Posted by: Indonesian Children | January 14, 2009

treatment hiv and aids with ARV

ARV (antiretroviral)

source : emedicine

The World Health Organization estimates that approximately 2.3 million children are living with the human immunodeficiency virus (HIV) as of 2006. In 2006 alone, 530,000 children were newly infected, an improvement from the 640,000 newly infected in 2004. Not only are the children themselves ravaged by disease, but their primary caregivers have also often succumbed to acquired immune deficiency syndrome (AIDS). This is most prevalent in sub-Saharan Africa, where 18 million children are predicted to be orphaned by AIDS by the end of 2010. Worldwide, the United Nations Children’s Fund (UNICEF) predicts the number of children orphaned and made vulnerable by HIV/AIDS is expected to reach 25 million by the end of the decade.

based on CD4+ counts.

Drug Category: Antiretroviral agents

These agents inhibit reverse transcriptase, thereby causing chain termination when incorporated into a growing viral strand.

Drug Name

Zidovudine (AZT, Retrovir)

Description

Thymidine analog that inhibits viral replication. Inhibits activity of HIV reverse transcriptase by competing with natural substrate for use by and incorporation into viral DNA.

Pediatric Dose

Neonate: 2 mg/kg PO q6h
3 months to 12 years: 180 mg/m2 PO q6h; not to exceed 200 mg q6h
If neonates cannot tolerate PO administration, IV medication can be instituted at 1.5 mg/kg over 30 min q6h

Contraindications

Documented hypersensitivity

Interactions

Acetaminophen may decrease bioavailability; toxicity increases when administered concurrently with amphotericin B, flucytosine, interferon alfa, doxorubicin, vincristine, vinblastine, dapsone, cimetidine, indomethacin, probenecid, lorazepam, aspirin, acyclovir, ganciclovir, and pentamidine; fluctuations in levels are associated with coadministration of phenytoin, methadone, fluconazole, atovaquone, valproic acid, lamivudine, and rifampin

Pregnancy

C – Safety for use during pregnancy has not been established.

Precautions

Anemia and granulocytopenia have been reported, especially in advanced HIV disease, necessitating discontinuation and/or transfusions in some patients; caution in bone marrow suppression (eg, granulocyte count <1000 cells/mL or hemoglobin levels <9.5 g/dL); lactic acidosis and severe hepatomegaly with steatosis have been noted; caution in hepatobiliary disease; headache, insomnia, myalgia, myopathy, arthralgia, anxiety, adverse GI tract effects, cough, dyspnea, and changes in skin pigmentation have been reported; adjust dose in renal impairment

 

Drug Name

Didanosine (Videx)

Description

Synthetic nucleoside analog of deoxyadenosine. Inhibits activity of HIV reverse transcriptase by competing with the natural substrate for use by and incorporation into viral DNA.

Pediatric Dose

120 mg/m2 PO bid

Contraindications

Documented hypersensitivity

Interactions

Avoid coadministration with other drugs causing pancreatitis; history of neuropathy or use of neurotoxic drugs can increase risk of neuropathy; coadministration with allopurinol not advised because of increase in levels of didanosine; antacids can affect drug levels; may alter absorption of ketoconazole, itraconazole (because of gastric pH changes), ganciclovir, quinolone antibiotics, delavirdine, and indinavir

Pregnancy

B – Usually safe but benefits must outweigh the risks.

Precautions

Fatal and nonfatal pancreatitis have occurred; discontinue therapy in patients with pancreatitis; lactic acidosis, hepatomegaly with steatosis, retinal depigmentation, and optic neuritis have been reported

 

Drug Name

Lamivudine (Epivir)

Description

Thymidine analog that inhibits viral replication by way of DNA-chain termination after the nucleoside analog is incorporated.

Pediatric Dose

3 months to 16 years: 4 mg/kg PO bid; not to exceed 150 mg bid

Contraindications

Documented hypersensitivity

Interactions

Bioavailability increases with coadministration of trimethoprim and sulfamethoxazole; lamivudine increases concentration of zidovudine when administered concurrently

Pregnancy

C – Safety for use during pregnancy has not been established.

Precautions

Adjust dose in renal impairment; caution in history of pancreatitis; lactic acidosis and life-threatening hepatomegaly with steatosis have been reported; recurrent hepatitis may be experienced in patients with HIV and hepatitis B–induced liver disease upon cessation of lamivudine

 

Drug Name

Stavudine (Zerit)

Description

Nucleoside analog of thymidine that inhibits activity of HIV reverse transcriptase.

Pediatric Dose

<30 kg: 1 mg/kg/dose PO q12h
30-60 kg: 30 mg PO bid
>60 kg: 40 mg PO bid

Contraindications

Documented hypersensitivity

Interactions

Zidovudine coadministration can inhibit intracellular phosphorylation of stavudine

Pregnancy

C – Safety for use during pregnancy has not been established.

Precautions

Modify dose in patients with reduced CrCl; severe hepatomegaly, lactic acidosis, and peripheral neuropathy have been reported

 

Drug Name

Nevirapine (Viramune)

Description

Binds to reverse transcriptase. The RNA- and DNA-dependent DNA polymerase functions are blocked because of a disruption of the catalytic site of the enzyme.

Pediatric Dose

2 months to 8 years: 4 mg/kg PO qd for 14 d, then 7 mg/kg PO bid
>8 years: 4 mg/kg PO qd for 14 d, then 4 mg/kg PO bid; not to exceed 400 mg/d

Contraindications

Documented hypersensitivity

Interactions

Trough plasma concentration increases with coadministration of cimetidine and macrolides; trough concentration decreases with coadministration of rifabutin or rifampin; levels are increased with ketoconazole coadministration; closely monitor levels of drugs metabolized by CYP3A because nevirapine is a CYP3A inducer

Pregnancy

C – Safety for use during pregnancy has not been established.

Precautions

Life-threatening skin reactions, including Stevens-Johnson syndrome and toxic epidermal necrolysis, may occur; hepatic necrosis has been reported

 

Drug Name

Nelfinavir (Viracept)

Description

Inhibits HIV-1 protease, resulting in the production of an immature and noninfectious virus.

Pediatric Dose

<2 years: Not established
2-13 years: 20-30 mg/kg/dose PO tid with meals

Contraindications

Documented hypersensitivity; concurrent use of cisapride, triazolam, midazolam, ergot derivatives, amiodarone, or quinidine because of altered hepatic metabolism

Interactions

Increases blood concentrations of astemizole (recalled from US market), cisapride, midazolam, isoniazid, stavudine, trimethoprim, terfenadine (recalled from US market), triazolam, and oral contraceptives; fluconazole and rifampin decrease blood concentrations; quinidine and ketoconazole increase blood concentrations; decreases blood concentrations of lamivudine; do not use with lovastatin or simvastatin because of CYP3A4 pathway inhibition and risk of myopathy; caution with sildenafil coadministration because of increased sildenafil concentrations; suboptimal levels of nelfinavir occur with St. John’s wort; inhibitor of CYP3A and close monitoring of levels of nelfinavir and drugs metabolized by the CYP3A system advised when administered concomitantly

Pregnancy

B – Usually safe but benefits must outweigh the risks.

Precautions

Caution in hepatic impairment; increase in bleeding in patients with hemophilia has been reported; lipodystrophy and diabetes mellitus have been reported

 

Drug Name

Ritonavir (Norvir)

Description

HIV PI used as a part of a double or triple therapy with nucleosides and other PIs. Inhibition of the protease thwarts the gag-pol polyprotein cleavage, which results in a noninfectious virus.

Pediatric Dose

400 mg/m2 PO bid; not to exceed 600 mg bid

Contraindications

Documented hypersensitivity; concomitant administration with cisapride, triazolam, midazolam, ergot derivatives, amiodarone, quinidine, bepridil, flecainide, propafenone, and pimozide because of altered hepatic metabolism

Interactions

Coadministration with propoxyphene, quinidine, amiodarone, bupropion, cisapride, clozapine, encainide, astemizole (recalled from US market), bepridil, flecainide, meperidine, rifabutin, piroxicam, propafenone, or terfenadine (recalled from US market) may cause arrhythmias, hematologic abnormalities, and seizures; coadministration with alprazolam, clorazepate, diazepam, estazolam, flurazepam, midazolam, triazolam, or zolpidem may significantly increase toxicity; do not use with lovastatin or simvastatin because of CYP3A4 pathway inhibition and risk of myopathy; caution with sildenafil coadministration because of increased sildenafil concentrations; suboptimal levels of ritonavir with St. John’s wort reported; inhibitor of CYP3A and close monitoring of levels of ritonavir and drugs metabolized by CYP3A system is advised when administered concomitantly

Pregnancy

C – Safety for use during pregnancy has not been established.

Precautions

Caution in hepatic insufficiency and antiarrhythmic treatments; increased bleeding in hemophilia, lipodystrophy, increased triglyceride and cholesterol levels, and diabetes mellitus have been reported

 

Drug Name

Emtricitabine (Emtriva)

Description

Synthetic nucleoside cytosine analog classified as NRTI. Competes with deoxycytidine-5′-triphosphate and incorporates into viral DNA, causing chain termination. Not recommended as monotherapy.

Adult Dose

200 mg PO qd

Pediatric Dose

Cap and sol not bioequivalent
❤ months: 3 mg/kg sol PO qd
3 months to 17 years: 6 mg/kg sol PO qd; alternatively, 200 mg PO qd if patient can swallow cap and is >33 kg
Not to exceed 240 mg/d for sol

Contraindications

Documented hypersensitivity to drug, class, or component

Interactions

Concomitant use with ribavirin (with or without interferon alfa) or nucleoside analogs may increase toxicity, resulting in pancreatitis or lactic acidosis

Pregnancy

B – Usually safe but benefits must outweigh the risks.

Precautions

Common adverse effects include headache, diarrhea, nausea, rash, rhinitis, asthenia, cough, abdominal pain, hypertriglyceridemia, depression, insomnia, dyspepsia, paresthesias, myalgia, arthralgia, palmar-plantar hyperpigmentation, and elevated CK level; reduce dose for CrCl <50 mL/min; serious or fatal pancreatitis and lactic acidosis reported; may cause hyperpigmentation on soles or palms; may cause fat redistribution; additional serious reactions include hepatomegaly with steatosis, hepatotoxicity, neutropenia, and immune reconstitution syndrome
Caution in impaired liver disease, long-term nucleoside treatment, or hepatitis B co-infection (may cause hepatitis B exacerbation posttreatment); breastfeeding not recommended

 

Drug Name

Efavirenz (Sustiva)

Description

NNRTI with activity against HIV-1 by binding to reverse transcriptase. Blocks RNA- and DNA-dependent DNA polymerase activities, including HIV-1 replication. Does not require intracellular phosphorylation for antiviral activity.

Adult Dose

600 mg PO qhs on empty stomach

Pediatric Dose

❤ years: Not established
>3 years
10-15 kg: 200 mg PO qhs on empty stomach
15-20 kg: 250 mg PO qhs on empty stomach
20-25 kg: 300 mg PO qhs on empty stomach
25-32.5 kg: 350 mg PO qhs on empty stomach
32.5-40 kg: 400 mg PO qhs on empty stomach
>40 kg: 600 mg PO qhs on empty stomach

Contraindications

Documented hypersensitivity to drug, class, or component; coadministration with astemizole, cisapride, midazolam, triazolam, or ergot derivatives

Interactions

Increases toxicity of cisapride, midazolam, triazolam, and ergot alkaloids, resulting in life-threatening toxicities; may increase effect of warfarin; may increase levels of CYP2C9, including bosentan, dapsone, fluoxetine, glimepiride, glipizide, losartan, montelukast, paclitaxel, phenytoin, or zafirlukast; may increase levels of CYP2C19, including citalopram, diazepam, phenytoin, propranolol, and sertraline
CYP2B6 inducers that may decrease levels include carbamazepine, phenobarbital, phenytoin, and rifampin; may reduce concentrations of atazanavir, indinavir, lopinavir, saquinavir, methadone, or sertraline

Pregnancy

D – Unsafe in pregnancy

Precautions

Caution in psychiatric illness, impaired liver function, hepatitis, or seizure history; unsafe during breastfeeding
Serious adverse effects include Stevens-Johnson syndrome, erythema multiforme, exfoliative dermatitis, depression (possibly severe), suicidality, psychiatric disorders, fat redistribution, immune reconstitution syndrome, hepatotoxicity, pancreatitis, seizures, and teratogenicity (first trimester)
Other adverse effects include rash, anxiety, depression, nervousness, drowsiness, impaired concentration, insomnia, abnormal dreams, hyperlipidemia, elevated liver transaminase levels, diarrhea, nausea, and fever

 

Drug Name

Abacavir (Ziagen)

Description

NRTI that interferes with HIV viral RNA-dependent DNA polymerase and inhibits viral replication.

Adult Dose

300 mg PO qd; alternatively, 600 mg PO qd.

Pediatric Dose

❤ months: Not established
3 months to 16 years: 16 mg/kg/d PO divided bid, not to exceed 600 mg/d
>16 years: 300 mg PO bid; alternatively, 600 mg PO qd

Contraindications

Documented hypersensitivity to drug, class, or component; breastfeeding not recommended

Interactions

Ethanol may increase risk of toxicity; methadone concentrations may decrease with concomitant administration; concomitant use of ribavirin with or without interferon alfa may cause lactic acidosis or pancreatitis

Pregnancy

C – Safety for use during pregnancy has not been established.

Precautions

Fatal hypersensitivity may occur following reintroduction of therapy; caution in hepatic dysfunction, prior liver disease, and prolonged use
Serious adverse effects include liver failure, renal failure, severe hypotension, ARDS, respiratory failure, death, Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme, lactic acidosis, hepatomegaly with steatosis, fat redistribution, pancreatitis, and immune reconstitution syndrome
Other adverse effects include nausea, headache, fatigue, vomiting, hypersensitivity, diarrhea, fever/chills, depression, rash, anxiety, URI, elevated liver transaminase levels, and hypertriglyceridemia

 

Drug Name

Tenofovir (Viread)

Description

Antiretroviral agent used in the treatment of AIDS. Inhibits activity of HIV reverse transcriptase by competing with the natural substrate deoxyadenosine 5′-triphosphate and, after incorporation into DNA, by DNA chain termination. Administered as prodrug bis-isopropoxycarbonyloxymethyl ester derivative of tenofovir, which is converted, through various enzymatic processes, to tenofovir, an acyclic nucleoside phosphonate (nucleotide) analog of adenosine 5′-monophosphate.
Bioavailability enhanced by a high-fat meal. Prolonged intracellular distribution allows for once-daily dosing.

Adult Dose

300 mg PO qd; adjust dosing frequency in renal insufficiency (ie, CrCl 30-49 mL/min, give q48h; CrCl 10-29 mL/min, give twice weekly; CrCl <10 mL/min, no recommendations; hemodialysis, give q7d after hemodialysis)

Pediatric Dose

Not established

Contraindications

Documented hypersensitivity to drug, class, or component

Interactions

Coadministration with drugs eliminated by active tubular secretion in kidney may increase serum concentrations of either tenofovir or coadministered drug; drugs that decrease renal function (eg, acyclovir, ganciclovir, cidofovir) may increase serum concentrations of tenofovir

Pregnancy

B – Usually safe but benefits must outweigh the risks.

Precautions

Serious adverse effects include lactic acidosis, hepatomegaly with steatosis, hepatotoxicity, nephrotoxicity, renal failure, hypophosphatemia pancreatitis, fractures, dyspnea, allergic reaction, fat redistribution, Fanconi syndrome, renal tubular necrosis (acute), hepatitis B exacerbation (posttreatment), and immune reconstitution syndrome
Other adverse effects include rash, hypercholesterolemia, headache, elevated CK level, pain, diarrhea, depression, elevated amylase levels, back pain, fever, nausea/vomiting, abdominal pain, hematuria, asthenia, anxiety, arthralgia/myalgia, insomnia, pneumonia, dyspepsia, dizziness, and elevated liver transaminase levels

 


REFERENCES

  • Blanche S, Tovo PA. European epidemiology. In: Pizzo PA, Wilfert CM. Pediatric AIDS: The Challenge of HIV Infection in Infants, Children, and Adolescents. 3rd ed. Philadelphia, Pa: Lippincott Williams & Wilkins; 1998:13-22.
  • Epocrates. Drug Information. Epocrates Online. Available at http://www.epocrates.com/. Accessed 2007.
  • Kovacs A, Scott GB. Advances in the management and care of HIV-positive newborns and infants. In: Pizzo PA, Wilfert CM. Pediatric AIDS: The Challenge of HIV Infection in Infants, Children, and Adolescents. 3rd ed. Philadelphia, Pa: Lippincott Williams & Wilkins; 1998:567-92.
  • Laude TA. Manifestations of HIV disease in children. Clin Dermatol. Jul-Aug 2000;18(4):457-67.  Layton TL, Davis-McFarland E. Pediatric human immunodeficiency virus and acquired immunodeficiency syndrome: an overview. Semin Speech Lang. 2000;21(1):7-17. 
  • Mastro TD, Zhang KL, Panda S. HIV infection and AIDS in Asia. In: Pizzo PA, Wilfert CM, eds. Pediatric AIDS: The Challenge of HIV Infection in Infants, Children, and Adolescents. 3rd ed. Philadelphia, Pa: Lippincott Williams & Wilkins; 1998:47-63.
  • McIntosh K. Human immunodeficiency virus: the virus and its pathogenicity. In: Yogev R, Connor E. Management of HIV Infection in Infants and Children. Mosby-Year Book; 1992::35-51.
  • World Health Organization. Paediatric HIV and treatment of children living with HIV. Available at http://www.who.int/hiv/paediatric/en/index.html. Accessed 2006.
  • World Health Organization. The World Health Report: Global Health–today’s challenges. Available at http://www.who.int/whr/2003/en/Chapter1.pdf. Accessed 2005.

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FIGHT AGAINTS AIDS,
SAVE INDONESIAN CHILDRENS

Yudhasmara Foundation

Working together against HIV and AIDS in Indonesia, Save our Children From HIV-AIDS

 

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phone : 62(021) 70081995 – 5703646

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phone : 62(021) 70081995 – 62(021) 5703646, mobile : 0817171764

email : judarwanto@gmail.com

 

 

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