Dexamethasone + Neomycin Pharmacology

Dexamethasone + Neomycin

About Dexamethasone + Neomycin
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Mechanism of Action of Dexamethasone + Neomycin
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Pharmacokinets of Dexamethasone + Neomycin
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Onset of Action for Dexamethasone + Neomycin
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Duration of Action for Dexamethasone + Neomycin
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Half Life of Dexamethasone + Neomycin
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Side Effects of Dexamethasone + Neomycin
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Contra-indications of Dexamethasone + Neomycin
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Special Precautions while taking Dexamethasone + Neomycin
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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 Dexamethasone + Neomycin
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Interactions for Dexamethasone + Neomycin
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Typical Dosage for Dexamethasone + Neomycin
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Schedule of Dexamethasone + Neomycin
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Storage Requirements for Dexamethasone + Neomycin
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Effects of Missed Dosage of Dexamethasone + Neomycin
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Effects of Overdose of Dexamethasone + Neomycin
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Dexamethasone

About Dexamethasone
A potent synthetic glucocorticoid, Antiasthmatic, anti-inflammatory and immunosuppressant.
Mechanism of Action of Dexamethasone
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-a, GM-CSF (granulocyte macrophage colony stimulating factor), Gama interferon and suppresses fibroblast proliferation and T-lymphocyte functions and interferes chemo taxis. 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.
Dexamethasone has antiemetic properties, particularly against acute and delayed vomiting induced by cancer chemotherapy. It may be used alone for prevention of acute symptoms associated with moderately-emetogenic treatment and is combined with a 5-HT3 antagonist for highly-emetogenic treatment. Dexamethasone is also effective for the prevention of postoperative nausea and vomiting, and may be used to manage nausea and vomiting in palliative care.
Pharmacokinets of Dexamethasone
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.
Onset of Action for Dexamethasone
1 to 2hours
Duration of Action for Dexamethasone
2 or more days
Half Life of Dexamethasone
36 to 54 hours
Side Effects of Dexamethasone
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.Thromoembolic disorders
14.Myopahy
15.Weaknss
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
Eye preparation:
1.Burning
2.Redness
3.Stinging in the eye
4.Blurred vision


Contra-indications of Dexamethasone
1.Hypersensitivity to the drug
2.Psychosis
3.Tuberculosis
4.Untreated infections
5.Systemic fungal infections
6.Osteoporosis
7.Congestive heart failure
8.Renal impairment
Special Precautions while taking Dexamethasone
1.Avoid sudden discontinuation of the drug
2.Use lower dosages as much as possible
3.Ocular herpes simplex
4.Primary glaucoma
5.Peptic ulcer
6.Epilepsy
7.Recent myocardial infarction
8.Heart failure
9.Diabetes mellitus
10.Hypothyroidism
11.Cirrhosis
12.Stress
13.Sepsis
14.Hypertension
15.Myasthenia gravis
16.Hepatic impairment
17.Non specific Ulcerative colitis
18.Diverticulitis
19.Recent intestinal anastomosis
20.Thromboembolic disorders
Eye preparation:
1.Cataracts
2.Contact lens wearer
3.Diabetes
4.Glaucoma



Pregnancy Related Information
Contraindicated.
Old Age Related Information
Use with caution.
Breast Feeding Related Information
Use with caution.
Children Related Information
Use with caution.
Neonates: Contraindicated
Indications for Dexamethasone
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.Acute gout
14.Nausea and vomiting induced by cancer chemotherapy
15. Pemphigus
Interactions for Dexamethasone
ENDOCRINE SYSTEM: Barbiturates: Decreases efficacy of dexamethasone.
Carbamazepine, Primidone: Decreases efficacy.
Oral contraceptives: Increases efficacy of dexamethasone.
Ephedrine: Decrease efficacy of dexamethasone.
Oestrogens: Decrease efficacy of dexamethasone
Hydantoins: Decrease efficacy of dexamethasone
Ketoconazole: Increase efficacy of dexamethasone
Rifampicin: Decreases efficacy.
Dexamethasone effects the actions of the following:
Anticholinesterases: Efficacy antagonised in myasthenia gravis.
Oral anticoagulants: Altered response.
Cyclosporine: Increased cyclosporine efficacy leading to enhanced toxicity.
Digitalis glycosides: Increased toxicity associated with hypokalaemia.
Isoniazid: Decreased serum levels of isoniazid.
Salicylates: Decreased serum levels of salicylates.
Diuretics: Increase efficacy may cause increased hypokalaemia and increased hyperglycemia.
Non-depolarising muscle relaxants: Altered response.
Theophyllines: Altered response of either agent.
IUCDs: contraceptive failure.
Lab. Tests: a) Increases serum cholesterol levels.
Increases urine glucose levels.
Decreases Thyroid I131 uptake. Decreases T3 serum levels. Decreases serum potassium.
Brain Scan: Dexamethasone alters result of brain scan due to decreased uptake of radioactive material.

Typical Dosage for Dexamethasone
Oral: 0.5 to 10mg/day depending up on the severity of the condition.
I.M. or I.V.: 0.5 to 20mg/day I.M. or as slow I.V. injection depending up on the severity of the condition; repeated as required up to 80mg/day.
Antiemetic: 4 to 8 mg by mouth immediately before moderately-emetogenic chemotherapy and 20 mg by intravenous injection for more severely emetogenic chemotherapy.
Children: 100mcg to 500mcg/kg/day
Schedule of Dexamethasone
H
Storage Requirements for Dexamethasone
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 Dexamethasone
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 Dexamethasone
Provide symptomatic treatment and supportive measures.

Neomycin

About Neomycin
An aminoglycoside, Antibiotic, Ammonium Detoxicant.
Mechanism of Action of Neomycin
This aminoglycoside cause protein synthesis inhibition by "irreversibly" bind to specific 30S-subunit proteins and 16S rRNA. Specifically Neomycin binds to four nucleotides of 16S rRNA and a single amino acid of protein S12. This interferes with decoding site in the vicinity of nucleotide 1400 in 16S rRNA of 30S subunit. This region interacts with the wobble base in the anticodon of tRNA. This leads to interference with the initiation complex, misreading of mRNA so incorrect amino acids are inserted into the polypeptide leading to nonfunctional or toxic peptides and the breakup of polysomes into nonfunctional monosomes.
Pharmacokinets of Neomycin
Absorption- Poorly absorbed after oral administration
Distribution- Rapidly distributed in the body after oral administration. 30% bound to the plasma proteins. It crosses the placenta
Metabolism- Not metabolized
Excretion- Excreted through urine and feces (primarily as unchanged form). It also excreted through breast milk
Onset of Action for Neomycin
1 to 4 hr after oral administration
Duration of Action for Neomycin
8hrs after oral administration
Half Life of Neomycin
Its plasma half life is 2 to 3 hrs
Side Effects of Neomycin
1. Rash
2. Diarrhoea
3. Inflammation of the large intestine (colitis)
4. Nausea
5. Vomiting
6. Ototoxicity
7. Damage to the kidneys
8. Damage to vestibular function within the ear
Contra-indications of Neomycin
1. Hypersensitivity to the drug or any ingredients of it
2. Hypersensitivity to other amino glycosides
3. Intestinal obstruction
Special Precautions while taking Neomycin
1. Impaired renal function
2. Neuromuscular disorder
3. Ulcerative bowel lesions
4. Extensive dermatologic conditions
5. Any other eye infection or condition
6. Glaucoma
7. Cataract surgery
8. Blockage of the bowel
9. Eighth-cranial-nerve disease (loss of hearing and/or balance)
10. Kidney disease
11. Myasthenia gravis
12. Parkinson`s disease
13. Ulcers of the bowel
Pregnancy Related Information
Contraindicated
Old Age Related Information
Use with caution
Breast Feeding Related Information
Contraindicated
Children Related Information
Use with caution
Indications for Neomycin
1. Coma due to liver disease
2. Preventing infection following surgery
3. Topical infections
4. Systemic infections
Interactions for Neomycin
N/A
Typical Dosage for Neomycin
Ophthalmic suspension:
Adults-
1 or 2 drops every three or four hours- For eye infection
Oral (solution, tablets):
Adults and teenagers-
1 to 3 grams every six hours for five or six days- coma from liver disease
Adults and teenagers-
1 gram every hour for four hours, then 1 gram every four hours for the rest of a twenty-four hour period; or 1 gram nineteen hours before surgery, 1 gram eighteen hours before surgery, and 1 gram nine hours before surgery- cleaning the bowel before surgery.
Children-
14.7 milligrams mg/kg or 6.7 mg/ pound every four hours for three days
Ear preparation:
Adults and children-
2 to 5 drops into ear canal 3 to 4 times daily for 7 to 10 days- External ear canal infection
Schedule of Neomycin
C
Storage Requirements for Neomycin
Eye preparations store in the refrigerator protected from strong light. Do not freeze. Others are stored at <250C. Keep out of reach of children.
Effects of Missed Dosage of Neomycin
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 Neomycin
Give symptomatic and supportive treatment. Provide haemodialysis or peritoneal dialysis to remove the drug. Treated with calcium salts or anticholinesterase to reverses neuromuscular blockade. Administer activated charcoal to prevent the further absorption of drug

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