What Are the Most Common Ketoprofen Side Effects?

Ketoprofen sustained-release capsules, prescription drugs, capsules, the main ingredient is ketoprofen, which is mainly used for rheumatoid or rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, gout, dysmenorrhea, etc. It can also be used for joint sprains , Soft group severe injury, fracture pain and postoperative pain.

Foreign name: Ketoprofen Sustained Release Capsules
Whether prescription drugs: prescription

Dosage form: Capsule
Drug type: chemical
Specifications: 0.1g

Ketoprofen sustained-release capsules ingredients:

The main ingredient of this product is ketoprofen.
Chemical name: a-methyl-3-benzoyl-phenylacetic acid.
Molecular formula: C ₁₆ H ₁₄ O ₃
Molecular weight: 254.29

Ketoprofen sustained-release capsules

Chemicals & Biological Products >> Antipyretic Analgesic Anti-inflammatory Drugs >> Organic Acids >> Carboxylic Acids

Ketoprofen sustained-release capsule properties:

This product is a hard capsule with white or off-white spherical contents

Ketoprofen sustained-release capsules indications:

Mainly used for rheumatoid or rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, gout, dysmenorrhea, etc. It can also be used for joint sprains, soft injury, fracture pain and postoperative pain.

Ketoprofen sustained-release capsules specifications:

75mg; 0.2g; 0.1g

Ketoprofen sustained-release capsules

Adults, take orally during meals.
Commonly used quantities are:
75mg (1 capsule) or 0.1g (1 capsule) twice a day;
0.2 g once daily (75 mg 3 capsules; 0.1 g 2 capsules; 0.2 g 1 capsule).

Ketoprofen Sustained Release Capsules Adverse Reactions:

According to foreign literature reports: The incidence of common adverse reactions in 855 ketoprofen capsules in a 4-54 week double-blind controlled trial and 622 ketoprofen sustained-release capsules in a 4-16 week double-blind controlled trial is approximately 1%. In the crossover trial, there was no significant difference in the incidence of adverse reactions in the upper and lower digestive tracts between patients who took 200 mg sustained-release capsules daily and those who took ordinary capsules 75 mg X 3 times / day. Gastric ulcer and gastrointestinal bleeding symptoms were less than 1% during controlled clinical trials (1076); during the later open phase, the incidence of these symptoms rose to much greater than 2% (1292).
The incidence of gastrointestinal ulcers during nonsteroidal anti-inflammatory drugs is related to multiple risk factors, such as age, gender, smoking, alcohol, diet, stress, combined medications such as aspirin, cortisol, and the dosage And maintenance time. The adverse reactions of the central nervous system are second only to those of the gastrointestinal tract, and are manifested as headache, dizziness, and lethargy. The incidence of this adverse reaction was dose-dependent.
The following is a summary based on the incidence of adverse reactions and the decreasing incidence:
Incidence> 1% (most likely causal)
Digestive tract: indigestion (11%) nausea, abdominal pain, diarrhea, constipation, flatulence, anorexia, vomiting, stomatitis.
Nervous system: headache, dizziness, central nervous system depression or excitement (eg insomnia, nervousness, dreaminess, etc.)
Special sensations: tinnitus, visual disturbance of skin and limbs: rash, urinary system: renal dysfunction (edema, increased BUN), symptoms of urinary tract irritation, etc.
Incidence rate <1% (most likely causal)
Systemic: chills, facial edema, infection, pain, allergic reactions.
Cardiovascular: Hypertension, palpitations, tachycardia, congestive heart failure, peripheral vascular disease, vasodilation.
Digestive tract: increased appetite, dry mouth, snoring, gastritis, rectal bleeding, black stool, occult blood in stool, increased saliva, gastric ulcer, gastrointestinal perforation, bleeding, intestinal ulcer, liver dysfunction, hepatitis, bile hepatitis ,jaundice.
Blood: agranulocytosis, anemia, hemolysis, purpura, thrombocytopenia.
Metabolism and nutrition: thirst, weight gain or loss, impaired renal cortex function.
Muscle system: myalgia.
Nervous system: forgetfulness, confusion, weakness, paresthesia, migraine, dizziness.
Respiratory system: dyspnea, hemoptysis, nosebleeds, pharyngitis, rhinitis, bronchospasm, and edema of the throat.
Skin and limbs: alopecia, eczema, pruritus, purple rash, sweating, urticaria, herpes, scaly exfoliation of skin, photosensitivity, skin discoloration, epidermal necrosis, multiple forms of erythema, Stevenson Johnson syndrome.
Special sensations: conjunctivitis, dry eye conjunctivitis, eye pain, hearing impairment, retinal hemorrhage, hyperpigmentation, and perverted taste.
Urinary system: menstruation, hematuria, renal insufficiency, interstitial nephritis, nephrotic syndrome.
The following are rare adverse reactions, whether they are related to taking ketoprofen, there is no clear, are introduced from top to bottom according to the severity of symptoms:
Systemic system: sepsis, shock.
Cardiovascular: arrhythmia, myocardial strain.
Digestive tract: bad oral cavity, ulcerative colitis, arterial fatty lesions, pancreatitis, endocrine system: exacerbation of diabetes.
Nervous system: irritability, hallucinations, sexual impulses, nightmares, discomfort, meningitis, urinary system: acute tubular nephritis, male feminized breasts

Ketoprofen extended-release capsules contraindications:

Active gastrointestinal ulcers and bleeding;
People who are allergic to this product, aspirin or other non-steroidal anti-inflammatory analgesics.

Ketoprofen Sustained Release Capsules Warning:

When the elderly use this product, the plasma protein binding rate and drug excretion rate can be reduced, resulting in an increase in blood drug concentration and prolonged half-life, so attention should be paid to dose adjustment.

Ketoprofen sustained-release capsules :

Alcohol use or concurrent use with other non-steroidal anti-inflammatory drugs can increase gastrointestinal side effects and risk of causing ulcers. Long-term use with acetaminophen can increase toxic and side effects on the kidney;
When used with aspirin or other salicylic acid drugs, it can reduce the protein binding rate of this product, so it is prohibited to use with aspirin;
Use with heparin, dicoumarin and other anticoagulants and platelet aggregation inhibitors, which may increase the risk of bleeding;
Used together with furosemide, the latter can reduce the sodium excretion and hypotensive effect of the latter;
Used together with verapamil and nifedipine, the blood concentration of this product increases;
This product can increase the blood concentration of digoxin. At the same time, pay attention to adjust the dose of digoxin;
This product can enhance the effect of anti-diabetic drugs (including oral hypoglycemic drugs);
This product is used in combination with antihypertensive drugs, which can affect the antihypertensive effect of the latter;
Probenecid can reduce the excretion of this product, increase its blood concentration, and even reach toxic levels, so this product should not be used with medium or large doses of methotrexate.
Use with caution in patients with gastrointestinal disorders, asthma, cardiac insufficiency, hypertension, hemophilia or other bleeding disorders, liver and kidney dysfunction, pregnant women, lactating women, children, and the elderly.

Ketoprofen sustained-release capsules for pregnant and lactating women:

There are not enough controlled studies on the use of this product in pregnant women, although teratogenicity studies have not shown teratogenicity and fetal toxicity. However, because animal experiments cannot fully predict the effects of the drug on humans, it is not recommended for pregnant women unless the benefits of treatment outweigh the risks.
This product is not clear about the delivery and productivity of pregnant women. Animal experiments have shown that administering ketoprofen at 6 mg / kg / d (36 mg / m / d) in rats, equivalent to one fifth of the highest daily recommended human dose of 185 mg / m / d, will prolong the pregnancy process. Knowing the fatal effects of prostaglandin-inhibiting drugs on the cardiovascular system (arterial embolism), this product should be avoided in late pregnancy. 3. The effect of taking this product on milk secretion is not clear. Animal tests have shown that giving rats up to 9 mg / kg / d (54 mg / m / d), which is equivalent to 30% of the maximum daily human recommended dose of 185 mg / m / d, will not affect this process. For lactating dogs, the level of ketoprofen in milk is about 4-5% of the blood concentration. Since other drugs are excreted from milk, it is not recommended to be given to lactating women.

Ketoprofen sustained-release capsules for children:

still uncertain.

Ketoprofen sustained-release capsules for elderly:

Ketoprofen sustained-release capsule drug interactions:

Drug Interactions The following drug interaction studies are based on a 200 mg ketoprofen daily dose. If more than 200 mg of ketoprofen sustained-release capsules are taken daily, drug interactions will increase due to increased drug-binding rates.
1. Antacids: When ketoprofen capsules are given at the same time, antacids such as magnesium hydroxide and aluminum hydroxide will not affect the absorption rate and total absorption of ketoprofen.
2. Aspirin: Taking ketoprofen does not affect aspirin absorption; however, in a study of 12 healthy volunteers, cross-administration of aspirin reduced the plasma protein binding rate of ketoprofen and increased the plasma clearance of ketoprofen. The dose of 0.07L / kg / h from aspirin was never increased to 0.11L / kg / h of aspirin. No further research has been conducted on this clinical sign. Therefore, the simultaneous use of aspirin and ketoprofen is not recommended.
3. Diuretics: When ketoprofen is given at the same time as hydrochlorothiazide, the excretion of potassium and chlorine is reduced in the urine compared to hydrochlorothiazide alone. Patients taking diuretics while taking ketoprofen have a significantly increased risk. The second reason is that ketoprofen inhibits prostaglandin synthesis, which reduces the rate of renal blood perfusion.
4. Digoxin: In a study of 12 patients with congestive heart failure, patients took ketoprofen while taking digoxin, and the results showed that ketoprofen did not affect the serum level of digoxin.
5. Farwaring: In a short-term study of 14 normal volunteers, taking ketoprofen while taking Farwaring did not significantly affect the prothrombin time of Farwaring. However, because prostaglandins have very significant effects on hemostasis, and ketoprofen also affects platelet function, if ketoprofen is combined with farwaring, various indicators need to be closely monitored.
6. Probenecid: Probenecid reduces ketoprofen's plasma clearance by one-third and increases plasma free and bound ketoprofen. Therefore, the combined use of these two drugs is not recommended.
7. Methotrexate: Like other non-steroidal anti-inflammatory drugs, the combined use of methotrexate will cause the elimination of methotrexate to change, leading to increased plasma concentrations and increased toxicity.
8. Lithium preparation: It has been reported that taking non-steroidal anti-inflammatory drugs will cause the steady state concentration of lithium preparation to change. Therefore, it is recommended to monitor the lithium concentration when taking lithium preparation and ketoprofen at the same time.
Interaction of pharmacological laboratory tests with coagulation experiments. Ketoprofen reduces platelet adhesion and aggregation. Therefore, taking ketoprofen will prolong the bleeding time, which is about 3-4 minutes longer than the baseline time. This did not significantly affect platelet count, prothrombin time, prothrombin kinase time, and thrombin time.

Ketoprofen extended-release capsules overdose:

Signs of overdose of non-steroidal anti-inflammatory drugs include weakness, drowsiness, nausea, vomiting, and upper abdominal pain. Conventional supportive methods should be used if they occur.

Ketoprofen overdose may cause reduced breathing, coma, and convulsions. Gastrointestinal bleeding, hypotension, hypertension, or acute renal failure may also occur, but the incidence is very low.
Patients should be given supportive treatment based on signs after overdose. There are currently no special remedies. Ketoprofen capsules should be taken within 4 hours after symptoms of overdose (slow-release capsules can be prolonged) or when taking ketoprofen 5-10 times the usual dose, by cleaning the stomach and intestines, and using emetic, taking activated carbon (adults 60-100 g, children 1-2 g / kg) and cathartic or add polysorbide in the first dose. Diuretic measures, alkaline urine and other measures are taken, but hemodialysis may not work because ketoprofen and plasma proteins have a high binding rate.
There are currently 26 reports of overdose, 6 children, 16 adolescents, and 4 adults. Five patients had only mild symptoms (4 vomiting, 1 drowsiness for children). A 12-year-old girl took unknowing amounts of ketoprofen and bupropion and hydrocodone for 1-2 hours and found irritable convulsions. The ketoprofen blood concentration of 1156 mg / L was detected 3-4 hours after taking the drug ( 56 times the conventional dose of 20 mg / L) after intubation, given diazepam and activated carbon, recovered. A 45-year-old woman took 200mg of ketoprofen sustained-release capsules and drank 375ml of vodka. She recovered completely after vomiting and supportive assistance. She only complained of mild upper abdominal pain after recovery.

Ketoprofen sustained-release capsules pharmacology and toxicology:

1. Toxicological studies Carcinogenic effects and mutagenic effects on fertility disorders Long-term toxicity tests (up to 32 mg / kg / d; 96 mg / m ² / d) in mice have not shown potential carcinogenic effects. The highest recommended dose for human treatment is 300mg / day, and the body surface area of 60kg body weight is about 1.6m2, which is about 5mg / kg / d; 185mg / m2 / d. Based on body surface area calculations, the dose for mice is half of the highest recommended dose for humans. The 2-year long-term toxicity test (up to 6.0 mg / kg / d; 36 mg / m ² / d) in rats did not show potential tumorigenicity. All test groups except female rats were administered for up to 104 weeks (up to 6.0 mg / kg / d; 36 mg / m ² / d), but the experiment was terminated at 81 weeks because of the low survival rate. The remaining rats were gradually sacrificed after 87 weeks. In the control trial, the 104-week survival rate in the administration group was less than 6%. A long-term toxicity test of up to 12.5 mg / kg / d; (75 mg / m ² / d) for 2 years has also been performed, but because of the low survival rate, no conclusion can be drawn, but it can also prove that there is no potential carcinogenicity. Ketoprofen has also not been shown to be mutagenic in animal tests. Male rats take up to 9.0 mg / kg / d (54 mg / m ² / d, and have no effect on fertility behavior and fertility. Female rats take up to 6.0-9.0 mg / kg / d (36-54 mg / m ² / d), the number of children is reduced. 36mg / m ² / d is equivalent to one-fifth of the highest recommended daily dose of 185mg / m ² / d in humans. High-dose administration can lead to abnormal sperm production or reduced sperm counts in rats. Testicle weight can also be reduced in dogs and baboons. Teratogenicity studies Teratogenicity studies were performed on mice up to 12 mg / kg / d (36 mg / m ² / d) and rats up to 9 mg / kg / d ( 54mg / m ² / d), equivalent to one-fifth of the human daily recommended maximum dose of 185mg / m ² / d. It does not show teratogenic toxicity and fetal toxicity. In other rabbit tests, pregnant rabbits were produced. The toxic dose is only related to fetal toxicity, but not teratogenic. There are not enough controlled studies on pregnant women taking this product. However, because animal experiments cannot fully predict the effect of the drug on humans, it is not recommended for pregnant women unless treatment is evaluated Benefits outweigh risks.
2. Pharmacological effects Ketoprofen is a non-steroidal anti-inflammatory drug with antipyretic and analgesic effects. The anti-inflammatory, antipyretic and analgesic effects of this product have been proven through classic animal tests and in vitro testing systems. Its anti-inflammatory model shows that the anti-inflammatory effect of ketoprofen is achieved by blocking the synthesis of prostaglandins and leukotrienes, which has an anti-bradykinin effect and stabilizes the lysozyme cell membrane.

Ketoprofen sustained-release capsules pharmacokinetics:

This product can be quickly and completely absorbed in the gastrointestinal tract by oral administration. Healthy subjects reach a peak blood concentration of 3-5 hours after a single dose of 200 mg, and the Cmax is 3.46 ± 0.69ug / ml. This product is mainly in the form of plasma. The hydroxylated metabolites and the corresponding glucoglycerate metabolites exist. The binding rate of this product to albumin in plasma is 99%, and about 60% of the drugs are mainly excreted from the urine as glucuronic acid conjugates.