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Aspirin
Allopathy
Prescription Required
DCGI (Drugs Controller General of India)
Schedule H
Aspirin is a cyclooxygenase-1 (COX-1) inhibitor belonging to Nonsteroidal Anti-inflammatory Drugs (NSAIDs) / Nonopioid Analgesics.
Aspirin is a salicylate used to treat pain, fever, inflammation, and migraines, and reduce the risk of major adverse cardiovascular events.
Rapidly absorbed from the gastrointestinal tract; less reliable (rectal); absorbed through the skin. Partially hydrolyzed by esterases to salicylate during absorption in the GI tract. Bioavailability: 50-75% (immediate release). Time to peak plasma concentration: Approx 1-2 hours (non-enteric-coated); 3-4 hours (enteric-coated); Approx 2 hours (extended-release cap). Widely and rapidly distributed into most body tissues and fluids. Aspirin crosses the placenta and enters breast milk. The volume of distribution is about 170 mL/kg. Plasma protein binding: 80-90%. It metabolized in the liver into salicylic acid, salicyl phenolic glucuronide, salicylic acyl glucuronide, gentisic acid, and gentisuric acid. Undergoes first-pass metabolism. It is excreted via urine (75% as salicylic acid, 10% as salicylic acid). The elimination half-life of Aspirin was found to be 15-20 minutes.
Aspirin shows common side effects like Nausea, vomiting, stomach pain, heartburn, etc.
Aspirin is available in the form of Oral Tablets, Oral capsules, and Rectal suppositories.
Aspirin is available in India, the US, the UK, Germany, Canada, Mexico, Japan, New Zealand, Spain, China, and Australia.
Aspirin belonging to the Nonsteroidal Anti-inflammatory Drugs (NSAIDs) / Nonopioid Analgesic, acts as a cyclooxygenase-1 (COX-1).
Aspirin [acetylsalicylic acid (ASA)] inhibits prostaglandin synthesis resulting in the inhibition of platelet aggregation for a lifespan of about 7-10 days. The acetyl group of aspirin binds with a serine residue of cyclooxygenase-1 (COX-1), resulting in the irreversible inactivation of the enzyme. Inhibition of COX-1 prevents the conversion of arachidonic acid to thromboxane A2 (TXA2), which is a potent agonist of platelet aggregation.
The Onset of action of Aspirin is for immediate release: Platelet inhibition: Nonenteric-coated: <1 hour; enteric-coated: 3 to 4 hours.
The Tmax of Aspirin is for immediate release: ~1 to 2 hours (non-enteric-coated), 3 to 4 hours (enteric-coated); Extended-release capsule: ~2 hours.
The Duration of Action of Aspirin is for immediate release: 4 to 6 hours; however, platelet inhibitory effects last the lifetime of the platelet (~10 days) due to its irreversible inhibition of platelet COX-1.
Aspirin is available in the form of Oral Tablets, Oral Capsules,s and Rectal Suppositories.
Aspirin tablets and capsules are taken orally after a meal. This reduces irritating gastrointestinal effects.
Aspirin Suppository-Remove suppository from the plastic packet and insert it into the rectum as far as possible.
Aspirin is an antiplatelet drug that is used to prevent clots in blood vessels and also relieves pain and inflammation. It can be taken in combination with other antiplatelets for better action. It is not recommended in patients with bleeding disorders.
Aspirin is a cyclooxygenase-1 (COX-1) inhibitor belonging to Nonsteroidal Anti-inflammatory Drugs (NSAIDs) / Nonopioid Analgesics.
Aspirin is a selective and irreversible inhibitor of the cyclooxygenase-1 (COX-1) enzyme resulting in direct inhibition of the biosynthesis of prostaglandins and thromboxanes from arachidonic acid. Additionally, it also inhibits platelet aggregation.
Aspirin is approved for use in the following clinical indications
Adult Indications
- Analgesic and antipyretic
- Anti-inflammatory for arthritis associated with rheumatic disease
- Atherosclerotic cardiovascular disease
- Carotid endarterectomy
- Valvular heart disease
Pediatric Indications
- Analgesic
- Anti-inflammatory
- Antiplatelet effects
- Kawasaki disease
- Multisystem inflammatory syndrome in children associated with SARS-CoV-2
- Rheumatic fever
Although not approved, there have been certain off-label indications. These include
- Carotid artery stenting
- Colorectal cancer risk reduction, primary prevention
- Migraine, acute treatment
- Pericarditis, acute or recurrent
- Polycythemia vera, prevention of thrombosis
- Preeclampsia prevention
- Venous thromboembolism prevention, indefinite therapy
- Venous thromboembolism prophylaxis for total hip or total knee arthroplasty.
Adult Dose
- Analgesic and antipyretic
Immediate release: Oral: 325 mg to 1 g every 4 to 6 hours as needed; usual maximum daily dose: 4 g/day.
- Anti-inflammatory for arthritis associated with rheumatic disease
Immediate release: Oral: 4 to 8 g/day in 4 to 5 divided doses as needed; titrate dose based on response and tolerability. Continue treatment until symptoms resolve (typically 1 to 2 weeks, but potentially up to 8 weeks). Use of aspirin at these high doses (4 to 8 g/day) may be limited by adverse effects (tinnitus, diminished auditory acuity, GI intolerance), making other available NSAIDs preferred.
- Atherosclerotic cardiovascular disease
- Acute coronary syndrome
Non–ST-elevation acute coronary syndromes or ST-elevation myocardial infarction:
Initial:
Immediate release (non-enteric coated)
Oral: 162 to 325 mg administered once (chew and swallow) at the time of diagnosis.
Rectal (alternative route): 600 mg administered once at the time of diagnosis if an IR oral formulation is unavailable or the oral route is not feasible.
Maintenance (secondary prevention):
Immediate release
Oral: 75 to 100 mg once daily.
- Percutaneous coronary intervention for stable ischemic heart disease (off-label use):
Initial:
Immediate release (non–enteric-coated): Oral: 325 mg given ≥2 hours
(Preferably 24 hours) before the procedure.
Maintenance:
Immediate release: Oral: 75 to 100 mg once daily in combination with clopidogrel or ticagrelor (DAPT); upon completion of DAPT, continue aspirin indefinitely.
- Atherosclerotic cardiovascular disease, primary prevention (off-label use)
Immediate release: Oral: 75 to 100 mg once daily
- Atherosclerotic cardiovascular disease, secondary prevention
Carotid artery atherosclerosis, asymptomatic or symptomatic (off-label use)
Immediate release: Oral: 75 to 325 mg once daily.
Coronary artery bypass graft surgery
Immediate release: Oral: 75 to 81 mg once daily beginning preoperatively; continue indefinitely following surgery.
- Ischemic stroke/Transient ischemic attack:
Intracranial atherosclerosis (50% to 99% stenosis of a major intracranial artery),
secondary prevention
Immediate release: Oral: 162 to 325 mg once daily; for patients with recent stroke or transient ischemic attack (TIA) (within 30 days) may consider short-term use of clopidogrel (for 21 or up to 90 days depending on the degree of stenosis and severity of stroke or TIA) in combination with aspirin followed by single-agent antiplatelet therapy with aspirin, clopidogrel, or aspirin/ER dipyridamole indefinitely.
Noncardioembolic ischemic stroke/transient ischemic attack
Initial:
Immediate release
Oral: 160 to 325 mg administered once at the time of diagnosis.
Rectal (alternative route): 300 mg administered once at the time of diagnosis if the oral route is not feasible.
Maintenance (alternative agent):
Immediate release: Oral: 50 to 325 mg once daily; some experts recommend 50 to 100 mg once daily.
- Peripheral atherosclerotic disease (upper or lower extremity; with or without a revascularization procedure) (off-label use)
Immediate release: Oral: 75 to 100 mg once daily.
- Stable ischemic heart disease
Immediate release: Oral: 75 to 100 mg once daily.
- Carotid endarterectomy
Immediate release: Oral: 75 to 325 mg once daily starting prior to surgery and continued indefinitely.
- Valvular heart disease
Surgical prosthetic heart valve replacement, thromboprophylaxis
- Bioprosthetic aortic or mitral heart valve replacement (off-label use)
Immediate release: Oral: 75 to 100 mg once daily.
- Mechanical aortic or mitral heart valve replacement (off-label use)
Immediate release: Oral: 75 to 100 mg once daily in combination with warfarin.
- Transcatheter aortic valve replacement, thromboprophylaxis (off-label use)
Immediate release
Oral: 75 to 100 mg once daily; may use in combination with clopidogrel for 3 to 6 months after transcatheter aortic valve replacement, depending on the type of valve implanted. To minimize the risk of bleeding complications, may give aspirin or clopidogrel alone and reserve dual antiplatelet therapy during the first 3 to 6 months for patients at high risk of a thrombotic event; for either strategy, continue aspirin indefinitely after the initial 3 to 6 months of therapy.
- Transcatheter mitral valve repair with MitraClip device, thromboprophylaxis (off-label use)
Immediate release: Oral:
Loading dose: 325 mg once immediately following MitraClip insertion or within 24 hours prior to the procedure; use in combination with clopidogrel.
Maintenance: 81 mg once daily for at least 6 months; may use as monotherapy or in combination with clopidogrel.
Pediatric Indications
- Analgesic
Oral, rectal:
Infants, Children, and Adolescents weighing <50 kg: 10 to 15 mg/kg/dose every 4 to 6 hours; maximum daily dose: 90 mg/kg/day or 4,000 mg/day whichever is less.
Children ≥12 years and Adolescents weighing ≥50 kg: 325 to 650 mg every 4 to 6 hours; maximum daily dose: 4,000 mg/day.
- Anti-inflammatory
Oral:
Infants, Children, and Adolescents: Initial: 60 to 90 mg/kg/day in divided doses; usual maintenance: 80 to 100 mg/kg/day divided every 6 to 8 hours; monitor serum concentrations.
- Antiplatelet effects
Oral:
Infants, Children, and Adolescents: Adequate pediatric studies have not been performed; pediatric dosage is derived from adult studies. The usual adult maximum daily dose for antiplatelet effects is 325 mg/day.
- Kawasaki disease
Oral:
Infants, Children, and Adolescents:
Initial therapy (acute phase): Recommended dosing regimens vary. Use in combination with IV immune globulin (within the first 10 days of symptom onset) and corticosteroids in some cases.
High dose: 80 to 100 mg/kg/day divided every 6 hours for up to 14 days until fever resolves for at least 48 to 72 hours.
Moderate dose: 30 to 50 mg/kg/day divided every 6 hours for up to 14 days until fever resolves for at least 48 to 72 hours.
Subsequent therapy (low dose; antiplatelet effects): 3 to 5 mg/kg/day once daily; reported dosing range: 1 to 5 mg/kg/day; initiate after fever resolves for at least 48 to 72 hours (or after 14 days). In patients without coronary artery abnormalities, administer the lower dose for 6 to 8 weeks. In patients with coronary artery abnormalities, low-dose aspirin should be continued indefinitely (in addition to therapy with warfarin).
- Multisystem inflammatory syndrome in children associated with SARS-CoV-2
Oral:
Infants, Children, and Adolescents: 3 to 5 mg/kg/day once daily; maximum daily dose: 81 mg/day; continue until normalization of platelet count, confirmed normal coronary arteries at ≥4 weeks after diagnosis, and ejection fraction >35%.
- Rheumatic fever
Oral:
Infants, Children, and Adolescents: Initial: 100 mg/kg/day divided into 4 to 5 doses; if response inadequate, may increase the dose to 125 mg/kg/day; continue for 2 weeks; then decrease dose to 60 to 70 mg/kg/day in divided doses for an additional 3 to 6 weeks.
Although not approved, there have been certain off-label indications. These include
- Carotid artery stenting
- Percutaneous approach
Initial:
Initiation ≥48 hours before procedure: Immediate release: Oral: 325 mg twice daily in combination with clopidogrel.
Initiation <48 hours before procedure: Immediate release: Oral: 650 mg once at least 4 hours before procedure in combination with clopidogrel.
Maintenance:
Immediate release: Oral: 75 to 325 mg once daily in combination with clopidogrel for at least 4 weeks, then discontinue clopidogrel and continue aspirin 75 to 325 mg once daily indefinitely thereafter. In patients with a history of neck irradiation, some experts recommend continuing aspirin plus clopidogrel indefinitely.
- Transcarotid approach
Initial:
Initiation ≥72 hours before procedure: Immediate release: Oral: 75 to 325 mg once daily in combination with clopidogrel.
Initiation <72 hours before procedure: Immediate release: Oral: 650 mg once at least 4 hours before procedure in combination with clopidogrel.
Maintenance:
Immediate release: Oral: 75 to 325 mg once daily in combination with clopidogrel for at least 4 weeks, then discontinue clopidogrel and continue aspirin 75 to 325 mg once daily indefinitely thereafter. In patients with a history of neck irradiation, some experts recommend continuing aspirin plus clopidogrel indefinitely.
- Colorectal cancer risk reduction, primary prevention
Immediate release: Oral: 75 to 325 mg once daily.
- Migraine, acute treatment
Immediate release: Oral: 900 mg or 1 g once.
- Pericarditis, acute or recurrent
Immediate release: Oral: Initial: 650 mg to 1 g every 8 hours until resolution of symptoms for at least 24 hours and normalization of inflammatory biomarkers (eg, C-reactive protein) if monitored; initial therapy typically lasts for ≥1 to 2 weeks. Gradually taper over several weeks by decreasing each dose by 250 to 500 mg every 1 to 2 weeks; during taper, ensure the patient remains asymptomatic and inflammatory biomarkers remain normal (if monitored). Use in combination with colchicine. In patients at risk of NSAID-related GI toxicity, prophylaxis (generally with a proton pump inhibitor) is recommended.
- Polycythemia vera, prevention of thrombosis
Immediate release: Oral: 75 to 100 mg once or twice daily.
- Preeclampsia prevention
Immediate release: Oral: 81 to 162 mg once daily, ideally beginning between 12 to 16 weeks gestation but may be started up to 28 weeks gestation; continue therapy until delivery.
- Venous thromboembolism prevention, indefinite therapy
Immediate release: Oral: 100 mg once daily after completion of a conventional treatment course with therapeutic anticoagulation.
- Venous thromboembolism prophylaxis for total hip or total knee arthroplasty
Immediate release: Oral: After a 5-day course of postoperative rivaroxaban prophylaxis, initiate aspirin 81 mg once daily on postoperative day 6 and continue for 9 days for TKA (total duration: 14 days) or 30 days for THA (total duration: 35 days).
Aspirin is available in various strengths as 800 mg; 500 mg; 325 mg; 81 mg; buffered 500 mg; buffered 325 mg; buffered 81 mg; 975 mg; 650 mg; 125 mg; 600 mg; 60 mg; 300 mg; 162 mg; 1 g; 81 mg with phytosterols; 227.5 mg; 1200 mg; 162.5 mg.
Aspirin is available in the form of Oral Tablets, Oral capsules, and Rectal suppositories.
Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo Biloba.
Aspirin is contraindicated in patients with
● In patients with a hypersensitivity to nonsteroidal anti-inflammatory drugs (NSAIDs).
● In patients with the syndrome of asthma, rhinitis, and nasal polyps. Aspirin may cause severe urticaria, angioedema, or bronchospasm.
- Risk of Bleeding
ASPIRIN increases the risk of bleeding. Risk factors for bleeding include the use of other drugs that increase the risk of bleeding (e.g., anticoagulants, antiplatelet agents, and chronic use of NSAIDs).
- Peptic Ulcer Disease
Aspirin may cause gastric ulceration and bleeding. Avoid Aspirin in patients with active peptic ulcer disease.
- Fetal Toxicity
Aspirin can cause fetal harm when administered to a pregnant woman. Maternal aspirin use during later stages of pregnancy may cause low birth weight, increased incidence of intracranial hemorrhage in premature infants, stillbirths, and neonatal death. Because NSAIDs may cause premature closure of the fetal ductus arteriosus, avoid Aspirin in the third trimester of pregnancy.
Alcohol Warning
Avoid consumption of alcohol. It may increase the risk of gastrointestinal bleeding.
Breast Feeding Warning
Because of the potential for serious adverse reactions in nursing infants from Aspirin, choose either to discontinue Aspirin or discontinue nursing.
Pregnancy Warning
Salicylate is present in the umbilical cord and newborn serum following maternal use of Aspirin prior to delivery. Salicylic acid and other metabolites can also be detected in the newborn urine following in-utero exposure. Fetal outcomes are influenced by maternal dose; low-dose aspirin (≤150 mg/day) is not associated with the same risks as higher doses and has a positive effect on some pregnancy outcomes. Adverse effects reported in the fetus following maternal use of high-dose aspirin include mortality, intrauterine growth retardation, salicylate intoxication, bleeding abnormalities, and neonatal acidosis. Use of aspirin close to delivery may cause premature closure of the ductus arteriosus. Adverse effects reported in the mother include anemia, hemorrhage, prolonged gestation, and prolonged labor.
Food Warning
Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo Biloba.
- Common Adverse effects
Cardiac arrhythmia, hypotension, tachycardia, Dehydration, hyperglycemia, hyperkalemia, hypoglycemia (children), increased thirst, metabolic acidosis, Abdominal pain, dyspepsia, gastrointestinal perforation, gastrointestinal ulcer, heartburn, nausea, vomiting, Postpartum hemorrhage, post-term pregnancy, prolonged labor, proteinuria, stillborn infant, Disorder of hemostatic components of blood, disseminated intravascular coagulation, hemorrhage, prolonged bleeding time, prolonged prothrombin time, thrombocytopenia, Hepatitis, increased liver enzymes, Agitation, brain edema, coma, confusion, dizziness, headache, hypothermia, lethargy, seizure, Increased blood urea nitrogen, increased serum creatinine, interstitial nephritis, renal failure syndrome, renal insufficiency, renal papillary necrosis, Hyperventilation, laryngeal edema, pulmonary edema, respiratory alkalosis, tachypnea, Fever, low birth weight.
- Rare Adverse effects
Urticaria, Gastrointestinal hemorrhage, pancreatitis, Anaphylaxis, angioedema, Drug reaction with eosinophilia and systemic symptoms, intracranial hemorrhage, Reye's syndrome, Rhabdomyolysis, Macular degeneration (age-related), Hearing loss, tinnitus, Asthma, bronchospasm.
- Renin-angiotensin system (RAS) inhibitors: In patients who are elderly, volume-depleted (including those on diuretic therapy), or who have compromised renal function, coadministration of NSAIDs, including Aspirin, with RAS inhibitors may result in deterioration of renal function, including possible acute renal failure. These effects are usually reversible. Monitor renal function periodically in patients receiving RAS inhibitors and Aspirin. NSAIDs, including Aspirin, may attenuate the antihypertensive effects of RAS inhibitors.
- Anticoagulant and antiplatelets: Increased risk of bleeding Anticonvulsants: Salicylate can displace protein-bound phenytoin and valproic acid, leading to a decrease in the total concentration of phenytoin and an increase in serum valproic acid levels.
- Methotrexate: Salicylate can inhibit renal clearance of methotrexate, leading to bone marrow toxicity, especially in the elderly or the renal impaired.
- Nonsteroidal Anti-inflammatory Drugs (NSAIDs): The concurrent use of Aspirin with other NSAIDs increases the risk of bleeding and may result in renal impairment. Ibuprofen can interfere with the anti-platelet effect of low-dose aspirin. Patients who use Aspirin and take a single dose of ibuprofen 400 mg should dose the ibuprofen at least 2-4hours or longer after ingestion of Aspirin. Wait 8 hours after ibuprofen dosing, before giving aspirin, to avoid significant interference. Nonselective NSAIDs may interfere with the antiplatelet effect of low-dose aspirin.
The common side effects of Aspirin include the following
- Common
Nausea, vomiting, stomach pain, heartburn.
- Rare
Hives, rash, swelling of the eyes, face, lips, tongue, or throat, wheezing or difficulty breathing, hoarseness, fast heartbeat, fast breathing, cold, clammy skin, ringing in the ears, loss of hearing, bloody vomit, vomit that looks like coffee grounds, bright red blood in stools, black or tarry stools.
- Pregnancy
Pregnancy Category C (D if full-dose aspirin in 3rd trimester)
Avoid use during the third trimester of pregnancy because NSAIDs such as Aspirin may cause premature closure of the fetal ductus arteriosus. Salicylate products have also been associated with alterations in maternal and neonatal hemostasis mechanisms, decreased birth weight, and perinatal mortality.
- Nursing Mothers
Because of the potential for serious adverse reactions in nursing infants from Aspirin, choose either to discontinue Aspirin or discontinue nursing.
- Pediatric Use
As per FDA, safety and effectiveness in pediatric patients have not been established.
- Geriatric Use
In a large collaborative overview of aspirin for vascular event prevention, including over 14000 patients over 65 years of age, no overall differences in safety or effectiveness were observed between these subjects and younger subjects, and other reported clinical experience has not identified differences in responses between the elderly and younger patients.
- Salicylate toxicity may result from acute ingestion (overdose) or chronic intoxication. The early signs of salicylic overdose (salicylism), including tinnitus (ringing in the ears), occur at plasma concentrations approaching 200 mcg/mL. Plasma concentrations of aspirin above 300 mcg/mL are clearly toxic. Severe toxic effects are associated with levels above 400 mcg/mL. A single lethal dose of aspirin in adults is not known with certainty but death may be expected at 30 g. For real or suspected overdose, contact a Poison Control Center immediately.
- Signs and Symptoms: In acute overdose, severe acid-base and electrolyte disturbances may occur and are complicated by hyperthermia and dehydration. Respiratory alkalosis occurs early while hyperventilation is present but is quickly followed by metabolic acidosis.
- Treatment: Treatment consists primarily of supporting vital functions, increasing salicylate elimination, and correcting the acid-base disturbance. Gastric emptying or lavage is recommended as soon as possible after ingestion, even if the patient has vomited spontaneously. After lavage or emesis, administer activated charcoal, as a slurry, if less than 3 hours have passed since ingestion.
The severity of aspirin intoxication is determined by measuring the blood salicylate level. Monitor acid-base status with serial blood gas and serum pH measurements. Maintain fluid and electrolyte balance.
In severe cases, hyperthermia and hypovolemia are the major immediate threats to life. Replace fluid intravenously and correct acidosis. Monitor plasma electrolytes and pH to promote alkaline diuresis of salicylate if renal function is normal. Glucose may be required to control hypoglycemia.
Hemodialysis and peritoneal dialysis can reduce the body's aspirin content. In patients with renal insufficiency or in cases of life-threatening intoxication, dialysis is usually required. Exchange transfusion may be indicated in infants and young children.
Pharmacodynamic
The dose-response relationship for Aspirin and immediate release (IR) aspirin towards COX-1 inhibition was characterized by examining the inhibition of serum TXB2 and urine 11 dehydro-TXB2 at 24 h following a single dose. Doses over the range of 20 mg to 325 mg for Aspirin and 5 mg to 81 mg for IR aspirin respectively were studied. Half-maximal inhibition of serum TXB2 and urine 11-dehydro-TXB2 occurred with doses of Aspirin (ID50) about 2-fold the dose of immediate release (IR) aspirin. Based on this relationship, the pharmacodynamic effect of Aspirin 162.5 mg is similar to that attained with IR aspirin 81 mg. The mean inhibition of serum TXB2 following Aspirin (82%) is lower when compared to IR aspirin 81 mg (93%) following the first dose. However, upon repeat administration, near maximal inhibition of serum TXB2 is achieved, similar to what is achieved following repeated daily doses of IR Aspirin.
Pharmacokinetics
- Absorption
Rapidly absorbed from the gastrointestinal tract; less reliable (rectal); absorbed through the skin. Partially hydrolyzed by esterases to salicylate during absorption in the GI tract. Bioavailability: 50-75% (immediate release). Time to peak plasma concentration: Approx 1-2 hours (non-enteric-coated); 3-4 hours (enteric-coated); Approx 2 hours (extended-release cap).
- Distribution
Widely and rapidly distributed into most body tissues and fluids. Crosses the placenta and enters breast milk. The volume of distribution: 170 mL/kg. Plasma protein binding: 80-90%.
- Metabolism and Excretion
Metabolised in the liver into salicyluric acid, salicyl phenolic glucuronide, salicylic acyl glucuronide, gentisic acid, and gentisuric acid. Undergoes first-pass metabolism.
Via urine (75% as salicylic acid, 10% as salicylic acid). Elimination half-life: 15-20 minutes.
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