ESOQUIN 40MG CAPSULE

Indications

• Gastroesophageal reflux disease (GERD)
• Erosive esophagitis
• Peptic ulcers
• Helicobacter pylori eradication
• Zollinger-Ellison syndrome

Dosage

Adults: The usual oral dose

Mechanism of action

Esomeprazole exerts its stomach acid-suppressing effects by covalently binding to cysteine residues on the H+/K+-ATPase enzyme at the secretory surface of gastric parietal cells. This action inhibits both basal and stimulated gastric acid secretion irreversibly, requiring the synthesis of new enzyme to restore acid production. By blocking the final step of gastric acid production, esomeprazole reduces gastric acidity in a dose-dependent manner.

Pharmacodynamics

Esomeprazole is a substituted benzimidazole that inhibits gastric acid secretion without exhibiting anticholinergic or H2 receptor antagonistic properties. It is indicated for the treatment of GERD, healing of erosive esophagitis, and eradication of H. pylori to reduce duodenal ulcer recurrence. The suppression of gastric acid secretion is dose-related and effective against various stimuli that promote acid secretion.

Pharmacokinetics

Esomeprazole is rapidly absorbed after oral administration, with peak plasma concentrations typically occurring within 1-2 hours. It undergoes extensive hepatic metabolism primarily by the cytochrome P450 system, especially CYP2C19, resulting in several metabolites. The elimination half-life is approximately 1-2 hours, though its antisecretory effects last longer. It is excreted predominantly in the urine. Dose adjustments may be necessary in patients with hepatic impairment.

Contra-indications

• Hypersensitivity to esomeprazole or any of its components
• Concomitant use with rilpivirine-containing products

Adverse effects

• Abdominal pain
• Constipation
• Diarrhea
• Dizziness
• Dry mouth
• Headache
• Insomnia
• Nausea
• Skin reactions
• Vomiting
• Bone fractures
• Confusion
• Depression
• Drowsiness
• Leucopenia
• Malaise
• Myalgia
• Paraesthesia
• Peripheral edema
• Thrombocytopenia
• Vertigo
• Vision disorders
• Agranulocytosis
• Alopecia
• Gynaecomastia
• Hallucination
• Hepatic disorders
• Hyperhidrosis
• Hyponatraemia
• Nephritis
• Tubulointerstitial nephritis
• Pancytopenia
• Photosensitivity reaction
• Severe cutaneous adverse reactions (SCARs)
• Stomatitis
• Taste altered
• Hypomagnesaemia

Interactions

• Esomeprazole may increase the exposure to cannabidiol
• Esomeprazole may increase the exposure to cilostazol

Precautions

• Increased risk of fractures, particularly in the elderly and when used at high doses for over a year
• Caution in patients at risk of osteoporosis; adequate intake of calcium and vitamin D is recommended
• May increase the risk of gastrointestinal infections, including Clostridioides difficile
• Symptoms of gastric cancer should be ruled out before treatment
• Use with caution in patients with hepatic impairment

Pregnancy

Use with caution. The manufacturer advises avoiding use unless necessary since the effects on the fetus are not fully known.

Breast-feeding

Manufacturer advises avoiding use as esomeprazole is present in breast milk and may cause diarrhea in nursing infants. However, amounts are probably too small to be harmful.

Storage

Store in a cool, dry place below 25°C. Keep out of

Dosage

Children: Refer to the specific active ingredient for appropriate dosing guidelines.

Adults: Refer to the specific active ingredient for appropriate dosing guidelines.

Mechanism of action

The mechanism of action varies depending on the specific active ingredient. Generally, active substances interact with biological targets such as receptors, enzymes, or ion channels to elicit a pharmacological response. This may involve agonistic or antagonistic activity at receptor sites, modulation of enzyme activity, or alteration of cellular signaling pathways, leading to the desired therapeutic effects.

Pharmacodynamics

Pharmacodynamics describes the effects of the active drug on the body, including the relationship between drug concentration, receptor binding, and the resultant biological effect. The dynamics can vary significantly based on the drug's class, with different pharmacological profiles influencing efficacy, potency, and safety. Factors such as receptor affinity, intrinsic activity, and the presence of any allosteric modulators can impact how the active drug performs therapeutically.

Pharmacokinetics

Pharmacokinetics involves the absorption, distribution, metabolism, and excretion (ADME) of the active drug. Following administration, the drug is absorbed into the bloodstream, distributed throughout the body, metabolized primarily by the liver, and eventually excreted via the kidneys or other routes. The pharmacokinetic profile is crucial for determining dosing regimens and understanding the duration of action, peak plasma concentrations, and the potential for drug interactions.

Pregnancy

Consult healthcare provider for potential risks versus benefits.

Breast-feeding

Consult healthcare provider as it may affect milk production or composition.

Storage

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

Dosage

Children: Refer to specific ingredient guidelines for paediatric dosing; consult a pharmacological database or prescribing information.

Adults: Refer to specific ingredient guidelines for adult dosing; consult a pharmacological database or prescribing information.

Mechanism of action

The mechanism of action of an ingredient depends on its specific chemical nature. Active ingredients typically interact with biological systems through various pathways, such as enzyme inhibition, receptor activation, or modulation of physiological processes. Understanding the specific mechanisms requires knowledge of the individual ingredient.

Pharmacodynamics

Pharmacodynamics of an ingredient refers to the effects it has on the body, including the relationship between drug concentration and effect. This can involve receptor binding, post-receptor effects, and the overall therapeutic outcomes. The pharmacodynamic profile varies significantly between different ingredients.

Pharmacokinetics

Pharmacokinetics describes how an ingredient is absorbed, distributed, metabolized, and excreted in the body. It includes parameters such as bioavailability, half-life, volume of distribution, and clearance. These parameters are influenced by the ingredient's chemical properties, formulation, and the patient's individual characteristics.

Pregnancy

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

Breast-feeding

Consult a healthcare professional before use, as safety during breastfeeding has not been established.

Storage

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

Dosage

Children: Refer to specific drug guidelines for dosing information in pediatric patients, as pediatric dosing is determined based on age, weight, and clinical condition.

Adults: Refer to specific drug guidelines for dosing information, as it varies significantly based on the drug and the condition being treated.

Mechanism of action

The mechanism of action varies by drug. For example, analgesics may work by inhibiting cyclooxygenase enzymes, while antibiotics may target bacterial cell wall synthesis. Understanding the specific drug is crucial for identifying its mechanism.

Pharmacodynamics

Pharmacodynamics involves how a drug affects the body, including its therapeutic effects, side effects, and the relationship between drug concentration and effect. This varies widely among different classes of drugs.

Pharmacokinetics

Pharmacokinetics describes how the body absorbs, distributes, metabolizes, and excretes a drug. Parameters such as bioavailability, half-life, volume of distribution, and clearance are important but differ based on specific drugs.

Indications

• Condition A (common term)
• Condition B (clinical term)
• Condition C (common term)
• Condition D (clinical term)

Dosage

Children: Refer to the BNF for Children for specific dosing guidelines in paediatric patients, as these doses are determined based on age, weight, and clinical condition.

Adults: Refer to the appropriate clinical guidelines and dosing recommendations for adults, as specific doses can vary based on indication and patient factors.

Mechanism of action

Name acts by binding to specific receptors or enzymes in the body, leading to a cascade of biochemical events that result in its therapeutic effects. This mechanism often involves modulation of neurotransmitter levels, alteration of cellular signaling pathways, or inhibition of certain biological processes. Such interactions typically enhance or inhibit physiological functions relevant to the condition being treated.

Pharmacodynamics

The pharmacodynamics of Name involve the study of the drug's effects on the body and the relationship between drug concentration and effect. The drug may exhibit dose-dependent responses, where higher concentrations lead to increased efficacy or adverse effects. The time course of action, therapeutic window, and potential side effects are critical considerations in the clinical use of this medication.

Pharmacokinetics

Pharmacokinetics describes the absorption, distribution, metabolism, and excretion (ADME) of Name. After administration, the drug is absorbed into the bloodstream and distributed throughout the body. It is metabolized primarily by the liver, where it may undergo biotransformation into active or inactive metabolites. The elimination half-life of the drug determines the frequency of dosing and helps inform therapeutic monitoring.

Pregnancy

Consult healthcare provider for risks and benefits.

Breast-feeding

Consult healthcare provider for risks and benefits.

Storage

Store in a cool, dry place away from light.

Dosage

Children: Paediatric dosing is typically based on weight or body surface area, and varies significantly by drug class and indication. Refer to specific paediatric dosing guidelines or pharmacological references for detailed information.

Adults: Dosage varies widely depending on the specific pharmaceutical, its formulation, and the condition being treated. Refer to specific drug guidelines or pharmacological references for detailed dosing information.

Mechanism of action

The mechanism of action of pharmaceuticals varies widely depending on the class and specific drug. Generally, pharmaceuticals interact with biological systems at the molecular level, affecting cellular processes, signaling pathways, or biochemical reactions. They may act as agonists or antagonists at receptors, inhibit enzymes, or modify the activity of transport proteins.

Pharmacodynamics

Pharmacodynamics refers to the effects of pharmaceuticals on the body and their mechanisms of action. This encompasses the relationship between drug concentration and therapeutic effect, including the onset, duration, and intensity of action. Pharmaceuticals may exhibit dose-response relationships where higher doses lead to greater effects, but can also lead to toxicity beyond a certain threshold. The pharmacodynamic profile is crucial for determining the appropriate dosing regimens for safe and effective therapy.

Pharmacokinetics

Pharmacokinetics involves the study of how the body absorbs, distributes, metabolizes, and excretes pharmaceuticals. Key parameters include absorption rates, volume of distribution, half-life, and clearance. Pharmaceuticals can be administered through various routes such as oral, intravenous, and topical, each affecting their pharmacokinetic properties. Understanding these factors is essential for optimizing therapeutic regimens and minimizing adverse effects.

Mechanism of action

Esomeprazole exerts its stomach acid-suppressing effects by preventing the final step in gastric acid production by covalently binding to sulfhydryl groups of cysteines found on the (H+, K+)-ATPase enzyme at the secretory surface of gastric parietal cells. This effect leads to inhibition of both basal and stimulated gastric acid secretion, irrespective of the stimulus. As the binding of esomeprazole to the (H+, K+)-ATPase enzyme is irreversible and new enzyme needs to be expressed in order to resume acid secretion, esomeprazole's duration of antisecretory effect that persists longer than 24 hours. Esomeprazole is a proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of the H+/K+-ATPase in the gastric parietal cell. The S- and R-isomers of omeprazole are protonated and converted in the acidic compartment of the parietal cell forming the active inhibitor, the achiral sulphenamide. By acting specifically on the proton pump, esomeprazole blocks the final step in acid production, thus reducing gastric acidity. This effect is dose-related up to a daily dose of 20 to 40 mg and leads to inhibition of gastric acid secretion.

Pharmacodynamics

Esomeprazole is a compound that inhibits gastric acid secretion and is indicated in the treatment of gastroesophageal reflux disease (GERD), the healing of erosive esophagitis, and <i>H. pylori</i> eradication to reduce the risk of duodenal ulcer recurrence. Esomeprazole belongs to a new class of antisecretory compounds, the substituted benzimidazoles, that do not exhibit anticholinergic or H2 histamine antagonistic properties, but that suppress gastric acid secretion by specific inhibition of the H⁺/K⁺ ATPase at the secretory surface of the gastric parietal cell. By doing so, it inhibits acid secretion into the gsatric lumen. This effect is dose-related and leads to inhibition of both basal and stimulated acid secretion irrespective of the stimulus. Esomeprazole is the s-isomer of [DB00338], which is a racemate of the S- and R-enantiomer. Esomeprazole has been shown to inhibit acid secretion to a similar extent as [DB00338], without any significant differences between the two compounds _in vitro_. PPIs such as esomeprazole have also been shown to inhibit the activity of dimethylarginine dimethylaminohydrolase (DDAH), an enzyme necessary for cardiovascular health. DDAH inhibition causes a consequent accumulation of the nitric oxide synthase inhibitor asymmetric dimethylarginie (ADMA), which is thought to cause the association of PPIs with increased risk of cardiovascular events in patients with unstable coronary syndromes. Due to their good safety profile and as several PPIs are available over the counter without a prescription, their current use in North America is widespread. Long term use of PPIs such as esomeprazole has been associated with possible adverse effects, however, including increased susceptibility to bacterial infections (including gastrointestinal _C. difficile_), reduced absorption of micronutrients including iron and B12, and an increased risk of developing hypomagnesemia and hypocalcemia which may contribute to osteoporosis and bone fractures later in life.