Candez

Indications

• Hypertension
• Heart failure
• Left ventricular dysfunction post-myocardial infarction

Dosage

Children: For children aged 1 to 17 years, the dose is based on body weight. The recommended starting dose is 0.05 to 0.1 mg/kg once daily, with a maximum dose of 0.4 mg/kg or 32 mg, whichever is lower.

Adults: The typical adult starting dose for hypertension is 8 mg once daily, which may be increased to a maximum of 32 mg once daily based on blood pressure response.

Mechanism of action

Candesartan selectively antagonizes the type I angiotensin II receptor (AT1), preventing angiotensin II from exerting its vasoconstrictive and aldosterone-secreting effects. This inhibition allows for vasodilation and decreased aldosterone release, promoting sodium excretion and lowering blood pressure. Candesartan does not affect the degradation of bradykinin, thus minimizing the common side effects associated with ACE inhibitors, such as cough and angioedema.

Pharmacodynamics

Candesartan effectively reduces systemic vascular resistance and lowers blood pressure, which can lead to a decrease in myocardial oxygen demand. Its long duration of action allows for once-daily dosing, and it has shown efficacy in both monotherapy and in combination with other antihypertensive agents. It also demonstrates cardioprotective effects, making it beneficial in the management of heart failure.

Pharmacokinetics

Candesartan is well-absorbed following oral administration, with peak plasma concentrations occurring approximately 1 to 3 hours after dosing. It has a bioavailability of around 15% due to extensive first-pass metabolism. Candesartan is primarily excreted via the kidneys, with a half-life of about 9 hours. The presence of food does not significantly affect its absorption.

Contra-indications

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

Adverse effects

• Dizziness
• Fatigue
• Hypotension
• Hyperkalemia
• Renal impairment
• Angioedema

Interactions

• Other antihypertensive agents may increase the hypotensive effect
• Potassium-sparing diuretics or potassium supplements may increase the risk of hyperkalemia
• Non-steroidal anti-inflammatory drugs (NSAIDs) may reduce the antihypertensive effect and increase the risk of renal impairment

Precautions

• Caution in patients with renal artery stenosis
• Monitor renal function, especially in patients with pre-existing renal impairment
• Caution in patients with aortic stenosis or hypertrophic cardiomyopathy
• Use with caution in patients with a history of angioedema

Pregnancy

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

Breast-feeding

Candesartan is excreted in breast milk, and caution should be exercised when administering to breastfeeding women.

Storage

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

Formulations

• Tablets: 4 mg, 8 mg, 16 mg, 32 mg

Indications

• Hypertension
• Heart failure
• Certain cardiovascular conditions

Dosage

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

Adults: Refer to the BNF for specific dosing information.

Mechanism of action

Cilexetil is converted to its active form, which blocks the action of angiotensin II, a potent vasoconstrictor involved in blood pressure regulation. By inhibiting the angiotensin II receptor, cilexetil promotes vasodilation and decreases peripheral vascular resistance, leading to a reduction in blood pressure.

Pharmacodynamics

Cilexetil's antihypertensive effects are realized through its antagonistic action on the angiotensin II receptors, which results in decreased levels of aldosterone, inhibition of vasoconstriction, and reduced secretion of antidiuretic hormone. The overall pharmacodynamic profile contributes to improved cardiac output and reduced workload on the heart.

Pharmacokinetics

Cilexetil is well-absorbed following oral administration and undergoes extensive first-pass metabolism to its active metabolite. The pharmacokinetic profile indicates a moderate half-life, allowing for once-daily dosing. The distribution of cilexetil is extensive, with high protein binding rates, primarily to serum albumin. Metabolism occurs mainly in the liver, and renal excretion is the primary route for elimination of the drug and its metabolites.

Pregnancy

There is limited data on the use of cilexetil in pregnancy. Caution is advised.

Breast-feeding

It is not known whether cilexetil is excreted in human milk. Caution is recommended.

Storage

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

Indications

• Used as a disintegrant in tablet formulations
• Enhances the bioavailability of active pharmaceutical ingredients

Dosage

Children: Refer to the specific formulation guidelines, as dosage will vary based on the active ingredient and formulation type.

Adults: Refer to the specific formulation guidelines, as dosage will vary based on the active ingredient and formulation type.

Mechanism of action

Croscarmellose sodium works by swelling and absorbing water when it comes into contact with gastrointestinal fluids. This swelling leads to the rapid disintegration of the tablet or capsule matrix, facilitating the release and absorption of the active pharmaceutical ingredients.

Pharmacodynamics

Croscarmellose sodium is classified as a superdisintegrant. Its ability to rapidly disintegrate solid dosage forms can significantly enhance the dissolution rate of the active ingredient, which is crucial for achieving therapeutic effects in a timely manner.

Pharmacokinetics

Croscarmellose sodium is not absorbed in the gastrointestinal tract and does not exert pharmacological effects in the body. It is considered non-toxic and is excreted unchanged. Its main role is as an excipient, influencing the formulation's characteristics rather than the pharmacokinetics of the active ingredients.

Precautions

• Use with caution in patients with known hypersensitivity to croscarmellose or its components.

Pregnancy

Safety in pregnancy has not been established. Use only if clearly needed.

Breast-feeding

Caution is advised when using during breastfeeding, as safety has not been established.

Storage

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

Formulations

• Powder
• 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

Mechanism of action

Oxides do not have a single mechanism of action as they are a broad category of compounds. However, in general, metal oxides can exhibit catalytic properties, while non-metal oxides may participate in biochemical reactions by forming acids or bases upon dissolution in water.

Pharmacodynamics

The pharmacodynamics of oxides depend on the specific type of oxide and its interaction with biological systems. For instance, metal oxides may have antimicrobial properties, while certain non-metal oxides can influence metabolic pathways through their acid-base chemistry. The effects vary widely, necessitating specific studies for each oxide's role in therapeutic contexts.

Pharmacokinetics

The pharmacokinetics of oxides are also variable. Many metal oxides are poorly soluble and thus have limited absorption when ingested. Non-metal oxides, such as carbon dioxide, can be readily absorbed and utilized in metabolic processes. The distribution, metabolism, and excretion of oxides depend on their chemical form and the biological system in which they are involved.

Pregnancy

Not applicable as oxide is not a drug but a class of chemical compounds.

Breast-feeding

Not applicable as oxide is not a drug but a class of chemical compounds.

Storage

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

Indications

• Skin irritation prevention
• Moisture absorption
• Prevention of friction-related skin conditions
• Use in cosmetic formulations

Dosage

Children: Refer to the BNF for Children for specific dosing recommendations, as talcum powder should be used cautiously in children.

Adults: Apply talcum powder as needed to the affected area, ensuring it is applied to clean, dry skin.

Mechanism of action

Talcum works primarily as an absorbent, reducing moisture and friction on the skin. Its fine particle size allows it to coat surfaces effectively, providing a smooth application that helps to prevent irritation and chafing. It does not have a pharmacological mechanism of action like traditional medications but serves a physical purpose in topical formulations.

Pharmacodynamics

Talcum's pharmacodynamics are largely related to its physical properties rather than biochemical effects. By absorbing moisture and reducing friction, talcum helps to maintain skin integrity and prevents conditions such as rashes and irritation. Its inert nature ensures that it does not provoke significant biological responses when applied topically in appropriate amounts.

Pharmacokinetics

Talcum is not absorbed systemically when applied topically. Its pharmacokinetic profile is characterized by local effects at the site of application. When used as a powder, it remains on the skin surface and acts as a barrier without entering the bloodstream. However, inhalation of talcum powder can lead to respiratory issues, as it may cause irritation in the lungs.

Pregnancy

Talcum powder should generally be avoided during pregnancy due to potential risks of inhalation and respiratory complications.

Breast-feeding

Use with caution, as talcum powder may be inhaled by the infant, posing a risk of respiratory issues.

Storage

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

Mechanism of action

Although these agents /angiotensin II receptor antagonists/ are similar to ACE inhibitors in that they decrease the effects of angiotensin II, rather than decreasing the formation of angiotensin II, drugs antagonize angiotensin II at the type I angiotensin receptor. This allows the drugs to inhibit the vasoconstrictive and aldosterone promoting effects of angiotensin II without interfering with bradykinin degradation, significantly reducing the adverse effects of cough and angioedema seen with ACE inhibitor therapy. ... /Angiotensin II receptor antagonists/ Angiotensin II is formed from angiotensin I in a reaction catalyzed by angiotensin-converting enzyme (ACE, kininase II). Angiotensin II is the principal pressor agent of the renin-angiotensin system, with effects that include vasoconstriction, stimulation of synthesis and release of aldosterone, cardiac stimulation, and renal reabsorption of sodium. Candesartan blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor in many tissues, such as vascular smooth muscle and the adrenal gland. Its action is, therefore, independent of the pathways for angiotensin II synthesis. There is also an AT2 receptor found in many tissues, but AT2 is not known to be associated with cardiovascular homeostasis. Candesartan has much greater affinity (>10,000-fold) for the ATI receptor than for the AT2 receptor. Blockade of the renin-angiotensin system with ACE inhibitors, which inhibit the biosynthesis of angiotensin II from angiotensin I, is widely used in the treatment of hypertension. ACE inhibitors also inhibit the degradation of bradykinin, a reaction also catalyzed by ACE. Because candesartan does not inhibit ACE (kininase II), it does not affect the response to bradykinin. Whether this difference has clinical relevance is not yet known. Candesartan does not bind to or block other hormone receptors or ion channels known to be important in cardiovascular regulation. Blockade of the angiotensin II receptor inhibits the negative regulatory feedback of angiotensin II on renin secretion, but the resulting increased plasma renin activity and angiotensin II circulating levels do not overcome the effect of candesartan on blood pressure.