Diclofenac, with an IC50 of 7±3 nM, efficiently inhibits COX-1-mediated microsomal synthesis of prostaglandins in U937 cells[1]. Neural stem cells (NSCs) undergo concentration-dependent apoptosis when exposed to diclofenac sodium (1–60 μM; 1 day) [3]. Cloned (activated) caspase-3 is expressed more when exposed to Diclofenac Sodium (10–60 μM) for six hours [3].

Rats' fecal 51Cr excretion is greatly increased by diclofenac sodium (3 mg/kg, bid) for five days. This effect was also seen in squirrel monkeys, who received 1 mg/kg twice daily for four days [1]. In Wistar rats, oral administration of Diclofenac Sodium (10 mg/kg) prior to development of inflammation exhibits anti-inflammatory action [1].

Cell Viability Assay[3]
Cell Types: Neural stem cells (NSCs)
Tested Concentrations: 1, 3, 10, 30, 60 μM
Incubation Duration: 1 day
Experimental Results: Induction of cell death was concentration-dependent and the effect was not saturated at a concentration of up to 60 μM.

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Western Blot Analysis[3]
Cell Types: Neural stem cells (NSCs)
Tested Concentrations: 10, 30 or 60 μM
Incubation Duration: 6 hrs (hours)
Experimental Results: The activation of caspase-3 was increased in a concentration-dependent manner.

Animal/Disease Models: Male SD (Sprague-Dawley) rats (150±200 g)[1]
Doses: 3 mg/kg
Route of Administration: Oral administration, bid, for 5 days
Experimental Results: Resulted in a significant increase in faecal 51Cr excretion.

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Animal/Disease Models: Wistar rats (150-175 g) bearing Formalin-induced rat foot paw edema model[2]
Doses: 10 mg/kg
Route of Administration: Administered via oral route just prior to induction of inflammation
Experimental Results: demonstrated in vivo anti-inflammatory activity (% edema inhibition= 29.2, 1 h; 22.2, 3 h; 20, 6 h).

Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
Data on excretion of diclofenac into milk are poor, but the drug has a short half-life and little glucuronide metabolite formation. Levels in milk appear to be quite low. Most reviewers consider diclofenac to be acceptable during breastfeeding. Other agents having more published information may be preferred, especially while nursing a newborn or preterm infant.
Maternal use of diclofenac topical gel or eye drops would not be expected to cause any adverse effects in breastfed infants. To substantially diminish the amount of drug that reaches the breastmilk after using eye drops, place pressure over the tear duct by the corner of the eye for 1 minute or more, then remove the excess solution with an absorbent tissue.
◉ Effects in Breastfed Infants
In one study, 30 mothers undergoing elective cesarean section were allowed to use 25 mg diclofenac suppositories along with either spinal or spinal and epidural anesthesia with a local anesthetic after delivery. The spinal anesthetic group used an average of 56 mg of diclofenac on the day of delivery and 33 mg on the next day whereas the women receiving both spinal and epidural anesthesia used 21 and 18 mg. No mention was made of adverse effects on the breastfed infants.
A breastfed infant developed urticaria on day 15 of life. Her mother had been taking diclofenac (dosage unspecified) for pain since her cesarean section delivery. Diclofenac is a possible cause of the urticaria; however, the infant had also received hepatitis B vaccination 7 days before and the authors thought that it was a more likely cause of the reaction.
◉ Effects on Lactation and Breastmilk
A randomized, double-blind study was performed in pregnant women scheduled for cesarean section under spinal anesthesia with bupivacaine and fentanyl. Patients received either 100 mg diclofenac (n = 100), 100 mg tramadol (n = 100) or placebo (glycerin suppositories) n = 100, all given as rectal suppositories every 8 hours for the first 24 hours after surgery. The time to initiate breastfeeding was significantly shorter among mothers who received diclofenac than a placebo, 1.5 vs 4.1 hours with breastfeeding support and 3.5 vs 6.2 hours without support. Diclofenac was slightly more effective than tramadol among mothers who received no support (3.5 vs 3.7 hours).

[1]. Biochemical and pharmacological profile of a tetrasubstituted furanone as a highly selective COX-2 inhibitor. Br J Pharmacol. 1997 May;121(1):105-17.

[2]. Design, synthesis of novel isoindoline hybrids as COX-2 inhibitors: Anti-inflammatory, analgesic activities and docking study. Bioorg Chem. 2018 Oct;80:70-80.

[3]. Diclofenac Inhibits Proliferation and Differentiation of Neural Stem Cells. Biochem Pharmacol. 2003 Jul 15;66(2):289-95.

Diclofenac sodium is the sodium salt of diclofenac. It contains a diclofenac(1-).
Diclofenac Sodium is the sodium salt form of diclofenac, a benzene acetic acid derivate and nonsteroidal anti-inflammatory drug (NSAID) with analgesic, antipyretic and anti-inflammatory activity. Diclofenac sodium is a non-selective reversible and competitive inhibitor of cyclooxygenase (COX), subsequently blocking the conversion of arachidonic acid into prostaglandin precursors. This leads to an inhibition of the formation of prostaglandins that are involved in pain, inflammation and fever.
A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt.
See also: Diclofenac (brandname of); Omeprazole (has active ingredient); Capsicum Oleoresin (has active ingredient) ... View More ...

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Drug Indication
Treatment of inflammation, Treatment of pain

C14H10CL2NNAO2

318.13

316.998

15307-79-6

Diclofenac;15307-86-5;Diclofenac diethylamine;78213-16-8;Diclofenac-d4 sodium;154523-54-3;Diclofenac potassium;15307-81-0;Diclofenac-13C6 sodium heminonahydrate;Diclofenac-13C6 Sodium;1261393-73-0

5018304

White to off-white solid powder

412ºC at 760 mmHg

288-290°C

203ºC

3.102

1

3

4

20

310

0

KPHWPUGNDIVLNH-UHFFFAOYSA-M

1S/C14H11Cl2NO2.Na/c15-10-5-3-6-11(16)14(10)17-12-7-2-1-4-9(12)8-13(18)19;/h1-7,17H,8H2,(H,18,19);/q;+1/p-1

Benzeneacetic acid, 2-((2,6-dichlorophenyl)amino)-, monosodium salt

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility in Formulation 1: 4.55 mg/mL (14.30 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).

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 (Please use freshly prepared in vivo formulations for optimal results.)