Anusol Soothing Relief Suppositories

Uses

This ointment is used for the comprehensive symptomatic treatment of internal and external hemorrhoids and pruritus ani.

Anusol Soothing Relief Suppositories is also used to associated treatment for these conditions: Lice, ScabiesHemorrhoidsAnal Fissures, Hemorrhoids, Malodorous flatulence, Pruritus Ani, Malodorous stoolAcute, Inflammatory Superficial Cutaneous Lesions caused by susceptible bacteria, Adrenal cortical hypofunctions, Anal Fissures, Anal inflammation, Androgenital syndrome, Conjunctivitis, Conjunctivitis allergic, Corneal Inflammation, Dermatitis infected, Diaper Dermatitis, Eczema infected, Episcleritis, Hemorrhoids, Iridocyclitis, Iritis, Ocular Inflammation, Ocular Irritation, Postoperative pain, Proctitis, Pruritus, Pruritus Ani, Radiation Induced Proctitis, Rheumatoid Arthritis, Scleritis, Skin Infections, Skin Irritation, Superficial ocular bacterial infections caused by susceptible bacteria, Thyroiditis, Ulcerative Colitis, Anal eczema, Bacterial blepharitis, Corneal clouding, Corticosteroid responsive Dermatosis of the anal region, Corticosteroid-responsive dermatoses, Cryptitis, Localized uninfected hemorrhoids, Mild Anal Fissures, Pruritus associated with bowel movements, Skin and skin-structure infections caused by susceptible bacteria, Postoperative Eye CareAcute Wounds, Burns first degree, Burns second degree, Dermatitis, Eczematous, Diaper Rash, Herpes Labialis, Injuries to the Nipple (Fissures and Cracks) Resulting Breastfeeding, Intertrigo, Pain, Pruritus, Sensitive Skin, Skin Irritation, Skin candida, Sunburn, Wounds, Chafing, Damaged skin, Dry, cracked skin, Facial rash, Heat rash, Superficial Wounds, Watery skin lesions, Astringent, Nutritional supplementation

How Anusol Soothing Relief Suppositories works

Benzyl benzoate exerts toxic effects on the nervous system of the parasite, resulting in its death. It is also toxic to mite ova, though its exact mechanism of action is unknown. In vitro, benzyl benzoate has been found to kill the Sarcoptes mite within 5 minutes.

Bismuth salts exert their action largely in the upper gastrointestinal tract by way of local activity from luminal bismuth in the stomach and duodenum .

In terms of bismuth subgallate's ability to deodorize flatulence and stools as an internal deodorant - although not fully elucidated - it is believed that when the substance is administered orally, its relative insolubility and poor absorption allows it to remain within the gastrointestinal lumen and inhibit colonic bacteria from acting on fermentable food residues in the GI tract .

Moreover, when bismuth subgallate is taken orally, various salts like bismuth citrate, bismuth oxychloride, and others are formed . These salts are then taken up into surrounding gastric mucus as well as bound to protein within the base of any ulcers that may be present after coming into contact with gastric juice . Additionally, bismuth compounds like bismuth subgallate are also believed to have the capacity to trigger the secretion of prostaglandins, epithelial growth factor (EGF), and mucosal bicarbonate as a means to inhibit the action of pepsin in gastric juice . These actions subsequently protect gastric mucous from peptic luminal degradation as well as enhance the properties of mucous to assist in the healing of both duodenal and gastric ulcers . In this way, bismuth subgallate works to absorb extra water and/or toxins in the large intestine, allowing it to form a protective coat on the intestinal mucosa and over ulcers that may or may not be associated with infections like those of Helicobacter pylori .

Furthermore, studies have shown that bismuth compounds like bismuth subgallate are capable of demonstrating antimicrobial effects against various gastrointestinal tract pathogens like E. coli, Salmonella, Shigella, Vibrio cholera, Campylobacter jejuni, H. pylori, and some enteric viruses like Rotaviruses . Although the exact mechanism(s) of action by which bismuth compounds are able to elicit such antimicrobial effects remains unclear , a number of experimental observations suggest that bismuth has been able to complex with the bacterial wall and periplasmic membrane; inhibit bacterial enzymes like urease, catalase, and lipase; inhibit bacterial protein and ATP synthesis; and also inhibit or decrease the adherence of bacteria like H. pylori to epithelial cells . In essence, ultrastructural studies have shown evidence of the binding of bismuth complexes to the bacterial wall and periplasmic space between the inner and outer bacterial membrane of H.pylori with subsequent ballooning and disintegration of the pathogen . To various extents, these antimicrobial actions may also illustrate how bismuth subgallate is capable of neutralizing colonic bacteria from acting on fermentable foods as well.

Numerous studies have and continue to study the possible hemostatic action that bismuth subgallate may have. As the bismuth salt of gallic acid, bismuth subgallate's chemical structure shares similarities to ellagic acid, another gallic acid derivative . Ellagic acid itself is a clot-promoting agent that initiates thrombin formation by way of the intrinsic pathway via an action on Hageman factor (clotting factor XII) . It is believed that bismuth subgallate's ability to activate factor XII is associated with the chemical's negatively charged moieties - whose contact with factor XII would theoretically initiate the intrinsic pathway to blood clotting .

Other studies have also suggested that bismuth subgallate is capable of inducing macrophages to secrete growth factors to facilitate wound healing, decreasing lesion area, enhancing granulation tissue formation and re-epithelialization, the initiation of the proliferation of collagen via the activation of fibroblasts, the accelerated re-establishment of blood vessels, and also the restriction of nitric oxide formation .

Given such studies regarding bismuth subgallate's potential hemostatic abilities, there has been and continues to be interest in indicating the agent for use in otolaryngology as in tonsillectomies or adenotonsillectomies to achieve reduced bleeding and surgery times; topical treatment in various open wound surgeries to facilitate faster and earlier clotting between tissues; ileostomy; dental surgeries; epistaxis management; among others . Nevertheless, study results are conflicting; where there may be experimental results suggesting some improvements in reduced operation time and operative blood loss when bismuth subgallate is used as a hemostatic agent in tonsillectomies there are also study results that observed bismuth subgallate having a negative influence on the healing processes of wounds inflicted in animal models, in which the use of the agent actually delayed the rate of new vessel formation and optimal wound healing .

Finally, bismuth subgallate also demonstrates a strong astringent ability - an action that can facilitate both its deodorant and hemostatic effects and assists in its indication as an active ingredient in a number of non-prescription products for hemorrhoid suppositories or topical applications, diarrhea, etc .

Hydrocortisone binds to the cytosolic glucocorticoid receptor. After binding the receptor the newly formed receptor-ligand complex translocates itself into the cell nucleus, where it binds to many glucocorticoid response elements (GRE) in the promoter region of the target genes. The DNA bound receptor then interacts with basic transcription factors, causing the increase in expression of specific target genes. The anti-inflammatory actions of corticosteroids are thought to involve lipocortins, phospholipase A2 inhibitory proteins which, through inhibition arachidonic acid, control the biosynthesis of prostaglandins and leukotrienes. Specifically glucocorticoids induce lipocortin-1 (annexin-1) synthesis, which then binds to cell membranes preventing the phospholipase A2 from coming into contact with its substrate arachidonic acid. This leads to diminished eicosanoid production. The cyclooxygenase (both COX-1 and COX-2) expression is also suppressed, potentiating the effect. In other words, the two main products in inflammation Prostaglandins and Leukotrienes are inhibited by the action of Glucocorticoids. Glucocorticoids also stimulate the lipocortin-1 escaping to the extracellular space, where it binds to the leukocyte membrane receptors and inhibits various inflammatory events: epithelial adhesion, emigration, chemotaxis, phagocytosis, respiratory burst and the release of various inflammatory mediators (lysosomal enzymes, cytokines, tissue plasminogen activator, chemokines etc.) from neutrophils, macrophages and mastocytes. Additionally the immune system is suppressed by corticosteroids due to a decrease in the function of the lymphatic system, a reduction in immunoglobulin and complement concentrations, the precipitation of lymphocytopenia, and interference with antigen-antibody binding.

It acts by providing a physical barrier to prevent skin irritation and help heal damaged skin.

Dosage

Anusol Soothing Relief Suppositories dosage

Adults (over 18 years): To be applied sparingly to the affected area at night, in the morning and after each evacuation up to a maximum of 4 applications a day. Thoroughly cleanse the affected area, dry and apply ointment on a gauze dressing. For internal conditions use the rectal applicator provided. Use for a maximum period of one week. This is topical administration only.

Pediatric Use: This medicine is not recommended for children under 18 years old.

Side Effects

Prolonged or excessive use may produce systemic corticosteroid effects, and use for periods longer than seven days is not recommended. Rarely, there are sensitivity reactions and Patients may occasionally experience transient burning on application especially if the anoderm is not intact.

Toxicity

Oral, rabbit: LD₅₀ = 1680 mg/kg; Skin, rabbit: LD₅₀ = 4000 mg/kg. Symptoms of overdose include blister formation, crusting, itching, oozing, reddening, or scaling of skin; difficulty in urinating (dribbling); jerking movements; sudden loss of consciousness.

Depending on the level of severity of a patient's renal impairment, administration of bismuth compounds may not be appropriate as the reduced renal clearance can lead to undesirably elevated blood levels of bismuth . Similarly, because of the biliary excretion of bismuth, severe liver disease may theoretically result in accumulation of bismuth as well .

Bismuth toxicity seemingly develops only from excessive dosage (perhaps from ingestion of bismuth over a prolonged time or intramuscular injections) and is characterized by nephrotoxicity, osteoarthropathy, encephalopathy, hepatotoxicity, stomatitis, and gingivitis . However, the insoluble inorganic bismuth compounds are reported to be mainly associated with reversible encephalopathy . In fact a number of studies have discussed how patients may experience a syndrome of subacute, progressive encephalopathy involving potential aphasia, myoclonous, and/or gait instability after taking bismuth subgallate in large quantities well over the usual recommended dosages . This kind of encephalopathy is usually reversible with the discontinuation of the bismuth subgallate usage however .

Side effects include inhibition of bone formation, suppression of calcium absorption and delayed wound healing

Acute oral toxicity (LD50): 7950 mg/kg [Mouse].

Precaution

As with all products containing topical steroids, the possibility of systemic absorption should be borne in mind. Prolonged or excessive use may produce systemic corticosteroid effects, and use for periods longer than seven days is not recommended. The product should be discontinued and the patient advised to consult a medical practitioner if symptoms do not improve or worsen or if rectal bleeding occurs.

Interaction

Concurrent use with other corticosteroid preparations either topically or orally may increase the likelihood of systemic effects.

Volume of Distribution

In general, oral administration is one of the most common routes of administration for non-prescription bismuth subgallate products and gastrointestinal and systemic absorption is usually very low.

Intended for local use only, no systemic absorption.

Elimination Route

No data are available on percutaneous absorption of benzyl benzoate. Some older studies have suggested some percutaneous absorption, however the amount was not quantified.

Bismuth subgallate is only slightly, if at all, absorbed after oral ingestion . The general human oral bioavailability of bismuth subgallate has been reported as low as 0.04% . Any absorption that does occur is likely to happen from the upper small intestine .

The gastrointestinal absorption of bismuth from bismuth compounds demonstrates a large interindividual variation . Factors affecting the absorption involve the formulation of the bismuth subgallate compound as well as the dietary factors of the individuals themselves . Nevertheless, absorption can be enhanced with the concomitant intake of citrate and sulfhydryl-group-containing compounds . Conversely, the simultaneous administration of antacids or a diet that is high in thiol content can lower absorption of bismuth subgallate .

Topical corticosteroids can be absorbed from normal intact skin. Inflammation and/or other disease processes in the skin increase percutaneous absorption.

No significant percutaneous absorption from topically applied zinc oxide.

Half Life

The bismuth component of bismuth subgallate is known to have a terminal half-life of 21-72 days .

6-8 hours

Intended for local use only, no systemic absorption.

Clearance

On average, the blood clearance of the bismuth component of a bismuth salt like bismuth subgallate is within the range of 50 to 95 ml/min .

Intended for local use only, no systemic absorption.

Elimination Route

Ingested bismuth is primarily eliminated unabsorbed by way of the faeces . Any absorbed bismuth is eliminated from the body by both the urinary and faecal (including bile) routes . Excretion of absorbed bismuth in the urine is rapid, with most of the metal excreted within 24 hours . About 10% of the absorbed bismuth is detected in faeces, presumably owing to biliary secretion .

Corticosteroids are metabolized primarily in the liver and are then excreted by the kidneys. Some of the topical corticosteroids and their metabolites are also excreted into the bile.

Intended for local use only, no systemic absorption.

Pregnancy & Breastfeeding use

There is inadequate evidence of safety in human pregnancy and there may be a very small risk of cleft palate and intrauterine growth retardation as well as suppression of the neonatal hypothalamic-pituitary-adrenal axis. No special precautions required for use during lactation, So Use in pregnancy only when there is no safer alternative and when the disease itself carries risks for the mother or child.

Contraindication

Tubercular, fungal and most viral lesions including herpes simplex vaccinia and varicella, History of sensitivity to any of the constituents.

Acute Overdose

Acute overdosage is very unlikely to occur, however, in the case of chronic overdosage or misuse, the features of hypercorticism may appear and in this situation topical steroids should be discontinued

No overdose related problem is yet reported.

Storage Condition

Do not store above 30°C & keep in a dry place. Protect from light. Do not freeze Keep out of the reach of children.

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