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66 Cards in this Set
- Front
- Back
- 3rd side (hint)
two types of cholinergic receptor agonist
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1. direct acting agonist
2. Indirect acting agonist |
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Direct acting cholinergic receptor agonist
examples: |
bind and activate cholinergic receptors
i.e. choline esters Ach, bethanecol,carbachol |
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Indirect acting cholinergic receptor agonsit do what?
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increase levels of Ach at synapse:
-inhibit cholinesterase -inhibit breakdown of Ach -inhibit release of Ach |
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General Properties of cholinergic agonist
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-similar to Ach
-do NOT cause CNS effects -are non specific for M receptors, stimulate all, thus cause wide variety of effects |
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Cholinergic agonist ocular effects
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-increase lacrimal gland secretions
-stimulate contraction of iris sphincter muscle and ciliary muscle (miosis) -enhance near vision -decrease night vision |
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cholinergic agonist toxic doses/overdoses can cause:
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-diarrhea
-salivates -cramps -shortness of breath -urniary incontinence |
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cholinergic agonist respiratory effects:
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-increase bronchial smooth muscle contraction
-increase secretions of mucus -contradicted in patients with uncontrolled asthma and COPD |
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Cholinergic agonsit cardiac effects:
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-reduced peripheral vascular reistance
-reduced HR -slows HR by decreasing sinus rhythm -increase PR interval by slowing conduction thru AV node |
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Cholinergic agonsit GI effects:
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-stimulate gastric motility via stimulus ENS
-stimulat salivary and gastric secretions -increase GI contractions; except sphincters |
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Cholinergic agonsit Urinary tract effects:
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-stimulate detrusor muscle; layer of muscle in the uterus that when contracted expels urine
-relax urinary sphincter and trigone -promotes micturition |
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Two types of indirect acting cholinergic agonsit
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1. reversible=short acting
*used to treat myasthenia graves- autoimmune 2.Irreversible=long lasting *used as nerve gases and pesticides |
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Cholinergic antagonist general effects:
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-relax smooth muscle
-decrease secretions -decrease lacrimination -increase heart rate -increase cardiac conduction |
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cholinergic antagonist ocular effects:
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-relax iris sphincter=pupil
dilation (mydriasis) -relax ciliary muscle causing cycloplegia(paralysis of accomodation) -decreases lacrimation= dry eyes |
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cholinergic antagonist cardiac effects:
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-increase HR
-icrease AV conduction |
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Cholinergic antagonist respiratory effects:
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-bronchial smooth muscle
relaxation -bronchial dilation -inhibit secretions of upper and lower resp tract |
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cholinergic antagonist GI effects
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-reduces LES tone and may promote reflux
-relaxes smooth muscles (except sphincters) -reduces motility -inhibit gastric secretions -lead to prolonged emptying time and consitpation |
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cholinergic antagonist Urinary tract effects
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-retract detrusor muscle leading to urinary retention
-CNS effects -sedation; across blood-brain barrier -acute confusional (delirium) -high doses cause hallucinations |
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cholinergic antagonsit inhibit_______ and causes___ ___ skin
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sweating;
hot;dry |
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cholinergic antagonist overdose causes
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Dry as bone
hot as pepper red as a beet mad as a hatter |
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adrengic receptors include
3 main types |
alpha 1 and alpha 2
beta 1 and beta 2 dopamine 1and 2 |
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alpha 1 primary function
i.e. |
smooth muscle contraction
bladder sphincter iris dilator vascular vasoconstriction increase peripheral vascular resistance increases BP mydriases urniary retetion |
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alpha 2 primarily pre-synaptic; functions to
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-inhibition of NE release
-decrease secretion of aqueous humor -decrease insulin secretion -mediates platelet aggregation |
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Beta-1 functions primarily
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caridac
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beta-1 functions
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-increase HR chronotropic effect
-increase contractility (inotropic) -increase heart conduction (dromotrpic) -increase renin secretion -tachycardia |
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beta-2 acts on which muscle
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smooth
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beta-2 functions to do what?
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-relaxation of smooth muscle:
*vascular *bronchial *uterine -glycogenolysis |
relax
breakdown of what? Ach effects |
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dopainne acts primarily in the ______
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brain
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dopamine functions to
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mediate vascular smooth muscle relaxation
modualte neruotransmitter relase in sympathetic and CNS *D receptors only st. by dopamine |
vascular ___ muscle _____
modulate _____release in sympathetic and CNS act only on |
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catecholamines ____ -OH group
natural synthetic |
have;
epi, NE , dopamine isoproterenol, dobutamine |
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non-catecholamines____-OH group
types |
lack;
phenylephrine, pseudoephedrine,amphetamine |
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adernergic agonist epinephrine potent at ___&____
constricts vessels in___ ____ and ____ dilates vessels to ____&____ |
-potent agonist at both A and B sites
-constricts vessles in skin,mucus membranes and visera -dilates vessels to liver and muscle |
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Adrenergic receptor antagonists consist of what 2 groups?
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Alpha 1&2 blockers
Beta 1&2 blockers |
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what are alpha blockers generally used to treat?
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used mainly to treat hypertension, cardiac dysrhythmias, angina and myocardial infarction. Also used to treat anxiety.
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effects of Alpha-1 blocker?
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cause smooth muscle relaxtion in vascular and uriary tissue
causes vasodilation and lower BP less reflex tachycardia then phentolamine can cause fast reduction in BP,dose low to start, prevent syncope |
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Alpha-1 blocker
-no change in _____ and ____ -improves _______ Use for ____&_____ |
cardiac output; renal flow
urinary flow; BPH; HTN |
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Side effects of Alpha-1 blockers?
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Dizziness
syncope othrostasis nasal congestion headache |
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Beta-1 blocker decreases HR by having negative effects on _____,_____,_____
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Chronotropic (change HR)
inotropic (contractility) dromotropic (conductivity of cardiac muscle fibers) |
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Beta-1 blocker
decreases_____ ____ from the kidneys |
renin secretion
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Beta-1 blocker
decreases____ ____ formation in the eyes lowers ____ _____ pressure |
aqueous humor;
intra ocular |
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Beta-2 blockers cause
-bronchial______ -_____ gylcogenolysis and glucagon secretion -masks signs of _____ in DM -decreased _____ _____ |
constriction
inhibits hypoglycemia renal perfusion |
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Therapeutic uses of beta blockers
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hypertension
hyperthyroidism angina glaucoma migraine HA MI prevention palpatations performance anxiety tremor pheochromocytoma |
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SE of beta blockers
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brochospasm
bradycardia heart block due to high doses Erectile dysfunction |
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Epinephrine Adrenergic agonist:
_________bronchial smooth muscle relieves ______ induced bronchospasm _______ tidal volume stimualtes ________ |
dilates;
histamine; increases; glycogenolysis |
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ephinephrine therapeutic uses include:
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*asthma
*glaucoma *anaphylaxis(epi pen) *anaphylactic shock *use to prolong effects of local anesthetics *reduce bleeding in surgery *in actue MI w/ cardiac arrest |
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Norepinephrine is more receptive to ____ then ____ receptors
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B1; B2
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NE
strong agonist at alpha receptors = |
vasoconstriction of most all vessels
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NE:
increase ___ |
BP
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Dopamine activates
___,___,&___ receptors |
D1; B1; alpha
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dopamine stimulates release of ____ from synaptic neurons
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NE
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Dopamine selectively dilates vessels in _____ and ____ vessels
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renal; sphlanchic
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Dopamine increases
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HR
contractility cardiac output |
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Dopamine is dose ______
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dependent
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Low dose of dopamine cause:
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renal failure; vasodilates and increase renal blodd flow
(D1 receptor) |
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medium dose of dopamine cause:
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Increase HR and CO so used in shock (B1 receptor)
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High dose of dopamine cause:
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stimulates alpha 1 and causes vasoconstriction and increases periperal resistance
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Dopamine side effects:
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short-lived
rapid metabolism HTN nausea disrhythmia |
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NE:
increase ___ |
BP
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Dopamine activates
___,___,&___ receptors |
D1; B1; alpha
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dopamine stimulates release of ____ from synaptic neurons
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NE
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Dopamine selectively dilates vessels in _____ and ____ vessels
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renal; sphlanchic
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Dopamine increases
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HR
contractility cardiac output |
similar to B1 effects
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Dopamine is dose ______
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dependent
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Low dose of dopamine cause:
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renal failure; vasodilates and increase renal blodd flow
(D1 receptor) |
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medium dose of dopamine cause:
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Increase HR and CO so used in shock (B1 receptor)
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High dose of dopamine cause:
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stimulates alpha 1 and causes vasoconstriction and increases periperal resistance
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Dopamine side effects:
are ____ have a ___ ___ consist of: ____ ____ ____ |
short-lived
rapid metabolism HTN nausea disrhythmia |
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