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- Pharmacology For Methocarbamol + Nimesulide
Methocarbamol + Nimesulide Pharmacology
Methocarbamol + Nimesulide
About Methocarbamol + NimesulideN/AMechanism of Action of Methocarbamol + NimesulideN/APharmacokinets of Methocarbamol + NimesulideN/AOnset of Action for Methocarbamol + NimesulideN/ADuration of Action for Methocarbamol + NimesulideN/AHalf Life of Methocarbamol + NimesulideN/ASide Effects of Methocarbamol + NimesulideN/AContra-indications of Methocarbamol + NimesulideN/ASpecial Precautions while taking Methocarbamol + NimesulideN/APregnancy Related InformationN/AOld Age Related InformationN/ABreast Feeding Related InformationN/AChildren Related InformationN/AIndications for Methocarbamol + NimesulideN/AInteractions for Methocarbamol + NimesulideN/ATypical Dosage for Methocarbamol + NimesulideN/ASchedule of Methocarbamol + NimesulideN/AStorage Requirements for Methocarbamol + NimesulideN/AEffects of Missed Dosage of Methocarbamol + NimesulideN/AEffects of Overdose of Methocarbamol + NimesulideN/AMethocarbamol
About MethocarbamolA centrally acting skeletal muscle relaxant, Carbamate derivative, Skeletal muscle relaxant.Mechanism of Action of MethocarbamolThis skeletal muscle relaxant depresses central nervous system by the preferential blockade of spinal and supraspinal polysynaptic reflexes. This leads to sedation and a reduction in skeletal muscle spasms. These effects are accompanied by relief of pain and an increase in the mobility of the affected muscles. Pain relief is postulated to be due to alterations in the perception of pain.Pharmacokinets of MethocarbamolAbsorption- Rapidly and completely absorbed after administration
Distribution- Widely distributed throughout the body. It crosses the placenta
Metabolism- Extensively metabolized in the liver to its metabolites, by dealkylation and hydroxylation
Excretion- Drug and its metabolites are excreted rapidly and completely in urineOnset of Action for Methocarbamol30 minutes after oral administration
Immediate after IV administration
Duration of Action for Methocarbamol4-6 hoursHalf Life of Methocarbamol0.9 to 2.2 hoursSide Effects of Methocarbamol1. Drowsiness
2. Dizziness
3. Upset stomach
4. Blurred vision
5. Fever
6. Rash
7. Itching
8. Dyspepsia
9. Jaundice
10. Nausea
11. Vomiting
12. Leucopenia
Contra-indications of Methocarbamol1. Hypersensitive to methocarbamol or to any of the tablet components
2. Epilepsy
3. Coma or pre-coma
4. Myasthenia gravis
Special Precautions while taking Methocarbamol1. Alcohol abuse
2. CNS depressants therapy
3. Impairment of hepatic function
4. Renal impairment
5. Any work which require mental alertness such as driving or operating machine
Pregnancy Related InformationUse with cautionOld Age Related InformationUse with cautionBreast Feeding Related InformationUse with cautionChildren Related InformationUse with cautionIndications for Methocarbamol1. Skeletal muscle spasm
2. Surgery
3. Orthopedic procedure
4. Neurological diseases
5. TetanusInteractions for MethocarbamolAlcohol and other CNS depressant drugs: CNS depressant effect potentiated.
Anorectics and anticholinergics: Efficacy increased by methocarbamol.
Lab tests: Causes colour interference in certain screening tests for 5-hydroxy-indoleacetic acid (5-HIAA) and Vanillyl mandelic acid (VMA).Typical Dosage for MethocarbamolAdults-
Oral-
500 mg -initial dosage, 3 tablets 4 times daily
Maintenance dosage- 2 tablets 4 times daily
750 mg - initial dosage, 2 tablets 4 times daily
Maintenance dosage, 1 tablet q.4 h, or 2 tablets 3 times daily
Intravenous-
Tetanus-
2-3g over 10-15 minutes
Then 2g ampules every 6 hours until oral therapy can be started by dose of 18-40 tablets of 500mg daily in divided doses, 4-6 hourly by nasogastric tube.
Children-
Initial dose -15mg / kg. Repeat every 6 hours.
Schedule of MethocarbamolHStorage Requirements for MethocarbamolStore at room temperature away from heat and direct light. Keep out of the reach of children.Effects of Missed Dosage of MethocarbamolTake 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 MethocarbamolGive symptomatic and supportive treatment. Induce emesis or gastric lavage. Monitor urine output and vital signs regularlyNimesulide
About NimesulideCOX-2 selective NSAID, Analgesic,antipyretic.Mechanism of Action of NimesulideThis 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 NimesulideAbsorption-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 Nimesulide30 to 60 minutesDuration of Action for Nimesulide8-10 hoursHalf Life of NimesulideIts plasma half life is long-nearly 2daysSide Effects of Nimesulide1. 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 Nimesulide1. Hypersensitivity to this drug
2. Active peptic ulcer
3. Hepatic impairment
Special Precautions while taking Nimesulide1. 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 InformationContraindicatedOld Age Related InformationUse with cautionBreast Feeding Related InformationContraindicatedChildren Related InformationUse with cautionIndications for Nimesulide1. 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 NimesulideFenofibrate, 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 NimesulideOral-
Adults - 100 mg two times daily.
Children - 5mg/kg/day divided in 2 or 3 doses.
Schedule of NimesulideHStorage Requirements for NimesulideStore in cool, dark, dry placeEffects of Missed Dosage of NimesulideTake 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 NimesulideEmpty the stomach if necessary. Symptomatic treatment should be given
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