ANTIVIRALS›NON-NUCLEOSIDE REVERSE
TRANSCRIPTASE INHIBITORS
Efavirenz
lINDICATIONS AND DOSE
HIV infection in combination with other antiretroviral
drugs
▶BY MOUTH USING CAPSULES
▶Child 3 months–17 years (body-weight 3.5–4 kg): 100 mg
once daily
▶Child 3 months–17 years (body-weight 5–7.4 kg): 150 mg
once daily
▶Child 3 months–17 years (body-weight 7.5–14 kg): 200 mg
once daily
▶Child 3 months–17 years (body-weight 15–19 kg): 250 mg
once daily
▶Child 3 months–17 years (body-weight 20–24 kg): 300 mg
once daily
▶Child 3 months–17 years (body-weight 25–32.4 kg): 350 mg
once daily
▶Child 3 months–17 years (body-weight 32.5–39 kg): 400 mg
once daily
▶Child 3 months–17 years (body-weight 40 kg and
above): 600 mg once daily
▶BY MOUTH USING TABLETS
▶Child (body-weight 40 kg and above): 600 mg once daily
▶BY MOUTH USING ORAL SOLUTION
▶Child 3–4 years (body-weight 13–14 kg): 360 mg once daily
▶Child 3–4 years (body-weight 15–19 kg): 390 mg once daily
▶Child 3–4 years (body-weight 20–24 kg): 450 mg once
daily
▶Child 3–4 years (body-weight 25–32.5 kg): 510 mg once
daily
▶Child 5–17 years (body-weight 13–14 kg): 270 mg once
daily
▶Child 5–17 years (body-weight 15–19 kg): 300 mg once
daily
▶Child 5–17 years (body-weight 20–24 kg): 360 mg once
daily
▶Child 5–17 years (body-weight 25–32.4 kg): 450 mg once
daily
▶Child 5–17 years (body-weight 32.5–39 kg): 510 mg once
daily
▶Child 5–17 years (body-weight 40 kg and above): 720 mg
once daily
DOSE EQUIVALENCE AND CONVERSION
▶The bioavailability ofSustiva®oral solution is lower
than that of the capsules and tablets; the oral solution
isnotinterchangeable with either capsules or tablets
on a milligram-for-milligram basis.lUNLICENSED USEOpening capsules and adding contents
to food is an unlicensed method of administration.
lCAUTIONSAcute porphyrias p. 603 .history of psychiatric
disorders.history of seizures
lINTERACTIONS→Appendix 1 : efavirenz
lSIDE-EFFECTS
▶Common or very commonAbdominal pain.anxiety.
concentration impaired.depression.diarrhoea.dizziness
.drowsiness.dyslipidaemia.fatigue.headache.
movement disorders.nausea.skin reactions.sleep
disorders.vomiting
▶UncommonBehaviour abnormal.confusion.flushing.
gynaecomastia.hallucination.hepatic disorders.memory
loss.mood altered.pancreatitis.psychosis.seizure.
Stevens-Johnson syndrome.suicidal tendencies.thinking
abnormal.tinnitus.tremor.vertigo.vision blurred
▶Rare or very rareDelusions.photosensitivity reaction
▶Frequency not knownImmune reconstitution
inflammatory syndrome.osteonecrosis
SIDE-EFFECTS, FURTHER INFORMATIONFor further
information regardingosteonecrosis, immune
reconstitution syndromeandlipodystrophy,see HIV
infection p.^409.
RashRash, usually in thefirst 2 weeks, is the most
common side-effect; discontinue if severe rash with
blistering, desquamation, mucosal involvement or fever; if
rash mild or moderate, may continue without
interruption—usually resolves within 1 month.
CNS effectsAdministration at bedtime especially infirst
2 – 4 weeks reduces CNS effects.
lPREGNANCYReports of neural tube defects when used in
first trimester.
lHEPATIC IMPAIRMENTGreater risk of hepatic side-effects
in chronic hepatitis B or C. Avoid in severe impairment.
MonitoringIn mild to moderate liver disease, monitor for
dose-related side-effects (e.g. CNS effects) and liver
function.
lRENAL IMPAIRMENTManufacturer advises caution in
severe renal failure—no information available.
lMONITORING REQUIREMENTSMonitor liver function if
receiving other hepatotoxic drugs.
lDIRECTIONS FOR ADMINISTRATIONCapsules may be
opened and contents added to food (contents have a
peppery taste).
lPRESCRIBING AND DISPENSING INFORMATIONFlavours of
oral liquid formulations may include strawberry and mint.
lPATIENT AND CARER ADVICE
Psychiatric disordersPatients or their carers should be
advised to seek immediate medical attention if symptoms
such as severe depression, psychosis or suicidal ideation
occur.lMEDICINAL FORMS
There can be variation in the licensing of different medicines
containing the same drug.
Tablet
CAUTIONARY AND ADVISORY LABELS 23
▶Efavirenz (Non-proprietary)
Efavirenz 600 mgEfavirenz 600 mg tablets| 30 tabletP
£ 30. 00 – £ 452. 94 | 30 tabletP£ 27. 87 (Hospital only)
▶Sustiva(Bristol-Myers Squibb Pharmaceuticals Ltd)
Efavirenz 600 mgSustiva 600 mg tablets| 30 tabletP£ 200. 27
(Hospital only)
Capsule
CAUTIONARY AND ADVISORY LABELS 23
▶Sustiva(Bristol-Myers Squibb Pharmaceuticals Ltd)
Efavirenz 50 mgSustiva 50 mg capsules| 30 capsuleP£ 16. 73
(Hospital only)
Efavirenz 100 mgSustiva 100 mg capsules| 30 capsuleP
£ 33. 41 (Hospital only)
Efavirenz 200 mgSustiva 200 mg capsules| 90 capsuleP
£ 200. 27 (Hospital only)Etravirine
lINDICATIONS AND DOSE
HIV infection resistant to other non-nucleoside reverse
transcriptase inhibitor and protease inhibitors in
combination with other antiretroviral drugs (including a
boosted protease inhibitor)
▶BY MOUTH
▶Child 6–17 years (body-weight 16–19 kg): 100 mg twice
daily
▶Child 6–17 years (body-weight 20–24 kg): 125 mg twice
daily
▶Child 6–17 years (body-weight 25–29 kg): 150 mg twice
daily
▶Child 6–17 years (body-weight 30 kg and above): 200 mg
twice dailylCONTRA-INDICATIONSAcute porphyrias p. 603BNFC 2018 – 2019 HIV infection 413
Infection5