Imiquimod 3.75% Cream S/use Pkt 28s
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 off certain skin growths, like rough, scaly patches (actinic keratosis) or genital/anal warts. It works by boosting your local immune response.
How to Use This Medicine
Proper Use of This Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. Adhere to the instructions carefully to minimize the risk of severe skin reactions or other side effects.
General Guidelines
Use this medication only as directed by your doctor, and do not exceed the recommended dosage or duration of treatment.
Apply this medication topically, only to the affected skin areas, and avoid ingestion or contact with mucous membranes, including the mouth, nose, and eyes, as it may cause burning.
Do not apply this medication to the vagina or anus.
Use this medication at bedtime, and wash your hands before and after application.
Clean the affected area before applying the medication, and ensure it is completely dry (at least 10 minutes) before use.
Apply a thin layer of the medication to the affected skin and gently rub it in.
Avoid applying this medication to sunburned skin, cuts, scrapes, burns, rashes, or infected or damaged skin, unless directed to do so by your doctor.
Do not apply this medication to healthy skin unless instructed by your doctor.
Refrain from using bandages or dressings unless advised by your doctor.
After applying the medication, avoid bathing, showering, or swimming.
Leave the medication on the skin for the duration specified by your doctor, then wash it off.
Specific 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: Be aware that the number of lesions may worsen before improving. Continue using the medication as directed by your doctor, even if the skin appears to be healed.
Packet and Pump Instructions
Packets: Discard any unused portion of the packet after use.
Pump: Prime the pump before the first use, but you will not need to re-prime it during subsequent uses.
Storage and Disposal
Store this medication at room temperature, and do not freeze.
Missed Dose
* If you miss a dose, skip it and resume your regular schedule. Do not apply two doses at once or use extra doses to make up for the missed dose.
To use this medication correctly, follow your doctor's instructions and read all the information provided. Adhere to the instructions carefully to minimize the risk of severe skin reactions or other side effects.
General Guidelines
Use this medication only as directed by your doctor, and do not exceed the recommended dosage or duration of treatment.
Apply this medication topically, only to the affected skin areas, and avoid ingestion or contact with mucous membranes, including the mouth, nose, and eyes, as it may cause burning.
Do not apply this medication to the vagina or anus.
Use this medication at bedtime, and wash your hands before and after application.
Clean the affected area before applying the medication, and ensure it is completely dry (at least 10 minutes) before use.
Apply a thin layer of the medication to the affected skin and gently rub it in.
Avoid applying this medication to sunburned skin, cuts, scrapes, burns, rashes, or infected or damaged skin, unless directed to do so by your doctor.
Do not apply this medication to healthy skin unless instructed by your doctor.
Refrain from using bandages or dressings unless advised by your doctor.
After applying the medication, avoid bathing, showering, or swimming.
Leave the medication on the skin for the duration specified by your doctor, then wash it off.
Specific 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: Be aware that the number of lesions may worsen before improving. Continue using the medication as directed by your doctor, even if the skin appears to be healed.
Packet and Pump Instructions
Packets: Discard any unused portion of the packet after use.
Pump: Prime the pump before the first use, but you will not need to re-prime it during subsequent uses.
Storage and Disposal
Store this medication at room temperature, and do not freeze.
Missed Dose
* If you miss a dose, skip it and resume your regular schedule. Do not apply two doses at once or use extra doses to make up for the missed dose.
Lifestyle & Tips
- Apply only a thin layer to the affected area at bedtime, as directed by your doctor.
- Wash your hands thoroughly before and after applying the cream.
- Do not apply to open wounds or broken skin.
- Avoid contact with eyes, lips, and nostrils.
- Wash the treated area with mild soap and water 8 hours after application.
- Avoid sun exposure or use protective clothing and sunscreen on treated areas, as the cream can increase sun sensitivity.
- Do not use occlusive dressings (bandages) over the treated area.
- For genital/perianal warts, avoid sexual contact while the cream is on the skin, and remember it does not protect against STIs or pregnancy.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
For Actinic Keratosis (AK): Apply once daily at bedtime for two 2-week treatment cycles separated by a 2-week non-treatment period. For External Genital/Perianal Warts (EGW): Apply once daily at bedtime for up to 8 weeks.
Condition-Specific Dosing:
actinicKeratosis:
Apply a thin layer to the entire treatment area (e.g., full face or scalp) once daily at bedtime for two 2-week treatment cycles separated by a 2-week non-treatment period. Wash off 8 hours after application.
externalGenitalPerianalWarts:
Apply a thin layer to the affected area once daily at bedtime until complete clearance of the warts or for a maximum of 8 weeks. Wash off 8 hours after application.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established (Safety and effectiveness not established in pediatric patients under 18 years of age for AK or EGW).
Dose Adjustments
Renal Impairment:
Mild:
No adjustment needed (minimal systemic absorption)
Moderate:
No adjustment needed (minimal systemic absorption)
Severe:
No adjustment needed (minimal systemic absorption)
Dialysis:
No specific considerations (minimal systemic absorption)
Hepatic Impairment:
Mild:
No adjustment needed (minimal systemic absorption)
Moderate:
No adjustment needed (minimal systemic absorption)
Severe:
No adjustment needed (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-6, IL-8). This local immune response helps to eliminate abnormal cells (e.g., actinic keratosis, warts).
Pharmacokinetics
Absorption:
Bioavailability:
Minimal systemic absorption (<0.9%) after topical application.
Tmax:
Not well-defined for topical application; systemic levels are very low and variable.
FoodEffect:
Not applicable (topical administration).
Distribution:
Vd:
Not clinically relevant due to minimal systemic absorption.
ProteinBinding:
Not clinically relevant due to minimal systemic absorption.
CnssPenetration:
Limited (minimal systemic absorption).
Elimination:
HalfLife:
Not clinically relevant for topical application; systemic half-life is short (approximately 2-3 hours) when detectable.
Clearance:
Not clinically relevant for topical application.
ExcretionRoute:
Systemically, metabolites are primarily excreted in urine and feces. However, the majority of the topically applied dose remains at the application site or is removed by washing.
Unchanged:
Not clinically relevant for topical application.
Pharmacodynamics
OnsetOfAction:
Local immune response begins within hours to days; clinical effects (lesion clearance) are observed over weeks of treatment.
PeakEffect:
Clinical peak effect typically seen after several weeks of consistent application.
DurationOfAction:
Clinical benefit can persist after cessation of treatment, indicating a sustained immune response.
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 when taking this medication. If you experience any of the following symptoms, contact your doctor or seek medical attention immediately:
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.
For genital or perianal warts, seek medical help right away if you experience:
Vaginal pain or swelling
Trouble passing urine
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to contact your doctor or seek medical help if you're bothered by any of the following:
Change in skin color that may not return to normal
Headache
Upset stomach
Feeling tired or weak
Signs of a common cold
* Sinus pain
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, consult your doctor. You can also 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 when taking this medication. If you experience any of the following symptoms, contact your doctor or seek medical attention immediately:
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.
For genital or perianal warts, seek medical help right away if you experience:
Vaginal pain or swelling
Trouble passing urine
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to contact your doctor or seek medical help if you're bothered by any of the following:
Change in skin color that may not return to normal
Headache
Upset stomach
Feeling tired or weak
Signs of a common cold
* Sinus pain
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, consult your doctor. You can also 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., intense redness, swelling, blistering, open sores, bleeding, scabbing) - contact your doctor immediately.
- Flu-like symptoms (fever, chills, body aches, fatigue) - contact your doctor.
- Swollen lymph nodes (glands) in the neck, armpits, or groin.
- Any signs of infection at the application site (pus, increasing pain, warmth).
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 allergic reaction you experienced, including any symptoms that occurred.
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 you determine if it is safe to take this medication with your existing medications and health conditions.
Remember, do not start, stop, or change the dose of any medication without first consulting your doctor to ensure your safety.
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 allergic reaction you experienced, including any symptoms that occurred.
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 you determine if it is safe to take this medication with your existing medications and health conditions.
Remember, do not start, stop, or change the dose of any medication without first consulting your doctor to ensure your safety.
Precautions & Cautions
Important Warnings and Cautions for This Medication
General Information
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Regular skin checks are crucial, as directed by your doctor. You may be more susceptible to sunburn, so it is vital to avoid exposure to the sun, sunlamps, and tanning beds. Protect yourself from the sun by using sunscreen and wearing protective clothing and eyewear.
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 you may still develop new warts while using it. Notify your doctor if you notice any new warts. Additionally, condoms and diaphragms may not be effective in preventing pregnancy while taking this medication, so consider using alternative birth control methods. Avoid engaging in sexual activity when the medication is applied to your genital or anal skin.
Specific Warnings 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 potential harm.
General Information
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Regular skin checks are crucial, as directed by your doctor. You may be more susceptible to sunburn, so it is vital to avoid exposure to the sun, sunlamps, and tanning beds. Protect yourself from the sun by using sunscreen and wearing protective clothing and eyewear.
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 you may still develop new warts while using it. Notify your doctor if you notice any new warts. Additionally, condoms and diaphragms may not be effective in preventing pregnancy while taking this medication, so consider using alternative birth control methods. Avoid engaging in sexual activity when the medication is applied to your genital or anal skin.
Specific Warnings 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 potential harm.
Overdose Information
Overdose Symptoms:
- Topical overdose is unlikely to cause systemic symptoms due to minimal absorption.
- Excessive topical application may lead to severe local skin reactions.
- Oral ingestion (e.g., by a child) could lead to systemic adverse events such as nausea, vomiting, headache, fever, and fatigue.
What to Do:
For severe local reactions, discontinue treatment and manage symptoms. For suspected oral ingestion, seek immediate medical attention. Call 1-800-222-1222 (Poison Control).
Drug Interactions
Monitoring
Baseline Monitoring
Diagnosis confirmation
Rationale: Ensure appropriate indication (Actinic Keratosis or External Genital/Perianal Warts).
Timing: Prior to initiation of therapy
Routine Monitoring
Local skin reactions (erythema, erosion, scabbing, flaking, edema, crusting)
Frequency: Daily or as advised by physician
Target: Mild to moderate reactions are expected; severe reactions may require temporary cessation or dose reduction.
Action Threshold: Severe local inflammatory reactions (e.g., severe erythema, erosion, ulceration, blistering) may necessitate a rest period of several days.
Resolution of lesions
Frequency: Weekly to bi-weekly during treatment, and at end of treatment period
Target: Complete clearance of lesions
Action Threshold: If no significant improvement after recommended treatment duration, re-evaluate diagnosis or consider alternative therapies.
Symptom Monitoring
- Local skin reactions (redness, swelling, itching, burning, pain, scabbing, flaking, crusting, erosion, ulceration, blistering)
- Flu-like symptoms (fever, fatigue, headache, myalgia) - rare but possible systemic effects
- Lymphadenopathy (swollen lymph nodes) - rare
Special Patient Groups
Pregnancy
Imiquimod is Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Systemic absorption is minimal.
Trimester-Specific Risks:
First Trimester:
Limited human data; animal studies show some developmental toxicity at high systemic exposures 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 minimal systemic absorption, significant transfer to breast milk is unlikely. Caution should be exercised when administered to a nursing woman.
Infant Risk:
Low risk to infant due to minimal systemic absorption of the drug in the mother.
Pediatric Use
Safety and effectiveness have not been established in pediatric patients under 18 years of age for Actinic Keratosis or External Genital/Perianal Warts. Not recommended for use in this population.
Geriatric Use
No specific dose adjustment is required for elderly patients. However, elderly patients may have more fragile skin and should be monitored closely for severe local skin reactions.
Clinical Information
Clinical Pearls
- Imiquimod 3.75% (Zyclara) is specifically formulated for broader field treatment of actinic keratosis (e.g., full face or scalp) and for external genital/perianal warts, with a different dosing schedule than the 5% cream (Aldara).
- Patients should be instructed to wash off the cream 8 hours after application to minimize severe local skin reactions.
- Temporary cessation of treatment may be necessary if severe local skin reactions occur; treatment can be resumed once the reaction subsides.
- Complete clearance of lesions may not occur until several weeks after the end of treatment.
- Imiquimod does not cure HPV infection, and new warts may appear during treatment.
- Avoid sexual contact while the cream is on the skin, as it can weaken condoms and diaphragms.
Alternative Therapies
- For Actinic Keratosis: 5-fluorouracil cream, ingenol mebutate gel, diclofenac sodium gel, photodynamic therapy (PDT), cryosurgery, surgical excision, chemical peels, laser resurfacing.
- For External Genital/Perianal Warts: Podofilox solution/gel, sinecatechins ointment, cryotherapy, surgical excision, laser therapy, trichloroacetic acid (TCA).
Cost & Coverage
Average Cost:
$500 - $1000+ per 28-packet box (3.75% cream)
Generic Available:
Yes
Insurance Coverage:
Tier 2 or Tier 3 (Specialty/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 an additional 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 your medication, don't hesitate to discuss them with 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 seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.