Posts Tagged ‘fp’

Mometasone Furoate

Saturday, July 17th, 2010

Drug Approvals

(BANM, US Adopted Name, rINNM)

Synonyms: Mometason-furoát; Mometasona, furoato de; Mometasonfuroat; Mometasoni Furoas; Mometasonifuroaatti; Mometazon-furoát; Mometazono furoatas; Sch-32088
BAN: Mometasone Furoate [BANM]
USAN: Mometasone Furoate
INN: Mometasone Furoate [rINNM (en)]
INN: Furoato de mometasona [rINNM (es)]
INN: Mométasone, Furoate de [rINNM (fr)]
INN: Mometasoni Furoas [rINNM (la)]
INN: Мометазона Фуроат [rINNM (ru)]
Chemical name: 9α,21-Dichloro-11β,17-dihydroxy-16α-methylpregna-1,4-diene-3,20-dione 17-(2-furoate)
Molecular formula: C27H30Cl2O6 =521.4
CAS: 105102-22-5 (mometasone); 83919-23-7 (mometasone furoate)
ATC code: D07AC13; R01AD09; R03BA07
Read code: y01DU

Pharmacopoeias. In Europe and US.

European Pharmacopoeia, 6th ed. (Mometasone Furoate). A white or almost white powder. Practically insoluble in water slightly soluble in alcohol soluble in acetone and in dichloromethane.

The United States Pharmacopeia 31, 2008 (Mometasone Furoate). A white to off-white powder. Soluble in acetone and in dichloromethane.

Profile

Mometasone furoate is a corticosteroid used topically for its glucocorticoid activity in the treatment of various skin disorders. It is usually used as a cream, ointment, or lotion containing 0.1%.

When applied topically, particularly to large areas, when the skin is broken, or under occlusive dressings, or when given intranasally, corticosteroids may be absorbed in sufficient amounts to cause systemic effects. The effects of topical corticosteroids on the skin are described. For recommendations concerning the correct use of corticosteroids on the skin, and a rough guide to the clinical potencies of topical corticosteroids.

A nasal suspension of mometasone furoate 0.05%, as the monohydrate, is given in the treatment and prophylaxis of the symptoms of allergic rhinitis. The usual adult dose is the equivalent of 100 micrograms of mometasone furoate in each nostril once daily, increased if necessary to 200 micrograms in each nostril daily. Once symptoms are controlled a dose of 50 micrograms in each nostril daily may be effective for maintenance. In the UK, the dose for children aged between 6 and 11 years is the equivalent of 50 micrograms in each nostril once daily. In the USA, similar doses may be given to treat allergic rhinitis in children from 2 years of age.

The nasal suspension is also given for the treatment of nasal polyps in patients 18 years and older the recommended initial dose in the UK is 100 micrograms into each nostril once daily, increased after 5 to 6 weeks to twice daily if needed. In the USA the recommended initial dose is 100 micrograms in each nostril twice daily, although once daily administration may be sufficient in some patients.

Mometasone furoate is used by dry powder inhaler for the prophylaxis of asthma. Doses may differ between countries and dosage units may be expressed differently, as either the amount of drug released per actuation or the amount delivered from the mouthpiece. UK licensed product information includes an initial dose of 400 micrograms inhaled once daily in the evening for mild to moderate asthma in adults and adolescents aged 12 years and older. This may be adjusted to a maintenance dose of 200 micrograms once or twice daily. In severe asthma, an initial dose of 400 micrograms twice daily is used, then titrated to the lowest effective dose once symptoms are controlled. US doses are provided in terms of the amount of drug released per actuation (an actuation that releases 110 micrograms delivers 100 micrograms from the mouthpiece). An initial dose of 220 micrograms once daily in the evening is used in adults and adolescents, aged 12 years and older, who have been treated with inhaled therapy only (bronchodilators or corticosteroids) this may be increased to a maximum of 440 micrograms daily as a single dose or 2 divided doses. Patients receiving oral corticosteroids may be started on 440 micrograms twice daily. Children aged 4 to 11 years may be given 110 micrograms once daily in the evening, regardless of prior therapy this is the maximum recommended daily dose.

Preparations

British Pharmacopoeia 2008: Mometasone Aqueous Nasal Spray Mometasone Cream Mometasone Ointment Mometasone Scalp Application

The United States Pharmacopeia 31, 2008: Mometasone Furoate Cream Mometasone Furoate Ointment Mometasone Furoate Topical Solution.

Proprietary Preparations

Argentina: Elocon Fenisona Metason Momeplus Nasonex Novasone Uniclar

Australia:: AllerMax † Elocon Nasonex Novasone

Austria: Asmanex Elocon Elovent Nasonex

Belgium: Elocom Nasonex

Brazil: Asmanexf Elocom Nasonex Topison

Canada: Elocom Nasonex

Chile: Dermenet Dermosona Elocom Flogocort Lisoder Momelab Nasonex Rinoval Uniclar

Czech Republic: Asmanex Elocom Nasonex

Denmark: Asmanex Elocon Nasonex

Finland: Asmanex Elocon Nasonex

France: Nasonex

Germany: Asmanex Ecural Nasonex

Greece: Asmanex Bioelementa Ecelecort Elocon Elovent Esine F-Din Fremomet Makiren Metason Mofur Molken Momecort Movesan Mozeton Nasamet Nasonex Pharmecort Yperod

Hong Kong: Elomet Nasonex Topcort

Hungary: Elocom Nasonex

India: Elocon Metaspray Momate Topcort

Indonesia: Dermovel Elocon Eloskin Elox Intercon Mefurosan Mesone Mofacort Mofulex Momet Motaderm Moteson Nasonex

Ireland: Asmanex Elocon Nasonex

Israel: Elocom Nasonex

Italy: Altosone Elocon Nasonex Rinelon Uniclar

Malaysia: Elomet Momate Nasonex

Mexico: Elica Elomet Elovent Rinelon Uniclar

The Netherlands: Asmanex Elocon Elovent Nasonex

Norway: Elocon Nasonex

New Zealand: Asmanex Bronconex Elocon

Philippines: Elica Elocon Momate Nasonex Rinelon

Poland: Elocom Elosone Nasonex

Portugal: Asmanex Elocom Elomet Elovent Nasomet Prospiril

Russia: Elocom Nasonex

South Africa: Elica Elocon Nasonex Rinelon

Singapore: Elomet Nasonex

Spain: Asmanexf Elica Elocom Nasonex Rinelon

Sweden: Asmanex Elocon Nasonex

Switzerland: Asmanex Elocom Nasonex

Thailand: Elomet Nasonex Rineloir †

Turkey: Elocon M-Furo Nasonex

UK: Asmanex Elocon Nasonex

USA: Asmanex Elocon Nasonex

Venezuela: Asmanex Cortynase Dergentil Elocon Eloconex † Elomet Nasonex Uniclar

Multi-ingredient

Argentina: Elosalic †

Austria: Elosalic

Chile: Velosalic

Czech Republic: Momesalic Monsalic †

Germany: Elosalic

Hong Kong: Elosalic

India: Momate-S

Indonesia: Elosalic

Poland: Elosalic

Portugal: Monsalic

Russia: Elocom-S

South Africa: Elosalic

Sweden: Elosalic

Thailand: Elosalic †

Turkey: Elosalic

Venezuela: Elosalic

Drugs in Allergic Disorders

Wednesday, February 17th, 2010

Allergy refers to a broad state of altered reactivity to a foreign substance, resulting from prior experience with the same substance. Used today, the term allergy generally refers to the unfavorable clinical consequences of an antigen-antibody interaction. Although the term allergic disorder implies an immune mechanism, in many allergic disorders, most notably bronchial asthma and atopic dermatitis, non-immune mechanisms may be of great importance. Many of the clinical conditions being treated by an allergist may be aggravated by non-immune factors such as pollution, psychic stress, cold air, and exertion -for example, exercise-induced asthma. We must always remember that there are three main principles in the therapy of allergic diseases:

1. Most important: avoidance of allergens and irritants known or suspected to be causing or aggravating the disorder.

2. The use of pharmacologic agents, restricted to as few as possible.

3. The use of specific immunotherapy or hyposensitization.

We must use a drug appropriate to the patient’s symptoms; antihistamines, for example, are useful for ear and nose complaints as well as pruritis of the skin (i.e. urticaria, eczema).

Drugs Used in the Treatment of Allergic Disorders

Antihistamines have been used in the treatment of allergic conditions for the past 30 years. They compete with the histamine released through either an antigen-antibody reaction, by physical trauma or by a histamine-liberating agent (eg. morphine, codeine). This histamine is released from the mast cells. The antihistamines compete for the cellular receptor sites, but they do not combine with the histamines in vivo or in vitro.

There are many commercially available antihistamines, which can be classified into five major groups. Physicians should be familiar with one member of each group. If the initial drug chosen does not give a good therapeutic response, use an antihistamine in another group. At times, it is necessary to try an antihistamine of one group after another, often in various combinations with sympathomimetic agents, to obtain reasonable results.

The classes of antihistamines are as follows:

1. Ethanolamines, e.g. diphenhydramine (Benadryl), dosage five mg/kg/day in three or four divided doses. A side effect is marked sedation.

2. Ethylenediamine; e.g. tripelennamine (Pyribenzamine), dosage five mg/kg/day in three or four divided doses. Side effects include moderate sedation.

3. Alkylamine; e.g. chlorpheniramine (Chlor-Tripolon), dosage 0.3 mg/kg/day in three or four divided doses. There is minimal sedation.

4. Piperazines; e.g. hydroxyzine (Atarax).

5.Phenothiazine, e.g. promethazine (Phenergan), dosage 0.5 mg/kg before retiring or 0.3 mg/kg/day. This has side effects of marked sedation.

Remember that antihistamines compete with the histamine already released in the body of the cell receptors, thus blocking the effect of the released histamine on the effector organs. Antihistamines do not combine chemically with the histamine, and they do not interfere with the antigen antibody reaction.

The sympathomimetic amine drugs or beta adrenergic agonists and theophylline are useful bronchodilators for bronchospasm.

The antibiotics used for infection in an allergic individual are tetracycline after age seven (five to ten mg/kg every six hours) and erythromycin, an unusually safe drug, orally, 10 mg/kg every six hours.

Steroids are used for more severe and acute symptoms.