How lercanidipine works
Lercanidipine is an active ingredient from the group of calcium channel blockers, more precisely from the group of dihydropyridines. It has a vasodilatory effect and thus lowers blood pressure. Lercanidipine is therefore an antihypertensive drug. By lowering blood pressure, it prevents serious secondary diseases such as heart attack and stroke.
The first calcium channel blockers that were developed also partially affected the “timing” of the heartbeat, which is also mediated by calcium – they slowed the heartbeat. However, newer agents such as lercanidipine act very precisely only on calcium channels in the wall of arteries and do not affect the heartbeat.
Absorption, degradation and excretion
Degradation occurs by enzymes in the liver (mainly CYP3A4). The degradation products are excreted in the urine and stool. Approximately eight to ten hours after ingestion, half of the absorbed active substance has been broken down.
When is lercanidipine used?
How lercanidipine is used
Lercanidipine is taken in the form of tablets. Because of its depot effect, it only needs to be swallowed once a day. It should be taken in the morning at least 15 minutes before breakfast.
The reason: meals, especially those containing fat, ensure that more active ingredient enters the circulation. If the drug is taken after a meal, for example, unpredictable fluctuations in blood pressure could occur.
If a stronger effect is desired, the active ingredient is combined with other antihypertensive agents (e.g., beta blockers, ACE inhibitors, or dehydrating agents) – increasing the dose would not improve the effect with lercanidipine.
Treatment of elevated blood pressure must be long-term.
What are the side effects of lercanidipine?
One in one thousand to ten thousand people treated experience side effects such as drowsiness, cardiac tachycardia, nausea, indigestion, diarrhea, vomiting, skin rashes, muscle pain, increased urination, and fatigue.
What should be considered when taking lercanidipine?
Contraindications
Lercanidipine should not be used in:
- decreased ejection rate of the heart
- @ women of childbearing age without a safe method of contraception
- heart failure (cardiac insufficiency)
- severe liver or kidney dysfunction
- patients who have had a heart attack in the last four weeks
- concomitant use of strong CYP3A4 inhibitors (including grapefruit juice, see below)
- concomitant use of ciclosporin (immunosuppressant)
Interactions
In addition to the above-mentioned CYP3A4 inhibitors (CYP3A4 inhibitors), there are also substances that have an opposite effect on the CYP3A4 enzyme system – they “induce” it. That is, they cause more of the enzyme to be produced. This causes lercanidipine to be broken down more quickly, which impairs its efficacy.
If lercanidipine is used together with digoxin (a drug for heart failure), the plasma level of digoxin may increase, thus enhancing its effect.
Consumption of alcohol may increase the antihypertensive effect of lercanidipine.
Age Limitation
Lercanidipine is approved for use in children 18 years of age and older. The safety and efficacy of therapy in children and adolescents under 18 years of age have not been established.
Pregnancy and lactation
Since data on its use during pregnancy and breastfeeding are still insufficient, lercanidipine should not be taken during this time.
How to obtain medicines containing lercanidipine
Preparations containing the active ingredient lercanidipine are available on prescription in Germany, Austria and Switzerland in any dosage and package size.
Since when is lercanidipine known?
In addition to fixed combinations with other antihypertensives, there are also preparations containing only the active ingredient lercanidipine. Since the patent expired, various generic versions have come onto the market.
