Intelence HIV medicine contains Etravirine. It is a non-nucleoside reverse transcriptase inhibitor that inhibits HIV replication.

• Indications of Ertavirine:

  • HIV-1 infection:

    • It is used in the treatment of HIV-1 infection in addition to  other antiretroviral agents in treatment-experienced patients aged  2 years and older.

Ertavirine Dose in adults

Intelence HIV Treatment dosage in Adults:

• Oral dose 200 mg 12 hourly every day.

Ertavirine Dose in Children

Note: Evaluation of gene mutation and ARV resistance patterns should be done when necessary.

Intelence HIV Treatment dosage in children:

It should be used in combination with other antiretroviral agents.

• Antiretroviral-experienced children ≥2 years weighing at least 10 kg and Adolescents:

  • 10 kg to <20 kg:

    • 100 mg b.i.d daily orally

  • 20 kg to <25 kg:

    • 125 mg b.i.d daily orally

  • 25 kg to <30 kg:

    • 150 mg b.i.d daily orally

  • ≥30 kg:

    • 200 mg b.i.d daily orally

Ertavirine pregnancy Risk Factor: B

• Etravirine's transfer through the human placenta is variable (moderate/high).
• There are not many data available on antiretroviral effects during pregnancy, and there is little information about teratogenic effects in humans.
• Preterm births are more likely when maternal antiviral therapy is initiated. However, it is important to consider other factors, such as maternal disease severity and gestational age at the initiation of therapy.
• Some studies have shown that stillbirth/low birth weight/small gestational age infants are more likely.
• It is important to not withhold maternal antiviral therapy because of concerns about adverse neonatal outcomes.
• All infants who have been exposed to antiretroviral medication should be followed up for a long time.
• Potential mitochondrial dysfunction should be checked for organ system abnormalities, such as those of the CNS and heart in infants.
• Women who are taking nonnucleoside reverse transcriptionase inhibitors (NNRTIs) antiviral therapy are at greater risk of developing hypersensitivity reactions like liver toxicity or rash.
• However, it is unknown if pregnancy may increase this risk.
• According to the Health and Human Services (HHS), Perinatal HIV Guidelines, pregnant women should not be given antiretroviral-naive drugs.
• Antiretroviral treatment is not recommended for pregnant women who have received antiretroviral treatment previously, but need to restart it, or who have a poor tolerance/poor response to the current regimen.
• If the drug is well tolerated and effective viral suppression is achieved, then pregnant women can continue to take etravirine.
• Pregnancy does not affect the pharmacokinetics and dosage adjustment is not necessary.
• To keep HIV-positive women pregnant, it is important to continue treatment. This will help lower the risk of perinatal transmission and suppress the virus load.
• Monitory during pregnancy is more common than for non-pregnant women.
• Postpartum HIV-positive women are encouraged to continue their antiretroviral treatment. This can also be modified after delivery.

Etravirine use during breastfeeding:

• Breast milk contains Etravirine.
• Postnatal HIV transmission is possible through infant or maternal antiretroviral treatment.
• Breastfeeding infants have been exposed to a multiclass resistant virus despite receiving adequate antiretroviral treatment.
• Therefore, in the US, where the formula is within easy access/safe/affordable/ sustainable, and the incidence of infant mortality due to diarrhea and respiratory infections is low, females with HIV infection should be advised against breastfeeding to reduce the potential transmission of HIV.

Intelence HIV (Etravirine) dose adjustment in renal disease:

• No dosage adjustment necessary.
• Significant removal by hemodialysis or peritoneal dialysis is unlikely due to extensive protein binding capacity.

Intelence HIV (Etravirine) dose adjustment in liver disease:

• Mild to moderate impairment (Child-Pugh class A or B):

  • No dosage adjustment is required.

• Severe impairment (Child-Pugh class C):

  • There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).

Common Side Effects of Etravirine (Intelence):

• Dermatologic:

  • Skin Rash

• Endocrine & Metabolic:

  • Increased Serum Cholesterol
  • Increased Serum Glucose
  • Increased LDL Cholesterol

Rare Side Effects Of Etravirine (Intelence):

• Cardiovascular:

  • Angina Pectoris
  • Atrial Fibrillation
  • Facial Edema
  • Myocardial Infarction
  • Syncope

• Central Nervous System:

  • Peripheral Neuropathy
  • Abnormal Dreams
  • Amnesia
  • Anxiety
  • Confusion
  • Disorientation
  • Disturbance In Attention
  • Drowsiness
  • Hypersomnia
  • Hypoesthesia
  • Lethargy
  • Nervousness
  • Nightmares
  • Paresthesia
  • Seizure
  • Sleep Disturbance
  • Vertigo

• Dermatologic:

  • Hyperhidrosis
  • Night Sweats
  • Prurigo
  • Xeroderma

• Endocrine & Metabolic:

  • Increased Serum Triglycerides
  • Increased Amylase
  • Diabetes Mellitus
  • Dyslipidemia
  • Gynecomastia
  • Lipohypertrophy

• Gastrointestinal:

  • Diarrhea
  • Abdominal Distention
  • Anorexia
  • Constipation
  • Flatulence
  • Gastritis
  • Gastroesophageal Reflux Disease
  • Hematemesis
  • Pancreatitis
  • Retching
  • Stomatitis
  • Xerostomia
  • Increased Serum Lipase

• Hematologic & Oncologic:

  • Hemolytic Anemia
  • Decreased White Blood Cell Count

• Hepatic:

  • Increased Serum Alanine Aminotransferase
  • Increased Serum Aspartate Aminotransferase
  • Hepatic Failure
  • Hepatitis
  • Hepatomegaly
  • Liver Steatosis

• Hypersensitivity:

  • Hypersensitivity Reaction

• Immunologic:

  • Immune Reconstitution Syndrome

• Neuromuscular & Skeletal:

  • Tremor

• Ophthalmic:

  • Blurred Vision

• Renal:

  • Increased Serum Creatinine
  • Acute Renal Failure

• Respiratory:

  • Bronchospasm
  • Dyspnea On Exertion

Contraindication to Etravirine (Intelence):

The US labeling of the manufacturer does not list any contraindications.

• Hypersensitivity to etravirine and any component of the formulation
• Concurrent therapy with hepatitis C combination regimen of ombitasvir, paritaprevir, ritonavir and with drugs containing dasabuvir.

Warnings and precautions

• Fat redistribution

  • Etravirine may cause fat redistribution, such as buffalo hump/peripheral wasting and increased abdominal girth/cushingoid appearance.

• Immune reconstitution syndrome:

  • It can lead to immune reconstitution syndrome, which causes an inflammatory response to any opportunistic infections during early HIV treatment.
  • This may also activate autoimmune disorders such as Graves' disease or polymyositis later in therapy.
  • Additional evaluation and treatment may also be required.

• Hypersensitivity/ skin reactions

  • You can see some fatal skin reactions like Stevens-Johnson Syndrome/toxic epidermal Necrolysis/erythema Multiforme.
  • Hypersensitivity reactions can occur with or without systemic involvement.
  • If you notice signs or symptoms of severe skin reactions or hypersensitivity, the drug should be immediately stopped.
  • It is usually self-limiting with long-term therapy.

Etravirine: Drug Interaction

Note: Drug Interaction Categories:

• Risk Factor C: Monitor When Using Combination
• Risk Factor D: Consider Treatment Modification
• Risk Factor X: Avoid Concomitant Use

Monitoring parameters:

Monitoring of

• Viral load
• CD4 count
• lipid profile
• liver function tests
• signs  or symptoms of skin rash or infection is recommended.

How to administer Etravirine (Intelence)?

• Etravirine is recommended to administer orally after meals.
• If tablets are difficult to swallow, they should be dispersed in  water (5 mL or at least enough to cover tablets) and stirred well until the water turns milky and should be mixed with 15 mL of water/milk/orange juice, and drink at once The tablets should not be placed in orange juice or milk without adding water previously.
• Rinse glass several times (with water, milk or orange juice) and swallow the whole solution to ensure administration of the drug Carbonated beverages or warm (>40°C) water should not be used.

Etravirine (Intelence) mechanism of action:

• Etravirine is a non-nucleoside reverse transcriptionase inhibitor and binds with reverse transcriptase to fight HIV-1.
• It inhibits RNA-dependent DNA polymerase activities and DNA-dependent DNA polymerase activities.
• This includes HIV-1 replication. Antiviral activity does not require intracellular phosphorylation.

Notification:

• Pharmacokinetic data show that exposure in children >=2 years old is comparable to adults with similar dosing.

Absorption:

• Increased 50% with food

Protein binding:

• 99.9%; primarily to albumin and alpha -acid glycoprotein

Metabolism:

• Hepatic, primarily by CYP3A4, 2C9, and 2C19; major metabolites exhibit ~10% of parent drug activity against wild-type HIV

Half-life elimination:

• 41 hours (± 20 hours)

Time to peak, plasma:

• 2.5 to 4 hours

Excretion:

• Feces (94%, up to 86% as unchanged drug); urine (1%)

Etravirine Brand Names (International):

• Intelence
• Intravir

Etravirine Brand Names in Pakistan:

No Brands Available in Pakistan.