drugs

CAPOTEN ® Captopril

CAPOTEN ® is a captopril-based drug

THERAPEUTIC GROUP: Antihypertensives - ACE inhibitors not associated

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

Indications CAPOTEN ® Captopril

CAPOTEN ® can be used both in monotherapy and in combination with other antihypertensive agents (especially thiazide diuretics), for the treatment of arterial hypertension.

CAPOTEN ® in combination with digitalis or diuretics, is also indicated in the treatment of congestive heart failure.

CAPOTEN ® can be used in post-infarction in patients with left ventricular dysfunction, and in patients with diabetic nephropathy with preventive action on the progression of renal damage.

Mechanism of action CAPOTEN ® Captopril

CAPOTEN ® in particular its active ingredient captopril, is rapidly absorbed in the gastro-intestinal tract, reaching its maximum plasma peak after about an hour. Its bioavailability, which averages around 75% of the total dose, can drop significantly in the case of concomitant food intake, up to 35%. The biological effect induced by the active principle is already observed after 15 minutes from the intake, to maximize within about an hour and a half.

The antihypertensive efficacy of captopril is due to the marked inhibition of the ACE enzyme, necessary to convert angiotensin I into its active metabolite, angiotensin II, thus preventing a series of biological effects - such as peripheral vasoconstriction and hydrosaline retention - at the base of the pathogenesis of arterial hypertension. The antihypertensive effect also appears to be supported by the inhibition of kininase II, an enzyme responsible for the degradation of some molecules with vasodilatory effect, such as bradykinin. After its action, captopril is eliminated by urine for over 75%.

In addition to the well documented and characterized hypotensive action, several studies also show a regressive action against left ventricular hypertrophy, with an improvement in ventricular contractile function.

These improvements, also accompanied by renal protection for patients with diabetic nephropathy, are able to guarantee a reduction in morbidity, hospitalization and mortality related to cardiovascular events.

Studies carried out and clinical efficacy

1 THE EFFECTIVENESS OF CAPTOPRIL IN THE HYPERTENSIVE CRISIS

This study tested the effectiveness of captopril in the management of hypertensive crisis. In as many as 53% of the patients treated, the administration of 25 mg of sublingual captopril ensured a 25% decrease in the initial blood pressure values ​​at a distance of only one hour from the intake. In the remaining cases, the further intake of 25 mg of captopril ensured optimal control of blood pressure. Careful evaluation established that non-responders to this therapy were patients who had previously undergone an antihypertensive therapy.

2. CAPTOPRIL AND COGNITIVE FUNCTIONALITY

One of the side effects of hypertension is a slow deterioration of the memory and cognitive abilities of the affected patient. The study in question shows how the administration of captopril can not only ensure better blood pressure control, but also significantly improve the patient's cognitive abilities, reducing the level of anxiety and depression.

3. CAPTOPRIL: experimental evidence for the regression of left ventricular hypertrophy

The left ventricular hypertrophy is one of the pathological conditions most associated with the incidence of infarction and of cardiovascular diseases such as heart failure. Having defined the role of captopril in the prevention of these diseases, and in the induction of the regression of left ventricular hypertrophy, the study in question tries to clarify the biological mechanisms underlying this effect. According to the Cleveland researchers, this action would be determined by the ability of captopril to inhibit the synthesis and secretion of NF-KB, a proinflammatory factor involved in the pathogenesis of hypertension and cardiac hypertrophy.

Method of use and dosage

CAPOTEN ® captopril 25/50 mg tablets: for the treatment of high blood pressure the initial dose should be 50 mg taken in one or two daily administrations. In case of reduced blood pressure control after at least 2/4 weeks of treatment, the doctor, after carefully evaluating the patient's clinical picture, may decide to increase the dose up to 100 mg daily, or to associate a low thiazide diuretic dosage; in the latter case the dosage of CAPOTEN ® should also be reviewed

For the treatment of congestive heart failure (hospital treatment), the dosage - which should always be between 25 mg / day and 150 mg / day - should be formulated by the doctor, after a careful evaluation of the pathological picture and with constant monitoring of blood pressure levels. Particular attention should be paid in case of concomitant administration of drugs, such as diuretics and digitalis, with a re-evaluation of the single doses.

For the treatment of diabetic nephropathy, the recommended dosage remains in the 75/100 mg daily range, taking into account that in case of reduced renal function the clearance of captopril could be reduced, with consequent increase in plasma levels. Under these conditions it would be advisable to review the dosage, lowering it.

IN ANY CASE, BEFORE TAKING CAPOTEN ® Captopril, THE REQUIREMENT AND CHECK OF YOUR DOCTOR IS NECESSARY.

Warnings CAPOTEN ® Captopril

Several studies in the literature associate conditions of ACE inhibitors with conditions of facial, lingual and laryngeal angioedema, which could compromise normal respiratory capacity. In this case it would be necessary to stop the therapy immediately and implement all possible interventions to avoid suffocation.

Particular attention in the formulation of the correct dosage should be placed in case of concomitant administration of other drugs with antihypertensive action, in order to avoid hypotensive crises. For the same reason it would be advisable to carry out, both before and during the pharmacological intervention, a constant monitoring of blood pressure levels.

For particular categories of patients at risk, such as immunosuppressed or patients with impaired renal function, it is also necessary to monitor the plasma levels of neutrophils, in order to avoid cases of neutropenia, potentially very dangerous.

Serum potassium levels should be monitored in the case of patients receiving concomitant therapy with potassium-sparing diuretics, or potassium salt supplements, in order to avoid cases of hyperkalemia.

Given the renal metabolism of captopril, an adjustment of the doses would be necessary in patients with renal insufficiency, in order to avoid a too marked and potentially dangerous biological effect. It is also important to remember that some side effects (mainly headache, dizziness and drowsiness) related to antihypertensive therapy could reduce the patient's normal perceptive and reactive capacities, making it dangerous to use machinery and drive vehicles.

PREGNANCY AND BREASTFEEDING

It would be necessary to avoid taking CAPOTEN ® during the entire pregnancy, in order to avoid even irreversible damage to the fetus, and prefer - in case of real need - other antihypertensive drugs with a reduced risk profile for the health of the fetus.

It would be necessary to suspend breast-feeding while taking CAPOTEN ® due to the presence of studies in the literature showing the secretion of ACE inhibitors in breast milk.

Interactions

There are several documented interactions for CAPOTEN ®, ​​some of which are used for therapeutic purposes. A classic example is the combination of captopril with other antihypertensive drugs, in order to improve therapeutic efficacy. In this case, however, if the correct dosage formulation allows a more effective blood pressure control, it is also true that - if the dose of the single compounds is not very balanced - the cases of severe hypotension could increase.

CAPOTEN ® can also interact with;

  • Potassium-supplementing potassium or diuretics, causing an increase in plasma levels of this element;
  • hypoglycemic drugs, with an increase in the hypoglycemic effect probably due to the increased sensitivity to insulin;
  • Non-steroidal corticosteroids and anti-inflammatory drugs, with increased salt and water retention and reduction of the antihypertensive effect;
  • Negatively charged membranes, such as those from hemodialysis, with an increase in anaphylactic episodes;
  • Lithium salts, with consequent accumulation and increase of cytotoxic effects.

Contraindications CAPOTEN ® Captopril

The use of CAPOTEN ® is not recommended in case of innate hypersensitivity to one of its components, aortic stenosis and severe renal function impairment.

CAPOTEN ® is also contraindicated in pregnancy and lactation.

Undesirable effects - Side effects

Quite frequent, but fortunately not clinically relevant, are episodes of skin rash and itchy rash following the administration of CAPOTEN ®

Rarer, but potentially more dangerous are the cases of angioedema, gastro-intestinal tract diseases and alteration of some blood parameters (neutrophilia, creatininemia and potassium).

In addition to these effects, there are all those caused by incorrect blood pressure monitoring, which could occur in the event of incorrect dosage formulation, hypersensitivity to the active ingredient or previous pathological condition (hypovolemia, renal insufficiency).

Note

CAPOTEN ® is salable only under medical prescription.