Abstract

A spasm is a sudden, involuntary contraction of a muscle, group of muscles, or hollow organ, such as the bladder. Spasms can be brief but severe and painful. Muscle spasms occur when your muscle involuntarily and forcibly contracts uncontrollably and can’t relax. Muscle spasms are normal and quite common. Spasmolytic drugs are also known as antispasmodic drugs or centrally acting muscle relaxant. A spasmolytic agent is a type of medication that reduces excessive smooth muscle contraction in body, commonly used to alleviate symptoms like abdominal cramps and pain associated with conditions such as irritable bowel syndrome. It is associated with cerebral palsy, multiple sclerosis, stroke. The generation of neuronal signals in motor neurons that cause muscle contraction depend on balance of synaptic excitation and inhibition of motor neuron receives.

Keywords

Introduction

Many diseases are cured by the therapeutic effects of different herbal plants. Now a days, one of the challenging concerns among the people are gastrointestinal diseases and discomfort. Typically, medications with spasmolytic properties are used to treat the symptoms of smooth muscle contraction and cramping in gastrointestinal disorders. They also help to reduce muscle spasms.   A spasmolytic is a type of medication or substance that helps relieve muscle spasms or cramps. These agents work by relaxing the muscles, which can alleviate pain and discomfort associated with conditions like gastrointestinal issues, menstrual cramps, or muscle strains. There are several types of spasmolytics, including over-the-counter treatments and prescription drugs. Common examples include anticholinergic drugs and certain muscle relaxants. Herbs with antispasmodic properties were important in the treatment of gastrointestinal disorders in alternative medicine. Some of the herbal plants which show spasmolytic effects are Foeniculum vulgare (Umbelliferae), Psidium guajava (Myrtaceae), Menthe piperita (Lamiaceae), Gentiana lutea (Gentianaceae), Calotropis gigantea (Apocynaceae).

Foeniculum Vulgare

Foeniculum vulgare is a shorted-lived perennial plant belonging to the family Umbelliferae. It is commonly known as fennel. It has antispasmodic qualities that are the main cause of its spasmolytic effects. Anethole, fenchone and estragole are among the chemicals found in fennel that are primarily responsible for these effects.

     
     
     
Mechanism of Action

• Spasmolytic Action: Anethole, the primary ingredient, has been found to relax smooth muscles, which can lessen spasms in the gastrointestinal tract and other areas. When methacholine tracheal chains are used to generate contractions in isolated guinea pigs, fennel oil has a strong antispasmodic or relaxing effect. This could be related to the potassium channel opening. The essential oil relieves pain and has positive benefits on primary dysmenorrhea.
• Muscle Relaxation: The presence of volatile oils in fennel can inhibit the contractions of smooth muscles, providing relief from cramps and spasms.
• Cholinergic Activity: Fennel may also influence the cholinergic system, reducing acetylcholine’s action on smooth muscle, which can further contribute to its spasmolytic effects.

Other phenolic chemicals, such as flavonoids, have anti-inflammatory and muscle-relaxing properties. Fennel’s capacity to promote easier digestion and lessen cramping or bloating by relaxing the smooth muscles of the digestive tract and increasing bile secretion. Because of these qualities, fennel can help with menstrual cramps, intestinal issues, and other ailments that cause muscle spasms. Trans-anethole is the main constituent of Foeniculum vulgare, and numerous research have demonstrated the smooth muscle relaxant properties of anethole. F. vulgare’s aqueous extract has been shown to have antiulcerogenic properties, while other extracts of the plant also exhibit analgesic, anti-inflammatory, and antioxidant properties.

Clinical Applications:

• Irritable Bowel Syndrome (IBS): By relaxing the smooth muscle in the intestines, fennel helps reduce the pain and cramping that come with IBS.
•  Infant colic: Fennel extracts are used to lessen gas and cramping in the abdomen.
• Bloating and dyspepsia: Fennel is frequently used to herbal teas and preparations to help ease indigestion, bloating, and discomfort caused by excessive gas.
•  Dysmenorrhea: Because fennel relaxes muscles, it has long been used to relieve menstrual cramps. By lessening the force of uterine muscle contraction, the anti-spasmodic effect lessens the severity of cramps.
•  Bronchial Spasms: The bronchial muscles relax when exposed to fennel essential oil. Asthma, bronchitis, and other respiratory disorders where bronchial spasms occur can all benefit from this.
• Urinary Tract Spasms: Fennel’s anti-spasmodic and mild diuretic qualities may help ease the discomfort associated with urinary tract spasms. Because it relaxes the smooth muscles of the bladder and encourages urination, it has been used in traditional medicine to treat ailments like cystitis and urinary retention.
• Skeletal Muscle Spasms: Fennel is more frequently used to treat smooth muscle spasms, such as those in the stomach.

Psidium Guajava

Psidium guajava (Myrtaceae) the common guava, yellow guava, lemon guava or apple guava is an evergreen shrub or small tree. Guava leaves spasmolytic action is caused by a substance known as aglycone quercetin, which is created when gastrointestinal fluids break down the flavonoids in the leaves.

       
       
       
Mechanism of Action:

The spasmolytic effect of Psidium guajava (guava) is thought to occur via several mechanisms:

• Smooth Muscle Relaxation: Essential oils such as eugenol and flavonoids help to relax smooth muscles, which prevents overly strong contractions in the gastrointestinal tract and other systems.
• Anti-inflammatory Action: A number of guava’s constituents contain anti-inflammatory qualities that aid in lowering the underlying inflammation that frequently causes muscle spasms. The anti-inflammatory qualities of guava leaves can lessen gastrointestinal tract discomfort and spasms.
• Antioxidant Effects: Quercetin, gallic acid, and ellagic acid are among the compounds that assist lower oxidative stress, which may contribute to muscle weakness and spasms.

The main substances responsible for the spasmolytic action of guava leaves are flavonoids, tannins, alkaloids, and saponins. Flavonoids found in guava leaves, such as kaempferol and quercetin, have been demonstrated to lessen spasms and relax smooth muscles. Guava leaf tannins have astringent qualities that aid in the overall spasmolytic action by toning and relaxing intestinal muscles. Guava leaves contain some alkaloids that may influence neurotransmitter activation and prevent excessive smooth muscle spasms. Experiments on isolated smooth muscle preparations (such as the guinea pig ileum) are the primary method used to test the antispasmodic properties of guava leaves. Because of these qualities, guava leaves are used in traditional medicine to treat stomach problems and ease cramping in the muscles. Psidium guajava works through the following mechanisms: calcium channel blockage, anticholinergic, anti-inflammatory, antioxidant phytochemical compounds that exhibit antispasmodic effects.

Clinical Application

• Gastrointestinal Disorders (Colic, Cramping, and Diarrhea): Traditional medicine frequently uses guava leaves to alleviate cramping in the abdomen and gastrointestinal spasms. Flavonoids (including quercetin and kaempferol), tannins, and essential oils (like eugenol) are among the substances found in the plant that aid to lessen the smooth muscle spasms in the stomach, which relieves indigestion, bloating, and colic.
• Dysmenorrhea, or menstrual cramps: Because of its spasmolytic properties, guava leaf extract has been used to treat menstrual cramps. It is thought to lessen the severity of cramps by relaxing the uterine muscles.
• Respiratory Spasms (Bronchial and Asthma Relief): The eugenol and other essential oils found in guavas have antispasmodic properties that affect the smooth muscles of the bronchi, which helps to relieve wheezing, shortness of breath, and asthma symptoms.
• Urinary Tract Spasms: Guava’s spasmolytic effects on the smooth muscles of the bladder and urinary system aid to reduce spasms in the urinary tract. This helps with ailments including urinary retention and cystitis (inflammation of the bladder), where spasms cause discomfort and make urinating difficult.

Mentha Piperita

Mentha piperita (Lamiaceae) commonly known as peppermint, is an herbaceous, rhizomatous, perennial plant.It is a hybrid of watermint and spearmint.The essential oil is obtained by steam distillation of the aerial parts of Mentha piperita, which is found on the under sides of the leaves. Menthone (14–32%) and menthol (30–55%) are the main ingredients. Other components include limonene, neomenthol, apinene, b-pinene, isomenthone, 1,8-cineole, and menthofuran. Peppermint’s spasmolytic action is caused by the menthol component. It has been used as an antispasmodic and carminative for respiratory disorders, irritable bowel syndrome, and esophageal spasm.

       
       
       
Mechanism of Action:

• Smooth Muscle Relaxation: Peppermint is frequently used to relieve the symptoms of irritable bowel syndrome (IBS) and other digestive issues because its menthol relaxes smooth muscles. By preventing calcium ions from entering muscle cells, menthol lessens muscular contraction and encourages relaxation.
• Effect on the Gastrointestinal Tract: Research has demonstrated that peppermint oil relaxes the gastrointestinal tract’s smooth muscles. This aids in the relief of gastrointestinal spasm symptoms such indigestion, bloating, and cramping in the abdomen. It is especially helpful in treating diseases like IBS, where bloating and muscular spasms are frequent symptoms.
• Anticholinergic Action: Menthol can inhibit the function of acetylcholine, a neurotransmitter that stimulates muscular contraction, due to its modest anticholinergic properties. Particularly in the digestive system, this may enhance its spasmolytic effects on smooth muscles.

Clinical Applications:

• Irritable Bowel Syndrome (IBS): Peppermint oil is frequently used to treat irritable bowel syndrome (IBS), which helps to lessen the frequency and severity of cramps and spasms.
• Muscle Spasms: Applying peppermint oil topically can help reduce muscle tension and spasms. Mostly used for ailments like headaches, tension, and back and neck muscle strains.
• Infant Colic: By calming the muscles in the digestive system, peppermint oil has been used to treat infant colic.
• Menstrual Cramps (Dysmenorrhea): By calming uterine muscles, peppermint may help reduce pain and suffering associated with menstrual cramps.

Calotropis Gigantea

Calotropis gigantea (Apocynacea), commonly known as giant milkweed or crown flower, is a plant traditionally used in herbal medicine for a variety of therapeutic purposes.  Although Calotropis gigantea is often used to treat ailments including pain, fever, and inflammation, there is also evidence that it may have antispasmodic (or spasmolytic) properties.

   
   
   
Mechanism of Action:

• Effect on Smooth Muscle: The smooth muscles of the gastrointestinal tract and other tissues are believed to be the site of Calotropis gigantea’s spasmolytic activity. Some studies have revealed that extracts from the plant can lessen the frequency and intensity of muscular contractions, presumably by suppressing the action of specific neurotransmitters or ion channels involved in muscle contraction.
• Neurotransmitter Modulation: The release or activity of neurotransmitters, such as acetylcholine or adrenergic chemicals, which are involved in muscular contraction and relaxation, may be influenced by certain substances found in Calotropis gigantea. Calotropis gigantea may help lessen spasm in a variety of tissues, including the smooth muscles of the gastrointestinal tract, by modifying these neurotransmitter systems.
• Regulation of Calcium Ions: Calotropis gigantea may also function by adjusting the calcium ion flux.

The spasmolytic effects of Calotropis gigantea are due to its bioactive compounds, including calotropin, gigantin, calotoxin, and cardenolides. These compounds are believed to interact with the nervous and muscular systems, which could influence smooth muscle contraction and relaxation.

Clinical Applications:

• Gastrointestinal Spasms: The plant may be useful in treating gastrointestinal diseases, including irritable bowel syndrome (IBS), spastic colitis, and other ailments involving smooth muscle spasms in the digestive tract, due to its spasmolytic properties.
• Respiratory Conditions: Treating bronchospasms, which are frequent in diseases like asthma and chronic obstructive pulmonary disease (COPD), may potentially benefit from the spasmolytic effects. Respiratory distress symptoms may be lessened by the plant's ability to relax the bronchial smooth muscles.
• Pain Relief: Calotropis gigantea may help reduce pain in cases of muscular cramps and spasms, such as musculoskeletal pain or menstrual cramps, by reducing tension and relaxing muscle spasms.

Gentiana Lutea

Gentiana lutea (Gentianaceae), commonly known as yellow gentian, is a traditional herbal remedy known for its various medicinal properties, including its potential spasmolytic (antispasmodic) effects. Several active chemicals, including gentiopicroside, gentisin, and swertiamarin, are responsible for the spasmolytic characteristics of Gentiana lutea. These compounds have a variety of pharmacological effects on the digestive system and smooth muscle.

     
     
       
Mechanism of Action:

The following methods could account for Gentiana lutea's spasmolytic effects:

• Direct Relaxation of Smooth Muscles: Gentiana lutea contains bitter chemicals, mainly gentiopicroside, which may directly affect the tone of smooth muscles. By altering the intracellular calcium signaling pathways that control muscle contraction, these substances are believed to prevent smooth muscle fibers from contracting.
• Effects on the Digestive Tract: Gentiana lutea's bitter components promote the synthesis of bile and digestive enzymes, which can aid in better digestion and lessen cramps and bloating, particularly those associated with indigestion. These substances have the potential to relax the gastrointestinal tract's smooth muscles and lessen spasms brought on by illnesses including functional gastrointestinal disorders and dyspepsia (indigestion).
• Effects on Inflammation: The anti-inflammatory properties of Gentiana lutea can also play a role in reducing spasms. Chronic inflammation in the gastrointestinal tract can lead to spasms and cramping, and by reducing inflammation, Gentiana lutea may help relieve these symptoms.

Clinical Applications:

• Digestive Disorders: Indigestion, bloating, and constipation are among the digestive issues that Gentiana lutea has historically been used to treat. The cramping brought on by these situations may be lessened by its spasmolytic properties.
• Irritable Bowel Syndrome (IBS): Gentiana lutea may help treat IBS since it relaxes the gut's smooth muscles, especially for those who suffer from discomfort and spasms brought on by abnormalities in gastrointestinal motility.
• Functional Dyspepsia: By easing spasms and facilitating digestion, it might lessen symptoms like bloating, fullness, and stomach cramps in those with functional dyspepsia, a form of indigestion for which there is no known underlying cause.
•  Gallbladder and Liver Problems: Due to its choleretic and digestive-stimulating qualities, it can be used to treat gallbladder and liver disorders.

CONCLUSION

Ultimately, spasmolytic activity is demonstrated by the plant species Gentiana lutea, Calotropis gigantea, Mentha piperita, Psidium guajava, and Foeniculum vulgare. The plant with the highest spasmolytic action among these is Gentiana lutea. The primary cause of Gentiana lutea's spasmolytic action is iridoid glycosides, specifically gentiopicroside and swertiamarin, which relax smooth muscles and lessen spasms, especially in the digestive tract. An overview of these spasmolytic properties is:

Fennel, or Foeniculum vulgare: It has a modest spasmolytic effect because its active ingredients, such as anethole and fenchone, are less potent and more helpful at promoting overall digestion and reducing gas than they are at directly relaxing muscles. Psidium guajava, or guava: Because of its flavonoids, tannins, and essential oils, which have anti-inflammatory, antioxidant, and astringent qualities that help calm the digestive tract and ease moderate cramping or discomfort, Psidium guajava (guava) has a modest spasmolytic activity. However, unlike stronger spasmolytic medicines like peppermint or Gentiana lutea, which focus on directly relaxing smooth muscle, guava's active components are primarily focused on aiding digestion and lowering inflammation, which results in milder spasmolytic effects. Guava works better for gastritis and minor digestive discomfort than it does for severe muscle spasms.

Peppermint, or Mentha piperita: It has minor anticholinergic effects and menthol, its main component, which modulates calcium channels to produce mild spasmolytic activity. However, because menthol has a milder and more limited action on smooth muscle, especially in the gastrointestinal tract, peppermint's spasmolytic effects are comparatively weak. Though not as strong or common as more potent spasmolytic drugs used to treat severe or acute spasms, its activity is helpful for minor spasms and stomach discomfort.

Calotropis gigantea: The mild spasmolytic activity of Calotropis gigantea is largely due to its cardenolides (e.g., calotropin), which affect smooth muscle in a general and less potent manner compared to other more targeted spasmolytic agents. These compounds primarily act on the cardiac muscle, and their effect on smooth muscle relaxation is weaker and less pronounced. Additionally, Calotropis gigantea is primarily used for cardiotonic and anti-inflammatory purposes rather than as a potent spasmolytic. The plant’s spasmolytic effects are secondary to its other therapeutic actions, and it is not as effective for acute or intense muscle spasms as other more potent antispasmodic plants.

REFERENCES

1. Dushyamnt Kumar, H.V Hedge.  Spasmolytic effect of Traditional herbal formulation on guinea pig ileum, Journal of Ayurveda and Integrative Medicine (2015) https://doi:10.4103/0975-9476.157954
2. Shankant B Badgujae. Foeniculum Vulgare Mill: A Review of Botany, Phytochemistry, Pharmacology, contemporary Application and Toxicology, journal of BioMed Research International (2014) https://doi.org/101155/2014/842074
3. Elisabetta Barocelli. Protective effect of Foeniculum vulgare essential oil and anethole in an experimental model of thrombosis, Journal of Pharmacological Research (2007) vol 56, https//doi.org/10.1016/j.phrs.2007.07.002
4. Abdur rauf. Antispasmodic potential of medicinal plant: A comprehensive review article of oxidative medicine and cellular longevity (2021) https://doi.org/10.1155/2021/4889719
5. Ruhul Amin. Pharmacological study on a potential medicinal herb Foeniculum Vulgare, Journal of Science and Technology (2019) https://www.science publishing group.com/j/pst
6. I Wayan Sudira, I M Merdana. Preliminary phytochemical analysis of guava leaves (psidium guajaval) as antidiarrheal in calves, journals of advances in Tropical Biodiversity and Environmental sciences (2019) https://ojs.unud.ac.id/index.php/ATBES/article/view/49860
7. G.M Masud parvez. A short review on a nutritional fruit: Guava. Review Article of Open Acess: Toxicology and Research (2018)
8. Afianti Sulastri. protective effect of guava supplementation in periodonititis rat model, Journal of Engineering and Science and Technology (2020)
9. Albertina Antonielly Sydney de Sousa. Antispasmodic effect of Mentha piperita essential oil on tracheal smooth muscle of rats, Journal of Ethnopharmacology (2010) https://doi.org/10.1016/j.jep.2010.05.012
10. Kamal Gholamipourfard, Mehdi Salehi. Mentha piperita phytochemicals in agriculture, food industry and medicine: Features and applications, South African Journal Of Botany (2021) https://doi.org/10.1016/j.sajb.2021.05.014
11. Ezekiel O. Iwalewaa. In vitro spasmolytic effect of aqueous extract of Calotropis procera on Guinea-pig trachea smooth muscle chain, short report published by Elsevier (2004)
12.  Jagtap V A. Anti-inflammatory Activity of Calotropis gigantea Linn. Leaves Extract on In-vitro Models, International Journal of Current Pharmaceutical Review and Research (2010)
13.  Arpit Dwivedi .Calotropis gigantea: An in-depth review of its therapeutic potential, Journal of Pharmacognosy and Phytochemistry (2024) DOI:10.22271/phyto.2024.v13.i2e.14915
14. Maria Ponticelli, Ludovica Lela. The healing bitterness of Gentiana lutea L., phytochemistry and biological activities: A systematic review, Review article of phytochemistry (2023)  https://doi.org/10.1016/j.phytochem.2022.113518
15. Nemanja Kitic.  Spasmolytic Activity of Gentiana lutea L. Root Extracts on the Rat Ileum: Underlying Mechanisms of Action (2024), MDPI Journals https://doi.org/10.3390/plants13030453