AIs

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ARIMIDEX
1MG/TAB * 28TAB

Pharmacology
Anastrozole is a potent and selective nonsteroidal aromatase inhibitor. By inhibiting aromatase, the conversion of androstenedione to estrone, and testosterone to estradiol, is prevented, thereby decreasing tumor mass or delaying progression in patients with tumors responsive to hormones. Anastrozole causes an 85% decrease in estrone sulfate levels.

Absorption
Well absorbed; extent of absorption not affected by food.

Metabolism
Extensively hepatic (~85%) via N-dealkylation, hydroxylation, and glucuronidation; primary metabolite (triazole) inactive.

Time to Peak
Plasma: ~2 hours without food; 5 hours with food.

Half-Life Elimination
~50 hours.

Detection Time
~14 days.


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$50.00
AROMASIN

25MG/TAB * 30TAB

Pharmacology
Exemestane is an irreversible, steroidal aromatase inactivator. It is structurally related to androstenedione, and is converted to an intermediate that irreversibly blocks the active site of the aromatase enzyme, leading to inactivation ("suicide inhibition") and thus preventing conversion of androgens to estrogens in peripheral tissues. Significantly lowers circulating estrogens in postmenopausal breast cancers where growth is estrogen-dependent.


Absorption
Rapid and moderate (~42%) following oral administration; AUC and Cmax increased by 59% and 39%, respectively, following a high-fat breakfast (compared to fasted state).


Metabolism
Extensively hepatic; oxidation (CYP3A4) of methylene group, reduction of 17-keto group with formation of many secondary metabolites; metabolites are inactive.


Time to Peak
1.2 hours.


Half-Life Elimination
~24 hours.


Detection Time
~14 days.

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$60.00
EXEMESTANE

25MG/TAB * 30TAB



Pharmacology
Exemestane is an irreversible, steroidal aromatase inactivator. It is structurally related to androstenedione, and is converted to an intermediate that irreversibly blocks the active site of the aromatase enzyme, leading to inactivation ("suicide inhibition") and thus preventing conversion of androgens to estrogens in peripheral tissues. Significantly lowers circulating estrogens in postmenopausal breast cancers where growth is estrogen-dependent.


Absorption
Rapid and moderate (~42%) following oral administration; AUC and Cmax increased by 59% and 39%, respectively, following a high-fat breakfast (compared to fasted state).


Metabolism
Extensively hepatic; oxidation (CYP3A4) of methylene group, reduction of 17-keto group with formation of many secondary metabolites; metabolites are inactive.


Time to Peak
1.2 hours.


Half-Life Elimination
~24 hours.


Detection Time
~14 days.


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$50.00
FEMARA
2,5MG/TAB * 30TAB


Pharmacology
Letrozole is a nonsteroidal competitive inhibitor of the aromatase enzyme system which binds to the heme group of aromatase, a cytochrome P450 enzyme which catalyzes conversion of androgens to estrogens (specifically, androstenedione to estrone and testosterone to estradiol). This leads to inhibition of the enzyme and a significant reduction in plasma estrogen (estrone, estradiol and estrone sulfate) levels. Does not affect synthesis of adrenal or thyroid hormones, aldosterone, or androgens.

Absorption
Rapid and well absorbed; not affected by food.

Metabolism
Hepatic via CYP3A4 and 2A6 to an inactive carbinol metabolite.

Time to Peak
Steady state, plasma: 2 to 6 weeks; steady state serum concentrations are 1.5 to 2 times higher than single-dose values.

Half-Life Elimination
Terminal: ~2 days.

Detection Time
~14 days.


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$70.00
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