Buy Cetrotide syringe 0.25 mg syringe 250 mcg, 7 pcs

Cetrotide® [Cetrorelix]

Brand Merck Serono

In stock 1273 Items

Available since: 2019-09-19

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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.

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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 nausea (31% in the group of cynacalcet; 19% in the placebo group) and vomiting (27% in the group of cinacalcet; 15% in the placebo group). Nausea and vomiting were mild to moderate in severity and in most cases were short-lived. Termination of therapy as a result of the development of undesirable effects was mainly caused by nausea (1% in the placebo group; 5% in the cinacalcet group) and vomiting (

Adverse reactions associated with the use of cinakalcet and more common in the Mimpara group compared to the placebo group in double-blind clinical studies are listed below with the following sequence: very often (> 1/10); often (> 1 / 100,1 / 1000,1 / 10 000,

From the digestive system: very often - nausea, vomiting; often - anorexia; sometimes dyspepsia, diarrhea.

From the side of the central nervous system and peripheral nervous system:often - dizziness, paresthesias; sometimes convulsions.

From the musculoskeletal system:often myalgia.

On the part of the endocrine system: often - a decrease in testosterone levels.

Dermatological reactions:often - rash.

Allergic reactions: sometimes - hypersensitivity reactions.

Other: often - asthenia, hypocalcemia.

Parathyroid carcinoma and primary hyperparathyroidism

Security profileMimpara in this group of patients, in general, corresponds to the picture observed in patients with chronic kidney disease. The most common side effects were nausea and vomiting.

Post-marketing observations

When using the drugMimpara in routine practice, the following adverse reactions have been identified, the frequency of which cannot be estimated based on the available data:

- in patients with heart failure and receiving cinacalcet, individual idiosyncratic cases of a decrease in blood pressure and / or worsening of the course of heart failure were recorded;

- Allergic reactions, including angioedema and urticaria.

Contraindications

Children's age up to 18 years (efficiency and safety are not studied); hypersensitivity to the drug.

Drug interactions

The effect of other drugs on cinnacalce

Tsinakaltset partially metabolized by the enzyme CYP3A4. The simultaneous intake of 200 mg of ketoconazole 2 times a day (a pronounced inhibitor of CYP3A4) resulted in an increase in levels of cinacaltce about 2 times. It may be necessary to adjust the dose of the drug Mimpara if the patient starts or stops taking a potent inhibitor (for example, ketoconazole, itraconazole, telithromycin, voriconazole, ritonavir) or inducers of this enzyme activity during therapy.

The data obtained during the experimentsin vitro, indicate that cinacalcet is partially metabolized by the CYP1A2 enzyme. Smoking stimulates CYP1A2 activity; It was noted that cinakaltcet clearance is 36–38% higher in smokers than in non-smokers. The effect of CYP1A2 inhibitors (fluvoxamine, ciprofloxacin) on plasma levels of tsinakaltseta has not been studied. Dosage adjustment may be necessary if, during drug therapy with Mimpara, the patient starts or stops smoking, or starts or stops the simultaneous use of powerful inhibitors of CYP1A2.

Calcium carbonate: the simultaneous use of calcium carbonate (a single dose of 1500 mg) did not alter the pharmacokinetics of cinacalcet.

Sevelamer: the simultaneous use of Sevelamer (2400 mg 3 times a day) did not affect the pharmacokinetics of cinacalcet.

Pantoprazole: the simultaneous use of Pantoprazole (80 mg 1 time per day) did not change the pharmacokinetics of cinacalcet.

The effect of tsinakaltseta on other drugs

Drugs metabolized by the enzyme P450 2D6 (CYP2D6): cinacalcet is a potent inhibitor of CYP2D6. It may be necessary to adjust the dosage of drugs while taking it with the drug Mimpara, if such drugs are mainly metabolized by CYP2D6, have a narrow therapeutic index and require an individual dose selection.

Desipramine: simultaneous administration of a dose of 90 mg of cinacalcet once a day with 50 mg of desipramine, a tricyclic antidepressant, predominantly metabolized by CYP2D6, significantly (3.6 times) increased the level of exposure of desipramine in patients with active CYP2D6 metabolism.

Warfarin: repeated oral intake of cinacalcet did not affect the pharmacokinetics or pharmacodynamics of warfarin (PV and VII coagulation factor were measured).

The lack of effect of cinacalcet on the pharmacokinetics of R- and S-warfarin and the lack of autoinduction of enzymes in patients after repeated dosing indicates that cinacalcet is not an inducer of CYP3A4, CYP1A2 or CYP2C9 in humans.

Pregnancy and Lactation

Clinical data on the use of cinnakaltse in pregnancy are not available. As shown by preclinical studies in rabbits, cinacalcet penetrates the placental barrier.In animal experiments, no direct adverse effect on the course of pregnancy, childbirth or postnatal development was detected. Neither embryotoxic nor teratogenic effects were detected during experiments on pregnant female rats and rabbits, with the exception of reducing the weight of embryos in rats using doses that are toxic to pregnant females. In pregnancy, the drug Mimpara should be used only in cases where the potential benefit justifies the potential risk to the fetus.

To date, the possibility of cinakaltcet in the milk of a nursing woman has not been studied. Tsinakaltset falls into the milk of lactating rats, while there is a high ratio of levels in the milk to the levels in the plasma. After a thorough assessment of the risk / benefit ratio, a decision should be made to discontinue breastfeeding or taking Mimpara.

Special instructions

In three studies involving patients with CKD who are on dialysis, 5% of patients in each of the groups treated with Mimpara or placebo, at the time of initiation of therapy were recorded information about the attacks of seizures. In these studies, convulsions were observed in 1.4% of patients receiving Mimpara and in 0.4% of patients from the placebo group. Although the reasons for the reported differences in convulsions are unclear, the threshold for the occurrence of convulsive seizures decreases with a significant decrease in serum calcium levels.

In patients with heart failure, taking cinacalcet, in the course of post-marketing studies, individual cases of idiosyncrasy of arterial hypotension and / or deterioration of heart failure were recorded, in which the cause-effect relationship with cinnacalce cannot be completely excluded and may be due to a decrease in serum calcium . Data from clinical studies have shown that arterial hypotension occurred in 7% of patients taking cinacalcet and in 12% of patients receiving placebo, and heart failure in 2% of patients who received cinacalcet or placebo.

Therapy with Mimpara should not be performed when the serum calcium concentration (adjusted for albumin) is below the minimum limit of the normal range. Since cinacalcet lowers serum calcium concentration, it is necessary to carefully monitor patients for the development of hypocalcemia. In patients with a diagnosis of CKD who are on dialysis, when taking the drug Mipara the concentration of calcium in serum in 4% of cases was below 7.5 mg / dl (1.875 mmol / l). In case of hypocalcemia, to increase the level of calcium in the blood serum, calcium-containing phosphate binders, vitamin D and / or correction of calcium concentration in the solution during dialysis can be used. With sustained hypocalcemia, reduce the dose or stop taking Mimpara. Potential signs of hypocalcemia can be paresthesia, myalgia, seizures, tetany.

Tsinakaltset is not indicated for patients with a diagnosis of CKD who are not on dialysis due to an increased risk of hypocalcemia (serum calcium concentration

In chronic suppression of the PTH concentration below a concentration of approximately 1.5% of VGN according to the results of the analysis of IPTG, an adynamic bone disease may develop. If the PTH concentration falls below the recommended range, reduce the dose of Mimpara and / or vitamin D, or discontinue therapy.

Testosterone concentrations are often below normal in patients with end-stage renal disease. Clinical data from patients with end-stage renal disease on dialysis showed that the concentration of free testosterone decreased, on average, by 31.3% in patients taking Mimpara, and by 16.3% in patients in the placebo group 6 months after the start therapy.The open prolonged phase of this study did not show a further decrease in the concentration of free and total testosterone in patients over a 3-year period of treatment with Mimpara. The clinical significance of reducing serum testosterone levels has not been established.

Since patients with moderate and severe liver failure (on the Child-Pugh scale), plasma levels of tsynakalcet can be 2-4 times higher, such patients should take Mimpara with caution and carefully monitor liver function during treatment.

Mimpara contains lactose as an excipient (each 30 mg tablet contains 2.74 mg of lactose, each 60 mg tablet contains 5.47 mg of lactose, each 90 mg tablet contains 8.21 mg of lactose). Patients with rare hereditary intolerance to galactose, lactase-deficient lapp or impaired glucose / galactose absorption should not take the drug.

Overdosage

Symptoms: hypocalcemia; in case of overdose, patients should monitor the symptoms and signs of hypocalcemia.

Treatment: symptomatic and supportive therapy. Since the degree of binding of cinacalcet to proteins is high, hemodialysis is not an effective therapeutic method for overdose.

Doses titrated up to 300 mg (1 time per day) are safe for patients on dialysis.

Studies and clinical trials of Cetrorelix (Click to expand)