INDERAL ® is a drug based on propranolol hydrochloride.
THERAPEUTIC GROUP: Beta-blockers
IndicationsAction mechanismStudies and clinical effectiveness Usage and dosage instructionsWarnings Pregnancy and lactationInteractionsContraindicationsUndesirable effects
Indications INDERAL ® Propranolol
INDERAL ® is used as a therapeutic pharmacological support for the long-term treatment of essential hypertension. The optimization of hypotensive efficacy could also be achieved thanks to the concomitant administration of diuretics or other antihypertensive drugs.
INDERAL ® is also indicated in the treatment of angina pectoris (in case of reduced efficacy of conventional, pharmacological and non-pharmacological treatments), in the treatment of heart rhythm disorders, in the prophylaxis of migraine, in the control of anxiety, and as an adjunct in the thyrotoxicosis therapy.
Mechanism of action INDERAL ® Propranolol
Propranolol, taken by mouth with INDERAL ®, is rapidly absorbed at the gastro-intestinal level, reaching maximum plasma concentrations in a very short time (1 - 2 hours).
It is mainly metabolised in the liver, where through a first-pass effect it gives rise to pharmacologically active metabolites; bound to plasma proteins, it can then spread freely through the circulatory stream.
The therapeutic effects of propranolol, a non-cardioselective beta-blocker and without intrinsic sympathomimetic activity, are mainly due to the cardiovascular action exercised through competitive inhibition against beta-adrenergic receptors. This activity results in decreased frequency and cardiac output, an increase in the duration of the systole and a decrease in resting blood pressure; these effects allow a significant reduction in total oxygen consumption of the myocardium and cardiac work.
Another important activity, perhaps the main one, is the antiarrhythmic action of propranolol, which appears to be accomplished through a control of the discharge frequency of the cardiac conduction tissue.
The direct antihypertensive action, on the other hand, although widely observed in various clinical trials, has not yet been fully characterized.
The various metabolites produced at the hepatic level are subsequently excreted via the urine.
Studies carried out and clinical efficacy
Propranolol IN ANXIETY TREATMENT
The scientific literature shows the efficacy of propranolol in the treatment of anxiety disorders, although the molecular mechanism of action has not yet been clarified.
Probably this effect seems to be linked to the action on the central nervous system, through a modest passage of the blood-brain barrier.
2.propranolol AND HYPERTENSION
The efficacy of propranolol in the treatment of hypertension has been evaluated by several studies. Although propranolol is not the drug of first choice in the treatment of arterial hypertension, studies show that blood pressure can be reduced in 80% of treated patients in a few weeks of treatment.
3. THE PROPRANOLOL IN THE TREATMENT OF ALZHEIMER
The administration of propranolol in patients suffering from Alzheimer's disease has guaranteed an improvement in symptoms with a particular effectiveness in reducing aggression and increasing co-operativity.
Method of use and dosage
INDERAL ® propranolol 40 mg tablets or 80 mg propranolol with gradual release: in the treatment of high blood pressure the recommended initial dose is 40 mg of propranolol, taken twice a day.
The adjustment of the dose can be foreseen both in case of reduced therapeutic effect, and in case of altered liver function; in both situations the doctor should always consider the patient's physiopathological situation.
In the treatment of angina pectoris, 40 mg is used for two or three times a day, increasing the dosage - under strict medical supervision and if really necessary - up to 240 mg / day.
In the treatment of cardiac arrhythmias the useful dose appears to be that of 40 mg, three times a day.
In all other conditions, for which a therapeutic indication persists (thyrotoxicosis, tachycardia on an anxious basis, etc.) the effective dosages are between 80 and 160 mg per day.
IN ANY CASE, BEFORE TAKING INDERAL ® Propranolol - THE PRESCRIPTION AND CONTROL OF ITS OWN DOCTOR IS NECESSARY.
Warnings INDERAL ® Propranolol
Before starting therapy with INDERAL ® it would be advisable to carefully evaluate the patient's physiopathological conditions. In fact, particular attention in the administration is required in case of patients suffering from inadequately treated heart failure (for whom the drug is contraindicated), in patients with first degree atrioventricular block and in patients with reduced liver function, for which may need a dosage adjustment.
It is also necessary to consider that propranolol could mask some classic effects of hypoglycemia, such as tremor, so that, especially in diabetic patients, constant monitoring of glycemic levels would be appropriate.
Furthermore, beta blockers seem to increase sensitivity to allergens, aggravating their symptomatology.
Should it be necessary to suspend therapy, it would be advisable to provide for a gradual reduction in dosage, in order to avoid reactive side reactions. Moreover, possible side effects, such as dizziness, headache and drowsiness, could make the use of machinery and driving vehicles dangerous.
PREGNANCY AND BREASTFEEDING
Although the active ingredient has been found to be free of embryotoxic and teratogenic effects, the intake of INDERAL ® during pregnancy and lactation is contraindicated for possible hemodynamic alterations, responsible for a reduced placental flow, and metabolic, which may be at the base of complications even lethal at the time of delivery.
It would be advisable to suspend breastfeeding during therapy with INDERAL ® due to the possible secretion of the active ingredient in breast milk.
Interactions
Given the multiple pathways in which propranolol is involved, different drugs and active ingredients can alter the pharmacokinetic properties of this drug.
More precisely:
- Concomitant use of dihydropyridine may determine the incidence of hypotensive crises;
- The administration of cimetidine, hydralazine, ergotamine-based drugs, dihydroergotamine, prostaglandin inhibitors, glycosidic drugs, antiarrhythmics, alcohol and drugs with antidepressant action, can alter the normal pharmacokinetic characteristics of propranolol, causing an alteration of biological effects with increased incidence of adverse reactions.
Furthermore, given a potential increase in the insulin effect and the masking action of propranolol on some signs of hypoglycemia, it is necessary to monitor blood glucose levels in diabetic patients and possibly correct the hypoglycemic drug dosage.
INDERAL ® Propranolol Contraindications
INDERAL ® is contraindicated in patients with bronchial asthma or bronchopathies, hypersensitivity to one of its components, marked bradycardia, cardiogenic shock, hypotension, metabolic acidosis, renal failure, atrioventricular block, pheochromocytoma monotherapy, prinzmetal angina and node disease otherwise.
Undesirable effects - Side effects
Although INDERAL ® appears, from well-tolerated clinical studies and post-marketing experience, especially in the initial phase of treatment, minor side effects such as
cold sensation in the extremities, dizziness, headache, sleep disturbances and gastro-intestinal disorders.
In particular categories of patients at risk, the presence of bradycardia, hypotension, respiratory difficulties, hallucinations, mood disorders and alteration of some hemato-clinical parameters was also observed.
In most cases, all the above symptoms turned out to be transient; therefore suspending the intake of INDERAL ® gradually is back to normal.
Note
INDERAL ® is salable only under medical prescription.
the use of INDERAL ® in athletes, in the absence of therapeutic necessity, to reduce the physiological response to stress and the related symptoms (tremor of the limbs, increase in arterial pressure, increase in emotional tension etc.) is a DOUBLE practice.
