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Most popular brand: Inderal
Active ingredient: Propranolol
Available dosage forms: 10, 20, 40, 80 mg

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Propranolol general information

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PROPRANOLOL (propranolol)

Individual. When administered an initial dose of 20 mg, single dose – 40 – 80 mg, the frequency of reception – 2 – 3 times / day.

In / jet slowly – an initial dose of 1 mg; then after 2 minutes, the same dose is administered repeatedly. In the absence of the effect of possible re-introduction.

The maximum doses: at intake – 320 mg / day; after repeated administration in / jet cumulative dose – 10 mg (under the control of blood pressure and ECG).

From the central and peripheral nervous system: fatigue, weakness, dizziness, headache, drowsiness or insomnia, vivid dreams, depression, anxiety, confusion, hallucinations, tremors, nervousness, restlessness.

From the senses: a decrease in the secretion of lacrimal fluid (dry and sore eyes).

Cardio – vascular system: sinus bradycardia, the AV – block (up to the development of a complete transverse blockade and heart failure), arrhythmia, development (worsening) of chronic heart failure, reduced blood pressure, orthostatic hypotension manifestation of vasospasm (strengthening of peripheral blood circulation, cooling of the lower extremities, Raynaud’s syndrome), pain in the chest.

From the digestive system: nausea, vomiting, discomfort in the epigastric region, constipation or diarrhea, abnormal liver function (dark urine, yellow skin or sclera, cholestasis), changes in taste, increase in liver transaminases , LDH.

The respiratory system: nasal congestion, bronchospasm.

From endocrine system: change in the concentration of blood glucose (hypo – or hyperglycemia).

From the hematopoietic system: thrombocytopenia (unusual bleeding and hemorrhage), leukopenia.

Dermatological reactions: sweating, psoriasiform skin reactions, exacerbation of psoriasis symptoms.

Allergic reactions: itching, skin rash, hives.

Other: back pain, arthralgia, reduced potency, withdrawal syndrome (increased angina attacks, myocardial infarction, increased blood pressure).

Contraindications

AV – block II and III degree sinoatrial block, bradycardia (heart rate less than 55 beats / min.), Sick sinus syndrome, hypotension (systolic blood pressure less than 90 mm Hg, especially myocardial infarction), congestive heart failure IIB – stage III, acute heart failure, cardiogenic shock, hypersensitivity to propranolol.

Pregnancy and breastfeeding

The use of propranolol during pregnancy is possible only when the intended benefits to the mother outweighs the potential risk to the fetus. If necessary, use during this period must be careful monitoring of the fetus, for 48 – 72 hours prior to delivery of propranolol should be discontinued.

It should be borne in mind that the possible negative impact on the fetus: intrauterine growth retardation, hypoglycemia, bradycardia.

Propranolol is excreted in breast milk. If necessary, use during lactation should be set-up of the child or to stop breastfeeding.

Application for violations of liver function

C caution in patients with liver failure.

Application for violations of renal function

C caution in patients with renal failure.

Use in children

C caution in children (efficacy and safety are not defined).

The use in elderly patients

C caution in elderly patients.

C caution in patients with bronchial asthma, COPD, bronchitis, decompensated heart failure, diabetes, renal and / or hepatic insufficiency, hyperthyroidism, depression, myasthenia gravis, psoriasis, occlusive peripheral vascular disease, during pregnancy, during lactation, elderly patients, children (efficacy and safety are not defined).

During treatment possible exacerbation of psoriasis.

When pheochromocytoma propranolol can be used only after taking an alpha – blocker.

After a long course of treatment propranolol should be withdrawn gradually, under the supervision of a physician.

The treatment with propranolol should be avoided intravenously the introduction of verapamil, diltiazem. A few days prior to anesthesia should stop taking propranolol or pick up an agent for anesthesia with minimal negative inotropic effect.

Effects on ability to drive vehicles and management mechanisms

In patients whose activities require increased attention, the issue of the use of propranolol outpatient should be addressed only after an assessment of an individual patient’s response.

While the use of hypoglycemic agents there is a risk of hypoglycaemia by increasing the action of hypoglycemic agents.

In an application with MAO inhibitors, there is a possibility of adverse manifestations of drug interactions.

There are cases of bradycardia in the application of propranolol on the arrhythmia induced by digitalis drugs.

In an application with the means for inhalation anesthesia increases the risk of depression and myocardial function of arterial hypotension.

While the use of amiodarone may be hypotension, bradycardia, ventricular fibrillation, asystole.

In an application with verapamil may be hypotension, bradycardia, dyspnea. Increased C _max in the plasma increases the AUC, propranolol reduced clearance due to inhibition of its metabolism in the liver under the influence of verapamil.

propranolol has no effect on the pharmacokinetics of verapamil.

A case of severe hypotension and cardiac arrest while the use of haloperidol.

In an application with hydralazine increased C _max in plasma and AUC of propranolol. It is believed that hydralazine hepatic blood flow may reduce or inhibit the activity of liver enzymes, which leads to slow metabolism of propranolol.

With simultaneous use of propranolol can inhibit the effects of glibenclamide, glyburide, chlorpropamide, tolbutamide, because selective beta ₂ – blockers are capable of blocking & beta; ₂ – adrenergic receptors of the pancreas related to insulin secretion.

due to the action of sulfonylurea derivatives release of insulin from the pancreas is inhibited by beta – blockers, which to some extent hindered the development of hypoglycemic effect.

While the use of diltiazem increases the concentration of propranolol in plasma due to inhibition of its metabolism under the influence of diltiazem. There is an additive inhibitory effect on the activity of the heart due to the slowing of impulse conduction through the AV – node caused by diltiazem. There is a risk of severe bradycardia, significantly reduced stroke and minute volume.

In an application described cases increasing the concentration of warfarin and phenindione plasma.

While the use of doxorubicin in experimental studies have shown increase in cardiotoxicity.

With simultaneous use of propranolol prevents the development of bronchodilatory effect of isoprenaline, salbutamol, terbutaline.

In an application described cases increase imipramine plasma concentrations.

In an application with indomethacin, naproxen, piroxicam, acetylsalicylic acid may reduce the antihypertensive effect of propranolol.

In an application with ketanserin may develop an additive antihypertensive effect.

In an application with clonidine increased antihypertensive effect.

In patients receiving propranolol, in the case of abrupt withdrawal of clonidine may develop severe hypertension. It is believed that this is due to an increase in levels of catecholamines in the blood circulation and strengthening their vasoconstrictor action.

While the use of caffeine may decrease the effectiveness of propranolol.

In an application may increase the effects of lidocaine and bupivacaine (including toxic), on – apparently due to slow metabolism of the local anesthetic in the liver.

In an application with lithium carbonate, a case of bradycardia.

In an application described a gain side effects of maprotiline, driven by – apparently slowing its metabolism in the liver and cumulation in the body.

While the use of mefloquine increases the QT interval, described the case of cardiac arrest; morphine – dampening effect on the central nervous system, caused by morphine; sodium amidotrizoat – Cases of severe hypotension are described.

While the use of nisoldipine may increase C _max and AUC of propranolol and nisoldipine plasma, resulting in severe hypotension. There is a message about strengthening the beta – blocking action.

There are cases of increase C _max and AUC of propranolol, hypotension and heart rate decrease while the use of nicardipine.

While the use of nifedipine in patients with coronary artery disease may develop severe hypotension, increased risk of heart failure and myocardial infarction, which may be due to increased negative inotropic effects of nifedipine.

In patients receiving propranolol, there is a risk of severe arterial hypotension after the first dose of prazosin.

In an application with prenylamine increase the QT interval.

While the use of propafenone increased propranolol plasma concentration and develops a toxic effect. It is believed that inhibits propranolol metabolism of propafenone in the liver, decreasing its ground clearance and increasing serum concentration.

With the simultaneous application of reserpine and other antihypertensive drugs increases the risk of hypotension and bradycardia.

In an application enhanced C _max and rizatriptan AUC; rifampicin – propranolol decreases the concentration in the blood plasma; with suxamethonium chloride, tubocurarine chloride – can change the muscle relaxant action.

With simultaneous use of reduced theophylline clearance due to slowing its metabolism in the liver. There is a risk of bronchospasm in patients with asthma or COPD. Beta – blockers may block the inotropic effect of theophylline.

In an application with phenindione described some cases increased bleeding and no change in blood clotting.

While the use of flecainide may cardiodepressive additive effect.

fluoxetine inhibits the isoenzyme CYP2D6, which leads to the inhibition of metabolism of propranolol and its accumulation, and may enhance the action cardiodepressive (including bradycardia). Fluoxetine and, mainly, its metabolites are characterized by a long T _1/2 . so the likelihood of drug interactions is retained even after a few days after discontinuation of fluoxetine.

quinidine inhibits isozyme of CYP2D6, resulting in inhibition of metabolism of propranolol, reducing its clearance. Possible increase in beta – adrenoceptor blocking action, orthostatic hypotension.

In an application in plasma concentrations of propranolol are increased, chlorpromazine, thioridazine. Perhaps a sharp decrease in blood pressure.

cimetidine inhibits the activity of hepatic microsomal enzymes (including CYP2D6 isoenzyme), this leads to the inhibition of metabolism of propranolol and its accumulation: there has been increasing negative inotropic action and development cardiodepressive action.

In an application enhanced hypertensive effects of epinephrine, there is a risk of severe life-threatening hypertensive reactions and bradycardia. Decreases effect of sympathomimetic bronchodilator (epinephrine, ephedrine).

With the simultaneous use cases reduce the effectiveness of ergotamine described.

There have been reports of change in hemodynamic effects of propranolol while the use of ethanol.

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