Captopril - for the treatment of Hypertension & Heart failure

Captopril is a medication primarily used to treat high blood pressure (hypertension) and various heart conditions. It belongs to a class of drugs known as angiotensin-converting enzyme (ACE) inhibitors. ACE inhibitors work by blocking the conversion of angiotensin I to angiotensin II, a substance in the body that narrows blood vessels and increases blood pressure. By inhibiting this conversion, captopril helps relax blood vessels and lower blood pressure.

The angiotensin-converting enzyme that changes angiotensin I into angiotensin II is competitively inhibited by captopril. Since, angiotensin II has potent vasoconstrictor properties, inhibiting it results in vasodilation. Thus, it is used primarily in the following conditions:

  • Treatment of Diabetic nephropathy in both Type 1 and Type 2 Diabetes Mellitus.

  • Treatment and of Heart failure with a reduced ejection fraction in asymptomatic patients 

  • Treatment of symptomatic patients with heart failure and a reduced ejection fraction to reduce morbidity and mortality

  • Management of hypertension

  • Reduce the likelihood of heart failure and subsequent hospitalisation after a myocardial infarction in clinically stable individuals with an ejection fraction of less than 40%. All patients with anterior wall MI, heart failure, or an ejection fraction less than 40% should start taking captopril within the first 24 hours.

  • Off Label Use of Captopril in Adults include:
    • For the diagnosis of Hyperaldosteronism
    • Hypertension in scleroderma renal crisis
    • Hypertensive crisis
    • Non–ST-elevation acute coronary syndrome
    • Raynaud phenomenon
    • Stable coronary artery disease
    • For the diagnosis of Anatomic renal artery stenosis
    • Bartter syndrome
    • Hypertension secondary to Takayasu Disease

Captopril Dose in Adults

  • Start with a low dose: Begin with a small amount of the medication.
  • Adjust as needed: Increase or decrease the dose based on how the patient's body reacts.
  • Find the right dose: The goal is to use the smallest amount that works effectively.
  • Personalized treatment: Each person may need a different dose for the best results.
  • Regular monitoring: Keep an eye on the patient's response and make changes as necessary.
  • Safety first: Always prioritize the patient's safety when adjusting medication doses.

Treatment of Diabetic nephropathy:  

  • Initial Dose: Start with 25 milligrams (mg) taken orally three times a day.
  • Additional Treatment: If necessary, captopril can be used alongside other medications for hypertension (high blood pressure) to further reduce blood pressure.

Treatment of Heart failure 

  • Initial Dose: Begin with a low initial dose of 6.25 milligrams (mg) taken orally three times a day.
  • Target Dose: The goal is to gradually increase the dose to a target of 50 mg taken orally three times a day.

Treatment of Hypertension:  

  • Initial Dose: Start with an initial dose of 12.5 to 25 milligrams (mg) taken orally 2 to 3 times a day.
  • Dose Adjustment: The dose can be adjusted based on the patient's response. This adjustment can be done at 1- to 2-week intervals.
  • Maximum Dose: The maximum recommended daily dose of captopril for hypertension is 450 mg per day.

Treatment of LV dysfunction following MI:

  • Initial Dose: Begin with a low initial dose of 6.25 milligrams (mg) taken orally.
  • Dose Increase: If the initial dose is tolerated well, increase to 12.5 mg three times a day during the next step.
  • Gradual Increase: Over the next several days, further increase the dose to 25 mg taken three times a day.
  • Target Dose: The ultimate goal is to gradually increase the dose over the next several weeks to reach a target dose of 50 mg taken three times a day.

Off label use in the treatment of Hypertensive Urgency or emergency:

  • Oral Administration: Begin with an initial dose of 25 milligrams (mg) taken orally.
  • Sublingual Administration: Captopril can also be given sublingually (under the tongue) at a dose of 25 mg.
  • Repeat Dosing: If necessary, the dose may be repeated as needed to lower blood pressure.
  • Response Time: Monitor the patient's blood pressure closely. If the blood pressure does not respond within 20 to 30 minutes, consider alternative therapy.

Off label use in the treatment of Raynaud phenomenon:

  • Initial Dose: Start with a low initial dose of 12.5 milligrams (mg) taken orally twice daily.
  • Dose Adjustment: If needed, the dose can be gradually increased to 25 mg taken three times a day.

Captopril Dose in Childrens

Heart failure Treatment:

Infants:

  • Initial Dose: Start with an initial dose of 0.1 to 0.3 milligrams per kilogram (mg/kg) per dose, administered every 6 to 24 hours.
  • Titration: Adjust the dose as needed. The reported daily dose range is 0.3 to 3.5 mg/kg per day, divided into doses given every 6 to 12 hours.
  • Maximum Daily Dose: The maximum daily dose for infants is 6 mg/kg per day.

Children and Adolescents:

  • Initial Dose: Begin with an initial dose of 0.3 to 0.5 mg/kg per dose, given every 8 to 12 hours.
  • Titration: Adjust the dose as necessary. In clinical trials, the usual reported dosage range was 0.9 to 3.9 mg/kg per day, divided into doses.
  • Maximum Daily Dose: The maximum daily dose for children and adolescents is 6 mg/kg per day.

For adults, the target dose is typically 150 mg per day for heart failure. However, the dosing recommendations provided here are specifically for infants, children, and adolescents, as dosages vary based on age and weight in this population.


Treatment of High Blood Pressure: 

Weight-Directed Dosing:

  • Infants:
    • Initial Dose: Begin with an initial dose of 0.05 milligrams per kilogram (mg/kg) per dose, administered every 6 to 24 hours.
    • Titration: Carefully adjust the dose upward as needed, but do not exceed a maximum daily dose of 6 mg/kg.
    • Monitoring: Monitor for hypotension (low blood pressure).
  • Children and Adolescents:
    • Initial Dose: Start with an initial dose of 0.3 to 0.5 mg/kg per dose, given every 8 hours.
    • Titration: Adjust the dose as needed, up to a maximum daily dose of 6 mg/kg/day, divided into 3 doses.
    • Maximum Daily Dose: The maximum daily dose for children and adolescents is 450 mg.

Fixed Dosing (Adolescents):

  • Adolescents:
    • Initial Dose: Begin with an initial dose of 12.5 to 25 mg per dose, given every 8 to 12 hours.
    • Titration: Increase the dose by 25 mg per dose at 1- to 2-week intervals based on the patient's response.
    • Maximum Daily Dose: The maximum daily dose for adolescents using fixed dosing is 450 mg.

Pregnancy Risk Factor D

  • Captopril and similar drugs that affect the renin-angiotensin system can be very harmful to a developing baby.
  • They may lead to serious problems like kidney and lung issues, as well as malformations.
  • If you're pregnant or planning to become pregnant, it's crucial to stop these medications as soon as you know you're expecting.
  • These drugs can also cause low amniotic fluid levels, which may harm the baby's development.
  • Avoid using them during pregnancy, especially in the later stages.
  • If you're already on these medications and become pregnant, talk to your healthcare provider immediately.
  • They'll help you switch to safer alternatives to manage your health during pregnancy.

Captopril use during breastfeeding:

  • Captopril can be found in breast milk, but the amount is relatively low, making it generally safe for breastfeeding.
  • The estimated infant dose through breast milk is quite small compared to what a baby would receive for therapeutic purposes, which is considered acceptable.
  • In a study with lactating women taking captopril, the highest concentration in breast milk was about 1% of what was in the mother's blood.
  • It's important to consider the benefits of the medication for the mother's health and the potential risks to the baby when deciding whether to breastfeed while taking captopril.
  • Most guidelines, including those from the World Health Organization (WHO), suggest that captopril is acceptable for use in breastfeeding women.

Captopril dose adjustment in renal disease:

Manufacturer's Recommendations:

  • Reduce Initial Dose: Start with a lower initial daily dose.
  • Titrate Slowly: Increase the dose gradually at 1- to 2-week intervals, using smaller increments.
  • Back Titrate: Once the desired therapeutic effect is achieved, slowly reduce the dose to determine the minimum effective dose.

Alternative Recommendations (Aronoff 2007):

  • Creatinine Clearance (CrCl) 10 to 50 mL/minute: Administer at 75% of the normal dose every 12 to 18 hours.
  • CrCl <10 mL/minute: Administer at 50% of the normal dose every 24 hours.
  • Intermittent Hemodialysis (IHD): Administer captopril after hemodialysis on dialysis days.
  • Peritoneal Dialysis: Use the dose appropriate for CrCl 10 to 50 mL/minute; supplemental doses are not typically necessary for peritoneal dialysis.

These alternative recommendations are especially important for patients with impaired kidney function, as their bodies may not process the medication as efficiently. Proper dosing adjustments can help avoid side effects and ensure that the medication is both safe and effective for the patient.

Captopril Dose in Liver Disease:

  • The manufacturer's labeling for captopril does not provide specific dosage adjustments for patients with hepatic (liver) impairment because such adjustments have not been studied extensively.
  • Hepatic impairment can affect the way the body processes medications, but the impact can vary widely among individuals.

Common Side Effects Of Captopril Include:

  • Cardiovascular:
    • Angina pectoris
    • Cardiac arrest
    • Cardiac arrhythmia
    • Cardiac failure
    • Flushing
    • Myocardial infarction
    • Orthostatic hypotension
    • Raynaud's phenomenon
    • Syncope
  • Central nervous system:
    • Ataxia
    • Cerebrovascular insufficiency
    • Confusion
    • Depression
    • Drowsiness
    • Myasthenia
    • Nervousness
  • Dermatologic:
  • Endocrine & metabolic:
    • Gynecomastia
    • Hyponatremia
  • Gastrointestinal:
    • Cholestasis
    • Dyspepsia
    • Glossitis
    • Pancreatitis
  • Genitourinary:
    • Impotence
    • Nephrotic syndrome
    • Oliguria
    • Urinary frequency
  • Hematologic & oncologic:
    • Agranulocytosis
    • Anemia
    • Pancytopenia
    • Thrombocytopenia
  • Hepatic:
    • Hepatic necrosis
    • Hepatitis
    • Increased serum alkaline phosphatase
    • Increased serum bilirubin
    • Increased serum transaminases
    • Jaundice
  • Hypersensitivity:
    • Anaphylactoid reaction
    • Angioedema
  • Neuromuscular & skeletal:
    • Myalgia
    • Weakness
  • Ophthalmic:
    • Blurred vision
  • Renal:
    • Polyuria
    • Renal failure
    • Renal insufficiency
  • Respiratory:
    • Bronchospasm
    • Eosinophilic pneumonitis
    • Rhinitis

Less Common Side Effects Of Captopril Include:

  • Cardiovascular:
    • Hypotension
    • Chest pain
    • Palpitations
    • Tachycardia
  • Dermatologic:
    • Skin rash
    • Pruritus
  • Endocrine & metabolic:
    • Hyperkalemia
  • Gastrointestinal:
    • Dysgeusia
  • Genitourinary:
    • Proteinuria
  • Hematologic & oncologic:
    • Neutropenia
  • Hypersensitivity:
    • Hypersensitivity reaction
  • Renal:
    • Increased serum creatinine
    • Renal insufficiency
  • Respiratory:
    • Cough
  • Miscellaneous:
    • Hypersensitivity reactions
    • Dysgeusia

Contraindication to Captopril include:

Captopril is contraindicated (should not be used) in certain situations due to the potential risks and interactions. These contraindications include:

  • Hypersensitivity: Do not use captopril if you have a known hypersensitivity or allergy to captopril, any other ACE inhibitor, or any component of the medication.
  • Angioedema: Avoid captopril if you have experienced angioedema (swelling of deeper layers of the skin, often around the eyes and lips) in the past as a result of treatment with an ACE inhibitor.
  • Concomitant Use with Aliskiren: Captopril should not be used in combination with aliskiren in patients with diabetes mellitus. This combination can increase the risk of certain side effects.
  • Coadministration with Neprilysin Inhibitors: Do not take captopril in combination with, or within 36 hours of switching to or from, a neprilysin inhibitor such as sacubitril. This combination can increase the risk of angioedema and other adverse effects.
  • Additional Canadian Contraindication: In Canada, there is an additional contraindication for captopril when used in combination with aliskiren in patients with moderate to severe renal impairment (glomerular filtration rate, GFR, less than 60 mL/minute/1.73 m²).

Warnings and Precautions

Angioedema

  • While taking ACE inhibitors like captopril, it's essential to be aware that rare but severe swelling known as angioedema can happen, potentially affecting the head, neck (which can be risky for breathing), or the intestines (causing stomach pain).
  • Some individuals, like African-Americans and those with certain types of angioedema, may be at a higher risk.
  • This risk can also increase if you're using medications like everolimus or sacubitril.
  • If angioedema occurs, especially involving the tongue, throat, or voice box, it can block your airway and requires careful monitoring and prompt treatment.
  • If you've had angioedema in the past due to ACE inhibitors, it's best not to use them again.
  • Always seek immediate medical attention if you experience any signs of angioedema while taking captopril.

Cholestatic jaundice

  • Rarely, ACE inhibitors like captopril can lead to a serious liver condition called cholestatic jaundice.
  • This condition can cause symptoms like yellowing of the skin and eyes (jaundice) and may even progress to severe liver damage (fulminant hepatic necrosis), which can be fatal in some cases.
  • If you experience a significant increase in liver enzymes or develop jaundice while taking captopril, it's crucial to discontinue the medication immediately and seek medical attention.
  • Monitoring liver function is important during ACE inhibitor therapy, and any signs of liver problems should not be ignored.

Cough:

  • Cough is a potential side effect of ACE inhibitors like captopril.
  • This type of cough is typically dry, persistent, and nonproductive.
  • It usually starts within the first few months of starting ACE inhibitor treatment and often goes away within 1 to 4 weeks after stopping the medication.
  • However, before discontinuing the ACE inhibitor, it's important to consider and rule out other possible causes of cough, especially in patients with heart failure where pulmonary congestion could be a factor.

Hematologic effects

  • Captopril can affect your blood cells, potentially leading to problems like neutropenia (a low count of certain white blood cells), myeloid hypoplasia (underdevelopment of bone marrow cells), and even agranulocytosis (a severe decrease in white blood cells).
  • Anemia (low red blood cell count) and thrombocytopenia (low platelet count) have also been reported.
  • People with kidney problems are at a higher risk of developing neutropenia, and those with both kidney issues and certain autoimmune diseases like lupus are at an even greater risk.

Hyperkalemia:

  • ACE inhibitors like captopril can sometimes cause high levels of potassium in the blood, known as hyperkalemia.
  • Certain factors increase this risk, including kidney problems, diabetes, and using medications that save potassium, potassium supplements, or potassium-rich salts.
  • If you have any of these risk factors, your healthcare provider may use ACE inhibitors cautiously or consider alternative treatments.
  • They'll also keep a close eye on your potassium levels to ensure they stay within a safe range.

Hypersensitivity reactions

  • Hypersensitivity reactions, including severe ones like anaphylactic or anaphylactoid reactions, can sometimes happen with ACE inhibitors like captopril.
  • In rare cases, these severe reactions have been observed during certain medical procedures, such as high-flux hemodialysis with specific membranes or low-density lipoprotein apheresis with dextran sulfate cellulose.
  • Additionally, there have been rare reports of such reactions in people receiving treatment for bee or wasp venom allergies while taking ACE inhibitors.

Syncope and hypotension:

  • ACE inhibitors like captopril can sometimes cause low blood pressure, which may lead to symptoms like feeling dizzy, lightheaded, or even fainting, known as syncope.
  • This is more likely to happen, especially with the first few doses of the medication, if you are dehydrated or don't have enough fluids in your body.
  • To prevent this, it's important to make sure you are well-hydrated before starting captopril.

Proteinuria:

  • In some rare cases, ACE inhibitors like captopril can lead to an increase in the amount of protein in the urine, a condition known as proteinuria.
  • This happens in less than 1% of people taking these medications.
  • In about one-fifth of these cases, proteinuria can become more severe, leading to a condition called nephrotic syndrome.
  • The good news is that in most cases, the excess protein in the urine gets better on its own, even if captopril is continued.
  • Typically, within six months, the proteinuria subsides or clears up.

Renal function deterioration:

  • Deterioration of kidney function can occur with ACE inhibitors like captopril, especially in patients with conditions like renal artery stenosis or heart failure, where the kidneys depend on certain blood vessel changes.
  • This deterioration may lead to problems like reduced urine production (oliguria), sudden kidney failure, or rising levels of substances like BUN and creatinine in the blood.
  • Sometimes, there can be small, non-harmful increases in serum creatinine when starting captopril.
  • However, discontinuation of the medication is typically considered only if there is a significant and progressive decline in kidney function.

Aortic stenosis

  • In individuals with aortic stenosis, it's important to use captopril cautiously.
  • This medication may reduce the blood flow to the coronary arteries, which could lead to a lack of oxygen supply to the heart muscle (ischemia).

Ascites:

  • Captopril should generally be avoided in patients with ascites (abdominal fluid accumulation) caused by cirrhosis or refractory ascites.
  • If, for some reason, it must be used in patients with ascites due to cirrhosis, close monitoring of blood pressure and kidney function is crucial.
  • This careful monitoring helps prevent the rapid development of kidney failure, which can be a serious complication in these patients.

Cardiovascular disease

  • When starting therapy with captopril in patients who have ischemic heart disease or cerebrovascular disease, it's important to closely monitor them because there's a risk of blood pressure dropping too low.
  • This drop in blood pressure could lead to serious consequences like a heart attack (MI) or a stroke.
  • If their blood pressure does drop, providing fluids may help raise it, and once their blood pressure stabilizes, therapy can be resumed.
  • However, if hypotension (low blood pressure) recurs and becomes a problem, it may be necessary to discontinue captopril.

Collagen vascular disease:

  • In patients with collagen vascular diseases, especially if they also have kidney problems, the use of captopril should be approached with caution.
  • These individuals may be at an increased risk of experiencing hematologic (blood-related) toxicity as a side effect of the medication.
  • Therefore, careful monitoring and close attention to potential hematologic side effects are essential.

Hypertrophic cardiomyopathy and outflow tract obstruction

  • In patients with hypertrophic cardiomyopathy (HCM) who also have outflow tract obstruction, caution should be exercised when considering the use of captopril.
  • This medication can reduce the afterload (the force the heart must overcome to pump blood), and in some cases, this reduction may worsen symptoms associated with HCM and outflow tract obstruction.
  • It's crucial to carefully evaluate the risks and benefits of captopril in these patients and to monitor their condition closely if the medication is prescribed.

Renal artery stenosis

  • Captopril should be used cautiously in patients with unstented unilateral or bilateral renal artery stenosis.
  • If a patient has unstented bilateral renal artery stenosis, the use of captopril is typically avoided.
  • This cautious approach is taken because there is an increased risk of worsening renal function in these individuals unless the potential benefits of the medication clearly outweigh the risks.

Renal impairment

  • If you have kidney problems, be careful when using this. You might need a lower dose. Don't increase the dose quickly, as it might harm your kidneys more.

Captopril: Drug Interaction

Note: Drug Interaction Categories:

  • Risk Factor C: Monitor When Using Combination
  • Risk Factor D: Consider Treatment Modification
  • Risk Factor X: Avoid Concomitant Use

Risk Factor C (Monitor therapy).

Ajmaline

High risk of Inhibitors increasing serum concentrations of CYP2D6 Substrates

Alfuzosin

Might increase the hypotensive effects of Blood Pressure Lowering Agents.

Amphetamines

May lessen the effects of antihypertensive medications in treating hypertension.

Angiotensin II

The therapeutic efficacy of angiotensin II may be enhanced by angiotensin-converting enzyme inhibitors.

Antacids

The serum levels of captopril could drop.

Antipsychotic Agents, Second Generation (Atypical)

Antipsychotic drugs can have a greater hypotensive effect when blood pressure-lowering medications are used (Second Gen [Atypical]).

Aprotinin

Angiotensin-Converting Enzyme Inhibitors may intensify their hyperkalemic effects.

AzaTHIOprine

AzaTHIOprine's myelosuppressive effects may be enhanced by angiotensin-converting enzyme inhibitors.

Barbiturates

May intensify blood pressure lowering medications' hypotensive effects.

Benperidol

May intensify blood pressure lowering medications' hypotensive effects.

Brigatinib

May lessen the effects of antihypertensive medications in treating hypertension. The bradycardic effects of antihypertensive medications may be exacerbated by brutinib.

Brimonidine (Topical)

May intensify blood pressure lowering medications' hypotensive effects.

CloBAZam

High likelihood that inhibitors will raise serum levels of CYP2D6 substrates

Cobicistat

High likelihood that inhibitors will raise serum levels of CYP2D6 substrates

Moderate CYP2D6 inhibitors

May reduce CYP2D6 substrate metabolism (High Risk with Inhibitors).

Dapoxetine

May increase the angiotensin-converting enzyme inhibitors' orthostatic hypotensive effects.

Darunavir

Danger of inhibitors is high raising CYP2D6 Substrates serum concentrations

Dexmethylphenidate

May worsen angiotensin-converting enzyme inhibitors' toxic or severe effects. The risk of angioedema in particular could rise.

Diazoxide

Antihypertensive agents may have a less therapeutic effect.

Dipeptidyl Peptidase-IV Inhibitors

May intensify blood pressure lowering medications' hypotensive effects.

Drospirenone

Drospirenone's hyperkalemic impact may be enhanced by angiotensin-converting enzyme inhibitors.

DULoxetine

By reducing blood pressure, DULoxetine may intensify the hypotensive effects.

Eplerenone

The effects of angiotensin-converting enzyme inhibitors on hyperkalemia may be enhanced.

Everolimus

May intensify angiotensin-converting enzyme inhibitors' harmful or hazardous effects. The risk of angioedema in particular could rise.

Ferric Gluconate

Angiotensin-Converting Enzyme Inhibitors might make ferric gluconate more harmful or poisonous.

Complex of Ferric Hydroxide Polymaltose

Ferric Hydroxide Polymaltose Complex may have a more negative or toxic effect when taken with angiotensin-converting enzyme inhibitors. Angioedema and allergic responses in particular may become more likely.

Gelatin (Succinylated).

Gelatin's harmful or toxic effects may be increased by angiotensin-converting enzyme inhibitors (Succinylated). Particularly, a higher risk of paradoxical hypotensive reactions to gelatin may exist (Succinylated).

Gold Sodium Thiomalate

Gold Sodium Thiomalate may have a more negative or toxic effect when used with angiotensin-converting enzyme inhibitors. Nitritoid responses have been linked to a higher risk, it has been highlighted.

Heparin

Angiotensin-Converting Enzyme Inhibitors may intensify their hyperkalemic effects.

Heparins (Low Molecular Weight)

Angiotensin-Converting Enzyme Inhibitors may intensify their hyperkalemic effects.

Herbs (Hypertensive Properties)

May lessen the effects of antihypertensive medications in treating hypertension.

Herbs (Hypotensive properties)

May intensify blood pressure lowering medications' hypotensive effects.

Hypotension-Associated Agents

The hypotensive action of hypotension-associated agents may be strengthened by blood pressure lowering medications.

Icatibant

Angiotensin-Converting Enzyme Inhibitors may intensify their hyperkalemic effects.

Imatinib

High likelihood that inhibitors will raise serum levels of CYP2D6 substrates

Levodopa-Containing Products

Levodopa-Containing Products' hypotensive effects may be amplified by blood pressure-lowering medications.

Loop Diuretics

May strengthen angiotensin-converting enzyme inhibitors' hypotensive effects. Angiotensin-Converting Enzyme Inhibitors' nephrotoxic effects may be increased by loop diuretics.

Lormetazepam

May intensify blood pressure lowering medications' hypotensive effects.

Lumefantrine

High likelihood that inhibitors will raise serum levels of CYP2D6 substrates

Methylphenidate

May lessen the effects of antihypertensive medications in treating hypertension.

Molsidomine

May intensify blood pressure lowering medications' hypotensive effects.

Naftopidil

May intensify blood pressure lowering medications' hypotensive effects.

Nicergoline

May intensify blood pressure lowering medications' hypotensive effects.

Nicorandil

Angiotensin-Converting Enzyme Inhibitors may intensify their hyperkalemic effects.

Nicorandil

May intensify blood pressure lowering medications' hypotensive effects.

Nitrogen

Blood pressure lowering medications may intensify Nitroprusside's hypotensive effects.

Nonsteroidal Anti-Inflammatory Drugs

Nonsteroidal Anti-Inflammatory Agents' negative/toxic effects may be increased by angiotensin-converting enzyme inhibitors. The combination can cause renal function to significantly decline. Angiotensin-Converting Enzyme Inhibitors' antihypertensive effects may be lessened by nonsteroidal anti-inflammatory drugs.

Panobinostat

High likelihood that inhibitors will raise serum levels of CYP2D6 substrates

Peginterferon Alfa-2b

Inhibitors carry a high danger. may reduce the level of CYP2D6 substrates in serum. Serum levels of CYP2D6 Substrates may rise after administration of peginterferon Alf-2b.

Pentoxifylline

May intensify blood pressure lowering medications' hypotensive effects.

Perhexiline

CYP2D6 Substrates may lead to an increase in perhexiline. The serum concentrations of CYP2D6 substrates can rise in response to perhexiline (High Risk with Inhibitors).

Pholcodine

By reducing blood pressure, pholocdine may exacerbate hypotension.

Phosphodiesterase 5 Inhibitors

May intensify blood pressure lowering medications' hypotensive effects.

Potassium Salts

Angiotensin-Converting Enzyme Inhibitors may intensify their hyperkalemic effects.

Potassium-Sparing Diuretics

Angiotensin-Converting Enzyme Inhibitors may intensify their hyperkalemic effects.

Pregabalin

Angiotensin-Converting Enzyme Inhibitors may intensify Pregabalin's negative/toxic effects. Risk of gioedema could rise.

Prostacyclin Analogues

May intensify blood pressure lowering medications' hypotensive effects.

Quinagolide

May intensify blood pressure lowering medications' hypotensive effects.

QuiNINE

Danger of inhibitors is high raising CYP2D6 Substrates serum concentrations

Racecadotril

May intensify angiotensin-converting enzyme inhibitors' harmful or hazardous effects. Angioedema may be more likely as a result of this combination.

Ranolazine

Angiotensin-Converting Enzyme Inhibitors may intensify their hyperkalemic effects.

Salicylates

May intensify angiotensin-converting enzyme inhibitors' nephrotoxic effects. The therapeutic benefit of angiotensin-converting enzyme inhibitors may be reduced by salicylates.

Sirolimus

Angiotensin-Converting Enzyme Inhibitors may intensify their hyperkalemic effects.

Tacrolimus (Systemic)

Angiotensin-Converting Enzyme Inhibitors may enhance the hyperkalemic effect of Tacrolimus (Systemic).

Temsirolimus

Angiotensin-Converting Enzyme Inhibitors may intensify their hyperkalemic effects.

Thiazide and Thiazide -Like Diuretics

May increase the angiotensin-converting enzyme inhibitors' hypotensive effects. Angiotensin-Converting Enzyme Inhibitors' nephrotoxic effects may be increased by thiazide and thiazide-like diuretics.

TiZANidine

Angiotensin-Converting Enzyme Inhibitors may intensify their hyperkalemic effects.

Tolvaptan

Angiotensin-Converting Enzyme Inhibitors may intensify their hyperkalemic effects.

Trimethoprim

Angiotensin-Converting Enzyme Inhibitors may intensify their hyperkalemic effects.

Yohimbine

May lessen the effects of antihypertensive medications in treating hypertension.

Risk Factor D (Consider therapy modifications)

Abiraterone Acetate

High chance that inhibitors will raise serum levels of CYP2D6 substrates. Avoid using abiraterone and CYP2D6 Substrates with a restricted therapeutic index together whenever possible. If concurrent usage cannot be avoided, constantly watch patients for symptoms/signs and administer therapy as necessary.

Aliskiren

Angiotensin-Converting Enzyme Inhibitors may intensify their hyperkalemic effects. Angiotensin-Converting Enzyme Inhibitors' hypotensive effects may be strengthened by aliskiren. Angiotensin-Converting Enzyme Inhibitors' nephrotoxic effects may be made worse by aliskiren. Aliskiren shouldn't be taken with ACEIs or ARBs if the patient has diabetes. In diabetic patients, it is best to avoid combining Aliskiren with ACEIs or ARBs, especially if CrCl is less than 60 mL/min. If present together, carefully watch blood pressure, potassium, and creatinine levels.

Allopurinol

Angiotensin-Converting Enzyme Inhibitors might make Allopurinol more likely to cause allergic or hypersensitive reactions.

Amifostine

The hypotensive effects of amifostine may be strengthened by blood pressure reducing medications. Treatment: Stop taking blood pressure medications at least 24 hours before taking amifostine. If taking blood pressure medicine cannot be stopped, amifostine should be avoided.

Angiotensin II Receptor Blockers

May worsen angiotensin-converting enzyme inhibitors' toxic or severe effects. Angiotensin-Converting Enzyme Inhibitors' serum levels may rise in response to angiotensin II receptor blockers. Management: Ramipril and telmisartan are not advised for US labelling. It is unknown whether another ACE inhibitor and ARB combo would be less dangerous. If at all possible, think about combining different elements.

Asunaprevir

High likelihood that inhibitors will raise serum levels of CYP2D6 substrates

Strong CYP2D6 inhibitors

May reduce CYP2D6 substrate metabolism (High Risk with Inhibitors).

Dacomitinib

High chance that inhibitors will raise serum levels of CYP2D6 substrates. Management: Dacomitinib should not be used in combination with CYP2D6 substrates that have a limited therapeutic index.

Grass Pollen Allergen Extract (5 Grass Extract)

Grass pollen allergen extract may have a more negative or toxic effect if angiotensin-converting enzyme inhibitors are used (5 Grass Extract). In particular, ACE inhibitors may raise the possibility of life-threatening allergic reactions to grass pollen allergen extract (5 Grass).

Iron Dextran Complex

Angiotensin-Converting Enzyme Inhibitors might make Iron Dextran Complex more harmful or poisonous. Patients who take ACE inhibitors may be more prone to responses of this nature. Management: Carefully follow the iron dextran instructions for setting up resuscitation equipment, educating staff before administering iron dextran, and using a test dosage before to the first therapeutic dose.

Lanthanum

May lower angiotensin-converting enzyme inhibitors' serum concentration. Angiotensin-converting enzyme inhibitors should be given at least two hours before or after lanthanum.

Lithium

The serum concentration of lithium may rise in response to angiotensin-converting enzyme inhibitors. It is likely that you will need to lower your lithium dosage after adding an ACE inhibitor. Observe how patients respond to lithium following the addition or discontinuation of concomitant ACE inhibitor medication.

Obinutuzumab

The effects of blood pressure lowering medications may become more hypotensive as a result. Treatment: Starting 12 hours before the obinutuzumab injection and continuing for 1 hour after the infusion, you may temporarily stop taking blood pressure-lowering medications.

Sodium Phosphates

The nephrotoxic impact of sodium phosphates may be enhanced by angiotensin-converting enzyme inhibitors. Particularly, there may be an elevated risk of acute phosphate nephropathy. Treatment: You can temporarily stop taking ACEIs or explore for alternatives to the oral sodium phosphate bowel preparation to prevent this combo. In the event that the combination is not possible, be sure to drink enough water and keep a close eye on your renal function.

Urapidil

Angiotensin-Converting Enzyme Inhibitors may interact with them through an unidentified method. Avoid taking urapidil and ACE inhibitors simultaneously as a management strategy.

Risk Factor X (Avoid Combination)

Bromperidol

The hypotensive effects of bromperidol may be strengthened by blood pressure-lowering medications. The hypotensive effects of blood pressure-lowering medications may be lessened by bromperidol.

Sacubitril

The negative or hazardous effects of sacubitril may be increased by angiotensin-converting enzyme inhibitors. Angioedema may be more likely as a result of this combination.

Monitor the following parameters while taking Captopril:

If someone has kidney problems or certain diseases:

  • Keep a close eye on certain blood tests like BUN, electrolytes, and serum creatinine.
  • Also, monitor blood pressure.
  • Check a full blood count especially in the first 3 months of treatment, and then every so often.

For people with heart failure:

  • After starting the treatment, within 1-2 weeks and then every now and then, check kidney function and the level of potassium in the blood.
  • This is very important for those who already have issues like low blood pressure, low sodium levels, diabetes, high BUN levels, or those taking potassium supplements.

High blood pressure guidelines:

  • If someone has high blood pressure with heart disease or a high risk of heart-related issues in the next 10 years: Aim for a blood pressure lower than 130/80.
  • If someone has high blood pressure without these risks: It might still be a good idea to aim for a blood pressure lower than 130/80.

For people with diabetes and high blood pressure:

  • Ages 18 to 65, no heart disease, and low 10-year heart disease risk: Try to keep blood pressure below 140/90.
  • Ages 18 to 65 with heart disease or high 10-year heart disease risk: Aiming for a blood pressure lower than 130/80 might be good if it's safe.
  • Over 65 years old and in good or average health: Try to keep blood pressure below 140/90.
  • Over 65 and in poor health: Try to keep blood pressure below 150/90.

How to take Captopril?

Take the medicine at least 1 hour before you eat. If you need to make it into a liquid, mix it just before you use it and take it within 10 minutes.

Mechanism of action:

  • This medicine blocks a specific enzyme in the body called ACE.
  • By doing this, it stops the creation of a substance that tightens the blood vessels.
  • This leads to more relaxed blood vessels, less of certain hormones, and helps control blood pressure.

Onset of action:

  • Starts working within 15 minutes.

Peak effect:

  • The most significant drop in blood pressure occurs around 1 to 1.5 hours after taking it.

Maximum effect for lowering blood pressure:

  • Typically takes about 60 to 90 minutes to achieve, and it may take several weeks of using the medicine before the full effect is seen.

Duration:

  • The length of time the effect lasts depends on the dose and may also require several weeks of therapy before reaching its full potential.

Absorption:

  • About 60% to 75% of the medicine is quickly absorbed into the body.

Distribution:

  • The medicine is distributed in the body with a volume of about 0.7 liters per kilogram of body weight.

Bioavailability:

  • Around 60% to 75% of the medicine that is taken orally is used by the body. This amount can be reduced by 30% to 40% if taken with food.

Protein binding:

  • About 25% to 30% of the medicine attaches to proteins in the blood.

Metabolism:

  • Half of the medicine is changed in the body.

Half-life elimination:

  • The time it takes for half of the medicine to leave the body is approximately:
    • Infants with CHF: 3.3 hours (can vary)
    • Children: 1.5 hours (can vary)
    • Adults, healthy volunteers: ~1.7 hours
    • In patients with severe kidney problems, the half-life can be much longer, up to 21 to 32 hours.

Time to peak:

  • The highest level of the medicine in the blood is usually reached within 1 to 2 hours after taking it.

Excretion:

  • The medicine is mostly removed from the body through urine, with more than 95% of it being eliminated within 24 hours, and around 40% to 50% of it remains unchanged.

Captopril international brand names:

  • APO-Capto
  • BCI Captopril
  • CO Captopril
  • DOM-Captopril
  • MYLAN-Captopril
  • PMS-Captopril
  • TEVA-Captopril
  • TRIA-Captopril
  • Ace-Bloc
  • Aceomel
  • Acepress
  • Acepril
  • Aceril
  • Acetab
  • Aceten
  • Adocor
  • Amipril
  • Angiopril
  • Angiopril-25
  • Antasten
  • Apuzin
  • Asisten
  • Atrisol
  • Bloc-Med
  • Brucap
  • Caipolex
  • Capace
  • Capocard
  • Capomed
  • Caporex
  • Capoten
  • Capotena
  • Capotril
  • Capril
  • Captace
  • Captarsan
  • Captensin
  • Captodoc
  • Captoflux
  • Captohexal
  • Captolane
  • Captolar
  • Captopren
  • Captor
  • Captotec
  • Captral
  • Catopil
  • Catoplin
  • Debax
  • Dexacap
  • Ecaten
  • Epsitron
  • Farcopril
  • Farmoten
  • Gemzil
  • Hiperil
  • Huma-Captopril
  • Hypopress
  • Hypotensor
  • Kaptopril
  • Ketanine
  • Kimapan
  • Lopirin
  • Lopril
  • Metopril
  • Midopril
  • Midrat
  • Minitent
  • Nolectin
  • Noyada
  • Orbace
  • Pertacilon
  • Prelat
  • Prilocapt
  • Primace
  • Properil
  • Retensin
  • Rilcapton
  • Ropril
  • Smarten
  • Tensicap
  • Tensiomen
  • Tensiomin
  • Tensobon
  • Topril
  • Vasosta
  • Zapto
  • Zedace

Captopril Brands in Pakistan:

Captopril [Tabs 25 Mg]

Abdopril

Innvotek Pharmaceuticals

Acetopril

Zafa Pharmaceutical Laboratories (Pvt) Ltd.

Apolex

Mediceena Pharma (Pvt) Ltd.

Aptil

Pearl Pharmaceuticals

Bantoril

Benson Pharamceuticals.

Biopril

Bio Labs (Pvt) Ltd.

Capace

Atco Laboratories Limited

Capoten

Glaxosmithkline

Capril

Efroze Chemical Industries (Pvt) Ltd.

Captil

Werrick Pharmaceuticals

Capto

Drugs Inn Pakistan

Captomak

Makson Pharmaceuticals

Cardiocap

Alfalah Pharma (Pvt) Ltd.

Cardiotil

Davis Pharmaceutical Laboratories

Cardopril

Bex Pharma (Pvt) Ltd.

Catoper

Pharmix Laboratories (Private) Limited.

Eptril

Fynk Pharmaceuticals

Garan

Siza International (Pvt) Ltd.

Katopil

Akhai Pharmaceuticals.

Mtopril

Macquins International

Nobeten

Bryon Pharmaceuticals (Pvt) Ltd.

Plumax

Evron (Pvt) Ltd.

Plumax

Evron (Pvt) Ltd.

Qutril

Novartis Pharma (Pak) Ltd

Spenpril

Spencer Pharma

Tensiomin

Medimpex Scientific Office

Valopril

Valor Pharmaceuticals

Vasokap

Helicon Pharmaceutek Pakistan (Pvt) Ltd.

Vasotone

Pharmacare Laboratories (Pvt) Ltd.

Captopril [Tabs 50 Mg]

Abdopril

Innvotek Pharmaceuticals

Bantoril

Benson Pharamceuticals.

Capoten

Glaxosmithkline

Capril

Efroze Chemical Industries (Pvt) Ltd.

Captil

Werrick Pharmaceuticals

Captomak

Makson Pharmaceuticals

Cardiotil

Davis Pharmaceutical Laboratories

Cardopril

Bex Pharma (Pvt) Ltd.

Garan

Siza International (Pvt) Ltd.

Katopil

Akhai Pharmaceuticals.

Plumax

Evron (Pvt) Ltd.

Qutril

Novartis Pharma (Pak) Ltd

Spenpril

Spencer Pharma

Valopril

Valor Pharmaceuticals

Captopril [Tabs 12.5 Mg]

Capace

Atco Laboratories Limited

Capril

Efroze Chemical Industries (Pvt) Ltd.

Nobeten

Bryon Pharmaceuticals (Pvt) Ltd.