Names and pronunciation
(ay-sye′kloe-veer) Sitavig, Zovirax
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Individual generic drug information
Extracted information for acyclovir only.
(ay-sye′kloe-veer) Sitavig, Zovirax
Source page 30
Func. class.: Antiviral
Source page 30
Chem. class.: Purine nucleoside analog
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Do not confuse: Zovirax/Zyvox/Valtrex/Zostrix
Source page 30
ACTION: Converted to acyclovir monophosphate by virus-specific thymi- dine kinase then further converted to acyclovir triphosphate by other cellular enzymes
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USES: Mucocutaneous herpes simplex virus, herpes genitalis (HSV-1, HSV-2), varicella infections, herpes zoster, herpes simplex encephalitis
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Unlabeled uses: Bell’s palsy, prevention of CMV, Epstein-Barr virus, esophagitis, hairy leukoplakia, prevention of herpes labialis, herpes simplex, herpes simplex ocular prophylaxis, keratoconjunctivitis, pharyngitis, pneumonitis, prevention of postherpetic neuralgia, proctitis, sto matitis, tracheobronchitis, varicella prophylaxis
Source page 30
Extracted information for acyclovir only.
CONTRAINDICATIONS: Hyper- sensitivity to this product, valACYclovir; milk protein (buccal) Precautions: Pregnancy, breastfeeding, renal/hepatic/neurologic disease, elec- trolyte imbalance, dehydration, hyper- sensitivity to famciclovir, ganciclovir, penciclovir, valGANciclovir, obesity
Source page 30
SIDE EFFECTS CNS: Tremors, confusion, lethargy, hal- lucinations, seizures, dizziness, head- ache, encephalopathic changes EENT: Gingival hyperplasia GI: Nausea, vomiting, diarrhea, increased ALT/AST, abdominal pain, colitis GU: Hematuria, acute renal failure, changes in menses HEMA: Thrombotic thrombocytopenia purpura, hemolytic uremic syndrome, leu- kopenia (immunocompromised patients) INTEG: Rash, urticaria, pruritus, pain or phlebitis at IV site, unusual sweating, alopecia, Stevens-Johnson syndrome MS: Joint pain SYST: Angioedema, anaphylaxis
Source page 32
INTERACTIONS Increase: CNS side effects—zidovudine Increase: levels, toxicity—probenecid, monitor for toxicity Increase: nephrotoxicity—aminoglycosides Increase: concentrations of—entecavir, PEMEtrexed, tenofovir, theophylline Decrease: action of hydantoins, valproic acid, monitor drug levels Drug/Lab Test Increase: BUN, creatinine Decrease: WBC
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TREATMENT OF OVERDOSE: Discontinue product; hemodialysis
Source page 33
Extracted information for acyclovir only.
DOSAGE AND ROUTES Base dose in obese patients on ideal body weight, not actual body weight Herpes simplex (recurrent) • Adult: PO 400 mg 3×/day for 5 days or 200 mg 5×/day × 5 days • Adult and child >12 yr: IV INFUSION 5 mg/kg over 1 hr q8hr × 7 days • Infant >3 mo/child <12 yr: IV INFU- SION 10 mg/kg q8hr × 7 days; if HIV in- fected, 5-10 mg/kg q8hr (moderate to severe) • Neonate: IV INFUSION 10 mg/kg q8hr × 10 days, may use higher dose Genital herpes, initial episodes • Adult: PO 400 mg tid or 200 mg 5×/ day × 7-10 days, may extend treatment if healing is not complete after 10 days; TOP × 5 days; IV 5 mg/kg q8hr or 750 mg/m2/day divided q8hr × 5-7 days Genital herpes, episodic treatment • Adult: PO 400 mg tid or 800 mg bid × 5 days or 800 mg tid × 2 days; initiate within 1 day of lesion onset Genital herpes, suppression therapy • Adult: PO 400 mg bid for up to 12 mo or 200 mg 3-5 times daily for up to 12 mo Genital herpes, initial limited, mucocutaneous HSV in immunocompromised patients, non–life-threatening • Adult/child ≥12 yr: TOP cover le- sions q3hr 6×/day Herpes simplex encephalitis • Adult: IV 10 mg/kg over 1 hr q8hr × 10 days • Child 3 mo-12 yr: IV 10-15 mg/kg q8hr × 4-21 days • Child birth-3 mo: IV 20 mg/kg q8hr × 21 days • Neonates/premature infants: IV 10 mg/kg q12hr × 14-21 days Herpes labialis, recurrent • Adult/child ≥12 yr: TOP apply cream 5×/day for 4 days; start as soon as symp- toms appear Herpes labialis, recurrent in immunocompetent patients • Adult: Buccal 50 mg as a single dose in upper gum region within 1 hr after prodromal symptoms and before cold sore formation Herpes zoster (immunocompetent) • Adult: PO 800 mg q4hr 5×/day while awake × 7-10 days; IV 10 mg/kg q8hr × 7 days Herpes zoster (shingles) immunocompromised patients • Adult/adolescent: PO 800 mg q4hr 5×/ day for 7-10 days; IV 10-15 mg/kg q8hr × 10-14 days • Infant/child <12 yr: IV 10 mg/kg/dose q8hr × 7-10 days Herpes zoster (shingles) immunocompetent • Adult: PO 800 mg q4hr 5×/day × 7-10 days; start within 48-72 hr of rash onset Varicella (chickenpox) • Adult/child ≥2 yr: PO 10 mg/kg/dose (max 800 mg) 4×/day × 5 days Mucosal/cutaneous herpes simplex infections in immunosuppressed patients • Adult and child >12 yr: IV 5 mg/kg q8hr × 7 days • Infant >3 mo/child <12: IV 10 mg/kg q8hr × 7 days Renal dose • Adult and child: PO/IV CCr >50 mL/min 100% dose q8hr, CCr 25-50 mL/min 100% dose q12hr, CCr 10-25 mL/min 100% dose q24hr, CCr 0-10 mL/min 50% dose q24hr Recurrent ocular herpes, prevention (unlabeled) • Adult/child ≥12 yr: PO 600-800 mg every day × 8-12 mo CMV prophylaxis (unlabeled) • Adult: IV 500 mg/m2 q8hr Herpes simplex in pneumonitis/ esophagitis/tracheobronchitis/ proctitis/stomatitis/pharyngitis (unlabeled) • Adult and adolescent: IV 5-10 mg/kg q8hr × 2-7 days or PO 200 mg q4hr 5×/ day × 7-10 days or 400 mg 3-5×/day × ≥10 days • Child 6 mo-12 yr: IV 1000 mg/day in 3-5 divided doses × 7-14 days Herpes simplex prophylaxis for chronic suppression therapy (unlabeled) • Adult and adolescent: PO 400 mg bid up to 12 mo
Source pages 30, 31
Available forms: Capsules 200 mg; tablets 400, 800 mg; powder for injection 500, 1000 mg; solution for injection 50 mg/mL; oral suspension 200 mg/5 mL; ointment/cream 5%; buccal tablet 50 mg
Source page 31
Administer: A PO route • Do not break, crush, or chew capsules • May give without regard to meals, with 8 oz of water • Shake suspension before use Buccal • Use on the same side as the herpes labialis lesion; after removing tablet from blister, place rounded side of tablet to the upper gum above incisor tooth; hold in place for 30 sec; once adhered, the tablet will dissolve; if tablet falls off within 6 hr, reposition the same tablet Topical route • Use finger cot or glove to cover all le- sions completely; do not get in eye; wash hands after use Intermittent IV INFUSION route • Increase fluids to 3 L/day to decrease crystalluria; most critical during first 2 hr after IV • Reconstitute 10 mL compatible solu- tion/500 mg or 20 mL/1 g of product, 50 mg/ mL, shake, further dilute in 50-125 mL compatible solution; use within 12 hr; give over at least 1 hr by infusion pump to prevent nephrotoxicity; do not reconstitute with solu- tion containing benzyl alcohol in neonates • Store at room temperature for up to 12 hr after reconstitution; if refrigerated, solution may show a precipitate that clears at room temperature; yellow dis- coloration does not affect potency Y-site compatibilities: Alemtuzumab, alfentanil, allopurinol, amikacin, ami nophylline, amphotericin B cholesteryl, amphotericin B liposome, ampicillin, anidulafungin, argatroban, atracurium, bivalirudin, buprenorphine, busulfan, butorphanol, calcium chloride/gluconate, CARBOplatin, cefazolin, cefonicid, cefotax- ime, cefoxitin, ceftazidime, ceftizoxime, cefTRIAXone, cefuroxime, chlorampheni- col, cholesteryl sulfate complex, cimetidine, clindamycin, dexamethasone sodium phos- phate, dimenhyDRINATE, DOXOrubicin, doxycycline, erythromycin, famotidine, fil- grastim, fluconazole, gallium, gentamicin, granisetron, heparin, hydrocortisone sodium succinate, HYDROmorphone, imipenem/cilastatin, LORazepam, magne- sium sulfate, melphalan, methylPREDNISo- lone sodium succinate, metoclopramide, metroNIDAZOLE, multivitamin, nafcillin, oxacillin, PACLitaxel, penicillin G potas- sium, PENTobarbital, perphenazine, piper- acillin, potassium chloride, propofol, raNITIdine, remifentanil, sodium bicarbon- ate, tacrolimus, teniposide, theophylline, thiotepa, ticarcillin, tobramycin, trime- thoprim-sulfamethoxazole, vancomycin, vasopressin, voriconazole, zidovudine
Source pages 31, 32
Extracted information for acyclovir only.
Assess: • Infection: type of lesions, area of body covered, purulent drainage, frequency of lesions • Hepatic, renal studies: AST, ALT; uri- nalysis, protein, BUN, creatinine, CCr, watch for increasing BUN and serum cre- atinine or decreased CCr; I&O ratio; report hematuria, oliguria, fatigue, weakness; may indicate nephrotoxicity; check for protein in urine during treatment • Skin eruptions: rash, urticaria, itching • Allergies before treatment, reaction to each medication; place allergies on chart in bright red letters • Neurologic status with herpes enceph- alitis • Provide adequate intake of fluids (2 L) to prevent deposits in kidneys, more likely to occur with rapid administration or in dehydration
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Evaluate: • Therapeutic response: absence of itch- ing, painful lesions; crusting and healed le- sions; decreased symptoms of chickenpox; healing, decreased pain with herpes zoster
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • To take as prescribed; if dose is missed, take as soon as remembered up to 1 hr before next dose; do not double dose • That product may be taken orally be- fore infection occurs; product should be taken when itching or pain occurs, usu- ally before eruptions • That sexual partners need to be told that patient has herpes because they can become infected; condoms must be worn to prevent reinfections • Not to touch lesions to avoid spreading infection to new sites, not to use topical products on lesions, spreading may occur • That product does not cure infection, just controls symptoms and does not prevent infecting others • That product must be taken in equal intervals around the clock to maintain blood levels for duration of therapy • That women with genital herpes are more likely to develop cervical cancer; to keep all gynecologic appointments • Topical: Not to use around eyes, to use enough ointment to cover lesions q3hr/6× per day, use finger cot or glove to apply • Pregnancy/breastfeeding: to identify if pregnancy is planned or suspected or if breastfeeding
Source pages 32, 33
Extracted information for acyclovir only.
PHARMACOKINETICS Distributed widely; crosses placenta; CSF concentrations are 50% of plasma; pro- tein binding 9%-33% PO: Absorbed minimally, onset unknown, peak 1.5-2 hr, half-life 2.5-3.3 hr (adult); 2-3 hr (child); up to 4 hr (neonates) Buccal: Peak 8 hr IV: Onset immediate, peak immediate, duration unknown, half-life 20 min-3 hr (terminal); metabolized by liver, excreted by kidneys as unchanged product (95%)
Source page 32
Filter the extracted dose blocks for this individual drug.
Base dose in obese patients on ideal body weight, not actual body weight Herpes simplex (recurrent)
• Adult: PO 400 mg 3×/day for 5 days or 200 mg 5×/day × 5 days
Candidate age grouping · source pages 30, 31
Base dose in obese patients on ideal body weight, not actual body weight Herpes simplex (recurrent)
• Adult and child >12 yr: IV INFUSION 5 mg/kg over 1 hr q8hr × 7 days
Candidate age grouping · source pages 30, 31
Base dose in obese patients on ideal body weight, not actual body weight Herpes simplex (recurrent)
• Infant >3 mo/child <12 yr: IV INFU- SION 10 mg/kg q8hr × 7 days; if HIV in- fected, 5-10 mg/kg q8hr (moderate to severe)
Candidate age grouping · source pages 30, 31
Base dose in obese patients on ideal body weight, not actual body weight Herpes simplex (recurrent)
• Neonate: IV INFUSION 10 mg/kg q8hr × 10 days, may use higher dose Genital herpes, initial episodes
Candidate age grouping · source pages 30, 31
Base dose in obese patients on ideal body weight, not actual body weight Herpes simplex (recurrent)
• Adult: PO 400 mg tid or 200 mg 5×/ day × 7-10 days, may extend treatment if healing is not complete after 10 days; TOP × 5 days; IV 5 mg/kg q8hr or 750 mg/m2/day divided q8hr × 5-7 days Genital herpes, episodic treatment
Candidate age grouping · source pages 30, 31
Base dose in obese patients on ideal body weight, not actual body weight Herpes simplex (recurrent)
• Adult: PO 400 mg tid or 800 mg bid × 5 days or 800 mg tid × 2 days; initiate within 1 day of lesion onset Genital herpes, suppression therapy
Candidate age grouping · source pages 30, 31
Base dose in obese patients on ideal body weight, not actual body weight Herpes simplex (recurrent)
• Adult: PO 400 mg bid for up to 12 mo or 200 mg 3-5 times daily for up to 12 mo Genital herpes, initial limited, mucocutaneous HSV in immunocompromised patients, non–life-threatening
Candidate age grouping · source pages 30, 31
Base dose in obese patients on ideal body weight, not actual body weight Herpes simplex (recurrent)
• Adult/child ≥12 yr: TOP cover le- sions q3hr 6×/day Herpes simplex encephalitis
Candidate age grouping · source pages 30, 31
Base dose in obese patients on ideal body weight, not actual body weight Herpes simplex (recurrent)
• Adult: IV 10 mg/kg over 1 hr q8hr × 10 days
Candidate age grouping · source pages 30, 31
Base dose in obese patients on ideal body weight, not actual body weight Herpes simplex (recurrent)
• Child 3 mo-12 yr: IV 10-15 mg/kg q8hr × 4-21 days
Candidate age grouping · source pages 30, 31
Base dose in obese patients on ideal body weight, not actual body weight Herpes simplex (recurrent)
• Child birth-3 mo: IV 20 mg/kg q8hr × 21 days
Candidate age grouping · source pages 30, 31
Base dose in obese patients on ideal body weight, not actual body weight Herpes simplex (recurrent)
• Neonates/premature infants: IV 10 mg/kg q12hr × 14-21 days Herpes labialis, recurrent
Candidate age grouping · source pages 30, 31
Base dose in obese patients on ideal body weight, not actual body weight Herpes simplex (recurrent)
• Adult/child ≥12 yr: TOP apply cream 5×/day for 4 days; start as soon as symp- toms appear Herpes labialis, recurrent in immunocompetent patients
Candidate age grouping · source pages 30, 31
Base dose in obese patients on ideal body weight, not actual body weight Herpes simplex (recurrent)
• Adult: Buccal 50 mg as a single dose in upper gum region within 1 hr after prodromal symptoms and before cold sore formation Herpes zoster (immunocompetent)
Candidate age grouping · source pages 30, 31
Base dose in obese patients on ideal body weight, not actual body weight Herpes simplex (recurrent)
• Adult: PO 800 mg q4hr 5×/day while awake × 7-10 days; IV 10 mg/kg q8hr × 7 days Herpes zoster (shingles) immunocompromised patients
Candidate age grouping · source pages 30, 31
Base dose in obese patients on ideal body weight, not actual body weight Herpes simplex (recurrent)
• Adult/adolescent: PO 800 mg q4hr 5×/ day for 7-10 days; IV 10-15 mg/kg q8hr × 10-14 days
Candidate age grouping · source pages 30, 31
Base dose in obese patients on ideal body weight, not actual body weight Herpes simplex (recurrent)
• Infant/child <12 yr: IV 10 mg/kg/dose q8hr × 7-10 days Herpes zoster (shingles) immunocompetent
Candidate age grouping · source pages 30, 31
Base dose in obese patients on ideal body weight, not actual body weight Herpes simplex (recurrent)
• Adult: PO 800 mg q4hr 5×/day × 7-10 days; start within 48-72 hr of rash onset Varicella (chickenpox)
Candidate age grouping · source pages 30, 31
Base dose in obese patients on ideal body weight, not actual body weight Herpes simplex (recurrent)
• Adult/child ≥2 yr: PO 10 mg/kg/dose (max 800 mg) 4×/day × 5 days Mucosal/cutaneous herpes simplex infections in immunosuppressed patients
Candidate age grouping · source pages 30, 31
Base dose in obese patients on ideal body weight, not actual body weight Herpes simplex (recurrent)
• Adult and child >12 yr: IV 5 mg/kg q8hr × 7 days
Candidate age grouping · source pages 30, 31
Base dose in obese patients on ideal body weight, not actual body weight Herpes simplex (recurrent)
• Infant >3 mo/child <12: IV 10 mg/kg q8hr × 7 days Renal dose
Candidate age grouping · source pages 30, 31
Base dose in obese patients on ideal body weight, not actual body weight Herpes simplex (recurrent)
• Adult and child: PO/IV CCr >50 mL/min 100% dose q8hr, CCr 25-50 mL/min 100% dose q12hr, CCr 10-25 mL/min 100% dose q24hr, CCr 0-10 mL/min 50% dose q24hr Recurrent ocular herpes, prevention (unlabeled)
Candidate age grouping · source pages 30, 31
Base dose in obese patients on ideal body weight, not actual body weight Herpes simplex (recurrent)
• Adult/child ≥12 yr: PO 600-800 mg every day × 8-12 mo CMV prophylaxis (unlabeled)
Candidate age grouping · source pages 30, 31
Base dose in obese patients on ideal body weight, not actual body weight Herpes simplex (recurrent)
• Adult: IV 500 mg/m2 q8hr Herpes simplex in pneumonitis/ esophagitis/tracheobronchitis/ proctitis/stomatitis/pharyngitis (unlabeled)
Candidate age grouping · source pages 30, 31
Base dose in obese patients on ideal body weight, not actual body weight Herpes simplex (recurrent)
• Adult and adolescent: IV 5-10 mg/kg q8hr × 2-7 days or PO 200 mg q4hr 5×/ day × 7-10 days or 400 mg 3-5×/day × ≥10 days
Candidate age grouping · source pages 30, 31
Base dose in obese patients on ideal body weight, not actual body weight Herpes simplex (recurrent)
• Child 6 mo-12 yr: IV 1000 mg/day in 3-5 divided doses × 7-14 days Herpes simplex prophylaxis for chronic suppression therapy (unlabeled)
Candidate age grouping · source pages 30, 31
Base dose in obese patients on ideal body weight, not actual body weight Herpes simplex (recurrent)
• Adult and adolescent: PO 400 mg bid up to 12 mo
Candidate age grouping · source pages 30, 31