Biosulin 30:70

Indications

• Diabetes mellitus (type 1 and type 2)
• Diabetic ketoacidosis
• Hyperglycemia due to other conditions
• Management of blood glucose levels during surgery
• Continuous subcutaneous insulin infusion therapy

Dosage

Children: For children aged 1-17 years, insulin is administered immediately before meals or when necessary shortly after meals, according to individual requirements. Specific dosing should be determined based on blood glucose monitoring and should be referred to the BNF for Children for precise guidance.

Adults: The dosage of insulin varies based on individual needs and is typically guided by blood glucose monitoring. It is recommended to consult local protocols for specific dosing instructions.

Mechanism of action

Insulin has a direct inhibitory effect on lipase, which is involved in the mobilization of fatty acids. In the absence of insulin, there is an abnormally high rate of conversion of protein to glucose, primarily in the liver. Insulin stimulates glycogen synthesis and enhances facilitated diffusion of glucose and the active transport of amino acids, although the exact mechanisms for these actions are not fully understood.

Pharmacodynamics

Insulin's primary pharmacodynamic effect is the reduction of blood glucose levels. It promotes the uptake of glucose by cells, increases glycogen synthesis in the liver, and inhibits gluconeogenesis. Insulin also influences lipid metabolism by inhibiting lipolysis and encouraging fat storage. Additionally, insulin enhances protein synthesis by promoting amino acid uptake into cells.

Pharmacokinetics

Insulin is administered by injection and is rapidly absorbed into the bloodstream. Its onset, peak, and duration of action depend on the formulation used (e.g., rapid-acting, short-acting). The half-life of insulin is typically around 5 to 10 minutes, but its effects can last several hours depending on the formulation. It is metabolized primarily in the liver and kidneys.

Contra-indications

• Hypersensitivity to insulin or any of its excipients
• Hypoglycemia

Adverse effects

• Hypoglycemia
• Injection site reactions
• Weight gain
• Allergic reactions
• Edema
• Lipodystrophy

Interactions

• Metreleptin may increase the risk of hypoglycemia when used with insulin
• Fibrates may increase the risk of hypoglycemia when used with insulin
• Macrolides may increase the risk of severe hypoglycemia when used with insulin
• Clarithromycin may increase the risk of severe hypoglycemia when used with insulin

Precautions

• Monitor blood glucose levels regularly, especially when changing insulin preparations
• Use caution in patients with renal impairment, as insulin clearance may be reduced
• Patients should be advised about the risks of hypoglycemia and how to manage it
• Should be used with caution in patients with cardiovascular disease

Pregnancy

Insulin is generally considered safe for use during pregnancy, but dosages may need to be adjusted.

Breast-feeding

Insulin is compatible with breastfeeding; insulin does not pass into breast milk in significant amounts.

Storage

Store unopened vials or pens in a refrigerator (2-8°C). Once opened, insulin can be stored at room temperature (below 25°C) for up to 28 days, depending on the formulation.

Formulations

• Insulin human 500 units/ml solution for injection
• Insulin human 100 units/ml solution for injection
• Insulin porcine 100 units/ml solution for injection

Indications

• Overdose of unfractionated heparin
• Management of digoxin toxicity

Dosage

Children: For children, the recommended dosage for reversing heparin overdose is 375–500 micrograms, administered at a rate not exceeding 5 mg/minute, with a maximum per dose of 50 mg.

Adults: For overdose of unfractionated heparin, the typical dose is 1 mg of protamine sulfate for every 100 units of heparin administered, administered intravenously at a rate not exceeding 5 mg/minute.

Mechanism of action

Protamine sulfate binds to heparin, neutralizing its anticoagulant effects by forming a stable protamine-heparin complex. This mechanism effectively reverses the actions of heparin in the body, restoring normal coagulation.

Pharmacodynamics

The pharmacodynamics of protamine sulfate are characterized by its rapid onset of action upon intravenous administration. The binding of protamine to heparin leads to an immediate reversal of heparin-induced anticoagulation, which can be crucial in emergency situations such as surgical bleeding or overdose.

Pharmacokinetics

Protamine sulfate is typically administered intravenously, allowing for quick distribution and action. The elimination half-life varies, but factors such as the extent of heparin overdose and the individual’s metabolic capacity can influence it. The drug is generally well-tolerated, but caution is advised in patients with hepatic impairment due to potential alterations in metabolism.

Contra-indications

• Life-threatening condition (e.g. raised intracranial pressure, status epilepticus) controlled by benzodiazepines

Adverse effects

• Hypotension
• Nausea
• Vomiting
• Palpitations
• Tremor
• Insomnia
• Dizziness
• Hyperventilation
• Abnormal hearing
• Arrhythmias
• Seizures (more common in patients with epilepsy)
• Withdrawal syndrome

Interactions

• Caution with other anticoagulants or antiplatelet agents due to increased bleeding risk

Precautions

• Avoid rapid injection following major surgery
• Caution in patients with hepatic impairment (risk of increased half-life)
• Caution in high-risk or anxious patients
• Benzodiazepine therapy for epilepsy due to risk of convulsions

Pregnancy

Not known to be harmful.

Breast-feeding

Avoid breast-feeding for 24 hours.

Storage

Store below 25°C. Protect from light.

Formulations

• Powder for solution for infusion
• Solution for injection

Indications

• Rectal and anal disorders
• Haemorrhoids
• Pruritus ani

Dosage

Children: Refer to the BNF for Children for appropriate dosing information.

Adults: For rectal use using aerosol spray: 1 spray up to 3 times a day for no longer than 7 days without medical advice. For ointment: apply several times daily, for short-term use only.

Mechanism of action

Phenol exerts its effects by acting as a potent proteolytic agent. At concentrations of 5% to 7%, it can dissolve tissue through proteolysis. When injected near a nerve, it produces chemical neurolysis, affecting nerve fibers nonselectively. Local anesthetic effects are typically observed within 5 to 10 minutes of application.

Pharmacodynamics

Phenol's pharmacodynamic properties include its ability to cause tissue dissolution and local anesthesia. The local anesthetic effects result from its action on the nerve fibers, leading to a temporary loss of sensation in the affected area. The proteolytic action can assist in the treatment of various skin and mucosal conditions by facilitating tissue breakdown.

Pharmacokinetics

Phenol is absorbed through mucosal surfaces when applied locally. Its metabolism involves biological oxidation and phase I functionalization, primarily through cytochrome P450 enzymes. The elimination of phenol occurs through metabolic pathways, and it can be detected in urine as a result of its metabolism.

Contra-indications

• Infection
• Known hypersensitivity to phenol or its components

Adverse effects

• Local irritation
• Burning sensation
• Paraesthesia
• Vision disorders
• Skin reactions
• Adrenal suppression

Interactions

• Caution with other local anesthetics due to potential additive effects

Precautions

• Use for short periods only-no longer than a few days
• Avoid excessive application, especially on sensitive areas
• Consult product literature for specific guidelines

Pregnancy

Data on the use of phenol during pregnancy is limited; caution is advised.

Breast-feeding

Limited information available; caution is recommended when used in breastfeeding mothers.

Storage

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

Formulations

• Ointment
• Suppository
• Aerosol spray

Indications

• Constipation
• Preparation for surgical or diagnostic procedures involving the rectum
• Decreasing intraocular pressure in certain ocular conditions

Dosage

Children: For children aged 2 to 6 years, 2 g to 5 g of glycerin may be used as a suppository. Children aged 6 to 12 years may use 5 g to 10 g as needed. For specific pediatric dosing, please refer to the BNF for Children.

Adults: For rectal use, 4 g to 10 g of glycerin may be administered as a suppository as needed.

Mechanism of action

When administered rectally, glycerin draws water from the tissues into the feces due to its hygroscopic action, which reflexively stimulates bowel evacuation. Additionally, glycerin creates an osmotic gradient that leads to a decrease in intraocular pressure by facilitating fluid movement from the aqueous and vitreous humors into the bloodstream.

Pharmacodynamics

Glycerin is classified as an osmotic laxative, which acts to retain water in the fecal matter, softening stools and making them easier to pass. Its local irritant effects also contribute to its laxative properties. Glycerin suppositories typically produce a bowel movement within 15 to 30 minutes of administration.

Pharmacokinetics

Glycerin is readily absorbed from the gastrointestinal tract when taken orally and is metabolized primarily in the liver. It is distributed widely throughout the body, with excretion occurring primarily via the kidneys. The onset of action for glycerin when used as a laxative is relatively quick, particularly when used rectally.

Contra-indications

• Severe dehydration
• Severe renal impairment
• Intestinal obstruction
• Appendicitis

Adverse effects

• Abdominal cramps
• Diarrhea
• Nausea
• Vomiting
• Electrolyte imbalance

Interactions

• May enhance the effects of other laxatives
• Caution with concurrent use of diuretics due to potential electrolyte imbalance

Precautions

• Use with caution in patients with renal impairment
• Monitor electrolytes in patients with prolonged use
• Not recommended for long-term use

Pregnancy

Glycerin is generally considered safe during pregnancy but should be used under medical advice.

Breast-feeding

Glycerin is excreted in breast milk in small amounts and is considered safe for use while breastfeeding.

Storage

Store at room temperature, away from moisture and heat.

Formulations

• Glycerin suppositories
• Glycerin oral solution

Dosage

Children: Dosage for human-derived biological products in pediatrics should be determined based on specific product guidelines and the clinical context.

Adults: Dosage for human-derived biological products varies widely. Refer to specific product information for appropriate dosing.

Mechanism of action

Human physiology is governed by complex biological systems involving various cellular and molecular pathways. The mechanisms of action for human-derived biological products vary widely depending on the specific context, including immune response, hormonal regulation, and metabolic processes.

Pharmacodynamics

Pharmacodynamics in humans involves the interaction of drugs with biological systems, resulting in therapeutic effects. This includes receptor binding, signal transduction, and physiological responses. The effects are influenced by genetic factors, existing health conditions, and concurrent medications.

Pharmacokinetics

Pharmacokinetics in humans involves the absorption, distribution, metabolism, and excretion (ADME) of substances. Factors such as age, sex, body weight, and organ function can significantly influence these processes. Drug absorption may occur via oral, intravenous, or other routes, while distribution depends on blood flow and tissue permeability. Metabolism typically occurs in the liver, and excretion primarily takes place through the kidneys.

Pregnancy

There is no specific information available; consult local guidelines.

Breast-feeding

There is no specific information available; consult local guidelines.

Storage

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

Indications

• Adjustment of pH in pharmaceutical formulations
• Facilitation of drug absorption
• Used in sterile preparations

Dosage

Children: Refer to specific product guidelines for dosing information, as hydrochloric acid is typically used in a controlled setting based on formulation requirements.

Adults: Refer to specific product guidelines for dosing information, as hydrochloric acid is typically used in a controlled setting based on formulation requirements.

Mechanism of action

Hydrochloric acid dissociates in aqueous solution to release hydrogen ions (H+), leading to a decrease in pH. This acidic environment promotes the activation of pepsinogen to pepsin, an enzyme essential for protein digestion. Additionally, the acidity aids in the absorption of certain minerals and drugs that require an acidic environment for optimal bioavailability.

Pharmacodynamics

The primary pharmacodynamic action of hydrochloric acid is the maintenance of gastric acidity, which is essential for normal digestive processes. The acidic environment helps in denaturing proteins, activating digestive enzymes, and providing a barrier against pathogenic microorganisms. Its effects can influence the absorption and efficacy of various medications, particularly those that are pH-dependent.

Pharmacokinetics

Hydrochloric acid does not undergo significant systemic absorption when used in its normal contexts, as it acts locally within the gastrointestinal tract. The amount of hydrochloric acid produced by the stomach varies with food intake and physiological needs. It is secreted by parietal cells in the gastric mucosa, and its secretion is regulated by neural, hormonal, and local factors. The half-life of hydrochloric acid is not applicable as it is continuously produced and neutralized within the gastrointestinal tract.

Contra-indications

• Hypersensitivity to hydrochloric acid or any of its components
• Severe renal impairment
• Active gastrointestinal bleeding

Adverse effects

• Abdominal pain
• Diarrhea
• Nausea
• Vomiting
• Esophageal irritation
• Gastric mucosal irritation
• Electrolyte imbalances

Interactions

• May interact with alkaline substances, potentially neutralizing hydrochloric acid
• Caution with antacids as they may affect the efficacy of hydrochloric acid

Precautions

• Use with caution in patients with a history of gastritis or gastric ulcers
• Monitor electrolytes in prolonged use
• Use cautiously in patients with respiratory conditions due to potential aspiration risks

Pregnancy

Hydrochloric acid is classified as a category C drug. Use during pregnancy only if clearly needed and the potential benefits justify the risks to the fetus.

Breast-feeding

There is limited data on the excretion of hydrochloric acid in human milk. Use with caution during breastfeeding.

Storage

Store in a cool, dry place away from direct sunlight and heat. Ensure the container is tightly closed.

Formulations

• Oral solutions
• Injectable forms
• Tablets

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.

Dosage

Children: Refer to specific medication guidelines for appropriate dosing in paediatric patients, as this can vary based on the active ingredient and therapeutic indication.

Adults: Refer to specific medication guidelines for appropriate dosing, as this can vary based on the active ingredient and therapeutic indication.

Mechanism of action

Liquified formulations may enhance the solubility and bioavailability of the active pharmaceutical ingredients (APIs), allowing for quicker absorption in the gastrointestinal tract. This mechanism is particularly beneficial for drugs with poor water solubility, improving their overall therapeutic effects.

Pharmacodynamics

The pharmacodynamic effects of liquified medications depend on the specific active ingredients within the formulation. Generally, liquified forms can lead to faster onset of action due to enhanced absorption rates. The therapeutic effects will vary based on the drug's mechanism of action, receptor interaction, and physiological pathways it influences.

Pharmacokinetics

The pharmacokinetics of liquified medications are influenced by the formulation's liquid state, which may lead to improved dissolution and absorption rates compared to solid forms. The distribution, metabolism, and excretion of the active ingredients will depend on their chemical properties and the body's physiological processes. Liquified medications may exhibit altered half-lives and bioavailability profiles compared to their solid counterparts.

Pregnancy

Safety during pregnancy has not been established. Use only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

Caution is advised when administering to breastfeeding mothers, as the effects on a nursing infant are unknown.

Storage

Store in a cool, dry place away from light. Ensure that the container is tightly closed.

Indications

• Disinfection of skin and mucous membranes
• Preservative in pharmaceutical formulations
• Antiseptic in medical and veterinary applications

Dosage

Children: Refer to BNF for Children for specific dosing recommendations tailored to paediatric patients.

Adults: Refer to BNF for specific dosing guidelines based on the formulation and condition being treated.

Mechanism of action

Metacresol exhibits antimicrobial activity by disrupting the cell membrane of bacteria, leading to cell lysis and death. Its effectiveness is attributed to its ability to denature proteins and dissolve lipid membranes, which is critical for maintaining the integrity of bacterial cells.

Pharmacodynamics

The pharmacodynamic effects of metacresol are primarily related to its antiseptic and disinfectant properties. It is effective against a wide range of pathogens, including bacteria, fungi, and some viruses. The concentration and exposure time are key factors that influence its efficacy, with higher concentrations generally leading to increased antimicrobial activity.

Pharmacokinetics

Metacresol is absorbed through the skin and mucous membranes, and its systemic absorption can vary based on the route of administration. It is metabolized primarily in the liver and excreted in the urine. The half-life and excretion rates can vary significantly based on individual factors such as age and liver function. Precautions should be taken to minimize exposure due to its potential toxicity.

Pregnancy

There is limited data on the use of metacresol in pregnancy. It is advisable to avoid use unless the potential benefits outweigh the risks.

Breast-feeding

Caution is advised when using metacresol during breastfeeding, as the effects on the nursing infant are not well studied.

Storage

Store in a tightly sealed container at room temperature, away from light and moisture.

Mechanism of action

Oxides do not have a single mechanism of action as they are a broad category of compounds. However, in general, metal oxides can exhibit catalytic properties, while non-metal oxides may participate in biochemical reactions by forming acids or bases upon dissolution in water.

Pharmacodynamics

The pharmacodynamics of oxides depend on the specific type of oxide and its interaction with biological systems. For instance, metal oxides may have antimicrobial properties, while certain non-metal oxides can influence metabolic pathways through their acid-base chemistry. The effects vary widely, necessitating specific studies for each oxide's role in therapeutic contexts.

Pharmacokinetics

The pharmacokinetics of oxides are also variable. Many metal oxides are poorly soluble and thus have limited absorption when ingested. Non-metal oxides, such as carbon dioxide, can be readily absorbed and utilized in metabolic processes. The distribution, metabolism, and excretion of oxides depend on their chemical form and the biological system in which they are involved.

Pregnancy

Not applicable as oxide is not a drug but a class of chemical compounds.

Breast-feeding

Not applicable as oxide is not a drug but a class of chemical compounds.

Storage

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

Indications

• Reversal of heparin anticoagulation during or after surgical procedures
• Management of heparin overdose

Dosage

Children: Refer to clinical guidelines for specific dosing based on the amount of heparin to be reversed in children.

Adults: Refer to clinical guidelines for specific dosing based on the amount of heparin to be reversed.

Mechanism of action

Protamine functions by forming stable complexes with heparin due to its positive charge, effectively neutralizing heparin's anticoagulant properties. This interaction occurs because heparin is negatively charged, leading to the formation of a protamine-heparin complex that is inactive.

Pharmacodynamics

The primary pharmacodynamic effect of protamine is the reversal of the anticoagulant effects of heparin. The onset of action is rapid, typically occurring within minutes of administration. The duration of action varies depending on the dose and the concentration of heparin present in the bloodstream.

Pharmacokinetics

Protamine is administered intravenously and has a rapid onset of action. It is metabolized in the liver and has a short half-life, typically ranging from 7 to 10 minutes. The elimination of protamine occurs through renal pathways, and its effects can be influenced by the presence of heparin in the bloodstream as well as by the dose of protamine administered.

Contra-indications

• Hypersensitivity to protamine
• Severe allergic reactions to fish
• Hypersensitivity to heparin

Adverse effects

• Hypotension
• Bradycardia
• Anaphylaxis
• Nausea
• Vomiting
• Flushing
• Rash
• Itching

Interactions

• Heparin
• Warfarin
• Anticoagulants
• Other blood thinners

Precautions

• Use with caution in patients with a history of allergies
• Monitor blood pressure and heart rate during administration
• Careful in patients with fish allergies
• Consider potential for heparin rebound effect

Pregnancy

Use only if clearly needed. Consult relevant guidelines and risk assessments.

Breast-feeding

Unknown whether excreted in human milk. Use caution and consider benefits vs risks.

Storage

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

Formulations

• Injection

Mechanism of action

INSULIN HAS DIRECT INHIBITORY EFFECT ON LIPASE CONCERNED WITH MOBILIZATION OF FATTY ACIDS, WHILE GROWTH HORMONE, GLUCOCORTICOIDS, THYROID HORMONES & CATECHOLAMINES ENHANCE LIPOLYSIS. IN ABSENCE OF INSULIN THERE IS ABNORMALLY HIGH RATE OF CONVERSION OF PROTEIN TO GLUCOSE. ... PROTEINS & AMINO ACIDS ARE CONVERTED TO GLUCOSE @ ABNORMALLY HIGH RATE IN INSULIN DEFICIENCY. THE LIVER IS SITE OF CONVERSION. PROTEIN & AMINO ACIDS ARE MOBILIZED FROM PERIPHERAL TISSUES. INSULIN ACTS TO.../STIMULATE/ GLYCOGEN SYNTHESIS. MECHANISM OF IMPORTANT ACTIONS OF INSULIN TO ENHANCE FACILITATED DIFFUSION OF GLUCOSE & ACTIVE TRANSPORT OF AMINO ACIDS ARE NOT KNOWN.

Mechanism of action

Phenol is a potent proteolytic agent. Concentrations in the 5% to 7% range dissolve tissue on contact via proteolysis. In high concentrations when injected next to a nerve, phenol produces a chemical neurolysis which is nonselective across nerve fiber size and most prominent on its outer aspect. Local anesthetic effects occur within 5-10 minutes. The effects of monoamine depletors and monoamine denervators on phenol induced tremor were studied in mice. The tremor induced by phenol was enhanced by pretreatment with reserpine or tetrabenazine, but not with syrosingopine. However, alpha-methyl-p-tyrosine, p-chlorophenylalanine or 6-hydroxydopamine did not affect the tremor. These results suggest that the depletion of central monoamines as a whole contribute to the enhancement of the tremor induced by phenol.

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.