Tecentriq

Indications

• Non-small cell lung cancer (specialist use only)
• Urothelial carcinoma (specialist use only)
• Small cell lung cancer (specialist use only)
• Breast cancer (specialist use only)
• Hepatocellular carcinoma (specialist use only)

Dosage

Adults: Consult product literature for specific dosing information.

Mechanism of action

Atezolizumab binds to PD-L1, blocking its interaction with PD-1 and CD80, which leads to the reactivation of T-cell responses against tumor cells. This mechanism enhances the immune response to malignancies.

Pharmacodynamics

As an immune checkpoint inhibitor, atezolizumab enhances T-cell mediated immune responses, which can lead to tumor regression. The blockade of PD-L1 allows for increased T-cell proliferation and activation, resulting in a more robust immune surveillance against cancerous cells.

Pharmacokinetics

Atezolizumab is administered via intravenous infusion. It has a half-life of approximately 27 days, allowing for infrequent dosing. The pharmacokinetics can be influenced by patient factors such as body weight and the presence of anti-drug antibodies, which may affect the drug's efficacy and safety profile.

Adverse effects

• Severe cutaneous adverse reactions (SCARs)
• Appetite decreased
• Asthenia
• Constipation
• Diarrhoea
• Dizziness
• Dry eye
• Electrolyte imbalance
• Hypoalbuminaemia
• Increased risk of infection
• Infusion-related reactions
• Mucositis
• Myalgia
• Nail disorders

Precautions

• Infusion-related reactions can occur; administer only when appropriately trained staff and resuscitation facilities are available.
• Pre-medication with an antipyretic, antihistamine, and corticosteroid is recommended.
• Patients should limit sun exposure during treatment and for 2 months after last treatment.
• Patients should be advised to discontinue contact lens use until worsening eye symptoms are evaluated.
• Patients and carers should be counselled on the effects on driving and performance of skilled tasks due to increased risk of dizziness and visual impairment.

Pregnancy

Avoid during pregnancy; no information available on safety.

Breast-feeding

Avoid during treatment and for 3 months after last treatment; no information available.

Storage

Store in a refrigerator (2-8°C) and protect from light; consult product literature for storage conditions after preparation of the infusion.

Formulations

• Atezolizumab 1200 mg per 20 ml solution for infusion vials
• Atezolizumab 840 mg per 14 ml solution for infusion vials

Indications

• Infections (topical treatment)
• Wound care (as an antiseptic)
• Ear infections (as an ear drop solution)
• Acid-base balance in metabolic acidosis

Dosage

Children: Refer to established guidelines as dosage may vary based on the formulation and indication.

Adults: Refer to established guidelines as dosage may vary based on the formulation and indication.

Mechanism of action

Acetic acid exerts its effects primarily through its ability to lower pH levels, creating an acidic environment which is inhospitable to many pathogens. It can disrupt the integrity of microbial cell membranes, leading to cell lysis and death. Additionally, acetic acid can promote the healing of wounds and enhance the absorption of certain medications when used as a solvent.

Pharmacodynamics

The pharmacodynamics of acetic acid involve its interaction with biological systems, leading to changes in cellular functions. Its acidic nature helps in the denaturation of proteins and disruption of microbial metabolism. This contributes to its antibacterial and antifungal activities, making it effective against a range of pathogens.

Pharmacokinetics

Acetic acid is rapidly absorbed in the gastrointestinal tract when ingested. It is metabolized primarily in the liver, converting to acetyl CoA and subsequently entering various metabolic pathways including the citric acid cycle. The elimination half-life varies but is generally short, with excretion occurring mainly via urine. When applied topically, absorption is minimal, and local effects are predominant.

Pregnancy

The safety of acetic acid during pregnancy has not been established. Use only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

There is no specific information available regarding the use of acetic acid during breastfeeding. Caution is advised.

Storage

Store in a cool, dry place away from direct sunlight. Keep tightly closed in a well-ventilated area.

Indications

• Topical treatment of localized infections
• Antiseptic for skin and mucous membrane applications
• Astringent in certain dermatological conditions

Dosage

Children: Refer to professional resources for specific dosing information, as it can vary based on formulation and condition treated.

Adults: Refer to professional resources for specific dosing information, as it can vary based on formulation and condition treated.

Mechanism of action

Glacial acetic acid exerts its effects primarily through its acidic properties, leading to protein denaturation and cell lysis in microbial cells. This action disrupts cellular integrity, promoting the death of bacteria and fungi. Additionally, it can alter the pH of tissues, which may contribute to its antiseptic effects.

Pharmacodynamics

The pharmacodynamic effects of glacial acetic acid are largely attributed to its ability to lower the pH in the local environment, which can inhibit the growth of certain pathogens. Its astringent properties help to reduce secretions and promote tissue contraction, which can be beneficial in managing conditions that involve inflammation or excessive exudation.

Pharmacokinetics

Glacial acetic acid is absorbed through the skin and mucous membranes when applied topically. Once absorbed, it can be metabolized by the liver, with elimination primarily occurring through urine. The exact pharmacokinetic parameters can vary based on the route of administration and the formulation used, but detailed data on half-life and volume of distribution are not well-characterized in standard references.

Pregnancy

Glacial acetic acid should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. It is classified as a category C drug.

Breast-feeding

It is not known whether glacial acetic acid is excreted in human milk. Caution should be exercised when administering to nursing mothers.

Storage

Store in a tightly closed container, in a cool, dry place away from incompatible substances.

Indications

• Rheumatoid arthritis
• Allergic diseases
• Peptic ulcers
• Anemia

Dosage

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

Adults: Refer to BNF for specific dosing information based on condition and individual patient factors.

Mechanism of action

The specific actions of supplemental L-histidine are not completely understood, but it is known that L-histidine serves as a precursor for histamine through the process of decarboxylation. Histamine is associated with immunomodulatory and antioxidant effects, which may help in conditions such as rheumatoid arthritis by activating suppressor T cells and reducing reactive oxygen species production in immune cells. Additionally, L-histidine can chelate metals that participate in oxidative reactions, potentially protecting tissues from oxidative damage.

Pharmacodynamics

Histidine is essential for the synthesis of proteins and is found in high concentrations in hemoglobin. Its metabolites, including histamine, play significant roles in immune response regulation and oxidative stress management. A deficiency in histidine can lead to various health issues, including impaired hearing and reduced immune function.

Pharmacokinetics

Histidine is readily absorbed in the intestines and distributed throughout the body. It undergoes metabolic conversion primarily in the liver, where it is transformed into histamine and other metabolites. The elimination of histidine occurs through various metabolic pathways, and it is excreted in urine primarily as metabolites.

Pregnancy

Histidine is generally regarded as safe during pregnancy when consumed in food. However, the safety of high-dose supplementation has not been established.

Breast-feeding

Histidine is considered safe during breastfeeding in dietary amounts. The effects of high-dose supplementation are not well studied.

Storage

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

Formulations

• L-histidine capsules
• L-histidine powder

Indications

• Emulsifying agent in drug formulations
• Stabilizer for parenteral preparations
• Solubilizer for hydrophobic drug compounds
• Ingredient in topical formulations

Dosage

Children: Refer to specific product guidelines, as dosing varies based on formulation and intended use.

Adults: Refer to specific product guidelines, as dosing varies based on formulation and intended use.

Mechanism of action

Polysorbate functions primarily as an emulsifying agent. It reduces the surface tension between immiscible liquids, allowing them to mix more easily. This property is particularly useful in stabilizing emulsions and suspensions, facilitating the delivery of active pharmaceutical ingredients in various formulations.

Pharmacodynamics

Polysorbate does not exert pharmacological effects in the traditional sense, as it does not bind to specific receptors to elicit a physiological response. Instead, it plays a crucial role in modifying the physical properties of drug formulations, thereby enhancing drug delivery and absorption. Its ability to solubilize drugs enhances their bioavailability, particularly for poorly soluble compounds.

Pharmacokinetics

Polysorbate is generally considered to be non-toxic and is not absorbed to a significant extent when administered orally. It is metabolized by the liver and excreted primarily through the gastrointestinal tract. The pharmacokinetic profile may vary depending on the route of administration and the specific formulation in which it is used.

Adverse effects

• Allergic reactions
• Skin irritation
• Gastrointestinal disturbances

Precautions

• Use cautiously in patients with known allergies to polysorbates or related compounds
• Monitor for allergic reactions in susceptible individuals

Pregnancy

Polysorbate is generally considered safe for use during pregnancy, but consult with a healthcare provider for specific cases.

Breast-feeding

Polysorbate is considered safe during breastfeeding, but consult with a healthcare provider for individual advice.

Storage

Store at room temperature, away from direct sunlight and moisture.

Formulations

• Polysorbate 20
• Polysorbate 80

Indications

• Sweetening agent in food and beverages
• Ingredient in pharmaceutical formulations
• Source of quick energy

Dosage

Children: Refer to specific formulations and clinical guidelines for dosing, as sucrose does not have a standardized dosage. Typically used as needed for sweetening.

Adults: Refer to specific formulations and clinical guidelines for dosing, as sucrose does not have a standardized dosage. Typically used as needed for sweetening.

Mechanism of action

Sucrose is metabolized in the body to glucose and fructose, which are then used as energy sources. It does not have a specific pharmacological mechanism of action but contributes to energy metabolism via the glycolytic and citric acid pathways.

Pharmacodynamics

Upon ingestion, sucrose is hydrolyzed by the enzyme sucrase into its constituent monosaccharides, glucose and fructose. These monosaccharides are absorbed in the small intestine and enter the bloodstream, leading to a rise in blood glucose levels. This process provides a quick source of energy for cellular functions.

Pharmacokinetics

Sucrose is rapidly absorbed in the gastrointestinal tract after hydrolysis. Its absorption depends on the presence of sucrase in the intestine. Once in the bloodstream, glucose can be utilized by cells or stored as glycogen in the liver and muscles. The elimination half-life of sucrose itself is not well-defined as it is quickly broken down and utilized.

Pregnancy

Sucrose is generally regarded as safe during pregnancy when consumed in moderation as part of a balanced diet.

Breast-feeding

Sucrose is considered safe during breastfeeding when consumed in normal dietary amounts.

Storage

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

Formulations

• Oral solution
• Granules
• Tablets

Mechanism of action

Since the actions of supplemental L-histidine are unclear, any postulated mechanism is entirely speculative. However, some facts are known about L-histidine and some of its metabolites, such as histamine and trans-urocanic acid, which suggest that supplemental L-histidine may one day be shown to have immunomodulatory and/or antioxidant activities. Low free histidine has been found in the serum of some rheumatoid arthritis patients. Serum concentrations of other amino acids have been found to be normal in these patients. L-histidine is an excellent chelating agent for such metals as copper, iron and zinc. Copper and iron participate in a reaction (Fenton reaction) that generates potent reactive oxygen species that could be destructive to tissues, including joints. L-histidine is the obligate precursor of histamine, which is produced via the decarboxylation of the amino acid. In experimental animals, tissue histamine levels increase as the amount of dietary L-histidine increases. It is likely that this would be the case in humans as well. Histamine is known to possess immunomodulatory and antioxidant activity. Suppressor T cells have H2 receptors, and histamine activates them. Promotion of suppressor T cell activity could be beneficial in rheumatoid arthritis. Further, histamine has been shown to down-regulate the production of reactive oxygen species in phagocytic cells, such as monocytes, by binding to the H2 receptors on these cells. Decreased reactive oxygen species production by phagocytes could play antioxidant, anti-inflammatory and immunomodulatory roles in such diseases as rheumatoid arthritis. This latter mechanism is the rationale for the use of histamine itself in several clinical trials studying histamine for the treatment of certain types of cancer and viral diseases. In these trials, down-regulation by histamine of reactive oxygen species formation appears to inhibit the suppression of natural killer (NK) cells and cytotoxic T lymphocytes, allowing these cells to be more effective in attacking cancer cells and virally infected cells.

Pharmacodynamics

Is found abundantly in hemoglobin; has been used in the treatment of rheumatoid arthritis, allergic diseases, ulcers and anemia. A deficiency can cause poor hearing.