CAPTOPRIL

Captopril  is an angiotensin-converting enzyme (ACE) inhibitor used for the treatment of hypertension and some types of congestive heart failure. Captopril was the first ACE inhibitor developed and was considered a breakthrough both because of its novel mechanism of action and also because of the revolutionary development process. Captopril is commonly marketed by Bristol-Myers Squibb under the trade name Capoten.
Captopril 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.

CAPOTEN is available in potencies of 12.5 mg, 25 mg, 50 mg, and 100 mg as scored tablets for oral administration.

(2S)-1-[(2S)-2-methyl-3-sulfanylpropanoyl]
pyrrolidine-2-carboxylic acid


USE AND DOSE

Captopril's main uses are based on its vasodilation and inhibition of some renal function activities. These benefits are most clearly seen in the following conditions:
1) Hypertension
2) Cardiac conditions such as congestive heart failure and after myocardial infarction
3) Preservation of kidney function in diabetic nephropathy
Additionally, it has shown mood-elevating properties in some patients. This is consistent with the observation that animal screening models indicate putative antidepressant activity for this compound, although there has been one negative study. Formal clinical trials in depressed patients have not been reported.
It has also been investigated for use in the treatment of cancer.
 BRANDS IN INDIA - ACETEN 25, ACETEN 12.5

Hypertension  -  Oral
Adult: Initially, 12.5 mg bid or 6.25 mg bid in combination with a diuretic, at bedtime to avoid precipitous fall in BP, gradually increased at 2-4-wk intervals according to response. Maintenance: 25-50 mg bid. Max: 50 mg tid.
Child: Neonate: Test dose: 10-50 mcg/kg (for neonates <37 1-12="" 1-2="" 10-50="" 100-300="" 100="" 10="" 12-18="" 12.5-25="" 150="" 1="" 2-3="" 2="" 300="" 4="" 6.25="" 6="" age:="" bp="" daily="" divided="" dose:="" doses.="" doses="" for="" give="" hr="" if="" in="" increased="" kg="" max:="" mcg="" mg="" monitor="" mth-12="" mth:="" nbsp="" needed.="" neonates="" or="" p="" postmenstrual="" test="" times="" tolerated="" wk="" yr:="">

Heart failure    -   Oral
Adult: Initially, 6.25-12.5 mg bid-tid. Maintenance: 25 mg bid-tid. Max: 50 mg tid.
Child: Neonate: Test dose: 10-50 mcg/kg (for neonates <37 1-12="" 1-2="" 10-50="" 100-300="" 100="" 10="" 12-18="" 12.5-25="" 150="" 1="" 2-3="" 2="" 300="" 4="" 6.25="" 6="" age:="" bp="" daily="" divided="" dose:="" doses.="" doses="" for="" give="" hr="" if="" in="" increased="" kg="" max:="" mcg="" mg="" monitor="" mth-12="" mth:="" needed.="" neonates="" or="" p="" postmenstrual="" test="" times="" tolerated="" wk="" yr:="">

Post myocardial infarction   -  Oral
Adult: May be started 3 days after MI. Initially, 6.25 mg/day increased after several wk to 150 mg daily in divided doses if tolerated.


Diabetic nephropathy   -   Oral
Adult: Proteinuria >500 mg per 24 hr (in patients with Type 1 diabetes mellitus and retinopathy): 25 mg tid. May be taken with other anti-hypertensives if patient requires further lowering of BP.
Child: Neonate: Test dose: 10-50 mcg/kg (for neonates <37 1-12="" 1-2="" 10-50="" 100-300="" 100="" 10="" 12-18="" 12.5-25="" 150="" 1="" 2-3="" 2="" 300="" 4="" 6.25="" 6="" age:="" bp="" daily="" divided="" dose:="" doses.="" doses="" for="" give="" hr="" if="" in="" increased="" kg="" max:="" mcg="" mg="" monitor="" mth-12="" mth:="" needed.="" neonates="" or="" p="" postmenstrual="" test="" times="" tolerated="" wk="" yr:="">
OVERDOSE   -  In case of overdose, call your local poison control center at 1-800-222-1222. If the victim has collapsed or is not breathing, call local emergency services at 911.

PREGNANCY - Do not take captopril if you are pregnant or breast-feeding. If you become pregnant while taking captopril, call your doctor immediately.


Special Populations: Patients with severe renal impairment: CrCl <30 12.5="" bid.="" initially="" mg="" min:="" ml="" p="">
Before taking captopril,
tell your doctor and pharmacist if you are allergic to captopril or any other drugs.
tell your doctor if you have diabetes (high blood sugar) and you are taking aliskiren (Tekturna, in Amturnide, Tekamlo, Tekturna HCT). Your doctor will probably tell you not to take captopril if you have diabetes and you are also taking aliskiren.
tell your doctor and pharmacist what prescription and nonprescription medications you are taking, especially diuretics ('water pills'), lithium (Eskalith, Lithobid), other medications for high blood pressure, potassium supplements, and vitamins.
tell your doctor if you have or have ever had heart or kidney disease or diabetes.
if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking captopril.


DRUG INTERACTIONS

captopril WITH  spironolactone
Using captopril together with spironolactone may increase the levels of potassium in your blood (hyperkalemia), especially if you are dehydrated or have kidney disease, diabetes, heart failure, or if you are an older adult. Hyperkalemia can cause symptoms such as weakness, confusion, numbness or tingling, and uneven heartbeats. If your doctor prescribes these medications together, you may need a dose adjustment or special tests to safely take both medications. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.

captopril WITH aliskiren
Using aliskiren together with captopril may increase potassium levels in the blood. High levels of potassium can develop into a condition known as hyperkalemia, which in severe cases can lead to kidney failure, muscle paralysis, irregular heart rhythm, and cardiac arrest. You may be more likely to develop hyperkalemia while using these medications if you are elderly, dehydrated, or have kidney disease, diabetes, or advanced heart failure. Regular or long-term use of nonsteroidal anti-inflammatory drugs such as ibuprofen or naproxen (Aleve) may also increase your risk. It is important that you maintain adequate fluid intake during treatment with these medications. Let your doctor know if you are diabetic or have kidney disease, as you may not be able to use these medications together. You should seek medical attention if you experience nausea, vomiting, weakness, confusion, tingling of the hands and feet, feelings of heaviness in the legs, a weak pulse, or a slow or irregular heartbeat, as these may be symptoms of hyperkalemia. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.


captopril WITH allopurinol
Talk to your doctor before using allopurinol together with captopril. Combining these medications may increase the risk of severe allergic reactions and infections. You should seek immediate medical attention if you develop shortness of breath; throat tightness; swelling of the face, lips, or tongue; itching; rash; fever; and/or muscle pain or weakness. Also let your doctor know if you notice signs of infection or experience fever, chills, sore throat, fatigue, body aches, or other flu-like symptoms. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.


captopril WITH amiloride
Using captopril together with aMILoride may increase the levels of potassium in your blood (hyperkalemia), especially if you are dehydrated or have kidney disease, diabetes, heart failure, or if you are an older adult. Hyperkalemia can cause symptoms such as weakness, confusion, numbness or tingling, and uneven heartbeats. If your doctor prescribes these medications together, you may need a dose adjustment or special tests to safely take both medications. It is important to tell your doctor about all other medications you use, including vitamins and herbs. Do not stop using any medications without first talking to your doctor.