imerman2002
New member
Any advice on taking Arimidex on my 10 week 400 mg week test cyp cycle. Someone told me to take 0.5 mg twice a week just incase but I dont want to f..up anything......Thanks
arimidex
- Thread starter imerman2002
- Start date
mailboxkillR
New member
a little late in the cycle now. post your cycle and I'll get you the info on arimidex for you.
mailboxkillR
New member
Anastrozle Common names= Arimidex/liquidex/ldex/ect
ARIMIDEX® (anastrozole) tablets for oral administration contain 1 mg of anastrozole, a non-steroidal aromatase inhibitor. It is chemically described as 1,3-Benzenediacetonitrile, a, a, a', a'-tetramethyl-5-(1H-1,2,4-triazol-1-ylmethyl). Its molecular formula is C17H19N5
Anastrozole is an off-white powder with a molecular weight of 293.4. Anastrozole has moderate aqueous solubility (0.5 mg/mL at 25°C); solubility is independent of pH in the physiological range. Anastrozole is freely soluble in methanol, acetone, ethanol, and tetrahydrofuran, and very soluble in acetonitrile.
Each tablet contains as inactive ingredients: lactose, magnesium stearate, hydroxypropylmethylcellulose, polyethylene glycol, povidone, sodium starch glycolate, and titanium dioxide.
CLINICAL PHARMACOLOGY
Mechanism of Action
Many breast cancers have estrogen receptors and growth of these tumors can be stimulated by estrogens. In post-menopausal women, the principal source of circulating estrogen (primarily estradiol) is conversion of adrenally-generated androstenedione to estrone by aromatase in peripheral tissues, such as adipose tissue, with further conversion of estrone to estradiol. Many breast cancers also contain aromatase; the importance of tumor-generated estrogens is uncertain.
Treatment of breast cancer has included efforts to decrease estrogen levels by ovariectomy premenopausally and by use of anti-estrogens and progestational agents both pre- and post-menopausally, and these interventions lead to decreased tumor mass or delayed progression of tumor growth in some women.
Anastrozole is a potent and selective non-steroidal aromatase inhibitor. It significantly lowers serum estradiol concentrations and has no detectable effect on formation of adrenal corticosteroids or aldosterone.
Pharmacokinetics
Inhibition of aromatase activity is primarily due to anastrozole, the parent drug. Studies with radiolabeled drug have demonstrated that orally administered anastrozole is well absorbed into the systemic circulation with 83 to 85% of the radiolabel recovered in urine and feces. Food does not affect the extent of absorption. Elimination of anastrozole is primarily via hepatic metabolism (approximately 85%) and to a lesser extent, renal excretion (approximately 11%), and anastrozole has a mean terminal elimination half-life of approximately 50 hours in post-menopausal women. The major circulating metabolite of anastrozole, triazole, lacks pharmacologic activity. The pharmacokinetic parameters are similar in patients and in healthy post-menopausal volunteers. The pharmacokinetics of anastrozole are linear over the dose range of 1 to 20 mg and do not change with repeated dosing. Consistent with the approximately 2-day terminal elimination half-life, plasma concentrations approach steady-state levels at about 7 days of once daily dosing, and steady-state levels are approximately three- to four-fold higher than levels observed after a single dose of ARIMIDEX. Anastrozole is 40% bound to plasma proteins in the therapeutic range.
Metabolism and Excretion: Studies in post-menopausal women demonstrated that anastrozole is extensively metabolized with about 10% of the dose excreted in the urine as unchanged drug within 72 hours of dosing, and the remainder (about 60% of the dose) excreted in urine as metabolites. Metabolism of anastrozole occurs by N-dealkylation, hydroxylation, and glucuronidation. Three metabolites of anastrozole have been identified in human plasma and urine. The known metabolites are triazole, a glucuronide conjugate of hydroxy-anastrozole, and a glucuronide of anastrozole itself. Several minor (less than 5% of the radioactive dose) metabolites have not been identified.
Because renal elimination is not a significant pathway of elimination, total body clearance of anastrozole is unchanged even in severe (creatinine clearance less than 30 mL/min/1.73 m2) renal impairment; dosing adjustment in patients with renal dysfunction is not necessary (see Special Populations and DOSAGE AND ADMINISTRATION sections). Dosage adjustment is also unnecessary in patients with stable hepatic cirrhosis (see Special Populations and DOSAGE AND ADMINISTRATION sections).
Special Populations
Geriatric: Anastrozole pharmacokinetics have been investigated in post-menopausal female volunteers and patients with breast cancer. No age related effects were seen over the range <50 to >80 years.
Race: Anastrozole pharmacokinetic differences due to race have not been studied.
Renal Insufficiency: Anastrozole pharmacokinetics have been investigated in subjects with renal insufficiency. Anastrozole renal clearance decreased proportionally with creatinine clearance and was approximately 50% lower in volunteers with severe renal impairment (creatinine clearance less than 30 mL/min/1.73 m2) compared to controls. Since only about 10% of anastrozole is excreted unchanged in the urine, the reduction in renal clearance did not influence the total body clearance (see DOSAGE AND ADMINISTRATION).
Hepatic Insufficiency: Hepatic metabolism accounts for approximately 85% of anastrozole elimination. Anastrozole pharmacokinetics have been investigated in subjects with hepatic cirrhosis related to alcohol abuse. The apparent oral clearance (CL/F) of anastrozole was approximately 30% lower in subjects with stable hepatic cirrhosis than in control subjects with normal liver function. However, plasma anastrozole concentrations in the subjects with hepatic cirrhosis were within the range of concentrations seen in normal subjects across all clinical trials (see DOSAGE AND ADMINISTRATION), so that no dosage adjustment is needed.
Drug-Drug Interactions: Anastrozole inhibited reactions catalyzed by cytochrome P450 1A2, 2C8/9, and 3A4 in vitro with Ki values, which were approximately 30 times higher than the mean steady-state Cmax values observed following a 1-mg daily dose. Anastrozole had no inhibitory effect on reactions catalyzed by cytochrome P450 2A6 or 2D6 in vitro. Administration of a single 30 mg/kg or multiple 10 mg/kg doses of anastrozole to subjects had no effect on the clearance of antipyrine or urinary recovery of antipyrine metabolites. Based on these in vitro and in vivo results, it is unlikely that co-administration of ARIMIDEX 1 mg with other drugs will result in clinically significant inhibition of cytochrome P450 mediated metabolism.
Pharmacodynamics
Effect on Estradiol: Mean serum concentrations of estradiol were evaluated in multiple daily dosing trials with 0.5, 1, 3, 5, and 10 mg of ARIMIDEX in post-menopausal women with advanced breast cancer. Clinically significant suppression of serum estradiol was seen with all doses. Doses of 1 mg and higher resulted in suppression of mean serum concentrations of estradiol to the lower limit of detection (3.7 pmol/L). The recommended daily dose, ARIMIDEX 1 mg, reduced estradiol by approximately 70% within 24 hours and by approximately 80% after 14 days of daily dosing. Suppression of serum estradiol was maintained for up to 6 days after cessation of daily dosing with ARIMIDEX 1 mg.
Effect on Corticosteroids: In multiple daily dosing trials with 3, 5, and 10 mg, the selectivity of anastrozole was assessed by examining effects on corticosteroid synthesis. For all doses, anastrozole did not affect cortisol or aldosterone secretion at baseline or in response to ACTH. No glucocorticoid or mineralocorticoid replacement therapy is necessary with anastrozole.
Other Endocrine Effects: In multiple daily dosing trials with 5 and 10 mg, thyroid stimulating hormone (TSH) was measured; there was no increase in TSH during the administration of ARIMIDEX. ARIMIDEX does not possess direct progestogenic, androgenic, or estrogenic activity in animals, but does perturb the circulating levels of progesterone, androgens, and estrogens.
ARIMIDEX® (anastrozole) tablets for oral administration contain 1 mg of anastrozole, a non-steroidal aromatase inhibitor. It is chemically described as 1,3-Benzenediacetonitrile, a, a, a', a'-tetramethyl-5-(1H-1,2,4-triazol-1-ylmethyl). Its molecular formula is C17H19N5
Anastrozole is an off-white powder with a molecular weight of 293.4. Anastrozole has moderate aqueous solubility (0.5 mg/mL at 25°C); solubility is independent of pH in the physiological range. Anastrozole is freely soluble in methanol, acetone, ethanol, and tetrahydrofuran, and very soluble in acetonitrile.
Each tablet contains as inactive ingredients: lactose, magnesium stearate, hydroxypropylmethylcellulose, polyethylene glycol, povidone, sodium starch glycolate, and titanium dioxide.
CLINICAL PHARMACOLOGY
Mechanism of Action
Many breast cancers have estrogen receptors and growth of these tumors can be stimulated by estrogens. In post-menopausal women, the principal source of circulating estrogen (primarily estradiol) is conversion of adrenally-generated androstenedione to estrone by aromatase in peripheral tissues, such as adipose tissue, with further conversion of estrone to estradiol. Many breast cancers also contain aromatase; the importance of tumor-generated estrogens is uncertain.
Treatment of breast cancer has included efforts to decrease estrogen levels by ovariectomy premenopausally and by use of anti-estrogens and progestational agents both pre- and post-menopausally, and these interventions lead to decreased tumor mass or delayed progression of tumor growth in some women.
Anastrozole is a potent and selective non-steroidal aromatase inhibitor. It significantly lowers serum estradiol concentrations and has no detectable effect on formation of adrenal corticosteroids or aldosterone.
Pharmacokinetics
Inhibition of aromatase activity is primarily due to anastrozole, the parent drug. Studies with radiolabeled drug have demonstrated that orally administered anastrozole is well absorbed into the systemic circulation with 83 to 85% of the radiolabel recovered in urine and feces. Food does not affect the extent of absorption. Elimination of anastrozole is primarily via hepatic metabolism (approximately 85%) and to a lesser extent, renal excretion (approximately 11%), and anastrozole has a mean terminal elimination half-life of approximately 50 hours in post-menopausal women. The major circulating metabolite of anastrozole, triazole, lacks pharmacologic activity. The pharmacokinetic parameters are similar in patients and in healthy post-menopausal volunteers. The pharmacokinetics of anastrozole are linear over the dose range of 1 to 20 mg and do not change with repeated dosing. Consistent with the approximately 2-day terminal elimination half-life, plasma concentrations approach steady-state levels at about 7 days of once daily dosing, and steady-state levels are approximately three- to four-fold higher than levels observed after a single dose of ARIMIDEX. Anastrozole is 40% bound to plasma proteins in the therapeutic range.
Metabolism and Excretion: Studies in post-menopausal women demonstrated that anastrozole is extensively metabolized with about 10% of the dose excreted in the urine as unchanged drug within 72 hours of dosing, and the remainder (about 60% of the dose) excreted in urine as metabolites. Metabolism of anastrozole occurs by N-dealkylation, hydroxylation, and glucuronidation. Three metabolites of anastrozole have been identified in human plasma and urine. The known metabolites are triazole, a glucuronide conjugate of hydroxy-anastrozole, and a glucuronide of anastrozole itself. Several minor (less than 5% of the radioactive dose) metabolites have not been identified.
Because renal elimination is not a significant pathway of elimination, total body clearance of anastrozole is unchanged even in severe (creatinine clearance less than 30 mL/min/1.73 m2) renal impairment; dosing adjustment in patients with renal dysfunction is not necessary (see Special Populations and DOSAGE AND ADMINISTRATION sections). Dosage adjustment is also unnecessary in patients with stable hepatic cirrhosis (see Special Populations and DOSAGE AND ADMINISTRATION sections).
Special Populations
Geriatric: Anastrozole pharmacokinetics have been investigated in post-menopausal female volunteers and patients with breast cancer. No age related effects were seen over the range <50 to >80 years.
Race: Anastrozole pharmacokinetic differences due to race have not been studied.
Renal Insufficiency: Anastrozole pharmacokinetics have been investigated in subjects with renal insufficiency. Anastrozole renal clearance decreased proportionally with creatinine clearance and was approximately 50% lower in volunteers with severe renal impairment (creatinine clearance less than 30 mL/min/1.73 m2) compared to controls. Since only about 10% of anastrozole is excreted unchanged in the urine, the reduction in renal clearance did not influence the total body clearance (see DOSAGE AND ADMINISTRATION).
Hepatic Insufficiency: Hepatic metabolism accounts for approximately 85% of anastrozole elimination. Anastrozole pharmacokinetics have been investigated in subjects with hepatic cirrhosis related to alcohol abuse. The apparent oral clearance (CL/F) of anastrozole was approximately 30% lower in subjects with stable hepatic cirrhosis than in control subjects with normal liver function. However, plasma anastrozole concentrations in the subjects with hepatic cirrhosis were within the range of concentrations seen in normal subjects across all clinical trials (see DOSAGE AND ADMINISTRATION), so that no dosage adjustment is needed.
Drug-Drug Interactions: Anastrozole inhibited reactions catalyzed by cytochrome P450 1A2, 2C8/9, and 3A4 in vitro with Ki values, which were approximately 30 times higher than the mean steady-state Cmax values observed following a 1-mg daily dose. Anastrozole had no inhibitory effect on reactions catalyzed by cytochrome P450 2A6 or 2D6 in vitro. Administration of a single 30 mg/kg or multiple 10 mg/kg doses of anastrozole to subjects had no effect on the clearance of antipyrine or urinary recovery of antipyrine metabolites. Based on these in vitro and in vivo results, it is unlikely that co-administration of ARIMIDEX 1 mg with other drugs will result in clinically significant inhibition of cytochrome P450 mediated metabolism.
Pharmacodynamics
Effect on Estradiol: Mean serum concentrations of estradiol were evaluated in multiple daily dosing trials with 0.5, 1, 3, 5, and 10 mg of ARIMIDEX in post-menopausal women with advanced breast cancer. Clinically significant suppression of serum estradiol was seen with all doses. Doses of 1 mg and higher resulted in suppression of mean serum concentrations of estradiol to the lower limit of detection (3.7 pmol/L). The recommended daily dose, ARIMIDEX 1 mg, reduced estradiol by approximately 70% within 24 hours and by approximately 80% after 14 days of daily dosing. Suppression of serum estradiol was maintained for up to 6 days after cessation of daily dosing with ARIMIDEX 1 mg.
Effect on Corticosteroids: In multiple daily dosing trials with 3, 5, and 10 mg, the selectivity of anastrozole was assessed by examining effects on corticosteroid synthesis. For all doses, anastrozole did not affect cortisol or aldosterone secretion at baseline or in response to ACTH. No glucocorticoid or mineralocorticoid replacement therapy is necessary with anastrozole.
Other Endocrine Effects: In multiple daily dosing trials with 5 and 10 mg, thyroid stimulating hormone (TSH) was measured; there was no increase in TSH during the administration of ARIMIDEX. ARIMIDEX does not possess direct progestogenic, androgenic, or estrogenic activity in animals, but does perturb the circulating levels of progesterone, androgens, and estrogens.
mailboxkillR
New member
and for your other anti e's and research products questions compliment of my hard work here you go.
http://board1.mantisforums.com/upload/showthread.php?threadid=21526
http://board1.mantisforums.com/upload/showthread.php?threadid=21526
imerman2002
New member
Thanks mailboxkillR , My cycle (first) is Test cyp. 400 mg week for 10 weeks. I just took my 4th shot today.
mailboxkillR
New member
.25mgs /ed should be sufficent. You are shooting 2x/week@200mgs right. BTW welcome to the board.
BLEED GREEN
New member
Welcome to the board and killer already let you know the correct daily dosage
imerman2002
New member
Registered: Oct 2001
Status: Online
Location:
Posts: 1445
quote:
--------------------------------------------------------------------------------
Originally posted by mailboxkillR
.25mgs /ed should be sufficent. You are shooting 2x/week@200mgs right. BTW welcome to the board.
--------------------------------------------------------------------------------
At least double it. I'm not talking about gyno prevention here. To me it's keeping estrogen levels low- period!
__________________
Wont to much anti-e's mess up my gains due to to little estrogen??
Status: Online
Location:
Posts: 1445
quote:
--------------------------------------------------------------------------------
Originally posted by mailboxkillR
.25mgs /ed should be sufficent. You are shooting 2x/week@200mgs right. BTW welcome to the board.
--------------------------------------------------------------------------------
At least double it. I'm not talking about gyno prevention here. To me it's keeping estrogen levels low- period!
__________________
Wont to much anti-e's mess up my gains due to to little estrogen??
V
viper10139
Guest
welcome to the board...mailbox is correct!!
Junkyard Dog
New member
Use Liquid_dex from [No promoting. ChemE] and you will save a boatload of money.
I use 0.5mg ED, it is cheap.
I HATE water retention and I am prone to gyno so I also take Letro/Nolv/Prov with my Dex
All liquid and all very inexpensive.
I am in week 3 of Sust/Deca/IGF and I have almost no water retention.
I use 0.5mg ED, it is cheap.
I HATE water retention and I am prone to gyno so I also take Letro/Nolv/Prov with my Dex
All liquid and all very inexpensive.I am in week 3 of Sust/Deca/IGF and I have almost no water retention.
BLEED GREEN
New member
:thumbsup:Chemical Evolution said:
Junkyard Dog
New member
Thanks, I see they got there site updated. I will try out their products next. I am about to run out (2 weeks). I wonder if they offer volume discounts.Chemical Evolution said:
Junkyard Dog
New member
I do not see Dex, Nolva, or Clomid.
Junkyard Dog
New member
I must be brain dead today! The last I looked at the site they only had equipment up there. Sorry about that. I see they are making great progress on their site!Chemical Evolution said:
Let's Compare apples with apples and see which is the better deal. I will buy wherever my money can get me the most product.
I am not trying to be a dickhead, honestly, I only have so much money to spend and I need to make it stretch as far as possible. If you order more than 3 bottles from LiqRes they will give you 30% off your order (they did it for me, I asked them).
Does CySol offer volume doscounts? I would be more than willing to support our advertisers. But the prices have to be at least comparable.
The problem is, I don't see any mg/ml indications on the CySol site. I am sure it is because they are still updating it. Can someone give me these numbers please?
Show me the numbers in the same fashion I showed for LiqRes (below), please.
[edited: NO Advertising allowed. ChemE]
---------------
Liquid-Dex
USP24 Anastrozole :: 1mg/ml
Price: $45.00
Liquid-Nolva
USP24 Tamoxifen Citrate :: 20mg/ml
Price: $40.00/50ml vial
Liquid-Nolva
USP24 Tamoxifen Citrate :: 20mg/ml
Price: $40.00/50ml vial
Liquid-Letro
USP24 Letrozole :: 2.5mg/ml
Price: $45.00/30ml vial
Liquid-Clen
USP24 Clenbuterol :: 125mcg/ml
Price: $35.00/50ml vial
Junkyard Dog
New member
I don't at all dispute their quality. We have to assume that the quality is equal unless we are able to prove otherwise. The rest is sheer speculation.radical_P said:
We have to assume they are both getting from labs that are USP24 quality. Hell, they are likely to be buying their products from the same lab!
radical_P
New member
Junkyard Dog said:
Bro I used the other products form the company you were talking about before. same amout and I got bloated. From Cy-sol no bloat. Also I have heard the same from others on the company you refered to. Hey check with Cy-sol because they have been running a special of buy one get the second 1/2 off. Now that's a deal.
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