acetaminophen and phenyltoloxamine

Action and Spectrum

Actions and spectrum: 

acetaminophen and phenyltoloxamine is a combination medication that has analgesic (pain-relieving) and antipyretic (fever-reducing) effects. acetaminophen works by inhibiting the synthesis of prostaglandins in the central nervous system, which reduces pain and fever.

phenyltoloxamine is an antihistamine with sedative properties that can also help to relieve pain and reduce inflammation. The combination of these two drugs provides greater pain relief than either drug used alone. The spectrum of action for this medication is limited to relief of mild to moderate pain and fever. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Angioedema 

Sedation 

Urticaria 

Agranulocytosis 

Neutropenia 

Thrombocytopenia 

Hepatotoxicity 

Anaphylactoid reaction 

Laryngeal edema 

Pruritic maculopapular rash 

Xerostomia 

Leukopenia 

Pancytopenia 

Thrombocytopenic purpura 

Blurred vision 

Black Box Warning

Black Box Warning: 

There is no black box warning for the combination of acetaminophen and phenyltoloxamine 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity or allergy to acetaminophen, phenyltoloxamine or any of the inactive ingredients in the formulation 
• Severe liver impairment or severe active liver disease 
• Severe renal impairment or severe active kidney disease 
• Glaucoma 
• Prostatic hypertrophy or bladder neck obstruction 
• Hypertension or severe cardiovascular disease 
• Severe respiratory depression or severe obstructive pulmonary disease 
• Known or suspected gastrointestinal obstruction, including paralytic ileus 
• Concurrent use of monoamine oxidase inhibitors (MAOIs) or within 14 days of stopping MAOI therapy

Caution: 

• Liver disease: acetaminophen can cause liver damage in high doses, so it should be used with caution in individuals with liver disease. 
• Renal impairment: acetaminophen is primarily metabolized by the liver, but a small percentage of it is metabolized by the kidneys. Therefore, individuals with renal impairment should use acetaminophen with caution. 
• Asthma: phenyltoloxamine can cause bronchospasms in individuals with asthma. It should be used with caution in individuals with this condition. 
• Prostate enlargement: phenyltoloxamine can cause urinary retention in individuals with prostate enlargement. 
• Pregnancy and breastfeeding: acetaminophen is considered safe to use during pregnancy and breastfeeding. However, phenyltoloxamine is not recommended during pregnancy or breastfeeding due to a lack of safety data.

Comorbidities: 

• Liver disease: acetaminophen can cause liver damage, especially if taken in high doses or for a long time. Patients with liver disease, including cirrhosis, should avoid using this medication or take it under the supervision of a healthcare provider. 
• Kidney disease: phenyltoloxamine is primarily eliminated through the kidneys. Patients with kidney disease may require a dose adjustment or close monitoring while taking this medication. 
• Asthma: phenyltoloxamine can cause bronchospasm and worsen asthma symptoms. Patients with asthma should avoid taking this medication. 
• Glaucoma: phenyltoloxamine can increase the intraocular pressure and worsen glaucoma symptoms. Patients with glaucoma should use this medication with caution and under the supervision of a healthcare provider. 
• Prostate enlargement: phenyltoloxamine can worsen symptoms of urinary retention in men with prostate enlargement.  
• Gastrointestinal problems: acetaminophen can irritate the stomach lining and cause gastrointestinal bleeding. Patients with a history of stomach ulcers, gastrointestinal bleeding, or inflammatory bowel disease should use this medication with caution. 
• Cardiovascular disease: phenyltoloxamine can cause changes in heart rate and rhythm, which can be dangerous in patients with cardiovascular disease. Patients with heart disease or a history of arrhythmias should use this medication with caution. 

Pregnancy / Lactation

Pregnancy consideration: N/A 

Lactation: N/A  

Pregnancy category: 

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester. 
• Category B: There is no evidence of risk to the fetus found in animal reproduction studies and there are not enough studies on pregnant women. 
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for an effect in humans, care must be taken for potential risks in pregnant women. 
• Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite potential risks may be used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh risks over benefits These category drugs should be prohibited for pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

acetaminophen is an antipyretic and analgesic medication that works by inhibiting the production of prostaglandins in the brain, which are involved in pain and fever. phenyltoloxamine, on the other hand, is a first-generation antihistamine that works by blocking the effects of histamine in the body, which is responsible for causing allergic symptoms such as sneezing, itching, and runny nose. 

When taken together, acetaminophen and phenyltoloxamine have a synergistic effect, providing both pain relief and relief from allergy symptoms. acetaminophen is metabolized in the liver, and its metabolites are excreted in the urine. phenyltoloxamine is metabolized in the liver and excreted in the urine as well.  

Pharmacodynamics: 

acetaminophen is a non-opioid analgesic that reduces pain by inhibiting the synthesis of prostaglandins, which are involved in the process of inflammation and pain. It is also thought to act centrally in the brain to increase the pain threshold. phenyltoloxamine is a first-generation antihistamine that blocks histamine receptors in the body, which can reduce inflammation and pain. 

The combination of acetaminophen and phenyltoloxamine provides a dual mechanism of action for pain relief and can be more effective than either medication alone. Additionally, the sedative effects of phenyltoloxamine can help with sleep disturbances that may be associated with pain.  

Pharmacokinetics: 

Absorption 

acetaminophen is well absorbed from the gastrointestinal tract, with peak plasma concentrations occurring within 30-60 minutes of oral administration. phenyltoloxamine is also readily absorbed from the gastrointestinal tract, but the onset of action may be delayed up to 2 hours after oral administration. 

Distribution 

Both acetaminophen and phenyltoloxamine are distributed throughout the body, and they readily cross the blood-brain barrier. acetaminophen is approximately 25% bound to plasma proteins, while phenyltoloxamine is highly protein-bound. 

Metabolism 

acetaminophen is primarily metabolized by the liver via glucuronidation and sulfation. A small portion is metabolized via the cytochrome P450 enzyme system to a toxic intermediate metabolite, which is normally detoxified by glutathione. However, in cases of acetaminophen overdose, this detoxification pathway can become overwhelmed, leading to liver damage. phenyltoloxamine is metabolized by the liver via oxidation and conjugation. 

Elimination and excretion 

Both acetaminophen and phenyltoloxamine are excreted in the urine. acetaminophen is primarily excreted as glucuronide and sulfate conjugates, while a small portion is excreted unchanged. The elimination half-life of acetaminophen is 2-3 hours. phenyltoloxamine is primarily excreted as metabolites in the urine, with an elimination half-life of approximately 6 hours. 

Adminstartion

Administration: 

acetaminophen and phenyltoloxamine are usually taken by mouth in the form of tablets or capsules. The usual adult dose of acetaminophen is 325-650 mg every 4-6 hours, while the usual adult dose of phenyltoloxamine is 20-40 mg every 4-6 hours.

The medication can be taken with or without food. It is important to follow the dosing instructions provided by the healthcare provider and not exceed the recommended dose. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: acetaminophen and phenyltoloxamine 

Pronounced: uh-SEE-tuh-MIN-oh-fen and fen-uhl-toh-LOX-uh-meen  

Why do we use acetaminophen and phenyltoloxamine? 

acetaminophen and phenyltoloxamine combination is used to relieve pain and discomfort associated with conditions such as tension headache, migraine, toothache, menstrual cramps, and muscle aches. acetaminophen is an antipyretic and analgesic while phenyltoloxamine is an antihistamine that helps to relieve pain and inflammation.