Helen Frankenthaler Foundation

Cetrorelix Acetate supplier

Buy Cetrotide® [Cetrorelix]

Buy Cetrotide® [Cetrorelix]

Brand Merck Serono

In stock 1273 Items

Available since: 2019-09-19

Dosage form

  • syringe

Brand & Manufacturer

Package Size

  • 0.25 mg syringe 250 mcg, 7 pcs

$373.56

Clinical Pharmacology

Cetrotide - antigonadotropic.

Pharmacodynamics

Cetrorelix, being an analogue of GnRH, binds to receptors of pituitary cell membranes and competitively inhibits the binding of endogenous GnRH to these receptors. Cetrorelix dose-dependently inhibits the secretion of gonadotropins by the pituitary gland: LH and FSH. In the absence of prior stimulation, the onset of inhibition of the pituitary secretory function begins almost immediately after the administration of the drug, the duration of the action of tsetrorelix depends on the dose administered. In women, tsetrorelix causes a delay in raising the level of LH and, therefore, ovulation. After a single injection of 3 mg of cetrorelix, the effect of the drug lasts for at least 4 days (on the 4th day after the administration, the secretory function is depressed by 70%). Regular injections of tsetrorelix 0.25 mg every 24 hours support the effect of the drug. The effect of Cetrorelix is completely reversible after cessation of treatment.

Pharmacokinetics

Suction and distribution. Rapidly absorbed after s / c injection, the absolute bioavailability is about 85%. V d equal to 1.1 l / kg

Pharmacokinetic parameters after a single p / to the introduction of 0.25 mg and repeated administration (within 14 days), respectively: C max in plasma, 4.17–5.92 ng / ml and 5.18–7.96 ng / ml; T max - 0.5–1.5 h and 0.5–2 h; AUC - 23.4–42 ng / h / ml and 36.7–54.2 ng / h / ml.

Derivation. T 1/2 makes 2,4–48,8 h and 4,1–179,3 h after single and repeated (within 14 days) p / to dose of 0,25 mg, respectively. When s / c administration of single doses of tsetrorelix (from 0.25 to 3 mg), as well as with daily administration for 14 days, the pharmacokinetics of the drug shows a linear relationship. Average end t 1/2 after the IV and SC injection, it is 12 and 30 hours, respectively, which indicates absorption at the site of administration.

Cetrorelix is excreted by the kidneys. The total plasma and renal clearance are respectively 1.2 ml / min · kg and 0.1 ml / min · kg. Final t 1/2 after i / v and s / c injection, respectively, an average of about 12 and 30 hours

Indications

Prevention of premature ovulation in patients with controlled stimulation of ovulation for egg production and assisted reproductive technologies.

Composition

1 bottle contains:

Active substance: cetrorelix acetate;

Excipients: mannitol.

Dosage and Administration

Inside during a meal or shortly after a meal, since research has shown that the bioavailability of tsinakaltseta increases when taking the drug with food. pills need to be taken entirely.

Liver failure

When treating patients suffering from liver failure, the initial dose is not required to change. The drug Mimpara should be taken with caution in patients suffering from liver failure in moderate and severe form. Treatment should be closely monitored during dose titration and with prolonged therapy.

Secondary hyperparathyroidism

Adults and Elderly (> 65 years): The recommended starting dose is 30 mg once a day. Titration of the dose should be carried out every 2–4 weeks to a maximum dose of 180 mg (1 time per day), at which the required PTH level in the range of 150–300 pg / ml (15.9–31.8 pmol / l), determined by the content of IPTG. Analysis of the level of PTH should be carried out no earlier than 12 hours after taking the drug Mimpara. In assessing the level of PTH should follow the current recommendations. Measurement of the level of PTH should be carried out 1-4 weeks after the start of therapy or dose adjustment of the drug Mimpara. When a maintenance dose is taken, the PTH level should be monitored approximately once every 1–3 months. To measure the level of PTH, you can use the content of IPTG or biointact PTH (biPTG); therapy with Mimpara does not change the ratio between IPPG and bIPTG.

During dose titration, it is necessary to frequently monitor the level of calcium in the blood serum, incl. 1 week after initiation of therapy or dose adjustment. When a maintenance dose is reached, the serum calcium level should be measured approximately 2 times per month. If the serum calcium level falls below the normal range, appropriate measures should be taken. Concomitant therapy with phosphate and / or vitamin D binders should be adjusted as needed.

Parathyroid carcinoma

Adults and Elderly (> 65 years): The recommended initial dose is 30 mg, the multiplicity of reception - 2 times a day. Titration of the dose should be carried out every 2-4 weeks in the sequence of changes in dosage: 30 mg 2 times a day; 60 mg 2 times a day; 90 mg 2 times a day and 90 mg 3 or 4 times a day (as necessary, to reduce the serum calcium concentration to the upper limit of the normal range or below this level). The maximum dose used in clinical trials was 90 mg with a dose rate 4 times a day. Serum calcium levels should be measured 1 week after initiation of therapy or dose adjustment. When a maintenance dose is reached, the serum calcium level should be measured every 2–3 months. After titration of doses until the maximum dosage is reached, periodic calcium levels in serum should be monitored; If it is not possible to maintain a clinically significant reduction in serum calcium levels, the issue of discontinuing therapy should be resolved.

Adverse reactions

Secondary hyperparathyroidism

In controlled clinical trials, data were obtained from 656 patients taking the drug.Mimpara, and 470 patients taking placebo for up to 6 months. The most frequently observed were