Dormifor 1% I.V. Emulsion

Indications

• Constipation
• Bowel cleansing

Dosage

Children: Child 1–11 months: 1 g as required, Child 1–11 years: 2 g as required, Child 12–17 years: 4 g as required.

Adults: 4 g as required, usually administered rectally.

Mechanism of action

When administered rectally, glycerol exerts a hygroscopic and/or local irritant action, drawing water from the tissues into the feces and reflexively stimulating evacuation. It decreases intraocular pressure by creating an osmotic gradient between the blood and intraocular fluid, causing fluid to move from the aqueous and vitreous humors into the bloodstream. Glycerol is classified as a hyperosmotic laxative and may also have lubricating and fecal softening effects.

Pharmacodynamics

Glycerol is commonly classified as an osmotic laxative, acting through its local irritant effects and possibly having lubricating and fecal softening actions. Glycerol suppositories usually produce effects within 15 to 30 minutes, providing quick relief from constipation.

Pharmacokinetics

Glycerol is rapidly absorbed through the gastrointestinal tract. It is metabolized in the liver and other tissues, with a half-life that varies depending on the route of administration. Following rectal administration, glycerol is primarily excreted in urine. The pharmacokinetics may vary based on dosage forms and individual patient factors.

Contra-indications

• Acute abdominal conditions
• Acute inflammatory bowel disease
• Intestinal obstruction
• Severe dehydration

Adverse effects

• Abdominal cramps
• Asthenia
• Gastrointestinal disorders
• Hypermagnesaemia
• Skin reactions
• Urine discolouration

Precautions

• Avoid prolonged contact with skin, especially in incontinent patients or infants wearing nappies due to the risk of irritation and excoriation.
• Excessive use may cause diarrhea and related effects such as hypokalaemia.

Pregnancy

Manufacturers advise avoidance due to limited information available.

Breast-feeding

Manufacturers advise avoidance as there is no information available.

Storage

Store at room temperature, away from direct sunlight.

Formulations

• Glycerol 1g suppositories
• Glycerol 2g suppositories
• Glycerol 4g suppositories
• Glycerol oral suspension

Indications

• Induction of general anesthesia
• Maintenance of general anesthesia
• Sedation for procedures

Dosage

Children: For children aged 1 month to 16 years, the usual dose for induction of anesthesia is 2.5–4 mg/kg, adjusted according to age, body weight, and response.

Adults: For induction of anesthesia, the usual adult dose is 1.5–2.5 mg/kg administered by slow intravenous injection. For maintenance, a continuous infusion of 4–12 mg/kg/hour may be used.

Mechanism of action

Propofol exerts its anesthetic effects by positively modulating the inhibitory neurotransmitter gamma-aminobutyric acid (GABA) at GABA-A receptors, leading to increased inhibitory neurotransmission and resulting in sedation and anesthesia.

Pharmacodynamics

As a sedative-hypnotic agent, propofol rapidly induces hypnosis with minimal excitation, typically within 40 seconds after intravenous administration. This rapid action is due to its high lipid solubility, allowing for quick distribution to the central nervous system. The drug also has a favorable recovery profile, with patients often regaining consciousness shortly after cessation of the infusion.

Pharmacokinetics

Propofol is highly lipophilic, leading to rapid distribution and a short half-life. It is primarily metabolized in the liver via conjugation and oxidation, and excreted in urine, mainly as metabolites. The drug has a volume of distribution of around 4 liters per kilogram, and its clearance is approximately 1.5 liters per minute, which results in a short duration of action.

Contra-indications

• Hypersensitivity to propofol or any of its components
• Severe respiratory depression
• Acute porphyrias
• Acute circulatory failure (shock)
• Adrenal insufficiency

Adverse effects

• Apnea
• Hypotension
• Nausea
• Respiratory disorders
• Skin reactions
• Vascular pain
• Vomiting
• Arrhythmias
• Cough
• Hiccups
• Hypertension
• Muscle rigidity
• Neuromuscular dysfunction
• Nystagmus
• Procedural complications

Interactions

• Valproate may increase propofol concentration
• Active component of sacituzumab govitecan may increase exposure to propofol

Precautions

• Careful monitoring of fluids and electrolytes
• Use with caution in patients with cardiovascular disease
• Elderly patients may require dose adjustment
• Avoid in patients with fixed cardiac output, hypovolaemia, or severe hypotension

Pregnancy

Propofol should be used during pregnancy only if clearly needed and after careful consideration of risks and benefits.

Breast-feeding

Propofol is excreted in breast milk; caution should be exercised when administered to breastfeeding women.

Storage

Store at room temperature, protect from light, and do not freeze.

Formulations

• Emulsion for injection
• 0.5% or 1% injection solution

Dosage

Children: Refer to specific guidelines for pediatric dosing; consult the BNF for Children for accurate dosage information.

Adults: Refer to specific guidelines for use; dosage may vary based on the context of use.

Mechanism of action

Hydroxide ions act primarily as bases, neutralizing acids to form water and salts. They participate in various biochemical pathways, including selenium metabolism and the degradation of reactive oxygen species. Hydroxide can influence enzyme activity and stability by altering the pH of the environment, thereby affecting metabolic reactions.

Pharmacodynamics

Hydroxide ions can impact biological processes by changing the local pH, which influences enzyme activity, ion transport, and the solubility of other compounds. Their ability to neutralize acids can help regulate physiological pH, contributing to homeostasis in living organisms.

Pharmacokinetics

As an inorganic ion, hydroxide does not undergo traditional pharmacokinetic processes like absorption, distribution, metabolism, or excretion. Instead, it is rapidly equilibrated in biological fluids and participates in acid-base reactions, having immediate effects on the local environment.

Pregnancy

There is limited information regarding the use of hydroxide during pregnancy. Consult a healthcare professional for advice.

Breast-feeding

Limited data is available on the excretion of hydroxide in breast milk. Consult a healthcare professional before use.

Storage

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

Indications

• Cryotherapy for the destruction of abnormal tissue
• Treatment of warts, moles, and other skin lesions
• Nitrogen narcosis in diving

Dosage

Children: Refer to the BNF for Children for appropriate dosing recommendations in paediatric patients.

Adults: For cryotherapy, the dosage and duration depend on the specific condition being treated and should be determined by the healthcare provider. Refer to specific guidelines for each condition.

Mechanism of action

In cryotherapy, the mechanism of action involves three stages: heat transfer, cell injury, and inflammation. The boiling point of liquid nitrogen is -196°C, which initiates heat transfer, leading to cell injury during the thawing process. The inflammation stage follows, characterized by edema and erythema, resulting from cellular death and contributing to local cell destruction. Additionally, nitrogen can cause direct toxic effects on brain functions, leading to nitrogen narcosis, which impairs cognitive abilities and motor functions due to its impact on nerve conduction.

Pharmacodynamics

Nitrogen's pharmacodynamics relate to its behavior in cryotherapy and asphyxiation. In cryotherapy, it induces tissue destruction through rapid cooling, leading to apoptosis of abnormal cells. In high-pressure environments, nitrogen narcosis affects the central nervous system, producing symptoms similar to alcohol intoxication, ultimately decreasing reasoning, decision-making abilities, and manual dexterity.

Pharmacokinetics

Nitrogen does not undergo metabolism in the traditional sense, as it is an inert gas at physiological conditions. Its pharmacokinetics involve physical principles of gas exchange and partial pressures. In the case of nitrogen narcosis, the effects are influenced by the partial pressure of nitrogen in the bloodstream, which increases with depth during diving. Nitrogen is primarily eliminated from the body through respiration.

Adverse effects

• Narcotic effect at high pressures
• Stupor or euphoria
• Decreased motor function and manual dexterity
• Asphyxiation due to oxygen displacement

Precautions

• Careful monitoring in environments with high nitrogen pressures
• Avoidance of rapid ascents in diving to prevent nitrogen narcosis
• Use in controlled settings to prevent asphyxiation risks

Pregnancy

Nitrogen is generally considered safe in terms of direct effects during pregnancy; however, the safety of exposure in high-pressure environments should be assessed.

Breast-feeding

Nitrogen is not known to affect breastfeeding; however, caution is recommended in environments where nitrogen levels may displace oxygen.

Storage

Store in a cool, dry place away from heat sources; liquid nitrogen should be handled with care due to extreme cold.

Formulations

• Liquid nitrogen
• Nitrogen gas (compressed)

Dosage

Children: Refer to specific formulations for dosing guidelines.

Adults: Refer to specific formulations for dosing guidelines.

Mechanism of action

Phospholipids primarily function as structural components of cell membranes, contributing to membrane fluidity and flexibility. They also play a critical role in cell signaling and the formation of lipid rafts, which are microdomains within the membrane that facilitate protein-protein interactions and signal transduction pathways.

Pharmacodynamics

Phospholipids are essential for maintaining the integrity and functionality of cellular membranes. They participate in the formation of lipid bilayers, which create a barrier to protect cellular contents and regulate the movement of ions and molecules in and out of the cell. Additionally, phospholipids are involved in the activation of various cell signaling pathways that influence cell growth, differentiation, and apoptosis.

Pharmacokinetics

Phospholipids are generally absorbed through dietary sources, where they are broken down into free fatty acids and glycerol in the gastrointestinal tract. They can be incorporated into lipoproteins and transported via the bloodstream to various tissues. The metabolism of phospholipids involves enzymatic hydrolysis by phospholipases, leading to the release of fatty acids and other bioactive lipid mediators.

Pregnancy

Phospholipids are generally considered safe during pregnancy as they are naturally occurring components of cell membranes, however, specific formulations should be evaluated on a case-by-case basis.

Breast-feeding

Phospholipids are present in breast milk and are considered safe during breastfeeding, but specific formulations should be discussed with a healthcare professional.

Storage

Store in a cool, dry place away from direct sunlight. Specific storage conditions may vary depending on the formulation.

Dosage

Children: Refer to specific drug formulations and product labels as purified substances can vary widely in their use and dosing.

Adults: Refer to specific drug formulations and product labels as purified substances can vary widely in their use and dosing.

Mechanism of action

The mechanism of action for purified compounds varies widely depending on the specific substance. Generally, purified drugs exert their effects by interacting with specific biological targets, such as receptors, enzymes, or ion channels, leading to a desired therapeutic effect. This interaction can involve binding to receptors to activate or inhibit signaling pathways, modulating enzymatic activity, or altering physiological processes.

Pharmacodynamics

Pharmacodynamics describes the effects of a drug on the body and the relationship between drug concentration and effect. For purified drugs, this can involve dose-response relationships and the time course of their action. The purified form often enhances potency and reduces variability in response among patients, which can lead to more predictable therapeutic outcomes. The overall effect is determined by the drug's affinity for its target, the efficacy of the drug-receptor interaction, and the downstream signaling pathways activated as a result of this interaction.

Pharmacokinetics

Pharmacokinetics involves the absorption, distribution, metabolism, and excretion (ADME) of a drug. For purified substances, absorption can be more efficient due to the absence of impurities that may affect solubility or stability. Distribution may also be enhanced, leading to higher bioavailability. Metabolism can be influenced by the structure of the purified compound, as it may be metabolized more readily by liver enzymes. Excretion typically occurs through the kidneys or liver, depending on the molecular characteristics of the purified drug.

Pregnancy

Consult with a healthcare professional, as the safety of purified forms of medications during pregnancy may vary depending on the specific substance.

Breast-feeding

Consult with a healthcare professional, as the safety of purified forms of medications during breastfeeding may vary depending on the specific substance.

Storage

Store in a cool, dry place, away from light and moisture, and keep out of reach of children.

Indications

• Cardiovascular health
• Menopausal symptom relief
• Bone health
• Cholesterol management
• Potential cancer risk reduction

Dosage

Children: Refer to specific product guidelines or consult a healthcare professional for appropriate dosage.

Adults: Refer to specific product guidelines or consult a healthcare professional for appropriate dosage.

Mechanism of action

Soybeans contain isoflavones, which are phytoestrogens that can mimic the effects of estrogen in the body. They exert their effects primarily through binding to estrogen receptors and modulating gene expression related to estrogen-responsive pathways. This interaction can influence various physiological processes, including bone density, lipid metabolism, and hormonal balance.

Pharmacodynamics

The pharmacodynamics of soybeans are attributed to their content of isoflavones, notably genistein and daidzein. These compounds may exhibit antioxidant properties, modulate lipid profiles by lowering LDL cholesterol, and influence bone metabolism. Additionally, the anti-inflammatory effects of soy isoflavones may contribute to cardiovascular benefits. The bioactive compounds in soybeans can also have protective effects against certain cancers, particularly hormone-sensitive types, by interfering with cancer cell growth and proliferation.

Pharmacokinetics

Isoflavones are absorbed in the gastrointestinal tract, with peak plasma concentrations typically occurring within 1 to 3 hours after ingestion. The bioavailability of isoflavones can be influenced by factors such as food matrix, gut microbiota, and individual metabolism. Soy isoflavones undergo extensive metabolism in the liver, resulting in various metabolites, some of which may exhibit different biological activities. The elimination half-life of isoflavones can vary widely, depending on individual factors and the form in which soy is consumed.

Adverse effects

• Allergic reactions
• Gastrointestinal disturbances
• Nausea
• Diarrhea
• Flatulence

Precautions

• Use with caution in individuals with a known allergy to soy products.
• Monitor for potential interactions with anticoagulants, as soybean contains vitamin K.

Pregnancy

Soybean is generally considered safe during pregnancy when consumed in food amounts. However, high doses or supplements should be avoided due to potential hormonal effects.

Breast-feeding

Soybean is likely safe in food amounts during breastfeeding, but high doses or supplements should be approached with caution.

Storage

Store in a cool, dry place, away from direct sunlight. Keep tightly closed to avoid moisture.

Formulations

• Whole soybeans
• Soy flour
• Soy protein isolate
• Soy milk
• Soy oil
• Soy lecithin

Mechanism of action

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. Glycerin (glycerol) and sorbitol are hyperosmotic laxatives. When administered rectally, glycerin and sorbitol exert a hygroscopic and/or local irritant action, drawing water from the tissues into the feces and reflexly stimulating evacuation. The extent to which the simple physical distention of the rectum and the hygroscopic and/or local irritant actions are responsible for the laxative effects of some of these drugs is not known. Only extremely high oral doses of sorbitol (25 g daily) or glycerin exert laxative action. /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. The physicochemical effects of a series of alkanols, alkanediols and glycerol on erythrocyte shape and hemolysis at 4 and 20 degrees C were examined. We calculated the dielectric constant of the incubation medium, Ds, and the dielectric constant of the erythrocyte membrane Dm in the presence of organic solutes. The ratio Ds/Dm = -38.48 at 20 degrees C defines the normal biconcave shape in a medium without hemolytic agents. A decrease in Ds/Dm favors externalization or internalization with consequent hemolysis. Alkanols and alkanediols convert biconcave erythrocytes into echinocytes, which is accompanied by an increase in the projected surface area. Glycerol converts biconcave erythrocytes into stomatocytes, which was accompanied by a marginal decrease in the projected surface area. Progressive externalization in alkanols and alkanediols or internalization in glycerol resulted in a decrease in the projected surface area and the formation of smooth spheres. The degree of shape change induced was related to the degree of hemolysis and the ratio Ds/Dm. A decrease in temperature reduced both the degree of shape change and hemolysis. .../Thus/ physicochemical toxicity may be a result of a temperature dependent hydrophobic interaction between the organic solutes and the membrane and is best interpreted by the ability of the solutes to change Ds and Dm.

Pharmacodynamics

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.

Mechanism of action

The action of propofol involves a positive modulation of the inhibitory function of the neurotransmitter gama-aminobutyric acid (GABA) through GABA-A receptors.

Pharmacodynamics

Propofol is a sedative-hypnotic agent for use in the induction and maintenance of anesthesia or sedation. Intravenous injection of a therapeutic dose of propofol produces hypnosis rapidly with minimal excitation, usually within 40 seconds from the start of an injection (the time for one arm-brain circulation).

Mechanism of action

In cryotherapy, mechanism of action could be classified into three stages: 1. heat transfer, 2. cell injury and 3. inflammation. Boiling point of liquid nitrogen is -196°C, which is the responsible for creating the initial stage which is heat transfer. The second stage is cell injury which is induced during thawing conditions of the cells. The last step in the cryotherapy is the inflammation stage which is characterized by edema and erythema. Inflammation occurs as a result of cellular death and it helps in local cell destruction. ... Nitrogen also has a direct toxic action of its own, affecting brain functions and inducing a stupor or euphoria. Nitrogen narcosis ("rapture of the deep" or "the martini effect") results from a direct toxic effect of high nitrogen pressure on nerve conduction and produces effects similar to alcohol intoxication. Complex reasoning, decision-making ability, motor function, and manual dexerity decrease. Individuals vary in this response widely, but it typically can be noticed among divers at depths exceeding 100 ft (30 m). For example, certain individuals experience no effect at depths of < or = 130 ft, whereas others feel some effect at around 80 ft. Nonetheless, the narcotic effect increases with increasing depth so that each additional 50 ft incrementally produces the effect of "another martini". A simple asphyxiant, nitrogen's main toxicty arises from its ability to displace O2 and generate an atmosphere that does not support the chemical reactions needed for maintenance of life. The displacement of O2 can be complete or incomplete, leading to varying degrees of hypoxia. Nitrogen is an inert substance and does not exert a direct toxicological effect. Nitrogen acts by the physiological effect of simple asphyxia on the target species within a Controlled Atmosphere Treatment (CAT) bubble. The biocide action of nitrogen is due to its displacement of oxygen from an atmospheric oxygen level of 20.8% to levels < 0.2% v/v in the CAT bubble. The level of oxygen is the critical factor. Victims exposed to atmospheres deficient in oxygen, i.e. < 19%, will begin to display signs and symptoms of oxygen-deficient exposure of air due to an increase in nitrogen.