What Factors Affect a Sufficient Amlodipine Dose?

Amlodipine tablets are dihydropyridine calcium antagonists, which can treat hypertension and angina pectoris.

Amlodipine tablets

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Amlodipine tablets are dihydropyridine calcium antagonists, which can treat hypertension and angina pectoris.

Drug Name

Amlodipine tablets

Main indications

Antiangina

(1) Hypertension (alone or combined with other drugs)

(2)

Amlodipine is a dihydropyridine calcium antagonist (calcium antagonist or slow channel blocker). Myocardial and smooth muscle contraction depends on extracellular calcium ions entering the cell through specific ion channels. This product selectively inhibits calcium ions from entering the smooth muscle cells and cardiomyocytes across the membrane, and has a greater effect on smooth muscle than the heart muscle. Its interaction with the calcium channel is determined by the progressive rate of its binding and dissociation with the receptor site, so the pharmacological effect is gradually produced. This product is a peripheral arterial dilator, which directly acts on vascular smooth muscle, reduces peripheral vascular resistance, and thereby lowers blood pressure. At therapeutic doses, negative inotropic effects were observed in vitro, but not seen in overall animal experiments. This product does not affect plasma calcium concentration. 15 randomized double-blind, placebo-controlled clinical trials have confirmed the antihypertensive effect of this product. Patients with mild to moderate hypertension who take the medicine once a day can reduce the supine and standing blood pressure for 24 hours. Long-term use does not cause significant changes in heart rate or plasma catecholamines. The effect of pressure reduction is stable, and there is not much difference between peak and valley values. The antihypertensive effect is related to the dose, the antihypertensive amplitude is related to the pre-treatment blood pressure, and those with moderate hypertension (

This product is completely but slowly absorbed after oral administration, reaching peak concentration in 6-12 hours. A single oral administration of 5mg resulted in a peak of 3.0ng / ml; a single oral administration of 10mg resulted in a peak of 5.9ng / ml. Absolute bioavailability is 64% -90% and is not affected by diet. About 95% of the drugs in circulation are bound to plasma proteins, and the volume of distribution is 21L / kg. Steady-state blood drug concentration was reached 7-8 days after continued administration. This product is eliminated from the plasma in a two-compartment model, and is extensively metabolized into non-pharmacologically active metabolites (90%) in the liver. Terminal

The usual oral starting dose is 5 mg once daily, and the maximum does not exceed 10 mg once daily. Thin people, weak people, elderly patients or people with impaired liver function start taking the medicine once a day from 2.5mg; those who use other antihypertensive drugs also start taking this dose. The dosage should be adjusted according to individual needs, and the adjustment period should be no less than 7-14 days so that the doctor can fully evaluate the patient's response to the dosage. But under the premise of clinical guarantee, the adjustment speed can be accelerated. The recommended dose for the treatment of angina pectoris is 5-10 mg, which should be reduced in elderly patients or those with impaired liver function.

This product has a good dose range of 10mg / day

(1) Those who are allergic to dihydropyridine calcium antagonists.

(2) Severe hypotension; aortic valve stenosis.

Angina pectoris and / or

Drug overdose can lead to excessive expansion of peripheral blood vessels, cause hypotension, and may also reflect tachycardia. After an overdose occurs, blood pressure must be monitored along with heart and respiratory monitoring. Once hypotension occurs, supportive therapies are performed, including raising the limbs and expanding as needed. If these measures do not work, booster agents (such as phenylephrine) can be considered if circulating blood volume and urine volume allow. Intravenous administration of calcium gluconate helps reverse calcium antagonistic effects. Because this product is highly bound to plasma proteins, dialysis treatment has no effect.

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