Microkleen

Indications

• Skin disinfection
• Preparation of skin before injections
• Cleansing minor wounds

Dosage

Children: Apply to the skin as required; consult product literature for specific guidance.

Adults: Apply to the skin as required for disinfection.

Mechanism of action

Alcohol exerts its antiseptic effect by denaturing proteins, disrupting cell membranes, and dehydrating microbial cells, leading to cell lysis and death.

Pharmacodynamics

Alcohol has broad-spectrum antimicrobial activity, effective against bacteria, fungi, and viruses. Its efficacy is influenced by concentration, with higher concentrations generally being more effective.

Pharmacokinetics

Alcohol is rapidly absorbed through the skin and mucous membranes. It is metabolized primarily in the liver, with a half-life that varies based on the individual's metabolic rate and the amount consumed.

Contra-indications

• Concomitant use with lithium
• Regular use in neonates
• Patients with severe burns when diathermy has been preceded by application of alcoholic skin disinfectants

Adverse effects

• Eye erythema
• Punctate keratitis
• Cytotoxicity
• Eye discolouration

Interactions

• Increases risk of visual disturbances with antiepileptics
• Increases concentration with methylphenidate
• Increases risk of facial flushing and skin irritation with topical pimecrolimus
• Increases concentration with retinoids
• Increases concentration with acitretin
• Increases risk of facial flushing and skin irritation with topical tacrolimus
• Decreases antidiuretic effect with vasopressin

Precautions

• Avoid regular application to inflamed or broken skin or mucosa
• Avoid broken skin
• Flammable

Pregnancy

Sufficient iodine may be absorbed to affect the fetal thyroid in the second and third trimester.

Breast-feeding

Avoid regular or excessive use.

Storage

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

Formulations

• Betadine 2.5% dry powder spray
• Industrial methylated spirit
• Povidone-Iodine 25 mg per 1 gram

Indications

• Seborrhoeic dermatitis
• Dandruff
• Scalp psoriasis
• Bacterial infections affecting the scalp

Dosage

Children: For children, apply 3 times a week for 1 week, then apply twice weekly as needed. Refer to BNF for Children for further details.

Adults: Apply to the affected area as directed, typically 1-3 times weekly depending on the condition being treated. Refer to specific product guidelines for detailed dosing.

Mechanism of action

Benzalkonium chloride exerts its antimicrobial effect by disrupting the cell membrane of microorganisms, leading to leakage of cellular contents and ultimately cell death. This is facilitated by its cationic nature, which allows it to bind to negatively charged bacterial surfaces.

Pharmacodynamics

Benzalkonium chloride demonstrates rapid bactericidal activity, with effectiveness observed against gram-positive and gram-negative bacteria, fungi, and some viruses. Its antiseptic properties may be enhanced in the presence of moisture and are typically influenced by the concentration of the solution used.

Pharmacokinetics

Benzalkonium chloride is poorly absorbed through the skin. After topical application, it remains primarily at the site of application, where it exerts localized effects. Systemic absorption is minimal, and it is primarily eliminated through the skin and urine. However, specific pharmacokinetic data may vary based on formulation and application site.

Pregnancy

Benzalkonium chloride should be used with caution during pregnancy. Refer to specific guidelines or consult a healthcare professional.

Breast-feeding

Benzalkonium chloride should be used with caution while breastfeeding. Refer to specific guidelines or consult a healthcare professional.

Storage

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

Formulations

• Shampoo
• Soap or detergent
• Topical solution

Indications

• Disinfection of surfaces
• Antiseptic for skin
• Preservative in pharmaceuticals
• Treatment of minor cuts and abrasions

Dosage

Children: Refer to the BNF for Children for specific dosing recommendations in pediatric populations.

Adults: Refer to the BNF for specific formulations and concentrations as doses may vary based on the application and preparation.

Mechanism of action

The bactericidal action of benzalkonium chloride is believed to result from the disruption of intermolecular interactions, which leads to the dissociation of cellular membrane lipid bilayers in bacteria. This disruption compromises cellular permeability, causing leakage of vital cellular contents. Moreover, the agent can deactivate important molecular complexes such as enzymes that regulate various respiratory and metabolic activities within the cells. Cationic surfactants like benzalkonium chloride can thus effectively disrupt critical intermolecular interactions and tertiary structures in biochemical systems, impairing bacterial function.

Pharmacodynamics

Benzalkonium chloride is classified as a biocidal agent with a relatively long duration of action. It exhibits a spectrum of activity against various microorganisms, including bacteria, certain viruses, fungi, and protozoa; however, it is ineffective against bacterial spores. The agent tends to demonstrate greater efficacy against gram-positive bacteria compared to gram-negative ones. The mode of action can be bacteriostatic (preventing growth) or bactericidal (killing bacteria), depending on its concentration. The activity of benzalkonium chloride is generally stable across different pH levels but is enhanced at elevated temperatures and with extended exposure.

Pharmacokinetics

The pharmacokinetic properties of benzalkonium chloride, including absorption, distribution, metabolism, and excretion, are not fully characterized. Its topical application limits systemic exposure, and it primarily exerts localized effects at the site of application. The duration of action and efficacy may be influenced by the formulation and concentration used.

Pregnancy

Benzalkonium chloride is generally considered safe for use during pregnancy when applied topically, but systemic absorption should be minimized. Always consult a healthcare provider for use during pregnancy.

Breast-feeding

Benzalkonium chloride is considered safe for topical application during breastfeeding, but care should be taken to avoid exposure to the infant. Consultation with a healthcare provider is recommended.

Storage

Store at room temperature, away from moisture and heat. Keep in a tightly closed container, protected from light.

Formulations

• Topical solution
• Disinfectant wipes
• Liquid antiseptics

Indications

• Type 2 diabetes mellitus
• Polycystic ovary syndrome (off-label use)

Dosage

Children: For children aged 10 years and older, the starting dose is typically 500 mg orally once or twice daily, with gradual increases as needed and tolerated.

Adults: The usual initial dose of metformin is 500 mg orally twice daily or 850 mg once daily, which may be increased gradually based on glycemic control and tolerance.

Mechanism of action

Biguanides, particularly metformin, primarily work by decreasing hepatic glucose production and increasing insulin sensitivity in peripheral tissues. This leads to enhanced uptake and utilization of glucose by the tissues, thereby reducing blood glucose levels. The exact mechanism involves activation of AMP-activated protein kinase (AMPK), which plays a crucial role in energy homeostasis.

Pharmacodynamics

Biguanides lower blood glucose levels without increasing insulin secretion, which helps mitigate the risk of hypoglycemia. They also have beneficial effects on lipid profiles and may reduce the risk of macrovascular complications associated with diabetes. Metformin has been shown to have cardioprotective effects and may aid in weight management in patients with type 2 diabetes.

Pharmacokinetics

Biguanides are absorbed in the gastrointestinal tract, with peak plasma concentrations typically occurring 2 to 3 hours after administration. They are primarily excreted unchanged by the kidneys, and their half-life is approximately 6.2 hours. Renal function significantly affects the pharmacokinetics of biguanides, necessitating dosage adjustments in patients with renal impairment.

Contra-indications

• Severe renal impairment
• Acute or chronic metabolic acidosis
• Diabetic ketoacidosis
• Hypersensitivity to biguanides

Adverse effects

• Gastrointestinal disturbances (nausea, vomiting, diarrhea)
• Lactic acidosis
• Vitamin B12 deficiency
• Hypoglycemia (when used in combination with other antidiabetic medications)

Interactions

• Cationic drugs (e.g., certain antihypertensives) may affect renal clearance
• Alcohol can increase the risk of lactic acidosis
• Diuretics may alter blood glucose levels

Precautions

• Monitor renal function regularly
• Use caution in patients with liver dysfunction
• Discontinue before surgical procedures or radiological studies involving iodinated contrast

Pregnancy

Biguanides should only be used in pregnancy if the potential benefit justifies the potential risk to the fetus. Metformin is the preferred agent in gestational diabetes.

Breast-feeding

Metformin is excreted in breast milk in small amounts. It is generally considered safe during breastfeeding.

Storage

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

Formulations

• Tablets
• Extended-release tablets
• Oral solution

Indications

• Antiseptic for skin disinfection
• Solvent in pharmaceutical formulations
• Cleaning agent in laboratories and healthcare settings

Dosage

Children: For pediatric use, consult specific guidelines in the BNF for Children, as dosing may vary based on age, weight, and clinical circumstances.

Adults: For skin antisepsis, apply isopropyl alcohol topically in a concentration of 70% to the affected area. Dosage may vary based on clinical indication and setting.

Mechanism of action

Isopropyl alcohol works primarily as an antiseptic by denaturing proteins and disrupting cell membranes of bacteria, viruses, and fungi, leading to cell lysis and death. Its efficacy is enhanced by the presence of water, which facilitates the penetration of the alcohol into microbial cells.

Pharmacodynamics

Isopropyl alcohol exhibits a rapid onset of action against a variety of pathogens, including gram-positive and gram-negative bacteria, fungi, and some viruses. Its antimicrobial activity is concentration-dependent, with higher concentrations generally providing a broader spectrum of activity. It is commonly used in concentrations ranging from 60% to 90%, with 70% being optimal for disinfection due to its ability to penetrate the cell wall effectively.

Pharmacokinetics

Isopropyl alcohol is readily absorbed through the skin and mucous membranes. After absorption, it is metabolized primarily in the liver to acetone, which is then further metabolized and excreted, mostly via urine. The elimination half-life of isopropyl alcohol varies but is typically around 2 to 3 hours. Its effects can be influenced by factors such as dosage, route of exposure, and individual metabolic differences.

Pregnancy

Isopropyl alcohol should be used with caution during pregnancy. It is a category C drug, indicating that risk cannot be ruled out.

Breast-feeding

Caution is advised when using isopropyl alcohol during breastfeeding, as it is not known if it is excreted in human milk.

Storage

Isopropyl alcohol should be stored at room temperature, away from heat and flame. Keep the container tightly closed and in a well-ventilated area.

Formulations

• Isopropyl alcohol 70% solution
• Isopropyl alcohol 99% solution

Indications

• Used as a solvent in various pharmaceutical formulations
• Applied in the manufacture of chemicals
• Utilized in personal care products

Dosage

Children: Refer to the BNF for Children for appropriate dosing guidelines for paediatric patients, as specific doses will depend on age, weight, and clinical condition.

Adults: Refer to the BNF for specific dosing recommendations based on the condition being treated. Doses may vary depending on the formulation and intended use.

Mechanism of action

Npropanol acts as a central nervous system depressant, primarily through its effects on GABA-A receptors, enhancing the inhibitory neurotransmitter GABA's effects, leading to sedative and anxiolytic properties. It may also influence other neurotransmitter systems, contributing to its pharmacological effects.

Pharmacodynamics

Npropanol exhibits sedative and anxiolytic effects, with a dose-dependent relationship. Its action can lead to decreased anxiety, sedation, and muscle relaxation. The pharmacodynamic profile is influenced by its ability to modulate neurotransmitter activity, particularly GABA, and it may also affect the release of dopamine and serotonin.

Pharmacokinetics

Npropanol is rapidly absorbed following oral administration. It is metabolized in the liver primarily through oxidation to propanal and further to propionic acid. The elimination half-life varies, typically ranging from 2 to 5 hours. Excretion occurs mainly via the kidneys, with metabolites eliminated in urine. The drug has a volume of distribution suggesting good tissue distribution.

Pregnancy

There is limited information on the safety of isopropanol in pregnancy. Use with caution and only if the benefits outweigh the risks.

Breast-feeding

Isopropanol is excreted in breast milk. Caution is advised when administering to breastfeeding mothers.

Storage

Store at room temperature, away from heat and direct sunlight. Keep out of reach of children.

Formulations

• Isopropyl alcohol solution

Indications

• Wound care
• Skin antisepsis
• Contact lens solution
• Surface disinfection
• Preoperative skin preparation

Dosage

Children: Refer to specific product guidelines for dosage recommendations, as they can vary based on formulation and intended use.

Adults: Refer to specific product guidelines for dosage recommendations, as they can vary based on formulation and intended use.

Mechanism of action

Polyhexamethylene biguanide exerts its antimicrobial effects primarily through disruption of microbial cell membranes. It binds to negatively charged components of the microbial cell surface, leading to membrane destabilization, leakage of cellular contents, and ultimately cell death. This mechanism allows PHMB to maintain effectiveness against a broad spectrum of pathogens.

Pharmacodynamics

The pharmacodynamic profile of polyhexamethylene biguanide indicates a rapid bactericidal effect, with activity increasing with concentration and time of exposure. It has a low toxicity to mammalian cells, allowing for safe application on human tissues. The effectiveness of PHMB can vary depending on the type of microorganism and environmental conditions such as pH and organic load.

Pharmacokinetics

Polyhexamethylene biguanide is poorly absorbed systemically when applied topically, which limits its systemic effects and adverse reactions. The compound is primarily excreted unchanged in urine when absorbed, although systemic absorption is minimal. Its local effects are sustained due to its high affinity for proteins and tissues, providing prolonged antimicrobial activity at the application site.

Adverse effects

• Skin irritation
• Allergic reactions
• Respiratory distress
• Gastrointestinal disturbances

Precautions

• Use with caution in individuals with known hypersensitivity to polyhexamethylene
• Avoid contact with eyes and mucous membranes
• Use in well-ventilated areas to prevent inhalation

Pregnancy

Safety during pregnancy has not been established. Use only if clearly needed and after discussing potential risks with a healthcare provider.

Breast-feeding

It is not known whether polyhexamethylene is excreted in breast milk. Use with caution and consult a healthcare professional.

Storage

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

Formulations

• Topical solutions
• Gels
• Disinfectant wipes

Mechanism of action

Ethanol affects the brain’s neurons in several ways. It alters their membranes as well as their ion channels, enzymes, and receptors. Alcohol also binds directly to the receptors for acetylcholine, serotonin, GABA, and the NMDA receptors for glutamate. The sedative effects of ethanol are mediated through binding to GABA receptors and glycine receptors (alpha 1 and alpha 2 subunits). It also inhibits NMDA receptor functioning. In its role as an anti-infective, ethanol acts as an osmolyte or dehydrating agent that disrupts the osmotic balance across cell membranes. ... Ethanol is known to affect a large number of membrane proteins that participate in signaling pathways such as neurotransmitter receptors, enzymes, and ion channels, and there is extensive evidence that ethanol interacts with a variety of neurotransmitters. The major actions of ethanol involve enhancing the inhibitory effects of gamma-aminobutyric acid (GABA) at GABAa receptors and blockade of the N-methyl-D-aspartate (NMDA) subtype of glutamate, an excitatory amine acid (EAA) receptor. Animal studies indicate that the acute effects of ethanol result from competitive inhibition of glycine binding to NMDA receptor and disruption of glutamatergic neurotransmission by inhibiting the response of the NMDA receptor. Persistent glycine antagonism and attenuation of glutamatergic neurotransmission by chronic ethanol exposure results in tolerance to ethanol by enhancing EAA neurotransmission and NMDA receptor upregulation. The latter appears to involve selective increases in NMDA R2B subunit concentrations and other molecular changes in specific brain loci. The abrupt withdrawal of ethanol thus produces a hyperexcitable state that leads to the ethanol withdrawal syndrome and excitotoxic neuronal death. GABA-mediated inhibition, which normally acts to limit excitation, is eliminated during ethanol withdrawal syndrome and further intensifies this excitation. In addition, NMDA receptors function to inhibit the release of dopamine in the nucleus accumbens and mesolimbic structures, which modulate the reinforcing action of addictive xenobiotics such as ethanol. By inhibiting NMDA receptor activity, ethanol could increase dopamine release from the nucleus accumbens and ventral tegmental area and could thus create dependence. Chronic ethanol administration also results in tolerance, dependence, and an ethanol withdrawal syndrome, mediated, in part, by desensitization and or downregulation of GABAa receptors. The development of alcoholic ketoacidosis (AKA) requires that a combination of physical and physiologic events occur. The normal response to starvation and depletion of hepatic glycogen stores is for amino acids to be converted to pyruvate. Pyruvate can serve as a substrate for gluconeogenesis, be converted to acetyl-CoA, which can enter the Krebs cycle or can be utilized in various biosynthetic pathways (eg, fatty acid, ketone bodies, cholesterol, and acetylcholine) ... Ethanol metabolism generates NADH, resulting in an excess of reducing potential. This high redox state favors the conversion of pyruvate to lactate, diverting pyruvate from being a substrate for gluconeogenesis. To compensate for the lack of normal metabolic substrates, the body mobilizes fat from adipose tissue and increased fatty acid metabolism as an alternative source of energy. This response is mediated by a decrease in insulin and an increased secretion of glucagon, catecholamines, growth hormone, and cortisol. Fatty acid metabolism results in the formation of acetyl-CoA and it combines with the excess acetate that is generated from ethanol metabolism to form acetoacetate. Most of the acetoacetate is reduced to beta-hydroxybutyrate due to the excess reducing potential or high redox state of the cell. Volume depletion interferes with the renal elimination of acetoacetate and beta-hydroxybutyrate, and contributes to the acidosis. An elevated lactate concentration may result from shunting from pyruvate or

Pharmacodynamics

Alcohol produces injury to cells by dehydration and precipitation of the cytoplasm or protoplasm. This accounts for its bacteriocidal and antifungal action. When alcohol is injected in close proximity to nerve tissues, it produces neuritis and nerve degeneration (neurolysis). Ninety to 98% of ethanol that enters the body is completely oxidized. Ethanol is also used as a cosolvent to dissolve many insoluble drugs and to serve as a mild sedative in some medicinal formulations. Ethanol also binds to GABA, glycine, NMDA receptors and modulates their effects. Ethanol is also metabolised by the hepatic enzyme alcohol dehydrogenase.

Mechanism of action

Although not entirely elucidated, the bactericidal action of benzalkonium chloride is believed to be due to the disruption of intermolecular interactions. Such disruption can cause the dissociation of cellular membrane lipid bilayers of bacteria, resulting in compromised cellular permeability control and the leakage of important cellular contents. Additionally, other important molecular complexes like enzymes which control the maintenance of a great range of respiratory and metabolic cellular activities, are also susceptible to such deactivation. Consequently, a variety of critical intermolecular interactions and tertiary structures in very highly specific biochemical systems that allow bacterial agents to function normally can be readily disrupted or deactivated by cationic surfactants like benzalkonium chloride..

Pharmacodynamics

Benzalkonium chloride solutions are generally categorized as biocidal agents with relative long durations of action. Their spectrum of activity has been demonstrated against bacteria, to some viruses, fungi, and protozoa, although bacterial spores are treated as being resistant to the agent. Additionally, the agent generally shows more activity against gram-positive than gram-negative bacteria. Finally, solutions of benzalkonium chloride are bacteriostatic or bactericidal based on their concentration. Bacteriostatic agents act to prevent further growth of bacterial organisms that are present while bactericidal agents function to kill bacteria that are present. In general, the activity of the agent is not largely affected by pH, but such activity does increase substantially at higher temperatures and prolonged exposure times.