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MAMAZOL Letrozole 2.5mg Film-Coated Tablet 1's

RXDRUG-DRP-6572-1pc
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Description

Indications/Uses

Letrozole is indicated for the first line treatment of advanced/metastatic breast cancer (hormone receptor positive or receptor status unknown) in postmenopausal women.
 

Dosage/Direction for Use

The recommended dose of Letrozole is 2.5 mg once daily. Treatment with Letrozole should continue as long as tumor response is seen. The drug should be discontinued if tumor stops responding as judged by tumor progression. For elderly patients, no modification of the normal adult dosage regimen is necessary.
No dosage adjustment is required for patients with mild to moderate hepatic impairment or renal impairment.
Method of administration: Oral Route of Administration
 

Overdosage

There is no clinical trial experience of overdosage. There is no specific antidote to letrozole.
Since letrozole is not highly protein bound, dialysis may be helpful. Emesis may be induced if the patient is alert. In general, supportive care and frequent monitoring of vital signs is appropriate.
 

Administration

May be taken with or without food.
 

Contraindications

Letrozole is contraindicated in known or suspected hypersensitivity to letrozole, other aromatase inhibitors, or to any of their ingredients. It is contraindicated during pregnancy, lactation and in premenopausal women. It is also contraindicated in severe hepatic dysfunction.
 

Special Precautions

Hepatic impairment: In breast cancer patients with moderate hepatic dysfunction, no dosage adjustment is necessary, but caution is recommended since letrozole elimination depends mainly on intrinsic metabolic clearance.
Renal impairment: Renal impairment (calculated creatinine clearance: 20 to 50 ml/min) did not affect steady state plasma letrozole concentration at a dose of 2.5 mg or 5 mg. Hence, no dose adjustment is necessary for such renal function impairment. It is anticipated that letrozole could be removed from blood by dialysis since it is weakly bound to plasma proteins. The potential risks and benefits to such patients should be considered carefully before prescribing letrozole.
In some cases, fatigue and dizziness have been observed with the use of Letrozole. Patients should therefore, be advised that their physical and/or mental abilities required for operating machinery or driving a car may be impaired.
 

Use In Pregnancy & Lactation

Pregnancy Category X.
Oral administration of Letrozole in pregnant rats resulted in teratogenicity and maternal toxicity at 0.03 mg/kg. Embryotoxicity and fetotoxicity were seen at doses 0.003 mg/kg and there was an increase in the incidence of foetal malformation among the animals treated. However, there are no adequate and well-controlled studies of letrozole in pregnant women and its use in these patients is not recommended.
It is not known whether letrozole is excreted in human milk. Because many drugs are excreted in human milk, letrozole should not be administered to a nursing woman.
 

Adverse Reactions

The most frequent adverse effects are gastrointestinal disturbances including anorexia, nausea and vomiting, and diarrhea; asthenia; hot flushes; dizziness; drowsiness; headache; and rash.
Other reported effects include hair thinning, vaginal dryness or bleeding, myalgia, arthralgia, and bone fractures. Abnormalities in liver enzyme values, thromboembolism, and increases in total cholesterol. Very rare cases of erythema multiforme, Stevens-Johnson syndrome, and allergic reactions (including angioedema, urticaria, and anaphylaxis) have occurred.
Reduction in bone mineral density can occur during use of Letrozole. Patients with or at risk of osteoporosis should therefore have their bone density assessed at the start of therapy and at regular intervals thereafter.
 

Storage

Store at temperature not exceeding 30°C. Protect from light.
Shelf-life: 24 months.
 

Action

Pharmacology: Pharmacodynamics: Letrozole is a potent and highly specific nonsteroidal aromatase inhibitor. It inhibits the aromatase enzyme by competitively binding to the heme of the cytochrome P450 subunit of the enzyme, resulting in a reduction of estrogen biosynthesis in all tissues.
Letrozole exerts its antitumor effect by depriving estrogen-dependent breast cancer cells of their growth stimulus. In postmenopausal women, estrogens are derived mainly from the action of the aromatase enzyme, which converts adrenal androgens primarily androstenedione and testosterone to oestrone (E1) and oestradiol (E2). The suppression of estrogen biosynthesis in the peripheral tissues and the malignant tissues can be achieved by specifically inhibiting the aromatase enzyme.
In healthy postmenopausal women, single doses of 0.1, 0.5 and 2.5 mg letrozole suppress serum oestrone and oestradiol by 75-78% and 78% from baseline respectively. Maximum suppression is achieved in 48-78 hours.
In postmenopausal patients, with advanced breast cancer, daily doses of 0.1 to 5 mg suppress plasma concentration of oestradiol, oestrone and oestrone sulphate by 78-95% from baseline in all patients treated.
Letrozole had no effect on plasma androgen concentrations (androstenedione and testosterone) among healthy postmenopausal women after single doses of 0.1 to 0.5 mg and 2.5 mg indicating that the blockade of estrogen biosynthesis does not lead to accumulation of androgenic precursors. Impairment of adrenal steroidogenesis has not been observed.
Pharmacokinetics: Letrozole is rapidly and completely absorbed from the gastrointestinal tract (absolute bioavailability 99.9%). Food slightly decreases the rate of absorption, but the extent of absorption remains unchanged. The minor effect of the absorption rate is not considered to be of clinical relevance and therefore Letrozole may be taken after, with or before food. Plasma protein binding of Letrozole is approximately 60%, mainly to albumin (55%). The concentration of Letrozole in erythrocytes is about 80% of that in plasma.
Metabolic clearance to a pharmacologically inactive carbinol metabolite is the major elimination pathway of Letrozole but is relatively slow when compared to hepatic blood flow. The cytochrome P450 isoenzymes 3A4 and 2A6 were found to be capable of converting Letrozole to this metabolite in vitro but their individual contributions to Letrozole metabolism in vivo have not been established.
 

MedsGo Class

Cancer Hormone Therapy

Features

Brand
Mamazol
Full Details
Dosage Strength
2.5 mg
Drug Ingredients
  • Letrozole
Drug Packaging
Film-Coated Tablet 1's
Generic Name
Letrozole
Dosage Form
Film-Coated Tablet
Registration Number
DRP-6572
Drug Classification
Prescription Drug (RX)
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