Presolar

Atenolol:

• Pharmacological action
• Pharmacokinetics
• Why is Presolar prescribed?
• Dosage and administration
• Presolar (Atenolol) side effects, adverse reactions
• Presolar contraindications
• Using during pregnancy and breastfeeding
• Special instructions
• Presolar drug interactions
• Presolar in case of emergency / overdose
• Presolar (Atenolol) reviews

Pharmacological action

Presolar is a cardioselective beta1-blocker without intrinsic sympathomimetic activity. This medication has antihypertensive, antianginal and antiarrhythmic action. Presolar (Atenolol) reduces the stimulatory effect on the heart sympathetic innervation and circulating catecholamines.

The hypotensive effect of this drug is associated with a decrease in minute volume of blood, decreased activity of the renin-angiotensin system (has a greater significance for patients with initial hypersecretion of renin), sensitivity of baroreceptors of the aortic arch (not going to enhance their activity in response to decreased blood pressure) and the effect on the CNS; manifested lower both systolic and diastolic blood pressure, decreasing stroke volume and cardiac output. In the medium therapeutic doses it has no effect on the tone of peripheral arteries.

The antianginal effect of Presolar (Atenolol) is associated with decreased myocardial oxygen demand by decreasing heart rate (lengthening of diastole and improved myocardial perfusion) and contractility, as well as reduced sensitivity to the effects of myocardial sympathetic innervation. Decrease in heart rate occurs at rest and during exercise.

The antiarrhythmic effect of this medicine is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increase of cAMP, hypertension), decrease in the rate of spontaneous excitation of the sinus and ectopic pacemakers and slowing of AV conduction.

The hypotensive effect lasts 24 hours, with regular admission is stabilized by the end of 2 weeks of treatment. The negative chronotropic effect is manifested by 1 h after administration, reaches a maximum after in 2-4 hours and lasts up to 24 hours.

Pharmacokinetics

After oral administration the absorption of Presolar (Atenolol) from the gastrointestinal tract is 50-60%, its bioavailability is 40-50%. This drug is practically not metabolized in the body; poorly penetrates the BBB. The plasma protein binding is 6-16%. T_1/2 is 6-9 h. Presolar (Atenolol) is primarily excreted by the kidneys in unchanged form. Renal dysfunction accompanied mainly to the increase of T_1/2 and cumulation. This medication is excreted during hemodialysis. For elderly patients T_1/2 of Presolar (Atenolol) is increased.

Why is Presolar prescribed?

Hypertension, hypertensive crisis, mitral valve prolapse, cardiac hyperkinetic syndrome of functional origin, neurocirculatory dystonia of hypertensive type.

Treatment: coronary artery disease, angina pectoris (stress, rest and unstable).

Treatment and prevention of: myocardial infarction (acute phase in stable hemodynamic parameters, secondary prevention).

Arrhythmias (including at the general anesthesia, congenital syndrome prolongation QT, myocardial infarction without signs of congestive heart failure, thyrotoxicosis), sinus tachycardia, paroxysmal atrial tachycardia, supraventricular and ventricular premature beats, supraventricular and ventricular tachycardia, atrial tachyarrhythmia, atrial flutter.

Essential and senile tremor, agitation and tremors withdrawal syndrome.

In the combined therapy: hypertrophic obstructive cardiomyopathy, pheochromocytoma (only in combination with alpha-blockers), hyperthyroidism; migraine (prophylaxis).

Dosage and administration

The dosing regimen of Presolar is set individually. The usual dose for adults for oral administration at the beginning of treatment is 25-50 mg 1 time / day. If necessary the dose is increased gradually. If impaired renal function in patients with CC 15-35 ml / min - 50 mg / day; with CC less than 15 ml / min - 50 mg every other day.

The maximum dose for adults for oral administration is 200 mg / day in 1 or 2 doses.

Presolar (Atenolol) side effects, adverse reactions

Cardiovascular system: in some cases - bradycardia, hypotension, AV-conduction disturbances, symptoms of heart failure.

Digestive system: at the beginning of therapy it is possible nausea, constipation, diarrhea, dry mouth.

CNS and peripheral nervous system: at the beginning of therapy may be fatigue, dizziness, depression, mild headache, sleep disturbances, coldness and paresthesia in extremities, reduced reactivity of the patient, reducing the secretion of tear fluid, conjunctivitis.

Endocrine system: reduced potency, hypoglycemic state in patients with diabetes.

Respiratory system: in predisposed patients - symptoms of bronchial obstruction.

Allergic reactions: itching.

Other: increased sweating, redness of the skin.

Presolar contraindications

AV-block II and III degree, sinoatrial block, SSS, bradycardia (HR < 40 bpm), hypotension (in case of myocardial infarction, systolic blood pressure less than 100 mm Hg), cardiogenic shock, congestive heart failure IIB-III stages, acute heart failure, Prinzmetal's angina, lactation, concomitant use of MAO inhibitors, hypersensitivity to Presolar (Atenolol).

Using during pregnancy and breastfeeding

Presolar crosses the placental barrier, so use during pregnancy is only possible if the intended benefits to the mother justifies potential risk to the fetus.

Presolar (Atenolol) is excreted in breast milk, so if you need to use during lactation is recommended to stop breastfeeding.

Category effects on the fetus by FDA - D.

Special instructions

With caution use this medication in hepatic failure.

Presolar (Atenolol) should be used with caution in diabetes, COPD (including asthma, emphysema), metabolic acidosis, hypoglycemia, allergic reactions, a history of chronic heart failure (compensated), obliterating peripheral arterial disease (intermittent claudication, Raynaud's syndrome), pheochromocytoma, liver failure, chronic renal insufficiency, myasthenia gravis, hyperthyroidism, depression (including in history), psoriasis, pregnancy, elderly patients, in pediatrics (the efficacy and safety are not defined).

While taking Presolar (Atenolol) it can decrease tear fluid production, which is important for patients who use contact lenses.

Cancellation of this drug after prolonged treatment should be carried out gradually under medical supervision.

Upon the termination of the combined use of Presolar (Atenolol) and clonidine, clonidine treatment continued for several days after discontinuation of Presolar (Atenolol), otherwise you may experience severe arterial hypertension.

When the need for inhaled anesthesia in patients receiving Presolar (Atenolol) Meliapharm, a few days before anesthesia to stop taking Presolar (Atenolol) or find a medication for anesthesia with minimal negative inotropic effects.

Patients whose work requires high concentration, the question of outpatient use of Presolar (Atenolol) should be addressed only after an assessment of individual response.

Presolar drug interactions

Antiarrhythmic and anesthetic facilities increase cardiodepressive action of this drug (increased risk of developing bradycardia, arrhythmia, hypotension, heart failure).

Reserpine, methyldopa, clonidine, guanfacine, cardiac glycosides potentiate the negative chrono-, drome- and bathmotropic effect, insulin and other antidiabetic funds - hypoglycemia.

NSAIDs, estrogens, sympathomimetics, xanthines weaken the anti-hypertensive effect, absorption; sympatholytic, nitroglycerin, hydralazine, and other antihypertensive drugs increase it; antacids slow down this medication absorption.

Cimetidine inhibits the metabolism of Presolar (Atenolol) Meliapharm.

This medication prolongs the action of anti-depolarizing muscle relaxant, anticoagulant effect of coumarins.

Three / tetracyclic antidepressants, antipsychotics, sedatives, hypnotics and alcohol potentiate CNS depression.

Presolar (Atenolol) is incompatible with MAO inhibitors.

Presolar in case of emergency / overdose

Symptoms: bradycardia, AV block II-III degree, heart failure, respiratory failure, hypotension, bronchospasm, hypoglycemia.

Treatment: gastric lavage and the appointment of adsorbing medications; Symptomatic treatment: atropine, isoprenaline, orciprenaline, cardiac glycosides or glucagon, diuretics, pressor agents (dopamine, dobutamine or norepinephrine), selective beta-adrenoceptor agonists, IV glucose solution, installation of an artificial pacemaker. Perhaps dialysis.

Nifedipine:

• Pharmacological action
• Pharmacokinetics
• Why is Presolar prescribed?
• Dosage and administration
• Presolar (Nifedipine) side effects, adverse reactions
• Presolar contraindications
• Using during pregnancy and breastfeeding
• Special instructions
• Presolar drug interactions
• Presolar in case of emergency / overdose
• Presolar (Nifedipine) reviews

Pharmacological action

Presolar is aSelective calcium channel blocker class II, a derivative of dihydropyridine. This medication inhibits the entry of calcium into cardiomyocytes and vascular smooth muscle cells. Presolar (Nifedipine) has antianginal and hypotensive action. This drug lowers the tone of vascular smooth muscle. Presolar (Nifedipine) dilates coronary and peripheral arteries, lowers blood pressure and slightly - myocardial contractility, reduces afterload and myocardial oxygen demand. This medicine improves coronary blood flow. Presolar (Nifedipine) practically does not possess antiarrhythmic activity, it does not inhibit the conductance of myocardium.

Pharmacokinetics

When administered orally Presolar (Nifedipine) is rapidly absorbed from the gastrointestinal tract. This drug undergoes metabolism in the "first pass" through the liver. The protein binding is 92-98%. Presolar (Nifedipine) metabolized in the liver to form inactive metabolites. T_1/2 is about 2 hours. This medication excreted mainly by the kidneys as metabolites in trace amounts in unchanged form; 20% is excreted from the gut in the form of metabolites.

Why is Presolar prescribed?

Prevention of angina attacks (including vasospastic angina), in some cases - relief of angina attacks, hypertension, hypertensive crises, Raynaud's disease.

Dosage and administration

The dosing regimen is individual. For oral administration the initial dose is 10 mg 3-4 times / day. If necessary the dose gradually increased up to 20 mg 3-4 times / day. In some cases for a short time the dose can be increased to 30 mg 3-4 times / day. For relief of hypertensive crisis, as well as angina attack this drug can be used sublingually in 10-20 mg (rarely 30 mg).

To IN relieve an angina attack or hypertensive crisis - 5 mg for 4-8 hours.

Intracoronary dose for relief of acute coronary artery spasm injected bolus is 100-200 mcg. With stenosis of major coronary vessels starting dose is 50-100 micrograms.

The maximum daily dose: oral - 120 mg, IV - 30 mg.

Presolar (Nifedipine) side effects, adverse reactions

Cardiovascular: flushing of the skin, a feeling of warmth, tachycardia, hypotension, peripheral edema; rarely - bradycardia, ventricular tachycardia, asystole, increased angina attacks.

Digestive system: nausea, heartburn, diarrhea, rarely - liver function impairment and in rare cases - gingival hyperplasia. The chronic administration in high doses may cause dyspeptic symptoms, elevated liver enzymes, intrahepatic cholestasis.

CNS and peripheral nervous system: headache. The chronic administration in high doses may cause paresthesia, muscle pain, tremors, visual disturbances light, and sleep disorders.

Hemopoietic system: in rare cases - leukopenia, thrombocytopenia.

Urinary system: an increase in daily diuresis. The chronic administration in high doses may cause renal dysfunction.

Endocrine system: in rare cases - gynecomastia.

Allergic reactions: skin rash.

Local reactions: for IV injections might burning at the injection site.

Within 1 min after intracoronary administration it can be a result in the negative inotropic action of Presolar (Nifedipine), the increase in heart rate, hypotension, and these symptoms gradually disappear within 5-15 minutes.

Presolar contraindications

Hypotension (systolic blood pressure below 90 mm Hg), collapse, cardiogenic shock, severe heart failure, severe aortic stenosis; increased sensitivity to Presolar (Nifedipine).

Using during pregnancy and breastfeeding

Adequate and well-controlled studies safety of Presolar in pregnancy was not been conducted. The use of Presolar (Nifedipine) in pregnancy is not recommended.

Because Presolar (Nifedipine) is excreted in breast milk, you should avoid its use during lactation or to stop breastfeeding during the treatment with this medication.

In experimental studies it have been revealed embryotoxic, fetotoxic and teratogenic effects of Presolar (Nifedipine).

Category effects on the fetus by FDA - C.

Special instructions

In patients with stable angina at the beginning of treatment paradoxical enhancement anginalnyh pain may occurs, with pronounced coronary sclerosis and unstable angina - the aggravation of myocardial ischemia. Not recommended to use short-acting drugs for long-term treatment of angina or hypertension, because it is possible the development of unpredictable changes in BP and reflex angina.

Presolar drug interactions

Nitrates, beta-blockers, diuretics, tricyclic antidepressants, fentanyl, alcohol increase the hypotensive effect of Presolar (Nifedipine) Quality Pharmaceutical Laboratory. This medication increases the activity of theophylline reduces the renal clearance of digoxin. Presolar (Nifedipine) increases the side effects of vincristine (reduced elimination); increases the bioavailability of cephalosporins (cefixime). Cimetidine and ranitidine increase the level of this drug in plasma. Diltiazem slows the metabolism (requires dose reduction of Presolar (Nifedipine)) of Presolar (Nifedipine) Quality Pharmaceutical Laboratory. This medicine is incompatible with rifampicin (accelerates biotransformation and does not allow to create effective concentration). Grapefruit juice (large quantity) increases its bioavailability.

Presolar in case of emergency / overdose

Symptoms: sudden bradycardia, bradyarrhythmia, hypotension, in severe cases - collapse, slowing conduction. When you receive a large number of retard-tablets symptoms of intoxication occur no earlier than 3-4 h and may additionally be expressed in loss of consciousness up to coma, cardiogenic shock, convulsions, hyperglycemia, metabolic acidosis, hypoxia.

Treatment: gastric lavage, activated charcoal method, injections of norepinephrine, calcium chloride or calcium gluconate in a solution of atropine (IV). Hemodialysis is ineffective.