TOUXSIL T

Indications

• Asthma
• Chronic Obstructive Pulmonary Disease (COPD)
• Exacerbation of reversible airways obstruction
• Prevention of exercise-induced bronchospasm
• Uncomplicated premature labor (under specialist supervision)

Dosage

Adults: Initially 2.5 mg 3 times a day for 1–2 weeks, then increased to

Mechanism of action

Terbutaline exerts its effects by selectively stimulating beta-2 adrenergic receptors located in the smooth muscle of the airways. This activation leads to the activation of adenylate cyclase, resulting in increased levels of cyclic AMP (cAMP). Elevated cAMP levels promote relaxation of the bronchial smooth muscle, leading to bronchodilation. Additionally, terbutaline may inhibit the release of mediators from mast cells, reducing bronchoconstriction and inflammation.

Pharmacodynamics

The pharmacodynamic profile of terbutaline includes rapid onset of action, typically within 5 to 15 minutes when inhaled, and a duration of action of approximately 3 to 6 hours. It provides symptomatic relief from bronchospasm associated with asthma and chronic obstructive pulmonary disease (COPD). The drug is also noted for its tocolytic effects, as it can inhibit uterine contractions, making it useful in managing premature labor.

Pharmacokinetics

Terbutaline is well absorbed following inhalation and oral administration, with peak plasma concentrations occurring within 1 to 3 hours. It exhibits a volume of distribution of approximately 3 L/kg, indicating extensive tissue distribution. The drug is metabolized primarily in the liver and has a half-life of about 3 to 5 hours. Terbutaline is excreted mainly in urine, both as unchanged drug and metabolites. Its pharmacokinetic profile may be affected by factors such as age, liver function, and concomitant medications.

Adverse effects

• Tachycardia
• Palpitations
• Tremors
• Headache
• Nausea
• Dizziness
• Hypokalemia
• Hyperglycemia

Interactions

• Beta-blockers may reduce the effectiveness of terbutaline
• Corticosteroids may enhance the effect of terbutaline
• Concomitant use with other sympathomimetics may increase cardiovascular side effects

Precautions

• Use with caution in patients with cardiovascular disorders
• Caution in patients with diabetes due to potential hyperglycemia
• Monitor potassium levels in patients at risk of hypokalemia
• Monitor for paradoxical bronchospasm

Pregnancy

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

Breast-feeding

Terbutaline is excreted in breast milk; caution should be exercised when administering to nursing mothers.

Storage

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

Formulations

• Tablets: 2.5 mg and 5 mg
• Nebuliser solution: 0.5 mg/ml
• Injection: 0.5 mg/1 ml

Indications

• Chronic obstructive pulmonary disease (COPD)
• Bronchitis
• Asthma
• Cystic fibrosis
• Post-operative respiratory complications

Dosage

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

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

Mechanism of action

Amroxol works primarily by increasing the production of surfactant in the lungs and promoting the secretion of mucus, thereby enhancing mucociliary clearance. It also has local anesthetic properties, which can provide relief from cough and irritation in the respiratory tract. The drug acts on the mucosal cells to decrease the viscosity of mucus, making it easier to expel.

Pharmacodynamics

Amroxol demonstrates mucolytic effects by hydrolyzing glycosaminoglycans and disrupting the polymeric structure of mucus. This results in the thinning of mucus, facilitating its expulsion through coughing or expectoration. Additionally, amroxol exhibits anti-inflammatory properties, which can help reduce airway inflammation associated with respiratory conditions.

Pharmacokinetics

Amroxol is absorbed rapidly from the gastrointestinal tract, reaching peak plasma concentrations within 1-2 hours after oral administration. It has a bioavailability of approximately 70%, with extensive distribution throughout body tissues, particularly in the lungs. The drug is metabolized in the liver and primarily excreted via the kidneys, with a half-life ranging from 8 to 12 hours.

Adverse effects

• Gastrointestinal disturbances
• Nausea
• Vomiting
• Diarrhea
• Headache
• Dizziness
• Skin rashes

Precautions

• Use with caution in patients with a history of peptic ulcer disease
• Not recommended for use in patients with severe hepatic or renal impairment
• Monitor for allergic reactions in patients with a history of hypersensitivity

Pregnancy

Amroxol should be used during pregnancy only if clearly needed and the benefits outweigh the risks. Consult relevant guidelines.

Breast-feeding

Amroxol is excreted in breast milk. Caution is advised when administered to breastfeeding women.

Storage

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

Formulations

• Tablets
• Syrup
• Injection

Indications

• Cough associated with colds
• Bronchitis
• Respiratory tract infections
• Allergic rhinitis-related cough
• Sinusitis

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 varies based on formulation and combination products.

Mechanism of action

Guaifenesin works by increasing the volume and reducing the viscosity of respiratory tract secretions. This action facilitates mucociliary clearance, allowing for easier expulsion of mucus from the lungs and airways. The exact biochemical pathways are not fully elucidated, but it is thought to act on the respiratory tract by irritating the gastric mucosa, leading to a reflex stimulation of respiratory secretions.

Pharmacodynamics

The pharmacodynamic effects of guaifenesin include increased mucous secretion and improved clearance of bronchial secretions. This can help alleviate cough and improve respiratory function in conditions characterized by excess mucus production. The onset of action is generally within 30 minutes to 1 hour after administration, with effects lasting for several hours.

Pharmacokinetics

Guaifenesin is well absorbed from the gastrointestinal tract, with peak plasma concentrations occurring within 1 to 2 hours after oral administration. Its metabolism primarily occurs in the liver, and it is excreted in the urine as both unchanged drug and metabolites. The elimination half-life is approximately 1 hour, which may vary based on individual factors such as age and liver function.

Adverse effects

• Nausea
• Vomiting
• Dizziness
• Headache
• Rash
• Diarrhea

Interactions

• May enhance the effects of other expectorants
• Potential interactions with alcohol, which may increase side effects

Precautions

• Should be used with caution in patients with chronic cough due to asthma or emphysema
• Not recommended for use in children under 2 years without medical advice
• May cause drowsiness or dizziness, caution advised when driving or operating machinery

Pregnancy

Guaifenesin is classified as category C. Risk cannot be ruled out, consult a healthcare provider before use.

Breast-feeding

Guaifenesin is excreted in breast milk, caution is advised, consult a healthcare provider.

Storage

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

Formulations

• Oral solution
• Tablets
• Extended-release 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

• Asthma
• Chronic Obstructive Pulmonary Disease (COPD)
• Bronchospasm

Dosage

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

Adults: Refer to specific guidelines and dosing information from authoritative sources for adult dosing, including inhalation therapy.

Mechanism of action

Rsalbutamol exerts its effects by selectively binding to beta-2 adrenergic receptors located on the smooth muscle cells of the bronchial tree. This binding activates adenylate cyclase, leading to an increase in cyclic AMP (cAMP) levels. Elevated cAMP results in the activation of protein kinase A (PKA), which subsequently inhibits the phosphorylation of myosin light chains, leading to smooth muscle relaxation and bronchodilation. Additionally, beta-2 agonists like rsalbutamol may also have anti-inflammatory effects in the airways.

Pharmacodynamics

The primary pharmacodynamic action of rsalbutamol is bronchodilation, which results in decreased airway resistance and improved airflow. The onset of action is typically within minutes when administered via inhalation, with peak effects usually observed within 1 to 2 hours. The duration of action can vary but is generally prolonged, allowing for effective management of bronchospasm in patients with reactive airway diseases.

Pharmacokinetics

Rsalbutamol is absorbed rapidly following inhalation, with a bioavailability that varies depending on the route of administration. The drug is extensively metabolized in the liver, primarily via sulfation and glucuronidation. The elimination half-life of rsalbutamol is approximately 4 to 6 hours, and it is excreted mainly in the urine as metabolites. Due to its rapid action and relatively short half-life, multiple doses may be required throughout the day for optimal management of symptoms.

Adverse effects

• Tremor
• Nervousness
• Headache
• Palpitations
• Muscle cramps
• Hypokalemia

Interactions

• Beta-blockers may reduce the effectiveness of salbutamol.
• Diuretics may potentiate hypokalemia when used with salbutamol.

Precautions

• Use with caution in patients with cardiovascular disorders.
• Patients with hyperthyroidism should be monitored closely.
• Caution is advised in patients with diabetes mellitus.

Pregnancy

Salbutamol should be used in pregnancy only if the benefits outweigh the risks.

Breast-feeding

Salbutamol is excreted in breast milk; caution is advised when administering to nursing mothers.

Storage

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

Formulations

• Inhaler
• Nebulizer solution
• Tablet
• Syrup

Indications

• Bronchospasm
• Asthma
• Chronic bronchitis
• Emphysema

Dosage

Children: Refer to the BNF for Children for specific paediatric dosing recommendations.

Adults: Refer to the BNF for specific dosing guidelines.

Mechanism of action

Terbutaline exerts its effects through selective agonism of beta-2 adrenergic receptors located in the bronchioles. This activation leads to the stimulation of adenylyl cyclase, which increases the levels of intracellular cyclic adenosine monophosphate (cAMP). The rise in cAMP reduces intracellular calcium concentrations, leading to the activation of protein kinase A. This enzyme inactivates myosin light-chain kinase and activates myosin light-chain phosphatase, ultimately resulting in the relaxation of smooth muscle within the bronchioles.

Pharmacodynamics

As a beta-2 adrenergic receptor agonist, terbutaline is indicated for the relief of bronchospasm in conditions such as asthma, chronic bronchitis, and emphysema. It has a rapid onset of action and a relatively short duration of effect, typically requiring administration up to three times daily in its inhaled form. The therapeutic window for terbutaline is wide, making it generally safe within prescribed doses.

Pharmacokinetics

Terbutaline is rapidly absorbed when administered via inhalation, allowing for quick therapeutic action. The drug undergoes extensive first-pass metabolism when taken orally, which may affect its bioavailability. It is primarily metabolized in the liver and has a half-life that supports frequent dosing. Excretion occurs mainly via the kidneys, with metabolites detectable in urine.

Contra-indications

• Hypersensitivity to terbutaline or any of its components
• Severe hypersensitivity to sympathomimetic amines
• Tachyarrhythmias
• Cardiac arrhythmias

Adverse effects

• Tremor
• Tachycardia
• Palpitations
• Headache
• Nausea
• Dizziness
• Muscle cramps
• Hypokalemia

Interactions

• Beta-blockers may reduce the effectiveness of terbutaline
• Concomitant use with other sympathomimetics may increase the risk of cardiovascular side effects
• Monoamine oxidase inhibitors (MAOIs) can potentiate the effects of terbutaline

Precautions

• Use with caution in patients with cardiovascular disorders
• Monitor potassium levels in patients with significant hypokalemia
• Caution in patients with diabetes mellitus as beta agonists may induce hyperglycemia

Pregnancy

Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Category C.

Breast-feeding

Terbutaline is excreted in human milk, and caution should be exercised when administered to a nursing woman.

Storage

Store below 25 degrees Celsius. Protect from light and moisture. Keep out of reach of children.

Formulations

• Inhalation aerosol
• Oral tablets
• Injection

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

Terbutaline is a selective beta-2 adrenergic receptor agonist. Agonism of these receptors in bronchioles activates adenylyl cyclase, increasing intracellular cyclic adenosine monophosphate (cAMP). Increased cAMP decreases intracellular calcium, activating protein kinase A, inactivating myosin light-chain kinase, activating myosin light-chain phosphatase, and finally relaxing smooth muscle in the bronchiole.

Pharmacodynamics

Terbutaline is a beta-2 adrenergic receptor agonist indicated to treat reversibly bronchospasm in asthmatic patients with bronchitis and emphysema. It has a short duration as the inhaled form is taken up to three times daily, and the therapeutic window is wide.