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Phloroglucinol, Discovery, Action, Uses side effects and Brands

Phloroglucinol, Discovery, Action, Uses side effects and Brands

  • May 9, 2024
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Introduction

Phloroglucinol is a pharmaceutical agent with antispasmodic properties also known as 1,3,5-trihydroxybenzene, is a naturally occurring organic compound belonging to the class of phenolic compounds. It is widely recognized for its pharmacological properties, particularly its role as an antispasmodic agent. It is found in various plant species, including certain fruits, vegetables, and medicinal herbs.

Phloroglucinol is a pharmaceutical agent with antispasmodic properties primarily used to alleviate gastrointestinal symptoms associated with smooth muscle spasms. It belongs to a class of compounds known as phenolic compounds and is chemically described as 1,3,5-trihydroxybenzene. Phloroglucinol is available in various formulations, including oral tablets and suppositories.

Discovery of phloroglucinol

The discovery of phloroglucinol traces back to the mid-19th century when it was first isolated from natural sources by the French chemist Auguste Laurent. Laurent obtained It through the decomposition of phlorizin, a compound found in the bark of certain apple trees. This early isolation laid the groundwork for further investigation into the properties and applications of phloroglucinol.

Later, in 1872, the German chemist Emil Fischer synthesized phloroglucinol through chemical processes, advancing its study and enabling its widespread availability for scientific research and industrial applications. Fischer’s synthesis of phloroglucinol contributed significantly to the understanding of its chemical structure and paved the way for its utilization in various fields, including chemistry, medicine, and industry.

Since its discovery and synthesis, phloroglucinol has attracted scientific interest due to its unique chemical properties and pharmacological effects. Ongoing research continues to explore its diverse applications, ranging from its role as an antispasmodic agent in medicine to its use as a chemical building block in organic synthesis.

The discovery of phloroglucinol represents a significant milestone in the history of organic chemistry, demonstrating the importance of natural product isolation and chemical synthesis in expanding our understanding of chemical compounds and their potential applications.

Mechanism of Action

Phloroglucinol exerts its pharmacological effects primarily by acting as an antispasmodic agent. Its mechanism of action involves several pathways:

Calcium Channel Modulation

Phloroglucinol interferes with calcium ion channels in smooth muscle cells. Calcium ions play a crucial role in muscle contraction. By inhibiting calcium influx, phloroglucinol induces muscle relaxation, thereby alleviating spasms and cramps.

Antioxidant Activity

Phloroglucinol exhibits antioxidant properties, scavenging free radicals and protecting cells from oxidative damage. This antioxidant activity may contribute to its therapeutic effects, particularly in conditions associated with inflammation and oxidative stress.

Neurotransmitter Modulation

Phloroglucinol may modulate the release or activity of certain neurotransmitters involved in smooth muscle contraction, such as acetylcholine. By influencing neurotransmitter signaling, it helps regulate muscle tone and reduce spasm-related symptoms.

Phloroglucinol Forms

Phloroglucinol is commonly available in various pharmaceutical forms to cater to different patient needs and routes of administration. Some of the common forms include:

Oral Tablets and Capsules

Phloroglucinol is frequently formulated into oral tablets or capsules for convenient administration. These solid dosage forms provide precise dosing and are typically taken with water.

They are suitable for systemic absorption and are commonly used in the treatment of gastrointestinal and urinary tract disorders.

Syrups and Suspensions

It is formulated into syrups or suspensions for oral administration, particularly for pediatric or geriatric patients who may have difficulty swallowing tablets or capsules.

These liquid formulations allow for flexible dosing and are often flavored for improved palatability.

Injectable Solutions

Injectable formulations of phloroglucinol are available for intravenous (IV) or intramuscular (IM) administration in clinical settings.

These solutions provide rapid onset of action and are suitable for patients who are unable to take oral medications or require more immediate symptom relief.

Medical uses

Phloroglucinol, its antispasmodic properties, finds diverse medical applications in the management of conditions characterized by smooth muscle spasms. Some common medical uses include:

Gastrointestinal Disorders

Phloroglucinol is utilized in the treatment of gastrointestinal disorders marked by spasms and cramps, such as:
Irritable bowel syndrome (IBS): Phloroglucinol helps alleviate abdominal pain and discomfort associated with IBS by relaxing smooth muscle in the gastrointestinal tract.

Functional gastrointestinal disorders

Conditions like functional dyspepsia and functional constipation may benefit from phloroglucinol therapy to relieve symptoms of abdominal pain and discomfort.

Urinary Tract Disorders

Phloroglucinol is effective in managing urinary tract disorders characterized by spasms and pain, including:
Kidney stones: Phloroglucinol helps relax smooth muscle in the urinary tract, relieving spasms and pain associated with the passage of kidney stones.

Urinary tract infections (UTIs)

Phloroglucinol can alleviate urinary urgency, frequency, and discomfort caused by UTIs by reducing spasms in the bladder and urethra.

Gynecological Conditions

In gynecology, phloroglucinol is used to manage conditions involving uterine spasms and associated pain, such as:

  • Dysmenorrhea (painful menstruation): It helps alleviate menstrual cramps by relaxing the uterine muscles, and reducing pain and discomfort during menstruation.
  • Endometriosis: Phloroglucinol is a part of the treatment regimen for endometriosis, a condition characterized by the growth of endometrial tissue outside the uterus, to relieve pelvic pain and spasms.

Analgesic Therapy

Phloroglucinol’s ability to relieve smooth muscle spasms also contributes to its analgesic (pain-relieving) properties. Reducing muscle tension and spasms.

Dosage guidelines

The dosage guidelines for some common medical uses of phloroglucinol:

For Gastrointestinal Disorders

Adults: The typical oral dosage for adults is 80 mg to 160 mg taken orally, usually 2 to 3 times per day. However, dosages vary based on the severity of symptoms and individual response.
Pediatric: Dosage for children should be determined by a healthcare provider based on weight and age.

For Urinary Tract Disorders

Adults: The recommended oral dosage for adults is similar to that for gastrointestinal disorders, typically ranging from 80 mg to 160 mg taken orally 2 to 3 times daily.
Pediatric: Dosage for children should be determined by a healthcare professional based on weight and age.

For Gynecological Conditions

Adults: The oral dosage for managing uterine spasms and associated pain varies but is typically in the range of 80 mg to 160 mg taken orally 2 to 3 times daily.
Pediatric: Dosage adjustments may be necessary for pediatric patients and should be determined by a healthcare provider.

Side Effects

phloroglucinol is generally considered safe and well-tolerated, like any medication, it causes side effects in some individuals. Common side effects associated with phloroglucinol use include:

Gastrointestinal Disturbances

  • Nausea
  • Vomiting
  • Diarrhea
  • Abdominal discomfort or pain.

Allergic Reactions:

  • Skin rash or itching
  • Swelling of the face, lips, tongue, or throat (angioedema)
  • Difficulty breathing.

Central Nervous System Effects

  • Headache
  • Dizziness
  • Fatigue.

Other Possible Side Effects

  • Hypotension (low blood pressure)
  • Flushing
  • Urinary retention (rare)
  • Hepatotoxicity (rare).

Phloroglucinol Brands in Pakistan

In Pakistan, phloroglucinol is available under various brand names, and the availability of specific brands can vary over time and by region. Some common brand names of phloroglucinol formulations in Pakistan include:

  1. Furosinol.  Manufacturer: Century Pharmaceuticals (Pvt) Ltd.
    Retail Price: 217.36 PKR.
  2. Spadix: 
    Manufacturer: Tabros Pharma
    Retail Price: 198.00 PKR
  3. Spasfon
    Manufacturer: Himont Pharmaceuticals (Pvt) Ltd.
    Retail Price: 425.57 PKR
  4. Spasrid
    Manufacturer: Barrett Hodgson Pakistan (Pvt) Ltd.
    Retail Price.221.00 PKR.
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