Pharmacology in ENT
Rogan J Corbridge in Essential ENT, 2011
The accessibility of the anatomical areas involved with disease often allows topical agents to be used more than is usual in most other specialties. A large number of different organisms are involved in infections of the ear. Streptococcus pneumoniae and Haemophilus influenzae are often the cause of otitis media and are implicated in infections of the external ear and otitis externa. Pseudomonas and Gram-negative rods are often found in otitis externa. There are many drug preparations used in the treatment of ENT disorders. Broad-spectrum penicillin such as amoxicillin, especially when combined with clavulanic acid, is often the drug of choice. Most topical drugs used in the nose aim to improve nasal airflow and often relieve rhinorrhoea. Long-term use of these drugs can cause rhinitis medicamentosa; therefore their application should be limited to short courses of 7–10 days. The mainstay of the treatment of rhinitis is topical steroid therapy.
Ear, nose and throat
Gina Johnson, Ian Hill-Smith, Chirag Bakhai in The Minor Illness Manual, 2018
Antibiotics are generally of marginal benefit in sore throat and may only shorten the illness by 16 hours. Most sore throats are viral. Symptoms resolve within 3 days in 40% of people and within 7 days in 85%, irrespective of whether the sore throat is viral or due to a streptococcal infection. Clinical scores and point-of-care tests have been developed with the aim of identifying those patients more likely to benefit from antibiotics. Harmless, commensal streptococci are present in the throats of 12%–40% of healthy people. Oral corticosteroids may be prescribed if the pain is very severe but carry significant risks of sepsis and venous thromboembolism. For children who are unable to swallow tablets, amoxicillin suspension may be used instead. It tastes much better than phenoxymethylpenicillin suspension, and concordance is likely to be better because it is given three times daily.
Febrile seizures
Samar Razaq in Difficult Cases in Primary Care, 2021
You see 15-month-old John in clinic with a 24-hour history of fever, runny nose and tugging at the right ear. On examination, the child appears well and is afebrile. You note that the right tympanic membrane is bulging, with an inflamed appearance. You make a diagnosis of otitis media and send mum home with a prescription of amoxicillin. Two days later mum, who is an orthopaedic nurse, returns with discharge papers from the paediatric ward. Later at night after you saw him, John developed a very high temperature of 39°C. As he lay in his cot, he suddenly started jerking. Mum says he appeared to go very stiff and he became unresponsive, with his eyes rolled upwards. Thinking that he was dying, mum dialled for the ambulance. By the time the ambulance crew arrived, the jerking had settled. John, however, remained semi-conscious and it was not until an hour later in the emergency department that he was completely back to normal. The paediatric discharge notes inform you that a lumbar puncture was performed. It, along with blood results, was normal. The final diagnosis was that of a simple febrile seizure (FS). Mum would like John to be referred for an electroencephalogram (EEG). She also enquires about prophylactic diazepam to stop seizures from occurring in the future.
In vivo–in vitro correlation for amoxicillin trihydrate 1000 mg dispersible tablet
Published in Drug Development and Industrial Pharmacy, 2009
Michał Ostrowski, Ewa Wilkowska, Tomasz Bączek
Objectives: An in vivo–in vitro correlation (IVIVC) for amoxicillin dispersible tablet was established. Methods: The model of absorption was constructed with type 2 dissolution apparatus and with the use of variable hydrodynamic conditions simulating passage through upper part of gastrointestinal tract. The in vivo test was performed on 24 volunteers. Summary of results: The predicted errors for AUC and Cmax were calculated. Conditions of the in vitro test were discriminative to capsules, which were claimed to have lower bioavailability. The zero-order process of amoxicillin absorption enabled to establish the IVIVC more easily. Overall conclusions: The described model showed features of level A correlation for immediate release dosage form and the zero-order process of amoxicillin absorption is an advantage for establishing IVIVC.
Concentration of amoxicillin in maternal serum, cord blood, amniotic fluid and the placenta after vaginal administration
Published in The Journal of Maternal-Fetal & Neonatal Medicine, 2015
Julia Zaręba-Szczudlik, Ewa Romejko-Wolniewicz, Zbigniew Lewandowski, Hanna Różańska, Krzysztof Czajkowski
Objective: The aim of this study was to assess the amoxicillin concentration in maternal serum, cord blood, amniotic fluid and the placenta, 2 h following vaginal administration and the factors influencing the drug level. Methods: Twenty-eight full-term pregnant women who qualified for elective cesarean delivery were included in the study. Vaginal suppositories containing 250 mg of amoxicillin were administered 2 h prior to the operation. Amoxicillin levels were determined using the diffusion microbial assay. Results: The amoxicillin level in amniotic fluid was significantly higher in comparison to that of maternal serum, cord blood or the placenta. Maternal age positively and gestational weight gain negatively correlated with the amoxicillin concentration in maternal serum. The maternal serum hemoglobin level and red blood cell count were positively correlated with amoxicillin concentration in the amniotic fluid. Neonatal birth weight was positively correlated with maternal serum and cord blood amoxicillin levels. Hypertensive women had significantly higher amoxicillin concentrations in amniotic fluid, and women with thrombocytopenia presented significantly higher cord blood amoxicillin concentrations. Conclusions: Amoxicillin presented poor concentration in maternal–fetal compartments after vaginal administration, but the factors influencing the drug level in different compartments require further investigation.
Floating modular drug delivery systems with buoyancy independent of release mechanisms to sustain amoxicillin and clarithromycin intra-gastric concentrations
Published in Drug Development and Industrial Pharmacy, 2016
Alessandra Rossi, Chiara Conti, Gaia Colombo, Luca Castrati, Carmelo Scarpignato, Pedro Barata, Giuseppina Sandri, Carla Caramella, Ruggero Bettini, Francesca Buttini, Paolo Colombo
Release modules of amoxicillin and clarithromycin combined in a single dosage form designed to float in the gastric content and to sustain the intra-gastric concentrations of these two antibiotics used for the eradication of Helicobacter pylori have been studied. The modules having a disc shape with curved bases were formulated as hydrophilic matrices. Two modules of clarithromycin were assembled by sticking the concave base of one module to the concave base of the other, creating an internal void chamber. The final dosage form was a floating assembly of three modules of clarithromycin and two of amoxicillin in which the drug release mechanism did not interfere with the floatation mechanism. The assembled system showed immediate in vitro floatation at pH 1.2, lasting 5 h. The in vitro antibiotics release profiles from individual modules and assembled systems exhibited linear release rate during buoyancy for at least 8 h. The predicted antibiotic concentrations in the stomach maintained for long time levels significantly higher than the respective minimum inhibitory concentrations (MIC). In addition, an in vivo absorption study performed on beagle dogs confirmed the slow release of clarithromycin and amoxicillin from the assembled system during the assembly’s permanence in the stomach for at least 4 h.
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