Piroxicam


Thông tin thuốc gốc
Chỉ định và Liều dùng
Oral
Ankylosing spondylitis, Osteoarthritis, Rheumatoid arthritis
Adult: As cap/orodispersible tab: Max: 20 mg daily as a single dose, or in divided doses if necessary. Review treatment benefit and tolerability within 14 days. Use lowest effective dose for the shortest possible duration based on individual overall risk assessment.
Elderly: Use the lowest effective dose for the shortest possible duration.

Topical/Cutaneous
Pain and inflammation
Adult: As 0.5% gel: Apply 1,000 mg (3 cm) to the affected area 3-4 times daily. Review treatment benefit and tolerability after 4 weeks.
Special Patient Group
CYP2C9 is the primary enzyme involved in the metabolism of piroxicam to form its major inactive metabolite, 5’-hydroxy-piroxicam. Individuals who lack CYP2C9 enzyme activity, known as CYP2C9 poor metabolisers, may experience higher exposure to piroxicam and increased risk of its side effects . CYP2C9*2 and *3 are the 2 allelic variants associated with reduced enzyme activity. The *2 allele is more common in Caucasians (10-20%) than in Asian (1-3%) or African (0-6%) population while the *3 allele is less common (<10% in most populations) and extremely rare in African populations.

CYP2C9 poor metabolisers (carriers of 2 decreased function alleles e.g. *2/*2, *3/*3, *2/*3)
May consider dose reduction in patients who are known or suspected to be CYP2C9 poor metabolisers (based on genotype or previous history/experience with other CYP substrates such as warfarin, phenytoin) as they may have abnormally high plasma piroxicam levels due to its reduced metabolic clearance.

CYP2C9*2 and CYP2C9*3 are genetic polymorphisms present in individuals with reduced CYP2C9 activity. Limited data from 2 published studies indicated that individuals with heterozygous CYP2C9*1/*2 (n=9), heterozygous CYP2C9*1/*3 (n=9), and homozygous CYP2C9*3/*3 (n=1) genotypes showed 1.7-, 1.7-, and 5.3-fold higher piroxicam systemic levels, respectively, as compared with individuals with CYP2C9*1/*1 (n=17) normal metaboliser genotype following single oral dose administration. The mean elimination half-life values of piroxicam for individuals with CYP2C9*1/*3 (n=9) and CYP2C9*3/*3 (n=1) genotypes were 1.7- and 8.8-fold higher as compared with CYP2C9*1/*1 (n=17).
Cách dùng
Should be taken with food.
Chống chỉ định
Hypersensitivity (including history of asthma, bronchospasm, nasal polyps, rhinitis, angioedema, urticaria, or other allergic-type reactions) to piroxicam, aspirin or other NSAIDs. Active peptic ulcer, gastrointestinal bleeding, inflammatory bowel disease; history of gastrointestinal disorders that predispose to bleeding disorders (e.g. ulcerative colitis, Crohn’s disease, cancer, diverticulitis); history of gastrointestinal ulceration, bleeding or perforation; history of serious cutaneous allergic reactions (e.g. erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis); severe heart failure. Treatment of perioperative pain in the setting of CABG surgery. Pregnancy (3rd trimester). Concomitant use with aspirin, anticoagulants, and other NSAIDs including COX-2 inhibitors.
Thận trọng
Patients with mild to moderate CHF, ischaemic heart disease, peripheral arterial disease, cerebrovascular disease, CV events risk factors (e.g. hypertension, hyperlipidaemia, diabetes mellitus, smoking); bronchial asthma, coagulation disorders, cirrhosis, nephrotic syndrome, overt renal disease, dehydration, hypovolaemia; undergoing surgical or dental procedures. Women with conceiving difficulties, undergoing infertility treatment or on investigation of infertility. Debilitated patients. Renal and hepatic impairment. Elderly. Children (topical). Pregnancy (1st-2nd trimester) and lactation. CYP2C9 poor metabolisers.
Phản ứng phụ
Significant: New onset or exacerbation of hypertension, hyperkalaemia, Na and fluid retention, oedema, bronchospasm, reversible female infertility, delayed ovulation, serum sickness, haematologic effects (e.g. anaemia, decreased platelet aggregation, prolonged bleeding time). Rarely, interstitial nephritis, papillary necrosis, nephrotic syndrome, renal failure.
Blood and lymphatic system disorders: Leucopenia, eosinophilia, thrombocytopenia.
Cardiac disorders: Palpitation.
Ear and labyrinth disorders: Tinnitus.
Eye disorders: Blurred vision, eye irritation and swelling.
Gastrointestinal disorders: Nausea, vomiting, constipation, flatulence, abdominal pain, diarrhoea, dyspepsia, stomatitis.
General disorders and admin site conditions: Malaise, application site reactions (e.g. irritation, erythema, pruritus, dermatitis).
Hepatobiliary disorders: Jaundice.
Investigations: Increased LFTs, increased weight.
Metabolism and nutrition disorders: Anorexia, hyperglycaemia, hypoglycaemia.
Nervous system disorders: Headache, dizziness, somnolence, vertigo, paraesthesia.
Psychiatric disorders: Depression, insomnia, confusion, mood alterations, nervousness, hallucination.
Respiratory, thoracic and mediastinal disorders: Dyspnoea.
Skin and subcutaneous tissue disorders: Rash, pruritus, photosensitivity (topical).
Vascular disorders: Vasculitis, epistaxis.
Potentially Fatal: Gastrointestinal inflammation, ulceration, bleeding and perforation; CV thrombotic events including MI and stroke, severe hepatic reactions (e.g. fulminant hepatitis, hepatic necrosis, hepatic failure), exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis, anaphylactoid reactions.
PO: C (prior to 30 weeks gestation), D (starting at 30 weeks gestation)
Thông tin tư vấn bệnh nhân
This drug may cause dizziness, drowsiness, fatigue and visual disturbances, if affected, do not drive or operate machinery. Topical: Do not apply to sites affected by open lesions, dermatoses or infection.
MonitoringParameters
Monitor blood pressure during initiation and throughout therapy; occult blood loss, Hb, haematocrit, serum electrolytes, renal and hepatic function tests periodically. Perform periodic ophthalmologic exam (prolonged use).
Quá liều
Symptoms: Lethargy, drowsiness, nausea, vomiting, epigastric pain, low-grade fever, sinus tachycardia. Rarely, hypertension, gastrointestinal bleeding, acute renal insufficiency, respiratory depression and coma. Management: Symptomatic and supportive treatment. May consider administration of activated charcoal within 1 hour of ingestion or osmotic cathartic within 4 hours of ingestion or with large overdosage.
Tương tác
Increased risk of gastrointestinal ulceration or bleeding with antiplatelet agents, SSRIs, corticosteroids. May exacerbate cardiac failure, decrease GFR, and increase plasma levels of cardiac glycosides. Increased risk of nephrotoxicity with ciclosporin and tacrolimus. May interfere with the natriuretic effects of diuretics. May increase plasma levels of lithium. May antagonise the hypotensive effects of antihypertensive agents. May decrease excretion of methotrexate, leading to acute toxicity. May increase risk of convulsion with quinolones. May interfere with mifepristone mediated termination of pregnancy.
Potentially Fatal: May enhance effects of anticoagulants (e.g. warfarin). Increased risk of serious gastrointestinal events with aspirin and other NSAIDs.
Food Interaction
May slightly delay the rate of absorption with food. Increased risk of gastrointestinal bleeding with alcohol.
Lab Interference
May result to false-positive aldosterone/renin ratio (ARR).
Tác dụng
Description: Piroxicam, an oxicam derivative NSAID, reversibly inhibits cyclooxygenase-1 and -2 (COX-1 and -2) enzymes thereby resulting in decreased formation of prostaglandin precursors. It has analgesic, anti-inflammatory and antipyretic properties.
Onset: Analgesia: Oral: Within 1 hour; Max effect: 3-5 hours.
Pharmacokinetics:
Absorption: Well absorbed from the gastrointestinal tract. Slightly delayed rate of absorption with food. Time to peak plasma concentration: 3-5 hours.
Distribution: Enters breast milk. Volume of distribution: 0.14 L/kg. Plasma protein binding: 99%.
Metabolism: Extensively metabolised in the liver via hydroxylation of the pyridyl ring side chain followed by conjugation with glucuronic acid.
Excretion: Via urine and faeces (<5% as unchanged drug). Elimination half-life: Approx 50 hours.
Đặc tính

Chemical Structure Image
Piroxicam

Source: National Center for Biotechnology Information. PubChem Database. Piroxicam, CID=54676228, https://pubchem.ncbi.nlm.nih.gov/compound/Piroxicam (accessed on Jan. 22, 2020)

Bảo quản
Store between 20-25°C.
Phân loại ATC
M02AA07 - piroxicam ; Belongs to the class of non-steroidal antiinflammatory preparations for topical use. Used in the treatment of joint and muscular pains.
M01AC01 - piroxicam ; Belongs to the class of non-steroidal antiinflammatory and antirheumatic products, oxicams.
References
Dean L. Piroxicam Therapy and CYP2C9 Genotype. Medical Genetics Summaries [Internet]. Bethesda (MD): National Center for Biotechnology Information (US). 2019 Feb. Accessed 24/07/2019. PMID: 30742401

Annotation of FDA Label for Piroxicam and CYP2C9. Pharmacogenomics Knowledgebase (PharmGKB). https://www.pharmgkb.org/. Accessed 24/07/2019.

Anon. CYP2C9 - Piroxicam. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 24/07/2019.

Anon. Piroxicam (Systemic). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 24/07/2019.

Anon. Piroxicam. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 24/07/2019.

Buckingham R (ed). Piroxicam. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 24/07/2019.

Feldene Melt 20 mg (Pfizer Limited). MHRA. https://products.mhra.gov.uk/. Accessed 24/07/2019.

Joint Formulary Committee. Piroxicam. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 24/07/2019.

Piroxicam 0.5% w/w Gel (Torrent Pharma Ltd.). MHRA. https://products.mhra.gov.uk/. Accessed 24/07/2019.

Piroxicam Capsule (Teva Pharmaceuticals USA, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 24/07/2019.

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