Miso-Fem

Indications

• Gastric ulcer
• Duodenal ulcer
• NSAID-induced peptic ulcer
• Termination of pregnancy following mifepristone
• Management of miscarriage

Dosage

Children: Oral preparations are not licensed for use in children under 3 years. For children aged 1–5 months, the dose is 1 mg/kg 3 times a day. For children aged 6 months to 2 years

Adults: For gastric and duodenal ulcers, the typical adult dose is 150 mg orally twice daily. For termination of pregnancy following mifepristone, the recommended dose is 400 micrograms orally.

Mechanism of action

Misoprostol stimulates prostaglandin E1 receptors on parietal cells in the stomach to reduce gastric acid secretion. It increases mucus and bicarbonate secretion, thickening the mucosal bilayer, and promotes the generation of new cells. In the uterus, Misoprostol binds to smooth muscle cells to enhance the strength and frequency of contractions, while also degrading collagen and reducing cervical tone.

Pharmacodynamics

Misoprostol acts as a prostaglandin E1 analog which is effective in reducing the risk of NSAID-induced gastric ulcers and is utilized in obstetric applications such as miscarriage management and abortion. Its onset of action varies by route: oral (8 minutes), sublingual (11 minutes), vaginal (20 minutes), and rectal (100 minutes), with durations of action ranging from approximately 2 to 4 hours.

Pharmacokinetics

Misoprostol is rapidly absorbed after oral administration, with bioavailability affected by food. It undergoes extensive first-pass metabolism, leading to a half-life of about 20-40 minutes. The drug is metabolized in the liver and its metabolites are eliminated primarily through the urine. The pharmacokinetic profile varies with administration route and formulation.

Contra-indications

• Hypersensitivity to misoprostol or any of its components
• Pregnancy (for certain indications such as termination)
• History of uterine rupture
• Severe cardiovascular disease
• Conditions where hypotension might precipitate severe complications

Adverse effects

• Diarrhea
• Abdominal pain
• Nausea
• Vomiting
• Headache
• Dizziness
• Uterine rupture (rare)
• Chills
• Fever
• Hot flushes
• Hypotension
• Malaise
• Toxic shock syndrome (rare)

Interactions

• Oxytocin (unknown additive effect)
• NSAIDs may have diminished efficacy when misoprostol is used concurrently

Precautions

• Monitor for coagulopathy during treatment
• Use with caution in patients with a history of inflammatory bowel disease
• Caution in patients with cardiovascular disease
• Patients should be informed about potential for diarrhea and other gastrointestinal side effects

Pregnancy

Not recommended during pregnancy except for specific medical indications such as termination of pregnancy following mifepristone, as it may induce contractions and lead to miscarriage.

Breast-feeding

Misoprostol is excreted in breast milk; caution is advised when administered to nursing mothers.

Storage

Store below 25°C. Protect from light and moisture.

Formulations

• Tablets: 200 micrograms, 400 micrograms
• Pessaries: 100 micrograms
• Oral solution

Indications

• Constipation
• Labor induction
• Topical treatment for skin conditions

Dosage

Children: Refer to the BNF for Children for appropriate pediatric dosing guidelines, as no specific doses are provided.

Adults: Refer to specific guidelines for adult dosing based on the formulation used and the condition being treated, as no standardized dose is provided.

Mechanism of action

Ricinoleic acid, the main active component of castor oil, acts as a stimulant laxative. It works by increasing the peristaltic movement of the intestines, which aids in the evacuation of stool. Additionally, it may inhibit the absorption of water in the intestines, resulting in softer stools. The oil is also believed to have anti-inflammatory properties, which can be beneficial in treating certain skin conditions.

Pharmacodynamics

The pharmacodynamic properties of castor oil include its ability to stimulate intestinal motility and increase the secretion of intestinal fluids. This leads to a faster transit time for stool through the bowel. In topical applications, castor oil exhibits emollient and moisturizing effects, promoting healing and soothing irritated skin. Its anti-inflammatory effects may also contribute to the reduction of swelling and pain in inflamed tissues.

Pharmacokinetics

Castor oil is absorbed in the gastrointestinal tract, where it is metabolized to ricinoleic acid. The onset of action for its laxative effect typically occurs within 2 to 6 hours after oral administration. The duration of action varies, but effects usually last for several hours. When applied topically, castor oil penetrates the skin and may provide localized effects without significant systemic absorption.

Adverse effects

• Abdominal cramps
• Diarrhea
• Nausea
• Vomiting
• Dehydration

Precautions

• Use with caution in patients with gastrointestinal disorders
• Not recommended for prolonged use
• Monitor for signs of dehydration

Pregnancy

Castor oil is generally not recommended during pregnancy due to potential uterine contractions and risk of premature labor.

Breast-feeding

Castor oil should be used with caution during breastfeeding as it may cause gastrointestinal discomfort in nursing infants.

Storage

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

Formulations

• Liquid
• Capsules

Indications

• Constipation
• Dietary fiber supplementation
• Irritable bowel syndrome
• Diverticular disease
• Weight management

Dosage

Children: Refer to appropriate guidelines for specific dosage; generally taken with adequate fluid intake.

Adults: Refer to appropriate guidelines for specific dosage; generally taken with adequate fluid intake.

Mechanism of action

Cellulose acts primarily as a bulk-forming laxative. It absorbs water in the intestines, which increases stool bulk and stimulates peristalsis, thus facilitating bowel movements. Additionally, cellulose is not digestible by human enzymes, leading to fermentation by gut bacteria, which may enhance gut health and alter gut microbiota composition.

Pharmacodynamics

Cellulose increases stool weight and frequency of bowel movements. It works by retaining water in the intestines, leading to softer stools and improved passage through the gastrointestinal tract. The bulking effect of cellulose can help alleviate constipation and promote overall digestive health. It may also play a role in cholesterol reduction and glycemic control through its effects on digestion and absorption of nutrients.

Pharmacokinetics

Cellulose is not absorbed into the bloodstream due to its indigestible nature. Instead, it passes through the gastrointestinal tract, where it adds bulk to the stool. Its fermentation by colonic bacteria produces short-chain fatty acids, which may have beneficial effects on colon health. The onset of action for cellulose as a laxative can vary but is generally within 24 to 72 hours after ingestion.

Adverse effects

• Bloating
• Flatulence
• Diarrhea
• Abdominal discomfort

Precautions

• Use with caution in patients with a history of gastrointestinal disorders.
• Monitor for potential allergic reactions in sensitive individuals.

Pregnancy

Cellulose is generally considered safe during pregnancy as it is a non-toxic, indigestible fiber.

Breast-feeding

Cellulose is also considered safe during breastfeeding; it is excreted in breast milk in negligible amounts.

Storage

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

Formulations

• Powder
• Capsules
• Tablets
• Granules

Dosage

Children: Refer to specific clinical guidelines for dosing in children, as no standard paediatric dosage is specified in the provided resources.

Adults: Refer to specific clinical guidelines for dosing, as no standard adult dosage is specified in the provided resources.

Mechanism of action

Ethylene glycol toxicity results from its metabolism to glycolic acid and other toxic metabolites. Glycolate accumulates in the body and is eliminated more slowly than ethylene glycol itself. The renal excretion of both compounds plays a crucial role in their elimination, accounting for a significant portion of the administered dose.

Pharmacodynamics

The pharmacodynamics of glycolate are closely tied to its role as a metabolite of ethylene glycol. Its accumulation can lead to metabolic acidosis, although minimal clinical effects have been observed at low doses. The relationship between glycolate and ethylene glycol indicates that glycolate may contribute to the overall toxic effects of ethylene glycol ingestion.

Pharmacokinetics

The pharmacokinetics of glycolate indicate that it reaches peak plasma levels between 4-6 hours after the administration of ethylene glycol. The elimination half-life of ethylene glycol is approximately 1.7 hours in rats and 3.4 hours in dogs. Glycolate is predominantly eliminated through renal excretion, with about 5% of the dose being excreted unchanged.

Pregnancy

There is limited data on the safety of glycolate in pregnancy. Caution is advised.

Breast-feeding

Data on the excretion of glycolate in human milk is not available. Caution is advised.

Storage

Store at room temperature, away from light and moisture.

Dosage

Children: Paediatric dosing information is not standardized and should be derived from specific product guidelines or expert consultation.

Adults: Dosage and usage depend on the specific hydrogenated compound and its intended therapeutic application. Refer to specific product guidelines for detailed dosing information.

Mechanism of action

Hydrogenation alters the molecular structure of fatty acids, transforming double bonds into single bonds. This process increases the saturation level of fats, which can influence their metabolic pathways and lipid profiles in the body.

Pharmacodynamics

The pharmacodynamic effects of hydrogenated compounds depend on the specific substance being hydrogenated. Generally, hydrogenated fats can affect lipid metabolism, potentially leading to increased levels of LDL cholesterol and decreased levels of HDL cholesterol when consumed in excess. The physiological effects may include changes in insulin sensitivity and inflammatory responses.

Pharmacokinetics

The pharmacokinetics of hydrogenated compounds vary widely based on the specific hydrogenated product. Generally, these compounds are absorbed in the gastrointestinal tract, where they may undergo further metabolism by enzymes. The bioavailability, distribution, metabolism, and excretion depend on the fatty acid composition and the presence of other dietary components.

Pregnancy

Hydrogenated compounds, depending on their specific type, may have varying safety profiles in pregnancy. It is essential to consult specific guidelines or studies related to the particular hydrogenated substance in question.

Breast-feeding

The safety of hydrogenated compounds during breastfeeding may vary. Consultation with healthcare professionals regarding specific substances is advisable.

Storage

Hydrogenated substances should be stored in a cool, dry place, away from direct sunlight and heat to maintain stability.

Indications

• Used as an excipient in tablet formulations
• Used as a bulking agent in capsule formulations
• Used in food products as a thickener or stabilizer

Dosage

Children: Refer to specific product guidelines as dosage will depend on the formulation and the active ingredients.

Adults: Refer to specific product guidelines as dosage will depend on the formulation and the active ingredients.

Mechanism of action

Microcrystalline cellulose acts as a non-digestible filler that enhances the flow properties of powders during the manufacturing of tablets and capsules. It does not have a direct pharmacological action on the body but ensures that the active ingredients are effectively delivered to the patient.

Pharmacodynamics

As a non-active ingredient, microcrystalline cellulose does not exert pharmacodynamic effects typical of active pharmaceutical ingredients. Its primary role is to provide a stable and consistent matrix for the drug, facilitating the release of the active compound once ingested.

Pharmacokinetics

Microcrystalline cellulose is not absorbed in the gastrointestinal tract; it passes through the digestive system largely unchanged. It adds bulk to the stool, which may aid in promoting regular bowel movements. The substance is excreted in feces, where it contributes to dietary fiber intake.

Pregnancy

Data regarding the use of microcrystalline cellulose during pregnancy is limited. It is advisable to consult with healthcare professionals before use.

Breast-feeding

Microcrystalline cellulose is considered safe during breastfeeding, as it is not absorbed systemically.

Storage

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

Indications

• Nutritional supplementation
• Energy source in enteral nutrition
• Excipient in pharmaceutical formulations

Dosage

Children: Refer to specific guidelines or product inserts for dosing information, as it can vary based on the context of use.

Adults: Refer to specific guidelines or product inserts for dosing information, as it can vary based on the context of use.

Mechanism of action

Starch is broken down into glucose units by enzymes such as amylase during digestion. The glucose is then absorbed in the intestines and utilized for energy production in the body's cells. This pathway involves hydrolysis of the glycosidic bonds, converting starch into simpler sugars.

Pharmacodynamics

Starch primarily serves as an energy source. Its digestion and absorption lead to an increase in blood glucose levels, which provides energy for metabolic processes. In this context, it plays a crucial role in maintaining energy homeostasis in the body.

Pharmacokinetics

Starch is not absorbed in its polymeric form; it must first be enzymatically hydrolyzed into simpler sugars such as maltose and glucose. The digestion and absorption of starch occur predominantly in the small intestine, with glucose being readily absorbed into the bloodstream. The rate of absorption can vary depending on the type of starch and its physical form.

Adverse effects

• Allergic reactions
• Gastrointestinal discomfort
• Diarrhea
• Constipation

Precautions

• Use with caution in individuals with known allergies to starch or starch derivatives
• Monitor for gastrointestinal symptoms in patients with a history of digestive disorders

Pregnancy

Starch is generally considered safe for use during pregnancy. However, it should be consumed in moderation as part of a balanced diet.

Breast-feeding

Starch is deemed safe for nursing mothers when used in moderation as part of a balanced diet.

Storage

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

Formulations

• Powder
• Granules
• Tablets
• Suspensions

Mechanism of action

Ethylene glycol toxicity results from its metabolism to glycolic acid and other toxic metabolites. The accumulation of glycolate and the elimination kinetics of ethylene glycol and its metabolites are not well understood, so studies with male Sprague-Dawley rats and mixed breed dogs have been carried out. Ethylene glycol was administered by gavage to rats and dogs which were placed in metabolic cages for urine and blood sample collection at timed intervals. The peak plasma level of ethylene glycol occurred at 2 hr after dosing and that of glycolate between 4-6 hr. The rate of ethylene glycol elimination was somewhat faster in rats with a half-life of 1.7 hr compared to 3.4 hr in dogs. The maximum plasma level of glycolate was greater in rats although the pattern of accumulation was similar to that in dogs. Glycolate disappeared from the plasma at the same time as ethylene glycol, suggesting a slower rate of elimination of the metabolite than that of ethylene glycol. Renal excretion of ethylene glycol was an important route for its elimination accounting for 20-30% of the dose. Renal excretion of glycolate represented about 5% of the dose. Ethylene glycol induced an immediate, but short lived diuresis compared to that in control rats. Minimal clinical effects (mild acidosis with no sedation) were noted at these doses of ethylene glycol (1-2 g/kg) in both rats and dogs. The results indicate that the toxicokinetics of ethylene glycol and glycolate were similar in both species. The effect of 0.35 to 0.8 mmol/kg glycolic acid and 1.0 to 4.4 mmol/kg sodium glycolate on cyclopropane-epinephrine induced cardiac arrhythmias was examined using dogs. Doses of 0.35 to 0.5 mmol/kg glycolic acid increased the duration of arrhythmias in the 13 dogs tested, whereas doses >0.5 mmol/kg decreased or totally eliminated the arrhythmias in each of 11 dogs. Depression was observed for many of the dogs at higher doses. Sodium glycolate was much less effective in decreasing the arrhythmias, with 3 mmol/kg being required and its action being transient.

Mechanism of action

Misoprostol is a synthetic prostaglandin E1 analog that stimulates prostaglandin E1 receptors on parietal cells in the stomach to reduce gastric acid secretion. Mucus and bicarbonate secretion are also increased along with thickening of the mucosal bilayer so the mucosa can generate new cells. Misoprostol binds to smooth muscle cells in the uterine lining to increase the strength and frequency of contractions as well as degrade collagen and reduce cervical tone. Misoprostol enhances natural gastromucosal defense mechanisms and healing in acid-related disorders, probably by increasing production of gastric mucus and mucosal secretion of bicarbonate. Misoprostol inhibits basal and nocturnal gastric acid secretion by direct action on the parietal cells; also inhibits gastric acid secretion stimulated by food, histamine, and pentagastrin. It decreases pepsin secretion under basal, but not histamine stimulation. Misoprostol has no significant effect on fasting or postprandial gastrin or intrinsic factor output.

Pharmacodynamics

Misoprostol is a prostaglandin E1 analog used to reduce the risk of NSAID induced gastric ulcers by reducing secretion of gastric acid from parietal cells. Misoprostol is also used to manage miscarriages and used alone or in combination with mifepristone for first trimester abortions. An oral dose of misoprostol has an 8 minute onset of action and a duration of action of approximately 2 hours, a sublingual dose has an 11 minute onset of action and a duration of action of approximately 3 hours, a vaginal dose has a 20 minute onset of action and a duration of action of approximately 4 hours, and a rectal dose has a 100 minute onset of action and a duration of action of approximately 4 hours.