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3.30 MB - Academy of Medicine of Malaysia

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MANAGEMENT OF HIV INFECTION IN CHILDREN<br />

Protease Inhibitors<br />

DRUG<br />

Adolescent/<br />

Adult Dose<br />

600 mg q12H<br />

To minimize<br />

nausea/vomiting,<br />

initiate therapy at<br />

300mg q12H and<br />

increase stepwise to<br />

full dose over 5 days<br />

as tolerated<br />

Lopinavir/Ritonavir<br />

(LPV/r)<br />

(KALETRA)<br />

Preparations:<br />

Pediatric oral solution<br />

80mg LPV/20mg RTV<br />

per ml<br />

S<strong>of</strong>t gelatin capsule:<br />

Each contain<br />

Lopinavir 133.3 mg<br />

Ritonavir 33.3mg<br />

Saquinavir<br />

INVIRASE<br />

(hard capsule)<br />

FORTOVASE (s<strong>of</strong>tgel<br />

capsule)<br />

Preparations:<br />

Capsule:<br />

200 mg<br />

DOSAGE ADVERSE<br />

REACTIONS<br />

Allergic<br />

reactionsincluding<br />

bronchospasm,<br />

urticaria and<br />

angioedema<br />

In children 6 months<br />

to 12 years <strong>of</strong> age,<br />

the recommended<br />

dose is as follows:<br />

7 to < 15kg<br />

12mg/kg LPV/<br />

3mg/kg RTV twice<br />

daily<br />

15 - 40kg:<br />

10mg/kg LPV/<br />

2.5mg/kg RTV twice<br />

daily<br />

< 40kg:<br />

400mg LPV/<br />

100mg RTV twice<br />

daily<br />

Adolescent/Adult:<br />

400mg/100mg<br />

(3 capsules or 5ml )<br />

twice daily<br />

Neonatal Dose:<br />

Unknown<br />

Pediatric Dose:<br />

SGC - Under Study in<br />

PACTG 397 : 50<br />

mg/kg tid<br />

Usual Dose:<br />

Adolescent/<br />

Adult Dose: 1200mg<br />

tid (Fortovase)<br />

600mg tid (Invirase)<br />

400mg bid (Invirase)<br />

In double PI regimens<br />

(e.g. with ritonavir or<br />

nelfinavir)<br />

More common:<br />

Diarrhea, headache,<br />

asthenia, nausea and<br />

vomiting and rash,<br />

lipid abnormalities<br />

Less common<br />

(more common):<br />

lipodystrophy<br />

syndrome<br />

Rare:<br />

New onset <strong>of</strong><br />

diabetes mellitus,<br />

hyperglycemia,<br />

ketoacidosis,<br />

exacerbation <strong>of</strong><br />

pre-existing diabetes<br />

mellitus, hemolytic<br />

anemia, pancreatitis,<br />

elevation in serum<br />

transaminases and<br />

hepatitis<br />

More common:<br />

Diarrhea, abdominal<br />

discomfort, nausea,<br />

headache, paresthesias<br />

skin rash and lipid<br />

abnormalities<br />

Less common (more<br />

severe): Exacerbation<br />

<strong>of</strong> chronic liver<br />

disease, lipodystrophy<br />

syndrome<br />

Rare: New onset<br />

diabetes mellitus,<br />

hyperglycemia,<br />

ketoacidosis,<br />

exacerbation <strong>of</strong><br />

pre-existing diabetes<br />

mellitus, pancreatitis<br />

and elevation in<br />

serum transaminases<br />

79<br />

DRUG<br />

INTERACTIONS<br />

Contraindicated<br />

with amiodarone,<br />

piroxicam,<br />

astemizole/terfinadine,<br />

cisapride, alprazolam,<br />

midazolam,zolpidem<br />

Drugs that induce<br />

CYP 3A4 may reduce<br />

saquinavir levels.<br />

Rifampicin reduces<br />

saquinavir levels<br />

greatly and should<br />

not be used in<br />

combination.<br />

Contraindicated<br />

Drugs: Terfenadine,<br />

Astemizole, Cisapride,<br />

Ergot Alkaloids,<br />

Midazolam, Rifampicin.<br />

Drugs that increase<br />

saquinavir levels:<br />

Ritonavir,<br />

Ketoconazole,<br />

Nelfinavir,<br />

Delavirdine.<br />

Appendix 4<br />

SPECIAL<br />

INSTRUCTIONS<br />

Oral solution has<br />

limited shelf-life (6<br />

months), use by<br />

product expiration<br />

date.<br />

To minimize nausea,<br />

therapy should be<br />

initiated at a low dose<br />

& increase to full dose<br />

as tolerated.<br />

Techniques to<br />

increase tolerance:<br />

Mix oral solution with<br />

milk, chocolate milk or<br />

pudding, ice cream.<br />

Dulling the taste buds<br />

before administration<br />

by chewing ice.<br />

Coat the mouth by<br />

giving peanut butter to<br />

eat before the dose or<br />

administer strongtasting<br />

foods such as<br />

cheese or strongflavored<br />

chewing<br />

gum immediately after<br />

dose<br />

LPV/r tablets can be<br />

administered without<br />

regard to food<br />

LPV/r oral solution<br />

should be<br />

administered with<br />

food. A high fat meal<br />

increases absorption,<br />

especially <strong>of</strong> the<br />

liquid preparation.<br />

Should be refrigerated<br />

and if kept at room<br />

temperature up to<br />

25oC , used within<br />

2 months<br />

If coadministered with<br />

ddI, ddI should be<br />

given 1 hour before or<br />

2 hours after LPV/r<br />

Administer within 2<br />

hours <strong>of</strong> a full meal to<br />

increase absorption<br />

(high fat meal<br />

preferred)<br />

Sun exposure can<br />

cause photosensitivity<br />

reactions; therefore,<br />

sunscreen or<br />

protective clothing is<br />

recommended<br />

Capsules should be<br />

kept refrigerated.<br />

Once brought to room<br />

temperature, use<br />

within 3 months.

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