Afitson

Afitson Uses, Dosage, Side Effects, Food Interaction and all others data.

Clove oil is a herbal medicine which main ingredient is clove oil. It contains a large amount of eugenol that is commonly used in the treatment of oral infections and inflammation of the mucous membranes of the mouth and throat. Clove oil is effective, safe and well tolerated for all age groups

Clove (Eugenia caryophyllata Thunb. [Myrtaceae]) essential oil (CEO) has been demonstrated to possess antimicrobial, antifungal, antiviral, antioxidant, anti-inflammatory, anti-histamine, and anticancer properties. However, few studies have focused on its topical use , .

Clove essential oil, used as an antiseptic in oral infections, inhibits gram-negative and gram-positive bacteria as well as yeast .

Eucalyptus oil is a distilled oil derived from the leaves of the tree Eucalyptus. It is shown to be effective in reducing pain, swelling, and inflammation via its modulatory effect on the immune response. It is also shown to exhibit antibacterial activity against some bacterial species and cough suppressant actions. Eucalyptus oil can be applied directly to the skin for pain and swelling of respiratory tract mucous membranes, joint pain, genital herpes, and nasal stuffiness.

Lipophilic monoterpene formulations of eucalyptus oil appear to be readily absorbed orally, with a primarily oxidative metabolism that might necessitate induction of the cytochrome P450 enzyme system and subsequent urinary excretion . Gastrointestinal absorption of eucalyptus appears to be rapid and may be enhanced by the intake of lipids and milk. 1,8-cineole (which makes up to as much as 90% of most commonly used cineole-based eucalyptus oils) has also been found in vitro and in animals to possess cytochrome P450 inducing activity .

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.

Peppermint Oil helps to relieve both the painful abdominal spasm and uncomfortable bloating of IBS. It has a relaxant, antispasmodic effect especially on the muscles of the large bowel or colon and in bowel spasm, particularly large-bowel spasm. It is carminative, antibacterial, mucolytic. Peppermint Oil helps to treat unpleasant sensations of fullness and bloating and facilitates the passing of bowel gases, so relieving accompanying cramp like pain.

Peppermint oil induces a dose-related antispasmodic effects on the gastrointestinal smooth muscles . A meta-analysis study and additional clinical studies of patients with IBS demonstrated that the treatment with peppermint oil improves abdominal symptoms compared to the placebo group, resulting in reduced severity of abdominal pain, decreased abdominal distension, reduced stool frequency, and reduced flatulence . The use of enteric-coated peppermint oil was shown to be effective in reducing gastrointestinal symptoms of non-ulcer dyspepsia . In rats, peppermint oil promoted a time-dependent choleretic effect in increasing bile production and biliary output . In randomized controlled trials, topical application of peppermint oil was associated with a significant analgesic effect and a reduction in headache intensity compared to placebo . In a study of C57BL/6 mice, topical application of peppermint oil for 4 weeks was associated with a prominent hair growth effects; a significant increase in dermal thickness, follicle number, and follicle depth .

Afitson
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Afitson
Generic	Methyl Salicylate + Menthol Camphora + Peppermint oil + Clove oil + Eucalyptus oil + dan Pseudo Capsaicin.
Type
Therapeutic Class
Manufacturer	PT Perseroan Dagang dan Industri Farmasi Afiat
Available Country	Indonesia
Last Updated:	September 19, 2023 at 7:00 am

Uses

Clove oil is used for Bad breath (Halitosis), Tooth decay, Oral thrush, Dental pain, Inflammation of the mouth and pharynx.

Eucalyptus oil is an ingredient used in a variety of natural health products.

As an active agent, eucalyptus oil has been indicated for relief of the symptoms of catarrhal colds, and/or the relief of the symptoms of minor muscular sprains and cramps .

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.

Each enteric coated liquid filled hard gelatin capsule contains 187 mg (0.2 ml) of peppermint oil.

Peppermint Oil is used in Irritable bowel syndrome (IBS), Functional dyspepsia, Abdominal pain and spasm, Abdominal distension/bloating

Peppermint leaf preparations consist of the fresh or dried leaf of Mentha x piperita L. The whole dried leaf must contain not less than 1.2% (ml/gm) and the cut leaf must contain not less than 0.9% volatile oil. Peppermint oil consists of the essential oil, obtained by steam-distilling freshly harvested, flowering springs and is neither partially nor wholly dementholized.

Afitson is also used to associated treatment for these conditions: Mild pain, ToothacheCough, Infection, Itching caused by Insect Bites, Nasal Congestion, Rash caused by Insect Bites, Soreness, Muscle, Infection in minor cuts, scrapes, or burns, Itching skin, Minor aches and pains, Topical AntisepsisAcute 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 painsColic, Cough, Flatulence, Hypertonicity of the small intestine, Irritable Bowel Syndrome (IBS), Mild pain, Nasal Congestion, Soreness, Muscle, Gas pain

How Afitson works

The chief constituent present in clove oil is the phenol "eugenol" which is present in amounts up to 85%. Clove oil acts as a germicide to Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa .

Clove oil is thought to inhibit prostaglandin synthesis, thereby reducing painful symptoms .

Eugenol, the main constituent of clove oil is purported to have anticancer action. In one study, eugenol-treated HL-60 cells showed features of apoptosis including DNA fragmentation and formation of DNA ladders in agarose gel electrophoresis. It was observed that eugenol transduced the apoptotic signal via reactive oxygen species (ROS) generation, inducing mitochondrial permeability transition (MPT), decreasing anti-apoptotic protein bcl-2 level, inducing cytochrome c release to the cytosol, and subsequent apoptotic cell death. When taken together, the study showed that ROS plays a critical role in eugenol-induced apoptosis in HL-60, and this is the first report on the mechanism of the anticancer effect of eugenol .

The general consensus is that the exact mechanism of action of eucalyptus oil is largely unknown at this time but comprises various hypotheses from various studies.

Cineol containing preparations of eucalyptus oil may contain up to 80% (or more) 1,8-cineole and is one of the most common types of eucalyptus oil formulations used. As an active agent indicated for relieving certain cold symptoms and/or certain muscular sprains and cramps, it is believed that eucalyptus oil may possess some antimicrobial and anti-inflammatory activities.

Some in vitro studies of human blood monocytes suggest a dose-dependent effect of eucalyptus oil to elicit significant inhibition of multiple cytokines, perhaps in the treatment of airway inflammation . Moreover, other studies in animal models discuss the possibility of eucalyptus oil demonstrating anti-inflammatory and anti-nociceptive effects that potentially account for inhibiting the formation of prostaglandins and cytokines by stimulated monocytes in vitro .

Furthermore, additional studies have observed eucalyptus oil anti-viral activity against herpes simplex virus (HSV-1, HSV-2) in cell cultures as well as the demonstration of broad antimicrobial activity of eucalyptus medicinal plant extracts against Alicyclobacillus acidoterretris, Bacillus cereus, E. coli, Enterococcus faecalis, MRSA, Propionibacterium acnes, S. aureus, fungus including C. albicans isolates, Trichophyton mentagrophytes, and other Gram-positive bacteria. Specific activity against periodontopathic bacteria, such as Porphyromonas gingivalis, Actinobacillus actinomycetemcomitans, Fusobacterium nucleatum, Streptococcus mutans, and Streptococcus sobrinus has also been observed .

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.

Dose-dependent antispasmodic effect of peppermint oil is largely mediated by its menthol constituent . It is proposed that peppermint oil relaxes gastrointestinal smooth muscle and attenuates contractile responses by reducing the influx of extracellular calcium ions. In rabbit jejunum smooth muscle cells investigated via whole cell clamp configuration technique, peppermint oil was shown to inhibit the potential-dependent calcium currents in a concentration-dependent manner . Both a reduction in peak current amplitude and an increase in the rate of current decay were observed, indicating that the pharmacological activity peppermint oil resembles that of dihydropyridine calcium antagonists . In a rat small intestine study, peppermint oil in the intestinal lumen inhibited enterocyte glucose uptake via a direct action on the brush border membrane and inhibited intestinal secretion . There is also evidence that menthol is an antagonist of L-type Ca2+ channels via interacting with dihydropyridine binding sites and blocks the currents of low-voltage-activated calcium channels . Peppermint oil may facilitate hair growth by promoting the conservation of vascularization of hair dermal papilla, which may contribute to the induction of early anagen stage of active growth phase of hair follicles .

Dosage

Afitson dosage

Adult: Should be taken 5 ml Clove oil with 10 ml-15 ml water and gurgle for 30 seconds of morning & bedtime daily.

Children: Should be taken 2.5 ml Clove oil with 10 ml water and gurgle for 30 seconds of morning & bedtime daily. Also undiluted clove oil is used in temporary relief of toothache due to dental cavity. Repeat administration after 20 minutes, then every 2 hours thereafter if necessary.

Adults: 1 capsule 3 times daily with a glass of water. The dose may be increased to a maximum of 2 capsules 3 times daily or as directed by a physician.

Children (8 years and above): 1 capsule 3 times daily with a glass of water or a directed by a physician.

Side Effects

In concentrated form oil of clove may be irritating to mucosal tissues.

Toxicity

Acute oral toxicity (LD50): 2650 mg/kg [Rat] .

Clove oil is considered safe in small quantities (< 1,500 ppm) as a food additive . the lethal oral dose is 3.75 g per kg body weight in humans .

Contact with skin or soft tissue may cause transient irritation, contact dermatitis, inflammation of the lips, and inflammation or ulceration of the mouth. The eugenol present in clove oil may act as an irritant to skin and mucous membranes; it may also cause hypersensitivity and is reported to inhibit prostaglandin synthesis. Patients may become sensitive to clove oil .

After oral administration of 5-10 ml of clove oil in children below 2 years of age, life-threatening conditions were observed. Adverse effects included coma, acidosis, a generalized seizure, disordered blood clotting, and acute liver damage .

Overdose may lead to CNS depression, urinary abnormalities, anion-gap acidosis, deterioration of liver function, coma, seizure and low blood glucose levels. Treatment should be supportive and symptomatic; there have been reports in the literature that N-acetylcysteine has been successfully used as an antidote .

There are no epidemiological studies of potential adverse human health effects related to exposure to clove leave oil or eugenol from any human exposure scenarios. Nor are there any studies of agricultural use, either in workers or those with bystander exposure or other applications. There are no occupational exposure standards for clove leaf oil or eugenol including OSHA PEL (Permissible Exposure Limit) or AGIHA TLVs (Threshold Limit Value) in air .

Overdose with eucalyptus oil may result in epigastric burning, nausea and vomiting, dizziness, muscular weakness, mitosis, tachycardia, a sensation of suffocation, cyanosis, ataxia, pulmonary damage, delirium, convulsions, CNS depression, coma. Deaths have been recorded from doses as low as 3.5 ml.

The given oral LD50 for rats is 2480 mg/kg

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 .

Oral LD50 value in rat is 2426 mg/kg . In fasted mice, the LD50 following oral administration was 2410 mg/kg . Higher doses of peppermint oil has the potential to induce menstruation, bronchospasm, tongue spasms, and, possibly, respiratory arrest in addition to potential hepatotoxicity and nephrotoxicity .

Overdose may cause severe gastrointestinal symptoms, diarrhoea, rectal ulceration, epileptic convulsions, loss of consciousness, apnoea, nausea, disturbances in cardiac rhythms, ataxia and other CNS problems, probably due to the presence of menthol . In the event of overdose, the stomach should be emptied by gastric lavage. Observation should be carried out with symptomatic treatment if necessary . A near fatal case of high dose peppermint oil ingestion was reported, the overdose was characterized by comatose and reduced heart rate .

Precaution

Should not be taken with food or immediately after meals. Should be taken 30 to 60 minutes before meals. Must be swallowed whole, with a little liquid. Capsules must not be chewed or crushed.

Interaction

Exacerbation of adverse effects if taken with alcohol; enteric-coated preparations containing peppermint oil should not be taken immediately with antacids.

Volume of Distribution

Studies have determined a large terminal volume of distribution for cineole or eucalyptol (which makes up to as much as 90% of most commonly used cineole-based eucalyptus oils) of 27 l/kg in brushtail possum (Trichosurus vulpecula) .

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.

No pharmacokinetic data available.

Elimination Route

Clove oil is rapidly absorbed through the skin and is used in patented systems for dermal drug delivery to enhance drug uptake from skin patch delivery systems .

Common monoterpenoid compound preparations of eucalyptus oil have been observed to be readily absorbed after dermal application, likely due to their lipophilic character . Although maximal plasma levels were demonstrated in as short a time period as 10 minutes even with thicker preparations like eucalyptus oil ointments, like many other topically applied agents, the extent of absorption is also likely largely dependent upon additional factors like the size of treated skin area, patient skin condition(s), concentrations of the applied substance, and time of exposure to the substance .

Currently, more data regarding the oral absorption of eucalyptus would be useful, given the relative lack of existing information . Lipophilic monoterpene compound formulations of eucalyptus oil seems to be readily absorbed orally . Regardless, there is some data that suggests that the upper part of the gastrointestinal tract has no particularly significant role in the absorption of cineole based eucalyptus oil .

Pulmonary absorption of eucalyptus oil is also possible although little information exists regarding this element at the moment. Nevertheless, 1,8-cineol (which makes up to as much as 90% of most commonly used cineole-based eucalyptus oils) appears to be well absorbed via inhalation with peak plasma levels observed reportedly at 18 minutes .

Given the three main constituents from Eucalyptus globulus Labill fruits, the intestinal absorption of macrocarpal A (M-A), macrocarpal B (M-B), and cypellocarpa C (Cy-C) is predominantly via passive diffusion while Cy-C demonstrates some partly ATP-dependent absorption .

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% .

After oral administration, peppermint is rapidly absorbed . Menthol is highly fat-soluble therefore rapidly absorbed from the proximal gut .

Half Life

In a pharmacokinetic study, average half-life values of eugenol in plasma and blood were long (14.0 and 18.3 h, respectively), suggesting a potential accumulation of the drug following repeated administrations .

Studies have determined a terminal half-life for cineole or eucalyptol (which makes up to as much as 90% of most commonly used cineole-based eucalyptus oils) of approximately 7h in brushtail possum (Trichosurus vulpecula) .

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.

No pharmacokinetic data available.

Clearance

Studies have determined a high clearance rate for cineole or eucalyptol (which makes up to as much as 90% of most commonly used cineole-based eucalyptus oils) of 43 ml/min/kg in brushtail possum (Trichosurus vulpecula) .

No pharmacokinetic data available.

Elimination Route

In a pharmacokinetic study, the metabolism of eugenol (the primary constituent of clove oil) was investigated in healthy male and female volunteers. It was quickly absorbed and metabolized after oral administration and was almost completely excreted in the urine within 24 hours of ingestion .

Studies suggest the route of elimination for cineole or eucalyptol (which makes up to as much as 90% of most commonly used cineole-based eucalyptus oils) in brushtail possum (Trichosurus vulpecula), rats, and rabbit subjects as being in the urine .

Excreted by kidneys as free salicylic acid (10%), salicyluric acid (75%), salicylic phenolic (10%) and acyl glucuronide (5%), and gentisic acid (less than 1%).

Peppermint oil is eliminated mainly via the bile following oral administration, with glucuronide and sulphate metabolites predominant . The metabolites, mainly menthol glucuronide and mono- or di-hydroxylated menthol derivatives, may also undergo approximately equal renal and fecal excretion . Renal recovery of total menthol within 24 hours was dose-dependent whereas the recovery in bile was substantially higher over 8 hours .

Pregnancy & Breastfeeding use

There are no known problems with the use of Clove oil during pregnancy and lactation.

No known restrictions.

Contraindication

Contraindicated in patients with achlorhydria. Also contraindicated for infants due to the potential risk of spasm of the tongue or respiratory arrest.