Pharmacokinetic-Pharmacodynamic Correlations of Corticosteroids
Hartmut Derendorf, Günther Hochhaus in Handbook of Pharmacokinetic/Pharmacodynamic Correlation, 2019
Saliva levels measured for drug monitoring reflect only the free and not the total HC plasma concentration.35 The HC/cortisone ratio in plasma is about 6:1.30,38 During the absorption phase of oral cortisone, this ratio is larger (10:1) as a result of an intensive first-pass metabolism to HC in the liver. The water-soluble hemisuccinate ester (HCHS), a prodrug for IV administration, is efficiently bioactivated to HC.32 Cortisone acetate (CA) is used for intramuscular and oral treatment. Orally given CA is immediately absorbed and quantitatively transformed into HC with a Cmax reached after approximately 1.7 h.30 However, there has been controversy concerning the efficacy of intramuscularly administered CA. The increased bioavailability of oral vs. i.m. administration is attributed to a better conversion to HC as a result of an intensive first-pass metabolism.39,40 Besides its intra-articular and epidural application in sustained release preparations,27,41 hydrocortisone acetate (HCA) is also used in local therapy of bowel diseases such as ulcerative colitis and Crohn’s disease.42 Rectal administration in the form of enemas or foams is clinically most effective. However, the information about systemic absorption is very inconsistent, since bioavailability values of 2 to 30% have been reported.31,42–44
Drug Delivery and Bioavailability in Short Bowel Syndrome
John K. DiBaise, Carol Rees Parrish, Jon S. Thompson in Short Bowel Syndrome Practical Approach to Management, 2017
Rectal administration of drugs can be a very practical and effective alternate route for drug administration in patients who have severe nausea and vomiting or who experience swallowing difficulties. The benefits of rectal route drug administration include easy application, requiring minimal educational efforts to the family and patient, and less expensive compared with the parenteral route. Additionally, patients can generally readily self-administer drugs using the rectal route without the assistance of others. Physical limitations associated with an infusion pump or other infusion devices are also avoided [25].
Management of breakthrough pain
Nigel Sykes, Michael I Bennett, Chun-Su Yuan in Clinical Pain Management, 2008
Transmucosal formulations comprise a variety of delivery systems that present the drug to the oral, nasal, bronchial, or rectal mucosa. Rectal administration has been used for many years and a number of short-acting opioids are commercially available in rectal formulations. These drugs may be useful when patients are temporarily unable to tolerate oral medication, or the parenteral route becomes compromised by a bleeding disorder or generalized edema. The use of rectal drugs for breakthrough pain is compromised by dose-to-dose variability in absorption and effects, and limited patient acceptance for long-term use.
Advances in rectal drug delivery systems
Published in Pharmaceutical Development and Technology, 2018
Trusha J. Purohit, Sara M. Hanning, Zimei Wu
Any solution, emulsion or suspension for rectal administration is referred to as an enema, or micro-enema if administration volume is small such as 5–10 ml. These formulations contain either oil, glycerin or low molecular weight macrogol as vehicle (van Hoogdalem et al. 1991). Administration volume may vary from 2.5 ml up to few hundred milliliters and applicators can be used to assist administration such as the Macy Catheter®, a recently FDA-approved medical device for rectal administration of fluids (Lam et al. 2016). Enemas are used for rectal stimulation to initiate defecation before operative procedures (Pittet et al. 2015) and for localized treatments of inflammatory bowel disease or ulcerative colitis (Spencer and McTavish 1995; Matuszyk et al. 2016) or as a medium to deliver contrast agent before radiographic examination. Despite micro-enemas being more advantageous than large volume enemas, the packaging and transportation costs make them a less favorable formulation than large volume enemas (Aulton and Taylor 2013).
Opportunities for enteral drug delivery for neonates, infants, and toddlers: a critical exploration
Published in Expert Opinion on Drug Delivery, 2022
Nicole Sheena Kaneria, Catherine Tuleu, Terry Ernest
Solid dosage forms are intuitively easier to administer than liquids and in terms of its retention within the rectum, hence why suppositories may be more prevalent [49]. Generally, opinion for their use has been regarded as relatively unsafe in pre-term neonates due to unpredictable absorption and also as mucosal damage may occur, consequently causing infection [11,49]. In fact, the suppositories and rectal capsule listed in Table 5 are licensed from infant age. However, in recent years, studies for rectal administration in this age group have increased and thus also the evidence for their safe use and possible superiority to other dosage form types (mentioned later). There are several recent papers detailing in vivo safety and efficacy studies in neonates of rectal formulations with various APIs for different conditions [127–130]. This said, exposure of the API via the rectal route can be variable due to inter-patient and intra-patient absorption variability within the rectum, especially between the different developmental age groups. This is illustrated in several studies [131–133].
Evaluation of the Macy Catheter®: a rectal catheter for rapid medication and fluid administration
Published in Expert Review of Medical Devices, 2018
Kim Marie C. Macygin, Erik Kulstad, Robert K. Mokszycki, Morgan Goldsmith
A variety of patients can reap the benefits of the Macy Catheter, including both the elderly and pediatric populations. In the United States, the FDA clearance does not state specific age, size, or weight for use. Clinical judgment should dictate appropriate placement. The catheter is 14fr, not much larger than a rectal thermometer. Roberts and Hedges’ Clinical Procedures in Emergency Medicine and Acute Care states: ‘IV access in small children may be very difficult to obtain and frightening to the child. In these situations, the option of rectal administration may outweigh the benefits of IV drug therapy. Patients who refuse parenteral drug administration may also benefit from rectal delivery, as well as those with nausea and vomiting or the inability to swallow’ [32]. This definitive textbook of emergency procedures specifically highlights the use of the Macy Catheter for rectal access.
Related Knowledge Centers
- Absorption
- First Pass Effect
- Nausea
- Circulatory System
- Blood Vessel
- Rectum
- Route of Administration
- Medication
- Bioavailability
- Oral Administration