History of clinically significant endocrine, gastrointestinal, cardiovascular, hematological, hepatic, immunological, renal, respiratory, or genitourinary abnormalities or diseases (excluding HIV); participants with a history of uncomplicated kidney stones or childhood asthma may be enrolled at the discretion of the investigator.
- Active neoplastic disease deemed unstable or progressing by the investigator
- Currently taking rifampin or unable to refrain from use of any proton pump inhibitor and any histamine-2 (H2)-blockers, over-the-counter antacids, calcium supplements, or multivitamins during the study
- Consumes excessive amounts of alcohol
- Consumes excessive amounts of coffee, tea, cola, or other caffeinated beverages
- Major surgery or blood donation within the past 4 weeks
- History of significant multiple and/or severe allergies or has had an anaphylactic reaction or significant intolerability to prescription or non-prescription drugs or food
- Regular user of any illicit drugs or history of drug (including alcohol) abuse within the past 6 months; current methadone or suboxone use is allowed.
Contacts and Locations More Information
No publications provided
| Responsible Party: | Merck |
| ClinicalTrials.gov Identifier: | NCT01622673 History of Changes |
| Other Study ID Numbers: | 0518-247 |
| Study First Received: | June 15, 2012 |
| Last Updated: | October 25, 2012 |
| Health Authority: | United States: Food and Drug Administration |
Additional relevant MeSH terms:
|
HIV Infections Acquired Immunodeficiency Syndrome Lentivirus Infections Retroviridae Infections RNA Virus Infections Virus Diseases Sexually Transmitted Diseases, Viral Sexually Transmitted Diseases |
Immunologic Deficiency Syndromes Immune System Diseases Slow Virus Diseases Antacids Aluminum hydroxide, magnesium hydroxide, drug combination Molecular Mechanisms of Pharmacological Action Pharmacologic Actions |
ClinicalTrials.gov processed this record on June 18, 2013