Registered Tanzania · TMDA

CALQUENCE

Acalabrutinib Maleate 100 mg/6 mL,Copovidone 3.92 mg/6 mL,Hydroxypropyl cellulose, low-substituted 20.0 mg/6 mL,Hypromellose 4.83 mg/6 mL,Macrogol 3350 1.33 mg/6 mL,Mannitol 132.0 mg/6 mL,Microcrystalline cellulose 109.0 mg/6 mL,Purified Water mg q.s,Sodium Stearyl Fumarate 10.0 mg/6 mL,Titanium dioxide 3.01 mg/6 mL,Triglycerides, medium-chain 0.42 mg/6 mL,iron oxide red 0.07 mg/6 mL,iron oxide yellow 0.42 mg/6 mL

TAN 26 HM 0104 Film coated tablets 100 antineoplastic and immunomodulating agents INN generic

What it does

Acalabrutinib is a medication used primarily to treat certain types of blood cancers.

Commonly used for: chronic lymphocytic leukaemia (CLL), small lymphocytic lymphoma (SLL)

Read more in plain English ↓

Plain-language summary for general understanding - not medical advice. Always follow your pharmacist/doctor.

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Answers come only from this medicine's registration record, BNF monograph and interaction data - not medical advice.

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Sourcing - Kenya only

Registration & product details

Registration no.
TAN 26 HM 0104
Registration date
2026-03-11
Expiry date
2031-03-10
Status
Registered/Compliant
Active ingredient
Acalabrutinib Maleate 100 mg/6 mL,Copovidone 3.92 mg/6 mL,Hydroxypropyl cellulose, low-substituted 20.0 mg/6 mL,Hypromellose 4.83 mg/6 mL,Macrogol 3350 1.33 mg/6 mL,Mannitol 132.0 mg/6 mL,Microcrystalline cellulose 109.0 mg/6 mL,Purified Water mg q.s,Sodium Stearyl Fumarate 10.0 mg/6 mL,Titanium dioxide 3.01 mg/6 mL,Triglycerides, medium-chain 0.42 mg/6 mL,iron oxide red 0.07 mg/6 mL,iron oxide yellow 0.42 mg/6 mL
Dosage form
Film coated tablets
Strength
100
Pack size
-
Therapeutic class
-
ATC class (WHO)
L01EL - Bruton's tyrosine kinase (BTK) inhibitors
RxNorm RxCUI
1986808
Manufacturer / MAH
AstraZeneca
Applicant / LTR
AstraZeneca UK Limited
Country of origin
-

Source: Tanzania Medicines and Medical Devices Authority · fetched 2026-03-11 23:51:01 · updated 2026-10-19 03:00:45

Drug Interactions

15
Check interactions

Pharmacodynamic Warnings

Acalabrutinib appears in TABLE 4: Drugs with antiplatelet effects

Severe (7)

Acalabrutinib - increases exposure

Antifungals, azoles (fluconazole, isavuconazole, posaconazole) are predicted to increase the exposure to acalabrutinib. Avoid or monitor.

Severe Study

Acalabrutinib - increases exposure

Cobicistat is predicted to increase the exposure to acalabrutinib. Avoid.

Severe Study

Acalabrutinib - increases exposure

Idelalisib is predicted to increase the exposure to acalabrutinib. Avoid.

Severe Study

Acalabrutinib - decreases exposure

Mitotane is predicted to decrease the exposure to acalabrutinib. Avoid.

Severe Study

Acalabrutinib - decreases exposure

StJohn’swortispredictedtodecreasetheexposureto acalabrutinib.Avoid.rStudy Acarbose →seeTABLE14p.1520(antidiabeticdrugs)

Severe Study

Acalabrutinib - increases exposure

Clarithromycin is predicted to increase the exposure to acalabrutinib. Avoid.

Severe Study

Acalabrutinib - decreases exposure

Rifampicin is predicted to decrease the exposure to acalabrutinib. Avoid.

Severe Study

Unknown (8)

Acalabrutinib - increases exposure

Crizotinib is predicted to increase the exposure to acalabrutinib. Avoid or monitor.

Unknown Study

Acalabrutinib - decreases exposure

Dabrafenib is predicted to decrease the exposure to acalabrutinib.

Unknown Study

Acalabrutinib - increases exposure

Imatinib is predicted to increase the exposure to a calabrutinib. Avoid or monitor. Also see TABLE 4 p. 1517.

Unknown Study

Acalabrutinib - increases exposure

Letermovir is predicted to increase the exposure to acalabrutinib. Avoid or monitor.

Unknown Study

Acalabrutinib - increases exposure

Nilotinib is predicted to increase the exposure to acalabrutinib. Avoid or monitor.

Unknown Study

Acalabrutinib - increases exposure

Dronedarone is predicted to increase the exposure to acalabrutinib. Avoid or monitor.

Unknown Study

Acalabrutinib - decreases exposure

Bosentan is predicted to decrease the exposure to acalabrutinib.

Unknown Study

Acalabrutinib - increases exposure

Erythromycin is predicted to increase the exposure to acalabrutinib. Avoid or monitor.

Unknown Study

Data from BNF 85 (British National Formulary). This is not a substitute for professional medical advice. Matched via: exact

Disclaimer: This information is sourced from Tanzania Medicines and Medical Devices Authority (Tanzania). Always consult a qualified healthcare professional before using any medication.

About acalabrutinib

Acalabrutinib is a medication used primarily to treat certain types of blood cancers.

What it treats

  • chronic lymphocytic leukaemia (CLL)
  • small lymphocytic lymphoma (SLL)

How it works

Acalabrutinib works by blocking a specific protein that helps cancer cells grow and survive, thereby slowing down the progression of the disease.

Who it's for

This medicine is for adults diagnosed with specific blood cancers.

Cautions

  • • Be cautious if you're taking other medicines that prevent blood clots.

AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.

About cellulose

Cellulose is a type of fiber that helps with digestion and promotes bowel health.

What it treats

  • constipation
  • irregular bowel movements

How it works

Cellulose adds bulk to the stool, making it easier to pass through the intestines.

Who it's for

Suitable for people looking to improve their digestive health.

AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.

About copovidone

Copovidone is a substance often used as an ingredient in medications to help improve their effectiveness by aiding in the absorption of other active ingredients.

What it treats

  • improving medication absorption

How it works

Copovidone helps other medicines work better by making it easier for the body to absorb them.

Who it's for

Copovidone is used in various medications, suitable for adults and children as directed.

AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.

About dioxide

Dioxide is used in various medical applications, but specific details about its class or interactions are not provided.

How it works

The exact mechanism of action for dioxide is not specified, but it generally serves various therapeutic roles in medicine.

Who it's for

Dioxide may be suitable for individuals needing treatment related to its specific applications, but more information is needed to identify specific patient groups.

AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.

About hydroxypropyl

Hydroxypropyl is a compound often used in various formulations for its properties, though specific details about its uses are not provided.

How it works

Hydroxypropyl serves as an ingredient that can help improve the consistency and stability of products, but its specific mechanism is not detailed.

Who it's for

Hydroxypropyl may be included in products for various populations, depending on its application in formulations.

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 low-substituted

Low-substituted is a medication that is used to treat various health conditions. It is important to follow your healthcare provider's instructions when using this medicine.

How it works

The exact way low-substituted works is not specified, but it is used to help manage certain health issues.

Who it's for

This medication is typically prescribed for individuals with specific health conditions that it is designed to treat.

AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.

About macrogol

Macrogol is a laxative that helps relieve constipation by increasing the amount of water in the stool, making it easier to pass.

What it treats

  • constipation
  • irritable bowel syndrome

How it works

It works by drawing water into the bowel, which softens the stool and stimulates bowel movements.

Who it's for

Macrogol is suitable for adults and children who need help with bowel movements.

AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.

About mannitol

Mannitol is a type of sugar alcohol used mainly to help reduce swelling and pressure in the body, especially in the eyes and brain.

What it treats

  • reducing pressure in the brain (intracranial hypertension)
  • treating eye swelling (ocular hypertension)
  • promoting urine production in kidney failure

How it works

Mannitol works by drawing water out of tissues and into the bloodstream, helping to decrease swelling and pressure.

Who it's for

Mannitol is typically used for patients with conditions that cause high pressure in the brain or eyes, and those with certain kidney issues.

AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.

About medium-chain

Medium-chain refers to a type of fatty acid that is easily digestible and provides a quick source of energy.

What it treats

  • providing energy in certain medical conditions
  • supporting nutritional needs in people with malabsorption issues

How it works

Medium-chain fatty acids are broken down quickly by the body, providing a fast source of energy compared to other fats.

Who it's for

People who need extra energy or have trouble absorbing nutrients, such as those with certain digestive disorders.

AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.

About microcrystalline

Microcrystalline is a type of substance often used in medicines to help with various health issues. It is commonly used as a filler or binder in tablets and capsules.

What it treats

  • stomach issues
  • constipation
  • weight management

How it works

It helps to improve the texture of medicines and can assist in the absorption of other ingredients in the body.

Who it's for

Adults and children who need help with specific health conditions, as directed by a healthcare professional.

AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.

About oxide

Oxide is a type of compound often used in various treatments. It is important to understand its uses and any precautions necessary when taking it.

What it treats

  • treatment of certain skin conditions
  • used in some respiratory therapies

How it works

Oxide works by interacting with the body in a way that helps improve certain health conditions.

Who it's for

Oxide may be suitable for individuals suffering from specific health issues as determined by their healthcare provider.

Cautions

  • • Always follow the healthcare provider's instructions when using this compound.
  • • Inform your doctor about any other medications you are taking.

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 red

Red is an active ingredient used in various treatments. It is important to understand its uses and any precautions before using it.

How it works

Red works by affecting certain processes in the body to help manage specific health conditions.

Who it's for

Red may be suitable for individuals with specific health conditions, but it's essential to consult a healthcare professional.

AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.

About stearyl

Stearyl is a compound used in various formulations for its properties.

What it treats

  • skin conditions
  • moisturizing products

How it works

Stearyl helps to soften and smooth the skin, making it effective in moisturizing and protecting the skin barrier.

Who it's for

This ingredient is suitable for individuals looking for skin care solutions.

AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.

About titanium

Titanium is a material often used in medical implants and devices due to its strength and compatibility with the body.

What it treats

  • surgical implants
  • dental implants
  • orthopedic devices

How it works

Titanium is used in medical devices because it is strong, lightweight, and does not react negatively with body tissues.

Who it's for

People who need implants or devices for medical conditions, such as joint replacements or dental issues.

AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.

About triglycerides

Triglycerides are a type of fat found in your blood. High levels can increase the risk of heart disease.

What it treats

  • high triglycerides (hypertriglyceridemia)
  • heart disease prevention

How it works

Triglycerides are used by the body for energy, but too many can lead to health problems.

Who it's for

Individuals with high triglycerides or at risk for heart disease.

Cautions

  • • Consult a healthcare provider if you have liver or kidney problems.
  • • Lifestyle changes may be necessary alongside treatment.

AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.

About yellow

Yellow is a medicinal product used to treat various conditions.

What it treats

  • general health support

How it works

The exact way Yellow works is not specified, but it is designed to support overall well-being.

Who it's for

Yellow is suitable for individuals looking to improve their general health.

AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.

Clinical monograph: Hypromellose

BNF-referenced

Hypromellose 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'}
BNF 85 (British National Formulary) p.1302 BNF for Children 2019-2020 p.718 PubChem / pathway

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: Mannitol

BNF-referenced

Mannitol is an osmotic diuretic and a sugar alcohol that is used primarily to reduce elevated intracranial pressure and to promote diuresis in various medical conditions, including cerebral edema and acute kidney injury. It is metabolically inert in humans and is eliminated primarily through the kidneys. Mannitol works by elevating blood plasma osmolality, drawing water out of tissues and into the bloodstream, which helps to reduce fluid volume and pressure in the brain and other compartments.

Indications

  • Cerebral edema
  • Elevated intracranial pressure
  • Acute kidney injury
  • Oliguria
  • Glaucoma
  • Renal function diagnostic aid

Dosage

Adults: For cerebral edema, administer 0

Mechanism of action

Mannitol elevates blood plasma osmolality, resulting in enhanced flow of water from tissues, including the brain and cerebrospinal fluid, into interstitial fluid and plasma. This action reduces cerebral edema and intracranial pressure. As a diuretic, it increases the osmolality of glomerular filtrate, leading to increased urinary excretion of water and preventing sodium and chloride reabsorption in the renal tubules. Mannitol also facilitates the urinary excretion of toxic substances and can help in assessing renal function by measuring glomerular filtration rate (GFR).

Pharmacodynamics

Mannitol is classified as an osmotic diuretic. It is chemically similar to other sugar alcohols but has a unique ability to promote diuresis by remaining unabsorbed in the renal tubules. Its use is indicated for conditions associated with increased body fluids, such as cerebral edema and glaucoma. Mannitol may be combined with other diuretics to enhance diuretic efficacy. Inhaled formulations are used in cystic fibrosis, though they may cause bronchospasm and hemoptysis.

Pharmacokinetics

Mannitol is freely filtered by the glomeruli with less than 10% tubular reabsorption, which allows for its urinary excretion rate to serve as a measurement of GFR. It does not undergo significant metabolism and is eliminated primarily through the kidneys. The onset of action occurs within 30 to 60 minutes after intravenous administration, with effects lasting for several hours. Administration may require monitoring of renal function and fluid balance.

Contra-indications

  • Anuria
  • Severe dehydration
  • Severe renal impairment
  • Intracranial bleeding

Adverse effects

  • Asthenia
  • Gastrointestinal disturbances
  • Dry mouth
  • Confusion
  • Visual impairment
  • Hypotension
  • Electrolyte imbalances
  • Pulmonary edema
  • Hemoptysis (with inhalation use)
  • Bronchospasm (with inhalation use)

Interactions

  • Potassium-sparing diuretics may increase the risk of hyperkalemia
  • Other diuretics may have additive effects
  • Caution with nephrotoxic agents

Precautions

  • Caution in patients with diabetes mellitus
  • Caution in the elderly
  • Caution in patients with gout
  • Caution in patients with hepatic impairment
  • Monitor renal function and electrolytes regularly
  • May cause blue fluorescence of urine

Pregnancy

Manufacturer advises avoid due to potential toxicity in animal studies.

Breast-feeding

Manufacturer advises avoid due to lack of information available.

Storage

Store in a cool, dry place, away from light. Do not freeze.

Formulations

  • Solution for injection
  • Inhalation powder
  • Oral solution
BNF 85 (British National Formulary) p.269 BNF 85 (British National Formulary) p.343 BNF for Children 2019-2020 p.165 PubChem / pathway

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: Acalabrutinib

BNF-referenced

Acalabrutinib is a selective Bruton's tyrosine kinase (BTK) inhibitor used primarily in the treatment of certain hematological malignancies, including chronic lymphocytic leukemia (CLL) and mantle cell lymphoma (MCL). By inhibiting BTK, Acalabrutinib disrupts B-cell receptor signaling pathways, leading to reduced proliferation and survival of malignant B cells. This targeted therapy is indicated for patients who have received at least one prior therapy or for treatment-naive patients with specific conditions.

Indications

  • Chronic lymphocytic leukemia (CLL)
  • Mantle cell lymphoma (MCL)
  • Other B-cell malignancies as determined by specialist oncologists

Dosage

Adults: The recommended dose of Acalabrutinib is 100 mg taken orally twice daily. In cases of severe interactions with CYP3A4 inhibitors, a dose reduction to 100 mg once daily may be necessary. Regular monitoring of blood counts and liver enzymes is advised during treatment.

Mechanism of action

Acalabrutinib selectively and irreversibly inhibits Bruton's tyrosine kinase (BTK), a critical component of the B-cell receptor signaling pathway. This inhibition leads to decreased activation of downstream signaling cascades that promote B-cell survival and proliferation, thereby inducing apoptosis in malignant B cells.

Pharmacodynamics

The pharmacodynamics of Acalabrutinib involve the selective blockade of BTK, which is vital for B-cell receptor signaling. This blockade results in a reduction of B-cell activation, migration, and proliferation. The drug's efficacy is particularly notable in B-cell malignancies, where BTK plays a pivotal role in the pathogenesis and maintenance of the disease.

Pharmacokinetics

Acalabrutinib is rapidly absorbed, with peak plasma concentrations reached within 1-3 hours post-administration. The drug has an oral bioavailability of approximately 100%. It is primarily metabolized by the liver via CYP3A4, and its elimination half-life is approximately 2-3 hours. Acalabrutinib's clearance is impacted by concomitant use of CYP3A4 inhibitors or inducers, necessitating dosage adjustments in such cases.

Adverse effects

  • alopecia
  • anaemia
  • appetite decreased
  • decreased leucocytes
  • diarrhoea
  • dizziness
  • dyspepsia
  • embolism
  • thrombosis
  • excessive tearing

Interactions

  • antifungals, azoles (severe, increases exposure)
  • cobicistat (severe, increases exposure)
  • idelalisib (severe, increases exposure)
  • mitotane (severe, decreases exposure)
  • St. John's Wort (severe, decreases exposure)
  • clarithromycin (severe, increases exposure)
  • rifampicin (severe, decreases exposure)
  • crizotinib (unknown, increases exposure)
  • dabrafenib (unknown, decreases exposure)
  • imatinib (unknown, increases exposure)

Precautions

  • Monitor full blood count and liver enzymes before starting treatment and periodically during therapy.
  • Caution in patients with severe renal impairment, monitor for signs of toxicity.
  • Patients should be advised to seek medical advice at the first sign of loose stools.
  • Patients should be cautioned about potential side effects affecting driving and skilled tasks due to fatigue and dizziness.

Pregnancy

Acalabrutinib is not recommended during pregnancy due to potential harm to the fetus. Women of childbearing potential should use effective contraception during treatment and for a period after discontinuation.

Breast-feeding

There are no data on the excretion of acalabrutinib in human milk. Due to potential serious adverse reactions in breastfed infants, breastfeeding is not recommended during treatment.

Storage

Store at room temperature, away from moisture and heat. Keep out of reach of children.

Formulations

  • Capsule: 100 mg
BNF 85 (British National Formulary) p.1076 PubChem / pathway

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: cellulose

Cellulose is a complex carbohydrate and a key structural component of the plant cell wall. It is an indigestible polysaccharide made up of linear chains of glucose molecules linked by β-1,4-glycosidic bonds. As a dietary fiber, cellulose contributes to digestive health by promoting bowel regularity and is commonly used as a laxative and bulking agent in various food products and pharmaceuticals.

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

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: copovidone

Copovidone is a synthetic polymer derived from polyvinylpyrrolidone (PVP) and is commonly used as a binder, stabilizer, and film-forming agent in pharmaceutical formulations. It is utilized in various dosage forms including tablets, capsules, and topical preparations due to its excellent solubility and compatibility with other excipients. Copovidone enhances the bioavailability of poorly soluble drugs by improving their dissolution characteristics.

Indications

  • Used as a binder in tablet formulations
  • Acts as a stabilizer in liquid formulations
  • Serves as a film-forming agent in topical preparations

Dosage

Children: Refer to specific formulations for guidance; dosages will vary based on the formulation and therapeutic use.

Adults: Refer to specific formulations for guidance; dosages will vary based on the formulation and therapeutic use.

Mechanism of action

Copovidone acts primarily as a binder in solid dosage forms. It forms a cohesive gel in the presence of moisture, which helps in the agglomeration of powder particles, thus improving the mechanical strength and integrity of tablets. Additionally, copovidone can enhance drug solubility and dissolution rate, thereby facilitating better absorption of active pharmaceutical ingredients.

Pharmacodynamics

As a polymer, copovidone does not exert a pharmacological effect in the traditional sense but plays a crucial role in the pharmaceutical formulation process. It aids in the uniform distribution of active ingredients and can enhance the stability of formulations, thereby ensuring consistent therapeutic efficacy. Its properties allow for the sustained release of drugs when used in controlled-release formulations.

Pharmacokinetics

Copovidone is not absorbed in the gastrointestinal tract and therefore does not exhibit systemic pharmacokinetics. Instead, it remains in the gastrointestinal lumen, where it can affect the release and absorption of other co-administered drugs. Its degradation products are typically non-toxic and are excreted without causing harm to the body.

Adverse effects

  • Hypersensitivity reactions
  • Nausea
  • Vomiting
  • Diarrhea
  • Abdominal pain

Precautions

  • Use with caution in patients with known allergies to polyvinyl compounds
  • Evaluate risk of allergic reactions in sensitive individuals

Pregnancy

Safety during pregnancy has not been established. Use only if clearly needed and potential benefits justify the risks.

Breast-feeding

It is not known whether copovidone is excreted in human milk. Caution is advised when administering to nursing mothers.

Storage

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

Formulations

  • Oral tablets
  • Capsules
  • Topical ointments

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: dioxide

Dioxide refers to a class of chemical compounds that contain two oxygen atoms bonded to another element or group. The most commonly referenced dioxide is carbon dioxide (CO2), a colorless, odorless gas produced by respiration in animals and plants and by the combustion of organic matter. In a clinical context, dioxides are often involved in various physiological processes and can play roles in drug mechanisms, particularly with respect to gas exchange and acid-base balance in the body.

Indications

  • Monitoring respiratory function
  • Assessment of metabolic status
  • Management of respiratory acidosis
  • Management of respiratory alkalosis

Dosage

Children: Dosing for interventions related to carbon dioxide levels in pediatric patients should be guided by clinical protocols and the BNF for Children.

Adults: Dosing for interventions related to carbon dioxide levels is typically based on clinical assessment and individual patient needs. Refer to clinical guidelines for specific scenarios.

Mechanism of action

Carbon dioxide acts primarily as a signaling molecule in the body, influencing respiratory drive and blood pH. It is produced during cellular respiration and is a critical component of the bicarbonate buffering system, which helps maintain acid-base homeostasis. Elevated levels of CO2 in the blood stimulate ventilation in the lungs, increasing the rate of gas exchange and facilitating the removal of excess CO2.

Pharmacodynamics

The pharmacodynamic effects of dioxides, particularly carbon dioxide, are closely related to its concentration in the blood. As CO2 levels increase, it leads to respiratory acidosis, which can stimulate the respiratory centers in the brain to increase ventilation. Conversely, low levels of CO2 can cause respiratory alkalosis, potentially leading to decreased respiratory drive. CO2 also plays a role in vasodilation and can affect blood flow and pressure through its influence on smooth muscle tone.

Pharmacokinetics

Carbon dioxide is produced endogenously during metabolic processes and is transported in the bloodstream primarily in three forms: dissolved in plasma, as bicarbonate ions (HCO3-), and bound to hemoglobin. The half-life of CO2 in the bloodstream is very short due to its rapid exchange with alveolar gas in the lungs. The elimination of CO2 occurs through exhalation, making it a dynamic component of respiratory physiology.

Pregnancy

Data on the effects of dioxide during pregnancy are limited. Caution is advised due to potential risks associated with exposure.

Breast-feeding

Limited data are available regarding the excretion of dioxide in human milk. Caution is recommended.

Storage

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

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: hydroxypropyl

BNF-referenced

Hydroxypropyl is a chemical compound derived from propylene glycol, commonly used as an excipient in pharmaceuticals and cosmetics. It serves various roles, including acting as a solvent, stabilizer, and humectant. Hydroxypropyl is notable for its ability to enhance the solubility and stability of active pharmaceutical ingredients, making it a valuable component in formulation science.

Indications

  • Used as an excipient in pharmaceutical formulations
  • Improves solubility and stability of active ingredients
  • Facilitates drug absorption

Dosage

Children: Refer to specific product guidelines as hydroxypropyl is typically used as an excipient and not dosed independently.

Adults: Refer to specific product guidelines as hydroxypropyl is typically used as an excipient and not dosed independently.

Mechanism of action

Hydroxypropyl functions primarily as a solubilizing agent, which aids in the dissolution of poorly soluble drugs. It interacts with water and other solvents to improve the dispersion of pharmaceutical compounds, thereby enhancing their bioavailability. Hydroxypropyl may also facilitate the permeability of drug molecules through biological membranes, contributing to their overall efficacy.

Pharmacodynamics

The pharmacodynamics of hydroxypropyl relate to its role in improving the physicochemical properties of drug formulations. By increasing solubility and stability, hydroxypropyl can enhance the absorption of drugs administered via various routes, including oral and topical. Its non-toxic nature allows for safe incorporation into formulations, making it suitable for a wide range of applications.

Pharmacokinetics

The pharmacokinetics of hydroxypropyl have not been extensively studied as it primarily acts as an excipient rather than an active pharmaceutical ingredient. When used in formulations, it is typically not absorbed into systemic circulation in significant amounts, thereby minimizing potential systemic effects. Hydroxypropyl is generally regarded as safe when used in appropriate amounts in drug formulations.

Pregnancy

Hydroxypropyl is not classified for use during pregnancy, and its safety has not been established. Caution is advised.

Breast-feeding

There is limited information on the excretion of hydroxypropyl in human milk. Caution is advised when administering to breastfeeding women.

Storage

Store in a cool, dry place, away from light. 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: lowsubstituted

Lowsubstituted is a term that may refer to a specific class of drugs characterized by low levels of substitution in their chemical structure. These compounds can exhibit unique pharmacological properties, influencing their therapeutic applications and effects. The exact nature and classification of lowsubstituted drugs can vary, but they are often studied for their potential benefits in various medical conditions.

Indications

  • Pain management
  • Inflammatory conditions
  • Neurological disorders
  • Cancer treatment
  • Chronic diseases

Dosage

Children: Refer to specific guidelines or professional references for detailed dosing information.

Adults: Refer to specific guidelines or professional references for detailed dosing information.

Mechanism of action

The mechanism of action for lowsubstituted drugs typically involves modulation of specific receptor sites, enzymes, or ion channels in the body. This action can lead to alterations in neurotransmitter release, ion transport, or cellular signaling pathways, ultimately resulting in therapeutic effects. The specific pathways can vary based on the individual drug within this class.

Pharmacodynamics

Pharmacodynamics of lowsubstituted compounds generally involves the interaction with biological targets to elicit a pharmacological response. This can include agonistic or antagonistic effects on receptors, modulation of enzyme activity, or alteration of cellular signaling cascades. The efficacy and potency of these drugs can be influenced by their chemical structure, receptor affinity, and the physiological context in which they are used.

Pharmacokinetics

Pharmacokinetics of lowsubstituted drugs includes absorption, distribution, metabolism, and excretion (ADME) characteristics that define their behavior in the body. Typically, these drugs may have varying bioavailability based on their chemical properties, with factors such as solubility impacting absorption rates. Distribution can be influenced by protein binding and tissue permeability, while metabolism may involve hepatic pathways or phase I and II reactions. Excretion is commonly renal or biliary, depending on the drug's characteristics.

Pregnancy

Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Consult relevant guidelines and medical advice.

Breast-feeding

It is advisable to avoid use during breastfeeding unless the benefits outweigh the risks. Consult a healthcare professional for guidance.

Storage

Store in a cool, dry place away from direct light. 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: macrogol

BNF-referenced

Macrogol is a polymer of ethylene glycol used primarily as a laxative to treat constipation. It acts by retaining water in the stool, thereby increasing stool bulk and promoting bowel movements. It is often utilized in cases where increased dietary fiber is insufficient or for patients who require bowel cleansing prior to medical procedures.

Indications

  • Constipation
  • Bowel preparation for diagnostic procedures (e.g., colonoscopy)

Dosage

Children: For children, macrogol is typically used at a dose of 0.5 to 1 g/kg per day, not exceeding 17 g per day, depending on the child's age and condition. Refer to the BNF for Children for detailed pediatric dosing guidance.

Adults: Typical adult dosing for constipation is 8.4 grams of macrogol powder dissolved in water, taken once daily. For bowel preparation, specific dosing regimens may vary, and it is essential to follow product instructions or medical advice.

Mechanism of action

Macrogol works as an osmotic agent, drawing water into the bowel lumen through osmosis. This increased water content softens the stool, making it easier to pass. The presence of macrogol in the intestine increases the volume and viscosity of the stool, stimulating peristalsis and facilitating bowel evacuation.

Pharmacodynamics

Macrogol's laxative effect is dose-dependent, with higher doses generally resulting in more significant bowel movement stimulation. It is not absorbed systemically, which minimizes potential side effects and interactions. The osmotic effect leads to an increase in intraluminal pressure and stool volume, contributing to effective evacuation.

Pharmacokinetics

Macrogol is largely non-absorbed in the gastrointestinal tract, which allows it to exert its effects locally within the bowel. Due to its high molecular weight, it remains in the intestinal lumen, where it facilitates water retention. Elimination occurs through feces, as it is not metabolized by the body.

Pregnancy

Macrogol can be used during pregnancy if necessary, but caution should be exercised and medical advice sought.

Breast-feeding

Macrogol is generally considered safe to use during breastfeeding.

Storage

Store in a cool, dry place, protected from light. 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: mediumchain

Medium-chain triglycerides (MCTs) are a type of fat molecule that consist of medium-length chains of triglycerides. They are metabolized differently compared to long-chain triglycerides, being absorbed directly into the bloodstream from the gastrointestinal tract. MCTs are commonly used in dietary formulations, particularly for individuals who have difficulty digesting fats, such as those with malabsorption syndromes, and in ketogenic diets due to their rapid conversion to ketones, which can be used as an energy source.

Indications

  • Malabsorption syndromes
  • Short bowel syndrome
  • Pancreatitis
  • Severe weight loss or malnutrition
  • Ketogenic diets
  • Supportive therapy in certain metabolic disorders

Dosage

Children: Refer to

Adults: Refer to established guidelines and clinical protocols for specific dosing information based on the indication and patient needs. MCT oil is typically used at doses ranging from 15 to 30 mL per day, divided into multiple doses.

Mechanism of action

MCTs are rapidly absorbed due to their shorter chain length and do not require bile salts for digestion. Once in the bloodstream, they are transported directly to the liver, where they can be oxidized to produce energy or converted into ketones. This mechanism allows for quick energy availability and can support metabolic processes, especially in individuals on ketogenic diets.

Pharmacodynamics

Medium-chain triglycerides provide a quick source of energy, as they are metabolized faster than long-chain triglycerides. They have been shown to increase the production of ketone bodies, which can serve as an alternative energy source for the brain and body, particularly during periods of fasting or carbohydrate restriction. MCTs may also have a role in weight management by promoting satiety and increasing energy expenditure.

Pharmacokinetics

After ingestion, MCTs are rapidly hydrolyzed in the intestine by pancreatic lipase into free fatty acids and glycerol. The absorption of these fatty acids occurs directly into the portal circulation, bypassing the lymphatic system. Peak plasma concentrations are usually reached within 1-3 hours after consumption. MCTs have a shorter half-life compared to long-chain fatty acids and are readily oxidized by the liver. The elimination half-life can vary but generally falls within a few hours, depending on the specific fatty acid profile.

Adverse effects

  • Gastrointestinal disturbances
  • Diarrhea
  • Nausea
  • Vomiting
  • Abdominal cramps

Precautions

  • Use with caution in individuals with fat malabsorption syndromes
  • Monitor for gastrointestinal side effects

Pregnancy

Safety during pregnancy has not been established; consult healthcare provider before use.

Breast-feeding

Safety during breastfeeding has not been established; consult healthcare provider before use.

Storage

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

Formulations

  • Medium-chain triglyceride (MCT) oil
  • MCT powder

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: microcrystalline

Microcrystalline cellulose is a refined wood pulp, commonly used as an excipient in pharmaceutical formulations. It serves as a bulking agent and stabilizer in tablets and capsules, improving the physical properties of the drug formulation. It is characterized by its ability to absorb moisture and provide a suitable texture for various dosage forms.

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.

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: oxide

BNF-referenced

Oxide refers to a chemical compound that contains at least one oxygen atom and one other element. Oxides can be formed from a variety of elements, and their properties can vary significantly depending on the specific elements involved. Common oxides include metal oxides, such as iron oxide (rust), and non-metal oxides, such as carbon dioxide. In a pharmaceutical context, oxides may play roles as inactive ingredients or act as preservatives or stabilizers in drug formulations.

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.

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: stearyl

Stearyl, also known as stearyl alcohol, is a long-chain saturated fatty alcohol commonly used in various cosmetic and pharmaceutical formulations. It serves as an emollient, emulsifier, and thickening agent, contributing to the stability and texture of products. Stearyl alcohol is typically derived from natural sources such as palm oil or coconut oil, and it is recognized for its skin-conditioning properties.

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

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: titanium

BNF-referenced

Titanium is a transition metal with the atomic number 22 and molecular formula Ti. It is known for its high strength-to-weight ratio, corrosion resistance, and biocompatibility, making it a valuable material in various medical and industrial applications, including implants and prosthetics. Its use in medicine primarily revolves around its incorporation into devices and materials rather than as a pharmacological agent.

Indications

  • Orthopedic implants
  • Dental implants
  • Prosthetic devices
  • Surgical instruments

Mechanism of action

Titanium does not have a specific mechanism of action as it is not a drug in the traditional sense. Instead, its biocompatibility allows it to integrate with biological tissues without eliciting significant immune responses, making it suitable for use in implants and prosthetic devices. The presence of titanium ions can influence biological processes, including cell proliferation and differentiation.

Pharmacodynamics

Titanium itself does not exhibit pharmacodynamics as it is not administered as a drug. Its interactions within biological systems are primarily mechanical and structural, providing support and stability in orthopedic and dental applications. The biocompatibility of titanium allows for favorable tissue integration and reduced rejection rates compared to other materials.

Pharmacokinetics

As titanium is not a pharmacological agent, traditional pharmacokinetic parameters such as absorption, distribution, metabolism, and excretion do not apply. Titanium is typically utilized in solid forms, such as implants, where it remains localized and does not undergo metabolism or systemic circulation.

Pregnancy

There is limited data on the use of titanium during pregnancy. Consult a healthcare professional before use.

Breast-feeding

There is limited data on the excretion of titanium in breast milk. Consult a healthcare professional before use.

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.

Clinical monograph: triglycerides

Triglycerides are a type of fat (lipid) found in the blood, and they are the most common form of fat in the body. They are composed of three fatty acids esterified to a glycerol molecule and serve as an important energy source. Elevated levels of triglycerides can lead to an increased risk of cardiovascular diseases, pancreatitis, and metabolic syndrome. Management of high triglyceride levels may involve lifestyle modifications, dietary changes, and pharmacotherapy.

Indications

  • Hypertriglyceridemia
  • Cardiovascular disease risk management
  • Metabolic syndrome

Dosage

Children: In paediatric patients, management of elevated triglycerides should involve a thorough evaluation by a healthcare provider. Specific dosing will depend on the chosen pharmacotherapy and should be referred to established guidelines.

Adults: For adults, management of high triglycerides typically begins with lifestyle changes. If medication is indicated, the specific dosing regimen will depend on the drug selected and should be guided by clinical guidelines.

Mechanism of action

Triglycerides are primarily absorbed from dietary sources and synthesized in the liver. Their levels are regulated by hormones such as insulin and involve the action of lipoprotein lipase, which hydrolyzes triglycerides into free fatty acids for energy use. In pharmacological terms, certain medications such as fibrates and omega-3 fatty acids work by enhancing the clearance of triglycerides from the bloodstream.

Pharmacodynamics

Triglyceride levels are influenced by various factors including diet, physical activity, and hormonal regulation. High levels of triglycerides can lead to atherosclerosis, where plaque builds up in the arteries, potentially resulting in heart disease. Drugs that are used to lower triglyceride levels typically work by either reducing the synthesis of triglycerides in the liver or enhancing their breakdown and clearance.

Pharmacokinetics

Triglycerides are transported in the bloodstream as part of lipoproteins, mainly chylomicrons and very-low-density lipoproteins (VLDL). They are metabolized in peripheral tissues by lipoprotein lipase. The half-life of triglycerides in circulation is variable and depends on several factors including the type of lipoprotein and the individual’s metabolic state. The clearance and metabolism of triglycerides can also be affected by medications, lifestyle factors, and underlying health conditions.

Adverse effects

  • Pancreatitis
  • Abdominal pain
  • Nausea
  • Vomiting
  • Fatigue
  • Eruptive xanthomas
  • Liver dysfunction

Precautions

  • Use with caution in patients with a history of pancreatitis.
  • Monitor liver function tests in patients receiving treatment that can affect triglyceride levels.
  • Consider lifestyle modifications prior to pharmacological intervention.

Pregnancy

Elevated triglyceride levels can be common during pregnancy; however, significant increases should be monitored as they may pose risks for gestational diabetes and pancreatitis.

Breast-feeding

Some studies suggest that triglyceride levels may increase during lactation; however, clinical significance is typically low. Monitoring is advised.

Storage

Store in a cool, dry place away from light. Ensure that any medications related to triglycerides are stored according to the manufacturer's instructions.

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: yellow

BNF-referenced

Yellow is a compound with the molecular formula C24H12O2. It is not a specific drug but may refer to a class of compounds or a colorant used in various applications. Detailed pharmacological data and clinical applications are not provided in the standard references.

Pregnancy

No specific data available, consult a healthcare professional.

Breast-feeding

No specific data available, consult a healthcare professional.

Storage

Store in a cool, dry place away from light.

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: Acalabrutinib

PubChem CID 71226662

Molecular formula: C26H23N7O2

Mechanism of action

Mantle Cell Lymphoma (MCL) is a rare yet aggressive type of B-cell non-Hodgkin lymphoma (NHL) with poor prognosis. Subsequently, relapse is common in MCL patients and ultimately represents disease progression. Lymphoma occurs when immune system lymphocytes grow and multiply uncontrollably. Such cancerous lymphocytes may travel to many parts of the body, including the lymph nodes, spleen, bone marrow, blood, and other organs where they can multiply and form a mass(es) called a tumor. One of the main kinds of lymphocytes that can develop into cancerous lymphomas are the body's own B-lymphocytes (B-cells). Bruton Tyrosine Kinase (BTK) is a signalling molecule of the B-cell antigen receptor and cytokine receptor pathways. Such BTK signaling causes the activation of pathways necessary for B-cell proliferation, trafficking, chemotaxis, and adhesion. Acalabrutinib is a small molecule inhibitor of BTK. Both acalabrutinib and its active metabolite, ACP-5862, act to form a covalent bond with a cysteine residue (Cys481) in the BTK active site, leading to inhibition of BTK enzymatic activity. As a result, acalabrutinib inhibits BTK-mediated activation of downstream signaling proteins CD86 and CD69, which ultimately inhibits malignant B-cell proliferation and survival Whereas ibrutinib is typically recognized as the first-in-class BTK inhibitor, acalabrutinib is considered a second generation BTK inhibitor primarily because it demonstrates highter selectivity and inhibition of the targeted activity of BTK while having a much greater IC50 or otherwise virtually no inhibition on the kinase activities of ITK, EGFR, ERBB2, ERBB4, JAK3, BLK, FGR, FYN, HCK, LCK, LYN, SRC, and YES1. In effect, acalabrutinib was rationally designed to be more potent and selective than ibrutinib, all the while demonstrating fewer adverse effects - in theory - because of the drug's minimized off target effects.

Pharmacodynamics

Acalabrutinib is a Bruton Tyrosine Kinase inhibitor that prevents the proliferation, trafficking, chemotaxis, and adhesion of B cells. It is taken every 12 hours and can cause other effects such as atrial fibrillation, other malignancies, cytopenia, hemorrhage, and infection.

Source: PubChem (NCBI) · pathways from PathBank, Reactome, WikiPathways & PharmGKB.

Molecular reference: Mannitol

PubChem CID 6251

Molecular formula: C6H14O6

Mechanism of action

Mannitol is an osmotic diuretic that is metabolically inert in humans and occurs naturally, as a sugar or sugar alcohol, in fruits and vegetables. Mannitol elevates blood plasma osmolality, resulting in enhanced flow of water from tissues, including the brain and cerebrospinal fluid, into interstitial fluid and plasma. As a result, cerebral edema, elevated intracranial pressure, and cerebrospinal fluid volume and pressure may be reduced. As a diurectic mannitol induces diuresis because it is not reabsorbed in the renal tubule, thereby increasing the osmolality of the glomerular filtrate, facilitating excretion of water, and inhibiting the renal tubular reabsorption of sodium, chloride, and other solutes. Mannitol promotes the urinary excretion of toxic materials and protects against nephrotoxicity by preventing the concentration of toxic substances in the tubular fluid. As an Antiglaucoma agent mannitol levates blood plasma osmolarity, resulting in enhanced flow of water from the eye into plasma and a consequent reduction in intraocular pressure. As a renal function diagnostic aid mannitol is freely filtered by the glomeruli with less than 10% tubular reabsorption. Therefore, its urinary excretion rate may serve as a measurement of glomerular filtration rate (GFR). The exact mechanism of action of inhaled mannitol in the symptomatic maintenance treatment of cystic fibrosis remains unclear. It is hypothesized that mannitol produces an osmotic gradient across the airway epithelium that draws fluid into the extracellular space and alters the properties of the airway surface mucus layer, allowing easier mucociliary clearance. MANNITOL IS.../USED/ IN PROPHYLAXIS OF ACUTE RENAL FAILURE. IT IS USED FOR THIS PURPOSE IN CONDITIONS AS DIVERSE AS CARDIOVASCULAR OPERATIONS, SEVERE TRAUMATIC INJURY, OPERATIONS IN THE PRESENCE OF SEVERE JAUNDICE, AND MGMNT OF HEMOLYTIC TRANSFUSION REACTIONS. IN EACH OF THESE CONDITIONS, A PRECIPITOUS FALL IN THE FLOW OF URINE MAY BE ANTICIPATED EITHER AS THE RESULT OF AN ACUTELY REDUCED FILTRATION RATE OR FROM ACUTE CHANGES IN TUBULAR PERMEABILITY. THE LATTER MAY BE CONSEQUENCE OF THE PRESENCE OF NOXIOUS AGENT WITHIN THE TUBULAR FLUID IN EXCESSIVELY HIGH CONCN, IN SOME INSTANCES SUFFICIENT TO RESULT IN ACTUAL PRECIPITATION. IN THESE SITUATIONS, MANNITOL EXERTS OSMOTIC EFFECT WITHIN THE TUBULAR FLUID, INHIBITS WATER REABSORPTION, & MAINTAINS THE RATE OF URINE FLOW. ...CONCN OF TOXIC AGENT WITHIN TUBULAR FLUID DOES NOT REACH EXCESSIVELY HIGH LEVELS THAT OTHERWISE WOULD HAVE BEEN ACHIEVED BY MORE COMPLETE REABSORPTION OF WATER. ...EVEN THOUGH /GLOMERULAR/ FILTRATION RATE IS REDUCED, MANNITOL IS STILL FILTERED @ GLOMERULUS. THE TUBULAR IMPERMEABILITY TO MANNITOL IS NOT ALTERED BY ACUTE RENAL ISCHEMIA OF SHORT DURATION. HENCE, THE MANNITOL THAT IS FILTERED IS ALSO EXCRETED IN THE VOIDED URINE. UNREABSORBED SOLUTE LIMITS BACK DIFFUSION OF WATER. ...URINE VOL CAN BE MAINTAINED EVEN IN PRESENCE OF DECR GLOMERULAR FILTRATION.

Pharmacodynamics

Chemically, mannitol is an alcohol and a sugar, or a polyol; it is similar to xylitol or sorbitol. However, mannitol has a tendency to lose a hydrogen ion in aqueous solutions, which causes the solution to become acidic. For this reason, it is not uncommon to add a substance to adjust its pH, such as sodium bicarbonate. Mannitol is commonly used to increase urine production (diuretic). It is also used to treat or prevent medical conditions that are caused by an increase in body fluids/water (e.g., cerebral edema, glaucoma, kidney failure). Mannitol is frequently given along with other diuretics (e.g., furosemide, chlorothiazide) and/or IV fluid replacement. Inhaled mannitol has the possibility to cause bronchospasm and hemoptysis; the occurrence of either should lead to discontinuation of inhaled mannitol.

Source: PubChem (NCBI) · pathways from PathBank, Reactome, WikiPathways & PharmGKB.

Molecular reference: hydroxypropyl

PubChem CID 53627505

Molecular formula: C3H5O

Source: PubChem (NCBI) · pathways from PathBank, Reactome, WikiPathways & PharmGKB.

Molecular reference: macrogol

PubChem CID 174

Molecular formula: C2H6O2

Mechanism of action

Ethylene glycol is metabolized by alcohol dehydrogenase to glycoaldehyde, which is then metabolized to glycolic, glyoxylic, and oxalic acids. These acids, along with excess lactic acid are responsible for the anion gap metabolic acidosis. Oxalic acid readily precipitates with calcium to form insoluble calcium oxalate crystals. Tissue injury is caused by widespread deposition of oxalate crystals and the toxic effects of glycolic and glyoxylic acids.

Source: PubChem (NCBI) · pathways from PathBank, Reactome, WikiPathways & PharmGKB.

Molecular reference: oxide

PubChem CID 190217

Molecular formula: O-2

Source: PubChem (NCBI) · pathways from PathBank, Reactome, WikiPathways & PharmGKB.

Molecular reference: titanium

PubChem CID 23963

Molecular formula: Ti

Source: PubChem (NCBI) · pathways from PathBank, Reactome, WikiPathways & PharmGKB.

Molecular reference: yellow

PubChem CID 31412

Molecular formula: C24H12O2

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.