New Emami Menthoplus Strong Pain Balm

Indications

• Localized neuropathic pain
• Post-herpetic neuralgia
• Painful diabetic neuropathy

Dosage

Adults: Apply 3–4 times a day, using 0.075% strength, apply sparingly, and not more often than every 4 hours.

Mechanism of action

Capsaicin acts as an agonist of the TRPV1 (transient receptor potential vanilloid 1) receptor. Upon activation by capsaicin, the TRPV1 receptor opens to allow the influx of cations, particularly calcium and sodium ions, leading to depolarization of sensory neurons. This results in the induction of pain responses initially, followed by desensitization or 'defunctionalization' of nociceptor fibers, which reduces pain signaling over time. Capsaicin reduces levels of substance P, a neuropeptide associated with pain transmission, contributing to its analgesic effects.

Pharmacodynamics

Capsaicin's interaction with TRPV1 receptors leads to a series of cellular responses, including temporary loss of membrane potential and alterations in neurotrophic factor transport. The prolonged exposure to capsaicin results in persistent activation of these receptors, causing a loss of response to sensory stimuli, which is described as defunctionalization. This process results in significant changes in neuronal excitability and pain perception.

Pharmacokinetics

Capsaicin is primarily applied topically, allowing for localized effects with minimal systemic absorption. The pharmacokinetics of capsaicin involve rapid uptake into the skin and subsequent receptor-mediated effects. The duration of action can vary based on the concentration and formulation used. Capsaicin undergoes metabolism in the liver, and its effects can last for hours to days due to the desensitization of nociceptive pathways.

Contra-indications

• Known hypersensitivity to capsaicin or any of the excipients
• History of cardiovascular disease in diabetic patients
• Uncontrolled hypertension

Adverse effects

• Burning sensation at the application site
• Skin irritation
• Eye irritation if in contact with eyes
• Cough
• Dry mouth
• Nausea
• Palpitations
• Taste alterations
• Throat irritation
• Muscle spasms
• Sneezing
• Watering eyes
• Peripheral edema
• Tachycardia

Interactions

• Use with caution in patients taking other analgesics
• May enhance the effects of medications that affect blood pressure
• Avoid using with other topical agents that may irritate the skin

Precautions

• Avoid contact with broken or inflamed skin
• Wash hands immediately after use
• Wear nitrile gloves when applying patches
• Avoid contact with eyes and mucous membranes
• Avoid hot showers or baths just before or after application
• Monitored use in diabetic patients with cardiovascular disease
• Regular monitoring for side effects in long-term therapy

Pregnancy

Capsaicin should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Consult with a healthcare provider.

Breast-feeding

Use with caution while breastfeeding. Consult a healthcare provider before use.

Storage

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

Formulations

• Topical cream (0.075%)
• Transdermal patches (Qutenza®)

Dosage

Children: Refer to specific formulations and usages, as dosing can vary widely depending on the application and regulatory guidelines.

Adults: Refer to specific formulations and usages, as dosing can vary widely depending on the application and regulatory guidelines.

Mechanism of action

Butylated hydroxyanisole (BHA) and butylated hydroxytoluene (BHT) act as antioxidants by inhibiting the oxidation of lipids. They scavenge free radicals and donate hydrogen atoms to reactive species, thus stabilizing and preventing oxidative damage to cellular components. This action helps to protect the integrity of cell membranes and prevent the formation of harmful peroxides.

Pharmacodynamics

The pharmacodynamic properties of butylated compounds are primarily related to their antioxidant activity. They exhibit a dose-dependent ability to inhibit lipid peroxidation, which is crucial in protecting cells from oxidative stress. Furthermore, they may modulate certain biochemical pathways involved in cell signaling and apoptosis, although these effects are less well-characterized.

Pharmacokinetics

Butylated compounds are absorbed from the gastrointestinal tract following oral ingestion. They undergo metabolic processing primarily in the liver, where they are conjugated and excreted in urine. The half-life of butylated compounds in humans is variable, influenced by factors such as dosage and individual metabolism. Accumulation in tissues is generally low, but prolonged exposure may lead to higher tissue concentrations.

Adverse effects

• Gastrointestinal disturbances
• Allergic reactions
• Potential carcinogenic effects with prolonged exposure

Precautions

• Use with caution in patients with a history of hypersensitivity to butylated compounds
• Avoid prolonged exposure due to potential toxicity

Pregnancy

Limited data available, use only if the benefits outweigh the risks.

Breast-feeding

Unknown, exercise caution and consult a healthcare provider.

Storage

Store in a cool, dry place away from light.

Formulations

• Butylated hydroxytoluene (BHT)
• Butylated hydroxyanisole (BHA)

Indications

• Topical antiseptic
• Analgesic for muscle and joint pain
• Respiratory conditions, such as colds and coughs
• Anti-inflammatory treatment

Dosage

Children: Pediatric use should be approached with caution. It is advisable to consult a healthcare professional before administering cajeput oil to children, ensuring appropriate dilution and method of application.

Adults: Application of cajeput oil should be done according to product-specific instructions, typically diluted with a carrier oil for topical use. For inhalation, a few drops can be added to a bowl of hot water to create steam.

Mechanism of action

Cajeput oil contains various bioactive compounds, including 1,8-cineole (eucalyptus oil), which contribute to its therapeutic properties. The primary mechanism of action includes modulation of ion channels and receptors, particularly influencing the TRPV1 receptor involved in pain and inflammation pathways. Additionally, its antimicrobial effects may arise from disrupting the cell membranes of bacteria and fungi.

Pharmacodynamics

The pharmacodynamics of cajeput oil involve its interaction with pain and inflammation pathways, leading to a reduction in discomfort. Its antiseptic and antimicrobial properties help in preventing infections, while its aromatic compounds may provide relief in respiratory ailments by promoting expectoration and calming respiratory tract irritation.

Pharmacokinetics

Cajeput oil is absorbed through the skin when applied topically and can also be inhaled to reach the lungs. The absorption may vary based on the method of application. Following absorption, its components are metabolized in the liver, and excreted primarily through urine. The half-life of the individual constituents can vary, influencing the duration of action.

Adverse effects

• Skin irritation
• Allergic reactions
• Gastrointestinal upset

Precautions

• Use with caution in individuals with allergies, particularly to plants in the Myrtaceae family
• Should not be applied to broken skin or open wounds

Pregnancy

Cajeput oil should be used with caution during pregnancy, as safety has not been established.

Breast-feeding

It is advisable to avoid the use of cajeput oil while breastfeeding due to insufficient safety data.

Storage

Store in a cool, dry place away from direct sunlight. Keep container tightly closed.

Formulations

• Essential oil

Indications

• Pain relief
• Anti-inflammatory conditions
• Antimicrobial applications
• Dental pain
• Digestive disorders

Dosage

Children: Refer to healthcare professional for appropriate dosing guidelines as clove oil is generally not recommended for children without medical supervision.

Adults: For topical application, clove oil can be diluted with a carrier oil and applied as needed. For oral use, standard culinary doses are generally considered safe, but specific therapeutic doses should be guided by a healthcare professional.

Mechanism of action

Eugenol, the primary active compound in clove, exhibits its effects through several pathways. It acts as an analgesic by inhibiting the synthesis of prostaglandins, which are mediators of pain and inflammation. Additionally, eugenol has been shown to interact with voltage-gated sodium channels, which may contribute to its analgesic effects. Its antimicrobial properties are partly due to its ability to disrupt the cell membranes of bacteria and fungi.

Pharmacodynamics

Clove has a variety of pharmacodynamic effects, primarily attributed to eugenol. It exhibits analgesic, anti-inflammatory, and antioxidant properties. Clove oil has been found to reduce pain and inflammation in various experimental models. Its antimicrobial activity is effective against a range of pathogens, making it a candidate for use in oral health products. Furthermore, the antioxidant properties help in neutralizing free radicals, thereby providing protective effects against cellular damage.

Pharmacokinetics

Clove oil is absorbed through the gastrointestinal tract when ingested and can also be absorbed through the skin when applied topically. The bioavailability of eugenol can be influenced by its formulation and method of administration. Once absorbed, eugenol is distributed throughout the body, metabolized primarily in the liver, and excreted via the kidneys. The half-life of eugenol varies but is generally short, necessitating frequent dosing for sustained effects in therapeutic use.

Adverse effects

• Allergic reactions
• Gastrointestinal irritation
• Liver toxicity with excessive use
• Hypoglycemia

Interactions

• May enhance the effects of anticoagulants
• May interact with antidiabetic medications
• May reduce the effectiveness of certain antiepileptic drugs

Precautions

• Use with caution in individuals with liver disease
• Caution in patients with bleeding disorders
• Monitor blood sugar levels in diabetics

Pregnancy

Use during pregnancy is not recommended due to potential effects on the fetus.

Breast-feeding

Limited data available; use with caution as clove can affect milk production.

Storage

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

Formulations

• Essential oil
• Dried whole cloves
• Powdered clove

Indications

• Nausea and vomiting (including motion sickness and morning sickness)
• Gastrointestinal discomfort
• Osteoarthritis
• Inflammation
• Cold and flu symptoms

Dosage

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

Adults: Refer to established guidelines for specific dosing; typically, doses range from 1 to 3 grams of dried ginger per day.

Mechanism of action

The active components of ginger, particularly gingerols, exert their effects primarily through the inhibition of pro-inflammatory cytokines and enzymes, such as cyclooxygenase and lipoxygenase. This action helps to reduce inflammation and pain. Additionally, ginger enhances gastrointestinal motility and has antiemetic properties, which are beneficial in treating nausea.

Pharmacodynamics

Ginger exhibits anti-inflammatory, antioxidant, and antinausea effects. Its ability to modulate the immune response and inhibit platelet aggregation contributes to its cardiovascular protective effects. The antiemetic properties of ginger are particularly effective in reducing nausea and vomiting associated with motion sickness and chemotherapy.

Pharmacokinetics

Ginger is rapidly absorbed in the gastrointestinal tract, with its active components being metabolized in the liver. The bioavailability of ginger compounds may vary, with gingerols being converted into shogaols during processing or heating. The elimination half-life and specific metabolic pathways have not been extensively studied, but the effects can be observed within 30 minutes to 2 hours after ingestion.

Contra-indications

• Gallstones
• Bleeding disorders
• Allergy to ginger or other plants in the Zingiberaceae family

Adverse effects

• Gastrointestinal disturbances (nausea, diarrhea, heartburn)
• Allergic reactions (skin rash, itching)
• Increased risk of bleeding

Interactions

• Anticoagulants (e.g., warfarin, aspirin)
• Antiplatelet agents
• Certain antihypertensives
• Diabetes medications (may enhance effects)

Precautions

• Use with caution in patients with diabetes, hypertension, or gallbladder disease
• Consult a healthcare provider before use in pregnancy or lactation

Pregnancy

Generally considered safe in food amounts, but high doses should be avoided due to potential effects on uterine contractions.

Breast-feeding

Considered safe in food amounts, but high doses should be avoided.

Storage

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

Formulations

• Dried ginger powder
• Ginger root (fresh)
• Ginger tea
• Ginger extract (liquid or capsule)
• Ginger oil

Indications

• Nausea and vomiting (including motion sickness)
• Digestive issues (such as dyspepsia)
• Inflammatory conditions (such as arthritis)
• Menstrual pain
• Cold and flu symptoms

Dosage

Children: Refer to established guidelines or specific product recommendations as doses may vary based on the preparation and indication.

Adults: Refer to established guidelines or specific product recommendations as doses may vary based on the preparation and indication.

Mechanism of action

Ginger exhibits anti-inflammatory and antioxidant effects primarily through the inhibition of pro-inflammatory cytokines and enzymes such as cyclooxygenase (COX) and lipoxygenase (LOX). It also modulates various signaling pathways, including the NF-kB pathway, which plays a crucial role in inflammation.

Pharmacodynamics

Ginger's pharmacodynamic effects are attributed to its active constituents, which have been shown to possess anti-nausea, antiemetic, anti-inflammatory, and analgesic properties. The compounds in ginger can also enhance gastrointestinal motility and reduce gastric irritation.

Pharmacokinetics

Ginger is well-absorbed in the gastrointestinal tract. Its bioactive compounds are metabolized in the liver and excreted in urine. The half-life of gingerol, one of the primary active components, is relatively short, necessitating multiple doses for sustained effects. However, specific pharmacokinetic parameters can vary based on the preparation and individual patient factors.

Adverse effects

• Gastrointestinal discomfort
• Diarrhea
• Heartburn
• Nausea
• Allergic reactions

Interactions

• May interact with anticoagulants, increasing the risk of bleeding
• May affect blood sugar levels, potentially interacting with antidiabetic medications

Precautions

• Use with caution in patients with gallbladder disease
• Use with caution in patients with bleeding disorders

Pregnancy

Ginger is generally considered safe in food amounts during pregnancy, but high doses should be avoided due to potential effects on uterine contractions.

Breast-feeding

Ginger is likely safe when consumed in food amounts during breastfeeding, but high doses should be avoided.

Storage

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

Formulations

• Dried ginger root
• Ginger extract
• Ginger powder
• Ginger tea

Indications

• Head lice infestation
• Body lice infestation
• Scabies

Dosage

Children: Refer to BNF for Children for specific dosing information.

Adults: Refer to BNF for specific dosing information.

Mechanism of action

Benzyl alcohol, a component of hydroxytoluene, inhibits lice from closing their respiratory spiracles. This action allows the vehicle to obstruct the spiracles, leading to asphyxiation of the lice.

Pharmacodynamics

The pharmacodynamics of hydroxytoluene involves its local anesthetic properties and its ability to disrupt the respiratory function of certain parasites. It exerts its effects primarily on ectoparasites like lice, leading to their death through suffocation. Its effectiveness is facilitated by its lipophilicity, which allows it to penetrate the cuticle of the lice and interfere with their respiratory system.

Pharmacokinetics

Hydroxytoluene is absorbed through the skin when applied topically. Its pharmacokinetic profile is influenced by its formulation, with variations in absorption rates based on the vehicle used. Once absorbed, it undergoes metabolic processes primarily in the liver, where it may be conjugated and excreted in urine. The elimination half-life and specific metabolic pathways are not well defined, requiring further research for comprehensive understanding.

Pregnancy

Hydroxytoluene should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

Caution is advised when administering hydroxytoluene during breastfeeding due to limited data on its excretion in human milk.

Storage

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

Indications

• Metabolic acidosis
• Lactic acidosis
• Support in shock or severe dehydration
• Exercise physiology research

Dosage

Children: Refer to clinical guidelines for specific dosing recommendations based on the clinical condition being treated.

Adults: Refer to clinical guidelines for specific dosing recommendations based on the clinical condition being treated.

Mechanism of action

Lactic acid primarily functions by contributing to the acid-base balance in the body. It can serve as a substrate for gluconeogenesis in the liver and is utilized in the Cori cycle, where it is converted back to glucose. Furthermore, lactic acid can act as a signaling molecule in various physiological processes, influencing metabolism and cellular responses during hypoxic conditions.

Pharmacodynamics

Lactic acid dissociates into lactate and hydrogen ions in solution, which can lead to a decrease in pH (acidosis) when produced in excess. Its accumulation in the body is indicative of anaerobic metabolism, often observed during intense exercise or in conditions of oxygen deprivation. The body can buffer the effects of lactic acid through bicarbonate and other mechanisms, maintaining homeostasis.

Pharmacokinetics

Lactic acid is rapidly absorbed and distributed throughout the body. It is metabolized primarily in the liver, where it can be converted to glucose or further metabolized to carbon dioxide and water. The elimination half-life of lactate varies depending on the metabolic state of the individual and the presence of underlying conditions. Renal function also plays a role in the clearance of lactate from the body.

Adverse effects

• Nausea
• Vomiting
• Abdominal pain
• Diarrhea
• Hypersensitivity reactions

Precautions

• Use with caution in patients with renal impairment
• Monitor for signs of metabolic acidosis
• Caution in patients with liver disease

Pregnancy

Lactic acid is generally regarded as safe, but clinical use should be evaluated on a case-by-case basis during pregnancy.

Breast-feeding

Considered safe for use during breastfeeding, but consult healthcare provider for individual cases.

Storage

Store at room temperature, away from direct sunlight and moisture.

Formulations

• Lactic acid injection
• Lactic acid oral solution

Dosage

Children: Refer to specific product information or clinical guidelines for appropriate dosing, as it varies widely by the formulation and intended use.

Adults: Refer to specific product information or clinical guidelines for appropriate dosing, as it varies widely by the formulation and intended use.

Mechanism of action

The mechanism of action of liquid formulations can vary significantly based on their components. For example, if liquidum refers to a hydration solution, the mechanism may involve the replenishment of fluids and electrolytes to maintain cellular function and homeostasis. In other contexts, the active ingredients may exert their effects through specific biochemical pathways or interactions with receptor sites in the body.

Pharmacodynamics

Pharmacodynamics relates to the effects of liquidum on the body, which will depend on its specific composition. Hydration solutions generally aim to restore fluid balance, while therapeutic liquids containing drugs may interact with specific receptors or enzymes, leading to various biological responses. The efficacy and safety profile will depend on the concentration and formulation of the active ingredients.

Pharmacokinetics

The pharmacokinetics of liquidum formulations will vary based on the specific agents included. Generally, pharmacokinetic properties such as absorption, distribution, metabolism, and excretion are influenced by the physical state of the medication (liquid), its solubility, and its formulation. For instance, oral liquid medications may have different absorption rates compared to intravenous formulations. The onset of action, peak effect, and duration of action will also depend on these factors.

Pregnancy

Consult a healthcare professional before use during pregnancy.

Breast-feeding

Consult a healthcare professional before use while breastfeeding.

Storage

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

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

• Allergic conditions
• Autoimmune diseases
• Asthma and chronic obstructive pulmonary disease (COPD)
• Certain cancers (e.g., leukemia, lymphoma)
• Skin conditions (e.g., dermatitis)
• Inflammatory bowel disease
• Multiple sclerosis exacerbations
• Severe infections requiring immunosuppression

Dosage

Children: Refer to BNF for Children for specific dosing; doses vary significantly based on the child's age, weight, and condition being treated.

Adults: Refer to BNF for specific dosing; typically, initial doses range from 4 to 48 mg depending on the severity of the condition.

Mechanism of action

Methylprednisolone exerts its effects by binding to glucocorticoid receptors, leading to the modulation of gene expression. This interaction influences the transcription of anti-inflammatory proteins while suppressing the expression of pro-inflammatory genes, ultimately resulting in reduced inflammation and immune response.

Pharmacodynamics

The pharmacodynamic effects of methylprednisolone are characterized by its ability to decrease inflammation, suppress the immune response, and affect carbohydrate metabolism. Therapeutic doses lead to various systemic effects, including modification of leukocyte distribution and inhibition of cytokine production.

Pharmacokinetics

Methylprednisolone is well absorbed after oral administration, with a bioavailability of approximately 50%. It has a volume of distribution that reflects extensive tissue binding. The drug is metabolized primarily in the liver through conjugation and reduction, and its metabolites are excreted in urine. The half-life varies based on the route of administration but is generally around 18 to 36 hours.

Adverse effects

• Increased blood pressure
• Hyperglycemia
• Weight gain
• Mood changes
• Insomnia
• Gastrointestinal disturbances
• Increased susceptibility to infections

Interactions

• methylphenidate+apraclonidine: Severe (decreases effects)
• methylthioninium chloride+bupropion: Severe (increases risk of severe hypertension)
• methylphenidate+linezolid: Severe (increases risk of elevated blood pressure)
• rasagiline+methylphenidate: Severe (increases risk of a hypertensive crisis)
• mao-inhibitors+methylphenidate: Severe (increases risk of a hypertensive crisis)
• dronedarone+methylprednisolone: Moderate (increases exposure)
• miconazole+methylprednisolone: Moderate (increases concentration)
• antifungals, azoles+methylprednisolone: Moderate (increases exposure)
• crizotinib+methylprednisolone: Moderate (increases exposure)

Precautions

• Use with caution in patients with hypertension
• Monitor blood glucose levels in diabetic patients
• Consider potential for infection risk due to immunosuppression
• Evaluate for psychiatric effects in susceptible individuals

Pregnancy

Corticosteroids may be used during pregnancy if the potential benefit justifies the risk to the fetus. Careful monitoring is advised.

Breast-feeding

Corticosteroids are excreted in breast milk; caution is advised. Monitor the infant for potential effects.

Storage

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

Formulations

• Tablets
• Injectable solutions
• Topical preparations

Mechanism of action

Methylsulphate functions as a methylating agent, transferring a methyl group to nucleophiles. This process involves the formation of a sulfonium ion, which is highly reactive and can readily react with nucleophilic sites on various substrates, leading to methylation reactions.

Pharmacodynamics

The pharmacodynamics of methylsulphate is primarily related to its role as a methylating agent in biochemical reactions. It can alter the structure and function of biological molecules, potentially affecting cellular processes and signaling pathways. However, detailed pharmacodynamic studies specific to therapeutic use are limited.

Pharmacokinetics

There is limited information on the pharmacokinetics of methylsulphate, given its typical use as a reagent in laboratory settings rather than a clinical drug. When used in chemical reactions, its reactivity and transformation into other compounds would dictate its pharmacokinetic profile, which could vary significantly based on the specific context of use.

Pregnancy

There is limited data on the use of methylsulphate in pregnancy. Consult relevant guidelines.

Breast-feeding

Data on the excretion of methylsulphate in human milk is not available. Caution is advised.

Storage

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

Indications

• Used as an excipient in tablet formulations
• Used as a bulking agent in capsule formulations
• Used in food products as a thickener or stabilizer

Dosage

Children: Refer to specific product guidelines as dosage will depend on the formulation and the active ingredients.

Adults: Refer to specific product guidelines as dosage will depend on the formulation and the active ingredients.

Mechanism of action

Microcrystalline cellulose acts as a non-digestible filler that enhances the flow properties of powders during the manufacturing of tablets and capsules. It does not have a direct pharmacological action on the body but ensures that the active ingredients are effectively delivered to the patient.

Pharmacodynamics

As a non-active ingredient, microcrystalline cellulose does not exert pharmacodynamic effects typical of active pharmaceutical ingredients. Its primary role is to provide a stable and consistent matrix for the drug, facilitating the release of the active compound once ingested.

Pharmacokinetics

Microcrystalline cellulose is not absorbed in the gastrointestinal tract; it passes through the digestive system largely unchanged. It adds bulk to the stool, which may aid in promoting regular bowel movements. The substance is excreted in feces, where it contributes to dietary fiber intake.

Pregnancy

Data regarding the use of microcrystalline cellulose during pregnancy is limited. It is advisable to consult with healthcare professionals before use.

Breast-feeding

Microcrystalline cellulose is considered safe during breastfeeding, as it is not absorbed systemically.

Storage

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

Indications

• Pellagra
• Hyperlipidaemia
• Nicotinic acid deficiency
• As a dietary supplement

Dosage

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

Adults: Refer to BNF for specific adult dosing guidelines.

Mechanism of action

Nicotinate functions primarily as a precursor to nicotinamide adenine dinucleotide (NAD) and nicotinamide adenine dinucleotide phosphate (NADP), which are essential for various enzymatic reactions, including those involved in energy metabolism and DNA repair. It is involved in multiple biosynthetic pathways including nicotine biosynthesis and pyridine nucleotide cycling.

Pharmacodynamics

Nicotinate's pharmacodynamic properties are attributed to its role in redox reactions as a coenzyme. It enhances the activity of dehydrogenases and participates in the synthesis of fatty acids and cholesterol, influencing lipid metabolism. Additionally, it has vasodilatory effects, possibly due to its ability to release prostaglandins, which can lead to improved blood flow.

Pharmacokinetics

Nicotinate is well absorbed from the gastrointestinal tract. It is extensively metabolized in the liver, where it is converted into its active form, NAD. The elimination half-life varies but is generally around 20 to 45 minutes. Renal excretion plays a significant role in the elimination of nicotinate and its metabolites.

Pregnancy

There is limited information available on the safety of nicotinate during pregnancy. Consult healthcare professionals for specific guidance.

Breast-feeding

Limited data on the excretion of nicotinate in breast milk. Consult healthcare professionals for advice.

Storage

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

Indications

• Wound healing
• Oral health (e.g., gingivitis, mouth ulcers)
• Anti-inflammatory conditions
• Gastrointestinal disorders (e.g., dyspepsia)
• Antimicrobial applications

Dosage

Children: Refer to established herbal guidelines as specific dosing information may vary based on preparation and condition being treated.

Adults: Refer to established herbal guidelines as specific dosing information may vary based on preparation and condition being treated.

Mechanism of action

The active compounds in officinale, such as resins and essential oils, exhibit their effects through various mechanisms, including the inhibition of pro-inflammatory cytokines and modulation of immune responses. These actions contribute to its analgesic and antimicrobial properties, making it beneficial in treating wounds and oral infections.

Pharmacodynamics

Myrrh has demonstrated a range of pharmacodynamic effects, including analgesia, anti-inflammatory activity, and antimicrobial action. The resin contains various terpenoids and phenolic compounds, which interact with biological pathways to exert these effects. Studies suggest that myrrh may inhibit the growth of certain bacteria and fungi, as well as reduce inflammation by blocking the synthesis of pro-inflammatory mediators.

Pharmacokinetics

The pharmacokinetics of myrrh are not well-defined due to variability in preparation and formulation. However, it is generally believed that the compounds are absorbed through the gastrointestinal tract when ingested, with some components potentially being metabolized in the liver. The onset of action may vary depending on the method of administration, with topical applications likely providing localized effects.

Pregnancy

Safety during pregnancy has not been established; consult a healthcare provider before use.

Breast-feeding

Consult a healthcare provider before using, as safety during breastfeeding is not well established.

Storage

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

Indications

• Constipation
• Dry skin
• Skin irritation

Dosage

Children: Refer to specific guidelines and prescribing information for paediatric dosing.

Adults: Refer to specific guidelines and prescribing information for adult dosing.

Mechanism of action

Paraffin acts as a lubricating agent in the gastrointestinal tract. It coats the stool and the intestinal walls, which helps to ease the passage of feces by reducing friction. This action promotes bowel movements and alleviates constipation. When used topically, it forms a barrier on the skin, which helps to retain moisture and protect against irritants.

Pharmacodynamics

Paraffin has a low viscosity and surface tension, which allows it to spread easily over surfaces. Its lubricating properties facilitate the movement of stool through the intestines, while its emollient properties help in maintaining skin hydration and barrier function. The onset of action for oral administration typically occurs within 6 to 8 hours, making it effective in treating occasional constipation.

Pharmacokinetics

Paraffin is not absorbed systemically when ingested; it remains in the gastrointestinal tract and is excreted unchanged in the feces. After oral administration, it acts locally in the intestines without significant systemic effects. When used topically, it remains on the skin surface and does not penetrate deeply, providing a protective layer without altering systemic pharmacokinetics.

Adverse effects

• Abdominal cramps
• Diarrhea
• Nausea
• Vomiting
• Lipid pneumonia (when aspirated)
• Electrolyte imbalances

Precautions

• Use with caution in patients with gastrointestinal obstruction
• Avoid in patients with a history of aspiration
• Monitor for signs of dehydration with prolonged use

Pregnancy

Use only if clearly needed. Consult a healthcare provider for advice.

Breast-feeding

Paraffin can be excreted in breast milk, use with caution.

Storage

Store at room temperature away from moisture and heat.

Formulations

• Liquid paraffin
• Soft paraffin (for topical use)

Indications

• Constipation
• Dry skin
• Dermatitis
• Eczema

Dosage

Children: Refer to the BNF for Children for specific dosing information tailored to pediatric patients.

Adults: Refer to the BNF for specific dosing information as it can vary based on the formulation and intended use.

Mechanism of action

Paraffinum works primarily by coating the stool and the intestinal lining, which helps to retain water in the intestines, facilitating softer stools and promoting bowel movements. This action reduces the absorption of water from the stool, making evacuation easier.

Pharmacodynamics

Paraffinum exhibits its effects as a lubricant and stool softener. Its hydrophobic nature allows it to create a barrier that reduces friction in the gastrointestinal tract, thus easing the passage of stool. The onset of its laxative effect can vary, often occurring within 6 to 8 hours when taken orally, depending on the individual’s digestive transit time.

Pharmacokinetics

Paraffinum is not significantly absorbed through the gastrointestinal tract, which means it primarily acts locally within the intestines. Its effects are predominantly topical, as it coats the lining of the intestines and stools without systemic absorption. The elimination of paraffinum is primarily through feces, as it is excreted unchanged.

Contra-indications

• Hypersensitivity to mineral oil
• Intestinal obstruction
• Severe abdominal pain of unknown origin

Adverse effects

• Abdominal cramps
• Diarrhea
• Nausea
• Vomiting
• Aspiration pneumonia
• Lipid pneumonia

Interactions

• May interfere with the absorption of fat-soluble vitamins (A, D, E, K)
• Caution with other laxatives

Precautions

• Use with caution in patients with renal impairment
• Avoid prolonged use
• Monitor for signs of aspiration

Pregnancy

Generally considered safe for use during pregnancy, but consult a healthcare provider.

Breast-feeding

Considered safe during breastfeeding, but consult a healthcare provider.

Storage

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

Formulations

• Liquid paraffin
• Soft paraffin

Indications

• Used as an acidulant in food and beverages
• Utilized in pharmaceutical formulations to enhance stability
• Serves as a buffering agent in various preparations

Dosage

Children: Refer to specific formulation guidelines for dosage; no standard dose established.

Adults: Refer to specific formulation guidelines for dosage; no standard dose established.

Mechanism of action

Tartaric acid acts primarily as a mild acid, contributing to the acidity of solutions and influencing the solubility and stability of compounds. It can also play a role in stabilizing the pH of formulations, which can enhance the bioavailability of specific drugs. The precise molecular interactions of tartaric acid in biological systems are not fully elucidated but involve the modulation of pH and ionic strength.

Pharmacodynamics

Tartaric acid does not exhibit significant pharmacological activity on its own but influences the properties of other compounds when used in pharmaceutical preparations. Its role as an acidulant can enhance the solubility of certain drugs, thereby improving their absorption and therapeutic efficacy. The acid's buffering capacity can also help maintain a stable environment for drug stability.

Pharmacokinetics

Tartaric acid is absorbed in the gastrointestinal tract, although specific pharmacokinetic parameters such as half-life, peak plasma concentration, and elimination pathways are not well-defined in the literature. It is generally metabolized in the body to various metabolites, primarily through normal metabolic pathways, with renal excretion of its conjugates. Its effects are more related to its role in formulations rather than systemic pharmacodynamics.

Pregnancy

Tartaric acid is generally recognized as safe when used in food and beverages. However, specific safety during pregnancy has not been extensively studied, thus caution is advised.

Breast-feeding

There is limited information on the safety of tartaric acid during breastfeeding, but it is considered to be safe in normal dietary amounts.

Storage

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

Formulations

• Tartaric acid powder
• Tartaric acid solution

Indications

• Immunological disorders
• Infections (bacterial and fungal)
• Inflammatory conditions

Dosage

Children: Refer to BNF for Children for specific dosages pertinent to paediatric patients.

Adults: Refer to BNF for specific dosages, as they can vary based on indication and formulation.

Mechanism of action

Thymol modulates macrophage activity by enhancing phagocytosis and increasing the proliferation of splenocytes, acting as a mitogen. It improves macrophage uptake capacity through increased membrane fluidity and enhances lysosomal activity. Thymol also stimulates the respiratory burst in macrophages, leading to increased generation of superoxide anions. Additionally, it shows anti-inflammatory effects by decreasing the secretion of pro-inflammatory cytokines such as TNF-alpha, IL-1beta, and PGE(2).

Pharmacodynamics

Thymol exhibits various pharmacodynamic effects including antimicrobial, antifungal, and immunomodulatory activities. Its ability to enhance macrophage function suggests a role in boosting the immune response, potentially benefiting conditions characterized by immune dysfunction. The compound also demonstrates antioxidant properties, contributing to its anti-inflammatory effects.

Pharmacokinetics

The pharmacokinetic profile of thymol is not fully characterized; however, it is known to be readily absorbed and distributed in the body due to its lipophilic nature. Metabolism occurs in the liver, with excretion primarily through the urine. The exact half-life and elimination pathways require further investigation to provide a comprehensive overview.

Pregnancy

There is insufficient data on the use of thymol during pregnancy. Caution is advised.

Breast-feeding

Limited information is available regarding the excretion of thymol in human milk. Caution is recommended.

Storage

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

Indications

• Musculoskeletal pain
• Arthritis
• Tendinitis
• Back pain
• Muscle strains and sprains

Dosage

Children: Refer to the BNF for Children for specific dosing guidelines.

Adults: Apply to the affected area, usually 3 to 4 times daily as needed, ensuring not to exceed the recommended amount.

Mechanism of action

Counter-irritation is thought to be effective at alleviating musculoskeletal pain as the irritation of the sensory nerve endings alters or offsets pain in the underlying muscle or joints served by the same nerves. When applied topically, methyl salicylate penetrates the skin and underlying tissues, where it reversibly inhibits cyclooxygenase enzyme and prevents the production of inflammatory mediators such as prostaglandin and thromboxane A2.

Pharmacodynamics

Methyl salicylate relieves musculoskeletal pain in muscles, joints, and tendons by causing irritation and reddening of the skin due to dilated capillaries and increased blood flow. It acts as a rubefacient and skin irritant, providing a soothing sensation of warmth. Its pharmacological profile is similar to that of aspirin and other NSAIDs.

Pharmacokinetics

Methyl salicylate is absorbed through the skin upon topical application, where it exerts its effects locally. It undergoes metabolism primarily in the liver, and its metabolites are excreted via urine. The onset of action is relatively rapid, given the local application.

Adverse effects

• Skin irritation
• Allergic reactions
• Burning sensation at the application site

Precautions

• Avoid contact with eyes and mucous membranes
• Do not apply to broken or irritated skin
• Use with caution in patients with sensitive skin or allergies

Pregnancy

Data on the safety of wintergreen during pregnancy is limited. Consult a healthcare professional before use.

Breast-feeding

Limited data available; consult a healthcare professional before use.

Storage

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

Formulations

• Topical ointment
• Topical gel
• Liniment

Mechanism of action

Capsaicin has been shown to reduce the amount of substance P associated with inflammation - however this is not believed to be its main mechanism in the relief of pain. Capsaicin's mechanism of action is attributed to "defunctionalization" of nociceptor fibers by inducing a topical hypersensitivity reaction on the skin. This alteration in pain mechanisms is due to many of the following: temporary loss of membrane potential, inability to transport neurotrophic factors leading to altered phenotype, and reversible retraction of epidermal and dermal nerve fiber terminals. Capsaicin, the pungent constituent of chili peppers, represents the paradigm for the capsaicinoids or vanilloids, a family of compounds shown to stimulate and then desensitize specific subpopulations of sensory receptors, including C-polymodal nociceptors, A-delta mechanoheat nociceptors and warm receptors of the skin, as well as enteroceptors of thin afferent fibers. ... ... In rats desensitized by intraperitoneal (ip) capsaicin (i.e., abdominal non-systemic desensitization), mainly the first but not the later fever phases were reduced. The postprandial hyperthermia to intragastric injection of BaSO4 suspension was attenuated by either ip or perineural capsaicin treatment. ... Heat and protons as well as capsaicin activate VR1 to induce the influx of cations, particularly Ca2+ and Na+ ions. Characteristic effects of capsaicin are the induction of a burning sensation after acute administration and the desensitization of sensory neurons after large doses and prolonged administration. ... Capsaicin alters several visceral functions. ... Capsaicin affects thermoregulation after intra-hypothalamic injection and releases glutamate from the hypothalamus and cerebral cortex slices, while VR1-like immunoreactivity is not apparent in these regions. ... 0.4 and 4 uM of capsaicin produced a significant tonic block on voltage-activated Na+ current (I(Na)) evoked by a depolarizing step to -40 mV from a holding potential of -100 mV (49 +/- 7% n=11, p<0.05 and 72 +/- 13% n=4, p<0.05 respectively). ... Capsaicin slowed the time decay of inactivation of I(Na), and increased the time constant of the recovery of inactivation. Capsaicin and tetrodotoxin (TTX) depressed contractility of isolated electrically driven left rat atria, being the depression of maximal velocity of force development (dF/dt(max)) with respect to control values of 19 +/- 3% at 1 uM of capsaicin and 22 +/- 2% at 1 uM of TTX. For more Mechanism of Action (Complete) data for CAPSAICIN (8 total), please visit the HSDB record page.

Pharmacodynamics

Capsaicin is a TRPV1 receptor agonist. TRPV1 is a trans-membrane receptor-ion channel complex activated by temperatures higher than 43 degrees Celsius, pH lower than 6, and endogenous lipids. When activated by a combination of these factors, the channel can transiently open and initiate depolarization due to the influx of calcium and sodium ions. Because TRPV1 is commonly expressed in A-delta and mostly C fibers, depolarization results in action potentials which send impulses to the brain and spinal cord. These impulses result in capsaicin effects of warming, tingling, itching, stinging, or burning. Capsaicin also causes more persistent activation of these receptors compared to the environmental agonists, resulting in a loss of response to many sensory stimuli, described as "defunctionalization". Capsaicin is associated with many enzymatic, cytoskeletal, and osmotic changes, as well as disruption of mitochondrial respiration, impairing nociceptor function for extended periods of time.

Mechanism of action

Benzyl alcohol inhibits lice from closing their respiratory spiracles, allowing the vehicle to obstruct the spiracles and causing the lice to asphyxiate.

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/

Mechanism of action

The potent role of thymol, a natural compound, in modulation of macrophage activity was evaluated by determining all the sequential steps involved during phagocytosis. We found a significant increase in the proliferation of splenocytes in the presence of thymol and it proved to be a good mitogen. Uptake capacity of macrophages was enhanced due to increased membrane fluidity after treatment with thymol and it also increases lysosomal activity of macrophages. Data of superoxide anion generation revealed the involvement of thymol in the generation of respiratory burst as it potentiated this property of macrophages at a concentration of 150 uM. In the case of TNF-a, IL-1beta and PGE(2) a decreased level of secretion was observed 154 pg/mL, 736.1 pg/mL, and 151 pg/mL respectively when compared with lipopolysaccharide treated cells, where the level of these cytokines was significantly high. We also determined the anti-complementary activity of thymol which showed to be more effective than rosmarinic acid. Thus, the results obtained from the study suggest the potential role of thymol as a natural immunostimulatory drug which can be used in the treatment of various immunological disorders.

Mechanism of action

Counter-irritation is thought to be effective at alleviating musculoskeletal pain as the irritation of the sensory nerve endings is thought to alter or offset pain in the underlying muscle or joints that are served by the same nerves. This is thought to mask the underlying musculoskeletal pain and discomfort. When applied topically, methyl salicylate is thought to penetrate the skin and underlying tissues where it reversibly inhibits cyclooxygenase enzyme and locally and peripherally prevents the production of inflammatory mediators such as prostaglandin and thromboxane A2.

Pharmacodynamics

Methyl salicylate relieve musculoskeletal pain in the muscles, joints, and tendons by causing irritation and reddening of the skin due to dilated capillaries and increased blood flow. It is pharmacologically similar to aspirin and other NSAIDs but as a topical agent it primarily acts as a rubefacient and skin irritant. Counter-irritation is believed to cause a soothing sensation of warmth.