Imiquimod 3.75% Cream Pump 28 Doses
It is used to treat genital warts.It is used to treat perianal warts.It is used to treat skin harmed by the sun and some skin cancers.
Drug Class
Immune response modifier
Pharmacologic Class
Toll-like receptor 7 (TLR7) agonist
Pregnancy Category
Category C
FDA Approved
Mar 2008
DEA Schedule
Not Controlled
Overview
What is this medicine?
Imiquimod cream is a medicine applied to the skin to help your body's immune system fight certain skin conditions like actinic keratosis (rough, scaly patches that can become skin cancer) or external genital and anal warts. It works by boosting your natural defenses.
How to Use This Medicine
Proper Use of This Medication
To use this medication safely and effectively, follow your doctor's instructions carefully. Read all the information provided to you and follow the instructions precisely.
General Guidelines
Use this medication only as directed by your doctor and for the recommended duration. Taking more than prescribed or using it for longer than recommended may increase the risk of severe skin reactions or other side effects.
Apply this medication only to your skin, as directed. Do not ingest it or apply it to your mouth, nose, or eyes, as it may cause burning.
Avoid applying this medication to the vagina or anus.
Use this medication at bedtime, as directed by your doctor.
Preparation and Application
Wash your hands before and after applying this medication.
Clean the affected area before applying the medication and dry it thoroughly (for at least 10 minutes).
Apply a thin layer of the medication to the affected skin and gently rub it in.
Do not apply this medication to sunburned skin, cuts, scrapes, burns, rashes, or infected or damaged skin.
Unless directed by your doctor, avoid applying this medication to healthy skin.
Do not cover the treated area with bandages or dressings unless instructed to do so by your doctor.
After applying the medication, do not bathe, shower, or swim.
Leave the medication on your skin for the recommended duration, then wash it off.
Special Instructions
For genital or perianal warts: If you are an uncircumcised male with warts under the foreskin, pull back the foreskin and clean the area daily.
For actinic keratosis: You may notice an increase in the number of lesions before they start to improve. Continue using the medication as directed by your doctor, even if the skin areas appear to be healed.
Packet and Pump Instructions
If using packets, discard any unused portion after each use.
If using a pump, prime the pump before the first use. You will not need to prime the pump again during use.
Storage and Disposal
Store this medication at room temperature, away from freezing temperatures.
Missed Dose
If you miss a dose, skip it and resume your regular schedule. Do not apply two doses at the same time or use extra doses to make up for the missed dose.
To use this medication safely and effectively, follow your doctor's instructions carefully. Read all the information provided to you and follow the instructions precisely.
General Guidelines
Use this medication only as directed by your doctor and for the recommended duration. Taking more than prescribed or using it for longer than recommended may increase the risk of severe skin reactions or other side effects.
Apply this medication only to your skin, as directed. Do not ingest it or apply it to your mouth, nose, or eyes, as it may cause burning.
Avoid applying this medication to the vagina or anus.
Use this medication at bedtime, as directed by your doctor.
Preparation and Application
Wash your hands before and after applying this medication.
Clean the affected area before applying the medication and dry it thoroughly (for at least 10 minutes).
Apply a thin layer of the medication to the affected skin and gently rub it in.
Do not apply this medication to sunburned skin, cuts, scrapes, burns, rashes, or infected or damaged skin.
Unless directed by your doctor, avoid applying this medication to healthy skin.
Do not cover the treated area with bandages or dressings unless instructed to do so by your doctor.
After applying the medication, do not bathe, shower, or swim.
Leave the medication on your skin for the recommended duration, then wash it off.
Special Instructions
For genital or perianal warts: If you are an uncircumcised male with warts under the foreskin, pull back the foreskin and clean the area daily.
For actinic keratosis: You may notice an increase in the number of lesions before they start to improve. Continue using the medication as directed by your doctor, even if the skin areas appear to be healed.
Packet and Pump Instructions
If using packets, discard any unused portion after each use.
If using a pump, prime the pump before the first use. You will not need to prime the pump again during use.
Storage and Disposal
Store this medication at room temperature, away from freezing temperatures.
Missed Dose
If you miss a dose, skip it and resume your regular schedule. Do not apply two doses at the same time or use extra doses to make up for the missed dose.
Lifestyle & Tips
- Apply only to the affected skin area as directed by your doctor. Do not apply to internal surfaces (e.g., inside the vagina, anus, or urethra).
- Wash your hands thoroughly before and after applying the cream.
- Apply at bedtime and leave on for the specified duration (8 hours for AK, 6-10 hours for EGW), then wash off with mild soap and water.
- Avoid showering, bathing, or swimming during the treatment period (while the cream is on).
- Do not cover the treated area with bandages or occlusive dressings.
- Avoid sun exposure to the treated area, as imiquimod can increase sun sensitivity. Use protective clothing and sunscreen.
- Sexual contact should be avoided while the cream is on for EGW, as it can weaken condoms/diaphragms and may irritate a partner's skin.
- Expect local skin reactions (redness, swelling, itching, burning, flaking, scabbing) â these are common and indicate the medicine is working. Report severe reactions to your doctor.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
For Actinic Keratosis (AK): Apply once daily at bedtime, 2 times per week (e.g., Monday and Thursday) for a full 16-week treatment course. For External Genital and Perianal Warts (EGW): Apply once daily at bedtime, 2 times per week (e.g., Monday and Thursday) for up to 8 weeks.
Condition-Specific Dosing:
Actinic Keratosis:
Apply a thin layer to the entire affected area (full face or balding scalp) once daily at bedtime, 2 times per week (e.g., Monday and Thursday) for a full 16-week treatment course. Wash off with mild soap and water 8 hours after application.
External Genital and Perianal Warts:
Apply a thin layer to the affected area once daily at bedtime, 2 times per week (e.g., Monday and Thursday) for up to 8 weeks. Wash off with mild soap and water 6 to 10 hours after application.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established for AK. For EGW, safety and efficacy not established in patients under 12 years of age.
Adolescent:
For EGW: Patients 12 years and older, same adult dosing (once daily at bedtime, 2 times per week for up to 8 weeks). Not indicated for AK in adolescents.
Dose Adjustments
Renal Impairment:
Mild:
No specific dose adjustment recommended due to minimal systemic absorption.
Moderate:
No specific dose adjustment recommended due to minimal systemic absorption.
Severe:
No specific dose adjustment recommended due to minimal systemic absorption.
Dialysis:
No specific considerations due to minimal systemic absorption.
Hepatic Impairment:
Mild:
No specific dose adjustment recommended due to minimal systemic absorption.
Moderate:
No specific dose adjustment recommended due to minimal systemic absorption.
Severe:
No specific dose adjustment recommended due to minimal systemic absorption.
Pharmacology
Mechanism of Action
Imiquimod is an immune response modifier. It acts as a Toll-like receptor 7 (TLR7) agonist, stimulating immune cells (e.g., monocytes, macrophages, dendritic cells) to release pro-inflammatory cytokines, including interferon-alpha (IFN-Îą), tumor necrosis factor-alpha (TNF-Îą), and interleukins (IL-1, IL-6, IL-8, IL-10, IL-12). These cytokines mediate an antiviral and antitumor immune response.
Pharmacokinetics
Absorption:
Bioavailability:
Minimal systemic absorption (less than 0.9% of applied dose) after topical application.
Tmax:
Not well-defined due to minimal systemic absorption; systemic concentrations are generally low or undetectable.
FoodEffect:
Not applicable for topical cream.
Distribution:
Vd:
Not applicable due to minimal systemic absorption.
ProteinBinding:
Not applicable due to minimal systemic absorption.
CnssPenetration:
Limited
Elimination:
HalfLife:
Systemic half-life is approximately 29.3 hours after topical application, but systemic levels are very low.
Clearance:
Not well-defined due to minimal systemic absorption.
ExcretionRoute:
Primarily renal and fecal excretion of metabolites.
Unchanged:
Less than 0.1% of applied dose excreted unchanged in urine.
Pharmacodynamics
OnsetOfAction:
Clinical effects are observed over weeks of treatment, reflecting the immune response modulation.
PeakEffect:
Peak immune response (cytokine induction) occurs within hours to days of application, but clinical lesion clearance takes weeks.
DurationOfAction:
Effects persist as long as treatment continues and for some time after cessation, depending on the immune response generated.
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor immediately or seek medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Flu-like symptoms, including:
+ Headache
+ Weakness
+ Fever
+ Chills
+ Aches
+ Pains
+ Sweating
Bleeding
Swollen glands
Skin reactions at the application site or surrounding area, such as:
+ Burning
+ Crusting
+ Dryness
+ Flaking
+ Itching
+ Oozing
+ Pain
+ Redness
+ Scabbing
+ Scaling
+ Sores or ulcers
+ Swelling
If these reactions become severe, your doctor may advise you to take a break from using the medication. Gently wash the affected area with mild soap and water, and consult your doctor.
If you experience a skin reaction that bothers you or interferes with your daily activities, contact your doctor right away.
Additional Side Effects for Genital or Perianal Warts:
Vaginal pain or swelling
Difficulty urinating
Other Possible Side Effects:
While many people may not experience side effects or may only have mild symptoms, it's essential to be aware of the following possible side effects:
Change in skin color that may not return to normal
Headache
Upset stomach
Feeling tired or weak
Signs of a common cold
* Sinus pain
If any of these side effects or other symptoms bother you or persist, contact your doctor for advice. Not all possible side effects are listed here. If you have questions or concerns about side effects, consult your doctor.
Reporting Side Effects:
You can report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor immediately or seek medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Flu-like symptoms, including:
+ Headache
+ Weakness
+ Fever
+ Chills
+ Aches
+ Pains
+ Sweating
Bleeding
Swollen glands
Skin reactions at the application site or surrounding area, such as:
+ Burning
+ Crusting
+ Dryness
+ Flaking
+ Itching
+ Oozing
+ Pain
+ Redness
+ Scabbing
+ Scaling
+ Sores or ulcers
+ Swelling
If these reactions become severe, your doctor may advise you to take a break from using the medication. Gently wash the affected area with mild soap and water, and consult your doctor.
If you experience a skin reaction that bothers you or interferes with your daily activities, contact your doctor right away.
Additional Side Effects for Genital or Perianal Warts:
Vaginal pain or swelling
Difficulty urinating
Other Possible Side Effects:
While many people may not experience side effects or may only have mild symptoms, it's essential to be aware of the following possible side effects:
Change in skin color that may not return to normal
Headache
Upset stomach
Feeling tired or weak
Signs of a common cold
* Sinus pain
If any of these side effects or other symptoms bother you or persist, contact your doctor for advice. Not all possible side effects are listed here. If you have questions or concerns about side effects, consult your doctor.
Reporting Side Effects:
You can report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Severe skin reactions (e.g., severe blistering, open sores, weeping, bleeding)
- Signs of infection at the application site (e.g., pus, spreading redness, fever)
- Severe flu-like symptoms (e.g., high fever, extreme fatigue, body aches)
- Swelling of lymph nodes that is painful or persistent
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If your skin has not fully healed from previous treatments or surgeries.
* If you are currently taking another medication that contains the same active ingredient as this drug.
This list is not exhaustive, and it is crucial to discuss all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, with your doctor and pharmacist. They will help determine if it is safe to take this medication with your existing medications and health conditions.
Remember, do not start, stop, or adjust the dosage of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If your skin has not fully healed from previous treatments or surgeries.
* If you are currently taking another medication that contains the same active ingredient as this drug.
This list is not exhaustive, and it is crucial to discuss all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, with your doctor and pharmacist. They will help determine if it is safe to take this medication with your existing medications and health conditions.
Remember, do not start, stop, or adjust the dosage of any medication without first consulting your doctor.
Precautions & Cautions
Important Warnings and Cautions for This Medication
General Precautions
Inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
Follow your doctor's instructions for regular skin checks.
Be aware that you may be more susceptible to sunburn. To minimize this risk, avoid exposure to direct sunlight, sunlamps, and tanning beds. Use a broad-spectrum sunscreen with a high SPF and wear protective clothing and eyewear when outdoors.
If you are pregnant, planning to become pregnant, or breastfeeding, consult your doctor to discuss the potential benefits and risks to you and your baby.
Specific Warnings for Genital or Perianal Warts
This medication will not cure your genital or perianal warts, and new warts may still develop during treatment. Notify your doctor if you notice any new warts.
Note that condoms and diaphragms may not be effective in preventing pregnancy while using this medication. Consider alternative birth control methods.
Avoid engaging in sexual activity when the medication is applied to your genital or anal skin.
Specific Precautions for Actinic Keratosis
If you are breastfeeding, take precautions to prevent the medication from coming into contact with your baby's mouth or eyes.
* Avoid applying the medication to areas that may come into contact with your baby's face, as this can cause irritation.
General Precautions
Inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
Follow your doctor's instructions for regular skin checks.
Be aware that you may be more susceptible to sunburn. To minimize this risk, avoid exposure to direct sunlight, sunlamps, and tanning beds. Use a broad-spectrum sunscreen with a high SPF and wear protective clothing and eyewear when outdoors.
If you are pregnant, planning to become pregnant, or breastfeeding, consult your doctor to discuss the potential benefits and risks to you and your baby.
Specific Warnings for Genital or Perianal Warts
This medication will not cure your genital or perianal warts, and new warts may still develop during treatment. Notify your doctor if you notice any new warts.
Note that condoms and diaphragms may not be effective in preventing pregnancy while using this medication. Consider alternative birth control methods.
Avoid engaging in sexual activity when the medication is applied to your genital or anal skin.
Specific Precautions for Actinic Keratosis
If you are breastfeeding, take precautions to prevent the medication from coming into contact with your baby's mouth or eyes.
* Avoid applying the medication to areas that may come into contact with your baby's face, as this can cause irritation.
Overdose Information
Overdose Symptoms:
- Systemic overdose is unlikely due to minimal absorption. However, excessive topical application could theoretically lead to more pronounced local skin reactions or systemic flu-like symptoms.
What to Do:
If swallowed, call a Poison Control Center immediately (1-800-222-1222). For excessive topical application, wash off the cream and manage local reactions symptomatically. Seek medical attention if systemic symptoms occur.
Drug Interactions
Monitoring
Baseline Monitoring
Diagnosis confirmation
Rationale: Ensure appropriate indication (AK or EGW).
Timing: Prior to initiation of therapy.
Baseline lesion assessment
Rationale: Document size, number, and location of lesions for monitoring treatment response.
Timing: Prior to initiation of therapy.
Routine Monitoring
Local skin reactions (erythema, erosion, flaking, dryness, edema, scabbing, itching, burning, pain)
Frequency: Daily during treatment, especially in the first few weeks.
Target: Mild to moderate reactions are expected and indicate drug activity. Severe reactions may require temporary cessation.
Action Threshold: Severe reactions (e.g., severe erosion, blistering, weeping) or intolerable discomfort may warrant temporary interruption of therapy or dose reduction (e.g., reducing frequency to once weekly) until reactions subside.
Resolution of lesions
Frequency: Periodically during treatment and at the end of the treatment course.
Target: Complete clearance of lesions.
Action Threshold: If no significant improvement after the recommended treatment course, re-evaluate diagnosis and consider alternative therapies.
Symptom Monitoring
- Local skin reactions (redness, swelling, itching, burning, pain, scabbing, flaking, erosion, ulceration)
- Flu-like symptoms (fever, fatigue, headache, myalgia)
- Lymphadenopathy (swollen lymph nodes near the treatment area)
Special Patient Groups
Pregnancy
Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Animal studies have shown adverse effects at high doses, but systemic exposure in humans is minimal.
Trimester-Specific Risks:
First Trimester:
Limited human data. Animal studies suggest potential for developmental toxicity at high systemic exposures, which are not typically achieved with topical use.
Second Trimester:
Limited human data.
Third Trimester:
Limited human data.
Lactation
It is not known whether imiquimod is excreted in human milk. Due to the potential for serious adverse reactions in breastfed infants from imiquimod, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Infant Risk:
Risk unknown; potential for adverse effects due to systemic absorption in infant, though maternal systemic absorption is minimal.
Pediatric Use
Not indicated for Actinic Keratosis in pediatric patients. For External Genital and Perianal Warts, safety and efficacy have not been established in patients under 12 years of age. Use in adolescents 12 years and older for EGW is based on adult data.
Geriatric Use
No specific dose adjustments are recommended for elderly patients. Clinical studies did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. However, no overall differences in safety or effectiveness were observed between these subjects and younger subjects.
Clinical Information
Clinical Pearls
- Imiquimod 3.75% (Zyclara) is specifically formulated for full-face/balding scalp AK and EGW, with a different dosing schedule (2x/week) than the 5% cream (3x/week for AK/sBCC, 3x/week for EGW). Ensure correct formulation and dosing frequency.
- Patient adherence to the specific application schedule (2 times per week, not daily) and duration (16 weeks for AK, up to 8 weeks for EGW) is crucial for efficacy.
- Educate patients that local skin reactions (erythema, flaking, crusting, erosion) are expected and indicate the drug is working. These reactions are generally reversible upon cessation of treatment.
- Temporary interruption of therapy may be necessary if local skin reactions are severe or intolerable, but treatment should be resumed once reactions subside.
- Advise patients to avoid sun exposure to treated areas and use sun protection, as imiquimod can increase photosensitivity.
- For EGW, advise patients that new warts may develop during treatment and that imiquimod does not cure HPV infection, nor does it prevent transmission.
Alternative Therapies
- For Actinic Keratosis: 5-fluorouracil cream, ingenol mebutate gel, diclofenac sodium gel, photodynamic therapy (PDT), cryosurgery, surgical excision, laser ablation.
- For External Genital and Perianal Warts: Podofilox solution/gel, sinecatechins ointment, cryotherapy, surgical excision, laser therapy, trichloroacetic acid (TCA).
Cost & Coverage
Average Cost:
Varies significantly, typically several hundred to over a thousand USD per 28-dose pump (250 mg/actuation)
Insurance Coverage:
Tier 3 or 4 (Non-preferred brand)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure safe and effective treatment, never share your medication with others or take someone else's medication. Some medications may come with a separate patient information leaflet, so it's a good idea to check with your pharmacist for more information. If you have any questions or concerns about this medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When reporting the incident, be prepared to provide details about the medication taken, the amount, and the time it occurred.