Effective Duration of Domperidone
Domperidone has a duration of effect of 7-14 hours, with a plasma half-life of approximately 7.5 hours. 1, 2
Pharmacokinetic Profile
- Domperidone is a dopamine D2-receptor antagonist that does not readily cross the blood-brain barrier, resulting in fewer central nervous system side effects compared to other antiemetics like metoclopramide 3, 4
- After oral administration, domperidone is rapidly absorbed with peak plasma concentrations reached within 30 minutes 2
- The elimination half-life ranges from 7.5 hours to 16 hours, with most guidelines citing a duration of action of 7-14 hours 1, 5
- Domperidone is extensively distributed in the body with a mean apparent volume of distribution of 6,272 L 5
- The drug is 91-93% bound to plasma proteins 6
Clinical Application
- Domperidone is typically administered at a dose of 10-20 mg three to four times daily for nausea and vomiting treatment 3
- The duration of antiemetic effect aligns with its pharmacokinetic profile, providing symptom relief for approximately 7-14 hours per dose 1, 2
- This contrasts with other antiemetics such as:
Metabolism and Elimination
- Domperidone undergoes extensive hepatic metabolism through hydroxylation and N-dealkylation 6
- Excretion occurs through both urinary (31%) and fecal (66%) routes 6
- Only a small proportion is excreted unchanged (10% in feces, approximately 1% in urine) 6
- The extensive first-pass metabolism contributes to its pharmacokinetic profile and duration of action 2
Clinical Efficacy Considerations
- When used for gastrointestinal symptoms, the clinical effects of domperidone can persist throughout the treatment period (studies show efficacy over 6-week treatment courses) 7
- For acute nausea and vomiting, domperidone shows significant cessation of vomiting at 6 hours (81% of patients) and 24 hours (85% of patients) after administration 8
- In breastfeeding women, domperidone has a milk:plasma ratio of 0.25 and a relative infant dose of 0.01-0.35%, making it one of the safer antiemetic options during lactation 1
Dosing Recommendations Based on Duration
- For optimal antiemetic coverage throughout the day, domperidone should be administered every 8 hours (three times daily) 3
- For more severe cases of nausea and vomiting, dosing every 6 hours (four times daily) may be warranted to maintain therapeutic effect 3
- The standard dosing of 10-20 mg three to four times daily aligns with its pharmacokinetic profile to provide continuous symptom relief 3, 2