Nifedipine swelling of the feet
Earlier I told about the group of calcium antagonists in general and preparations of the subgroup of verapamil. Today I will talk about the remaining (second) subgroup of nifedipine and its three main drugs - nifedipine, amlodipine and lercanidipine. Subgroup of nifedipine due to a similar chemical structure is also called dihydropyridine derivatives. This name is often found in the medical literature, so it is useful to remember it.
Common generic nifedipine: cordafen, cordafleks (including Cordaflex retard ), cordipin (incl. Kordipin XL ), Corinfar, nifecard XL, phenygidine.
The terms retard and XL mean preparations with delayed action. which are taken much less often than conventional dosage forms, usually 1-2 times per day.
Nifedipine is a common and relativelyinexpensive preparation. Produced in tablets of 10 and 20 mg, there are retard (delayed) forms of 20, 30, 40 and 60 mg. Nifedipine is almost not used for parenteral administration due to the photosensitivity of the drug (it is destroyed in the light).
Parenteral administration (from the Greek. para - about, enteron - gut) - the way of administration of medicines, bypassing the gastrointestinal tract. Parenteral administration includes subcutaneous, intramuscular and intravenous administration of drugs.
Nifedipine is the ancestor dihydropyridine subgroup calcium channel blockers - calcium antagonists that dilate peripheral vessels (including coronary vessels), but do not act on the heart itself. Unlike verapamil. nifedipine:
- does not have a significant effect on myocardial contractility,
- does not reduce heart rate and does not affect AV conduction,
- can be combined with beta-blockers.
Because nifedipine dilates the peripheral blood vessels (including the heart vessels) and does not affect the myocardium. then a decrease in blood pressure causes a reflex activation of sympathodrenal system by the principle of negative feedback. The blood concentration increases catecholamines (adrenaline, norepinephrine ), which increase heart rate and increasethe excitability of the myocardium, which contributes to the occurrence of cardiac arrhythmias. Vascular expansion and a drop in blood pressure lead to a decrease in the heart load (antianginal effect), which is leveled (smoothed) by the increase in heart rate. so It is recommended to combine nifedipine with a beta-blocker. which reduces heart rate and blood pressure.
Clinical researches nifedipine showed that short-acting forms of nifedipine (ie, conventional tablets, not retard) increased mortality of patients from heart attack. which is due to increased myocardial excitability, increased tachycardia (high heart rate), and an increase in the frequency of cardiac arrhythmias due to the activation of the sympathoadrenal system.
Nifedipine 10 mg valid up to 4-6 hours. therefore should be taken 3-4 times a day. which is inconvenient for the patient. Because of the need for frequent admission and an increased risk of death, nifedipine 10 mg It is impossible to use for constant treatment of arterial hypertension. For these purposes, only extended (retard) forms of nifedipine can be used (they are 20-60 mg each, taken no more often 1-2 times a day and should always swallow whole without chewing ) and preferably under the cover of beta-blockers. However, for the ongoing treatment of hypertension, there are now more modern, convenient and safe calcium antagonists: amlodipine. lercanidipine which will be discussed below.
Since nifedipine is not suitable for continuous use, it is usually used only for relief (treatment) of hypertensive crises. For this purpose a tablet of 5-10 mg must be chewed in the mouth. where the drug is absorbed sublingually ("under the tongue "). The onset of the effect begins in 10-15 minutes. reaches a maximum in 20-30 minutes and lasts up to 2-4 hours. In most cases, this is faster than an ambulance arrives. Self-healing crisis requires caution and re-measurement of blood pressure after administration. Excessive decrease Blood pressure is typical for 2 categories of patients:
- at stenosis (narrowing) of the carotid arteries. Stenosis is possible, for example, with atherosclerosis.
- in patients with myocardial infarction. in which the blood supply of the myocardium depends on the pressure in the arteries of the heart. As nifedipine expands and these vessels, the pressure in them decreases, which can worsen the blood supply to the myocardium.
Compared with verapamilcontraindications for nifedipine significantly less :
- individual hypersensitivity,
- arterial hypotension (too low blood pressure, upper below 90-100 mm Hg),
- cardiogenic shock,
- aortic stenosis (constriction of aortic valve aperture, impeding the exit of blood from the left ventricle into the aorta).
Side effects partially similar to side effect verapamil :
- headache, dizziness,
- arterial hypotension,
- redness of the face, sweating,
- Pastose on the ankles and legs, pour in until puffiness. Pastosity - initial, poorly expressed degree of puffiness of the skin (from Italy. pastoso - doughy),
- weight gain,
- hyperplasia (proliferation) of mucous gums,
- palpitation, tachycardia,
- muscle cramps,
- violations of sexual function (impotence).
When taking nifedipine, the so-called paradoxical effects. the increase in angina attacks, the appearance of episodes (periods) of myocardial ischemia at loads due to syndrome of stealing. There are also withdrawal syndrome (I described it in detail in the description of beta-adrenoblokatorov) - a marked rise in blood pressure, increased attacks of angina pectoris, etc.
With long-term administration of nifedipine occurs weakening of its antianginal action (those. reduces the ability of nifedipine to eliminate pain in the attack of angina ). For example, after 2 months of taking nifedipine at an average daily dose of 75-90 mg, it was noted significant shortening of the duration of the effect from 5.4 hours to 3.6 hours (third! ). With the resumption of admission after a break of 8-10 days, the effectiveness of nifedipine was only partially restored. I note that the effect verapamil reaches a maximum after 2 months of constant admission, the effect amlodipine - After 1 week, lercanidipine - After 2-4 weeks. Thus, of all the drugs listed nifedipine is an the most unfortunate for continuous reception.
This drug second generation from the group of nifedipine. Issued in tablets of 2.5, 5 and 10 mg .
Is different 24-hour action. that allows to take amlodipine only 1 time per day. Well reduces blood pressure and has an antianginal effect. Unlike nifedipine does not increase the heart rate. Amlodipine has also been identified antiatherogenic properties. those. it can slow the development of atherosclerosis.
In general, the drug is good and convenient, but it also has drawbacks. The main side effect - swelling of the legs and feet. These swelling are not associated with heart failure. Diuretics ineffective. According to my very subjective estimates, edema occurs in 30-40% of patients. I'll tell you a story from my experience.
The first time I came across severe swellingshins and feet after taking amlodipine almost 10 years ago. I still remember the patient with heart failure, who took among other things digoxin and amlodipine. Then I did not guess how to properly help her. Has written off edemas on intimate or cardiac insufficiency at which legs or foots really can swell. The solution came later, when a relative with similar pronounced edemas of the feet approached me, complaining that she could no longer wear her usual shoes. I had to think about it. Edema was significant, appeared in just a couple of weeks, and there were no visible reasons for the increase in heart failure (heart attacks and arrhythmias). I managed to remember that swelling of the shins was mentioned among the side effects nifedipine. But my cousin among other drugs took amlodipine. which belongs to the group nifedipine and therefore can also have a similar collateralEffect. And indeed, the edema of the shins was indicated in the instructions to amlodipine. I myself appointed this amlodipine a month ago because of high blood pressure. Now I advised amlodipine to cancel and promised that in a month there would be no swelling on my legs. Thinking like this: if they arose in a month, then for a month they should "disperse". The relative, of course, doubted that her legs would be normal in a month, but my calculation was correct. The authority of the "young doctor" also increased significantly
Summarizing all written, I can say that amlodipine - a good drug for the "price-quality ratio", if the patient does not develop swelling, because of which amlodipine has to be canceled.
At the moment in Russia is available Levamladipine (a drug that consists entirely of a levorotatory variety of Amlodipine) under the trade name Es Corinth. It does not cause edema, but is much more expensive. The details are below.
Lercanidipine is a new drug from the group of nifedipine, it has become widespread only in the last couple of years. The drug has lipophilicity ("loves fat ", I.e. fat-soluble), therefore accumulates in the lipid membranes of cells and acts for a long time. Because of the high lipophilicity, with fatty foods increases absorption 3-4 times. therefore to avoid overdose it is recommended to take lercanidipine at least 15 minutes before meals .
Like amlodipine, lercanidipine is taken only 1 time per day. Prolonged use of lercanidipine slows the pathological changes in the vascular wall. caused by increased arterial pressure (it reduces hypertrophy of the muscular layer of the vascular wall and weakens endothelial dysfunction). Lercanidipine also has a significant anti-ischemic (antianginal) action and has a cardioprotective effect, inhibiting oxidative stress and weakening the narrowing effect of endothelin-1 on cardiac vessels. There is evidence that lercanidipine improves cerebral blood flow. which is especially good for old people. All these effects of lercanidipine make it a first-line drug for treatment of arterial hypertension in patients with ischemic heart disease .
Lercanidipine does not affect the lipid composition of the blood. but in experiments he prevented the development of atherosclerosis. The antiatherogenic effect of lercanidipine does not depend on the effect on blood pressure level and lipid levels in the blood. Unlike verapamil and diltiazem. lercanidipine does not inhibit myocardium. but in comparison with nifedipine - does not cause tachycardia (palpitation).
In addition, lercanidipine has proven nephroprotective effect. that is, protects the kidneys from the effects of high blood pressure.
Lercanidipine is a the most selective (selective) drug from the group of nifedipine. acting only on the vessels and not affecting the myocardium. Due to the high selectivity, lercanidipine causes side effects less often other preparations of your group. Compared with nifedipine and amlodipine edema of the shins and other side effects (headache, palpitations, skin rashes) were recorded reliably less often - the differences in frequency were from 2 to 11 times depending on the clinical study.
For lercanidipine (as for amlodipine ) is characteristic slow increase in antihypertensive action. The maximum antihypertensive effect of the drug is detected after 2-4 weeks of treatment (a decrease in blood pressure by 10-20 mm Hg), so the initial dose of lercanidipine (10 mg once a day ) should be doubled no earlier than 2 weeks from the start of treatment.
It is recognized that lercanidipine is a modern, highly effective, long-acting antihypertensive drug for treatment of arterial hypertension of any stage and severity. It can be successfully used as a monotherapy, and in combination with any other (with the exception of dihydropyridine calcium antagonists) antihypertensive drugs.
- Nifedipine can be used only for the treatment of hypertensive crisis (urgent reduction of elevated blood pressure). Nifedipine is not suitable for permanent use.
If you have enough money, then after consulting with your doctor, you can start with lercanidipine. If there is little money, it is wiser to begin treatment with amlodipine. since depending on the trade names used, it costs many times cheaper lercamena. If there are significant side effects, then you need to switch to levalodipine (EsCord Cor) or lercam. EsCordi Cor is cheaper 2 times than Lercamen.
Important addition for July 2014
Amlodipine is a mixture in a 1:1 two optical isomers (levorotatory and dextrorotatory). Optical isomers are arranged identically and differ from each other in the same way as a person has a left and right hand or a left and right shoe. It turned out that for all the useful effects corresponds to the levorotatory S (-) isomer (Latin sinister - left), which is 1000 times more actively associated with dihydropyridine receptors than the R (+) isomer (Latin rectus - right). For this reason, dosages levmatodipina 2 times lower than amlodipine .
The S (-) isomer was internationally named Levamladipine .
Application Levamlodipina instead Amlodipine allows dramatically reduce the number of side effects and reduce the therapeutic dose by 2 times. After the transfer of 314 patients who experienced edema due to admission Amlodipine. on Levamladipineedema disappeared in 98.7% of patients. Read more: http://rmj.ru/articles_6163.htm
In Russia, only one drug of Levamlodipine is registered under the name Es Corinth. Produced in tablets of 2.5 and 5 mg, which are equivalent to 5 and 10 mg of amlodipine. Es Corinth costs many times more than usual Amlodipine. but 2 times cheaper Lercamena. Therefore, Es Corinth cheaper than Lercamenom .
In Belarus Es Corinth not registered.
In Ukraine it is sold Azomex .
Turchak Andrey (1 comment).
24 May, 2013 at 18:24
It is accessible and intelligibly all is written. All is spread out on the shelves. How do you feel about the S-isomer of Amlodipine?
The author's answer :
If pharmacologists prove the benefitsS-stereoisomer in comparison with the racemic mixture and a separate drug will be released, it will make sense to use it and evaluate the "price-benefit" ratio. At this time, instead of Amlodipine, it is more appropriate to use Lercanidipine.
8 November, 2013 at 17:09
S-isomer Amlodipine is not used anywhere except Russia, Ukraine, India and third world countries. This drug does not have all the properties of a full amlodipine, not to mention Lercamen
19 February, 2014 at 22:49
The drug S-amlodipine - Azomex, has long been coined. The advantage of levorotatory isomers, in comparison with racemic isomers, is proved even earlier. Google - and you will find.
The author's comment :
Thank you. It's a pity that Azomex is sold only in Ukraine. In Russia and Belarus it is not registered.
11 July, 2014 at 20:06
drug S-amlodipine (levorotatory molecule) -"EsCord Cor," working with him a long time, really works. when transferred from ordinary amlodipine, edema in 99% goes away, and Lercamena is 2 times cheaper. But our grannies do not particularly want to switch to it - they used to drink amlodipine for 20 rubles and they "scored" for swelling for a long time.
The author's comment :
Unfortunately, in EkCord Kor not sold.
20 February, 2015 at 00:11
The market for lercanidipine, producedthe Italian company "Recordati", under the name "Zanidip-Recordati" in dosages of 10 mg and 20 mg (tablets are divisible). It is cheaper than Lercamena, the price is within 400 rubles.
Elena Nikolaevna (2 comments).
February 25, 2015 at 14:18
What an inaccuracy!
Amlodipine is an antagonist of slow calcium channels of the 3rd generation and can in no way be referred to the group of nifedipine, a slow-release calcium channel antagonist of the 2nd generation.
The author's answer :
Here we used a simplified division of allantagonists of calcium on 3 groups on effects on the myocardium: do not act (nifedipine, amlodipine), act (verapamil) and partially act (diltiazem). This is what patients really need to know.
Elena Nikolaevna (2 comments).
February 26, 2015 at 01:19
It is generally known that calcium antagonists(English name) are divided into dihydropyridine and non-dihydropyridine and have a different degree of selectivity in the effects on the myocardium, vessels and the conducting system, and it is already incompatible to call dihydropyridines by the nifedipine group. As for the frequency of edema on amlodipine: it is wrong to mislead the patients with their subjective opinion: their frequency is from 4 to 10% (according to the data of randomized studies in Norvascus).
And one more inaccuracy: useful properties (antiatherosclerotic, antiproliferative, just provides the R-isomer of amlodipine, which is small in lercanidipine.In addition, amlodipine has a readout: stable and vasospastic angina, as it really reduces angina attacks, and in lercanidipine - alas, it is undesirable to prescribe it in IHD.
The author's comment :
The word "(not) dihydropyridine" to patients nothingI do not use it, so I do not use it. The division of calcium antagonists into groups based on the name of the parent drug is used (specifically), even in the textbook "Clinical Pharmacology", ed. Kukes (5th edition, 2015). As for the subjective opinion about the incidence of swelling, it is based on observations of Belarusian patients who are almost never treated with Norvac (an original drug). In Belarus, cheaper generics are used (the price is 2-10 times less). I completely admit that Norvasc will give a lower incidence of swelling.
1 March, 2015 at 21:27
Norvasc is a good drug, doroguschy truth,so few people take it, and it is less likely to swell than to cheap amlodipine. The golden mean is EsCordi Cor, it is quite affordable, 250 rubles in my opinion for 2.5 mg (this is like 5 amlodipine), and there is almost no edema.