Drotaverine + Aceclofenac Pharmacology
Drotaverine + Aceclofenac
2.Dysmenorrhoea
Drotaverine
Distribution: It is widely distributed in protein bound form.
Metabolism: Extensively metabolised in the liver.
Excretion: It is excreted mainly with the bile.
2.Headache
3.Tachycardia
4.Nausea
5.Vertigo
2.Severe renal impairment
3.Severe hepatic impairment
4.Severe cardiac impairment
2. Hepatic impairment
3. Cardiac impairment.
NEONATES: contraindicated
2.Gastrointestinal colic pain
3.Renal colic pain
4.Dysmenorrhoea
5.Uterine neck spasm
6.Post MTP(Medical termination of pregnancy)
7.Post D&C(Dilatation and curettage)
8.Post surgical spasm
9.Irritable bowel syndrome
Oral: 120 - 240 mg / day in 3 divided doses.
Children: 60 - 120 mg / day in 3 divided doses, dose is depending upon the age of the patient.
Parenteral (IM)
Induction of labour: 40 mg every 2 hours, maximum 3 doses.
Keep out of the reach of children
Aceclofenac
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
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
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.
2. Bleeding from the stomach or intestines
3. Moderate to severely decreased kidney function
4. Hypersensitivity to other NSAIDs
5. Active peptic ulcer
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
2. Osteoarthritis
3. Symptomatic treatment of pain and inflammation in Post-Traumatic pain
4. Cervical pain
5. Low back pain
6. Acute gout
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.
Adult (general dose)-
100mg twice daily
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