drugs

CATAPRESAN ® Clonidine

CATAPRESAN ® is a clonidine based drug

THERAPEUTIC GROUP: Antihypertensives - imidazoline receptor agonist

IndicationsAction mechanismStudies and clinical effectiveness Usage and dosage instructionsWarnings Pregnancy and lactationInteractionsContraindicationsUndesirable effects

Indications CATAPRESAN ® Clonidine

CATAPRESAN® is indicated in the treatment of all forms of high blood pressure.

Mechanism of action CATAPRESAN ® Clonidine

CATAPRESAN ® taken orally, is easily absorbed in the gastro-enteric tract, reaching good blood concentrations, also considering the absence of a first-pass metabolism. Once in circulation, clonidine - the active ingredient of CATAPRESAN ® is rapidly distributed in the various tissues, maintaining the active form for about 13 hours and being then metabolized in p-hydroxyclonidine (pharmacologically inactive) or eliminated intact mainly through the urine.

The antihypertensive action of CATAPRESAN ® is exerted by its active ingredient, clonidine, which, by easily crossing the blood-brain barrier, is able to act at the level of the central nervous system, reducing the activation of the sympathetic system, peripheral renal resistance, cardiac rhythm and arterial pressure, also thanks to the reduction of the sensitivity of the smooth muscle cells of the arterioles to constricting vessel mediators such as Norepinephrine.

These effects are guaranteed by the ability of the aforementioned active principle to selectively activate pre synaptic Alpha 2 receptors of the central nervous system, consequently reducing the production of catecholamines (especially norepinephrine), and thus shifting the balance towards the biological effects induced by the parasympathetic system.

Studies carried out and clinical efficacy

1 CLONIDINE AND HYPERTENSION

The treatment of arterial hypertension can include different useful drugs, each with a different mechanism of action and with a specific effectiveness. This study conducted on more than 1200 patients suffering from hypertension, tried to test the efficacy of various drugs taken alone (monotherapy) in reducing blood pressure. Among the tested medicines, clonidine was ranked third, after diltiazem and atenolol, guaranteeing a lowering of blood pressure up to normal values ​​in about 50% of treated patients.

Despite this, the choice of therapy should also take into account individual susceptibility to a certain type of drug, and the potential achievable side effects.

2. CLONIDINE AND CARDIAC INSUFFICIENCY

This study shows that the sympatholytic effect of clonidine may have a dual role in the management of the patient suffering from heart failure. The benefits deriving from low-dose therapy with clonidine would guarantee a significant attenuation of the sympathetic tone, not only at the cardiac level, but also at the renal level, thus allowing a better regulation of the hydro-saline retention.

3. CLONIDINE NOT ONLY AN ANTI-SUMMARY

Clonidine has for years been used solely for its marked antihypertensive actions. Recent studies, on the other hand, have evaluated a series of associated effects that could expand the range of therapeutic applications. In this study, in fact, the efficacy of clonidine in the perioperative phase as an anxiolytic, sedating and stabilizing heart rate and arterial pressure was evaluated. The results seem to be encouraging, both for the cardioprotective action and for the reduced need for pre-operative anesthetics and sedatives, required. In order for clonidine to enter into common clinical practice, it is still necessary to study its pharmacokinetics in order to reduce the potential side effects.

Method of use and dosage

CATAPRESAN ® tablets of 150 mcg of clonidine: it is suggested the initial intake of ½ - 1 tablet per day, taken in the evening in the case of mild hypertension or in patients particularly susceptible to the pharmacological action of clonidine.

CATAPRESAN ® tablets of 300 mcg of clonidine: it is used in the treatment of severe hypertension, resorting to attack doses equal to 1 tablet taken 2/3 times a day.

In any case, the correct dosage - both in the attack and maintenance phases - should be formulated by the doctor after a careful evaluation of the patient's physiopathological conditions and the severity of his pathology.

IN ANY CASE, BEFORE TAKING CATAPRESAN ® Clonidine - THE REQUIREMENT AND CHECK OF YOUR DOCTOR IS NECESSARY.

Warnings CATAPRESAN ® Clonidine

The hypotensive action of CATAPRESAN ® could be accompanied, especially in the first phase, by drowsiness and sedating effect, for which - in case of persistence of such effects - it would be appropriate to adapt the pharmacological therapy. The interruption of the use of CATAPRESAN ® must in any case take place gradually, with a progressive decrease in the dose taken in order to avoid a rebound hypertension accompanied by agitation, headache and nervousness.

In patients suffering from renal insufficiency, for whom the individual response is subject to enormous variability, when necessary, continuous monitoring for the eventual recalibration of the treatment plan would be important.

The same attention must be maintained also for patients suffering from severe coronary insufficiency, cerebrovascular diseases, cardiac affections such as recent myocardial infarctions and brady-arrhythmia, or Raynaud's disease (characterized by circulatory disorders, evident above all in the hands and feet).

It is also important to consider that the possible depressive effects induced by CATAPRESAN ® could worsen the condition of psychiatric patients, accentuating these symptoms.

The hypotensive action, but above all the sedative action of CATAPRESAN ® could reduce the patient's perceptive and reactive capacities, making the driving of vehicles and the use of machinery dangerous.

CATAPRESAN ® ineffective in case of pheochromocytoma-induced hypertension.

PREGNANCY AND BREASTFEEDING

Although data on the prolonged administration of CATAPRESAN ® on the health of the fetus are not yet known, its use is not recommended during pregnancy, as clonidine can easily pass the placental barrier and reduce the fetal heart rate, exposing it also to potential rebound risks at the time of delivery.

Given the absence of data on the effect of clonidine during lactation, it would be preferable to avoid taking it.

Interactions

The hypotensive action of CATAPRESAN ® can be enhanced by the simultaneous administration of other antihypertensive drugs, such as diuretics, calcium antagonists, ACE inhibitors. This synergy can be used for therapeutic purposes in the case of patients refractory to monotherapy, and must necessarily provide for an adjustment of the dosages of individual drugs.

In contrast, the therapeutic action of CATAPRESAN ® could be inhibited by non-steroidal anti-inflammatory drugs, tricyclic antidepressants or other drugs, which increase water-saline retention.

In addition, alcohol and digitalis glycosides can alter the normal function of clonidine.

Contraindications CATAPRESAN ® Clonidine

The use of CATAPRESAN ® in individuals who are hypersensitive to one of its components and metabolites is not recommended in the case of severe bradyarrhythmia and atrio-ventricular block.

Undesirable effects - Side effects

The side effects found following the use of CATAPRESAN ® are generally of minor clinical relevance and are destined to disappear once drug therapy is suspended.

In most cases these are gastro-enteric reactions such as dry mouth, nausea, vomiting, loss of appetite and constipation, accompanied by nervous symptoms such as sedation, fatigue, confusion, perceptive disorders, hallucinations, depression and general malaise.

Rare cases of impotence, reduced libido, and heart rhythm alterations have also been described.

The side effects due instead to hypersensitivity to one of the compounds of the drug are generally of a dermatological character and include skin rashes, hives, itching and alopecia.

Note

CATAPRESAN ® is salable only under medical prescription.