Captopril

Captopril is a sulfhydryl containing ACE inhibitor. Captopril is used to treat hypertension (high blood pressure), congestive heart failure and kidney diseases in diabetic patients.


Adult Dose
Dose: 12.5 to 50 mg
Single Dose: 31 (31.25)
Frequency: 12 hourly
Route: PO
Instructions:
Neonatal
Dose: 0.5 to 2 mg/kg
Single Dose: 1.2 (1.25)
Frequency: 8 hourly
Route: Oral
Instructions: Gradually increase the Dose
Paedriatic
Dose: 0.5 to 2 mg/kg
Single Dose: 1.2 (1.25)
Frequency: 8 hourly
Route: Oral
Instructions: Gradually increase the Dose
Characteristics
. It is of Synthetic origin and belongs to Mercapto L-Proline. It belongs to Angiotensin converting enzyme inhibitor-ACEI pharmacological group on the basis of mechanism of action and also classified in Antihypertensive Agents pharmacological group.The Molecular Weight of Captopril is 217.30. Its pKa is 3.7, 9.8.
Contraindications
Captopril is contraindicated in conditions like Renal diseases,Collagen vascular disease,Renal artery stenosis.
Effects
The severe or irreversible adverse effects of Captopril, which give rise to further complications include Renal damage, Proteinuria.Captopril produces potentially life-threatening effects which include Hyperkalemia, Neutropenia. which are responsible for the discontinuation of Captopril therapy.The signs and symptoms that are produced after the acute overdosage of Captopril include Hypotension, Respiratory distress, Angioedema, Laryngeal obstruction.The symptomatic adverse reactions produced by Captopril are more or less tolerable and if they become severe, they can be treated symptomatically, these include Skin rash, Taste disturbance, Cough.
Indications
Captopril is primarily indicated in conditions like Congestive heart failure, Congestive heart failure (adjunct), Diabetic nephropathy, Diabetic retinopathy, Essential hypertension, Essential hypertension (mild to moderate), severe hypertension resistant to other treatment, Gastric acid reduction during anaesthesia, Hypertension, Iron deficiency anaemia, Prophylaxis of acid aspiration, Renal hypertension, Scleroderma renal crisis.
Interactions
Captopril is known to interact with other drugs, the details of drug interactions is as follows:DrugDetailsSeverityOnsetManagementAlcoholEnhanced hypotensive effect when ACE inhibitors (e.g Captopril) given with Alcohol.AldesleukinEnhanced hypotensive effect when aldesleukin given with ACE inhibitors (e.g Captopril).AllopurinolIncreased risk of toxicity when Allopurinol given with Captopril especially in renal impairment. Captopril may enhance the potential for allergic or hypersensitivity reactions to Allopurinol. MajorImmediate (Sequence important)AlprostadilEnhanced hypotensive effects when alprostadil given with ACE inhibitors (e.g Captopril)AzathioprineAzathioprine increases risk of leucopenia with captopril.BaclofenEnhanced hypotensive effects when Baclofen given with ACE inhibitors (e.g Captopril)Bovine InsulinACE inhibitors (e.g Captopril) possibly enhance hypoglycemic effect of insulin. Clonidine (HCl)Previous treatment with clonidine possibly delays antihypertensive effect of captopril.CyclophosphamideCyclosporin ACaptopril may enhance the nephrotoxic effect of CycloSPORINE.MajorDelayedMonitor for increased signs and symptoms of nephrotoxicity during concomitant therapy with cyclosporine and Captopril. Maintenance of adequate hydration (caution with diuretic use) may reduce of risk of ill effects.DiazoxideEnhanced hypotensive effect when Diazoxide given with Captopril.DigoxinIncrease plasma concentration of digoxin.Monitor serum digoxin levels.Frusemide or FurosemideFrusemide may enhance the hypotensive effect of captopril. Specifically, postural hypotension which can accompany captopril initiation. Frusemide may enhance the nephrotoxic effect of captopril.Moderate (Sequence important)Monitor for evidence of significant postural hypotension if Captopril is initiated (first dose) in patient already receiving Furosemide, especially if the patient has signs or symptoms of hypovolemia or hyponatremia. May consider ensuring the patient remains supine for 3 or more hours following the administration of the first dose of the Captopril. Monitor for signs or symptoms of renal dysfunction if these two agents are used concomitantly long-term. Consider a reduced dosage of either Furosemide or Captopril if serum creatinine increases during concomitant therapy.Human InsulinACE inhibitors (e.g Captopril) possibly enhance hypoglycemic effect of insulin. IndomethacinIndomethacin may diminish the antihypertensive effect of Captopril.ModerateRapidConsider alternative anti-inflammatory therapy, especially in CHF patients, to avoid the potential negative consequences of concomitant nonsteroidal anti-inflammatory agent (NSAID) therapy (fluid accumulation/edema). Monitor for decreased therapeutic effects of Captopril if Indomethacin is initiated/dose increased, or increased effects if Indomethacin is discontinued/dose decreased. Monitor blood pressure, in particular. This is probably of most concern with chronic dosing of NSAID; however, blood pressure increases have been noted following a single NSAID dose. In addition, concomitant therapy with Indomethacin and Captopril increases the risk of renal dysfunction.LithiumCaptopril may increase the serum concentration of LithiumModerateDelayedMonitor for increased serum concentrations/toxic effects of lithium if Captopril is initiated/dose increased, or decreased effects if Captopril is discontinued/dose decreased. Lithium dosage reductions will likely be needed following the addition of Captopril.MetolazoneMetolazone may enhance the hypotensive effect of Captopril. Specifically, postural hypotension which can accompany Captopril initiation. Metolazone may enhance the nephrotoxic effect of Captopril.ModerateMonitor for evidence of significant postural hypotension if Captopril is initiated (first dose) in patient already receiving Metolazone, especially if the patient has signs or symptoms of hypovolemia or hyponatremia. May consider ensuring the patient remains supine for 3 or more hours following the administration of the first dose of the Captopril. Monitor for signs or symptoms of renal dysfunction if these two agents are used concomitantly long-term.Porcine InsulinACE inhibitors (e.g Captopril) possibly enhance hypoglycemic effect of insulin. Potassium GlycerophosphateConcurrent use may cause too much potassium in the blood.ProbenecidProbenecid reduces excretion of captopril.Procainamide (HCl)Procainamide increases risk of toxicity with captopril, especially in renal impairment.SpironolactoneSpironolactone may enhance the hyperkalemic effect of Captopril. ModerateThese agents are often, and appropriately so, used concomitantly in the treatment of severe CHF. It seems prudent to monitor for increased incidence of hyperkalemia if Spironolactone and Captopril are used concomitantly.Technetium Succimer Tc-99mIn patients with unilateral renal artery stenosis, use of Captopril may result in decreased uptake of technetium Tc 99m succimer by the affected kidney because of a loss of effective trans-membrane filtration pressure. These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Interfrence
False +ve test for Urinary Nitrites and Acetone
Risks
Drug should not be given to Pregnant Mothers, and Neonates.If prescribing authority justifies the benefits of the drug against the possible damages he/she should reevaluate them and consult the reference material and previous studies.
Storage
Tab Store in a well closed container, at room temperature, Below 30°C. Protect from Sunlight and Moisture.
Warnings
White blood cells (W.B.Cs) counts and urinary protein estimation should be done before and during treatment Captopril therapy can cause neutropenia or agranulocytosis. Patients with renal disease, patients with immunosuppression or receiving immunosuppressives, and patients with collagen vascular disease or autoimmune disease are at a greater risk for developing these complications. It should be used with caution in patients with pre-existing bone marrow depression. The dose should be adjusted in patients with renal impairment. It should be used cautiously in patients with congestive heart failure. Initial doses should be lower than in the treatment of hypertension becauseof a greater risk of developing hypotension. It should not be administered to patients with pre-existing renal artery stenosis. Renal function should be monitored closely during the first 2 weeks after initiating therapy. It should be discontinued if renal function worsens acutely. Other types of renal disease can actually improve during captopril therapy. The dose should be adjusted inpatients with renal impairment. It should be used with caution patients with hyperkalemia. It is classified as pregnancy category C and should be used with caution during pregnancy only if clearly needed.
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