Losar-denk

Indications

• Hypertension
• Chronic heart failure when ACE inhibitors are unsuitable
• Diabetic nephropathy in type 2 diabetes mellitus

Dosage

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

Adults: Initially 50 mg once daily for adults aged 18–75 years, and 25 mg once daily for adults aged 76 years and over. Doses may be increased to 100 mg once daily if necessary.

Mechanism of action

Losartan selectively blocks the binding of angiotensin II to the AT1 receptor, leading to vasodilation, decreased secretion of aldosterone, and reduced blood pressure. This mechanism also contributes to renal protection in diabetic patients by reducing glomerular pressure.

Pharmacodynamics

Losartan exhibits dose-dependent antihypertensive effects, with initial doses often resulting in a reduction of blood pressure within 6 hours. The peak effect is typically reached within 4 to 6 weeks of treatment. Additionally, losartan has a protective effect on renal function in patients with diabetic nephropathy.

Pharmacokinetics

Losartan is well absorbed after oral administration, with a bioavailability of approximately 33%. It is extensively metabolized in the liver to its active metabolite, E3174, which has a longer half-life than losartan itself. The elimination half-life of losartan is around 2 hours, while that of E3174 is approximately 6 to 9 hours. Both losartan and E3174 are primarily excreted in the urine, and renal impairment may affect their clearance.

Contra-indications

• Hypersensitivity to losartan or any of the excipients
• Severe hepatic impairment
• Pregnancy
• Bilateral renal artery stenosis or unilateral renal artery stenosis in a solitary kidney
• History of angioedema

Adverse effects

• Dizziness
• Hypotension
• Hyperkalaemia
• Fatigue
• Postural hypotension
• Abdominal pain
• Nausea
• Diarrhoea
• Headache
• Musculoskeletal pain
• Renal impairment

Interactions

• Other antihypertensive agents may enhance the hypotensive effect
• Potassium supplements or potassium-sparing diuretics may increase the risk of hyperkalaemia
• Non-steroidal anti-inflammatory drugs (NSAIDs) may reduce the antihypertensive effect
• Lithium levels may be increased when taken with losartan

Precautions

• Monitor renal function and electrolytes in patients with renal impairment
• Use with caution in patients with a history of angioedema
• Caution in patients with volume depletion
• Not recommended for use in patients with severe heart failure

Pregnancy

Losartan is contraindicated in pregnancy due to potential harm to the fetus, particularly during the second and third trimesters.

Breast-feeding

It is not known whether losartan is excreted in human milk; caution is advised when administering to breastfeeding women.

Storage

Store at room temperature (15 to 30 degrees Celsius), protected from light and moisture.

Formulations

• Losartan potassium 12.5 mg tablets
• Losartan potassium 25 mg tablets
• Losartan potassium 50 mg tablets
• Losartan potassium 100 mg tablets
• Losartan with hydrochlorothiazide 50 mg/12.5 mg tablets
• Losartan with hydrochlorothiazide 100 mg/12.5 mg tablets

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

• Lactose intolerance
• As a filler or excipient in pharmaceutical formulations

Dosage

Children: Refer to the BNF for Children for specific dosing information based on age and clinical context.

Adults: Refer to the BNF for specific dosing information based on clinical context.

Mechanism of action

Lactose is metabolized in the intestine by the enzyme lactase into its constituent monosaccharides, glucose and galactose. In individuals with lactase deficiency, unabsorbed lactose passes into the colon, where it is fermented by bacteria, leading to gas production and osmotic effects that contribute to diarrhea.

Pharmacodynamics

The pharmacodynamics of lactose are primarily related to its effects on gastrointestinal function. In healthy individuals, lactose is effectively broken down into glucose and galactose, which are absorbed and utilized for energy. In individuals with lactose intolerance, the unabsorbed lactose can cause osmotic diarrhea and colonic fermentation, leading to discomfort and symptoms associated with lactose intolerance.

Pharmacokinetics

Lactose is not absorbed in the gastrointestinal tract until it is hydrolyzed into glucose and galactose by lactase. The absorption of glucose and galactose occurs in the small intestine. The half-life is not applicable as lactose is not typically administered as a medication but is rather ingested as a natural component of food. Its metabolism primarily occurs in the intestine.

Adverse effects

• Bloating
• Diarrhea
• Abdominal pain
• Flatulence

Precautions

• Use with caution in patients with lactose intolerance.
• Consider potential for gastrointestinal upset in sensitive individuals.

Pregnancy

Lactose is generally considered safe for use during pregnancy. However, consult a healthcare professional for individual advice.

Breast-feeding

Lactose is safe to use while breastfeeding, as it is a natural sugar present in breast milk.

Storage

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

Formulations

• Powder
• Granules
• Tablets
• Syrup

Indications

• Hypertension
• Diabetic nephropathy
• Reduction of stroke risk in certain populations

Dosage

Children: For paediatric patients aged 6 years and older, the starting dose is usually 0.7 mg/kg once daily, with a maximum of 50 mg daily. Dosing should be adjusted based on blood pressure response and tolerance.

Adults: The typical adult dose for hypertension is 50 mg once daily, which may be increased to a maximum of 100 mg once daily, depending on response.

Mechanism of action

Losartan reversibly and competitively prevents angiotensin II from binding to the AT1 receptor in various tissues, including vascular smooth muscle and the adrenal gland. By doing so, it causes relaxation of vascular smooth muscle, leading to decreased blood pressure. Losartan's active metabolite is significantly more potent as an AT1 receptor inhibitor and further enhances the drug's efficacy in blocking the vasoconstrictor and aldosterone-secreting effects of angiotensin II.

Pharmacodynamics

Losartan is classified as an angiotensin II receptor blocker that effectively lowers blood pressure and is indicated for diabetic nephropathy. It has a long duration of action, which supports its once-daily administration. Regular monitoring of patients is recommended to assess for hypotension, renal function, and potassium levels, as the drug can affect these parameters.

Pharmacokinetics

Losartan is well absorbed and undergoes extensive first-pass metabolism, resulting in an active metabolite that contributes to its therapeutic effects. The drug is primarily eliminated through the urine and feces. The half-life of losartan and its active metabolite allows for stable plasma concentrations with once-daily dosing, but renal impairment may affect its clearance.

Contra-indications

• Hypersensitivity to losartan or any of its excipients
• Severe hepatic impairment
• Pregnancy

Adverse effects

• Dizziness
• Hypotension
• Hyperkalemia
• Renal impairment
• Fatigue
• Headache
• Diarrhea

Interactions

• Potassium-sparing diuretics may increase the risk of hyperkalemia
• Non-steroidal anti-inflammatory drugs (NSAIDs) may reduce the antihypertensive effect of losartan
• Lithium levels may increase when used concurrently with losartan

Precautions

• Monitor blood pressure regularly
• Assess renal function before and during treatment
• Caution in patients with a history of angioedema
• Use with caution in patients with renal artery stenosis

Pregnancy

Losartan is contraindicated in pregnancy due to potential harm to the fetus.

Breast-feeding

Losartan is excreted in breast milk, caution is advised when administering to nursing mothers.

Storage

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

Formulations

• Tablets: 25 mg, 50 mg, 100 mg

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.

Indications

• Tablet coating
• Granule coating
• Improvement of drug stability
• Taste masking
• Aesthetic enhancement of pharmaceuticals

Dosage

Children: Dosage will depend on the specific formulation and active ingredients of the medication being coated. Refer to the specific product information for guidance.

Adults: Dosage will depend on the specific formulation and active ingredients of the medication being coated. Refer to the specific product information for guidance.

Mechanism of action

Opadry functions primarily as a coating polymer that adheres to the surface of tablets or granules, creating a protective layer. This layer can control the release of the active ingredient and protect it from environmental factors such as moisture and light. The specific composition of Opadry can vary, but it typically includes film-forming agents, plasticizers, and colorants that work together to achieve the desired coating characteristics.

Pharmacodynamics

The pharmacodynamics of Opadry is largely focused on its physical and chemical properties rather than specific biological interactions. The coating alters the dissolution characteristics of the drug, potentially leading to modified release profiles. This can enhance drug bioavailability or control the release rate of the active ingredient, thereby impacting the therapeutic effect.

Pharmacokinetics

As a coating agent, Opadry itself is not absorbed into the systemic circulation and does not have pharmacokinetic properties related to absorption, distribution, metabolism, or excretion of an active pharmaceutical ingredient. Its impact on pharmacokinetics is indirect, as it affects how the active drug is released and absorbed in the gastrointestinal tract.

Pregnancy

Opadry is a film-coating agent, and specific studies on its effects during pregnancy are not well-documented. Generally, it is advisable to use medications cautiously during pregnancy. Consult a healthcare provider for guidance.

Breast-feeding

Limited data are available regarding the safety of Opadry during breastfeeding. It is recommended to consult a healthcare provider before use.

Storage

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

Formulations

• Opadry OY - a coating system for oral solid dosage forms
• Opadry II - a polymer-based coating system for tablet and capsule applications

Indications

• Hypokalemia
• Management of potassium deficiency
• Prevention of arrhythmias in patients on diuretics
• Certain kidney disorders

Dosage

Children: Refer to pediatric dosing guidelines based on specific indications and clinical context.

Adults: Refer to clinical guidelines for specific dosing adjustments based on individual patient needs and conditions.

Mechanism of action

Potassium ions (K+) are involved in many cellular processes, including the generation of action potentials in neurons and muscle cells. They help maintain the resting membrane potential and are essential for the depolarization and repolarization phases of the cardiac action potential. Potassium also plays a role in enzyme function and the regulation of acid-base balance.

Pharmacodynamics

Potassium's primary action is to facilitate normal muscle function, including cardiac and smooth muscle contraction. It is also critical for nerve impulse conduction. Adequate potassium levels are necessary to prevent complications such as arrhythmias, muscle weakness, and paralysis.

Pharmacokinetics

Potassium is absorbed through the gastrointestinal tract, with the majority being absorbed in the small intestine. The distribution of potassium in the body is primarily within cells, with a small amount present in extracellular fluid. The kidneys play a significant role in regulating potassium levels, excreting excess potassium to maintain homeostasis. The half-life of potassium in the body can vary based on dietary intake, renal function, and other factors.

Contra-indications

• Hyperkalemia
• Severe renal impairment
• Adrenal insufficiency

Adverse effects

• Hyperkalemia
• Cardiac arrhythmias
• Muscle weakness
• Nausea
• Diarrhea

Interactions

• Potassium-sparing diuretics (e.g., spironolactone) may increase potassium levels
• ACE inhibitors and ARBs can lead to elevated potassium levels
• Non-steroidal anti-inflammatory drugs (NSAIDs) may reduce renal clearance of potassium

Precautions

• Monitor serum potassium levels in patients with renal impairment
• Use cautiously in patients with heart disease or on digoxin
• Evaluate dietary potassium intake in patients receiving potassium supplementation

Pregnancy

Potassium is generally considered safe during pregnancy, but high doses should be avoided. Monitoring of potassium levels may be necessary.

Breast-feeding

Potassium is excreted in breast milk, but no adverse effects have been reported. Normal dietary intake is typically safe.

Storage

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

Formulations

• Oral tablets
• Oral solution
• Intravenous injection
• Intravenous infusion

Indications

• Used as a binder in tablet formulations
• Serves as a disintegrant to improve drug release
• Acts as a thickening agent in liquid formulations
• Enhances bioavailability of poorly soluble drugs

Dosage

Children: Dosage is dependent on the specific formulation and intended use. Refer to formulation guidelines for appropriate concentrations.

Adults: Dosage is dependent on the specific formulation and intended use. Refer to formulation guidelines for appropriate concentrations.

Mechanism of action

Pregelatinised starch acts primarily as a thickening agent and binder in pharmaceutical formulations. When mixed with water, it swells and forms a gel-like consistency, which helps in the uniform distribution of active ingredients and enhances their release and absorption in the gastrointestinal tract. Its ability to gel enables better disintegration of tablets upon administration, facilitating the dissolution of the drug.

Pharmacodynamics

The pharmacodynamics of pregelatinised starch is closely related to its physical properties as a polymer. Upon contact with water, it hydrates and expands, creating a viscous solution that can improve the release profile of drugs. This can lead to enhanced dissolution rates of poorly soluble compounds, improving their bioavailability. Additionally, it can impact the stability and shelf-life of formulations by providing a protective matrix for active ingredients.

Pharmacokinetics

Pregelatinised starch is not absorbed systemically as it primarily acts as an excipient. It undergoes gastrointestinal transit without significant degradation. Its function is to facilitate the release and absorption of the active pharmaceutical ingredients in the formulation rather than exhibiting pharmacokinetic properties of its own.

Pregnancy

Pregelatinised starch is generally considered safe for use during pregnancy, but it is recommended to consult a healthcare provider before use.

Breast-feeding

Pregelatinised starch is considered safe during breastfeeding, but it is advisable to seek medical advice.

Storage

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

Formulations

• Powder
• Capsules
• Tablets

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

• Nutritional supplementation
• Energy source in enteral nutrition
• Excipient in pharmaceutical formulations

Dosage

Children: Refer to specific guidelines or product inserts for dosing information, as it can vary based on the context of use.

Adults: Refer to specific guidelines or product inserts for dosing information, as it can vary based on the context of use.

Mechanism of action

Starch is broken down into glucose units by enzymes such as amylase during digestion. The glucose is then absorbed in the intestines and utilized for energy production in the body's cells. This pathway involves hydrolysis of the glycosidic bonds, converting starch into simpler sugars.

Pharmacodynamics

Starch primarily serves as an energy source. Its digestion and absorption lead to an increase in blood glucose levels, which provides energy for metabolic processes. In this context, it plays a crucial role in maintaining energy homeostasis in the body.

Pharmacokinetics

Starch is not absorbed in its polymeric form; it must first be enzymatically hydrolyzed into simpler sugars such as maltose and glucose. The digestion and absorption of starch occur predominantly in the small intestine, with glucose being readily absorbed into the bloodstream. The rate of absorption can vary depending on the type of starch and its physical form.

Adverse effects

• Allergic reactions
• Gastrointestinal discomfort
• Diarrhea
• Constipation

Precautions

• Use with caution in individuals with known allergies to starch or starch derivatives
• Monitor for gastrointestinal symptoms in patients with a history of digestive disorders

Pregnancy

Starch is generally considered safe for use during pregnancy. However, it should be consumed in moderation as part of a balanced diet.

Breast-feeding

Starch is deemed safe for nursing mothers when used in moderation as part of a balanced diet.

Storage

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

Formulations

• Powder
• Granules
• Tablets
• Suspensions

Dosage

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

Adults: Refer to the specific BNF guidelines for dosing information as it may vary based on the condition being treated.

Mechanism of action

The mechanism of action for White involves its interaction with specific biological pathways, leading to the desired pharmacological effects. The precise pathways may include modulation of receptor activity or alteration of enzyme function, although specific details are not provided.

Pharmacodynamics

Pharmacodynamics of White includes its effects on the body, including therapeutic effects and potential side effects. As a compound, it may exert its influence on multiple physiological systems, which can lead to changes in symptoms or disease progression.

Pharmacokinetics

Pharmacokinetics of White involves its absorption, distribution, metabolism, and excretion. Understanding these parameters can help predict how the drug behaves in the body, including onset of action and duration of effect. Detailed pharmacokinetic data is not specified.

Mechanism of action

Losartan reversibly and competitively prevents angiotensin II binding to the AT₁ receptor in tissues like vascular smooth muscle and the adrenal gland. Losartan and its active metabolite bind the AT₁ receptor with 1000 times more affinity than they bind to the AT₂ receptor. The active metabolite of losartan is 10-40 times more potent by weight than unmetabolized losartan as an inhibitor of AT₁ and is a non-competitive inhibitor. Losartan's prevention of angiotensin II binding causes vascular smooth muscle relaxation, lowering blood pressure. Angiotensin II would otherwise bind to the AT₁ receptor and induce vasoconstriction, raising blood pressure. Angiotensin II (formed from angiotensin I in a reaction catalyzed by angiotensin converting enzyme (ACE, kininase II)), is a potent vasoconstrictor, the primary vasoactive hormone of the renin-angiotensin system and an important component in the pathophysiology of hypertension. It also stimulates aldosterone secretion by the adrenal cortex. Losartan and its principal active metabolite block the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor found in many tissues, (e.g., vascular smooth muscle, adrenal gland). There is also an AT2 receptor found in many tissues but it is not known to be associated with cardiovascular homeostasis. Both losartan and its principal active metabolite do not exhibit any partial agonist activity at the AT1 receptor and have much greater affinity (about 1000-fold) for the AT1 receptor than for the AT2 receptor. In vitro binding studies indicate that losartan is a reversible, competitive inhibitor of the AT1 receptor. The active metabolite is 10 to 40 times more potent by weight than losartan and appears to be a reversible, non-competitive inhibitor of the AT1 receptor. Neither losartan nor its active metabolite inhibits ACE (kininase II, the enzyme that converts angiotensin I to angiotensin II and degrades bradykinin); nor do they bind to or block other hormone receptors or ion channels known to be important in cardiovascular regulation. We investigated the effects of angiotensin II (Ang II) type 1 receptor blockade with losartan on the renin-angiotensin-aldosterone system in hypertensive patients (supine diastolic blood pressure, 95 to 110 mm Hg). Qualifying patients (n = 51) were allocated to placebo, 25 or 100 mg losartan, or 20 mg enalapril. Blood pressure, plasma drug concentrations, and renin-angiotensin-aldosterone system mediators were measured on 4 inpatient days: end of placebo run-in, after first dose, and 2 and 6 weeks of treatment. Plasma drug concentrations were similar after the first and last doses of losartan. At 6 weeks, 100 mg losartan and 20 mg enalapril showed comparable antihypertensive activity. Four hours after dosing, compared with the run-in day, 100 mg losartan increased plasma renin activity 1.7-fold and Ang II 2.5-fold, whereas enalapril increased plasma renin activity 2.8-fold and decreased Ang II 77%. Both drugs decreased plasma aldosterone concentration. For losartan, plasma renin activity and Ang II increases were greater at 2 than at 6 weeks. Effects of losartan were dose related. After the last dose of losartan, plasma renin activity and Ang II changes were similar to placebo changes by 36 hours. These results indicate that long-term blockade of the feedback Ang II receptor in hypertensive patients produces modest increases of plasma renin activity and Ang II that do not appear to affect the antihypertensive response to the antagonist. /Salt not specified/ IL-1beta is a potent proinflammatory, pro-fibrogenetic and pro-athrosclerosis cytokine which has been shown to play an important role in an expanding number of noninfectious, chronic inflammatory conditions including cardiovascular disease, renal fibrosis, rheumatoid arthritis and even type 2 diabetes. Losartan is an angiot

Pharmacodynamics

Losartan is an angiotensin II receptor blocker used to treat hypertension, diabetic nephropathy, and to reduce the risk of stroke. Losartan has a long duration of action as it is given once daily. Patients taking losartan should be regularly monitored for hypotension, renal function, and potassium levels.