protopic
Protopic (Tacrolimus) is a calcineurin inhibitor immunosuppressant used to treat Atopic Dermatitis, Graft Vs Host Disease.
Tacrolimus · by Leo Pharma As
Available as a generic: Tacrolimus
Key facts
- Active ingredient
- Tacrolimus
- Drug class
- Calcineurin Inhibitor Immunosuppressant
- Form
- Topical
- Strength
- Tacrolimus 0.03% · Tacrolimus 0.1%
- Type
- Prescription (Rx)
- Brand or generic
- Brand-name
- May treat
- atopic dermatitis, graft vs host disease
- Manufacturer
- Leo Pharma As
- What the pharmacy pays
- ~$0.65 per gm — not your price
- FDA application
- NDA050777
What is Protopic?
From the FDA label:Tacrolimus Ointment contains tacrolimus, a macrolide immunosuppressant produced by Streptomyces tsukubaensis . It is for topical dermatologic use only. Chemically, tacrolimus is designated as [3 S -[3 R *[ E (1 S *,3 S *,4 S *)],4 S *,5 R *,8 S *,9 E ,12 R *,14 R *,15 S *,16 R *,18 S *,19 S *,26a R *]]-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 the following structural formula: Tacrolimus has an empirical formula of C 44 H 69 NO 12 ∙H 2 O and a formula weight of 822.03. Each gram of Tacrolimus Ointment contains (w/w) either 0.03% or 0.1% of tacrolimus in a base of mineral oil with all- rac -α-tocopherol, paraffin, propylene carbonate, white petrolatum with butylhydroxytoluene, and white wax. Chemical Structure
How to use
Adult Tacrolimus Ointment 0.03% and 0.1% Apply a thin layer of Tacrolimus 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 Tacrolimus Ointment should be avoided, and application should be limited to areas of involvement with atopic dermatitis. The safety of Tacrolimus Ointment under occlusion, which may promote systemic exposure, has not been evaluated. Tacrolimus Ointment should not be used with occlusive dressings. Pediatric – For Children 2-15 Years Tacrolimus Ointment 0.03% Apply a thin layer of Tacrolimus 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…
Side effects
No phototoxicity and no photoallergenicity were detected in clinical studies with 12 and 216 normal volunteers, respectively. One out of 198 normal volunteers showed evidence of sensitization in a contact sensitization study. In three 12 week randomized vehicle-controlled studies and four safety studies, 655 and 9,163 patients respectively, were treated with Tacrolimus Ointment. The duration of follow-up for adult and pediatric patients in the safety studies is tabulated below. Duration of Follow-up in Four Open-label Safety Studies Time on Study Adult Pediatrics Total < 1 year 4682 4481 9163 ≥ 1 year 1185 1349 2534 ≥ 2 years 200 275 475 ≥ 3 years 118 182 300 The following table depicts the adjusted incidence of adverse events pooled across the 3 identically designed 12-week controlled studies for patients in vehicle, Tacrolimus Ointment 0.03%, and Tacrolimus Ointment 0.1% treatment groups. The table also depicts the unadjusted incidence of adverse events in four safety studies, regardless of relationship to study drug. Incidence of Treatment Emergent Adverse Events 12-Week, Randomized, Double-Blind, Phase 3 Studies 12-Week Adjusted Incidence Rate (%) Open-Label Studies (up to 3 years) 0.1% and 0.03% Tacrolimus Ointment Incidence Rate (%) Adult Pediatric Adult Pediatric Total Vehicle (n=212) % 0.03% Tacrolimus Ointment (n=210) % 0.1% Tacrolimus Ointment (n=209) % Vehicle…
Warnings
Important safety information
WARNING Long-term Safety of Topical Calcineurin Inhibitors Has Not Been Established Although a causal relationship has not been established, rare cases of malignancy (e.g., skin and lymphoma) have been reported in patients treated with topical calcineurin inhibitors, including Tacrolimus Ointment. Therefore: Continuous long-term use of topical calcineurin inhibitors, including Tacrolimus Ointment, in any age group should be avoided, and application limited to areas of involvement with atopic dermatitis. Tacrolimus Ointment is not indicated for use in children less than 2 years of age. Only 0.03% Tacrolimus Ointment is indicated for use in children 2-15 years of age. Prolonged systemic use of calcineurin inhibitors for sustained immunosuppression in animal studies and transplant patients following systemic administration has been associated with an increased risk of infections, lymphomas, and skin malignancies. These risks are associated with the intensity and duration of immunosuppression. Based on the information above and the mechanism of action, there is a concern about potential risk with the use of topical calcineurin inhibitors, including Tacrolimus Ointment. While a causal relationship has not been established, rare cases of skin malignancy and lymphoma have been reported in patients treated with topical calcineurin inhibitors, including Tacrolimus Ointment. Therefore: Tacrolimus Ointment should not be used in immunocompromised adults and children. If signs and symptoms of atopic dermatitis do not improve within 6 weeks, patients should be re-examined by their healthcare provider and their diagnosis be confirmed (see PRECAUTIONS: General ). The safety of Tacrolimus Ointment has not been established beyond one year of non-continuous use. (See CLINICAL PHARMACOLOGY , boxed WARNING , INDICATIONS AND USAGE , and DOSAGE AND ADMINISTRATION ).
Who should not take Protopic
Tacrolimus Ointment is contraindicated in patients with a history of hypersensitivity to tacrolimus or any other component of the ointment.
Overdose — what happens if you take too much
Tacrolimus Ointment is not for oral use. Oral ingestion of Tacrolimus Ointment may lead to adverse effects associated with systemic administration of tacrolimus. If oral ingestion occurs, medical advice should be sought.
U.S. Poison Control: call or text 1-800-222-1222 (free, 24/7). In an emergency call 911. From the FDA label; not medical advice.
Interactions
Formal topical drug interaction studies with Tacrolimus Ointment have not been conducted. Based on its extent of absorption, interactions of Tacrolimus Ointment with systemically administered drugs are unlikely to occur but cannot be ruled out (see CLINICAL PHARMACOLOGY ). The concomitant administration of known CYP3A4 inhibitors in patients with widespread and/or erythrodermic disease should be done with caution. Some examples of such drugs are erythromycin, itraconazole, ketoconazole, fluconazole, calcium channel blockers and cimetidine.
Foods & drinks to be careful with
Well-established interactions for this medicine’s drug class, summarized from public health authorities. General information, not medical advice — always confirm with your pharmacist or the label.
Grapefruit & grapefruit juice
Watch out for: grapefruit and grapefruit juice (and, for some drugs, Seville oranges).
Grapefruit blocks a gut enzyme (CYP3A4) that normally breaks this medicine down, so more of it can enter your blood — raising the risk of side effects.
What to do: Avoid grapefruit and grapefruit juice with this medicine unless your pharmacist or the label says it's fine — check, because not every drug in a class is affected the same way.
Source: Grapefruit Juice and Some Drugs Don't Mix — U.S. FDA
Drug class
How this class works, per Calcineurin Inhibitors - StatPearls - NCBI Bookshelf.
May treat (source: NIH RxClass)
See how Protopic ranks — best-rated calcineurin inhibitor immunosuppressant for:
Dosage forms
Topical
The forms currently marketed in the U.S., per the FDA National Drug Code Directory.
Ways to save
Ask for the generic
Same active ingredient, far cheaper. Is there a generic? →
Request a 90-day supply
Bulk fills usually lower the per-dose price vs monthly refills.
Use copay cards
Manufacturer copay cards & patient-assistance programs — especially for brand drugs.
Compare alternatives
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Frequently asked questions
- What does Protopic treat?
- Protopic (Tacrolimus) may be used to treat atopic dermatitis, graft vs host disease, based on NIH RxClass drug-classification data (conditions a drug may treat — not a verbatim copy of the FDA-approved label). This is general reference, not medical advice.
- How does Protopic work?
- Protopic is a calcineurin inhibitor immunosuppressant. Calcineurin inhibitors block an enzyme called calcineurin inside immune T-cells, which stops the cells from making interleukin-2 and other signaling chemicals. This keeps T-cells from activating and multiplying, dialing down the immune attack that drives organ rejection or autoimmune disease.
- How much does Protopic cost?
- Nobody can tell you what you will pay — your price is set by your insurer's formulary, your deductible and the pharmacy's markup, and none of those are published. What IS published is what the pharmacy paid to acquire it: about $0.65 per gm, per the CMS NADAC survey. Treat that as the floor, not the quote — ask the pharmacist for the cash price as well as your copay, because for cheap generics the cash price often wins.
- Is there a coupon or discount for Protopic?
- pharmaranks is an independent ratings site, not a pharmacy — we don't issue coupons or sell Protopic. To pay less, ask your prescriber or pharmacist whether a generic equivalent exists, check the manufacturer's copay/savings card and patient-assistance program, and compare a pharmacy discount card against your insurance copay. Prices vary by pharmacy, insurance, and location, so always confirm at the counter. This is general reference, not medical or financial advice.
- Who makes Protopic?
- Protopic is marketed by Leo Pharma As. You can see Leo Pharma As's full profile, rating, and other products on pharmaranks.
- Is Protopic a brand-name or generic drug?
- Protopic is a brand-name product with the active ingredient Tacrolimus. Lower-cost generic equivalents containing Tacrolimus are available — ask your pharmacist.
- Is Protopic available over the counter?
- No. Protopic is a prescription (Rx) medication in the US — you need a prescription from a licensed clinician (in person or via telehealth); it isn't sold over the counter. For some conditions there are OTC alternatives — ask your pharmacist.
- What forms does Protopic come in?
- Protopic is currently marketed as topical, per the FDA's National Drug Code Directory.
- What class of drug is Protopic?
- Protopic is classified as calcineurin inhibitor immunosuppressant, per the FDA's Established Pharmacologic Class.
- Is Protopic FDA-registered?
- Protopic is on record with the U.S. FDA under application number NDA050777. You can verify this on its official FDA label.
- Is Protopic safe?
- There's no single safe-or-not verdict, and we don't yet have a composite recall-safety score for Protopic. Review its FDA-label side effects and warnings below, and always consult a licensed professional.
- What are the side effects of Protopic?
- Protopic's side effects are taken directly from its FDA label. From the label: No phototoxicity and no photoallergenicity were detected in clinical studies with 12 and 216 normal volunteers, respectively. One out of 198 normal volunteers showed evidence of sensitization in a contact sensitization study.… Both common and serious reactions are documented in full on this page. This is general reference from the FDA, not medical advice — always consult a professional.
Clinical content sourced from the FDA label via openFDA (U.S. FDA). View the FDA label on DailyMed → Provided for general reference only — not medical advice. Always consult a licensed professional and the current prescribing information.
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