LEQVIOTM SOLUTION FOR INJECTION

Indications

• Primary hypercholesterolaemia
• Mixed dyslipidaemia
• Homozygous familial hypercholesterolaemia

Dosage

Children: null

Adults: 420 mg every 2 weeks, or for specific cases, 284 mg initially for 1 dose, followed by 284 mg after 3 months for 1 dose, then 284 mg every 6 months.

Mechanism of action

Inclisiran acts by interfering with the messenger RNA (mRNA) for PCSK9, leading to a decrease in PCSK9 protein production. This action results in increased uptake of LDL cholesterol by the liver and a reduction in circulating LDL cholesterol levels. The inhibition of PCSK9 enhances the recycling of LDL receptors, which further contributes to lowering LDL cholesterol in the bloodstream.

Pharmacodynamics

The pharmacodynamic effects of Inclisiran include significant reductions in LDL cholesterol levels, observed within weeks of administration. The drug's effects are sustained over time, with maintenance doses leading to persistent reductions in LDL cholesterol. The efficacy of Inclisiran can be seen in various patient populations, including those with familial hypercholesterolaemia and those at high cardiovascular risk.

Pharmacokinetics

Inclisiran is administered subcutaneously, with peak plasma concentrations occurring approximately 2 to 4 hours post-injection. It has a long half-life, allowing for less frequent dosing. The drug is primarily eliminated by the liver, with renal excretion playing a minimal role in its pharmacokinetics. The pharmacokinetic profile is not significantly altered in patients with liver or renal impairment, but caution is advised in severe cases.

Contra-indications

• Hypersensitivity to inclisiran or any excipients
• Severe hepatic impairment
• Severe renal impairment

Adverse effects

• Arthralgia
• Back pain
• Increased risk of infection
• Nausea
• Skin reactions
• Influenza-like illness
• Angioedema

Precautions

• Caution in patients with moderate hepatic impairment
• Caution in patients with moderate to severe renal impairment
• Patients should be trained in subcutaneous injection technique

Pregnancy

Avoid unless potential benefit outweighs risk-limited information available.

Breast-feeding

Avoid-present in milk in animal studies.

Storage

Store in a refrigerator (2–8°C)-consult product literature for further information regarding storage outside refrigerator.

Formulations

• Solution for injection

Indications

• COVID-19
• SARS-CoV-2 infection

Dosage

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

Adults: Refer to the BNF for specific dosing recommendations based on clinical guidelines.

Mechanism of action

Nirmatrelvir is a selective inhibitor of the SARS-CoV-2 main protease (Mpro). By binding to the active site of this enzyme, nirmatrelvir prevents the cleavage of viral polyproteins, which is essential for the maturation of the virus. This ultimately inhibits viral replication.

Pharmacodynamics

Nirmatrelvir exhibits antiviral activity by specifically targeting the main protease of SARS-CoV-2. The inhibition of Mpro disrupts the viral life cycle, reducing the viral load in the body. The potency of nirmatrelvir is enhanced by ritonavir, which prolongs its action by slowing its metabolism.

Pharmacokinetics

Nirmatrelvir is rapidly absorbed after oral administration. The bioavailability is increased when combined with ritonavir, which inhibits CYP3A4, the enzyme responsible for nirmatrelvir's metabolism. The half-life of nirmatrelvir is approximately 7 hours, allowing for twice-daily dosing. It is primarily excreted via feces and urine, with minimal renal clearance.

Interactions

• nirmatrelvir boosted with ritonavir and containing ethinylestradiol: Unknown (decreases concentration)

Dosage

Children: Refer to specific drug information for detailed dosage recommendations.

Adults: Refer to specific drug information for detailed dosage recommendations.

Mechanism of action

The mechanism of action varies depending on the specific drug that 'contains' certain active ingredients. Each compound will have its own unique pharmacological pathway and target within the body, which can include receptor modulation, enzyme inhibition, or other biochemical interactions.

Pharmacodynamics

Pharmacodynamics will depend on the active ingredients in the formulation. It generally encompasses the biochemical and physiological effects of the drug and its mechanisms of action, including the relationship between drug concentration and effect.

Pharmacokinetics

Pharmacokinetics involves the absorption, distribution, metabolism, and excretion of the specific active ingredients within the formulation. This can vary significantly based on the drug's chemical properties, route of administration, and individual patient factors.

Pregnancy

Consult with a healthcare provider before use, as safety during pregnancy has not been established.

Breast-feeding

Consult with a healthcare provider before use, as it is not known if this drug is excreted in human milk.

Storage

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

Indications

• Administration of medications
• Vaccination
• Blood sampling
• Intravenous fluid delivery
• Intramuscular injection
• Subcutaneous injection

Dosage

Children: Refer to specific medication guidelines for dosing.

Adults: Refer to specific medication guidelines for dosing.

Mechanism of action

The syringe itself does not have a pharmacological mechanism of action, as it is a delivery system rather than a drug. Its function is to create a vacuum that allows for the drawing in or expulsion of fluids, relying on the movement of the plunger within the barrel to generate pressure differences.

Pharmacodynamics

As a non-pharmacological device, the pharmacodynamics of a syringe do not apply directly. However, the effectiveness of medications administered via syringe depends on the drug's own pharmacodynamics, which include the interactions with receptors, the onset of action, and the therapeutic effects of the drug delivered.

Pharmacokinetics

The pharmacokinetics of a syringe are not applicable, as it is a mechanical device. However, the pharmacokinetics of the medication administered through the syringe would include absorption, distribution, metabolism, and excretion, which are influenced by the route of administration (e.g., intravenous, intramuscular, subcutaneous).

Pregnancy

Syringes are generally safe for use during pregnancy when necessary for medication administration.

Breast-feeding

Syringes can be used during breastfeeding for medication administration without adverse effects.

Storage

Store syringes in a clean, dry place. Follow specific guidelines for pre-filled syringes or those with medications.

Formulations

• plastic syringes
• glass syringes
• pre-filled syringes
• safety syringes