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Alverine Citrate

Alverine Citrate: A Smooth Muscle Relaxant for Modern Gut Health

Introduction

Gastrointestinal (GI) disorders affect millions globally, with symptoms ranging from abdominal discomfort to bowel irregularities. One of the most prevalent among these is Irritable Bowel Syndrome (IBS), which often lacks a definitive cause but demands effective symptom relief. This is where Alverine Citrate comes in—a well-established smooth muscle relaxant that addresses GI spasms and discomfort, especially in functional bowel disorders.

With over half a century of clinical use, Alverine Citrate remains a staple in managing IBS and related conditions.

What is Alverine Citrate?

Alverine Citrate is a spasmolytic agent—a drug that helps reduce involuntary muscle contractions or spasms, particularly in the gastrointestinal and uterine smooth muscles.

It is chemically described as:

  • 1-Allyl-4-(2-dimethylaminoethyl)-2-isopropylbenzylamine citrate

  • It belongs to the class of antispasmodics, distinct from anticholinergics, as it doesn't significantly affect acetylcholine receptors or cause systemic side effects like dry mouth or blurred vision.

Pharmacological Action

Alverine Citrate works by:

  1. Direct action on smooth muscle to relax spasms without affecting normal peristalsis.

  2. No central nervous system (CNS) depression or sedative properties, making it safe for daytime use.

  3. No anticholinergic effects, which makes it preferable for elderly patients or those with glaucoma and urinary issues.

Mechanism of Action

Although the exact mechanism is not fully understood, key actions include:

  • Inhibiting calcium influx into smooth muscle cells.

  • Modifying intracellular signaling related to muscle contraction.

  • Possibly acting via non-cholinergic pathways to selectively reduce spasm without motility suppression.

Clinical Indications

Alverine Citrate is primarily indicated for:

1. Irritable Bowel Syndrome (IBS)

  • Helps reduce abdominal cramps, bloating, and irregular bowel movements.

  • Often combined with simeticone to relieve gas-related symptoms.

2. Diverticular Disease

  • Reduces spasmodic pain and pressure in the lower gut caused by inflamed or infected diverticula.

3. Dysmenorrhea

  • Alverine relaxes uterine smooth muscle, easing painful menstrual cramps.

4. Other GI Disorders

  • Functional bowel disorders without identifiable pathology.

  • Biliary colic and other nonspecific abdominal discomforts.

Formulations and Brand Names

Alverine Citrate is available in:

  • Capsules (most common): 60 mg, 120 mg

  • Combination products: With simethicone or mebeverine

  • Oral suspensions in pediatric or elderly care

Popular brand names include:

  • Spasmonal®

  • Alverine-S

  • Alverix

  • Relaxyl

Dosage and Administration

Condition Typical Dose
IBS & GI spasms 60-120 mg, up to 3 times daily
Dysmenorrhea 60 mg, 2–3 times daily
Elderly Lower dose initially recommended
Children Generally not recommended under age 12

Alverine Citrate should be taken with water, before meals when possible, to optimize its effectiveness against food-related spasms.

Pharmacokinetics

Property Details
Absorption Rapid oral absorption
Onset of action Within 30–60 minutes
Peak plasma level ~1–2 hours after ingestion
Half-life 3–5 hours
Excretion Primarily renal
Metabolism Hepatic, non-CYP450

It does not accumulate in tissues and is rapidly cleared, making it ideal for repeated daily use.

Efficacy in Clinical Trials

Numerous studies have demonstrated the effectiveness of Alverine Citrate:

  • A double-blind trial in the British Journal of Clinical Pharmacology showed significant reduction in IBS pain and urgency within two weeks of treatment.

  • Compared favorably with other antispasmodics like mebeverine and dicyclomine, with fewer side effects.

  • In combination with simethicone, it led to improved bloating and flatulence control in over 75% of participants.

Advantages Over Other Antispasmodics

Feature Alverine Citrate Mebeverine Hyoscine Dicyclomine
CNS effects None Minimal Sedation Drowsiness
Anticholinergic burden None Minimal High High
Rapid onset Yes Moderate Fast Fast
GI-specific action Yes Yes Less Yes

Alverine is ideal for long-term IBS management due to low risk of tolerance, minimal interaction, and patient tolerance.

Side Effects and Safety Profile

Alverine Citrate is well-tolerated, but side effects may occur in rare cases:

Common (mild):

  • Nausea

  • Dizziness

  • Headache

Rare but Serious:

  • Allergic reactions – rash, urticaria

  • Jaundice or liver enzyme elevations (very rare)

  • Dyspnea or bronchospasm in hypersensitive individuals

Safety in Special Populations:

  • Pregnancy: No conclusive evidence of harm, but use only if necessary.

  • Breastfeeding: Use with caution due to limited data.

  • Elderly: No specific contraindication, but start at lower doses.

Drug Interactions

Alverine has minimal drug interaction potential, as it:

  • Does not affect liver enzymes like CYP450.

  • Does not interact with antacids, proton-pump inhibitors, or antibiotics.

Still, caution is advised when combining with other CNS-active agents, although such interactions are not well-documented.

Patient Education Points

When prescribing or recommending Alverine Citrate, it's essential to inform patients:

  • Do not exceed the recommended dose.

  • It may take a few days for full relief.

  • Continue taking during symptom-free periods if advised by your doctor.

  • Report any signs of rash, yellowing of the eyes/skin, or breathing difficulty.

OTC vs Prescription Status

In many countries, Alverine Citrate is available:

  • OTC (over-the-counter) for IBS and dysmenorrhea.

  • Prescription-only in certain jurisdictions based on local regulations.

Its wide availability and favorable safety profile have made it a go-to antispasmodic in both community and hospital settings.

Market Trends and Usage

  • Alverine Citrate continues to be widely prescribed in Europe, the Middle East, Asia, and Latin America.

  • Its popularity has increased due to rising IBS diagnosis rates, better patient education, and preference for non-opioid, non-sedative GI relief.

  • In the pharmaceutical market, combination formulations (e.g., Alverine + Simethicone) have shown substantial sales growth.

Ongoing Research and Future Potential

While Alverine Citrate is an older drug, research is ongoing into:

  • Its role in functional dyspepsia

  • Possible use in post-operative ileus management

  • Combination therapies with probiotics, enzymes, or digestive bitters

  • Use in adolescents with functional abdominal pain

There's also interest in creating modified-release formulations to further enhance symptom targeting and compliance.

Conclusion

Alverine Citrate remains a highly effective, well-tolerated treatment for spasmodic GI and gynecological conditions, especially IBS and dysmenorrhea. With a mechanism focused on smooth muscle relaxation, minimal side effects, and wide availability, it continues to be a first-line option for both doctors and patients.

While newer drugs may emerge, the simplicity, safety, and clinical efficacy of Alverine Citrate ensure its ongoing relevance in modern medicine. As the global burden of IBS and functional GI disorders grows, well-established drugs like Alverine offer reliable relief and better quality of life for millions.

References

  1. British Journal of Clinical Pharmacology – Efficacy of Alverine in IBS.

  2. NICE Guidelines for IBS Management.

  3. Drugs.com – Alverine Citrate Drug Monograph.

  4. Spasmonal Product Information – Sanofi.

  5. WHO Essential Medicines Database.