For the use of a Registered Medical Practitioner or a Hospital or a Laboratory only.
Diclofenac Sodium Suppositories 12.5/25/50/100 mg.
Composition
Each suppository contains: Diclofenac Sodium BP Excipients 12.5 mg/25 mg/50 mg/100 mg.
Pharmacodynamics
Diclofenac sodium is a phenyl acetic acid derivative and a non-steroidal anti-inflammatory agent with analgesic, anti-inflammatory and anti- pyretic properties. Diclofenac is an inhibitor of cyclo-oxygenase and therefore reduces prostaglandin synthesis. Reduction in prostaglandin levels reduces the inflammatory response by the body.
Pharmacokinetics
Absorption: Absorption is rapid; although the rate of absorption is slower than from gastro-resistant tablets administered orally. After the administration of suppositories, peak plasma concentrations are attained on average within 1 hour, but maximum concentrations per dose unit are about two thirds of those reached after administration of gastro-resistant tablets (1.95±0.8g/ml (1.9μg/ml =5.9μmol/l).
Distribution: The active substance is 99.7 & protein bound, mainly to albumin (99.4%). Diclofenac enters the synovial fluid, where maximum concentrations are measured 2-4 hours after the peak plasma values have been attained. The apparent half-time for elimination from the synovial fluid is 3-6 hours. Two hours after reaching the peak plasma values, concentrations of the active substance are already higher in the synovial fluid than they are in the plasma and remain higher for up to 12 hours.
Metabolism: Biotransformation of diclofenac takes place partly by
glucuronidation of the intact molecule, but mainly by single and multiple
hydroxylation and methylation, resulting in several phenolic metabolites,
most of which are converted to glucuronide conjugates. Two phenolic metabolites
are biologically active, but to a much lesser extent than diclofenac.
Elimination: Total systemic clearance of diclofenac in plasma is 263+56 ml/min
(mean value SD). The terminal half-life in plasma is 1-2 hours. Four of the
metabolites, including the two active ones, also have short plasma half-lives
of 1-3 hours. About 60% of the administered dose is excreted in the urine as
the glucuronide conjugate of the intact molecule and as metabolites, most of
which are also converted to glucuronide conjugate. Less than 1% is excreted as
unchanged substance. The rest of the dose is eliminated as metabolites through
the bile in the feaces.
Indications
LOFNAC belongs to the group of non-steroidal agents with marked analgesic, anti-inflammatory and antipyretic properties. It is indicated in acute joint inflammations (arthritis), gout attacks, chronic joint inflammations, especially when several joints are affected (chronic polyarthritis/rheumatoid arthritis), Bechterew's disease (ankylosing spondylitis) and other inflammatory rheumatoid disorders of the spine. It is also used in acute inflammatory condition of degenerative joint or spinal disorders (arthroses and spondylarthroses), soft tissue rheumatisms, painful swelling or inflammation after injuries or minor surgeries.
Dosage and administration
Adults: (LOFNAC 50/100 preferably used) The usual dose is 75-150 mg daily, in
divided doses. The recommended maximum daily dose of is 150 mg. Children:
(LOFNAC 12.5/25 preferably used).
Children: (aged 1-12 years) with juvenile chronic arthritis: 1-3 mg/kg per day.
Children (aged 6-12 years) with Acute post-operative pain: 1-2 mg/kg per day.
In children, treatment of acute post-operative pain should be limited to 4 days
treatment (12.5 mg and 25 mg suppositories only). a Daily dosage can be
administered in 2-3 divided doses depending on the severity of the disease
condition OR as directed by the physician. Suppository should be inserted into
the anus preferably after clearing the bowel.
Contraindications
Hypersensitivity to the active substance or any of the excipients.
Active, gastric or intestinal ulcer, bleeding or perforation.
- History of gastrointestinal bleeding or perforation, relating to previous NSAID therapy.
- Active, or history of recurrent peptic ulcer/hemorrhage (two or more distinct episodes of proven ulceration or bleeding).
- Last trimester of pregnancy.
- Severe hepatic, renal or cardiac failure.
- Like other non-steroidal anti-inflammatory drugs (NSAIDs), diclofenac is also contraindicated in patients in whom attacks of asthma, angioedema, urticaria or acute rhinitis are precipitated by ibuprofen, acetylsalicylic acid or other nonsteroidal anti-inflammatory drugs.
- Proctitis.
- Established congestive heart failure (NYHAII-IV), ischemic heart disease, peripheral arterial disease and/or cerebrovascular disease.
Pregnancy and Lactation
Inhibition of prostaglandin synthesis may adversely affect the pregnancy andler the embryofetal development. Data from epidemiological studies an increased risk of miscarriage and or cardiac malformation and gastroschisis after use of a prostaglandin synthesis inhibitor in early pregnancy. Like other NSAIDs, diclofenac passes into breast milk in small amounts. Therefore, Diclofenac should not be administered during pregnancy and breast feeding in order to avoid undesirable effects in the infant.
Interactions
LOFNAC should be used with caution when concomitantly administered with drugs such as lithium, digoxin, diuretics, anti-hypertensives, glucocorticoids, methotrexate acetyl-salicylic acid, other NSAIDS, SSRI, cyclosporin, tacrolimus, drugs known to cause hyperkalemia, quinolone antibacterials, phenytoin, colestipol, cholestyramine, cardiac glycosides and potent CYP2C9 inhibitors.
NSAIDS should not be used for 8-12 days after mifepristone administration as NSAIDs can reduce the effect of mifepristone.
Side-effects
Common side effects observed are headache, dizziness, vertigo, increased transaminases nausea, vomiting, diarrhea, dyspepsia, abdominal pain, flatulence, anorexia and rash. Rare or very rare side effects may be seen are anemia, agranulocytosis, hypersensitivity, oedema, depression, insomnia, imitability, psychotic disorder, somnolence, tiredness, memory impairment, convulsion, anxiety, tremor, aseptic meningitis, taste disturbances, confusion, hallucinations, malaise, visual disturbance, tinnitus, hearing impaired, palpitations, hypertension, hypotension, asthma, pneumonitis, gastritis, gastrointestinal ulcer, constipation, stomatitis, pancreatitis, jaundice, liver disorder, eczema, erythema, dermatitis exfoliative, loss of hair, photosensitivity reaction, purpura, allergic purpura, pruritus, acute renal failure, hematuria, proteinuria, nephrotic syndrome, interstitial nephritis, renal papillary necrosis, application site irritation, oedema, impotence.
Overdose
There is no typical clinical picture resulting from diclofenac over dosage. Over dosage can cause symptoms such as headache, nausea, vomiting, epigastric pain, gastrointestinal bleeding, diarrhea, dizziness, disorientation, excitation, coma, drowsiness, tinnitus, fainting or convulsions. In the case of significant poisoning acute renal failure and liver damage are possible.
Storage
Store below 30°C, protect from light.
Keep out of the reach and sight of children.
Not to be taken orally.
For rectal administration only.
How to use Suppository
- When practical, clean the area around the rectum with mild soap and warm water and rinse thoroughly Gently dry by patting or blotting with toilet tissue or a soft cloth.
- Do not open suppository if it seems soft, hold the foil wrapper under cold water or place it in refrigerator for few minutes to harden it before removing the wrapper.
- Position the patient to lie on one side with knees bent up to their abdomen or lie on back with feet and legs held up.
- Detach the suppository by holding strip upright and carefully peel the wrapper evenly down both sides. (moisten the suppository if dry)
- Hold the suppository between index finger and thumb, locate the anus and gently insert suppository tip end first with the index finger. The suppository should be fully inserted into rectum against the wall of rectum.
- Hold buttocks together lying down for about 5 minutes to avoid having the suppository comes out.
- Discard used materials and wash your hands thoroughly.
BLISS GVS PHARMA LTD.
Mfd. by:
lobale Dewan Udyog Nagar, Aliyali, Palghar, Maharashtra - 401 404, INDIA, Regd. Off. 102, Hyde Park, Saki Vihar Road, Andheri (E), Mumbai - 400 072, INDIA.
email: 0018888306075/ drug.safety@blissgvs.com.
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