Eletriptan

Registered South African indications:

• Migraine

Contraindications

• Hypersensitivity to the active ingredient or to any of its excipients 
• Severe renal impairment
• Severe hepatic impairment
• Uncontrolled hypertension
• Coronary heart disease
• Coronary artery vasospasm 
• Significant arrhythmias 
• Cardiac failure
• Peripheral vascular disease
• History of cerebrovascular accident or transient ischaemic attack
• Coadministration with ergotamine or ergotamine derivatives within 24hrs before or after taking eletriptan
• Coadministration with other serotonin 5-HT1 receptor agonists

Cautions

• Pregnancy
• Breastfeeding
• Mild to moderate renal impairment
• Mild to moderate hepatic impairment
• Elderly
• Hypersensitivity to sunset yellow
• Hemiplegic, ophthalmoplegic or basilar migraine
• Atypical headaches
• Cardiovascular disease or risk factors thereof
• Prolonged use
• Galactose intolerance
• Lapp lactase deficiency
• Glucose-galactose malabsorption
• Co-administration of potent CYP3A4 inhibitors
• Prolonged use of any painkiller for headaches

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

Acute Migraine:

• Oral (tab): 40mg; Repeat dose after 2hrs if needed; Max single dose: 40 mg; Max: 80mg/24hrs.

---

Tablets: Do not cut/crush/chew/dissolve

---

Not to be used prophylactically

---

Coadministration with potent CYP3A4 inhibitors: Dose adjustment recommended: 20mg; Max: 40mg/24hrs

Not established for use in children below 18 years

Pregnancy

• Caution
• For eletriptan no clinical data on exposed pregnancies are available. Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/foetal development, parturition or postnatal development. Eletriptan should be used during pregnancy only if clearly needed

Breastfeeding

• Caution; not recommended
• Eletriptan is excreted in human breast milk. In one study of 8 women given a single dose of 80 mg, the mean total amount of eletriptan in breast milk over 24hrs in this group was 0.02% of the dose. Nevertheless, caution should be exercised when considering the administration of eletriptan to women who are breastfeeding. Infant exposure can be minimised by avoiding breastfeeding for 24hrs after treatment

Renal Impairment

• Mild to moderate: Caution; dose adjustment recommended
  Initial: 20mg; Max: 40mg/24hrs
• Severe: Contraindicated

Hepatic Impairment

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

Elderly

• Caution; no dose adjustment recommended

Porphyria Information

• Probably not porphyrinogenic (PNP)

Drugs in Sport

• Permitted - No warnings

Central Nervous System Disorders

• Abnormal thinking
• Agitation
• Confusion
• Depersonalisation
• Euphoria
• Depression
• Insomnia 
• Emotional lability
• Somnolence
• Headache
• Dizziness
• Tingling or abnormal sensation
• Hypertonia
• Hypoaesthesia
• Myasthenia
• Tremor
• Hyperaesthesia
• Ataxia
• Hypokinesia
• Speech disorder
• Stupor
• Taste perversion
• Fatigue

Cardiovascular Disorders

• Palpitation
• Tachycardia
• Bradycardia
• Flushing
• Peripheral vascular disorder
• Shock
• Oedema
• Chest pain

Respiratory Disorders

• Throat tightness
• Dyspnea
• Respiratory disorder
• Yawning
• Asthma
• Voice alteration
• Pharyngitis
• Rhinitis
• Respiratory tract infection

Gastrointestinal Disorders

• Abdominal pain
• Nausea
• Dry mouth
• Dyspepsia
• Diarrhoea
• Glossitis
• Constipation
• Oesophagitis
• Tongue oedema
• Eructation

Hepatobiliary Disorders

• Hyperbilirubinaemia
• Increased aspartate aminotransferase

Genitourinary Disorders

• Increased urinary frequency
• Urinary tract disorder 
• Polyuria
• Breast pain 
• Menorrhagia

Endocrine and Metabolic Disorders

• Anorexia
• Thirst

Musculoskeletal Disorders

• Back pain
• Myalgia
• Arthralgia
• Arthrosis
• Bone pain
• Arthritis
• Myopathy 
• Twitching

Skin and Subcutaneous Tissue Disorders

• Sweating
• Rash
• Pruritis
• Skin disorder
• Urticaria
• Facial oedema

Blood and Lymphatic System Disorders

• Lymphadenopathy

Sensory Disorders

• Abnormal vision
• Eye pain
• Photophobia
• Lacrimation disorder 
• Conjunctivitis
• Vertigo
• Ear pain
• Tinnitus

Others

• Feeling hot
• Chills

• Serotonin 5-HT1 receptor agonists
• CYP3A4 inhibitors
• Ergotamine or ergotamine derivatives
• St. John's wort
• Selective serotonin reuptake inhibitors
• Serotonin noradrenaline reuptake inhibitors
• CYP3A4 inhibitors (antifungals, macrolides)

None routine. Specific cases may require

• Vital signs
• ECG
• Renal function
• Hepatic function  

Acts on the serotonin (5-HT) receptors on the intracranial blood vessels and sensory nerves of the trigeminal system, resulting in cranial vessel constriction and inhibition of pro-inflammatory neuropeptide release.

Tablet 20mg

• Relpax (Pfizer) originator

Tablet 40mg

• Relpax (UpJohn) fct originator 

Tablet 80mg

• Relpax (Pfizer) originator