II. Mechanism
- Nucleoside Reverse Transcriptase Inhibitor
- Purine Analogue
- Degraded at an acidic pH (all preparations have buffer)
III. Pharmacokinetics
- Crosses the Blood brain barrier
- Actively excreted by the Kidney
IV. Efficacy
V. Dosing
VI. Adverse Effects
- See nRTI for adverse effects attributed to the class
- Adverse effects are increased when used in combination with Stavudine
- Peripheral Neuropathy
-
Pancreatitis - most serious toxicity!
- Incidence
- Dose 500 mg/day: 7% Pancreatitis
- Dose 750 mg/day: 9% Pancreatitis
- Increased risk if Hyperamylasemia
- Dose 500-750 mg/day: 18% Hyperamylasemia
- Interrupt therapy if suspect Pancreatitis
- Avoid other pancreatic toxins (e.g. Pentamidine)
- Incidence
- Eye related changes
- Retinal changes
- Optic Neuritis
- Hyperamylasemia
- Hyperuricemia
- Dry Mouth
- Gastrointestinal changes
- Gastrointestinal upset
- Hepatic toxicity
- Noncirrhotic Portal Hypertension
- Electrolyte imbalances (rare)
- Cardiac Arrhythmias (rare)