Description

Phloroglucinol is an organic compound that acts as an antispasmodic drug. It’s often used in combination with its derivative, trimethylphloroglucinol, to enhance its muscle-relaxing effects. This combination, sometimes referred to as “hydrated phloroglucinol + trimethylphloroglucinol,” is commonly formulated into suppositories, tablets, and solutions for injection.

Indications

This drug combination is used for the symptomatic treatment of pain caused by spasms of smooth muscles in various organs. Indications include:

• Digestive disorders: Pain associated with functional disorders of the gastrointestinal and biliary tracts.

• Urinary tract spasms: Acute painful episodes like renal colic.

• Gynecological conditions: Painful spasms of the uterus.

• Pregnancy contractions: As an adjuvant therapy, along with rest.

Mechanism of Action

Phloroglucinol and trimethylphloroglucinol work by directly relaxing smooth muscles, particularly in the digestive and urinary systems. Their mechanism of action is non-anticholinergic, meaning they don’t produce side effects like dry mouth or drowsiness.

The primary mechanism is the inhibition of phosphodiesterase enzymes. This inhibition leads to an increase in intracellular levels of cyclic AMP (cAMP) and cyclic GMP (cGMP), which are secondary messengers crucial for cellular signaling. Elevated levels of these molecules cause a reduction in the influx of calcium ions into the smooth muscle cells. Since calcium is essential for muscle contraction, its reduced availability leads to muscle relaxation and relief from spasms.

Additionally, the combination has been shown to:

• Directly inhibit voltage-dependent calcium channels, further decreasing the calcium concentration inside the cells.

• Inhibit the catechol-O-methyltransferase (COMT) enzyme, which breaks down catecholamines in smooth muscle tissue. By inhibiting this enzyme, the combination increases sympathetic tone, which also contributes to an antispasmodic effect.