Ketonal suppositories Recto. 100mg 12 pieces

Description

Composition
Active substance:
1 suppository contains: Ketoprofen – 100,000 mg.
Excipients:
Solid fat – 1850 mg; glyceryl kaprilokaprat (Miglyol 812) – 200 mg.
Description:
White, smooth, homogeneous suppositories.
Product form:
Rectal suppositories of 100 mg. 6 suppositories are placed in strips of laminated aluminum tape. As strip 2 is packed in a cardboard box, together with instructions for medical use.
Contraindications
Hypersensitivity to ketoprofen or other ingredients, and also salicylates or other NSAIDs; complete or partial combination of asthma, recurrent nasal polyposis and paranasal sinuses and the intolerance of acetylsalicylic acid (ASA) and other NSAIDs; erosive and ulcerative lesions of the gastrointestinal tract in the acute stage; hemophilia and other bleeding disorders; children’s age (15 years); severe hepatic failure, active liver disease; severe renal failure (creatinine clearance (CC) of less than 30 ml / min), progressive renal disease; confirmed by hyperkalemia; decompensated heart failure; postoperative period after coronary artery bypass surgery; gastrointestinal, and other cerebrovascular bleeding (bleeding or suspected); diverticular disease, inflammatory bowel disease in the acute stage (including ulcerative colitis, Crohn’s disease); chronic dyspepsia; III trimester of pregnancy; breastfeeding; inflammatory diseases of the rectum and / or bleeding from the rectum.
Precautions: asthma history, symptomatic cardiovascular disease, cerebrovascular disease and peripheral arterial disease, dyslipidemia, progressive liver disease, liver failure, hyperbilirubinemia, alcoholic cirrhosis, renal failure (creatinine clearance of 30-60 ml / min), chronic heart failure, hypertension, diseases of the blood, dehydration; diabetes, medical history of the development of ulcerative lesions of the gastrointestinal tract, the presence of infection Helicobacter pylori, severe physical illness, advanced age, smoking, concomitant treatment with anticoagulants (eg, warfarin), antiplatelet agents (for example, acetylsalicylic acid), corticosteroids for intake ( e.g., prednisone), selective serotonin reuptake inhibitors (e.g., citalopram, sertraline), prolonged use of NSAIDs; elderly patients taking diuretics; Patients with a decrease in circulating blood volume.
Indications
Symptomatic treatment of painful and inflammatory processes of various origins, including: inflammatory and degenerative diseases of the musculoskeletal system: reactive arthritis (Reiter’s syndrome); osteoarthritis; tendinitis, bursitis, myalgia, neuralgia, sciatica; pain, including mild, moderate and pronounced: headache; toothache; post-traumatic and postoperative pain; pain in cancer syndrome; algomenorrhea.
The drug is intended for the symptomatic therapy reduce pain and inflammation at the time of use, does not affect the progression of the disease.
Interaction with other drugs
Ketoprofen may weaken the effect of diuretics and antihypertensive agents, and enhance the effect of oral hypoglycemic and some anticonvulsants (phenytoin).
The combined use with other NSAIDs, salicylates, corticosteroids, ethanol increases the risk of adverse effects from the gastrointestinal tract.
The simultaneous use of anticoagulants (heparin, warfarin), thrombolytics, antiplatelet agents (ticlopidine, clopidogrel) increases the risk of bleeding.
The simultaneous use of potassium salts, potassium-sparing diuretics, ACE inhibitors, NSAIDs, low molecular weight heparin, cyclosporin, tacrolimus and trimethoprim increases the risk of hyperkalemia.
Increasing the concentration in the blood plasma of cardiac glycosides, calcium channel blockers slow, lithium drugs, cyclosporine, methotrexate and digoxin.
Increases the toxicity of methotrexate and cyclosporine nephrotoxicity.
Simultaneous use of probenecid significantly reduces the clearance of ketoprofen in plasma.
Interactions with glucocorticoid and other NSAIDs (including selective inhibitors TSOG2) increases the likelihood of adverse reactions (in particular from the gastrointestinal tract).
NSAIDs can reduce the effectiveness of mifepristone. NSAIDs should be started no earlier than 8-12 days after withdrawal of mifepristone.
Overdose
As with the other NSAIDs, ketoprofen overdose may experience nausea, vomiting, abdominal pain, vomiting of blood, melena, disturbance of consciousness, respiratory depression, convulsions, impaired kidney function and kidney failure.
In overdose shown gastric lavage, and the use of activated carbon.
Treatment – symptomatic; ketoprofen effect on the gastrointestinal tract can be reduced by means of reducing the secretion of gastric glands (e.g., proton pump inhibitors) and prostaglandins.
hemodialysis is recommended in case of renal failure.
pharmachologic effect
Pharmacological group:
Nonsteroidal anti-inflammatory drug (NSAID).
Pharmacodynamics:
Ketoprofen is a nonsteroidal anti-inflammatory drug having anti-inflammatory, analgesic and antipyretic action.
Ketoprofen blocks the action of the enzyme cyclooxygenase 1 and 2 (and TSOG1 TSOG2) and partially lipoxygenase, leading to the suppression of prostaglandin synthesis (including in the central nervous system, probably in the hypothalamus).
Stabilizes in vitro and in vivo liposomal membrane at high concentrations in vitro ketoprofen inhibits the synthesis of leukotrienes and bradykinin.
Ketoprofen has no negative impact on the status of the articular cartilage.
Pharmacokinetics:
Absorption
Ketoprofen is readily absorbed from the gastrointestinal tract (GIT) with ingestion. The time to reach maximum concentration (TCmax) at rectal administration – 1,4-4 hours.
Bioavailability is 90%. Food intake has no effect on overall bioavailability of ketoprofen, but reduces the rate of absorption.
Distribution
Ketoprofen is 99% bound to plasma proteins, mainly albumin fraction. The volume of distribution of 0.1 l / kg. Ketoprofen penetrates into the synovial fluid and it reaches a concentration equal to 30% of the plasma concentration. The plasma clearance of ketoprofen is approximately 0.08 l / kg / hr. Effective concentrations of ketoprofen determined in the blood, even at 24 hours after administration.
Metabolism and excretion
Ketoprofen undergoes extensive metabolism by the action of liver microsomal enzymes, the half-life of less than 2 hours. Ketoprofen binds to glucuronic acid and excreted as glucuronide.
No active metabolites of ketoprofen. To 80% ketoprofen excreted by the kidneys within 24 hours, mostly in the form of ketoprofen glucuronide. In applying the drug in a dosage of 100 mg or more renal excretion may be difficult.
In patients with severe renal insufficiency, most of the drug is released through the intestines. When receiving high doses of hepatic clearance also increases. Through the intestine is output to 40% of the formulation.
Patients with liver failure plasma concentration of ketoprofen doubled (possibly due to hypoalbuminemia, and therefore a high level of unbound ketoprofen active); Such patients should be administered the drug in the minimum therapeutic dose.
In patients with renal insufficiency, the clearance of ketoprofen reduced, however dose adjustment is required only in case of severe renal insufficiency.
Elderly patients metabolism and excretion of ketoprofen are slower, which has clinical significance only for patients with severe renal insufficiency.
Pregnancy and breast-feeding
Inhibition of prostaglandin synthesis may have an undesirable influence on the pregnancy and / or fetal development. The data obtained in epidemiological studies in the application of a prostaglandin synthesis inhibitor in early pregnancy, confirm an increased risk of spontaneous abortion and the formation of heart disease (~ 1-1.5%).
Use the drug to pregnant women in I and II trimesters of pregnancy is possible only when the benefits to the mother justifies the potential risk to the fetus.
Contraindicated the use of ketoprofen in pregnant women during the III trimester of pregnancy due to the possibility of uterine weakness generic activities and / or premature closure of the ductus arteriosus, a possible increase in bleeding time, water scarcity, and renal failure.
To date, no data on the allocation of ketoprofen into breast milk, so if you need to use ketoprofen nursing mothers should decide the issue of termination of breastfeeding.
Conditions of supply of pharmacies
Without a prescription.
side effects
According to the World Health Organization (WHO), undesirable effects are classified according to their rate of development as follows: very common (> 1/10), common (> 1/100,
special instructions
Patients with inflammatory diseases of the rectum should not be used rectal suppositories Ketonal®.
Not to be combined with the reception of ketoprofen taking other NSAIDs and / or TSOG2 inhibitors.
With prolonged use of NSAIDs is necessary to periodically evaluate the clinical analysis of blood and to control the function of the kidneys and liver, especially in elderly patients (65 years), to analyze the fecal occult blood.
Care should be taken more frequently monitor blood pressure during application of ketoprofen to treat patients suffering from hypertension, cardiovascular diseases, which result in fluid retention.
In the event of violations of the organs of vision, treatment should be immediately discontinued.
Like other NSAIDs, ketoprofen may mask the symptoms of infectious-inflammatory diseases. In the event of evidence of infection or degradation being against application of the drug to immediately seek medical attention.
With a history of contraindications of the gastrointestinal tract (bleeding, perforation, ulcers), conducting long-term therapy and the use of high doses of ketoprofen patient should be under close medical supervision.
Due to the importance of prostaglandins in maintaining renal blood flow should be particularly careful in the appointment of ketoprofen in patients with cardiac or renal insufficiency as well as in the treatment of elderly patients taking diuretics, and patients who, for whatever reason, decrease in circulating blood volume is observed. Use of the drug should be discontinued prior to major surgery.
Use of ketoprofen can affect female fertility, so patients with infertility (including passing examination) is not recommended to apply the preparation.
During treatment ketoprofen may reduce the rate of mental and motor reactions, so you must refrain from driving vehicles and other classes of potentially hazardous activities that require high concentration and psychomotor speed reactions.
Storage conditions
Store at a temperature not higher than 25 C.
Keep out of the reach of children.
Dosing and Administration
Suppositories Ketonal® 100 mg intended for rectal administration.
Typically prescribed 1 suppository (100 mg) rectally 1-2 times per day.
Rectal suppositories can be combined with oral forms Ketonala®, for example, the patient can take 1 capsule Ketonal® (50 mg) in the morning and in the middle of the day and enter 1 suppository (100 mg) rectally, in the evening, or 1 tablet, film-coated, 100 mg in the morning and enter 1 suppository Ketonal® (100 mg) rectally evening.
The maximum dose of ketoprofen is 200 mg / day.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist