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Agonist and Antagonists

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Review of Agonists and Antagonists
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AGONISTS VS ANTAGONISTS Alexia Clark – Billi Osman – Katey Gifford – Jackie Perez- Hicks
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  • 1. AGONISTS VSANTAGONISTSAlexia Clark Billi Osman Katey Gifford Jackie Perez-Hicks

2. AGONISTSMOLECULES WHICH BIND TO RECEPTORS ON CELLSTHINK OF LOCK AND KEY; ONLY CERTAIN KEYS WILLWORK IN CERTAIN LOCKSHORMONES, NEUROTRANSMITTERS, ANDENDOGENOUS REGULATORS OF THE BODYHORMONE: ESTROGENNEUROTRANSMITTER: HISTAMINEENDOGENOUS REGULATOR: SERATONINDRUGS WHICH ACT LIKE REGULATORY MOLECULESOF THE BODY 3. AGONIST FACTSREACTIONS MAY NOT PROCEED FASTER DUE TO AN AGONIST BINDINGJUST BECAUSE THE KEY IS IN THE LOCK DOES NOT MEAN THE DOOR WILL OPENANY FASTERSOME AGONIST ACTION MAY ACTUALLY RESULT IN A SLOWER BODYFUNCTIONA KEY MAY UNLOCK THE DOOR AND YOU WILL MOVE IN SLOW MOTION 4. BASELINELOW BASELINE ACTIVITY MAY BE POSSIBLE IN ANY SYSTEM WITHOUT ANAGONIST TO REPRESENT THE RECEPTOR/EFFECTOR; BRIEF ACTIVATION ISPOSSIBLETHERE IS NOT ALWAYS A NEED FOR A KEY TO UNLOCKSOME DOORS; THEY CAN OPEN WITHOUTA KEYTHESE DOORS DONT STAY OPEN VERYLONG, BUT THEY ARE SUFFICIENT ENOUGHTO ALLOW OTHERS TO ENTER AND EXIT(Maybaum 2014) 5. HIGH EFFICACY AGONISTSLOW CONCENTRATIONS OF A FULL AGONIST MEANSTHAT ONLY SOME AVAILABLE RECEPTORS WILLACTUALLY BE OCCUPIED AT ANY GIVEN TIMEWHEN THERE ARE A LOT OF DOORS AND NOT ENOUGHKEYS AVAILABLE, NOT ALL DOORS WILL BE OPENEDTHE EFFECTOR SYSTEM IS ACTIVATED BY EACH EVENTOF BINDING COMPLETED BY THE AGONIST HIGHEFFICACYKEYS REALLY LIKE DOOR LOCKS; THEY WILL ENTER ALOCK AS OFTEN AS POSSIBLE; A KEY UNLOCKING ADOOR SIMPLY MEANS THAT THIS DOOR CAN BEOPENED(Maybaum 2014) 6. HIGH EFFICACY/CONCENTRATIONALMOST ALL RECEPTORS MAY BEOCCUPIED WHEN A FULL AGONIST ISPRESENT AT A HIGH CONCENTRATIONWHEN A DOOR LOCK HAS A KEY IN ITALREADY, YOU CANNOT ADD ANOTHERKEY; THIS LEAVES MANY UNUSED KEYS(Maybaum 2014) 7. LOW AFFINITY AGONISTSEVEN IN HIGH CONCENTRATIONS, A LOWAFFINITY AGONIST WILL NOT BE ABLE TO BINDAS EFFICIENTLY TO THE RECEPTOR SYSTEMSOME KEYS ARE JUST NOT AS GOOD ASOTHERS, AND YOU CAN HAVE A LOT OFKEYS THAT DONT FIT THE LOCKS; LESSDOORS ARE UNLOCKED WHEN WE HAVE THEWRONG KEYTHE LOW AFFINITY AGONIST WILL COME OFFOF THE BINDING SITE MUCH FASTER THAN THEHIGH AFFINITY AGONISTWHEN A BAD KEY IS BEING USED, IT WILL BEEASIER NOT TO USE THAT KEY, BUT RATHER AGOOD KEY, RESULTING IN AN OPEN DOOR(Maybaum 2014) 8. ANTAGONISTS INHIBITORS OF REGULATORY DRUGS AND MOLECULES; THEY PRODUCE THEIR OWNEFFECTS BY BLOCKING RECEPTORSCHILD SAFETY LOCKS ON THE DOORS; THEY WILL NOT ALLOW THE KEY TO ENTER THELOCKRECEPTOR FUNCTION IS LIMITED DUE TO AN AFFINITY, BUT THERE IS LITTLE TO NOINTRINSIC ACTIVITY WITHIN THE CELLTHESE CHILD SAFETY LOCKS LIKE TO ATTACH THEMSELVES AND DO NOT ASSIST THE KEYNOT ALL ANTAGONIST ACTIVITY IS BAD; AN AGONIST MAY BE UNABLE TO FULLY BINDAND GENERATE A RESPONSE, ALLOWING THE ANTAGONIST TO ELIMINATE HARM TOTHE PATIENTSOME DOORS ARE BETTER OFF CLOSED; IF LEFT OPENED, THERE MAY BE UNWANTEDENTRY OR EXIT 9. HIGH AFFINITY ANTAGONISTSEFFECTORS ARE NOT ACTIVATEDALTHOUGH THE ANTAGONIST BINDS WITHTHE HIGH AFFINITY RECEPTORCHILD SAFETY LOCKS ARE REALLYEFFECTIVE AT KEEPING KEYS FROMENTERING A LOCK; SOME UNLOCKEDDOORS MAY NOT EVEN OPEN WHEN ACHILD SAFETY LOCK IS IN PLACE(Maybaum 2014) 10. COMPETING AGONISTS &ANTAGONISTSTHE AGONIST CANNOT FULLY BIND TOTHE RECEPTOR AS IT IS BEING BLOCKEDBY THE ANTAGONISTSOME CHILD SAFETY LOCKS ARE WEAKAND KEYS CAN STILL GET TO THE LOCK;NOT ALL KEYS WILL BE EFFICIENTENOUGH TO REACH THE DOOR LOCK(Maybaum 2014) 11. COMPETING HIGH AGONISTS & ANTAGONISTSTHE ANTAGONIST IS PRESENT HOWEVER THEAGONIST IS IN HIGH ENOUGHCONCENTRATION THAT IT CAN COMPETEFOR BINDING SITESCHILD SAFETY LOCKS AND KEYS WILLCOMPETE WITH ONE ANOTHER TO SEE WHOGETS TO THE DOOR FIRST; SOMETIMES THEKEYS WIN; MORE KEYS = MORE UNLOCKEDDOORS 12. VALUE IN NURSING The value of combination therapy with inhaled corticosteroids and long-actingb-agonists (ICS/LABA) is well recognized in the management ofasthma and chronic obstructive pulmonary disease (COPD). (Maple & Roberts,2014) BETA AGONISTS KEY BETA ANDRENERGIC RECEPTORS IN THE SMOOTH MUSCLE OF THE LUNGS DOOR LOCK THE USE OF THE KEY IN THE DOOR LOCK RESULTS IN RELAXATION OF THE SMOOTH MUSCLE INTHE LUNGS WHICH LEADS TO BRONCHODILATION 13. VALUES IN NURSING BETA AGONISTS HAVE A AN AFFINITY FOR BETA 1 RECEPTORS WHICH MAY ALSOEFFECT MUSCLES IN THE HEART AND SKELETAL MUSCLE COMMON SIDE EFFECTS INCLUDE: FAST HEART BEAT (TACHYCARDIA) HEART FLUTTERING FEELING IN THE CHEST (PALPITATIONS) HEART SHAKINESS AND CRAMPING OF EXTREMITIES SKELETAL ANXIETY AND NERVOUSNESS COMBINATION APPLICATION IN NURSING ASSESS IF BENEFITS OF DRUG USE ARE GREATER THAN SIDE EFFECTS TEACH PATIENT PROPER TECHNIQUE OF ADMINISTRATION I.E. SPACERS TEACH PATIENT TO UNDERSTAND HOW OFTEN MEDICATION SHOULD BE TAKEN TEACH PATIENT WHAT ALLERGIC REACTIONS TO WATCH FOR 14. REFERENCESAmerican Thoracic Society. (2014). What are beta agonists? Retrieved fromhttp://www.thoracic.org/clinical/copd-guidelines/for-patients/what-kind-of-medications-are-there-for-copd/what-are-beta-agonists.phpLehne, R. (2012). Pharmacodynamics. Pharmacology for nursing care (8th ed., pp. 51-58). St. Louis,Mo.: Saunders Elsevier.Mapel, D., & Roberts, M. (2014). Management of asthma and chronic obstructive pulmonary diseasewith combination inhaled corticosteroids and long-acting -agonists: A review ofcomparative effectiveness research drugs, 74(7), 737-755. doi:10.1007/s40265-014-0214-8Maybaum, J. (n.d.). Pharmacology Principles / Dental IMS-II. Retrieved August 26, 2014, fromhttp://sitemaker.umich.edu/maybaum.pharmacology.principles/noncompetitive_antagonist


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