clotrimazole

Action and Spectrum

Actions and spectrum: 

clotrimazole is an antifungal medication that works by inhibiting the growth of fungi. It is used to treat various fungal infections, including those caused by Candida and dermatophytes. clotrimazole has a broad spectrum of activity and can be effective against a range of fungal species.

It is available in creams, powders, and solutions, for topical application. clotrimazole works by disrupting the cell membrane of the fungus, leading to its death. 

Drug Interaction

Adverse Reaction

Frequency defined 

1-10% 

Mild burning, vaginal area or stinging to skin, irritation,  

vomiting/ Nausea (troches)  

>10% 

Abnormal LFTs 

Black Box Warning

Black Box Warning: 

clotrimazole does not have a black box warning. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

clotrimazole is contraindicated in individuals with a known hypersensitivity or allergy to clotrimazole or any of its components. It is important to see the product labeling or consult with a healthcare professional for specific contraindications related to a particular formulation or product containing clotrimazole. Additionally, clotrimazole should not be used in the eyes, ears, or intravaginally unless specifically prescribed by a healthcare professional.  

Caution: 

• Hypersensitivity reactions: Although rare, some individuals may develop allergic reactions to clotrimazole.  
• Skin irritation: clotrimazole may cause skin irritation in some individuals, especially if used in excessive amounts or for prolonged periods. It is advisable to use the medication as directed and discontinue use if significant irritation or rash develops. 
• Drug interactions: clotrimazole may interact with other medications, including those taken orally or applied topically.  
• Pregnancy and lactation: The safety of clotrimazole use during pregnancy and breastfeeding is not well-established. 
• Pre-existing medical conditions: Individuals with certain medical conditions, such as immune system disorders or liver disease, may require special caution when using clotrimazole.

Comorbidities: 

• Diabetes: Individuals with diabetes may be at an increased risk of developing fungal infections, and proper glucose control is important for effective treatment.  
• Immune system disorders: Patients with weakened immune systems, such as those with HIV/AIDS, organ transplant recipients, or individuals undergoing chemotherapy, may be more susceptible to fungal infections. Close monitoring and appropriate management of these conditions are essential when using clotrimazole. 
• Allergies or sensitivities: Individuals with known allergies or sensitivities to clotrimazole or other antifungal medications should exercise caution and consult a healthcare professional before using clotrimazole. 
• Open wounds or broken skin: clotrimazole should not be applied on open wounds or broken skin as it may cause irritation or delay wound healing.

Pregnancy / Lactation

Pregnancy consideration: </b>pregnancy category B   

Lactation: N/A  

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.   
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

clotrimazole is an antifungal medication that belongs to the azole class of drugs. It acts by inhibiting the ergosterol synthesis, a crucial component of the fungal cell membrane. By interfering with ergosterol production, clotrimazole disrupts the integrity and function of the fungal cell membrane, leading to the death of the fungus. 

clotrimazole has a broad spectrum of activity against various fungal organisms, including dermatophytes (such as Trichophyton, Microsporum, and Epidermophyton species), yeasts (such as Candida species), and some other fungi. It is primarily used topically, meaning it is applied directly to the affected skin or mucous membranes.  

Pharmacodynamics: 

The pharmacodynamics of clotrimazole involve its mechanism of action and its effects on the body. 

clotrimazole belongs to the azole class of antifungal drugs. It exerts pharmacological effects by inhibiting the ergosterol synthesis, a vital component of the fungal cell membrane. Ergosterol is essential for the structural integrity and proper functioning of the fungal cell membrane. By blocking the synthesis of ergosterol, clotrimazole disrupts the fungal cell membrane, leading to increased permeability and leakage of essential cellular components. This disruption ultimately results in the death of the fungus. 

In addition to its action against fungal organisms, clotrimazole also possesses mild anti-inflammatory properties. It can reduce inflammation and relieve associated symptoms, such as itching and redness, commonly observed in fungal infections.  

Pharmacokinetics: 

Absorption 

clotrimazole is available in various formulations, including creams, lotions, powders, and oral tablets. When applied topically, clotrimazole is minimally absorbed through the skin or mucous membranes. It primarily acts locally at the site of application. Oral clotrimazole is rapidly and almost completely absorbed from the gastrointestinal tract. 

Distribution 

clotrimazole has a low plasma protein binding, which allows it to distribute widely throughout the body. However, after topical application, clotrimazole remains mainly localized at the site of application and does not exhibit significant systemic distribution. 

Metabolism 

clotrimazole undergoes extensive hepatic metabolism through cytochrome P450 enzymes, primarily CYP3A4. It undergoes biotransformation to inactive metabolites. The metabolites are primarily excreted in the feces. 

Elimination and excretion 

The majority of clotrimazole and its metabolites are excreted in the feces. Renal excretion is minimal. 

Adminstartion

Administration: 

• Topical Cream/Lotion/Powder: Apply a thin layer of the cream, lotion, or powder to the affected area of the skin. Gently rub it in until it gets absorbed. Wash hands before and after the application, unless the hands are the affected area. 
• Vaginal Cream/Suppository: Follow the instructions provided with the product. It may involve inserting the cream or suppository deep into the vagina using an applicator. It is usually recommended to use these formulations at bedtime to allow for maximum absorption. 
• Oral Lozenge/Tablet: Place the lozenge or tablet in the mouth and allow it to slowly dissolve. Avoid chewing or swallowing it whole. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: clotrimazole 

Pronounced: [ kloe-TRIM-a-zole ]  

Why do we use clotrimazole? 

• Treatment of Fungal Infections: clotrimazole is primarily used to treat fungal infections and yeast infections. It helps to relieve itching, redness, and discomfort associated with these infections. 
• Vaginal Yeast Infections: clotrimazole is also used for the treatment of vaginal yeast infections. It can be administered as cream or suppository directly into the vagina. 
• Oral Thrush: clotrimazole can be used to treat oral thrush, a fungal infection that affects the mouth and throat. It is typically available as a lozenge or oral tablet for this purpose. 
• Prevention of Fungal Infections: In some cases, clotrimazole may be used as preventive measure to reduce the risk of fungal infections, especially in individuals with a higher susceptibility to such infections.