Bystrumcaps, 200 mg capsules, 20 pcs.

Pharmgroup:

NSAIDs.

Pharmic action:

Ketoprofen is a non-steroidal anti-inflammatory drug from the group of propionic acid derivatives. It has the following properties:

has an analgesic effect
has a antipyretic effect
shows anti-inflammatory effects
inhibits platelet aggregation

All the above properties are the result of the reduction of prostaglandin synthesis, by non-selective inhibition of cyclooxygenase activity of types 1 and 2.

Pharmacokinetics:

BYSTRUMCAPS 200 mg capsules contain granules with controlled-release active ingredient that are intended to be taken once daily.

The release of ketoprofen from the pellets occurs gradually in the intestinal tract.

Intake
After oral administration, ketoprofen is almost completely absorbed from the intestinal tract and has a “first pass” effect through the liver.

The maximum plasma concentration is reached 6 – 8 hours after oral administration of a dose of 200 mg. It does not accumulate in the body. Food does not affect the overall bioavailability of ketoprofen.

Distribution
Ketoprofen is 99% bound to plasma proteins. Ketoprofen penetrates into the synovial fluid, where it reaches higher concentrations than in plasma.

In a small amount penetrates through the placental barrier.

Metabolism
Biotransformation of ketoprofen proceeds in two main ways: by hydroxylation, as well as connection with glucuronic acid; the latter is the main way of metabolism.

Less than 1% of the dose of ketoprofen received is found unchanged in the urine, the rest are metabolites, of which 65 to 75% are metabolites of glucuronic acid.

Elimation
Excreted by the kidneys.
The half-life (T1/2) is about 8 hours.

In 5 days after ingestion, 70 to 90% of the dose is excreted in the urine and 1 to 8% in the feces.

In the elderly, the elimination period of ketoprofen is shorter and the T1/2 is longer, and in those with impaired renal function, the T1/2 is longer, depending on the degree of renal impairment.

Indications

Active ingredient

Composition

Active substance:

ketoprofen 200 mg

Associates:

Macrogol 4000,

Ethylcellulose,

Stearic acid,

ammonium methacrylate copolymer,

talk,

neutral granules (sugar and corn starch [3:1]).

Capsule shell:

gelatin, titanium dioxide.

How to take, the dosage

Bystrumcaps is administered orally.

Adults and adolescents over 15 years of age: One capsule 200 mg once daily with meals.

Interaction

Avoid concomitant use with:

Accelerates the effects of anticoagulants, antiaggregants, fibrinolytics, ethanol, side effects of GCS and MKS, estrogen.
Increases plasma concentration of verapamil and nifedipine.

Myelotoxic drugs increase the manifestations of hematotoxicity of the drug.

Reduces the hypotensive effect of beta-blockers.

Increases the risk of nephrotoxic effects of beta-blockers.

Increases the risk of nephrotoxic effects of cyclosporine and tacrolimus, especially in elderly patients.

Decreases the contraceptive effectiveness of IUDs. Increases the risk of bleeding when using thrombolytics.

Caution should be used with:

As with other NSAIDs it is possible:

Special Instructions

During treatment, peripheral blood counts and functional status of the liver and kidneys should be monitored.
If it is necessary to determine 17 – ketosteroids, the drug should be discontinued 48 hours before the study.

Ketoprofen administration may mask signs of infectious disease.

In case of impaired renal and hepatic function, dose reduction and close monitoring are necessary.

During treatment, caution should be exercised when driving motor vehicles and engaging in other potentially hazardous activities requiring increased concentration and rapid psychomotor reactions.

To reduce the risk of gastrointestinal adverse events, the lowest effective dose should be used in as short a course as possible.

Contraindications

Side effects

The digestive system – NSAIDs – gastropathy, heartburn, nausea, vomiting, diarrhea, constipation, flatulence, decreased appetite, stomatitis, pain in the stomach and in the epigastrium, rarely – change of taste. If prolonged use in high doses – gastrointestinal mucosa ulceration, gingival, hemorrhoidal bleeding, intestinal perforation.

Urinary system disorders – rarely: cystitis, urethritis, renal dysfunction, acute renal failure, interstitial nephritis, nephrotic syndrome, hematuria, edema (especially in patients with arterial hypertension).

Hepatic disorders: changes of transaminase activity may be observed; rarely – hepatitis.

Nervous system disorders: agitation, nervousness, drowsiness, depression, asthenia, headache, dizziness, sleep disturbance, insomnia, tinnitus, rarely – confusion or loss of consciousness, forgetfulness, migraine, peripheral neuropathy.

Cardiovascular system: heart failure, increased arterial pressure, rarely – tachycardia.
Hypersensitivity reactions: rhinitis, angioedema, anaphylactic shock, rash, pruritus, urticaria, asthma, especially in patients with hypersensitivity to acetylsalicylic acid, as well as to other medicines from the group of NSAIDs.

Skin reactions: photosensitization, alopecia, erythema multiforme, erythema exudative, including Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell’s syndrome).

Hematopoietic system disorders: anemia, leukopenia, thrombocytopenia, agranulocytosis, pancytopenia, rarely – hemolytic anemia.

Senses: reversible toxic amblyopia, blurred vision or double vision, rarely – conjunctivitis, dry mucous membrane of the eye, pain in the eye, conjunctival hyperemia, decreased hearing.

Others: increased sweating, rarely – haemoptysis, nasal bleeding, myalgia, muscle twitching, shortness of breath, thirst; with prolonged use in high doses – vaginal bleeding.

In case of any side effects the drug should be stopped immediately.

Overdose

In case of ketoprofen overdose symptoms of acute poisoning may appear such as: headache, dizziness, drowsiness, nausea, vomiting, diarrhea, epigastric pain, decreased blood pressure, bronchospasm, bleeding from the GI tract.
In case of suspected overdose you should immediately consult a physician.

Treatment in case of overdose: immediate discontinuation of the drug.

If from overdose of the drug passed within 1 hour, gastric lavage with activated charcoal in a dose of 60 – 100 g in adults, 1 – 2 g/kg body weight in children.

Symptomatic treatment.

Similarities