LOTENSINE Tablets (Captopril)

Lotensine Pamphlet

LOTENSINE   Tablets
(Captopril)
Angiotensin Converting Enzyme Inhibitor ( A C E I).
Composition:
Each tablet contains:
Captopril 25 mg.
Poperties:
Captopril, the active principle of "LOTENSINE" is an
‘Angiotensin Converting Enzyme inhibitor, thus inhibits the conversion of Angiotisin 1” to the potent vasoconstrictor substance “Angiotensin II”. The reduction of Angiotensin II” aLso decreases aldosterone secretion, and as a result, small increases in serum potassium may occur along with sodium and fluid loss. Increased pros- taglandin E. or bradykiniri con- centrations may also play a role in the antihypertensive action of Captopril.
In hyperten1ve patients Captopril reduces peripheral arterial resistance and either no change or an increase in cardiac output. Captopril’s blood pressure reduction is often maximal 60 to 90 minutes after oral administration. The duration of action Is dose - dependent and may persist for 6 • 12 hours. Reduction in blood pressure is usually progressive and to achieve maximal therapeutic effects of a given dosage regimen several weeks of therapy may be required.
in patients with congestive heart !t Captopril decreases peripheral vascular resistance (afterload), pulmonary
capillary wedge pressure (preload), and pulmonary vascular resistance ; and so improves cardiac output and cx- cercise tolerance. These effects occur after the first dose and persist for duration of therapy.
After oral .administratjon Captopril is rapidly absorbed from gastrointestinal tract. The presence of food reduces absorption by 30 — 40%. Approximately 25 — 30% is bound to plasma proteins and in a 24 - hour period, over 95% of the absorbed dose is excret ed in the urine as unchanged

drug (40 • 50%) and the remain- der as metabolites.
Indications:
— For the treatment of hypertension. It may be used alone or in combination with other an- tihypertensive agents special- ly thiazide diuretics. The blood pressure lowering effects of “t..OTENSINE’and thiazides are additive.
— For the treatment of congeslive heart failure in patients who have not responded adequatly to, or cannot be con- trolled by, conventional diii- retic and digitalis therapy. Use in combination with diuretics and digitalis or with diuretics.
Side effects:
Caplopril is usually well tolcrated at doses below ISO mg. daily, and as assessed by well established psychometric tests, it does not compromise the pa. heft quality of life. Side effects tend to be dose — related and more frequent in patients with impaired renal function. The side ‘effects which have been observed include;
- Skin rash (usually maculopapular, rarely urticarial, and may be accompanied by pruritus, fever, and eosinophilia) has been infrequently ob’ served with the currently rec ommended therapeutic dos age (150 mg. daily or less), The rash is usually mild and disappears with eduction of dosage, treatment with anti- h1stamlnics, or discontinualion of therapy. in some cases remission may occur even if Captopril is continued.
.- Dry cough may occur.
— Transient hypotension may occur at the start of therapy. particularly in patients with congestive heart failure aid in sodium - or volume - depleted patients. This transient hypotension can be minimized by starting therapy with low doses.
- Dysgeusia may occur depend-

ing on renal status and dose. It is infrequently observed with the currently recommend- ed dosage. Taste impairment is reversible and usually self limited even with continued drug use. Weight loss may be associated with taste impair. ment.
— Proteinuria has occurred in less than I % of patients, most of them had evidence of prior renal disease
- Transient elevation of BUN and serum creatini may occur, specially in volume - depleted or renovascular hyper. tensive patients.
— Small increases in serum potassium concentration, spedaily in patients with renal impairment.
— Rarely, elevations of liver en- zymes occur, but no causal relation has been established.
— Neutropenia and agranulocytosis occur rarely in patients with normal renal function, but have been reported in pa. tients with renal failure or cal- lagen vascular disorders such as lupus erythematosus and scieroderma Neutropenla is also “dose - dependent”, rare- ly occurs at the recommended therapeutic dosage.
. Other side effects which have been rarely observed : abdominal pain, nausea vomiting, diziiness, headache, fatigue, insomnia, tachycardia, chest pain, and angloedema (reversible on discontinuance of Captopril therapy).
Contraindications:
- Hypersensitivity to A C E I s.
— Aortic stenosis or out flow tract obstruction.
- Pregnancy and lactation.
Warnings and precautions:
Risk - benefit should be con- sidered when one or more of the following conditions ecist:
Renal function irnpainnent: iii- creased risk of hyperkalemia, proteinuria, neutropenia, and agranulocytosis. Patients with impaired renal fuction may re

quire lower or less frequent doses and smaller increments in dose. Periodic monitoring of white blood cell count should be considered.
— Renal disease specially bilateral renal artery stenosis, may develop increases In BUN and serum creatinine after reduction of blood pressure with Captopril. Monitor renal function in such patients during first few weeks of therapy and dosage reduction or discontinuation of the diuretic or both may be required.
— Autoimmune diseases specia.lly systemic lupus erythematosus and scieroderma : in- creased risk of development of neutropenia or agranulocytosis. As with other angiotensin converting enzyme inhibitars, periodic monitoring of white blood cell counts in pa- tients with collagen vascular disease should be considered.
- Bone marrow depression.
- Treatment with immunosuppressives or drugs that cause leukopenia or agranuocytosis.
‘ - Cerebrovascular or coronary insufficiency : ischernia may
be aggravated as a result of reduced blood pressure.
- Hyperkalernia.
I Severe dietary salt restriction or dialysis.
— Surgery I anesthesia : in pa- tients undergoing major surgery or during anesthesia,
Captopnl may cause hypotension which can be correct- ed by volume expansion.
Use in pregnancy:
Contraindicated.
Use In nursing mothers:
Small amounts of Captopril are excreted in breast milk, therefore, breast - feeding should be dLsconftnued.
Main drug interactions:
- With diuretics : concurrent use with Captopnl may pro- duce additive hypotensive effects.
- With potassium containing preparations or potassium - sparing diuretics : hyperkalemia may occur.
With beta - adrenergic block-

ers : concurrent use produces an increase in the antihypertensive effrct but less than fully additive.
— With nonstcroidal anti - in- flammatory drugs specially indomethacin : concurrent us ol these agents may reduce the antihypertensive effect of Captopril.
— With nitroglycerin, other nitrates or other vasodilators data on use of other vasodilators in patients receiving Cap- topril for congestive heart fail- ure are not available
therefore, discontinue if possi. ble before starting Captopril. If resumed during Captopril therapy, administer such agents cautiously. and per- haps at lower dosage.
Drug I laboratory test inter- actions:
Captopril may cause false — positive urine test for acetone.
Dosage:
. Dosage must be individual- ized.
. Tablets arc to be ikcn 1 hour before meals.
— Adults:
I - Hypertension:
. If possible, discontinue previous antihypertensive drug regimen (including diuretics) I week before starting
“LOTENSINE’
Initial dose:
. Used alone in patients with normal renal function :J. tablet twice daily. 2
. Used in addition to a diuretic, in elderly patients, or in renal impairment :1 tab- let twice daily.
Usual maintenance dose:
I tablet twice daily. Maximum dose:
2 tablets twice daily (rarely
2 tablets 3 tImes daily in - vere hypertension).
a . Congestive heart
The initial dose ls’ -
tablet 2 or 3 times daily. given under close medical supervision; the usual maintenancedoseis ltablet2or3 times daily, and should not exceed 2 tablets 3 times dal NB.:

1 - The first dose of Captopril may cause a preciptious fall in blood pressure in patients with renal impairment or receiving diuretics and it is recommended that such patients should be given a test dose of + tablet under close medical supervision (preferably in a hospital) for one hour.
2 - The dose oI Captopril should be kept as low as possible in eldvrly patients and those with renal impairment.
Packing:
Boxes of 20 tablets (2 strips x
10 tablets).
Boxes ofl000 tablets(wOstrips c
10 tablets).
or(50 stripsx2O tablets).
Storage:
Store at room temperature.

Produced by

KAHIRA PHARM. & CHEM. IND. Co.
CAIRO - EGYPT