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Lipcor 50

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LIPCOR 50

Keep out of reach of children.

Read all of this leaflet carefully before you start taking this medicine.

For prescription only.

QUALITATIVE AND QUANTITATIVE COMPOSITION:

Active ingredients:

Losartan potassium .................................... 50 mg

Excipients:

Lactose monohydrate, pregelatinized starch, sodium starch glycolate, aerosil, magnesium stearate, PVP K30, HPMC, PEG 6000, talc, titanium dioxide.

PHARMACEUTICAL FORM: Film coated tablet.

Product description: An oval white to off-white, film-coated tablet, plain on one side and a break line on the other, intact edges.

THERAPEUTIC INDICATIONS:

Treatment of hypertension in patients aged > 6 years.

Treatment of renal disease in adult patients with hypertension and type 2 diabetes mellitus with proteinuria ≥ 0.5 g/day.

Treatment of chronic heart failure in adult patients when treatment with Angiotensin-converting enzyme (ACE) inhibitors is not considered suitable due to incompatibility, especially cough, or contraindication.

Reduction in the risk of stroke in adult hypertensive patients with left ventricular hypertrophy documented by ECG.

POSOLOGY AND METHOD OF ADMINISTRATION:

Losartan tablets may be administered with or without food.

The usual adult starting dose is 50 mg once daily. The maximal antihypertensive effect is attained 3 - 6 weeks after initiation of therapy. Some patients may receive an additional benefit by increasing the dose to 100 mg once daily (in the morning).

Losartan may be administered with other antihypertensive agents, especially with diuretics (e.g. hydrochlorothiazide).

Hypertensive type II diabetic adult patients with proteinuria ≥ 0.5 g/day: The usual starting dose is 50 mg once daily. The dose may be increased to 100 mg once daily based on blood pressure response. Losartan may be administered with other antihypertensive agents (e.g. diuretics, calcium channel blockers, alpha- or beta-blockers, and centrally acting agents) as well as with insulin and other commonly used hypoglycemic agents (e.g. sulfonylureas, glitazones and glucosidase inhibitors).

Heart failure: The usual initial dose of losartan in patients with heart failure is 12.5 mg once daily. The dose should generally be titrated at weekly intervals (i.e. 12.5 mg daily, 25 mg daily, 50 mg daily, 100 mg daily, up to a maximum dose of 150 mg once daily) as tolerated by the patient.

Reduction in the risk of stroke in hypertensive patients with left ventricular hypertrophy documented by ECG.

The usual starting dose is 50 mg of losartan once daily. A low dose of hydrochlorothiazide should be added and/or the dose of losartan should be increased to 100 mg once daily based on blood pressure response.

Special populations:

Use in patients with intravascular volume depletion: A starting dose of 25 mg once daily should be considered.

Use in patients with renal impairment and haemodialysis patients: No initial dosage adjustment is necessary.

Use in patients with hepatic impairment: A lower dose should be considered for patients with a history of hepatic impairment. There is no therapeutic experience in patients with severe hepatic impairment. Therefore, losartan is contraindicated in patients with severe hepatic impairment.

Children aged 6 months to less than 6 years: no recommendation.

Children aged 6 years to 18 years:

- Patients >20 to <50 kg: For patients who can swallow tablets, the recommended dose is 25 mg once daily. (In exceptional cases the dose can be increased to a maximum of 50 mg once daily). Dosage should be adjusted according to blood pressure response.

In patients >50 kg, the usual dose is 50 mg once daily. In exceptional cases the dose can be adjusted to a maximum of 100 mg once daily. Doses above 1.4 mg/kg (or in excess of 100 mg) daily have not been studied in paediatric patients.

It is not recommended in children with glomerular filtration rate < 30 ml/min/1.73 m2.

Losartan is also not recommended in children with hepatic impairment.

Use in elderly: Although consideration should be given to initiating therapy with 25 mg in patients over 75 years of age, dosage adjustment is not usually necessary for the elderly.

Or as directed by the physician.

CONTRAINDICATIONS:

Hypersensitivity to any ingredients of the drug.

2nd and 3rd trimester of pregnancy.

Severe hepatic impairment.

The concomitant use of losartan with aliskiren-containing products is contraindicated in patients with diabetes mellitus or renal impairment (GFR < 60 ml/min/1.73 m2).

SPECIAL WARNINGS AND PRECAUTIONS FOR USE:

Hypersensitivity: Patients with a history of angiooedema (swelling of the face, lips, throat, and/or tongue) should be closely monitored.

Hypotension and electrolyte/fluid imbalance: after the first dose and after increasing of the dose, may occur in patients who are volume- and/or sodium-depleted by vigorous diuretic therapy, dietary salt restriction, diarrhoea or vomiting.

Electrolyte imbalances: Electrolyte imbalances are common in patients with renal impairment, with or without diabetes.

Hepatic impairment: A lower dose should be considered for patients with a history of hepatic impairment. There is no recommendation with losartan in patients with severe hepatic impairment.

Losartan may increase blood urea and serum creatinine in patients with unilateral or bilateral renal artery stenosis, patients with a solitary kidney. These patients should be closely monitored during the treatment.

There is no experience in patients with recent kidney transplantation.

Patients with aldosteronism generally will not respond to medicinal products acting through inhibition of the renin-angiotensin system. Therefore, the use of losartan is not recommended.

Excessive blood pressure decrease in patients with ischaemic cardiovascular and cerebrovascular disease could result in a myocardial infarction or stroke.

There is no sufficient therapeutic experience with losartan in patients with heart failure and concomitant severe renal impairment, in patients with severe heart failure (NYHA class IV) as well as in patients with heart failure and symptomatic life-threatening cardiac arrhythmias. Therefore, losartan should be used with caution in these patient groups. The combination of losartan with a beta-blocker should be used with caution.

As with other vasodilators, special caution is indicated in patients suffering from aortic or mitral stenosis, or obstructive hypertrophic cardiomyopathy.

This medicinal product contains lactose. Patients with rare hereditary problems of galactose intolerance, lactase deficiency or glucose-galactose malabsorption should not take this medicine.

USE IN PREGNANCY AND LACTATION:

Losartan is not recommended in the first trimester of pregnancy and it contraindicated in the second trimester and third trimester of pregnancy.

The drug is contraindicated for breastfeeding women.

EFFECTS ON ABILITY TO DRIVE AND USE MACHINES:

When driving vehicles or operating machines it must be borne in mind that dizziness or drowsiness may occasionally occur when taking antihypertensive therapy, in particular during initiation of treatment or when the dose is increased.

INTERACTIONS:

Other antihypertensive agents may increase the hypotensive action of losartan. Concomitant use with tricyclic antidepressants, antipsychotics, baclofen and amifostine may increase the risk of hypotension.

Concomitant use of potassium-sparing diuretics, potassium supplements or salt substitutes containing potassium may lead to increases in serum potassium.

No significant pharmacokinetic interactions have been found with hydrochlorothiazide and digoxin given by oral route or intravenous injection.

Co-administration of losartan and cimetidine leads to an increase of about 18% in AUC of losartan but did not affect the pharmacokinetics of its active metabolite.

Co-administration of losartan and phenobarbital leads to a reduction of about 20% in the AUC of losartan and that of its active metabolite.

Decreased plasma concentrations of losartan and its active metabolite observed when losartan is used concomitantly with rifampicin, aminoglutethimide, carbamazepine, nafcilin, nevirapine, phenytoin.

Losartan may enhance the effect of medicinal products including amifostine, antihypertensives, carvedilol, hypoglycemic drugs, lithium, potassium-sparing diuretics, rituximab.

Renal impairment has been reported when losartan is used concomitantly with nonsteroidal anti-inflammation agents (NSAIDs), including COX-2. Renal function should be monitored periodically.

UNDESIRABLE EFFECTS:

Adverse effects are mostly mild and disappear slowly with time.

Common, ADR > 1/100

Cardiac disorders: hypotension, chest pain.

Nervous system disorders: insomnia, dizziness, fatigue.

Endocrine - metabolic disorders: hyperkalemia, hypoglycaemia.

Gastrointestinal disorders: diarrhea, indigestion.

Blood disorders: mild decreases in hemoglobin and hematocrit.

Musculoskeletal disorders: back pain, leg pain, myalgia.

Renal disorders: decreased blood uric acid (use of high doses), urinary tract infections.

Respiratory disorders: cough (lesser when using ACE inhibitors), nasal congestion, sinusitis.

Uncommon, 1/1000 < ADR < 1/100

Cardiovascular disorders: orthostatic hypotension, chest pain, 2nd degree AV block, palpitations, sinus bradycardia, tachycardia, facial edema, blushing.

Nervous system disorders: anxiety, ataxia, confusion, depression, migraines, headache, sleep disturbances, fever, dizziness.

Skin disorders: alopecia, dermatitis, dry skin, erythema, photosensitivity, itching, urticaria, bruising, rash.

Endocrine - metabolic disorders: gout.

Gastrointestinal disorders: anorexia, constipation, flatulence, vomiting, loss of appetite, gastritis.

Genitourinary disorders: impotence, decreased sex, polyuria, nocturia.

Hepatic disorders: slight increases in liver function tests and bilirubin.

Musculoskeletal disorders: paraesthesia, tremor, bone pain, muscle weakness, joint edema, myalgia.

Eye disorders: blurred vision, conjunctivitis, decreased vision, burning eyes.

Ear disorders: Tinnitus.

Renal disorders: urinary tract infections, slight increases in creatinine or urea.

Respiratory disorders: dyspnea, bronchitis, epistaxis, rhinitis, respiratory congestion, discomfort in the throat.

Others: sweating.

Treatment of ADRs: 

The dosage should be reduced or discontinued when the adverse effects occur.

Inform your physician about any adverse effects occur during the treatment.

OVERDOSE:

Limited data are available with regard to overdose in humans. The most likely manifestation of overdose would be hypotension and tachycardia. Bradycardia could occur from parasympathetic (vagal) stimulation. If symptomatic hypotension should occur, supportive treatment should be instituted. Neither losartan nor the active metabolite can be removed by haemodialysis.

PHARMACODYNAMIC PROPERTIES

ATC code: C09CA01

Losartan is the first substance belonging to a group of new generation of antihypertensive agents, is angiotensin II receptor (type AT1) antagonist.

Losartan and its principal active metabolite block the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor found in many tissues (e.g., vascular smooth muscle, adrenal gland). Both losartan and its principal active metabolite do not exhibit any partial agonist activity at the AT1 receptor and have much greater affinity (about 1000-fold) for the AT1 receptor than for the AT2 receptor. Losartan is a reversible, competitive inhibitor of the AT1 receptor. The active metabolite is 10 to 40 times more potent by weight than losartan. Angiotensin II antagonists also have hemodynamic action as ACE inhibitors, but they appear less likely than ACE inhibitors to cause a common adverse effect - dry cough.

PHARMACOKINETIC PROPERTIES:

Following oral administration, losartan is well absorbed and undergoes substantial first-pass metabolism by cytochrome P450 enzymes; the bioavailability of losartan is approximately 33%. About 14% of an orally-administered dose of losartan is converted to the active metabolite that is responsible for most of the angiotensin II receptor antagonism. The half-life of losartan is about 2 hours and of the metabolite is about 6-9 hours. Mean peak concentrations of losartan and its active metabolite are reached in 1 hour and in 3-4 hours, respectively.

Both losartan and its active metabolite are highly bound to plasma proteins, primarily albumin, they do not cross the blood-brain barrier. Following oral administration in patients with mild to moderate cirrhosis, the AUC of losartan and its active metabolite were, respectively, 5 times and about 2 times those in normal subjects.

PRESENTATION: Box of 3 blisters x 10 tablets.    

SHELF-LIFE: 36 months from the manufacturing.

STORAGE CONDITIONS: Store in dry places, not exceeding 30oC, protect from light.

SPECIFICATIONS: Manufacturer’s.

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