Captopril
- Captopril
- No Brand Name
- Tablet
- 50mg
- Blister
- 100 Tablets
-
• Hypertension
Mechanism of Action
Angiotensin converting enzyme (ACE) inhibitors dilate arteries and veins by competitively inhibiting the conversion of angiotensin I to angiotensin II (a potent endogenous vasoconstrictor) and by inhibiting bradykinin metabolism, these actions result in preload and afterload reductions on the heart
ACE inhibitors also promote sodium and water excretion by inhibiting angiotensin-II induced aldosterone secretion, elevation in potassium may also be observed
ACE inhibitors also elicit renoprotective effects through vasodilation of renal arterioles
ACE inhibitors reduce cardiac and vascular remodeling associated with chronic hypertension, heart failure, and myocardial infarction
Pharmacokinetics
Bioavailability: 70-75%
Onset: 15-30 min
Duration: 8-12 hr
Excretion: mainly urine (95%)
Contraindications
• Hypersensitivity to ACE inhibitors
• Anuria
• History of ACEI-induced angioedema
• Hereditary or idiopathic angioedema
• Coadministration with neprilysin inhibitors (eg, Sacubitril)
• Bilateral renal artery stenosis
• Coadminister with Aliskiren in patients with diabetes mellitus or with renal impairment
Adverse Reactions
Hyperkalemia, Hypersensitivity, Skin rash, Dysgeusia, Hypotension, Pruritus, Cough, Chest pain, Palpitations, Proteinuria, Tachycardia
Major Drug Interactions
Aliskiren - Mavorixafor - Sacubitril/Valsartan
Warnings
• Discontinue as soon as possible when pregnancy detected, affects renin-angiotensin system causing oligohydramnios, which may result in fetal injury and/or death
Recommendations for Patient
• Avoid concomitant use with lithium
• Food decreases absorption
Pregnancy Considerations
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
Breastfeeding Considerations
Because of the low levels of captopril in breastmilk, amounts ingested by the infant are small and would not be expected to cause any adverse effects in breastfed infants.
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: Maybe acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Angiotensin converting enzyme (ACE) inhibitors dilate arteries and veins by competitively inhibiting the conversion of angiotensin I to angiotensin II (a potent endogenous vasoconstrictor) and by inhibiting bradykinin metabolism, these actions result in preload and afterload reductions on the heart
ACE inhibitors also promote sodium and water excretion by inhibiting angiotensin-II induced aldosterone secretion, elevation in potassium may also be observed
ACE inhibitors also elicit renoprotective effects through vasodilation of renal arterioles
ACE inhibitors reduce cardiac and vascular remodeling associated with chronic hypertension, heart failure, and myocardial infarction
Pharmacokinetics
Bioavailability: 70-75%
Onset: 15-30 min
Duration: 8-12 hr
Excretion: mainly urine (95%)
Contraindications
• Hypersensitivity to ACE inhibitors
• Anuria
• History of ACEI-induced angioedema
• Hereditary or idiopathic angioedema
• Coadministration with neprilysin inhibitors (eg, Sacubitril)
• Bilateral renal artery stenosis
• Coadminister with Aliskiren in patients with diabetes mellitus or with renal impairment
Adverse Reactions
Hyperkalemia, Hypersensitivity, Skin rash, Dysgeusia, Hypotension, Pruritus, Cough, Chest pain, Palpitations, Proteinuria, Tachycardia
Major Drug Interactions
Aliskiren - Mavorixafor - Sacubitril/Valsartan
Warnings
• Discontinue as soon as possible when pregnancy detected, affects renin-angiotensin system causing oligohydramnios, which may result in fetal injury and/or death
Recommendations for Patient
• Avoid concomitant use with lithium
• Food decreases absorption
Pregnancy Considerations
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
Breastfeeding Considerations
Because of the low levels of captopril in breastmilk, amounts ingested by the infant are small and would not be expected to cause any adverse effects in breastfed infants.
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: Maybe acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
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