captopril 12.5 mg Tablet, 100-count
🆔 Identity & classification
Where does this data come from?
🏷️ RxNorm drug class
This medicine belongs to the Angiotensin Converting Enzyme Inhibitor class.
Where does this data come from?
🏭 Manufacturer & labeler
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🩺 Clinical
- Food in your stomach can reduce how much captopril your body actually absorbs by about 30 to 40 percent. Taking it on an empty stomach — about an hour before a meal — helps make su...
- Why do I need to take captopril an hour before I eat?
- Yes, a dry, persistent cough is a well-known side effect of ACE inhibitors like captopril. It happens because the drug affects certain natural substances in your airway. The cough...
- I've developed a dry cough since starting captopril. Is that normal?
Patient education
Supplement & herbal interactions
Some supplements/herbs that may interact with Captopril — tap one for details:
Captopril may be associated with lower levels of 2 nutrients — worth a chat with your pharmacist, not a cause for alarm.
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Ask a licensed pharmacist directly — free, answered by our team.
💊 What it looks like
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🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
💡 Tap an ingredient (hover on desktop) to see what it is and why it’s used.
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Lactose monohydrate is a natural sugar derived from milk. It serves as a filler and binder in tablets and capsules, helping create the proper size, texture, and consistency of the medicine.
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UNII OP1R32D61U
Microcrystalline cellulose is a purified form of cellulose, a natural fiber from plant sources. It acts as a binder and filler in tablets and capsules, helping hold ingredients together and give the medicine its shape and size.
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UNII 461P5CJN6T
Modified corn starch derived from cornstarch and treated with octenyl succinic anhydride. It acts as a thickener, stabilizer, and emulsifier to improve texture and prevent separation in the medicine.
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UNII 4ELV7Z65AP
Stearic acid is a fatty acid derived from plant or animal sources. It acts as a binder and lubricant in tablets and capsules, helping them hold together and flow smoothly during manufacturing.
4 inactive ingredients listed in the exact product block matched to this NDC.
Where does this data come from?
ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.Inactive ingredient FAQ
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💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per ea | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | $0.230 | $22.95 / 100 tablets |
| Medicaid paysCMS SDUD · 12 mo | No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data. | |
| Medicare drug plans payPart D · Q2 2026 | $0.4929 | $49.29 / 100 tablets |
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Captopril 12.5 mg 00143-1171-01 | Hikma | 100 tablets | $0.229 | AB | Availability likely | — |
| Captopril 12.5 mg 00904-7105-61 | Major | 100 tablets | $0.229 | AB | Availability likely | — |
| Captopril 12.5 mg 11788-0135-01 | AiPing | 100 tablets | $0.229 | AB | Availability likely | — |
| Captopril 12.5 mg 27241-0160-01 | Ajanta | 100 tablets | $0.229 | AB | Availability likely | — |
| Captopril 12.5 mg 31722-0141-01 | Camber | 100 tablets | $0.229 | AB | Availability likely | — |
| Captopril 12.5 mg 43547-0363-10 | Solco | 100 tablets | $0.229 | AB | Availability likely | — |
| captopril 12.5 mgthis 58657-0735-01 | Method | 100 tablets | $0.229 | AB | Availability likely | — |
| captopril 12.5 mg 58657-0935-01 | Method | 100 tablets | $0.229 | AB | Availability likely | — |
| Captopril 12.5 mg 60687-0304-21 | American | 30 tablets | $0.229 | AB | Availability likely | — |
| captopril 12.5 mg 69292-0522-01 | AMICI | 100 tablets | $0.229 | AB | Availability likely | — |
| Captopril 12.5 mg 51407-0600-01 | Golden | 100 tablets | — | AB | FDA listed | — |
| Captopril 12.5 mg 73190-0026-01 | AvKARE | 100 tablets | — | AB | FDA listed | — |
Where does this data come from?
⏳ Availability & generic status
This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.
Where does this data come from?
📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
🔬 Reported adverse events (FAERS)
Top reported reactions
Age at onset
Reporter sex
Serious outcomes
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📦 Packaging — all sizes for this product
| Package NDC | Description | Per unit | Per pack | Marketing start | Status |
|---|---|---|---|---|---|
| 58657-0735-01 You're viewing this | 100 TABLET in 1 BOTTLE (58657-735-01) | $0.2295 / ea | $22.95 | 2024-06-15 | Active |
| 58657-0735-10 | 1000 TABLET in 1 BOTTLE (58657-735-10) | — | — | 2024-06-15 | Active |
You're viewing the smallest of 2 pack sizes for this product.
Pack size FAQ
What quantity is in NDC 58657-0735-01?
What is the difference between NDC 58657-0735-01 and NDC 58657-0735-10?
What NDC number is used to bill for this package of captopril 12.5 mg Tablet?
Prices are the latest CMS NADAC pharmacy acquisition cost per NDC; per-pack figures are per-unit × pack quantity, shown only when the pack is denominated in the same measure NADAC prices.
📄 Full prescribing information FDA SPL
🚨 Boxed Warning ▾
WARNING: FETAL TOXICITY When pregnancy is detected, discontinue captopril tablets as soon as possible. Drugs that act directly on the renin-angiotensin system can cause injury and death to the developing fetus. See WARNINGS: Fetal Toxicity
🎯 Indications and Usage ▾
Hypertension Captopril tablets are indicated for the treatment of hypertension. In using captopril tablets, consideration should be given to the risk of neutropenia/agranulocytosis (see WARNINGS). Captopril tablets may be used as initial therapy for patients with normal renal function, in whom the risk is relatively low.
In patients with impaired renal function, particularly those with collagen vascular disease, captopril should be reserved for hypertensives who have either developed unacceptable side effects on other drugs, or have failed to respond satisfactorily to drug combinations. Captopril tablets are effective alone and in combination with other antihypertensive agents, especially thiazide- type diuretics. The blood pressure lowering effects of captopril and thiazides are approximately additive.
Heart Failure Captopril tablets are indicated in the treatment of congestive heart failure usually in combination with diuretics and digitalis. The beneficial effect of captopril in heart failure does not require the presence of digitalis, however, most controlled clinical trial experience with captopril has been in patients receiving digitalis, as well as diuretic treatment. Left Ventricular Dysfunction After Myocardial Infarction Captopril tablets are indicated to improve survival following myocardial infarction in clinically stable patients with left ventricular dysfunction manifested as an ejection fraction 40% and to reduce the incidence of overt heart failure and subsequent hospitalizations for congestive heart failure in these patients.
Diabetic Nephropathy Captopril tablets are indicated for the treatment of diabetic nephropathy (proteinuria > 500 mg/day) in patients with type I insulin-dependent diabetes mellitus and retinopathy. Captopril tablets decrease the rate of progression of renal insufficiency and development of serious adverse clinical outcomes (death or need for renal transplantation or dialysis). In considering use of captopril tablets, it should be noted that in controlled trials ACE inhibitors have an effect on blood pressure that is less in black patients than in non-blacks.
In addition, ACE inhibitors (for which adequate data are available) cause a higher rate of angioedema in black than in non-black patients (see WARNINGS: Head and Neck Angioedema and Intestinal Angioedema).
⏱️ Dosage and Administration ▾
DOSAGE AND ADMINISTRATION Captopril tablets should be taken one hour before meals. Dosage must be individualized. Hypertension Initiation of therapy requires consideration of recent antihypertensive drug treatment, the extent of blood pressure elevation, salt restriction, and other clinical circumstances.
If possible, discontinue the patient’s previous antihypertensive drug regimen for one week before starting captopril tablets. The initial dose of captopril tablets is 25 mg b.i.d. or t.i.d. If satisfactory reduction of blood pressure has not been achieved after one or two weeks, the dose may be increased to 50 mg b.i.d. or t.i.d.
Concomitant sodium restriction may be beneficial when captopril tablets are used alone. The dose of captopril tablets in hypertension usually does not exceed 50 mg t.i.d. Therefore, if the blood pressure has not been satisfactorily controlled after one to two weeks at this dose, (and the patient is not already receiving a diuretic), a modest dose of a thiazide-type diuretic (e.g., hydrochlorothiazide, 25 mg daily), should be added.
The diuretic dose may be increased at one- to two-week intervals until its highest usual antihypertensive dose is reached. If captopril tablets are being started in a patient already receiving a diuretic, captopril tablets therapy should be initiated under close medical supervision (see WARNINGS and PRECAUTIONS: Drug Interactions regarding hypotension), with dosage and titration of captopril tablets as noted above. If further blood pressure reduction is required, the dose of captopril tablets may be increased to 100 mg b.i.d. or t.i.d. and then, if necessary, to 150 mg b.i.d. or t.i.d.
(while continuing the diuretic). The usual dose range is 25 to 150 mg b.i.d. or t.i.d. A maximum daily dose of 450 mg captopril tablets should not be exceeded.
For patients with severe hypertension (e.g., accelerated or malignant hypertension), when temporary discontinuation of current antihypertensive therapy is not practical or desirable, or when prompt titration to more normotensive blood pressure levels is indicated, diuretic should be continued but other current antihypertensive medication stopped and captopril tablets dosage promptly initiated at 25 mg b.i.d. or t.i.d., under close medical supervision. When necessitated by the patient’s clinical condition, the daily dose of captopril tablets may be increased every 24 hours or less under continuous medical supervision until a satisfactory blood pressure response is obtained or the maximum dose of captopril tablets is reached.
In this regimen, addition of a more potent diuretic, e.g., furosemide, may also be indicated. Beta-blockers may also be used in conjunction with captopril tablets therapy (see PRECAUTIONS: Drug Interactions), but the effects of the two drugs are less than additive. Heart Failure Initiation of therapy requires consideration of recent diuretic therapy and the possibility of severe salt/volume depletion.
In patients with either normal or low blood pressure, who have been vigorously treated with diuretics and who may be hyponatremic and/or hypovolemic, a starting dose of 6.25 or 12.5 mg t.i.d. may minimize the magnitude or duration of the hypotensive effect (see WARNINGS: Hypotension); for these patients, titration to the usual daily dosage can then occur within the next several days. For most patients the usual initial daily dosage is 25 mg t.i.d. After a dose of 50 mg t.i.d. is reached, further increases in dosage should be delayed, where possible, for at least two weeks to determine if a satisfactory response occurs.
Most patients studied have had a satisfactory clinical improvement at 50 or 100 mg t.i.d. A maximum daily dose of 450 mg of captopril tablets should not be exceeded. Captopril tablets should generally be used in conjunction with a diuretic and digitalis.
Captopril tablets therapy must be initiated under very close medical supervision. Left Ventricular Dysfunction After Myocardial Infarction The recommen…
⛔ Contraindications ▾
CONTRAINDICATIONS Captopril tablets are contraindicated in patients who are hypersensitive to this product or any other angiotensin- converting enzyme inhibitor (e.g., a patient who has experienced angioedema during therapy with any other ACE inhibitor). Do not co-administer aliskiren with captopril tablets in patients with diabetes (see PRECAUTIONS: Drug Interactions). Captopril tablets are contraindicated in combination with a neprilysin inhibitor (e.g., sacubitril).
Do not administer captopril tablets within 36 hours of switching to or from sacubitril/valsartan, a neprilysin inhibitor (see PRECAUTIONS: Drug Interactions).
⚠️ Warnings ▾
Anaphylactoid and Possibly Related Reactions Presumably because angiotensin-converting enzyme inhibitors affect the metabolism of eicosanoids and polypeptides, including endogenous bradykinin, patients receiving ACE inhibitors (including captopril tablets) may be subject to a variety of adverse reactions, some of them serious. Head and Neck Angioedema Angioedema involving the extremities, face, lips, mucous membranes, tongue, glottis or larynx has been seen in patients treated with ACE inhibitors, including captopril.
If angioedema involves the tongue, glottis or larynx, airway obstruction may occur and be fatal. Emergency therapy, including but not necessarily limited to, subcutaneous administration of a 1:1000 solution of epinephrine should be promptly instituted. Swelling confined to the face, mucous membranes of the mouth, lips and extremities has usually resolved with discontinuation of captopril; some cases required medical therapy (see PRECAUTIONS: Information for Patients and ADVERSE REACTIONS).
Patients receiving coadministration of ACE inhibitor and mTOR (mammalian target of rapamycin) inhibitor (e.g., temsirolimus, sirolimus, everolimus) therapy or a neprilysin inhibitor may be at increased risk for angioedema (see PRECAUTIONS: Drug Interactions). Intestinal Angioedema Intestinal angioedema has been reported in patients treated with ACE inhibitors. These patients presented with abdominal pain (with or without nausea or vomiting); in some cases there was no prior history of facial angioedema and C-1 esterase levels were normal.
The angioedema was diagnosed by procedures including abdominal CT scan or ultrasound, or at surgery, and symptoms resolved after stopping the ACE inhibitor. Intestinal angioedema should be included in the differential diagnosis of patients on ACE inhibitors presenting with abdominal pain. Anaphylactoid Reactions During Desensitization Two patients undergoing desensitizing treatment with hymenoptera venom while receiving ACE inhibitors sustained life-threatening anaphylactoid reactions.
In the same patients, these reactions were avoided when ACE inhibitors were temporarily withheld, but they reappeared upon inadvertent rechallenge. Anaphylactoid Reactions During Membrane Exposure Anaphylactoid reactions have been reported in patients dialyzed with high-flux membranes and treated concomitantly with an ACE inhibitor. Anaphylactoid reactions have also been reported in patients undergoing low-density lipoprotein apheresis with dextran sulfate absorption.
Neutropenia/Agranulocytosis Neutropenia (< 1000/mm3) with myeloid hypoplasia has resulted from use of captopril. About half of the neutropenic patients developed systemic or oral cavity infections or other features of the syndrome of agranulocytosis. The risk of neutropenia is dependent on the clinical status of the patient: In clinical trials in patients with hypertension who have normal renal function (serum creatinine less than 1.6 mg/dL and no collagen vascular disease), neutropenia has been seen in one patient out of over 8,600 exposed.
In patients with some degree of renal failure (serum creatinine at least 1.6 mg/dL) but no collagen vascular disease, the risk of neutropenia in clinical trials was about 1 per 500, a frequency over 15 times that for uncomplicated hypertension. Daily doses of captopril were relatively high in these patients, particularly in view of their diminished renal function. In foreign marketing experience in patients with renal failure, use of allopurinol concomitantly with captopril has been associated with neutropenia but this association has not appeared in U.S. reports.
In patients with collagen vascular diseases (e.g., systemic lupus erythematosus, scleroderma) and impaired renal function, neutropenia occurred in 3.7 percent of patients in clinical trials. While none of the over 750 patients in formal clinical trials of heart failure developed neutropenia, it has occurred during the subsequent clinical experience. A…
🤒 Adverse Reactions ▾
ADVERSE REACTIONS Reported incidences are based on clinical trials involving approximately 7000 patients. Renal About one of 100 patients developed proteinuria (see WARNINGS). Each of the following has been reported in approximately 1 to 2 of 1000 patients and are of uncertain relationship to drug use: renal insufficiency, renal failure, nephrotic syndrome, polyuria, oliguria, and urinary frequency.
Hematologic Neutropenia/agranulocytosis has occurred (see WARNINGS). Cases of anemia, thrombocytopenia, and pancytopenia have been reported. Dermatologic Rash, often with pruritus, and sometimes with fever, arthralgia, and eosinophilia, occurred in about 4 to 7 (depending on renal status and dose) of 100 patients, usually during the first four weeks of therapy.
It is usually maculopapular, and rarely urticarial. The rash is usually mild and disappears within a few days of dosage reduction, short-term treatment with an antihistaminic agent, and/or discontinuing therapy; remission may occur even if captopril is continued. Pruritus, without rash, occurs in about 2 of 100 patients.
Between 7 and 10 percent of patients with skin rash have shown an eosinophilia and/or positive ANA titers. A reversible associated pemphigoid-like lesion, and photosensitivity, have also been reported. Flushing or pallor has been reported in 2 to 5 of 1000 patients.
Cardiovascular Hypotension may occur; see WARNINGS and PRECAUTIONS: Drug Interactions for discussion of hypotension with captopril therapy. Tachycardia, chest pain, and palpitations have each been observed in approximately 1 of 100 patients. Angina pectoris, myocardial infarction, Raynaud’s syndrome, and congestive heart failure have each occurred in 2 to 3 of 1000 patients.
Dysgeusia Approximately 2 to 4 (depending on renal status and dose) of 100 patients developed a diminution or loss of taste perception. Taste impairment is reversible and usually self-limited (2 to 3 months) even with continued drug administration. Weight loss may be associated with the loss of taste.
Angioedema Angioedema involving the extremities, face, lips, mucous membranes, tongue, glottis or larynx has been reported in approximately one in 1000 patients. Angioedema involving the upper airways has caused fatal airway obstruction (see WARNINGS: Head and Neck Angioedema, Intestinal Angioedema and PRECAUTIONS: Information for Patients). Cough Cough has been reported in 0.5 to 2% of patients treated with captopril in clinical trials (see PRECAUTIONS: General: Cough).
The following have been reported in about 0.5 to 2 percent of patients but did not appear at increased frequency compared to placebo or other treatments used in controlled trials: gastric irritation, abdominal pain, nausea, vomiting, diarrhea, anorexia, constipation, aphthous ulcers, peptic ulcer, dizziness, headache, malaise, fatigue, insomnia, dry mouth, dyspnea, alopecia, paresthesias. Other clinical adverse effects reported since the drug was marketed are listed below by body system. In this setting, an incidence or causal relationship cannot be accurately determined.
Body as a Whole: Anaphylactoid reactions (see WARNINGS: Anaphylactoid and Possible Related Reactions and PRECAUTIONS: Hemodialysis). General: Asthenia, gynecomastia. Cardiovascular: Cardiac arrest, cerebrovascular accident/insufficiency, rhythm disturbances, orthostatic hypotension, syncope.
Dermatologic: Bullous pemphigus, erythema multiforme (including Stevens-Johnson syndrome), exfoliative dermatitis. Gastrointestinal: Pancreatitis, glossitis, dyspepsia. Hematologic: Anemia, including aplastic and hemolytic.
Hepatobiliary: Jaundice, hepatitis, including rare cases of necrosis, cholestasis. Metabolic: Symptomatic hyponatremia. Musculoskeletal: Myalgia, myasthenia.
Nervous/Psychiatric: Ataxia, confusion, depression, nervousness, somnolence. Respiratory: Bronchospasm, eosinophilic pneumonitis, rhinitis. Special Senses: Blurred vision.
Urogenital: Impotence. As with other ACE inhibitors, a syndr…
🔄 Drug Interactions ▾
Drug Interactions Dual Blockade of the Renin-Angiotensin System (RAS) Dual blockade of the RAS with angiotensin receptor blockers, ACE inhibitors, or aliskiren is associated with increased risks of hypotension, hyperkalemia, and changes in renal function (including acute renal failure) compared to monotherapy. Most patients receiving the combination of two RAS inhibitors do not obtain any additional benefit compared to monotherapy. In general, avoid combined use of RAS inhibitors.
Closely monitor blood pressure, renal function and electrolytes in patients on captopril tablets and other agents that block the RAS. Do not coadminister aliskiren with captopril tablets in patients with diabetes. Avoid use of aliskiren with captopril tablets in patients with renal impairment (GFR < 60 ml/min).
Non-Steroidal Anti-Inflammatory Agents including Selective Cyclooxygenase-2 Inhibitors (COX-2 Inhibitors) In patients who are elderly, volume-depleted (including those on diuretic therapy), or with compromised renal function, coadministration of NSAIDs, including selective COX-2 inhibitors, with ACE inhibitors, including captopril, may result in deterioration of renal function, including possible acute renal failure. These effects are usually reversible. Monitor renal function periodically in patients receiving captopril and NSAID therapy.
The antihypertensive effect of ACE inhibitors, including captopril, may be attenuated by NSAIDs. Hypotension–Patients on Diuretic Therapy Patients on diuretics and especially those in whom diuretic therapy was recently instituted, as well as those on severe dietary salt restriction or dialysis, may occasionally experience a precipitous reduction of blood pressure usually within the first hour after receiving the initial dose of captopril. The possibility of hypotensive effects with captopril can be minimized by either discontinuing the diuretic or increasing the salt intake approximately one week prior to initiation of treatment with captopril tablets or initiating therapy with small doses (6.25 or 12.5 mg).
Alternatively, provide medical supervision for at least one hour after the initial dose. If hypotension occurs, the patient should be placed in a supine position and, if necessary, receive an intravenous infusion of normal saline. This transient hypotensive response is not a contraindication to further doses which can be given without difficulty once the blood pressure has increased after volume expansion.
Agents Having Vasodilator Activity Data on the effect of concomitant use of other vasodilators in patients receiving captopril tablets for heart failure are not available; therefore, nitroglycerin or other nitrates (as used for management of angina) or other drugs having vasodilator activity should, if possible, be discontinued before starting captopril tablets. If resumed during captopril tablets therapy, such agents should be administered cautiously, and perhaps at lower dosage. Agents Causing Renin Release Captopril’s effect will be augmented by antihypertensive agents that cause renin release.
For example, diuretics (e.g., thiazides) may activate the renin-angiotensin-aldosterone system. Agents Affecting Sympathetic Activity The sympathetic nervous system may be especially important in supporting blood pressure in patients receiving captopril alone or with diuretics. Therefore, agents affecting sympathetic activity (e.g., ganglionic blocking agents or adrenergic neuron blocking agents) should be used with caution.
Beta-adrenergic blocking drugs add some further antihypertensive effect to captopril, but the overall response is less than additive. Agents Increasing Serum Potassium Since captopril decreases aldosterone production, elevation of serum potassium may occur. Potassium-sparing diuretics such as spironolactone, triamterene, or amiloride, or potassium supplements should be given only for documented hypokalemia, and then with caution, since they may lead to a significant increase of serum pota…
🔄 Drug / Laboratory Test Interactions ▾
Drug/Laboratory Test Interaction Captopril may cause a false-positive urine test for acetone.
🤰 Pregnancy ▾
Pregnancy Female patients of childbearing age should be told about the consequences of exposure to captopril tablets during pregnancy. Discuss treatment options with women planning to become pregnant. Patients should be asked to report pregnancies to their physicians as soon as possible.
🧒 Pediatric Use ▾
Pediatric Use Neonates with a History of In Utero Exposure to Captopril Tablets If oliguria or hypotension occurs, direct attention toward support of blood pressure and renal perfusion. Exchange transfusions or dialysis may be required as a means of reversing hypotension and/or substituting for disordered renal function. While captopril may be removed from the adult circulation by hemodialysis, there is inadequate data concerning the effectiveness of hemodialysis for removing it from the circulation of neonates or children.
Peritoneal dialysis is not effective for removing captopril; there is no information concerning exchange transfusion for removing captopril from the general circulation. Safety and effectiveness in pediatric patients have not been established. There is limited experience reported in the literature with the use of captopril in the pediatric population; dosage, on a weight basis, was generally reported to be comparable to or less than that used in adults.
Infants, especially newborns, may be more susceptible to the adverse hemodynamic effects of captopril. Excessive, prolonged and unpredictable decreases in blood pressure and associated complications, including oliguria and seizures, have been reported. Captopril tablets should be used in pediatric patients only if other measures for controlling blood pressure have not been effective.
🆘 Overdosage ▾
OVERDOSAGE Correction of hypotension would be of primary concern. Volume expansion with an intravenous infusion of normal saline is the treatment of choice for restoration of blood pressure. While captopril may be removed from the adult circulation by hemodialysis, there is inadequate data concerning the effectiveness of hemodialysis for removing it from the circulation of neonates or children.
Peritoneal dialysis is not effective for removing captopril; there is no information concerning exchange transfusion for removing captopril from the general circulation.
🧬 Mechanism of Action ▾
Mechanism of Action The mechanism of action of captopril tablets have not yet been fully elucidated. Its beneficial effects in hypertension and heart failure appear to result primarily from suppression of the renin-angiotensin-aldosterone system. However, there is no consistent correlation between renin levels and response to the drug.
Renin, an enzyme synthesized by the kidneys, is released into the circulation where it acts on a plasma globulin substrate to produce angiotensin I, a relatively inactive decapeptide. Angiotensin I is then converted by angiotensin converting enzyme (ACE) to angiotensin II, a potent endogenous vasoconstrictor substance. Angiotensin II also stimulates aldosterone secretion from the adrenal cortex, thereby contributing to sodium and fluid retention.
Captopril tablets prevent the conversion of angiotensin I to angiotensin II by inhibition of ACE, a peptidyldipeptide carboxy hydrolase. This inhibition has been demonstrated in both healthy human subjects and in animals by showing that the elevation of blood pressure caused by exogenously administered angiotensin I was attenuated or abolished by captopril. In animal studies, captopril did not alter the pressor responses to a number of other agents, including angiotensin II and norepinephrine, indicating specificity of action.
ACE is identical to “bradykininase”, and captopril tablets may also interfere with the degradation of the vasodepressor peptide, bradykinin. Increased concentrations of bradykinin or prostaglandin E may also have a role in the therapeutic effect of captopril tablets. Inhibition of ACE results in decreased plasma angiotensin II and increased plasma renin activity (PRA), the latter resulting from loss of negative feedback on renin release caused by reduction in angiotensin II.
The reduction of angiotensin II leads to decreased aldosterone secretion, and, as a result, small increases in serum potassium may occur along with sodium and fluid loss. The antihypertensive effects persist for a longer period of time than does demonstrable inhibition of circulating ACE. It is not known whether the ACE present in vascular endothelium is inhibited longer than the ACE in circulating blood.
📦 How Supplied / Storage and Handling ▾
HOW SUPPLIED Captopril Tablets, USP are available containing 12.5 mg, 25 mg, 50 mg or 100 mg of captopril, USP. The 12.5 mg tablets are white to off-white, arc diamond shaped tablets with bisect on one side and “131” on the other side. They are available as follows: Bottles of 100 Tablets NDC 58657-735-01 Bottles of 1000 Tablets NDC 58657-735-10 Carton of 30 tablets (10 tablets per blister pack x 3) NDC 58657-935-03 Carton of 100 tablets (10 tablets per blister pack x 10) NDC 58657-935-01 The 25 mg tablets are white to off-white, arc diamond shaped tablets with quadrisect on one side and “132” on the other side.
They are available as follows: Bottles of 100 Tablets NDC 58657-736-01 Bottles of 1000 Tablets NDC 58657-736-10 Carton of 30 tablets (10 tablets per blister pack x 3) NDC 58657-936-03 Carton of 100 tablets (10 tablets per blister pack x 10) NDC 58657-936-01 The 50 mg tablets are white to off-white, arc diamond shaped tablets with bisect on one side and “133” on the other side. They are available as follows: Bottles of 100 Tablets NDC 58657-737-01 Bottles of 1000 Tablets NDC 58657-737-10 Carton of 30 tablets (10 tablets per blister pack x 3) NDC 58657-937-03 Carton of 100 tablets (10 tablets per blister pack x 10) NDC 58657-937-01 The 100 mg tablets are white to off-white, capsule shaped tablets with bisect on one side and “134” on the other side.
They are available as follows: Bottles of 100 Tablets NDC 58657-738-01 Bottles of 500 Tablets NDC 58657-738-50 Carton of 30 tablets (10 tablets per blister pack x 3) NDC 58657-938-03 Carton of 100 tablets (10 tablets per blister pack x 10) NDC 58657-938-01 Bottles contain a desiccant-charcoal canister. All captopril tablets are white and may exhibit a slight sulfurous odor.
📦 Storage and Handling ▾
Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature]. Protect from moisture. Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure. To report SUSPECTED ADVERSE REACTIONS, contact Innogenix, LLC at 1-844-466-6469 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch
📋 Description ▾
DESCRIPTION Captopril is a specific competitive inhibitor of angiotensin I-converting enzyme (ACE), the enzyme responsible for the conversion of angiotensin I to angiotensin II. Captopril is designated chemically as 1-[(2S)-3-mercapto-2-methylpropionyl]-L-proline [MW 217.29] and has the following structure: Captopril, USP is a white to off-white crystalline powder that may have a slight sulfurous odor; it is soluble in water (approx. 160 mg/mL), methanol, and ethanol and sparingly soluble in chloroform and ethyl acetate.
Each tablet for oral administration contains 12.5 mg, 25 mg, 50 mg or 100 mg of captopril and the following inactive ingredients: corn starch, lactose monohydrate, microcrystalline cellulose and stearic acid. chemical structure Mechanism of Action The mechanism of action of captopril tablets have not yet been fully elucidated. Its beneficial effects in hypertension and heart failure appear to result primarily from suppression of the renin-angiotensin-aldosterone system. However, there is no consistent correlation between renin levels and response to the drug.
Renin, an enzyme synthesized by the kidneys, is released into the circulation where it acts on a plasma globulin substrate to produce angiotensin I, a relatively inactive decapeptide. Angiotensin I is then converted by angiotensin converting enzyme (ACE) to angiotensin II, a potent endogenous vasoconstrictor substance. Angiotensin II also stimulates aldosterone secretion from the adrenal cortex, thereby contributing to sodium and fluid retention.
Captopril tablets prevent the conversion of angiotensin I to angiotensin II by inhibition of ACE, a peptidyldipeptide carboxy hydrolase. This inhibition has been demonstrated in both healthy human subjects and in animals by showing that the elevation of blood pressure caused by exogenously administered angiotensin I was attenuated or abolished by captopril. In animal studies, captopril did not alter the pressor responses to a number of other agents, including angiotensin II and norepinephrine, indicating specificity of action.
ACE is identical to “bradykininase”, and captopril tablets may also interfere with the degradation of the vasodepressor peptide, bradykinin. Increased concentrations of bradykinin or prostaglandin E may also have a role in the therapeutic effect of captopril tablets. Inhibition of ACE results in decreased plasma angiotensin II and increased plasma renin activity (PRA), the latter resulting from loss of negative feedback on renin release caused by reduction in angiotensin II.
The reduction of angiotensin II leads to decreased aldosterone secretion, and, as a result, small increases in serum potassium may occur along with sodium and fluid loss. The antihypertensive effects persist for a longer period of time than does demonstrable inhibition of circulating ACE. It is not known whether the ACE present in vascular endothelium is inhibited longer than the ACE in circulating blood.
Pharmacokinetics After oral administration of therapeutic doses of captopril tablets, rapid absorption occurs with peak blood levels at about one hour. The presence of food in the gastrointestinal tract reduces absorption by about 30 to 40 percent; captopril therefore should be given one hour before meals. Based on carbon-14 labeling, average minimal absorption is approximately 75 percent.
In a 24-hour period, over 95 percent of the absorbed dose is eliminated in the urine; 40 to 50 percent is unchanged drug; most of the remainder is the disulfide dimer of captopril and captopril-cysteine disulfide. Approximately 25 to 30 percent of the circulating drug is bound to plasma proteins. The apparent elimination half-life for total radioactivity in blood is probably less than 3 hours.
An accurate determination of half-life of unchanged captopril is not, at present, possible, but it is probably less than 2 hours. In patients with renal impairment, however, retention of captopril occurs (see DOSAGE AND ADMINISTRATION). Adminis…
💬 Information for Patients ▾
Information For Patients Patients should be advised to immediately report to their physician any signs or symptoms suggesting angioedema (e.g., swelling of face, eyes, lips, tongue, larynx and extremities; difficulty in swallowing or breathing; hoarseness) and to discontinue therapy (see WARNINGS: Head and Neck Angioedema and Intestinal Angioedema). Patients should be told to report promptly any indication of infection (e.g., sore throat, fever), which may be a sign of neutropenia, or of progressive edema which might be related to proteinuria and nephrotic syndrome.
All patients should be cautioned that excessive perspiration and dehydration may lead to an excessive fall in blood pressure because of reduction in fluid volume. Other causes of volume depletion such as vomiting or diarrhea may also lead to a fall in blood pressure; patients should be advised to consult with the physician. Patients should be advised not to use potassium-sparing diuretics, potassium supplements or potassium- containing salt substitutes without consulting their physician (see PRECAUTIONS: General and Drug Interactions; ADVERSE REACTIONS).
Patients should be warned against interruption or discontinuation of medication unless instructed by the physician. Heart failure patients on captopril therapy should be cautioned against rapid increases in physical activity. Patients should be informed that captopril tablets should be taken one hour before meals (see DOSAGE AND ADMINISTRATION).