Because metoprolol, a β1-selective adrenergic blocking agent used for treatment of hypertension and stable angina, has a short half-life after oral injection, reduction of systolic blood pressure was measured in male spontaneously hypertensive rats after administration of the drug through a transdermal patch. Systolic pressure was reduced from a pretreatment pressure of 209 ± 16 mmHg to a post-treatment pressure of 188 ± 13 mmHg (P < 0·001) within 4 h. Pressure continued to fall until 12 h when it became steady at 173 ± 10 mmHg and remained in that range for up to 24 h. When the patch was removed after 24 h the pressure gradually increased and reached its pretreatment value within 2 h. These results indicate that the systemic availability of metoprolol can be increased by transdermal administration.
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Ghosh et al. (1996) studied this question.