Valacyclovir
Hydrochloride
Classification:
ANTIVIRAL
ACTION & THERAPEUTIC EFFECT
An antiviral agent
hydrolyzed in the intestinal wall or liver to acyclovir, which interferes with
viral DNA synthesis. Active against herpes simplex virus types 1 (HSV-1) and 2 (HSV-2),
varicella zoster virus, and cytomegalovirus. Inhibits viral replication.
Herpes zoster (shingles) in
immunocompetent adults. Treatment and suppression of recurrent genital herpes;
suppression of recurrent herpes in HIV-positive patients; treatment of cold
sores.
Hypersensitivity to, or
intolerance of valacyclovir or acyclovir.
Renal impairment, patients
receiving nephrotoxic drugs, advanced HIV disease, allogeneic bone marrow transplant
and renal transplant recipients, treatment of disseminated herpes zoster,
immunocompromised patients, pregnancy (category B); lactation; children younger
than 2 y.
PO 1 g (2 × 500 mg) t.i.d. for 7 days, start within 48 h of onset
of zoster rash
Renal
Impairment Dosage Adjustment
Treatment of
Recurrent Genital Herpes
Adult: PO
500 mg b.i.d. × 3 days
Renal
Impairment Dosage Adjustment
CrCl 29 mL/min or less: 500 mg daily
Suppression
of Recurrent Genital Herpes
Adult: PO
1 g daily; concurrent HIV
infection 500 mg b.i.d.
Adult/Child: PO
2 g 12 h × 2 doses
Adolescent/Child (2 y or older): PO 20 mg/kg t.i.d. × 5 days (max: 1 g t.i.d.)
- Start
drug as soon as possible after diagnosis of herpes zoster, preferably within 48
h of onset of rash.
- Note:
Dosage reduction is recommended for patients with renal impairment.
- Give
valacyclovir after hemodialysis.
- Store at
15°–30° C (59°–86° F).
CNS: Headache, weakness,
somnolence, dizziness, fatigue, lethargy, confusion. GI: Nausea,
vomiting, diarrhea, abdominal pain, dyspepsia,
flatulence. Urogenital: Glomerulonephritis, renal
tubular damage, acute renal failure. Skin: Rash,
urticaria, pruritus.
Drug: Probenecid, cimetidine decrease
valacyclovir elimination. Zidovudine may cause
increased drowsiness and lethargy.
Absorption: Rapidly absorbed from GI tract;
54% reaches systemic circulation as acyclovir. Peak: 1.5 h. Distribution:
13.5–17.9% bound to plasma proteins; distributes into plasma,
cerebrospinal fluid, saliva, and major body organs; crosses placenta; excreted
in breast milk. Metabolism: Rapidly converted to acyclovir
during first pass through intestine and liver. Elimination: 40– 50% in
urine. Half-Life: 2.5–3.3 h.
Assessment & Drug Effects
- Monitor
kidney function in patients with kidney impairment or those receiving
potentially nephrotoxic drugs.
- Monitor for
S&S of hypersensitivity; if present, withhold drug and notify prescriber.
Patient & Family Education
- Be aware of
potential adverse effects and do not discontinue drug until full course is
completed.
- Note:
Post-herpes pain is likely to be present for several months after completion of
therapy.
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