GLP-1 - PLAN B - 6 MONTH PRESCRIPTION
GLP-1(glucagon-likepeptide-1)
Whatitis
GLP-1 is a cretin hormone produced mainly by intestinal L-cells (andinsmallamountsbycertainneurons) in response to nutrient intake.
Majoractions
Stimulatesglucose-dependentinsulinsecretionfrompancreaticβ-cells(lowerspostprandialbloodglucose).
Suppressesglucagonsecretionfrompancreaticα-cellswhenglucoseiselevated.
Slowsgastricemptying,reducingpost-mealglucosespikesandappetite.
Actsonthecentralnervoussystemtoreduceappetiteandfoodintake.
Promotesβ-cellsurvivalandmayenhanceβ-cellproliferationinsomecontexts.
Physiologyandkinetics
Releasedrapidlyaftereating;shortendogenoushalf-life(~1–2minutes)becauseitiscleavedandinactivatedbytheenzymedipeptidylpeptidase-4(DPP-4).
NativeGLP-1existsmainlyasGLP-1(7–36)amideanditsmetaboliteGLP-1(9–36).
Clinicalrelevance
GLP-1receptoragonists(e.g.,exenatide,liraglutide,semaglutide)mimicGLP-1actionsandareusedtotreattype2diabetesand,athigherdoses,obesity.Theyimproveglycemiccontrol,promoteweightloss,andhavecardiovascularandrenaloutcomebenefitsinsomeagents.
DPP-4inhibitorsincreaseendogenousGLP-1levelsmodestlybyblockingitsdegradationandareusedintype2diabetes.
CommonsideeffectsofGLP-1receptoragonists:gastrointestinal(nausea,vomiting,diarrhea),potentialriskofpancreatitis(rare),andinjection-sitereactions;individualagentshavespecificsafetyprofiles.
Mechanismofaction(brief)
BindsGLP-1receptor(aGprotein–coupledreceptor)onpancreaticβ-cellsandCNSneurons→activatesadenylatecyclase/cAMP→enhancesinsulinsecretioninaglucose-dependentmannerandmodulatesneuronalcircuitscontrollingappetite.
Typicalclinicaleffects
HbA1creduction(variesbyagent),weightloss(modesttosignificantdependingondoseandagent),reducedpostprandialandfastingglucose,andinsometrialsreducedmajoradversecardiovascular events.
w/L-Carnitine
Carnitine is a quaternary ammonium compound involved in metabolism in most mammals, plants, and some bacteria. In support of energy metabolism, carnitine transports long-chain fatty acids from the cytosol into mitochondria to be oxidized for free energy production, and also participates in removing products of metabolism from cells. Given its key metabolic roles, carnitine is concentrated in tissues like skeletal and cardiac muscle that metabolize fatty acids as an energy source
GLP-1(glucagon-likepeptide-1)
Whatitis
GLP-1 is a cretin hormone produced mainly by intestinal L-cells (andinsmallamountsbycertainneurons) in response to nutrient intake.
Majoractions
Stimulatesglucose-dependentinsulinsecretionfrompancreaticβ-cells(lowerspostprandialbloodglucose).
Suppressesglucagonsecretionfrompancreaticα-cellswhenglucoseiselevated.
Slowsgastricemptying,reducingpost-mealglucosespikesandappetite.
Actsonthecentralnervoussystemtoreduceappetiteandfoodintake.
Promotesβ-cellsurvivalandmayenhanceβ-cellproliferationinsomecontexts.
Physiologyandkinetics
Releasedrapidlyaftereating;shortendogenoushalf-life(~1–2minutes)becauseitiscleavedandinactivatedbytheenzymedipeptidylpeptidase-4(DPP-4).
NativeGLP-1existsmainlyasGLP-1(7–36)amideanditsmetaboliteGLP-1(9–36).
Clinicalrelevance
GLP-1receptoragonists(e.g.,exenatide,liraglutide,semaglutide)mimicGLP-1actionsandareusedtotreattype2diabetesand,athigherdoses,obesity.Theyimproveglycemiccontrol,promoteweightloss,andhavecardiovascularandrenaloutcomebenefitsinsomeagents.
DPP-4inhibitorsincreaseendogenousGLP-1levelsmodestlybyblockingitsdegradationandareusedintype2diabetes.
CommonsideeffectsofGLP-1receptoragonists:gastrointestinal(nausea,vomiting,diarrhea),potentialriskofpancreatitis(rare),andinjection-sitereactions;individualagentshavespecificsafetyprofiles.
Mechanismofaction(brief)
BindsGLP-1receptor(aGprotein–coupledreceptor)onpancreaticβ-cellsandCNSneurons→activatesadenylatecyclase/cAMP→enhancesinsulinsecretioninaglucose-dependentmannerandmodulatesneuronalcircuitscontrollingappetite.
Typicalclinicaleffects
HbA1creduction(variesbyagent),weightloss(modesttosignificantdependingondoseandagent),reducedpostprandialandfastingglucose,andinsometrialsreducedmajoradversecardiovascular events.
w/L-Carnitine
Carnitine is a quaternary ammonium compound involved in metabolism in most mammals, plants, and some bacteria. In support of energy metabolism, carnitine transports long-chain fatty acids from the cytosol into mitochondria to be oxidized for free energy production, and also participates in removing products of metabolism from cells. Given its key metabolic roles, carnitine is concentrated in tissues like skeletal and cardiac muscle that metabolize fatty acids as an energy source