DOVERIN INJECTION

Indications

• Visceral spasms
• Cervical dilation during labor
• Pain associated with gastrointestinal tract spasms

Dosage

Children: Refer to the BNF for Children for appropriate paediatric dosing information.

Adults: Refer to the specific BNF guidelines for dosing recommendations.

Mechanism of action

Drotaverine inhibits phosphodiesterase 4 (PDE4), an enzyme that breaks down cyclic adenosine monophosphate (cAMP). By preventing the degradation of cAMP, drotaverine increases its levels within cells, leading to smooth muscle relaxation. Additionally, research has indicated a potential role for PDE4 inhibitors in addressing tumorigenesis, suggesting further therapeutic applications.

Pharmacodynamics

Drotaverine is classified as a spasmolytic agent, exhibiting a relaxing effect on smooth muscles. It is effective in relieving visceral spasms and enhancing cervical dilation. Furthermore, drotaverine has demonstrated cytostatic effects on various human tumor cell lines and nonmalignant mouse fibroblasts in vitro. It may also exhibit minor allosteric blocking properties on calcium channels, functioning similarly to voltage-dependent L-type calcium channel blockers.

Pharmacokinetics

The pharmacokinetic profile of drotaverine includes absorption, distribution, metabolism, and excretion characteristics that are typical for spasmolytic agents. Specific data regarding the half-life, peak plasma concentrations, and elimination routes are not detailed in the provided information, thus requiring further literature reference for comprehensive understanding.

Adverse effects

• Nausea
• Vomiting
• Dizziness
• Palpitations
• Allergic reactions

Precautions

• Use with caution in patients with liver or kidney impairment
• Monitor for potential hypotensive effects

Pregnancy

There is limited data on the use of drotaverine during pregnancy. It should only be used if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

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

Storage

Store in a cool, dry place, away from direct sunlight. Keep out of reach of children.

Formulations

• Tablets
• Injectable solution

Mechanism of action

Drotaverine is an inhibitor of phosphodiesterase 4 (PDE4), which is an enzyme responsible for the degradation of cyclic adenosine monophosphate (cAMP). Inhibition of PDE4 leads to elevated levels of cAMP, leading to smooth muscle relaxation. Recent research showed that low levels of cAMP have been associated with brain tumorigenesis, leading to the investigation of PDE4 inhibitors as potential anticancer agents.

Pharmacodynamics

Drotaverine is an e spasmolytic agent with a relaxing effect on smooth muscles. It works to relieve visceral spasms and improve cervical dilation. _In vitro_, drotaverine mediated cytostatic effects on several human tumor cell lines and nonmalignant mouse fibroblasts. Drotaverine may have minor allosteric calcium channel blocking properties: _in vitro_, drotaverine behaves like voltage-dependent L-type calcium channel blockers.