Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2019 Publisher: RPH Pharmaceuticals AB, Lagervägen 7, 136 50 Haninge, Sweden
Labetalol lowers the blood pressure by blocking peripheral arteriolar alphaadrenoceptors thus reducing peripheral resistance, and by concurrent betablockade, protects the heart from reflex sympathetic drive that would otherwise occur. Cardiac output is not significantly reduced at rest or after moderate exercise. Increases in systolic blood pressure during exercise are reduced but corresponding changes in diastolic pressure are essentially normal.
In patients with angina pectoris co-existing with hypertension, the reduced peripheral resistance decreases myocardial afterload and oxygen demand. All these effects would be expected to benefit hypertensive patients and those with co-existing angina.
The plasma half-life of labetalol is about 4 hours. About 50% of labetalol in the blood is protein bound. Labetalol is metabolised mainly through conjugation to inactive glucuronide metabolites. These are excreted both in urine and via the bile into the faeces.
Only negligible amounts of the drug cross the blood brain barrier in animal studies.
Not applicable since Trandate Tablets have been used in clinical practice for many years and its effects in man are well known.
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