Flurbiprofen

Registered South African indications:

• Pain (sore throat)

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Previous hypersensitivity reactions (e.g. asthma, bronchospasm, rhinitis, angioedema, or urticaria) in response to acetylsalicylic acid or other non-steroidal anti-inflammatory drugs
• Third trimester of pregnancy
• Severe renal impairment
• Severe hepatic impairment
• Active or history of recurrent peptic ulcer/haemorrhage (two or more distinct episodes of proven ulceration) and intestinal ulceration
• History of gastrointestinal bleeding or perforation, severe colitis, haemorrhagic or haematopoietic disorders related to previous non-steroidal anti-inflammatory drug therapy
• Severe heart failure

Cautions 

• First and second trimesters of pregnancy
• Breastfeeding
• Mild to moderate renal impairment
• Mild to moderate hepatic impairment
• Elderly
• History of bronchial asthma or allergic disease
• Systemic lupus erythematosus and mixed connective tissue disease
• Impaired cardiac function
• History of hypertension and/or heart failure
• Prolonged use or beyond regulated use
• History of gastrointestinal disease
  - Ulcerative colitis
  - Crohn's disease
  - History of ulcer particularly if complicated with haemorrhage or perforation
• History of gastrointestinal toxicity
• Worsening bacterial infection
• Fructose intolerance
• Glucose-galactose malabsorption
• Sucrase-isomaltase insufficiency

Forms avail. in SA and covered in this monograph: loz

Pain - sore throat (short term symptomatic relief)

• Oral (loz):  1 loz, 3-6hrly; Max: 5 loz/24hrs; Max duration: 3 days

As with all lozenges, to avoid local irritation, flurbiprofen lozenges should be moved around the mouth whilst sucking

If symptoms get worse or if new symptoms occur, the treatment should be re-evaluated

If mouth irritation occurs, treatment should be withdrawn

Paed. forms avail. in SA and covered in this monograph: loz

Pain - sore throat (short term symptomatic relief)

<12 years

• Not established for use

>12 years

• See adult dosage

Pregnancy

• First and second trimesters: Caution; not recommended
  Third trimester: Contraindicated
• Inhibition of prostaglandin synthesis may adversely affect the pregnancy and/or the embryo/foetal development. Data from epidemiological studies suggest an increased risk of miscarriage and of cardiac malformation and gastroschisis after use of a prostaglandin synthesis inhibitor in early pregnancy. The absolute risk for cardiovascular malformation was increased from less than 1%, up to approximately 1.5 %. The risk is believed to increase with dose and duration of therapy
•  In animals, administration of a prostaglandin synthesis inhibitor has been shown to result in increased pre- and post-implantation loss and embryo-foetal lethality. In addition, increased incidences of various malformations, including cardiovascular, have been reported in animals given a prostaglandin synthesis inhibitor during the organogenetic period
• During the first and second trimester of pregnancy, flurbiprofen should not be given unless clearly necessary. If flurbiprofen is used by a woman attempting to conceive, or during the first and second trimester of pregnancy, the dose should be kept as low and duration of treatment as short as possible
• During the third trimester of pregnancy, all prostaglandin synthesis inhibitors may expose the foetus to:
  - cardiopulmonary toxicity (with premature closure of the ductus arteriosus and pulmonary hypertension)
  - renal dysfunction, which may progress to renal failure with oligo-hydroamniosis
• During the third trimester of pregnancy, all prostaglandin synthesis inhibitors may expose the mother and the neonate, at the end of pregnancy to:
  - possible prolongation of bleeding time, an anti-aggregating effect which may occur even at very low doses
  - inhibition of uterine contractions resulting in delayed or prolonged labour
• Consequently, flurbiprofen is contraindicated during the third trimester of pregnancy

Breastfeeding

• Caution; not recommended 
• In limited studies, flurbiprofen appears in the breast milk in very low concentration and is unlikely to affect the breastfed infant adversely
• However, because of possible adverse effects of NSAIDs on breastfed infants, flurbiprofen lozenges are not recommended for use in breastfeeding mothers

Fertility

• There is some evidence that drugs which inhibit cyclo-oxygenase/ prostaglandin synthesis may cause impairment of female fertility by an effect on ovulation. This is reversible on withdrawal of treatment

Renal Impairment

• Mild to moderate: Caution; no dose adjustment recommended 
• Severe: Contraindicated 

Hepatic Impairment

• Mild to moderate: Caution; no dose adjustment recommended 
• Severe: Contraindicated 

Elderly

• Caution; no information available 
  A general dose recommendation cannot be given, since to date clinical experience is limited. The elderly are at increased risk of the serious consequences of adverse reactions 

Porphyria Information

• Not yet classified (NC)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Insomnia
• Dizziness
• Headache
• Paraesthesia
• Somnolence

Cardiovascular Disorders

• Oedema
• Hypertension
• Cardiac failure

Respiratory Disorders

• Throat irritation
• Exacerbation of asthma and bronchospasm
• Dyspnoea
• Wheezing
• Oropharyngeal blistering
• Pharyngeal hypoaesthesia

Gastrointestinal Disorders

• Diarrhoea
• Mouth ulceration
• Nausea and vomiting
• Oral pain
• Oral paraesthesia
• Oropharyngeal pain
• Oral discomfort (warm or burning feeling or tingling of the mouth)
• Abdominal distension
• Abdominal pain
• Constipation
• Dry mouth
• Dyspepsia
• Flatulence
• Glossodynia
• Oral dysaesthesia

Hepatobiliary Disorders

• Hepatitis

Skin and Subcutaneous Tissue Disorders

• Various skin rashes
• Pruritus
• Stevens-Johnson syndrome

Immune, Blood and Lymphatic Disorders

• Hypersensitivity reactions
  - Non-specific allergic reactions and anaphylaxis
  - Respiratory tract reactivity e.g. asthma, aggravated asthma, bronchospasm, dyspnoea
  - Various skin reactions e.g. pruritis, urticaria, angioedema, exfoliative and bullous dermatoses
  - Epidermal necrolysis
  - Erythema multiforme
• Anaemia
• Thrombocytopenia
• Anaphylactic reaction
• Fever

Sensory Disorders

• Dysgeusia

Others

• Pain

• Non-steroidal anti-inflammatory drugs
• COX-II selective inhibitors
• Acetylsalicylic acid (low dose)
• Anticoagulants
• Warfarin
• Antiplatelet agents
• Antihypertensive agents
• Diuretics
• Angiotensin-converting-enzyme inhibitors
• Angiotensin-II-antagonists
• Cardiac glycosides
• Ciclosporin
• Corticosteroids
• Lithium
• Methotrexate
• Mifepristone
• Oral hypoglycaemic agents
• Phenytoin
• Potassium-sparing diuretics
• Probenecid
• Sulfinpyrazone
• Quinolone antibiotics
• Selective serotonin reuptake inhibitors
• Tacrolimus
• Zidovudine

Other interactions

• Alcohol

None routine. Specific cases may require

• Complete blood count
• Renal function
• Hepatic function
• Blood pressure
• Ophthalmologic examination

Additional observations

• Signs or symptoms of gastrointestinal bleeding

Flurbiprofen is a propionic acid derivative non-steroidal anti-inflammatory drug which acts through inhibition of prostaglandin synthesis. In humans flurbiprofen has potent analgesic, antipyretic and anti-inflammatory properties and the 8.75mg dose dissolved in artificial saliva has been shown to reduce prostaglandin synthesis in cultured human respiratory cells. According to studies using the whole blood assay, flurbiprofen is a mixed COX-1/COX-2 inhibitor with some selectivity towards COX-1. 

Lozenges 8,75mg

• Strepsils Intensive (Reckitt Benckiser) originator