Captopril – composition, action, dosage and side effects of the drug regulating blood pressure

Proven content

Captopril is a prescription drug mainly used in cardiology to treat diseases of the cardiovascular system. The active substance is captopril, an angiotensin converting enzyme inhibitor. Captopril is a drug that has been present on the pharmaceutical market for many years and has been successfully used in the treatment of hypertension, chronic heart failure, myocardial infarction and nephropathy. Currently, Captopril Jelfa and Captopril Polfarmex are available on the pharmacological market.

How does Captopril work and what is its composition? What indications and contraindications exist for its use? How to use Captopril and with what drugs not to combine it? What precautions should be taken while using it? Can taking this preparation cause side effects?

Captopril – general characteristics of the drug

Captopril is a drug used to treat cardiovascular diseases such as hypertension, chronic heart failure, myocardial infarction and nephropathy.

The active substance of the preparation is captoprylwhich belongs to angiotensin converting enzyme inhibitors.

The drug Captopril has been present on the pharmaceutical market for many years and its international name is Captoprilumi. Two preparations are available on the Polish pharmaceutical market: Captopril Jelfa and Captopril Polfarmex.

Captopril, regardless of the manufacturer, is in the form of tablets and comes in three doses: 12,5 mg, 25 mg and 50 mg. In both cases, the drug can only be purchased with a prescription issued by a doctor.

Captopril Jelfa is available in the following packages:

1. 20 tablets (for a dose of 50 mg);
2. 30 tablets (applies to all doses);
3. 40 tablets (for a 25 mg dose).

While Captopril Polfarmex is available in the following packages:

1. 30 tablets (applies to all doses);
2. 40 tablets (for a dose of 25 mg and 50 mg);
3. 90 tablets (for a dose of 25 mg and 50 mg).

The price of the drug from both manufacturers is non-refundable and depends on the dose and number of tablets in the package, ranging from PLN 5 to a maximum of PLN 12. Captopril should be kept out of the reach and sight of children in the original packaging at a temperature below 25 degrees Celsius.

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Captopril – composition and action of the drug

The active substance in Captopril is captopril, which belongs to a group of medicines called angiotensin-converting enzyme inhibitors. Medicines in this class work in common by inhibiting the enzyme angiotensin converting enzyme, which is responsible for the formation of angiotensin.

It acts by converting inactive angiotensin I into active angiotensin II. This substance causes arterial vessels to narrow and spasm. Its effect is also to increase the release of aldosterone, leading to an increase in blood pressure.

Action of Captopril it mainly reduces angiotensin II levels, thereby lowering blood pressure. In addition, drugs from this group intensify the effects that depend on a substance that has a vasodilating effect, i.e. bradykinin, having an antiatherosclerotic effect on the vessels.

Due to its properties, Captopril causes a decrease in blood pressure, increases venous capacity and lowers peripheral vascular resistance.

Captopril is used as a drug that lowers blood pressure and in the treatment and prevention of cardiovascular diseases, as well as in the treatment of kidney diseases (diabetic and non-diabetic nephropathy).

The active substance of the drug is rapidly absorbed and its antihypertensive effect begins 15-30 minutes after taking the drug, and is strongest after 60-90 minutes.

In addition to the active substance, Captopril contains auxiliary substances, including: colloidal anhydrous silica, lactose monohydrate, croscarmellose sodium and magnesium stearate.

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Captopril – indications for the use of the drug

Captopril is a drug which is always included in the treatment by the doctor. It is used in the treatment of diseases of the cardiovascular system.

Captopril is indicated primarily for the treatment of:

1. arterial hypertension;
2. chronic heart failure, in combination with diuretics, digitalis glycosides (which stimulate the heartbeat) and beta-blockers (used to treat high blood pressure) in the presence of decreased systolic function of the heart chambers;
3. Diabetic nephropathy (kidney disease) in type I diabetes mellitus: treatment of diabetic nephropathy with proteinuria in patients with type I diabetes;
4. patients after myocardial infarction – short-term, from 24 hours to 4 weeks after myocardial infarction, if the patient is clinically good or long-term;
5. asymptomatic left ventricular dysfunction after myocardial infarction in a clinically stable patient.

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Captopril – contraindications to the use of the drug

Captopril medicinal preparation, despite the indications for its use, cannot always be included in the treatment. The doctor individually assesses the risk that treatment with this preparation may cause in the patient.

The main contraindication to the use of Captopril is allergic (hypersensitive) to any of the ingredients or to any other angiotensin converting enzyme (ACE) inhibitor.

In addition, this drug is contraindicated for use if:

1. have ever had angioedema caused by treatment with angiotensin converting enzyme inhibitors or have hereditary (hereditary) angioedema;
2. the patient is in the second or third trimester of pregnancy (the use of the drug in the first trimester is also not recommended) and during breastfeeding;
3. you have diabetes or impaired kidney function and you are treated with a blood pressure lowering medicine containing aliskiren;
4. you are currently or have been taking a combination medicine containing sacubitril and valsartan (used to treat some type of long-term (chronic) heart failure in adults) as there is an increased risk of angioedema (rapid swelling of the tissue under the skin in an area such as the throat).

Particular caution should be exercised in patients with certain diseases or other circumstances that may constitute a contraindication to use or an indication for a change in the dosage of Captopril.

There are also situations in which, before using this preparation, it is necessary to make a detailed medical interview, and even carry out specific check-ups.

Particular caution should be exercised in some cases, because the preparation does not cause a sudden and significant reduction in blood pressure. The increased risk of arterial hypotension after taking the preparation and requiring close medical supervision applies especially to people:

1. with decreased circulating blood volume, dehydrated or electrolyte deficiency;
2. with increased activation of the renin-angiotensin-aldosterone system;
3. with severe congestive heart failure;
4. with an increased risk of myocardial or cerebral ischemia in severe hypotension.

If in doubt about the possibility of using Captopril, consult your doctor or pharmacist and inform about any diseases, ailments and medications you are taking.

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Captopril – dosage

Captopril is a prescription drug and it should be used only on the recommendation of a doctor, in accordance with his guidelines, who selects the dosage method, taking into account the individual situation and the patient’s health condition.

Dosage of Captopril it is also adjusted to the patient’s blood pressure. The recommended maximum dose of the drug is 150 mg daily.

Captopril should be administered before, during or after a meal. The tablets should be swallowed whole. The line on them is only to assist the swallowing of the tablet and should not be used to divide the tablet into equal doses. Sublingual administration of the drug is also allowed. This form of taking a tablet is recommended for high pressure surges.

The method of dosing and taking the drug Captopril it depends on the type of disease and individual response to the drug.

In case of high blood pressure, the recommended starting dose is 25 to 50 mg daily and should be given in two divided doses. Your doctor may gradually increase the dose, at intervals of at least two weeks, to a dose of 100-150 mg per day in two divided doses.

Captopril can be used alone or with other antihypertensive drugs, especially with thiazide diuretics, in which case it may be appropriate to administer the drug once a day.

Patients with a high activity of the renin-angiotensin-aldosterone system may be prescribed a single dose of 6,25 mg or 12,5 mg. Then your doctor will prescribe this dose twice a day. The dose may be gradually increased to 2 mg daily in one or two divided doses, and if necessary, up to 50 mg in one or two divided doses.

In patients with heart failure, a starting dose of 6,25 to 12,5 mg, given two or three times a day, is recommended. Depending on the patient’s response, clinical condition and drug tolerance, the doctor may increase the dose to 75-150 mg daily. Your doctor may decide to gradually increase the dose, at intervals of at least two weeks, to ensure your response is always under close supervision.

For the treatment of short-term myocardial infarction, the recommended initial test dose is 6,25 mg, 2 mg after 12,5 hours and 12 mg after 25 hours. If the patient does not experience any adverse haemodynamic symptoms (blood circulation problems), starting the next day, 100 mg Captopril is administered daily in two divided doses over a period of 4 weeks.

Long-term treatment of myocardial infarction requires an initial dose of 6,25 mg, then 2 mg three times a day for 12,5 days, then 3 mg three times a day. unless there are undesirable haemodynamic symptoms. The recommended dose for effective cardioprotective effects in chronic treatment is 75 to 150 mg daily in two or three divided doses. Treatment should be started in a hospital setting under strict medical supervision.

Type I diabetes nephropathy requires a daily dose of 75-100 mg in divided doses. If further blood pressure reduction is required, other antihypertensive drugs may be added.

Patients with renal impairment should be prescribed lower doses by their doctor. If concomitant treatment with diuretics is necessary in patients with severe renal insufficiency, your doctor may recommend the use of loop diuretics (such as furosemide) in place of thiazide diuretics.

The dosage of Captopril is also dependent on the age of the patient. Elderly patients are started with a lower initial dose (6,25 mg twice a day). However, in the case of children and adolescents, there are no complete data on the safety and effectiveness of the preparation.

For this reason, treatment should only be initiated in this age group under close medical supervision. The dose and the interval between doses will be determined by the doctor in each case individually. The usual starting daily dose is 0,3 mg / kg body weight. The daily dose is usually administered in 3 divided doses.

If you have any doubts about the use of the preparation, consult your doctor. You should never make your own decisions about increasing or decreasing the dose of a drug, as this will not increase the effectiveness of the drug and may harm the health and life of the patient.

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Captopril – side effects and side effects

Like any other Captopril medicinal product may cause side effects that do not have to occur in every person using this medicine. After authorization of the medicinal product, it is important to report any suspected adverse reactions so that the benefit / risk balance of the medicinal product can be monitored.

The general classification of the frequency of adverse body reactions (ADRs) is based on the following principles: very common (≥1 / 10), common (≥1 / 100 to <1/10), uncommon (≥1 / 1 to <000/1), rare ( ≥100 / 1 to <10 / 000), very rare (<1 / 1), not known (cannot be estimated from the available data).

The most common side effect after taking Captopril there are problems related to sleep disorders, dizziness, shortness of breath, persistent cough, as well as digestive system ailments, rash or taste disturbances.

Side effects and side effects of using Captopril can be divided according to the frequency of their occurrence:

1. common side effects after taking Captopril (at least 1 in 100 but less than 1 in 10): sleep disturbances, disturbances in the sense of taste, dry and persistent cough, shortness of breath, nausea, vomiting, gastric irritation, abdominal pain, diarrhea, constipation, dry mucosa mouth, itching with or without rash, rash and alopecia;
2. not very common side effects after taking Captopril (at least 1 in 1000 but less than 1 in 100): tachycardia (fast heart beat) or tachyarrhythmia (abnormal heart rhythm), angina pectoris (chest pain), palpitations, hypotension, Raynaud’s syndrome (paroxysmal fingers or toes turn pale when exposed to cold or emotions), flushing, pale skin, angioedema, tiredness, feeling unwell
3. rare side effects after taking Captopril (at least 1 in 10000 people but less than 1 in 1000): anorexia (loss of appetite and weight loss), sleepiness, headache and paraesthesia (pins and needles), stomatitis / aphthous ulceration, kidney problems, including renal failure, polyuria, oliguria, increased frequency of urination;
4. very rare side effects after taking Captopril (less than 1 patient in 10000): neutropenia / agranulocytosis (decreased / absent certain type of white blood cells), pancytopenia (decreased number of all blood cells), thrombocytopenia, lymphadenopathy, eosinophilia (increased amount of a certain type of white blood cells), autoimmune disorders , hyperkalaemia (increased potassium levels), hypoglycaemia (low serum sugar), confusion, depression, cerebrovascular accidents including stroke, syncope, blurred vision, cardiac arrest, cardiogenic shock, bronchospasm, rhinitis, peptic ulcer, pancreatitis, liver dysfunction and cholestasis, hepatitis including necrosis, urticaria, erythema multiforme, Stevens-Johnson syndrome, photosensitivity, erythroderma (redness and peeling of the skin), pemphigus-like skin lesions and exfoliative dermatitis , myalgia, arthralgia, nephrotic syndrome, impotence, gynecomastia, hot hives, changes in laboratory test results.

In case of occurrence of other, not mentioned and unexpected side effects after using Captopril, a doctor should be consulted.

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Captopril and pregnancy and breastfeeding

Pregnancy and the later period of breastfeeding are a natural condition in a woman’s life, but it should be remembered that not everything that is allowed will be appropriate on a daily basis also during pregnancy or breastfeeding. One of such issues is taking medicinal preparations that should not be used by pregnant or lactating women without consulting a doctor.

The use of Captopril requires consultation with a doctor in order to clarify beyond any doubt the potential risks and benefits associated with the use of the drug. Women who are pregnant or planning pregnancy should inform their doctor, who is going to include Captopril in treatment.

Treatment with this preparation is not recommended during pregnancy in the first trimester, while in the later stages, i.e. the second and third trimesters of pregnancy, the drug is completely contraindicated, both when starting treatment or in continuing treatment.

Women who plan to become pregnant should inform their doctor about this fact, as he will then consider replacing Captopril with other drugs that are safer and will not pose a risk to the developing fetus in the womb.

The use of this preparation may cause serious complications related to the development of the fetus, including: renal dysfunction, oligohydramnios or delays in the ossification of the skull in newborns whose mother took Captopril during pregnancy. There is also a risk of developing hypotension.

Also, the period of lactation and breastfeeding of premature babies and newborns in the first weeks of life is a contraindication to the use of Captopril by the woman. This preparation, along with milk, enters the child’s body, negatively affecting the cardiovascular system and kidneys.

In the case of older children who are still breastfed, the benefits to the mother of taking Captopril under the tongue should be carefully weighed against the risks to the baby. If therapy is restarted then constant monitoring is necessary to capture any possible side effects.

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Captopril – interactions with other drugs

The initiation of therapy with the use of Captopril requires a detailed interview regarding all recently taken medications, including over-the-counter medications. The use of certain medications at the same time as taking Captopril can cause serious side effects.

The doctor should be informed about taking any of the following medications:

1. drugs with analgesic, antipyretic and anti-inflammatory effects – the so-called non-steroidal anti-inflammatory drugs (NSAIDs), diclofenac, piroxicam, ibuprofen, acetylsalicylic acid;
2. the drugs most commonly used to prevent organ rejection (sirolimus, everolimus and other mTOR inhibitors);
3. antihypertensive drugs and vasodilators such as nitrates;
4. anti-diabetic drugs;
5. thrombolytic drugs (to dissolve blood clots and decongest the vessels), e.g. streptokinase;
6. potassium supplements (including salt substitutes), potassium-sparing diuretics (spironolactone, amiloride, triamterene) and other drugs that increase blood potassium levels (e.g. trimethoprim and cotrimoxazole, used for bacterial infections; cyclosporine, an immunosuppressant used to prevent organ transplant rejection and heparin, a medicine used to thin the blood, to prevent clots);
7. cytostatics (drugs for the treatment of cancer);
8. lithium (used to treat mania and depression);
9. tricyclic antidepressants, antipsychotics;
10. vasoconstrictor drugs sympathomimetics, e.g., adrenaline;
11. allopurinol (used to treat gout);
12. procainamide (used to treat abnormal heart rhythms);
13. immunosuppressants.

Some drugs can affect the way Captopril works and it may be necessary to change the dosage or stop taking the preparation altogether and replace it with other drugs.

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Captopril – warnings and precautions

Before using Captopril, read the leaflet, which contains indications, contraindications, information on side effects, dosage and information on precautions when using this drug.

Special precautions should be taken while taking Captopril:

1. in patients with impaired renal function, bilateral stenosis of the arteries of the kidney, or stenosis of the artery of a single functioning kidney;
2. in patients undergoing desensitisation therapy, for example to reduce allergic reaction to insect stings;
3. in patients undergoing low-density lipoprotein apheresis (removal of cholesterol from the blood);
4. in patients with known risk factors for arterial hypotension, such as fluid and electrolyte disturbances, severe renin-dependent hypertension or symptomatic heart failure;
5. in patients undergoing dialysis;
6. if you have aortic and mitral valve (heart valve) stenosis or hypertrophic cardiomyopathy (a disease of the heart muscle);
7. in patients with impaired liver function;
8. in patients with known collagen vascular disease (connective tissue disease) or patients being treated with immunosuppressants such as azathioprine;
9. in patients with known gout treated with allopurinol;
10. in patients with cardiac arrhythmias treated with procainamide;
11. in diabetic patients;
12. women who are pregnant or planning to breastfeed;
13. in patients for whom surgery is planned with anesthesia causing hypotension;
14. in patients taking drugs such as racecadotril, a drug used to treat diarrhea, drugs used to prevent organ transplant rejection and to treat cancer (e.g. temsirolimus, sirolimus, everolimus), vildagliptin, a drug used to treat diabetes, valsartan, telmisartan, irbesartan , aliskiren.

Black patients should be especially careful when taking Captopril as they have an increased risk of angioedema and the drug has been shown to be less effective in lowering blood pressure in these patients.

Alcohol should not be consumed while taking Captopril. This medicine may also have a negative influence on the ability to drive a car or operate machinery. Before using Captopril, talk to your doctor or pharmacist about the risks of using the drug.