Kelaprofen 10%
Kelaprofen 10% Uses, Dosage, Side Effects, Food Interaction and all others data.
Kelaprofen 10% is a non-steroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic actions. In addition to the inhibition of prostaglandin synthesis, it stabilizes lysosomal membranes in vitro and in vivo, inhibits leukotriene synthesis in vitro at high concentrations, and also exhibits antibradykinin activity in vivo. Kelaprofen 10% produces analgesia by inhibiting the synthesis of prostaglandins peripherally and centrally. It has also been suggested that Kelaprofen 10% causes the suppression of prostaglandin synthesis in the CNS (probably in the hypothalamus) leading to its antipyretic effect.
Kelaprofen 10% is rapidly and almost completely absorbed from the GI tract. It is approximately 99% bound to plasma protein, mainly albumin. Following single or multiple oral doses in healthy adults, the elimination half-life of the drug has averaged 1.1-4 hours. It is rapidly and extensively metabolized in the liver, principally via conjugation with glucoronic acid. Following a single oral dose of Kelaprofen 10% in healthy adults, about 50-90% of the drug is excreted in urine and about 1-8% in faeces within 1-5 days ; most urinary excretion occurs within 12-24 hours and most faecal excretion occurs within 24-48 hours. In case of IM injection, peak concentration of approximately 10 mg/L is reached at about 0.5-0.75 hour after a 100 mg dose. The elimination half-life is approximately 1.88 hour.
Kelaprofen 10% is a nonsteroidal anti-inflammatory agent (NSAIA) with analgesic and antipyretic properties. Kelaprofen 10% has pharmacologic actions similar to those of other prototypical NSAIDs, which inhibit prostaglandin synthesis. Kelaprofen 10% is used to treat rheumatoid arthritis, osteoarthritis, dysmenorrhea, and alleviate moderate pain.
| Trade Name | Kelaprofen 10% |
| Availability | Rx and/or OTC |
| Generic | Ketoprofen |
| Ketoprofen Other Names | Ketoprofen, Ketoprofeno |
| Related Drugs | Humira, Buprenex, aspirin, prednisone, ibuprofen, acetaminophen, tramadol, meloxicam, duloxetine, cyclobenzaprine |
| Type | |
| Formula | C16H14O3 |
| Weight | Average: 254.2806 Monoisotopic: 254.094294314 |
| Protein binding | 99% bound, primarily to albumin |
| Groups | Approved, Vet approved |
| Therapeutic Class | Drugs for Osteoarthritis, Drugs used for Rheumatoid Arthritis, Non-steroidal Anti-inflammatory Drugs (NSAIDs) |
| Manufacturer | |
| Available Country | New Zealand |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Kelaprofen 10% is used for musculoskeletal and joint disorders such as ankylosing spondylitis, osteoarthritis, and rheumatoid arthritis, in periarticular disorders such as bursitis and tendinitis, in mild to moderate pain such as dysmenorrhoea or postoperative pain, and in other painful and inflammatory conditions such as acute gout or soft tissue disorders.
Kelaprofen 10% is used for symptomatic relief of mild to moderate pain, such as postoperative (including that associated with dental surgery) postpartum and orthopedic (including musculoskeletal strains or sprains) pain and visceral pain associated with cancer.
Kelaprofen 10% IM injection is used for management of acute exacerbations of: Rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, periarticular conditions such as fibrositis, bursitis, capsulitis, tendinitis, and tenosynovitis, low back pain of musculoskeletal origin, sciatica, other musculoskeletal conditions, acute gout and control of pain and inflammation following orthopaedic surgery.
Kelaprofen 10% 2.5% Gel is an anti-inflammatory and analgesic preparation to be applied topically to the painful area. It is used for a short-term treatment for traumatic lessions (sprains, tendinitis, edema, bruises) and pain.
Kelaprofen 10% is also used to associated treatment for these conditions: Ankylosing Spondylitis (AS), Migraine, Osteoarthritis (OA), Pain, Postpartum pain, Primary Dysmenorrhoea, Rheumatoid Arthritis
How Kelaprofen 10% works
The anti-inflammatory effects of ketoprofen are believed to be due to inhibition cylooxygenase-2 (COX-2), an enzyme involved in prostaglandin synthesis via the arachidonic acid pathway. This results in decreased levels of prostaglandins that mediate pain, fever and inflammation. Kelaprofen 10% is a non-specific cyclooxygenase inhibitor and inhibition of COX-1 is thought to confer some of its side effects, such as GI upset and ulceration. Kelaprofen 10% is thought to have anti-bradykinin activity, as well as lysosomal membrane-stabilizing action. Antipyretic effects may be due to action on the hypothalamus, resulting in an increased peripheral blood flow, vasodilation, and subsequent heat dissipation.
Dosage
Kelaprofen 10% dosage
Kelaprofen 10% Tablet: Oral treatment with Kelaprofen 10% is 50-100 mg daily, taken with food to minimize gastrointestinal disturbance. For rheumatic disease, 100-200 mg daily in 2-4 divided doses with food. For pain and dysmenorrhoea, 50 mg up to 3 times daily.
Kelaprofen 10% SR Capsule: 100-200 mg once daily, depending on patient’s weight and on severity of symptomsKelaprofen 10% IM injection:
- Adults: 50 to 100 mg every four hours, repeated up to a maximum of 200 mg in twenty-four hours for up to 3 days. Following a satisfactory response oral therapy should be instituted with Kelaprofen 10% tablet. It is recommended that the injection should not normally be continued for longer than three days.
- Elderly: As with other medications it is generally advisable in the elderly to begin ketoprofen therapy at the lower end of the dose range and to maintain such patients on the lowest effective dosage.
- Paediatric dosage: Not established for intramuscular use. It is not used as intravenous injection.
Kelaprofen 10% 2.5% Gel: Thisis to be applied to the painful area twice daily.The gel can be used with an occlusive dressing. Rub gently into the skin to ensure penetration.
For children: There is no contraindication to the use of this drug in children, but the appropriate dosage has not yet been established. Dosage of Kelaprofen 10% must be carefully adjusted according to individual requirements and response, using the lower possible effective dosage. Dosage exceeding 300 mg daily has not been adequately studied and are not recommended.
Suppository: 1 suppository (100 mg) late at night supplemented as required with Kelaprofen 10% capsules during daytime. Kelaprofen 10% suppositories are especially appropriate for controlling overnight symptoms (severity of night and morning pain; duration and severity of morning stiffness). Suppositoriesadministered late at night provide more consistent effective control of overnight symptoms than oral medication.
Side Effects
Adverse reactions to Kelaprofen 10% are usually mild and mainly involve the GI tract, particularly upper GI tract. Most Kelaprofen 10%-induced adverse effects occur during the first month of treatment, and the frequency of adverse effects generally decreases with continued therapy.
Adverse reactions involving digestive system are dyspepsia, nausea, abdominal pain, diarrhoea, constipation, flatulence, anorexia, vomiting, stomatitis and that involving nervous system are headache, dizziness, malaise, depression, nervousness, dreams, etc. Other reactions are tinnitus, visual disturbance, rash, impairment of renal function, signs or symptoms of urinary-tract irritation.
Toxicity
LD50=62.4 mg/kg (rat, oral).
Symptoms of overdose include drowsiness, vomiting and abdominal pain.
Side effects are usually mild and mainly involved the GI tract. Most common adverse GI effect is dyspepsia (11% of patients). May cause nausea, diarrhea, abdominal pain, constipation and flatulence in greater than 3% of patients.
Precaution
Kelaprofen 10% should be used with caution in patients who may be adversely affected by a prolongation of bleeding time (e.g. patients receiving anticoagulant therapy), since the drug may inhibit platelet function.
Kelaprofen 10% should be used with caution in patients with heart failure, hypertension, or other conditions associated with fluid retention, since peripheral edema has been observed in some patients receiving the drug.
Liver function should be monitored periodically during long-term Kelaprofen 10% therapy.
Kelaprofen 10% injection must not be given intravenously.
Kelaprofen 10% gel should not be applied to patients who have allergy toketoprofen, other anti-inflammatory agents and aspirin.
Interaction
As Kelaprofen 10% may cause GI bleeding, inhibit platelet aggregation and prolong bleeding time, the drug should be used with caution and the patient should be carefully observed if the drug is used concomitantly with any anticoagulant or thrombolytic agent. Concomitant administration of Kelaprofen 10% and hydrochlorothiazide has resulted in decreased urinary excretion of potassium and chloride compared with hydrochlorothiazide alone. Kelaprofen 10% and salicylates appear to interact in a complex manner and they should not be used concomitantly. Concomitant use of Kelaprofen 10% and probenecid is also not recommended. Kelaprofen 10% should be avoided in patients receiving methotrexate.
Food Interaction
- Avoid alcohol.
- Take with food. Food reduces irritation.
Kelaprofen 10% Alcohol interaction
[Moderate] GENERALLY AVOID:
The concurrent use of aspirin or nonsteroidal anti-inflammatory drugs (NSAIDs) and ethanol may lead to gastrointestinal (GI) blood loss.
The mechanism may be due to a combined local effect as well as inhibition of prostaglandins leading to decreased integrity of the GI lining.
Patients should be counseled on this potential interaction and advised to refrain from alcohol consumption while taking aspirin or NSAIDs.
Kelaprofen 10% Hypertension interaction
[Major] Fluid retention and edema have been reported in association with the use of nonsteroidal anti-inflammatory drugs (NSAIDs).
Therapy with NSAIDs should be administered cautiously in patients with preexisting fluid retention, hypertension, or a history of heart failure.
Blood pressure and cardiovascular status should be monitored closely during the initiation of NSAID treatment and throughout the course of therapy.
Hypertension interaction[Moderate] Nonsteroidal anti-inflammatory drugs (NSAIDs), including topicals, can lead to new onset of hypertension or worsening of preexisting hypertension, either of which can contribute to the increased incidence of cardiovascular events.
NSAIDs should be used with caution in patients with hypertension.
Blood pressure should be monitored closely during the initiation of NSAID therapy and throughout the course of therapy.
Kelaprofen 10% Drug Interaction
Moderate: aspirin, aspirin, duloxetine, duloxetine, escitalopram, escitalopramUnknown: zolpidem, zolpidem, pregabalin, pregabalin, esomeprazole, esomeprazole, acetaminophen, acetaminophen, acetaminophen, acetaminophen, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol
Kelaprofen 10% Disease Interaction
Major: asthma, fluid retention, GI toxicity, rash, renal toxicities, thrombosisModerate: anemia, heart failure, hepatotoxicity, hyperkalemia, hypertension, platelet aggregation inhibition
Elimination Route
Kelaprofen 10% is rapidly and well-absorbed orally, with peak plasma levels occurring within 0.5 to 2 hours.
Half Life
Conventional capsules: 1.1-4 hours
Extended release capsules: 5.4 hours due to delayed absorption (intrinsic clearance is same as conventional capsules)
Clearance
- Oral-dose cl=6.9 +/- 0.8 L/h [Kelaprofen 10% Immediate-release capsules (4 × 50 mg)]
- Oral-dose cl=6.8 +/- 1.8 L/h [Kelaprofen 10% Extended-release capsules (1 × 200 mg)]
- 0.08 L/kg/h
- 0.7 L/kg/h [alcoholic cirrhosis patients]
Elimination Route
In a 24 hour period, approximately 80% of an administered dose of ketoprofen is excreted in the urine, primarily as the glucuronide metabolite.
Pregnancy & Breastfeeding use
Embryopathic effects have not been recorded with Kelaprofen 10%, but it is recommended to avoid medication during pregnancy. Trace amounts of the drug appear in breast milk and it should not be used during breast feeding unless unavoidable.
Contraindication
Kelaprofen 10% is contraindicated in patients with known hypersensitivity to the drug. Kelaprofen 10% is contraindicated in patients in whom asthma, urticaria, or other sensitivity reaction is precipitated by aspirins or other NSAIDs, since severe, rarely fatal, anaphylactic reactions to Kelaprofen 10% have been reported in these patients.
The risk of potentially serious adverse GI effects should be considered in patients receiving Kelaprofen 10%, particularly in patients receiving chronic therapy with the drug. Kelaprofen 10% should be used in patients with GI bleeding or active peptic ulceration only when the potential benefits justify the possible risks.
Storage Condition
Store at cool and dry place, protect from light and moisture. Keep out of the children’s reach.
Innovators Monograph
You find simplified version here Kelaprofen 10%
Kelaprofen 10% contains Ketoprofen see full prescribing information from innovator Kelaprofen 10% Monograph, Kelaprofen 10% MSDS, Kelaprofen 10% FDA label
FAQ
What is the Kelaprofen 10% used for?
Kelaprofen 10% is used to treat mild to moderate pain, such as menstrual cramps or arthritis. Kelaprofen 10% is used to relieve minor aches and pain from headaches, menstrual periods, toothaches, the common cold, muscle aches, and backaches, and to reduce fever. Kelaprofen 10% is in a class of medications called NSAIDs.
How safe is Kelaprofen 10%?
Kelaprofen 10% can increase your risk of fatal heart attack or stroke, even if you don't have any risk factors. Do not use this medicine just before or after heart bypass surgery (coronary artery bypass graft, or CABG). Kelaprofen 10% may also cause stomach or intestinal bleeding, which can be fatal.
How does Kelaprofen 10% work?
Kelaprofen 10% works by reducing hormones that cause inflammation and pain in the body.
What are the common side effects of Kelaprofen 10%?
Common side effects of Kelaprofen 10% are include of:
- constipation
- diarrhea
- sores in the mouth
- headache
- dizziness
- nervousness
- drowsiness
- difficulty falling asleep or staying asleep
- ringing in the ears
Is Kelaprofen 10% safe during pregnancy?
Kelaprofen 10% is only recommended for use during pregnancy when benefits outweigh the risks.
Is Kelaprofen 10% safe during breastfeeding?
Use of Kelaprofen 10% is compatible with prolonged breastfeeding, after the early post-partum stage.
Can I drink alcohol with Kelaprofen 10%?
Do not drink alcohol while taking Kelaprofen 10%. Alcohol can increase your risk of stomach bleeding caused by Kelaprofen 10%.
Can I drink alcohol with Kelaprofen 10%?
Do not drive, use machinery, or do anything that needs alertness until you can do it safely. Avoid alcoholic beverages. Talk to your doctor if you are using marijuana (cannabis). This medicine may cause stomach/intestinal bleeding.
How often can I take Kelaprofen 10%?
The capsules are usually taken three or four times a day for arthritis or every 6 to 8 hours as needed for pain.
Can I take Kelaprofen 10% on an empty stomach?
Ask your doctor or pharmacist if you have any questions. To lessen stomach upset, you may take this medicine with food, milk, or antacid unless your doctor tells you otherwise.
How much Kelaprofen 10% can I take daily?
Adults, 25 to 50 milligrams (mg) every 6 to 8 hours as needed. Some people may need to take as much as 75 mg every 6 to 8 hours. Doses larger than 75 mg are not likely to give better relief. Children, Use and dose must be determined by your doctor.
How long does Kelaprofen 10% take to work?
Typically, pain relief may occur within 30 minutes and last for up to six hours after taking a Kelaprofen 10% dose.
How long does Kelaprofen 10% stay in my system?
Kelaprofen 10% is available in oral form and reaches its peak plasma level in 0.5 to 2 hours. Its half-life is 2.4 hours, with an analgesic duration of 4 to 6 hours.
How long can I take Kelaprofen 10%?
Do not increase your dose, take it more frequently, or take it for a longer time than prescribed. Do not take the over-the-counter product for more than 10 days unless otherwise directed.
What happens if I miss a dose?
Since Kelaprofen 10% is used when needed, you may not be on a dosing schedule. Skip any missed dose if it's almost time for your next dose. Do not use two doses at one time.
What happens if I overdose?
Seek emergency medical attention. Overdose symptoms may include nausea, vomiting, stomach pain, drowsiness, black or bloody stools, coughing up blood, shallow breathing, fainting, or coma.
Who should not take Kelaprofen 10%?
You should not use ketoprofen if you are allergic to it, or if you have ever had an asthma attack or severe allergic reaction after taking aspirin or an NSAID.Ask a doctor or pharmacist if this medicine is safe to use if you have ever had:
heart disease, high blood pressure, high cholesterol, diabetes, or if you smoke;a heart attack, stroke, or blood clot;stomach ulcers or bleeding;asthma; liver or kidney disease; or fluid retention.
Can Kelaprofen 10% affects my heart ?
Kelaprofen 10% can increase your risk of fatal heart attack or stroke, especially if you use it long term or take high doses, or if you have heart disease.
Can Kelaprofen 10% affects my kidney?
Acute renal failure is a known complication with oral non-steroidal anti-inflammatory drugs. In contrast, topical application of such drugs is usually considered safe because of marginal percutaneous absorption (5-8%).
Can Kelaprofen 10% affects my liver?
Kelaprofen 10% has been linked to a low rate of serum enzyme elevations during therapy and to rare instances of clinically apparent acute liver injury.
Can Kelaprofen 10% make me sleepy?
Lightheadedness, drowsiness, loss of appetite, or headache may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.
Does Kelaprofen 10% raise blood pressure?
Kelaprofen 10% can increase your blood pressure, so your doctor may monitor it regularly.
