Uses for imiquimod

Imiquimod topical is used to treat external warts around the genital and rectal areas called condyloma acuminatum. It is not used on warts inside the vagina, penis, or rectum. Imiquimod is also used to treat a skin condition of the face and scalp called actinic keratosis (AK), which is caused by too much sun exposure. Imiquimod may be used to treat certain types of skin cancer called superficial basal cell carcinoma (sBCC).

Imiquimod works on the immune system to help the body fight viruses that cause warts. It does not destroy the viruses directly. It is not known how imiquimod works for actinic keratosis or skin cancer.

This medicine is available only with your doctor’s prescription.

Before using imiquimod

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Appropriate studies performed to date have not demonstrated pediatric-specific problems that would limit the usefulness of imiquimod topical for external warts in children older than 12 years of age. However, safety and efficacy have not been established in children younger than 12 years of age.

Appropriate studies on the relationship of age to the effects of imiquimod topical for actinic keratosis or skin cancer have not been performed in the pediatric population. Safety and efficacy have not been established.

Geriatric

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of imiquimod topical in the elderly.

Breast Feeding

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. Tell your healthcare professional if you are taking any other prescription or nonprescription (over-the-counter [OTC]) medicine.

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Other Medical Problems

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

• Autoimmune disorders, history of or
• Infection of the skin at or near the place of application or
• Large sores, broken skin, or severe skin injury at the place of application or
• Rheumatoid arthritis, juvenile or adult (chronic, always present) or
• Sun exposure, including sunlamps or
• Surgery, recent, at the place of application or
• Systemic lupus erythematosus (SLE), history of or
• Vulvar swelling (swelling near the opening of the vagina)—The chance of side effects may be increased.

• Basal cell nervus syndrome or
• Human papilloma viral disease (cervical, intra-anal, intravaginal, rectal, urethral) or
• Weak immune system or
• Xeroderma pigmentosum (a rare, inherited skin disease)—It is not known if this medicine will work in patients with these conditions.

Proper use of imiquimod

It is very important that you use this medicine only as directed by your doctor. Do not use more of it, do not use it more often, and do not use it for a longer time than your doctor ordered. To do so may cause unwanted side effects or skin irritation.

This medicine is for use on the skin only. Do not get it in your eyes, nose, mouth, vagina, or anus. Do not use it on skin areas that have cuts, scrapes, or burns. If it does get on these areas, rinse it off right away with water.

This medicine comes with a patient information leaflet. Read and follow the instructions in the leaflet carefully. Ask your doctor if you have any questions.

This medicine should only be used for skin conditions that your doctor is treating. Check with your doctor before using it for other conditions, especially if you think that a skin infection may be present. This medicine should not be used to treat certain kinds of skin infections or conditions, such as severe burns.

If you are using the Zyclara® cream pump for the first time, prime it by pressing the top of the pump until the cream appears.

To use the cream:

• Wash your hands with soap and water before and after using the medicine.
• Use one or two packets or actuations of the pump of cream for each dose as directed by your doctor.
• Apply a thin layer to the affected area of the skin just before bedtime. Rub it in gently.
• Allow the medicine to stay on the treated skin for 8 hours (for actinic keratosis or basal cell carcinoma) or 6 to 10 hours (for genital warts). Do not take a bath, swim, or get the treated area wet during this time.
• After the right amount of time has passed, wash the treated area with mild soap and water.
• Men who are not circumcised and are treating genital warts under the foreskin should retract the foreskin and clean the area daily.
• Do not bandage or otherwise wrap the skin being treated, unless directed to do so by your doctor. Materials that are not airtight, such as cotton gauze or cotton underwear, may be used if needed.
• Throw out any unused cream from the single-dose packet.

Use only the brand of this medicine that your doctor prescribed. Different brands may not work the same way.

Do not use this medicine together with any other products containing imiquimod in the same treatment area. This may increase risk for more serious side effects.

Dosing

The dose of this medicine will be different for different patients. Follow your doctor’s orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

• For topical dosage form (cream):
  • For actinic keratosis:
    • Adults—If you use Zyclara®, apply a thin film to the affected area of skin once a day at bedtime for 2 weeks. Your doctor will repeat the treatment after you go 2 weeks without medicine. If you use Aldara®, apply a thin film to the affected area of skin once a day at bedtime 2 times per week for 16 weeks. Your doctor will tell you which days are best during the week.
    • Children—Use and dose must be determined by your doctor.
  • For skin cancer:
    • Adults—Apply a thin film to the affected area of skin once a day at bedtime 5 times per week for 6 weeks. Your doctor will tell you which days are best during the week.
    • Children—Use and dose must be determined by your doctor.
  • For external warts:
    • Adults and children 12 years of age and older—If you use Zyclara®, apply a thin film to the wart once a day at bedtime for up to 8 weeks or until the wart is gone. If you use Aldara®, apply a thin film to the wart once a day at bedtime 3 times per week. Your doctor will tell you which days are best during the week. Use the medicine until the wart is gone, but for no longer than 16 weeks.
    • Children younger than 12 years of age—Use and dose must be determined by your doctor.

Missed Dose

If you miss a dose of this medicine, apply it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule.

Storage

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Store the Zyclara® cream pump upright.

Precautions while using imiquimod

It is very important that your doctor check the progress of you or your child at regular visits for any unwanted effects that may be caused by this medicine.

Stop using this medicine and check with your doctor right away if you or your child have a skin rash, burning, pain, redness, swelling, bleeding, oozing, scabbing, or peeling on the skin where the medicine was applied.

Stop using this medicine and check with your doctor right away if you have severe swelling near the opening of the vagina. This may cause painful urination, trouble in passing urine, or not able to urinate.

Stop using this medicine and check with your doctor right away if you or your child have severe skin irritation or flu-like symptoms, such as diarrhea, fever, chills, headache, nausea, muscle or joint pain, or unusual tiredness or weakness.

Avoid exposing your skin to sunlight, sunlamps, or tanning beds while you are using this medicine. Always use sunscreen or sun-blocking lotions and wear protective clothing and hats.

If you are being treated for external warts, avoid having genital, oral, or anal sex while the medicine is on your skin. Make sure you wash the cream off your skin before you engage in any sexual activity. The medicine contains oils that can weaken latex (rubber) condoms and diaphragms, which will prevent them from working properly.

Imiquimod is not a cure for genital warts. New warts may develop while you are using the cream. Imiquimod will also not keep you from spreading genital warts to other people.

Do not use cosmetics or any other skin care products on the treated areas, unless directed to do so by your doctor.

Side Effects of imiquimod

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

More common

• Blisters on the skin
• body aches or pain
• chills
• cough
• difficulty with breathing
• ear congestion
• itching in the genital or other skin areas
• loss of voice
• open sores or scabs on the skin
• pain or tenderness around the eyes and cheekbones
• redness of the skin (severe)
• scaling
• shortness of breath or troubled breathing
• skin rash
• sneezing
• sore throat
• stuffy or runny nose
• tightness of the chest or wheezing
• unusual tiredness or weakness

Less common

• Abdominal or stomach pain
• ankle, knee, or great toe joint pain
• bladder pain
• bloody or cloudy urine
• blurred vision
• chest pain
• cold flu-like symptoms
• difficult, burning, or painful urination
• dizziness
• fainting
• fast or irregular heartbeat
• frequent urge to urinate
• hoarseness
• joint stiffness or swelling
• lower back or side pain
• lump in the abdomen or stomach
• nervousness
• persistent non-healing sore
• pink growth on the skin
• pounding in the ears
• reddish patch or irritated area
• severe headache
• shiny bump on the skin
• slow or fast heartbeat
• swollen, painful, or tender lymph glands in the neck, armpit, or groin
• white, yellow or waxy scar-like area

Incidence not known

• Blue lips and fingernails
• convulsions
• coughing that sometimes produces a pink frothy sputum
• dilated neck veins
• extreme fatigue
• fast, irregular, or pounding heartbeat
• headache
• irregular breathing
• nausea or vomiting
• pain in the shoulders, arms, jaw, or neck
• slurred speech
• sudden and severe inability to speak
• suicide
• sweating
• swelling of the face, fingers, feet, or lower legs
• temporary blindness
• weakness in the arm or leg on one side of the body
• weight gain

Get emergency help immediately if any of the following symptoms of overdose occur:

Symptoms of overdose

• Confusion
• dizziness, faintness, or lightheadedness when getting up suddenly from a lying or sitting position

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common

• Burning or stinging of the skin (mild)
• flaking of the skin
• mild headache
• pain, soreness, or tenderness of the skin (mild)
• rash
• redness of the skin (mild)
• swelling at place of application

Less common

• Back pain
• lightening of the treated skin

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

What is Klisyri ointment?

Klisyri (tirbanibulin) ointment is a first-in-class microtubule inhibitor that may be used on the skin to treat actinic keratosis of the face or scalp. Actinic keratosis is a precancerous skin condition caused by damage from repeated exposure to ultraviolet light from the sun or indoor tanning.

Klisyri (tirbanibulin) targets tubulin which inhibits microtubule polymerization (a process that allows microtubules to adopt spatial arrangements that can change rapidly in response to cellular needs or sometimes to perform mechanical work), causing cell cycle arrest and cell death by apoptosis (a type of programmed cell death). This has an antiproliferative action (suppresses cell growth) and is thought to be the way that Klisyri works to clear actinic keratosis lesions.

Klisyri was FDA-approved on December 14, 2020.

Klisyri side effects

The most common side effects of Klisyri affecting 2% or more people include:

• local skin reactions, such as redness, flaking, or peeling
• itch at the site of the application
• pain at the site of application.

Warnings and serious side effects

Get emergency medical help if you have signs of an allergic reaction to Klisyri such as hives; difficulty breathing; or swelling of your face, lips, tongue, or throat.

Klisyri can cause serious side effects including:

• Eye irritation if Klisyri gets into the eye. Avoid transfer of the drug into the eyes or applying it around the eye area. If accidental exposure occurs, flush your eyes with water and seek medical care
• Severe local skin reactions can occur, such as blisters, pus, ulcers, or skin breakdown in the treated area. Do not start using Klisyri until your skin has healed from any previous drug or surgical treatment. Call your doctor at once if you have severe skin irritation or swelling. Some redness, flaking, scaling, or peeling of treated skin is to be expected.

It is not known if Klisyri ointment is safe and effective in children less than 18 years of age.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to the FDA .

Before taking this medicine

Tell your doctor about all other medicines or treatments you are receiving to treat actinic keratosis. You may need to delay starting Klisyri until your skin has healed from other treatments. Also, tell your doctor:

• if you have other skin problems in the areas you will treat with this medicine
• are pregnant or intending to become pregnant
• are breastfeeding.

Pregnancy

There is no data on the use of Klisyri during pregnancy, but animal studies using many times the recommended dosage have shown an association with birth defects. Talk to your doctor about the risks versus benefits of using Klisyri during pregnancy.

Breastfeeding

It is not known if Klisyri passes into human milk. Talk to your doctor about the best way to feed your baby if you are breastfeeding.

How should I use Klisyri ointment?

Use Klisyri ointment exactly as prescribed by your doctor. Follow all directions on your prescription label and read all medication guides or instruction sheets.

Use Klisyri only on the face or scalp and only on the skin areas affected by actinic keratosis.

• Do not take it by mouth or put it near your eyes. Rinse with water if this medicine gets in your mouth or on your lips. Wipe away from your eyes if it gets near your eyes.

Klisyri is usually applied once per day for 5 days in a row. Follow your doctor’s dosing instructions very carefully.

• Apply a thin layer of Klisyri to the affected area only enough Klisyri ointment to cover the skin area affected by actinic keratosis.
• Do not cover the treated skin area with a bandage.
• Avoid washing or touching the treated skin for at least 8 hours after applying this medicine.
• Wash your hands with soap and water after applying this medicine.

Klisvri dosing information

• Each single dose packet of Klisyri is for one day use. Throw away the packet after use, even if there is still medicine left inside.
• Use another packet from the carton for the next day.
• Apply Klisvri for 5 days in a row then stop applying it.
• Only apply to affected areas on the face and scalp. Avoid the eyes, mouth, and nostrils.

There is enough Klisyri in a 1-unit dose packet to cover up to 25 cm² treatment field on the face or balding scalp.

Each carton of Klisyri contains 5 single-dose packets. Use one packet a day for 5 consecutive days. Throw away each packet after use, do not save for the next day.

What to avoid

Do not use Klisyri ointment in, around, or near your eyes, mouth, or lips. If contact does occur, rinse with water and call your doctor right away.

Do not share Klisyri with another person, even if they have the same symptoms you have.

What happens if I miss a dose?

Apply the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not apply two doses at one time.

What is Opzelura?

Opzelura is used to treat atopic dermatitis (eczema) and nonsegmental vitiligo. It is a topical cream that is applied thinly twice a day. Do not exceed the maximum dose of (1 x 60-gram tube/week or 1 x 100-gram tube/week).

Opzelura works by blocking JAK1 and JAK2 enzymes, which normally help immune signals communicate between cells. These enzymes activate STAT proteins that travel to the cell nucleus to control gene expression. By inhibiting JAKs, Opzelura disrupts this signaling pathway, reducing overactive immune responses that cause inflammatory skin conditions like vitiligo and atopic dermatitis. It belongs to the drug class called kinase inhibitors.

Opzelura (ruxolitinib 1.5%) gained FDA approval on September 21, 2021. There is no generic.

FDA approvals and indications

Opzelura is FDA approved for:

• Mild to moderate atopic dermatitis in non-immunocompromised adults and children 12 years of age and older whose disease is not well-controlled with topical prescription therapies or when those therapies are not recommended (short-term and non-continuous chronic treatment only)
• Nonsegmental vitiligo in adults and children 12 years of age and older.

The use of Opzelura along with therapeutic biologics, other JAK inhibitors, or strong immunosuppressants such as azathioprine or cyclosporine is not recommended.

It is not known if this medicine is safe and effective in children less than 12 years of age with atopic dermatitis or nonsegmental vitiligo.

Important: Opzelura is for use on the skin only. Do not use Opzelura in your eyes, mouth, or vagina.

Side effects

The most common side effects of Opzelura for atopic dermatitis are:

• common cold (nasopharyngitis)
• diarrhea
• bronchitis
• ear infection
• increase in a type of white blood cell
• (eosinophil) count
• hives
• inflamed hair pores (folliculitis)
• swelling of the tonsils (tonsillitis)
• runny nose (rhinorrhea).

The most common side effects of Opzelura for non-segmental vitiligo are:

• acne at the application site
• itching at the application site
• common cold (nasopharyngitis)
• headache
• urinary tract infection
• redness at the application site
• fever.

Serious side effects and warnings

Opzelura may cause the following serious side effects:

• Serious Infections. Opzelura contains ruxolitinib. Ruxolitinib belongs to a class of medicines called Janus kinase (JAK) inhibitors. JAK inhibitors are medicines that affect your immune system. JAK inhibitors can lower the ability of your immune system to fight infections. Some people have had serious infections while taking JAK inhibitors by mouth, including tuberculosis (TB), and infections caused by bacteria, fungi, or viruses that can spread throughout the body. Some people have been hospitalized or died from these infections. Some people have had serious infections of their lungs while using Opzelura.
  • Your healthcare provider should watch you closely for signs and symptoms of TB during treatment with Opzelura.
  • Opzelura should not be used in people with an active, serious infection, including localized infections. You should not start using Opzelura if you have any kind of infection unless your healthcare provider tells you it is okay. You may be at a higher risk of developing shingles (herpes zoster) while using Opzelura.
  • Before starting Opzelura, tell your healthcare provider about all your current medical conditions (see below).

After starting Opzelura, call your healthcare provider right away if you have any symptoms of an infection. Opzelura can make you more likely to get infections or make any infections worse that you have. If you get a serious infection, your healthcare provider may stop your treatment with Opzelura until your infection is controlled.

• Increased risk of death due to any reason (all causes). Increased risk of death has occurred in people 50 years of age and older who have at least 1 heart disease (cardiovascular) risk factor and are taking a medicine in the class of medicines called JAK inhibitors by mouth.
• Cancer and immune system problems. Opzelura may increase your risk of certain cancers by changing the way your immune system works.
  • Lymphoma and other cancers have happened in people taking a medicine in the class of medicines called JAK inhibitors by mouth.
  • People taking JAK inhibitors by mouth have a higher risk of certain cancers, including lymphoma and lung cancer, especially if they are a current or past smoker.
  • Some people have had skin cancers while using Opzelura. Your healthcare provider will regularly check your skin during your treatment with Opzelura. Limit the amount of time you spend in the sunlight. Wear protective clothing when you are in the sun and use a broad-spectrum sunscreen.
  • Tell your healthcare provider if you have ever had any type of cancer.
• Increased risk of major cardiovascular events. Increased risk of major cardiovascular events such as heart attack, stroke, or death has occurred in people 50 years of age and older who have at least 1 heart disease (cardiovascular) risk factor and are taking a medicine in the class of medicines called JAK inhibitors by mouth, especially in current or past smokers. Get emergency help right away if you have any symptoms of a heart attack or stroke while using Opzelura, including:
  • discomfort in the center of your chest that lasts for more than a few minutes, or that goes away and comes back
  • severe tightness, pain, pressure, or heaviness in your chest, throat, neck, or jaw
  • pain or discomfort in your arms, back, neck, jaw, or stomach
  • shortness of breath with or without chest discomfort
  • breaking out in a cold sweat
  • nausea or vomiting
  • feeling lightheaded
  • weakness in one part or on one side of your body
  • slurred speech.
• Blood clots. Blood clots in the veins of your legs (deep vein thrombosis, DVT) or lungs (pulmonary embolism, PE) can happen in some people taking Opzelura. This may be life-threatening. Blood clots in the veins of the legs (deep vein thrombosis, DVT) and lungs (pulmonary embolism, PE) have happened more often in people who are 50 years of age and older and with at least 1 heart disease (cardiovascular) risk factor, taking a medicine in the class of medicines called JAK inhibitors by mouth. Tell your healthcare provider if you have had blood clots in the veins of your legs or lungs in the past.

Tell your healthcare provider right away if you have any signs and symptoms of blood clots during treatment with Opzelura, including:

• • swelling, pain, or tenderness in one or both legs
  • sudden, unexplained chest or upper back pain
  • shortness of breath or difficulty breathing
• Low blood cell counts. Opzelura may cause low platelet counts (thrombocytopenia), low red blood cell counts (anemia), and low white blood cell counts (neutropenia). If needed, your healthcare provider will do a blood test to check your blood cell counts during your treatment with Opzelura and may stop your treatment if signs or symptoms of low blood cell counts happen. Tell your healthcare provider right away if you develop or have worsening of any of these symptoms:
  • unusual bleeding o shortness of breath
  • bruising
  • fever
  • tiredness.
• Cholesterol increases. An increase in cholesterol levels has been reported in people when ruxolitinib is taken by mouth. Tell your healthcare provider if you have high levels of fat in your blood (high cholesterol or triglycerides)

These are not all of the possible side effects of Opzelura. Call your doctor for medical advice about side effects.

Before applying

Before using Opzelura, tell your healthcare provider about all of your medical conditions, including if you:

• have an infection
• are a current or past smoker
• have had a heart attack, other heart problems, or a stroke
• have or have had low white or red blood cell counts
• have high levels of fat in your blood (high cholesterol or triglycerides)
• are pregnant or plan to become pregnant
• are breastfeeding or plan to breastfeed.

Pregnancy

It is not known if Opzelura will harm your unborn baby.

Pregnancy Exposure Registry. There is a pregnancy exposure registry for individuals who use Opzelura during pregnancy. The purpose of this registry is to collect information about your health and your baby’s. If you become exposed to Opzelura during pregnancy, you and your healthcare provider should report exposure to Incyte Corporation at 1-855-463-3463 or by visiting www.opzelura.pregnancy.incyte.com.

Breastfeeding

It is not known if Opzelura passes into your breast milk. Do not breastfeed during treatment with Opzelura and for about 4 weeks after the last dose.

How should I use Opzelura?

Opzelura is for use on the skin only. Do not use Opzelura in your eyes, mouth, or vagina. Use it exactly as your healthcare provider tells you. Ask your healthcare provider if you have questions about applying Opzelura.

• Apply a thin layer of Opzelura 2 times a day to affected areas.

Do not use more than one 60-gram tube each week or more than one 100-gram tube every 2 weeks.

If you are using Opzelura for atopic dermatitis, stop using Opzelura when your signs and symptoms of atopic dermatitis, such as itching, rash, and redness, go away, or as directed by your healthcare provider.

• Tell your healthcare provider if your symptoms do not improve within 8 weeks of treatment.

If you are using Opzelura for non-segmental vitiligo, tell your healthcare provider if your treated skin does not improve within 24 weeks of treatment.

• Wash your hands after applying Opzelura, unless your hands are being treated. If someone else applies Opzelura, they should wash their hands after applying Opzelura.

Dosing information

Dose of Opzelura for atopic dermatitis

• Apply a thin layer 2 times a day to affected areas of up to 20% body surface area.

Dose of Opzelura for nonsegmental vitiligo

• Apply a thin layer 2 times a day to affected areas of up to 10% body surface area.

What other drugs will affect Opzelura?

Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.

Know the medicines you take. Keep a list of them to show your healthcare provider and pharmacist when you get a new medicine.