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Diclofenac mechanism of action
inhibits the biosynthesis of prostaglandins.
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Therapeutic indications diclofenac
rheumatoid arthritis, ankylopoietic spondyloarthritis, osteoarthritis, spondyloarthritis, extra-articular rheumatism, tto. symptomatic of the acute attack of gout, inflammations and post-traumatic swellings. Treatment symptomatic of: pain associated with renal colic, musculoskeletal pain; severe acute pain associated with low back pain, postoperative and post-traumatic pain; mild to moderate pain (headache, dental, menstrual, muscle or back pain). Dysmenorrhea 1 aria .
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Dosage diclofenac
– Rheumatoid arthritis, ankylopoietic spondyloarthritis, osteoarthritis, spondyloarthritis, extra-articular rheumatism, tto. symptomatic of acute attack of gout, inflammations and post-traumatic swellings ad.: oral: 50 mg/8-12 h before meals; max. 150mg/day. Retard: 75-150 mg/day. Rectal: 100 mg/day, at bedtime. IM: 75 mg/day (exceptionally 75 mg/12 h on the 1st day in severe cases).
– Treatment symptomatic of pain associated with renal colic, musculoskeletal pain, ads.: rectal: 100 mg/day. IM: 75 mg/day.
– Treatment symptomatic of intense acute pain associated with low back pain, postoperative and post-traumatic pain, ads.: IM: 75 mg/day.
– Treatment symptomatic of mild to moderate pain (headache, dental, menstrual, muscular or back pain): oral. ads. and children > 14 years: 25 mg followed by 12.5 or 25 mg/4-6 h; max: 75 mg/day. Treatment duration for pain relief: 5 days and for feverish conditions: 3 days.
Rectal: If higher doses are necessary, supplement with 50 mg orally.
MI: max. 2 days, continue tto. orally or rectally.
– Dysmenorrhea 1 aria : oral and rectal: initial: 50-100 mg/day, adjust individually up to 200 mg/day.
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Mode of administration diclofenac
N/A
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Contraindications diclofenac
hypersensitivity to diclofenac; when the administration of ASA or other NSAIDs has triggered asthma attacks, urticaria or acute rhinitis; sick active Crohn’s; active ulcerative colitis; severe RI; IHa serious; coagulation disorders; history of treatment-related gastrointestinal bleeding or perforation. previous with NSAIDs; active gastrointestinal ulcer/bleeding/perforation; Established CHF (NYHA classification II-IV), ischemic heart disease, enf. peripheral arterial and/or enf. cerebrovascular; third trimester of pregnancy; proctitis (rectal).
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Warnings and precautions diclofenac
Mild to moderate IR, mild to moderate IH, elderly, porphyria, history of ulcerative colitis or disease. of Crohn’s, history of AHT and/or insuf. cardiac arrest, concomitant use of oral corticosteroids and SSRI antidepressants. In patients with asthma, seasonal allergic rhinitis, inflammation of the nasal mucosa (nasal polyps), enf. Chronic obstructive pulmonary disease or chronic respiratory tract infections (allergic rhinitis) are more frequent exacerbations of asthma, Quincke’s edema or urticaria. With cardiovascular risk factors (diabetes mellitus, hypertension, hypercholesterolemia, smoking), assess benefit/risk. Do not use in patients with severe cardiovascular pathology such as heart failure. cardiac, ischemic heart disease, enf. peripheral arterial disease or cerebrovascular. Risk of gastrointestinal bleeding, ulceration or perforation is > at increasing doses of NSAIDs. in treatment prolonged risk of atherothrombotic events (AMI or stroke). Allergic reactions, including anaphylactic/anaphylactoid reactions, may occur in rare cases with diclofenac when there has been no prior exposure to the drug. Hypersensitivity reactions can also progress to Kounis syndrome, a severe allergic reaction that can lead to myocardial infarction.; mask signs and symptoms of an infection and impair female fertility. Avoid concomitant use with other NSAIDs including selective cyclooxygenase-2 inhibitors. Liver, kidney and blood count control. Not recommended in < 14 years. Use the lowest possible dose and duration of tto. shortest possible time to control the symptoms according to the established therapeutic objective. Concomitant with anticoagulants, could increase the risk of bleeding. NSAIDs, including diclofenac, may increase the risk of gastrointestinal anastomotic leak. Close monitoring and caution when using diclofenac after gastrointestinal surgery.
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Hepatic insufficiency diclofenac
Contraindicated in severe IH. Caution in mild to moderate IH, it can cause liver enzyme elevations; tto. prolonged control liver function.
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Kidney failure diclofenac
Contraindicated in severe IR. Caution in mild to moderate IR, control of renal function.
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Diclofenac interactions
see Prec. In addition:
Increases plasma concentration of: lithium and digoxin.
Increases action and toxicity of: methotrexate.
Increases nephrotoxicity of: cyclosporine.
Decreases action of: diuretics or antihypertensive drugs such as beta-blockers, ACE inhibitors.
Decreases efficacy of: isradipine, verapamil.
Reduced efficacy by: cholestyramine, colestipol.
Close monitoring with: anticoagulants.
Increased frequency of occurrence of adverse effects with systemic NSAIDs.
Potency toxicity of: misoprostol and corticosteroids.
Plasma concentration increased by: strong CYP2C9 inhibitors (sulfinpyrazone and voriconazole).
Plasma concentrations decreased with: CYP2C9 inducers (such as rifampin).
Increases exposure of: phenytoin (monitor plasma levels).
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Pregnancy diclofenac
During the first and second trimester of pregnancy, it should not be administered unless it is considered strictly necessary. If used in a woman trying to become pregnant or during the first and second trimesters of pregnancy, the dose and duration of treatment should be reduced as much as possible.
During the third trimester of pregnancy, all prostaglandin synthesis inhibitors can expose the fetus to: cardiopulmonary toxicity (with premature closure of the ductus arteriosus and pulmonary hypertension); renal dysfunction, which may progress to renal failure with oligohydroamniosis; possible prolongation of bleeding time, due to an antiplatelet-like effect that can occur even at very low doses; inhibition of uterine contractions, which may cause delay or prolongation of labour. Consequently it’s contraindicated during the third trimester of pregnancy.
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Breastfeeding diclofenac
Diclofenac passes into breast milk, in small amounts. Therefore, it should not be administered during lactation to avoid unwanted effects in the infant.
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Adverse reactions diclofenac
headache, dizziness; Vertigo; nausea, vomiting, diarrhea, dyspepsia, abdominal pain, flatulence, anorexia; rash; ischemic colitis; irritation at the application site (rectal); reaction, pain and induration at the injection site. (IM), strictly follow the instructions for IM administration to avoid adverse reactions such as muscle weakness, muscle paralysis, hypoesthesia and necrosis at the injection site. Lab: increased serum transaminases.
Pregnancy
Breastfeeding: caution
Produces photosensitivity reactions.
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