Table 13. Characteristics of Nucleoside Reverse Transcriptase Inhibitors (NRTIs)

Generic Name

Trade Name
Stavudine
(d4T)
Zerit
Lamivudine
(3TC)
Epivir
Abacavir
(ABC)
Ziagen
Form 15, 20, 30, 40 mg capsules
1mg/mL for oral solution
150 mg tablets
10 mg/mL oral solution
300 mg tablets
20 mg/mL oral solution
Dosing Recommendations >60kg: 40 mg bid

<60kg: 30 mg bid
150 mg bid
<50kg: 2 mg/kg bid
or with ZDV as Combivir, 1 bid, or with
ZDV and abacavir as Trizivir +#, 1 bid
300 mg bid
or with ZDV and 3TC as Trizivir +#, 1 bid
Food Effect Take without regard to mealsTake without regard to mealsTake without regard to meals
Alcohol Image f3644_up-arrow.jpgABC levels 41%; no effect on alcohol
Oral bioavailability 86%86%83%
Serum half-life 1.0 hour3-6 hours1.5 hours
Intracellular half-life 3.5 hours12 hours3.3 hours


Elimination
Renal excretion 50%Renal excretion unchangedMetabolized by alcohol dehydrogenase and glucuronyl transferase.

Renal excretion of metabolites 82%


Adverse Events
Pancreatitis

Peripheral neuropathy

Lactic acidosis with hepatic steatosis is a rare but potentially life-threatening toxicity with the use of NRTIs. #
(Minimal toxicity)

Lactic acidosis with hepatic steatosis is a rare but potentially life-threatening toxicity with the use of NRTIs.
Hypersensitivity reaction (can be fatal) ** ; fever, rash, nausea, vomiting, malaise or fatigue, and loss of appetite. Respiratory symptoms may also be component (sore throat, cough, SOB).

Lactic acidosis with hepatic steatosis is a rare but potentially life-threatening toxicity with the use of NRTIs.

* For once daily dosing only. Twice daily dosing is preferred; however, once daily dosing may be appropriate for patients who require a simplified dosing schedule.

+ Each Combivir tablet contains 300 mg ZDV and 150 mg 3TC.

+# Each Trizivir tablet contains 300 mg ZDV, 150 mg 3TC, and 300 mg abacavir.

§ Twice daily dosing is preferred; however, once daily dosing may be appropriate for patients who require a simplified dosing schedule.

¶ Cases of fatal and nonfatal pancreatitis have occurred in treatment-naive and treatment-experienced patients during therapy with ddI or in combination with other drugs, particularly d4T or d4T + hydroxyurea.

#

Pregnant women may be at increased risk for lactic acidosis and liver damage when treated with the combination of stavudine and didanosine. This combination should be used in pregnant women only when the potential benefit clearly outweighs the potential risk.

** Patients who develop signs or symptoms of hypersensitivity (which may include fever, rash, fatigue, nausea, vomiting, diarrhea, and abdominal pain) should discontinue abacavir as soon as a hypersensitivity reaction is suspected. Abacavir should not be re-started, because more severe symptoms will recur within hours and may include life-threatening hypotension and death. Cases of abacavir hypersensitivity syndrome should be reported to the Abacavir Hypersensitivity Registry at 1-800-270-0425.

From: Guidelines for the Use of Antiretroviral Agents in HIV-Infected Adults and Adolescents

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