Captopril

One of the homochiral starting materials (45) for the acetylcholinesterase (ACE) inhibitor captopril [62571 -86-2] (47) is produced by a Hpase enzyme-catalyzed resolution of racemic 3-methyl-4-acetylthiobutyric acid (44) and L-proline (46) (65). 

Folic acid deficiency Hyperthermia Phenylketonuria Rheumatic disease Virilizing tumors Drugs and chemicals Androgenic chemicals Angiotensin-converting enzyme inhibitors Captopril, enalapril Antibiotics... 

Captopril 3, 128 Caramiphen 1, 90 Carbacephal othin 1, 420 Carbadox 390 Carbamazepine 403 Carbantel 57 Carbaprost 1 Carbazeran 195 Carbenicillin l, 414 2, 437 Carbetidine 1, 90 Carbidopa 2 119 Carbimazole 1, 240... 

The structural relationship of pivopril to the commercially important analogues captopril (51) and enalaprilat (52) is readily apparent. 

Finally,Captopril is produced. Thethioester (0.85g) isdissolved in5.5N methanolicammonia and the solution is kept at room temperature for 2 hours. The solvent is removed in vacuo and the residue Is dissolved in water, applied to an ion exchange column on the H cycle (Dowex 50, analytical grade) and eluted with water. The fractions that give positive thiol reaction are pooled and freeze dried. The residue Is crystallized from ethyl acetate-hexane, yield 0.3 g. The 1 -(3-mercapto-2-D-methylpropanoyl)-L-proline has a melting point of 103°C to 104°C. 

Metyrapone Acetylsalicylic acid Caraspirin calcium Acetylsalicylic acid chloride Benoryiate Phenprocoumon N-Acetylsulfanilyl chloride Sulfacytine Sulfamethoxazaole 3-Acetylthiomethyl propanoic acid Captopril... 

More than 15 ACE inhibitors are presently available. They belong to three different chemical classes sul-fhydryl compounds such as captopril, carboxyl compounds such as enalapril, and phopshorus compounds... 

Most ACE inhibitors are prodrugs, with the exceptions of captopril, lisinopril, and ceranapril. Prodrugs exert improved oral bioavailability, but need to be converted to active compounds in the liver, kidney, and/or intestinal tract. In effect, converting enzyme inhibitors have quite different kinetic profiles with regard to half time, onset and duration of action, or tissue penetration. 

Angiotensm-converting enzyme (ACE) inhibitors— for example, captopril (Capoten), enalapril (Vasotec), and lismopril (Prinivil)... 

ADMINISTERING ACE INHIBITORS. The nurse administers captopril and moexipril 1 hour before or 2 hours after meals to enhance absorption. Some patients taking an ACE inhibitor experience a dry cough that does not subside until the drug therapy is discontinued. This reaction may need to be tolerated. If the cough becomes too bothersome, the primary care provider may discontinue use of the drug. 

Discuss important preadministration assessments that should be performed on a patient prescribed captopril for hypertendon. 

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