{"id":10872,"date":"2026-09-19T15:06:41","date_gmt":"2026-09-19T15:06:41","guid":{"rendered":"https:\/\/europepharmacy.eu\/?post_type=product&#038;p=10872"},"modified":"2026-09-19T15:06:42","modified_gmt":"2026-09-19T15:06:42","slug":"abacavir-sulfate-tablets","status":"publish","type":"product","link":"https:\/\/europepharmacy.eu\/it\/shop\/abacavir-sulfate-tablets\/","title":{"rendered":"Abacavir sulfate tablets"},"content":{"rendered":"<p data-path-to-node=\"11\">Abacavir sulfate (Ziagen\u00ae) is a synthetic carbocyclic analogue of the endogenous nucleoside deoxyguanosine. As a foundational component of dual- and triple-agent antiretroviral therapy (ART)\u2014often co-formulated in fixed-dose combinations such as abacavir\/lamivudine or abacavir\/dolutegravir\/lamivudine\u2014abacavir suppresses viral replication, elevates <span class=\"math-inline\" data-math=\"\\text{CD4}^+\" data-index-in-node=\"350\">$\\text{CD4}^+$<\/span> T-cell counts, and mitigates the progression of HIV-associated clinical immunodeficiency.<\/p>\n<p data-path-to-node=\"12\"><b data-path-to-node=\"12\" data-index-in-node=\"0\">Clinical Profile &amp; Pharmaceutical Formulations<\/b><\/p>\n<ul data-path-to-node=\"13\">\n<li>\n<p data-path-to-node=\"13,0,0\"><b data-path-to-node=\"13,0,0\" data-index-in-node=\"0\">Active Pharmaceutical Ingredient:<\/b> Abacavir sulfate (chemical name: <span class=\"math-inline\" data-math=\"(1S,4R)\\text{-4-[2-amino-6-(cyclopropylamino)-9}H\\text{-purin-9-yl]cyclopent-2-en-1-yl}\\text{methanol sulfate}\" data-index-in-node=\"67\">$(1S,4R)\\text{-4-[2-amino-6-(cyclopropylamino)-9}H\\text{-purin-9-yl]cyclopent-2-en-1-yl}\\text{methanol sulfate}$<\/span>).<\/p>\n<\/li>\n<li>\n<p data-path-to-node=\"13,1,0\"><b data-path-to-node=\"13,1,0\" data-index-in-node=\"0\">Dosage Forms &amp; Strengths:<\/b><\/p>\n<ul data-path-to-node=\"13,1,1\">\n<li>\n<p data-path-to-node=\"13,1,1,0,0\"><i data-path-to-node=\"13,1,1,0,0\" data-index-in-node=\"0\">Film-Coated Tablets:<\/i> 300 mg abacavir (equivalent to 351 mg abacavir sulfate), typically scored, biconvex, and debossed with manufacturer identifiers.<\/p>\n<\/li>\n<li>\n<p data-path-to-node=\"13,1,1,1,0\"><i data-path-to-node=\"13,1,1,1,0\" data-index-in-node=\"0\">Oral Solution:<\/i> 20 mg\/mL strawberry-banana flavored aqueous solution for pediatric or liquid-dependent regimens.<\/p>\n<\/li>\n<li>\n<p data-path-to-node=\"13,1,1,2,0\"><i data-path-to-node=\"13,1,1,2,0\" data-index-in-node=\"0\">Fixed-Dose Combinations:<\/i> Frequently formulated with lamivudine (600 mg\/300 mg) or lamivudine and dolutegravir (600 mg\/300 mg\/50 mg).<\/p>\n<\/li>\n<\/ul>\n<\/li>\n<\/ul>\n<p data-path-to-node=\"14\"><b data-path-to-node=\"14\" data-index-in-node=\"0\">Pharmacodynamics &amp; Mechanism of Action<\/b><\/p>\n<ul data-path-to-node=\"15\">\n<li>\n<p data-path-to-node=\"15,0,0\"><b data-path-to-node=\"15,0,0\" data-index-in-node=\"0\">Intracellular Phosphorylation:<\/b> Abacavir is a prodrug that requires a unique three-step intracellular metabolic cascade catalyzed by cellular enzymes:<\/p>\n<ol start=\"1\" data-path-to-node=\"15,0,1\">\n<li>\n<p data-path-to-node=\"15,0,1,0,0\">Phosphorylation by adenosine phosphotransferase to abacavir monophosphate.<\/p>\n<\/li>\n<li>\n<p data-path-to-node=\"15,0,1,1,0\">Deamination by cytosolic enzymes to carbovir monophosphate (<span class=\"math-inline\" data-math=\"\\text{CBV-MP}\" data-index-in-node=\"60\">$\\text{CBV-MP}$<\/span>).<\/p>\n<\/li>\n<li>\n<p data-path-to-node=\"15,0,1,2,0\">Sequential phosphorylation by cellular kinases to the active moiety: carbovir 5&#8242;-triphosphate (<span class=\"math-inline\" data-math=\"\\text{CBV-TP}\" data-index-in-node=\"95\">$\\text{CBV-TP}$<\/span>).<\/p>\n<\/li>\n<\/ol>\n<\/li>\n<li>\n<p data-path-to-node=\"15,1,0\"><b data-path-to-node=\"15,1,0\" data-index-in-node=\"0\">Reverse Transcriptase Inhibition &amp; Chain Termination:<\/b> <span class=\"math-inline\" data-math=\"\\text{CBV-TP}\" data-index-in-node=\"54\">$\\text{CBV-TP}$<\/span> structurally mimics natural deoxyguanosine triphosphate (<span class=\"math-inline\" data-math=\"\\text{dGTP}\" data-index-in-node=\"125\">$\\text{dGTP}$<\/span>) and acts as a competitive substrate inhibitor against the HIV-1 reverse transcriptase enzyme.<\/p>\n<\/li>\n<li>\n<p data-path-to-node=\"15,2,0\"><b data-path-to-node=\"15,2,0\" data-index-in-node=\"0\">Chain Termination:<\/b> Once incorporated into nascent viral cDNA strands, the lack of a 3&#8242;-hydroxyl (<span class=\"math-inline\" data-math=\"3'\\text{-OH}\" data-index-in-node=\"97\">$3&#8217;\\text{-OH}$<\/span>) group prevents the formation of standard <span class=\"math-inline\" data-math=\"3'\\text{-to-}5'\" data-index-in-node=\"152\">$3&#8217;\\text{-to-}5&#8217;$<\/span> phosphodiester bonds required to attach subsequent nucleotides, resulting in irreversible premature viral DNA chain termination.<\/p>\n<\/li>\n<li>\n<p data-path-to-node=\"15,3,0\"><b data-path-to-node=\"15,3,0\" data-index-in-node=\"0\">Cellular DNA Polymerase Selectivity:<\/b> Exhibits low inhibitory affinity for host human nuclear DNA polymerases <span class=\"math-inline\" data-math=\"\\alpha\" data-index-in-node=\"109\">$\\alpha$<\/span>, <span class=\"math-inline\" data-math=\"\\beta\" data-index-in-node=\"117\">$\\beta$<\/span>, and <span class=\"math-inline\" data-math=\"\\gamma\" data-index-in-node=\"128\">$\\gamma$<\/span>, resulting in significantly lower mitochondrial toxicity compared to earlier-generation didactic NRTIs (such as zidovudine or didanosine).<\/p>\n<\/li>\n<\/ul>\n<p data-path-to-node=\"16\"><b data-path-to-node=\"16\" data-index-in-node=\"0\">Pharmacokinetics &amp; Biotransformation<\/b><\/p>\n<ul data-path-to-node=\"17\">\n<li>\n<p data-path-to-node=\"17,0,0\"><b data-path-to-node=\"17,0,0\" data-index-in-node=\"0\">Absorption &amp; Bioavailability:<\/b> Rapidly and extensively absorbed following oral administration, demonstrating an absolute bioavailability of approximately 83% to 86%. Food does not significantly alter systemic exposure (AUC).<\/p>\n<\/li>\n<li>\n<p data-path-to-node=\"17,1,0\"><b data-path-to-node=\"17,1,0\" data-index-in-node=\"0\">Distribution:<\/b> Lipophilic properties facilitate penetration across the blood-brain barrier, achieving cerebrospinal fluid (CSF) concentrations approximately 18% to 36% of concurrent plasma concentrations. Low plasma protein binding (~50%).<\/p>\n<\/li>\n<li>\n<p data-path-to-node=\"17,2,0\"><b data-path-to-node=\"17,2,0\" data-index-in-node=\"0\">Non-CYP Hepatic Clearance:<\/b> Extensively metabolized hepatically without significant involvement of the cytochrome P450 enzyme system, avoiding typical CYP-mediated drug-drug interactions. Clearance occurs via two primary pathways:<\/p>\n<ul data-path-to-node=\"17,2,1\">\n<li>\n<p data-path-to-node=\"17,2,1,0,0\">Alcohol dehydrogenase (<span class=\"math-inline\" data-math=\"\\text{ADH}\" data-index-in-node=\"23\">$\\text{ADH}$<\/span>), converting abacavir to the 5&#8242;-carboxylic acid derivative (~30%).<\/p>\n<\/li>\n<li>\n<p data-path-to-node=\"17,2,1,1,0\">UDP-glucuronosyltransferase (<span class=\"math-inline\" data-math=\"\\text{UGT}\" data-index-in-node=\"29\">$\\text{UGT}$<\/span>), forming the 5&#8242;-glucuronide conjugate (~36%).<\/p>\n<\/li>\n<\/ul>\n<\/li>\n<li>\n<p data-path-to-node=\"17,3,0\"><b data-path-to-node=\"17,3,0\" data-index-in-node=\"0\">Elimination &amp; Kinetics:<\/b> Displays a short terminal plasma elimination half-life of 1.5 to 2.0 hours. However, the intracellular active metabolite (<span class=\"math-inline\" data-math=\"\\text{CBV-TP}\" data-index-in-node=\"146\">$\\text{CBV-TP}$<\/span>) exhibits an extended half-life exceeding 20 hours, supporting once-daily clinical dosing schedules. Renal excretion of unchanged abacavir accounts for less than 2% of the dose.<\/p>\n<\/li>\n<\/ul>\n<p data-path-to-node=\"18\"><b data-path-to-node=\"18\" data-index-in-node=\"0\">Critical Pharmacogenomic Warning: HLA-B*5701 &amp; Hypersensitivity<\/b><\/p>\n<ul data-path-to-node=\"19\">\n<li>\n<p data-path-to-node=\"19,0,0\"><b data-path-to-node=\"19,0,0\" data-index-in-node=\"0\">Mandatory Pre-Treatment Screening:<\/b> Clinical guidelines mandate that all patients undergo pharmacogenomic screening for the human leukocyte antigen allele <span class=\"math-inline\" data-math=\"\\text{HLA-B*5701}\" data-index-in-node=\"154\">$\\text{HLA-B*5701}$<\/span> prior to initiating abacavir.<\/p>\n<\/li>\n<li>\n<p data-path-to-node=\"19,1,0\"><b data-path-to-node=\"19,1,0\" data-index-in-node=\"0\">Abacavir Hypersensitivity Reaction (AHR):<\/b> Carriage of the <span class=\"math-inline\" data-math=\"\\text{HLA-B*5701}\" data-index-in-node=\"58\">$\\text{HLA-B*5701}$<\/span> allele is directly linked to an immune-mediated multi-organ hypersensitivity reaction. Abacavir binds non-covalently within the antigen-binding cleft of the <span class=\"math-inline\" data-math=\"\\text{HLA-B*5701}\" data-index-in-node=\"233\">$\\text{HLA-B*5701}$<\/span> molecule, altering its peptide presentation specificity and triggering widespread activation of self-reactive <span class=\"math-inline\" data-math=\"\\text{CD8}^+\" data-index-in-node=\"361\">$\\text{CD8}^+$<\/span> T-cells.<\/p>\n<\/li>\n<li>\n<p data-path-to-node=\"19,2,0\"><b data-path-to-node=\"19,2,0\" data-index-in-node=\"0\">Clinical Presentation:<\/b> Symptoms typically manifest within the first six weeks of therapy and involve at least two of the following organ systems:<\/p>\n<ul data-path-to-node=\"19,2,1\">\n<li>\n<p data-path-to-node=\"19,2,1,0,0\">Systemic: High fever, extreme fatigue, malaise.<\/p>\n<\/li>\n<li>\n<p data-path-to-node=\"19,2,1,1,0\">Cutaneous: Maculopapular, generalized, or confluent rash.<\/p>\n<\/li>\n<li>\n<p data-path-to-node=\"19,2,1,2,0\">Gastrointestinal: Severe nausea, vomiting, diarrhea, abdominal pain.<\/p>\n<\/li>\n<li>\n<p data-path-to-node=\"19,2,1,3,0\">Respiratory: Dyspnea, cough, pharyngitis.<\/p>\n<\/li>\n<\/ul>\n<\/li>\n<li>\n<p data-path-to-node=\"19,3,0\"><b data-path-to-node=\"19,3,0\" data-index-in-node=\"0\">Absolute Rechallenge Contraindication:<\/b> If an AHR is suspected or diagnosed, abacavir must be <b data-path-to-node=\"19,3,0\" data-index-in-node=\"93\">permanently discontinued immediately<\/b>. Rechallenging a patient following an AHR can cause rapid hemodynamic collapse, severe multi-organ failure, and death within hours.<\/p>\n<\/li>\n<\/ul>\n<p data-path-to-node=\"20\"><b data-path-to-node=\"20\" data-index-in-node=\"0\">Important Safety Information &amp; Boxed Warnings<\/b><\/p>\n<ul data-path-to-node=\"21\">\n<li>\n<p data-path-to-node=\"21,0,0\"><b data-path-to-node=\"21,0,0\" data-index-in-node=\"0\">Fatal Hypersensitivity Reactions:<\/b> Outlined in a dedicated Boxed Warning. Patients who test positive for <span class=\"math-inline\" data-math=\"\\text{HLA-B*5701}\" data-index-in-node=\"104\">$\\text{HLA-B*5701}$<\/span> must not be prescribed abacavir-containing regimens.<\/p>\n<\/li>\n<li>\n<p data-path-to-node=\"21,1,0\"><b data-path-to-node=\"21,1,0\" data-index-in-node=\"0\">Lactic Acidosis &amp; Severe Hepatomegaly with Steatosis:<\/b> Class warning applicable to nucleoside analogues, typically secondary to rare mitochondrial toxicity. Manifests with elevated serum lactate, tachypnea, nausea, and acute hepatic failure.<\/p>\n<\/li>\n<li>\n<p data-path-to-node=\"21,2,0\"><b data-path-to-node=\"21,2,0\" data-index-in-node=\"0\">Ethanol Interaction:<\/b> Co-administration with ethanol competitively inhibits alcohol dehydrogenase (<span class=\"math-inline\" data-math=\"\\text{ADH}\" data-index-in-node=\"98\">$\\text{ADH}$<\/span>), reducing abacavir clearance and increasing abacavir AUC by approximately 41%.<\/p>\n<\/li>\n<li>\n<p data-path-to-node=\"21,3,0\"><b data-path-to-node=\"21,3,0\" data-index-in-node=\"0\">Cardiovascular Considerations:<\/b> Large observational cohort studies (such as the D:A:D study) have reported an association between current\/recent abacavir use and an elevated risk of myocardial infarction. Caution is warranted in patients with substantial underlying cardiovascular risk factors<\/p>\n<\/li>\n<\/ul>\n\n    <div class=\"xs_social_share_widget xs_share_url after_content \t\tmain_content  wslu-style-1 wslu-share-box-shaped wslu-fill-colored wslu-none wslu-share-horizontal wslu-theme-font-no wslu-main_content\">\n\n\t\t\n        <ul>\n\t\t\t        <\/ul>\n    <\/div> \n","protected":false},"excerpt":{"rendered":"<p>Abacavir sulfate (oral tablets or oral solution) is a prescription-only carbocyclic nucleoside reverse transcriptase inhibitor (NRTI) indicated for the treatment of Human Immunodeficiency Virus type 1 (HIV-1) infection in combination with other antiretroviral agents. By undergoing intracellular biotransformation into its active triphosphate metabolite (carbovir triphosphate), it competitively inhibits HIV-1 reverse transcriptase and forces premature viral DNA chain termination. Administration mandates prior genetic screening for the <span class=\"math-inline\" data-math=\"\\text{HLA-B*5701}\" data-index-in-node=\"539\">$\\text{HLA-B*5701}$<\/span> allele to avoid life-threatening, multi-organ hypersensitivity reactions. Dispensed strictly by medical prescription.<\/p>","protected":false},"featured_media":10874,"comment_status":"open","ping_status":"closed","template":"","meta":{"postBodyCss":"","postBodyMargin":[],"postBodyPadding":[],"postBodyBackground":{"backgroundType":"classic","gradient":""}},"product_brand":[],"product_cat":[506,1073],"product_tag":[1075,1074,1082,1079,1078,1080,1077,1083,1081,1076],"class_list":["post-10872","product","type-product","status-publish","has-post-thumbnail","product_cat-anti-viral","product_cat-hivaid","product_tag-abacavir-300mg","product_tag-abacavir-sulfate","product_tag-antiviral-therapy","product_tag-carbovir-triphosphate","product_tag-hiv-1-antiretroviral","product_tag-hla-b5701-screening","product_tag-nrti-medication","product_tag-prescription-hiv-drug","product_tag-reverse-transcriptase-inhibitor","product_tag-ziagen-generic","instock","shipping-taxable","purchasable","product-type-simple"],"yoast_head":"<!-- This site is optimized with the Yoast SEO Premium plugin v26.5 (Yoast SEO v28.4) - https:\/\/yoast.com\/product\/yoast-seo-premium-wordpress\/ -->\n<title>Abacavir sulfate tablets<\/title>\n<meta name=\"description\" content=\"Abacavir sulfate 300 mg tablets: NRTI antiretroviral for HIV-1 combination therapy. Mechanism of action, carbovir triphosphate kinetics, and HLA-B*5701 boxed warning.\" \/>\n<meta name=\"robots\" content=\"index, follow, max-snippet:-1, max-image-preview:large, max-video-preview:-1\" \/>\n<link rel=\"canonical\" href=\"https:\/\/europepharmacy.eu\/it\/shop\/abacavir-sulfate-tablets\/\" \/>\n<meta property=\"og:locale\" content=\"it_IT\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Abacavir sulfate tablets\" \/>\n<meta property=\"og:description\" content=\"Abacavir sulfate (oral tablets or oral solution) is a prescription-only carbocyclic nucleoside reverse transcriptase inhibitor (NRTI) indicated for the treatment of Human Immunodeficiency Virus type 1 (HIV-1) infection in combination with other antiretroviral agents. By undergoing intracellular biotransformation into its active triphosphate metabolite (carbovir triphosphate), it competitively inhibits HIV-1 reverse transcriptase and forces premature viral DNA chain termination. Administration mandates prior genetic screening for the $text{HLA-B*5701}$ allele to avoid life-threatening, multi-organ hypersensitivity reactions. 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Mechanism of action, carbovir triphosphate kinetics, and HLA-B*5701 boxed warning.","robots":{"index":"index","follow":"follow","max-snippet":"max-snippet:-1","max-image-preview":"max-image-preview:large","max-video-preview":"max-video-preview:-1"},"canonical":"https:\/\/europepharmacy.eu\/it\/shop\/abacavir-sulfate-tablets\/","og_locale":"it_IT","og_type":"article","og_title":"Abacavir sulfate tablets","og_description":"Abacavir sulfate (oral tablets or oral solution) is a prescription-only carbocyclic nucleoside reverse transcriptase inhibitor (NRTI) indicated for the treatment of Human Immunodeficiency Virus type 1 (HIV-1) infection in combination with other antiretroviral agents. By undergoing intracellular biotransformation into its active triphosphate metabolite (carbovir triphosphate), it competitively inhibits HIV-1 reverse transcriptase and forces premature viral DNA chain termination. 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