Klafenac

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

Klafenac Eye Drops contains Klafenac Sodium, a potent non-steroidal anti-inflammatory drug with analgesic property. Klafenac Sodium produces anti-inflammatory effect by inhibiting cyclooxygenase activity with a reduction in the tissue prostaglandin ( such as PgE2 and Pg F2α) .

Klafenac reduces inflammation and by extension reduces nociceptive pain and combats fever. It also increases the risk of developing a gastrointestinal ulcer by inhibiting the production of protective mucus in the stomach.

Trade Name Klafenac
Availability Prescription only
Generic Diclofenac
Diclofenac Other Names Diclofenac, Diclofenac acid, Diclofenaco, Diclofenacum
Related Drugs Humira, Ubrelvy, Buprenex, Botox, aspirin, prednisone, ibuprofen, acetaminophen, tramadol, meloxicam
Type
Formula C14H11Cl2NO2
Weight Average: 296.149
Monoisotopic: 295.016684015
Protein binding

Diclofenac is over 99.7% bound to serum proteins, primarily albumin. It is undergoes limited binding to lipoproteins as well with 1.1% bound to HDL, 0.3% to LDL, and 0.15% to VLDL.

Groups Approved, Vet approved
Therapeutic Class Ophthalmic Non-Steroid drugs
Manufacturer
Available Country Chile
Last Updated: September 19, 2023 at 7:00 am
Klafenac
Klafenac

Uses

Klafenac Sodium ophthalmic preparation is used for-

  • Inhibition of miosis during cataract surgery.
  • Post-operative inflammation after cataract surgery and other ocular surgical procedures.
  • Pre-operative and post-operative prevention of cystoid macular edema (CME) associated with lens extraction & intraocular lens implantation.
  • Post-traumatic inflammation in penetrating and non- penetrating wounds (as an adjuvant to local anti-infective therapy).
  • Non-infected chronic conjunctivitis, keratoconjunctivitis.

Klafenac is also used to associated treatment for these conditions: Actinic Keratosis (AK), Acute Arthritis, Acute Gouty Arthritis, Acute Migraine, Acute Musculoskeletal Pain, Ankylosing Spondylitis (AS), Common Cold, Fever, Gouty Arthritis, Inflammation, Inflammatory Disease of the Oral Cavity, Inflammatory Disease of the throat, Inflammatory Reaction of the Nerve, Joint Pain, Juvenile Idiopathic Arthritis (JIA), Menstrual Distress (Dysmenorrhea), Muscle Inflammation, Ocular Inflammation, Operation site inflammation, Osteoarthritis (OA), Osteoarthritis of the Knee, Pain, Pain, Nerve, Pericarditis, Photophobia, Postoperative pain, Primary Dysmenorrhoea, Radicular Pain, Rheumatic Pain, Rheumatism, Rheumatoid Arthritis, Seasonal Allergic Conjunctivitis, Soreness, Muscle, Spinal pain, Tendon pain, Vertebral column pain, Acute Musculoskeletal injury, Acute, moderate, severe Pain, Inflammatory, Localized soft tissue rheumatism, Mild to moderate joint pain, Mild to moderate pain, Minor pain, Perioperative miosis

How Klafenac works

Klafenac inhibits cyclooxygenase-1 and -2, the enzymes responsible for production of prostaglandin (PG) G2 which is the precursor to other PGs. These molecules have broad activity in pain and inflammation and the inhibition of their production is the common mechanism linking each effect of diclofenac.

PGE2 is the primary PG involved in modulation of nociception. It mediates peripheral sensitization through a variety of effects. PGE2 activates the Gq-coupled EP1 receptor leading to increased activity of the inositol trisphosphate/phospholipase C pathway. Activation of this pathway releases intracellular stores of calcium which directly reduces action potential threshold and activates protein kinase C (PKC) which contributes to several indirect mechanisms. PGE2 also activates the EP4 receptor, coupled to Gs, which activates the adenylyl cyclase/protein kinase A (AC/PKA) signaling pathway. PKA and PKC both contribute to the potentiation of transient receptor potential cation channel subfamily V member 1 (TRPV1) potentiation, which increases sensitivity to heat stimuli. They also activate tetrodotoxin-resistant sodium channels and inhibit inward potassium currents. PKA further contributes to the activation of the P2X3 purine receptor and sensitization of T-type calcium channels. The activation and sensitization of depolarizing ion channels and inhibition of inward potassium currents serve to reduce the intensity of stimulus necessary to generate action potentials in nociceptive sensory afferents. PGE2 act via EP3 to increase sensitivity to bradykinin and via EP2 to further increase heat sensitivity. Central sensitization occurs in the dorsal horn of the spinal cord and is mediated by the EP2 receptor which couples to Gs. Pre-synaptically, this receptor increases the release of pro-nociceptive neurotransmitters glutamate, CGRP, and substance P. Post-synaptically it increases the activity of AMPA and NMDA receptors and produces inhibition of inhibitory glycinergic neurons. Together these lead to a reduced threshold of activating, allowing low intensity stimuli to generate pain signals. PGI2 is known to play a role via its Gs-coupled IP receptor although the magnitude of its contribution varies. It has been proposed to be of greater importance in painful inflammatory conditions such as arthritis. By limiting sensitization, both peripheral and central, via these pathways NSAIDs can effectively reduce inflammatory pain.

PGI2 and PGE2 contribute to acute inflammation via their IP and EP2 receptors. Similarly to β adrenergic receptors these are Gs-coupled and mediate vasodilation through the AC/PKA pathway. PGE2 also contributes by increasing leukocyte adhesion to the endothelium and attracts the cells to the site of injury. PGD2 plays a role in the activation of endothelial cell release of cytokines through its DP1 receptor. PGI2 and PGE2 modulate T-helper cell activation and differentiation through IP, EP2, and EP4 receptors which is believed to be an important activity in the pathology of arthritic conditions. By limiting the production of these PGs at the site of injury, NSAIDs can reduce inflammation.

PGE2 can cross the blood-brain barrier and act on excitatory Gq EP3 receptors on thermoregulatory neurons in the hypothalamus. This activation triggers an increase in heat-generation and a reduction in heat-loss to produce a fever. NSAIDs prevent the generation of PGE2 thereby reducing the activity of these neurons.

Dosage

Klafenac dosage

Ophthalmic (Adult)-

  • Postoperative ocular inflammation: Instill into the appropriate eye 4 times daily starting 24 hr after surgery for up to 28 days.
  • Inflammation and discomfort after strabismus surgery: Instill 1 drop 4 times daily for the 1st wk; then tid in the 2nd wk, bid in the 3rd wk, and as required for the 4th wk.
  • Pain and discomfort after radial keratotomy: Instill 1 drop before surgery followed by 1 drop immediately after surgery, and then 1 drop 4 times daily for up to 2 days.
  • Pain after accidental trauma: Instill 1 drop 4 times daily for up to 2 days.
  • Control of inflammation after argon laser trabeculoplasty:Instill 1 drop 4 times during the 2 hr before procedure followed by 1 drop 4 times daily, up to 7 days after procedure.
  • Prophylaxis of intra-operative miosis: Instill into appropriate eye 4 times w/in 2 hr before surgery.
  • Post-photorefractive keratectomy pain:Instill into the affected eye twice, an hr before surgery, then 1 drop twice at 5-min intervals immediately after surgery, then every 2-5 hr while awake for up to 24 hr.
  • Seasonal allergic conjunctivitis:Instill 1 drop before surgery followed by 1 drop immediately after surgery, and then 1 drop 4 times daily for up to 2 days.

Side Effects

Mild to moderate burning sensation in 5-15% patients which is transient in nature and almost never necessitated discontinuation of treatment. Other less common side-effects are sensitivity to light, bad taste, feeling of pressure, allergic reactions etc.

Toxicity

Symptoms of overdose include lethargy, drowsiness, nausea, vomiting, and epigastric pain, and gastrointestinal bleeding. Hypertension, acute renal failure, respiratory depression and coma occur rarely. In case of overdose, provide supportive care and consider inducing emesis and administering activated charcoal if overdose occurred less than 4 hours prior.

Precaution

Klafenac eye drops may mask the signs of infection. So physicians should be alert to the development of infections in patients receiving the drug. During prolonged use, it is recommended that physicians conduct periodic examinations of the eye, including measurement of the intraocular pressure. Contact lenses should not be worn during treatment.

Interaction

No drug interaction is reported. There should be at least 5 minutes interval when another ophthalmic solution (e.g., steroid) is given.

Food Interaction

  • Avoid excessive or chronic alcohol consumption. Co-administration with alcohol may increase the risk of gastrointestinal side effects, such as ulceration.
  • Take with food. Food reduces gastric irritation.

Klafenac Alcohol interaction

[Moderate] GENERALLY AVOID:

The concurrent use of aspirin or nonsteroidal anti-inflammatory drugs (NSAIDs) and ethanol may lead to gastrointestinal (GI) blood loss.

The mechanism may be due to a combined local effect as well as inhibition of prostaglandins leading to decreased integrity of the GI lining.



Patients should be counseled on this potential interaction and advised to refrain from alcohol consumption while taking aspirin or NSAIDs.

Klafenac Hypertension interaction

[Major] Fluid retention and edema have been reported in association with the use of nonsteroidal anti-inflammatory drugs (NSAIDs).

Therapy with NSAIDs should be administered cautiously in patients with preexisting fluid retention, hypertension, or a history of heart failure.

Blood pressure and cardiovascular status should be monitored closely during the initiation of NSAID treatment and throughout the course of therapy.

Hypertension interaction

[Moderate] Nonsteroidal anti-inflammatory drugs (NSAIDs), including topicals, can lead to new onset of hypertension or worsening of preexisting hypertension, either of which can contribute to the increased incidence of cardiovascular events.

NSAIDs should be used with caution in patients with hypertension.

Blood pressure should be monitored closely during the initiation of NSAID therapy and throughout the course of therapy.

Volume of Distribution

Klafenac has a total volume of distribution of 5-10 L or 0.1-0.2 L/kg. The volume of the central compartment is 0.04 L/kg. Klafenac distributes to the synovial fluid reaching peak concentration 2-4h after administration. There is limited crossing of the blood brain barrier and cerebrospinal fluid concentrations only reach 8.22% of plasma concentrations. Doses of 50 mg delivered via intramuscular injection produced no detectable diclofenac concentrations in breast milk, however metabolite concentrations were not investigated. Klafenac has been shown to cross the placenta in mice and rats but human data is unavailable.

Elimination Route

Klafenac is completely absorbed from the GI tract but likely undergoes significant first pass metabolism with only 60% of the drug reaching systemic circulation unchanged . Many topical formulations are absorbed percutaneous and produce clinically significant plasma concentrations. Absorption is dose proportional over the range of 25-150 mg. Tmax varies between formulations with the oral solution reaching peak plasma concentrations in 10-40min, the enteric coated tablet in 1.5-2h, and the sustained- and extended-release formulations prolonging Tmax even further. Administration with food has no significant effects on AUC but does delay Tmax to 2.5-12h.

Half Life

The terminal half-life of diclofenac is approximately 2 h, however the apparent half-life including all metabolites is 25.8-33 h.

Clearance

Klafenac has a plasma clearance 16 L/h.

Elimination Route

Klafenac is mainly eliminated via metabolism. Of the total dose, 60-70% is eliminated in the urine and 30% is eliminated in the feces. No significant enterohepatic recycling occurs.

Pregnancy & Breastfeeding use

The safety of Klafenac eye drops in pregnancy & lactation has not been established and its use therefore is not recommended unless the potential benefit to the mother outweighs the possible risk to the child.

Contraindication

Hypersensitivity to any of the components Like other non steroidal anti-inflammatory agents, Klafenac Sodium eye drops is contraindicated in patients in whom attacks of asthma, urticaria or acute rhinitis have been observed following application of acetyl salicylic acid or other cyclo-oxygenase inhibitors

Acute Overdose

Accidental ingestion of Klafenac Sodium presents virtually no risk of unwanted effects, since one 5 ml bottle of eye drop solution contains only 5 mg of Klafenac Sodium, which is equivalent to about 3% of the recommended maximum oral dose for adults.

Storage Condition

Close the bottle immediately after use. Do not use for more than four weeks after opening. Store at room temperature.

Innovators Monograph

You find simplified version here Klafenac

Klafenac contains Diclofenac see full prescribing information from innovator Klafenac Monograph, Klafenac MSDS, Klafenac FDA label

FAQ

What is Klafenac used for?

Klafenac used to treat aches and pains, as well as problems with joints, muscles and bones.Klafenac is a medicine that reduces swelling (inflammation) and pain.

What are the most common side effects of Klafenac?

Common side effects

  • feeling sick (nausea)
  • being sick (vomiting) or diarrhoea.
  • feeling dizzy or vertigo.
  • headaches.
  • stomach ache, wind or loss of appetite.
  • mild rash.

What are the dangers of taking Klafenac?

Klafenac can increase your risk of fatal heart attack or stroke, even if you don't have any risk factors. Do not use this medicine just before or after heart bypass surgery.

How safe Klafenac is?

For most people, taking Klafenac is safe.If you have high blood pressure, high cholesterol, diabetes, your kidneys do not work very well or you smoke, you should check with your healthcare professional that this medicine is appropriate.

Is Klafenac safe during pregnancy?

Use of Klafenac during pregnancy is not advised unless prescribed by a doctor, especially if you are 30 or more weeks pregnant.

Is Klafenac safe during breastfeeding?

Most reviewers consider diclofenac to be acceptable during breastfeeding.Data on excretion of Klafenac into milk are poor, but the drug has a short half-life and little glucuronide metabolite formation.

can I take alcohol with Klafenac?

Yes, you can drink alcohol while taking diclofenac. But drinking too much alcohol may irritate your stomach.

What kind of pain does Klafenac relieve?

Klafenac is a nonsteroidal anti-inflammatory drug (NSAID) used to treat mild-to-moderate pain, and helps to relieve symptoms of arthritis such as inflammation, swelling, stiffness, and joint pain.

Why is Klafenac bad for the heart?

Klafenac topical can increase your risk of fatal heart attack or stroke, even if you don't have any risk factors. Do not use this medicine just before or after heart bypass surgery .Klafenac topical may also cause stomach or intestinal bleeding, which can be fatal.

Is Klafenac harmful to kidneys?

Klafenac and other non-steroidal anti-inflammatory drugs cause the kidney to lose the capacity to make these protective hormones and over time, can result in progressive kidney damage

Can Klafenac cause liver damage?

Liver injury from Klafenac can happen weeks to months after you start taking it and affects susceptible individuals for reasons we don't yet know.

Does Klafenac help nerve pain?

This drug can be used to relieve neuropathic pain.

Is Klafenac a muscle relaxer?

Klafenac is a muscle relaxer. It is used to treat muscle aches, backaches, dental pain, menstrual cramps, and sports injuries.

Is Klafenac a narcotic?

No, Klafenac is a non-steroidal anti inflammatory drug and in no way related to narcotics.

Can Klafenac cause nerve damage?

Klafenac induced severe nerve damage not only after direct injection in the sciatic nerve but also after injection in the area around the nerve.

Can I take Klafenac for a long time?

brans is best to take the lowest dose that works for the shortest possible time.Klafenac tablets and capsules can cause an ulcer in your stomach or gut if you take them for a long time or in big doses. There's also a small risk of heart failure or kidney failure if you take very big doses (150mg a day) for a long time.

How does Klafenac work?

Klafenac works by reducing hormones that cause inflammation and pain in the body. When you apply Klafenac  gel, plasters or patches to your skin, it works in the same way as when you take it as a tablet or capsule.

*** Taking medicines without doctor's advice can cause long-term problems.
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