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Plendil (Felodipine)

Description

Plendil is a dihydropyridine derivative, providing high selectivity in action on smooth muscle walls of arterioles. The recommended dosages neither have impact on myocardial contractility nor on conductivity. A decline of peripheral vascular resistance provided by the drug, helps to press for a blood pressure heart afterload reduction. The preparation helps to increase coronary blood flow and offers weakly pronounced diuretic and natriuretic properties, so they don’t cause fluid retention. Neither the drug causes orthostatic hypotension.

Pharmacokinetics

After ingestion the medication is absorbed almost completely from the gastrointestinal tract, regardless of food intakes. Its bioavailability is estimated at 15-20% (a pronounced effect of first pass through the liver); binding to plasma proteins level is marked at 99% (so it can traverse diffuse quite effectively). It penetrates through the blood-brain barrier, placenta, enters the timing. The preparation is metabolized in the liver to the level of inactive metabolites. 70% of the preparation is excreted in the urine, the rest is excreted with faeces. Renal impairment has no impact on the drug’s pharmacokinetics.

Indications

Plendil is prescribed to patients with with arterial hypertension angina and those suffering from Raynaud's disease.

Application

Dose is picked individually. The initial dose is 0.005 g once a day (in the morning). With the lack of severity of the hypotensive effect of the dose can be increased up to 0.01g or the treatment course can switch to another antihypertensive drug therapy. The pills must be swallowed without chewing with plenty of water. Patients taking felodipine, should avoid alcohol because it increases the risk of hypotension.

Side effects

The reception of the preparation may cause adverse reactions affecting the following parts:

- cardiovascular system manifestation: tachycardia, hypotension; transient flushing of the skin of the face.

- central nervous system: transient headache, dizziness, fatigue, and weakness.

The medication may also cause swelling in the ankle (as a result of precapillary vasodilation). Those suffering from gingivitis (periodontitis) may experience gums swelling. The drug may cause skin rash and itching.

Contraindications

Pregnancy, including the early period, tachycardia, hypotension, cardiovascular and cardiogenic shock, 1st week of acute myocardial infarction, vascular insufficiency, hypersensitivity to dihydropyridine derivatives.

Overdose

An excessive dosage may lead to hypotension and in some cases to abnormally slow heart action (bradycardia).

Treatment. An individual must take a horizontal position with legs raised. As bradycardia develops a 0.5-0.1mg of atropine must be injected intravenously. If a non-sufficient result is achieved, it’s necessary to increase blood plasma volume with an glucose, sodium chloride or dextran solutions.

Interaction properties

In the event of simultaneous reception with cimetidine the plasma concentration is increased by 50%. Other inhibitors of microsomal liver enzymes also increase the drug’s concentration in plasma. Simultaneous reception with microsomal enzyme inducers leads to a decrease of its concentration in plasma.

At the same time taking the drug increases digoxin concentration. NSAIDs doesn’t affect the hypotensive effect. Despite the high level of binding to plasma proteins, the medication has no impact on protein binding of other drugs. Beta-blockers, verapamil, antidepressants, diuretics increase the hypotensive effect of felodipine. Avoid using the drug with grapefruit juice.