testosterone cypionate

Plasma gastrin testosterone cypionate level was raised first 2-8 weeks, which reflects an inhibitory effect on the secretion of acid.
The concentration of gastrin returned to baseline levels usually within 1-2 weeks after cessation of treatment.

Effect on enterohromafinno-like cells
In the investigation of human gastric biopsy samples from the antrum region and fundus of 500 patients treated with sodium rabeprazole or a reference drug for 8 weeks, lasting changes in morphological structure enterohromafinno-like cells, the severity of gastritis, incidence of atrophic gastritis intestinal metaplasia or distribution of infection of Helicobacter pylori were detected.
In a study of over 400 patients receiving sodium rabeprazole (10 mg / day or 20 mg / day) for up to 1 year, the incidence of hyperplasia was low and comparable to that of omeprazole (20 mg / kg). He was not registered a single case of adenomatous changes or carcinoid tumors observed in rats.

Other effects
Systemic effects of rabeprazole sodium in the central nervous system, cardiovascular and respiratory systems are not currently detected. It has been shown that sodium rabeprazole when administered orally at a dose of 20 mg for 2 weeks did not affect thyroid function, carbohydrate metabolism, the level of parathyroid hormone in the blood, as well as cortisol, estrogen, testosterone, prolactin, glucagon, follicle-stimulating hormone (FSH), luteinizing hormone (LH), renin, aldosterone, and growth hormone.

Pharmacokinetics

Testosterone cypionate.
Rabeprazole is rapidly absorbed from the intestine, and peak plasma concentrations are achieved in about 3.5 hours after receiving a dose of 20 mg. Changing the peak plasma concentration (C max; ) and area under the curve values ​​”concentration-time» (AUC) of rabeprazole are linear over a dose range from 10 to 40 mg. The absolute bioavailability after oral administration of 20 mg (as compared to intravenous administration) is about 52%.
In addition, the bioavailability is not changed during repeated reception rabeprazole. In healthy volunteers the plasma half-life of about 1 hour (ranging from 0.7 to 1.5 hours) and the total clearance is 3.8 ml / min / kg. Patients with chronic increased liver lesion AUC doubled compared with healthy volunteers, suggesting a decrease first-pass metabolism, and plasma half-life is increased by 2-3 times. Neither time dosing during a day or antacids do not affect the absorption of rabeprazole. The drug with fatty food slows the rabeprazole absorbance at 4 hours or more, but neither C max; , nor the degree of absorption is not changed.

Distribution.
In humans, the degree of binding of rabeprazole to plasma proteins is approximately 97%.

Metabolism and excretion. In healthy subjects after receiving a single oral dose of 20 mg of 14 C-labeled rabeprazole sodium unchanged drug was found in urine. About 90% of rabeprazole excreted in the urine mainly as two metabolites: Conjugate mercapturic acid (M5) and a carboxylic acid (M6), and in the form of two unknown metabolites identified in the toxicological analysis. The remaining portion of the received rabeprazole sodium is excreted in the faeces. The total removal was 99.8%. These data indicate a small breeding metabolites of rabeprazole sodium in the bile. The major metabolite is a thioether (M1). The only active desmethyl metabolite is (M3), but it was observed at a low concentration in only one study participant after receiving 80 mg of rabeprazole.

End-stage renal failure
in patients with stable renal insufficiency in terminal stage, which requires maintenance hemodialysis (creatinine clearance <5 ml / min / 1,73m 2 ), rabeprazole sodium excretion is similar to testosterone cypionate that of healthy volunteers. AUC and Cmax for these patients were about 35% lower than in healthy volunteers. The average half-life of rabeprazole was 0.82 hours in healthy volunteers, 0.95 hours in patients during hemodialysis and 3.6 hours post dialysis. The clearance of the drug in patients who require hemodialysis renal disease, was approximately two times higher than in healthy volunteers.

Chronic compensated cirrhosis
patients with compensated chronic liver cirrhosis transferred rabeprazole sodium in a dose of 20 mg 1 time per day, although the AUC is doubled and C max; is increased by 50% as compared with gender matched healthy volunteers.

Elderly patients.
In elderly patients, elimination of rabeprazole has slowed somewhat. After 7 days of rabeprazole 20 mg per day in the elderly AUC were approximately twice as C max; enhanced by 60% compared with young healthy volunteers. However, evidence of rabeprazole accumulation was observed.

CYP2C19 polymorphism
in patients with delayed metabolism CYP2C19 after 7 days of rabeprazole in a dose of 20 mg per day AUC increased 1.9 times, and the half-life of 1.6 times in comparison with the same parameters as the “rapid metabolizers”, while as C max; increased by 40%.

Indications

– Peptic ulcer in the acute stage and anastomotic ulcer;
– Duodenal ulcer in the acute stage;
– erosive and ulcerative gastroesophageal reflux disease or reflux esophagitis;
– Maintenance treatment of gastroesophageal reflux disease; br- non-erosive gastroesophageal reflux disease;
– Zollinger-Ellison syndrome and other conditions characterized by pathological hypersecretion;
– In combination with appropriate antibiotic therapy for eradication of Helicobacter pylori in patients with peptic ulcer disease.

Contraindications

– Hypersensitivity to rabeprazole, substituted benzimidazoles or to the auxiliary components of the preparation;
– pregnancy;
– lactation
– Children under 12 years old.

With care
– children’s age;
– severe renal insufficiency.

Pregnancy and lactation

Safety Data application rabeprazole during pregnancy does not. Reproduction studies in rats and rabbits revealed no evidence of impaired fertility or fetal development defects caused by rabeprazole; but rats in small quantities drug crosses the placental barrier. Pariet ® should not be used during pregnancy except in cases where the expected positive effect for the mother outweighs the potential harm to the fetus.
It is not known whether rabeprazole is excreted in breast milk. Appropriate studies in lactating women have not been conducted. However, rabeprazole was found in the testosterone cypionate milk of lactating rats, and therefore Pariet ® should not be administered to nursing women.

Dosing and Administration

The tablets of the drug Pariet ® can not chew or crush. The tablets should be swallowed whole. It is established that no time of day, meal or no effect on the activity of rabeprazole sodium.

In gastric ulcer in the acute stage and anastomotic ulcer
it is recommended to be taken orally 20 mg once a day. Typically, recovery occurs after 6 weeks of treatment, but in some cases, the duration of treatment can be extended for another 6 weeks.

In duodenal ulcer in the acute stage
it is recommended to be taken orally 20 mg once a day. The duration of treatment is from 2 to 4 weeks. If necessary, the duration of treatment can be increased a further 4 weeks.

In the treatment of erosive gastroesophageal reflux disease (GERD) or reflux esophagitis
recommended to ingest 20 mg once a day. The duration of treatment is from 4 to 8 weeks. If necessary, the duration of treatment can be increased another 8 weeks.

When the maintenance treatment of gastroesophageal reflux disease (GERD)
is recommended to ingest 20 mg once a day. The duration of treatment depends on the patient’s condition.

When non-erosive gastroesophageal reflux disease (NERD) without esophagitis
is recommended to be taken orally 20 mg once a day.
If after four weeks of treatment, the symptoms do not disappear, it is necessary to conduct a further study of the patient.
After the relief of symptoms in order to prevent their further occurrence should take the drug orally once a day on demand.

For the treatment of Zollinger-Ellison syndrome and other conditions characterized by pathological hypersecretion,
dose picked individually. Initial dose – 60 mg a day, and then increase the dose administered drug dose to 100 mg per day in single dose or 60 mg twice a day. For some patients, the fractional drug dosing is preferred. Treatment should continue as clinically necessary. Some patients with Zollinger-Ellison rabeprazole treatment duration was up to one year.

For Helicobacter pylori eradication
is recommended to ingest 20 mg 2 times a day in a specific pattern with the appropriate combination of antibiotics. Treatment duration was 7 days.

Patients with renal and hepatic insufficiency
dose adjustment for patients with renal failure is necessary.
Patients with mild to moderate hepatic impairment concentration of rabeprazole blood is generally higher than in healthy patients.
When assigning drug Pariet ® patients with severe liver failure caution .

Elderly patients
No dose adjustment is required.

Children
The safety and efficacy of sodium rabeprazole 20 mg for short-term (up to 8 weeks) treatment of GERD in children aged 12 years or more was confirmed by extrapolating the results of adequate and well-controlled studies, reinforcing the effectiveness of sodium rabeprazole for adults and studies of the safety and pharmacokinetics for pediatric patients.
The recommended dose for children aged 12 years testosterone cypionate and over is 20 mg 1 time per day for up to 8 weeks.
The safety and efficacy of rabeprazole sodium for the treatment of GERD in children aged under 12 years has not been established. The safety and efficacy of rabeprazole sodium for use in other indications has not been established for pediatric patients.

eurochem labs