Observations on Some Properties of a Long-Acting Preparation of Propranolol

1979 ◽  
Vol 57 (s5) ◽  
pp. 409s-411s ◽  
Author(s):  
R. G. Shanks ◽  
J. D. Neill ◽  
W. J. Leahey ◽  
M. P. S. Varma
Keyword(s):  
Healthy Subjects ◽  
Slow Release ◽  
Peak Effect ◽  
Exercise Tachycardia ◽  
Repeated Dosing ◽  
Long Acting

1. The effects of 160 mg of propranolol and 160 mg of a long-acting (LA) formulation of propranolol were studied in healthy subjects. 2. Both drugs reduced an exercise tachycardia but the peak was less and the 24 h effect greater after long-acting propranolol than after propranolol. 3. These differences were maintained on repeated dosing for 8 days. 4. In contrast to single doses of 400 mg of sotalol, 160 mg of oxprenolol and 160 mg of slow-release oxprenolol, the peak effect of long-acting propranolol was less and that at 24 h was greater.

scholarly journals Opicapone: a short lived and very long acting novel catechol-O-methyltransferase inhibitor following multiple dose administration in healthy subjects

2013 ◽  
Vol 76 (5) ◽  
pp. 763-775 ◽  
Author(s):  
José Francisco Rocha ◽  
Luis Almeida ◽  
Amílcar Falcão ◽  
P. Nuno Palma ◽  
Ana I. Loureiro ◽  
...  
Keyword(s):  
Healthy Subjects ◽  
Multiple Dose ◽  
Dose Administration ◽  
Multiple Dose Administration ◽  
Long Acting

Population pharmacokinetics of the rilpivirine long-acting formulation after intramuscular dosing in healthy subjects and people living with HIV

2021 ◽  
Author(s):  
M Neyens ◽  
H M Crauwels ◽  
J J Perez-Ruixo ◽  
S Rossenu
Keyword(s):  
Population Pharmacokinetics ◽  
Healthy Subjects ◽  
Phase Iii ◽  
Intramuscular Administration ◽  
Population Pharmacokinetic ◽  
People Living With Hiv ◽  
Concentration Data ◽  
Flip Flop ◽  
Long Acting ◽  
Living With Hiv

Abstract Objectives To characterize the population pharmacokinetics of the rilpivirine long-acting (LA) formulation after intramuscular administration. Methods Rich and sparse rilpivirine plasma concentration data were obtained from seven clinical studies. In total, 18 261 rilpivirine samples were collected from 986 subjects (131 healthy subjects from Phase I studies and 855 people living with HIV from Phase IIb/III studies). Doses ranged from 300 to 1200 mg, as single-dose or multiple-dose regimens (every 4 or 8 weeks). In Phase III studies, an initiation injection of 900 mg followed by continuation injections of 600 mg every 4 weeks was used. Non-linear mixed-effects modelling was performed using NONMEM® software. Results A one-compartment model with linear elimination and two parallel absorption pathways (fast and slow) with sequential zero-first-order processes adequately captured rilpivirine flip-flop pharmacokinetics after intramuscular administration of the LA formulation. The estimated apparent elimination half-life of rilpivirine LA was 200 days. None of the evaluated covariates (age, body weight, BMI, sex, race, health status and needle length) had a clinically relevant impact on rilpivirine pharmacokinetics. Conclusions The population pharmacokinetic model suitably describes the time course and associated variability of rilpivirine plasma concentrations after rilpivirine LA intramuscular administration. The monthly regimen consists of an oral lead-in period (rilpivirine 25 mg tablets once daily for 4 weeks), followed by an initiation injection of 900 mg rilpivirine LA, then 600 mg rilpivirine LA continuation injections monthly. The absence of a clinically relevant effect of covariates on rilpivirine pharmacokinetics suggests that rilpivirine LA dose adjustments for specific subgroups are not warranted.

Aclidinium Bromide, a Long-Acting Antimuscarinic, Does Not Affect QT Interval in Healthy Subjects

2011 ◽  
Vol 51 (6) ◽  
pp. 923-932 ◽  
Author(s):  
Kenneth C. Lasseter ◽  
Jordi Aubets ◽  
Ferran Chuecos ◽  
Esther Garcia Gil
Keyword(s):  
Qt Interval ◽  
Healthy Subjects ◽  
Aclidinium Bromide ◽  
Long Acting

scholarly journals Electrocardiographic Safety of Repeated Monthly Dihydroartemisinin-Piperaquine as a Candidate for Mass Drug Administration

2018 ◽  
Vol 62 (12) ◽  
Author(s):  
Pere Millat-Martínez ◽  
Rhoda Ila ◽  
Moses Laman ◽  
Leanne Robinson ◽  
Harin Karunajeewa ◽  
...  
Keyword(s):  
Drug Administration ◽  
Mass Drug Administration ◽  
Malaria Elimination ◽  
Safety Data ◽  
Repeated Administration ◽  
Risk Difference ◽  
Safety Endpoint ◽  
The Difference ◽  
Repeated Dosing ◽  
Long Acting

ABSTRACT Mass drug administration (MDA) of sequential rounds of antimalarial drugs is being considered for use as a tool for malaria elimination. As an effective and long-acting antimalarial, dihydroartemisinin-piperaquine (DHA-PQP) appears to be suitable as a candidate for MDA. However, the absence of cardiac safety data following repeated administration hinders its use in the extended schedules proposed for MDA. We conducted an interventional study in Lihir Island, Papua New Guinea, using healthy individuals age 3 to 60 years who received a standard 3-day course of DHA-PQP on 3 consecutive months. Twelve-lead electrocardiography (ECG) readings were conducted predose and 4 h after the final dose of each month. The primary safety endpoint was QT interval correction (QTc using Fridericia’s correction [QTcF]) prolongation from baseline to 4 h postdosing. We compared the difference in prolongations between the third course postdose and the first course postdose. Of 84 enrolled participants, 69 (82%) participants completed all treatment courses and ECG measurements. The average increase in QTcF was 19.6 ms (standard deviation [SD], 17.8 ms) and 17.1 ms (SD, 17.1 ms) for the first-course and third-course postdosing ECGs risk difference, −2.4 (95% confidence interval [95% CI], −6.9 to 2.1; P = 0.285), respectively. We recorded a QTcF prolongation of >60 ms from baseline in 3 (4.3%) and 2 (2.9%) participants after the first course and third course (P = 1.00), respectively. No participants had QTcF intervals of >500 ms at any time point. Three consecutive monthly courses of DHA-PQP were as safe as a single course. The absence of cumulative cardiotoxicity with repeated dosing supports the use of monthly DHA-PQP as part of malaria elimination strategies.

Long-acting antibacterial agents

1970 ◽  
Vol 8 (26) ◽  
pp. 101-103
Keyword(s):  
Plasma Proteins ◽  
Antibacterial Agents ◽  
Renal Excretion ◽  
Slow Release ◽  
Blood Levels ◽  
Prolonged Action ◽  
Procaine Penicillin ◽  
High Doses ◽  
Long Acting ◽  
Release Form

A number of antibacterial agents have recently been developed which are recommended because they need to be administered infrequently. Examples are Deteclo (Lederle), Kelfizine W (Pharmitalia), and Vibramycin (Pfizer). The advantage claimed for these preparations is that adequate blood levels can be maintained with infrequent dosage. A prolonged action may be achieved in various ways - for example, by using a mixture of antibiotics which are absorbed and excreted at different rates, as in Deteclo;1 by giving high doses of a well absorbed preparation which is slowly excreted, e. g. doxycycline (Vibramycin),2 by administration in a slow-release form, e. g. procaine penicillin; or by giving probenecid to lessen renal excretion. Where prolongation of action depends on increased binding to plasma proteins, the drug may be more likely to act as a hapten and so to induce allergic reactions.

scholarly journals Long-acting Insulin: Slow Release of Insulin from a Biodegradable Matrix Implanted in Diabetic Rats

Diabetes ◽  
1983 ◽  
Vol 32 (5) ◽  
pp. 478-481 ◽  
Author(s):  
M. F. A. Goosen ◽  
Y. F. Leung ◽  
G. M. O'Shea ◽  
S. Chou ◽  
A. M. Sun
Keyword(s):  
Slow Release ◽  
Diabetic Rats ◽  
Acting Insulin ◽  
Long Acting

The effect of a new slow-release, long-acting somatostatin analogue, lanreotide, in acromegaly

1996 ◽  
Vol 45 (4) ◽  
pp. 415-421 ◽  
Author(s):  
M. Al-Maskari ◽  
Jan Gebbie ◽  
P. Kendall-Taylor
Keyword(s):  
Slow Release ◽  
Somatostatin Analogue ◽  
Long Acting

scholarly journals Trace Element Supplementation of Livestock in New Zealand: Meeting the Challenges of Free-Range Grazing Systems

2012 ◽  
Vol 2012 ◽  
pp. 1-8 ◽  
Author(s):  
Neville D. Grace ◽  
Scott O. Knowles
Keyword(s):  
New Zealand ◽  
Trace Element ◽  
Mineral Nutrition ◽  
Slow Release ◽  
Dairy Farms ◽  
Free Range ◽  
Grazing Systems ◽  
Long Acting ◽  
Grazing Livestock ◽  
Cobalt Copper

Managing the mineral nutrition of free-range grazing livestock can be challenging. On farms where grazing animals are infrequently yarded, there are limited opportunities to administer trace element supplements via feeds and concentrates. In New Zealand, where the majority of sheep, cattle, and deer graze pasture year round, inadequate intake of cobalt, copper, iodine and selenium is prevalent. Scientists and farmers have developed efficient strategies to monitor and treat these dietary deficiencies. Supplementation methods suited to grazing livestock include long-acting injections, slow-release intraruminal boluses, trace element-amended fertilisers, and reticulated water supplies on dairy farms.

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