LANPRO 30 MG CPASULES

Indications

• Gastro-oesophageal reflux disease
• Duodenal ulcer
• Benign gastric ulcer
• NSAID-associated gastric or duodenal ulcer
• Zollinger-Ellison syndrome

Dosage

Adults: 30 mg once daily for 4 weeks for duodenal ulcers, 30 mg once daily for 8 weeks for gastric ulcers, and 15 mg once daily for maintenance treatment. For gastro-oesophageal reflux disease, the usual dose is 15 mg

Mechanism of action

Lansoprazole is a prodrug that becomes activated in an acidic environment. Once protonated, it forms stable disulfide bonds with cysteine residues on the H+,K+-ATPase enzyme in parietal cells. This covalent binding leads to prolonged inhibition of gastric acid secretion, affecting both basal and stimulated acid production regardless of the stimulus.

Pharmacodynamics

Lansoprazole decreases gastric acid secretion by specifically targeting the H+,K+-ATPase enzyme, which catalyzes the final step in gastric acid secretion. It effectively heals duodenal ulcers and alleviates symptoms associated with acid secretion, such as heartburn, while also reducing pepsin secretion. Its action is effective in both daytime and nocturnal acid secretion, making it useful in treating various acid-related disorders.

Pharmacokinetics

Lansoprazole is absorbed after oral administration, with peak plasma concentrations usually occurring within 1-2 hours. It is extensively metabolized in the liver primarily via cytochrome P450 enzymes, leading to various metabolites that are excreted in urine. The half-life of lansoprazole is approximately 1.5 hours, but its acid-suppressive effects last longer due to its mechanism of action. The presence of food can affect the absorption rate, so it is typically recommended to take lansoprazole before meals.

Contra-indications

• Hypersensitivity to lansoprazole or any of its excipients
• Concurrent use with rilpivirine-containing products

Adverse effects

• Headache
• Diarrhoea
• Nausea
• Abdominal pain
• Constipation
• Flatulence
• Dizziness
• Fatigue
• Skin rash
• Elevated liver enzymes
• Acute interstitial nephritis
• Clostridium difficile-associated diarrhoea
• Bone fractures
• Hypomagnesemia

Interactions

• Increased risk of gastrointestinal infections due to reduced gastric acidity
• Apalutamide may decrease exposure when used with lansoprazole
• May alter the absorption of drugs that require an acidic environment for optimal absorption

Precautions

• Use with caution in patients with hepatic impairment
• Monitor for signs of Clostridium difficile infection in patients with prolonged therapy
• Consider risk of hypomagnesemia and associated complications

Pregnancy

Manufacturer advises to avoid use during pregnancy due to lack of adequate human data.

Breast-feeding

Specialist sources indicate use with caution, as lansoprazole is likely to be present in human milk, but in small amounts probably too low to be harmful.

Storage

Store below 25°C in a dry place, protect from light.

Formulations

• Gastro-resistant capsules
• Oral suspension
• Gastro-resistant tablets
• Gastro-resistant granules

Indications

• Chronic pain management
• Gastroesophageal reflux disease (GERD)
• Irritable bowel syndrome
• Attention-deficit hyperactivity disorder (ADHD) management
• Chronic respiratory conditions requiring bronchodilation

Dosage

Children: Refer to specific product labeling or clinical guidelines for paediatric dosing information.

Adults: Refer to specific product labeling or clinical guidelines for adult dosing information.

Mechanism of action

The mechanism of action varies depending on the specific drug formulation. Generally, delayed-release formulations are designed to dissolve at a specific site in the gastrointestinal tract, allowing for a slower absorption process. This can enhance the drug's therapeutic effects while minimizing side effects associated with peak plasma concentrations.

Pharmacodynamics

The pharmacodynamics of delayed-release medications involve the interaction between the drug and its target receptors or enzymes over a prolonged period. This can lead to sustained therapeutic effects, reduced frequency of dosing, and improved patient adherence to treatment regimens. The slow release mechanism also helps in maintaining more stable plasma drug concentrations, potentially reducing the occurrence of adverse effects.

Pharmacokinetics

Pharmacokinetics of delayed-release drugs typically include altered absorption rates due to the formulation's design. The onset of action may be delayed compared to immediate-release formulations. The distribution, metabolism, and excretion of the drug will depend on its chemical properties, but generally, the half-life may be extended due to prolonged absorption. Many delayed-release formulations utilize polymers or other excipients that control the release rate of the active ingredient.

Pregnancy

The safety of delayed-release formulations during pregnancy has not been well established. Consultation with a healthcare provider is recommended.

Breast-feeding

Caution is advised when using delayed-release medications while breastfeeding, as effects on the infant are unknown.

Storage

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

Indications

• Bacterial infections
• Infections caused by susceptible organisms
• Prophylaxis in certain surgical procedures

Dosage

Children: Refer to the BNF for Children for specific dosing recommendations based on age, weight, and condition.

Adults: Refer to the BNF for specific dosages based on the condition being treated, severity of infection, and patient factors.

Mechanism of action

Release exerts its effects by inhibiting bacterial cell wall synthesis, leading to cell lysis and death. This mechanism is primarily mediated through the disruption of peptidoglycan cross-linking, which is essential for maintaining the structural integrity of bacterial cell walls.

Pharmacodynamics

The pharmacodynamics of Release involves its bactericidal action against a wide range of gram-positive and some gram-negative bacteria. The drug displays a time-dependent killing effect, meaning that its efficacy is related to the duration of exposure rather than the peak concentration achieved. Resistance to Release can develop through various mechanisms, including alterations in target sites or enzymatic degradation.

Pharmacokinetics

Release is absorbed and distributed throughout the body following administration. Peak plasma concentrations are typically achieved within a few hours. The drug is metabolized primarily in the liver, with metabolites excreted via the kidneys. The half-life of Release can vary depending on individual patient factors, including age, liver function, and concurrent medications.

Mechanism of action

As a PPI, lansoprazole is a prodrug and requires protonation via an acidic environment to become activated. Once protonated, lansoprazole is able to react with cysteine residues, specifically Cys813 and Cys321, on parietal H+,K+-ATPase resulting in stable disulfides. PPI's in general are able to provide prolonged inhibition of acid secretion due to their ability to bind covalently to their targets. Lansoprazole is a selective and irreversible proton pump inhibitor. In the acidic environment of the gastric parietal cell, lansoprazole is converted to active sulphenamide derivatives that bind to the sulfhydryl group of (H+, K+)-adenosine triphosphatase ((H+,K+)-ATPase), also known as the proton pump (H+,K+)-ATPase catalyzes the final step in the gastric acid secretion pathway. Lansoprazole's inhibition of (H+,K+)-ATPase results in inhibition of both centrally and peripherally mediated gastric acid secretion. The inhibitory effect is dose-related. Lansoprazole inhibits both basal and stimulated gastric acid secretion regardless of the stimulus.

Pharmacodynamics

Lansoprazole decreases gastric acid secretion by targeting H+,K+-ATPase, which is the enzyme that catalyzes the final step in the acid secretion pathway in parietal cells. Conveniently, lansoprazole administered any time of day is able to inhibit both daytime and nocturnal acid secretion. The result is that lansoprazole is effective at healing duodenal ulcers, reduces ulcer-related pain, and offers relief from symptoms of heartburn Lansoprazole also reduces pepsin secretion, making it a useful treatment option for hypersecretory conditions such as Zollinger-Ellison syndrome.