Ortserin 50 mg (30 capsules) hard gelatine

ORTsERIN

the Trade name
Ortserin

Mezhdunarodnoye the unlicensed


name Diatserein Lekarstvennaya
the Capsule form firm gelatinous 50 mg

Structure
One capsule contains
active agent - diatserein 50 mg,
excipients: beta cyclodextrin (betadex), sodium lauryl sulfate, lactose monohydrate, sodium of a kroskarmelloz, silicon dioxide colloidal anhydrous, magnesium stearate,
solid gelatin capsule
body: diamond blue E 133, quinolinic yellow E104, ponso 4R E 127, the titan E171 dioxide, preservatives, sodium lauryl sulfate, water purified, gelatin,
a lid: diamond blue E 133, quinolinic yellow E104, ponso 4R E 127, the titan E171 dioxide preservatives, sodium lauryl sulfate, water purified, gelatin.

The description
Solid gelatin capsules No. 1 with the blue body and a blue lid. Contents of capsules - powder of yellow color

Pharmacotherapeutic group
Non-steroidal anti-inflammatory drugs
Non-steroidal anti-inflammatory drugs others
the ATX M01 AX21 Code

the Pharmacological

Pharmacokinetics Absorption properties: at intake diatserein Rhine even before hit in a system blood stream is exposed to full deacetylation in its active metabolite. Visible bioavailability of Rhine of 35-60%. Stable concentration is reached to the third reception and elimination half-life averages 7-8 hours. Reception of a diatserein with food delays system absorption, but increases amount of the soaked-up substance by 25%. After intake at most concentration in plasma is reached in 2.2 hours and makes 3.2 mg/l.
Distribution: distribution volume after intake of a single dose of a diatserin of 50 mg is 13.2 l. The active metabolite Rhine well contacts proteins of plasma – up to 99%.
Metabolism and removal: the active metabolite Rhine turns in a liver into a glucuronide (60%) or sulfate (20%). Up to 20% of not changed Rhine and the main part of metabolites are removed by kidneys. After introduction of a single dose of a diatserein of 50 mg the elimination half-life made 4.3 hours, visible general clearance of plasma – 1.6 l/hour, renal clearance of 0.13 l/hour.

Ortserin's pharmacodynamics represents a derivative of anthraquinone which possesses anesthetic, antipyretic and anti-inflammatory action, at the same time does not suppress cyclooxygenase or a lipoxygenase. It is proved that it inhibits products of interleukin-1 which promotes a degeneration of an articulate cartilage, stimulating cells to production of proteolytic enzymes and reducing anabolism of chondrocytes and also reduces the content of metalproteinases in an osteoartrozny cartilage of the person. On the other hand, it stimulates synthesis of glikozaminoglikan and hyaluronic acid in a cartilage matrix and also effectively reduces synovial inflammation and a degeneration of cartilaginous tissue.

Indications
- an osteoarthritis, an osteoarthrosis
- a coxarthrosis, gonartroz


to Accept the Route of administration and doses on 50 mg (1 capsule) inside twice a day at meal time. To swallow the capsule entirely, without chewing. Patients with a renal failure (clearance of creatinine less than 30 ml/min.) need to lower a dose half. The course of treatment makes not less than 6 months or is defined by the doctor.
In view of that Ortserin can cause strengthening of a vermicular movement of intestines in an initiation of treatment, it is recommended to take within the first 4 weeks the drug on 1 capsule a day during evening meal. Further it is possible to increase a dose to 100 mg/days, breaking it into two receptions (in the morning and in the evening).
Duration of treatment is defined by the attending physician depending on the clinical answer.
As the clinical effect of an ortserin appears in 2-4 weeks of treatment, for this period it is possible not to cancel non-steroidal anti-inflammatory drugs or analgetik.
In a heavy renal failure (the clearance of a kreatinan is lower than 30 ml/min.) it is recommended to lower an initial dose by 50% as at insufficient function of kidneys the pharmacokinetics of a diatserein is modified.
In a liver failure of easy and average degree the pharmacokinetics of a diatserein does not change therefore there is no need for correction of a dose of an ortserin in cirrhosis.

Side effects
- nausea, vomiting, an abdominal pain, dyspepsia, diarrhea and the related symptoms and/or constipations
- allergic skin reactions, a bronchospasm, a Quincke's disease, an acute anaphylaxis
-

Contraindication urine discoloration
- hypersensitivity to an ortserin and derivatives of anthraquinone and also to any of drug ingredients
- hereditary intolerance of fructose of a galactose, a galactosemia or a malyadsorbtion of glucose galactose
- pregnancy and the period of a lactation
- children's and teenage age up to 18 years

Medicinal interactions
Ortserin it is not necessary to accept along with the drugs strengthening an intestines vermicular movement, or affecting qualitative structure of contents of a small intestine (for example, a large amount of cellulose, etc.). It is necessary to avoid a concomitant use of the drugs containing a hydroxide of aluminum and/or magnesium not to reduce bioavailability of a diatserein. Treatment ortseriny can cause strengthening of symptoms of colitis in the patients accepting antibiotics and/or chemotherapy, affecting composition of indestinal flora.

Special instructions
Each 6 months of treatment it is necessary to conduct full blood test, including the level of hepatic transaminases, the analysis of urine.
At reception of a diatserein with food the increase is observed (up to 25%) its absorptions, on the contrary, the serious deficit of food reduces bioavailability of a diatserein. As the frequency of side effects (such as the accelerated intestines contents passage) is directly proportional to quantity of not absorbed diatserein, administration of drug during a post (starvation) or with a small amount of food can become the reason of increase in frequency of side effects.
Diarrhea independently passes within 2 weeks without the treatment termination. It is necessary to consider a question of the treatment termination if diarrhea has the significant character.
At reception of an ortserin it is not necessary to accept depletive.
At treatment by antibiotics which can influence structure of microflora or kinetics of intestines it is necessary to consider a question of temporary suspension of treatment.

There Is no feature of influence of medicine on ability to run vehicles and potentially dangerous mechanisms data

Overdose
Symptoms: it is necessary to expect strengthening of side effects, mainly, of diarrhea, and its consequences.
Treatment: symptomatic. Specific antidote is unknown. Owing to high extent of linking with proteins it is not necessary to expect efficiency of a hemodialysis.

A form of release and packing
On 10 capsules in blister strip packaging.
On the 3rd blister strip packagings together with the instruction for medical use in the state and Russian languages place in a cardboard pack.


To Store storage conditions in the place protected from light at a temperature not above 30ºС
to Store in places inaccessible for children!


3 years
not to apply a period of storage after an expiration date.

Prescription status
According to the prescription

the Name and the country
of the Macleods Pharmaceuticals Limited manufacturing organization
The pharmacological Center