Actions of Acetaminophen Elixir in details
Pharmacology: Pain is a very common experience and analgesic drugs such as paracetamol plays an important role in providing general pain relief for both acute and chronic pain. Paracetamol is widely recommended as the initial drug of choice for the treatment of mild to moderate musculoskeletal pain and symptomatic osteoarthritis as it is regarded as having a more acceptable safety profile in chronic use than nonsteroidal anti-inflammatory drugs (NSAIDs).
Acetaminophen Elixir provides analgesic action via its inhibition activity on the central prostaglandin synthetase and its antipyretic action is thought to be due to selective inhibition of prostaglandin synthesis in the central nervous system (CNS).
Acetaminophen Elixir is readily absorbed from the upper small intestine, has absolute oral bioavailability (70-90%) and is extensively metabolized in the liver.
Pharmacokinetics: Acetaminophen Elixir formulation consists of a bilayer tablet containing 665 mg of paracetamol: One layer containing an immediate-release (IR) formulation and providing 31% of the total dose and a 2nd layer containing a sustained release (SR) formulation that provides the remaining 69% of the total dose.
Pharmacokinetics of Acetaminophen Elixir have been investigated in 2 pivotal biostudies. In the First study, Acetaminophen Elixir and Panadol tablets were compared in fed and fasted volunteers. Both were bioequivalent with respect to dose-corrected AUC(0-t) and AUC(0-inf) in both fed and fasted states. The bioavailability of paracetamol from Acetaminophen Elixir is not affected by food thus indicating that the formulation can be taken with or without food.
In the Second study, where Acetaminophen Elixir was again compared with Panadol; Acetaminophen Elixir showed a clear pattern of controlled release of paracetamol, and the formulations were bioequivalent based on the comparison of AUCs for the final 24 hours of the 48-hour dosing period. This shows that there is no additional accumulation of paracetamol from the Acetaminophen Elixir formulation. Besides that, steadier concentrations of paracetamol were achieved with Acetaminophen Elixir. Thus, Acetaminophen Elixir may be particularly appropriate for patients who require repeat doses as it maintains a continuous therapeutic effect when taken every 8 hours (2 x 665 mg tablets per dose).
How should I take Acetaminophen Elixir?
Use Acetaminophen Elixir exactly as directed on the label, or as prescribed by your doctor. Do not use in larger or smaller amounts or for longer than recommended.
Do not take more of this medication than is recommended. An overdose of Acetaminophen Elixir can damage your liver or cause death.
Measure liquid medicine with a special dose-measuring spoon or medicine cup, not with a regular table spoon. If you do not have a dose-measuring device, ask your pharmacist for one.
If you are treating a child, use a pediatric form of Acetaminophen Elixir. Use only the special dose-measuring dropper or oral syringe that comes with the specific pediatric form you are using. Carefully follow the dosing directions on the medicine label.
Acetaminophen Elixir made for infants is available in two different dose concentrations, and each concentration comes with its own medicine dropper or oral syringe. These dosing devices are not equal between the different concentrations. Using the wrong device may cause you to give your child an overdose of Acetaminophen Elixir. Never mix and match dosing devices between infant formulations of Acetaminophen Elixir.
You may need to shake the liquid before each use. Follow the directions on the medicine label.
The chewable tablet must be chewed thoroughly before you swallow it.
Make sure your hands are dry when handling the Acetaminophen Elixir disintegrating tablet. Place the tablet on your tongue. It will begin to dissolve right away. Do not swallow the tablet whole. Allow it to dissolve in your mouth without chewing.
To use the Acetaminophen Elixir effervescent granules, dissolve one packet of the granules in at least 4 ounces of water. Stir this mixture and drink all of it right away. To make sure you get the entire dose, add a little more water to the same glass, swirl gently and drink right away.
Stop taking Acetaminophen Elixir and call your doctor if:
-
you still have a fever after 3 days of use;
-
you still have pain after 7 days of use (or 5 days if treating a child);
-
you have a skin rash, ongoing headache, or any redness or swelling; or
-
if your symptoms get worse, or if you have any new symptoms.
This medication can cause unusual results with certain lab tests for glucose (sugar) in the urine. Tell any doctor who treats you that you are using Acetaminophen Elixir.
Store at room temperature away from heat and moisture.
Acetaminophen Elixir administration
Take exactly as directed on the label, or as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended.
Do not take more of this medication than is recommended. An overdose of Acetaminophen Elixir can damage your liver or cause death.
Measure liquid medicine with a special dose-measuring spoon or medicine cup, not with a regular table spoon. If you do not have a dose-measuring device, ask your pharmacist for one.
If you are treating a child, use a pediatric form of Acetaminophen Elixir. Use only the special dose-measuring dropper or oral syringe that comes with the specific pediatric form you are using. Carefully follow the dosing directions on the medicine label.
Acetaminophen Elixir made for infants is available in two different dose concentrations, and each concentration comes with its own medicine dropper or oral syringe. These dosing devices are not equal between the different concentrations. Using the wrong device may cause you to give your child an overdose of Acetaminophen Elixir. Never mix and match dosing devices between infant formulations of Acetaminophen Elixir.
You may need to shake the liquid before each use. Follow the directions on the medicine label.
The chewable tablet must be chewed thoroughly before you swallow it.
Make sure your hands are dry when handling the Acetaminophen Elixir disintegrating tablet. Place the tablet on your tongue. It will begin to dissolve right away. Do not swallow the tablet whole. Allow it to dissolve in your mouth without chewing.
To use the Acetaminophen Elixir effervescent granules, dissolve one packet of the granules in at least 4 ounces of water. Stir this mixture and drink all of it right away. To make sure you get the entire dose, add a little more water to the same glass, swirl gently and drink right away.
Stop taking Acetaminophen Elixir and call your doctor if:
- you still have a fever after 3 days of use;
- you still have pain after 7 days of use (or 5 days if treating a child);
- you have a skin rash, ongoing headache, or any redness or swelling; or
- if your symptoms get worse, or if you have any new symptoms.
This medication can cause unusual results with certain lab tests for glucose (sugar) in the urine. Tell any doctor who treats you that you are using Acetaminophen Elixir.
Store at room temperature away from heat and moisture.
Acetaminophen Elixir pharmacology
Mechanism of Action
The precise mechanism of the analgesic and antipyretic properties of Acetaminophen Elixir is not established but is thought to primarily involve central actions.
Pharmacodynamics
Acetaminophen Elixir has been shown to have analgesic and antipyretic activities in animal and human studies.
Single doses of Acetaminophen Elixir up to 3,000 mg and repeated doses of 1,000 mg every 6 hours for 48 hours have not been shown to cause a significant effect on platelet aggregation. Acetaminophen Elixir does not have any immediate or delayed effects on small-vessel hemostasis. Clinical studies of both healthy subjects and patients with hemophilia showed no significant changes in bleeding time after receiving multiple doses of oral Acetaminophen Elixir.
Pharmacokinetics
Distribution
The pharmacokinetics of Acetaminophen Elixir have been studied in patients and healthy subjects up to 60 years old. The pharmacokinetic profile of Acetaminophen Elixir has been demonstrated to be dose proportional in adults following administration of single doses of 500, 650, and 1,000 mg.
The maximum concentration (Cmax) occurs at the end of the 15 minute intravenous infusion of Acetaminophen Elixir. Compared to the same dose of oral Acetaminophen Elixir, the Cmax following administration of Acetaminophen Elixir is up to 70% higher, while overall exposure (area under the concentration time curve [AUC]) is very similar.
Pharmacokinetic parameters of Acetaminophen Elixir (AUC, Cmax, terminal elimination half-life [T½], systemic clearance [CL], and volume of distribution at steady state [Vss]) following administration of a single intravenous dose of 15 mg/kg in children and adolescents and 1,000 mg in adults are summarized in Table 5.
| Subpopulations | Mean (SD) | ||||
| AUC 0-6h (mcg× h/mL) | C max (mcg/mL) | T½ (h) | CL (L/h/kg) | Vss (L/kg) | |
| Children | 38 (8) | 29 (7) | 3.0 (1.5) | 0.34 (0.10) | 1.2 (0.3) |
| Adolescents | 41 (7) | 31 (9) | 2.9 (0.7) | 0.29 (0.08) | 1.1 (0.3) |
| Adults | 43 (11) | 28 (21) | 2.4 (0.6) | 0.27 (0.08) | 0.8 (0.2) |
The concentrations of Acetaminophen Elixir observed in neonates greater than 32 weeks gestational age at birth treated with 12.5 mg/kg dose are similar to infants, children and adolescents treated with a 15 mg/kg dose, and similar to adults treated with a 1,000 mg dose.
At therapeutic levels, binding of Acetaminophen Elixir to plasma proteins is low (ranging from 10% to 25%). Acetaminophen Elixir appears to be widely distributed throughout most body tissues except fat.
Metabolism and Excretion
Acetaminophen Elixir is primarily metabolized in the liver by first-order kinetics and involves three principal separate pathways: Conjugation with glucuronide, conjugation with sulfate, and oxidation via the cytochrome P450 enzyme pathway, primarily CYP2E1, to form a reactive intermediate metabolite (N-acetyl-p-benzoquinone imine or NAPQI). With therapeutic doses, NAPQI undergoes rapid conjugation with glutathione and is then further metabolized to form cysteine and mercapturic acid conjugates.
Acetaminophen Elixir metabolites are mainly excreted in the urine. Less than 5% is excreted in the urine as unconjugated (free) Acetaminophen Elixir and more than 90% of the administered dose is excreted within 24 hours.
References
- DailyMed. "ACETAMINOPHEN; ASPIRIN; CAFFEINE: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
- NCIt. "Acetaminophen: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).
- EPA DSStox. "Acetaminophen: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).
Reviews
The results of a survey conducted on ndrugs.com for Acetaminophen Elixir are given in detail below. The results of the survey conducted are based on the impressions and views of the website users and consumers taking Acetaminophen Elixir. We implore you to kindly base your medical condition or therapeutic choices on the result or test conducted by a physician or licensed medical practitioners.User reports
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Information checked by Dr. Sachin Kumar, MD Pharmacology
