Intamab 500

Indications

• Non-Hodgkin's lymphoma (specialist use only)
• Chronic lymphocytic leukaemia (specialist use only)
• Rheumatoid arthritis (specialist use only)
• Granulomatosis with polyangiitis and microscopic polyangiitis (specialist use only)

Dosage

Children: Refer to BNF for Children for specific paediatric dosing information related to indicated conditions

Adults: By intravenous infusion: 1 g, then 1 g after 2 weeks. Consult product literature for information on retreatment.

Mechanism of action

Rituximab binds specifically to the CD20 antigen on B cells, leading to their destruction through various mechanisms including complement-dependent cytotoxicity, antibody-dependent cellular cytotoxicity, and induction of apoptosis. This results in a reduction of B cell populations, which is beneficial in conditions where B cells are pathologically active, such as in certain malignancies and autoimmune diseases.

Pharmacodynamics

The pharmacodynamics of rituximab involve the modulation of B cell activity and reduction in B cell counts. The drug's action leads to decreased levels of immunoglobulins and altered immune responses, which can be advantageous in treating autoimmune conditions. However, this immunosuppressive effect also increases the risk of infections, particularly during treatment and for some time after cessation, due to the depletion of B lymphocytes.

Pharmacokinetics

Rituximab exhibits a monoclonal antibody pharmacokinetic profile, characterized by a long half-life, which allows for less frequent dosing schedules. The drug is primarily eliminated through the reticuloendothelial system. After intravenous administration, peak serum concentrations are reached approximately 3 to 6 hours post-infusion. The clearance of rituximab can be influenced by factors such as the presence of anti-drug antibodies, body weight, and the presence of disease.

Contra-indications

• Severe infection
• Progressive multifocal leucoencephalopathy
• Severe heart failure
• Uncontrolled heart disease
• Active hepatitis B infection

Adverse effects

• Angioedema
• Anxiety
• Decreased appetite
• Arrhythmias
• Bone marrow disorders
• Bursitis
• Cancer pain
• Cardiac disorders
• Chest pain
• Chills
• Dizziness
• Fatigue
• Fever
• Headaches
• Hypertension
• Hypotension
• Insomnia
• Nausea
• Oedema
• Skin reactions
• Throat irritation
• Tinnitus
• Tumour lysis syndrome
• Vision changes

Interactions

• Filgotinib (increases risk of immunosuppression)

Precautions

• Monitor for cognitive, neurological, or psychiatric signs
• Effective contraception required during and for 12 months post-treatment
• Pre-medication recommended to minimise adverse reactions
• Patients with positive hepatitis B serology should be monitored closely

Pregnancy

Avoid unless potential benefit to mother outweighs risk of B-lymphocyte depletion in fetus.

Breast-feeding

Avoid breastfeeding during and for 12 months after treatment.

Storage

Store in a refrigerator at 2 to 8 degrees Celsius. Protect from light.

Formulations

• Solution for infusion 100 mg/10 ml
• Concentrate for solution for infusion 500 mg/50 ml

Dosage

Children: Specific dosing information is not applicable without a defined drug.

Adults: Specific dosing information is not applicable without a defined drug.

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.

Indications

• Acute pain management
• Nausea and vomiting control
• Antibiotic therapy
• Vaccinations
• Insulin administration for diabetes
• Chemotherapy for cancer treatment
• Emergency medications for cardiac arrest or anaphylaxis

Dosage

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

Adults: Refer to specific drug guidelines in the BNF for appropriate dosing.

Mechanism of action

The mechanism of action for injectable drugs varies widely depending on the specific drug. Generally, injectable medications can act through various pathways such as receptor agonism or antagonism, enzyme inhibition, or modulation of cellular processes. For instance, antibiotics may inhibit bacterial cell wall synthesis, while analgesics may act on pain receptors in the nervous system.

Pharmacodynamics

Pharmacodynamics refers to the effects of injectable drugs on the body and their mechanisms of action at the target sites. This includes the relationship between drug concentration and effect, the duration of action, therapeutic indices, and potential side effects. Injectable drugs may exhibit dose-dependent effects, with higher doses typically leading to more pronounced therapeutic or adverse effects.

Pharmacokinetics

Pharmacokinetics describes the absorption, distribution, metabolism, and excretion of injectable drugs. Following injection, drugs rapidly enter the bloodstream, allowing for immediate therapeutic action. Factors that influence pharmacokinetics include the injection site, formulation, and patient-specific variables such as age, weight, and organ function. The drug's half-life will determine the frequency of dosing and the potential for accumulation in the body.

Pregnancy

The use of injectable drugs during pregnancy depends on the specific drug. It is essential to assess the risk versus benefit for both mother and fetus. Some injectable drugs may be contraindicated during pregnancy.

Breast-feeding

Many injectable drugs can pass into breast milk. It is crucial to consider the safety of the drug for the breastfeeding infant and the necessity of the drug for the mother.

Storage

Injectable drugs should be stored according to manufacturer specifications, typically in a cool, dry place, away from light. Some may require refrigeration.

Indications

• Used as an emulsifier in pharmaceutical formulations
• Facilitates the solubilization of hydrophobic drugs
• Commonly included in vaccines to enhance efficacy and stability
• Acts as a stabilizer in food and cosmetic products

Dosage

Children: Refer to specific formulation guidelines for paediatric dosing, as polysorbate 80 is typically used in small amounts as an excipient.

Adults: Refer to specific formulation guidelines for adult dosing, as polysorbate 80 is typically used in small amounts as an excipient.

Mechanism of action

Polysorbate 80 functions by reducing the surface tension between two immiscible phases, such as oil and water. It contains both hydrophilic (water-attracting) and lipophilic (fat-attracting) components, which allows it to stabilize emulsions by preventing the coalescence of dispersed droplets. This mechanism enhances the bioavailability of hydrophobic substances by improving their solubility in aqueous environments.

Pharmacodynamics

As a surfactant, polysorbate 80 can improve the absorption and bioavailability of co-administered drugs by enhancing their solubility. Its ability to modify membrane permeability can also affect drug delivery and release profiles. However, polysorbate 80 is generally considered non-toxic at typical concentrations used in formulations.

Pharmacokinetics

Polysorbate 80 is not extensively absorbed through the gastrointestinal tract and is primarily eliminated through feces. It may undergo limited metabolism, with some hydrolysis occurring in the body. Due to its large molecular weight, it does not readily cross biological membranes. The pharmacokinetics can vary depending on the formulation and administration route, such as oral, intravenous, or topical.

Adverse effects

• Hypersensitivity reactions
• Gastrointestinal disturbances
• Injection site reactions
• Headache

Precautions

• Use with caution in patients with known allergies to polysorbates
• Monitor for hypersensitivity reactions, especially in parenteral formulations

Pregnancy

Polysorbate 80 is generally considered safe for use during pregnancy, but it should be used only if clearly needed.

Breast-feeding

Polysorbate 80 is considered safe during breastfeeding, as it is unlikely to affect the nursing infant.

Storage

Store in a cool, dry place, protected from light. Follow specific manufacturer's storage instructions for formulations.

Formulations

• Injectable solution
• Oral liquid
• Topical cream