Vapour Rub

Indications

• Pruritus
• Eczema
• Acne
• Rosacea

Dosage

Children: For children aged 12-17 years, apply up to 3 grams 3-4 times a day, ensuring coverage is less than 10% of body surface area.

Adults: Apply thinly to the affected area 1-2 times a day. Maximum application should cover less than 10% of body surface area, with a total daily maximum of 12 grams.

Mechanism of action

Levomenthol primarily activates the cold-sensitive TRPM8 receptors in the skin. This stimulation leads to a feeling of coolness by inhibiting calcium ion currents in neuronal membranes. Additionally, menthol may exhibit analgesic properties through kappa-opioid receptor agonism, further contributing to its pain-relieving effects.

Pharmacodynamics

Levomenthol is a covalent organic compound that can be synthesized or extracted from peppermint and other mint oils. It induces a cooling sensation when applied topically, inhaled, or ingested, by stimulating cold-sensitive receptors located in the skin. Notably, this effect occurs without a decrease in actual skin temperature, making it useful in topical formulations for managing discomfort.

Pharmacokinetics

Levomenthol is absorbed through the skin upon topical application. Its effects are localized, and it does not significantly enter systemic circulation when used as directed. The onset of action is typically rapid, providing immediate symptomatic relief from conditions like itching and irritation.

Contra-indications

• Severe heart disease
• Severe hepatic impairment
• Glaucoma
• Urinary retention
• History of mania or arrhythmias

Adverse effects

• Drowsiness
• Dizziness
• Headache
• Nausea
• Vomiting
• Dry mouth
• Dry eyes
• Diarrhea
• Constipation
• Skin reactions
• Altered taste
• Blurred vision
• Suicidal behaviors

Interactions

• Tricyclic antidepressants
• Other central nervous system depressants

Precautions

• Avoid application to large areas of the skin
• Use caution in patients with a history of psychiatric disorders
• Caution advised for driving and skilled tasks due to potential somnolence or dizziness

Pregnancy

Manufacturer advises use only if potential benefit outweighs risk.

Breast-feeding

Manufacturer advises use only if potential benefit outweighs risk.

Storage

Store in a cool, dry place, protected from light.

Formulations

• AquaSoothe 1% cream (Menthol 10 mg per 1 gram)
• AquaSoothe 2% cream (Menthol 20 mg per 1 gram)
• Arjun 0.5% cream (Menthol 5 mg per 1 gram)
• Arjun 1% cream (Menthol 10 mg per 1 gram)
• Dermacool 0.5% cream (Menthol 5 mg per 1 gram)
• Dermacool 1% cream (Menthol 10 mg per 1 gram)
• Menthoderm 0.5% cream (Menthol 5 mg per 1 gram)
• Menthoderm 1% cream (Menthol 10 mg per 1 gram)
• Menthoderm 2% cream (Menthol 20 mg per 1 gram)
• Menthoderm 5% cream (Menthol 50 mg per 1 gram)

Indications

• Topical pain relief
• Muscle aches
• Joint pain
• Inflammation

Dosage

Children: For children, the

Adults: For topical application, camphor is usually applied as needed to the affected area, following the instructions on the specific product used. Consult the product label or a healthcare professional for detailed dosing guidelines.

Mechanism of action

Camphor activates the transient receptor potential vanilloid 1 (TRPV1) and TRPV3 channels, which are involved in sensing pain and temperature. It requires higher concentrations to activate TRPV1 compared to capsaicin but notably desensitizes TRPV1 more rapidly and completely. This action is enhanced under inflamed conditions through phospholipase C-coupled receptor stimulation. The distinct activation pathways of camphor contribute to its analgesic effects, making it effective in reducing pain sensitivity.

Pharmacodynamics

The pharmacodynamic properties of camphor are primarily related to its interaction with TRPV1 and TRPV3 channels. By activating these receptors, camphor induces a sensation of warmth and can result in analgesia through sensory nerve excitation and subsequent desensitization. This mechanism is similar to that of other topical analgesics like capsaicin and menthol but is characterized by a faster desensitization of TRPV1. Additionally, camphor's effects may include local vasodilation and increased blood flow to the area of application, which can further alleviate pain and inflammation.

Pharmacokinetics

Camphor is absorbed through the skin when applied topically. Its pharmacokinetic profile involves distribution to various tissues, where it can exert local effects. The metabolism of camphor occurs primarily in the liver, and it is eliminated from the body mainly through urine. The onset of action is typically rapid due to its topical application, and the duration of effect may vary depending on the formulation and concentration used.

Adverse effects

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

Precautions

• Use with caution in individuals with sensitive skin
• Avoid contact with eyes and mucous membranes
• Do not apply to broken or irritated skin
• Keep out of reach of children

Pregnancy

Camphor should be used with caution during pregnancy. It is advisable to consult a healthcare professional before use.

Breast-feeding

Camphor should be used with caution while breastfeeding. Consult a healthcare professional for advice.

Storage

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

Formulations

• Topical ointments
• Liniments
• Creams
• Gels

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)

Dosage

Children: Refer to specific product guidelines for dosing, as formulations vary widely.

Adults: Refer to specific product guidelines for dosing, as formulations vary widely.

Mechanism of action

The mechanism of action for jelly formulations as drug carriers involves the physical properties of gelatin, which can encapsulate active ingredients, allowing for controlled release and enhanced bioavailability. This can facilitate the absorption of drugs when used topically or as part of a gastrointestinal formulation.

Pharmacodynamics

The pharmacodynamics of jelly formulations can vary widely depending on the active ingredients they contain. Generally, jellies provide a moist environment that can enhance the absorption of drugs through mucosal membranes. The viscosity and gel structure can also influence the release rate of the active compound, potentially leading to prolonged therapeutic effects.

Pharmacokinetics

The pharmacokinetics of jelly formulations will depend largely on their composition and the active pharmaceutical ingredients they contain. For topical jellies, absorption through the skin may occur, while oral jellies can undergo digestion before reaching systemic circulation. Factors such as the molecular weight of the drug, the presence of enhancers, and the formulation's pH can all impact absorption rates and bioavailability.

Pregnancy

Safety during pregnancy has not been established. Consult a healthcare provider for advice.

Breast-feeding

Consult a healthcare provider before using during breastfeeding.

Storage

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

Indications

• Dry skin
• Chapped lips
• Minor skin irritations
• Eczema
• Psoriasis
• Protection of minor cuts and abrasions

Dosage

Children: Apply as needed to affected area, typically 1-3 times daily depending on the severity of the condition.

Adults: Apply as needed to affected area, typically 1-3 times daily depending on the severity of the condition.

Mechanism of action

Petroleum acts as an occlusive agent when applied to the skin, creating a barrier that reduces water evaporation. This helps to maintain skin hydration and protect damaged or irritated skin. The hydrocarbons in petroleum can also have a soothing effect on the skin and may help in the healing of minor abrasions.

Pharmacodynamics

The primary pharmacodynamic action of petroleum is its ability to form a protective film over the skin, which aids in moisture retention. It does not penetrate deeply into the skin and primarily acts at the stratum corneum level. This mechanism makes it effective for treating dry skin conditions and preventing transepidermal water loss.

Pharmacokinetics

Petroleum is not systemically absorbed through the skin when used topically, hence it has a low bioavailability. Its effects are localized to the area of application. The onset of action is immediate upon application, and the duration of effect can last for several hours, depending on the surface area covered and the amount applied.

Adverse effects

• Skin irritation
• Allergic reactions
• Gastrointestinal disturbances if ingested

Precautions

• Avoid contact with open wounds or mucous membranes
• Use with caution in patients with a history of skin sensitivities

Pregnancy

Considered safe when used topically, but ingestion should be avoided.

Breast-feeding

Generally regarded as safe for topical use, but ingestion should be avoided.

Storage

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

Formulations

• Topical ointments
• Creams
• Lotions

Dosage

Children: Refer to the BNF for Children or specific drug guidelines for appropriate paediatric dosing.

Adults: Refer to the specific drug formulation for appropriate dosing guidelines, as racemic mixtures encompass a wide range of drugs with varying indications and dosing regimens.

Mechanism of action

The mechanism of action of racemic mixtures depends on the specific drug in question. Generally, enantiomers can interact differently with biological targets such as receptors, enzymes, and transporters, leading to varied pharmacological effects. One enantiomer may have a stronger affinity for a receptor or may activate a different signaling pathway than the other.

Pharmacodynamics

Pharmacodynamics of racemic drugs can be complex, given that the two enantiomers may exert different actions. Typically, one enantiomer may be responsible for the desired therapeutic effect, while the other may contribute to side effects or have no effect at all. The overall effect of a racemic mixture will depend on the relative potency and efficacy of each enantiomer.

Pharmacokinetics

The pharmacokinetics of racemic mixtures can vary based on the enantiomers' absorption, distribution, metabolism, and excretion (ADME) properties. Differences in these properties can lead to discrepancies in plasma concentration levels and half-lives of the enantiomers. It is essential to evaluate the pharmacokinetics of each enantiomer individually, as one may be metabolized more quickly or have a different volume of distribution than the other.

Pregnancy

Data on the safety of racemic mixtures during pregnancy is limited. Caution is advised, and usage should only be considered if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

It is not known if racemic mixtures are excreted in human milk. Caution is advised when administering to nursing mothers.

Storage

Store in a cool, dry place, away from direct light and moisture. Ensure that the medication is kept out of reach of children.

Indications

• Local antiseptic
• Irritant for mucous membranes
• Traditional medicinal uses

Dosage

Children: Refer to established guidelines and clinical practice for specific dosages, as turpentine is not commonly used in modern medicine.

Adults: Refer to established guidelines and clinical practice for specific dosages, as turpentine is not commonly used in modern medicine.

Mechanism of action

Turpentine acts as a local irritant, leading to increased blood flow and inflammatory response in tissues. It may also exert some antimicrobial effects, although the exact pathways are not well defined. The main active components are terpenes, which can affect cellular membranes and interfere with microbial function.

Pharmacodynamics

Turpentine exhibits irritant properties, resulting in stimulation of sensory nerves and local inflammatory responses. It may also have some systemic effects when absorbed, which can lead to toxicity if ingested or inhaled in large amounts. The pharmacological effects are primarily due to its terpene content, which can impact various biological pathways.

Pharmacokinetics

Turpentine is rapidly absorbed through mucous membranes and skin. It is metabolized in the liver, where it undergoes oxidation and conjugation. The metabolites are primarily excreted via the urine. Due to its volatile nature, turpentine can also be inhaled, leading to rapid absorption into the bloodstream. The half-life of turpentine varies based on the method of exposure and individual metabolism.

Contra-indications

• Hypersensitivity to turpentine or any component of the formulation
• Pregnancy and lactation due to potential harmful effects

Adverse effects

• Skin irritation or dermatitis upon topical application
• Gastrointestinal disturbances such as nausea, vomiting, and diarrhea
• Respiratory irritation from inhalation
• Central nervous system effects including headache, dizziness, and confusion
• Kidney damage with prolonged exposure or high doses

Interactions

• May interact with other CNS depressants, increasing sedation
• Potentially enhances the effects of certain medications metabolized by the liver

Precautions

• Use with caution in individuals with pre-existing respiratory conditions
• Should not be ingested or applied to broken skin
• Avoid inhalation of vapors

Pregnancy

Not recommended. Potentially harmful effects on the fetus have been reported.

Breast-feeding

Not recommended. Potential for excretion in breast milk and harmful effects on the infant.

Storage

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

Formulations

• Topical ointments or liniments
• Inhalation solutions
• Oral preparations (not commonly recommended due to toxicity)

Dosage

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

Adults: Refer to the specific BNF guidelines for dosing information as it may vary based on the condition being treated.

Mechanism of action

The mechanism of action for White involves its interaction with specific biological pathways, leading to the desired pharmacological effects. The precise pathways may include modulation of receptor activity or alteration of enzyme function, although specific details are not provided.

Pharmacodynamics

Pharmacodynamics of White includes its effects on the body, including therapeutic effects and potential side effects. As a compound, it may exert its influence on multiple physiological systems, which can lead to changes in symptoms or disease progression.

Pharmacokinetics

Pharmacokinetics of White involves its absorption, distribution, metabolism, and excretion. Understanding these parameters can help predict how the drug behaves in the body, including onset of action and duration of effect. Detailed pharmacokinetic data is not specified.

Mechanism of action

Menthol primarily activates the cold-sensitive TRPM8 receptors in the skin. Menthol, after topical application, causes a feeling of coolness due to stimulation of 'cold' receptors by inhibiting Ca++ currents of neuronal membranes. It may also yield analgesic properties via kappa-opioid receptor agonism.

Pharmacodynamics

Menthol is a covalent organic compound made synthetically or obtained from peppermint or other mint oils. Menthol induces a cooling sensation on the skin upon inhalation, oral ingestion, or topical application by stimulating the cold-sensitive receptors expressed on the skin, without actually causing a drop in the skin temperature.

Mechanism of action

Camphor is a naturally occurring compound that is used as a major active ingredient of balms and liniments supplied as topical analgesics. ... Capsaicin and menthol, two other topically applied agents widely used for similar purposes, are known to excite and desensitize sensory nerves by acting on two members of transient receptor potential (TRP) channel superfamily: heat-sensitive TRP vanilloid subtype 1 (TRPV1) and cold-sensitive TRP channel M8, respectively. Camphor has recently been shown to activate TRPV3, and here /investigators/ show that camphor also activates heterologously expressed TRPV1, requiring higher concentrations than capsaicin. Activation was enhanced by phospholipase C-coupled receptor stimulation mimicking inflamed conditions. Similar camphor-activated TRPV1-like currents were observed in isolated rat DRG neurons and were strongly potentiated after activation of protein kinase C with phorbol-12-myristate-13-acetate. Camphor activation of rat TRPV1 was mediated by distinct channel regions from capsaicin, as indicated by camphor activation in the presence of the competitive inhibitor capsazepine and in a capsaicin-insensitive point mutant. Camphor did not activate the capsaicin-insensitive chicken TRPV1. TRPV1 desensitization is believed to contribute to the analgesic actions of capsaicin. /The authors/ found that, although camphor activates TRPV1 less effectively, camphor application desensitized TRPV1 more rapidly and completely than capsaicin. Conversely, TRPV3 current sensitized after repeated camphor applications, which is inconsistent with the analgesic role of camphor. /Investigators/ also found that camphor inhibited several other related TRP channels, including ankyrin-repeat TRP 1 (TRPA1). The camphor-induced desensitization of TRPV1 and block of TRPA1 may underlie the analgesic effects of camphor.