Onset of Blood Pressure Reduction with Amlodipine
Amlodipine begins lowering blood pressure within 6-12 hours after the first dose, with peak plasma concentrations and maximal blood pressure reduction occurring during this timeframe, though steady-state therapeutic effects require 7-8 days of consecutive daily dosing. 1
Pharmacokinetic Timeline
Absorption and Initial Effect:
- Peak plasma concentrations occur between 6-12 hours after oral administration 1
- The drug has a gradual onset of effect due to its slow rate of association with calcium channel receptors 1
- Absolute bioavailability ranges from 64-90% 1
Steady-State Achievement:
- Steady-state plasma levels are reached after 7-8 days of consecutive daily dosing 1
- The terminal elimination half-life is 30-50 hours, contributing to sustained blood pressure control 1
Clinical Blood Pressure Response
Short-Term Response (First 2 Weeks):
- In clinical trials, mean supine blood pressure decreased from 169/104 mmHg to 153/95 mmHg after just 2 weeks of amlodipine 5 mg daily 2, 3, 4
- After 6 weeks of treatment, blood pressure was further reduced to 146/92 mmHg 2, 3, 4
24-Hour Blood Pressure Control:
- Once daily administration produces statistically significant blood pressure reductions at 24 hours post-dose, averaging 12/6 mmHg in standing position and 13/7 mmHg in supine position 1
- Antihypertensive effectiveness is maintained for at least 24 hours with chronic once-daily oral administration 1
- Ambulatory monitoring studies demonstrate effective blood pressure reduction throughout the entire 24-hour period without altering the normal circadian pattern 2, 3, 4
Magnitude of Effect:
- Mean daytime blood pressure was reduced from 165/103 to 147/89 mmHg 2, 3
- Mean nighttime blood pressure was reduced from 137/79 to 121/69 mmHg 2, 3
- Systematic review of >5000 patients showed mean SBP decreased by 17.5 mmHg from baseline with amlodipine monotherapy 5
Important Clinical Considerations
Gradual Blood Pressure Lowering:
- Amlodipine's gradual onset of effect makes it particularly suitable for patients with coronary artery disease where rapid blood pressure reduction should be avoided 6
- In patients with elevated diastolic blood pressure who have CAD and evidence of myocardial ischemia, blood pressure should be lowered slowly 6
Dosing Strategy:
- Initial dose is typically 5 mg once daily 6
- Dose can be increased to 10 mg after at least 2 weeks if blood pressure control is inadequate 6, 2, 3
- The median daily dose in clinical trials was 5 mg (range 1.25-15 mg) 5
Patient-Specific Factors:
- Greater systolic blood pressure reduction occurs in elderly patients, likely due to higher baseline systolic pressures 1
- Patients with moderate hypertension (diastolic 105-114 mmHg) had approximately 50% greater response than those with mild hypertension (diastolic 90-104 mmHg) 1
- Elderly patients and those with hepatic insufficiency have decreased clearance with 40-60% increase in AUC, potentially requiring lower initial doses 1
Monitoring Timeline: