Lafalos Plus Cream
Lafalos Plus Cream Uses, Dosage, Side Effects, Food Interaction and all others data.
Although the precise mechanism of action of Capsaicin is not fully understood, current evidence suggests that Capsaicin exerts an analgesic effect by depleting and preventing reaccumulation of Substance P in peripheral sensory neurons. Substance P is thought to be the principal chemomediator of pain impulses from the periphery to the central nervous system.
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.
Eugenol is a naturally occurring phenolic molecule found in several plants such as cinnamon, clove, and bay leaves. It has been used as a topical antiseptic as a counter-irritant and in dental preparations with zinc oxide for root canal sealing and pain control. Although not currently available in any FDA-approved products (including OTC), eugenol has been found to have anti-inflammatory, neuroprotective, antipyretic, antioxidant, antifungal and analgesic properties. Its exact mechanism of action is unknown, however, it has been shown to interfere with action potential conduction.There are a number of unapproved OTC products available containing eugenol that advertise its use for the treatment of toothache.
Methyl salicylate (oil of wintergreen or wintergreen oil) is an organic ester naturally produced by many species of plants, particularly wintergreens. The compound was first extracted and isolated from plant species Gaultheria procumbens in 1843. It can be manufactured synthetically and it used as a fragrance, in foods, beverages, and liniments. It forms a colorless to yellow or reddish liquid and exhibits a characteristic odor and taste of wintergreen. For acute joint and muscular pain, methyl salicylate is used as a rubefacient and analgesic in deep heating liniments. It is used as a flavoring agent in chewing gums and mints in small concentrations and added as antiseptic in mouthwash solutions.
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.
Vitamin E Capsule is a Vitamin E preparation. Vitamin E acts as an antioxidant in the body. Vitamin E protects polyunsaturated fatty acids (which are components of cellular membrane) and other oxygen-sensitive substances such as vitamin A & vitamin C from oxidation. Vitamin E reacts with free radicals, which is the cause of oxidative damage to cell membranes, without the formation of another free radical in the process. The main pharmacological action of vitamin E in humans is its antioxidant effect.
In premature neonates irritability, edema, thrombosis and hemolytic anemia may be caused due to vitamin E deficiency. Creatinuria, ceroid deposition, muscle weakness, decreased erythrocyte survival or increased in vitro hemolysis by oxidizing agents have been identified in adults and children with low serum tocopherol concentrations.
Vitamin E is a collective term used to describe 8 separate fat soluble antioxidants, most commonly alpha-tocopherol. Vitamin E acts to protect cells against the effects of free radicals, which are potentially damaging by-products of the body's metabolism. Vitamin E deficiency is seen in persons with abetalipoproteinemia, premature, very low birth weight infants (birth weights less than 1500 grams, or 3½ pounds), cystic fibrosis, and cholestasis and severe liver disease. Preliminary research suggests vitamin E may help prevent or delay coronary heart disease and protect against the damaging effects of free radicals, which may contribute to the development of chronic diseases such as cancer. It also protects other fat-soluble vitamins (A and B group vitamins) from destruction by oxygen. Low levels of vitamin E have been linked to increased incidence of breast and colon cancer.
| Trade Name | Lafalos Plus Cream |
| Generic | Eugenol + Menthol + Methyl salicylate + Capsaicin + Vitamin E |
| Weight | 14mg, 55mg, 102mg, 3mg, 30mg |
| Type | Cream |
| Therapeutic Class | |
| Manufacturer | Sanbe Farma |
| Available Country | Indonesia |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Capsaicin is indicatd for- Rheumatoid arthritis, Osteoarthritis, Pain due to diabetic neuropathy, Joint pain, Post-herpetic neuralgia, Post-surgical neuropathic pain, Nerve Pain, Back pain, Muscle pain, Fibromyalgia, Bursitis, Pruritis (itching)
Eugenol is a phenol used for the temporary relief of toothaches.
Eugenol is not currently available in any FDA-approved drug products. There are a number of unapproved OTC products that advertise it for the use of toothache. Eugenol is is also commonly used in combination with zinc oxide in dental procedures for the cementation of temporary prostheses and the temporary restoration of teeth and cavities.
Methyl salicylate is a topical counter-irritant used for the symptomatic relief of acute musculoskeletal pain in the muscles, joints, and tendons.
Ointments or liniments containing methyl salicylate are applied topically as counter irritant for relief of acute pain associated with lumbago,sciatica and rheumatic conditions. Local analgesics for human and veterinary medicine.
As a dietary supplement:
- Vitamin E deficiency resulting from impaired absorption.
- Increased requirements due to diet rich in polyunsaturated fats.
- For healthy hair & skin
- As an Antioxidant
- Hemolytic anemia due to Vitamin E deficiency
Therapeutic use
: Heavy metal poisoning, Hepatotoxin poisoning, Hemolytic anemia, Oxygen therapy and replacement therapy in nutritional deficiency states for the betterment of skin and hair.
Lafalos Plus Cream is also used to associated treatment for these conditions: Arthritis, Back Pain Lower Back, Backache, Bursitis, Contusions, Inflammatory Reaction caused by Rheumatism, Muscle Cramps, Musculoskeletal Pain, Osteoarthritis (OA), Periarthritis, Post-Herpetic Neuralgia (PHN), Rheumatic Pain, Soft Tissue Injury, Tendinitis, Acute nonspecific tenosynovitisContusions, Insect Bites, Soreness, Muscle, Sprains, Itching skin, Oral discomfort and painAcute Muscle Pain, Arthritis, Back Pain Lower Back, Backache, Contusions, Joint Pain, Ligament pain, Muscle Inflammation, Muscle Injuries, Muscle Strain, Muscle swelling, Pain, Pain of the Bone and Bones, Pain, Nerve, Partial-Onset Seizures, Postherpetic Neuralgia, Soreness, Muscle, Sprains, Tendon pain, Minor aches, Muscle, joint painsVitamin Deficiency, Long-chain omega-3 fatty acid supplementation, Dietary supplementation
How Lafalos Plus Cream works
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.
The exact mechanism of action of eugenol is unknown. However, eugenol has been shown to interrupt action potentials, which may be involved in its anti-pain activity. Research has also shown eugenol to have anti-inflammatory, neuroprotective, antipyretic, antioxidant, antifungal and analgesic properties.
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.
The mechanism of action for most of vitamin E's effects are still unknown. Vitamin E is an antioxidant, preventing free radical reactions with cell membranes. Though in some cases vitamin E has been shown to have pro-oxidant activity.
One mechanism of vitamin E's antioxidant effect is in the termination of lipid peroxidation. Vitamin E reacts with unstable lipid radicals, producing stable lipids and a relatively stable vitamin E radical. The vitamin E radical is then reduced back to stable vitamin E by reaction with ascorbate or glutathione.
Dosage
Lafalos Plus Cream dosage
18 years of age and older:Apply a thin film of Capsaicin cream to affected area 3 to 4 times daily. A burning sensation may occur upon application, but generally disappears with regular use. Application schedules of 3 to 4 times a day for 2 weeks provides optimum pain relief.
Betterment of Cardiovascular health: 400 mg - 800 mg / day
Deficiency syndrome in adults: 200 mg - 400 mg / day
Deficiency syndrome in children: 200 mg / day
Thalassemia: 800 mg / day
Sickle-cell anemia: 400 mg / day
Betterment of Skin & Hair: 200 mg - 400 mg / day (Topical use is also established for beautification)
Chronic cold in adults: 200 mg / day
Side Effects
Capsaicin may cause transient burning on application. This burning is observed more frequently when the application schedules are more than 3-4 times daily. The burning can be enhanced if too much cream is used and if it is applied just before or after a bath or shower.
Overdoses (>1g) have been associated with minor side effects, including hypertension, fatigue, diarrhea and myopathy
Toxicity
Acute oral LD50 and dermal LD50 in mouse are 47.2 mg/kg and >512 mg/kg, respectively . Capsaicin is shown to be mutagenic for bacteria and yeast .
Capsaicin can cause serious irritation, conjunctivitis and lacrimation via contact with eyes. It induces a burning sensation and pain in case of contact with eyes and skin. As it is also irritating to the respiratory system, it causes lung irritation and coughing as well as bronchoconstriction. Other respiratory effects include laryngospasm, swelling of the larynx and lungs, chemical pneumonitis,respiratory arrest and central nervous system effects such as convulsions and excitement . In case of ingestion, gastrointestinal tract irritation may be observed along with a sensation of warmth or painful burning . Symptoms of systemic toxicity include disorientation, fear, loss of body motor control including diminished hand-eye coordination, hyperventilation, tachycardia, and pulmonary oedema . Careful early decontamination is recommended and medical intervention should be initiated for any life-threatening symptoms. In case of contact, individual must be removed from the source of exposure and the contacted skin and mucous membranes should be thoroughly washed with copious amounts of water .
Oral LD50 values (mg/kg) for mouse, rat and rabbit are 1110, 887 and 1300, respectively. Oral LD50 values for child and adult human (mg/kg) are 228 and 506, respectively. Although systemic toxicity from topical administration is rare, methyl salicylate can be absorbed in intract skin to cause stimulation of the central nervous system respiratory center, disturbance of lipid and carbohydrate metabolism, and disturbance of intracellular respiration. Severe toxicity can result in acute lung injury, lethargy, coma, seizures, cerebral edema, and death. In case of salicylate poisoning, the treatment consists of general supportive care, gastrointestinal decontamination with activated charcoal in cases of salicylate ingestion, and monitoring of serum salicylate concentrations. Bicarbonate infusions or hemodialysis can be used to achieve enhanced salicylate elimination .
There is no data available for effects in pregnancy, breast feeding, hepatic impairment, or renal impairment. However, it appears that the process of vitamin E elimination is strict and self regulating enough that vitamin E toxicity is exceedingly rare. Studies showing adverse effects from excess vitamin E generally involve people consuming more than 1000mg/day for weeks to months.
Precaution
Capsaicin cream should not be applied to broken or irritated skin. Applied area should not be tightly bandaged. Do not get on mucous membranes and into eyes or on contact lenses. If this occurs, rinse the affected area thoroughly with water. Do not apply the cream on the heat treated area as this may increase the burning sensation. In case of accidental ingestion, seek physician advice immediately.
Vitamin E may enhance the anticoagulant activity of anticoagulant drugs. Caution is advised in premature infants with high dose Vitamin E supplementation, because of reported risk of necrotizing enterocilitis.
Interaction
Vitamin E may impair the absorption of Vitamin A. Vitamin K functions impairement happens at the level of prothrombin formation and potentiates the effect of Warfarin.
Volume of Distribution
After absorption, methyl salicylate is distributed throughout most body tissues and most transcellular fluids, primarily by pH dependent passive processes. Salicylate is actively transported by a low-capacity, saturable system out of the CSF across the choroid plexus. The drug readily crosses the placental barrier.
0.41L/kg in premature neonates given a 20mg/kg intramuscular injection.
Elimination Route
Oral: Following oral administration, capsaicin may be absorbed by a nonactive process from the stomach and whole intestine with an extent of absorption ranging between 50 and 90%, depending on the animal . The peak blood concentration can be reached within 1 hour following administration . Capsaicin may undergo minor metabolism in the small intestine epithelial cells post-absorption from the stomach into the small intestines. While oral pharmacokinetics information in humans is limited, ingestion of equipotent dose of 26.6 mg of pure capsaicin, capsaicin was detected in the plasma after 10 minutes and the peak plasma concentration of 2.47 ± 0.13 ng/ml was reached at 47.1 ± 2.0 minutes .
Systemic: Following intravenous or subcutaneous administration in animals, the concentrations in the brain and spinal cord were approximately 5-fold higher than that in blood and the concentration in the liver was approximately 3-fold higher than that in blood .
Topical: Topical capsaicin in humans is rapidly and well absorbed through the skin, however systemic absorption following topical or transdermal administration is unlikely . For patients receiving the topical patch containing 179 mg of capsaicin, a population analysis was performed and plasma concentrations of capsaicin were fitted using a one-compartment model with first-order absorption and linear elimination. The mean peak plasma concentration was 1.86 ng/mL but the maximum value observed in any patient was 17.8 ng/mL .
Approximately 12-20% of topically applied methyl salicylate may be systemically absorbed through intact skin within 10 hours of application, and absorption varies with different conditions such as surface area and pH. Dermal bioavailability is in the range of 11.8 – 30.7%. For the assessment of potential oral exposure to salicylates, bioavailability is assumed to be 100% .
10-33% of deuterium labelled vitamin E is absorbed in the small intestine. Absorption of Vitamin E is dependant upon absorption of the fat in which it is dissolved. For patients with poor fat absorption, a water soluble form of vitamin E may need to be substituted such as tocopheryl polyethylene glycol-1000 succinate.
In other studies the oral bioavailability of alpha-tocopherol was 36%, gamma-tocotrienol was 9%. The time to maximum concentration was 9.7 hours for alpha-tocopherol and 2.4 hours for gamma-tocotrienol.
Half Life
Following oral ingestion of equipotent dose of 26.6 mg of pure capsaicin, the half life was approximately 24.9 ± 5.0 min . Following topical application of 3% solution of capsaicin, the half-life of capsaicin was approximately 24 h . The mean population elimination half-life was 1.64 h following application of a topical patch containing 179 mg of capsaicin .
The plasma half-life for salicylate is 2 to 3 hr in low doses and about 12 hr at usual anti-inflammatory doses. The half-life of salicylate may be as long as 15 to 30 hr at high therapeutic doses or when there is intoxication.
44 hours in premature neonates given a 20mg/kg intramuscular injection. 12 minutes in intravenous injection of intestinal lymph.
Clearance
6.5mL/hr/kg in premature neonates given a 20mg/kg intramuscular injection.
Elimination Route
It is proposed that capsaicin mainly undergoes renal excretion, as both the unchanged and glucuronide form. A small fraction of unchanged compound is excreted in the feces and urine. In vivo animal studies demonstrates that less than 10 % of an administered dose was found in faces after 48 h .
Excreted by kidneys as free salicylic acid (10%), salicyluric acid (75%), salicylic phenolic (10%) and acyl glucuronide (5%), and gentisic acid (less than 1%).
Alpha tocopherol is excreted in urine as well as bile in the feces mainly as a carboxyethyl-hydrochroman (CEHC) metabolite, but it can be excreted in it's natural form .
Pregnancy & Breastfeeding use
The safety of Capsaicin during pregnancy or lactation has not been established in either humans or animals.
Use in pregnancy: Vitamin E may be used in pregnancy in the normally recommended dose but the safety of high dose therapy has not been established.
Use in lactation: There appears to be no contraindication to breast feeding by mothers taking the normally recommended dose.
Contraindication
Capsaicin cream is contraindicated on broken or irritated skin. It is also contraindicated in patients with known hypersensitivity to capsaicin or any of the excipients used in this product.
No known contraindications found.
Special Warning
Use in Children: Vitamin E is safe for children
Acute Overdose
Sufficient information on overdose of Capsaicin is not available.
Large doses of vitamin E (more than 1 gm/day) have been reported to increase bleeding tendency in vitamin K deficient patients such as those taking oral anticoagulants.
Storage Condition
Keep at cool and dry place, away form light. Keep out of the reach of children.
Store at a cool and dry place, Protect from light and moisture.
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