Phenacetin Powder CAS:62-44-2

    What is Phenacetin?

    Chemical Information

    ●Chemical Name: N-(4-Ethoxyphenyl)acetamide

    ●Molecular Formula: C10H13NO2

    ●Molecular Weight: 179.22 g/mol

    ●Appearance: White crystalline powder

    ●Melting Point: 134-137°C

    ●Solubility: Moderately soluble in water, soluble in ethanol and acetone.

    Phenacetin is an organic compound categorized under acetanilides. Its mechanism of action lies in its capacity to inhibit the synthesis of prostaglandins, which are inflammatory mediators in the body, making it effective for pain relief and fever reduction. The compound has been metabolically linked to acetaminophen, which partly explains its therapeutic properties.

    1.Pharmacological Effects

    ●Phenacetin operates by blocking cyclooxygenase (COX) enzymes, preventing the formation of prostaglandins. This action reduces inflammation, pain, and fever.

    2.Metabolic Conversion

    ●After ingestion, Phenacetin is metabolized in the liver into paracetamol (acetaminophen), which is primarily responsible for its analgesic and antipyretic properties.

    3.Physical Properties

    ●It is a stable compound with a crystalline form, allowing it to be easily formulated into tablets or powders.

    4.Mild Sedative Effects

    ●In addition to its primary uses, Phenacetin may exert mild sedative effects, which can enhance its utility in managing discomfort.

    5.Historical Prevalence

    ●First introduced in 1887, Phenacetin became a key ingredient in many over-the-counter pain-relief formulations until the mid-20th century, when its risks were better understood.

    1. Pain Management

    Phenacetin was widely used to treat mild to moderate pain, including:

    ●Headaches

    ●Toothaches

    ●Musculoskeletal pain

    ●Menstrual discomfort

    Its efficacy in managing pain made it a cornerstone in analgesic formulations, often combined with other active ingredients like caffeine.

    2. Fever Reduction

    As an antipyretic, Phenacetin was effective in lowering elevated body temperature associated with infections and illnesses. It acted on the hypothalamic heat-regulating center, restoring normal body temperature.

    3. Combination Therapy

    Phenacetin was commonly included in combination drugs with substances like aspirin, codeine, or caffeine to enhance its efficacy. These combinations targeted multiple symptoms such as pain, inflammation, and fatigue.

    4. Historical Experimental Uses

    Although not common today, Phenacetin was occasionally explored in research settings for its effects on prostaglandin synthesis and its metabolic pathways.

    Despite its risks, Phenacetin offered several benefits that contributed to its historical popularity:

    1.Effective Pain Relief

    ●Its capacity to alleviate various types of pain made it a versatile analgesic for widespread use.

    2.Fever Control

    ●Phenacetin provided significant relief from fever, making it valuable during flu outbreaks and other febrile illnesses.

    3.Combination Compatibility

    ●Phenacetin was easily paired with other drugs, creating multifunctional medications that addressed a range of symptoms.

    4.Cost-Effectiveness

    ●Phenacetin was inexpensive to produce, which contributed to its accessibility during its peak usage period.

    The dosage of Phenacetin varied based on its formulation and intended application. These guidelines reflect historical practices before the compound's risks were fully understood.

    Standard Dosage

    ●Adults: 250–500 mg every 4–6 hours, not exceeding 3–4 grams daily.

    ●Children: Dosage was typically weight-based, with great caution due to the higher risk of adverse effects.

    Administration Guidelines

    ●Taken orally in tablet or powder form.

    ●Often combined with other compounds for synergistic effects.

    Safety Considerations

    ●Prolonged use or doses exceeding the recommended levels were linked to serious side effects, including nephrotoxicity and carcinogenicity.

    Phenacetin was not used in cycles like some modern pharmacological compounds. However, it was generally recommended for short-term use to manage acute symptoms.

    Short-Term Use

    ●Typically administered for 3–7 days for pain or fever.

    ●Extended use was discouraged due to cumulative toxicity risks.

    Chronic Use Risks

    ●Long-term use was associated with the development of phenacetin nephropathy, a condition characterized by kidney damage.

    ●Regular, prolonged consumption also raised concerns about bladder cancer.

    The pharmacokinetics of Phenacetin are influenced by its metabolism.

    Half-Life: Approximately 1–3 hours.

    ●Phenacetin is rapidly metabolized in the liver into active metabolites, such as acetaminophen.

    ●Due to this rapid metabolism, the effects of Phenacetin are short-lived, necessitating multiple doses throughout the day to maintain efficacy.

    Phenacetin is not a substance that necessitates traditional post-cycle therapy (PCT) as seen with anabolic steroids or hormonal treatments.  However, for individuals who used Phenacetin extensively, addressing potential organ damage was crucial.

    Key PCT Considerations

    1.Kidney Health Monitoring

    ●Regular renal function tests to detect early signs of nephropathy or kidney impairment.

    2.Hydration

    ●Adequate water intake to support kidney filtration and reduce the burden on renal tissues.

    3.Liver Support

    ●Supplements like N-acetylcysteine (NAC) or milk thistle may support liver detoxification, particularly given Phenacetin's metabolism.

    4.Cancer Screening

    ●Long-term Phenacetin users may require bladder and kidney cancer screenings due to its carcinogenic potential.

    5.General Health Optimization

    ●A balanced diet, regular exercise, and avoiding other nephrotoxic substances are crucial for recovery.

    The risks associated with Phenacetin are well-documented and were the primary reason for its global discontinuation.

    1. Kidney Damage

    Prolonged use can lead to renal papillary necrosis, a form of kidney damage that can progress to end-stage renal disease.

    2. Carcinogenicity

    Phenacetin has been classified as a potential carcinogen by health authorities, with links to bladder and kidney cancers.

    3. Liver Toxicity

    Phenacetin's metabolism into acetaminophen can stress the liver, particularly at high doses.

    4. Blood Disorders

    Chronic use has been associated with methemoglobinemia, a condition where the blood's ability to carry oxygen is impaired.

    5. Hypersensitivity Reactions

    Some individuals may experience allergic reactions, including rash, itching, or swelling.

    Phenacetin is no longer widely used or recommended in modern medicine due to its risks. Safer alternatives, such as acetaminophen and nonsteroidal anti-inflammatory drugs (NSAIDs), offer similar benefits with fewer side effects. Nevertheless, Phenacetin remains a compound of historical and research interest.

Trade names	Clomiphene, Clomifene, Clomid
CAS	62-44-2
Molar mass	179.216
MF	C10H13NO2
Purity	Above 98%
Apprarance	White crystalline powder

 

 

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    Phenacetin played a pivotal role in the evolution of pain and fever management but has been largely replaced due to its safety profile. Understanding its properties, applications, and risks provides valuable insights into the development of modern analgesics. While it holds historical significance, Phenacetin serves as a reminder of the importance of safety and efficacy in pharmaceutical advancements.

 

 

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