Parecoxib

Registered South African indications:

• Pain - mild to moderate
• Inflammation

Contraindications 

• Hypersensitivity to the active ingredient or any of its excipients
• Hypersensitivity to sulphonamides 
• History of previous serious allergic drug reaction of any type
• History of acetylsalicylic acid or non-steroidal anti-inflammatory drug allergy
• Pregnancy >30 weeks
• Breastfeeding
• Severe hepatic impairment 
• Active peptic ulceration or gastrointestinal bleeding
• Inflammatory bowel disease
• Congestive heart failure
• Treatment of post-operative pain following coronary artery bypass graft surgery 
• Established ischaemic heart disease, peripheral arterial disease and/or cerebrovascular disease

Cautions

• Pregnancy <30 weeks
• Severe renal impairment
• Mild to moderate hepatic impairment
• Elderly < 50kg
• Use in trauma with hypovolaemic shockross 
• Hypertension
• Hyperlipidaemia
• Diabetes mellitus
• Compromised cardiac function, pre-existing oedema, or other conditions predisposed to fluid retention 
• History of gastrointerstinal disease
• Smoking
• Dehydration 
• May mask fever and other signs of inflammation

Forms avail in SA and covered in this monograph: inj

Postoperative pain

• IV/IM: 40mg; Followed by 20-40mg, 6-12hrly; Max 80mg/24hrs; Max duration: 3 days

IV bolus injection may be given rapidly and directly into a vein or into an existing IV line; IM injection should be given slowly and deeply into the muscle

The shortest duration possible and the lowest effective daily dose should be used

Do not use for more than 72hrs

Not established for use in children under 18 years

Pregnancy 

• Contraindicated in pregnancy  >30 weeks
• Caution in pregnancy <30 weeks
• Parecoxib is suspected to cause serious birth defects when administered during the last trimester of pregnancy because as with other medicinal products known to inhibit prostaglandin, it may cause premature closure of the ductus arteriosus or uterine inertia
• NSAID use during the second or third trimester of pregnancy may cause foetal renal dysfunction which may result in a reduction of amniotic fluid volume or oligohydramnios in severe cases. Such effects may occur shortly after treatment initiation and are usually reversible. Pregnant women on NSAIDs should be closely monitored for amniotic fluid volume
• There are no adequate data from the use of parecoxib in pregnant women or during labour. However, inhibition of prostaglandin synthesis might adversely affect pregnancy. Data from epidemiological studies suggest an increased risk of miscarriage after use of prostaglandin synthesis inhibitors in early pregnancy. In animals, administration of prostaglandin synthesis inhibitors, including parecoxib, has been shown to result in increased pre-and post-implantation loss and embryo-foetal lethality. During the first and second trimester of pregnancy, parecoxib should not be given unless clearly necessary

Breastfeeding 

• Contraindicated
• Administration of a single dose of parecoxib to breastfeeding women following caesarean section resulted in the transfer of a relatively small amount of parecoxib and its active metabolite valdecoxib into human milk, and this resulted in a low relative dose for the infant (approximately 1% of the weight-adjusted maternal dose). Parecoxib must not be administered to women who breastfeed

Renal Impairment 

• Mild to moderate: No dose adjustment recommended
• Severe: Caution; dose adjustment recommended
  Lowest recommended dose: 20mg, dly

Hepatic Impairment 

• Moderate: Caution; dose adjustment recommended
  Initial: 20 mg; Followed by 20 mg, 6-12hrly; Max: 40 mg/24hrs
• Severe: Contraindicated

Elderly 

• > 50kg: No dose adjustment recommended
• < 50kg: Caution; dose adjustment recommended
  Reduce dose by 50%; Max: 40mg/24hrs

Porphyria Information

• Probably not porphyrinogenic (PNP)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders 

• Hypoaesthesia 
• Dizziness 
• Agitation 
• Insomnia
• Aesthenia

Cardiovascular Disorders

• Myocardial infarction 
• Bradycardia 
• Circulatory collapse 
• Congestive heart failure 
• Tachycardia 
• Hypertension 
• Hypotension
• Hypertension  
• Orthostatic hypotension

Respiratory Disorders 

• Respiratory insufficiency 
• Pulmonary embolism 
• Dyspnoea
• Pharyngitis
• Alveolar osteitis

Gastrointestinal Disorders 

• Nausea and vomiting
• Abdominal pain 
• Constipation 
• Dyspepsia 
• Flatulence 
• Gastroduodenal ulceration 
• Gastro-oesophageal reflux disease 
• Dry mouth
• Gastrointestinal sounds abnormal 
• Pancreatitis 
• Oesophagitis 
• Oedema mouth (perioral swelling)

Genitourinary Disorders 

• Oliguria 
• Renal failure

Endocrine and Metabolic Disorders

• Hypokalaemia 
• Hyperglycaemia 
• Anorexia
• Increrased creatinine 
• Increased creatine phosphokinase
• Increased lactate dehydrogenase 
• Increased serum glutamic oxaloacetic transaminase
• Increased serum glutamic-pyruvic transaminase
• Increased blood urea nitrogen

Muscularskeletal Disorders

• Back pain 
• Arthralgia

Skin and Subcutaneous Disorders 

• Pruritus 
• Hyperhidrosis ecchymosis 
• Rash
• Urticarial 
• Stevens-Johnson syndrome 
• Erythema multiforme 
• Exfoliative dermatitis
• Injection site pain 
• Injection site reaction 
• Wound infection 
• Abnormal sternal serous wound drainage 
• Peripheral oedema 

Immune, Blood and Lymphatic System Disorders 

• Anaemia postoperative 
• Thrombocytopenia 
• Hypersensitivity reactions including anaphylaxis and angioedema

Sensory Organs 

• Ear and labyrinth disorders 
• Ear pain

• Anticoagulant therapy
• Angiotensin converting enzyme inhibitors
• Angiotensin II antagonists
• Beta blockers
• Diuretics
• Cyclosporin
• Tacrolimus    
• Fluconazole
• Ketoconazole
• CYP3A4 inducers
• CYP2D6 substrates  
• CYP2C19 substrates
• Lithium

None routine. Specific cases may require

• Renal function
• Hepatic function
• Vital signs

Inhibits prostaglandin synthesis by selective inhibition of cyclooxygenase-2.

Injection (per vial) 40mg

• Rayzon (Pfizer) originator
• Perodyn 40 (Trinity Pharma)