Phloroglucinol Injection Introduction

1. General Information

Phloroglucinol Injection is a non - anticholinergic spasmolytic medication. The active ingredient, phloroglucinol, is a trihydroxybenzene derivative. It is formulated as a sterile solution for intravenous, intramuscular, or subcutaneous administration, typically available in vials with concentrations such as 40 mg/4 mL. This injection is widely used in clinical practice to relieve smooth muscle spasm - related pain, offering a targeted approach to symptom management without the typical side - effects associated with anticholinergic drugs.

2. Mechanism of Action

Phloroglucinol exerts its spasmolytic effect by directly acting on smooth muscle cells. It inhibits the activity of myosin light chain kinase, an enzyme crucial for the contraction of smooth muscles. By blocking this enzyme, phloroglucinol reduces the phosphorylation of myosin light chains, preventing the interaction between actin and myosin filaments. As a result, the smooth muscles relax, effectively relieving spasm. Unlike anticholinergic drugs, it does not act on cholinergic receptors, minimizing the occurrence of adverse effects such as dry mouth, blurred vision, and urinary retention that are commonly associated with anticholinergic agents.

3. Indications

3.1 Gastrointestinal Spasms

It is commonly used to treat spasms in the gastrointestinal tract, including those caused by gastritis, peptic ulcer, irritable bowel syndrome, and intestinal colic. By relaxing the smooth muscles of the stomach and intestines, phloroglucinol relieves abdominal pain, bloating, and discomfort associated with these conditions, improving patients' quality of life.

3.2 Biliary and Pancreatic Spasms

In cases of biliary colic due to gallstones or inflammation of the biliary tract, as well as pancreatic spasm resulting from pancreatitis, phloroglucinol injection can provide significant pain relief. It helps to relax the smooth muscles of the bile ducts and pancreatic ducts, reducing the pressure and pain caused by spasms.

3.3 Urogenital Spasms

Phloroglucinol is also effective in relieving spasms in the urogenital system. It can be used to treat renal colic caused by kidney stones, as well as spasms during dysmenorrhea (menstrual pain) and other gynecological conditions associated with uterine smooth muscle spasm.

4. Dosage and Administration

4.1 Adult Dosage

For adults, the usual dose is 40 - 80 mg administered either intramuscularly, subcutaneously, or intravenously. The injection can be repeated 2 - 3 times a day if necessary, with a maximum daily dose not exceeding 320 mg. When given intravenously, it should be injected slowly over 2 - 4 minutes to avoid adverse reactions.

4.2 Pediatric Dosage

In pediatric patients, the dosage is calculated based on body weight, typically at a rate of 1 - 2 mg/kg per dose. Similar to adult use, the injection can be administered via intramuscular, subcutaneous, or intravenous routes, and the frequency of administration depends on the patient's response and the severity of the condition. However, careful monitoring is required, as children may be more sensitive to the drug's effects.

5. Precautions and Contraindications

5.1 Contraindications

Phloroglucinol Injection is contraindicated in patients with a known hypersensitivity to phloroglucinol or any of the components of the formulation. It should not be used in patients with severe hepatic or renal impairment without careful consideration, as the drug's metabolism and excretion may be affected, potentially leading to drug accumulation and increased risk of adverse effects.

5.2 Drug Interactions

There is limited information regarding significant drug interactions with phloroglucinol. However, caution should be exercised when using it in combination with other central nervous system - depressant drugs, as it may potentially enhance their sedative effects. Additionally, concurrent use with other medications that affect smooth muscle function may require close monitoring to avoid unexpected interactions.

5.3 Special Populations

In elderly patients, the dosage may need to be adjusted with caution due to potential age - related changes in organ function. Pregnant and breastfeeding women should use phloroglucinol injection only when the potential benefit justifies the potential risk, as the safety of the drug during these periods has not been fully established.

6. Adverse Reactions

The most common adverse reactions associated with Phloroglucinol Injection are mild and include headache, dizziness, and allergic reactions such as skin rashes. In rare cases, more severe allergic reactions, including anaphylaxis, may occur. Some patients may also experience nausea, vomiting, or transient changes in blood pressure or heart rate. If any of these adverse reactions occur, appropriate medical measures should be taken, including reducing the dose or discontinuing the drug if necessary.

In conclusion, Phloroglucinol Injection is a valuable therapeutic option for the treatment of smooth muscle spasm - related pain across various systems. When used appropriately, with careful consideration of dosage, potential drug interactions, and patient - specific factors, it can effectively relieve pain while minimizing the risk of adverse reactions.