Captopril
Captopril-Tedapharm
Antihypertensive
Vasodilator, Congestive heart failure. (USPDI)
Captopril inhibits ACE . ACE catalyzes the conversion of angiotensin I to the vasoconstrictor substance, angiotensin II.
Angiotensin II also stimulates aldosterone secretion by the adrenal cortex. Inhibition of ACE results in decreased plasma angiotensin II , which leads to decreased vasopressor activity
and to decreased aldosterone secretion. (PDR)
Pharmacokinetics properties
(Facts,USPDI)
Indications
Hypertension; Heart failure; Left ventricular dysfunction (LVD) post - MI ; Diabetic nephropathy. (Martindale-PDR-Facts)
Contraindications
Captopril is contraindicated in patients who are hypersensitivity to this product and in patients with a history of angioedema
related to previous treatment with an ACEI. (PDR)
Warnings and precautions
- The neutropenia has usually been detected within three months after captopril was started.
- Angioedema of face, extremities, lips, tongue, glottis and/or larynx has been reported in patient treated with captopril and other ACE inhibitors. Patient with a history of angioedema unrelated to ACE inhibitor therapy may be at increased risk of angioedema.
- Anaphylactoid reaction have been reported in a patients dialyzed with high-flux membranes and treated concomitantly with an ACE inhibitor.
- Excessive hypotension is rare in uncomplicated hypertensive patients treated with captopril alone. caution should be observed when intiating therapy.
- Periodic monitoring of white blood cell counts in patients with collagen vascular disease and renal disease should be considerd.
- Captopril and other ACE inhibitor’s have been associated with a syndrome that start with cholestatic jundice and progresses
to fulminant hepatic necrosis, and (some times) death.
- Total urinary proteins greater than 19 per day were seen in
about 0.7 percent of patient receiving captopril.(PDR)
Pregnancy
Category C (first trimester) and D (second and third trimesters)
Captopril and other ACE inhibitors can cause fetal and neonatal morbidity and death when administered to pregnant women.
( PDR) Breast - feeding
It have been detected in human breast milk adecision should be made whether to discontinue nursing or captopril taking
into account the importance of the drug to the mother. ( PDR)
Drug Interactions
- Excessive hypotension may occure when captopril are used with diuretics; other hypotensive agents; alcohol; phenothiazines; interleukin-3 and general anaesthesia.
- An additive hyperkalaemia effect is possible in patients receiving captopril with potassium-sparing diuretics, potassium supplements and other drugs that can cause hyperkalaemia, blood from blood bank, low-salt milk, ciclosporin and drug like epoetins. Potassium-sparing agents should generally not
be used in patients with HF receiving captopril.
- Lithium toxicity has been reported in patients taking captopril.
- Indomethacin and other NSAIDs including ASA may reduce the antihypertensive effect of captopril.
- No significant pharmacokinetic interaction occured when
captopril and allopurinol, loop diuretics and digoxin.
- Agents affecting sympathetic activity e.g ganglionic blockers, or adrenergic neuron blockers should be used with caution.
- Nitroglycerin and other nitrates or vasadilators should, if
possible, be discountinued before starting captopril.
- The nitritoid reaction (flushing, nausea, dizziness, hypotension) occured soon after commencing treatment with gold salts and an ACEI.
- Coadministration of captopril with azathioprine don’t recommended. (Martindale-USPDI-PDR-Facts)
Adverse reactions
Taste disturbances; hypotension; orthostatic effect; asthenia; dizziness; fatigue; headache; malaise; insomnia; nausea; vomiting; diarrhea; anorexia; dry mouth; constipation; dyspepsia; oliguria; renal failures polyuria; urinary frequency; gyneocomastia; myocardial infraction; CHF; raynaud’s syndrome; stroke; tachycardia; bradycardia; palpitation; chest pain; syncope; angina pectoris; cough; rhinitis; bronchospasm; dyspnea; eosinophilic pneumonitis; angioedema; skin rashes; erythema multiforme; flushing; pruritus; pemphigoid-like lesion; alopecia; photosensivity; neutropenia; agranulocytosis; thrombocytopenia; anemia; pancytopenia; abdominal pain; pancreatitis; hepatitis; jaundice; paraesthesia; confusion; somnolence; ataxia; nervousness; impotence; proteinuria; anaphylactoid reaction; blurred vision; myalgia; myasthenia;
symptomatic hyponatremia. (Martindale-USPDI-PDR-Facts)
Overdosage
The most likely manifestation of overdosage would be hypotension for which the usual treatment would be IV infusion of normal saline solution. (PDR)
Dosage and Administration
For congestive heart failure:
Adults - 25 to 100 mg two or three times a day.
Children - Dose must be determined by your doctor.
For high blood pressure:
Adults - 25 to 50 mg two or three times a day.
Children - Dose must be determined by your doctor.
For kidney problems related to diabetes:
Adults - 25 mg three times a day.
For treatment after a heart attack:
Adults - 12.5 to 50 mg three times aday. (USPDI)
Because captopril is excreted primarily by the kidneys, excretion rates are reduced in patients with impaired renal function. (PDR)
Storage
Store below 30 and away from heat,moisture&direct light. (USPDI)Supplied
Captopril tablets are available as 25, 50 mg Captopril, round, white and scored tablets. There are blisters of 10 10 in a box of 100’s.
Reference