Captopril

DEA Class; Rx

Common Brand Names; Capoten, Captoril

• ACE Inhibitors

Shortest acting, oral ACE inhibitor; contains a sulfhydryl group; side effects increase at higher doses; may be used for HTN, CHF, and various renal syndromes (e.g., diabetic nephropathy, proteinuria, scleroderma renal crisis).

Indicated for the treatment of hypertension

Hypersensitivity to ACE inhibitors

Anuria

History of ACEI-induced angioedema

Hereditary or idiopathic angioedema

Coadministration of neprilysin inhibitors (eg, sacubitril) with ACE inhibitors may increase angioedema risk; do not administer ACE inhibitors within 36 hr of switching to or from sacubitril/valsartan

Bilateral renal artery stenosis

Do not coadminister with aliskiren in patients with diabetes mellitus or with renal impairment (ie, GFR <60 mL/min/1.73 m²)

• Hyperkalemia (1-11%)
• Hypersensitivity rxns (4-7%)
• Skin rash (4-7%)
• Dysgeusia (2-4%)
• Hypotension (1-2.5%)
• Pruritus (2%)
• Cough (0.5-2%)
• Chest pain (1%)
• Palpitations (1%)
• Proteinuria (1%)
• Tachycardia (1%)
• Cardiac arrest
• Orthostatic hypotension
• Ataxia
• Confusion
• Depression
• Somnolence
• Angioedema
• Photosensitivity
• Neutropenia
• ARF if renal artery stenosis
• Renal impairment
• Impotence

Aortic stenosis/hypertrophic cardiomyopathy, hypotension, biliary cirrhosis or biliary obstruction, myelosuppression, electrolyte imbalance, hyperuricemia or gout, SLE, hepatic or renal impairment

Avoid concomitant use with lithium

Less effective in African-Americans

Excessive hypotension if concomitant diuretics or volume-depleted; start with 6.25 mg q8hr

Risk of hyperkalemia, especially with K+ sparing diuretics

Dual blockade of the renin angiotensin system with ARBs, ACE inhibitors, or aliskiren associated with increased risk for hypotension, hyperkalemia, and renal function changes (including acute renal failure) compared to monotherapy

Blood levels don’t correlate with BP response

Food decreases absorption

ACE inhibition also causes increased bradykinin levels which putatively mediates angioedema

Coadministration with mTOR inhibitors (eg, temsirolimus, everolimus, sirolimus) may increase risk for angioedema

Intestinal angioedema, that presented with abdominal pain, reported in patients treated with ACE inhibitors

Neutropenia (<1000/mm³ with myeloid hypoplasia reported with captopril; risk is dependent on clinical status of patient

Causes false positive urine acetone

Pregnancy Category: C; D in 2nd & 3rd trimesters

Discontinue as soon as pregnancy detected; during the second and third trimesters of pregnancy, drugs that act directly on the renin-angiotensin have been associated with fetal injury that includes hypotension, neonatal skull hypoplasia, anuria, reversible or irreversible renal failure, and death

Lactation: enters breast milk/not recommended (AAP states compatible with nursing)