3-Ethyl-5-methyl (±) - 2 - [(2 - aminoethoxy)methyl] - 4 - (2 - chlorophenyl) - 1,4 - dihydro - 6 - methyl - 3,5 - pyridinedicarboxylate, monobenzenesulphonate monohydrate
3-methyl-2- [pentanoyl-[ [4-[2-(2H-tetrazol-5-yl) phenyl] phenyl] methyl]amino] -butanoic acid
Amlodipine可選擇性地抑制鈣離子流入細胞膜，尤其對血管平滑肌細胞的作用更甚於心肌細胞。血清鈣離子濃度並不會受到amlodipine的影響。在生理酸鹼值範圍內，amlodipine是一種游離化合物(pKa=8.6)，其和鈣離子通道受體的動能交互作用特性為：其與受體的結合和分離速率是漸進性的，因而造成作用為漸進性。Amlodipine是一種周邊動脈血管擴張劑，可直接作用於血管平滑肌，減低周邊血管阻力並減低血壓。
Valsartan血管收縮素II係透過血管收縮素轉化酶(ACE，激酶II)的催化反應，從血管收縮素I轉化而來。血管收縮素II是腎素-血管收縮素系統主要的升血壓藥物，其作用包括血管收縮、刺激醛固酮的合成與釋放、刺激心臟，以及腎臟的鈉離子再吸收作用。
Amlodipine：Absorption
Tmax is 6 to 12 h.
Distribution
Bioavailability is 64% to 90%. About 93% is protein bound.
Metabolism
About 90% is converted to inactive metabolites in the liver.
Elimination
10% of the parent compound and 60% of the metabolites are excreted in the urine. Elimination is biphasic. T½ is about 30 to 50 h.
Duration
24 h.
Special Populations
Hepatic Function Impairment
Clearance is decreased and AUC may increase about 40% to 60%. May require lower initial dose.
Elderly
Clearance is decreased and AUC may increase about 40% to 60%. May require lower initial dose.
Moderate to severe heart failure
Clearance is decreased and AUC may increase about 40% to 60%. May require lower initial dose.
Valsartan：Absorption
T max is 2 to 4 h after dosing. Bioavailability is about 10% to 35%. Food decreases AUC about 40% and decreases C max about 50%.
Distribution
Vd is about 17 L. Highly bound to albumin (about 95%).
Metabolism
The major metabolite, valeryl 4-hydroxy valsartan, accounts for about 9% of the dose.
Elimination
Half-life is about 6 h. Valsartan is primarily recovered in the feces (about 83%) and urine (about 13%). Recovery is mainly unchanged drug, with only about 20% of the dose recovered as metabolite. The plasma Cl is about 2 L/h.
Special Populations
Renal Function Impairment
No correlation between renal function and exposure to the drug.
Hepatic Function Impairment
Patients with mild to moderate chronic liver disease have about twice the AUC value.
Elderly
AUC is about 70% higher and t ½ is about 35% longer in elderly patients.
Conivaptan, diltiazem, protease inhibitors (eg, ritonavir)
Amlodipine plasma concentrations may be elevated, increasing the pharmacologic effects and adverse reactions.
Lithium
Plasma concentrations may be elevated by valsartan, increasing the pharmacologic and toxic effects of lithium.
Potassium-sparing diuretics (eg, spironolactone), potassium supplements
Coadministration with valsartan may cause elevated potassium concentrations and, in heart failure patients, increased serum creatinine. Amlodipine plasma concentrations may be elevated.
