Clotrimazole + Betamethasone Pharmacology

Clotrimazole + Betamethasone

About Clotrimazole + Betamethasone
N/A
Mechanism of Action of Clotrimazole + Betamethasone
N/A
Pharmacokinets of Clotrimazole + Betamethasone
N/A
Onset of Action for Clotrimazole + Betamethasone
N/A
Duration of Action for Clotrimazole + Betamethasone
N/A
Half Life of Clotrimazole + Betamethasone
N/A
Side Effects of Clotrimazole + Betamethasone
N/A
Contra-indications of Clotrimazole + Betamethasone
N/A
Special Precautions while taking Clotrimazole + Betamethasone
N/A
Pregnancy Related Information
Use with caution
Old Age Related Information
N/A
Breast Feeding Related Information
Use with caution
Children Related Information
N/A
Indications for Clotrimazole + Betamethasone
It is a combination of imidazole antifungal Clotrimazole and corticosteroid Betamethasone.
1.Fungal infections of the skin, vagina and mouth.
Interactions for Clotrimazole + Betamethasone
N/A
Typical Dosage for Clotrimazole + Betamethasone
Apply the medicament to the affected area twice daily.
Schedule of Clotrimazole + Betamethasone
N/A
Storage Requirements for Clotrimazole + Betamethasone
N/A
Effects of Missed Dosage of Clotrimazole + Betamethasone
N/A
Effects of Overdose of Clotrimazole + Betamethasone
N/A

Clotrimazole

About Clotrimazole
A broad-spectrum antifungal antibiotic, imidazole derivative, Oral Nonabsorbed Antifungal Agent.
Mechanism of Action of Clotrimazole
Clotrimazole is fungicidal or fungistatic depending on the drug concentrations. It inhibits the conversion of Lanosterol to 14 demethyl Lanosterol by inhibiting the cytochromeP450 enzyme 14 alpha demethylase and impair ergosterol synthesis which is an essential constituent of cell membrane. Inhibition of ergosterol synthesis will alter the membrane permeability of the susceptible fungus and kill or inhibit them.
Pharmacokinets of Clotrimazole
Absorption: Absorption is minimal after topical administration.
Onset of Action for Clotrimazole
N/A
Duration of Action for Clotrimazole
3 hours
Half Life of Clotrimazole
N/A
Side Effects of Clotrimazole
1.Stinging
2.Erythema
3.Burning
4.Pruritis
5.Vesication
6.Desquamation
7.Urticaria
8.Burning
9.Peeling
10.Irritation
Contra-indications of Clotrimazole
Hypersensitivity to Clotrimazole
Special Precautions while taking Clotrimazole
1.Avoid contact with eyes, nose and mouth.
2.Do not wear occlusive dress over the medicament.
Pregnancy Related Information
Use with caution.
Old Age Related Information
Use with caution.
Breast Feeding Related Information
Use with caution.
Children Related Information
Use with caution.
NEONATES: contraindicated
Indications for Clotrimazole
1.Tinea pedis
2.Tinea cruris
3.Tinea versicolor
4.Tinea corporis
5.Cutaneous candidiasis
6.Vulvovaginal candidiasis
Interactions for Clotrimazole
Polyene Antibiotics : Antagonises effects of polyene antibiotics.
Typical Dosage for Clotrimazole
Topical: Clotrimazole cream, lotion and solution 1 % is used.
Clean and dry the affected area and apply the medicament with gentle massage 2 -3 times daily for 2 - 4 weeks.
Vaginal candidiasis: Insert 1 applicator full (vaginal cream 1%) intravaginally at night for 1 -2 weeks.
Vaginal tablets 100. 200 and 500mg tablet is available.
Vulvovaginal candidiasis: Insert 100mg tablet intravaginally at bed time for 7 consecutive days or 200 mg tablet for 3 consecutive days or 500 mg tablet for 1 day at night.
Oral lozenge 10 mg is available
Oropharyngeal candidiasis: 1 lozenge orally 5 times daily for 2 weeks
Prophylaxis of Oropharyngeal candidiasis: 1 lozenge is used 3 times daily
Gel: Insert with an applicator intravaginally at night for 1 - 2 weeks.
Powder (1% w/ w): dusted over the body parts as required
Schedule of Clotrimazole
H
Storage Requirements for Clotrimazole
Store at room temperature (15 - 25 degree C). Protect from heat and moisture. Keep out of the reach of children
Effects of Missed Dosage of Clotrimazole
Apply the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.
Effects of Overdose of Clotrimazole
Give supportive measures and symptomatic treatment.

Betamethasone

About Betamethasone
Potent glucocorticoid, Anti-inflammatory, immunosuppressent.
Mechanism of Action of Betamethasone
The drug exerts it`s pharmacological action by penetrating and binding to cytoplasmic receptor protein and causes a structural change in steroid receptor complex. This structural change allows it`s migration in to the nucleus and then binding to specific sites on the DNA which leads to transcription of specific m-RNA and which ultimately regulates protein synthesis. It exerts highly selective glucocorticoid action. It stimulates the enzymes needed to decrease the inflammatory response.
The drug exerts anti-inflammatory and immunosuppressant actions as follows: - 1) Induce lipocortins in macrophages, endothelium, and fibroblasts which inhibits phospholipase A2 and thus decreases the production of Prostaglandins, leukotriens (LT), and platelet activating factor, 2) Causes negative regulation of genes for cytokines in macrophages, endothelial cells and lymphocytes and thus decreases the production of interleukins (IL-1, IL-2, IL-3, IL-6), TNF-alpha, GM-CSF (granulocyte macrophage colony stimulating factor), Gama interferon and suppresses fibroblast proliferation and T-lymphocyte functions and interferes chemotaxis. 3) Decreases the production of acute phase reactants from macrophages and endothelial cells and interferes complement function. 4) Decreases the production of ELAM-1(Endothelial leukocyte adhesion molecule-1) and ICAM-1(intracellular adhesion molecule-1) in endothelial cells. 5) Inhibit IgE mediated histamine and LT-C4 release from basophiles and the effects of antigen-antibody reaction is not mediated 6) Reduces the production of collagenase and stromolysin and thus prevents tissue destruction.
Pharmacokinets of Betamethasone
Absorption: Well absorbed orally, Distribution: Distributed in to muscle, liver, kidney, skin, and intestine. It crosses the placenta and also secreted in breast milk, Metabolism: Metabolized in liver in to inactive metabolites by glucuronide and sulfate conjugation. Excretion: Metabolites are excreted mainly through urine and a small amount is excreted through faeces.
Topical:-Absorption: It is absorbed in to the systemic circulation and the amount is depending on the potency, amount applied and the nature of the skin at the site of application. Absorption increases at the site of skin damage, inflammation or occlusion
Onset of Action for Betamethasone
N/A
Duration of Action for Betamethasone
3 to 25 days
Half Life of Betamethasone
36 to 54 hours
Side Effects of Betamethasone
1.Susceptibility to infection
2.Peptic ulcer
3.Haemorrhage
4.Glycosuria
5.Hyperglycaemia
6.Osteoporosis
7.Atrophy of adrenal cortex(on prolonged therapy)
8.Suppression of adrenocorticotropic hormone
9.Cushing`s syndrome
10.Inhibition of growth in children
11.Amenorrhoea
12.Behavioral disturbances
13.Thromboembolic disorders
14.Myopathy
15.Weakness
16.Lymphocytopenia
17.Muscle wasting
18.Gastrointestinal discomfort
19.Increased appetite
20.Delayed wound healing
21.Headache
22.Euphoria
23.Insomnia
24.Seizures
25.Heart failure
26.Arrhythmias
27.Posterior sub capsular cataract
28.Glaucoma
29.Hirsutism
30.Increased intracranial pressure.
Topcal:
1.Burning
2.Irritation
3.Dryness
4.Erythema
5.Folliculitis
6.Striae
7.Skin atrophy
8.tching
Contra-indications of Betamethasone
1.Hypersensitivity to the drug
2.Untreated infections
3.Systemic fungal infections
Topical:
1.Hypersensitivity to Betamethasone and other corticosteroids
2.Untreated bacterial, virus or fungal infections
3.Acne vulgaris
4.Peri-oral dermatitis
5.Scabies
6.Leg ulcers
7.Tuberculosis of the skin
8. Varicose ulcers
9. Skin lesions caused by infections with ring worm, fungi (e.g. Candida, Tinea) or bacteria (e.g. impetigo)
10.Discoid lupus Erythematosus
Special Precautions while taking Betamethasone
1.Avoid sudden discontinuation of the drug
2.Use lower dosages as much as possible
3.Concurrent vaccination
4.Ocular herpes simplex
5.Primary glaucoma
6.Peptic ulcer
7.Psychosis
8.Tuberculosis
9.Epilepsy
10.Osteoporsis
11.Congestive heart failure
12.Renal impairment
13.Recent myocardial infarction
14.Heart failure
15.Diabetes mellitus
16.Hypothyroidism
17.Cirrhosis
18.Stress
19.Sepsis
20.Hypertension
21.Myasthenia gravis
22.Hepatic impairment
23.Non specific Ulcerative colitis
24.Diverticulitis
25.Recent intestinal anastomosis
26.Thromboembolic disorders
27.Avid contact of the topical dosage form with the eyes
Pregnancy Related Information
Use with caution
Old Age Related Information
Use with caution
Breast Feeding Related Information
Use with caution
Children Related Information
Use with caution
Neonates: Contraindicated
Indications for Betamethasone
1.Inflammatory conditions
2.Allergic reactions
3.Shock
4.Anaphylaxis
5.Intra-articular and soft tissue inflammation
6.Asthma
7.Rheumatoid arthritis
8.Adrenal insufficiency
9.Tuberculous meningitis
10.Respiratory diseases
11.Malignancies
12.Cerebral oedema
13.Collagen diseases
14.Addison`s disease
15.Simmond`s disease
16.Hypopitutarism following adrenalectomy
17.Taenosynovitis.
Interactions for Betamethasone
Barbiturates: Decrease efficacy of Betamethasone
Carbamazepine, Primidone: Decreases efficacy.
Oral contraceptives: Increase efficacy of Betamethasone.
Oestrogens: Decreases efficacy of Betamethasone.
Ketoconazole: Increases efficacy of Betamethasone.
Rifampicin: Decreases efficacy.
Betamethasone effects the actions of the following:
Anticholinesterases: Efficacy antagonised in myasthenia gravis.
Oral anticoagulants: Altered response.
Cyclosporine: Increases efficacy leading to enhanced toxicity.
Digitals glycosides: Increases toxicity associated with hypokalaemia.
Isoniazid: Decreases serum levels.
Salicylates: Decreases serum levels.
Diuretics: Increases efficacy may cause increased hypokalaemia and increased hyperglycaemia.
Non-depolarising muscle relaxants - Altered response.
Somatrem: Growth promoting effect inhibited.
Theophyllines: Altered response of either agent.
IUCD: Contraceptive failure.
Lab. Tests:
a) Increases serum cholesterol levels.
b) Increases urine glucose levels.
c) Decreases Thyroid l 131 uptake; Decreases T3 serum levels.
d) Decreases serum potassium.
Typical Dosage for Betamethasone
Oral: Starts with 0.5 to 6mg/day. Reduces to minimum effective; maintenance dosage.
Children:
1 to 6 years: 25 to 50%
7 to 12 years: 50 to 75%
I.M. or I.V.: 4 to 20mg I.M. or as slow I.V. injection. Repeated if required; up to 4 times daily depending up on the severity of condition.
Children: Administered by slow I.V. injection;
<1year: 1mg
1 to 5 years: 2mg
6 to 12 years: 4mg
Intra-articular or soft tissue injection: 0.5 to 9mg depending up on the severity of the condition.
Topical:
Betamethasone Valerate: Apply to the affected area as thin film 1 - 4 times daily depending upon the severity, skin and rate of absorption.
Dermatoses of the scalp: (Betamethasone Valerate 0.12%): Small amount of foam is applied in to the scalp with gentle massage 2 times a day for up to 2 weeks.
Betamethasone dipropionate: Apply to the affected area as thin film 1 -2times daily
Schedule of Betamethasone
H
Storage Requirements for Betamethasone
Store at room temperature in a well closed; light resistant container. Protect from excess heat and moisture. Keep out of reach of children.
Effects of Missed Dosage of Betamethasone
Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.
Effects of Overdose of Betamethasone
Provide symptomatic treatment and supportive measures.

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