Diclofenac Sodium

Registered South African indications:

• Inflammatory and degenerative forms of rheumatism: rheumatoid arthritis, ankylosing spondylitis, osteoarthrosis and spondylarthritis
• Painful musculoskeletal conditions
• Non-articular rheumatism
• Acute attacks of gout
• Mild to moderately painful post-operative and post-traumatic inflammation and swelling, pain following dental surgery or orthopaedic surgery
• Symptomatic treatment of primary dysmenorrhoea
• Migraine attacks

Registered South African contraindications

• Hypersensitivity to the active ingredient or any of the excipients
• History of gastrointestinal perforation, ulceration, or bleeding. Active or history of recurrent ulcer/haemorrhage/perforations
• Pregnancy (last trimester) due to the risk of oligohydramnios/ foetal renal dysfunction
• Breastfeeding
• Hepatic failure
• Renal failure (GFR<15ml/min/1.73m²)
• Porphyria
• Severe cardiac failure
• Heart failure, established ischaemic heart disease and/or cerebrovascular disease (stroke) and peripheral arterial disease
• Patients in whom the use of acetylsalicylic acid or other NSAIDs can precipitate asthma, angioedema, urticaria, or acute rhinitis (i.e. NSAID-induced cross-reactivity reactions)
• Children under the age of two years
• Proctitis

• Pregnancy (<30 weeks) (South African recommendations)
• Pregnancy (first and second trimester) (Recommendations in other jurisdictions) 
• Breastfeeding (Recommendations in other jurisdictions) 
• Female patients of reproductive potential
• Elderly
• Hepatic porphyria
• Hypertension
• Mild to moderate congestive cardiac failure
• Risk factors for cardiovascular events
• Gastrointestinal disorders
• Ulcerative collitis
• Crohn's disease
• Inflammatory bowel disease
• History of gastrointestinal toxicity
• Use after gastrointestinal surgery
• History of haematemesis or melaena
• Defects of haemostasis
• Haematological abnormalities
• Bleeding diathesis
• Asthma
• Seasonal allergic rhinitis
• Nasal polyps
• Substantial extracellular volume depletion
• Chronic obstructive pulmonary diseases
• Chronic infections of the respiratory tract
• Systemic lupus erythematosus
• Mixed connective tissue disease
• Masking of the signs and symptoms of infection
• Prolonged treatment
• Persistence of or worsening of abnormal liver function tests
• Clinical signs or symptoms of hepatic disease
• Appearance of skin rash or mucosal lesions
• Driving and the use of machinery

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

South African registered indications and dosages

Inflammatory and degenerative forms of rheumatism: rheumatoid arthritis, ankylosing spondylitis, osteoarthrosis and spondylarthritis
Painful musculoskeletal conditions
Non-articular rheumatism
Acute attacks of gout
Mild to moderately painful post-operative and post-traumatic inflammation and swelling, pain following dental surgery or orthopaedic surgery
Symptomatic treatment of primary dysmenorrhoea
Migraine attacks

• Rectal (sup): 100mg, daily

As a general recommendation, the dose should be individually adjusted. Use the lowest effective dose for the shortest possible duration of treatment

Not to be taken by mouth, as per rectal use only. The suppositories should be inserted well into the rectum. It is recommended to use the suppositories after passing stools

Suppositories should never be divided for administration or stored under incorrect storage conditions as this may lead to an uneven distribution of active medicine in the suppository

Do not use suppositories deformed by exposure to temperatures above 30°C

To suppress nocturnal pain and morning stiffness, treatment with tablets (see Diclofenac Sodium INJ/CAP/DSP/DRP/TAB/SAC/SRT/SRC) during the day can be supplemented by the administration of one diclofenac sodium suppository at bedtime, up to a maximum dosage of 150mg daily

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

South African registered indications and dosages

Painful musculoskeletal conditions
Acute attacks of gout
Mild to moderately painful post-operative and post-traumatic inflammation and swelling, pain following dental surgery or orthopaedic surgery
Symptomatic treatment of primary dysmenorrhoea
Migraine attacks

Younger than 2 years

• Contraindicated

Older than 2 years

• Rectal (supp): 0.5-2mg/kg body weight, dly, in 2-3 divided doses depending on the severity of the disorder

Juvenile rheumatoid arthritis

Younger than 2 years

• Contraindicated

Older than 2 years

• Rectal (supp): Daily dose can be raised up to max. 3mg/kg daily, given in divided doses

100mg suppositories are NOT indicated for use in children; Use 12.5mg and 25mg only

As a general recommendation, the dose should be individually adjusted. Use the lowest effective dose for the shortest possible duration of treatment

Not to be taken by mouth, as per rectal use only. The suppositories should be inserted well into the rectum. It is recommended to use the suppositories after passing stools

Suppositories should never be divided for administration or stored under incorrect storage conditions as this may lead to an uneven distribution of active medicine in the suppository

Do not use suppositories deformed by exposure to temperatures above 30°C

Pregnancy

South African recommendations

• First and second trimester: Caution; not recommended
• Last trimester: Contraindicated
• Use during the third trimester of pregnancy is contraindicated owing to the possibility of uterine inertia, foetal renal impairment with subsequent oligohydramnios/ foetal renal dysfunction and/or premature closure of the ductus arteriosus and pulmonary hypertension
• Complications of prolonged oligohydramnios include limb contractures and delayed lung maturation, which may require invasive procedures such as exchange transfusion or dialysis, in some cases
• The onset of labour may be delayed, and its duration increased

Breastfeeding

South African recommendations

• Contraindicated
• Diclofenac sodium passes into the breast milk in small amounts
• Therefore, diclofenac sodium should not be administered during breastfeeding in order to avoid undesirable effects in the infant

Fertility

South African recommendations

• The use of diclofenac sodium may impair female fertility and is not recommended in women attempting to conceive
• In women who have difficulties conceiving or who are undergoing investigation of infertility, withdrawal of diclofenac sodium should be considered

South African recommendations

• Renal failure (GFR<15ml/min/1.73m²): Contraindicated

South African recommendations

• Hepatic failure: Contraindicated

South African recommendations

• Caution; no dose adjustment recommended
  No adjustment of the starting dose is generally required for elderly patients. However, caution is indicated on basic medical grounds, especially for frail elderly patients or patients with a low body weight
  Treatment should be initiated and maintained at the lowest effective dose

Central Nervous System Disorders

• Drowsiness
• Disorientation
• Depression
• Insomnia
• Nightmare
• Irritability
• Psychotic disorder
• Headache
• Dizziness
• Somnolence
• Paraesthesia
• Memory impairment
• Convulsion
• Anxiety
• Tremor
• Aseptic meningitis
• Cerebrovascular accident
• Confusion
• Hallucinations
• Disturbances of sensation
• Malaise

Cardiovascular Disorders

• Palpitations
• Chest pain
• Cardiac failure
• Myocardial infarction
• Hypertension
• Hypotension
• Vasculitis
• Kounis syndrome

Respiratory Disorders

• Asthma
• Pneumonitis

Gastrointestinal Disorders

• Nausea and vomiting
• Diarrhoea
• Dyspepsia
• Abdominal pain
• Flatulence
• Anorexia
• Gastritis
• Gastrointestinal haemorrhage
• Haematemesis
• Haemorrhagic diarrhoea
• Malaena
• Gastrointestinal ulcer with or without bleeding or perforation
• Colitis
• Exacerbation of ulcerative colitis or Crohn's disease
• Constipation
• Stomatitis
• Glossitis
• Oesophageal disorder
• Diaphragm-like intestinal strictures
• Pancreatitis
• Ischaemic colitis

Hepatobiliary Disorders

• Increased transaminases
• Hepatitis
• Jaundice
• Fulminant hepatitis
• Hepatic necrosis
• Hepatic failure

Genitourinary Disorders

• Acute renal failure
• Haematuria
• Proteinuria
• Nephrotic syndrome
• Interstitial nephritis
• Renal papillary necrosis
• Impotence

Skin and Subcutaneous Tissue Disorders

• Rash
• Urticaria
• Bullous eruptions
• Eczema
• Erythema
• Erythema multiforme
• Stevens-Johnson syndrome
• Toxic epidermal necrolysis
• Dermatitis exfoliative
• Loss of hair
• Photosensitivity reaction
• Purpura
• Allergic purpura
• Pruritus
• Application site irritation
• Oedema

Immune, Blood and Lymphatic System Disorders

• Hypersensitivity
• Anaphylactic reactions
• Angioneurotic oedema
• Thrombocytopenia
• Leucopoenia
• Anaemia (including haemolytic and aplastic)
• Agranulocytosis

Sensory Disorders

• Visual disturbance
• Vision blurred
• Diplopia
• Optic neuritis
• Vertigo
• Tinnitus
• Hearing impaired
• Taste disturbances

• CYP2C9 inhibitors
• Voriconazole
• Lithium
• Digoxin
• Non-steroidal anti-inflammatory drugs (NSAIDs)
• Corticosteroids
• Diuretics
• Antihypertensive agents
• Beta-blockers
• Angiotensin converting enzyme (ACE) inhibitors
• Agents that increase serum potassium
• Anticoagulants
• Antiplatelet agents
• Selective serotonin reuptake inhibitors
• Antidiabetic agents
• Methotrexate
• Ciclosporin
• Trimethoprim
• Mifepristone
• Quinolone antibacterials
• Phenytoin
• Tacrolimus
• Colestipol
• Cholestyramine

None routine. Specific cases may require

• Renal function
• Hepatic function
• Full blood count

Cardiovascular and significant cardiovascular risk factors

• Diclofenac is contraindicated in patients with established congestive heart failure (NYHA II-IV), ischaemic heart disease, peripheral arterial disease and/or cerebrovascular disease
• Patients with congestive heart failure (NYHA-I) or significant risk factors for CVS should be treated with diclofenac only after careful consideration. Since CV risks with diclofenac may increase with dose and duration exposure, the lowest effective daily dose should be used and for the shortest duration possible

Diclofenac sodium is a nonsteroidal agent with marked analgesic/anti- inflammatory properties. It is an inhibitor of prostaglandin synthetase, (cyclo-oxygenase). Diclofenac sodium in vitro does not suppress proteoglycan biosynthesis in cartilage at concentrations equivalent to the concentrations reached in human beings. 

Suppository 12.5mg

• Panamor (Pharmacare)
• Voltaren (Novartis) originator

Suppository 25mg

• Panamor (Pharmacare)
• Voltaren (Novartis) originator

Suppository 100mg

• A-Lennon Diclofenac (Pharmacare)
• Diclohexal (Sandoz SA)
• Panamor  (Pharmacare)
• Voltaren (Novartis) originator

Also available in the following forms: Tablet, capsule, sachet, drop, injection, eye drop, gel, patch and lotion.