Nimesulide + Racemethionine Pharmacology

Nimesulide + Racemethionine

About Nimesulide + Racemethionine
N/A
Mechanism of Action of Nimesulide + Racemethionine
Nimesulide leads to inhibition of superoxide anion generation in vitro by activated neutrophils, inhibition of histamine release from tissue mast cells and basophils, it causes inhibition of platelet activating factor synthesis in stimulated human neutrophils and inhibition of synthesis of metaloproteinase thus preventing breakdown of osteoarthritic human cartilage. Racemethionine restores the hepatic concentrations of glutathione. Thus, it serves as a precursor for the synthesis of glutathione and sulfate. It is also a great antioxidant as the sulfur it supplies inactivates free radicals. It thus has a role in the treatment of arthritis pain as well as chronic liver disease. Racemethionine contributes to the synthesis of S-adenosylmethionine, which promotes production of cartilage proteoglycans, and is therapeutically beneficial in osteoarthritis.
Pharmacokinets of Nimesulide + Racemethionine
N/A
Onset of Action for Nimesulide + Racemethionine
N/A
Duration of Action for Nimesulide + Racemethionine
N/A
Half Life of Nimesulide + Racemethionine
N/A
Side Effects of Nimesulide + Racemethionine
1.Nausea
2.Diarrhea
3.Vomiting
4.Rash
5.Dizziness
6.Somnolence
7.Headache
Contra-indications of Nimesulide + Racemethionine
1.Active peptic ulcer
2.Moderate-to-severe hepatic impairment
Special Precautions while taking Nimesulide + Racemethionine
1.Renal impairment
2.Heart failure
3.Cirrhosis
4.Vol or salt depleted patients
5.Metabolic acidosis,
6.Patients with a history of severe hepatic impairment
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
N/A
Indications for Nimesulide + Racemethionine
Pain and inflammation
Interactions for Nimesulide + Racemethionine
1.Fenofibrate, salicylic acid, valproic acid and tolbutamide displace nimesulide from its plasma binding sites
2.Nimesulide displaces methotrexate and furosemide from plasma proteins
3.Nimesulide should be used with caution along with warfarin since efficacy may be increased
4.Nimesulide may decrease the efficacy of slow release theophylline preparations
5.Concurrent use of levodopa with racemethionine may decrease the therapeutic effects of levodopa
Typical Dosage for Nimesulide + Racemethionine
Adult: Per tablet contains nimesulide 100 mg and racemethionine 50 mg: 1 tablet bid.
Child: 5 mg/kg/day (Nimesulide) divided in 2-3 daily doses.
Schedule of Nimesulide + Racemethionine
N/A
Storage Requirements for Nimesulide + Racemethionine
N/A
Effects of Missed Dosage of Nimesulide + Racemethionine
N/A
Effects of Overdose of Nimesulide + Racemethionine
N/A

Nimesulide

About Nimesulide
COX-2 selective NSAID, Analgesic,antipyretic.
Mechanism of Action of Nimesulide
This Non Steroidal Anti Inflammatory Drug reduces prostaglandin synthesis by the inhibition of cyclo oxygenase enzyme2 selectively. This is a weaker inhibition .So it produces weaker analgesic property. Its potent anti-inflammatory activity is due to its action on various stages of inflammation. This leads to the inhibition of super oxide anion formation invitro by activated neutrophil, inhibition of histamine release from tissue mast cells and basophiles. Additionally it also prevents platelet activating factor synthesis and metalloproteinase synthesis thus prevents the breakdown of osteoarthritic human cartilage. It also prevent tumor necrosis factor alpha and thus reduce the formation of cytokines. This drug can activate glucocorticoid receptors in the body.
Pharmacokinets of Nimesulide
Absorption-Completely absorbed after oral administration.
Distribution-Widely distributed in the body and extensively bind to the plasma proteins i.e.99%.
Metabolism-It is metabolized in liver to its metabolites.4-hydroxyl derivative is its one active metabolite.
Excretion - Excreted via urine and bile.
Onset of Action for Nimesulide
30 to 60 minutes
Duration of Action for Nimesulide
8-10 hours
Half Life of Nimesulide
Its plasma half life is long-nearly 2days
Side Effects of Nimesulide
1. Nausea
2. Vomiting
3. Diarrhea
4. Heart burn
5. Epigastric pain
6. Pruritis
7. Skin rash
8. Headache
9. Dizziness
10.Somnolence
Contra-indications of Nimesulide
1. Hypersensitivity to this drug
2. Active peptic ulcer
3. Hepatic impairment
Special Precautions while taking Nimesulide
1. Renal impairment
2. Heart failure
3. Alcohol abuse
4. Colitis
5. Crohns disease
6. Diverticulitis
7. Gastric ulcer
8. Diabetis mellitus
9. Hemarrhoids
10. Hepatic failure
11. Rectal irritation or bleeding
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Use with caution
Indications for Nimesulide
1. Painful inflammatory conditions associated with -
Musculoskeletal system, Dysmenorrhea, Thrombophlebitis, Gout
2. Dental pain
3. ENT infection
4. Osteoarthritis
5. Rheumatoid arthritis
6. Gynecological disorder
7. Low back pain
8. Post operative pain
9. Fever


Interactions for Nimesulide
Fenofibrate, Salicyclic acid, Valproic acid and Tolbutamide: These drugs displace nimesulide from the plasma binding sites.
Methotrexate and Frusemide: These drugs may be displaced from plasma proteins by nimesulide.
Warfarin: Exercise caution since efficacy may be increased.
Theophylline: Efficacy of slow release theophylline preparations reduced.
Typical Dosage for Nimesulide
Oral-
Adults - 100 mg two times daily.
Children - 5mg/kg/day divided in 2 or 3 doses.
Schedule of Nimesulide
H
Storage Requirements for Nimesulide
Store in cool, dark, dry place
Effects of Missed Dosage of Nimesulide
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose

Effects of Overdose of Nimesulide
Empty the stomach if necessary. Symptomatic treatment should be given

Racemethionine

About Racemethionine
A sulfur containing essential amino acid , Urinary Acidifier, paracetamol antidote.
Mechanism of Action of Racemethionine
Racemethionine is a urine acidifier. Racemethionine produces ammonia-free urine by lowering the urinary pH. Along with Paracetamol, Racemethionine provides a liver friendly analgesic and antipyretic Acidifier.
Racemethionine enhances the synthesis of glutathione and is used as an alternative to Acetylcysteine in the treatment of paracetamol poisoning to prevent hepatotoxicity.
It maintain hepatic concentrations of glutathione which is required to inactivate an hepatotoxic intermediate metabolite of acetaminophen.In acetaminophen overdose, excessive quantities of this metabolite are formed because the primary metabolic pathways (glucuronide and sulfate conjugation) become saturated. The excess metabolite binds irreversibly to essential hepatic proteins and enzymes, causing cell damage and death. Racemethionine serves as a precursor for the synthesis of glutathione and sulfate.

Pharmacokinets of Racemethionine
N/A
Onset of Action for Racemethionine
N/A
Duration of Action for Racemethionine
N/A
Half Life of Racemethionine
N/A
Side Effects of Racemethionine
1.Drowsiness
2.Nausea
3.Vomiting
Contra-indications of Racemethionine
1.Acidosis
2.Severe liver disease
Special Precautions while taking Racemethionine
1.Acidosis
2.Hepatic impairment
3.Allergies
Pregnancy Related Information
May be used
Old Age Related Information
May be used
Breast Feeding Related Information
Use with caution
Children Related Information
May be used
Indications for Racemethionine
1. Urinary acidifier
2. Paracetamol poisoning
Interactions for Racemethionine
N/A
Typical Dosage for Racemethionine
As directed by the physician
As urinary acidifier:
Adults : 200 mg 3 or 4 times a day.
Children: Same as adult dose


Schedule of Racemethionine
N/A
Storage Requirements for Racemethionine
Store away from heat and direct light. Keep out of the reach of children. Keep the medicine from freezing. Do not refrigerate.

Effects of Missed Dosage of Racemethionine
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Do not double the dose. Continue the regular schedule
Effects of Overdose of Racemethionine
Give supportive measures and symptomatic treatment.

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