Amlodipine + Nebivolol - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

Beta-blockers

Calcium channel blockers

Included in the formulation

Nebilong AM

pills inwards

Micro Labs Limited India

АТХ:

C.07.F.B Selective beta-1 blockers in combination with other antihypertensive drugs

Pharmacodynamics:

Combined antihypertensive drug.

Amlodipine

Selective calcium channel blocker II class. Has antianginal and antihypertensive effect. 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.

Nebivolol

The racemate, which consists of two enantiomers: SRRR-nebivolol (Dnebivolol) and RSSS-nebivolol (LNebivolol), combining two pharmacological actions:

D-nebivolol is a highly selective competitive blocker of β₁-adrenoceptors;

L-nebivolol stimulates the release of the relaxing factor (NO) from the vascular endothelium, providing a vasodilating action.

Competitively and selectively blocks synaptic and postsynaptic β₁-adrenoceptors, making them inaccessible to catecholamines, modulates the release of the endothelial vasodilating factor of nitric oxide. Reduces high blood pressure under stress, physical stress and at rest. It reduces the frequency of cardiac contractions during physical activity and at rest, reduces the activity of the renin-angiotensin-aldosterone system.

Slows atrioventricular conduction, suppresses pathological automatism of the heart muscle.

Pharmacokinetics:

Amlodipine

After oral administration up to 80% absorbed in the gastrointestinal tract. The maximum concentration in the blood plasma is achieved in 6-12 hours. It binds to plasma proteins by 97.5%. Penetrates through the blood-brain barrier. Metabolised in the liver.

The half-life is 30-50 hours.

Elimination by the kidneys in the form of metabolites. It is not removed during hemodialysis.

Nebivolol

After oral administration, up to 80% is absorbed in the gastrointestinal tract.The maximum concentration in the blood plasma is achieved after 0.5-2 hours. The connection with plasma proteins is 97%.

The hypotensive effect develops 1-2 weeks after the start of the treatment. Metabolism in the liver.

Half-life is 6-7 days. Elimination by the kidneys and with feces.

Indications:

It is used for the treatment of arterial hypertension, prevention of angina attacks. Used as part of complex therapy for heart failure.

ICD-10

IX.I10-I15.I15 Secondary Hypertension

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

IX.I20-I25.I20 Angina pectoris [angina pectoris]

IX.I30-I52.I50.0 Congestive heart failure

Contraindications:

Severe renal and hepatic insufficiency, acute myocardial infarction, aortic stenosis, arterial hypotension, anuria, hereditary angioedema, shock, pheochromocytoma, metabolic acidosis, Reynaud syndrome, sinus node weakness syndrome, bradycardia (heart rate below 60 beats per minute), individual intolerance, children under 18 years.

Carefully:

Hypokalemia, hyponatremia, Renovascular hypertension, psoriasis, hypersensitivity.

Pregnancy and lactation:

Recommendations for FDA - Category C. Contraindicated in pregnancy and lactation.

Dosing and Administration:

Inside for 2.5-5 mg once a day in the morning. If necessary, increase the dose to 10 mg per day. A stable therapeutic effect is achieved in 2-4 weeks.

The highest daily dose: 10 mg.

The highest single dose: 10 mg.

Side effects:

Nebivolol

Central and peripheral nervous system: dizziness, headache, depression, drowsiness, nightmares, hallucinations, fainting.

Respiratory system: shortness of breath, bronchospasm.

The cardiovascular system: orthostatic hypotension, atrioventricular blockade, cardialgia, Raynaud's syndrome, edema.

Digestive system: dry mouth, nausea, vomiting, diarrhea, constipation.

Dermatological reactions: itching, aggravation of psoriasis.

Sense organs: dry eyes.

Allergic reactions.

Amlodipine

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

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

Digestive system: nausea, gingival hyperplasia.

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

urinary system: rarely - polyuria.

Reproductive system: gynecomastia, erectile dysfunction.

Allergic reactions.

Overdose:

Nebivolol

Cardiogenic shock, loss of consciousness, coma, cardiac arrest.

Treatment. Intravenous 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.

Amlodipine

Headache, arrhythmia. In severe cases - loss of consciousness, coma.

Treatment is symptomatic. Antidotes are calcium preparations. Hemodialysis is ineffective, plasmapheresis is recommended.

Interaction:

Amlodipine

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 inhalational anesthetics, tricyclic antidepressants, nitrates, cimetidine, diuretics causes an increase in hypotensive effect.

Incompatible with rifampicin, as it accelerates the metabolism of slow calcium channel blockers.

Increases the concentration of indirect anticoagulants in the blood plasma.

Nebivolol

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 nebivolol together with cimetidine.

Special instructions:

In chronic renal failure, the dose of the drug is adjusted: creatinine clearance of 15-35 ml / min - 50 mg per day, with creatinine clearance less than 15 ml / min - 50 mg every other day.

When giving general anesthesia to patients receiving nebivolol, means with minimal inotropic action are used. Before surgery, it is recommended to stop taking the medication 48 hours before the operation.

Stop taking the drug should be gradual.

In the treatment it is not recommended to drive vehicles and work with moving mechanisms.

Instructions

Amlodipine + Nebivolol (Amlodipinum + Nebivololum)