Routes of administration
Pamela E Macintyre, Suellen M Walker, David J Rowbotham in Clinical Pain Management, 2008
In surgical patients, oral ibuprofen arginine has a similar efficacy profile to intramuscular ketorolac, both being superior to placebo, 6[II] whilst in postcesarian section pain, the time to maximum analgesia of ibuprofen arginine is similar to intramuscular ketorolac.7[II] Feldene “melt,” a matrix of freeze-dried piroxicam in a fast dissolving excipient, rapidly dissolves in saliva and is swallowed as a solution. In a double-blind, randomized, double-dummy study, Feldene “melt” provided equivalent analgesia to rectal diclofenac when given 1 hour before surgery.8[II] Speed of absorption is also increased using a single isomer compared with a racemic mixture of the same NSAID. Median values for tmax are shorter (30 versus 75 minutes) and for Cmax are higher and less variable with dexketoprofen trometamol than for racemic ketoprofen.9[III] At least one clinical study has confirmed a rapid onset of analgesic action of dexketoprofen. Following removal of impacted third molars, the time to reduce pain by at least 50 percent was shorter in patients treated with oral dexketoprofen trometamol than in patients who had received oral ibuprofen (mean 0.9 versus 2.1 hours).10[II] There are a limited number of trials of the few coxibs that are licensed for postoperative pain relief. A Cochrane review has concluded that single-dose oral celecoxib is at least as effective as paracetamol for relieving postoperative pain, despite finding only two trials of celecoxib that met their inclusion criteria.11[I] A subsequent larger systematic review of 22 trials (2246 patients) concluded that preoperative oral coxibs (mainly celecoxib and rofecoxib) were effective in reducing postoperative pain, but were unable to draw any conclusions from three trials comparing coxibs with traditional NSAIDs.12[I]
Monographs of Topical Drugs that Have Caused Contact Allergy/Allergic Contact Dermatitis
Anton C. de Groot in Monographs in Contact Allergy, 2021
Dexketoprofen is a propionic acid derivative and nonsteroidal anti-inflammatory drug (NSAID) with analgesic, anti-inflammatory, and antipyretic properties. It is the (S)-enantiomer and active isomer of ketoprofen and works by blocking the action of cyclooxygenase. Dexketoprofen is indicated for short-term treatment of mild to moderate pain, including dysmenorrhea, musculoskeletal pain and toothache. It is available in topical and oral formulations (1).
A review of dexketoprofen trometamol in acute pain
Published in Current Medical Research and Opinion, 2019
Two RCTs of oral dexketoprofen in patients with postoperative pain following non-dental procedures were identified. Single doses of oral dexketoprofen trometamol provided effective analgesia in patients experiencing pain after orthopedic (hip arthroplasty) or gynecological (abdominal hysterectomy) surgery in double-blind placebo-controlled RCTs33,34. This was confirmed by a meta-analysis (which also included two unpublished studies), which found that more than half of recipients of dexketoprofen trometamol 12.5 or 25 mg experienced ≥50% pain relief at 4–6 hours compared with approximately one-third of placebo recipients (Table 1)22. No studies provided data on the use of rescue medication after single-dose dexketoprofen trometamol therapy in patients with non-dental postoperative pain.
Combined site-specific release retardant mini-matrix tablets (C-SSRRMT) for extended oral delivery of dexketoprofen trometamol: in vitro evaluation and single versus multiple doses pharmacokinetic study in human volunteers
Published in Drug Development and Industrial Pharmacy, 2019
Nabila M. Sweed, Emad B. Basalious, Samia A. Nour
Racemic ketoprofen is used as an analgesic and an anti-inflammatory agent, and is one of the most potent in vitro inhibitors of prostaglandin synthesis. The analgesic effect is due to the S (+)-enantiomer (dexketoprofen), while the R (–)-enantiomer has no analgesic activity. It was found that the separation of the R (–)-enantiomer from the racemic mixture results in doubling of the analgesic effect of dexketoprofen [1]. Dexketoprofen trometamol (DT), a water soluble salt of (S)-(+)-2-(3-benzoylphenyl)propionic acid, is well absorbed orally throughout the gastrointestinal tract [2]. The usual dose of dexketoprofen is 25 mg (equivalent to 36.9 mg of DT) every 8 h or 12.5 mg every 4–6 h. A maximum daily dose of 75 mg (equivalent to 110.7 mg of DT) may be applicable [3]. DT peak plasma levels are reached within 0.25–0.75 h. The current oral dexketoprofen tablets present two main drawbacks. The first is rapid elimination which necessitates three times daily administration due to the short elimination half-life of the drug (1.2–2.5 h) [3,4]. The second is gastrointestinal disturbances, such as gastrointestinal discomfort, nausea, diarrhea, and gastrointestinal bleeding [5]. The oral dosage form is the most widely accepted route of administration [6]. Therefore, a once-daily sustained-release oral formulation of DT can reduce the frequency of administration, adverse effects, and improve patient compliance.
The role of “Integrated Pulmonary Index” monitoring during morphine-based intravenous patient-controlled analgesia administration following supratentorial craniotomies: a prospective, randomized, double-blind controlled study
Published in Current Medical Research and Opinion, 2018
Eren Fatma Akcil, Ozlem Korkmaz Dilmen, Hayriye Ertem Vehid, Ercument Yentur, Yusuf Tunali
Patients were randomized to one of three groups using a computer-generated list (in opaque sealed envelopes). All patients were previously instructed on the PCA pumps (Abbott Provider, Chicago, IL) and numerical rating scale (NRS) from 0–10, with 0 being no pain and 10 being the worst pain imaginable. The PCA solutions of Groups 1 and 2 contained 100 mg morphine in 100 mL normal saline. In Group 1, PCA was set to administer a bolus dose of 1 mg morphine on demand with a lockout period of 10 min and a maximum 20 mg for 4 h. In Group 2, PCA was set to administer a bolus dose of 0.5 mg morphine on demand with a lockout period of 10 min and a maximum 10 mg for 4 h. In Group 3, PCA contained only 100 mL normal saline. Patient controlled analgesia (or placebo) was initiated as soon as the patient was admitted to the ICU post-operatively and continued for 24 hours in all groups. Dexketoprofen (50 mg IV) was first administered when the patient awakened and was repeated every 8 h in Group 3 for post-operative analgesia. After awakening, 2 mg IV morphine was administered as a rescue treatment in Groups 1 and 2, 1 g IV paracetamol was administered in Group 3 as a rescue treatment if the pain scores were above 4.
Related Knowledge Centers
- Cyclooxygenase
- Dysmenorrhea
- Stereoisomerism
- Prostaglandin
- Pain
- NONsteroidal Anti-Inflammatory Drug
- Over-The-Counter Drug
- Optical Rotation
- Ketoprofen
- Chiral Switch