Opthomycin Actions

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Actions of Opthomycin in details

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Description: Opthomycin inhibits bacterial protein synthesis by binding to 50s subunit of the bacterial ribosome, thus preventing peptide bond formation by peptidyl transferase. It has both bacteriostatic and bactericidal action against H. influenzae, N. meningitidis and S. pneumoniae.

Duration: Typhoid: 8-10 days; meningitis: 7-10 days; brain abscess: Up to 4 wk.

Pharmacokinetics:

Absorption: Readily absorbed with peak plasma concentrations after 1 or 2 hr (oral).

Distribution: Distributed widely into tissues and fluids, CSF (up to 50% even in the absence of meningitis), eye (aqueous and vitreous humours); crosses the placenta and enters the breast milk. Protein-binding: 60%.

Metabolism: Hydrolysed to the free drug in the GI tract (palmitate); liver by conjugation with glucuronic acid, lungs and kidneys after parenteral admin (sodium succinate).

Excretion: Via the urine (30% as unchanged before hydrolysis, 5-10% of an oral dose), via the bile (3%), via the faeces (1% as inactive form); 1.5-4 hr (elimination half-life).

How should I take Opthomycin?

For patients using the eye drop form of Opthomycin:

To use the eye ointment form of Opthomycin:

To help clear up your infection completely, keep using Opthomycin for the full time of treatment, even if your symptoms begin to clear up after a few days. If you stop using Opthomycin too soon, your symptoms may return. Do not miss any doses.

Dosing

The dose of Opthomycin 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 Opthomycin. 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.

Missed Dose

If you miss a dose of Opthomycin, 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.

Opthomycin administration

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IV: For IV use only; do not administer IM. Can be administered IVP over at least 1 minute at a concentration of 100 mg/mL.

Opthomycin pharmacology

Reversibly binds to 50S ribosomal subunits of susceptible organisms preventing amino acids from being transferred to growing peptide chains thus inhibiting protein synthesis

Distribution

To most tissues and body fluids (Ambrose 1984); good CSF and brain penetration

CSF concentration with uninflamed meninges: 21% to 50% of plasma concentration

CSF concentration with inflamed meninges: 45% to 89% of plasma concentration

V: Opthomycin: 0.6 to 1 L/kg; Opthomycin succinate: 0.2 to 3.1 L/kg (Ambrose 1984)

Metabolism

Opthomycin: Hepatic to metabolites (inactive); Opthomycin succinate: Hydrolyzed in the liver, kidney and lungs to Opthomycin (active) (Ambrose 1984)

Excretion

Urine (~30% as unchanged Opthomycin succinate in adults, 6% to 80% in children; 5% to 15% as Opthomycin) (Ambrose 1984; Powell 1982)

Half-Life Elimination

Neonates: 1 to 2 days: 24 hours; 10 to 16 days: 10 hours

Opthomycin: Infants: Significantly prolonged (Powell 1982); Children 4 to 6 hours; Adults: ~4 hours (Ambrose 1984)

Hepatic disease: Prolonged (Ambrose 1984)

Protein Binding

Opthomycin: ~60%; decreased with hepatic or renal dysfunction and 30% to 40% in newborn infants (Ambrose 1984)


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References

  1. DailyMed. "CHLORAMPHENICOL: 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. NCIt. "Chloramphenicol: 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).
  3. EPA DSStox. "Chloramphenicol: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).

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Information checked by Dr. Sachin Kumar, MD Pharmacology

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