Etravirine
Indications
Registered South African indications:
- HIV-1 infection
- In antiretroviral treatment-experienced patients with non-nucleoside reverse transcriptase inhibitor (NNRTI) resistance
Cautions
Contraindications
- Hypersensitivity to the active ingredient or any of its excipients
- Coadministration with elbasvir/grazoprevir
Cautions
- Pregnancy
- Breastfeeding
- Moderate to severe hepatic impairment
- Elderly
- Porphyria
- History of a severe cutaneous drug reaction
- Female patients
- Hepatitis B or C co-infection
- Galactose intolerance
- Lapp lactase deficiency
- Glucose-galactose malabsorption
Adult dosage
Forms avail. in SA and covered in this monograph: tab
HIV-1 infection (additional agents required)
- In combination with a boosted protease inhibitor and other antiretroviral medicinal products for the treatment of HIV-1 infection in antiretroviral treatment-experienced patients
- Oral (tab): 200mg, 12hrly, after a meal
Etravirine must always be given in combination with other antiretroviral medicinal products
If a dose has been missed by less than 6 hours, it should be taken following a meal as soon as possible. If a dose has been missed by more than 6 hours, the missed dose should not be taken and the usual dosing schedule should be resumed
Paediatric dosage
Not registered for use in South Africa for children: tab (100mg)
Paed. forms avail. in SA and covered in this monograph: tab (25mg)
Internationational manufacturer recommendations
HIV-1 infection (additional agents required)
- In combination with a boosted protease inhibitor and other antiretroviral medicinal products for the treatment of HIV-1 infection in antiretroviral treatment-experienced patients
25mg, 100mg
Younger than 2 years
- Not established for use
Between 2-18 years and ≥10kg
| Body weight | Dose | Tablets |
| ≥10 - <20kg | 100mg, 12hrly |
Four 25 mg tablets, 12hrly OR One 100 mg tablet, 12hrly |
| ≥20 - <25kg | 125mg, 12hrly |
Five 25 mg tablets, 12hrly OR One 100 mg tablet and one 25 mg tablet, 12hrly |
| ≥25 - <30kg | 150mg, 12hrly |
Six 25 mg tablets, 12hrly OR One 100 mg tablet and two 25 mg tablets, 12hrly |
| ≥30kg | 200mg, 12hrly |
Eight 25 mg tablets, 12hrly OR Two 100 mg tablets, 12hrly OR One 200 mg tablet, 12hrly |
South African manufacturer recommendations
HIV-1 infection (additional agents required)
- In combination with other antiretroviral medicines for the treatment of HIV-1 infection in antiretroviral treatment-experienced paediatric patients, including those with NNRTI resistance
25mg
Younger than 6 years
- Not established for use
Between 6-18 years and ≥16kg
| Weight | Dose (taken after a meal) |
| ≥16 - <20kg | 100mg, 12hrly |
| ≥20 - <25kg | 125mg, 12hrly |
| ≥25 - <30kg | 150mg, 12hrly |
| ≥30kg | 200mg, 12hrly |
Etravirine must always be given in combination with other antiretroviral medicinal products
Treatment history and, when available, resistance testing, should guide the use of etravirine 25mg. In patients who have experienced virological failure on an NNRTI- and nucleoside or nucleotide reverse transcriptase inhibitor (N(t)RTI)-containing regimen, etravirine 25 mg is not recommended for use in combination with N(t)RTIs only
Special populations
Consult HIV/infectious disease specialists prior to any decisions related to ARV regimen termination/switch
Pregnancy
- Caution; no evidence of risk in studies
- As a general rule, when deciding to use antiretroviral agents for the treatment of HIV infection in pregnant women, and consequently for reducing the risk of HIV vertical transmission to the newborn, the animal data as well as the clinical experience in pregnant women should be taken into account in order to characterise the safety for the foetus
- Placental transfer has been seen in pregnant rats, but it is not known whether placental transfer of etravirine also occurs in pregnant women. Studies in animals do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/foetal development, parturition or postnatal development. Based on animal data the malformative risk is unlikely in humans. The clinical data do not raise safety concern but are very limited
Breastfeeding
- Caution
- Etravirine is excreted in human milk
Renal Impairment
Hepatic Impairment
Elderly
Porphyria Information
Drugs in Sport
- Permitted - No warning
Adverse reactions
Central Nervous System Disorders
- Anxiety
- Insomnia
- Confusional state
- Disorientation
- Nightmares
- Sleep disorders
- Nervousness
- Peripheral neuropathy
- Headache
- Seizures
- Syncope
- Amnesia
- Tremor
- Somnolence
- Paraesthesia
- Hypoaesthesia
- Hypersomnia
- Disturbance in attention
- Fatigue
Cardiovascular Disorders
- Myocardial infarction
- Atrial fibrillation
- Angina pectoris
- Hypertension
Respiratory Disorders
- Bronchospasm
- Exertional dyspnoea
Gastrointestinal Disorders
- Gastrooesophageal reflux disease
- Diarrhoea
- Nausea and vomiting
- Abdominal pain
- Flatulence
- Gastritis
- Pancreatitis
- Haematemesis
- Stomatitis
- Constipation
- Abdominal distension
- Dry mouth
- Retching
Hepatobiliary Disorders
- Hepatitis
- Hepatic steatosis
- Cytolytic hepatitis
- Hepatomegaly
Genitourinary Disorders
- Renal failure
Endocrine and Metabolic Disorders
- Diabetes mellitus
- Hyperglycaemia
- Hypercholesterolaemia
- Hypertriglyceridaemia
- Hyperlipidaemia
- Anorexia
- Dyslipidaemia
- Gynaecomastia
Skin and Subcutaneous Tissue Disorders
- Rash
- Night sweats
- Swollen face
- Hyperhidrosis
- Prurigo
- Dry skin
Immune, Blood and Lymphatic System Disorders
- Thrombocytopaenia
- Anaemia
- Immune reconstitution syndrome
- Drug hypersensitivity
Sensory Disorders
- Blurred vision
- Vertigo
Interactions
- CYP3A4 inducers
- CYP3A4 inhibitors
- CYP3A4 substrates
- CYP2C9 inducers
- CYP2C9 inhibitors
- CYP2C19 inducers
- CYP2C19 inhibitors
- Non-nucleoside reverse transcriptase inhibitors
- Indinavir
- Nelfinavir
- Fosamprenavir/ritonavir
- Tipranavir/ritonavir
- Atazanavir/cobicistat
- Darunavir/cobicistat
- Dolutegravir
- Antiarrhythmics
- Clarithromycin
- Carbamazepine
- Phenobarbital
- Phenytoin
- Artemether/lumefantrine
- Rifampicin
- Rifapentine
- Rifabutin
- Diazepam
- Dexamethasone
- Boceprevir
- Daclatasvir
- Elbasvir/grazoprevir
- Simeprevir
- St John's wort
- Atorvastatin
- Fluvastatin
- Lovastatin
- Pravastatin
- Rosuvastatin
- Simvastatin
- Immunosuppressants
- Phosphodiesterase-5 inhibitors
- Clopidogrel
Monitoring
- Viral load
- CD4 count
- Lipid profile
- Blood glucose
Specific cases may require
- Hepatic function
Mechanism of action
Etravirine is a non-nucleoside reverse transcriptase inhibitor of human immunodeficiency virus type 1. Etravirine binds directly to reverse transcriptase and blocks the RNA-dependent and DNA-dependent DNA polymerase activities by causing a disruption of the enzyme's catalytic site.
Dosage forms
- Tablet
Formulation
References
1. SAMF 12th edition page 342 2. SmPC: Intelence 25mg, 100 mg and 200mg tablets, Janssen-Cilag Ltd:Last updated on eMC: 30 Oct 2018 [https://www.medicines.org.uk/emc/medicine/21185] 3. PI: Intelence tablets, Pharmacare Limited:Date of registration: 01 Feb 2011 [https://drive.google.com/drive/folders/1c3nXMzviIgdHSg6fXuWoI7n2EncB3GIv] 4. U2D: Etravirine: Drug information; Uptodate;Downloaded online 04 Feb 2019 [https://www.uptodate.com/contents/etravirine-drug-information?source=search_result&search=Etravirine%20drug%20information&selectedTitle=1~31] 5. Drugs.com: Etravirine ; Downloaded online 01 Feb 2019 [https://www.drugs.com/pregnancy/etravirine.html] 6. NAPOS: The Drug Database for Acute Porphyria: Etravirine; Accessed online 04 Feb 2019 [http://www.drugs-porphyria.org/languages/UnitedKingdom/s3.php?l=gbr&atc_code=J05AG04] 7. South African Institute for Drug-Free Sport: Intelence; Accessed online 04 Feb 2019 [http://www.drugfreesport.org.za/online-medication-check/] 8. PI: Intelence 100mg, Janssen Pharmaceutica; Date of Registration: 05 Aug 2011 [https://drive.google.com/drive/u/0/folders/1L3UdCFnBozhm3VJSP8opz3U8WXbbfbrv] 9. SmPC: Intelence 100 mg tablets, Janssen-Cilag Ltd: Last updated on eMC: 12 May 2020: Downloaded online: 01 Feb 2021 [https://drive.google.com/drive/u/0/folders/1L3UdCFnBozhm3VJSP8opz3U8WXbbfbrv] 10. PI: Intelence 25mg, Janssen Pharmaceutica; Date of Registration: 30 September 2016 [https://drive.google.com/drive/u/0/folders/1L3UdCFnBozhm3VJSP8opz3U8WXbbfbrv]
Brands & products
2 products · stale NAPPI snapshot · refreshed 5/28/2026 · 159 days oldtabletGeneric· 2 products
from R2.50/unit| Product | Strength | Pack | Sched | SEP | Unit | Disp fee | NAPPI |
|---|---|---|---|---|---|---|---|
| Intelence 25Mg | 25 mg | 120 | S4 | R300.43 | R2.50 | R107.86 | 720247001 |
| Intelence | 100 mg | 120 | S4 | R974.06 | R8.12 | R227.76 | 713800002 |
- Intelence
Medical aid coverage
data not yet integrated- Comprehensive Series—
- Executive Plan—
- KeyCare Series—
- Priority Series—
- Saver Series—
Formulary scraper pending — coverage tier, co-pay and authorisation requirements will appear here once data is ingested.
- BonClassic—
- BonComprehensive—
- BonEssential—
- BonFit Select—
- BonSave—
- BonStart—
Formulary scraper pending — coverage tier, co-pay and authorisation requirements will appear here once data is ingested.
- Beryl—
- Emerald—
- Onyx—
- Ruby—
- Sapphire—
- Tanzanite One—
Formulary scraper pending — coverage tier, co-pay and authorisation requirements will appear here once data is ingested.
- Aquarium Option—
- Efficiency Option—
- Marine Option—
Formulary scraper pending — coverage tier, co-pay and authorisation requirements will appear here once data is ingested.
Interacts with 32 known drugs
Check against other drugs →- Atazanavir
- Atorvastatin
- Brigatinib
- Carbamazepine
- Cariprazine Hydrochloride
- Clarithromycin
- Clofazimine
- Clopidogrel
- Darunavir
- Dexamethasone
- Diazepam
- Dolutegravir
- Fluvastatin
- Fosamprenavir
- Indinavir
- Letermovir
- Lovastatin
- Lurasidone
- Maraviroc
- Neratinib
- Osimertinib
- Phenytoin
- Pravastatin
- Rifabutin
- Rifampicin
- Rifapentine
- Rilpivirine
- Ritonavir
- Rosuvastatin
- Simvastatin
- Venetoclax
- Zanubrutinib