GYNOSPAN

Indications

• Abdominal pain due to spasm
• Irritable bowel syndrome
• Renal colic
• Biliary colic
• Dysmenorrhea

Dosage

Children: For paediatric doses, refer to the BNF for Children as specific dosing may vary based on age and condition.

Adults: The usual adult dose is 80 mg to 160 mg taken three times daily, depending on the severity of the condition.

Mechanism of action

Phloroglucinol acts as a spasmolytic agent by inhibiting the contraction of smooth muscles, which is mediated through its interaction with the phosphodiesterase enzyme. This leads to increased levels of cyclic AMP and cyclic GMP, resulting in relaxation of smooth muscle and relief from spasms. The compound may also influence neurotransmitter release and modulate pain perception in the gastrointestinal tract.

Pharmacodynamics

Phloroglucinol exhibits dose-dependent effects on smooth muscle relaxation. Its spasmolytic activity is attributed to its ability to decrease muscle tone and motility, thereby providing symptomatic relief from painful spasms. The onset of action is typically rapid, and the duration of effect can vary based on the route of administration and the specific condition being treated.

Pharmacokinetics

After oral administration, phloroglucinol is rapidly absorbed and reaches peak plasma concentrations within 1 to 2 hours. It is metabolized primarily in the liver, with a significant first-pass effect. The elimination half-life is relatively short, necessitating multiple doses for sustained effect. Renal excretion is the primary route of elimination for its metabolites.

Pregnancy

There is limited data on the use of phloroglucinol during pregnancy. Use only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

Phloroglucinol is excreted in breast milk. Caution should be exercised when administering to nursing mothers.

Storage

Store at room temperature, away from light and moisture.

Formulations

• Tablets
• Oral solution

Indications

• Abdominal colic
• Irritable bowel syndrome
• Biliary colic
• Renal colic
• Dysmenorrhea

Dosage

Children: Refer to BNF for Children for specific dosing recommendations for paediatrics.

Adults: Refer to BNF for specific dosing recommendations for adults.

Mechanism of action

Trimethylphloroglucinol acts as a competitive inhibitor of phosphodiesterase, leading to increased levels of cyclic adenosine monophosphate (cAMP) within cells. This elevation in cAMP results in relaxation of smooth muscle, thereby alleviating spasms and reducing pain associated with conditions like abdominal colic.

Pharmacodynamics

The pharmacodynamic profile of trimethylphloroglucinol involves its ability to inhibit smooth muscle contraction through the modulation of intracellular signaling pathways. By enhancing cAMP levels, it promotes smooth muscle relaxation, which is beneficial in the context of conditions characterized by involuntary muscle contractions.

Pharmacokinetics

Trimethylphloroglucinol is absorbed from the gastrointestinal tract following oral administration. It is metabolized in the liver, and its elimination half-life allows for effective dosing intervals. The pharmacokinetic properties of the drug support its use in acute symptomatic relief of spasmodic conditions.

Pregnancy

Trimethylphloroglucinol should be used in pregnancy only if the potential benefit justifies the potential risk to the fetus. Consult with healthcare professionals for risk assessment.

Breast-feeding

It is not known whether trimethylphloroglucinol is excreted in human milk. Caution is advised when administering to breastfeeding mothers.

Storage

Store at room temperature, away from moisture and heat.

Formulations

• {'formulation_name': 'Trimethylphloroglucinol', 'molecular_formula': 'C9H12O3'}