Aceclofenac + Paracetamol Pharmacology

Aceclofenac + Paracetamol

About Aceclofenac + Paracetamol
N/A
Mechanism of Action of Aceclofenac + Paracetamol
N/A
Pharmacokinets of Aceclofenac + Paracetamol
N/A
Onset of Action for Aceclofenac + Paracetamol
N/A
Duration of Action for Aceclofenac + Paracetamol
N/A
Half Life of Aceclofenac + Paracetamol
N/A
Side Effects of Aceclofenac + Paracetamol
N/A
Contra-indications of Aceclofenac + Paracetamol
N/A
Special Precautions while taking Aceclofenac + Paracetamol
N/A
Pregnancy Related Information
Contraindicated. Since Aceclofenac is contraindicated in pregnancy, the combination cannot be used in pregnancy
Old Age Related Information
Use with caution
Breast Feeding Related Information
Lactation: Contraindicated. Since Aceclofenac is contraindicated in lactation, the combination cannot be used in lactation
Children Related Information
N/A
Indications for Aceclofenac + Paracetamol
1.Ankylosing spondylitis
2.Osteoarthritis
3.Rheumatoid Arthritis
4.Dentalgia
5.Pre and post operative pains
6.Acute gout
Interactions for Aceclofenac + Paracetamol
N/A
Typical Dosage for Aceclofenac + Paracetamol
Oral
Adult: 1 tablet should be taken 1 - 2 times daily
Each tablet contains Aceclofenac 100 mg + Paracetamol 500 mg
Schedule of Aceclofenac + Paracetamol
N/A
Storage Requirements for Aceclofenac + Paracetamol
N/A
Effects of Missed Dosage of Aceclofenac + Paracetamol
N/A
Effects of Overdose of Aceclofenac + Paracetamol
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Aceclofenac

About Aceclofenac
NSAID, Analgesic, Antiinflammatory, Anti arthritic.
Mechanism of Action of Aceclofenac
This drug has several mechanism of action.
1. It inhibits cyclooxygenase (COX) activity and to suppress the PGE2 production by inflammatory cells, by inhibiting IL-Beta & TNF in the inflammatory cells (Intracellular Action).
2. It blocks degeneration and stimulates synthesis of extra cellular matrix of cartilages by inhibiting the action of different cytokines.
3. Drug and its metabolites inhibit IL-6 production by human chondrocytes. This leads to inhibition of increase of inflammatory cells in synovial tissue, inhibition of IL-1 amplification, inhibition of increased MMP synthesis and thus ensuring proteoglycan production.
4. It inhibits IL-1 and TNF production by human chondrocytes, inflammatory cells and synovial cells and therefore blocks suppression of GAG and collagen synthesis and stimulates growth factors mediated synthesis of GAG and collagen.
5. 4`-hydroxyaceclofenac a metabolite of aceclofenac inhibits pro MMP1 and pro MMP3 produced by synovial cells (Rheumatoid Synovial Cells) in serum and in synovial fluid and thus inhibits progressive joint destruction by MMPs.
6. Aceclofenac inhibits Neutrophil Adhesion & Accumulation at the inflammatory site in the early phase and thus blocks the pro-inflammatory actions of Neutrophils.
7. Aceclofenac is also an NSAID with greater COX-2 specificity
Pharmacokinets of Aceclofenac
Absorption- It is rapidly and completely absorbed after oral administration
Distribution- Widely distributed in the body as protein-bound form. It is highly protein-bound (>99.7%). Aceclofenac penetrates into the synovial fluid, where the concentrations reach approximately 60% of those in plasma.
Metabolism- Metabolized into metabolites in the liver. Main metabolite is 4-hydroxyaceclofenac
Excretion- It is excreted through urine mainly as conjugated hydroxymetabolites
Onset of Action for Aceclofenac
N/A
Duration of Action for Aceclofenac
N/A
Half Life of Aceclofenac
The mean plasma elimination half-life is 4 - 4.3 hours
Side Effects of Aceclofenac
1. Dyspepsia
2. Abdominal pain
3. Dizziness
4. Vertigo
5. Pruritis
6. Rash
7. Dermatitis
8. Nausea
9. Diarrhoea
10. Flatulence
11. Gastritis
12. Constipation
13. Vomiting
14. Ulcerative stomatitis
15. Elevation of circulating levels of hepatic enzymes.
Contra-indications of Aceclofenac
1. Hypersensitivity to the drug
2. Bleeding from the stomach or intestines
3. Moderate to severely decreased kidney function
4. Hypersensitivity to other NSAIDs
5. Active peptic ulcer
Special Precautions while taking Aceclofenac
1. Hepatic porphyria
2. Bleeding tendencies
3. Blood disorders
4. Crohn`s disease
5. Decreased heart function
6. History of peptic ulcers
7. Inflammation of the bowel and back passage
8. Mildly decreased kidney function
9. Recent major surgery
10. Stomach disorders
11. Decreased liver function
12. Intestinal disorders
Pregnancy Related Information
Contraindicated.
Old Age Related Information
Use with caution.
Breast Feeding Related Information
Contraindicated.
Children Related Information
Use with caution
Indications for Aceclofenac
1. Ankylosing spondylitis
2. Osteoarthritis
3. Symptomatic treatment of pain and inflammation in Post-Traumatic pain
4. Cervical pain
5. Low back pain
6. Acute gout
Interactions for Aceclofenac
Lithium, digoxin and methotrexate: Aceclofenac may increase plasma concentrations of lithium, digoxin and methotrexate.
Anticoagulants: Activity of anticoagulants may be increased.
Diuretics : Aceclofenac inhibits the activity of diuretics. When concomitantly administrated with potassium sparing diuretics, serum potassium should be monitored.
Cyclosporin: Aceclofenac may enhance cyclosporin nephrotoxicity.
Quinolones : Aceclofenac may precipitate convulsions when coadministered with quinolone antibiotics.
Typical Dosage for Aceclofenac
Oral-
Adult (general dose)-
100mg twice daily
Schedule of Aceclofenac
H
Storage Requirements for Aceclofenac
Store below 25?C
Effects of Missed Dosage of Aceclofenac
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 Aceclofenac
Give symptomatic and supportive treatment. Induce gastric lavage and administer charcoal in repeated doses. Treated with antacid if necessary.

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.

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