Paracetamol + Nimesulide + Tizanidine Pharmacology

Paracetamol + Nimesulide + Tizanidine

About Paracetamol + Nimesulide + Tizanidine
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Mechanism of Action of Paracetamol + Nimesulide + Tizanidine
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Pharmacokinets of Paracetamol + Nimesulide + Tizanidine
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Onset of Action for Paracetamol + Nimesulide + Tizanidine
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Duration of Action for Paracetamol + Nimesulide + Tizanidine
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Half Life of Paracetamol + Nimesulide + Tizanidine
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Side Effects of Paracetamol + Nimesulide + Tizanidine
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Contra-indications of Paracetamol + Nimesulide + Tizanidine
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Special Precautions while taking Paracetamol + Nimesulide + Tizanidine
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Pregnancy Related Information
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Old Age Related Information
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Breast Feeding Related Information
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Children Related Information
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Indications for Paracetamol + Nimesulide + Tizanidine
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Interactions for Paracetamol + Nimesulide + Tizanidine
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Typical Dosage for Paracetamol + Nimesulide + Tizanidine
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Schedule of Paracetamol + Nimesulide + Tizanidine
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Storage Requirements for Paracetamol + Nimesulide + Tizanidine
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Effects of Missed Dosage of Paracetamol + Nimesulide + Tizanidine
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Effects of Overdose of Paracetamol + Nimesulide + Tizanidine
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Paracetamol

About Paracetamol
Acetanilide derivative, Non narcotic Analgesic,Antipyretic.
Mechanism of Action of Paracetamol
Paracetamol has analgesic and antipyretic action.
It is more active on cyclo-oxygenase enzyme in brain. Peripherally it is a poor inhibitor of prostaglandin synthesis.
Analgesic action: Paracetamol raises the pain threshold and produces analgesic effect.
Antipyretic action: Paracetamol lowers fever by direct action on the thermoregulatory centre in the Hypothalamus and block the effects of endogenous pyrogen.
Pharmacokinets of Paracetamol
Absorption: Paracetamol is rapidly and completely absorbed after oral administration.
Distribution: It is distributed mostly in the body in unbound form.
Metabolism: It is extensively metabolised in the liver.
Excretion: Excreted in the urine.
Onset of Action for Paracetamol
30 - 60 minutes
Duration of Action for Paracetamol
6 hours
Half Life of Paracetamol
1-4 hours
Side Effects of Paracetamol
1. Nausea
2. Abdominal distress
3. Allergic reactions
4. Rash
Contra-indications of Paracetamol
1. Hypersensitivity to Paracetamol
Special Precautions while taking Paracetamol
1. Hepatic impairment
2. Renal impairment
3. Hypertension
Pregnancy Related Information
Use with caution
Old Age Related Information
Use with caution
Breast Feeding Related Information
Use with caution
Children Related Information
Use with caution
NEONATES : Contraindicated
Indications for Paracetamol
1. To relieve pain and fever
2. Acute gout
3. Migraine
Interactions for Paracetamol
Cholestyramine: Reduces absorption of paracetamol.
Charcoal: Activated, administered immediately reduces absorption of paracetamol.
Domperidone and metochlopramide: Enhance absorption of paracetamol.
Alcohol: Chronic excessive ingestion of alcohol potentiates hepatotoxicity of paracetamol.
Zidovudine: Effects zidovudine may be decreased.
Typical Dosage for Paracetamol
Adult:
500 - 1000 mg in 3 times daily
Maximum dose: 4 g / day
For migraine: 500 mg to be taken at the first sign of migraine attack and repeated 4 - 6 hourly until suppress mild attacks.
Children:
60 mg / kg body weight /day in 4 divided doses.
Schedule of Paracetamol
H
Storage Requirements for Paracetamol
Store at 15-30 degree C in a tightly closed container. Protect from heat and moisture. Keep out of the reach of children.
Effects of Missed Dosage of Paracetamol
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 Paracetamol
Give supportive measures and symptomatic treatment. Drug can be removed from the body by gastric lavage or by inducing emesis. Absorption of the drug can be reduced by administration of activated charcoal. N-acetylcysteine is the specific antidote for Paracetamol poisoning. Dose: 150 mg /kg body weight as IV infusion over 15 minutes followed by same dose over 20 hours.
Maintenance dose: 75 mg / kg orally every 4 - 6 hours for 2 - 3 days. Haemodialysis can be done in emergency conditions.

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

Tizanidine

About Tizanidine
A centrally acting a-2 adrenergic agonist, Centrally acting muscle relaxant (short-acting).
Mechanism of Action of Tizanidine
This drug is a centrally acting alpha2 agonist at alpha2-adrenergic receptor sites and presumably reduces spasticity by increasing presynaptic inhibition of motor neurons. This results the blocking of nerve impulses (or pain sensations) that are sent to your brain.
Pharmacokinets of Tizanidine
Absorption- Completely absorbed after oral administration.
Distribution- Widely distributed throughout the body. 30% bound to the plasma proteins.
Metabolism- Metabolized in the liver to its metabolites.
Excretion- Excreted through urine.
Onset of Action for Tizanidine
1 to 2 hrs after oral administration
Duration of Action for Tizanidine
N/A
Half Life of Tizanidine
N/A
Side Effects of Tizanidine
1. Dizziness
2. Upset stomach
3. Vomiting
4. Tingling sensation in the arms, legs, hands, and feet
5. Dry mouth
6. Increased muscle spasms
7. Yellowing of the skin or eyes
8. Unexplained flu-like symptoms
Contra-indications of Tizanidine
1. Contraindicated in patients with hypersensitivity to the drug or any ingredients of it
Special Precautions while taking Tizanidine
1. Kidney disease
2. Liver disease
3. Low blood pressure or are on medication to treat high blood pressure
4. Birth control pills use
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Use with caution
Indications for Tizanidine
1. Painful muscle spasm associated with static and functional disorders of the spine
2. Following surgery for disc prolapse/osteoarthritis of the hip
Interactions for Tizanidine
Alcohol & other CNS depressants : CNS effects of tizanidine potentiated.
Typical Dosage for Tizanidine
Oral-
Adult-
Muscle spasm - 2 mg thrice a day.
Spasticity- Initial dose 6 mg/day in 3 divided doses, then increase stepwise to 12-36 mg/day.
Schedule of Tizanidine
N/A
Storage Requirements for Tizanidine
Store at room temperature away from moisture and heat.
Effects of Missed Dosage of Tizanidine
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 Tizanidine
Give symptomatic and supportive treatment.

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