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Medication Safety Issues
Sound-alike/look-alike issues:
Miconazole may be confused with Micronase®, Micronor®
Lotrimin® may be confused with Lotrisone®, Otrivin®
Micatin® may be confused with Miacalcin®
Pronunciation
(mi KON a zole)
U.S. Brand Names
Index Terms
Generic Available
Yes
Canadian Brand Names
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Treatment of vulvovaginal candidiasis and a variety of skin and mucous membrane fungal infections
Pregnancy Risk Factor
C
Lactation
Excretion in breast milk unknown/use caution
Contraindications
Hypersensitivity to miconazole or any component of the formulation
Warnings/Precautions
Concerns related to adverse effects:
• Irritation: Discontinue if sensitivity or irritation occurs.
Special populations:
• Pediatrics: Topical products are not for self-medication (OTC use) in children <2 years of age; vaginal products are not for OTC use in children <12 years of age.
Dosage form specific issues:
• Fungoid® tincture: Patients with diabetes, circulatory problems, renal or hepatic dysfunction should contact healthcare provider prior to self-medication (OTC use).
• Petrolatum-based: Vaginal products are petrolatum-based and may damage rubber or latex condoms or diaphragms; separate use by 3 days.
• Vaginal products: Consult with healthcare provider prior to self-medication (OTC use) if experiencing vaginal itching/discomfort, lower abdominal pain, back or shoulder pain, chills, nausea, vomiting, foul-smelling discharge, if this is the first vaginal yeast infection, or if exposed to HIV. Contact healthcare provider if symptoms do not begin to improve after 3 days or last longer than 7 days. May damage condoms or diaphragms.
Other warnings/precautions:
• Appropriate use: For topical use only; avoid contact with eyes.
Adverse Reactions
Frequency not defined.
Topical: Allergic contact dermatitis, burning, maceration
Vaginal: Abdominal cramps, burning, irritation, itching
Metabolism/Transport Effects
Substrate of CYP3A4 (major); Inhibits CYP1A2 (moderate), 2A6 (strong), 2B6 (weak), 2C9 (strong), 2C19 (strong), 2D6 (strong), 2E1 (moderate), 3A4 (strong)
Drug Interactions
Alfentanil: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Alfentanil. Risk D: Consider therapy modification
Alosetron: CYP3A4 Inhibitors (Strong) may increase the serum concentration of Alosetron. Risk C: Monitor therapy
Aprepitant: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Aprepitant. Risk C: Monitor therapy
Benzodiazepines (metabolized by oxidation): Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Benzodiazepines (metabolized by oxidation). Exceptions: Quazepam. Risk D: Consider therapy modification
Bosentan: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Bosentan. Risk C: Monitor therapy
BusPIRone: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of BusPIRone. Risk D: Consider therapy modification
Busulfan: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Busulfan. Risk C: Monitor therapy
Calcium Channel Blockers: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Calcium Channel Blockers. Risk D: Consider therapy modification
Carbamazepine: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Carbamazepine. Risk C: Monitor therapy
Ciclesonide: CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ciclesonide. Specifically, concentrations of the active des-ciclesonide metabolite may be increased. Risk C: Monitor therapy
Cilostazol: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Cilostazol. Risk D: Consider therapy modification
Cinacalcet: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Cinacalcet. Risk C: Monitor therapy
Cisapride: Antifungal Agents (Azole Derivatives, Systemic) may increase the serum concentration of Cisapride. Risk X: Avoid combination
Codeine: CYP2D6 Inhibitors (Strong) may diminish the therapeutic effect of Codeine. These CYP2D6 inhibitors may prevent the metabolic conversion of codeine to its active metabolite morphine. Risk D: Consider therapy modification
Conivaptan: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Conivaptan. Risk X: Avoid combination
Corticosteroids (Orally Inhaled): Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Corticosteroids (Orally Inhaled). Exceptions: Beclomethasone; Flunisolide; Triamcinolone. Risk C: Monitor therapy
Corticosteroids (Systemic): Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Corticosteroids (Systemic). Risk C: Monitor therapy
Coumarin Derivatives: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Coumarin Derivatives. Risk D: Consider therapy modification
CycloSPORINE: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of CycloSPORINE. Risk D: Consider therapy modification
CYP1A2 Substrates: CYP1A2 Inhibitors (Moderate) may decrease the metabolism of CYP1A2 Substrates. Risk C: Monitor therapy
CYP2A6 Substrates: CYP2A6 Inhibitors (Strong) may decrease the metabolism of CYP2A6 Substrates. Risk D: Consider therapy modification
CYP2B6 Substrates: CYP2B6 Inhibitors (Strong) may decrease the metabolism of CYP2B6 Substrates. Risk D: Consider therapy modification
CYP2C19 Substrates: CYP2C19 Inhibitors (Strong) may decrease the metabolism of CYP2C19 Substrates. Risk D: Consider therapy modification
CYP2C9 Substrates (High risk with Highly Effective Inhibitors): CYP2C9 Inhibitors (Strong) may decrease the metabolism of CYP2C9 Substrates (High risk with Highly Effective Inhibitors). Risk D: Consider therapy modification
CYP2D6 Substrates: CYP2D6 Inhibitors (Strong) may decrease the metabolism of CYP2D6 Substrates. Risk D: Consider therapy modification
CYP2E1 Substrates: CYP2E1 Inhibitors (Moderate) may decrease the metabolism of CYP2E1 Substrates. Risk C: Monitor therapy
CYP3A4 Inducers (Strong): May increase the metabolism of CYP3A4 Substrates. Risk C: Monitor therapy
CYP3A4 Substrates: CYP3A4 Inhibitors (Strong) may decrease the metabolism of CYP3A4 Substrates. Risk D: Consider therapy modification
Docetaxel: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Docetaxel. Risk D: Consider therapy modification
Dofetilide: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Dofetilide. Risk X: Avoid combination
Eletriptan: Antifungal Agents (Azole Derivatives, Systemic) may increase the serum concentration of Eletriptan. Risk D: Consider therapy modification
Eplerenone: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Eplerenone. Risk D: Consider therapy modification
Erlotinib: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Erlotinib. Risk C: Monitor therapy
Eszopiclone: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Eszopiclone. Risk C: Monitor therapy
Fosaprepitant: Antifungal Agents (Azole Derivatives, Systemic) may increase the serum concentration of Fosaprepitant. Specifically, concentrations of aprepitant are likely to be increased. Risk C: Monitor therapy
Gefitinib: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Gefitinib. Risk C: Monitor therapy
Herbs (CYP3A4 Inducers): May increase the metabolism of CYP3A4 Substrates. Risk C: Monitor therapy
HMG-CoA Reductase Inhibitors: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of HMG-CoA Reductase Inhibitors. Exceptions: Fluvastatin; Rosuvastatin. Risk D: Consider therapy modification
Imatinib: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Imatinib. Risk C: Monitor therapy
Irinotecan: Antifungal Agents (Azole Derivatives, Systemic) may enhance the adverse/toxic effect of Irinotecan. Risk D: Consider therapy modification
Ixabepilone: CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ixabepilone. Risk D: Consider therapy modification
Losartan: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Losartan. Risk C: Monitor therapy
Macrolide Antibiotics: May decrease the metabolism of Antifungal Agents (Azole Derivatives, Systemic). Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Macrolide Antibiotics. Exceptions: Azithromycin; Dirithromycin [Off Market]; Spiramycin. Risk D: Consider therapy modification
Maraviroc: CYP3A4 Inhibitors may increase the serum concentration of Maraviroc. Risk D: Consider therapy modification
Methadone: Antifungal Agents (Azole Derivatives, Systemic) may increase the serum concentration of Methadone. Risk C: Monitor therapy
Nebivolol: CYP2D6 Inhibitors (Strong) may increase the serum concentration of Nebivolol. Risk C: Monitor therapy
Nilotinib: CYP3A4 Inhibitors (Strong) may increase the serum concentration of Nilotinib. Risk X: Avoid combination
Phosphodiesterase 5 Inhibitors: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Phosphodiesterase 5 Inhibitors. Risk D: Consider therapy modification
Pimecrolimus: CYP3A4 Inhibitors (Strong) may decrease the metabolism of Pimecrolimus. Risk C: Monitor therapy
Pimozide: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Pimozide. Risk X: Avoid combination
Quinidine: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Quinidine. Management: Itraconazole, voriconazole, and posaconazole are specifically contraindicated with quinidine. Use of quinidine with any azole antifungal may require quinidine dose adjustment and should be done with caution and close monitoring. Risk X: Avoid combination
Ramelteon: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Ramelteon. Risk C: Monitor therapy
Ranolazine: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Ranolazine. Risk X: Avoid combination
Saccharomyces boulardii: Antifungal Agents may diminish the therapeutic effect of Saccharomyces boulardii. Risk D: Consider therapy modification
Salmeterol: CYP3A4 Inhibitors (Strong) may increase the serum concentration of Salmeterol. Risk X: Avoid combination
Sirolimus: Antifungal Agents (Azole Derivatives, Systemic) may increase the serum concentration of Sirolimus. Management: Sirolimus dose reductions of up to 50-90% may be necessary when starting an azole antifungal. Use of sirolimus with the azole antifungals voriconazole and posaconazole is contraindicated. Risk D: Consider therapy modification
Solifenacin: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Solifenacin. Risk D: Consider therapy modification
Sorafenib: CYP3A4 Inhibitors (Strong) may increase the serum concentration of Sorafenib. Risk C: Monitor therapy
Sunitinib: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Sunitinib. Risk D: Consider therapy modification
Temsirolimus: Antifungal Agents (Azole Derivatives, Systemic) may increase the serum concentration of Temsirolimus. Concentrations of the active metabolite, sirolimus, are likely to be increased more substantially than those of the parent temsirolimus. Risk D: Consider therapy modification
Thioridazine: CYP2D6 Inhibitors may decrease the metabolism of Thioridazine. Risk X: Avoid combination
Tolterodine: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Tolterodine. This is likely only of concern in CYP2D6-deficient patients (ie, "poor metabolizers") Risk D: Consider therapy modification
Tramadol: CYP2D6 Inhibitors (Strong) may diminish the therapeutic effect of Tramadol. These CYP2D6 inhibitors may prevent the metabolic conversion of tramadol to its active metabolite that accounts for much of its opioid-like effects. Risk C: Monitor therapy
VinCRIStine: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of VinCRIStine. Risk D: Consider therapy modification
Ziprasidone: Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Ziprasidone. Risk C: Monitor therapy
Ethanol/Nutrition/Herb Interactions
Herb/Nutraceutical: St John's wort may decrease miconazole levels.
Mechanism of Action
Inhibits biosynthesis of ergosterol, damaging the fungal cell wall membrane, which increases permeability causing leaking of nutrients
Pharmacodynamics/Kinetics
Absorption: Topical: Negligible
Distribution: Widely to body tissues; penetrates well into inflamed joints, vitreous humor of eye, and peritoneal cavity, but poorly into saliva and sputum; crosses blood-brain barrier but only to a small extent
Protein binding: 91% to 93%
Metabolism: Hepatic
Half-life elimination: Multiphasic: Initial: 40 minutes; Secondary: 126 minutes; Terminal: 24 hours
Excretion: Feces (?50%); urine (<1% as unchanged drug)
Dosage
Topical: Children and Adults: Note: Not for OTC use in children <2 years:
Tinea corporis: Apply twice daily for 4 weeks
Tinea pedis: Apply twice daily for 4 weeks
Effervescent tablet: Dissolve 1 tablet in ~1 gallon of water; soak feet for 15-30 minutes; pat dry
Tinea cruris: Apply twice daily for 2 weeks
Vaginal: Children ?12 years and Adults: Vulvovaginal candidiasis:
Cream, 2%: Insert 1 applicatorful at bedtime for 7 days
Cream, 4%: Insert 1 applicatorful at bedtime for 3 days
Suppository, 100 mg: Insert 1 suppository at bedtime for 7 days
Suppository, 200 mg: Insert 1 suppository at bedtime for 3 days
Suppository, 1200 mg: Insert 1 suppository (a one-time dose); may be used at bedtime or during the day
Note: Many products are available as a combination pack, with a suppository for vaginal instillation and cream to relieve external symptoms. External cream may be used twice daily, as needed, for up to 7 days.
Patient Education
Inform prescriber of all prescriptions, OTC medications, or herbal products you are taking, and any allergies you have. Do not take any new medication during therapy. Use full course of therapy as directed; do not discontinue without consulting prescriber. Some infections may require long periods of therapy. Practice good hygiene measures to prevent reinfection. If you have diabetes, you should test serum glucose regularly - this medication may inhibit the metabolism of oral sulfonylureas. Report persistent burning, itching, or irritation to healthcare provider. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Consult prescriber if breast-feeding.
Topical: Wash and dry area before applying medication; apply thinly. Do not get in or near eyes. Not for OTC use in children <2 years of age.
Vaginal: Consult with healthcare provider if using for a vaginal yeast infection for the first time. Insert high in vagina. Refrain from intercourse during treatment. Condoms and diaphragms may not be effective during therapy. Do not use tampons, douches, spermicides, or other vaginal products during treatment. Deodorant-free pads or panty shields may be used to protect clothing during use.
Geriatric Considerations
No specific data for the elderly; use does not require alteration in dose or dose intervals. Assess patient's ability to self administer, may be difficult in patients with arthritis or limited range of motion.
Dental Health: Effects on Dental Treatment
No significant effects or complications reported
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
None reported
Mental Health: Effects on Psychiatric Treatment
None reported
Nursing: Physical Assessment/Monitoring
Assess potential for interactions with other prescriptions, OTC medications, or herbal products patient may be taking. Caution patients with diabetes to test serum glucose regularly; may inhibit the metabolism of oral sulfonylureas. Teach patient proper use, possible side effects/appropriate interventions (eg, bleeding precautions), and adverse symptoms to report.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Combination products: Miconazole nitrate vaginal suppository 200 mg (3s) and miconazole nitrate external cream 2%
Monistat® 1 Combination Pack: Miconazole nitrate vaginal insert 1200 mg (1) and miconazole nitrate external cream 2% (5 g) [Note: Do not confuse with 1-Day™ (formerly Monistat® 1) which contains tioconazole]
Monistat® 3 Combination Pack:
Miconazole nitrate vaginal insert 200 mg (3s) and miconazole nitrate external cream 2%
Miconazole nitrate vaginal cream 4% and miconazole nitrate external cream 2%
Monistat® 7 Combination Pack:
Miconazole nitrate vaginal suppository 100 mg (7s) and miconazole nitrate external cream 2%
Miconazole nitrate vaginal cream 2% (7 prefilled applicators) and miconazole nitrate external cream 2%
Cream, topical, as nitrate: 2% (15 g, 30 g, 45 g)
Baza® Antifungal: 2% (4 g, 57 g, 142 g) [zinc oxide based formula]
Carrington Antifungal: 2% (150 g)
Micaderm®, Neosporin® AF, Podactin: 2% (30 g)
Micatin® Athlete's Foot, Micatin® Jock Itch: 2% (15 g)
Micro-Guard®, Mitrazol™: 2% (60 g)
Monistat-Derm®: 2% (15 g, 30 g, 85 g) [DSC]
Secura® Antifungal: 2% (60 g, 98 g)
Cream, vaginal, as nitrate [prefilled or refillable applicator]: 2% (45 g)
Monistat® 3: 4% (15 g, 25 g)
Monistat® 7: 2% (45 g)
Liquid, spray, topical, as nitrate:
Micatin® Athlete's Foot: 2% (90 mL) [contains alcohol]
Neosporin AF®: 2% (105 mL)
Lotion, powder, as nitrate (Zeasorb®-AF): 2% (56 g) [contains alcohol 36%]
Ointment, topical, as nitrate:
Aloe Vesta® 2-n-1 Antifungal: 2% (60 g, 150 g)
Critic-Aid® Clear AF: 2% (4 g, 57 g, 142 g)
DermaFungal: 2% (113 g)
Dermagran® AF: (113 g ) [contains vitamin A and zinc]
Powder, topical, as nitrate:
Lotrimin® AF: 2% (160 g)
Micro-Guard®: 2% (90 g)
Mitrazol™: 2% (30 g)
Zeasorb®-AF: 2% (70 g)
Powder spray, topical, as nitrate:
Lotrimin® AF, Lotrimin® AF Jock Itch: 2% (140 g)
Micatin® Athlete's Foot, Micatin® Jock Itch: 2% (90 g) [contains alcohol]
Neosporin® AF: 2% (85 g)
Suppository, vaginal, as nitrate: 100 mg (7s); 200 mg (3s)
Monistat® 3: 200 mg (3s)
Monistat® 7: 100 mg (7s)
Tablet, for solution, topical, as nitrate [effervescent]:
DiabetAid™ Antifungal Foot Bath: 2% (10s)
Tincture, topical, as nitrate (Fungoid®): 2% (30 mL, 473 mL) [contains isopropyl alcohol 30%]; 30 mL size also available in a treatment kit which contains nail scrub and nail brush]
Pricing: U.S. (www.drugstore.com)
Cream (Miconazole Nitrate)
2% (28.35): $12.99
Cream (Monistat-Derm)
2% (15): $24.99
2% (28.35): $41.99
Powder (Zeasorb-AF)
2% (70): $14.99
Solution (Fungoid Tincture)
2% (29.57): $29.99
Suppository (Miconazole 3)
200 mg (3): $34.99
Suppository (Monistat 3)
200 mg (3): $52.99
References
Coulthard K, Martin J, and Matthews N, “Convulsions After Miconazole Overdose,” Med J Aust, 1987, 146(1):57-8.
Fainstein V and Bodey GP, “Cardiorespiratory Toxicity Due to Miconazole,” Ann Intern Med, 1980, 93:432-3.
Kanarek KS and Williams PR, “Toxicity of Intravenous Miconazole Overdosage in a Preterm Infant,” Pediatr Infect Dis, 1986, 5(4):486-8.
International Brand Names
Lexi-Comp.com
Last full review/revision August 2008
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