Compounds > diclofenac hydroxyethylpyrrolidine
Page last updated: 2024-12-07

diclofenac hydroxyethylpyrrolidine

Cross-References

ID SourceID
PubMed CID114753
CHEMBL ID1201180
CHEBI ID48296
SCHEMBL ID1006944
MeSH IDM0176789

Synonyms (34)

Synonym
diclofenac-n-(2-hydroxyethyl) pyrrolidine
n-(2-hydroxyethyl)pyrrolidinium (2-((2,6-dichlorophenyl)amino)phenyl)acetate
flector
CHEBI:48296 ,
diclofenac hydroxyethylpyrrolidine
119623-66-4
diclofenac epolamine
diep
diclofenac 1-(2-hydroxyethyl)pyrrolidinium salt
diclofenac-epolamine
diclofenac epolaminum
CHEMBL1201180
D07818
flector (tn)
dhep plaster
unii-x5f8ekl9zg
x5f8ekl9zg ,
diclofenac epolamine [who-dd]
diclofenac epolamine [orange book]
diclofenac epolamine [vandf]
diclofenac hydroxyethylpirrolidine
licart
diclofenac epolamine [mart.]
S5737
SCHEMBL1006944
DTXSID80152531 ,
2-[2-(2,6-dichloroanilino)phenyl]acetic acid;2-pyrrolidin-1-ylethanol
Q27121125
diclofenac epolamine (mart.)
1-(2-hydroxyethyl)pyrrolidinium (2-((2,6-dichlorophenyl)amino)phenyl)acetate
dtxcid5075022
HY-109547
CS-0031292
AKOS040745030

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" Fourteen adverse events (none serious) in nine patients (8."( Safety and Efficacy of the FLECTOR (Diclofenac Epolamine) Topical System in Children with Minor Soft Tissue Injuries: A Phase IV Non-randomized Clinical Trial.
Frangione, V; Hoehler, FK; Jones, C; Jones, CA; Ledesma, G; Wisman, PP, 2022)		0.72
"The FLECTOR topical system safely and effectively provided pain relief for minor soft tissue injuries in the pediatric population, with minimal systemic nonsteroidal anti-inflammatory drug exposure and low potential risk of local or systemic adverse events."( Safety and Efficacy of the FLECTOR (Diclofenac Epolamine) Topical System in Children with Minor Soft Tissue Injuries: A Phase IV Non-randomized Clinical Trial.
Frangione, V; Hoehler, FK; Jones, C; Jones, CA; Ledesma, G; Wisman, PP, 2022)		0.72
" This study shows that FDETS can safely and effectively provide pain relief for soft tissue injuries in children, with minimal systemic NSAID exposure and a low potential risk of either local or systemic adverse events."( Safety and Efficacy of the FLECTOR (Diclofenac Epolamine) Topical System in Children with Minor Soft Tissue Injuries: A Phase IV Non-randomized Clinical Trial.
Frangione, V; Hoehler, FK; Jones, C; Jones, CA; Ledesma, G; Wisman, PP, 2022)		0.72
" No serious adverse events (SAEs) were registered, and the most commonly detected adverse events were skin reactions at the application site."( Efficacy and safety of Diclofenac sodium plaster in patients with acute pain of the limbs: a randomized, placebo and active-controlled, double-blind, parallel-group trial.
Barbaro, B; Giordan, N; Gruber, G; Pabst, H; Picciotto, R, 2023)		0.91

Pharmacokinetics

ExcerptReferenceRelevance
" The paper deals with local tolerability and pharmacokinetic (percutaneous absorption) studies carried out both on animals and on volunteers."( Local tolerability and pharmacokinetic profile of a new transdermal delivery system, diclofenac hydroxyethylpyrrolidine plaster.
Assandri, A; Canali, S; Giachetti, C, 1993)		0.51
" Oral and topical diclofenac had no pharmacokinetic effects on furosemide."( Randomized, open-label, 5-way crossover study to evaluate the pharmacokinetic/pharmacodynamic interaction between furosemide and the non-steroidal anti-inflammatory drugs diclofenac and ibuprofen in healthy volunteers.
Jacobs, D; McGuinness, N; Paterson, CA; Rasmussen, S; Youngberg, SP, 2011)		0.37
" Furosemide also affected plasma and urine pharmacokinetic profiles."( Randomized, open-label, 5-way crossover study to evaluate the pharmacokinetic/pharmacodynamic interaction between furosemide and the non-steroidal anti-inflammatory drugs diclofenac and ibuprofen in healthy volunteers.
Jacobs, D; McGuinness, N; Paterson, CA; Rasmussen, S; Youngberg, SP, 2011)		0.37

Bioavailability

ExcerptReferenceRelevance
" We performed a bioavailability randomized, cross-over study to compare the plasma profiles of diclofenamic acid after repeated epicutaneous administration of the new topical formulation with those of the marketed DHEP formulation without lecithin."( Effect of lecithin on epicutaneous absorption of diclofenac epolamine.
Conte, A; Mautone, G; Petrini, M; Ronca, G, 2002)		0.31
" The bioavailability in terms of systemic exposure from the patch compared with oral intake (75 mg/day) is in the order of 1%."( Diclofenac epolamine (Flector) patch: evidence for topical activity.
Petersen, B; Rovati, S, 2009)		0.35
"The data was consistent with the concept that heparin increased the clinical activity of the DHEP plus medicated plaster versus the reference DHEP medicated plaster through improved bioavailability due to enhanced movement of diclofenac from the plaster."( Rationale and evidence for the incorporation of heparin into the diclofenac epolamine medicated plaster.
Jones, C; Nencioni, A; Rainsford, KD; Roberts, MS, 2019)		0.51

Dosage Studied

ExcerptRelevanceReference
"A phamacokinetic study in man has been made of a new dosage form of diclofenac hydroxyethylpyrrolidine (DIEP); soluble salt packed in sachets was compared with diclofenac sodium as enteric coated tablets."( Comparative bioavailability of diclofenac hydroxyethylpyrrolidine vs diclofenac sodium in man.
Lualdi, P; Maggi, CA; Mautone, G, 1990)		0.8
"The aim of this study was the assessment of blood and synovial levels of diclofenac after repeated epicutaneous dosing with DHEP plasters in patients with joint effusion."( Pharmacokinetics of diclofenac hydroxyethylpyrrolidine (DHEP) plasters in patients with monolateral knee joint effusion.
Gallacchi, G; Marcolongo, R, 1993)		0.61
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
organic salt
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Research

Studies (44)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's14 (31.82)18.2507
2000's12 (27.27)29.6817
2010's14 (31.82)24.3611
2020's4 (9.09)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 19.66

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index19.66 (24.57)
Research Supply Index4.20 (2.92)
Research Growth Index4.57 (4.65)
Search Engine Demand Index18.60 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (19.66)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials21 (46.67%)5.53%
Reviews6 (13.33%)6.00%
Case Studies1 (2.22%)4.05%
Observational0 (0.00%)0.25%
Other17 (37.78%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (16)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Efficacy of PENNSAID® for Pain Management in the Emergency Department [NCT01350622]0 participants (Actual)Interventional2011-12-31Withdrawn(stopped due to Study never initiated)
Pilot Study to Test Uniformity of Transdermal Drug Delivery to the Breast Using Diclofenac Epolamine as a Model [NCT01380353]Early Phase 130 participants (Actual)Interventional2011-06-30Completed
The Relationship Between Patient Preferences, Analgesic Delivery Method and Pain Reduction in Spine Patients [NCT01263652]0 participants (Actual)Interventional2010-12-31Withdrawn(stopped due to inability to complete recruitment as planned)
ESPBs vs TAPs for Satisfactory Analgesia Following DIEP Surgery [NCT06091241]102 participants (Anticipated)Interventional2023-11-01Not yet recruiting
Randomized, Double Blind, Parallel-groups, Non-inferiority Versus Flector® and Superiority Versus Placebo, Phase III Clinical Trial With Diclofenac Sodium 140 mg Medicated Plaster in Patients With Impact Injuries of the Limbs [NCT04976088]Phase 3214 participants (Actual)Interventional2018-05-25Completed
Multicenter, Open-Label Study to Assess the Effectiveness and Safety of FLECTOR Patch for Treatment of Acute Back Strain [NCT01054820]Phase 4123 participants (Actual)Interventional2010-01-31Completed
Intramuscular Diclofenac vs. Placebo in a Randomized Double Blind Controlled Trial, In Post ERCP Pancreatitis. [NCT01946984]Phase 1182 participants (Actual)Interventional2012-06-30Completed
Comparative Bioavailability and Local Tolerability of Two Topical Diclofenac Plasters Applied Once and Twice a Day to Healthy Volunteers With a Repeat Dose Regimen [NCT04585321]Phase 152 participants (Actual)Interventional2017-11-28Completed
[NCT00514748]0 participants Interventional2007-01-31Completed
Optimation of Treatment of the Sprained Ankle by Help of NSAID-Plaster (Flector). A Questionnaire. [NCT00284765]200 participants Interventional2006-02-28Recruiting
Use of Dermal Microdialysis to Evaluate the Effect of Skin Properties and Application Site on the Topical Bioequivalence of Diclofenac: The Main Study [NCT01592019]Early Phase 16 participants (Actual)Interventional2012-04-30Completed
Randomized, Double-Blind, Multiple-Center, Placebo-Controlled Study Comparing the Safety and Efficacy of Generic Diclofenac Epolamine to Flector® Patch in the Treatment of Acute Pain Due to Minor Ankle Sprain [NCT02324270]Phase 3658 participants (Actual)Interventional2014-05-31Completed
Evaluation of Bioavailability of Diclofenac Dermal Products [NCT03145259]Early Phase 112 participants (Actual)Interventional2017-04-19Completed
Non-contrast Magnetic Resonance Angiography Efficacy and Safety Assessment for Perforators Mapping in Deep Inferior Epigastric Perforator Flap Breast Reconstruction [NCT06061835]135 participants (Anticipated)Interventional2023-05-06Recruiting
An Open-label, Prospective, Uncontrolled Study of the Safety and Local Tolerability of the Diclofenac Epolamine Patch (Flector Patch) in Pediatric Patients With Minor Soft Tissue Injuries [NCT02132247]Phase 4104 participants (Actual)Interventional2014-05-31Completed
A Multi-center, Prospective, Open-label, Controlled Study of the Pharmacokinetics and Safety of the LicartTM Topical System in Pediatric and Adult Participants With Minor Soft Tissue Injuries [NCT05171673]Phase 3150 participants (Anticipated)Interventional2021-10-31Recruiting
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT01054820 (11) [back to overview]Mean Change From Baseline to End of Treatment (EOT) in Response to Modified Brief Pain Inventory (mBPI) Question 5: Average Pain Over the Last 24 Hours
NCT01054820 (11) [back to overview]Mean Change From Baseline to EOT in Beck Depression Inventory® Il
NCT01054820 (11) [back to overview]Mean Change From Baseline to EOT in Response to Modified Brief Pain Inventory (mBPI) Question 3: Pain at Its Worst in the Last 24 Hours
NCT01054820 (11) [back to overview]Mean Change From Baseline to EOT in Response to Modified Brief Pain Inventory (mBPI) Question 4: Pain at Its Least in the Last 24 Hours
NCT01054820 (11) [back to overview]Mean Change From Baseline to EOT in Response to Modified Brief Pain Inventory (mBPI) Question 6: Pain Right Now
NCT01054820 (11) [back to overview]Mean Change From Baseline to EOT in Response to Modified Brief Pain Inventory (mBPI) Question 8: Percent Reduction in Pain From Baseline
NCT01054820 (11) [back to overview]Number of Participants Per Global Pain Relief Scores at the End of Treatment as Assessed by the Investigator
NCT01054820 (11) [back to overview]Number of Participants Per Global Pain Relief Scores at the End of Treatment as Assessed by the Participant
NCT01054820 (11) [back to overview]Number of Participants Per Patch Satisfaction Response at the End of Treatment as Assessed by Participant
NCT01054820 (11) [back to overview]Number of Participants Per Patch Satisfaction Response at the End of Treatment as Assessed by the Investigator
NCT01054820 (11) [back to overview]Number of Participants With Change From Baseline (Bsl) to EOT in Response to Modified Brief Pain Inventory (mBPI) Question 1: Pain Other Than Everyday Kind of Pain
NCT02132247 (4) [back to overview]Dermatologic Assessment at the Patch Application Site
NCT02132247 (4) [back to overview]Investigator Assessment of the Global Response to Therapy on a 5-point Scale
NCT02132247 (4) [back to overview]Patient Assessment of Pain on a 6-point Scale
NCT02132247 (4) [back to overview]Plasma Concentration of Diclofenac
NCT02324270 (2) [back to overview]Visual Analogue Scale (VAS) Scores at Baseline and Post Treatment
NCT02324270 (2) [back to overview]Visual Analogue Scale (VAS) Scores at Baseline and Post Treatment
NCT03145259 (1) [back to overview]Serum Diclofenac Concentrations

Mean Change From Baseline to End of Treatment (EOT) in Response to Modified Brief Pain Inventory (mBPI) Question 5: Average Pain Over the Last 24 Hours

Participant-rated instrument to assess functional activities (general activity, mood, walking ability, relations with other people, sleep, normal work, and enjoyment of life) in past 24 hours. Question 5: Please rate your pain by marking the box beside the number that best describes your pain on the average (over the last 24 hours); rated on an 11 point Likert rating scale ranging from 0 (no pain) to 10 (pain as bad as you can imagine). (NCT01054820)
Timeframe: Baseline, End of Treatment (last visit up to Day 15)

Interventionscores on a scale (Mean)
BaselineChange from baseline to EOT
FLECTOR® Patch (Diclofenac Epolamine Topical Patch) 1.3%.6.46-3.95

[back to top]

Mean Change From Baseline to EOT in Beck Depression Inventory® Il

The Beck Depression Inventory® II consisted of 21 items, each with 4 categorical responses ranging from 0 (I do not feel sad) to 3 (I am so sad or unhappy that I can't stand it) with maximum possible score of 63; increase in the number reflected an increase in severity. Total Beck Depression Inventory® II scores classified as follows: 1 to 10=normal ups and downs; 11 to 16=mild mood disturbance; 17 to 20=borderline clinical depression; 21 to 30=moderate depression; 31 to 40=severe depression; and >40=extreme depression. (NCT01054820)
Timeframe: Baseline, End of Treatment (last visit up to Day 15)

Interventionscores on a scale (Mean)
BaselineChange from baseline to EOT
FLECTOR® Patch (Diclofenac Epolamine Topical Patch) 1.3%.3.44-1.54

[back to top]

Mean Change From Baseline to EOT in Response to Modified Brief Pain Inventory (mBPI) Question 3: Pain at Its Worst in the Last 24 Hours

Participant-rated instrument to assess functional activities (general activity, mood, walking ability, relations with other people, sleep, normal work, and enjoyment of life) in past 24 hours. Question 3: Rate your pain at its worst in the last 24 hours; rated on an 11 point Likert rating scale ranging from 0 (no pain) to 10 (pain as bad as you can imagine). (NCT01054820)
Timeframe: Baseline, End of Treatment (last visit up to Day 15)

Interventionscores on a scale (Mean)
BaselineChange from baseline to EOT
FLECTOR® Patch (Diclofenac Epolamine Topical Patch) 1.3%.7.59-4.50

[back to top]

Mean Change From Baseline to EOT in Response to Modified Brief Pain Inventory (mBPI) Question 4: Pain at Its Least in the Last 24 Hours

Participant-rated instrument to assess functional activities (general activity, mood, walking ability, relations with other people, sleep, normal work, and enjoyment of life) in past 24 hours. Question 4: Rate your pain at its least in the last 24 hours; rated on an 11 point Likert rating scale ranging from 0 (no pain) to 10 (pain as bad as you can imagine). (NCT01054820)
Timeframe: Baseline, End of Treatment (last visit up to Day 15)

Interventionscores on a scale (Mean)
BaselineChange from baseline to EOT
FLECTOR® Patch (Diclofenac Epolamine Topical Patch) 1.3%.5.46-3.50

[back to top]

Mean Change From Baseline to EOT in Response to Modified Brief Pain Inventory (mBPI) Question 6: Pain Right Now

Participant-rated instrument to assess functional activities (general activity, mood, walking ability, relations with other people, sleep, normal work, and enjoyment of life) in past 24 hours. Question 6: Rate your pain right now; rated on an 11 point Likert rating scale ranging from 0 (no pain) to 10 (pain as bad as you can imagine). (NCT01054820)
Timeframe: Baseline, End of Treatment (last visit up to Day 15)

Interventionscores on a scale (Mean)
BaselineChange from baseline to EOT
FLECTOR® Patch (Diclofenac Epolamine Topical Patch) 1.3%.6.49-4.28

[back to top]

Mean Change From Baseline to EOT in Response to Modified Brief Pain Inventory (mBPI) Question 8: Percent Reduction in Pain From Baseline

Participant-rated instrument to assess functional activities (general activity, mood, walking ability, relations with other people, sleep, normal work, and enjoyment of life) in past 24 hours. Question 8: Rate your percent reduction in pain from Baseline (0% = no relief to 100% = complete relief). (NCT01054820)
Timeframe: Baseline, End of Treatment (last visit up to Day 15)

Interventionpercent (Mean)
BaselineChange from baseline to EOT
FLECTOR® Patch (Diclofenac Epolamine Topical Patch) 1.3%.2.9467.30

[back to top]

Number of Participants Per Global Pain Relief Scores at the End of Treatment as Assessed by the Investigator

Participants' global pain relief as assessed by investigator using a 5-point scale where 5 = complete relief, 4=a lot of improvement, 3=moderate improvement, 2=slight improvement, and 1=no change. (NCT01054820)
Timeframe: End of Treatment (up to Day 15)

Interventionparticipants (Number)
5=Complete Relief4=A Lot Of Improvement3=Moderate Improvement2=Slight Improvement1=No Change
FLECTOR® Patch (Diclofenac Epolamine Topical Patch) 1.3%.58428105

[back to top]

Number of Participants Per Global Pain Relief Scores at the End of Treatment as Assessed by the Participant

Global pain relief as assessed by participant using a 5-point scale where 5 = complete relief, 4=a lot of improvement, 3=moderate improvement, 2=slight improvement, and 1=no change. (NCT01054820)
Timeframe: End of Treatment (up to Day 15)

Interventionparticipants (Number)
5=Complete Relief4=A Lot Of Improvement3=Moderate Improvement2=Slight Improvement1=No Change
FLECTOR® Patch (Diclofenac Epolamine Topical Patch) 1.3%.534212124

[back to top]

Number of Participants Per Patch Satisfaction Response at the End of Treatment as Assessed by Participant

Participant satisfaction with the FLECTOR® Patch rated on a 5-point scale scored as 5=Very Satisfied, 4=Satisfied, 3=No Preference, 2=Dissatisfied, and 1=Very Dissatisfied. (NCT01054820)
Timeframe: End of Treatment (last visit up to Day 15)

Interventionparticipants (Number)
5=Very Satisfied4=Satisfied3=No Preference2=Dissatisfied1=Very Dissatisfied
FLECTOR® Patch (Diclofenac Epolamine Topical Patch) 1.3%.6345681

[back to top]

Number of Participants Per Patch Satisfaction Response at the End of Treatment as Assessed by the Investigator

Investigator's assessment of participants' satisfaction with the FLECTOR® Patch rated on a 5-point scale scored as 5=Very Satisfied, 4=Satisfied, 3=No Preference, 2=Dissatisfied, and 1=Very Dissatisfied. (NCT01054820)
Timeframe: End of Treatment (last visit up to Day 15)

Interventionparticipants (Number)
5=Very Satisfied4=Satisfied3=No Preference2=Dissatisfied1=Very Dissatisfied
FLECTOR® Patch (Diclofenac Epolamine Topical Patch) 1.3%.6639981

[back to top]

Number of Participants With Change From Baseline (Bsl) to EOT in Response to Modified Brief Pain Inventory (mBPI) Question 1: Pain Other Than Everyday Kind of Pain

Participant-rated instrument to assess functional activities (general activity, mood, walking ability, relations with other people, sleep, normal work, and enjoyment of life) in past 24 hours. Question 1: Have you had pain other than everyday kinds of pain?; response = Yes or No. (NCT01054820)
Timeframe: Baseline, End of Treatment (last visit up to Day 15)

Interventionparticipants (Number)
Change at EOT: Bsl=Yes, EOT=YesChange at EOT: Bsl=Yes, EOT=NoChange at EOT: Bsl=No, EOT=YesChange at EOT: Bsl=No, EOT=No
FLECTOR® Patch (Diclofenac Epolamine Topical Patch) 1.3%.932109

[back to top]

Dermatologic Assessment at the Patch Application Site

None - 0; Faint redness - 1; Moderate redness - 2; Intense redness - 3; Redness with edema or papules - 4; Redness with weeping vesicles, blisters or bullae - 5; Redness with extension of effect beyond margin of contact site - 6. (NCT02132247)
Timeframe: Up to 2 weeks, depending upon pain resolution

,
InterventionUnits on a scale (Mean)
Day1-2Day 3-4Day 5-7Day 8-11Day 12-15
Flector Patch/Age 12-160.040.060.000.060.00
Flector Patch/Age 6-110.100.040.110.000.00

[back to top]

Investigator Assessment of the Global Response to Therapy on a 5-point Scale

5-point scale: No clinical improvement in pain intensity and/or functional performance - 1; Slight clinical improvement in pain intensity and/or functional performance - 2; Moderate clinical improvement in pain intensity and/or functional performance - 3; Marked clinical improvement in pain intensity and/or functional performance - 4; Restoration of normal functional performance in the absence of any pain - 5. (NCT02132247)
Timeframe: Up to 2 weeks, depending upon pain resolution

,
InterventionParticipants (Count of Participants)
No clinical improvementSlight clinical improvementModerate clinical improvementMarked clinical improvementNormal function with no pain
Flector Patch/Age 12-16102940
Flector Patch/Age 6-11102247

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Patient Assessment of Pain on a 6-point Scale

"Wong-Baker FACES Scale 6-point scale:~No Hurt - 0; Hurts Little Bit - 1; Hurts Little More - 2; Hurts Even More - 3; Hurts Whole Lot - 4; Hurts Worst - 5." (NCT02132247)
Timeframe: Up to 2 weeks, depending upon pain resolution

,
Interventionunits on a scale (Mean)
BaselineFinal Visit
Flector Patch/Age 12-163.580.27
Flector Patch/Age 6-113.370.12

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Plasma Concentration of Diclofenac

(NCT02132247)
Timeframe: Day 2 and either Day 4, 7 or 14, depending upon pain resolution

,
Interventionng/mL (Mean)
24-hourFinal Visit
Flector Patch/Age 12-161.461.11
Flector Patch/Age 6-111.832.49

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Visual Analogue Scale (VAS) Scores at Baseline and Post Treatment

"To demonstrate the superiority (P<0.05) of the efficacy of the test and reference products over that of the vehicle control in the treatment of acute pain utilizing a 100 mm VAS (in the mITT population) - changes from baseline.~The Visual Analogue Scale (VAS) consists of a straight line with the endpoints defining extreme limits such as lower values of 'no pain at all' and higher values relating to 'pain as bad as it could be' ." (NCT02324270)
Timeframe: Baseline, 3 days

,,
Interventionscore on a scale (Mean)
Baseline72 hours after Initial treatmentChange from baseline
Diclofenac Epolamine Patch (Test Product)68.7525.83-42.91
Flector (Reference Product)68.9326.16-42.80
Placebo70.0927.16-42.88

[back to top]

Visual Analogue Scale (VAS) Scores at Baseline and Post Treatment

"To evaluate the therapeutic equivalence (90% CI) of generic diclofenac epolamine 1.3% patch (Watson Laboratories, Inc.) and Flector® (diclofenac epolamine 1.3% patch) (Pfizer) using a 100mm VAS scoring in the treatment of acute pain due to minor ankle sprain (in the per protocol population); changes from baseline.~The Visual Analogue Scale (VAS) consists of a straight line with the endpoints defining extreme limits such as lower values of 'no pain at all' and higher values relating to 'pain as bad as it could be' .~Percent improvement in VAS score is the percentage part of - change from baseline in VAS / Baseline VAS." (NCT02324270)
Timeframe: Baseline, 3 days

,
Interventionscore on a scale (Mean)
Baseline72 Hours after Initial treatmentChange from Baseline
Diclofenac Epolamine Patch (Test Product)68.5625.34-43.22
Flector (Reference Product)69.0325.78-43.25

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Serum Diclofenac Concentrations

Study Session 1: within 60 min prior to dosing, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 24, 27, 30, 32, 51 h Study Session 2: within 60 min prior to dosing, 1, 2, 3, 4, 5, 6, 7, 23, 26, 29, 31, 47 h Study Session 3: no blood samples obtained (NCT03145259)
Timeframe: blood samples obtained over 51 hour time period for study session 1 and over 47 hour time period for study session 2; through study completion

Interventionng/mL (Mean)
Diclofenac Epolamine Patches5.6
Diclofenac Sodium Solution40.0

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SubstanceRelationship StrengthStudiesTrialsClassesRoles
phthalic acid
phthalic acid: RN given refers to parent cpd; structure in Merck Index, 9th ed, #7178. phthalic acid : A benzenedicarboxylic acid cosisting of two carboxy groups at ortho positions.		2.610benzenedicarboxylic acidhuman xenobiotic metabolite
acetaminophen
Acetaminophen: Analgesic antipyretic derivative of acetanilide. It has weak anti-inflammatory properties and is used as a common analgesic, but may cause liver, blood cell, and kidney damage.. paracetamol : A member of the class of phenols that is 4-aminophenol in which one of the hydrogens attached to the amino group has been replaced by an acetyl group.		3.411acetamides;
phenols		antipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
cyclooxygenase 3 inhibitor;
environmental contaminant;
ferroptosis inducer;
geroprotector;
hepatotoxic agent;
human blood serum metabolite;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
diclofenac
Diclofenac: A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt.. diclofenac : A monocarboxylic acid consisting of phenylacetic acid having a (2,6-dichlorophenyl)amino group at the 2-position.		13.544321amino acid;
aromatic amine;
dichlorobenzene;
monocarboxylic acid;
secondary amino compound		antipyretic;
drug allergen;
EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor;
environmental contaminant;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
xenobiotic
ddt
1,1-bis(p-chlorophenyl)-2,2,2-trichloroethane: structure in first source		3.1110benzenoid aromatic compound;
chlorophenylethane;
monochlorobenzenes;
organochlorine insecticide		bridged diphenyl acaricide;
carcinogenic agent;
endocrine disruptor;
persistent organic pollutant
furosemide
Furosemide: A benzoic-sulfonamide-furan. It is a diuretic with fast onset and short duration that is used for EDEMA and chronic RENAL INSUFFICIENCY.. furosemide : A chlorobenzoic acid that is 4-chlorobenzoic acid substituted by a (furan-2-ylmethyl)amino and a sulfamoyl group at position 2 and 5 respectively. It is a diuretic used in the treatment of congestive heart failure.		3.4511chlorobenzoic acid;
furans;
sulfonamide		environmental contaminant;
loop diuretic;
xenobiotic
ibuprofen
Midol: combination of cinnamedrine, phenacetin, aspirin & caffeine		3.4511monocarboxylic acidantipyretic;
cyclooxygenase 1 inhibitor;
cyclooxygenase 2 inhibitor;
drug allergen;
environmental contaminant;
geroprotector;
non-narcotic analgesic;
non-steroidal anti-inflammatory drug;
radical scavenger;
xenobiotic
epolamine
[no description available]		4.7211pyrrolidines
dinoprostone
prostaglandin E2 : Prostaglandin F2alpha in which the hydroxy group at position 9 has been oxidised to the corresponding ketone. Prostaglandin E2 is the most common and most biologically potent of mammalian prostaglandins.		3.4711prostaglandins Ehuman metabolite;
mouse metabolite;
oxytocic
dinoprost
Dinoprost: A naturally occurring prostaglandin that has oxytocic, luteolytic, and abortifacient activities. Due to its vasocontractile properties, the compound has a variety of other biological actions.. prostaglandin F2alpha : A prostaglandins Falpha that is prosta-5,13-dien-1-oic acid substituted by hydroxy groups at positions 9, 11 and 15. It is a naturally occurring prostaglandin used to induce labor.		3.4711monocarboxylic acid;
prostaglandins Falpha		human metabolite;
mouse metabolite
8-epi-prostaglandin f2alpha
8-epi-prostaglandin F2alpha: a potent preglomerular vasoconstrictor acting principally through thromboxane A2 receptor activation. 8-epi-prostaglandin F2alpha : An isoprostane that is prostaglandin F2alpha having inverted stereochemistry at the 8-position.		3.4711F2-isoprostanebiomarker;
bronchoconstrictor agent;
vasoconstrictor agent
phosphatidylcholines
Phosphatidylcholines: Derivatives of PHOSPHATIDIC ACIDS in which the phosphoric acid is bound in ester linkage to a CHOLINE moiety.		5331,2-diacyl-sn-glycero-3-phosphocholine
ConditionIndicatedRelationship StrengthStudiesTrials
Injuries, Soft Tissue
[description not available]		07.3553
Acute Pain
Intensely discomforting, distressful, or agonizing sensation associated with trauma or disease, with well-defined location, character, and timing.		17.7622
Cancer of Prostate
[description not available]		03.420
Prostatic Neoplasms
Tumors or cancer of the PROSTATE.		03.420
Osteoarthritis of Knee
[description not available]		03.420
Innate Inflammatory Response
[description not available]		06.0441
Ache
[description not available]		08.28113
Inflammation
A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.		06.0441
Pain
An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.		08.28113
Osteoarthritis, Knee
Noninflammatory degenerative disease of the knee joint consisting of three large categories: conditions that block normal synchronous movement, conditions that produce abnormal pathways of motion, and conditions that cause stress concentration resulting in changes to articular cartilage. (Crenshaw, Campbell's Operative Orthopaedics, 8th ed, p2019)		03.420
Breast Cancer
[description not available]		03.3820
Breast Neoplasms
Tumors or cancer of the human BREAST.		15.3820
Injuries
Used with anatomic headings, animals, and sports for wounds and injuries. Excludes cell damage, for which pathology is used.		03.4711
Wounds and Injuries
Damage inflicted on the body as the direct or indirect result of an external force, with or without disruption of structural continuity.		03.4711
Anasarca
[description not available]		05.7154
Edema
Abnormal fluid accumulation in TISSUES or body cavities. Most cases of edema are present under the SKIN in SUBCUTANEOUS TISSUE.		05.7154
Nociceptive Pain
Dull or sharp aching pain caused by stimulated NOCICEPTORS due to tissue injury, inflammation or diseases. It can be divided into somatic or tissue pain and VISCERAL PAIN.		03.511
Allodynia
[description not available]		03.511
Muscle Disorders
[description not available]		06.1643
Bone Diseases
Diseases of BONES.		02.9610
Muscular Diseases
Acquired, familial, and congenital disorders of SKELETAL MUSCLE and SMOOTH MUSCLE.		06.1643
Orthopedic Disorders
[description not available]		02.9610
Musculoskeletal Diseases
Diseases of the muscles and their associated ligaments and other connective tissue and of the bones and cartilage viewed collectively.		02.9610
Sore Throat
[description not available]		03.4311
Complication, Postoperative
[description not available]		03.4311
Pharyngitis
Inflammation of the throat (PHARYNX).		03.4311
Postoperative Complications
Pathologic processes that affect patients after a surgical procedure. They may or may not be related to the disease for which the surgery was done, and they may or may not be direct results of the surgery.		03.4311
Pregnancy
The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.		03.4311
Sprains
[description not available]		07.3874
Acute Disease
Disease having a short and relatively severe course.		02.0510
Sprains and Strains
A collective term for muscle and ligament injuries without dislocation or fracture. A sprain is a joint injury in which some of the fibers of a supporting ligament are ruptured but the continuity of the ligament remains intact. A strain is an overstretching or overexertion of some part of the musculature.		19.3874
Bruise
[description not available]		06.1843
Contusions
Injuries resulting in hemorrhage, usually manifested in the skin.		06.1843
Hematoma
A collection of blood outside the BLOOD VESSELS. Hematoma can be localized in an organ, space, or tissue.		03.4411
Arthropathies
[description not available]		03.4411
Ankle Injuries
Harm or hurt to the ankle or ankle joint usually inflicted by an external source.		06.1743
Joint Diseases
Diseases involving the JOINTS.		03.4411
Injuries, Knee
[description not available]		03.411
Injuries, Leg
[description not available]		03.411
Knee Injuries
Injuries to the knee or the knee joint.		03.411
Benign Neoplasms
[description not available]		02.9310
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		02.9310
Arthritis, Degenerative
[description not available]		09.386
Osteoarthritis
A progressive, degenerative joint disease, the most common form of arthritis, especially in older persons. The disease is thought to result not from the aging process but from biochemical changes and biomechanical stresses affecting articular cartilage. In the foreign literature it is often called osteoarthrosis deformans.		09.386
Athletic Injuries
Injuries incurred during participation in competitive or non-competitive sports.		04.721
Joint Pain
[description not available]		02.0310
Arthralgia
Pain in the joint.		02.0310
Calcification, Pathologic
[description not available]		02.0410
Calcinosis
Pathologic deposition of calcium salts in tissues.		02.0410
Contracture
Prolonged shortening of the muscle or other soft tissue around a joint, preventing movement of the joint.		02.0410
Tendinitis
Inflammation of TENDONS. It is characterized by the degeneration of tendons accompanied by an inflammatory repair response, fibroblastic proliferation, and formation of granulation tissue. Tendinitis is not a clinical diagnosis and can be confirmed only by histopathological findings.		04.3322
Rheumatoid Arthritis
[description not available]		03.3711
Rheumatism
[description not available]		04.3422
Arthritis, Rheumatoid
A chronic systemic disease, primarily of the joints, marked by inflammatory changes in the synovial membranes and articular structures, widespread fibrinoid degeneration of the collagen fibers in mesenchymal tissues, and by atrophy and rarefaction of bony structures. Etiology is unknown, but autoimmune mechanisms have been implicated.		03.3711
Rheumatic Diseases
Disorders of connective tissue, especially the joints and related structures, characterized by inflammation, degeneration, or metabolic derangement.		04.3422
Tendinopathy
Clinical syndrome describing overuse tendon injuries characterized by a combination of PAIN, diffuse or localized swelling, and impaired performance.		04.3322
Polyarthritis
[description not available]		03.3711
Arthritis
Acute or chronic inflammation of JOINTS.		03.3711
Back Ache
[description not available]		01.9910
Curling Ulcer
Acute stress DUODENAL ULCER, usually observed in patients with extensive third-degree burns.		01.9910
Hemorrhage, Peptic Ulcer
[description not available]		01.9910
Stasis Ulcer
[description not available]		01.9910
Back Pain
Acute or chronic pain located in the posterior regions of the THORAX; LUMBOSACRAL REGION; or the adjacent regions.		01.9910
Duodenal Ulcer
A PEPTIC ULCER located in the DUODENUM.		01.9910
Varicose Ulcer
Skin breakdown or ulceration in the drainage area of a VARICOSE VEIN, usually in the leg.		01.9910
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