Captopril drug

Captopril drug was developed in 1975 by three researchers at the U.S. drug company Squibb (now Bristol-Myers Squibb): Miguel Ondetti, Bernard Rubin and David Cushman. Squibb filed for U.S. patent protection on the drug in February 1976 and U.S. Patent 4,046,889 was granted in September 1977.

Captopril
Systematic (IUPAC) name
(2S)-1-[(2S)-2-methyl-3-sulfanylpropanoyl]
pyrrolidine-2-carboxylic acid

Captopril drug is an angiotensin-converting enzyme (ACE) inhibitor. It works by decreasing a chemical that tightens blood vessels. This causes blood vessels to relax (dilate), which lowers blood pressure and decreases the workload on the heart. 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.

Do NOT use Captopril drug if:

    * you are allergic to any ingredient in Captopril
    * you are in the second or third trimester of pregnancy
    * you have had a severe allergic reaction (eg, rash; hives; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue) to any other ACE inhibitor (eg, enalapril)
    * you are currently taking dextran sulfate

If Captopril drug is used in patients with impaired renal function, white blood cell and differential counts should be evaluated prior to starting treatment and at approximately two-week intervals for about three months, then periodically.

In patients with collagen vascular disease or who are exposed to other drugs known to affect the white cells or immune response, particularly when there is impaired renal function, captopril should be used only after an assessment of benefit and risk, and then with caution.

All patients treated with captopril should be told to report any signs of infection (e.g., sore throat, fever). If infection is suspected, white cell counts should be performed without delay.

Use Captopril drug as directed by your doctor. Check the label on the medicine for exact dosing instructions.

    * Take Captopril 1 hour before meals, on an empty stomach.
    * Captopril works best if it is taken at the same time each day.
    * Continue to use Captopril even if you feel well. Do not miss any doses.
    * If you miss a dose of Captopril , take it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not take 2 doses at once.

The use of ACE inhibitors during the second and third trimesters of pregnancy has been associated with fetal and neonatal injury, including hypotension, neonatal skull hypoplasia, anuria, reversible or irreversible renal failure, and death. Oligohydramnios has also been reported, presumably resulting from decreased fetal renal function; oligohydramnios in this setting has been associated with fetal limb contractures, craniofacial deformation, and hypoplastic lung development. Prematurity, intrauterine growth retardation, and patent ductus arteriosus have also been reported, although it is not clear whether these occurrences were due to the ACE-inhibitor exposure.

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.

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.

Pregnancy: Female patients of childbearing age should be told about the consequences of second and third-trimester exposure to ACE inhibitors, and they should also be told that these consequences do not appear to have resulted from intrauterine ACE- inhibitor exposure that has been limited to the first trimester. These patients should be asked to report pregnancies to their physicians as soon as possible.

The adverse drug reaction (ADR) profile of Captopril drug is similar to other ACE inhibitors, with cough being the most common ADR (Rossi, 2006). However, captopril is also commonly associated with rash and taste disturbances (metallic or loss of taste), which are attributed to the unique sulfhydryl moiety (Atkinson & Robertson, 1979).

Captopril drug also has a relatively poor pharmacokinetic profile. The short half-life necessitates 2–3 times daily dosing, which may reduce patient compliance.