Agonist and Antagonists

Review of Agonists and Antagonists

1. Agonists Vs Antagonists Alexia Clark – Billi Osman – Katey Gifford – Jackie Perez-Hicks

2. Agonists MOLECULES WHICH BIND TO RECEPTORS ON CELLS THINK OF LOCK AND KEY; ONLY CERTAIN KEYS WILL WORK IN CERTAIN LOCKS HORMONES, NEUROTRANSMITTERS, AND ENDOGENOUS REGULATORS OF THE BODY HORMONE : ESTROGEN NEUROTRANSMITTER : HISTAMINE ENDOGENOUS REGULATOR : SERATONIN DRUGS WHICH ACT LIKE REGULATORY MOLECULES OF THE BODY

3. Agonist facts REACTIONS MAY NOT PROCEED FASTER DUE TO AN AGONIST BINDING JUST BECAUSE THE KEY IS IN THE LOCK DOES NOT MEAN THE DOOR WILL OPEN ANY FASTER SOME AGONIST ACTION MAY ACTUALLY RESULT IN A SLOWER BODY FUNCTION A KEY MAY UNLOCK THE DOOR AND YOU WILL MOVE IN SLOW MOTION

4. BASELINE LOW BASELINE ACTIVITY MAY BE POSSIBLE IN ANY SYSTEM WITHOUT AN AGONIST TO REPRESENT THE RECEPTOR/EFFECTOR; BRIEF ACTIVATION IS POSSIBLE THERE IS NOT ALWAYS A NEED FOR A KEY TO UNLOCK SOME DOORS; THEY CAN OPEN WITHOUT A KEY THESE DOORS DON’T STAY OPEN VERY LONG, BUT THEY ARE SUFFICIENT ENOUGH TO ALLOW OTHERS TO ENTER AND EXIT ( Maybaum 2014 )

5. HIGH EFFICACY AGONISTS LOW CONCENTRATIONS OF A FULL AGONIST MEANS THAT ONLY SOME AVAILABLE RECEPTORS WILL ACTUALLY BE OCCUPIED AT ANY GIVEN TIME WHEN THERE ARE A LOT OF DOORS AND NOT ENOUGH KEYS AVAILABLE, NOT ALL DOORS WILL BE OPENED THE EFFECTOR SYSTEM IS ACTIVATED BY EACH EVENT OF BINDING COMPLETED BY THE AGONIST – “HIGH EFFICACY“ KEYS REALLY LIKE DOOR LOCKS; THEY WILL ENTER A LOCK AS OFTEN AS POSSIBLE; A KEY UNLOCKING A DOOR SIMPLY MEANS THAT THIS DOOR CAN BE OPENED ( Maybaum 2014 )

6. HIGH EFFICACY/CONCENTRATION ALMOST ALL RECEPTORS MAY BE OCCUPIED WHEN A FULL AGONIST IS PRESENT AT A HIGH CONCENTRATION WHEN A DOOR LOCK HAS A KEY IN IT ALREADY, YOU CANNOT ADD ANOTHER KEY; THIS LEAVES MANY UNUSED KEYS ( Maybaum 2014 )

7. LOW AFFINITY AGONISTS EVEN IN HIGH CONCENTRATIONS, A LOW AFFINITY AGONIST WILL NOT BE ABLE TO BIND AS EFFICIENTLY TO THE RECEPTOR SYSTEM SOME KEYS ARE JUST NOT AS GOOD AS OTHERS, AND YOU CAN HAVE A LOT OF KEYS THAT DON’T FIT THE LOCKS; LESS DOORS ARE UNLOCKED WHEN WE HAVE THE WRONG KEY THE LOW AFFINITY AGONIST WILL COME OFF OF THE BINDING SITE MUCH FASTER THAN THE HIGH AFFINITY AGONIST WHEN A BAD KEY IS BEING USED, IT WILL BE EASIER NOT TO USE THAT KEY, BUT RATHER A GOOD KEY, RESULTING IN AN OPEN DOOR ( Maybaum 2014 )

8. ANTAGONISTS INHIBITORS OF REGULATORY DRUGS AND MOLECULES; THEY PRODUCE THEIR OWN EFFECTS BY BLOCKING RECEPTORS CHILD SAFETY LOCKS ON THE DOORS; THEY WILL NOT ALLOW THE KEY TO ENTER THE LOCK RECEPTOR FUNCTION IS LIMITED DUE TO AN AFFINITY, BUT THERE IS LITTLE TO NO INTRINSIC ACTIVITY WITHIN THE CELL THESE CHILD SAFETY LOCKS LIKE TO ATTACH THEMSELVES AND DO NOT ASSIST THE KEY NOT ALL ANTAGONIST ACTIVITY IS BAD; AN AGONIST MAY BE UNABLE TO FULLY BIND AND GENERATE A RESPONSE, ALLOWING THE ANTAGONIST TO ELIMINATE HARM TO THE PATIENT SOME DOORS ARE BETTER OFF CLOSED; IF LEFT OPENED, THERE MAY BE UNWANTED ENTRY OR EXIT

9. High affinity Antagonists EFFECTORS ARE NOT ACTIVATED ALTHOUGH THE ANTAGONIST BINDS WITH THE HIGH AFFINITY RECEPTOR CHILD SAFETY LOCKS ARE REALLY EFFECTIVE AT KEEPING KEYS FROM ENTERING A LOCK; SOME UNLOCKED DOORS MAY NOT EVEN OPEN WHEN A CHILD SAFETY LOCK IS IN PLACE ( Maybaum 2014 )

10. COMPETING AGONISTS & ANTAGONISTS THE AGONIST CANNOT FULLY BIND TO THE RECEPTOR AS IT IS BEING BLOCKED BY THE ANTAGONIST SOME CHILD SAFETY LOCKS ARE WEAK AND KEYS CAN STILL GET TO THE LOCK; NOT ALL KEYS WILL BE EFFICIENT ENOUGH TO REACH THE DOOR LOCK ( Maybaum 2014 )

11. COMPETING HIGH AGONISTS & ANTAGONISTS THE ANTAGONIST IS PRESENT HOWEVER THE AGONIST IS IN HIGH ENOUGH CONCENTRATION THAT IT CAN COMPETE FOR BINDING SITES CHILD SAFETY LOCKS AND KEYS WILL COMPETE WITH ONE ANOTHER TO SEE WHO GETS TO THE DOOR FIRST; SOMETIMES THE KEYS WIN; MORE KEYS = MORE UNLOCKED DOORS

12. Value in Nursing “The value of combination therapy with inhaled corticosteroids and long-acting b-agonists (ICS/LABA) is well recognized in the management of asthma 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 IN THE LUNGS WHICH LEADS TO BRONCHODILATION

13. VALUES IN NURSING BETA AGONISTS HAVE A AN AFFINITY FOR BETA 1 RECEPTORS WHICH MAY ALSO EFFECT 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. references American Thoracic Society. (2014). What are beta agonists? Retrieved from http :// www.thoracic.org/clinical/copd-guidelines/for-patients/what-kind-of-medications- are-there-for- copd /what-are-beta- agonists.php Lehne , 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 o bstructive p ulmonary d isease with c ombination i nhaled c orticosteroids and long-acting β-agonists : A review of comparative e ffectiveness research d rugs ,  74 (7), 737-755. doi:10.1007/s40265-014-0214-8 Maybaum , J. (n.d . ). Pharmacology Principles / Dental IMS-II . Retrieved August 26, 2014, from http :// sitemaker.umich.edu/maybaum.pharmacology.principles/noncompetitive_antagonist