Miconazole + Gentamicin + Betamethasone Pharmacology

Miconazole + Gentamicin + Betamethasone

About Miconazole + Gentamicin + Betamethasone
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Mechanism of Action of Miconazole + Gentamicin + Betamethasone
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Pharmacokinets of Miconazole + Gentamicin + Betamethasone
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Onset of Action for Miconazole + Gentamicin + Betamethasone
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Duration of Action for Miconazole + Gentamicin + Betamethasone
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Half Life of Miconazole + Gentamicin + Betamethasone
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Side Effects of Miconazole + Gentamicin + Betamethasone
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Contra-indications of Miconazole + Gentamicin + Betamethasone
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Special Precautions while taking Miconazole + Gentamicin + Betamethasone
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Pregnancy Related Information
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Old Age Related Information
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Breast Feeding Related Information
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Children Related Information
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Indications for Miconazole + Gentamicin + Betamethasone
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Interactions for Miconazole + Gentamicin + Betamethasone
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Typical Dosage for Miconazole + Gentamicin + Betamethasone
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Schedule of Miconazole + Gentamicin + Betamethasone
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Storage Requirements for Miconazole + Gentamicin + Betamethasone
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Effects of Missed Dosage of Miconazole + Gentamicin + Betamethasone
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Effects of Overdose of Miconazole + Gentamicin + Betamethasone
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Miconazole

About Miconazole
An imidazole derivative, Broad spectrum Antifungal.
Mechanism of Action of Miconazole
Miconazole is fungicidal or fungistatic depending on the drug concentrations. I t inhibits the conversion of Lanosterol to 14 demethyl Lanosterol by inhibiting the cytochromeP450 enzyme 14 alpha demethylase and impair ergosterol synthesis
Pharmacokinets of Miconazole
Absorption: Oral absorption of Miconazole is poor. Distribution: It is distributed in the body in protein bound form Metabolism: It undergoes metabolism in the liver. Excretion: It is excreted in urine and faeces.
Onset of Action for Miconazole
N/A
Duration of Action for Miconazole
N/A
Half Life of Miconazole
1 day
Side Effects of Miconazole
1.Vulvovaginal burning
2.Burning
3.Irritation
4.Pruritis
5.Maceration
6.Dermatitis
Contra-indications of Miconazole
1.Hypersensitivity to Miconazole and other Azole antifungals
Special Precautions while taking Miconazole
1.Hepatic dysfunction
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Use with caution
NEONATES: contraindicated
Indications for Miconazole
1.Tinea versicolor
2.Vulvovaginal candidiasis
3.Tinea pedis
4.Tinea corporis
5.Tinea cruris
6.Otomycosis
7.Onychomycosis
8.Oral candidiasis
9.Intestinal candidiasis
10.Diaper dermatitis
Interactions for Miconazole
Benzoyl peroxide: Antibacterial synergism.
Typical Dosage for Miconazole
Adult: Topical use:
Cutaneous infections: Apply the cream twice daily on the affected part for about 1 month
Tinea versicolor: Apply the cream once daily on the affected part
Vaginal use: Insert 300 mg suppository at bed time for 3 days or Insert 100 mg suppository at bed time for 7 days

CHILDREN:
Topical use:
Cutaneous infections: Apply the cream twice daily on the affected part for about 1 month
Tinea vericolor: Apply the cream once daily on the affected part

Schedule of Miconazole
H
Storage Requirements for Miconazole
The drug should be stored at 15 - 30 degree C.
Effects of Missed Dosage of Miconazole
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 Miconazole
Give supportive measures and treatment.

Gentamicin

About Gentamicin
Aminoglycoside antibiotic.
Mechanism of Action of Gentamicin
Gentamicin exerts its bactericidal action against gram negative organisms & some of gram positive organisms by inhibiting bacterial protein synthesis. The process involves 1. Penetration of bacterial cell membrane & binding directly to the bacterial ribosome, 2. Misleading of m-RNA codon by bacterial ribosome, 3. Formation of peptide chains with wrong amino acid sequence which gets incorporated into bacterial cell membrane and alters its permeability, 4. Bacterial cell lysis. Some bacterial strains resistant to other amino glycosides are sensitive to Gentamicin.
Pharmacokinets of Gentamicin
Absorption: Poorly absorbed orally
Distribution: Distributed extracellularly. CSF penetration & intraocular penetration poor.
Metabolism: Not metabolized
Excretion: Excreted mainly through urine.

Onset of Action for Gentamicin
1 hour
Duration of Action for Gentamicin
8 hours
Half Life of Gentamicin
2 hours
Side Effects of Gentamicin
1. Vestibular damage & Ototoxicity
2. Allergic manifestations
3. Nephrotoxicity
4. Dizziness
5. Nausea
6. Vomiting
7. Seizures
Contra-indications of Gentamicin
1. Hypersensitive to the drug or other amino glycosides
2. Along with chloramphenicol or tetracycline
3. Renal impairment
4. Labyrinthine disorders

Special Precautions while taking Gentamicin
1. Renal impairment
2. Neuromuscular disorders
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Use with caution
Infants : Use with caution
Indications for Gentamicin
1. Infections caused by staphylococci, pseudomonas, proteous, klebsiella, enterobacter & serratia.
2. Meningitis.
3. Endocarditis
4. Urinary Tract Infections.
5. Otitis & Ocular infections.
6. Infections of burns & Skin ulcers
Interactions for Gentamicin
Amphotericin B, Cisplatin, Cephalosporin, Vancomycin, Methoxyflurane, Frusemide, Bumetanide: Increased nephrotoxicity.
Anaesthetics, Neuromuscular blocking agents (Tubocurarine): Risk of neuromuscular blockade and respiratory paralysis.
Penicillin, Cephalosporins, Carbenicillin, Ticarcillin: Exert antibiotic synergism, especially useful in Pseudomonas infections.
Loop diuretics: Concurrent use of these agents may increase the risk of respiratory paralysis and renal dysfunction.
Lab Tests: Aminoglycoside serum levels: Guard against in vitro inactivation of aminoglycosides by b-lactum antibiotics in patients on combination therapy.
Typical Dosage for Gentamicin
Dosage:
Adults: 2 to 5mg/kg/day; Thrice daily for a week or more
Children: 2 to 2.5mg/kg; Thrice daily.
Schedule of Gentamicin
H
Storage Requirements for Gentamicin
Store below 30 degree Celsius and protect from light.
Effects of Missed Dosage of Gentamicin
Take the missed dose as soon as noticed and if it is the time to next dose then skip the missed dose.Continue the regular schedule. Do not double the dose.
Effects of Overdose of Gentamicin
An overdose results in ototoxicity, nephrotoxicity, neuromuscular disorders & hypersensitivity manifestations.Treatment includes removal of drug by dialysis or by treatment with anticholinesterase like neostigmine and by administration of Ca , Prednisolone etc.

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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