Plaquverazon Actions

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Actions of Plaquverazon in details

infoThe action of the drug on the human body is called Pharmacodynamics in Medical terminology. To produce its effect and to change the pathological process that is happening the body and to reduce the symptom or cure the disease, the medicine has to function in a specific way. The changes it does to the body at cellular level gives the desired result of treating a disease. Drugs act by stimulating or inhibiting a receptor or an enzyme or a protein most of the times. Medications are produced in such a way that the ingredients target the specific site and bring about chemical changes in the body that can stop or reverse the chemical reaction which is causing the disease.
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Pharmacology: Pharmacodynamics: Calcipotriol (Plaquverazon) is a vitamin D analogue. In vitro data suggest that Calcipotriol (Plaquverazon) induces differentiation and suppresses proliferation of keratinocytes. This is the proposed basis for its effect in psoriasis.

Gel: Like other topical corticosteroids, Betamethasone (Plaquverazon) dipropionate has anti-inflammatory, antipruritic, vasoconstrictive and immunosuppresive properties, however, without curing the underlying condition. Through occlusion, the effect can be enhanced due to increased penetration of the stratum corneum. The incidence of adverse events will increase because of this. In general, the mechanism of the anti-inflammatory activity of the topical steroids is unclear.

Pharmacokinetics: Gel: The human transdermal absorption of calcipotrol and Betamethasone (Plaquverazon), respectively, has been shown to be <1% of the administered dose for both substances. The systemic absorption under normal conditions of use is not expected to have any influence on systemic parameters. The pharmacokinetic behavior for the 2 active constituents is not influenced by the presence of each other.

The systemic exposure to Calcipotriol (Plaquverazon) and Betamethasone (Plaquverazon) dipropionate from topically applied Plaquverazon gel is comparable to Plaquverazon ointment in rats and minipigs.

Clinical studies with radiolabelled ointment indicate that the systemic absorption of Calcipotriol (Plaquverazon) and Betamethasone (Plaquverazon) from Plaquverazon ointment formulation is <1% of the dose (2.5 g) when applied to normal skin (625 cm2) for 12 hrs. Application to psoriasis plaques and under occlusive dressings may increase the absorption of topical corticosteroids.

Following systemic exposure, both active ingredients, Calcipotriol (Plaquverazon) and Betamethasone (Plaquverazon) dipropionate, are rapidly and extensively metabolised. The main route of excretion of Calcipotriol (Plaquverazon) is via feces (rats and minipigs) and for Betamethasone (Plaquverazon) dipropionate it is via urine (rats and mice).

Calcipotriol (Plaquverazon) and Betamethasone (Plaquverazon) dipropionate were below the lower limit of quantification in all blood samples of 34 patients treated for 4 or 8 weeks with both Plaquverazon gel and Plaquverazon ointment for extensive psoriasis involving the body and scalp. One (1) metabolite of Calcipotriol (Plaquverazon) and 1 metabolite of Betamethasone (Plaquverazon) dipropionate were quantifiable in some of the patients.

How should I take Plaquverazon?

This section provides information on the proper use of a number of products that contain Betamethasone (Plaquverazon) and calcipotriene. It may not be specific to Plaquverazon. Please read with care.

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 should only be used on the skin or scalp only. Do not get it in your eyes, nose, mouth, vagina, or apply it on your face, under your arms, or on your groin area. Do not use it on skin or scalp areas that have cuts or scrapes. If it does get on these areas, rinse it off right away with water.

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

To help clear up your skin or scalp problem completely, it is very important that you keep using this medicine for the full time of treatment. Do not miss any doses.

This medicine should only be used for skin conditions that your doctor is treating. Check with your doctor before using it for other skin 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.

The treated areas should not be bandaged or covered after the medicine is applied.

To use the ointment:

  • Wash your hands with soap and water before and after using this medicine.
  • Apply a thin layer to the affected areas of the skin and rub it in gently.
  • Do not use the ointment for more than 8 weeks unless your doctor has told you to.

To use the topical suspension:

  • Wash your hands with soap and water before and after using this medicine.
  • Shake the bottle before using the medicine.
  • Part your hair so you can see the patches on your scalp.
  • Apply enough medicine to the affected areas on your scalp and rub it in gently.
  • Do not wash your hair or take a bath or shower right after applying this medicine.
  • Do not apply this medicine in the 12 hours before or after using any hair chemical treatments. Talk with your doctor first about it.
  • Do not use the topical suspension for more than 8 weeks unless your doctor has told you to.

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 (ointment):
    • For plaque psoriasis:
      • Adults—Apply to the affected area of the skin once a day for up to 4 weeks or until the area is cleared or as determined by your doctor. Do not use more than 100 grams per week.
      • Children 12 to 17 years of age—Apply to the affected area of the skin once a day for up to 4 weeks or until the area is cleared or as determined by your doctor. Do not use more than 60 grams per week.
      • Children younger than 12 years of age—Use and dose must be determined by your doctor.
  • For topical dosage form (suspension):
    • For plaque psoriasis of the body:
      • Adults—Apply to the affected area of the skin once a day for up to 8 weeks or until the area is cleared or as determined by your doctor. Do not use more than 100 grams per week.
      • Children—Use and dose must be determined by your doctor.
    • For plaque psoriasis of the scalp:
      • Adults—Apply to the affected area on the scalp once a day for up to 8 weeks or until the area is cleared or as determined by your doctor. Do not use more than 100 grams per week.
      • Children 12 to 17 years of age—Apply to the affected area on the scalp once a day for up to 8 weeks or until the area is cleared or as determined by your doctor. Do not use more than 60 grams per week.
      • 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

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.

Keep the bottle of topical suspension in the carton when not in use. Use it within 6 months after it has been opened.

Plaquverazon administration

infoAdministration of drug is important to know because the drug absorption and action varies depending on the route and time of administration of the drug. A medicine is prescribed before meals or after meals or along with meals. The specific timing of the drug intake about food is to increase its absorption and thus its efficacy. Few work well when taken in empty stomach and few medications need to be taken 1 or 2 hrs after the meal. A drug can be in the form of a tablet, a capsule which is the oral route of administration and the same can be in IV form which is used in specific cases. Other forms of drug administration can be a suppository in anal route or an inhalation route.
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Use Betamethasone (Plaquverazon) and calcipotriene exactly as it was prescribed for you. Do not use it in larger doses or for longer than recommended by your doctor.

This medication comes with patient instructions for safe and effective use. Follow these directions carefully. Ask your doctor or pharmacist if you have any questions.

Wash your hands before and after applying this medicine.

Betamethasone (Plaquverazon) and calcipotriene topical is for use on the skin only. However, do not apply the medicine to your face, underarms, or groin (genital area).

Shake the liquid form of this medication before using it.

Apply a thin layer of the medication and rub it in completely.

Do not cover treated skin areas with a bandage or tight clothing, unless your doctor has told you to.

Do not use Betamethasone (Plaquverazon) and calcipotriene for longer than 4 weeks unless your doctor has told you to.

While you are using this medication, your blood and urine may need to be tested on a regular basis. It is important that you not miss any scheduled visits to your doctor.

Store this medicine at room temperature away from moisture and heat. Keep the tube capped and tightly closed when not in use.

Plaquverazon pharmacology

infoPharmacokinetics of a drug can be defined as what body does to the drug after it is taken. The therapeutic result of the medicine depends upon the Pharmacokinetics of the drug. It deals with the time taken for the drug to be absorbed, metabolized, the process and chemical reactions involved in metabolism and about the excretion of the drug. All these factors are essential to deciding on the efficacy of the drug. Based on these pharmacokinetic principles, the ingredients, the Pharmaceutical company decides dose and route of administration. The concentration of the drug at the site of action which is proportional to therapeutic result inside the body depends on various pharmacokinetic reactions that occur in the body.
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Mechanism of Action

Plaquverazon® Ointment combines the pharmacological effects of calcipotriene hydrate as a synthetic vitamin D3 analogue and Betamethasone (Plaquverazon) dipropionate as a synthetic corticosteroid. However, while their pharmacologic and clinical effects are known, the exact mechanisms of their actions in plaque psoriasis are unknown.

Pharmacodynamics

Vasoconstriction:

In a vasoconstrictor trial in healthy subjects, the skin blanching response of Plaquverazon® Ointment was consistent with that of a potent corticosteroid when compared with other topical corticosteroids. However, similar blanching scores do not necessarily imply therapeutic equivalence.

Hypothalamic-Pituitary-Adrenal (HPA) Axis Suppression:

HPA axis suppression was evaluated in four trials (Trial A, B, C and D) following the application of Plaquverazon® Ointment.

In Trial A, Plaquverazon® Ointment was applied once daily for 4 weeks to adult subjects (N = 12) with plaque psoriasis to study its effects on the hypothalamic-pituitary-adrenal (HPA) axis. Of eleven subjects tested, none demonstrated adrenal suppression as indicated by a 30-minute post-stimulation cortisol level ≤ 18 mcg/dL.

In Trial B, Plaquverazon® Ointment was evaluated in adult subjects with plaque psoriasis (N = 19). One subject demonstrated adrenal suppression.

In Trial C, HPA axis suppression was evaluated in adult subjects (N=32) with extensive plaque psoriasis involving at least 30% of the scalp and, in total, 15-30% of the body surface area. Treatment consited of once daily application of Talconex Scalp®

Topical Suspension on the scalp in combination with Plaquverazon® Ointment on the body. Adrenal suppression as indicated by a 30-minutes post-stimulation cortisol level < 18 mcg/dL was observed in 5 of 32 subjects (15.6%) after 4 weeks of treatment as per the recommended duration of use.

In Trial D, HPA axis suppression was evaluated in subjects 12 to 17 years (N=32) with plaque psoriasis of the body involving 5-30% of the body surface area. Treatment consisted of once daily application of Plaquverazon® Ointment to the affected areas for up to 4 weeks. Mean weekly dose was 29.6 g with a range of 8.1-55.8 g/week. Adrenal suppression as indicated by a 30-minute post-stimulation cortisol level ≤18 mcg/dL was observed in none of 32 evaluable subjects after 4 weeks of treatment.

Effects on Calcium Metabolism

In Trial C described above, the effects of once daily application of Plaquverazon® Ointment on the body in combination with Plaquverazon Scalp®

Topical Suspension on the scalp on calcium metabolism were also examined. Elevated urinary calcium levels outside the normal range were observed in 1 of 35 subjects (2.9%) after 4 weeks of treatment.

In Trial D described above, calcium metabolism was evaluated in a total of 33 subjects aged 12 to 17 years with plaque psoriasis involving 5-30% of the body surface area who underwent once daily application of Plaquverazon® Ointment for up to 4 weeks. No cases of hypercalcemia and no clinically relevant changes in urinary calcium were reported. However, one subject had a normal urinary calcium:creatinine ratio at baseline (3.75 mmol/g), which increased above the normal range at week 4 (16 mmol/g). There were no relevant changes in albumin-corrected serum calcium or other markers of calcium metabolism for this subject. The clinical significance of this finding is unknown.

Pharmacokinetics

Absorption

In Trial C described above, the systemic effect of Plaquverazon® Ointment in extensive plaque psoriasis was investigated. In this study, the serum levels of calcipotriene and Betamethasone (Plaquverazon) dipropionate and their major metabolites were measured after 4 weeks (maximum recommended duration of treatment) and also after 8 weeks of once daily application of Plaquverazon® Ointment on the body in combination with Plaquverazon Scalp®

Topical Suspension on the scalp. Both calcipotriene and Betamethasone (Plaquverazon) dipropionate were below the lower limit of quantification in all serum samples of the 34 subjects evaluated. However, one major metabolite of calcipotriene (MC1080) was quantifiable in 10 of 34 (29.4%) subjects at week 4 and in five of 12 (41.7%) subjects at week 8. The major metabolite of Betamethasone (Plaquverazon) dipropionate, Betamethasone (Plaquverazon) 17-propionate (B17P) was also quantifiable in 19 of 34 (55.9%) subjects at week 4 and seven of 12 (58.3%) subjects at week 8. The serum concentrations for MC1080 ranged from 20-75 pg/mL. The clinical significance of this finding is unknown.

Metabolism

Calcipotriene:

Calcipotriene metabolism following systemic uptake is rapid and occurs in the liver. The primary metabolites of calcipotriene are less potent than the parent compound.

Calcipotriene is metabolized to MC1046 (the alpha,beta-unsaturated ketone analogue of calcipotriene), which is metabolized further to MC1080 (a saturated ketone analogue). MC1080 is the major metabolite in plasma. MC1080 is slowly metabolized to calcitroic acid.

Betamethasone (Plaquverazon) dipropionate:

Betamethasone (Plaquverazon) dipropionate is metabolized to Betamethasone (Plaquverazon) 17-propionate and Betamethasone (Plaquverazon), including the 6beta-hydroxy derivatives of those compounds by hydrolysis. Betamethasone (Plaquverazon) 17-propionate (B17P) is the primary metabolite.



References

  1. DailyMed. "CALCIPOTRIENE HYDRATE: 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. DailyMed. "BETAMETHASONE: 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).
  3. NCIt. "Betamethasone: 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).

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The results of a survey conducted on ndrugs.com for Plaquverazon 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 Plaquverazon. 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.

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Information checked by Dr. Sachin Kumar, MD Pharmacology

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