Motasone 0.1% Actions

• Actions of Motasone 0.1% in details
• Motasone 0.1% pharmacology
• Motasone 0.1% reviews

Actions of Motasone 0.1% in details

Motasone 0.1%, a synthetic corticosteroid, exhibits anti-inflammatory, antipruritic and vasoconstrictive properties.

Pharmacology: Pharmacodynamics: The pharmacologic profile of Motasone 0.1% was determined by standard laboratory methods. Relative to betamethasone valerate, anti-inflammatory activity and antipsoriatic activity of Motasone 0.1% was evaluated in mice and guinea pigs, respectively. Hypothalamic-pituitary-adrenal (HPA) axis suppression, thymolysis and skin atrophy were evaluated in mice.

In the croton oil assay in mice, Motasone 0.1% (ED₅₀=0.02 mcg/ear) was equipotent to betamethasone valerate after single application and was approximately 8 times as potent as betamethasone valerate after 5 daily applications (ED₅₀=0.02 mcg/ear/day versus 0.014 mcg/ear/day). In guinea pigs, Motasone 0.1% was approximately twice as potent as betamethasone valerate in reducing M. ovalis-induced epidermal acanthosis after 14 daily applications.

With respect to other pharmacologic activities commonly associated with corticosteroids, Motasone 0.1% (ED₅₀=5.3 mcg/ear/day) was less potent than betamethasone valerate (ED₅₀=3.1 mcg/ear/day) in suppressing the HPA axis in mice after 5 daily application. In the thymolysis assay, Motasone 0.1% (ED₅₀=26.6 mcg/ear/day) was approximately 2 times as potent as betamethasone valerate (ED₅₀=51.6 mcg/ear/day) when applied topically, and following SC administration for 5 days, Motasone 0.1% (ED₅₀=11.2 mcg/mouse) was approximately 6 times as potent as betamethasone valerate (ED₅₀=59.8 mcg/mouse). At doses 5-5000 times the effective anti-inflammatory doses, Motasone 0.1% was 3-8 times more potent than betamethasone valerate with respect to skin thinning in mice. Based on the ratio of systemic potency (HPA suppression or thymolysis) to topical anti-inflammatory potency, the therapeutic indices for Motasone 0.1% were approximately 3-10 times greater than those for the comparative, betamethasone valerate. Therefore, Motasone 0.1% would be expected to have a superior safety margin to that of betamethasone valerate.

Pharmacokinetics: The percutaneous absorption and excretion of ³H-Motasone 0.1% cream and/or ointment was evaluated in rats, rabbits and dogs with doses ranging from 5.2-22 mcg/cm². Additionally, the tissue distribution of absorbed radioactivity was determined in rabbits.

Systemic absorption of ³H-Motasone 0.1% was minimal in all species studied, ranging from approximately 2% in dogs to 6% in rabbits over a 5-day to 7-day period. The cream and ointment formulations were comparable with respect to systemic absorption. Plasma levels were low ranging from <0.1 ng/mL to <1 ng/mL. Less than 1.3% of the applied dose was excreted in urine of all species and from 1.5-4.2% was excreted in feces. Characterization of urinary metabolites was not possible due to the low levels of Motasone 0.1% in urine. However, it is well known that corticosteroids are metabolized into inactive water-soluble substances eg, sulfate esters or glucuronides and are excreted as such. In rabbits, there was no unusual accumulation of radioactivity in any tissue.

Human Pharmacokinetics: Lotion: Due to the occlusive nature of the ointment base, the percutaneous absorption following application of a corticosteroid ointment is greater than that of a topical corticosteroid in a cream or lotion formulation. Consequently, absorption following application of Motasone 0.1% lotion 0.1% is expected to be no greater than that which may occur after application of the ointment formulation.

Cream: The percutaneous absorption of Motasone 0.1% cream 0.1% was evaluated in subjects receiving a single application of radiolabeled ³H-Motasone 0.1% cream 0.1% which remained on intact skin for 8 hrs. Based on the amount of radioactivity excreted in the urine and feces during the 5-day study period, approximately 0.4% of the applied dose was absorbed systematically. The radioactive content found in plasma and red blood cells remained a few counts above background levels (corresponding to <0.1 ng/mL) throughout the study.

Ointment: A percutaneous absorption study with radiolabeled ³H-Motasone 0.1% ointment was conducted in adult male volunteers with intact skin. Based on the amounts of radioactivity excreted after an 8-hr application of the active ointment and analysis of urine and feces, approximately 0.7% of the applied dose was absorbed systematically without occlusion.

Onset of Action: Lotion: Motasone 0.1% lotion 0.1% showed rapid onset of action after 1 treatment week in patients with scalp psoriasis. As demonstrated by results at day 8 in 1 study, improvement in total sign/symptom scores was significantly greater (p<0.01) in Motasone 0.1%-treated patients than in those treated with betamethasone valerate 0.1%.

Cream: Onset of action was investigated in several clinical trials with both pediatric and adult patients with various dermatologic conditions. A rapid onset of action with Motasone 0.1% cream 0.1% was demonstrated after 1 week of treatment by percent improvement from baseline in total disease sign/symptom score (ranging from 25-81%). In these studies, percent improvement for the comparative agents were: Betamethasone valerate (ranged from 43-81%), clobetasone butyrate (59%); hydrocortisone butyrate (54%); fluocinolone acetonide (24%); triamcinolone acetonide (36%); and for the vehicle alone (15 and 28%). Furthermore, in 2 of these studies, Motasone 0.1% cream 0.1% was significantly more effective than fluocinolone acetonide (p<0.001) and hydrocortisone butyrate (p≤0.05) at day 4 evaluation.

Ointment: Motasone 0.1% ointment 0.1% once daily also had a rapid onset of action in psoriatic patients as evidenced by percent improvement from baseline in total disease sign/symptom scores after 1 treatment week (ranging from 38-59%). Percent improvement for comparative agents were triamcinolone acetonide (28%), fluocinolone acetonide (33%), betamethasone dipropionate (23%), betamethasone valerate (56%) and vehicle alone (43%). In 2 of these studies Motasone 0.1% was significantly more effective than triamcinolone acetonide or fluocinolone acetonide at day 4 evaluation (p≤0.01).

The effects of Motasone 0.1% ointment 0.1% in the treatment of patients with atopic dermatitis also were rapid in onset as demonstrated by mean percent improvement and mean global evaluation score at day 4 and week 1. Motasone 0.1%-treated patients showed an improvement in total sign/symptom score that ranged from 27-47% at day 4 and 51-64% at week 1. In comparison, hydrocortisone butyrate and betamethasone valerate demonstrated 17% and 43% improvement, respectively, at day 4 and 24% and 65%, respectively, at week 1.

Global scores at 1-week indicated moderate improvement in patients treated with Motasone 0.1% or betamethasone valerate and slight improvement in those treated with hydrocortisone butyrate.

How should I take Motasone 0.1%?

It is very important that you use Motasone 0.1% 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.

Motasone 0.1% is for use on the skin only. Do not get it in your eyes. 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.

Motasone 0.1% 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. Motasone 0.1% should not be used to treat certain kinds of skin infections or conditions, such as severe burns.

Do not use Motasone 0.1% on the face, groin, or underarms unless directed to do so by your doctor.

Do not use Motasone 0.1% in the diaper area of an infant. Diapers or plastic pants will increase the amount of medicine absorbed through the skin and cause unwanted side effects.

To use:

• Wash your hands with soap and water before and after using Motasone 0.1%.
• Apply a thin layer of Motasone 0.1% to the affected area of the skin. Rub it in gently.
• Do not bandage or otherwise wrap the skin being treated unless directed to do so by your doctor.
• If your doctor ordered an occlusive dressing or airtight covering to be applied over the medicine, make sure you know how to apply it. Occlusive dressings increase the amount of medicine absorbed through your skin, so use them only as directed. If you have any questions about this, check with your doctor.

Dosing

The dose of Motasone 0.1% 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 Motasone 0.1%. 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 redness, itching, and swelling of the skin:
  • For topical dosage forms (cream and ointment):
    • Adults—Apply to the affected area of the skin once per day.
    • Children 2 years of age and older—Apply to the affected area of the skin once per day.
    • Children younger than 2 years of age—Use is not recommended.
  • For topical dosage form (lotion):
    • Adults—Apply to the affected area of the skin once per day.
    • Children 12 years of age and older—Apply to the affected area of the skin once per day.
    • Children younger than 12 years of age—Use is not recommended.

Missed Dose

If you miss a dose of Motasone 0.1%, 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

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

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.

Motasone 0.1% pharmacology

Motasone 0.1% is a medium-potency synthetic corticosteroid with antiinflammatory, antipruritic, and vasoconstrictive properties. Studies in asthmatic patients have demonstrated that Motasone 0.1% provides a favorable ratio of topical to systemic activity due to its primary local effect along with the extensive hepatic metabolism and the lack of active metabolites. Though effective for the treatment of asthma, glucocorticoids do not affect asthma symptoms immediately. Maximum improvement in symptoms following inhaled administration of Motasone 0.1% may not be achieved for 1 to 2 weeks or longer after starting treatment. When glucocorticoids are discontinued, asthma stability may persist for several days or longer. Motasone 0.1% has been shown in vitro to exhibit a binding affinity for the human glucocorticoid receptor which is approximately 12 times that of dexamethasone, 7 times that of triamcinolone acetonide, 5 times that of budesonide, and 1.5 times that of fluticasone. The clinical significance of these findings is unknown.

References

1. DailyMed. "FORMOTEROL FUMARATE; MOMETASONE FUROATE: 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. NCIt. "Mometasone Furoate: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).
3. EPA DSStox. "Mometasone furoate: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).

Reviews

The results of a survey conducted on ndrugs.com for Motasone 0.1% are given in detail below. The results of the survey conducted are based on the impressions and views of the website users and consumers taking Motasone 0.1%. We implore you to kindly base your medical condition or therapeutic choices on the result or test conducted by a physician or licensed medical practitioners.

User reports

Consumer reviews

There are no reviews yet. Be the first to write one!

Your name:  Email:  Spam protection:  < Type 19 here

Information checked by Dr. Sachin Kumar, MD Pharmacology