It belongs to the group of dihydropyridines, which act in muscle contraction.
These affect the relaxation of blood vessels, reducing the heart’s workload.
Amlodipine is an antagonist which blocks the calcium ion channels, blocking them in the cardiac, smooth muscle membrane, influencing the amount of calcium present in the cells and muscles of the heart.
This medication lowers blood pressure, and its antihypertensive action is associated with this relaxing effect on vascular smooth muscle blood vessels, allowing blood to flow more easily.
- (RS)-3-etil-5-metil-2-(2-aminoetoximetil)-4-(2-chlorofenil)-1,4-dihidro-6-metil-3,5- piridinadicarboxilato.
- Tablets of 5 mg and 10 mg.
Mechanism of action
Amlodipine inhibits the flow through the cell membrane of calcium ions because it binds by changing its affinity to the alpha1 subunit of L-type calcium channels, preventing its opening.
This results in a reduction in the entry of calcium ions, modifying the contractility of the heart muscle and smooth muscle.
Those who depend on the movement of these extracellular calcium ions from cardiac or muscle cells through specific channels for cardiac contractility and oxygen demand.
Because it is a peripheral arterial vasodilator, it acts immediately on vascular smooth muscle, decreasing peripheral vascular resistance and consequently blood pressure.
It can also dilate the coronary arteries and arterioles, decreasing total peripheral resistance.
Because the heart rate remains stable, this relief of the heart decreases the energy consumption in the myocardium; it also reduces the need for oxygen.
This drug is indicated to treat coronary diseases such as chronic stable angina (due to physical or emotional stress), vasospastic angina (Prinzmetal’s angina or variant angina), and arterial management hypertension.
In adults: Initially, a dose of 5 mg/day is recommended once a day.
The maximum antihypertensive effects usually take weeks to be fully instituted, and in case of increasing, the dose can not exceed 10 mg/day.
Half should reduce the first doses in patients who have liver insufficiencies.
The first doses should be 2.5 mg once a day in older adults, adjusting the dose every seven to fourteen days, depending on the patient’s responses and tolerance.
In children and adolescents from 6 to 17 years of age, the recommended dose as oral antihypertensive is 2.5 mg once a day as the initial dose.
If the blood pressure goal is not reached after four weeks, it rises to 5 mg; in children under six years, the starting dose is 0.05-0.1 mg/kg/day.
It increases after a week of starting the treatment, little by little, at a maximum dose of 0.6 mg/kg/day.
Remember your administration; it can be administered simultaneously every day.
Amlodipine is generally well-tolerated in doses that do not exceed 10 mg/day.
Mild adverse reactions have been reported almost always linked with peripheral vasodilatory effects of this drug.
Migraines and edema are two of the most common side effects.
Dizziness, weakness, palpitations, and hot flushes usually related to the doses have also been reported.
There have been sporadic cases of pancreatitis.
There are reports of other rare side effects such as allergic reactions, angioedema, and erythema multiforme.
The cases of intense pruritus associated with amlodipine that has been reported disappeared when the treatment was discontinued.
A few cases have been reported as gynecomastia, sinus bradycardia, tremor, vasculitis, angina, peripheral neuropathy, peripheral ischemia, orthostatic hypotension, syncope, paresthesias, anorexia, and dysphagia.
Also, cases of vertigo, blurred vision, constipation, diarrhea, and flatulence, but its relationship with the amlodipine has not been established with certainty.
Precautions and contraindications
Amlodipine is organically related to nifedipine (1,4-dihydropyridine) and is not recommended in patients who are sensitive to the types of dihydropyridines.
Amlodipine should be used with caution in cases of patients who have severe bradycardia or the presence of heart failure (mainly when associated with a β-blocker) due to the eventuality of cardiogenic shock since it has harmful inotropic properties and its practical hypotensive effects.
Patients suffering from left ventricular dysfunction who have been prescribed amlodipine for angina treatments have to be constantly monitored to show that the medication does not aggravate heart failure.
According to the New York Heart Association, amlodipine should be prescribed in Class IV heart failure patients.
Amlodipine is powerful hypotension; it should not be administered in patients with less than 90 mmHg of systolic blood pressure.
In case of liver failure, as occurs with calcium channel blockers, the half-life of amlodipine is prolonged in patients with variations in liver function.
Since the amlodipine is metabolized using this route, indications for its dosage have not yet been established.
Therefore, in these patients, the doses should be adjusted according to the patient’s response, starting treatment with lower doses than those recommended in normal adults.
Amlodipine is partially contraindicated in patients suffering from advanced aortic stenosis because the pressure difference associated with this condition may worsen.
Amlodipine is located in category C risk in the case of pregnancy.
This drug can only be administered when the benefits outweigh the potential risks.
It is unknown if the drug manages to pass through breast milk, so it is recommended to avoid it during lactation.
It is recommended to monitor plasma levels when amlodipine is administered simultaneously with these drugs.
- Phenobarbital (or primidone).
They can reduce the bioavailability of amlodipine, so it may be necessary to increase the doses of amlodipine in patients who use these drugs.