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Pharmacogenetics and Genomics Jul 2022
Topics: Acyclovir; Antiviral Agents; Ganciclovir; Humans
PubMed: 35665708
DOI: 10.1097/FPC.0000000000000474 -
Archives of Internal Medicine Jun 1984Acyclovir is a selective antiherpes agent. Its selective activity is by exploitation of differences between the herpes-specific and host cell enzymes. The major route of... (Review)
Review
Acyclovir is a selective antiherpes agent. Its selective activity is by exploitation of differences between the herpes-specific and host cell enzymes. The major route of elimination of acyclovir is via the kidney by glomerular filtration and renal tubular secretion. In immunocompromised patients, acyclovir is effective for the prophylaxis and therapy of herpes simplex virus infections and for the treatment of herpes zoster and varicella. In nonimmunocompromised patients, acyclovir is beneficial in the therapy of herpes keratoconjunctivitis and in the therapy of genital herpes, with maximal benefit seen in those patients who have primary genital herpes. There is some benefit from acyclovir administration in patients with herpes zoster who are otherwise normal. The toxic reactions to acyclovir consist of phlebitis, local irritation, and occasionally, reversible renal dysfunction. Dose reduction is recommended in patients with impaired renal function.
Topics: Acyclovir; Drug Interactions; Drug Resistance, Microbial; Herpesviridae; Herpesviridae Infections; Humans; Immunosuppression Therapy; Kinetics
PubMed: 6329117
DOI: 10.1001/archinte.144.6.1241 -
Drugs Nov 1983Acyclovir (aciclovir) is a nucleoside analogue antiviral drug related to cytarabine, idoxuridine, trifluridine and vidarabine. In common with these earlier antivirals,... (Clinical Trial)
Clinical Trial Review
Acyclovir (aciclovir) is a nucleoside analogue antiviral drug related to cytarabine, idoxuridine, trifluridine and vidarabine. In common with these earlier antivirals, acyclovir is active against some members of the herpesvirus group of DNA viruses. The efficacy of topical acyclovir has been convincingly demonstrated in ocular herpetic keratitis, and in initial and primary initial genital herpes infection, but little or no clinical benefit was seen when non-primary initial genital infections were assessed separately. Acyclovir ointment demonstrated little benefit in recurrent genital herpes but topical acyclovir cream decreased the course of the infection by 1 to 2 days. Orally and intravenously administered acyclovir were beneficial in initial genital herpes infections, and oral therapy shortened the duration of recurrent infections by 1 to 2 days but did not ameliorate pain. In non-immunocompromised patients with recurrent herpes simplex labialis, generally little clinical benefit was seen with the use of topical acyclovir ointment even when therapy was initiated during the prodromal phase, while topical acyclovir cream effected small but significant improvements in the clinical but not the symptomological course of the disease. However, in immunocompromised patients, both intravenous and topical acyclovir shortened the clinical course of herpes simplex virus infections occurring mainly on the lips, oral mucosa and face, and prophylaxis with either oral or intravenous acyclovir suppressed the appearance of recurrent lesions from latent virus for the period of drug administration, but acyclovir did not eradicate latent herpesviruses. In non-immunocompromised patients, intravenous acyclovir was shown to decrease the acute pain of zoster, especially in the elderly, but postherpetic neuralgia was not ameliorated. When immunocompromised patients were studied, intravenous acyclovir inhibited the progression of zoster infections and shortened the healing time and duration of viral shedding in patients with cutaneous disseminated zoster. However, acute and post-herpetic pain were not significantly affected. Well designed controlled studies are underway to establish the efficacy of acyclovir in herpes simplex encephalitis and cytomegalovirus infections in immunocompromised patients, infections due to Epstein-Barr virus, and neonatal herpesvirus infections. Despite some aspects of the drug's use which require further clarification, acyclovir will make a major impact on the treatment of herpesviral infections. Barring unexpected findings with wider clinical use, it will become the agent of choice in several conditions.
Topics: Acyclovir; Animals; Clinical Trials as Topic; Cytomegalovirus; Drug Resistance, Microbial; Encephalitis; Female; Herpes Genitalis; Herpes Simplex; Herpes Zoster; Herpesvirus 4, Human; Humans; Immunity; Keratitis, Dendritic; Kinetics; Male; Mutagens; Recurrence
PubMed: 6315332
DOI: 10.2165/00003495-198326050-00002 -
Molecules (Basel, Switzerland) Oct 2021Acyclovir (ACV) is an effective and selective antiviral drug, and the study of its toxicology and the use of appropriate detection techniques to control its toxicity at... (Review)
Review
Acyclovir (ACV) is an effective and selective antiviral drug, and the study of its toxicology and the use of appropriate detection techniques to control its toxicity at safe levels are extremely important for medicine efforts and human health. This review discusses the mechanism driving ACV's ability to inhibit viral coding, starting from its development and pharmacology. A comprehensive summary of the existing preparation methods and synthetic materials, such as 5-aminoimidazole-4-carboxamide, guanine and its derivatives, and other purine derivatives, is presented to elucidate the preparation of ACV in detail. In addition, it presents valuable analytical procedures for the toxicological studies of ACV, which are essential for human use and dosing. Analytical methods, including spectrophotometry, high performance liquid chromatography (HPLC), liquid chromatography/tandem mass spectrometry (LC-MS/MS), electrochemical sensors, molecularly imprinted polymers (MIPs), and flow injection-chemiluminescence (FI-CL) are also highlighted. A brief description of the characteristics of each of these methods is also presented. Finally, insight is provided for the development of ACV to drive further innovation of ACV in pharmaceutical applications. This review provides a comprehensive summary of the past life and future challenges of ACV.
Topics: Acyclovir; Antiviral Agents; Humans; Molecular Structure
PubMed: 34770975
DOI: 10.3390/molecules26216566 -
Journal of Medical Virology 1993The reasons for acyclovir's activity and selectivity in cells infected with HSV or VZV may be summarized as follows: 1. Activation by a HSV- or VZV-specified TK. 2.... (Review)
Review
The reasons for acyclovir's activity and selectivity in cells infected with HSV or VZV may be summarized as follows: 1. Activation by a HSV- or VZV-specified TK. 2. Greater sensitivity of viral DNA polymerase than of the cellular polymerases to ACV-TP. 3. Inactivation of the viral DNA polymerase, but not the cellular polymerases, by ACV-TP. 4. Chain termination of viral DNA by incorporation of ACV-MP. For the Epstein-Barr virus, which is also sensitive to acyclovir, there is no selective activation in infected cells [Colby et al., 1981], but the viral polymerase can be inhibited by very low levels of ACV-TP [Datta et al., 1980]. For HCMV, the activation of acyclovir is very poor but the viral polymerase is also more sensitive to ACV-TP than the cellular polymerases. One of the important contributions of acyclovir was the demonstration for the first time that a compound could prevent the DNA replication of a DNA virus at concentrations far below those that affect cellular DNA synthesis. As we all know, in the past 15 years there has been a complete rejuvenation of antiviral chemotherapy. I think it is very fortunate that we changed our outlook on the possibility of making potent and selective antiviral agents in time so that, when the AIDS epidemic came along, we did not feel completely at a loss on ways to attack viral disease.
Topics: Acyclovir; Base Sequence; Herpesviridae; Humans; Molecular Sequence Data
PubMed: 8245887
DOI: 10.1002/jmv.1890410503 -
Drugs Mar 1989Acyclovir (aciclovir) is a nucleoside antiviral drug with antiviral activity in vitro against members of the herpes group of DNA viruses. As an established treatment of... (Review)
Review
Acyclovir (aciclovir) is a nucleoside antiviral drug with antiviral activity in vitro against members of the herpes group of DNA viruses. As an established treatment of herpes simplex infection, intravenous, oral and to a lesser extent topical formulations of acyclovir provide significant therapeutic benefit in genital herpes simplex and recurrent orofacial herpes simplex. The effect of acyclovir therapy is maximised by early initiation of treatment, especially in non-primary infection which tends to have a less protracted course than the primary episode. Long term prophylactic oral acyclovir, in patients with frequent episodes of genital herpes simplex, totally suppresses recurrences in the majority of subjects; as with other infections responding to acyclovir, viral latency is not eradicated and pretreatment frequencies of recurrence return after discontinuation of treatment. Caution should accompany the prophylactic use of acyclovir in the general population, due to the theoretical risk of the emergence of viral strains resistant to acyclovir and other agents whose mechanism of action is dependent on viral thymidine kinase. Intravenous acyclovir is the treatment of choice in biopsy-proven herpes simplex encephalitis in adults, and has also been successful in the treatment of disseminated herpes simplex in pregnancy and herpes neonatorium. Intravenous and oral acyclovir protect against dissemination and progression of varicella zoster virus infection, but do not protect against post-herpetic neuralgia. In immunocompromised patients, intravenous, oral and topical acyclovir shorten the clinical course of herpes simplex infections while prophylaxis with oral or intravenous dosage forms suppresses reactivation of infection during the period of drug administration. Ophthalmic application of 3% acyclovir ointment rapidly heals herpetic dendritic corneal ulcers and superficial herpetic keratitis. Thus, despite an inability to eradicate latent virus, acyclovir administered in therapeutic or prophylactic fashion is now the standard antiviral therapy in several manifestations of herpes simplex virus infection, and indeed represents a major advance in this regard. With the exception of varicella zoster virus infections, early optimism concerning the use of the drug in diseases due to other herpes viruses has generally not been supported in clinical investigations.
Topics: Acyclovir; Animals; Humans; Virus Diseases
PubMed: 2653790
DOI: 10.2165/00003495-198937030-00002 -
Antimicrobial Agents and Chemotherapy Mar 1987ACV is an effective agent for the treatment and prophylaxis of HSV infections in both IC and immunologically normal individuals. The drug is well tolerated in both... (Review)
Review
ACV is an effective agent for the treatment and prophylaxis of HSV infections in both IC and immunologically normal individuals. The drug is well tolerated in both populations and is not significantly associated with clinical or laboratory toxicities. Because of the great potential benefit and low risk, organ transplant recipients and patients with hematologic malignancies undergoing induction chemotherapy should be screened routinely for HSV antibodies; seropositive individuals should receive prophylactic ACV during the period of most profound immunosuppression. Immunologically normal individuals with frequently recurring genital HSV or serious complications associated with outbreaks are candidates for long-term suppression with ACV.
Topics: Acquired Immunodeficiency Syndrome; Acyclovir; Drug Resistance, Microbial; Herpes Simplex; Humans; Immune Tolerance
PubMed: 3555331
DOI: 10.1128/AAC.31.3.361 -
Expert Review of Anti-infective Therapy Mar 2014The treatment of recurrent herpes labialis remains a challenge in the 21st century. The virus is ubiquitous and there is no vaccine against the disease. Although... (Review)
Review
The treatment of recurrent herpes labialis remains a challenge in the 21st century. The virus is ubiquitous and there is no vaccine against the disease. Although recurrence episodes are usually of shorter duration than the primary episode, they are debilitating to patients and there is significant stigma associated with the disease. Acyclovir Lauriad(®) is a new topical agent that was approved by the US FDA in 2013 for the treatment of recurrent herpes labialis, which affects approximately 20-40% of the population worldwide. The drug is a muco-adhesive tablet, applied to the upper gum at the onset of prodromal symptoms. Utilizing Lauriad(®) technology, a biologically active compound traverses the mucous membrane to deliver a high concentration of acyclovir directly to the site of the herpes simplex virus infection. Data from a Phase III clinical trial shows that this may be a promising therapy for patients with recurrent herpes labialis.
Topics: Acyclovir; Administration, Buccal; Clinical Trials, Phase III as Topic; Herpes Labialis; Humans; Recurrence
PubMed: 24456534
DOI: 10.1586/14787210.2014.880337 -
Clinical Pharmacy 1982
Clinical Trial Review
Topics: Acyclovir; Animals; Chemical Phenomena; Chemistry; Clinical Trials as Topic; Drug Interactions; Herpesviridae Infections; Humans; Immunosuppression Therapy; Kidney Failure, Chronic; Kinetics; Ointments; Rabbits
PubMed: 6307582
DOI: No ID Found -
Infection Control : IC Apr 1986
Topics: Acyclovir; Administration, Oral; Administration, Topical; Body Weight; Drug Resistance, Microbial; Half-Life; Herpesviridae; Humans; Kinetics
PubMed: 3634762
DOI: 10.1017/s0195941700084009