ROSE REFRESH SPRAY

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®)

Indications

• Gastrointestinal discomfort
• Irritable bowel syndrome (IBS)
• Nausea
• Respiratory congestion
• Headaches

Dosage

Children: Refer to appropriate guidelines based on the specific formulation and condition being treated, as there is no standard dosage provided.

Adults: Refer to appropriate guidelines based on the specific formulation and condition being treated, as there is no standard dosage provided.

Mechanism of action

The primary active constituents of menta, such as menthol, exert their effects by activating TRPM8 (transient receptor potential cation channel subfamily M member 8) receptors, which are responsible for the sensation of coolness and pain relief. Menthol also has local anesthetic properties and can induce vasodilation, providing a soothing effect on mucous membranes.

Pharmacodynamics

Menta has antispasmodic, carminative, and analgesic properties, making it effective in relieving symptoms associated with digestive disorders, such as bloating and gas. Its ability to relax smooth muscle in the gastrointestinal tract contributes to its effectiveness in alleviating symptoms of irritable bowel syndrome (IBS) and other digestive complaints.

Pharmacokinetics

Menthol is rapidly absorbed through the gastrointestinal tract and has a bioavailability that allows for effective systemic and local action. It undergoes hepatic metabolism, primarily through glucuronidation. The elimination half-life is relatively short, and metabolites are primarily excreted in urine. The onset of action is typically within a few minutes when used topically or ingested.

Pregnancy

There is limited data on the use of menta during pregnancy. It is advisable to use with caution and consult a healthcare provider.

Breast-feeding

Menta is generally considered safe during breastfeeding, but it is recommended to consult a healthcare provider before use.

Storage

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

Indications

• Anxiety
• Depression
• Skin wounds
• Inflammation
• Aromatherapy for relaxation

Dosage

Children: Refer to relevant guidelines and literature for specific dosing recommendations, as rose extracts vary widely in concentration and formulation.

Adults: Refer to relevant guidelines and literature for specific dosing recommendations, as rose extracts vary widely in concentration and formulation.

Mechanism of action

The essential oil from rose contains various compounds such as phenyl ethanol, geraniol, and citronellol, which may exert their effects through the modulation of neurotransmitter systems. It is believed to influence the central nervous system, promoting relaxation and reducing anxiety. Additionally, rose extracts possess antioxidant properties, which may contribute to their anti-inflammatory effects.

Pharmacodynamics

Rose extracts have been shown to have anxiolytic and antidepressant effects, likely through the enhancement of serotonin and dopamine levels in the brain. The anti-inflammatory properties are attributed to the inhibition of pro-inflammatory cytokines and modulation of immune responses. The antioxidant activity helps protect cells from oxidative stress.

Pharmacokinetics

The pharmacokinetics of rose extracts are not well-documented due to variations in preparation and formulation. However, the constituents are generally absorbed through the skin or mucous membranes when used topically or in aromatherapy. The bioavailability and half-life of specific compounds can vary widely, influenced by factors such as formulation, dosage, and individual metabolism.

Pregnancy

Insufficient data on the safety of rose during pregnancy. Consult healthcare provider before use.

Breast-feeding

Limited information available. Consult healthcare provider before use.

Storage

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

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.