Indications
Treatment of cytomegalovirus (CMV) retinitis in HIV-infected
patients (alone or with ganciclovir). Treatment
of acyclovir-resistant mucocutaneous herpes simplex
virus (HSV) infections in immunocompromised patients.
Action
Prevents viral replication by inhibiting viral DNA-polymerase
and reverse transcriptase. Therapeutic Effects:
Virustatic action against susceptible viruses including
CMV.
Pharmacokinetics
Absorption: IV administration results in complete
bioavailability.
Distribution: Variable penetration into CSF. May
concentrate in and be slowly released from bone.
Metabolism and Excretion: 80–90% excreted
unchanged in urine.
Half-life: 3 hr (in patients with normal renal function);
longer half-life of 90 hr may reflect release of
drug from bone.
TIME/ACTION PROFILE
ROUTE ONSET PEAK DURATION
IV rapid end of infusion
8–24 hr
Contraindications/Precautions
Contraindicated in: Hypersensitivity; HF (due to
sodium content); Patients on sodium-restricted diets;
Hemodialysis; Lactation: Avoid breast feeding.
Use Cautiously in: Renal impairment (doseprequired
if CCr 1.4–1.6 mL/min/kg; see product information);
History of seizures; History of QT interval prolongation
or cardiovascular disease; Concurrent use of
other QT interval prolonging medications; Hypokalemia
or hypomagnesemia (must be corrected prior to therapy);
OB, Pedi: Safety not established.
Adverse Reactions/Side Effects
CNS: SEIZURES, headache, anxiety, confusion, dizziness,
fatigue, malaise, mental depression, weakness.
EENT: conjunctivitis, eye pain, vision abnormalities.
Resp: coughing, dyspnea. CV: TORSADE DE POINTES,
chest pain, edema, palpitations, QT interval prolongation.
GI: diarrhea, nausea, vomiting, abdominal pain,
abnormal taste sensation, anorexia, constipation, dyspepsia.
GU: renal failure, albuminuria, dysuria, nocturia,
polyuria, urinary retention. Derm:qsweating,
pruritus, rash, skin ulceration. F and E: hypocalcemia,
hypokalemia, hypomagnesemia, hyperphosphatemia,
hypophosphatemia. Hemat: anemia, granulocytopenia,
leukopenia, neutropenia. Local: pain/
inflammation at injection site. MS: arthralgia, myalgia,
back pain, involuntary muscle contraction. Neuro:
ataxia, hypoesthesia, neuropathy, paresthesia, tremor.
Misc: HYPERSENSITIVITY REACTIONS (including anaphylaxis,
urticaria, and angioedema), fever, chills, flu-like
syndrome, lymphoma, sarcoma.
Interactions
Drug-Drug: Avoid use of drugs known to prolong
the QTc interval including quinidine, procainamide,
amiodarone, sotalol, chlorpromazine, thioridazine,
moxifloxacin, pentamidine, and methadone.
Concurrent use with parenteral pentamidine may result
in severe, life-threatening hypocalcemia. Risk of nephrotoxicity may beqby concurrent use of other nephrotoxic
agents (amphotericin B, aminoglycosides,
cyclosporine, acyclovir, methotrexate, tacrolimus,
pentamidine (IV)).
Route/Dosage
IV (Adults): CMV retinitis—60mg/kg q 8 hr or 90
mg/kg q 12 hr for 2–3 wk, then 90–120 mg/kg/day as
a single dose. Doseprequired for any degree of renal
impairment; HSV—40 mg/kg q 8–12 hr for 2–3 wk
or until healing occurs.
Availability (generic available)
Solution for injection: 24 mg/mL.
No comments:
Post a Comment