ABSTRACT
The aim of the study was to get insight into the rationale of scored tablets. This was pursued by studying patient's reasons for subdividing ("breaking") scored and unscored tablets. Patients who picked up their prescriptions in 5 community pharmacies in The Netherlands were questioned. Two-hundred and seventy-five prescriptions were studied. Of all dispensed tablets, 31% were subdivided, mostly because a dose that needed subdivision was prescribed. However, 30% were subdivided upon the initiative of the patient himself: 13% for ease of swallowing and 17% because the patient chose to take a lower dose. Even unscored tablets were subdivided: because the dose prescribed was half the tablet dose (6%), for ease of swallowing (1%) and the wish of the patient to take a lower dose (3%). It was also inquired about the patient's perception of the ease of subdivision of scored tablets. Problematic subdivision of scored tablets was reported in 55% of the cases, 42% of which was attributed to a disfunctioning score line. We also studied the possibility to prescribe and dispense other medicinal products as alternatives for tablets that needed to be subdivided. For 46% a dosage form with a lower dose was on the market, for 54% it was not. We conclude that scored tablets still fulfil an important role. Even when lower dosed tablets would become available, there remains a substantial wish of patients to subdivide tablets for ease of swallowing and adapting the dose. Improving the functioning of score lines may be a more practical approach than banning this dosage form.
Subject(s)
Tablets/administration & dosage , Tablets/standards , Administration, Oral , Chemistry, Pharmaceutical , Deglutition , Dose-Response Relationship, Drug , Drug Compounding/methods , Drug Prescriptions , Humans , Netherlands , Patient Compliance , Patients , Pharmacies/statistics & numerical data , Surveys and QuestionnairesABSTRACT
OBJECTIVE: The aim of this study was to measure the experience of patients with score line tablets where breaking was necessary for dosing. METHOD: In three community pharmacies in the Netherlands, patients were asked about their experiences with the functioning of the score line. The survey was restricted to scored tablets that had to be broken to obtain the prescribed dose. It was also asked what actions were taken by the patient when breaking problems were encountered. RESULTS: Of all the score line prescriptions included in the study, 36% received a negative evaluation by the patient. The main negative experiences were related to loss of mass after breaking the tablets and difficulty in breaking, reported in 32% and 15%, respectively, of the prescriptions included in the study. In only 28% of the negative experiences had this been reported back to the pharmacy. CONCLUSION: Many patients experience an unsatisfactory performance of tablets with score lines. Improvement will need a combination of technically better score lines and the alertness of the dispensing pharmacy for breaking problems.
Subject(s)
Patient Satisfaction , Tablets/standards , Adult , Aged , Data Collection , Humans , Middle Aged , Netherlands , Pharmacies , Stress, Mechanical , Tablets/administration & dosageABSTRACT
The present study describes the synthesis and in vitro pharmacology of a novel series of dopaminergic agents in which the classical phenylethylamine pharmacophore is replaced by a thienylethylamine moiety. In general, the novel compounds showed a moderate affinity for the dopamine (DA) D(2) and D(3) receptors. When the thienylethylamine moiety is fixed in a rigid system, the affinity for the DA receptor is significantly increased. However, in the tricyclic hexahydrothianaphthoxazine structure, the affinity for the DA receptors is diminished.
Subject(s)
Dopamine Agonists/chemical synthesis , Receptors, Dopamine D2/metabolism , Thiophenes/chemical synthesis , Animals , Binding, Competitive , Biological Availability , CHO Cells , Cricetinae , Dopamine Agonists/chemistry , Dopamine Agonists/pharmacology , Humans , Magnetic Resonance Spectroscopy , Microdialysis , Radioligand Assay , Rats , Receptors, Dopamine D3 , Structure-Activity Relationship , Thiophenes/chemistry , Thiophenes/pharmacologyABSTRACT
After decades of research around dopamine agonists, we have found a promising compound in S-PD148903 that represents a new type of prodrug, which in the rat is bioactivated to the catecholamine S-5,6-diOH-DPAT, known to display mixed dopamine D(1)/D(2) receptor agonist properties just like apomorphine. This prodrug has an enone structure which by an oxidative bioactivation mechanism is converted to the corresponding catechol and is delivered enantioselectively into the CNS. This novel concept has the potential to revolutionize the treatment of Parkinson's disease by competing with L-DOPA, the current treatment of choice.
