(dibasic · DailyMed)
AKUGLIP 100
Anhydrous Dibasic Calcium Phosphate 60.00 mg/6 mL,Croscarmellose Sodium 10.00 mg/6 mL,Isopropyl Alcohol q.s q.s,Magnesium Stearate 04.00 mg/6 mL,Microcrystalline cellulose 167.94 mg/6 mL,Opadry Complete Film Coating System 85F570205 Beige 16.00 mg/6 mL,Povidone 12.00 mg/6 mL,Purified Water q.s q.s,Sitagliptin phosphate 100 mg,Sodium Stearyl Fumarate 12.00 mg/6 mL
What it does
Alcohol is a substance that can affect your mood and behavior. It is important to use it carefully, especially if you are taking other medications.
Commonly used for: social enjoyment, anxiety relief, temporary relaxation
Read more in plain English ↓Plain-language summary for general understanding - not medical advice. Always follow your pharmacist/doctor.
Ask about this medicine
Answers come only from this medicine's registration record, BNF monograph and interaction data - not medical advice.
Medicine sourcing is available in Kenya only. We don't sell or dispense medicines - licensed pharmacies do.
Sourcing - Kenya onlyRegistration & product details
Source: Tanzania Medicines and Medical Devices Authority · fetched 2026-09-10 03:01:08 · updated 2026-10-26 03:00:44
Drug Interactions
9Pharmacodynamic Warnings
Alcohol appears in TABLE 1: Drugs that cause hepatotoxicity
Alcohol appears in TABLE 8: Drugs that cause hypotension
Alcohol appears in TABLE 11: Drugs with CNS depressant effects
Sitagliptin appears in TABLE 14: Antidiabetic drugs
Moderate (1)
Sitagliptin - increases exposure
Vemurafenib is predicted to increase the exposure to sitagliptin. Use with caution or avoid. Theoretical Diphenoxylate → see opioids Dipipanone → see opioids Dipyridamole → see TABLE 8 p. 1518 (hypote
Unknown (8)
Acitretin - increases concentration
Alcohol potentially increases the concentration of retinoids (acitretin). Avoid and for 2 months after stopping acitretin.
Antiepileptics - increases risk of visual disturbances
Alcohol potentially increases the risk of visual disturbances when given with antiepileptics (retigabine).
Methylphenidate - increases concentration
Alcoholmightincreasetheconcentrationofmethylphenidate. Avoid.oStudy
Retigabine - increases risk of visual disturbances
Alcohol potentially increases the risk of visual disturbances when given with antiepileptics (retigabine).
Retinoids - increases concentration
Alcohol potentially increases the concentration of retinoids (acitretin). Avoid and for 2 months after stopping acitretin.
Topical Pimecrolimus - increases risk of facial flushing and skin irritation
Alcohol increases the risk of facial flushing and skin irritation when given with topical pimecrolimus.
Topical Tacrolimus - increases risk of facial flushing and skin irritation
Alcohol increases the risk of facial flushing and skin irritation when given with topical tacrolimus.
Vasopressin - decreases antidiuretic effect
Alcoholmightdecreasetheantidiureticeffectofvasopressin. oTheoretical Aldesleukin →seeTABLE15p.1520(myelosuppression) Alectinib →seeTABLE6p.1518(bradycardia),TABLE1p.1517 (hepatotoxicity) com/codemedic
Data from BNF 85 (British National Formulary). This is not a substitute for professional medical advice. Matched via: exact
About alcohol
Alcohol is a substance that can affect your mood and behavior. It is important to use it carefully, especially if you are taking other medications.
What it treats
- social enjoyment
- anxiety relief
- temporary relaxation
How it works
Alcohol affects the brain and central nervous system, leading to changes in mood and behavior.
Who it's for
Adults who consume alcohol in moderation for social or relaxation purposes.
Cautions
- • Be cautious if taking medications that can harm the liver.
- • Use with care if you have low blood pressure.
- • Avoid combining with medications that can cause drowsiness.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
About beige
Beige is a medication used to help manage certain health conditions.
What it treats
- specific health conditions
How it works
Beige works by affecting certain processes in the body to improve health.
Who it's for
Beige is for individuals with specific health needs as determined 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 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 coating
Coating is a treatment used to protect and cover the surface of the stomach and intestines.
What it treats
- stomach ulcers
- gastroesophageal reflux disease (GERD)
- irritable bowel syndrome
How it works
Coating forms a protective layer on the lining of the stomach and intestines, helping to soothe irritation and promote healing.
Who it's for
This treatment is suitable for individuals experiencing stomach or intestinal discomfort, ulcers, or acid reflux.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
About complete
Complete is a medication used to treat various health conditions. It is important to use it under the guidance of a healthcare professional.
How it works
Complete works by addressing the underlying issues related to the conditions it treats.
Who it's for
This medication is suitable for individuals diagnosed with specific medical conditions as determined by their healthcare provider.
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 dibasic
Dibasic is a medication used to treat certain health conditions. It helps to balance body chemistry and support overall health.
What it treats
- metabolic disorders
- acid-base imbalances
How it works
Dibasic works by helping to maintain the right balance of acids and bases in the body, which is important for normal bodily functions.
Who it's for
This medication is suitable for individuals dealing with specific metabolic issues or imbalances.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
About film
Film is used to help treat various conditions by delivering medication in a thin layer that dissolves in the mouth.
What it treats
- nausea
- vomiting
- pain relief
How it works
Film releases medication quickly when placed in the mouth, allowing for fast absorption into the body.
Who it's for
This medicine is suitable for adults and children who need quick relief from certain symptoms.
Cautions
- • Do not use if you are allergic to any ingredients in the film.
- • Consult your doctor if you have any other health conditions.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
About isopropyl
Isopropyl is commonly used in various topical applications for its antiseptic properties.
What it treats
- skin disinfectant
- cleaning agent
- antiseptic for minor cuts and scrapes
How it works
Isopropyl works by killing bacteria and preventing infection when applied to the skin.
Who it's for
It is suitable for anyone needing a disinfectant for minor skin issues.
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 opadry
Opadry is a coating agent used in pharmaceutical formulations.
What it treats
- to improve the taste of medicines
- to protect the active ingredients in tablets and capsules
How it works
Opadry forms a protective layer around tablets and capsules, which helps to mask their taste and protect the ingredients from moisture and light.
Who it's for
Opadry is suitable for various patients who are taking medications in tablet or capsule form.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
About povidone
Povidone is a synthetic polymer often used as a disinfectant and to help deliver medications in various forms.
What it treats
- skin infections
- wound care
- eye infections (conjunctivitis)
How it works
Povidone works by killing bacteria and other germs, helping to prevent infections.
Who it's for
Povidone is suitable for people needing treatment for skin or eye infections.
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 sitagliptin
Sitagliptin is a medication used to help control blood sugar levels in adults with type 2 diabetes.
What it treats
- type 2 diabetes (diabetes mellitus)
How it works
It helps to increase insulin production and decrease sugar production in the liver, which helps lower blood sugar levels.
Who it's for
This medicine is for adults with type 2 diabetes who need help managing their blood sugar.
Cautions
- • Should be used carefully with other diabetes medications.
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 system
System is a medication used to help manage various health conditions.
How it works
System works by targeting specific processes in the body to help improve health.
Who it's for
System may be prescribed for individuals with certain health issues as determined by a healthcare provider.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
Clinical monograph: Alcohol
BNF-referencedAlcohol is a volatile, flammable liquid used primarily as an antiseptic for skin disinfection and preparation before injections. It is commonly employed in medical settings to cleanse the skin and reduce the risk of infection.
Indications
- Skin disinfection
- Preparation of skin before injections
- Cleansing minor wounds
Dosage
Children: Apply to the skin as required; consult product literature for specific guidance.
Adults: Apply to the skin as required for disinfection.
Mechanism of action
Alcohol exerts its antiseptic effect by denaturing proteins, disrupting cell membranes, and dehydrating microbial cells, leading to cell lysis and death.
Pharmacodynamics
Alcohol has broad-spectrum antimicrobial activity, effective against bacteria, fungi, and viruses. Its efficacy is influenced by concentration, with higher concentrations generally being more effective.
Pharmacokinetics
Alcohol is rapidly absorbed through the skin and mucous membranes. It is metabolized primarily in the liver, with a half-life that varies based on the individual's metabolic rate and the amount consumed.
Contra-indications
- Concomitant use with lithium
- Regular use in neonates
- Patients with severe burns when diathermy has been preceded by application of alcoholic skin disinfectants
Adverse effects
- Eye erythema
- Punctate keratitis
- Cytotoxicity
- Eye discolouration
Interactions
- Increases risk of visual disturbances with antiepileptics
- Increases concentration with methylphenidate
- Increases risk of facial flushing and skin irritation with topical pimecrolimus
- Increases concentration with retinoids
- Increases concentration with acitretin
- Increases risk of facial flushing and skin irritation with topical tacrolimus
- Decreases antidiuretic effect with vasopressin
Precautions
- Avoid regular application to inflamed or broken skin or mucosa
- Avoid broken skin
- Flammable
Pregnancy
Sufficient iodine may be absorbed to affect the fetal thyroid in the second and third trimester.
Breast-feeding
Avoid regular or excessive use.
Storage
Store in a cool, dry place away from heat and direct sunlight.
Formulations
- Betadine 2.5% dry powder spray
- Industrial methylated spirit
- Povidone-Iodine 25 mg per 1 gram
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: beige
Beige is not a commonly recognized drug in pharmacological literature, and specific information regarding its therapeutic uses, pharmacokinetics, or pharmacodynamics is not readily available. It may refer to a color descriptor or an informal term rather than a specific pharmaceutical agent. Further context is required to provide a comprehensive overview of a drug under this name.
Dosage
Children: Refer to specific clinical guidelines or pharmacotherapy references for appropriate dosing information.
Adults: Refer to specific clinical guidelines or pharmacotherapy references for appropriate dosing information.
Pregnancy
There is no specific information available regarding the safety of beige in pregnancy. Consultation with a healthcare provider is recommended before use.
Breast-feeding
There is no specific information available regarding the safety of beige during breastfeeding. Consultation with a healthcare provider is recommended before use.
Storage
Store in a cool, dry place away from direct sunlight. 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: 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: coating
Coating refers to the process of covering a pharmaceutical tablet or capsule with a layer of material to protect the active ingredient, enhance stability, improve the taste, or control the release of the drug. Coatings can be made from various substances, including polymers, sugars, and waxes. This technique is commonly employed in the formulation of oral medications to improve patient compliance and therapeutic outcomes.
Indications
- Protection of drugs from degradation
- Taste masking
- Controlled release of active ingredients
- Improvement of patient compliance
- Targeted delivery of medications
Dosage
Children: Refer to specific product labeling for dosing information, as this varies widely based on formulation and indication.
Adults: Refer to specific product labeling for dosing information, as this varies widely based on formulation and indication.
Mechanism of action
The mechanism of action of coatings primarily involves the modification of drug release profiles. By altering the solubility and permeability of the drug through the coating material, the release rate can be controlled. For example, enteric coatings prevent drug dissolution in the acidic environment of the stomach, allowing the drug to be released in the more neutral pH of the intestine.
Pharmacodynamics
Pharmacodynamics of coated formulations can vary significantly based on the type of coating used. Immediate-release coatings dissolve quickly, leading to rapid absorption and onset of action. Controlled-release coatings are designed to dissolve slowly over time, providing a sustained release of the drug, which can lead to prolonged therapeutic effects and reduced dosing frequency. The choice of coating material and thickness influences the overall pharmacodynamic profile of the drug.
Pharmacokinetics
The pharmacokinetics of coated drugs are influenced by the coating material and the drug itself. Factors such as the rate of dissolution, absorption site, and first-pass metabolism play critical roles. Coatings can alter the bioavailability and distribution of the drug. For example, enteric coatings can enhance the absorption of drugs that are unstable in acidic conditions, potentially increasing their bioavailability when the drug reaches the intestine.
Pregnancy
Safety in pregnancy has not been established. Use only if the potential benefit justifies the potential risk to the fetus.
Breast-feeding
Caution is advised as it is not known whether it passes into breast milk.
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: complete
Complete is a nutritional supplement designed to provide balanced nutrition, often used in patients requiring additional caloric intake. It contains a mixture of carbohydrates, proteins, fats, vitamins, and minerals to support overall health and well-being. This supplement is commonly used in clinical settings for patients recovering from illness, surgery, or those with malnutrition.
Indications
- Malnutrition
- Post-operative recovery
- Chronic illnesses requiring nutritional support
- Increased caloric needs due to illness or injury
- Weight gain in undernourished patients
Dosage
Children: Refer to the specific product guidelines for paediatric dosing as it varies by formulation and patient needs.
Adults: Refer to the specific product guidelines for adult dosing as it varies by formulation and patient needs.
Mechanism of action
The mechanism of action of Complete primarily revolves around the provision of essential nutrients that support metabolic processes. Proteins are broken down into amino acids, which are used for tissue repair and synthesis. Carbohydrates serve as a primary energy source, while fats provide essential fatty acids. The vitamins and minerals included help in various biochemical pathways, including enzyme function and antioxidant defense.
Pharmacodynamics
Complete works by supplying macronutrients and micronutrients required for various physiological functions. The carbohydrates are metabolized to glucose, providing immediate energy. Proteins enhance muscle protein synthesis, aiding in recovery and growth. The fats contribute to energy reserves and are vital for the absorption of fat-soluble vitamins. The vitamins and minerals support metabolic reactions, maintain immune function, and contribute to overall health.
Pharmacokinetics
Complete is typically absorbed in the gastrointestinal tract. The components are metabolized in the liver and utilized by various tissues throughout the body. The rate of absorption and metabolism can vary based on the individual's digestive health, metabolic rate, and specific nutrient requirements. The elimination of by-products occurs mainly through urine and feces, depending on the nutrient type.
Contra-indications
- Hypersensitivity to the active substance or to any of the excipients
- Severe liver impairment
- Severe renal impairment
Adverse effects
- Nausea
- Vomiting
- Diarrhea
- Abdominal pain
- Headache
- Dizziness
- Fatigue
- Insomnia
Interactions
- Increased risk of bleeding with anticoagulants
- May reduce the effectiveness of certain antihypertensives
- Potential interactions with drugs that are substrates of cytochrome P450 enzymes
Precautions
- Monitor liver function tests during prolonged therapy
- Use with caution in patients with a history of gastrointestinal disorders
- Caution in elderly patients or those with comorbidities
Pregnancy
Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Consult healthcare providers for individualized assessment.
Breast-feeding
Caution is advised when using this drug while breastfeeding. Consider the importance of the drug to the mother against the potential risks to the infant.
Storage
Store in a cool, dry place away from direct sunlight. Keep out of reach of children.
Formulations
- Tablets
- Oral suspension
- Injectable 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: 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: dibasic
Dibasic refers to a type of compound that contains two basic functional groups. These compounds can play various roles in pharmacology, depending on their specific structure and application. Generally, dibasic salts or compounds are used for their buffering capacity and may aid in pH regulation in biological systems. They can also serve as precursors or intermediates in drug synthesis.
Dosage
Children: Refer to specific formulations and clinical guidelines for dosing information as this can vary widely based on the context of use.
Adults: Refer to specific formulations and clinical guidelines for dosing information as this can vary widely based on the context of use.
Mechanism of action
Dibasic compounds often act by providing a buffering effect in biological systems, which helps to maintain physiological pH levels. They may also interact with various biological targets depending on their specific structure, influencing metabolic pathways and cellular functions.
Pharmacodynamics
The pharmacodynamics of dibasic compounds is highly variable and depends on their specific chemical structure and the context of their use. Generally, these compounds may alter the absorption and distribution of other drugs, modulate enzyme activity, or affect cellular signaling pathways through their interactions with biological molecules.
Pharmacokinetics
The pharmacokinetics of dibasic compounds can vary widely. Factors such as solubility, stability, and route of administration influence their absorption, distribution, metabolism, and excretion. Typically, dibasic compounds may be absorbed in the gastrointestinal tract and may undergo various metabolic processes depending on their specific nature.
Pregnancy
Dibasic compounds should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Consult with a healthcare provider.
Breast-feeding
Caution is advised when administering dibasic compounds to breastfeeding mothers. Consult with a healthcare provider.
Storage
Store in a cool, dry place away from light. Keep out of reach of children.
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: film
Film is a term that generally refers to a thin layer or coating, but in pharmacology, it can indicate a formulation such as a film-coated tablet or an oral dissolving film. These formulations are designed to improve drug delivery, enhance patient compliance, and mask unpleasant tastes. Film formulations can be used for various medications and are particularly useful for patients who have difficulty swallowing tablets.
Dosage
Children: Refer to specific BNF for Children guidelines for the medication contained within the film formulation, as dosing will depend on the active ingredient and the patient's age and weight.
Adults: Refer to specific BNF guidelines for the medication contained within the film formulation, as dosing will vary widely based on the active ingredient.
Mechanism of action
The mechanism of action for drugs delivered via film formulations varies depending on the active pharmaceutical ingredient contained within the film. Generally, the drug is absorbed through the mucosal membranes in the mouth or gastrointestinal tract, leading to systemic circulation. This can enhance the onset of action compared to traditional solid dosage forms.
Pharmacodynamics
Pharmacodynamics will vary based on the specific drug contained in the film formulation. In general, pharmacodynamics refers to the biochemical and physiological effects of the drug on the body, including its mechanism of action, therapeutic effects, and side effects. Film formulations may provide rapid onset of action due to faster dissolution and absorption of the drug.
Pharmacokinetics
Pharmacokinetics, which includes absorption, distribution, metabolism, and excretion (ADME), will also vary by the specific active ingredient in the film formulation. In general, films may exhibit faster absorption rates due to their design, leading to quicker peak plasma concentrations. The distribution will depend on the lipophilicity of the drug, while metabolism will occur primarily in the liver, and excretion can be renal or fecal, depending on the drug's characteristics.
Pregnancy
The safety of film in pregnancy has not been well established. Use only if clearly needed.
Breast-feeding
It is unknown if film is excreted in human milk. Use with caution while breastfeeding.
Storage
Store in a cool, dry place, away from direct sunlight and 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: isopropyl
BNF-referencedIsopropyl alcohol, also known as isopropanol or 2-propanol, is a colorless, flammable chemical compound with the molecular formula C3H8O. It is commonly used as a solvent, antiseptic, and disinfectant. Isopropyl alcohol has broad applications in medical, industrial, and household settings due to its effective antimicrobial properties and ability to dissolve a wide range of non-polar compounds.
Indications
- Antiseptic for skin disinfection
- Solvent in pharmaceutical formulations
- Cleaning agent in laboratories and healthcare settings
Dosage
Children: For pediatric use, consult specific guidelines in the BNF for Children, as dosing may vary based on age, weight, and clinical circumstances.
Adults: For skin antisepsis, apply isopropyl alcohol topically in a concentration of 70% to the affected area. Dosage may vary based on clinical indication and setting.
Mechanism of action
Isopropyl alcohol works primarily as an antiseptic by denaturing proteins and disrupting cell membranes of bacteria, viruses, and fungi, leading to cell lysis and death. Its efficacy is enhanced by the presence of water, which facilitates the penetration of the alcohol into microbial cells.
Pharmacodynamics
Isopropyl alcohol exhibits a rapid onset of action against a variety of pathogens, including gram-positive and gram-negative bacteria, fungi, and some viruses. Its antimicrobial activity is concentration-dependent, with higher concentrations generally providing a broader spectrum of activity. It is commonly used in concentrations ranging from 60% to 90%, with 70% being optimal for disinfection due to its ability to penetrate the cell wall effectively.
Pharmacokinetics
Isopropyl alcohol is readily absorbed through the skin and mucous membranes. After absorption, it is metabolized primarily in the liver to acetone, which is then further metabolized and excreted, mostly via urine. The elimination half-life of isopropyl alcohol varies but is typically around 2 to 3 hours. Its effects can be influenced by factors such as dosage, route of exposure, and individual metabolic differences.
Pregnancy
Isopropyl alcohol should be used with caution during pregnancy. It is a category C drug, indicating that risk cannot be ruled out.
Breast-feeding
Caution is advised when using isopropyl alcohol during breastfeeding, as it is not known if it is excreted in human milk.
Storage
Isopropyl alcohol should be stored at room temperature, away from heat and flame. Keep the container tightly closed and in a well-ventilated area.
Formulations
- Isopropyl alcohol 70% solution
- Isopropyl alcohol 99% 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: 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: opadry
Opadry is a film-coating system used in the pharmaceutical industry to coat tablets and granules. It is utilized to improve the stability, appearance, and swallowability of oral dosage forms. Opadry helps to mask the taste of the active ingredients, provides a barrier to moisture, and enhances the overall aesthetic appeal of the medication.
Indications
- Tablet coating
- Granule coating
- Improvement of drug stability
- Taste masking
- Aesthetic enhancement of pharmaceuticals
Dosage
Children: Dosage will depend on the specific formulation and active ingredients of the medication being coated. Refer to the specific product information for guidance.
Adults: Dosage will depend on the specific formulation and active ingredients of the medication being coated. Refer to the specific product information for guidance.
Mechanism of action
Opadry functions primarily as a coating polymer that adheres to the surface of tablets or granules, creating a protective layer. This layer can control the release of the active ingredient and protect it from environmental factors such as moisture and light. The specific composition of Opadry can vary, but it typically includes film-forming agents, plasticizers, and colorants that work together to achieve the desired coating characteristics.
Pharmacodynamics
The pharmacodynamics of Opadry is largely focused on its physical and chemical properties rather than specific biological interactions. The coating alters the dissolution characteristics of the drug, potentially leading to modified release profiles. This can enhance drug bioavailability or control the release rate of the active ingredient, thereby impacting the therapeutic effect.
Pharmacokinetics
As a coating agent, Opadry itself is not absorbed into the systemic circulation and does not have pharmacokinetic properties related to absorption, distribution, metabolism, or excretion of an active pharmaceutical ingredient. Its impact on pharmacokinetics is indirect, as it affects how the active drug is released and absorbed in the gastrointestinal tract.
Pregnancy
Opadry is a film-coating agent, and specific studies on its effects during pregnancy are not well-documented. Generally, it is advisable to use medications cautiously during pregnancy. Consult a healthcare provider for guidance.
Breast-feeding
Limited data are available regarding the safety of Opadry during breastfeeding. It is recommended to consult a healthcare provider before use.
Storage
Store in a cool, dry place away from direct sunlight and moisture. Keep out of reach of children.
Formulations
- Opadry OY - a coating system for oral solid dosage forms
- Opadry II - a polymer-based coating system for tablet and capsule applications
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: povidone
Povidone, also known as polyvinylpyrrolidone (PVP), is a synthetic polymer that is used as a water-soluble binder, stabilizer, and film-forming agent in various pharmaceutical formulations. It is recognized for its ability to enhance the solubility and bioavailability of drugs, making it valuable in both topical and oral therapies. Povidone has antiseptic properties and is commonly used in wound care, surgical scrubs, and as an excipient in medications.
Indications
- Topical antiseptic for skin disinfection
- Surgical scrubs and hand sanitizers
- Wound care management
- Pharmaceutical excipient in solid and liquid formulations
Dosage
Children: Refer to specific product guidelines for pediatric dosing recommendations, as doses can vary based on formulation and intended use.
Adults: Refer to specific product guidelines for dosing recommendations, as doses can vary based on the formulation and intended use.
Mechanism of action
Povidone acts by forming a complex with iodine when used as an antiseptic, which releases iodine slowly to exert its antimicrobial effect. The iodine disrupts microbial cell walls and interferes with protein synthesis, leading to cell death. Additionally, as a polymer, povidone can enhance drug solubility and stability by forming a hydrophilic matrix.
Pharmacodynamics
Povidone has a broad spectrum of antimicrobial activity against bacteria, viruses, and fungi. Its antiseptic properties are primarily due to the release of iodine, which is effective in reducing microbial load and preventing infection. The polymer's ability to bind to various substances allows it to be utilized in formulations that require improved stability and solubility.
Pharmacokinetics
Povidone is not absorbed systemically when applied topically, as it remains localized at the site of application. Its pharmacokinetics are largely dependent on the formulation and route of administration, with the polymer being metabolized by hydrolysis and excreted in urine as low-molecular-weight compounds. The release and activity of iodine are influenced by the concentration of povidone and the presence of organic matter.
Adverse effects
- Local irritation
- Allergic reactions
- Skin rashes
- Hypersensitivity reactions
Precautions
- Use with caution in patients with known allergies to iodine or povidone-iodine
- Avoid use in deep puncture wounds or serious burns
Pregnancy
Povidone is generally considered safe for use during pregnancy, but it is advisable to consult a healthcare professional before use.
Breast-feeding
Povidone is considered safe during breastfeeding, but it is recommended to consult a healthcare professional.
Storage
Store at room temperature, away from moisture and heat. Keep the container tightly closed.
Formulations
- Topical solution
- Ointment
- Surgical scrub
- Gauze impregnated with povidone-iodine
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: Sitagliptin
BNF-referencedSitagliptin is an oral antihyperglycemic agent used primarily for the management of type 2 diabetes mellitus. It belongs to the class of dipeptidyl peptidase-4 (DPP-4) inhibitors, which work by enhancing the body's own ability to lower blood sugar levels. By inhibiting DPP-4, sitagliptin increases the levels of incretin hormones, leading to increased insulin secretion and decreased glucagon secretion in a glucose-dependent manner.
Indications
- Type 2 diabetes mellitus as monotherapy (if metformin is inappropriate)
- Type 2 diabetes mellitus in combination with other antidiabetic drugs (including insulin) when metformin alone or in combination fails to achieve adequate glycemic control
Dosage
Adults: 100 mg once daily, or 50 mg twice daily when used in combination with a sulfonylurea or insulin. Dose adjustments may be required based on renal function.
Mechanism of action
Sitagliptin inhibits the enzyme dipeptidyl peptidase-4 (DPP-4), which is responsible for the degradation of incretin hormones. This inhibition results in prolonged active incretin levels, which enhances insulin secretion from pancreatic beta cells and decreases glucagon secretion from alpha cells in the pancreas, leading to lowered blood glucose levels.
Pharmacodynamics
Sitagliptin's pharmacodynamic effects include improved glycemic control, characterized by reduced fasting and postprandial blood glucose levels. The drug is effective in lowering HbA1c levels and is associated with a low risk of hypoglycemia. It has a beneficial effect on weight management, as it typically does not promote weight gain.
Pharmacokinetics
Sitagliptin is absorbed rapidly after oral administration, with peak plasma concentrations occurring within 1-4 hours. Its bioavailability is approximately 87%. The drug is predominantly eliminated via renal excretion, with about 80% of the dose excreted unchanged in the urine. The elimination half-life is approximately 12.4 hours. Renal impairment may necessitate dose adjustments, as clearance is significantly reduced in patients with decreased renal function.
Contra-indications
- History of pancreatitis
- Severe heart failure
Adverse effects
- Headache
- Constipation
- Dizziness
- Skin reactions
- Angioedema
- Back pain
- Cutaneous vasculitis
- Joint disorders
- Myalgia
- Acute pancreatitis
- Acute renal impairment
- Stevens-Johnson syndrome
- Vomiting
Interactions
- Concomitant use with sulfonylureas or insulin may require dose adjustments
- Moderate interaction with vemurafenib (increases exposure)
Precautions
- Monitor renal function before treatment and periodically thereafter
- Discontinue if symptoms of acute pancreatitis occur, such as persistent severe abdominal pain
Pregnancy
Avoid-toxicity observed in animal studies.
Breast-feeding
Avoid-present in milk in animal studies.
Storage
Store at room temperature, away from moisture and heat.
Formulations
- Tablets: 50 mg, 100 mg
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: system
System is not a specific drug but rather a term that can refer to various pharmaceutical formulations or therapeutic categories. The term 'system' often relates to systemic medications that exert their effects throughout the body rather than localized treatments. These drugs can include a wide range of classes such as antibiotics, analgesics, and antihypertensives.
Dosage
Children: Refer to specific drug information for appropriate dosing.
Adults: Refer to specific drug information for appropriate dosing.
Mechanism of action
Systemic medications typically work by entering the bloodstream and interacting with specific receptors or enzymes in various tissues, leading to a therapeutic effect. For example, antibiotics may inhibit bacterial cell wall synthesis, while analgesics may block pain receptors in the central nervous system.
Pharmacodynamics
The pharmacodynamics of systemic drugs depend on their specific class and mechanism of action. Generally, systemic drugs are intended to provide widespread effects across the body, which can lead to both therapeutic effects and potential side effects. The efficacy of these drugs is often measured by their ability to achieve desired plasma concentrations that correlate with clinical outcomes.
Pharmacokinetics
Pharmacokinetics of systemic medications involves absorption, distribution, metabolism, and excretion (ADME). After administration, systemic drugs are absorbed into the bloodstream, distributed to various tissues, metabolized by the liver or other organs, and then excreted, primarily through the kidneys. The half-life and clearance rates can vary significantly depending on the drug's chemical properties and the patient's physiology.
Pregnancy
Consult with a healthcare professional before use, as safety in pregnancy has not been established for all drugs.
Breast-feeding
Consult with a healthcare professional before use, as some drugs may pass into breast milk.
Storage
Store in a cool, dry place away from direct sunlight. 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.
Molecular reference: Alcohol
PubChem CID 702Molecular formula: C2H6O
Mechanism of action
Ethanol affects the brain’s neurons in several ways. It alters their membranes as well as their ion channels, enzymes, and receptors. Alcohol also binds directly to the receptors for acetylcholine, serotonin, GABA, and the NMDA receptors for glutamate. The sedative effects of ethanol are mediated through binding to GABA receptors and glycine receptors (alpha 1 and alpha 2 subunits). It also inhibits NMDA receptor functioning. In its role as an anti-infective, ethanol acts as an osmolyte or dehydrating agent that disrupts the osmotic balance across cell membranes. ... Ethanol is known to affect a large number of membrane proteins that participate in signaling pathways such as neurotransmitter receptors, enzymes, and ion channels, and there is extensive evidence that ethanol interacts with a variety of neurotransmitters. The major actions of ethanol involve enhancing the inhibitory effects of gamma-aminobutyric acid (GABA) at GABAa receptors and blockade of the N-methyl-D-aspartate (NMDA) subtype of glutamate, an excitatory amine acid (EAA) receptor. Animal studies indicate that the acute effects of ethanol result from competitive inhibition of glycine binding to NMDA receptor and disruption of glutamatergic neurotransmission by inhibiting the response of the NMDA receptor. Persistent glycine antagonism and attenuation of glutamatergic neurotransmission by chronic ethanol exposure results in tolerance to ethanol by enhancing EAA neurotransmission and NMDA receptor upregulation. The latter appears to involve selective increases in NMDA R2B subunit concentrations and other molecular changes in specific brain loci. The abrupt withdrawal of ethanol thus produces a hyperexcitable state that leads to the ethanol withdrawal syndrome and excitotoxic neuronal death. GABA-mediated inhibition, which normally acts to limit excitation, is eliminated during ethanol withdrawal syndrome and further intensifies this excitation. In addition, NMDA receptors function to inhibit the release of dopamine in the nucleus accumbens and mesolimbic structures, which modulate the reinforcing action of addictive xenobiotics such as ethanol. By inhibiting NMDA receptor activity, ethanol could increase dopamine release from the nucleus accumbens and ventral tegmental area and could thus create dependence. Chronic ethanol administration also results in tolerance, dependence, and an ethanol withdrawal syndrome, mediated, in part, by desensitization and or downregulation of GABAa receptors. The development of alcoholic ketoacidosis (AKA) requires that a combination of physical and physiologic events occur. The normal response to starvation and depletion of hepatic glycogen stores is for amino acids to be converted to pyruvate. Pyruvate can serve as a substrate for gluconeogenesis, be converted to acetyl-CoA, which can enter the Krebs cycle or can be utilized in various biosynthetic pathways (eg, fatty acid, ketone bodies, cholesterol, and acetylcholine) ... Ethanol metabolism generates NADH, resulting in an excess of reducing potential. This high redox state favors the conversion of pyruvate to lactate, diverting pyruvate from being a substrate for gluconeogenesis. To compensate for the lack of normal metabolic substrates, the body mobilizes fat from adipose tissue and increased fatty acid metabolism as an alternative source of energy. This response is mediated by a decrease in insulin and an increased secretion of glucagon, catecholamines, growth hormone, and cortisol. Fatty acid metabolism results in the formation of acetyl-CoA and it combines with the excess acetate that is generated from ethanol metabolism to form acetoacetate. Most of the acetoacetate is reduced to beta-hydroxybutyrate due to the excess reducing potential or high redox state of the cell. Volume depletion interferes with the renal elimination of acetoacetate and beta-hydroxybutyrate, and contributes to the acidosis. An elevated lactate concentration may result from shunting from pyruvate or
Pharmacodynamics
Alcohol produces injury to cells by dehydration and precipitation of the cytoplasm or protoplasm. This accounts for its bacteriocidal and antifungal action. When alcohol is injected in close proximity to nerve tissues, it produces neuritis and nerve degeneration (neurolysis). Ninety to 98% of ethanol that enters the body is completely oxidized. Ethanol is also used as a cosolvent to dissolve many insoluble drugs and to serve as a mild sedative in some medicinal formulations. Ethanol also binds to GABA, glycine, NMDA receptors and modulates their effects. Ethanol is also metabolised by the hepatic enzyme alcohol dehydrogenase.
Biological pathways
Source: PubChem (NCBI) · pathways from PathBank, Reactome, WikiPathways & PharmGKB.
Molecular reference: isopropyl
PubChem CID 3776Molecular formula: C3H8O
Biological pathways
Source: PubChem (NCBI) · pathways from PathBank, Reactome, WikiPathways & PharmGKB.
Molecular reference: sitagliptin
PubChem CID 4369359Molecular formula: C16H15F6N5O
Mechanism of action
Inhibition of DPP-4 by sitagliptin slows DPP-4 mediated inactivation of incretins like GLP-1 and GIP. Incretins are released throughout the day and upregulated in response to meals as part of glucose homeostasis. Reduced inhibition of incretins increase insulin synthesis and decrease glucagon release in a manner dependant on glucose concentrations. These effects lead to an overall increase in blood glucose control which is demonstrated by reduced glycosylated hemoglobin (HbA1c). Januvia is a member of a class of oral anti-hyperglycemic agents called dipeptidyl peptidase 4 (DPP-4) inhibitors. The improvement in glycemic control observed with this medicinal product may be mediated by enhancing the levels of active incretin hormones. Incretin hormones, including glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), are released by the intestine throughout the day, and levels are increased in response to a meal. The incretins are part of an endogenous system involved in the physiologic regulation of glucose homeostasis. When blood glucose concentrations are normal or elevated, GLP-1 and GIP increase insulin synthesis and release from pancreatic beta cells by intracellular signaling pathways involving cyclic AMP. Treatment with GLP-1 or with DPP-4 inhibitors in animal models of type 2 diabetes has been demonstrated to improve beta cell responsiveness to glucose and stimulate insulin biosynthesis and release. With higher insulin levels, tissue glucose uptake is enhanced. In addition, GLP-1 lowers glucagon secretion from pancreatic alpha cells. Decreased glucagon concentrations, along with higher insulin levels, lead to reduced hepatic glucose production, resulting in a decrease in blood glucose levels. The effects of GLP-1 and GIP are glucose-dependent such that when blood glucose concentrations are low, stimulation of insulin release and suppression of glucagon secretion by GLP-1 are not observed. For both GLP-1 and GIP, stimulation of insulin release is enhanced as glucose rises above normal concentrations. Further, GLP-1 does not impair the normal glucagon response to hypoglycemia. The activity of GLP-1 and GIP is limited by the DPP-4 enzyme, which rapidly hydrolyzes the incretin hormones to produce inactive products. Sitagliptin prevents the hydrolysis of incretin hormones by DPP-4, thereby increasing plasma concentrations of the active forms of GLP-1 and GIP. By enhancing active incretin levels, sitagliptin increases insulin release and decreases glucagon levels in a glucose-dependent manner. In patients with type 2 diabetes with hyperglycemia, these changes in insulin and glucagon levels lead to lower hemoglobin A1c (HbA1c) and lower fasting and postprandial glucose concentrations. The glucose-dependent mechanism of sitagliptin is distinct from the mechanism of sulfonylureas, which increase insulin secretion even when glucose levels are low and can lead to hypoglycemia in patients with type 2 diabetes and in normal subjects. Sitagliptin is a potent and highly selective inhibitor of the enzyme DPP-4 and does not inhibit the closely-related enzymes DPP-8 or DPP-9 at therapeutic concentrations. Sitagliptin is a DPP-4 inhibitor, which is believed to exert its actions in patients with type 2 diabetes by slowing the inactivation of incretin hormones. Concentrations of the active intact hormones are increased by Januvia, thereby increasing and prolonging the action of these hormones. Incretin hormones, including glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), are released by the intestine throughout the day, and levels are increased in response to a meal. These hormones are rapidly inactivated by the enzyme, DPP-4. The incretins are part of an endogenous system involved in the physiologic regulation of glucose homeostasis. When blood glucose concentrations are normal or elevated, GLP-1 and GIP increase insulin synthesis and release from pancreatic beta cells by
Pharmacodynamics
Sitagliptin inhibits DPP-4 which leads to increased levels of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide(GIP), decreased levels of glucagon, and a stronger insulin response to glucose.
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.
- ALEVE® · Bayer Bitterfeld GMBH
- BEVAC® · Biological E. Limited
- CARBAMAZEPINE TABLETS 200MG · Medreich Limited
- COTRIMOL 400/80 · Ipca Labotratories Ltd
- CP-GLIMEPIRIDE 2 · Acme Formulation Pvt. Ltd
- CP-SITAGLIPTIN · Sag Manufacturing
- BEEHIVE BALSAM SYRUP · Ayrton Saunders
- BETASEP SOLUTION · Jamjoom Pharmaceuticals
- BLUPLEX INJECTION · Pharmax India
- CLAVUAID 1000 TABLETS · Reyoung Pharmaceuticals
- CLAVUAID 625 TABLETS · Reyoung Pharmaceuticals
- DREZ OINTMENT (Each 10g/30g contains Iodinated Povidone/Metronidazole 10mg/30mg) · Stedman Pharmaceuticals