SAMALIN ADULT LOZENGES

Indications

• Dyspepsia
• Flatulence
• Bloating
• Cough relief
• Antimicrobial support

Dosage

Children: Consult appropriate pediatric herbal guidelines, as specific dosing is not universally established.

Adults: Refer to herbal supplement guidelines for dosing, as specific doses can vary widely based on preparation and concentration.

Mechanism of action

Aniseed contains several active compounds, including anethole, which is believed to exert its effects primarily through modulation of the gastrointestinal system. Anethole can stimulate the secretion of digestive enzymes and has been shown to possess antispasmodic properties, potentially alleviating symptoms related to gastrointestinal discomfort. Additionally, its antimicrobial properties may contribute to inhibiting the growth of certain pathogens.

Pharmacodynamics

The pharmacodynamic profile of aniseed is characterized by its ability to enhance digestive function and alleviate symptoms of dyspepsia. Its antispasmodic effects are mediated through inhibition of smooth muscle contractions in the gut. Aniseed may also exhibit mild sedative properties, contributing to its use as a calming herbal remedy. The overall effect is a combination of digestive support and potential relief from gastrointestinal discomfort.

Pharmacokinetics

The pharmacokinetics of aniseed components, particularly anethole, involve oral absorption followed by distribution throughout the body. Anethole is metabolized in the liver and excreted primarily in the urine. The onset of action can vary based on the form of administration, with herbal teas generally producing effects within a few hours, while concentrated extracts may have a more rapid onset. The duration of action is also influenced by the dose and form used.

Adverse effects

• Allergic reactions
• Dermatitis
• Gastrointestinal upset

Interactions

• May interact with anticoagulants, increasing the risk of bleeding
• Can enhance the effects of sedative medications

Precautions

• Use with caution in individuals with a history of allergies, particularly to plants in the Apiaceae family
• May cause skin irritation in sensitive individuals

Pregnancy

Generally considered safe when used in culinary amounts, but high doses should be avoided due to potential hormonal effects.

Breast-feeding

Considered safe when used in culinary amounts, but high doses should be avoided.

Storage

Store in a cool, dry place away from direct sunlight and moisture.

Formulations

• Whole seeds
• Essential oil
• Ground powder

Indications

• Topical pain relief for conditions such as osteoarthritis and neuropathic pain
• Management of postherpetic neuralgia
• Supportive treatment for muscle and joint pain
• Stimulation of digestion and appetite

Dosage

Children: Dosage for pediatric patients should be determined by a healthcare provider, taking into consideration

Adults: Topical formulations generally recommend application to the affected area, with specific dosing instructions provided by the product label. For oral supplements, follow the manufacturer's guidelines or consult a healthcare professional.

Mechanism of action

Capsaicin, the main active component in Capsicum, exerts its effects by binding to the TRPV1 (transient receptor potential vanilloid 1) receptor, which is a cation channel involved in the transmission of pain and heat sensations. This binding leads to the depolarization of sensory neurons, resulting in the release of substance P, a neuropeptide associated with pain signaling. Continuous exposure to capsaicin results in the desensitization of these receptors, leading to decreased pain perception over time.

Pharmacodynamics

The analgesic properties of Capsicum are attributed to its ability to alter the perception of pain. Capsaicin induces a sensation of warmth and pain initially, which is followed by a prolonged analgesic effect due to the depletion of substance P from the nerve endings. Additionally, Capsicum may exhibit anti-inflammatory effects through the modulation of cytokine release and inhibition of inflammatory pathways, contributing to its therapeutic applications in pain management and inflammatory conditions.

Pharmacokinetics

Capsaicin is poorly absorbed when ingested orally, but it can be effectively absorbed through the skin when applied topically. After application, it is metabolized by the liver, and its metabolites are excreted primarily through the kidneys. The onset of action for topical preparations can vary, with effects often observed within hours. The duration of action may last from several hours to days, depending on the formulation and the area of application.

Adverse effects

• Burning sensation at the site of application
• Skin irritation or rash
• Gastrointestinal upset (if ingested)
• Allergic reactions

Precautions

• Avoid contact with eyes and mucous membranes
• Use caution in patients with sensitive skin
• Consult a healthcare professional before use in patients with underlying health conditions

Pregnancy

Capsicum is generally considered unsafe during pregnancy due to potential effects on the fetus. Pregnant women should consult a healthcare provider before use.

Breast-feeding

Capsicum should be used with caution during breastfeeding as it may affect milk production or flavor.

Storage

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

Formulations

• Topical ointments or creams
• Capsules
• Powdered form for oral use

Indications

• Respiratory infections
• Cough and cold symptoms
• Sinusitis
• Bronchitis
• Muscle pain and inflammation

Dosage

Children: Refer to specific product guidelines or consult a healthcare professional for appropriate dosing of eucalyptus oil in children, as it varies based on formulation and indication.

Adults: Refer to specific product guidelines or consult a healthcare professional for appropriate dosing of eucalyptus oil, as it varies based on formulation and indication.

Mechanism of action

Eucalyptus oil contains compounds such as eucalyptol (1,8-cineole) that exhibit antimicrobial properties. It acts on the respiratory system by promoting bronchodilation and reducing mucus production. The oil also has a cooling effect, which can provide relief from symptoms of respiratory distress. Additionally, the oil's anti-inflammatory properties help decrease inflammation in the airways.

Pharmacodynamics

The primary active ingredient in eucalyptus oil, eucalyptol, interacts with the body's inflammatory response and can modulate the activity of neurotransmitters involved in pain signaling. It may enhance mucociliary clearance in the respiratory tract, facilitating the expulsion of mucus and pathogens. The analgesic effects can help relieve discomfort associated with respiratory infections.

Pharmacokinetics

Eucalyptus oil is typically administered via inhalation or topical application. When inhaled, components like eucalyptol are absorbed through the mucous membranes of the respiratory tract and rapidly distributed throughout the body. The oil is metabolized primarily in the liver, and its metabolites are excreted in urine. The half-life of eucalyptol varies but is generally short, necessitating frequent dosing for sustained effects.

Adverse effects

• Allergic reactions
• Skin irritation
• Nausea
• Vomiting
• Diarrhea
• Dizziness

Interactions

• May interact with anticoagulants, potentially increasing bleeding risk
• May enhance the effects of other medications that cause sedation

Precautions

• Use with caution in individuals with asthma or other respiratory conditions
• Avoid use in young children without medical supervision
• Eucalyptus oil should not be ingested in large quantities due to toxicity

Pregnancy

Eucalyptus oil is generally considered unsafe in pregnancy due to potential toxicity and should be avoided unless prescribed by a healthcare professional.

Breast-feeding

Caution is advised when using eucalyptus during breastfeeding, as it may pass into breast milk and could affect the infant.

Storage

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

Formulations

• Eucalyptus oil (topical, inhalation, or oral preparations)
• Eucalyptus leaves (dried for teas or extracts)

Indications

• General wellness support
• Anti-inflammatory effects
• Antioxidant activity
• Digestive aid
• Support for immune function

Dosage

Children: Paediatric dosing should be determined based on the specific extract and its intended use. Consultation with a healthcare provider is recommended for accurate dosing.

Adults: Dosage varies widely depending on the specific extract and formulation. It is essential to follow the manufacturer's instructions or consult a healthcare professional for appropriate dosing.

Mechanism of action

The mechanism of action of herbal extracts can vary significantly based on their constituents. Commonly, they exert their effects through multiple pathways including modulation of neurotransmitter systems, interference with inflammatory processes, or direct antioxidant activity. Some extracts may activate certain receptors or inhibit enzymes related to disease processes.

Pharmacodynamics

The pharmacodynamics of extracts is complex due to the presence of multiple active compounds which can have synergistic or antagonistic effects. These compounds may influence cellular signaling pathways, alter gene expression, or modulate immune response. The overall pharmacological profile is determined by the specific composition of the extract, its concentration, and the biological target it interacts with.

Pharmacokinetics

The pharmacokinetics of extracts involves absorption, distribution, metabolism, and excretion of the active compounds. Generally, herbal extracts are absorbed in the gastrointestinal tract, with bioavailability influenced by factors such as formulation, the presence of food, and individual metabolic differences. Compounds may undergo hepatic metabolism, and elimination can occur through urine or feces, depending on their chemical nature.

Pregnancy

Consult a healthcare professional before use, as the safety of the extract during pregnancy has not been established.

Breast-feeding

Consult a healthcare professional before use, as the safety of the extract during breastfeeding has not been established.

Storage

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

Indications

• Cough and respiratory tract disorders
• Peptic ulcer disease
• Gastroesophageal reflux disease (GERD)
• Adrenal insufficiency
• Inflammatory conditions

Dosage

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

Adults: Refer to reputable clinical guidelines or pharmacopoeias for appropriate dosing.

Mechanism of action

Glycyrrhizin inhibits the enzyme 11β-hydroxysteroid dehydrogenase type 2 (11β-HSD2), which typically converts active cortisol to its inactive form, cortisone. This inhibition leads to increased cortisol levels, resulting in mineralocorticoid-like effects such as sodium retention and potassium excretion, which can influence blood pressure and fluid balance. Additionally, liquorice exhibits antioxidant properties and may modulate immune responses.

Pharmacodynamics

Liquorice displays a variety of pharmacological effects including anti-inflammatory, antiviral, and gastroprotective actions. Its anti-inflammatory effects are attributed to the inhibition of pro-inflammatory cytokines and the suppression of immune cell activation. The antiviral properties are primarily linked to its action against viruses such as herpes simplex and hepatitis C. Moreover, liquorice can enhance mucus secretion in the respiratory tract, facilitating the expulsion of phlegm.

Pharmacokinetics

Liquorice is absorbed from the gastrointestinal tract, with glycyrrhizin being the most bioactive compound. Its metabolites can be detected in the plasma, and the elimination half-life is variable, generally between 6 to 12 hours. The metabolism of glycyrrhizin occurs primarily in the liver, and it undergoes phase I and phase II metabolic processes. Excretion mainly occurs through urine, with both active and inactive metabolites present.

Contra-indications

• Hypersensitivity to liquorice or any of its components
• Severe hypertension
• Heart disease
• Kidney disease
• Cirrhosis of the liver

Adverse effects

• Hypertension
• Hypokalemia
• Edema
• Headache
• Fatigue
• Gastrointestinal disturbances
• Muscle weakness
• Arrhythmias

Interactions

• Corticosteroids - may enhance the effects of corticosteroids
• Digoxin - may increase the risk of digoxin toxicity due to hypokalemia
• Diuretics - may reduce effectiveness of potassium-sparing diuretics and increase potassium loss
• Antihypertensives - may counteract the effects of antihypertensive medications

Precautions

• Use with caution in patients with hypertension
• Monitor electrolytes, particularly potassium levels in long-term use
• Avoid excessive consumption, particularly in patients with underlying cardiovascular conditions

Pregnancy

Use during pregnancy is not well studied; consult a healthcare provider before use.

Breast-feeding

Limited information available; consult a healthcare provider before use.

Storage

Store in a cool, dry place away from direct sunlight.

Formulations

• Dried root
• Powder
• Extracts
• Syrups

Indications

• Topical analgesic for muscle and joint pain
• Cough suppressant in cough drops and lozenges
• Relief of minor throat irritation
• Cooling agent in various cosmetic and personal care products

Dosage

Children: Refer to BNF for Children for specific dosing guidelines, as doses may vary based on age and formulation.

Adults: For topical use, apply a thin layer to the affected area not more than 3 to 4 times daily. For cough drops, follow the product-specific instructions as per the formulation.

Mechanism of action

Menthol acts as an agonist for the transient receptor potential subtype M8 (TRPM8), a non-selective cation channel that is activated by cold temperatures. This activation leads to calcium influx in mast cells, inducing the release of histamine, which can trigger allergic responses such as urticaria, asthma, and rhinitis. Menthol's ability to induce histamine release via TRPM8 suggests potential therapeutic applications for TRPM8 antagonists in managing cold- and menthol-induced allergies.

Pharmacodynamics

Menthol produces a cooling effect by stimulating sensory neurons that convey cold sensations. It interacts with TRPM8 channels, leading to the activation of intracellular signaling pathways that can result in vasodilation and increased blood flow to the area of application. This cooling sensation can provide symptomatic relief in conditions characterized by pain or irritation.

Pharmacokinetics

Menthol is absorbed through the skin and mucous membranes, with systemic effects depending on the route of administration. Its bioavailability can vary, and it is metabolized primarily in the liver. The elimination half-life and excretion pathways have not been extensively characterized, but menthol is generally considered to have a rapid onset of action with effects lasting for a few hours.

Adverse effects

• Allergic reactions
• Urticaria
• Asthma
• Rhinitis
• Skin irritation

Precautions

• Use with caution in patients with known allergies to menthol or related compounds
• May exacerbate asthma in sensitive individuals

Pregnancy

There are no well-controlled studies of menthol in pregnant women. Menthol should be used during pregnancy only if clearly needed.

Breast-feeding

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

Storage

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

Formulations

• Topical ointment
• Cream
• Liquid

Indications

• Antimicrobial treatment
• Antioxidant therapy
• Flavoring agent in food
• Natural preservative
• Traditional medicine applications

Dosage

Children: Refer to specific product guidelines or consult a healthcare professional for appropriate dosing.

Adults: Refer to specific product guidelines or consult a healthcare professional for appropriate dosing.

Mechanism of action

The mechanism of action of oleoresin varies depending on its source and the specific compounds it contains. Generally, oleoresins exhibit antimicrobial activity, which may involve the disruption of microbial cell membranes or interference with metabolic processes. Additionally, some components may have anti-inflammatory and antioxidant effects, contributing to their therapeutic potential.

Pharmacodynamics

Oleoresins exhibit a range of pharmacodynamic effects, including antimicrobial, antioxidant, and anti-inflammatory activities. The specific effects will depend on the source of the oleoresin and its chemical composition. These properties are attributed to the various phytochemicals present, such as terpenes, phenolics, and other bioactive compounds, which can modulate biological pathways and influence physiological responses.

Pharmacokinetics

The pharmacokinetics of oleoresin are not well-defined due to the complexity of its composition. Generally, the absorption and metabolism of oleoresins can vary widely based on the individual compounds they contain. Lipophilic components may be absorbed through the gastrointestinal tract and metabolized in the liver, while other components may undergo different metabolic pathways. The elimination half-life is also variable, reflecting the diverse nature of its constituents.

Pregnancy

Safety in pregnancy has not been established, consult healthcare provider.

Breast-feeding

Consult healthcare provider before use during breastfeeding.

Storage

Store in a cool, dry place away from direct sunlight.

Indications

• Gastrointestinal discomfort
• Irritable bowel syndrome (IBS)
• Nausea
• Headaches
• Cold symptoms
• Oral health issues

Dosage

Children: Refer to product-specific guidelines for dosing, as peppermint is available in various forms and pediatric dosing should be determined based on age

Adults: Refer to product-specific guidelines for dosing, as peppermint is available in various forms (e.g., oil, capsules, tea) and doses may vary based on the formulation and condition being treated.

Mechanism of action

Peppermint exhibits its effects primarily through the menthol component, which acts as a calcium channel blocker and triggers the release of cold-sensitive ion channels. This action provides a cooling sensation and may help relax the smooth muscles in the gastrointestinal tract, promoting relief from symptoms such as bloating and discomfort. Additionally, menthol has anti-inflammatory properties that contribute to its therapeutic effects.

Pharmacodynamics

The pharmacodynamic effects of peppermint are attributed to its active compounds, including menthol, menthone, and other monoterpenes. These compounds exert spasmolytic effects on the gastrointestinal smooth muscle, enhance bile flow, and possess analgesic properties. The overall impact is a reduction in gastrointestinal spasms and improved digestive comfort. Peppermint oil is also noted for its antimicrobial properties, which can help in managing oral health issues.

Pharmacokinetics

Peppermint oil is absorbed through the gastrointestinal tract when ingested, with peak plasma concentrations occurring within a few hours. The metabolism of menthol occurs primarily in the liver, and it is excreted through urine as glucuronide conjugates. The half-life of menthol is approximately 1.5 hours, but this can vary based on individual metabolic rates and the form of peppermint used. Topical applications of peppermint oil result in localized effects with minimal systemic absorption.

Adverse effects

• Allergic reactions
• Heartburn
• Nausea
• Vomiting
• Diarrhea

Precautions

• Use with caution in individuals with gastroesophageal reflux disease (GERD)
• Avoid in patients with known allergies to mint or peppermint oil
• Consult a healthcare professional before use in children

Pregnancy

Peppermint is generally considered safe in moderate amounts during pregnancy; however, high doses should be avoided.

Breast-feeding

Peppermint is often considered safe during breastfeeding when used in food amounts; consult a healthcare provider for medicinal use.

Storage

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

Formulations

• Peppermint oil
• Peppermint leaves
• Peppermint tea

Indications

• Cognitive dysfunction
• Sleep disorders
• Attention deficit hyperactivity disorder (ADHD)
• Neurodegenerative disorders

Dosage

Children: Refer to the appropriate clinical guidelines or the prescribing information for specific dosing recommendations as they may vary based on individual patient factors.

Adults: Refer to the appropriate clinical guidelines or the prescribing information for specific dosing recommendations as they may vary based on individual patient factors.

Mechanism of action

Pulmilopine selectively antagonizes the histamine H3 receptor, which is primarily located in the central nervous system. By blocking this receptor, pulmilopine increases the release of several neurotransmitters, including acetylcholine, norepinephrine, and serotonin, which may improve alertness and cognitive function. The H3 receptor is known to play a crucial role in regulating the release of these neurotransmitters, thus its antagonism can lead to enhanced neurotransmission and improved cognitive activity.

Pharmacodynamics

The pharmacodynamic effects of pulmilopine include improved cognitive function, increased alertness, and enhanced wakefulness due to the modulation of neurotransmitter release. Its action on the H3 receptor may also have implications for the treatment of neurodegenerative disorders and attention deficit hyperactivity disorder (ADHD), where cognitive enhancement is desirable.

Pharmacokinetics

Pulmilopine is absorbed following oral administration, with peak plasma concentrations typically occurring within a few hours. It undergoes hepatic metabolism, with liver enzymes playing a significant role in its biotransformation. The elimination half-life of pulmilopine can vary based on individual factors such as age, liver function, and concurrent medications. It is primarily excreted through the urine, with a portion eliminated unchanged.

Contra-indications

• Hypersensitivity to pulmilopine or any of its components
• Severe hypotension
• Acute myocardial infarction
• Heart block
• Severe liver impairment

Adverse effects

• Headache
• Dizziness
• Fatigue
• Nausea
• Hypotension
• Palpitations
• Peripheral edema

Interactions

• Caution with concurrent use of other antihypertensives as it may potentiate the effects
• May interact with medications that affect liver enzymes
• Caution with diuretics due to potential for additive hypotensive effects

Precautions

• Monitor blood pressure regularly
• Use with caution in patients with renal impairment
• Consider risk of syncope in elderly patients
• Caution in patients with a history of cardiovascular disease

Pregnancy

Data on the use of pulmilopine in pregnancy is limited. It should be used only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

There is insufficient information on the excretion of pulmilopine in human milk. Caution is advised when administering to breastfeeding mothers.

Storage

Store at room temperature, away from moisture and heat. Keep out of reach of children.

Formulations

• Tablets
• Oral solution

Mechanism of action

Exposure to low temperatures often causes allergic responses or urticaria. Similarly, menthol, a common food additive is also known to cause urticaria, asthma, and rhinitis. However, despite the obvious clinical implications, the molecular mechanisms responsible for inducing allergic responses to low temperatures and menthol have not been determined. Because a non-selective cation channel, transient receptor potential subtype M8 (TRPM8) is activated by cold and menthol, we hypothesized that this channel mediates cold- and menthol-induced histamine release in mast cells. Here, we report that TRPM8 is expressed in the basophilic leukemia mast cell line, RBL-2H3, and that exposure to menthol or low temperatures induced Ca(2+) influx in RBL-2H3 cells, which was reversed by a TRPM8 blocker. Furthermore, menthol, a TRPM8 agonist, induced the dose-dependent release of histamine from RBL-2H3 cells. When TRPM8 transcripts were reduced by siRNA (small interfering RNA), menthol- and cold-induced Ca(2+) influx and histamine release were significantly reduced. In addition, subcutaneous injection of menthol evoked scratching, a typical histamine-induced response which was reversed by a TRPM8 blocker. Thus, our findings indicate that TRPM8 mediates the menthol- and cold-induced allergic responses of mast cells, and suggest that TRPM8 antagonists be viewed as potential treatments for cold- and menthol-induced allergies. /DL-Menthol/ Menthol's characteristic cooling sensation is due, in part, to the activation of sensory neurons generally termed transient receptor potential (TRP) channels, in particular transient receptor potential melastatin family member 8 (TRPM8) and transient receptor potential subfamily A, member 1 (TRPA1). Menthol acts upon TRPM8 receptors by rapidly increasing intracellular calcium and mobilizing calcium flux through the channels to induce cold response signals at the application site. Aside from its cold-inducing sensation capabilities, menthol exhibits cytotoxic effects in cancer cells, induces reduction in malignant cell growth, and engages in synergistic excitation of GABA receptors and sodium ion channels resulting in analgesia. /DL-Menthol/ In recent years, the transient receptor potential melastatin member 8 (TRPM8) channel has emerged as a promising prognostic marker and putative therapeutic target in prostate cancer. We have found that forced overexpression of TRPM8 in PC-3 cells can inhibit the cell proliferation and motility probably through the TRPM8 activation. In this study, we aimed to investigate whether activating the TRPM8 channel by its selective agonist menthol can inhibit the proliferation and motility of androgen-independent prostate cancer (AIPC) with remarkable expression of TRPM8. Menthol is a naturally occurring compound, which has been widely used in cosmetics and pharmaceutical products, and also as flavoring in food. DU145 cells are androgen-independent but have a remarkable expression of TRPM8. The demonstration of the existence of TRPM8 and the absence of TRPA1 in DU145 cells provided the foundation for the following experiments, because both TRPM8 and TRPA1 are molecular targets of menthol. The outcome of MTT assay indicated that menthol inhibited the cell growth (p < 0.01). Cell cycle distribution and scratch assay analysis revealed that menthol induced cell cycle arrest at the G(0)/G(1) phase (p < 0.01). Furthermore, menthol inhibited the migration of DU145 cells by downregulating the focal-adhesion kinase. So it suggests that the activation of the existing TRPM8 channels may serve as a potential and pragmatic treatment for those AIPC with remarkable expression of TRPM8, and menthol is a useful compound for future development as an anticancer agent. /DL-Menthol/