zalcitabine; dideoxycytosine; ddC (Hivid)

Introduction

Tradename: Hivid.

Indications

• management of patients with HIV in combination with other retroviral agents

Contraindications

Caution:

• may exacerbate liver dysfunction in patient with liver disease or history of alcohol abuse

pregnancy category = c

safety in lactation = -

Dosage

0.75 mg PO every 8 hours

Tabs: 0.375 & 0.75 mg.

Dosage adjustment in renal failure

Table

creatinine clearance	dosage
10-40 mL/min	0.75 mg every 12 hours
< 10 mL/min*	0.75 mg every 24 hours

* dose after hemodialysis

Pharmacokinetics

• elimination 1/2life 2.0 hours (> 8 hours ESRD)

elimination via kidney

1/2life = 2.0 hours

Adverse effects

• common (> 10%)
  • oral ulcers
• less common (1-10%)
  • nausea/vomiting, dysphagia, anorexia, abdominal pain, diarrhea, rash, pruritus, headache, dizziness, myalgia, foot pain, fatigue, pharyngitis, chest pain, weight loss
• uncommon (< 1%)
  • constipation, night sweats, fever, pain, malaise, asthenia, edema, hypertension, palpitations, syncope, atrial fibrillation, tachycardia, epistaxis, hyperglycemia, hypocalcemia, jaundice, hepatitis, myositis
• other
  • peripheral neuropathy
    • dose-dependent
    • painful
      • predominantly distal, symmetric sensory polyneuropathy
  • rash
  • fatal pancreatitis (rare)

• drug adverse effects of antiretroviral agents

Drug interactions

• DO NOT USE in combination with
  • stavudine (d4T)
  • didanosine (ddI)
  • lamivudine (3TC)
• antacids may reduce levels of ddC

• drug interaction(s) of antibiotics with warfarin

Mechanism of action

• a cytidine analog
• transported by SLC28A1

More general terms

• nucleoside reverse transcriptase inhibitor (NRTI)

Database

• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=24066
• PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=5718