University:
University of Wolverhampton
Course:
4PY019 | Pharmacy
Academic year:

2024
Views:

387

Pages:

3
Author:

Sara

1. what is an anaipratropium logue of the muscarinic antagonist, atropine? 2. where is ipratropi- the brain & causes hallucinogenic effects um able to enter & what does it cause? 3. what does the hinders the penetration of blood brain barrier quaternary nitrogen of ipratropium impede? 4. inhaled ipratropi- a low degree of systemic absorption um medication is associated with... 5. tiotropium has a high potency but a low dissociation rate from the receptor 6. tiotropium-functional group epoxide, which is a 3 membered ring with oxygen. 7. why is epoxide because is very strained and usually really reactive. rarely seen in drug molecules? 8. Nucleophile An electron pair donor e.g DNA,water,amino acid 9. nucleto open epoxide the nucleophile it would have to attack ophile-tiotropium from inside the cage 10. What does steric hindrance of the rings and other groups=not enough hindrance mean? space for nucleophile to access area 11. Theophylline a Methylxanthine 12. 1/3 What is theophylline? a bronchodilator and its given orally since its not feasible to administer by inhalation 13. How can theoorally phylline be administered? 14. what can theoaminophylline-often the methylxanthine prescribed phylline be formulated to? 15. 3 potential mecha- inhibition of intracellular enzyme phosphodinisms of action for esterase(PDE) methylxanthines? Competitive antagonism at adenosine (a1 + a2) receptors Activation of histone deacetylase 16. inhibition of inraises intracellular levels of cAMP. usually PDE inactitracellular envates cAMP by converting it to 5'-AMP. If PDE is inhibited, zyme phosphodi- the intracellular levels of cAMP ^ = bronchodilation esterase(PDE) 17. Competitive antagonism at adenosine (a1 + a2) receptors adenosine acts as a bronchoconstrictor and ^ histamine release from lung mast cells. antagonism of endogenous adenosine may contribute to anti-inflammatory actions of theophylline. however the PDE inhibitor, enprofylline is a potent bronchodilator but not adenosine antagonist 18. Activation of histone deacetylase enzyme that inhibits acetylation of core histones needed for the transcription of inflammatory genes 19. unwanted effects of methylxanthines produces weak diuretic effect since ^^ renal blood flow = ^^glomerular filtration rate interfere with sleep patterns ^^ nervousness 2/3 cause tremors they vasodilate other vessels when vasoconstricting cerebral blood vessels and stimulating heart GI upsets 20. additional effects CNS stimulants + cause increase alertness of methylxanthines vasoconstrict cerebral blood vessels and stimulating heart 21. therapeutic innarrow dex of methylxanthines therapuetic plasma conc=30-100umol/l while adverse effects occur >110umol/l 22. what happens at serious CNS + cardiovascular effects e.g cardiac dysa plasma conc of rhythmia(IV admin of aminophylline) and seizures (fatal >200umol/l of a in patients with impaired respiration) methylxanthines? 3/3