Lumerax 80/480 tablets
Artemether 80 mg,Colloidal anhydrous silica 16.800 mg,Croscarmellose Sodium 67.200 mg,Croscarmellose Sodium 78.400 mg,Hypromellose 16.800 mg,Lactose Anhydrous 159.360 mg,Lactose Anhydrous 60.040 mg,Lumefantrine 480 mg,Magnesium Stearate 16.800 mg,Polysorbate 80 3.00 mg,Purified Talc. 4.800 mg
What it does
Artemether is a medication used to treat malaria, a serious illness caused by parasites.
Commonly used for: malaria
Read more in plain English ↓Plain-language summary for general understanding - not medical advice. Always follow your pharmacist/doctor.
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Sourcing - Kenya onlyRegistration & product details
Source: Zambia Medicines Regulatory Authority · fetched 2026-03-12 00:06:34 · updated 2026-05-22 02:46:07
Drug Interactions
5Pharmacodynamic Warnings
Artemether appears in TABLE 9: Drugs that prolong the QT interval
Severe (2)
Artemether - decreases exposure
Mitotane is predicted to decrease the exposure to antimalarials (artemether) with lumefantrine. Avoid.
Artemether - decreases exposure
Rifampicin is predicted to decrease the exposure to antimalarials (artemether) with lumefantrine. Avoid.
Unknown (3)
Artemether - increases exposure
Grapefruit juice increases the exposure to artemether.
Artemether - decreases concentration
Efavirenz decreases the concentration of antimalarials (artemether). Also see TABLE 9 p. 1519
Artemether - decreases exposure
Etravirine decreases the exposure to antimalarials (artemether).
Data from BNF 85 (British National Formulary). This is not a substitute for professional medical advice. Matched via: exact
About artemether
Artemether is a medication used to treat malaria, a serious illness caused by parasites.
What it treats
- malaria
How it works
Artemether works by attacking and killing the parasites that cause malaria in the blood.
Who it's for
Artemether is for people diagnosed with malaria.
Cautions
- • Avoid using with other drugs that can affect heart rhythm.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
About colloidal
Colloidal solutions are often used in various medical treatments and can help improve the delivery of certain medications.
What it treats
- supporting hydration
- helping with nutrient absorption
- improving medication effectiveness
How it works
Colloidal solutions contain small particles that can help carry and deliver substances in the body more effectively.
Who it's for
Adults and children who need assistance with hydration or nutrient delivery.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
About croscarmellose
Croscarmellose is a substance used in medicines to help them dissolve and be absorbed in the body.
What it treats
- helps improve the effectiveness of oral medications
How it works
It works by breaking down the medicine so that it can be easily absorbed in the stomach and intestines.
Who it's for
It is used in various oral medicines that require better absorption.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
About hypromellose
Hypromellose is a substance that helps to keep the eyes moist and can be used to soothe irritation.
What it treats
- dry eyes (keratoconjunctivitis sicca)
- eye irritation
How it works
It forms a protective layer over the eye, which helps to retain moisture and relieve discomfort.
Who it's for
This medication is suitable for anyone experiencing dry or irritated eyes.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
About lactose
Lactose is a sugar found in milk and dairy products. It is often used as an excipient in medications.
What it treats
- lactose intolerance
- as a filler in tablets and capsules
How it works
Lactose helps improve the texture and stability of medications and is sometimes used as a sweetener.
Who it's for
Individuals who require lactose as part of their medication or those who consume dairy products.
Cautions
- • May cause digestive issues in people with lactose intolerance.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
About lumefantrine
Lumefantrine is a medicine used to treat malaria, a serious disease caused by parasites transmitted through mosquito bites.
What it treats
- malaria
- malaria caused by Plasmodium falciparum
How it works
Lumefantrine works by killing the malaria parasites in the blood, helping to clear the infection.
Who it's for
It is for people diagnosed with malaria, particularly those with the type caused by Plasmodium falciparum.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
About polysorbate
Polysorbate is a substance often used as an emulsifier, helping to mix ingredients that usually don't blend well together in medications and food products.
What it treats
- used in various medications and food products to stabilize mixtures
How it works
It helps to keep ingredients mixed evenly, preventing separation and improving texture.
Who it's for
Suitable for individuals who need products containing polysorbate for various health or dietary reasons.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
About purified
Purified ingredients are often used in various medicines to ensure safety and effectiveness by removing impurities.
What it treats
- various medical conditions
How it works
Purified ingredients help in delivering the intended effects of the medicine without the risk of contaminants.
Who it's for
People who need medications with safe and effective ingredients.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
About silica
Silica is a natural substance that can be found in various forms and is often used to help with digestion and absorb excess moisture.
What it treats
- digestive issues
- absorption of moisture
How it works
Silica helps improve digestion by supporting the body's ability to break down food and absorb nutrients.
Who it's for
Silica may be suitable for adults experiencing digestive discomfort or needing help with moisture control.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
About talc
Talc is a mineral used primarily to absorb moisture and reduce friction. It is commonly found in various personal care products.
What it treats
- skin irritation
- diaper rash
- chafing
- sweating
How it works
Talc works by absorbing moisture and providing a smooth surface, which helps to prevent irritation and discomfort on the skin.
Who it's for
Talc is suitable for anyone needing relief from moisture-related skin issues, including babies and adults.
Cautions
- • Avoid using on broken or irritated skin.
- • Keep away from the eyes and mouth.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
Clinical monograph: Hypromellose
BNF-referencedHypromellose is a semisynthetic polymer derived from cellulose, primarily used as an ocular lubricant in the management of dry eye conditions. It acts by forming a protective layer over the eye surface, providing moisture and relief from irritation, thereby improving comfort and protecting the corneal epithelium.
Indications
- Dry eye conditions
- Tear deficiency
- Keratoconjunctivitis sicca
Dosage
Children: Apply as required, typically in the form of eye drops.
Adults: Apply as required, typically in the form of eye drops.
Mechanism of action
Hypromellose acts by forming a viscous gel upon contact with the ocular surface, which helps to retain moisture and protect against irritants. This gel-like property enhances the stability of the tear film and reduces evaporation, thereby alleviating symptoms associated with dry eye conditions.
Pharmacodynamics
The pharmacodynamic effects of hypromellose are primarily related to its ability to mimic natural tears, providing lubrication to the ocular surface. This lubrication reduces friction during blinking and maintains corneal hydration, which is critical for ocular comfort and health. Its high viscosity also contributes to prolonged retention time on the eye surface.
Pharmacokinetics
Hypromellose is administered topically as eye drops and is not significantly absorbed systemically. The retention time of hypromellose on the ocular surface is enhanced due to its viscosity, allowing for extended relief of dry eye symptoms. The elimination of hypromellose occurs primarily through drainage from the eye and dilution by the natural tear fluid.
Adverse effects
- Temporary visual disturbance
- Eye irritation
Precautions
- Should not be used during contact lens wear
- Use with caution in patients with known hypersensitivity to any component of the formulation
Pregnancy
Hypromellose is generally considered safe for use during pregnancy. However, it should be used only if clearly needed and after consulting a healthcare provider.
Breast-feeding
Hypromellose is unlikely to affect breastfed infants when used as directed, but consultation with a healthcare provider is advisable.
Storage
Store in a cool, dry place away from direct sunlight. Once opened, use within a specified period as indicated on the packaging.
Formulations
- {'name': 'Teardew', 'concentration': '0.3%', 'form': 'eye drops', 'volume': '10 ml'}
- {'name': 'Xailin Hydrate', 'concentration': '0.3%', 'form': 'eye drops', 'volume': '10 ml'}
- {'name': 'AacuLose', 'concentration': '0.3%', 'form': 'eye drops', 'volume': '10 ml'}
- {'name': 'Artelac', 'concentration': '0.32%', 'form': 'eye drops', 'volume': '10 ml'}
- {'name': 'Lacrilube', 'concentration': '2 mg/g', 'form': 'eye ointment', 'volume': '3.5 g'}
- {'name': 'Celluvisc', 'concentration': '1%', 'form': 'eye drops', 'volume': '0.4 ml unit dose'}
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.
Clinical monograph: artemether
BNF-referencedArtemether is an antimalarial drug derived from artemisinin, an extract from the herb Artemisia annua L. It is primarily used for the treatment of uncomplicated malaria, particularly caused by Plasmodium falciparum. Artemether acts as a schizontocide, effectively reducing the number of malarial parasites in the bloodstream. It is often administered in combination with lumefantrine to enhance therapeutic efficacy and improve clinical outcomes.
Indications
- Uncomplicated malaria caused by Plasmodium falciparum
- Malaria treatment in combination with lumefantrine
Dosage
Children: Refer to the BNF for Children for appropriate dosing information.
Adults: Refer to specific guidelines; typically, artemether is administered in a combination therapy regimen with lumefantrine.
Mechanism of action
Artemether interacts with ferriprotoporphyrin IX (heme) in the acidic vacuole of malaria parasites, leading to the generation of cytotoxic radical species. This interaction involves the activation of the drug by reduced heme or ferrous iron, resulting in the formation of oxygen-centered radicals that subsequently convert into carbon-centered radicals. These radicals are toxic to the parasites, thereby inhibiting their growth and reproduction.
Pharmacodynamics
Artemether is rapidly metabolized to its active metabolite, dihydroartemisinin. It primarily targets the erythrocytic stages of Plasmodium falciparum by inhibiting nucleic acid and protein synthesis. The drug has a rapid onset of action, providing quick symptomatic relief by significantly reducing the number of circulating malarial parasites. In combination therapy with lumefantrine, artemether enhances overall treatment effectiveness and contributes to a higher clinical cure rate.
Pharmacokinetics
Artemether is absorbed quickly, with a rapid onset of action. It is metabolized in the liver to dihydroartemisinin, which is the active form responsible for its antimalarial effects. The drug is eliminated from the body relatively quickly, while lumefantrine, which has a longer half-life, aids in clearing any residual parasites. This pharmacokinetic profile supports the use of artemether in combination therapies for malaria.
Adverse effects
- nausea
- vomiting
- dizziness
- headache
- fatigue
- abdominal pain
- anemia
- QT prolongation
Interactions
- mitotane+artemether with lumefantrine: Severe (decreases exposure)
- mitotane+artemether: Severe (decreases exposure)
- rifampicin+artemether: Severe (decreases exposure)
- grapefruit juice+artemether: Unknown (increases exposure)
- efavirenz+artemether: Unknown (decreases concentration)
- etravirine+artemether: Unknown (decreases exposure)
Precautions
- Monitor for signs of hypersensitivity reactions
- Use with caution in patients with pre-existing QT prolongation
- Assess liver function before use, as hepatic impairment may alter drug metabolism
Pregnancy
Artemether is categorized as pregnancy category C. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Breast-feeding
Artemether is excreted in breast milk. Caution should be exercised when administering to nursing mothers.
Storage
Store at room temperature, away from moisture and heat. Protect from light.
Formulations
- artemether/lumefantrine combination tablets
- artemether oral solution
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.
Clinical monograph: colloidal
Colloidal solutions are mixtures in which small particles are dispersed throughout a continuous medium. They can be used in various medical applications, including as intravenous fluids for volume expansion and as drug delivery systems. Colloidal solutions can improve the solubility and stability of drugs, enhancing their therapeutic effects.
Indications
- Hypovolemic shock
- Severe burns
- Postoperative fluid replacement
- Sepsis
- Trauma management
Dosage
Children: Refer to established guidelines for specific dosing, as it varies based on the type of colloidal solution used and the clinical condition being treated.
Adults: Refer to established guidelines for specific dosing, as it varies based on the type of colloidal solution used and the clinical condition being treated.
Mechanism of action
Colloidal solutions work by maintaining oncotic pressure in the blood, thus helping to retain fluid within the vascular system. This is primarily due to the large molecular weight of the colloidal particles, which cannot easily pass through capillary walls. The presence of colloids in the blood helps to draw water into the circulation, increasing blood volume and improving tissue perfusion.
Pharmacodynamics
The pharmacodynamics of colloidal solutions are centered on their ability to exert osmotic pressure, which helps maintain blood volume and pressure. This effect is particularly important in conditions such as hypovolemia and shock, where fluid replacement is necessary to restore hemodynamic stability. The efficacy of colloidal solutions can vary depending on the type of colloid used, as well as the underlying clinical condition being treated.
Pharmacokinetics
Colloidal solutions are typically administered intravenously and their pharmacokinetics can vary based on the specific formulation. Generally, colloids are distributed throughout the vascular compartment and have a longer duration of action compared to crystalloids, as they remain in circulation longer. The elimination of colloids is primarily through the reticuloendothelial system, where they are metabolized or eliminated by the liver and spleen. Factors such as particle size and composition can influence their distribution and clearance.
Adverse effects
- Allergic reactions
- Injection site reactions
- Nausea
- Vomiting
- Headache
- Fever
Precautions
- Use with caution in patients with known allergies to any component of the formulation
- Monitor for signs of hypersensitivity during administration
- Consider volume overload in patients with cardiac or renal impairment
Pregnancy
The safety of colloidal solutions during pregnancy has not been established. Use only if the potential benefit justifies the potential risk to the fetus.
Breast-feeding
It is not known whether colloidal solutions are excreted in human milk. Caution should be exercised when administering to breastfeeding mothers.
Storage
Store at room temperature, protect from light, and do not freeze. Keep out of reach of children.
Formulations
- Colloidal silver
- Colloidal gold
- Colloidal iron
- Other metal colloids
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.
Clinical monograph: croscarmellose
Croscarmellose sodium is a pharmaceutical excipient widely used as a disintegrant in oral dosage forms. It enhances the dissolution of active pharmaceutical ingredients by promoting rapid disintegration of tablets and capsules upon contact with moisture. This characteristic makes it essential in improving the bioavailability of various medications.
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
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.
Clinical monograph: lactose
BNF-referencedLactose is a disaccharide sugar composed of galactose and glucose, primarily found in milk and dairy products. It serves as a source of energy and is metabolized by the enzyme lactase. In individuals with lactase deficiency, lactose can lead to gastrointestinal symptoms such as bloating, diarrhea, and abdominal pain.
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
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.
Clinical monograph: lumefantrine
BNF-referencedLumefantrine is an antimalarial agent that is primarily used in combination with artemether for the treatment of uncomplicated malaria caused by Plasmodium falciparum. It exhibits a blood schizonticidal effect and is particularly effective against the erythrocytic stages of the malaria parasite.
Indications
- Uncomplicated malaria due to Plasmodium falciparum
- Coartem (lumefantrine and artemether) for rapid malaria treatment
Dosage
Children: Refer to the BNF for Children for specific dosing guidelines.
Adults: Refer to the BNF for specific dosing guidelines.
Mechanism of action
The exact mechanism by which lumefantrine exerts its antimalarial effect is unknown. However, it is suggested that lumefantrine inhibits the formation of beta-hematin by forming a complex with hemin and inhibits nucleic acid and protein synthesis.
Pharmacodynamics
Lumefantrine is active against the erythrocytic stages of Plasmodium falciparum. When administered with artemether, it is believed to have cooperative antimalarial effects, with artemether providing rapid symptom relief and lumefantrine clearing residual parasites due to its longer half-life.
Pharmacokinetics
Lumefantrine has a long half-life, allowing for sustained effects after administration. It is absorbed from the gastrointestinal tract and is extensively metabolized in the liver. Its pharmacokinetic profile supports its use in combination therapy with rapidly acting agents like artemether.
Adverse effects
- Nausea
- Vomiting
- Diarrhea
- Abdominal pain
- Headache
- Fatigue
- Dizziness
- Palpitations
Interactions
- Drug interactions with artemether; co-administration may enhance antimalarial effects
- Potential interactions with drugs that affect liver enzymes, which may alter lumefantrine metabolism
Precautions
- Use with caution in patients with a history of cardiac arrhythmias
- Monitor for signs of hepatotoxicity in patients with pre-existing liver disease
- Consider potential for drug interactions in patients receiving multiple medications
Pregnancy
Lumefantrine should only be used in pregnancy if clearly needed; consult guidelines for specific considerations.
Breast-feeding
Use with caution while breastfeeding; consult healthcare provider for recommendations.
Storage
Store in a cool, dry place away from direct sunlight. Keep out of reach of children.
Formulations
- Tablets
- Oral suspension
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.
Clinical monograph: polysorbate
Polysorbate is a non-ionic surfactant and emulsifier used in various pharmaceutical formulations. It is derived from sorbitol and fatty acids and is known for its capacity to enhance the solubility of hydrophobic compounds in aqueous solutions. Polysorbate is commonly utilized in the preparation of oral, parenteral, and topical pharmaceutical products, as well as in food and cosmetic industries.
Indications
- Emulsifying agent in drug formulations
- Stabilizer for parenteral preparations
- Solubilizer for hydrophobic drug compounds
- Ingredient in topical formulations
Dosage
Children: Refer to specific product guidelines, as dosing varies based on formulation and intended use.
Adults: Refer to specific product guidelines, as dosing varies based on formulation and intended use.
Mechanism of action
Polysorbate functions primarily as an emulsifying agent. It reduces the surface tension between immiscible liquids, allowing them to mix more easily. This property is particularly useful in stabilizing emulsions and suspensions, facilitating the delivery of active pharmaceutical ingredients in various formulations.
Pharmacodynamics
Polysorbate does not exert pharmacological effects in the traditional sense, as it does not bind to specific receptors to elicit a physiological response. Instead, it plays a crucial role in modifying the physical properties of drug formulations, thereby enhancing drug delivery and absorption. Its ability to solubilize drugs enhances their bioavailability, particularly for poorly soluble compounds.
Pharmacokinetics
Polysorbate is generally considered to be non-toxic and is not absorbed to a significant extent when administered orally. It is metabolized by the liver and excreted primarily through the gastrointestinal tract. The pharmacokinetic profile may vary depending on the route of administration and the specific formulation in which it is used.
Adverse effects
- Allergic reactions
- Skin irritation
- Gastrointestinal disturbances
Precautions
- Use cautiously in patients with known allergies to polysorbates or related compounds
- Monitor for allergic reactions in susceptible individuals
Pregnancy
Polysorbate is generally considered safe for use during pregnancy, but consult with a healthcare provider for specific cases.
Breast-feeding
Polysorbate is considered safe during breastfeeding, but consult with a healthcare provider for individual advice.
Storage
Store at room temperature, away from direct sunlight and moisture.
Formulations
- Polysorbate 20
- Polysorbate 80
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.
Clinical monograph: purified
Purified refers to a substance that has been processed to remove impurities, contaminants, or unwanted substances, resulting in a more concentrated and effective form of the original compound. In pharmacology, purified compounds are often used to enhance therapeutic efficacy and reduce adverse effects. The purification process can apply to a variety of substances, including drugs, biological products, and chemical compounds.
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.
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.
Clinical monograph: silica
BNF-referencedSilica, primarily in the form of silicon dioxide (SiO2), is a naturally occurring mineral found in various forms, including crystalline and amorphous structures. It is widely used in various industries, including construction, manufacturing, and as a food additive. Silica is known for its high melting point and chemical stability. In clinical contexts, exposure to crystalline silica has been linked to respiratory diseases such as silicosis and lung cancer due to its cytotoxic effects on lung cells. The different forms of silica exhibit varying degrees of biological activity, with crystalline silica being more hazardous than amorphous types.
Indications
- Silicosis
- Chronic obstructive pulmonary disease (COPD)
- Lung cancer associated with silica exposure
Dosage
Adults: Silica is not administered as a drug, but rather
Mechanism of action
Silica, particularly crystalline forms like quartz and cristobalite, can induce cytotoxicity and morphological transformation in cells. The cytotoxic effects are attributed to the presence of silanol groups and trace iron on the silica surface, which can generate reactive oxygen species. These interactions lead to cellular damage and transformation, suggesting multiple molecular mechanisms underlying silica's biological effects. The activity is sensitive to the silica's surface structure and composition, indicating that the biological response is a phenomenon originating from the silica's surface characteristics.
Pharmacodynamics
Silica's pharmacodynamic effects are largely related to its cytotoxic and transforming properties, particularly in lung tissue. The inhalation of crystalline silica can lead to the activation of inflammatory pathways, oxidative stress, and apoptosis in alveolar macrophages and epithelial cells. This can result in chronic inflammation, fibrosis, and ultimately, diseases such as silicosis and lung cancer. The degree of these effects varies based on the type of silica, its crystalline structure, and the presence of surface modifications.
Pharmacokinetics
The pharmacokinetics of silica is complex as it is not absorbed systemically when inhaled or ingested. Instead, inhaled silica particles can deposit in the alveolar region of the lungs, where they may persist for long periods. The body responds to silica exposure through inflammatory processes, and macrophages attempt to phagocytize silica particles. However, the persistence of these particles can lead to chronic lung conditions. Clearance mechanisms are inefficient, leading to prolonged retention in lung tissue.
Adverse effects
- Cytotoxicity
- Morphological transformation of cells
- Respiratory issues
- Silicosis
- Lung cancer
Precautions
- Use caution in occupational settings with silica dust exposure
- Regular monitoring of lung function in exposed individuals
Pregnancy
There is insufficient data on the effects of silica on pregnancy. It is advised to minimize exposure.
Breast-feeding
Limited data available; caution is advised due to potential respiratory effects.
Storage
Store in a cool, dry place, away from moisture and incompatible materials.
Formulations
- Crystalline silica
- Amorphous silica (diatomaceous earth)
- Silica gel
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.
Clinical monograph: talc
BNF-referencedTalc is a mineral composed of magnesium, silicon, and oxygen, commonly used in various pharmaceutical applications due to its excellent absorptive properties. It is often employed as an excipient in drug formulations and as a bulking agent in tablets and powders. Talc is also utilized in some medical procedures, such as pleurodesis, to prevent the recurrence of pleural effusions.
Indications
- Used as an excipient in drug formulations
- Pleurodesis for the management of recurrent pleural effusions
Dosage
Children: Refer to specific guidelines for paediatric use, as dosing may differ based on age and clinical condition.
Adults: Refer to specific guidelines for the appropriate dosage in pleurodesis and other applications, as it may vary based on clinical context.
Mechanism of action
Talc exhibits very good absorptive properties, allowing it to absorb moisture and other substances effectively. This characteristic is particularly useful in pharmaceutical formulations, where it may enhance the stability and texture of the drug product.
Pharmacodynamics
Talc's primary pharmacodynamic effect is its ability to act as an inert filler and bulking agent in pharmaceutical preparations. It does not have any intrinsic pharmacological activity but serves to improve the physical properties of formulations, such as flowability and compressibility.
Pharmacokinetics
Talc is not absorbed systemically when used as an excipient or in medical procedures. Its effects are local, and it remains in the site of application, where it functions primarily as a mechanical agent. The pharmacokinetics of talc in the context of its use in pleurodesis involves its ability to promote adhesion of the pleural surfaces, thereby preventing fluid accumulation.
Pregnancy
Talc is classified as a substance with minimal systemic absorption, but safety during pregnancy has not been well established. Consult relevant guidelines.
Breast-feeding
Talc is not expected to be absorbed in significant amounts; however, caution is advised and consult guidelines.
Storage
Store in a cool, dry place, away from direct sunlight.
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.
Molecular reference: artemether
PubChem CID 68911Molecular formula: C16H26O5
Mechanism of action
Involves an interaction with ferriprotoporphyrin IX (“heme”), or ferrous ions, in the acidic parasite food vacuole, which results in the generation of cytotoxic radical species. The generally accepted mechanism of action of peroxide antimalarials involves interaction of the peroxide-containing drug with heme, a hemoglobin degradation byproduct, derived from proteolysis of hemoglobin. This interaction is believed to result in the formation of a range of potentially toxic oxygen and carbon-centered radicals. Artemether (AM) is an antimalarial drug derived from artemisinin (Qinghaosu), an extract of the herb Artemisia annua L., sweet wormwood. Its antiparasitic effect is that of a schizontocide and is explained by rapid uptake by parasitized erythrocytes and interaction with a component of hemoglobin degradation resulting in formation of free radicals. It has been shown to exhibit a high clinical cure rate. Two theories have been put forward for the mode of antimalarial action of the artemisinin antimalarials, in accodance with the known properties of peroxides with medicinal activity. The first assumes that the artemisinins must be activated by contact with either reduced haem (ferrous haem, Fe(ll)PPIX) or non-haem ferrous iron (exogenous iron), causing cleavage of the peroxide to generate oxygen-centered radicals (alkoxy radicals') which are then presumed to be converted into carbon-centered radicals by transfer of proximate hydrogen atoms from the periphery of the peroxide molecule. These carbon-centered radicals are then thought to alkylate sensitive, yet unspecified, biomolecules in the parasite. A second theory argues for a process in which the intact artemisinin binds to a site within a vital protein in the parasite. The act of binding causes the peroxide to be converted to hydroperoxide or similar open peroxide, which in accordance with known properties of such compounds, generates one or more active chemical entities, either oxidizing agents or oxygen transfer agents per se, or oxygen-centered free radicals. This would be associated with the binding process. In such a way, the artemisinins might act as (irreversibile) inhibitors. Iron may, or may not, be associated with the activation process. No specific biological target in the parasite has yet been identified in support of this theory, but it may be membrane-bound proteins. A 2025 systematic review notes Artemether's pharmacological activity is antimalarial.
Pharmacodynamics
In the body, artemether is metabolized into the active metabolite metabolite dihydroartemisinin. The drug works against the erythrocytic stages of <i>P. falciparum</i> by inhibiting nucleic acid and protein synthesis. Artemether is administered in combination with lumefantrine for improved efficacy. Artemether has a rapid onset of action and is rapidly cleared from the body. It is thought that artemether provides rapid symptomatic relief by reducing the number of malarial parasites. Lumefantrine has a much longer half life and is believed to clear residual parasites.
Biological pathways
Source: PubChem (NCBI) · pathways from PathBank, Reactome, WikiPathways & PharmGKB.
Molecular reference: lactose
PubChem CID 6134Molecular formula: C12H22O11
Source: PubChem (NCBI) · pathways from PathBank, Reactome, WikiPathways & PharmGKB.
Molecular reference: lumefantrine
PubChem CID 6437380Molecular formula: C30H32Cl3NO
Mechanism of action
The exact mechanism by which lumefantrine exerts its antimalarial effect is unknown. However, available data suggest that lumefantrine inhibits the formation of β-hematin by forming a complex with hemin and inhibits nucleic acid and protein synthesis.
Pharmacodynamics
Lumefantrine is a blood schizonticide active against erythrocytic stages of <i>Plasmodium falciparum</i>. It is thought that administration of lumefantrine with artemether results in cooperate antimalarial clearing effects. Artemether has a rapid onset of action and is rapidly cleared from the body. It is thus thought to provide rapid symptomatic relief by reducing the number of malarial parasites. Lumefantrine has a much longer half life and is believed to clear residual parasites.
Source: PubChem (NCBI) · pathways from PathBank, Reactome, WikiPathways & PharmGKB.
Molecular reference: silica
PubChem CID 24261Molecular formula: O2Si
Mechanism of action
...Some quartz and cristobalite dusts (crystalline) as well as the diatomaceous earths (amorphous), but not the pyrogenic amorphous silica, were cytotoxic and induced morphological transformation of SHE cells in a concentration-dependent manner. The ranking in cytotoxicity was different from that in transforming potency, suggesting two separate molecular mechanisms for the two effects. The cytotoxic and transforming potencies were different from one dust to another, even among the same structural silicas. The type of crystalline structure (quartz vs cristobalite) and the crystalline vs biogenic amorphous form did not correlate with cytotoxic or transforming potency of silica dusts. Comparison of cellular effects induced by original and surface modified samples revealed that several surface functionalities modulate cytotoxic and transforming potencies. The cytotoxic effects appeared to be related to the distribution and abundance of silanol groups and to the presence of trace amounts of iron on the silica surface. Silica particles with fractured surfaces and/or iron-active sites, able to generate reactive oxygen species, induced SHE cell transformation. The results show that the activity of silica at the cellular level is sensitive to the composition and structure of surface functionalities and confirm that the biological response to silica is a surface originated phenomenon. In vivo exposure of rat lungs to crystalline silica either by intratracheal instillation or by inhalation results in an increase in mRNA levels for inducible nitric oxide synthase (iNOS) in bronchoalveolar lavage cells (BALC), elevated nitric oxide (.NO) production by BALC, and an increase in .NO-dependent chemiluminescence (CL) from alveolar macrophages (AM). Induction of iNOS message occurs in both AM and polymorphonuclear leukocytes (PMN) harvested from silica-exposed lungs but is not significantly elevated in lavaged lung tissue. This review presents characteristics of simple and complicated coal workers' pneumoconiosis (CWP) as well as pathologic indices of acute and chronic silicosis by summarizing results of in vitro, animal, and human investigations. These results support four basic mechanisms in the etiology of CWP and silicosis: a) direct cytotoxicity of coal dust or silica, resulting in lung cell damage, release of lipases and proteases, and eventual lung scarring; b) activation of oxidant production by pulmonary phagocytes, which overwhelms the antioxidant defenses and leads to lipid peroxidation, protein nitrosation, cell injury, and lung scarring; c) activation of mediator release from alveolar macrophages and epithelial cells, which leads to recruitment of polymorphonuclear leukocytes and macrophages, resulting in the production of proinflammatory cytokines and reactive species and in further lung injury and scarring; d) secretion of growth factors from alveolar macrophages and epithelial cells, stimulating fibroblast proliferation and eventual scarring. Results of in vitro and animal studies provide a basis for proposing these mechanisms for the initiation and progression of pneumoconiosis. Data obtained from exposed workers lend support to these mechanisms. /The authors/ reported previously that freshly fractured silica (FFSi) induces activator protein-1 (AP-1) activation through extracellular signal-regulated protein kinases (ERKs) and p38 kinase pathways. In the present study, the biologic activities of FFSi and aged silica (ASi) were compared by measuring their effects on the AP-1 activation and phosphorylation of ERKs and p38 kinase. The roles of reactive oxygen species (ROS) in this silica-induced AP-1 activation were also investigated. FFSi-induced AP-1 activation was four times higher than that of ASi in JB6 cells. FFSi also caused greater phosphorylation of ERKs and p38 kinase than ASi. FFSi generated more ROS than ASi when incubated with the cells as measured by electron spin resonance (ESR). Studies using ROS-sensitive dyes and
Source: PubChem (NCBI) · pathways from PathBank, Reactome, WikiPathways & PharmGKB.
Molecular reference: talc
PubChem CID 165411828Molecular formula: H2Mg3O12Si4
Mechanism of action
It has very good absorptive properties.
Source: PubChem (NCBI) · pathways from PathBank, Reactome, WikiPathways & PharmGKB.
This drug in other countries
The same active ingredient registered across other registries we cover - including different brands.
- AL (DS) TABLETS · Centurion Laboratories
- AL (SS) TABLETS · Centurion Laboratories
- AL-FORTE TABLETS ( Artemether / Lumefantrine 80mg / 480mg) · Centurion Laboratories
- ALCETHER TABLETS (Each tablets contains Artemether/Lumefantrine 80 /480 ) · Stallion Laboratories
- ALCETHER (formerly ARTETRINE) TABLETS (Each tablet contains Artemether/Lumefantrine 20mg/ 120mg) · Stallion Laboratories
- ALCETHER 20 /120 TABLETS · Stallion Laboratories