LOPINAVIR/RITONAVIR = LPV/r oral

Prescription under medical supervision


Therapeutic action

– Antiretrovirals, HIV protease inhibitors

Indications

– HIV infection, in combination with other antiretroviral drugs

Forms and strengths

– 40 mg lopinavir/10 mg ritonavir capsule and sachet of oral pellets
– 100 mg lopinavir/25 mg ritonavir and 200 mg lopinavir/50 mg ritonavir film coated tablets
– 80 mg lopinavir/20 mg ritonavir per ml oral solution, containing 42% alcohol (v/v), with a graduated syringe for oral administration

Dosage

– Child from 14 days to 6 months: 16/4 mg/kg 2 times daily
– Child over 6 months:
• 7 to < 15 kg: 12/3 mg/kg 2 times daily
• 15 to 35 kg: 10/2.5 mg/kg 2 times daily
– Child ≥ 35 kg and adult: 400/100 mg 2 times daily

Weight

80/20 mg/ml
oral sol.

40/10 mg capsule
or sachet of oral pellets

100/25 mg tablet

200/50 mg tablet

3 to < 6 kg

1 ml x 2

6 to < 10 kg

1.5 ml x 2

3 capsules or sachets x 2

10 to < 14 kg

2 ml x 2

4 capsules or sachets x 2

2 tab morning
and 1 tab evening

14 to < 20 kg

2.5 ml x 2

5 capsules or sachets x 2

2 tab x 2

20 to < 25 kg

3 ml x 2

6 capsules or sachets x 2

2 tab x 2

25 to < 35 kg

3 tab x 2

≥ 35 kg

4 tab x 2

2 tab x 2

Duration

– The duration of treatment depends on the efficacy and tolerance of lopinavir and ritonavir.

Contra-indications, adverse effects, precautions

– Do not administer to patients with severe hepatic impairment or hypokalaemia.
– Do not administer oral solution to patients with renal or hepatic impairment and capsules to children under 3 months.
– Administer with caution and monitor use in patients with haemophilia (increased bleeding).
– May cause:
• gastrointestinal disturbances (mainly diarrhoea), skin rash, fatigue, headache, insomnia, paraesthesia, muscle pain, hypertriglyceridaemia, hypercholesterolemia, hyperglycaemia, conduction disorders, lipodystrophy;
• hepatic and pancreatic disorders; in this event, stop treatment immediately.
– Administer with caution and monitor combination with:
• drugs that prolong the QT interval (amiodarone, co-artemether, mefloquine, quinine, haloperidol, etc.);
• metronidazole when using LPV/r oral solution that contains alcohol (risk of antabuse reaction).
– LPV/r reduces the efficacy of oral contraceptives: use a non-hormonal contraception or injectable medroxyprogesterone or an oral contraceptive containing 50 micrograms ethinylestradiol per tablet.
– Avoid combination with rifampicin; preferably use rifabutin. If only rifampicin is available, adjust LPV/r dosage.
– Pregnancy: oral solution is CONTRA-INDICATED; no contra-indication for tablets and capsules

Remarks

– Tablets may be taken with meals or on an empty stomach. The oral solution must be taken with meals.
– The tablets must not be cut, crushed or chewed.
– Capsules or sachets must be opened then oral pellets must be poured into a small amount of breast milk or soft foods and administered to the child immediately. Pellets must not be stirred, crushed, dissolved/dispersed in food, or chewed.
– Storage:
• Tablets, capsules and sachets of oral pellets: below 25 °C -  - 
• Oral solution: between 2 °C and 8 °C. 
If refrigeration is not available, oral solution kept below 25 °C may be stored for 6 weeks maximum.