Use of Oral Pharmaceuticals in Optometry

In optometry settings, the integration of oral pharmaceuticals has become a valuable tool in addressing a diverse range of ocular conditions. These medications play a crucial role in treating not only bacterial and viral infections affecting the eye but also in managing allergic conditions and even dry eye disease. Beyond traditional topical treatments, oral pharmaceuticals offer a systemic approach to address underlying causes and provide comprehensive relief. Optometrists strategically employ these medications to combat microbial threats, modulate immune responses in allergic conditions, and enhance tear production in dry eye disease. Understanding the nuances of each oral pharmaceutical's mechanism of action and potential side effects is essential for optometrists to create effective and personalized treatment plans, ultimately contributing to improved patient outcomes and enhanced overall ocular health.

The use of oral antibiotics may play an important role in the treatment of various ocular conditions. Oral antibiotics can effectively address bacterial infections affecting the eyes, such as blepharitis, preseptal cellulitis and more severe cases involving the orbit. Chronic lid diseases like meibomian gland dysfunction can also benefit from systemic oral antibiotics. The class of antibiotics are chosen based on their specific mechanisms of action and spectrum of activity against different bacteria. These medications provide a comprehensive approach to managing ocular infections, allowing practitioners to tailor treatment plans to the unique characteristics of each patient's condition.

Penicillins, cephalosporins, macrolides, and tetracyclines are essential classes of antibiotics with distinct mechanisms of action, playing crucial roles in addressing bacterial infections. Understanding their unique properties and applications is pivotal for healthcare practitioners in providing effective treatment strategies for various microbial threats.

 

Penicillins are a class of antibiotics that combat bacterial infections by inhibiting the synthesis of bacterial cell walls, exhibiting bactericidal effects. The presence of a beta-lactam ring is essential for their antimicrobial activity. However, the efficacy of penicillins is compromised by the natural selection of bacteria producing beta-lactamase (penicillinase). Notably, Staph aureus and Staph epidermidis are frequent beta-lactamase producers. Dicloxacillin and methicillin are generally resistant to beta-lactamase, while ampicillin and amoxicillin offer broad-spectrum activity but lack penicillinase resistance. Augmentin, a combination of amoxicillin and clavulinate (a penicillinase inhibitor), addresses this limitation. Major side effects include allergic hypersensitivity reactions, ranging from type IV to type 1, with disruptions in intestinal flora leading to gastrointestinal disturbances. Prescriptions for various penicillins are chosen based on the specific clinical scenario, emphasizing the importance of understanding their spectrum of activity and resistance profiles in clinical practice.

 

Cephalosporins, derived from penicillins, exert their bactericidal effects by interfering with cell wall synthesis. Their effectiveness varies across four generations, distinguished by unique chemical side chains. While 1st-generation cephalosporins are more potent against gram-positive bacteria, 2nd and 3rd generations show increased efficacy against gram-negative strains, and the 4th generation is particularly active against resistant bacteria and gram-positives. Despite their structural similarities to penicillins, some beta-lactamases that deactivate penicillins may not affect cephalosporins. However, caution is advised, as about 5-10% of patients allergic to penicillins may cross-react with cephalosporins. Hypersensitivity reactions, especially type IV, are common side effects. Cephalosporins can disrupt normal intestinal flora, causing gastrointestinal disturbances, and may interfere with vitamin K synthesis, potentially leading to impaired clotting. Prescription options include Keflex, Ceclor, Duracef, and Cefzil, each tailored to specific clinical needs.

 

Macrolides, characterized by a large macrolide ring with attached sugars, exert their bacteriostatic effects by interfering with bacterial ribosomal protein synthesis, turning bactericidal at higher doses. Effective against both gram-positive and gram-negative bacteria, macrolides also demonstrate efficacy against chlamydia. Erythromycin, a notable macrolide, boasts anti-inflammatory properties, making it a valuable alternative when tetracyclines are contraindicated. While generally safe, common side effects, such as nausea, vomiting, and diarrhea, primarily affect the gastrointestinal tract. Prescription options include erythromycin in various formulations, including ethylsuccinate and delayed-release forms, as well as clarithromycin and azithromycin. Azithromycin stands out with increased absorption rates, a longer half-life, better tolerance, less frequent dosing, and improved compliance. However, caution is advised, as macrolide antibiotics may interact with statin medications and may potentially cause a prolonged QT interval, a form of ventricular fibrillation.

 

Tetracyclines emerge as the preferred antibiotics for chronic lid diseases, including meibomitis, chronic blepharitis, recurrent chalazia, and recurrent corneal erosions (RCEs). In contrast, acute hordeola are better addressed with macrolides, cephalosporins, or penicillins. Tetracyclines showcase both antibacterial and anti-inflammatory properties, acting by inhibiting polymorphonuclear leukocytes (PMNs), matrix metalloproteinases (MMPs), and collagenase. By inhibiting lipase production in Staphylococcus epidermidis, they enhance the metabolism of meibomian gland secretions, promoting a more stable tear film. However, their antimicrobial effectiveness is limited by a high resistance rate. These antibiotics are minimally absorbed from the digestive tract and should be taken on an empty stomach, as they bind to calcium-containing foods like dairy products. Side effects include accumulation in calcium reservoirs, potentially affecting bone and teeth development, gastrointestinal toxicity, photosensitivity, tinnitus, vertigo, and, rarely, idiopathic intracranial hypertension (IIH). Minocycline, in particular, demonstrates extended bioavailability, reduced recurrence rates, and neuroprotective effects implicated in various clinical conditions, including cerebral ischemia, traumatic brain injury, and degenerative brain diseases. Moreover, minocycline has shown promise in delaying retinal ganglion cell apoptosis in animal models of transected optic nerves and induced glaucoma.

 

In addition to treatment of bacterial conditions, oral pharmaceuticals can be effectively used in the management of viral ocular diseases. The diagnostic criteria for herpes simplex virus (HSV) keratitis involve a thorough ophthalmic examination, including slit-lamp microscopy, corneal staining, and polymerase chain reaction (PCR) testing for viral DNA. Clinical manifestations often include dendritic corneal ulcers, characteristic lesions on the corneal surface. Treatment typically involves oral antiviral medications like acyclovir, valacyclovir, or famciclovir, alongside topical antiviral eye drops such as trifluridine or ganciclovir. In herpes zoster ophthalmicus, a clinical diagnosis is made based on the presence of characteristic skin lesions and ocular involvement. Ophthalmic evaluation is crucial, including assessment for corneal involvement, uveitis, and retinitis. Oral antiviral drugs are commonly prescribed, and topical corticosteroids may be considered to manage inflammation. Prompt diagnosis and appropriate antiviral therapy are essential in both HSV keratitis and herpes zoster ophthalmicus to mitigate complications and optimize visual outcomes.

Oral antiviral drugs, including acyclovir, valacyclovir, and famciclovir, are essential components in the treatment of viral infections, particularly those caused by herpes simplex virus (HSV) and herpes zoster. These medications belong to the class of nucleoside analogs, inhibiting viral DNA synthesis by targeting the viral thymidine kinase enzyme. Acyclovir, the prototype drug, undergoes phosphorylation to its active form in infected cells. Valacyclovir, a prodrug of acyclovir, undergoes a similar activation process, while famciclovir is converted to its active form through sequential metabolic steps. These oral antivirals are widely used to manage conditions such as genital herpes, herpes labialis, HSV keratitis, and herpes zoster. They play a crucial role in suppressing viral replication, reducing the severity and duration of symptoms, and preventing recurrent outbreaks. The choice of medication and dosage depends on the specific clinical presentation and the patient's overall health.

Ocular allergies, notably allergic conjunctivitis, present a common and bothersome condition affecting the eyes. Diagnosing allergic conjunctivitis involves a thorough clinical examination, including patient history, symptom assessment, and ocular findings. Typically, individuals with allergic conjunctivitis experience itching, redness, tearing, and swelling of the eyes. In diagnosing this condition, practitioners may utilize skin testing or blood tests to identify specific allergens triggering the allergic response. Treatment often involves a multi-faceted approach, with oral pharmaceuticals playing a crucial role. Antihistamines, such as cetirizine or loratadine, can be administered orally to alleviate systemic allergy symptoms, including ocular discomfort. Additionally, mast cell stabilizers, corticosteroids, or combination medications may be prescribed based on the severity and chronicity of symptoms. Optometrists may consider incorporating oral pharmaceuticals to address ocular allergies to ensure hollistic management of this condition, providing relief and improved overall quality of life.

The use of oral pharmaceuticals in practice may be considered daunting to many eye care practitioners due to the wide scope of drug classes available. However, thorough understanding of oral drugs allows practitioners to create a comprehensive management plan for patients, opening up new avenues for consideration. Oral medications, with their systemic reach, offer a deeper and more expansive coverage for specific ocular conditions, presenting a valuable complement to traditional topical treatments. This enhanced therapeutic approach not only accelerates the alleviation of patient symptoms but also contributes to a more efficient and holistic management of ocular diseases. Antibiotics, antivirals, and allergy medications are just some examples of oral pharmaceuticals that can be utilized in eye care settings, each drug class presenting options for each unique patient scenario. Optometrists should understand the full arsenal of oral medications at their disposal in order to combat ocular diseases and elevate patient care.

If you are interested in hearing more about this important topic, register for our upcoming two part series, “Oral Pharmaceuticals” and receive up to 4 hours of free CE.

Click here to register for day 1 of the course with Dr. James Fanelli and Dr. Jim Thimons

Click here to register for day 2 of the course with Dr. Blair Lonsberry and Dr. Nathan Lighthizer









Written by Dr. Hannah Alegado, O.D.

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