| Drug ID: | D002 |
| Drug Name: | Acetaminophen |
| Synonyms: |
4-(Acetylamino)phenol; 4-acetamidophenol; 4'-hydroxyacetanilide; Acenol; Acetaminophen; APAP; N-acetyl-p-aminophenol; p-acetamidophenol; p-acetaminophenol; p-Acetylaminophenol; p-hydroxy-acetanilid; p-hydroxyacetanilide; p-hydroxyphenolacetamide
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| Type: | Chemical drug |
| DrugBank ID: |
DB00316
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| DrugBank Description: |
Acetaminophen (paracetamol), also commonly known as _Tylenol_, is the most commonly taken analgesic worldwide and is recommended as first-line therapy in pain conditions by the World Health Organization (WHO). It is also used for its antipyretic effects, helping to reduce fever. This drug was initially approved by the U.S. FDA in 1951 and is available in a variety of forms including syrup form, regular tablets, effervescent tablets, injection, suppository, and other forms.
Acetaminophen is often found combined with other drugs in more than 600 over the counter (OTC) allergy medications, cold medications, sleep medications, pain relievers, and other products. Confusion about dosing of this drug may be caused by the availability of different formulas, strengths, and dosage instructions for children of different ages. Due to the possibility of fatal overdose and liver failure associated with the incorrect use of acetaminophen, it is important to follow current and available national and manufacturer dosing guidelines while this drug is taken or prescribed.
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| PubChem ID: |
1983
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| CasNo: |
103-90-2
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| Repositioning for NAFLD: |
Yes
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| SMILES: |
N(C(=O)C)c1ccc(cc1)O
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| Structure: |
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| InChiKey: |
RZVAJINKPMORJF-UHFFFAOYSA-N
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| Molecular Weight: |
151.165
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| DrugBank Targets: |
Prostaglandin E synthase 3 inhibitor; Prostaglandin G/H synthase 2 inhibitor; Prostaglandin G/H synthase 1 inhibitor; Transient receptor potential cation channel subfamily V member 1 activator
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| DrugBank MoA: |
According to its FDA labeling, acetaminophen's exact mechanism of action has not been fully established - despite this, it is often categorized alongside NSAIDs (nonsteroidal anti-inflammatory drugs) due to its ability to inhibit the cyclooxygenase (COX) pathways. It is thought to exert central actions which ultimately lead to the alleviation of pain symptoms.
One theory is that acetaminophen increases the pain threshold by inhibiting two isoforms of cyclooxygenase, COX-1 and COX-2, which are involved in prostaglandin (PG) synthesis. Prostaglandins are responsible for eliciting pain sensations. Acetaminophen does not inhibit cyclooxygenase in peripheral tissues and, therefore, has no peripheral anti-inflammatory effects. Though acetylsalicylic acid (aspirin) is an irreversible inhibitor of COX and directly blocks the active site of this enzyme, studies have shown that acetaminophen (paracetamol) blocks COX indirectly. Studies also suggest that acetaminophen selectively blocks a variant type of the COX enzyme that is unique from the known variants COX-1 and COX-2. This enzyme has been referred to as _COX-3_. The antipyretic actions of acetaminophen are likely attributed to direct action on heat-regulating centers in the brain, resulting in peripheral vasodilation, sweating, and loss of body heat. The exact mechanism of action of this drug is not fully understood at this time, but future research may contribute to deeper knowledge.
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| DrugBank Pharmacology: |
Animal and clinical studies have determined that acetaminophen has both antipyretic and analgesic effects. This drug has been shown to lack anti-inflammatory effects. As opposed to the _salicylate_ drug class, acetaminophen does not disrupt tubular secretion of uric acid and does not affect acid-base balance if taken at the recommended doses. Acetaminophen does not disrupt hemostasis and does not have inhibitory activities against platelet aggregation. Allergic reactions are rare occurrences following acetaminophen use.
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| DrugBank Indication: |
In general, acetaminophen is used for the treatment of mild to moderate pain and reduction of fever. It is available over the counter in various forms, the most common being oral forms.
Acetaminophen _injection_ is indicated for the management of mild to moderate pain, the management of moderate to severe pain with adjunctive opioid analgesics, and the reduction of fever.
Because of its low risk of causing allergic reactions, this drug can be administered in patients who are intolerant to salicylates and those with allergic tendencies, including bronchial asthmatics. Specific dosing guidelines should be followed when administering acetaminophen to children.
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| Targets: |
PTGES3 inhibitor; TRPV1 activator
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| Therapeutic Category: |
Antipyretic drug; non-narcotic analgesic
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| Clinical Trial Progress: |
Clinical trial withdrawn (NCT02194894: (No patients enrolled)
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| Latest Progress: |
Under clinical trials
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