Felodipine

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

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Indications Felodipine

Presence of pathologies for taking the medication:
Felodipine is indicated for use if the patient has:

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

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Release form

Felodipine is released to the pharmaceutical market in the form of prolonged-release tablets with different amounts of the active substance: two and a half, five and ten milligrams.
A plate may contain ten, fifteen or thirty tablets. With the presence in the package of:

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

Each package contains official instructions for use of the medication.

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Pharmacodynamics

The drug has a blood pressure-lowering and antianginal effect. It belongs to the dihydropyridine group of "slow" calcium passage blockers. Blood pressure is reduced due to a decrease in the resistance of distant vessels. Felodipine has a dose-dependent anti-ischemic effect. It has virtually no effect on the cardiac conduction system. It also does not have a negative inotropic effect, protects against complications of blood flow restoration and reduces the size of myocardial infarction.

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Pharmacokinetics

Due to the fact that Felodipine tablets are isolated with an additional shell, its slow release occurs. This helps to increase the adsorption period, so the accumulation of the drug occurs evenly throughout the day. Absorption occurs in the gastrointestinal tract almost without residue. Bioavailability does not depend on the dose and is about fifteen percent. The drug binds to proteins, mainly albumins, almost one hundred percent.
Producing inactive metabolites, the metabolism occurs entirely in the liver. The half-life is about twenty-five hours. Accumulation of the drug does not occur even with prolonged use.
Special groups of patients
In people who belong to the elderly category of the population compared to the young, the density of Felodipine in the blood serum is higher.
In people with impaired renal function, as well as those undergoing hemodialysis, the pharmacokinetics is no different.
Seventy percent of the drug is excreted in the urine, the rest, in the form of metabolites, in the feces. Half a percent is excreted unchanged in urine.
There is information about Felodipine penetration through the placenta and into mother's milk.

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Dosing and administration

It is advisable to take the medication orally in the morning, before eating or after a light breakfast. The pills do not need to be chewed, crushed, divided or crushed.
Recommendations for taking the drug vary depending on the pathological process:
High blood pressure
For adults and the elderly, the dose is selected individually. The initial dose is five milligrams once a day. If such treatment does not bring the desired effect, the dose can be gradually increased to ten milligrams. In patients with impaired liver function and the elderly, treatment should begin with two and a half milligrams.
Stable angina
The dose is also selected individually. 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 keeping in mind that such treatment can enhance the hypotensive effect of Felodipine, so 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.

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Use Felodipine during pregnancy

Data from animal tests indicate that the drug cannot be used during gestation and lactation.

Contraindications

Felodipine should not be used in case of the following pathological conditions:
1. Individual hypersensitivity to the drug or any of its components;
2. Unstable angina;
3. Myocardial infarction, as well as the period lasting one month after it;
4. Cardiogenic shock;
5. Clinically important stenosis of the aorta;
6. The period of gestation and breastfeeding;
7. Chronic heart failure in the decompensation stage;
8. Low blood pressure;
9. If the patient is under eighteen years of age.

Side effects Felodipine

Like other similar drugs, Felodipine may have such undesirable effects as: increased heart rate, facial erythema, increased fatigue. This effect may occur at the beginning of treatment or with an increase in dose, and is reversible. Due to precapillary vasodilation, the patient may experience remote edema. If the patient suffers from periodontitis, he may experience slight swelling of the gums. To prevent this from happening, you need to carefully monitor oral hygiene.
Possible systemic undesirable effects:

• cardiovascular: increased blood flow to the skin of the face and its pronounced hyperemia, increased heart rate, fainting, severe decrease in blood pressure, leukocyte vasculitis;
• nervous system: paresthesia;
• Gastrointestinal tract - nausea, stomach pain, vomiting, increased activity of liver enzymes, inflammation of the gums;
• musculoskeletal system: joint pain, muscle pain;
• allergy: skin rash, itching, increased sensitivity to ultraviolet radiation;
• urinary system: increased frequency of urination.

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Overdose

If the recommended dosage of Felodipine is significantly exceeded, the patient may experience the following symptoms: a strong decrease in blood pressure and bradycardia.
To relieve this condition, it is necessary to conduct therapy aimed at the symptoms.
With a greatly reduced pressure, the patient should lie on his back and raise his legs. And with bradycardia, 0.5 - 1.0 mg of Atropine should be administered intravenously immediately.
If these measures are not enough, it is necessary to increase the amount of blood by intravenous administration of Dextrose, NaCl or Dextran. And it is also necessary to conduct treatment with a group of drugs aimed at alpha-adrenoreceptors.

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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 this does not require changing the recommended dose of Felodipine;
• with such drugs as: Erythromycin, Ketoconazole, Cimetidine and Itraconazole, when interacting, there is an increase in the level of Felodipine density in the serum, with a simultaneous slowdown in its metabolism;
• when interacting with such medications as: Carbamazepine, Phenytoin, Rifampicin and barbiturates, the level of Felodipine density in the blood decreases;
• drugs that are classified as non-steroidal anti-inflammatory drugs do not affect its hypotensive effect;
• the high level of Felodipine binding to drugs does not affect the binding of free union of some drugs (for example, Warfarin);
• This medication should not be taken with grapefruit juice;
• the hypotensive effect of Felodipine will increase if it is used together with beta-blockers, diuretics and Verapamil;
• Serum Tacrolimus levels should be monitored and dosage adjustments may be necessary if used with Felodipine;
• Felodipine, when used together, has virtually no effect on the pharmacokinetics of Cyclosporine. And Cyclosporine increases its maximum density (by 150%) and AUC (by 60%).
• Cimetidine increases Cmax and AUC of Fedodipine by fifty-five percent.

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Storage conditions

Felodipine is a potent drug. It should be kept in places safe from light and children.

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Special instructions

Reviews
Due to the different reactions of patients to the use of Felodipine, opinions about it, as well as about almost all drugs that reduce blood pressure, are ambiguous.
There are no negative reviews about the action and undesirable effects if the drug is suitable for the patient. But if the drug is not suitable, in the information space you can find a lot of information about its various side effects.
That is why you should not judge whether you need to use the drug or not by reading reviews of Felodipine. If a patient needs to use drugs that reduce blood pressure, he must definitely consult a doctor. This is necessary to prescribe the necessary dosage and treatment regimen for the patient, according to his medical history and the severity of symptoms.

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Shelf life

The medicine can be stored for two years.

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