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Aciclovir information from DrugsUpdate  

See Available Brands of Aciclovir in India

P - Caution when used during pregnancy
L - Caution when used during lactation

Acilovir belongs to the family of medicines called antivirals, which are used to treat infections caused by viruses. Usually these medicines work for only one kind or group of virus infections. Acyclovir is used to treat the symptoms of chickenpox, shingles, herpes virus infections of the genitals (sex organs), the skin, the brain, and mucous membranes (lips and mouth), and widespread herpes virus infections in newborns. Acyclovir is also used to prevent recurrent genital herpes infections. Although acyclovir will not cure herpes, it does help relieve the pain and discomfort and helps the sores (if any) heal faster. Aciclovir is marketed under trade names such as Cyclovir, Herpex, Acivir, Acivirax, Zovirax, Aciclovir (Sanofi-Aventis) and Zovir (GSK).

Pharmacodynamics

Aciclovir differs from previous nucleoside analogues in that it contains only a partial nucleoside structure: the sugar ring is replaced by an open-chain structure. It is selectively converted into acyclo-guanosine monophosphate (acyclo-GMP) by viral thymidine kinase, which is far more effective (3000 times) in phosphorylation than cellular thymidine kinase. Subsequently, the monophosphate form is further phosphorylated into the active triphosphate form, acyclo-guanosine triphosphate (acyclo-GTP), by cellular kinases. Acyclo-GTP is a very potent inhibitor of viral DNA polymerase; it has approximately 100 times greater affinity for viral than cellular polymerase. As a substrate, acyclo-GTP is incorporated into viral DNA, resulting in chain termination. It has also been shown that viral enzymes cannot remove acyclo-GTP from the chain, which results in inhibition of further activity of DNA polymerase. Acyclo-GTP is fairly rapidly metabolised within the cell, possibly by cellular phosphatases. In sum, aciclovir can be considered a prodrug: it is administered in an inactive (or less active) form and is metabolised into a more active species after administration.

Pharmacokinetics

Activity against HSV types I and II and varicella-zoster virus is due to intracellular conversion of aciclovir to the monophosphate by viral thymidine kinase with subsequent conversion to the diphosphate and active triphosphate by cellular enzymes. This active form inhibits viral DNA synthesis and replication by interfering with viral DNA polymerase enzyme and being incorporated into viral DNA.

Absorption
15-30% is absorbed from the GI tract (oral), slightly absorbed from the skin (topical), absorbed from the eye (ophthalmic).

Distribution

CSF (50% of conc is similar to those in plasma); crosses the placenta and enters breast milk (concentrations 3 times higher than in maternal serum). Protein-binding: 9-33%.

Excretion

Via kidney by glomerular filtration and tubular secretion (14% as unchanged), via faeces (2%); elimination half-life: 2-3 hours (normal renal function), 19.5% (anuric patients), 5-7% (haemodialysis patients).

Aciclovir Indications / Aciclovir Uses

Information Not Available

Aciclovir Adverse Reactions / Aciclovir Side Effects

Nausea, vomiting, headache, diarrhoea, rash, haematological changes (occasional), increase in liver enzymes, burning, itching or erythema (topical use). Eye application may produce stinging, superficial punctate keratopathy, blepharitis or conjunctivitis. IV administration: Local reaction, pain, inflammation, phlebitis, extravasation leads to ulceration. Increase in BUN and/or creatinine. Rarely, renal failure. Potentially Fatal: Occasionally neurotoxicity after IV use: Lethargy, confusion, agitation, tremors, seizures, coma.

Precautions

More Common
For acyclovir injection only pain, swelling, or redness at place of injection

Less Common
Abdominal or stomach pain; decreased frequency of urination or amount of urine; increased thirst; loss of appetite; nausea or vomiting; unusual tiredness or weakness.


Rare
Black, tarry stools; blood in urine or stools; chills, fever, or sore throat; confusion; convulsions (seizures); hallucinations (seeing, hearing, or feeling things that are not there); hives; pinpoint red spots on skin; trembling; unusual bleeding or bruising.


Frequency not determined
Bleeding or oozing from puncture sites or mucous membranes (bowel, mouth, nose, or urinary bladder), continuing; blistering, peeling, or loosening of skin; bluish coloring, especially of the hands and feet; blurred vision; bruising at the place of injection; changes in facial skin color; changes in vision; clumsiness; coughing; decreased consciousness; difficulty in breathing or swallowing; dizziness or feeling faint, severe; fast heartbeat; irritability; itching or skin rash; large hive-like swelling on face, eyelids, lips, tongue, throat, hands, legs, feet, sex organs; mood or mental changes; muscle cramps, pain, or weakness; pale skin; red or irritated eyes; sense of agitation or uneasiness; shakiness and unsteady walk; sores, ulcers, or white spots in mouth or on lips; swelling of eyelids, face, feet, hands, lower legs or lips; swollen, painful, or tender lymph nodes (glands) in neck, armpit, or groin; unsteadiness or other problems with muscle control or coordination; yellow eyes or skin.

More common
Especially seen with high doses. General feeling of discomfort or illness

Less common
Especially seen with long-term use or high doses Diarrhea; headache

Frequency not determined
Burning, prickling, or tingling sensations; drowsiness; loss of hair

Special Precautions

Renal impairment. Pregnancy, lactation. Neurological abnormalities with significant hypoxia, serious hepatic or electrolyte abnormalities. Maintain adequate hydration.

Other Drug Interactions

Probenecid decreases urinary excretion and increases half-life. Risk of renal impairment increased by other nephrotoxic drugs.

Other Interactions

Information Not Available

Dosage

Oral
Primary herpes simplex infections
Adult: 200 mg 5 times daily every 4 hours for 5-10 days; for severely immunocompromised patients and those with impaired absorption: 400 mg 5 times daily for 5 days.

CrCl (ml/min)     Dosage Recommendation
<10                   200 mg every 12 hours.

Suppression of recurrent herpes simplex
Adult: 800 mg daily in 2-4 divided doses. May reduce to 400-600 mg daily if necessary. Reassess the condition every 6-12 months. For mild or infrequent recurrences: Episodic treatment may be used: 200 mg 5 times daily for 5 days, preferably begun during the prodromal period.

CrCl (ml/min)     Dosage Recommendation:
<10                   200 mg every 12 hours.

Oral
Prophylaxis of herpes simplex in immunocompromised patients
Adult: 200-400 mg 4 times daily. Child: ≥2 years: 200-400 mg 4 times daily; <2 years: 100-200 mg 4 times daily.

CrCl (ml/min)     Dosage Recommendation:
<10                   200 mg every 12 hours
 
Oral
Varicella zoster
Adult: >40 kg: 800 mg 4 times daily for 5 days. Child: ≥2 years and ≤40 kg: 20 mg/kg (up to 800 mg) 4 times daily for 5 days.

CrCl (ml/min)     Dosage Recommendation
10-25                800 mg tid.
<10                   800 mg every 12 hours

Oral
Herpes zoster (shingles)
Adult: 800 mg 5 times daily for 7-10 days.
Child: ≥6 years: 800 mg 4 times daily; 2-5 years: 400 mg 4 times daily; <2 years: 200 mg 4 times daily.

CrCl (ml/min)     Dosage Recommendation
<10                   800 mg every 12 hours
10-25                 800 mg tid.

Intravenous
Mucocutaneous herpes simplex in immunocompromised patients
Adult: 5 mg/kg every 8 hours for 7 days. Dose to be given as IV infusion over 1 hour.
Child: 10 mg/kg every 8 hours for 7 days.

Renal impairment: Peritoneal dialysis: Half the usual dose once daily. Haemodialysis: Half the usual dose every 24 hours and an additional half-dose after haemodialysis.
CrCl (ml/min)     Dosage Recommendation
25-50                Increase dose interval to 12 hours
10-25                Increase dose interval to 24 hours

Intravenous
Herpes simplex encephalitis
Adult: 10 mg/kg every 8 hours for 10 days.
Child: ≥3 months: 20 mg/kg every 8 hours for 10 days.

Renal impairment: Peritoneal dialysis: Half the usual dose once daily. Haemodialysis: Half the usual dose every 24 hours and an additional half-dose after haemodialysis.
CrCl (ml/min)     Dosage Recommendation
25-50                Increase dose interval to 12 hours.
10-25                Increase dose interval to 24 hours.

Intravenous
Genital herpes
Adult: 5 mg/kg every 8 hours  for 5-7 days.

Renal impairment: Peritoneal dialysis: Half the usual dose once daily. Haemodialysis: Half the usual dose every 24 hours and an additional half-dose after haemodialysis.
CrCl (ml/min)     Dosage Recommendation
25-50                Increase dose interval to 12 hours.   
10-25                Increase dose interval to 24 hours.

Intravenous
Neonatal herpes simplex virus infections
Child: Birth - 3 months: 10 mg/kg every 8 hours for 10 days.

Renal impairment: Peritoneal dialysis: Half the usual dose once daily. Haemodialysis: Half the usual dose every 24 hours and an additional half-dose after haemodialysis.
CrCl (ml/min)     Dosage Recommendation
25-50                Increase dose interval to 12 hours.
10-25                Increase dose interval to 24 hours

Intravenous
Herpes zoster in immunocompromised patients
Adult: ≥12 years: 10 mg/kg every 8 hours for 7 days.
Child: 20 mg/kg every 8 hours for 7 days.

Renal impairment: Peritoneal dialysis: Half the usual dose once daily. Haemodialysis: Half the usual dose every 24 hour and an additional half-dose after haemodialysis.
CrCl (ml/min)     Dosage Recommendation
25-50                Increase dose interval to 12 hours.
10-25                Increase dose interval to 24 hours.

Ophthalmic
Herpes simplex keratitis
Adult: Apply a 3% ointment 5 times daily until the 3rd day of complete healing.

Topical/Cutaneous
Herpes simplex infections of skin
Adult: Apply a 5% ointment/cream 5-6 times daily every 3-4 hours for 5-10 days.

Reconstitution
Remove the calculated dose and add it to any appropriate IV solution at a volume selected for admin during each 1-hr infusion. Recommended infusion concentrations: About 7 mg/mL or lower. Higher concentrations (e.g. 10 mg/mL) may cause phlebitis or inflammation at the inj site if there is extravasation. Standard, commercially available electrolyte and glucose solutions are suitable for IV admin; biologic or colloidal fluids (e.g. blood products, protein solutions) are not recommended.

Incompatibility

Y-site incompatibility: Ondansetron, piperacillin/tazobactam, sargramostim, tacrolimus, vinorelbine, amifostine, amsacrine, aztreonam, cefepime, dobutamine, dopamine, fludarabine, foscarnet, gemcitabine, idarubicin, levofloxacin. Syringe incompatibility: Pantoprazole, caffeine citrate. Admixture incompatibility: Dobutamine, dopamine.

Food(before/after)

May be taken with or without food. (May be taken w/ meals to reduce GI discomfort.)

List of Contraindications

Aciclovir and Pregnancy

Caution when used during pregnancy


Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).

Aciclovir and Lactation

Caution when used during lactation

Aciclovir and Children

Safety and efficacy in children under 2 years of age not established.

Aciclovir and Geriatic

Agitation, confusion, dizziness, and drowsiness may be especially likely to occur in elderly patients who are usually more sensitive than younger adults to the central nervous system effects of acyclovir. Use with caution because of the greater frequency of decreased hepatic, renal, or cardiac function, and concomitant diseases or other drug therapy.

Aciclovir and Other Contraindications

Hypersensitivity.

Storage

Intravenous
Vial: Store between 15-25°C.
Once diluted for admininstration, solution should be used within 24 hours.

Ophthalmic

Store at 15-25°C. Oral: Store at 15-25°C.

Topical/Cutaneous

Store at 15-25°C.

Lab interference

Intravenous
Vial: Store between 15-25°C.
Once diluted for admininstration, solution should be used within 24 hours.

Ophthalmic

Store at 15-25°C. Oral: Store at 15-25°C.

Topical/Cutaneous

Store at 15-25°C.

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