Tapentadol Hydrochloride

Registered South African indications:

• Pain

Contraindications

• Hypersensitivity to the active ingredient or any of its excipients
• Significant respiratory depression
• Acute or severe bronchial asthma or hypercapnia
• Known or suspected paralytic ileus 
• Acute intoxication with alcohol, hypnotics, centrally acting analgesics, or psychotropic active substances 

Cautions

• Pregnancy
• Breastfeeding
• Severe renal impairment
• Moderate to severe hepatic impairment
• Elderly
• History of substance abuse, abuse potential or dependence
• Impaired respiratory function
• Raised intracranial pressure
• Impaired consciousness
• Coma
• Head injury
• Brain tumor
• History of seizure disorder
• Biliary tract disease
• Acute pancreatitis
• Galactose intolerance
• Lapp lactase deficiency
• Glucose-galactose malabsorption
• May impair ability to drive and operate machinery

Forms avail. in SA and covered in this monograph: tab, slow release tab (SR tab)

Pain 
- Acute, moderately severe post-operative pain

• Oral (tab): 50-100mg, 4-6hrly; Max duration: 10 days; Max: 600mg/24hrs

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First day of dosing: The second dose may be admin. as soon as 1hr after first dose if adequate pain relief is not achieved. Max. dose on first day: 700mg

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Pain
- Moderate to severe chronic pain
- Unresponsive to non-narcotic analgesia

• Oral (SR tab): Initial: 50mg, 12hrly; Titrate by 50mg, 12hrly at intervals of 3 days; Max: 500mg/24hrs

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When switching from opioids to tapentadol, the nature of the previous medication, administration and mean daily dose should be considered when choosing the initial dose of tapentadol

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Gradual discontinuation advised due to risk of withdrawal

Not established for use in children below 18 years

Pregnancy

• FDA Pregnancy Category C

Breastfeeding

• Caution; not recommended

Renal impairment

• Mild to moderate: No dose adjustment recommended
• Severe: Caution; no information available

Hepatic impairment

• Mild: No dose adjustment recommended
• Moderate: Caution; dose adjustment recommended
• Severe: Caution; no information available

Elderly

• Caution; no dose adjustment recommended

Central Nervous System Disorders

• Anxiety
• Confusional state
• Hallucination
• Sleep disorder
• Abnormal dreams
• Depressed mood
• Disorientation
• Agitation
• Nervousness
• Restlessness
• Euphoric mood
• Abnormal thinking
• Dizziness
• Somnolence
• Headache
• Tremor
• Disturbance in attention
• Memory impairment
• Presyncope
• Sedation
• Ataxia
• Dysarthria
• Hypoaesthesia
• Paraesthesia
• Involuntary muscle contractions 
• Seizures
• Depressed level of consciousness
• Abnormal coordination
• Fatigue
• Feeling of body temperature change
• Feeling abnormal
• Feeling drunk
• Feeling of relaxation
• Irritability

Cardiovascular Disorders

• Increased heart rate
• Palpitations
• Decreased heart rate 
• Flushing
• Deceased blood pressure
• Oedema

Respiratory Disorders

• Respiratory depression
• Decreased oxygen saturation
• Dyspnoea

Gastrointestinal Disorders

• Nausea and vomiting
• Constipation
• Diarrhoea
• Dyspepsia
• Dry mouth
• Abdominal discomfort
• Impaired gastric emptying

Genitourinary Disorders

• Urinary hesitation
• Pollakiuria

Endocrine and Metabolic Disorders

• Decreased appetite

Musculoskeletal Disorders

• Muscle spasms
• Sensation of heaviness

Skin and Subcutaneous Tissue Disorders

• Pruritus
• Hyperhidrosis
• Rash
• Urticaria

Immune, Blood and Lymphatic System Disorders

• Drug Hypersensitivity

Sensory Disorders

• Visual disturbance

Others

• Drug withdrawal syndrome

• Central nervous system depressant agents
• Mixed mu-opioid agonist/antagonists 
• Partial mu-opioid agonists
• Serotoninergic agents
• UGT inhibitors
• CYP450 enzyme-inducers
• Monoamine oxidase inhibitors 

None routine. Specific cases may require

• Respiratory function
• Cardiovascular function
• Vital signs

Tapentadol is a strong analgesic with µ-agonistic opioid and additional noradrenaline reuptake inhibition properties, which results in increased levels of extracellular norepinephrine.

Tablet 50mg

• Palexia (Janssen Pharma)

Tablet 100mg

• Palexia (Janssen Pharma)

Tablet sr 50mg

• Palexia SR (Janssen Pharma)

Tablet sr 100mg

• Palexia SR (Janssen Pharma)

Tablet sr 200mg

• Palexia SR (Janssen Pharma)