What is Clonidine?
Clonidine acts in the brain rather than on blood vessels: it stimulates alpha-adrenoreceptors in the brain stem, which reduces sympathetic nerve output to the heart, kidneys and blood vessels. Peripheral resistance, heart rate and blood pressure fall, while kidney blood flow and filtration remain essentially unchanged.
It works quickly after a dose, and beyond a certain blood level a higher dose does not lower pressure further. Tolerance can develop in some patients, making reassessment of treatment necessary; the figures are in the clinical details.1
This page covers the immediate-release tablets for high blood pressure. Extended-release clonidine for ADHD is a separate product, Kapvay. The original Catapres tablets were approved in 1974 and have been discontinued; generic tablets remain on prescription.2
▶Clinical detailspharmacokinetics
| Measure | Value |
|---|---|
| Bioavailability | 70% to 80%; not affected by food or race |
| Peak plasma level | 1 to 3 hours after a dose |
| Elimination half-life | 12 to 16 hours; up to 41 hours in severe kidney impairment |
| Elimination | 40% to 60% of the absorbed dose in urine unchanged within 24 hours; about 50% metabolised in the liver |
| Distribution | Crosses the placenta; passes into breast milk |
| Dialysis | Only a minimal amount removed by routine haemodialysis |
Source: 1
