(+977) 4110791, 01-4110761 info@opl.com.np
A smart solution to relieve pain and inflammation…

ALOFEN 100

Generic Name:                    Aceclofenac

Therapeutic Category:     Non-Steroidal Anti-inflammatory Drugs (NSAID)

Pharmacological Class:   Non-selective COX inhibitor

Composition:                      Each film-coated tablet contains Aceclofenac BP 100 mg

Pregnancy Category:        C (up to second trimester) and D (in third trimester)

Presentation:                      Available in the pack size as 10 tablets X 20 blisters

What is Alofen and what is it used for?

Alofen contains Aceclofenac 100 mg in tablet form. Aceclofenac Tablets belongs to a group of medicines called non-steroidal anti-inflammatory drugs (NSAIDs). It is used in

  • arthritis of the joints (osteoarthritis). This commonly occurs in patients over the age of 50 and causes the loss of the cartilage and bone tissue next to the joint.
  • autoimmune disease that causes chronic inflammation of the joints (rheumatoid arthritis).
  • arthritis of the spine which can lead to the fusion of the vertebrae (ankylosing spondylitis).

How does it work?

Alofen works by blocking the effect of natural substances called cyclo-oxygenase (COX) enzymes. These enzymes help to make other chemicals in the body, called prostaglandins. They have anti-inflammatory and painkiller properties causing a lowering of swelling, redness (inflammation) and pain.

 

How to take Alofen?

The recommended dose in adults is 200 mg a day. One 100mg tablet should be taken in the morning and one in the evening. It must be taken preferably with or after food.

 

Children:

Alofen is not recommended for use in children under the age of 18.

 

  • Tablets should be swallowed whole with plenty of water and should be taken with or after food.
  • Do not crush or chew the tablets.
  • Do not exceed the stated daily dose.

 

 

What if you miss a dose?

Take the next dose when needed. Do not take a double dose to make up for a forgotten dose.

                                                                                             

What to do in case of overdose?

If you accidentally take too many Alofen, contact your doctor immediately or go to your nearest hospital casualty department. Please take this leaflet or the box the Alofen came in, with you to the hospital so that they will know what you have taken.

What do you need to know before you take Alofen?

Do not take Alofen:

  • If you are allergic to aceclofenac or any of the other ingredients of this medicine
  • If you are allergic to aspirin or any other NSAIDs (such as ibuprofen, naproxen or diclofenac).
  • If you have taken aspirin or any other NSAIDs and experienced one of the following:
  • asthma attack causing tightness in the chest wheezing and difficulty breathing.
  • runny nose, itching and/or sneezing (irritation of the nose).
  • raised red circular patchy rash on the skin which may have felt itchy or like a sting or burn .
  • a severe allergic reaction known as anaphylactic shock. The symptoms may be life threatening and include difficulty breathing, wheezing, abdominal pain and vomiting.
  • If you have a history of, suffer from, or suspect that you have a ulcer or have vomited blood or passed blood in your feces (black tarry stools).
  • If you have severe kidney disease.
  • If you have established heart disease
  • If you have or have had problems with your blood circulation
  • If you suffer from, or suspect that you have severe liver failure.
  • If you suffer from bleeding or any type of blood clotting
  • If you are pregnant (unless your doctor considers it essential for you to continue to take this medicine)
  • It is not recommended for use in children

 

Warning and Precautions

  • If you suffer from any other form of kidney or liver disease.
  • If you have any of the following disorders, as they may worsen:

– Disorders of the stomach or gut/bowel

– inflammatory bowel disease (ulcerative colitis)

– chronic inflammatory bowel disease (Crohn’s disease)

– ulceration, bleeding or perforation of the stomach or bowel

  • If you suffer from a rare inherited disorder known as porphyria.
  • If you smoke or have diabetes
  • If you have angina, blood clots, high blood pressure, raised cholesterol or other raised body fats such as triglycerides
  • If you suffer from an autoimmune condition known as systemic lupus erythematosus or other connective tissue disorders.
  • If you are infected with chicken pox, the use of this medicine should be avoided because a rare serious infection of the skin may develop.
  • If you are recovering from major surgery.
  • If you are elderly (your doctor will prescribe you the lowest effective dose over the shortest duration).

 

 

Alofen and other medications

Tell your doctor or pharmacist if you are taking, have recently taken or might take any other medicines.

 

Pregnancy, breast-feeding and fertility

If you are pregnant or breast-feeding, think you may be pregnant or are planning to have a baby, ask your doctor or pharmacist for advice before taking this medicine. You should inform your doctor if you have problems becoming pregnant. NSAIDs may make it more difficult to become pregnant. Do not take Alofen if you are pregnant or think you are pregnant. It is not recommended for use in pregnancy unless considered essential by your doctor. It must not be used during the last three months of pregnancy.

 

Alofen should not be used if you are breast-feeding. It is not known if this medicine passes into breast milk. It is not recommended for use during breast-feeding unless considered essential by your doctor.

 

Driving and using machines

If you are taking this medication and you experience dizziness, drowsiness, vertigo, tiredness or any difficulty with your eyesight, you must not drive or use machinery.

 

What are the possible side effects?

Common side effects are: Abdominal pain, Constipation, Diarrhea, Nausea and vomiting, Skin rash.

Mechanism of action:

Aceclofenac is a NSAID that inhibits both isoforms of Cyclooxygenase enzyme, a key enzyme involved in the inflammatory cascade. COX-1 enzyme is a constitutive enzyme involved in prostacyclin production and protective functions of gastric mucosa whereas COX-2 is an inducible enzyme involved in the production of inflammatory mediators in response to inflammatory stimuli. Aceclofenac displays more selectivity towards COX-2 than COX-1, which promotes its gastric tolerance compared to other NSAIDs. Although the mode of action of aceclofenac is thought to mainly arise from the inhibition of synthesis of prostaglandins (PGE2), aceclofenac also inhibits the production of inflammatory cytokines, interleukins (IL-1β, IL-6), and tumor necrosis factors (TNF). It is also reported that aceclofenac also affects the cell adhesion molecules from neutrophils.

 

 

 

Pharmacokinetic properties:

Absorption:  Aceclofenac is rapidly and completely absorbed from the gastrointestinal tract and circulates mainly as unchanged drug following oral administration. Peak plasma concentrations are reached around 1.25 to 3 hours post-ingestion, and the drug penetrates into the synovial fluid where the concentration may reach up to 60% of that in the plasma.

 

Volume of distribution: The volume of distribution is approximately 25 L.

 

Protein binding: It is reported to be highly protein-bound (>99%).

 

Metabolism: 4′-hydroxyaceclofenac is the main metabolite detected in plasma however other minor metabolites include diclofenac, 5-hydroxyaceclofenac, 5-hydroxydiclofenac, and 4′-hydroxydiclofenac 2. It is probable that the metabolism of aceclofenac is mediated by CYP2C9.

 

Route of elimination: The main route of elimination is via the urine where the elimination accounts for 70-80% of clearance of the drug 2. Approximately two thirds of the administered dose is excreted via the urine, mainly as glucuronidated and hydroxylated forms of aceclofenac 11. About 20% of the dose is excreted into feces.

 

Half–life: The mean plasma elimination half-life is approximately 4 hours.

 

Drug Interactions:

Tell your doctor or pharmacist if you are taking , have recently taken or might take any other medicines. Please tell your doctor if you are taking:

  • medicines used to treat mental health problems like depression (selective serotonin-reuptake inhibitors (SSRIs) such as citalopram, escitalopram, fluoxetine, fluvoxamine, paroxetine and sertraline) or manic depression (lithium)
  • medicines used to treat heart failure and irregular heart beats (cardiac glycosides such as digoxin)
  • medicines used to treat high blood pressure (antihypertensives: ACE inhibitors such as enalopril, lisinopril; angiotensin II receptor antagonists such as losartan, candesartan; also hydralazine, methyldopa, clonidine, moxonidine, propranalol)
  • medicines to treat infection (quinolone antibiotics such as ciprofloxacin, ofloxacin, levofloxacin, moxifloxacin)
  • drugs used to increase the rate of urine excretion (diuretics such as thiazides, furosemide amiloride hydrochloride)
  • medicines that stop blood clotting (anticoagulants) such as warfarin, heparin
  • methotrexate which is used to treat cancer and autoimmune disorders such as arthritis and skin conditions
  • mifepristone
  • any steroids for the treatment of swelling and inflammation (glucocorticoids such as hydrocortisone, prednisolone,)
  • medicines used to suppress the immune system after organ transplant (ciclosporin or tacrolimus)
  • medicines used to treat HIV (zidovudine)
  • medicines used to lower blood sugar levels in diabetes (antidiabetics such as glibenclamide, glicazide, tolbutamide)
  • any other painkiller NSAID drugs (aspirin, ibuprofen, naproxen, COX-2 inhibitors such as celecoxib and etoricoxib)
  • antiplatelet drugs such as clopidogrel.
x