NEOPEPTINE 100/100/30MG CAPSULE

Indications

• Hypertension
• Benign prostatic hyperplasia
• Urinary retention related to prostate enlargement

Dosage

Children: Refer to the BNF for Children for appropriate dosing guidelines in the paediatric population.

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

Mechanism of action

Alpha acts by selectively blocking alpha-1 adrenergic receptors, which are responsible for mediating vasoconstriction in blood vessels. By inhibiting these receptors, alpha promotes vasodilation, leading to a decrease in peripheral vascular resistance and subsequently lowering blood pressure. Additionally, this action can help alleviate urinary symptoms associated with an enlarged prostate.

Pharmacodynamics

The pharmacodynamics of alpha involve its competitive antagonism at alpha-1 adrenergic receptors, resulting in decreased vasoconstriction and increased blood flow. This mechanism is beneficial in conditions characterized by high blood pressure and urinary retention due to prostatic enlargement. The onset of action typically occurs within hours, with peak effects observed within a few days of consistent dosing.

Pharmacokinetics

Alpha is absorbed well from the gastrointestinal tract, with peak plasma concentrations achieved within 1-3 hours post-administration. The drug undergoes hepatic metabolism, primarily via cytochrome P450 enzymes, resulting in active and inactive metabolites. The elimination half-life varies, but it generally is around 6-12 hours, allowing for once-daily dosing in many cases. Renal excretion is a significant route for its metabolites, necessitating caution in patients with renal impairment.

Interactions

• maois, irreversible + alpha blockers: Severe (increases effects)
• ribociclib + alpha blockers: Severe (increases exposure)
• cobicistat + alpha blockers: Moderate (increases exposure)
• idelalisib + alpha blockers: Moderate (increases exposure)
• dronedarone + alpha blockers: Unknown (increases exposure)
• antifungals, azoles + alpha blockers: Unknown (increases exposure)
• crizotinib + alpha blockers: Unknown (increases exposure)
• imatinib + alpha blockers: Unknown (increases exposure)
• letermovir + alpha blockers: Unknown (increases exposure)
• clarithromycin + alpha blockers: Unknown (increases exposure)

Indications

• Pancreatitis
• Salivary gland disorders
• Carbohydrate malabsorption syndromes

Dosage

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

Adults: Refer to the specific guidelines and dosing recommendations in the BNF.

Mechanism of action

Amylase facilitates the breakdown of starch and glycogen into maltose and dextrins by cleaving the α-1,4-glycosidic bonds in these polysaccharides. Its action begins in the mouth with salivary amylase and continues in the small intestine with pancreatic amylase, where it further digests carbohydrates.

Pharmacodynamics

Amylase increases the rate of carbohydrate digestion, thereby influencing blood glucose levels. The enzyme's activity can be affected by pH levels, temperature, and the presence of inhibitors or activators. In clinical settings, elevated levels of amylase in the blood can indicate pancreatitis or other pancreatic disorders.

Pharmacokinetics

Amylase is absorbed and metabolized in the gastrointestinal tract. Its activity is measured through serum levels, with normal ranges indicating proper pancreatic function. The half-life of amylase in the bloodstream can vary based on individual metabolic rates and health conditions.

Pregnancy

Amylase is generally considered safe during pregnancy but should be used under medical supervision.

Breast-feeding

Amylase is excreted in breast milk; it is advisable to consult a healthcare provider before use while breastfeeding.

Storage

Store in a cool, dry place away from direct sunlight.

Indications

• Digestive disorders
• Protein digestion aid
• Wound healing
• Anti-inflammatory treatment

Dosage

Children: Refer to specific product guidelines or consult a healthcare professional for pediatric dosing recommendations.

Adults: Refer to specific product guidelines or consult a healthcare professional for dosing recommendations, as doses can vary based on formulation and indication.

Mechanism of action

Papain works by hydrolyzing peptide bonds in proteins, which facilitates their digestion and absorption. It acts primarily in the gastrointestinal tract, where it helps convert complex proteins into simpler forms that can be easily absorbed. Papain's proteolytic action also contributes to its anti-inflammatory properties, as it can help reduce swelling and promote healing in tissues.

Pharmacodynamics

Papain exhibits its effects through its enzymatic activity on proteins. The breakdown of proteins into smaller peptides and amino acids aids in the digestive process. This enzymatic action is complemented by papain's ability to modulate inflammatory responses, which can be beneficial in treating conditions associated with tissue damage and inflammation.

Pharmacokinetics

Papain is typically administered orally or topically. When taken orally, it is subject to the acidic environment of the stomach, which may affect its stability and activity. However, it is generally well absorbed in the gastrointestinal tract. Topically applied papain is absorbed through the skin, where it can exert local effects. The half-life and specific metabolic pathways of papain are not well characterized due to its natural origin and the variability in formulations.

Contra-indications

• Hypersensitivity to papain or any of its components
• History of allergic reactions to other proteolytic enzymes

Adverse effects

• Allergic reactions including rash, itching, or swelling
• Gastrointestinal disturbances such as nausea, vomiting, or diarrhea
• Potential irritation or inflammation at the site of application

Precautions

• Use with caution in individuals with known allergies to other enzymes or related substances
• Consult a healthcare provider before use in patients with gastrointestinal disorders
• Not recommended for use in infants and young children without medical supervision

Pregnancy

Safety during pregnancy has not been established. Use only if clearly needed and prescribed by a healthcare professional.

Breast-feeding

There is insufficient data on the excretion of papain in human milk. Caution is advised when administering to nursing mothers.

Storage

Store at room temperature away from moisture and heat. Keep tightly closed in a cool, dry place.

Formulations

• Oral tablets
• Topical creams or ointments
• Powder for solution

Indications

• Flatulence
• Bloating
• Gastroesophageal reflux disease
• Functional dyspepsia

Dosage

Children: For children, refer to the BNF for Children for specific dosing recommendations.

Adults: The usual adult dose is 40 to 125 mg taken after meals and at bedtime, as needed.

Mechanism of action

Simethicone is a surfactant that decreases the surface tension of gas bubbles in the gastrointestinal tract, facilitating their expulsion. It acts by forming a film of low surface tension that promotes the coalescence of mucus-surrounded gas bubbles, allowing for easier passage of gas.

Pharmacodynamics

Simethicone decreases the surface tension of gas bubbles in the gastrointestinal tract, facilitating their expulsion. Its effects are generally short-lived, as it is typically administered as needed. The therapeutic index is wide since it is not absorbed systemically, making it safe for use in various patient populations.

Pharmacokinetics

Simethicone is not systemically absorbed following oral administration, which contributes to its safety profile. Due to its lack of systemic absorption, specific pharmacokinetic parameters such as half-life, clearance, and volume of distribution are not applicable.

Pregnancy

Simethicone can be used during pregnancy as there are no known risks associated with its use.

Breast-feeding

Simethicone is considered safe to use during breastfeeding, as it is not absorbed systemically.

Storage

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

Formulations

• Oral suspension
• Chewable tablets
• Soft gels

Mechanism of action

Simethicone is a surfactant that decreases the surface tension of gas bubbles in the gastrointestinal tract, more easily allowing gas to exit the body. The clinical use of simethicone is based on its antifoam properties. Silicone antifoams spread on the surface of aqueous liquids, forming a film of low surface tension and thus causing collapse of foam bubbles. Simethicone reportedly allows mucus-surrounded gas bubbles in the GI tract to coalesce and be expelled.

Pharmacodynamics

Simethicone decreases the surface tension of gas bubbles in the gastrointestinal tract, facilitating their expulsion. It has a short duration of action as it is generally given as needed, and a wide therapeutic index as it is not systemically absorbed.