CASPOFUNGIN / ANFARM

Indications

• Asthma
• Chronic obstructive pulmonary disease (COPD)
• Acute bronchospasm
• Apnea of prematurity

Dosage

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

Adults: Refer to the BNF for specific dosing information.

Mechanism of action

Aminophylline acts as a non-selective phosphodiesterase inhibitor, leading to an increase in intracellular cyclic AMP (cAMP). This elevation in cAMP levels causes relaxation of bronchial smooth muscle, resulting in bronchodilation. Additionally, aminophylline can also have anti-inflammatory effects and may enhance mucociliary clearance.

Pharmacodynamics

The therapeutic effects of aminophylline occur due to its bronchodilator properties, which help alleviate symptoms of airway obstruction. Its anti-inflammatory effects contribute to reducing airway hyper-responsiveness, while the increased cAMP also enhances cardiac contractility and improves diaphragmatic function.

Pharmacokinetics

Aminophylline is administered intravenously or orally and is absorbed well from the gastrointestinal tract. It undergoes hepatic metabolism, primarily through cytochrome P450 enzymes, and has a half-life of approximately 3 to 12 hours. The drug is excreted mainly in the urine as metabolites. Factors such as age, smoking status, and liver function can influence its pharmacokinetics.

Pregnancy

The safety of anfarm during pregnancy has not been established. It is recommended to avoid use unless the potential benefits outweigh the risks.

Breast-feeding

Use of anfarm during breastfeeding is not recommended due to the lack of data on excretion in breast milk.

Storage

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

Indications

• Invasive candidiasis
• Invasive aspergillosis
• Empirical treatment of systemic fungal infections in patients with neutropenia

Dosage

Adults: For adults with a body weight up to 81 kg: Loading dose of 70 mg once daily for 1 day, then maintenance dose of 50 mg once daily. For adults with a body weight

Mechanism of action

Caspofungin inhibits the synthesis of beta-(1,3)-D-glucan, an essential component of the cell wall of Aspergillus and Candida species. This inhibition occurs through the blockade of the enzyme beta-(1,3)-glucan synthase, which is crucial for fungal cell wall integrity. The absence of beta-(1,3)-D-glucan in mammalian cells means that Caspofungin selectively targets fungal cells while sparing human cells.

Pharmacodynamics

As an antifungal agent, Caspofungin has shown efficacy against various strains of Candida and Aspergillus. By inhibiting cell wall synthesis, it disrupts fungal growth and replication. While resistance can develop through mutations in the FKS1 gene, in vitro studies have not shown significant resistance development in Aspergillus species to Caspofungin, indicating good efficacy in treating these infections.

Pharmacokinetics

Caspofungin is administered intravenously and has a pharmacokinetic profile characterized by extensive protein binding (about 97%). It is metabolized primarily in the liver and does not undergo significant renal clearance. The drug has a half-life of approximately 9 to 11 hours, allowing for once-daily dosing after the initial loading dose. Its pharmacokinetics may be influenced by factors such as liver function and co-administration with other medications.

Adverse effects

• Nausea
• Vomiting
• Fever
• Rash
• Hypotension
• Elevated liver enzymes
• Anemia
• Headache

Interactions

• Efavirenz: moderate decrease in concentration
• Nevirapine: moderate decrease in concentration
• Ciclosporin: unknown effect on exposure
• Dexamethasone: unknown decrease in concentration
• Rifampicin: unknown decrease in concentration

Precautions

• Liver dysfunction should be monitored due to potential hepatotoxicity
• Hypersensitivity reactions could occur; monitor for signs
• Use with caution in patients with renal impairment
• Monitor for infusion-related reactions

Pregnancy

Manufacturer advises to avoid unless potential benefit outweighs risk; toxicity observed in animal studies.

Breast-feeding

Manufacturer advises to avoid unless potential benefit outweighs risk; present in milk in animal studies.

Storage

Store at room temperature, protect from light. Reconstituted solution should be used immediately or stored at 2-8°C for 24 hours.

Formulations

• Caspofungin 50 mg powder for solution for infusion
• Caspofungin 70 mg powder for solution for infusion

Mechanism of action

Caspofungin inhibits the synthesis of beta-(1,3)-D-glucan, an essential component of the cell wall of <i>Aspergillus</i> species and <i>Candida</i> species. beta-(1,3)-D-glucan is not present in mammalian cells. The primary target is beta-(1,3)-glucan synthase. Caspofungin inhibits the synthesis of beta(1,3)-d-glucan, an integral component of the fungal cell wall that is not present in mammalian cells. Caspofungin acetate ... /belongs to a class of drugs/ referred to as echinocandins, which inhibit the formation of beta(1,3)-D-glucans in the fungal cell wall. Resistance is conferred by mutations in the FKS1 gene, which codes for a large subunit of (1,3)beta-glucan synthase. /Caspofungin acetate/ Caspofungin acetate, the active ingredient of cancidas, inhibits the synthesis of alpha(1,3)-D-glucan, an essential component of the cell wall of susceptible Aspergillus species and Candida species. (1,3)-D-glucan is not present in mammalian cells. Caspofungin has shown activity against Candida species and in regions of active cell growth of the hyphae of Aspergillus fumigatus. /Caspofungin acetate/

Pharmacodynamics

Caspofungin is an antifungal drug, and belongs to a new class termed the echinocandins. It is used to treat <i>Aspergillus</i> and <i>Candida</i> infection, and works by inhibiting cell wall synthesis. Antifungals in the echinocandin class inhibit the synthesis of glucan in the cell wall, probably via the enzyme 1,3-beta glucan synthase. There is a potential for resistance development to occur, however <i>in vitro</i> resistance development to Caspofungin by Aspergillus species has not been studied.