Topenoid
Topenoid Uses, Dosage, Side Effects, Food Interaction and all others data.
Topenoid is a retinoid prodrug which is converted to its active form, the cognate carboxylic acid of tazarotene, by rapid deesterification in animals and man. In cell culture and in vitro models of skin, tazarotene suppresses expression of MRP8, a marker of inflammation present in the epidermis of psoriasis patients at high levels. In human keratinocyte cultures, it inhibits cornified envelope formation, whose build-up is an element of the psoriatic scale.
Following topical application, tazarotene undergoes esterase hydrolysis to form its active metabolite, tazarotenic acid. When treating acne tazarotene may be taken in conjunction with an oral antibiotic. Topenoid has been shown in peer-reviewed double blinded studies to reduce: mottling and hyperpigmentation, sallowness, fine wrinkling and coarse wrinkling in sun damaged skin. Histological studies have shown that long term (greater than 1 year) use of Topenoid is associated with a significant reduction in atypical melanocytes and keratocytes - cells considered to be precursors of skin cancer. Some studies have shown long term use of Topenoid to be associated with increased collagen production and better organization of skin collagen bundles.
| Trade Name | Topenoid |
| Generic | Tazarotene |
| Tazarotene Other Names | Tazarotene, Tazarotène, Tazaroteno, Tazarotenum |
| Type | |
| Formula | C21H21NO2S |
| Weight | Average: 351.462 Monoisotopic: 351.129299611 |
| Protein binding | The active form of the drug, tazarotenic acid, is highly bound to plasma proteins (>99%). |
| Groups | Approved, Investigational |
| Therapeutic Class | Topical retinoid and related preparations |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Topenoid is used to treat plaque psoriasis of the skin. It also works to treat acne on the face.
Topenoid is also used to associated treatment for these conditions: Psoriasis Vulgaris (Plaque Psoriasis), Benign facial lentigines, Facial fine wrinkling, Facial hyperpigmentation, Facial hypopigmentation, Mild Acne vulgaris, Moderate Acne vulgaris
How Topenoid works
Although the exact mechanism of tazarotene action is not known, studies have shown that the active form of the drug (tazarotenic acid) binds to all three members of the retinoic acid receptor (RAR) family: RARa, RARb, and RARg, but shows relative selectivity for RARb, and RARg and may modify gene expression. It also has affinity for RXR receptors.
Dosage
Topenoid dosage
For psoriasis: Topenoid cream should be applied once per day, in the evening, to psoriatic lesions, using enough (2 mg/cm2) to cover only the lesion with a thin film. If a bath or shower is taken prior to application, the skin should be dried before applying the cream. If emollients are used, they should be applied at least one hour before application of Topenoid cream.
For acne: Cleanse the face gently. After the skin is dry, apply a thin layer (2mg/cm2) of Topenoid cream 0.1% once per day, in the evening, to the skin areas where acne lesions appear. Use enough to cover the entire affected area.
Side Effects
The most frequent adverse events reported with Topenoid cream were limited to the skin. Those occurring in 10 to 23% of patients, in descending order, included pruritus, erythema and burning. For acne treatment, in 10 to 30% patients, it is reported desquamation, dry skin, face pain, irritation and stinging sensation.
Toxicity
Excessive topical use may lead to marked redness, peeling, or discomfort. Oral ingestion of the drug may affect liver function causing hypertriglyceridemia. Other symptoms may include conjunctival irritation, hair loss, headache, edema, fatigue, dermatitis, nausea, and visual disturbances. Oral administration of this material to rats and rabbits at doses of 0.20 mg/kg/day (rabbits) and 0.25 mg/kg/day (rats) resulted in developmental toxicity. A no effect level of 0.05 mg/kg/day was established. Similar teratogenic effects have been reported for other retinoid compounds.
Precaution
Topenoid cream should be applied only to the affected areas. For external use only. Avoid contact with eyes, eyelids and mouth. If contact with eyes occurs, rinse thoroughly with water. Retinoids should not be used on eczematous skin, as they may cause severe irritation. Patients must be warned to use sunscreens and protective clothing when using Topenoid cream. Some individuals may experience excessive pruritus, burning, skin redness or peeling. If these effects occur, the medication should either be discontinued until the integrity of the skin is restored, or the dosing should be reduced
Interaction
Concomitant dermatologic medications and cosmetics that have a strong drying effect should be avoided. It is also advisable to "rest" a patient’s skin until the effects of such preparations subside before use of Topenoid cream is begun. Topical steroid may be hazardous in psoriasis; careful patient supervision is important. Consider if infection spreads. Do not use near a naked flame.
Food Interaction
No interactions found.Elimination Route
Minimal systemic absorption of tazarotene occurs due to its rapid metabolism in the skin to the active metabolite, tazarotenic acid, which can be systemically absorbed and further metabolized. Gender had no influence on the systemic bioavailability of tazarotenic acid.
Half Life
The half-life of the active form of the drug, tazarotenic acid, is approximately 18 hours in normal and psoriatic patients.
Elimination Route
Topenoid and tazarotenic acid were metabolized to sulfoxides, sulfones and other polar metabolites which were eliminated through urinary and fecal pathways.
Pregnancy & Breastfeeding use
Pregnancy: Topenoid is not recommended during pregnancy. It has been shown to cause serious birth defects and problems in animals. Be sure you have discussed this with your doctor.
Nursing Mothers: It is not known whether tazarotene passes into breast milk. However, Topenoid is not recommended during breast-feeding because it may cause unwanted effects in nursing babies.
Contraindication
Retinoids may cause fetal harm when administered to a pregnant woman. Topenoid cream is contraindicated in women who are or may become pregnant. If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug, treatment should be discontinued and the patient should be apprised of the potential hazard to the fetus. Women of childbearing potential should be warned to the potential risk and use adequate birth-control measures when Topenoid cream is used.
Special Warning
Pediatric Use: Studies of this medicine have been done only in adult patients, and there is no specific information comparing use of Topenoid in children up to 12 years of age (gel) and up to 18 years of age (cream) with use in other age groups.
Elderly Use (Over 65 year): There is no specific information comparing the use of Topenoid in the elderly with use in other age groups.
Acute Overdose
Excessive topical use cause marked redness, peeling or discomfort. Accidental oral ingestion produces similar adverse effects as those associated with excessive oral intake of Vitamin A or other retinoids. Monitor and take supportive measures as necessary.
Storage Condition
Store at 25° C.
Innovators Monograph
You find simplified version here Topenoid
Topenoid contains Tazarotene see full prescribing information from innovator Topenoid Monograph, Topenoid MSDS, Topenoid FDA label
FAQ
What is Topenoid used for?
Topenoid is used to treat acne.It is also used to treat psoriasis (a skin disease in which red, scaly patches form on some areas of the body).
How safe is Topenoid?
Topenoid was an effective, safe, and generally well-tolerated therapy for the treatment of acne vulgaris.
What are the common side effect of Topenoid?
More common side effects are include:
- Burning or stinging of the skin (severe)
- changes in color of the treated skin.
- deep grooves or lines in the skin.
- dryness, itching, peeling, or redness of the skin (severe)
- pain or swelling of the treated skin.
- skin rash (in patients with psoriasis only)
Should I use Topenoid every night?
You'll typically apply Topenoid once a day, in the evening. However, if your skin gets very irritated during treatment, talk with your doctor. (Skin irritation may appear as skin peeling, redness, or discomfort.) You may need to use Topenoid less often or stop using it for a time.
Is Topenoid safe during pregnancy?
Do not use Topenoid topical if you are pregnant.It could harm the unborn baby or cause birth defects. Use effective birth control to prevent pregnancy while you are using this medicine.
Is Topenoid safe during breastfeeding?
Topenoid is not contraindicated during breastfeeding and if Topenoid is required by the mother, it is not a reason to discontinue breastfeeding. However, some experts feel it should not be used on greater than 20% of the body surface area while nursing because of possible absorption.
Can I drink alcohol with Topenoid?
Topenoid do not have interactions with alcoholic beverages.
How long does it take for Topenoid to work?
If you are using Topenoid to treat acne, your symptoms should improve in about 4 weeks. If you are using Topenoid to treat psoriasis, your symptoms should improve in about 1 to 4 weeks with treatment with Topenoid.
How long does Topenoid stay in my system?
The half-life of Topenoid was approximately 18 hours.
Is Topenoid toxic?
This medicine may be harmful if swallowed. If someone has overdosed and has serious symptoms such as passing out or trouble breathing.
Does cause hair loss?
Good idea in general to keep the Topenoid away from the hair line by about an inch. You could use a acne pad system like this Glycolix product or something similar around the hairline. It's very unlikely this type of hair loss would persist.
Can Topenoid be used long term?
Longer-term Topenoid regimens are routinely used in treatment of acne without issue.
Will Topenoid affect my contraception?
It could harm the unborn baby or cause birth defects. Use effective birth control to prevent pregnancy while you are using this medicine. Stop using Topenoid topical and tell your doctor right away if you become pregnant.
What happens if I use too much Topenoid?
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 your skin to be irritated. You may need to use this medicine for several weeks or months before your skin starts to look better. Applying extra medicine will not make it work faster.
When can I stop using Topenoid?
Stop using Topenoid if you have:
- severe skin irritation (pain, dryness, flaking, peeling, burning, stinging, itching) after applying the medicine;
- blistering or peeling skin;
- severe redness or discomfort; or.
- swelling, warmth, oozing, or other signs of skin infection.
How often should I use Topenoid?
Adults and children 12 years of age and older apply a thin layer to the affected area of the skin once a day, usually in the evening or at bedtime. Children younger than 12 years of age se and dose must be determined by the doctor.
How do I use Topenoid ?
After the skin is dry, apply a thin layer of Topenoid Gel 0.1% once per day, in the evening, to the skin where acne lesions appear. Use enough to cover the entire affected area.Topenoid was investigated for up to 12 weeks during clinical trials for acne.
