Nasaflam

Nasaflam Uses, Dosage, Side Effects, Food Interaction and all others data.

Ketoprofen 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. Ketoprofen produces analgesia by inhibiting the synthesis of prostaglandins peripherally and centrally. It has also been suggested that Ketoprofen causes the suppression of prostaglandin synthesis in the CNS (probably in the hypothalamus) leading to its antipyretic effect.

Ketoprofen 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 Ketoprofen 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.

Ketoprofen is a nonsteroidal anti-inflammatory agent (NSAIA) with analgesic and antipyretic properties. Ketoprofen has pharmacologic actions similar to those of other prototypical NSAIDs, which inhibit prostaglandin synthesis. Ketoprofen is used to treat rheumatoid arthritis, osteoarthritis, dysmenorrhea, and alleviate moderate pain.

Nasaflam
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Nasaflam
Generic	Ketoprofen + Ketoprofen
Weight	50mg, 100mg
Type	Tablet
Therapeutic Class
Manufacturer	Pratapa Nirmala
Available Country	Indonesia
Last Updated:	September 19, 2023 at 7:00 am

Uses

Ketoprofen 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.

Ketoprofen 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.

Ketoprofen 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.

Ketoprofen 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.

Nasaflam is also used to associated treatment for these conditions: Ankylosing Spondylitis (AS), Migraine, Osteoarthritis (OA), Pain, Postpartum pain, Primary Dysmenorrhoea, Rheumatoid Arthritis

How Nasaflam 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. Ketoprofen 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. Ketoprofen 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

Nasaflam dosage

Ketoprofen Tablet: Oral treatment with Ketoprofen 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.

Ketoprofen SR Capsule: 100-200 mg once daily, depending on patient’s weight and on severity of symptomsKetoprofen 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 Ketoprofen 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.

Ketoprofen 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 Ketoprofen 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 Ketoprofen capsules during daytime. Ketoprofen 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 Ketoprofen are usually mild and mainly involve the GI tract, particularly upper GI tract. Most Ketoprofen-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

Ketoprofen 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.

Ketoprofen 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 Ketoprofen therapy.

Ketoprofen injection must not be given intravenously.

Ketoprofen gel should not be applied to patients who have allergy toketoprofen, other anti-inflammatory agents and aspirin.

Interaction

As Ketoprofen 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 Ketoprofen and hydrochlorothiazide has resulted in decreased urinary excretion of potassium and chloride compared with hydrochlorothiazide alone. Ketoprofen and salicylates appear to interact in a complex manner and they should not be used concomitantly. Concomitant use of Ketoprofen and probenecid is also not recommended. Ketoprofen should be avoided in patients receiving methotrexate.

Elimination Route

Ketoprofen 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 [Ketoprofen Immediate-release capsules (4 × 50 mg)]
Oral-dose cl=6.8 +/- 1.8 L/h [Ketoprofen 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 Ketoprofen, 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

Ketoprofen is contraindicated in patients with known hypersensitivity to the drug. Ketoprofen 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 Ketoprofen have been reported in these patients.

The risk of potentially serious adverse GI effects should be considered in patients receiving Ketoprofen, particularly in patients receiving chronic therapy with the drug. Ketoprofen should be used in patients with GI bleeding or active peptic ulceration only when the potential benefits justify the possible risks.