GLIPINN 50

Indications

• Constipation
• Dietary fiber supplementation
• Irritable bowel syndrome
• Diverticular disease
• Weight management

Dosage

Children: Refer to appropriate guidelines for specific dosage; generally taken with adequate fluid intake.

Adults: Refer to appropriate guidelines for specific dosage; generally taken with adequate fluid intake.

Mechanism of action

Cellulose acts primarily as a bulk-forming laxative. It absorbs water in the intestines, which increases stool bulk and stimulates peristalsis, thus facilitating bowel movements. Additionally, cellulose is not digestible by human enzymes, leading to fermentation by gut bacteria, which may enhance gut health and alter gut microbiota composition.

Pharmacodynamics

Cellulose increases stool weight and frequency of bowel movements. It works by retaining water in the intestines, leading to softer stools and improved passage through the gastrointestinal tract. The bulking effect of cellulose can help alleviate constipation and promote overall digestive health. It may also play a role in cholesterol reduction and glycemic control through its effects on digestion and absorption of nutrients.

Pharmacokinetics

Cellulose is not absorbed into the bloodstream due to its indigestible nature. Instead, it passes through the gastrointestinal tract, where it adds bulk to the stool. Its fermentation by colonic bacteria produces short-chain fatty acids, which may have beneficial effects on colon health. The onset of action for cellulose as a laxative can vary but is generally within 24 to 72 hours after ingestion.

Adverse effects

• Bloating
• Flatulence
• Diarrhea
• Abdominal discomfort

Precautions

• Use with caution in patients with a history of gastrointestinal disorders.
• Monitor for potential allergic reactions in sensitive individuals.

Pregnancy

Cellulose is generally considered safe during pregnancy as it is a non-toxic, indigestible fiber.

Breast-feeding

Cellulose is also considered safe during breastfeeding; it is excreted in breast milk in negligible amounts.

Storage

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

Formulations

• Powder
• Capsules
• Tablets
• Granules

Indications

• Tablet formulation
• Capsule formulation
• Rapid release of active pharmaceutical ingredients

Dosage

Children: Refer to specific product guidelines for exact formulations. Typically used in concentrations of 1-5% in solid dosage forms.

Adults: Refer to specific product guidelines for exact formulations. Typically used in concentrations of 1-5% in solid dosage forms.

Mechanism of action

Crosscarmellose sodium works by swelling upon contact with water, leading to the rapid disintegration of the dosage form. This process increases the surface area of the active ingredient, promoting faster dissolution and absorption in the gastrointestinal tract. It does not possess any pharmacological activity of its own but acts as a functional excipient.

Pharmacodynamics

As a disintegrant, crosscarmellose sodium aids in the breakdown of solid dosage forms, allowing for quicker release and absorption of active ingredients. Its effectiveness is influenced by factors such as the formulation's composition, the presence of other excipients, and the conditions within the gastrointestinal environment.

Pharmacokinetics

Crosscarmellose sodium is not absorbed in the gastrointestinal tract and does not undergo metabolism. It functions primarily as a physical agent that enhances the disintegration of the dosage form. Its safety profile is well-established, and it is considered non-toxic and non-irritating.

Pregnancy

Crosscarmellose is considered safe for use during pregnancy as it is not systemically absorbed, but consult a healthcare provider for specific cases.

Breast-feeding

Crosscarmellose is not absorbed systemically and is generally considered safe during breastfeeding, but consult a healthcare provider for specific cases.

Storage

Store in a cool, dry place away from moisture and heat.

Formulations

• Tablets
• Capsules
• Powders

Dosage

Children: Refer to specific formulations and clinical guidelines for dosing information as this can vary widely based on the context of use.

Adults: Refer to specific formulations and clinical guidelines for dosing information as this can vary widely based on the context of use.

Mechanism of action

Dibasic compounds often act by providing a buffering effect in biological systems, which helps to maintain physiological pH levels. They may also interact with various biological targets depending on their specific structure, influencing metabolic pathways and cellular functions.

Pharmacodynamics

The pharmacodynamics of dibasic compounds is highly variable and depends on their specific chemical structure and the context of their use. Generally, these compounds may alter the absorption and distribution of other drugs, modulate enzyme activity, or affect cellular signaling pathways through their interactions with biological molecules.

Pharmacokinetics

The pharmacokinetics of dibasic compounds can vary widely. Factors such as solubility, stability, and route of administration influence their absorption, distribution, metabolism, and excretion. Typically, dibasic compounds may be absorbed in the gastrointestinal tract and may undergo various metabolic processes depending on their specific nature.

Pregnancy

Dibasic compounds should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Consult with a healthcare provider.

Breast-feeding

Caution is advised when administering dibasic compounds to breastfeeding mothers. Consult with a healthcare provider.

Storage

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

Indications

• Used as an excipient in tablet formulations
• Used as a bulking agent in capsule formulations
• Used in food products as a thickener or stabilizer

Dosage

Children: Refer to specific product guidelines as dosage will depend on the formulation and the active ingredients.

Adults: Refer to specific product guidelines as dosage will depend on the formulation and the active ingredients.

Mechanism of action

Microcrystalline cellulose acts as a non-digestible filler that enhances the flow properties of powders during the manufacturing of tablets and capsules. It does not have a direct pharmacological action on the body but ensures that the active ingredients are effectively delivered to the patient.

Pharmacodynamics

As a non-active ingredient, microcrystalline cellulose does not exert pharmacodynamic effects typical of active pharmaceutical ingredients. Its primary role is to provide a stable and consistent matrix for the drug, facilitating the release of the active compound once ingested.

Pharmacokinetics

Microcrystalline cellulose is not absorbed in the gastrointestinal tract; it passes through the digestive system largely unchanged. It adds bulk to the stool, which may aid in promoting regular bowel movements. The substance is excreted in feces, where it contributes to dietary fiber intake.

Pregnancy

Data regarding the use of microcrystalline cellulose during pregnancy is limited. It is advisable to consult with healthcare professionals before use.

Breast-feeding

Microcrystalline cellulose is considered safe during breastfeeding, as it is not absorbed systemically.

Storage

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

Dosage

Children: Refer to specific drug formulations and product labels as purified substances can vary widely in their use and dosing.

Adults: Refer to specific drug formulations and product labels as purified substances can vary widely in their use and dosing.

Mechanism of action

The mechanism of action for purified compounds varies widely depending on the specific substance. Generally, purified drugs exert their effects by interacting with specific biological targets, such as receptors, enzymes, or ion channels, leading to a desired therapeutic effect. This interaction can involve binding to receptors to activate or inhibit signaling pathways, modulating enzymatic activity, or altering physiological processes.

Pharmacodynamics

Pharmacodynamics describes the effects of a drug on the body and the relationship between drug concentration and effect. For purified drugs, this can involve dose-response relationships and the time course of their action. The purified form often enhances potency and reduces variability in response among patients, which can lead to more predictable therapeutic outcomes. The overall effect is determined by the drug's affinity for its target, the efficacy of the drug-receptor interaction, and the downstream signaling pathways activated as a result of this interaction.

Pharmacokinetics

Pharmacokinetics involves the absorption, distribution, metabolism, and excretion (ADME) of a drug. For purified substances, absorption can be more efficient due to the absence of impurities that may affect solubility or stability. Distribution may also be enhanced, leading to higher bioavailability. Metabolism can be influenced by the structure of the purified compound, as it may be metabolized more readily by liver enzymes. Excretion typically occurs through the kidneys or liver, depending on the molecular characteristics of the purified drug.

Pregnancy

Consult with a healthcare professional, as the safety of purified forms of medications during pregnancy may vary depending on the specific substance.

Breast-feeding

Consult with a healthcare professional, as the safety of purified forms of medications during breastfeeding may vary depending on the specific substance.

Storage

Store in a cool, dry place, away from light and moisture, and keep out of reach of children.

Indications

• Hyperpigmentation
• Melasma
• Post-inflammatory hyperpigmentation
• Dermatitis

Dosage

Children: Refer to specific guidelines based on age and condition; consult the BNF for Children for appropriate dosing.

Adults: Apply a thin layer to the affected area once or twice daily, as directed by a healthcare provider.

Mechanism of action

The precise mechanism of action for pvawhite involves the inhibition of melanin production in melanocytes, the cells responsible for skin pigmentation. It is believed to interfere with the enzymatic activity of tyrosinase, a key enzyme in the melanin biosynthesis pathway. Additionally, pvawhite may possess antioxidant properties that help reduce oxidative stress in the skin, further aiding in the prevention of skin darkening.

Pharmacodynamics

Pvawhite exhibits its pharmacological effects primarily through its action on the skin. It is absorbed locally and works to inhibit melanin synthesis, leading to decreased pigmentation. The anti-inflammatory properties help alleviate symptoms associated with skin conditions such as redness and irritation. Its effectiveness may vary based on the concentration of the active ingredient and the duration of treatment.

Pharmacokinetics

When applied topically, pvawhite demonstrates limited systemic absorption, which minimizes potential systemic side effects. The drug is primarily localized at the site of application, where it exerts its effects. The onset of action can vary, generally appearing within a few weeks of consistent use. The metabolism and excretion pathways for pvawhite are not well established, but local metabolism may occur in the skin tissues.

Pregnancy

Consult a healthcare professional before use. Safety during pregnancy has not been established.

Breast-feeding

Consult a healthcare professional before use. Safety during breastfeeding has not been established.

Storage

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

Dosage

Children: Refer to clinical guidelines or consult a healthcare professional for dosing information.

Adults: Refer to clinical guidelines or consult a healthcare professional for dosing information.

Pregnancy

Safety during pregnancy has not been established. Use only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

Caution is advised when administering during breastfeeding. Monitor for any potential adverse effects in the infant.

Storage

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

Indications

• Type 2 diabetes mellitus as monotherapy (if metformin is inappropriate)
• Type 2 diabetes mellitus in combination with other antidiabetic drugs (including insulin) when metformin alone or in combination fails to achieve adequate glycemic control

Dosage

Adults: 100 mg once daily, or 50 mg twice daily when used in combination with a sulfonylurea or insulin. Dose adjustments may be required based on renal function.

Mechanism of action

Sitagliptin inhibits the enzyme dipeptidyl peptidase-4 (DPP-4), which is responsible for the degradation of incretin hormones. This inhibition results in prolonged active incretin levels, which enhances insulin secretion from pancreatic beta cells and decreases glucagon secretion from alpha cells in the pancreas, leading to lowered blood glucose levels.

Pharmacodynamics

Sitagliptin's pharmacodynamic effects include improved glycemic control, characterized by reduced fasting and postprandial blood glucose levels. The drug is effective in lowering HbA1c levels and is associated with a low risk of hypoglycemia. It has a beneficial effect on weight management, as it typically does not promote weight gain.

Pharmacokinetics

Sitagliptin is absorbed rapidly after oral administration, with peak plasma concentrations occurring within 1-4 hours. Its bioavailability is approximately 87%. The drug is predominantly eliminated via renal excretion, with about 80% of the dose excreted unchanged in the urine. The elimination half-life is approximately 12.4 hours. Renal impairment may necessitate dose adjustments, as clearance is significantly reduced in patients with decreased renal function.

Contra-indications

• History of pancreatitis
• Severe heart failure

Adverse effects

• Headache
• Constipation
• Dizziness
• Skin reactions
• Angioedema
• Back pain
• Cutaneous vasculitis
• Joint disorders
• Myalgia
• Acute pancreatitis
• Acute renal impairment
• Stevens-Johnson syndrome
• Vomiting

Interactions

• Concomitant use with sulfonylureas or insulin may require dose adjustments
• Moderate interaction with vemurafenib (increases exposure)

Precautions

• Monitor renal function before treatment and periodically thereafter
• Discontinue if symptoms of acute pancreatitis occur, such as persistent severe abdominal pain

Pregnancy

Avoid-toxicity observed in animal studies.

Breast-feeding

Avoid-present in milk in animal studies.

Storage

Store at room temperature, away from moisture and heat.

Formulations

• Tablets: 50 mg, 100 mg

Indications

• Dry skin conditions
• Cosmetic formulations
• Emollient in topical creams and lotions
• Emulsifying agent in pharmaceutical preparations

Dosage

Children: For pediatric use, refer to specific product formulations and guidelines, as dosing may vary based on the formulation and concentration.

Adults: Stearyl alcohol is used topically in various formulations. Specific dosing is typically determined by the formulation and intended use, refer to product guidelines for detailed instructions.

Mechanism of action

Stearyl alcohol functions primarily as an emollient and emulsifier. It aids in the formation of stable emulsions by reducing the surface tension between oil and water phases, allowing for the creation of creams and lotions. Its hydrophobic tail interacts with lipids, while the hydroxyl group can form hydrogen bonds with water, enhancing moisture retention in the skin.

Pharmacodynamics

Stearyl alcohol acts by providing a protective barrier on the skin, reducing transepidermal water loss and enhancing hydration. Its emollient properties make it effective in softening and smoothing the skin, which can alleviate dryness and improve the overall appearance of the skin. Additionally, it can enhance the delivery of other active ingredients in topical formulations.

Pharmacokinetics

Stearyl alcohol is not significantly absorbed systemically when applied topically. Its primary action is local to the site of application, where it exerts its emollient effects. The compound is metabolized in the body to various fatty acids and alcohols, and it is excreted primarily through the skin and gastrointestinal tract, with minimal systemic exposure.

Pregnancy

Stearyl is generally considered safe for use during pregnancy; however, specific formulations should be evaluated for their ingredients.

Breast-feeding

Stearyl can be used while breastfeeding, but it's recommended to consult a healthcare provider for specific concerns regarding topical applications.

Storage

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

Formulations

• Cream
• Ointment
• Lotion

Mechanism of action

Inhibition of DPP-4 by sitagliptin slows DPP-4 mediated inactivation of incretins like GLP-1 and GIP. Incretins are released throughout the day and upregulated in response to meals as part of glucose homeostasis. Reduced inhibition of incretins increase insulin synthesis and decrease glucagon release in a manner dependant on glucose concentrations. These effects lead to an overall increase in blood glucose control which is demonstrated by reduced glycosylated hemoglobin (HbA1c). Januvia is a member of a class of oral anti-hyperglycemic agents called dipeptidyl peptidase 4 (DPP-4) inhibitors. The improvement in glycemic control observed with this medicinal product may be mediated by enhancing the levels of active incretin hormones. Incretin hormones, including glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), are released by the intestine throughout the day, and levels are increased in response to a meal. The incretins are part of an endogenous system involved in the physiologic regulation of glucose homeostasis. When blood glucose concentrations are normal or elevated, GLP-1 and GIP increase insulin synthesis and release from pancreatic beta cells by intracellular signaling pathways involving cyclic AMP. Treatment with GLP-1 or with DPP-4 inhibitors in animal models of type 2 diabetes has been demonstrated to improve beta cell responsiveness to glucose and stimulate insulin biosynthesis and release. With higher insulin levels, tissue glucose uptake is enhanced. In addition, GLP-1 lowers glucagon secretion from pancreatic alpha cells. Decreased glucagon concentrations, along with higher insulin levels, lead to reduced hepatic glucose production, resulting in a decrease in blood glucose levels. The effects of GLP-1 and GIP are glucose-dependent such that when blood glucose concentrations are low, stimulation of insulin release and suppression of glucagon secretion by GLP-1 are not observed. For both GLP-1 and GIP, stimulation of insulin release is enhanced as glucose rises above normal concentrations. Further, GLP-1 does not impair the normal glucagon response to hypoglycemia. The activity of GLP-1 and GIP is limited by the DPP-4 enzyme, which rapidly hydrolyzes the incretin hormones to produce inactive products. Sitagliptin prevents the hydrolysis of incretin hormones by DPP-4, thereby increasing plasma concentrations of the active forms of GLP-1 and GIP. By enhancing active incretin levels, sitagliptin increases insulin release and decreases glucagon levels in a glucose-dependent manner. In patients with type 2 diabetes with hyperglycemia, these changes in insulin and glucagon levels lead to lower hemoglobin A1c (HbA1c) and lower fasting and postprandial glucose concentrations. The glucose-dependent mechanism of sitagliptin is distinct from the mechanism of sulfonylureas, which increase insulin secretion even when glucose levels are low and can lead to hypoglycemia in patients with type 2 diabetes and in normal subjects. Sitagliptin is a potent and highly selective inhibitor of the enzyme DPP-4 and does not inhibit the closely-related enzymes DPP-8 or DPP-9 at therapeutic concentrations. Sitagliptin is a DPP-4 inhibitor, which is believed to exert its actions in patients with type 2 diabetes by slowing the inactivation of incretin hormones. Concentrations of the active intact hormones are increased by Januvia, thereby increasing and prolonging the action of these hormones. Incretin hormones, including glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), are released by the intestine throughout the day, and levels are increased in response to a meal. These hormones are rapidly inactivated by the enzyme, DPP-4. The incretins are part of an endogenous system involved in the physiologic regulation of glucose homeostasis. When blood glucose concentrations are normal or elevated, GLP-1 and GIP increase insulin synthesis and release from pancreatic beta cells by

Pharmacodynamics

Sitagliptin inhibits DPP-4 which leads to increased levels of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide(GIP), decreased levels of glucagon, and a stronger insulin response to glucose.