Metoprolol + Felodipine (Metoprololum + Felodipinum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Beta-blockers

Calcium channel blockers

Included in the formulation
  • Logimax®
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    AstraZeneca AB     Sweden
    • АТХ:

    C.07.F.B.02   Metoprolol in combination with other antihypertensive agents

    Pharmacodynamics:

    Metoprolol

    Selective β1-blocker, which does not have internal sympathomimetic activity. Has antihypertensive, antiarrhythmic, antianginal action. In therapeutic doses does not affect the tone of peripheral arteries.

    Reduces the effect of catecholamines on the heart muscle, thereby reducing the heart rate, minute and shock volumes of blood within 24 hours.

    Eliminates the effects of arrhythmogenic factors: tachycardia, arterial hypertension, increased content of cyclic AMP.

    Antianginal action is due to a decrease in myocardial oxygen demand with prolonged diastole and improved perfusion of the heart muscle.

    Felodipine

    Vasoselective blocker of slow calcium channels. Has antianginal and hypertensive action. Prevents the entry of extracellular calcium into the muscle cells of the coronary and peripheral arteries. In high doses, it inhibits the release of calcium ions from intracellular stores. Does not affect the tone of the veins.

    Strengthens the coronary blood flow, improving the blood supply of ischemic zones of the myocardium, does not cause a "robbery syndrome". Expands peripheral arteries, reduces overall peripheral resistance, postnagruzku and the need for myocardium in oxygen. Does not affect the drivers of rhythm: sinoatrial and atrioventricular nodes. Has a weak antiarrhythmic effect.

    It enhances kidney blood flow, causes a moderate natriuresis.

    The clinical effect is noted 2-4 hours after administration and lasts for 1 day.

    Pharmacokinetics:

    Metoprolol

    The maximum concentration is achieved in 2-4 hours. Metoprolol binds to plasma proteins up to 16%. Poorly penetrates the blood-brain barrier, penetrates the placenta.

    The half-life of metoprolol is 3-7 hours. Partially metabolized in the liver, eliminated by the kidneys: 5% unchanged and 95% - in the form of metabolites. When hemodialysis is not excreted from the blood plasma.

    Felodipine

    After oral administration, it absorbs up to 50% in the gastrointestinal tract. The maximum concentration in the blood plasma is reached after 3-5 hours. It binds to plasma proteins by 65%.Penetrates through the blood-brain barrier. Metabolised in the liver.

    The elimination half-life is 25 hours. For repeated application, up to 45 hours.

    Elimination in the form of inactive metabolites 70% with feces, 30% with urine. It is not removed during hemodialysis.

    Indications:

    It is used for the treatment of hypertension in cases where monotherapy with beta-blockers or blockers of slow calcium channels does not have the desired clinical effect.

    ICD-10

    IX.I10-I15.I10   Essential [primary] hypertension

    Contraindications:

    Cardiogenic shock, atrioventricular blockade of II-III degree, bradycardia, chronic cardiac insufficiency, resistant to the action of cardiac glycosides, bronchial asthma, renal and hepatic insufficiency.

    Individual intolerance.

    Carefully:

    Chronic bronchitis with an asthmatic component, obliterating arterial diseases, atrioventricular blockade of the 1st degree, disturbances of the water-electrolyte balance; stenosis of the mitral valve, acute disorders of cerebral circulation, renal and hepatic insufficiency.

    Pregnancy and lactation:Recommendations for FDA - Category D without teratogenicity.Not applicable in pregnancy and lactation.
    Dosing and Administration:

    Inside 1 tablet (50 mg metoprolol and 5 mg felodipine) in the morning, if necessary - 2 times a day.

    The highest daily dose: 2 tablets.

    The highest single dose: 1 tablet.

    Side effects:

    Metoprolol

    Central nervous system: dizziness, insomnia, asthenia.

    Respiratory system: shortness of breath, rarely - bronchospasm

    The cardiovascular system: bradycardia, atrioventricular blockage, cold extremities.

    Blood System: neutropenia, thrombocytopenia.

    Sense organs: "dry eye syndrome", transient visual impairment.

    Gastrointestinal tract: dyspepsia, diarrhea, or constipation.

    Reproductive system: lowering the potency.

    Leather: hyperhidrosis.

    Allergic reactions.

    Felodipine

    Central and peripheral nervous system: dizziness, headache, with prolonged use - paresthesia of the extremities, depression.

    The cardiovascular system: possibly exacerbation of angina in the first days of taking the drug, flushing of the blood to the skin of the face, tachycardia.

    Musculoskeletal system: myalgia, convulsions of the upper and lower extremities.

    Digestive system: nausea, gingival hyperplasia.

    Urinary system: rarely - polyuria.

    Allergic reactions.

    Overdose:

    Metoprolol

    Symtomas: pronounced bradycardia, arterial hypotension.

    Treatment: intravenously 1-2 mg. atropine, 2.5 μg / kg dobutamine, intravenously bolus 10 mg glucagon, intravenously drop 10-20 μg isoprenaline at a rate of not more than 5 μg / min.

    Felodipine

    Symtomas: headache, arrhythmia. In severe cases - loss of consciousness, coma.

    Treatment: symptomatic. Antidotes are calcium preparations. Hemodialysis is ineffective, it is recommended that plasmapheresis is performed.

    Interaction:

    Metoprolol

    Increases the concentration of ethanol in the blood and lengthens its excretion.

    Potentiates the effect of lidocaine in systemic application.

    Negative dromo-, foreign, chromotropic influences are intensified with simultaneous admission with amiodarone, anesthetics, antiarrhythmics, digoxin, diltiazem, verapamil.

    Increases the bioavailability of metoprololol with cimetidine.

    Felodipine

    Incompatible with alcohol. The intake of grapefruit juice slows the absorption of the drug.

    Simultaneous use of the drug with antihypertensive drugs, as well as inhalation anesthetics,tricyclic antidepressants, nitrates, cimetidine, diuretics leads to an intensification of the hypotensive effect.

    It is not compatible with rifampicin, as it accelerates the metabolism of slow calcium channel blockers.

    Increases the concentration of indirect anticoagulants in blood plasma.
    Special instructions:

    Discontinue taking the drug gradually (for 8-10 days).

    Before an operative intervention it is necessary to inform the anesthesiologist about taking the drug by the patient.

    Instructions
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