Tilidine [Discontinued in SA Market]

Please note that the products associated with this active ingredient monograph have all been discontinued in the South African market (Effective: October 2021).

The information in this monograph has not been updated and remains on the EMGuidance platform for reference purposes only.

• Pain

Please note that the products associated with this active ingredient monograph have all been discontinued in the South African market (Effective: October 2021).

The information in this monograph has not been updated and remains on the EMGuidance platform for reference purposes only.

Contraindications 

• Hypersensitivity to the active ingredient or any of its excipients
• End-stage renal impairment (eGFR ≤10ml/ml/1.73m²)
• Severe hepatic impairment
• Porphyria
• Increased intracranial pressure
• Management of head injuries
• Acute alcoholism
• After operations on the biliary tract
• Presence of cyanosis
• Significant disturbances of respiratory function/ respiratory depression
• Myocardial ischaemia
• Coadministration with monoamine oxidase inhibitors or within 14 days of their use

Cautions

• Pregnancy
• Breastfeeding
• Moderate to severe renal impairment (eGFR  ≥11-49ml/min/1.73m²)
• Mild to moderate hepatic impairment
• Elderly
• Debilitated patients
• Hypothyroidism
• Adrenocortical insufficiency
• Prostatic hypertrophy
• Shock
• Inflammatory or obstructive bowel disorders
• History of addiction
• History of depression
• May impair ability to drive and operate machinery  

Please note that the products associated with this active ingredient monograph have all been discontinued in the South African market (Effective: October 2021).

The information in this monograph has not been updated and remains on the EMGuidance platform for reference purposes only.

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

Acute pain - moderate to severe
Chronic cancer-related pain

• Oral (dro): 50mg (20 drops), 6-8hrly OR 1mg/kg/dose; 6-8hrly; Max: 100mg (40 drops) (if required) 

Number of drops (2.5 mg/drop) = Total body weight divided by 2.5 (e.g. 35kg = 14 drops; 50kg = 20 drops) 

If required, the indicated daily dosage may be increased at the discretion of the physician to 100mg followed by the same dosage 2hrs later, followed by 100mg 4-5hrs later; Thereafter 20 drops 6-8hrly

May be taken with sugar; use undiluted perilingually or sublingually

Please note that the products associated with this active ingredient monograph have all been discontinued in the South African market (Effective: October 2021).

The information in this monograph has not been updated and remains on the EMGuidance platform for reference purposes only.

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

Acute pain - moderate to severe
Chronic cancer-related pain

Younger than 1 year

• Not established for use

Older than 1 year

• Oral (dro): 1mg/kg/dose; 6-8hrly; Max single dose: 1mg/kg/dose

1 drop = 2.5mg

Dose must be calculated based on body weight  

Weight in kg divided by 2.5 = number of drops required

May be taken with sugar; Use undiluted perilingually or sublingually

Please note that the products associated with this active ingredient monograph have all been discontinued in the South African market (Effective: October 2021).

The information in this monograph has not been updated and remains on the EMGuidance platform for reference purposes only.

Pregnancy  

• Caution
• There is inadequate evidence available on the safety of tilidine in human pregnancy. Therefore tilidine should not be used in pregnant women

Breastfeeding 

• Caution; not recommended
• Enters breast milk. Safety and compatibility in breastfeeding have not been established therefore, tilidine is not recommended during breastfeeding

Renal Impairment 

• eGFR ≥30-89ml/min/1.73m²: No dose adjustment recommended
• eGFR ≥11-49ml/min/1.73m²: Caution; dose adjustment recommended
  Max: 50mg (20 drops)/24hrs 
• eGFR ≤10ml/min/1.73 m²: Contraindicated

Hepatic Impairment 

• Mild to moderate (Child-Pugh class A and B): Caution; no dose adjustment recommended
  In moderate hepatic impairment closely monitor liver function (ALT) and discontinue if ALT increases by more than two-folds from baseline
• Severe (Child-Pugh class C): Contraindicated

Elderly 

• Caution; dose adjustment recommended 
• Use with caution. Only for short analgesia use

Porphyria Information

• Not yet classified (NC)

Drugs in Sport

• Permitted - No warnings

Please note that the products associated with this active ingredient monograph have all been discontinued in the South African market (Effective: October 2021).

The information in this monograph has not been updated and remains on the EMGuidance platform for reference purposes only.

Central Nervous System Disorders

• Drowsiness
• Confusion
• Vertigo
• Raised intracranial pressure
• Restlessness
• Changes of mood

Cardiovascular Disorders

• Bradycardia
• Palpitations
• Orthostatic hypotension

Respiratory Disorders

• Respiratory depression

Gastrointestinal Disorders

• Nausea and vomiting
• Constipation
• Dry mouth

Genitourinary Disorders

• Micturition difficulty

Endocrine and Metabolic Disorders

• Hypothermia

Skin and Subcutaneous Tissue Disorders

• Sweating
• Facial flushing
• Urticaria
• Pruritus
• Contact dermatitis

Sensory Disorders

• Miosis

Please note that the products associated with this active ingredient monograph have all been discontinued in the South African market (Effective: October 2021).

The information in this monograph has not been updated and remains on the EMGuidance platform for reference purposes only.

• Selective serotonin reuptake inhibitors (SSRIs)
• Serotonin and norepinephrine reuptake inhibitors (SNRI)
• Tricyclic antidepressants (TCA)
• Triptans
• Serotonin (5-HT3) receptor antagonists
• Atypical antidepressants
• Monoamine oxidase inhibitors
• Opioids
• Sedatives
• Hypnotics
• Neuroleptics

Please note that the products associated with this active ingredient monograph have all been discontinued in the South African market (Effective: October 2021).

The information in this monograph has not been updated and remains on the EMGuidance platform for reference purposes only.

Respiratory function

Please note that the products associated with this active ingredient monograph have all been discontinued in the South African market (Effective: October 2021).

The information in this monograph has not been updated and remains on the EMGuidance platform for reference purposes only.

Acts on the opioid receptors. Following oral administration, it is converted to the active analgesic metabolite, nortilidine.