Ophtagram

Ophtagram Uses, Dosage, Side Effects, Food Interaction and all others data.

Ophtagram sulphate actively transported across the bacterial cell membrane, binds to a specific receptor protein on the 30S subunit of bacterial ribosomes and interferes with an initiation complex between mRNA (messenger RNA) and the 30 S subunit, inhibiting protein synthesis. DNA may be misread, thus producing nonfunctional proteins; polyribosomes are split apart and are unable to synthesize protein.

Eye drops may be absorbed following topical application to the eye. Ear drops may be absorbed following topical application to the ear, especially if the eardrum is perforated or if tissue damage is present.

Ophtagram sulphate is active against many strains of the following microorganisms: Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus pyogenes, Streptococcus pneumoniae, Escherichia coli, Haemophilus influenzae, Klebsiella pneumoniae, Niesseria gonorrhoea, Pseudomonus aeruginosa, and Serratia marcescens.

Trade Name Ophtagram
Availability Prescription only
Generic Gentamicin
Gentamicin Other Names Gentamicin, Gentamicina
Related Drugs amoxicillin, doxycycline, ciprofloxacin, cephalexin, metronidazole, azithromycin, clindamycin, ceftriaxone, levofloxacin, Augmentin
Type
Formula C21H43N5O7
Weight Average: 477.5954
Monoisotopic: 477.316248755
Protein binding

Studies have determined that plasma protein binding of gentamicin is between 0-30% depending on the method of testing.

Groups Approved, Vet approved
Therapeutic Class Ophthalmic antibacterial drugs
Manufacturer
Available Country Switzerland
Last Updated: September 19, 2023 at 7:00 am
Ophtagram
Ophtagram

Uses

Blepharitis, blepharoconjunctivitis, conjunctivitis, dacryocystitis, keratitis, keratoconjunctivitis, acute meibomianitis, and corneal ulcers caused by susceptible organisms. Otorrhea associated with external otitis, chronic suppurative otitis media or subacute purulent otitis media; or postoperative otorrhea, such as that following fenestration, mastoidectomy or tympanoplasty.

Ophtagram cream is used for the topical treatment of the primary and secondary bacterial infections of the skin caused by the organisms sensitive to Ophtagram. Ophtagram may clear infections that have not responded to other topical antibiotics.

Ophtagram is also used to associated treatment for these conditions: Bacterial Conjunctivitis, Bacterial Infections, Bacterial Peritonitis, Bacterial dacryocystitis, Blepharoconjunctivitis, Central Nervous System Infections, Conjunctivitis allergic, Corneal infection, Dermatitis infected, Ecthyma, Eczematous dermatitis infected, Folliculitis, Furunculosis, Gram-negative enteric bacilli neonatal sepsis, Impetigo contagious, Inflammation, Keratitis bacterial, Keratoconjunctivitis, Meibomianitis, Meningitis, Bacterial, Ocular Inflammation, Pustular Psoriasis (PP), Pustular acne, Pyoderma Gangrenosum, Seborrheic Dermatitis, Septicemia gram-negative, Skin Infections, Skin Infections, Bacterial, Skin and Subcutaneous Tissue Bacterial Infections, Sycosis barbae, Bacterial blepharitis, Bacterial corneal ulcers, Bacterial dermatoses, Complicated Bacterial Urinary Tract Infections, Complicated Respiratory tract infection bacterial, Corticosteroid-responsive dermatoses, Ocular bacterial infections, Severe Endocarditis enterococcal, Severe Infection Pseudomonas aeruginosa, Severe Staphylococcal infection

How Ophtagram works

There are 3 key phases of aminoglycoside entry into cells. The first “ionic binding phase” occurs when polycationic aminoglycosides bind electrostatically to negatively charged components of bacterial cell membranes including with lipopolysaccharides and phospholipids within the outer membrane of Gram-negative bacteria and to teichoic acids and phospholipids within the cell membrane of Gram-positive bacteria. This binding results in displacement of divalent cations and increased membrane permeability, allowing for aminoglycoside entry. The second “energy-dependent phase I” of aminoglycoside entry into the cytoplasm relies on the proton-motive force and allows a limited amount of aminoglycoside access to its primary intracellular target - the bacterial 30S ribosome. This ultimately results in the mistranslation of proteins and disruption of the cytoplasmic membrane.[A233320] Finally, in the “energy-dependent phase II” stage, concentration-dependent bacterial killing is observed. Aminoglycoside rapidly accumulates in the cell due to the damaged cytoplasmic membrane, and protein mistranslation and synthesis inhibition is amplified. The necessity of oxygen-dependent active transport explains why aminoglycosides are ineffective against anaerobic bacteria. Hence, aminoglycosides have both immediate bactericidal effects through membrane disruption and delayed bactericidal effects through impaired protein synthesis; observed experimental data and mathematical modeling support this two-mechanism model. Inhibition of protein synthesis is a key component of aminoglycoside efficacy. Structural and cell biological studies suggest that aminoglycosides bind to the 16S rRNA in helix 44 (h44), near the A site of the 30S ribosomal subunit, altering interactions between h44 and h45. This binding also displaces two important residues, A1492 and A1493, from h44, mimicking normal conformational changes that occur with successful codon-anticodon pairing in the A site.[A232324, A232329] Overall, aminoglycoside binding has several negative effects including inhibition of translation, initiation, elongation, and ribosome recycling. Recent evidence suggests that the latter effect is due to a cryptic second binding site situated in h69 of the 23S rRNA of the 50S ribosomal subunit.[A232329, A232339] Also, by stabilizing a conformation that mimics correct codon-anticodon pairing, aminoglycosides promote error-prone translation.[A232344] Mistranslated proteins can incorporate into the cell membrane, inducing the damage discussed above.

Dosage

Ophtagram dosage

Eye: 1-2 drops instilled in affected eye up to 6 times a day or more frequently if required (severe infections may require 1-2 drops every 15-20 minutes initially, reducing the frequency of instillation gradually as the infection is controlled).

Ear: The area should be cleaned and 2-3 drops should be instilled every 3-4 times a day and at night, or more frequently if required.

A small amount of Ophtagram should be applied gently to the affected areas three to four times daily. The area treated may be covered with a gauze dressing if desired. Before applying the medication the affected area should be properly cleaned.

Side Effects

In patients with dermatoses treated with gentamicin, irritation (erythema and pruritus) had been reported in small number of cases. Itching, redness, swelling or other signs of irritation may develop. With the eye/ear drop bacterial and corneal ulcer have developed during treatment with gentamicin. Most frequently reported adverse reactions are ocular burning and irritation upon drug instillation, non specific conjunctivitis, conjunctival epithelial defects, and conjunctival hyperemia.

Ophtagram cream is well tolerated. There has been no evidence of irritation and sensitization after using Ophtagram cream.

Toxicity

As with other aminoglycosides, nephrotoxicity and ototoxicity are associated with gentamicin. Signs of nephrotoxicity include an increase in plasma creatinine and urea, while signs of ototoxicity include issues with balance, nausea, tinnitus, and hearing loss. It is important to note that aminoglycoside-induced nephrotoxicity is typically reversible, while ototoxicity is more likely to be permanent. The risk of both toxicities increases with long-term gentamicin therapy. Ophtagram is considered to be more vestibulotoxic than cochleotoxic compared to other aminoglycosides. Unfortunately, gentamicin-related ototoxicity does not correlate with cumulative dosing, peak and trough levels, or dosing schedule. The unpredictability of ototoxicity supports close monitoring of the patient throughout treatment. In cases of toxicity or overdose, the medication should be discontinued immediately; hemodialysis may be initiated to lower gentamicin serum concentrations.

Precaution

If these occurs or if irritation, sensitization develops, treatment with gentamicin should be discontinued and appropriate therapy instituted. Ophtagram ear/eye drops is not for injection. It should never be injected subconjunctivally, nor it should be directly introduced into the anterior chamber of the eye.

Use of topical antibiotics occasionally cause overgrowth of nonsusceptible organisms including fungi. If this occurs or if irritation, sensitisation or super infection develops, treatment with Ophtagram should be discontinued and appropriate therapy should be instituted.

Interaction

None has been reported so far with topical and Eye/Ear drops.

Food Interaction

No interactions found.

Half Life

One study assessing the pharmacokinetics of gentamicin in children and adults reported a mean half-life of 75 minutes after intravenous administration. The mean half-life associated with intramuscular administration was about 29 minutes longer. Fever and anemia may result in a shorter half-life although dose adjustments are not usually necessary. Severe burns are also associated with a shorter half-life and may result in lower gentamicin serum concentrations.

Clearance

The renal clearance of gentamicin is comparable to individual creatinine clearance.

Elimination Route

Ophtagram is excreted primarily by the kidneys. In patients with normal renal function, 70% or more of an initial gentamicin dose can be recovered in the urine within 24 hours. Excretion of gentamicin is significantly reduced in patients with renal impairment.

Pregnancy & Breastfeeding use

Consideration should be given the possibility of foetal ototoxicity when gentamicin is applied topically to large denuded areas of skin. For Ophtagram Eye/Ear Drops safety profile in pregnancy is not yet established and should be administered when considered essential.

Contraindication

Ophtagram is contraindicated in individuals with a history of sensitivity reaction to any of its components. Use of topical Ophtagram may occasionally allow overgrowth of nonsusceptible organisms, including fungi.

Storage Condition

To avoid contamination, do not touch the tip of the container to the eye, eyelid or any surface.

Innovators Monograph

You find simplified version here Ophtagram

Ophtagram contains Gentamicin see full prescribing information from innovator Ophtagram Monograph, Ophtagram MSDS, Ophtagram FDA label

FAQ

What is Ophtagram used for?

Ophtagram is an antibiotic used to treat several types of bacterial infections. This may include bone infections, endocarditis, pelvic inflammatory disease, meningitis, pneumonia, urinary tract infections, and sepsis among others.


How safe is Ophtagram?

Ophtagram is safe and has similar outcomes to alternative Gram-negative antimicrobial regimens for empirical coverage in severe CAP patients admitted to the ICU. Ophtagram can harm your kidneys, and may also cause nerve damage or hearing loss, especially if you have kidney disease or use certain other medicines. Tell your doctor about all your medical conditions and all the medicines you are using.

How does Ophtagram work?

Ophtagram works by killing bacteria or preventing their growth.

What are the common side effects of Ophtagram?

Common side effects of Ophtagram are include:

  • nausea
  • vomiting
  • diarrhea
  • decreased appetite
  • pain at the injection site
  • headache
  • fever
  • joint pain
  • unusual tiredness

Is Ophtagram safe during pregnancy?

If this Ophtagram is used during pregnancy, or if the patient becomes pregnant while taking this drug, the patient should be apprised of the potential harm to the fetus.

Is Ophtagram safe during breastfeeding?

Small amounts of this medicine pass into breast milk, but it is not thought to be harmful to nursing babies. New mothers, however, should avoid breastfeeding when taking this Ophtagram.

Can I drink alcohol with Ophtagram?

Using alcohol with certain medicines may also cause interactions to occur.

Can I drive after taking Ophtagram?

Your vision may become slightly blurred for a short while after using the drops. If so, do not drive and do not use tools or machines until you can see clearly again.

How long does it take for Ophtagram to leave my system?

Ophtagram is not metabolized in the body but is excreted unchanged in microbiologically active form predominantly via the kidneys. In patients with normal renal function the elimination halflife is about 2 to 3 hours.

How long can I take Ophtagram?

Do not use Ophtagram in larger or smaller amounts or for longer than recommended. Ophtagram is usually given for 7 to 10 days. Ophtagram is injected into a muscle, or into a vein through an IV.

Can Ophtagram be taken orally?

It is not absorbed from the gut when administered orally, and is therefore predominantly administered via intramuscular or intravenous injection.

How often can Ophtagram be given?

Apply 1 drop at least every 2 hours, reduce frequency as infection is controlled and continue for 48 hours after healing, frequency of eye drops depends on the severity of the infection and the potential for irreversible ocular damage; for less severe infection 3–4 times daily is generally sufficient.

When should be best taken of Ophtagram?

When Ophtagram is injected intravenously, it is usually infused over a period of 30 minutes to 2 hours once every 6 or 8 hours. The length of your treatment depends on the type of infection you have.

Should Ophtagram be taken with food?

In some cases, this may be harmful and your doctor may advise you to avoid certain foods. In the case of Ophtagram, there are no specific foods that you must exclude from your diet when receiving this medication.

Who should not take Ophtagram?

Ophtagram can harm your kidneys, and may also cause nerve damage or hearing loss, especially if you have kidney disease or use certain other medicines. Tell your doctor about all your medical conditions and all the medicines you are using. If you need surgery, tell the surgeon ahead of time that you are using gentamicin.

When should Ophtagram be stopped?

Ophtagram should be discontinued if the patients suffers severe diarrhoea and/or bloody diarrhoea during treatment and an appropriate treatment should be initiated. Ophtagram that inhibit peristalsis should not be administered.

How long does Ophtagram take to work?

You should start to feel better within a few days.

What should if I miss a dose?

If you miss a dose of this medicine, 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.

What happens if I give too much Ophtagram?

Ophtagram toxicity is known to cause any of the following: Kidney damage and renal failure. Nerve damage. Ototoxicity (damage to the ear, such as hearing loss, vertigo or ringing in the ears)

Will Ophtagram affect my fertility?

They may reduce the number of sperm a man produces, and make the sperm he does produce swim more slowly. These are some of the antibiotics that could affect sperm quantity and movement.

Can Ophtagram affects my liver?

Ophtagram has not been definitively linked to instances of clinically apparent liver injury.

Can Ophtagram affect my kidneys?

Ophtagram can harm your kidneys, and may also cause nerve damage or hearing loss, especially if you have kidney disease or use certain other medicines.

*** Taking medicines without doctor's advice can cause long-term problems.
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