gumex

Indications

• Rectal and anal disorders
• Haemorrhoids
• Pruritus ani

Dosage

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

Adults: For rectal use using aerosol spray: 1 spray up to 3 times a day for no longer than 7 days without medical advice. For ointment: apply several times daily, for short-term use only.

Mechanism of action

Phenol exerts its effects by acting as a potent proteolytic agent. At concentrations of 5% to 7%, it can dissolve tissue through proteolysis. When injected near a nerve, it produces chemical neurolysis, affecting nerve fibers nonselectively. Local anesthetic effects are typically observed within 5 to 10 minutes of application.

Pharmacodynamics

Phenol's pharmacodynamic properties include its ability to cause tissue dissolution and local anesthesia. The local anesthetic effects result from its action on the nerve fibers, leading to a temporary loss of sensation in the affected area. The proteolytic action can assist in the treatment of various skin and mucosal conditions by facilitating tissue breakdown.

Pharmacokinetics

Phenol is absorbed through mucosal surfaces when applied locally. Its metabolism involves biological oxidation and phase I functionalization, primarily through cytochrome P450 enzymes. The elimination of phenol occurs through metabolic pathways, and it can be detected in urine as a result of its metabolism.

Contra-indications

• Infection
• Known hypersensitivity to phenol or its components

Adverse effects

• Local irritation
• Burning sensation
• Paraesthesia
• Vision disorders
• Skin reactions
• Adrenal suppression

Interactions

• Caution with other local anesthetics due to potential additive effects

Precautions

• Use for short periods only-no longer than a few days
• Avoid excessive application, especially on sensitive areas
• Consult product literature for specific guidelines

Pregnancy

Data on the use of phenol during pregnancy is limited; caution is advised.

Breast-feeding

Limited information available; caution is recommended when used in breastfeeding mothers.

Storage

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

Formulations

• Ointment
• Suppository
• Aerosol spray

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

• 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

• Constipation
• Decreased intraocular pressure

Dosage

Children: For children, refer to the BNF for Children for appropriate glycerin dosing guidelines.

Adults: For constipation, glycerin can be administered rectally as a suppository. Follow specific product guidelines for dosage.

Mechanism of action

When administered rectally, glycerine exerts a hygroscopic and/or local irritant action, drawing water from the tissues into the feces and reflexively stimulating evacuation. Additionally, glycerine decreases intraocular pressure by creating an osmotic gradient between the blood and intraocular fluid, leading to fluid movement out of the aqueous and vitreous humors into the bloodstream.

Pharmacodynamics

Glycerine is commonly classified as an osmotic laxative but may also exert local irritant effects, lubricating, and fecal softening actions. Its onset of action typically occurs within 15 to 30 minutes when used as a suppository.

Pharmacokinetics

Glycerine is readily absorbed and metabolized in the body. It undergoes glycerol metabolism pathways, contributing to various biochemical processes including phospholipid biosynthesis. The pharmacokinetic profile of glycerine indicates a rapid onset of action due to its osmotic properties.

Adverse effects

• Abdominal cramps
• Diarrhea
• Nausea
• Vomiting
• Electrolyte imbalance

Precautions

• Use with caution in patients with renal impairment
• May cause dehydration if used excessively
• Monitor for electrolyte disturbances in prolonged use

Pregnancy

Glycerin is generally considered safe to use during pregnancy for indicated conditions. Always consult a healthcare provider before use.

Breast-feeding

Glycerin is unlikely to be harmful in breastfeeding mothers. Consult a healthcare provider for specific guidance.

Storage

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

Formulations

• Suppositories
• Oral solution

Indications

• Iodine deficiency
• Hypothyroidism
• Goiter
• Thyroiditis

Dosage

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

Adults: Refer to the BNF for specific dosing information.

Mechanism of action

Iodide functions as a substrate for the synthesis of thyroid hormones. It undergoes metabolism through various pathways, including thyroid hormone metabolism via conjugation and degradation, deiodination, and biosynthesis. In the thyroid gland, iodide is actively transported into cells where it is oxidized to iodine, which then combines with the amino acid tyrosine to form T3 and T4, essential hormones for metabolic regulation.

Pharmacodynamics

Iodide is crucial for maintaining thyroid hormone levels in the body. Adequate iodide levels are necessary to prevent hypothyroidism and associated conditions such as goiter. The pharmacodynamic effects include modulation of metabolic processes, enhancement of growth and development, and regulation of energy expenditure. Insufficient iodide can lead to decreased thyroid hormone production and subsequent metabolic disturbances.

Pharmacokinetics

Iodide is absorbed from the gastrointestinal tract and is distributed throughout the body, particularly accumulating in the thyroid gland. The half-life of iodide in the serum is approximately 10-20 days, depending on dietary intake and physiological status. It is excreted primarily through the kidneys. The bioavailability of iodide can be influenced by various factors, including the presence of certain food components and the overall dietary iodide intake.

Pregnancy

Iodide is generally considered safe during pregnancy when used in appropriate doses, as it is essential for fetal thyroid function.

Breast-feeding

Iodide is excreted in breast milk, but it is usually safe in normal dietary amounts.

Storage

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

Indications

• Iodine deficiency
• Goiter
• Hypothyroidism
• Thyroiditis
• Fibrocystic breast disease

Dosage

Children: Refer to the BNF for Children for appropriate dosing guidelines based on age and weight.

Adults: Refer to the BNF for appropriate dosing guidelines based on condition and clinical judgment.

Mechanism of action

Molecular iodine inhibits the induction and promotion of carcinogenesis in mammary tissues and has shown beneficial effects in fibrocystic breast disease. It temporarily decreases thyroid hormone production through the acute Wolff-Chaikoff effect, followed by a return to normal hormone synthesis due to down regulation of the sodium-iodide symport. This mechanism can lead to a transient hypothyroid state in some individuals with underlying thyroid conditions.

Pharmacodynamics

Iodine is vital for the synthesis of thyroid hormones thyroxine (T4) and triiodothyronine (T3). It affects the metabolism of amine-derived hormones and plays a role in amino acid metabolism. The acute excess of iodide can lead to decreased circulating levels of T4 and T3 in susceptible individuals, while most people can escape this effect and maintain normal thyroid function.

Pharmacokinetics

Iodine is absorbed primarily in the gastrointestinal tract and is distributed throughout the body, particularly in the thyroid gland, where it is concentrated for hormone synthesis. The kidney plays a significant role in the excretion of excess iodine. The half-life of iodine in the body varies and can be influenced by dietary intake and underlying health conditions.

Adverse effects

• Hypothyroidism
• Hyperthyroidism
• Iodine allergy
• Gastrointestinal disturbances

Interactions

• Thyroid hormones
• Antithyroid drugs
• Lithium
• Diuretics

Precautions

• Use with caution in patients with thyroid dysfunction
• Monitor thyroid function periodically during treatment
• Pregnant or breastfeeding women should consult a healthcare provider before use

Pregnancy

Iodine is essential for fetal thyroid hormone synthesis, but excessive iodine intake should be avoided.

Breast-feeding

Iodine is excreted in breast milk; consult a healthcare provider regarding supplementation.

Storage

Store in a cool, dry place away from light.

Formulations

• Iodine solution
• Iodine tincture
• Potassium iodide tablets

Indications

• Digestive issues
• Nausea
• Headaches
• Muscle pain
• Respiratory conditions such as cough and nasal congestion

Dosage

Children: Refer to specific formulations and product guidelines for pediatric dosing, as formulations may vary and should be used with caution in children.

Adults: Refer to specific formulations and product guidelines for dosing, as mentha is available in various forms including teas, extracts, and topical applications.

Mechanism of action

Mentha species contain essential oils, primarily menthol and menthone, which exert their effects through several mechanisms. Menthol acts as a competitive antagonist of the transient receptor potential cation channel subfamily M member 8 (TRPM8), which is involved in the sensation of cold. This interaction provides a cooling sensation and can help alleviate pain. Additionally, menthol has been shown to have antispasmodic effects on smooth muscle, which may contribute to its use in digestive disorders.

Pharmacodynamics

The pharmacodynamic properties of mentha are attributed to its active constituents, particularly menthol. It exhibits analgesic, anti-inflammatory, and antispasmodic effects. The cooling sensation produced by menthol can also trigger the release of endorphins, which may enhance its analgesic properties. Furthermore, menthol can increase local blood flow, which aids in the relief of muscle tension and pain.

Pharmacokinetics

Mentha's pharmacokinetics can vary based on the method of administration (oral, topical, or inhalation). When ingested, menthol is rapidly absorbed in the gastrointestinal tract and metabolized in the liver. Peak plasma concentrations are usually achieved within 30 to 60 minutes. The elimination half-life of menthol is approximately 2 to 4 hours. Topically applied menthol may provide localized effects with minimal systemic absorption, reducing the risk of systemic side effects.

Adverse effects

• Allergic reactions
• Heartburn
• Nausea
• Vomiting
• Skin irritation

Interactions

• May interact with anticoagulants
• May affect the absorption of certain medications due to its effects on gastrointestinal motility

Precautions

• Use with caution in individuals with gastroesophageal reflux disease (GERD)
• Caution in patients with liver disease
• Avoid use in infants and young children due to potential respiratory issues

Pregnancy

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

Breast-feeding

Mentha is likely safe in food amounts during breastfeeding, but high doses should be avoided due to potential effects on milk supply and infant health.

Storage

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

Formulations

• Essential oil
• Tea
• Extracts
• Capsules

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

• Diarrhea
• Wound healing
• Topical treatment of skin irritations
• As astringent for mucosal surfaces
• Antioxidant supplementation

Dosage

Children: Paediatric dosing has not been established; consult specific guidelines or a healthcare professional.

Adults: Dosing varies depending on the form and indication. Generally, refer to specific preparation guidelines for appropriate dosing.

Mechanism of action

Tannic acid exerts its effects through the formation of complexes with proteins, leading to the precipitation of proteins and astringency. This mechanism is thought to contribute to its anti-inflammatory and wound-healing properties. Additionally, its antioxidant activity may help reduce oxidative stress by scavenging free radicals.

Pharmacodynamics

The pharmacodynamic effects of tannic acid include its astringent action, which can lead to tissue contraction and reduced secretions. Its anti-inflammatory properties may be attributed to the inhibition of pro-inflammatory cytokines and enzymes, thereby modulating the inflammatory response. The antioxidant role of tannic acid also plays a significant part in protecting cells from oxidative damage.

Pharmacokinetics

Tannic acid is poorly absorbed in the gastrointestinal tract when taken orally, which limits its systemic effects. Its bioavailability is low, and it primarily acts locally in the gastrointestinal system. The metabolism of tannic acid involves hydrolysis into smaller phenolic compounds, which may exert various biological effects. The elimination pathways are not well-defined, but it is likely excreted in urine in conjugated forms.

Adverse effects

• Nausea
• Vomiting
• Abdominal pain
• Constipation
• Diarrhea

Interactions

• May interfere with the absorption of certain medications, especially iron supplements and tetracycline antibiotics

Precautions

• Use with caution in patients with gastrointestinal disorders
• Monitor for potential allergic reactions in sensitive individuals

Pregnancy

Limited data available; consult healthcare provider before use.

Breast-feeding

Limited data available; consult healthcare provider before use.

Storage

Store in a cool, dry place away from light.

Formulations

• Oral tablets
• Powder for oral solution
• Topical preparations

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.

Dosage

Children: Refer to specific drug guidelines for pediatric dosing based on the units of measurement applicable to that drug.

Adults: Refer to specific drug guidelines for dosing based on the units of measurement applicable to that drug.

Mechanism of action

The mechanism of action for any drug labeled as a 'unit' would depend on the specific drug in question. Generally, a unit may refer to the potency of a drug, indicating how much of a drug is required to produce a therapeutic effect. For example, insulin units refer to the amount of insulin needed to lower blood glucose levels effectively.

Pharmacodynamics

Pharmacodynamics relates to the effects of a drug on the body. For drugs measured in units, pharmacodynamics can vary significantly. For instance, in the case of insulin, it acts by facilitating the uptake of glucose into cells, thereby reducing blood sugar levels. The relationship between dose (measured in units) and effect can be described by dose-response curves.

Pharmacokinetics

Pharmacokinetics encompasses the absorption, distribution, metabolism, and excretion of drugs. The pharmacokinetic profile of a drug measured in units will depend on the specific drug. For example, insulin is rapidly absorbed after subcutaneous injection, with a peak effect typically occurring within 1 to 3 hours, and it is metabolized primarily in the liver and kidneys.

Pregnancy

Consult healthcare professional, as safety data may be limited.

Breast-feeding

Consult healthcare professional, as safety data may be limited.

Storage

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

Mechanism of action

Phenol is a potent proteolytic agent. Concentrations in the 5% to 7% range dissolve tissue on contact via proteolysis. In high concentrations when injected next to a nerve, phenol produces a chemical neurolysis which is nonselective across nerve fiber size and most prominent on its outer aspect. Local anesthetic effects occur within 5-10 minutes. The effects of monoamine depletors and monoamine denervators on phenol induced tremor were studied in mice. The tremor induced by phenol was enhanced by pretreatment with reserpine or tetrabenazine, but not with syrosingopine. However, alpha-methyl-p-tyrosine, p-chlorophenylalanine or 6-hydroxydopamine did not affect the tremor. These results suggest that the depletion of central monoamines as a whole contribute to the enhancement of the tremor induced by phenol.

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.

Mechanism of action

When administered rectally, glycerin exerts a hygroscopic and/or local irritant action, drawing water from the tissues into the feces and reflexively stimulating evacuation. Glycerin decreases intraocular pressure by creating an osmotic gradient between the blood and intraocular fluid, causing fluid to move out of the aqueous and vitreous humors into the bloodstream. Glycerin (glycerol) and sorbitol are hyperosmotic laxatives. When administered rectally, glycerin and sorbitol exert a hygroscopic and/or local irritant action, drawing water from the tissues into the feces and reflexly stimulating evacuation. The extent to which the simple physical distention of the rectum and the hygroscopic and/or local irritant actions are responsible for the laxative effects of some of these drugs is not known. Only extremely high oral doses of sorbitol (25 g daily) or glycerin exert laxative action. /Glycerin/ decreases intraocular pressure by creating an osmotic gradient between the blood and intraocular fluid, causing fluid to move out of the aqueous and vitreous humors into the bloodstream. The physicochemical effects of a series of alkanols, alkanediols and glycerol on erythrocyte shape and hemolysis at 4 and 20 degrees C were examined. We calculated the dielectric constant of the incubation medium, Ds, and the dielectric constant of the erythrocyte membrane Dm in the presence of organic solutes. The ratio Ds/Dm = -38.48 at 20 degrees C defines the normal biconcave shape in a medium without hemolytic agents. A decrease in Ds/Dm favors externalization or internalization with consequent hemolysis. Alkanols and alkanediols convert biconcave erythrocytes into echinocytes, which is accompanied by an increase in the projected surface area. Glycerol converts biconcave erythrocytes into stomatocytes, which was accompanied by a marginal decrease in the projected surface area. Progressive externalization in alkanols and alkanediols or internalization in glycerol resulted in a decrease in the projected surface area and the formation of smooth spheres. The degree of shape change induced was related to the degree of hemolysis and the ratio Ds/Dm. A decrease in temperature reduced both the degree of shape change and hemolysis. .../Thus/ physicochemical toxicity may be a result of a temperature dependent hydrophobic interaction between the organic solutes and the membrane and is best interpreted by the ability of the solutes to change Ds and Dm.

Pharmacodynamics

Glycerin is commonly classified as an osmotic laxative but may act additionally or alternatively through its local irritant effects; it may also have lubricating and fecal softening actions. Glycerin suppositories usually work within 15 to 30 minutes.

Mechanism of action

Molecular iodine is known to inhibit the induction and promotion of N-methyl-n-nitrosourea-induced mammary carcinogenesis, to regress 7,12-dimethylbenz(a)anthracene-induced breast tumors in rats.It has also been shown to have beneficial effects in fibrocystic human breast disease. An acute iodide excess (above the preexisting dietary intake) transiently decreases the production of thyroid hormones in the thyroid gland; this is referred to as the acute Wolff-Chaikoff effect. In normal people, this is followed by a return to normal levels of hormone synthesis, referred to as escape from the acute Wolff-Chaikoff effect, without a significant change in circulating hormone levels. Escape is thought to be the result of down regulation of the sodium-iodide symport (NIS), the iodide transporter in the thyroid gland, resulting in a decrease in the intrathyroidal iodine and the resumption of normal hormone synthesis. An acute or chronic excess of iodide can also decrease circulating T4 and T3 levels and induce a hypothyroid state in some people who have underlying thyroid disorders. These effects are the result of a failure to escape from the acute Wolff-Chaikoff effect. Most people who experience iodine-induced hypothyroidism recover when the excess iodine intake is discontinued.

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.