CAPOTEN ® Captopril

CAPOTEN ® is a captopril-based drug

THERAPEUTIC GROUP: Antihypertensives - ACE inhibitors not associated

Indications CAPOTEN ® Captopril

CAPOTEN ® can be used both alone 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 post-infarct 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 principle captopril, is rapidly absorbed in the gastro-intestinal tract, reaching its maximum plasma peak after about one "hour. Its bioavailability, which on average is around 75% of the total dose taken, can significantly decrease. in case of concomitant ingestion of food, up to 35%. The biological effect induced by the active principle is observed already after 15 minutes from the intake, to be maximized 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 salt and water retention - at the base of the pathogenesis of arterial hypertension. The antihypertensive effect also appears to be supported by the inhibition of kininase II, the enzyme responsible for the degradation of some molecules with a vasodilatory effect, such as bradykinin. At the end of its action, more than 75% of captopril is eliminated in the urine.
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

Singapore Med J. 2009 Apr; 50: 400-2.

Clinical efficacy of sublingual captopril in the treatment of hypertensive urgency.

Kazerani H, Hajimoradi B, Amini A, Naseri MH, Moharamzad Y.

This study tested the efficacy of captopril in the management of hypertensive crisis. In 53% of treated patients, the administration of 25 mg of sublingual captopril guaranteed a 25% decrease in initial blood pressure values ​​only one hour after "assumption. In the remainder, the additional intake of 25 mg of captopril ensured optimal control of blood pressure. A careful evaluation established that the non-responders to this therapy were patients who had previously undergone antihypertensive therapy.

2. CAPTOPRIL AND COGNITIVE FUNCTIONALITY

J Basic Clin Physiol Pharmacol. 2003; 14: 323-43.

Captopril and enalapril improve cognition and depressed mood in hypertensive patients.

Braszko JJ, Karwowska-Polecka W, Halicka D, Gard PR.

One of the side effects of hypertension is a slow deterioration of the mnemonic 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

Am J Physiol Heart Circ Physiol. 2005 Jul; 289: H20-9. Epub 2005 Mar 4.

Inhibition of NF-kappaB induces regression of cardiac hypertrophy, independent of blood pressure control, in spontaneously hypertensive rats.

Gupta S, Young D, Sen S.

Left ventricular hypertrophy is one of the pathological conditions most associated with the incidence of heart attack and cardiovascular diseases such as heart failure. Having defined the role of captopril in the prevention of these diseases, and in the induction of regression of left ventricular hypertrophy, the study in question seeks to elucidate 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 arterial hypertension the initial dose should be 50mg taken in one or two daily administrations. In case of reduced blood pressure control following at least 2/4 weeks of treatment, the doctor, after carefully evaluating the clinical picture of the patient, may decide to increase the dose up to 100 mg daily, or to combine a low-dose thiazide diuretic; 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 individual doses.
For the treatment of diabetic nephropathy, the recommended dosage remains in the range 75/100 mg daily, taking into account that in the case of impaired renal function the clearance of captopril may be reduced, with consequent increase in plasma levels. In these conditions it would be advisable to review the dosage, lowering it.
IN ANY CASE, BEFORE TAKING CAPOTEN ® Captopril - YOU NEED THE PRESCRIPTION AND CONTROL OF YOUR DOCTOR.

CAPOTEN ® Captopril warnings

Several studies in the literature associate the treatment with ACE inhibitors with conditions of facial, lingual and laryngeal angioedema, which could compromise normal respiratory capacity. In this case it would be necessary to immediately suspend the therapy, and to implement all possible interventions to avoid suffocation.
Particular attention in the formulation of the correct dosage should be paid in case of concomitant administration of other drugs with antihypertensive action, in order to avoid hypotensive crisis. For the same reason it would be advisable to carry out constant monitoring of blood pressure levels both before and during pharmacological intervention.
For particular categories of patients at risk, such as immunosuppressed or patients with impaired renal function, it is also necessary to monitor plasma levels of neutrophils, in order to avoid potentially very dangerous cases of neutropenia.
Serum potassium levels should be monitored in patients receiving concomitant therapy with potassium-sparing diuretics, or potassium salt supplements, in order to avoid cases of hyperkalaemia.
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 abilities, making the use of machinery and driving cars dangerous.

PREGNANCY AND BREASTFEEDING

It would be necessary to avoid taking CAPOTEN ® during the whole pregnancy, in order to avoid even irreversible damage to the fetus, and to 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 stop breastfeeding while taking CAPOTEN ® given the presence of studies in the literature that show 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 the therapeutic efficacy. In this case, however, if the correct dosage formulation allows a more effective blood pressure control, it is equally true that - if the dose of single compounds are unbalanced - they could increase cases of severe hypotension.
CAPOTEN ® can also interact with;

• Potassium supplements or potassium-sparing diuretics, resulting in 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;
• Corticosteroids and non-steroidal anti-inflammatory drugs, with increased salt and water retention and decreased antihypertensive effect;
• Negatively charged membranes, such as those from hemodialysis, with an increase in anaphylactic episodes;
• Salts of lithium, 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 impairment.
CAPOTEN ® is also contraindicated in pregnancy and breastfeeding.

Undesirable Effects - Side Effects

Rather frequent, but fortunately not clinically relevant, are episodes of skin rash and itchy erythema following the administration of CAPOTEN ®
Rarer, but potentially more dangerous, are the cases of angioedema, diseases of the gastro-inestinal tract and alteration of some blood parameters (neutrophilia, creatininemia and potassium).
To the aforementioned effects are added all those caused by incorrect blood pressure control, which could occur in case of incorrect dosage formulation, hypersensitivity to the active ingredient or a previous pathological condition (hypovolemia, renal insufficiency).

Note

CAPOTEN ® can only be sold under medical prescription.

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