Treosil

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

Glycerin is a hyperosmotic laxative, given rectally, which usually produces a bowel movement within 15 minutes to 1 hour. Hyperosmotic laxatives encourage bowel movements by drawing water into the bowel from surrounding tissues. This produces a softer stool mass and increased bowel action. These products are used for fast, predictable relief of occasional constipation.

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.

Ketoconazole interferes with biosynthesis of triglycerides and phopholipids by blocking fungal CYP450, thus altering cell membrane permeability in susceptible fungi. It also inhibits other fungal enzymes resulting in the accumulation of toxic concentrations of hydrogen peroxide.

Ketoconazole, similarly to other azole antifungals, is a fungistatic agent which causes growth arrest in fungal cells thereby preventing growth and spread of the fungus throughout the body.

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 .

Tea tree oil is an essential oil derived mainly from the Australian native plant Melaleuca alternifolia via steam distillation of the of the leaves and terminal branches . It may be referred to as Melaleuca alternifolia oil. It has been a popular ingredient in a variety of household and cosmetic products due to its antiseptic, anti-inflammatory, broad-spectrum antimicrobial and antioxidant properties . The dermatological use of tea tree oil has been investigated by various studies, where several studies have suggested the uses of this oil for the treatment of acne vulgaris, seborrheic dermatitis, and chronic gingivitis . Terpene hydrocarbons and related alcohols constitute tea tree oil, with Terpinen-4-ol being the major antimicrobial component .

Tea tree oil exhibits antibacterial, antifungal, antiviral, and antiprotozoal activities . It mostly mediates bactericidal actions at concentrations of 1.0% or less in most bacteria such as Staphylococcus aureus and Escherichia coli, and causes bacteriostatic effects at lower concentrations . Organisms such as commensal skin staphylococci and micrococci, Enterococcus faecalis, and Pseudomonas aeruginosaemphasized text were susceptible to tea tree oil concentrations of 2% . It is proposed that water-soluble components of tea tree oil are capable in inducing anti-inflammatory actions; terpinen-4-ol attenuates the vasodilation and plasma extravasation associated with histamine-induced inflammation in humans .

Trade Name Treosil
Generic Aloe Vera + D Panthenol + Glycerin + Ketoconazole + Peppermint Oil + Tea Tree Oil
Weight 5%
Type Shampoo
Therapeutic Class
Manufacturer Caviar Dermacare
Available Country India
Last Updated: September 19, 2023 at 7:00 am
Treosil
Treosil

Uses

For the relief of occasional constipation

Treatment of superficial and deep mycoses:

  • Infections of the skin, hair and nails by dermatophytes and/or yeasts (dermatomycosis, onychomycosis, perionyxis, pityriasis versicolor, chronic mucocutaneous candidiasis etc.) especially when topical treatment is difficult or not very effective, owing to involvement of large skin surfaces or to lesions affecting deeper dermal layers, nails and hairs
  • Yeast infection of the mouth (oral thrush, perleche) and the gastrointestinal tract
  • Vaginal candidiasis, especially chronic recurrent cases or cases responding poorly to topcial treatment
  • Systemic mycotic infections such as systemic candidiasis, paracoccidioidomycosis, histoplasmosis, coccidioidomycosis etc.

Maintenance treatment to prevent recurrence in systemic mycotic infections and in chronic mucocutaneous candidiasis.Prophylactic treatment to prevent mycotic infection in patients with reduced host defenses, e.g., patients with cancer, organ transplant and burns.

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.

Indicated for topical use to help protect against infection in minor cuts, scrapes, and burns. No FDA-approved therapeutic indications.

Treosil is also used to associated treatment for these conditions: Cold Sore, Constipation, Dry Mouth, Dry Skin, Dry throat, Edema of the cerebrum, Hypertension Intracranial, Occasional Constipation, Ocular Discomfort, Ocular Hypertension, Ocular Irritation, Skin Infections, Sore Throat, Mouth soreness, Ocular burning, Bowel preparation therapy, Topical Antisepsis, Skin protectionBacterial Vaginosis (BV), Blastomycosis, Candidiasis, Systemic, Chromomycosis, Chronic Mucocutaneous Candidiasis (CMC), Coccidioidomycosis, Dandruff, Endogenous Cushing's Syndrome, Histoplasmosis, Infections, Fungal, Paracoccidioidomycosis, Seborrheic Dermatitis, Tinea Corporis caused by Epidermophyton floccosumin, Tinea Corporis caused by Trichophyton mentagrophytes, Tinea Corporis caused by Trichophyton rubrum, Tinea Cruris caused by Epidermophyton floccosumin, Tinea Cruris caused by Trichophyton mentagrophytes, Tinea Cruris caused by Trichophyton rubrum, Tinea Pedis caused by Epidermophyton floccosumin, Tinea Pedis caused by Trichophyton mentagrophytes, Tinea Pedis caused by Trichophyton rubrum, Vaginal Candidiasis, Vulvovaginal Candidiasis, Cutaneous candidiasis, Recalcitrant Dermatophytosis, Tinea versicolor caused by Malassezia infectionColic, Cough, Flatulence, Hypertonicity of the small intestine, Irritable Bowel Syndrome (IBS), Mild pain, Nasal Congestion, Soreness, Muscle, Gas pain

How Treosil works

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.

Ketoconazole interacts with 14-α-sterol demethylase, a cytochrome P-450 enzyme necessary for the conversion of lanosterol to ergosterol. This results in inhibition of ergosterol synthesis and increased fungal cellular permeability due to reduced amounts of ergosterol present in the fungal cell membrane. This metabolic inhibition also results in accumulation of 14α-methyl-3,6-diol, a toxic metabolite. The increase in membrane fluidity is also thought to produce impairment of membrane-bound enzyme systems as components become less closely packed.

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 .

The components of tea tree oil, particularly terpinen-4-ol and α-terpineol, mediate antimicrobial actions by disrupting the structural and functional integrity of bacterial membrane. Hydrocarbons are capable of partitioning into the cell and cytoplasmic membrane of microorganisms and disrupt their vital functions, which may result in leakage of ions such as potassium, and the inhibition of respiration . Eventually, cell lysis may occur due to weakening of the cell wall, and loss of turgor pressure and subsequent rupture of the cytoplasmic membrane . The loss of 260-nm-absorbing material may be indicative of a damaged cytoplasmic membrane and loss of nucleic acids . In E. coli, perturbed potassium homeostasis, glucose-dependent respiration, cell morphology, and ability to exclude propidium iodide was observed.

Tea tree oil also mediates its antifungal actions in a similar way, where it alters the permeability of Candida albicans and inhibits its respiration in a dose-dependent manner . Plasma and mitochondrial membranes of fungal species are also thought to be negatively affected by inhibition of glucose-induced medium acidification by tea tree oil, which involves inhibition of membrane ATPase responsible for the expulsion of protons . Tea tree oil also inhibits the formation of germ tubes, or mycelial conversion, in C. albicans, thereby disrupting cell morphogenesis . Water-soluble fraction of TTO, terpinen-4-ol, and α-terpineol, can inhibit the lipopolysaccharide-induced production of the inflammatory mediators such as TNF-α, IL-1β and IL-10 by human peripheral monocytes by approximately 50% and that of prostaglandin E2 by about 30% after 40 h . These components of tea tree oil may also suppress superoxide production by agonist-stimulated monocytes and decrease the production of reactive oxygen species by both stimulated neutrophils and monocytes .

Dosage

Treosil dosage

Children under 2 years: Consult a physician.

Children (2 to 6 years): only 1 Glycerin 1.15 suppository per 24 hours or as directed by a physician.

Adults and Children (From 6 years): only 1 Glycerin 2.30 suppository per 24 hours or as directed by a physician

Insert suppository well up into rectum. Suppository need to melt completely to produce laxative action.

Oral-

Fungal infections:

  • Adult: 200 mg once daily; may increase to 400 mg once daily if clinical response is insufficient. Continue treatment until symptoms have cleared and cultures have become negative.
  • Child: ≥2 yr 3.3-6.6 mg/kg once daily. Treatment duration: 1-2 wk for candidiasis; at least 4 wk in recalcitrant dermatophyte infections and up to 6 mth for other systemic mycoses.
  • Elderly: No dosage adjustment needed.

Topical (Adult)-

Pityriasis versicolor, Skin fungal infections:

  • As 2% cream: Apply 1-2 times daily to cover affected and surrounding area until at least a few days after disappearance of symptoms.
  • As 2% shampoo: Apply on scalp once daily for up to 5 days. For prophylaxis: As 2% shampoo, use once daily for a max of 3 days before exposure to sunlight.

Seborrhoeic dermatitis:

  • As 2% foam: Apply to the affected area bid for 4 wk.
  • As 1 or 2% shampoo: Apply on the scalp twice wkly for 2-4 wk. For prophylaxis: As 2% shampoo, use once every 1-2 wk.

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.

Duration of Treatment

  • Pityriasis versicolor: 1 to 6 weeks
  • Dermatomycoses: 2 to 8 weeks
  • Onychomycoses: 1 to 12 months
  • Mycoses of hair and scalp: 1 to 2 months
  • Chronic mucocutaneous candidiasis : 1 to 12 months
  • Oral mycoses: 5 to 10 days
  • Systemic candidiasis: 1 to 2 months
  • Paracoccidioidomycosis,histoplasmosis
  • and other systemic mycosis: 1 month to 2 years

Side Effects

Glycerin when used rectally may cause rectal discomfort or a burning sensation

Ketoconazole is very well tolerated. Nausea and itching may occasionally occur. In some patients, an idosyncratic liver reaction may occur (incidence 1 : 10,000).

Toxicity

Glycerol has very low toxicity when ingested ; Rat LD50 (oral)-12600mg/kg Mice LD50 (oral )-4090mg/kg Human TDLo (oral) - 1428mg/kg

Symptoms of overdose include acute liver injury, which may include both hepatocellular and cholestatic injury, accompanied by anorexia, fatigue, nausea, and jaundice. In case of overdose, gastric lavage with activated charcoal may be used if within one hour of ketoconazole ingestion otherwise provide supportive care. If the patient shows signs of adrenal insufficiency, administer 100 mg hydrocortisone once together with saline and glucose infusion and monitor the patient closely. Blood pressure and fluid and electrolyte balance should be monitored over the next few days.

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 .

The 50% lethal dose for TTO in a rat model is 1.9 to 2.6 mL/kg, and doses ≤1.5 g/kg was associated with ataxia and lethargy. Dermal patches containing 10% of tea tree oil was not associated with any irritant reactions. Topically-applied tea tree oil rarely causes systemic toxicity . Dermal application of approximately 120 ml of undiluted tea tree oil to three cats with shaved but intact skin resulted in symptoms of hypothermia, uncoordination, dehydration, and trembling and in the death of one of the cats .

Precaution

Predisposition to adrenocortical insufficiency. Admin with acidic drink in patients with achlorhydria. Pregnancy and lactation.

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

Reduced absorption with antimuscarinics, antacids, H2-blockers, PPIs and sucralfate. Reduced plasma concentrations with rifampicin, isoniazid, efavirenz, nevirapine, phenytoin. May also reduce concentrations of isoniazid and rifampicin. May reduce efficacy of oral contraceptives. May increase serum levels of CYP3A4 substrates e.g. digoxin, oral anticoagulants, sildenafil, tacrolimus.

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

Volume of Distribution

Glycerin is distributed throughout the blood. Although glycerin generally does not appear in ocular fluids, it may enter the orbital sac when the eye is inflamed, with a consequent decrease in osmotic effect.

Ketoconazole has an estimated volume of distribution of 25.41 L or 0.36 L/kg. It distributes widely among the tissues, reaching effective concentrations in the skin, tendons, tears, and saliva. Distribution to vaginal tissue produces concentrations 2.4 times lower than plasma. Penetration into the CNS, bone, and seminal fluid are minimal. Ketoconazole has been found to enter the breast milk and cross the placenta in animal studies.

No pharmacokinetic data available.

No pharmacokinetic data available.

Elimination Route

Well absorbed orally, poorly absorbed rectally. Studies in humans and animals indicate glycerol is rapidly absorbed in the intestine and the stomach

Ketoconazole requires an acidic environment to become soluble in water. At pH values above 3 it becomes increasingly insoluble with about 10% entering solution in 1 h. At pH less than 3 dissolution is 85% complete in 5 min and entirely complete within 30 min. A single 200 mg oral dose produces a Cmax of 2.5-3 mcg/mL with a Tmax of 1-4 h. Administering ketoconazole with food consistently increases Cmax and delays Tmax but literature is contradictory regarding the effect on AUC, which may experience a small decrease. A bioavailablity of 76% has been reported for ketoconazole.

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

No pharmacokinetic data available.

Half Life

30 - 45 minutes

Ketoconazole experiences biphasic elimination with the first phase having a half-life of 2 hours and a terminal half life of 8 hours.

No pharmacokinetic data available.

No pharmacokinetic data available.

Clearance

Ketoconazole has an estimated clearance of 8.66 L/h.

No pharmacokinetic data available.

No pharmacokinetic data available.

Elimination Route

Approx 7-14% of dose is excreted unchanged in the urine within 2.5 hr.

Only 2-4% of the ketoconazole dose is eliminated unchanged in the urine. Over 95% is eliminated through hepatic metabolism.

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 .

No pharmacokinetic data available.

Pregnancy & Breastfeeding use

Pregnancy category C. There are no controlled data in human pregnancy

Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

No known restrictions.

Contraindication

Sensitivity to the ingredients. Do not use unless the patient to be treated is, in fact, constipated.

Hypersensitivity; preexisting liver disease. Concurrent use with CYP3A4 substrates e.g. HMG-CoA reductase inhibitors (e.g. lovastatin, simvastatin), midazolam, triazolam, cisapride, dofetilide, eplerenone, nisoldipine, pimozide, quinidine, terfenadine, astemizole, ergot alkaloids (e.g. ergotamine, dihydroergotamine).

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

Special Warning

Renal Impairment: Oral: No dosage adjustment needed.

Hepatic Impairment: Oral: Contraindicated.

Storage Condition

Store below 25° C. Protect from moisture.

Store between 15-25° C. Protect from moisture and light.

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

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