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Brand Name :
Zorvolex, Zipsor, Cambia, Dyloject, Voltaren-XR, Cataflam
Synonyms :
diclofenac
Class :
NSAIDs
Brand Name :
Zorvolex, Zipsor, Cambia, Dyloject, Voltaren-XR, Cataflam
Synonyms :
diclofenac
Class :
NSAIDs
Dosage Forms & Strengths
diclofenac potassium
Packet
50mg single-dose packet
Tablet
50mg
Capsule
25mg
diclofenac sodium
Delayed release tablet
25mg
50mg
75mg
Extended-release tablet
100mg
Capsule
Zorvolex
18mg
35mg
diclofenac potassium- 50 mg orally 2-3 times daily
diclofenac sodium- 50 mg orally thrice daily or 75 mg orally every 12 hours
Extended-release- 100 mg orally once daily, may increase the dose to 100 mg every 12 hours
diclofenac potassium- 50 mg orally 2-3 times daily
diclofenac sodium- 50 mg orally thrice daily or 75 mg orally every 12 hours
Extended-release- 100 mg orally once daily, may increase the dose to 100 mg every 12 hours
diclofenac potassium- 50 mg orally 2-3 times daily
diclofenac sodium- 50 mg orally thrice daily or 75 mg orally every 12 hours
Extended-release- 100 mg orally once a day; may increase the dose to 100 mg twice daily
Zorvolex- 35 mg orally thrice a day
diclofenac potassium- 25 mg orally 4-5 times daily
diclofenac sodium- 50 mg orally every 12 hours
Immediate-release- 100 mg orally once, later 50 mg orally thrice daily as required
Indicated to treat moderate to mild acute pain in adults
Immediate-release- 100 mg orally once, later 50 mg orally thrice daily as required
Extended-release tablets-
Zipsor- 25 mg orally four times daily as required
Zorvolex- 18-35 mg orally thrice daily
Keeping individual treatment goals, use the potent dose for a short duration
Indicated to treat acute migraine attacks with/without aura
Cambia- 50 mg packet in 30-60ml water, shake well and consume immediately
It is not used for preventive treatment
Keeping individual treatment goals, use the potent dose for a short duration
Dose Modification
In the case of hepatic impairment, start over with the lowest potent dose, and consider substitute treatment if efficacy is not achieved
Dosage Forms & Strengths
diclofenac potassium
Capsule
Zipsor
25 mg
For <12 years, safety and efficacy are not seen
For ≥12 years, indicated to relieve moderate to mild pain
25 mg orally 4 times daily
Dose Modification
In the case of hepatic impairment, start over with the lowest potent dose, and consider substitute treatment if efficacy is not achieved
Refer to the adult dosing
increases serum concentration and toxic effect on GI, avoid the combination
increases serum concentration and toxic effect on GI, avoid the combination
acemetacin may enhance the adverse/toxic effect of Nonsteroidal Anti-Inflammatory Agents
may enhance the risk of angioedema when combined with Diclofenac
the toxicity of either of the drugs is increased due to pharmacokinetic synergism
It may enhance the toxicity when combined with mipomersen
may increase the anticoagulation when combined with ginkgo biloba
Combining diclofenac with pranlukast may cause a reduction in the diclofenac’s metabolism
when bromazepam and diclofenac are used together, there is a potential reduction in the bromazepam's metabolism
diclofenac has the potential to reduce the rate of excretion of idebenone, leading to an elevation in levels of serum
Combining tegafur with diclofenac can reduce tegafur’s metabolism
When loracarbef is used together with diclofenac, the risk or seriousness of nephrotoxicity is enhanced
When diclofenac is used together with sertraline, the risk or seriousness of bleeding may be enhanced
When diclofenac is used together with piroxicam, this leads to enhanced risk or seriousness of adverse outcomes
When diclofenac is used together with somatotropin, this leads to a rise in diclofenac metabolism
When diclofenac is used together with andrographolide, this leads to enhanced risk or seriousness of bleeding
When cefmenoxime is used together with diclofenac, this leads to enhanced risk or seriousness of nephrotoxicity
When diclofenac is used together with proglumetacin, this leads to enhanced risk or seriousness of adverse events
When diclofenac is used together with bufexamac, this leads to enhanced risk or seriousness of adverse outcomes
diclofenac leads to a reduction in the rate of excretion of nitric oxide, which leads to an increased level of serum
When diclofenac is used together with nifenazone, this leads to enhanced risk or seriousness of adverse events
When diclofenac is used together with adenine, this leads to a reduction in the diclofenac's metabolism
diclofenac: it may increase the risk of gastrointestinal bleeding with risedronic acid
diclofenac: it may decrease the excretion rate of metheglobinemia associated agents
diclofenac: it may decrease the excretion rate of metheglobinemia associated agents
diclofenac: it may decrease the excretion rate of metheglobinemia associated agents
diclofenac: it may decrease the excretion rate of metheglobinemia associated agents
diclofenac: it may decrease the excretion rate of metheglobinemia associated agents
When diclofenac is used together with diazoxide, this leads to reduction in therapeutic effectiveness of diazoxide
diclofenac: it may decrease the excretion of CYP3A inhibitors
diclofenac: it may decrease the excretion of CYP3A inhibitors
diclofenac: it may decrease the excretion of CYP3A inhibitors
diclofenac: it may decrease the excretion of CYP3A inhibitors
diclofenac: it may decrease the excretion of CYP3A inhibitors
when both drugs are combined, there may be a decreased level of serum concentration of diclofenac
the effect of diclofenac is increased by fluorouracil by the action on CYP2C9/10 hepatic enzyme metabolism
it enhances the serum potassium levels
may enhance the serum concentration of CYP2C9 inhibitors
voriconazole: they may enhance the serum concentration of diclofenac
the toxicity of either of the drugs is increased due to pharmacokinetic synergism
may have a decrease in excretion when combined with diclofenac
the risk of gastrointestinal bleeding may be increased
both forskolin and diclofenac enhance anticoagulation
diclofenac might lead to a reduction in the rate of excretion of telavancin, potentially leading to elevated levels of serum
When diclofenac is aided by hesperetin, it reduces hesperetin’s metabolism
may enhance the renal tubular clearance for anionic drug competition
may enhance the renal tubular clearance for anionic drug competition
Actions and Spectrum:
diclofenac is an NSAID and works as an anti-inflammatory drug which prevents the synthesis of certain substances named prostaglandins. Prostaglandins assist in increasing the degree of inflammation, pain, and swelling. Diclofenac thereby inhibits the production of these substances and hence leads to relief of pain, reduction in inflammation and hence an improvement in the movements of joints.
diclofenac is useful in the treatment of multiple forms of pain especially musculoskeletal pain which include osteoarthritis, rheumatoid arthritis, ankylosing spondylitis and gout. It may also be useful in treatment of peri-operative pain such as post operative pain and menstrual cramps.
Frequency defined
>10%
Edema (33%)
Nausea (27%)
Headache (13%)
1-10%
Dizziness (10%)
Flatulence (3%)
Pain in extremities (3%)
Vomiting (9%)
Constipation (8%)
Pruritus (7%)
Dyspepsia (2%)
<1%
Flushing (0.2%)
Utricaria (0.2%)
Black Box Warning:
NSAIDs increase the risk of myocardial infarction, stroke, and severe CV thrombotic agents. They increase the risk with more extended usage.
NSAIDs increase the risk of serious gastrointestinal events.
Contraindication/Caution:
Pregnancy/Lactation
Pregnancy consideration: Not recommended for fertile females.
Breastfeeding warnings: No data is available regarding the excretion of drugs in breast milk.
Pregnancy category:
Pharmacology
diclofenac has anti-inflammatory and antipyretic properties. Its pharmacological effects are primarily mediated through inhibiting cyclooxygenase (COX) enzymes, specifically COX-1 and COX-2. COX enzymes synthesize prostaglandins, mediating pain, inflammation, and fever.
By inhibiting COX enzymes, diclofenac reduces the production of prostaglandins, leading to the alleviation of pain, suppression of inflammation, and reduction of fever. It mainly acts by inhibiting the action of COX-2, which is involved in the inflammatory response.
Pharmacodynamics
By inhibiting COX enzymes, diclofenac reduces the production of prostaglandins, leading to the alleviation of pain, suppression of inflammation, and reduction of fever. It mainly acts by inhibiting the action of COX-2, which is involved in the inflammatory response.
Pharmacokinetics
Absorption
Absolute Bioavailability: Diclofenac potassium: 55%
Peak Plasma Concentration:
Cambia: ~0.25 hr
Zipsor: 1,087 ng/mL (adults), 699 ng/mL (aged 12 to 17 years)
Peak Plasma Time:
Diclofenac potassium: 1 hr
Zipsor: 0.47 hr (adults), 0.94 hr (aged 12 to 17 years)
Area Under the Curve (AUC):
Zipsor: 597 ng⋅hr/mL (adults), 659 ng⋅hr/mL (aged 12-17 years)
No significant effect on the extent of diclofenac absorption, but a reduction in peak plasma levels of ~70%.
Distribution
Diclofenac diffuses into and out of synovial fluid; it is unknown whether diffusion into the joint plays a role in its effectiveness.
Volume of Distribution (Vd): 1.3 L/kg
Protein Binding: Diclofenac potassium: >99%
Metabolism
Metabolites: 4’-hydroxy-, 5-hydroxy-, 3’-hydroxy-, 4’,5-dihydroxy-, and 3’-hydroxy-4’-methoxy diclofenac.
Formation of 4’-hydroxy-diclofenac is primarily mediated by CYP2C9.
CYP3A4 is responsible for the formation of minor metabolites, 5-hydroxy and 3’-hydroxy-diclofenac.
Elimination:
Half-life: Unchanged diclofenac: ~2 hr
Mean: 1.9 hour
Zipsor: 1.07 hour (adults), 1.81 hour (aged 12 to 17 years)
Urine: ~65%
Bile: ~35%
Administration:
It is administered orally in the form of tablets or capsules by mouth with a full glass of water
Patient information leaflet
Generic Name: diclofenac
Pronounced: dye-KLOE-fen-ak
Why do we use diclofenac?
Diclofenac is a non-steroidal anti-inflammatory drug with analgesic, anti-inflammatory, and antipyretic effects. Here are its primary uses:
Musculoskeletal Pain: Used in the management of diseases such as sprains, strains and other conditions that cause pain including injuries in athletic activities.
Postoperative Pain: Applied in cases of pain administration after operations have been conducted.
Arthritis: It is used in the management of different types of arthritis such as osteoarthritis, rheumatoid arthritis and ankylosing spondylitis.
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