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Information for Doctors

Arthritis and Drug Therapy
Nonsteroidal Anti Inflammatory Drugs                    Jointace Tablets  750 mg (B.I.D) Glucosamine + MSM + Co-factors
Classification of NSAIDs                                      The  most trusted & widely prescribed glucosamine brand
Mechanism of Action
Prescribing information on drugs used in arthritis
OPIOD ANALGESICS
  Tramadol hydrochloride

NONOPIOD ANALGESICS

  Aspirin:
  Celecoxib

  Propionic acid derivatives: Ibuprofen, Naproxen, Ketoprofen, Fenoprofen, Flurbiprofen:

Indol derivatives
  Indomethacin
Gold compounds
  Auranofin
Para-amino phenol derivatives
  Phenacetin and paracetamol (Acetaminophen)
Anthranilic acid derivates:
  Mephenamic acid and flufenamic acid
  Piroxicam
  Meloxicam
  Diclofenac sodium
  Nimesulide
  Sulphasalazine
Newer drug therapies
  Glucosamine sulphate
  Rofecoxib
  Intra-articular sodium hyaluronate injection description
  Leflunomide
  Nabumetone

Introduction

Nonsteroidal Anti Inflammatory Drugs:

NSAID are commonly prescribed for the management of arthritis, dysmenorrhea, ureteric and postoperative pain, soft tissue injuries etc.

Clasification of NSAIDs:

  1. Salicyclic acid derivatives: Aspirin
  2. Propionic acid derivatives: Ibuprofen, ketoprofen
  3. Fenamates (anthranilic acids): Mefenamic acid
  4. Paraaminophenol derivatives: paracetamol
  5. Pyrazolones: phenylbutazone, oxyphenbutazone
  6. Indol derivatives: Indomethacin
  7. Aryl acetic acid derivatives: Diclofenac
  8. Oxicam derivatives: piroxicam, tenoxicam, meloxicam
  9. Pyrrolo - pyrrole derivatives: ketorolac
  10. Alkanones: Nabumatone
  11. Sulfonanilide derivatives: Nimesulide

Mechanism of Action:

Most of the currently available NSAIDs inhibit both cyclooxygenase isoenzymes. The aim in developing selective COX-2 inhibitors is to improve NSAIDs tolerability. Although all NSAIDs inhibit prostaglandin

(PG) synthesis by blocking cyclooxygenase (COX) activitiy, the older and newer generation NSAIDs differ in their effect on two cyclooxygenase isoenzymes. A drug profile characterised by preferential COX-l inhibition is associated with greater potential for gastrotoxicity, while preferential or selective cox-2 inhibition is associated with decreased gastrotoxicity. The selective COX-2 inhibitors seem to have similar other effects, increasing blood pressure and reducing renal function, as the nonselective COX inhibitors. Patients with history of aspirin sensitivity should not be given selective COX-2 inhibitors as yet no published data is available to show that this is safe for patients.

NSAIDs should be used with caution in patients of impaired renal or cardiac function or patients with previous history of peptic ulcer and in elderly.

Prescribing information on drugs used in arthritis:

OPIOD ANALGESICS:

 

Tramadol hydrochloride: It is a analgestic which acts on opiate receptors in the C.N.S. to produce opiate like analgesia, but at therapeutic doses of 1mg/kg it does not produce respiratory depression or other side effects typical of a opiate analgesic. It has anti-tussive effects. No drug dependence or tolerance occurs.

Indications: Severe acute and chronic pain, diagnostic procedures and surgical pains.

 

Dosage: 50 to 100mg 2 to 3 times daily. Max: 4Omg total daily dose.

 

Contraindications: Hypersensitivity, acute C. N. S intoxication due to alcohol, analgesics, or psychotropics.

 

Special precautions: Alcohol, not to drive or operate machinery.

 

Paediatrics: Should not be used in children below 16 years.

 

Pregnancy: Safety not established

 

Lactation: Not recommended

 

Elderly: Reduced dose may be necessary.

 

Side effects: Sweating, nausea, vomiting, animation, stupor.

 

Drug interactions: Concomitantly administrated tranquilisers, hypnotics intensifies sedative effects. Fatal interaction with MAOIs. Opioid analgesics like buprenophine, butorphanol, and pentazocine precipitate withdrawal symptoms.

NONOPIOD ANALGESICS:

Aspirin: It is acetylsalicyclic acid which is potent anti-inflammatory and good analgesic.

 

Indications: Analgesic (headache, backache, myalgia, joint pain, toothache, neuralgias, dysmenorrhoea), antipyretic, acute rheumatic fever, rheumatoid arthritis, osteoarthritis.

 

Dosage: Analgesic antipyretic: 0.3 -0.6gm three times. Acute rheumatic conditions: 4 -6 gm or 75 -100 mg/kg/day in divided doses.

 

Contra-indications: Hypersensitivity, peptic ulcer, liver disease, bleeding tendencies and haemophilia, children suffering from chicken pox or influenza, pregnancy, avoided in diabetics and in juvenile rheumatoid arthritis and should be stopped before surgery.

 

Special- precautions: Aspirin may precipitate bronchospasm and induce asthmatic attack in susceptible subjects. It may induce gastro intestinal haemorrhage, occassionaly major. Use with caution in subjects with gout.

 

Paediatrics: Not recommended under 12 years

 

Pregnancy: Contraindicated

 

Lactation: Use With caution

 

Elderly: No special problem

 

Side effects: Nausea, vomiting, epigastric distress, occult blood loss in stools, dizziness, tinnitus, vertigo, impairment of hearing and vision, excitment and mental confusion, hyperventilation and electrolyte imbalance. Drug interaction following concurrent use of aspirin with heparin, coumarin or corticoid derivatives, methotrexate, sulfonylureas, probenecid and sulfinpyrazone and spironolactone.

Celecoxib:

It is a NSAID, which has COX -2 selectivity. Chemically, it is a diary substituted pyrazole.

 

Indications: Relief of the signs and symptoms of osteoarthritis, rheumatoid arthritis in adults.

 

Dosage and administration: Osteoarthritis: 200 mg per day administered as a single dose or as 100mg twice per day.

 

Rheumatoid arthritis: 100 -200mg twice per day

 

Contraindications: It is contraindicated in patients with known hypersensitivity to celecoxib. It should not be.given to patients who have experienced allergic type reactions to sulfonamides / aspirin or other NSAIDs.

 

Special precautions: Geriatric: Dosage adjustment in the elderly is not generally necessary.

 

Pediatric: Not investigated in pediatric patients below 18 years of age.

 

Hepatic insufficiency: Patients with moderate hepatic impairment requires dose reduction. Celecoxib is generally not recommended in severe hepatic patients.

 

Renal insufficiency: No significant relationship was found between GFR and Celecoxib clearance.

 

Side effects: Most commonly reported adverse effect include headache, diarrhoea, rhinitis, nausea, sinusitis, dyspepsia and abdominal pain.

 

Special precautions: Patients with prior history of ulcer disease or GI bleeding, moderate to severe hepatic impairment. GI toxicity can occur with or without warning symptoms in patients treated with NSAIDs.

 

Drug Interactions: Concomitant use of celecoxib with aspirin or other NSAIDs may increase the incidence of gastric ulcer. Fluconazole increases the concentration of celecoxib.

Celecoxib increases the concentration of lithium in the blood.

Propionic acid derivatives:

Ibuprofen, Naproxen, Ketoprofen, Fenoprofen, Flurbiprofen: All have similar pharmacodynamic properties but vary considerably in potency and to some extent in duration of action.

 

Indications: Analgesic, antipyretic, rheumatoid arthritis, osteoarthritis, musculoskeletal disorders, soft tissue injuries, post operatively, acute gout.

 

Dosage: Ibuprofen 200 -600mg daily or as required.

 

Naproxen: 250mg twice daily, ketoprofen: 50mg twice or thrice daily

 

Fenoprofen: 300 -600mg thrice daily, flurbiprofen: 150 -200mg daily in divided doses, max. 300mg.

 

Contra-indications: Pregnancy, active peptic ulcer, G.I. bleeding, lactation

 

Special Precautions: Asthma, bleeding disorders, cardiovascular disease and those receiving coumarin anticoagulants, Aspirin / anti-inflammatory induced allergy

 

Side - Effects: G. I. intolerance, rash, rarely jaundice, thrombocytopenia, oedema.

 

Drug Interactions: Asprin displaces ibuprofen from serum binding sites, reduces serum levels of flurbiprofen. N aproxen and Ketoprofen enhances effects of oral anticoagulants, phenytoin, methotrexate, sulphonamides, sulphonylureas, hypoglycaemics. Probenecid increase their concentration.

Indol derivatives:

Indomethacin: It is a potent anti-inflammatory and promptly acting antipyretic but it relieves only inflammatory or tissue injury related pain.

 

Indication: Rheumatoid arthritis not controlled by aspirin, ankylosing spondylitis, destructive arthropathies and psoriatic arthritis, acute gout.

 

Dosage: Adults: 25 -50mg 2. -6 times daily

 

Neonates: 0.2 mg/kg/dose for 3 doses 12 hourly.

 

Contraindication: Machinery operators, drivers, psychiatric patients, epileptics, kidney disease, hypersensitivity.

 

Special Precautions: Active peptic ulcer, Renal or hepatic dysfunction.

 

Paetiiatrics: Usually not prescribed.

 

Lactation: Unsafe

 

Elderly: Reduced dose is necessary

 

Side effects: Gastric inrritation, nausea, anorexia, gastric bleeding diarrhoea, frontal headache, dizziness, mental confusion, hallucination, depression, psychosis, can induce asthma.

 

Drug Interaction: With salicylates, lithium, anticoagulants, corticosteroids, diuretics, B-blockers, probenecid

Gold compounds:

Auranofin: It is considered to be the most effective agent for arresting the rheumatoid process. It reduces macrophage and lysosomal activity but the exact mechanism is not known. It has an effect on synovial membrane and collagen to prevent joint destruction; may induce healing of bony erosions. It is effective in psoriatic arthropathy also.

Indications: Rheumatoid arthritis

Dosage: 6 mg daily in 2 div. doses or as a single dose for minimum 3 –6 months. If response inadequate increase to max. 3 mg thrice daily

Contra-indications: Pregnancy, lactation, severe blood dyscrasias, progressive renal disease, severe hepatic disorder, SLE, history of necrotising enterocolitis, pulmonary fibrosis, exfoliative dermatitis, bone marrow aplasia.

Special precautions: Periodically monior blood counts and urinary protein. Women of child bearing potential should use effective contraception during and atleast 6 months after treatment. Renal and hepatic dysfunction. History of bone marrow depression

Paediatrics: Not recommended

Pregnancy: Contraindicated

Lactation: Contraindicated

Elderly: No special problems

Side effects: Diarrhoea, nausea, abdominal pain, ulcerative enterocolitis, taste disturbance, pulmonary fibrosis, nephrotic syndrome.

Drug interactions: Potentiation of other myelosuppressive drugs, increased level of phenytoin, penicillamine, chelates gold.

Para-amino phenol derivatives:

Phenacetin and paracetamol (Acetaminophen): Paracetamol is a valuable central analgesic but weak peripheral anti-inflammatory agent and exhibits good and prompt antipyretic action. It does not stimulate respiration, or alter acid base balance and causes less gastric irritation and have no effect on cellular metabolism or clotting factors. It is not uricosuric.

Indications: Pain, fever.

Dosage: 0.5 –1 gm upto 4gm daily in divided doses

Special precautions: Renal and hepatic impairment

Side-Effects: Nausea, rashes, leukopenia is rare.

Drug interactions: Enhances oral anticoagulant activity. Absorption increased by metaclopromide. Absorption reduced by pethidine, propanthline. Alcohol (chronic use) potentiates hepatotoxicity by paracetamol.

Anthranilic acid derivates:

Mephenamic acid and flufenamic acid: Mephenamic acid exerts peripheral as well as central analgesic action.

Indications: Analgesic in muscle, joint and soft tissue pain. Dysmennorrhoea. Rheumatoid and osteo arthritis, antipyretic

Dosage: 250 -500mg thrice daily

Contra-indications: Hypersensitivity, Epilepsy.

Special precautions: Pregnancy, lactation, C. N. S. depressants.

Side -effects: Diarrhoea, epigastric distress, skin rashes, dizziness, haemolytic anaemia.

Drug Interactions: Enhances activity of oral anticoagulants.

Piroxicam:

It is anti-inflammatory potency is similar to indomethacin and analgesic action is greater than aspirin. It has useful antipyretic property.

Indications: Rheumatoid arthritis, osteoarthritis, ankylosing spondylitis. Acute musculo-skeletal disorders. Acute gout.

Dosage: Rheumatoid arthritis, osteoarthritis, ankylosing spondylitis: 20mg daily as single dose. Maint.10-30mg.

Acute Musculo-skeletal disorders: 40 mg in a single or divided doses for 7-14 days.

Acute gout:40 mg as a single dose. Maint: 40mg in single or divided doses for 4-6 days.

Contra-indications: Hypersensitivity, Pregnancy, children, patients who develop asthma or allergy with other inflammtory drugs, lactation.

Special precautions: Renal or hepatic dysfunction, asthma, surgery, haemorrhagic disorders, hypertension, cardiovascular disease.

Paediatrics: Not recommended in age below 6 yrs.

Pregnancy: Contraindicated, may affect the foetus.

Lactation: Safety not established.

Side-Effects: Heartburn, nausea, anorexia, rashes, pruritus, C.N.S. manifestations, Oedema.

Drug Interactions: Potentiate anticoagulants. Diuretics increase risk of renal damage. Monitor lithium levels. Aspirin reduces serum levels.

Meloxicam:

It is a new NSAID which has greater inhibitory action against the inducible form of cyclo-oxygenase (cox-2) which is implicated in the inflammatory response than against the constitutive form of this enzyme (cox-I) inhibition of, which is associated with gastric, renal and other adverse effects.

Indication: Rheumatoid arthritis, osteoarthritis and ankylosing spondylitis.

Dosage: 7.5 to 15mg once daily.

Contraindications: Hypersensitivity

Drug interactions: No special drug interaction.

Diclofenac sodium:

It has a powerful anti-inflammatory action besides its analgesic and antipyretic actions. It is an inhibitor of prostaglandin synthesis.

Indications: Rheumatoid arthritis, osteoarthritis, low back pain, ankylosing spondylitis, gout, acute musculo skeletal disorders, periarthritis (Frozen shoulder), tendinitis, tenosynovitis, bursitis, sprains and dislocation, painful post-operative condition, pain following dental surgery, painful inflammatory conditions in gynaecology.

Dosage: 100-500mg daily in 2-3 divided doses. Maintenance therapy: 50-100mg in divided doses.

Contra-indication: Active or recurrent peptic ulcers. Hypersensitivity, asthmatic patients in whom attacks of asthma are precipitated by aspirin or other NSIDS, pregnancy, lactation.

Special precautions: Patients having history of G.I. ulceration, haematemesis or malena, ulcerative colitis, Crohn's disease, cardiac, and renal insufficiency, elderly patients.

Side effects: Epigastric pain, nausea, diarrhoea, tiredness, insomnia, skin rash, itching, retention of fluid.

Drug interactions: Increase blood levels of lithium and digoxin, inhibits diuretics but potentiates potassium sparing diuretics. Methotrexate toxicity enhanced.

Nimesulide:

It is a analgesic and antipyretic in action apart from its anti inflammatory action. It is absorbed rapidly and completely after oral administration. It acts by inhibiting the release of tumor necrosis factor-alpha, acts as a competitive inhibitor of histamine release and reduces superoxide anion formation.

Indication: Rheumatoid arthritis, osteoarthritis, other degenerative joint disorders, muscloskeletal disorders, low back pain and in ENT inflammations.

In children: Fever and URTI.

Dosage: Adults: l00mg twice daily

Children: 5mg/kg/day in 2 or 3 divided doses.

Contraindications: Hypersensitivity, active peptic ulcer disease, hepatic impairment.

Special precautions: Active peptic ulcer, elderly patients with moderate renal impairment, congestive heart failure or cirrhosis.

Paediatrics: Reduced dose is necessary.

Pregnancy: Contraindicated

Lactation: Use with c~ution

Elderly: Use only, if clearly indicated.

Side Effects: Epigastric pain, heart bum, nausea, diarrohea, vomiting, skin rash, pruritis, dizziness, somnolescence, headache.

Drug Interactions: Displace methotrexate from its binding sites, decrease the plasma level of theophyline, oral bioavailability of frusemide may be reduced, displaced by the concomitant use of fenofibrate, salicyclic acid, valproic acid.

Sulphasalazine:

Indications: Rheumatoid arthritis

Dosage: 1g/day for 3-5 days, increase over next 3-5 days to 1.5g/day, and thereafter 2g/day. Max: 3g/day or more may be needed for clinical improvement.

Contraindications: Hypersensitivity to sulphas and salicylates, G6PD deficiency, intestinal or urinary obstruction, acute intermittent porphyria, blood dyscrasias.

Special precautions: Hepatic/renal damage, Uraemia, proteinuria, allergic bronchial asthma, neonates, diabetes, rheumatoid arthritis.

Paediatrics: Not recommended, under 2 years. Reduce dose in children above 2 years.

Pregnancy: No evidence of risk to developing baby. Folic acid supplement may be required.

Lactation: The drug passes into the breast milk, and may affect the baby.

Side-Effects: Hypersensitivity, renal and hepatic toxicity, fibrosing alveolitis, anorexia, ringing in ears, fever, headache, nausea, loss of apetite, nephritis, myocarditis.

Drug Interactions: Plasma levels reduced by rifampicin and ethambutol. Interferes with absorption of digoxin, and folic acid.

Newer Drug Therapies

Glucosamine sulphate:

Glucosamine sulphate is an amino sugar, which builds up the volume of naturally present glucosamine in the body. This increased glucosamine level, in turn, accelerates the biosynthesis of building blocks of cartilage, i.e., proteoglycans and collagens.

Indications: In painful conditions of osteoarthritis and rheumatoid arthritis, where aspirin and other NSAIDs fail to provide a satisfactory relief

Dosage: 500mg orally three times daily for up to three months. This intake may have to be adjusted for obese individuals (at approximately 20mg/kg body weight) including those taking diuretics, thereafter 1000mg/day as a nutritional maintenance, as the arthritic condition improves.

Safety: Glucosamine sulphate has an excellent safety record in both animal and human investigations, should be considered as a supplement of choice for nutritional correction of rheumatic disorders, can be safely taken alongside orthodox pain controlling medications.

Contradications: Not recommeneded in pregnancy and lactation.

Side effects: Adverse effects are reported as minimal. The most common side effects were epigastric pain, tenderness (3.5%ofpatients), heartburn (2.7%), diarrhoea (2.5%) and nausea   (1 %). Drowsiness, headache and insomnia occured rarely (less than 1 %)

Drug interactions: No reports of drug interactions were located.

Rofecoxib

Introduction: Rofecoxib is a new NSAID that exhibits anti -inflammatory, analgesic and antipyretic activities in animal models. The mechanism of action of rofecoxib is believed to be due to inhibition of prostaglandin synthesis, via cox -2 inhibition. At therapeutic concentrations in humans Roficoxib does not inhibit the COX -I isoenzyme. Clinical studies have demonstrated that rofecoxib is an effective therapy for the management of acute pain and hip or knee osteoarthritis.

Indication, dosage and administration: Osteoarthritis (OA) -12.5mg OD. May be increased to 25mg OD. Acute pain and primary dysmenorrhoea -50mg OD

Contradiction: Hypersensitivity, asthma, urticaria, or allergic –type reaction after taking aspirin or other NSAIDs

Precaution and warnings: Not recommended in patients with prior history of ulcer disease or GI bleeding, elderly debilitated patients, moderate or severe hepatic insufficiency, advanced kidney disease and preexisting asthma.

Pregnancy: Use only if clearly needed. Avoid use during third trimester.

Lactation: Taking into account the importance of the drug to the mother discontinue nursing or discontinue the drug.

Paediatric use: Safety and effectiveness below the age of 18 years have not been evaluated.

Geriatric use: Initiate therapy with the lowest recommended dose.

Adverse effects: Generally well tolerated, Side effects are mild and transient. Commonly reported side effects: nausea, dyspepsia, epigastric discomfort, heartburn, diarrhoea, headache and dizziness, abdominal pain, oedema / fluid retention, hypertension, pruritus, increase in ALT/AST, decreased haematocrit have also been reported.

Drug interaction: No clinically important interaction reported with antacids or cimetidine, ketoconazole, prednisolone, oral contraceptives and digoxin ACE -inhibitors, furosemide, low-dose aspirin, methotrexate, midazolam, rifampicin, warfarin.

Overdosage: In the event of overdose, general supportive measures may be used.

Storage: Store below 25 C, protected from moisture.

Intra-articular sodium hyaluronate injection description:

The drug used for viscosupplementation is a sterile, nonpyrogenic, elastoviscous fluid containing sodium hyaluronate, a derivative of hyaluronan (sodium salt of hyaluronic acid) and consists of repeating disacharide units of N-acetylglucosamine and sodium glucuronate. It is in buffered physiological sodium chloride solution (pH 6.8-7.5)

Indications:

  • Used in temporary replacement and supplement for synovial fluid
  • Indicated for the treatment of pain in osteoarthritis
  • Beneficial in patients with early stage joint pathology

Contradications:

  • Do not administer to patients with known hypersensitivity to hyaluronate preperations.
  • Do not give if venous or lymphatic stasis is present in leg
  • Should not be used in infected or severely inflamed joints
  • Intra-articular injections are contraindicated in cases of infections or skin diseases in the area of injection site.

Warnings:

  • Do not inject intravascularly
  • Do not concomitantly use disinfectants containing quarternary ammonium salts for skin preperation because hyaluronic acid precipitate in their presence.
  • Anaphylactoid and allergic reactions have been reported with this product.

Dosage and administration:

The recommened treatment is 5 injections in the knee, 1 week apart. The maximum recommended dosage is 6 injections within 6 months with a minimum of 4 weeks between treatment regimens.

Leflunomide:

Description: Leflunomide is a pyrimidine synthesis inhibitor.

Mechanism of Action: Is an isoxazole immunomodulatory agent which inhibits dihydroorotate dehydrogenase (an enzyme invloved in de novo pyrimidine synthesis) and has antiproliferative activity. Several in vivo and in vitro experimental models have demonstrated an anti-inflammatory effect.

Elimination: The active metabolite MI is eliminated by further metabolism and subsequent renal excretion as well as by direct biliary excretion.

Hepatic insufficiency: The use in patients with hepatic insufficiency is not recommended.

Drug infections: No significant drug interaction with oral contraceptives, cimetidine and warfarin. Can be coprescribed with NSAlDs.

Methotrexate: No pharmacokinetic interaction between the drugs. However, co-administration increased risk of hepatotoxicity.

Rifampin: Caution should be used if patients are to receive both leflunomide and rifampin.

Indications and usage: It is indicated in adults for the treatment of active rheumatoid arthritis (RA) to reduce signs and symptoms and to retard structural damage as evidenced by radiological erosions and joint space

narrowing. Aspirin, nonsteroidal anti-inflammatory agents and/or low dose corticosteroids may be continued during treatment with it. The combined use with antimalarials, intramuscular or oral gold, D penicillamine, azathioprine, or methotrexate has not been adequately studied.

Contradications: It is contraindicated in patients with known hypersensitivity to it or any of the other components of it. It can cause fetal harm when administered to a pregnant woman. It is contraindicated in women who are or may become pregnant. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential hazard to the fetus.

Warnings: Immunosuppression potential: It is not recommended for patients with severe immunodeficiency bone marrow dysplasia, or severe uncontrolled infections. There have been rare reports of pancytopenia in patients receiving this drug. If evidence of bone marrow supression occurs in a patient taking the medication treatment should be stopped, and cholestyramine or charcoal should be used to reduce the plasma concentration of active metabolite.

Skin reactions: Rare cases of stevens-johnson syndrome and toxic epidermal necrolysis have been reported in patients receiving the drug.

Hepatotoxicity: In clinical trials, treatment was associated with elevations of liver enzymes, primarily ALT and AST, in a significant number of, patients; these effects were generally reversible.

Pre-existing Hepatic Disease: Given the possible risk of increased hepatotoxicity, and the role of the liver in drug activation, elimination and recycling, the use is not recommended in patients with significant hepatic impairment or evidence of infection with hepatitis B or C viruses.

Malingancy: Longer-term studies would be needed to determine whether there is an increased risk of malignancy or lymphoproliferative disorders.

Use in women of childbearing potential: There are no adequate and well-controlled studies evaluating leflunomide in pregnant women. However, based on animal studies, may increase the risk of fetal death or teratogenic effects when administered to a pregnant woman.

Nursing Mothers: It should not be used by nursing mothers

Use in males: To minimize any possible risk, men wishing to father a child should consider discontinuing use of medicine and talking cholestyramine 8 grams 3 times daily for 11 days.

Pediatric use: The safety and efficacy of 1eflunomide in the pediatric population have not been studied. Use in patients less than 18 years of age is not recommended.

Geriatric use: No dosage adjustment is needed in patients over 65.

Adverse reactions: Adverse reactions associated with the use in RA include diarrhea, elevated liver enzymes (ALT and AST), alopecia and rash.

Drug abuse and dependence: It has no known potential for abuse or dependence.

Dosage and administration: Loading dose therapy to be initiated with a loading dose of 100mg per day for 3 days. Maintenance Therapy: Daily dose of 20mg is recommended for treatment of patients with RA.

Nabumetone (Naphthylkanone derivatives)

Action: Inhibits prostaglandin synthesis

 

Metabolism: It is a pro-drug that is activated by oxidation in the liver.

 

Adverse reactions:

  • Lesser gastrointestinal side effects

  • Hepatotoxicity

Caution:

  • Since it is inactivated in liver, caution should be excersised in hepatic impairement.

Dosage: 1,000 to 2,000 mg daily in single or decided dose

 

Availability: 500 and 750 mg tablets