CLOTRIMAZOLE

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CLOTRIMAZOLE

Clotrimazole 1

1.       TYPE OF DRUG- CLOTRIMAZOLE
Azoles (specifically imidazole)

 

2.       INDICATIONS (USE) – CLOTRIMAZOLE
For the local treatment of oropharyngeal candidiasis and vaginal yeast infections, also used in fungal infections of the skin such as ringworm, athlete’s foot, and jock itch.

 

3.       MECHANISM OF ACTION (MOA) – CLOTRIMAZOLE
Clotrimazole interacts with yeast 14-α demethylase, a cytochrome P-450 enzyme that converts lanosterol to ergosterol, an essential component of the membrane. In this way, clotrimazole inhibits ergosterol synthesis, resulting in increased cellular permeability. Clotrimazole may also inhibit endogenous respiration, interact with membrane phospholipids, inhibit the transformation of yeasts to mycelial forms and the uptake of purine, impair triglyceride and/or phospholipid biosynthesis, and inhibit the movement of calcium and potassium ions across the cell membrane by blocking the ion transport pathway known as the Gardos channel.

 

4.       ROUTES OF ADMINISTRATION- CLOTRIMAZOLE
  • Cream, topical: 1% (15g, 30g, 45g, 90g)
  • Cream, vaginal:  1% (45g, 90g), 2% (25g)
  • Lotion: 1% (30 mL)
  • Solution, topical: 1% (10 mL, 30 mL)
  • Tablet, vaginal:  100mg, 200mg, 500mg
  • Troche: 10mg

 

5.       ONSET OF EFFECT OR ACTION- CLOTRIMAZOLE
Within 2-3 days

 

6.     DOSAGE (DOSING INFORMATION) – CLOTRIMAZOLE
Adults and children > 3 years:

Troche:  10 mg troche dissolved 5 times/day for 14 days.

 

7.       HALF LIFE (DURATION OF ACTION) – CLOTRIMAZOLE
Upto 12 hrs.

 

8.       ADVERSE EFFECTS OR SIDE EFFECTS – CLOTRIMAZOLE
The most common side effects of clotrimazole are redness, blistering, peeling, stinging, swelling, itching, hives, or burning at the site of application. Clotrimazole may also cause stomach pain, nausea, vomiting, fever, or foul-smelling discharge

 

9.       CONTRAINDICATIONS – CLOTRIMAZOLE
Hypersensitivity to imidazole. First trimester of pregnancy.

 

10.   DRUG INTERACTIONS – CLOTRIMAZOLE
There are no known significant drug interactions with topical clotrimazole. However, with oral (troche) clotrimazole, there are multiple interactions as the medication is a CYP450 enzyme inhibitor, primarily CYP3A4. Thus, any medication that is metabolized by the CYP3A4 enzyme will potentially have elevated levels when oral clotrimazole is used. The prescribing physician should be aware of any medication the patient is taking prior to starting oral clotrimazole. Certain medications should not be taken with oral clotrimazole.

 

11.     EXCRETION- CLOTRIMAZOLE
Only 0.5% or less of the applied radioactivity was excreted in the urine.

 

 

Clotrimazole 2

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