Captopril is an ACE inhibitor. ACE stands for Angiotensin Converting Enzyme. Captopril is used to treat high blood pressure (hypertension), congestive heart failure, kidney problems caused by diabetes, and to improve survival after a heart attack.
Mechanism Of Action
The mechanism of action of Captopril has not yet been fully elucidated. Its beneficial effects in hypertension and heart failure appear to result primarily from suppression of the renin-angiotensinaldosterone system. However, there is no consistent correlation between renin levels and response to the drug. Renin, an enzyme synthesized by the kidneys, is released into the circulation where it acts on a plasma globulin substrate to produce angiotensin I, a relatively inactive decapeptide. Angiotensin I is then converted by angiotensin converting enzyme (ACE) to angiotensin II, a potent endogenous vasoconstrictor substance. Angiotensin II also stimulates aldosterone secretion from the adrenal cortex, thereby contributing to sodium and fluid retention.
Captopril prevents the conversion of angiotensin I to angiotensin II by inhibition of ACE, a peptidyldipeptide carboxy hydrolase. This inhibition has been demonstrated in both healthy human subjects and in animals by showing that the elevation of blood pressure caused by exogenously administered angiotensin I was attenuated or abolished by captopril. In animal studies, captopril did not alter the pressor responses to a number of other agents, including angiotensin II and norepinephrine, indicating specificity of action.
Related Article
- Amlodipine (Anti-Hypertensive Drug)
- Angiotensin Converting Enzyme (ACE) Inhibitors
- Contraindications of Beta Blockers [ Mnemonic ]
ACE is identical to ''bradykininase'', and Captopril may also interfere with the degradation of the vasodepressor peptide, bradykinin. Increased concentrations of bradykinin or prostaglandin E2 may also have a role in the therapeutic effect of Captopril.
Inhibition of ACE results in decreased plasma angiotensin II and increased plasma renin activity (PRA), the latter resulting from loss of negative feedback on renin release caused by reduction in angiotensin II. The reduction of angiotensin II leads to decreased aldosterone secretion, and, as a result, small increases in serum potassium may occur along with sodium and fluid loss.
The antihypertensive effects persist for a longer period of time than does demonstrable inhibition of circulating ACE. It is not known whether the ACE present in vascular endothelium is inhibited longer than the ACE in circulating blood.
Indication
1. Hypertension
2. Heart Failure
3. Left Ventricular Dysfunction After Myocardial Infarction
4. Diabetic Nephropathy
Side Effects
1. Cough
2. Flushing (warmth, redness, or tingly feeling)
3. Numbness, tingling, or burning pain in your hands or feet;
4. Loss of taste sensation
5. Mild skin itching or rash.
6. Stomach pain
7. Difficulty breathing
Contraindications
Captopril tablets are contraindicated in patients who are hypersensitive to this product or any other angiotensin-converting enzyme inhibitor (e.g., a patient who has experienced angioedema during therapy with any other ACE inhibitor).
1. Narrowing of the Aortic Heart Valve,
2. Renal Artery Stenosis,
3. Abnormally Low Blood Pressure,
4. Kidney Disease,
5. Cough,
6. Giant Hives,
7. Transplant of an Organ,
8. Pregnancy,
9. Brain Blood Flow Problem,
10. Low Amount of Sodium in the Blood,
11. High Amount of Potassium in the Blood,
12. Inherited Disorder of Continuing Episodes of Swelling,
13. Decreased Function of Bone Marrow,
14. Decreased Neutrophils a Type of White Blood Cell.
Reference
1. DRUGS.COM
www.drugs.com/captopril.html
2. RxList, The internet Drug index.
http://www.rxlist.com/capoten-drug/clinical-pharmacology.htm
3. DrugLib.com
http://www.druglib.com/druginfo/captopril/interactions_overdosage_contraindications/
4. WebMD
http://www.webmd.com/drugs/2/drug-964/captopril+oral/details/list-contraindications
5. Image from : www.worldmedicine.co.uk
Related Article
- Amlodipine (Anti-Hypertensive Drug)
- Angiotensin Converting Enzyme (ACE) Inhibitors
- Contraindications of Beta Blockers [ Mnemonic ]
Mechanism Of Action
The mechanism of action of Captopril has not yet been fully elucidated. Its beneficial effects in hypertension and heart failure appear to result primarily from suppression of the renin-angiotensinaldosterone system. However, there is no consistent correlation between renin levels and response to the drug. Renin, an enzyme synthesized by the kidneys, is released into the circulation where it acts on a plasma globulin substrate to produce angiotensin I, a relatively inactive decapeptide. Angiotensin I is then converted by angiotensin converting enzyme (ACE) to angiotensin II, a potent endogenous vasoconstrictor substance. Angiotensin II also stimulates aldosterone secretion from the adrenal cortex, thereby contributing to sodium and fluid retention.
Captopril prevents the conversion of angiotensin I to angiotensin II by inhibition of ACE, a peptidyldipeptide carboxy hydrolase. This inhibition has been demonstrated in both healthy human subjects and in animals by showing that the elevation of blood pressure caused by exogenously administered angiotensin I was attenuated or abolished by captopril. In animal studies, captopril did not alter the pressor responses to a number of other agents, including angiotensin II and norepinephrine, indicating specificity of action.
Related Article
- Amlodipine (Anti-Hypertensive Drug)
- Angiotensin Converting Enzyme (ACE) Inhibitors
- Contraindications of Beta Blockers [ Mnemonic ]
ACE is identical to ''bradykininase'', and Captopril may also interfere with the degradation of the vasodepressor peptide, bradykinin. Increased concentrations of bradykinin or prostaglandin E2 may also have a role in the therapeutic effect of Captopril.
Inhibition of ACE results in decreased plasma angiotensin II and increased plasma renin activity (PRA), the latter resulting from loss of negative feedback on renin release caused by reduction in angiotensin II. The reduction of angiotensin II leads to decreased aldosterone secretion, and, as a result, small increases in serum potassium may occur along with sodium and fluid loss.
The antihypertensive effects persist for a longer period of time than does demonstrable inhibition of circulating ACE. It is not known whether the ACE present in vascular endothelium is inhibited longer than the ACE in circulating blood.
Indication
1. Hypertension
2. Heart Failure
3. Left Ventricular Dysfunction After Myocardial Infarction
4. Diabetic Nephropathy
Side Effects
1. Cough
2. Flushing (warmth, redness, or tingly feeling)
3. Numbness, tingling, or burning pain in your hands or feet;
4. Loss of taste sensation
5. Mild skin itching or rash.
6. Stomach pain
7. Difficulty breathing
Contraindications
Captopril tablets are contraindicated in patients who are hypersensitive to this product or any other angiotensin-converting enzyme inhibitor (e.g., a patient who has experienced angioedema during therapy with any other ACE inhibitor).
1. Narrowing of the Aortic Heart Valve,
2. Renal Artery Stenosis,
3. Abnormally Low Blood Pressure,
4. Kidney Disease,
5. Cough,
6. Giant Hives,
7. Transplant of an Organ,
8. Pregnancy,
9. Brain Blood Flow Problem,
10. Low Amount of Sodium in the Blood,
11. High Amount of Potassium in the Blood,
12. Inherited Disorder of Continuing Episodes of Swelling,
13. Decreased Function of Bone Marrow,
14. Decreased Neutrophils a Type of White Blood Cell.
Reference
1. DRUGS.COM
www.drugs.com/captopril.html
2. RxList, The internet Drug index.
http://www.rxlist.com/capoten-drug/clinical-pharmacology.htm
3. DrugLib.com
http://www.druglib.com/druginfo/captopril/interactions_overdosage_contraindications/
4. WebMD
http://www.webmd.com/drugs/2/drug-964/captopril+oral/details/list-contraindications
5. Image from : www.worldmedicine.co.uk
Related Article
- Amlodipine (Anti-Hypertensive Drug)
- Angiotensin Converting Enzyme (ACE) Inhibitors
- Contraindications of Beta Blockers [ Mnemonic ]
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