Felodipine

Felodipine is a medical product that belongs to the group of calcium channel blockers.

[1], [2], [3]

Indications of the felodipine

Presence of pathologies for the use of medication:
Felodipine is indicated for admission in case the patient:

• arterial hypertension;
• angina (stable type or Prinzmetal, if there is an individual intolerance to beta-blockers or nitrates);
• pathology Reynaud.

[4], [5]

Release form

Felodipine is released to the pharmaceutical market in the form of long-acting tablets with different amounts of active substance: two and a half, five and ten milligrams.
The plate can be ten, fifteen or thirty tablets. With the presence in the package by:

• one, two, three or six cell plates (if ten tablets);
• one, two or four cell plates (if on fifteen tablets);
• one or two cell plates (if on thirty tablets).

In each package there is an official instruction on the use of the medication.

[6], [7], [8]

Pharmacodynamics

The drug has a reducing pressure and antianginal effect. It belongs to the blockers of the dihydropyridine group of "unhurried" calcium passages. Reduction of blood pressure occurs as a consequence of reducing the counteraction of distant vessels. The anti-ischemic effect of Felodipine is dose-dependent. The conductive system of the heart muscle has virtually no effect. Also not distinguished by a negative inotropic effect, protects from complications of resumption of blood flow and reduces the size of myocardial infarction.

[9], [10], [11], [12]

Pharmacokinetics

Due to the fact that Felodipine pills are isolated by an additional coating, its delayed release occurs. This contributes to an increase in the period of adsorption, so the accumulation of the drug occurs evenly throughout the day. Absorption is virtually without residue in the digestive tract. Bioavailability does not depend on the dose and is about fifteen percent. With proteins, mainly with albumins, the drug binds almost one hundred percent.
Producing inactive metabolites, the metabolism entirely passes in the liver. The half-life is about twenty five hours. Accumulation of medicament even with prolonged admission does not happen.
Special groups of patients
In people who belong to the elderly population compared to the young, the greater the density of Felodipine in the serum.
In people with impaired renal function, as well as those who undergo hemodialysis, the pharmacokinetics is not different.
Seventy percent of the drug is excreted with urine, the remainder, in the form of metabolites, with feces. At the same time, a half percent is displayed in unchanged form with urine.
There is information about the penetration of Felodipine through the placenta and into the mother's milk.

[13], [14], [15], [16], [17]

Dosing and administration

It is advisable to use the medication in the morning, before eating or after a small breakfast. Pills do not need to chew, crack, divide or grind.
Recommendations for the use of the drug differ depending on the pathological process:
Elevated pressure
For adults and the elderly, the dose is selected personally. The primary dose is five milligrams once a day. If such treatment does not bring the desired effect, you can gradually increase the dose to ten milligrams. In patients with impaired liver function and the elderly category, treatment should begin with two and a half milligrams.
Stenocardia of a stable type The
Dose is also selected personally. The initial dose should not exceed five milligrams per day, but if necessary, it can be slowly increased to ten milligrams. The maximum daily dose is twenty milligrams.
The drug can be used as a combination therapy, together with beta-blockers, angiotensin-converting enzyme (ACE) inhibitors or diuretics. But it is worth bearing in mind that such treatment can strengthen the hypotensive effect of Felodipine, therefore it is necessary to monitor the possible development of hypotension.
The recommended dose for patients with impaired liver function should be reduced.
Pharmacokinetics for patients with impaired renal function remains unchanged.

[19], [20], [21], [22], [23]

Use of the felodipine during pregnancy

The data on the carried out tests on animals testify to the impossibility of using the medication during gestation and lactation.

Contraindications

You can not use Felodipine in the case of such pathological conditions:
1. Individual hypersensitivity to the medicine or to any of its components;
2. Stenocardia of unstable type;
3. Myocardial infarction, and also a period of duration one month after it;
4. Cardiogenic shock;
5. Clinically important aortic narrowing;
6. Periods of gestation and breastfeeding;
7. Heart failure of a chronic nature in the stage of decompensation;
8. Low pressure;
9. If the patient is not yet eighteen years old.

Side effects of the felodipine

Like other similar drugs, Felodipine can have such undesirable effects as heart palpitations, face erythema, increased fatigue. This effect can occur at the beginning of treatment or with a dose increase, and have a reversible character. Because of precapillary vasodilation, the patient may have a distant swelling. If the patient suffers from periodontitis, he may have a small swelling of the gums. To avoid this, you need to carefully monitor the oral hygiene.
Possible unwanted effects on the system:

• cardiovascular: the flow of blood to the skin of the face and its pronounced hyperemia, rapid heart rate, blotch, a pronounced decrease in arterial pressure, leukocytic vasculitis;
• nervous system: paresthesia;
• Gastrointestinal tract, nausea, stomach pain, vomiting, increased activity of liver enzymes, inflammation of the gums;
• musculoskeletal system: pain in the joints, pain in the muscles;
• allergy: skin rash, seizure, increased sensitivity to ultraviolet radiation;
• urinary system: increased frequency of urination.

[18],

Overdose

If the recommended dosage of Felodipine is significantly exceeded, the patient may experience such symptoms: a marked decrease in blood pressure and a bradycardia.
To stop this condition, you need to conduct therapy aimed at symptoms.
With a greatly reduced pressure, the patient needs to lie on his back and raise his legs. And with bradycardia - should immediately intravenously lead 0.5 - 1.0 mg of Atropine.
In the event that these activities are not enough, you need to increase the amount of blood by intravenous injection of Dextrose, NaCl or Dextran. And also it is necessary to conduct treatment by a group of medicines directed action on alpha - adrenoreptors.

[24], [25], [26]

Interactions with other drugs

When using Felopin with certain medications, it is worth considering that:

• it increases the density of Digoxin in the blood serum, but it does not require a change in the recommended dose of Felodipine;
• with such drugs as: Erythromycin, ketoconazole, cimetidine and Itraconazole, the interaction increases the level of Felodipine in the serum, with a one-time slowing of its metabolism;
• when interacting with medications such as: carbamazepine, phenytoin, rifampicin and barbiturates, the level of Felodipine density in the blood decreases;
• medicines that belong to non-steroidal anti-inflammatory drugs do not affect its hypotensive effect;
• on the linkage of the free association of certain medical personnel (for example, Warfarin) is not affected in any way by the high level of Felodipine bonding with blebs;
• You can not combine this drug with grapefruit juice;
• There will be an increase in the hypotensive effect of Felodipine, if used together with beta-blockers, diuretics and Verapamil;
• It is necessary to control the level of Tacrolimus tightness in the blood serum and there will probably be a need to adjust the dose if used together with Felodipine;
• Felodipine, when used together, almost does not affect the pharmacokinetics of Cyclosporine. A Cyclosporin increases its maximum density (by 150%) and AUC (by 60%).
• Cimetidine increases Cmax and AUC of Fedodipine by fifty-five percent.

[27], [28], [29], [30], [31]

Storage conditions

Felodipine refers to a potent drug. It is worth keeping in places safe from the light and for children.

[32], [33], [34]

Special instructions

Reviews
Because of the different reactions of patients to the use of Felodipine, opinions about him, as in other and almost all medications that reduce blood pressure, are ambiguous.
There are no negative reviews about the action and undesirable actions if the medication is suitable for the patient. But if, the medicine has not approached, in the information space one can find a lot of information about its various side effects.
That is why it is necessary to judge whether a medication should be used or not, after reading the reviews about Felodin, it is not worth it. If a patient needs to use medications that reduce blood pressure, he must definitely consult a doctor. This is necessary for prescribing the patient the necessary dosage and treatment regimen, according to his anamnesis and the severity of the symptoms.

[35], [36], [37], [38]

Shelf life

The medication can be stored for two years.

[39], [40], [41], [42],