What is Protopic?

Protopic (Protopic)is a topical macrolide immunosuppressant. It works by decreasing cell activity in the body’s immune system which helps to slow down the growth of atopic dermatitis (eczema) on your skin.

Protopic is used to treat severe atopic dermatitis (eczema).

Protopic may also be used for purposes not listed in this medication guide.

Protopic indications

Protopic, both 0.03% and 0.1% for adults, and only 0.03% for children aged 2 to 15 years, is indicated as second-line therapy for the short-term and non-continuous chronic treatment of moderate to severe atopic dermatitis in non-immunocompromised adults and children who have failed to respond adequately to other topical prescription treatments for atopic dermatitis, or when those treatments are not advisable.

Protopic is not indicated for children younger than 2 years of age.

How should I use Protopic?

Use Protopic as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• Protopic comes with an extra patient information sheet called a Medication Guide. Read it carefully. Read it again each time you get Protopic refilled.
• Protopic is for external use only. Do not get Protopic in your eyes, nose, or mouth.
• Dry your skin completely after a bath or shower before applying Protopic.
• Wash your hands before using Protopic.
• Apply a thin layer of Protopic to the affected area only. Use the smallest amount needed to control your condition. Gently rub the medicine in until it is evenly distributed. Wash your hands after applying Protopic (if hands are not an area of treatment).
• If you are a caregiver applying Protopic to someone else’s skin, wash your hands with soap and water after applying Protopic.
• Do not bathe, shower, or swim right after applying Protopic. This could wash off the ointment.
• Do not cover the treated area with bandages or other dressings or wraps, unless otherwise directed by your doctor.
• Stop using Protopic when the signs and symptoms of the condition (eg, itching, rash, redness) go away, unless your doctor directs you otherwise.
• If you miss a dose of Protopic, use it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not use 2 doses at once.

Ask your health care provider any questions you may have about how to use Protopic.

Uses of Protopic in details

Protopic is used to treat atopic dermatitis (dry and itchy skin; also called eczema) of moderate to severe grade.

Protopic description

Each gram of ointment also contains a base of mineral oil, paraffin, propylene carbonate, white petrolatum and white wax.

Protopic, a macrolide immunosuppressant produced by Streptomyces tsukubaensis, is [3S-[3R*[E(1S*,3S*,4S*)],4S*,5R*,8S*,9E,12R*,14R*,15S*,16R*,18S*,19S*,26aR*]]-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-hexadecahydro-5,19-dihydroxy-3[2-(4-hydroxy-3-methoxycyclohexyl)-1-methylethenyl]-14,16-dimethoxy-4,10,12,18-tetramethyl-8-(2-propenyl)-15,19-epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclotricosine-1,7,20,21(4H,23H)-tetrone monohydrate. It has an empirical formula of C44H69NO12·H2O and a formula weight of 822.05.

Protopic is for dermatologic use only and not for ophthalmic use.

Protopic dosage

Adult Protopic 0.03% and 0.1%

• Apply a thin layer of PROTOPIC (Protopic) Ointment to the affected skin twice daily. The minimum amount should be rubbed in gently and completely to control signs and symptoms of atopic dermatitis. Stop using when signs and symptoms of atopic dermatitis resolve.
• If signs and symptoms (e.g. itch, rash, and redness) do not improve within 6 weeks, patients should be re-examined by their healthcare provider to confirm the diagnosis of atopic dermatitis.
• Continuous long-term use of topical calcineurin inhibitors, including Protopic should be avoided, and application should be limited to areas of involvement with atopic dermatitis.

The safety of Protopic under occlusion, which may promote systemic exposure, has not been evaluated. Protopic should not be used with occlusive dressings.

Pediatric – For Children 2-15 Years Protopic 0.03%

• Apply a thin layer of PROTOPIC (Protopic) Ointment, 0.03% to the affected skin twice daily. The minimum amount should be rubbed in gently and completely to control signs and symptoms of atopic dermatitis. Stop using when signs and symptoms of atopic dermatitis resolve.
• If signs and symptoms (e.g. itch, rash, and redness) do not improve within 6 weeks, patients should be re-examined by their healthcare provider to confirm the diagnosis of atopic dermatitis.
• Continuous long-term use of topical calcineurin inhibitors, including Protopic should be avoided, and application should be limited to areas of involvement with atopic dermatitis.

The safety of Protopic under occlusion, which may promote systemic exposure, has not been evaluated. Protopic should not be used with occlusive dressings.

How supplied

PROTOPIC® (Protopic) Ointment 0.03%NDC 0469-5201-30 Product Code 520130 30 gram laminate tube NDC 0469-5201-60 Product Code 520160 60 gram laminate tube NDC 0469-5201-11 Product Code 520111 100 gram laminate tube

PROTOPIC® (Protopic) Ointment 0.1% NDC 0469-5202-30 Product Code 520230 30 gram laminate tube NDC 0469-5202-60 Product Code 520260 60 gram laminate tubeStore at room temperature 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F).

Marketed by: Astellas Pharma US, Inc. Deerfield, IL 60015-2548. Manufactured by: Astellas Toyama Co., Ltd. Toyama Plant, 2-178 Kojin-machi, Toyama 9300809, Japan. Revised: 11/2011

Protopic interactions

Formal topical drug interaction studies with Protopic ointment have not been conducted.Protopic is not metabolised in human skin, indicating that there is no potential for percutaneous interactions that could affect the metabolism of Protopic.

Systemically available Protopic is metabolised via the hepatic cytochrome P-450 3A4 (CYP3A4). Systemic exposure from topical application of Protopic ointment is low (<1 ng/mL) and is unlikely to be affected by concomitant use of substances known to be inhibitors of CYP3A4. However, the possibility of interactions cannot be ruled out and the concomitant systemic administration of known CYP3A4 inhibitors (eg, erythromycin, itraconazole, ketoconazole and diltiazem) in patients with widespread and/or erythrodermic disease should be done with caution.

A potential interaction between vaccination and application of Protopic has not been investigated. Because of the potential risk of vaccination failure, vaccination should be administered prior to commencement of treatment, or during a treatment-free interval with a period of 14 days between the last application of Protopic and the vaccination. In case of live attenuated vaccination, this period should be extended to 28 days or the use of alternative vaccines should be considered.

Incompatibilities: Not applicable.

Protopic side effects

Applies to Protopic: topical ointmentAs well as its needed effects, Protopic (the active ingredient contained in Protopic) may cause unwanted side effects that require medical attention.

Major Side Effects

If any of the following side effects occur while taking Protopic, check with your doctor immediately:

Incidence not known:

• Agitation
• black, tarry stools
• bloody urine
• burning or stinging sensation of the face
• change in size, shape, or color of an existing mole
• coma
• confusion
• convulsions
• decreased frequency or amount of urine
• depression
• fever
• general feeling of illness
• growth or bump on skin
• hostility
• increase in bone pain
• increased blood pressure
• increased thirst
• irritability
• lethargy
• looks very ill
• loss of appetite
• loss of bladder control
• lower back or side pain
• mole that leaks fluid or bleeds
• muscle spasm or jerking of all extremities
• muscle twitching
• nausea
• new mole
• rapid weight gain
• red rash with watery, yellow-colored, or pus filled blisters
• redness of the face
• seizures
• small, red skin lesion, growth, or bump usually on the face, ears, neck, hands, or arms
• sore that will not heal
• spider-like blood vessels on the face
• stupor
• sudden loss of consciousness
• swelling of the face, ankles, lower legs, hands, or fingers
• swollen glands
• thick, yellow to honey-colored crusts
• unusual tiredness or weakness
• vomiting
• weight gain
• weight loss
• yellow skin and eyes

Minor Side Effects

Some Protopic side effects may not need any medical attention. As your body gets used to the medicine these side effects may disappear. Your health care professional may be able to help you prevent or reduce these side effects, but do check with them if any of the following side effects continue, or if you are concerned about them:

More common:

• Cough
• fever
• general aches and pains
• headache
• itching skin—in children
• loss of appetite
• skin burning
• skin flushing in areas of ointment application when drinking alcohol
• sneezing
• weakness

Less common:

• Acid or sour stomach
• acne
• back pain
• belching
• burning, itching, or pain in hairy areas
• chills
• cyst
• flushing
• heartburn
• increased sensitivity to sunlight
• increased skin sensitivity
• indigestion
• itching eyes
• joint pain
• muscle aches or pain
• pain in the eye
• pain or tenderness around the eyes and cheekbones
• pus at root of the hair
• rash
• redness in the eye
• runny nose
• severe skin rash or hives
• skin blisters—in children
• skin tingling
• stomach discomfort, upset, or pain
• stuffy nose
• swelling of the eye, eyelid, or inner lining of the eyelid
• swollen glands
• tightness of the chest
• troubled breathing or wheezing
• watery eyes

Protopic contraindications

You should not use Protopic if you are allergic to it.

Before using Protopic, tell your doctor if you have skin cancer or a skin infection (including herpes or chickenpox), any genetic skin disorder (such as Netherton’s syndrome), a weak immune system, kidney disease, or swelling, redness, or irritation of large areas of your skin.

Protopic can lower the blood cells that help your body fight infections. This can make it easier for you to get sick from a virus such as chicken pox or herpes (cold sores or shingles). Tell your doctor if you have been exposed to any illness.

Avoid sunlight, sun lamps, tanning beds, and phototherapy treatments with UVA or UVB light. If you must be outdoors, wear loose clothing over the skin areas treated with Protopic. Do not use sunscreen on treated skin unless your doctor has told you to.

Talk to your doctor if your skin condition does not improve after using Protopic for 6 weeks.

Do not use this medication on a child younger than 2 years old.

Some people have developed skin cancer or lymphoma after using Protopic or pimecrolimus (Elidel). However, it is not known if either of these medicines causes skin cancer or lymphoma. Talk to your doctor about your individual risk.

Active ingredient matches for Protopic:

Tacrolimus topical in Argentina, Austria, Belgium, Canada, Chile, China, Colombia, Czech Republic, Denmark, Ecuador, Finland, France, Georgia, Germany, Greece, Hong Kong, Hungary, Iceland, Indonesia, Ireland, Israel, Italy, Japan, Latvia, Lithuania, Malaysia, Mexico, Netherlands, Norway, Oman, Peru, Philippines, Poland, Portugal, Romania, Singapore, Slovakia, Slovenia, South Africa, South Korea, Spain, Sweden, Switzerland, Taiwan, Thailand, Turkey, United Kingdom, United States, Uruguay, Venezuela, Vietnam.

03% Ointment/Tacrolimus 0

Tacrolimus in United States, United Kingdom, Japan, Sweden, France, Finland, Norway, Italy, Germany, Canada, Portugal, Netherlands, Poland, Indonesia, Czech Republic, Ireland, Spain, Romania.

Tacrolimus monohydrate in Thailand.

Unit description / dosage (Manufacturer)Price, USD Ointment; Topical; Tacrolimus 0.03% Ointment; Topical; Tacrolimus 0.1% Protopic 0.03 % x 10 g x 1’s$ 23.08 Protopic 0.1 % x 10 g x 1’s$ 28.68 Protopic 0.03 % x 10 g$ 43.36 Protopic 0.1 % x 10 g$ 47.78 Protopic 0.03 % x 5 g Protopic 0.03 % x 30 g Protopic 0.1 % x 5 g Protopic 0.1 % x 30 g Protopic 0.03 % x 30 g x 1’s Protopic 0.1 % x 30 g x 1’s Protopic 0.03 % x 1 tube 10 g Protopic 0.1 % x 1 tube 10 g Protopic oint 0.03% 10 g x 1’s (Johnson & Johnson)$ 45.53 Protopic oint 0.1% 10 g x 1’s (Johnson & Johnson)$ 50.18 Protopic oint 0.03 % 10 g x 1’s (Janssen) Protopic oint 0.1 % 10 g x 1’s (Janssen) Protopic oint 0.03 % 30 g x 1’s (Janssen) Protopic oint 0.1 % 30 g x 1’s (Janssen) Protopic ointment .3 mg/g (Astellas Pharma US Inc. (US)) Protopic Ointment 0.1 % (Leo Pharma A/S (EU)) Protopic ointment 1 mg/g (LEO Pharma Inc. (US)) Protopic ointment 0.03 % (Leo Pharma Inc (Canada))

List of Protopic substitutes (brand and generic names):

Prograft-5 (Luxembourg) Protopic 0,03% (Austria, Hungary) Protopic 0,1% (Austria, Hungary) Protopic 0.01% (Croatia (Hrvatska)) Protopic Ointment Protopic topical Protopy (Latvia) Ointment; Topical; Tacrolimus Monohydrate 0.03% (Astellas) Regraf (Georgia) RENGRAF RENGRAF 0.5MG CAPSULE 1 strip / 10 capsules each (Abbott India Ltd)$ 2.97 RENGRAF 1MG CAPSULE 1 strip / 10 capsules each (Abbott India Ltd)$ 5.81 Rengraf 0.5mg Capsule (Abbott India Ltd)$ 0.30 Rengraf 1mg Capsule (Abbott India Ltd)$ 0.58 Rocimus (Vietnam) Rocimus oint 0.03% w/w 10 g x 1’s (Mega Lifesciences)$ 12.00 ROLIMUS ROLIMUS 5MG TABLET 1 strip / 10 tablets each (Cipla Ltd)$ 131.14 ROLIMUS TABLET 1 strip / 10 tablets each (Cipla Ltd)$ 370.37 Rolimus 10mg Tablet (Cipla Ltd)$ 38.89 Sandoz Tacrolimus (Canada) Sandoz Tacrolimus capsule / immediate release 1 mg (Sandoz Canada Incorporated (Canada)) Sandoz Tacrolimus capsule / immediate release 5 mg (Sandoz Canada Incorporated (Canada)) Sandoz Tacrolimus capsule / immediate release 0.5 mg (Sandoz Canada Incorporated (Canada)) Seagraf Seagraf 1 mg Capsule (Micro Labs Ltd)$ 0.59 Seegraf (India) Seegraf 0.5mg TAB / 10 (Foresee (Micro Labs))$ 3.20 Seegraf 1mg TAB / 10 (Foresee (Micro Labs))$ 5.87 0.5 mg x 10’s (Foresee (Micro Labs))$ 3.20 1 mg x 10’s (Foresee (Micro Labs))$ 5.87 Seegraf 1 mg Tablet (Foresee (Micro Labs))$ 0.59 Seegraf 0.5 mg Tablet (Foresee (Micro Labs))$ 0.32 SEEGRAF 1MG CAPSULE 1 strip / 10 capsules each (Foresee (Micro Labs))$ 8.65 Seegraf cap 0.5 mg 6 x 10’s (Foresee (Micro Labs)) Seegraf cap 1 mg 6 x 10’s (Foresee (Micro Labs)) SEEGRAF tab 0.5 mg x 10’s (Foresee (Micro Labs))$ 3.20 SEEGRAF tab 1 mg x 10’s (Foresee (Micro Labs))$ 7.38 Seegraf 1mg Capsule (Foresee (Micro Labs))$ 0.87 Sineczem (Colombia) Supregraf (Poland) Susciter (Georgia) T Lim Power T Lim Power Skin 20 gm Ointment (La Med India)$ 5.56 T-Inmun (Chile, Peru) Capsule; Oral; Tacrolimus 1 mg Ointment; Topical; Tacrolimus 0.03% Ointment; Topical; Tacrolimus 0.1% T-TOP (India) T-TOP Cream/ Gel/ Ointment / 0.03% / 10gm units (Wallace (Rivella))$ 1.57 T-TOP Cream/ Gel/ Ointment / 0.1% / 10gm units (Wallace (Rivella))$ 4.44 T-Top 0.03%w/w OINT / 10g (Wallace (Rivella))$ 1.71 See 969 substitutes for Protopic

References

1. DailyMed. “TACROLIMUS: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).”. https://dailymed.nlm.nih.gov/dailyme… (accessed September 17, 2018).
2. PubChem. “tacrolimus”. https://pubchem.ncbi.nlm.nih.gov/com… (accessed September 17, 2018).
3. DrugBank. “tacrolimus”. http://www.drugbank.ca/drugs/DB00864 (accessed September 17, 2018).