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332 Cards in this Set
- Front
- Back
most potent to least potent alpha adrenergic receptors
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alpha: epi>norepi>isoproterenol
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most potent to least potent beta adrenergic receptors
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beta: isoproterenol>norepi=epi
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Drug of choice for the treatment of urethral hyperreflexia and functional urethral obstruction
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phenoxybenzamine
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tolazoline
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reversal agent of xylazine
|
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alpha 2 adrenergic agonist-for hypertension
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clonidine
|
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natural catecholamines
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norepi
epi dopamine |
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synthetic catecholamines
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isoproterenol
dobutamine |
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noncatecholamines
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ephedrine
amphetamine metaraminol phenylephrine phenylpropanolamine |
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epi mostly stimulates what receptors?
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alpha and beta
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norepi mostly stimulates what receptors?
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alpha and beta, but mostly alpha
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isoproterenol stimulates what receptors?
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pure beta
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Alpha 1 receptors located where?
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postsynaptic
smooth muscle cause vasoconstriction |
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phenylephrine?
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nephrosplenic entrapment
|
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epinephrine #1 drug for?
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CPR-vasoconstriction
|
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Alpha 1 adrenergic receptors stimulate what kind of G coupled proteins?
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Gq=decrease IP3 and DAG
|
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Alpha 2 adrenergic agonist receptors located where?
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presynaptically
postsynaptically |
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presynaptic alpha 2 adrenergic receptors do what when stimulated?
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cause vasodilation-negative feedback on NE release=vasodilation
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postsynaptic alpha 2 adrenergic receptors do what?
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vasoconstriction
|
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Beta receptors activate what kinds of G coupled proteins?
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Gs=increased adenylyl cyclase, increased cAMP=increased cell activity
|
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Beta 1 receptors work on?
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cardiac stimulation
release rennin |
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Beta 2 receptors do what?
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Vasodilate:
increase aq humor (contra for glaucoma) bronchodilation decrease release of glucagon in response to low blood glucose so you become hypoglycemic |
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In general stimulation of D1 and D2 receptors causes dilation or constriction of vessels?
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vasodilate
|
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Dopamine? Know it all.
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Dose dependent pharmacologic effect
2mg/kg/min: diuresis 2-10mg/kg/min: positive inotropic effect=hypotension and show above 10mg/kg/min: vasoconstriction=hypotension and shock |
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Three things you should know about catecholamines?
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ineffective orally
slow when applied SQ (vasoconstriction) Do not cross the BBB |
|
Epi in glaucoma?
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decreases intraocular pressure in OPEN angle glaucoma, might be contraindicated in other types of glaucoma
|
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What are the two goals of giving drugs during shock?
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maintain normal bp
bronchodilation |
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dobutamine half life?
|
short half life
|
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For renal failure patients, what drug can you use to increase peeing?
|
dopamine increases diuresis at 2mg/kg/min. dose dependent pharm effect!
|
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Adrenergic drug's effect on the GIT?
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inhibit GI activity, but we don't use them for this, we still use atropine (re: block SLUD)
|
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If you give epi after you give acepromazine?
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BAD! hypovolemic shock
|
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If epi becomes extravascular when you give it what happens?
|
local necrosis, sloughing of the skin at injection site bc of vasoconstriction and ischemia
|
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what was the handout on that he gave us? why should we know that?
|
epinephrine reversal...it has to do with using acepromazine then epi...it can be hard to reverse
|
|
Ephedrine: directly or indirectly acting noncatecholamine?
|
indirectly acting noncatecholamine
|
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Any advantage to using ephedrine over epi?
|
longer duration of action
given orally we dont really use it though |
|
why would you use ephedrine on an eye?
|
mydriatic agent
|
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Can you develop tachyphylaxis with ephedrine?
|
yes
|
|
Amphetamine sulfate?
|
not used in vet med
noncatecholamine |
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What drug has an advantage over epi because it can treat hypotension without causing vasoconstriction and stimulating the heart?
|
phenylephrine
|
|
phenylpropanolamine: indirect or direct acting noncatecholamine?
|
indirect acting noncatecholamine
|
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Beta adrenergic antagonists can only block directly acting or indirectly acting agonists?
|
indirectly acting agonists
|
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Example of a beta 2 agonist?
|
clenbuterol
|
|
Best way to give beta 2 agonists?
|
through inhalation
|
|
Why would you want to give beta 2 agonists via inhalation?
|
bc they act on the bronchioles. so this way you can give a lower dose than if you were to give it orally, meaning you have less chance of side effects
|
|
How do adrenergic antagonists work?
|
they sit in the receptor sit and block agonists from accessing the site (aka receptor antagonism, takes an agonist and an antagonist)
|
|
Nonselective beta blocker?
|
propanalol
|
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Selective beta blocker that has some use in glaucoma patients?
|
timolol
|
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selective beta blocker that has some use in cardio protection bc it can scavenge free radicals?
|
carvedilol
|
|
prototype drug for beta blockers
|
atenolol: can be give 1x/day
|
|
what is the beta blocker used on cats with hypertrophic cardiomyopathy?
|
atenolol
|
|
Why should you not use nonselective beta blockers in vet med?
|
bronchoconstriction
|
|
On what patients should you not use beta blockers at all?
|
1. heart failure
2. hepatic disease 3. diabetes mellitus (hypoglycemic...remember Beta 2?) |
|
Nonselective beta 2 blockers should not be used in animals about to undergo glycemic tests bc?
|
beta 2 blockers block the effect of hypoglycemia (beta 2)
|
|
If you give beta 2 blocker, will you see an increase, decrease or no change in the amount of glucagon in your patient?
|
see a decrease in glucagon, bc it is normally released in response to low blood glucose, but blockers block this effect and decrease glucagon release.
|
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Would alpha 1 dilate pupil or constrict?
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dilate pupil bc causes vasoconstriction, constricts the radial muscles=dilation of pupil
|
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How does alpha 2 have the effect to cause vasodilation?
|
supresses sympathetic output...remember alpha 2 presynaptic have a negative feedback on Norepi release...causes vasodilation
|
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what do alpha 2's do on to beta cells in the pancreas? Which does what to insulin?
|
stimulates them which inhibits insulin release
|
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Drugs that stimulate alpha 2 cause vasodilation and hypotension, why?
|
stimulate alpha 2 adrenergic receptors in the CNS, if you do this, you will suppress the outflow of sympathetic neurtransmitters from the braine. why they are used in humans for hypertension
|
|
first alpha antagonists id'ed?
|
ergot alkaloids
|
|
What kind of tranquilizer is acepromazine?
|
phenothiazine tranquilizer
|
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In general, which agonists (alpha or beta) do you want to use for glaucoma?
|
beta
|
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most drugs are competitive or noncompetitive antagonists?
|
competitive antagonists
|
|
phenoxybenzamine increases or decreases sympathetic outflow?
|
increase sympathetic outflow
|
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phenoxybenzamine is competitive or noncompetitive?
|
competitive (covalently binds=irreversible)
|
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phenoxybenzamine is more competitive against alpha 1 or alpha 2
|
alpha 1
|
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What is the drug of choice for functional urethral obstruction caused by internal urethral spincter tone increased in cats and dogs?
|
phenoxybenzamine
|
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Drug(s) of choice for external urethral sphincter tone being excessive?
|
dandrolene or diazepam
|
|
What drug do you use for pheochromocytoma?
|
phenoxybenzamine
|
|
You would want to use phenoxybenzamine with what drugs before surgery to prevent what?
|
phenoxybenzamine with beta blockers to prevent tachycardia during surgery
|
|
Do you want to use phenoxybenzamine in glaucoma patients?
|
no. it increases aq humor production by causing vasodilation bc of blocking alpha receptors.
|
|
tolazoline?
|
competitive alpha 1 and 2 antagonist
reversal agent for xylazine |
|
prazosin?
|
competitive
selective alpha 1 antagonist vasodilation and hypotension |
|
Does prazosin cause an increase, decrease or no change in NE release?
|
exerts less reflex sympathomimetic response than nonselective alpha 1 and 2 antagonists, so it DOES NOT cuase an increase in NE release, so it only causes a little tachycardia bc alpha 2 receptors are not being blocked
|
|
Prazosin can decrease sympathetic tone to treat?
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functional urethral obstruction aka urethral hyperreflexia (like phenoxybenzamine)
|
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What is the bummer about prazosin use?
|
tachyphylaxis
|
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What are the three alpha 2 receptor antagonists that we should know everything about?
|
yohimbine, tolazine, atipamezole
|
|
Alpha 2 agonists are given for the treatment of?
|
systemic hypertension
|
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alpha 2 agonists are used for what three things we must know! ***
|
For dose dependent:
1. sedation 2. analgesia 3. muscle relaxation |
|
What is the order of most potent sedative to least potent sedative?
|
metadomidine>detomidine>romifidine>xylazine
|
|
Can alpha 2 receptors stimulate alpha 1 receptors?
|
yes they can even though they are called alpha 2 receptors
|
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xylazine has its highest activity on alpha 1 or alpha 2 receptors?
|
alpha 1 receptors
|
|
detomidine acts mostly on alpha 1 or alpha 2?
|
detomidine middle activity on alpha 1
|
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metadomidine mostly works on what receptors?
|
very selective for alpha 2 receptors, has very little activity on alpha 1
|
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What species are least sensitive to the effects of alpha antagonists and which are most sensitive to antagonists?
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pigs-least sensitive
ruminants-most sensitive (give them 1/10 the dose of xylazine) |
|
alpha 2 agonists have their effect by?
|
in general by stimulating alpha 2 receptors in the brain stem they cause sedation
|
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which has longer duration of sedation, detomidine or xylazine?
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detomidine
|
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Duration of analgesia depends on?
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dose. it is dose depedent
|
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xylazine?
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alpha 2 AGONIST
use in horse with colic short duration of action |
|
what do you have to remember when you give xylazine to a horse?
|
sedation lasts much longer than analgesia! So be careful. they might be sedated, but after 15 min or so they can feel everything again!
|
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xylazine should be used with what drugs to increase analgesia?
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opioids
|
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How do alpha 2 agonists cause skm relaxation?
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by interupting the intraneuronal impulse transmission to muscle
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Can you give xylazine IV to sheep?
|
causes hypoxia
|
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Alpha 2 agonists should not be used in animals with?
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1. unstable cardio activity (they decrease CO by 30-50%)!!! this is significant
2. exercise tolerance (they already have very low HR) |
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Alpha 2 agonists intitially cause what kind of tension, followed by what kind of tension?
|
Alpha 2 agonists initially: hypertension
followed by: hypotension |
|
If you experience bradycardia when you give xylazine, what can you give the animal?
|
atropine or glycopyrrolate
|
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If you experience bradycardia when you give detomidine or demetadomidine, what can you give?
|
atipamezole, don't give atropine or glycopyrrolate bc you will cause more severe arrhythmias
|
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What species are most likely to develop bradycardia when you give alpha 2 agonists?
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cats and dogs, humans and primates are least likely to get bradycardia
|
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If an owner tells you that her horse has been on sulfonamides, right before you reach for detomidine to sedate it, what should you do?
|
Think otherwise. Never give detomidine to an animal that has been on sulfonamides=fatal cardiac dysrhythmias!
|
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Alpha 2 agonists are commonly used as preanesthetics, what must you keep in mind when you are doing this though?
|
animal vomit 3-5 minutes after they are given alpha 2 agonists, so you should wait for this time to pass before you induce general anesthesia
|
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What is the emetic drug of choice in cats?
|
xylazine
|
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You shouldn't give beta 2 agonist when you are doing a glucagon test, but what other agonists shouldn't you give either and why?
|
no Alpha 2 agonists=stimulate beta cells in pancrea=hyperglycemia transiently=can throw off your glucose tolerance test
-also decreases cortisol levels (which can be bad bc surgery is stressful and you have a lot of cortisol then) |
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Alpha 2 agonists increase, decrease or do not change urine output. why?
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increase urine output bc they decrease ADH
|
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xylazine is an alpha 2 agonists, so why do I have to be careful when I use it on pregnant animals?
|
can still stimulate alpha 1 receptors that are present on uterus=causes oxytocin like effect=dont use in late pregnancy cows!
|
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Xylazine is closely related to?
|
clonidine
|
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If you have already given ketamine, can you give xylazine?
|
no! you will cause cardiopulmonary dysfunction w/ the two.
|
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If you cause a seizure when you give xylazine, what should you reach for?
|
IV diazepam=cannot block with an alpha 2 antagonist, bc the seizure is being caused by alpha 1, so you have to give diazepam, not yohimbine
|
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Detomidine mostly used in what species?
|
horses
not used in small animals at all |
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Most potent alpha 2 agonist in vet med?
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medetomidine: had develop atipamezole just to reverse it
|
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Why should you never use potent alpha 2 agonists in horses or ruminants?
|
not dexmetadomidine or metadomidine in horses or ruminants bc it causes severe ataxia
|
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Can you use xylazine with other tranquilizers?
|
no! it causes significant hypotension (dont use with acepromazine...so far no using ace with epi or xylazine with ace or keta...only with yohimbine, tolazine....)
|
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who is most sensitive to xylazine?
|
ruminants
|
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what is the advantage of using alpha 2 agonists?
|
reversible
|
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What are some potent inducers of p450s?
|
barbituates (phenobarbital)
|
|
yohimbine?
|
reverses xylazine
-cannot reverse metadomidine or dexmetadomidine (that is what atipamezole is for) |
|
What is a good alpha 2 antagonists for ruminants?
|
tolazine (reverses xylazine better in ruminants than yohimbine)
|
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What is a drawback of atipamezole?
|
it is expensive
|
|
what alpha 2 antagonists causes piloerection in horses?
|
tolazine
|
|
When you are treating an epileptic patient, what should you keep in mind?
|
you need to figure out the underlying cause of the seizures and try to treat that
|
|
what is excessive discharge of neurons in the brain, characertized by loss of consciousness, increase muscle tone or movement, altered sensation and other neuro changes?
|
-seizure
|
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What are seizures characterized by spastic movement?
|
convulsions
|
|
recurrent seizures are called?
|
epilepsy
|
|
What is the difference between primary and secondary epilepsy?
|
primary: inherited, aka idopathic
secondary: acquired, caused by various conditions |
|
Seizures can be classified as?
|
general or focal
(general can become focal and focal can become general) |
|
What are the three phases of a seizure?
|
1. preictal phase
2. ictus 3. postictal phase |
|
Status epilepticus is what?
|
seizure lasting 30 minutes or more or a seizure representing multiple short seizures with no consciousness
|
|
what are the four mechanisms by which seizures can begin?
|
1. altered neuronal membrane function
2. decrease inhibitory neurotransmitter (GABA) 3. increased excitatory neurotransmitter (glutamate) 4. altered extracellular K and Ca concentration |
|
Because it is hard to control seizures what should you always remember to practice?
|
therapeutic monitoring
|
|
Three most common seizure controlling drugs?
|
phenobarbital, primidone and diazepam
|
|
Can anticonvulsants cross the bbb?
|
yes
|
|
what is the most lipid soluble anticonvulsant?
|
diazepam
|
|
emergency drug of choice for status epilepticus?
|
IV diazepam
|
|
where are a majority of anticonvulsants metabolized?
|
liver
|
|
what is half life?
|
time to eliminate 50% of the drug from the body
helps you determine dosing interval |
|
Diazepam: long or short half life?
|
short: why we give it IV
|
|
If a patient misses a dose of what drug, it is likely to have a seizure?
|
diazepam, short half life, so big difference between peak and trough=seizure with missed dose
|
|
when you trying to monitor diazepam in the body, how many blood samples should you take and when? Why?
|
take two blood samples:
1. at peak (which would be 4-6 hours after you gave the initial dose) 2. at trough (right before you are getting ready to give the second dose) you do this bc it has such a short half life |
|
phenobarb: long or short half life?
|
long half life
|
|
if you are monitoring a dog to see how it will do with phenobarbital, how many blood samples should you take, when should you take them and why?
|
take one blood sample
take it at trough (right before you are going to give another dose) you do this bc it has such a long half life |
|
With what anticonvulsant, should you not be too worried if the client forgets to give a dose?
|
phenobarbital: it has a long half life so if the patient misses a dose it probably will not seizure
|
|
With what anticonvulsant can you give an extra dose in the middle of the seizure and stop it?
|
diazepam: bc of its short half life
|
|
Does giving an extra dose of phenobarbital do any good in a seizuring patient?
|
no, just give IV diazepam
|
|
which anticonvulsant induces its effect at doses lower than those required to induce profound CNS depression?
|
phenobarbital
|
|
which anticonvulsant has the widest spectrum of activity?
|
phenobarbital
|
|
How do anticonvulsants have there effect?
|
allosteric modifiers of GABA so that it stays attached to its buddy longer and increases the time the Cl channels are open which increases the seizure threshold by causing hyperpolarization
|
|
which anticonvulsant has good oral bioavailability? is inexpensive and lasts a long time?
|
phenobarbital
|
|
since phenobarbital doesn't start having its effect on the body until 8-15 days after you give it, what should you do?
|
Give a loading dose
-use volume of distritbution X conc steady state to get loading dose |
|
If you are giving phenobarbital at 3 to 40 mg/ml, what should you monitor for?
|
liver failure, it is hepatotoxic
|
|
If you are giving phenobarbital with other drugs, what should you keep in mind?
|
it is a potent inducer of p450 which means it will also increase the metabolism of other drugs that are in the system
|
|
The fact that phenobarb stimulates p450 means that it causes?
|
autoinduction: it increases its own metabolism
|
|
what is the only other anticonvulsant you can combine phenobarb with?
|
bromide
|
|
If you are monitoring liver function in a patient on phenobarbital and you find elevated serum alkaline phosphate enzymes, what should you think?
|
-elevated serum alkaline phosphate enzymes in a patient on phenobarb is not indicative of liver disease-with phenobarbital administration
|
|
Since phenobarb can be hepatoxic what other anticonvulsant that isn't hepatotoxic can you give it with?
|
bromide
|
|
which anticonvulsant is not hepatotoxic?
|
bromide
|
|
If a client accidentally gives too much phenobarbital to a dog, what can you do to try to avoid hepatotoxicity?
|
-give bicarb, since it is a weak acid it will increase the urine excretion of phenobarbital
|
|
which drug has some anticonvulsant activity but most of its anticonvulsant activity is coming from it being metabolized to phenobarbital?
|
primidone: it might work ok in dogs that don't repsond well to phenobarbital though
|
|
What is the most potent hepatotoxic anticonvulsant?
|
primidone
|
|
You should never use primidone with what?
|
phenobarbital or phenytoin
|
|
How should you give phenytoin?
|
oral, rectal
IV: severe hypotension IM: tissue necrosis |
|
What is a disadvantage of phenytoin?
|
saturaton kinetics: difficult to maintain plasma conc in dogs, doses necessary to have its effect affect the enzyme system to eliminate it and become saturated.
|
|
By what order elimination process is phenytoin eliminated?
|
zero order elimination process, nonlinear kinetics (makes it a pain bc you can't just double the dose and double the concentration in the blood like with first order kinetics)
|
|
What is the drug of choice for alkaloid induced ventricular dysrythmias in dogs?
|
phenytoin
|
|
Why should you never ever use phenytoin with primidone or phenobarbital?
|
enhanced hepatotoxicity
|
|
when you run for diazepam when a patient is seizuring, what should be careful of when you get the IV set and start giving it?...if you can get an IV started...
|
dont give an rapid IV bolus=cardiotoxic
give slowly |
|
Can diazepam cause increase or decrease appetite?
|
appetite stimulant
|
|
Diazepam is rapidly metabolized which means?
|
it cant be used long term=tachyphylaxis
|
|
Can you give bromide to cats?
|
no. bronchial asthma like symptoms
|
|
what is flumazenil?
|
reverses diazepam
but! its carrier is ethylene glycol=hepatotoxic |
|
What are the two metabolites of diazepam?
|
nordiazepam
oxazepam -both are less active than diazepam,but are still active |
|
How many blood samples of diazepam when you are monitoring?
|
2: short half life!
|
|
What is one drawback to using diazepam in cats?
|
hepatoxicity can happen at any time, it is unpredictable
|
|
what is a drug that dogs do not develop tolerance to, commonly used with phenobarbital or bromide for long term control of seizures and is a prodrug?
|
clorazepate
|
|
If you use clorazepate with phenobarbital what should you do?
|
decrease the dose of phenobarbital given with it
|
|
which drug is hepatotoxic to cats like diazepam?
|
clorazepate
|
|
which anticonvulsant is more potent and better absorbed orally than diazepam, can't be used long term in dogs, but can be used long term in cats, but is still hepatotoxic in cats?
|
clonazepam
|
|
what anticonvulsant can be used as an alternative to diazepam in status epilepticus, has minimal hepatoxocity in cats, dosen't have to metabolized in the body to work, can be used in geriatric patients?
|
lorazepam
|
|
If you give a cat bromide and it develops bronchial asthma like symptoms, what should you give it?
|
treat with glucocorticosteroids
|
|
Is bromide toxic?
|
yes! very potent
|
|
Is bromide toxic to the liver?
|
no. not hepatotoxic, but in general it is toxic.
|
|
what is the treatment of choice for bromide toxicity?
|
NaCl (salt)
-or give diuretics like furosemide |
|
why can bromide be given orally?
|
high osmolality
|
|
gabapentin?
|
neuropatic pain control
|
|
Drug of choice of REFRACTORY status epilepticus?
|
pentobarbital sodium
|
|
what are drugs that stimulate the CNS called?
|
Analeptics
|
|
What do respirotary analeptics work on?
|
stimulate depressed respiratory centers
|
|
what is respiratory analeptic that can be used to stimulate respiration after surgery or in new borns, can be given sublingually or in the umbilical vein in pups, causes medulla oblongata stimulation, safe drug to be used in vet med, can cause acidosis bc of its preparation
|
doxapram
|
|
What are the four methylxanthine derivatives?
|
Caffeine
theophylline theobrimide aminophylline |
|
what do methylxanthines do in the CNS?
|
stimulate the CNS
|
|
what do methylxanthines do to the coronary blood vessels
|
dilate coronary bvs
|
|
Liver disease will increase, decrease or not change the length of pharm action with methylxanthines?
|
increase pharmacological action
|
|
what are the four barbituates we talked about in class?
|
1. phenobarbital
2. pentobarbital 3. methohexital 4. thiopental |
|
what is an example of a substituted phenol?
|
propofol
|
|
what are the two cyclohexylamines aka dissociative anesthetics?
|
1. ketamine
2. tiletamine (telazol) |
|
Imidazole derivatives? (2 of them)
|
1. etomidate
2. metomidate |
|
What the four GROUPS of barbituates?
|
1. thiobarbituates
2. ultrashort acting oxybarbituates 3. short acting oxybarbituates 4. long acting oxybarbituates (oral anti-epilepsy barbituates=phenobarbital) |
|
Barbituates are weak acids or weak bases?
|
weak acids
|
|
why is significant that barbituates are formulated as sodium salts?
|
no perivascular leakage
|
|
Based on chemical structure barbituates are organized into what two groups?
|
1. oxybarbituates
2. thiobarbituates |
|
what is the difference in structure bt oxybarbituates and thiobarbituates?
|
1. oxybarbituates: have o2 at C2
2. thiobarbituates: have sulfur at C2 |
|
The R1 and R2 of oxybarbituates is aryl or alkyl?
|
both
|
|
The R1 and R2 of thiobarbituates is aryl or alkyl?
|
both are aryl groups
|
|
By what routes are barbituates absorbed?
|
absorbed by all routes
|
|
How should ultra short acting barbituates be given?
|
only by IV
|
|
Do barbituates have a low or high volume of distribution?
|
high volume of distribution
|
|
what form do barbituates have to be in to cross the BBB?
|
unionized
|
|
If you an acidotic cat and you want to give it thiopental to induce anesthesia should you increase or decrease the dose of anesthesia, why?
|
decrease the dose bc:
acidosis: increase cellular penetration by anesthetics=deeper anesthesia |
|
If you have a cat with a lot of bicarb in its system and you want to induce anesthesia should you increase or decrease the dose, why?
|
increase the dose bc:
alkalosis: decreases cellular penetration by anesthetics=lighter anesthesia |
|
If you have a dog that is hyproteinemic and you are going to give a barbituates, what should you note?
|
barbituates are not active when they are protein bound
hypoproteinemic=less protein to bind barbituate=more active drug floating around=deeper anesthesia |
|
which structural group of barbituates is more lipid soluble?
|
thiobarbituates are more lipid soluble
|
|
Termination of barbituate anesthesia is by what three methods?
|
1. physical redistribution
2. metabolic degradation 3. renal excretion |
|
Do the kidneys affect long acting barbituates?
|
nope
|
|
What are examples of:
1. a long acting barbituate 2. a short acting barbituate 3. an ultra short acting barbituate |
1. long=phenobarbital
2. short=pentobarbital 3. ultra short=thiopental |
|
How does recovery from thiopental occur?
|
by redistribution
|
|
Recovery from methohexital is primarily due to?
|
biodegradation in liver and plasma
|
|
How do barbituates induce skeletal muscle relaxation peripherally?
|
cause skeletal muscle relaxation peripherally by decreasing binding and sensitivity of Ach to postsynaptic membranes
|
|
The pharmacologic effect of barbituates ultimately is to?
|
cause dose dependent depression of all organ systems and functions
|
|
If you overdose an animal on barbituates and the heart continues to beat, what can you do?
|
artificially respirate for several minutes
|
|
when you give an IV injection of a barbituate you get transient__________and sustained_________.
|
transient hypotension
sustained tachycardia |
|
40% of dogs develop bigeminy when they are given this drug?
|
thiopental
|
|
The affects on the CNS by barbituates at:
1. subtherapeutic doses 2. anesthetic doses 3. high doses 4. overdose are.... |
1. subtherapeutic: sedation w/o analgesia
2. anesthetic: general anesthesia, poor analgesia, good muscle relaxation 3. high dose: deep anesthesia w/ depression of medullary centers and motor function 4. overdose: respiratory arrest, then cardioarrest, then death |
|
what drug is given IV to treat strychnine poisoning?
|
phenobarbital sodium
|
|
Which drug is more potent than thiobarbituates, may cause excitement during recovery, and IS SAFE for sight hounds?
|
methohexital
|
|
Which drug has reconstituted solution that is unstable, cumulates after multiple doses, causes ventricular bigeminy in some dogs, IS NOT safe to use in sight hounds, causes poor muscle relaxation and analgesia?
|
Thiopental
|
|
What is the cheapest drug in vet med for short term anesthesia?
|
thiopental
|
|
why should you never give thiopental alone to a horse? What should you do instead?
|
excitement and ataxia-premedicate with xyalzine or opioids first
|
|
Dissociative anesthetics are characterized by?
|
1. sensory loss
2. analgesia 3. amnesia **But without actual loss of consciousness |
|
Dissociative anesthesia is characterized by?
|
1. CNS excitement
2. analgesia 3. skm rigidity 4. amnesia with superficial sleep 5. dissociation from the environment 6. intact protective reflexes |
|
Large doses of dissociative anesthetics do what to the heart?
|
depress the cardio system by directly depressing myocardium
|
|
What drugs cause an apneustic breathing patter in cats?
|
Dissociative anesthetics (ketamine and telazol)
|
|
where is ketamine metabolized?
|
In the liver
|
|
If you give ketamine alone to cats, what will recovery be like?
|
-smooth
-can have "tennis match" cats |
|
If you give ketamine alone to dogs, what will recovery be like?
|
-stormy recovery
|
|
Which drug causes skeletal muscle rigidity instead of relaxation and as a result should not be used for abdominal or thoracic surgery alone?
|
-ketamine
|
|
why should you use caution when you give dissociate anesthetics to animals with renal function that is compromise?
|
-more than 50% of the drug is excreted in the urine unchanged
|
|
what is in triple drip?
|
xylazine + ketamine + guaifenesin
or alpha 2 agonist, dissociative anesthetic and guaifenesin |
|
which dissociative anesthetic an you use for a c-section?
|
ketamine
|
|
which anesthetics should you never use alone in horses and why?
|
dissociative anesthetics (ketamine and telazol) cause prolonged ataxia
|
|
Telazol works better in cats or dogs?
|
cats
|
|
What is the prototype phenol drug?
|
propofol
|
|
What is a huge negative of propofol?
|
microbial growth
|
|
which drug do you have to throw away after 6 hours because it supports microbial growth?
|
propofol
|
|
what is an advantage of propofol over thiopental?
|
maintains short term anesthesia with a smooth, short recovery
|
|
What is another disadvantage of propofol besides its supporting microbial growth?
|
-expensive $$$
|
|
Which drug causes heinz body anemia in cats?
|
propofol
|
|
Which phenol can be given IV for control of status epilepticus?
|
propofol
|
|
What is one imidazole derivative?
|
etomidate
|
|
which drug inhibits adrenal steroidogenesis?
|
etomidate
|
|
What is neuroleptalgesia?
|
neurolpetis: lack of anxiety
analgesia: lack of pain so anesthetics with a lack of pain and anxiety |
|
What is the prototype opioid?
|
morphine
|
|
Benzodiazepam antagonist?
|
flumazenil
|
|
You should remember to combine opioids with other two types of drugs?
|
1. sedatives
2. tranquilizers |
|
what drugs cause a loss of sensation in a body part w/o loss of consciousness and sensation?
|
local anesthetics
|
|
These are advantages of what group of drugs?
1. Avoid physio abnormalities of general anesthesia 2. neurophysiological responses to pain and stress can be modified beneficially |
local anesthetics
|
|
In local anesthetics, addition of carbon to the aromatic ring or the amine group of the molecule increase, decrease or do nothing to its lipid solubility?
|
addition of carbon increase the lipid solubility
|
|
why can benzocaine be used topically?
|
it has a hydrophilic domain
|
|
These are idea characteristics of what type of drugs:
1. reversible nerve block 2. non-irritating to tissue 3. low systemic toxicity 4. effective whether injected or applied topically 5. rapid onset, sufficient duration, prompt recovery |
ideal characteristics of a local anesthetic
|
|
Local anesthetics are weak acids or weak bases?
|
weak bases
|
|
Local anesthetics are water soluble or insoluble?
|
water insoluble
|
|
How does pKa relate to the onset of action of a local anesthetic?
|
pka close to body's pH=rapid onset of action
pka higher than the body's pH=slower onset of action |
|
If you injected local anesthetic into inflammed tissue, will onset of action be faster or slower? pharm action?
|
slower onset of action
pharm action: less-inflammation is acidic so a majority of the drug will be in the ionized form, which can't cross tissue membranes |
|
Lipophilicity will do what to toxicity?
|
increase toxicity (decrease the TI)
|
|
If I increase the protein binding of local anesthetics will this increase, decrease or not change the duration of action?
|
increase protein binding=increased duration of action (less "free" active drug available at once)
|
|
why would vasoconstriction be a good thing in regard to local anesthetics?
|
vasoconstriction=limits absorption=increases the duration of action and decreases systemic toxicity
|
|
T/F. Local anesthetics are generally more effective when they are applied to intact skin bc they can be absorbed more readily.
|
False. local anesthetics are generally less effective on intact skin. they are more effective on broken skin.
|
|
what is the mechanism of action of local anesthetics?
|
block voltage gated channels thus preventing the initial phase of depolarization and subsequent development of an action potential.
|
|
Amide type local anesthetics have rapid or slow elimination?
|
rapid elimination bc they are widely distributed
|
|
why is ester type local anesthetics distribution limited?
|
bc they have a short half life which limits distribution, they are hydrolyzed and inactivated by plasma esterases
|
|
If I give a local anesthetic to a pregnant cow will I have more time to work on her with the anesthetic or less time? why?
|
more time. bc plasma esterases that eliminate local anesthetics are low in pregnant animals
|
|
if you give local anesthetics intrathecally, what does this do to the action of the anesthetic?
|
prolongs the action of the anesthetic bc spinal fluid is low in plasma esterase (like a pregnant animal)
|
|
Where are amide local anesthetics metabolized? Why might this be an issue?
|
They are metabolized in the liver, bad for cats bc they lack glucuronic acid
|
|
what is the first sign of local anesthetic toxicity?
|
muscle twitching
|
|
what local anesthetic should you never give IV? why?
|
bupivacaine=cardiotoxic=death
|
|
what is a negative about ester type local anesthetics?
|
they can cause allergic type reactions
|
|
what drugs can cause methemoglobinemia?
|
benzocaine, lidocaine, procaine
|
|
What species is most suscetible to methemoglobinemia, with administration of what drugs?
|
cats with administration of local anesthetics (ie benzocaine, lidocaine, procaine)
|
|
which local anesthetic can be used IV for control of premature ventricular contractions?
|
lidocaine
|
|
What is a local anesthetic for horses with ectopic foci, atrial fibrillation and atrial flutter
|
quinidine
|
|
Can you give lidocaine orally?
|
nope. first pass effect
|
|
why use lidocaine with thiopental?
|
decrease the dose of thiopental and prevent ventricular bigeminy
|
|
why give IV lidocaine to horses?
|
for gastric reflux
-it improves GI motility, that way you don't have to be tubing them all the time! |
|
what two local anesthetics are commonly used for opthalmology?
|
-benoxinate
-procaracaine |
|
These are hormonal like substances that are synthesized and function in a localized area. In general they do not function like circulating hormones.
|
autacoids (histamine and serotonin)
|
|
These inhibit the senthesis, release or effects of autacoids.
|
autacoid antagonists
|
|
three major groups of autacoids?
|
1. biogenic amines
2. polypeptide 3. phospholipid derived autacoids |
|
where are H1 receptors located?
|
smm cell-contraction
|
|
where are H2 receptors located?
|
on parietal cells in the stomach
|
|
where are H3 receptors located?
|
in the CNS (located presynaptically)
|
|
where is histamine made?
|
in almost all mammalian cells
|
|
What are two stores of histamine?
|
1. mast cells and basophils store histamine
2. nonmast cells-histamine is synthesized and released constantly |
|
where is the highest concentration of histamine found?
|
-in the hypothalamus
|
|
what are three ways that histamine can be release?
|
1. physical trauma to the membrane of mast cells or basophils
2. immune mediated release 3. drugs, peptides, venoms, others |
|
Describe the process involved when histamine is released during an immune mediated response.
|
body produces Abs the first time it sees an antigen. it makes IgE from plasma cells, binds to receptors on mast cells and basophils which sensitizes these cells. So the second time the body encounters the same antigen there is release of histamine from mast cells and basophils that are already bound to IgE for that antigen (they are sensitized). this is an energy dependent process
|
|
with histamine release will you see an increase or decrease in HR? vasodilation or vasoconstriction? hypertension or hypotension?
|
increase HR=vasodilation=hypotension
|
|
What do histamine antagonists do specifically?
|
inhibit H1 receptors (antihistamines only inhibit H1 receptors, none of the other H receptors)
|
|
What are the two types of antihistamines?
|
first generation
second generation |
|
Which generation antihistamines block H1 receptors, muscarinics, dopamine, alpha adrenergics and serotonin?
|
first generation
|
|
which generation of antihistamines does cyproheptadine belong to?
|
second generation
|
|
Cyproheptidine blocks?
|
serotonin
|
|
which generation antihistamines are potent inducers of cytochrome p450s?
|
second generation
|
|
what is the main goal of antihistamine therapy?
|
increase bronchodilation while maintaining normal blood pressure
|
|
will antihistamines block gastric acid production?
|
no. antihistamines only block H1 receptors, gastric acid come from parietal cells which have H2 receptors
|
|
which generation antihistamines can cross the BBB?
|
first generation=cause sedation
|
|
what drugs do you use as antiemetics for motion sickness?
|
can use antihistamines (benadryl)
|
|
Cyproheptidine is used for what in cats?
|
appetite stimulant
-and for photic head shaking in horses |
|
Antihistamines shouldn't be given to pregnant animals, why?
|
teratogenic=cause abnormalities
|
|
why do antihistamines work better in dogs?
|
they have more histaminergic receptors than cats
|
|
what are some examples of H2 receptor antagonists?
|
-cimetidine, ranitidine, famotidine, nizatidine
|
|
cimetidine and ranitidine are weak or potent inducers or inhibitors of p450s?
|
weak INHIBITORS
|
|
what two antihistamines are prokinetic and why?
|
cimetidine and ranitidine bc they increase Ach levels=make you poo
|
|
What drug stabilizes the membranes of cells and thus inhibits the release of histamine?
|
cromolyn sodium
|
|
You can give what drug IV to treat the immediate effects of anaphylaxis?
|
IV epinephrine
|
|
what drug is a potent antagonist of serotonin, is an appetite stimulant in cats, and is used in horses with cushing's disease
|
cyproheptadine
|
|
Elimination of Na ions?
|
naturetic
|
|
Elimination of solutes and water?
|
diuretic
|
|
Elimination of NaCl?
(which could affect bromide elimination) |
Saluretic
|
|
In general we use these drugs for heart failure, mobilization of edema, prophylaxis of renal failure
|
diuretics
|
|
This is an osmotic diuretic for reduction of cerebral edema?
|
-mannitol
|
|
this type of diuretic is the most effective for prophylaxis of renal failure by initiating urine flow after shock, cardiac emergencies, and surgery?
|
-osmotic diuretic
|
|
What is an acidifying agent diuretic?
|
ammonium chloride
|
|
How does ammonium chloride work as a diuretic?
|
Cl- being excreted in the urine drags some amount of Na with it which in turn draws water along with it
|
|
How do you get tolerance to ammonium chloride?
|
-acidic state initiates the formation of NH3. NH3 and H+ give NH4+ which replaces Na+ as the equivalent cation for Cl- secretion=decreases osmotic drag and diuresis is lost
|
|
what is an example of a carbonic anhydrase inhibitor (diuretic)
|
acetazolamide
|
|
Can you use carbonic anhydrase inhibitors chronically for glaucoma?
|
-yes. use topically you get no tolerance
|
|
How do thiazide diuretics work?
|
-inhibit Na resorption,
|
|
With thiazide diuretics, where is the point of action? why is this significant?
|
point of action is proximal to aldosterone controlled Na-K exchange. So K+ loss can be significant=hypokalemia
|
|
These diuretics are diabetogenic in subclinical diabetes mellitus but show beneficial effects in reducing urine flow in diabetes insipidus. But you have to have K+ to convert proinsulin to insulin, so you get an increased glucose level, esp in those with diabetes mellitus
|
thiazide diuretics
|
|
what diuretics are used for nephrogenic diabetes insipidus, systemic hypertension
|
thiazide diuretics
|
|
How can thiazide diuretics cause hypocalcemia?
|
-they increase the number of calcium binding receptors
|
|
what is the prototype anthranilic acid derivative?
|
-aka look diuretic
-prototype: furosemide=lasix |
|
What is the most potent, most commonly used diuretic in vet med?
|
furosemide
|
|
What drugs could cause ototoxicity in cats?
|
furosemide (loop diuretics)
|
|
what is the mechanism of action of K sparing diuretics?
|
-act on collecting tubule to diminish Na reabsorption and K excretion
-there is potential for hyperkalemia |
|
Since there is potential for hyperkalemia with K sparing diuretics, what other diuretic can you use in conjunction to correct for this?
|
thiazide, tends to loose too much K
|
|
What diuretic should be used in conjuction with thiazide for congestive heart failure patients?
|
K sparing diuretics
|