drug high points Flashcards
which muscarinic agonist is contraindicated in narrow angle glaucoma and iritis
Cevimeline (Evoxac)
which muscarinic agonist is linked to an increased incidence of UTIs
Cevimeline
what topical muscarinic agonist is used to treat glaucoma
Pilocarpine
also approved for xerostomia from Sjogren syndrome or from salivary gland damage from radiation therapy
treatment of Muscarinic poisoning
Atropine and supportive therapy
drug of choice for treating poisoning by atropine and other drugs that cause muscarinic blockade such as antihistamines and phenothiazine antipsychotics but not tricyclic antidepressants (due to r/o causing seizures and cardiotoxicity)
Physostigmine
drug sometimes used in diagnosis of MG or to distinguish between myasthenic or cholinergic crisis
Edrophonium (Enlon)
what 3 reversible cholinesterase inhibitors are approved for management of Alzheimer Disease
Donepezil (Aricept)
Galantamine (Razadyne)
Rivastigmine (Exelon)
which reversible cholinesterase inhibitor is approved for mgmt of Alzheimer Disease and Dementia of Parkinson Disease
Rivastigmine (Exelon)
irreversible cholinesterase inhibitors are only approved for
what drug?
treatment of glaucoma
Echothiophate (Phospoline Iodide)
pharm treatment of irreversible cholinesterase inhibitor poisoning
Atropine to reduce muscarinic stim
pralidoxime to reverse inhibition of cholinesterase
Benzodiazepine such as diazepam to suppress convulsions
Resp depression from cholinesterase inhibitors - mechanical ventilation
drug of choice for MG
Pyridostigmine (Mestinon, Regonol)
which drug is used in keratoconjunctivitis sicca
Cevimeline
when should you take muscarinic agonists and cholinesterase inhibitors in relation to food and why
1 hr before meals or 2h after to decrease incidence of n/v
what is the diff between cholinergic and muscarinic
they are the same. 2 diff terms mean the same
what class
Bethanechol
Cevimeline
Muscarinic Agonists
What class Pyridostimine physostigmine
reversible cholinesterase Inhibitors
what class echothiophate
irreversible cholinesterase inhibitors
what class Atropine Scopolamine Ipratropium (Atrovent) Dicyclomine Oxybutynin Solifenacen Darifenacin Tolterodine Fesoterodine Trospium
muscarinic Antagonists (can also be interchangeably called parasympatholytic drugs, antimuscarinic drugs, muscarinic blockers, anticholinergic drugs)
what anticholinergic is safe to take in pregnancy
Oxybutynin
Can you give antimuscarinic drugs to older adults
no
antidote to anticholinesterase poisoning
Atropine
what drug is used for treatment of sinus bradycardia
and AV block
Atropine
what are the problems associated with xerostomia
dry mouth promotes tooth, gum problems and oral infections.
Pt ed for Xerostomia
sipp fluids
chew sugar free gum
use salivary stimulants (citrus-flavored or tart sugarless candies, maltose lozenges)
salivary substitutes such as biotene dry mouth spray and Xylimelts are available OTC
Avoid sugary gum and hard candy
How can someone decrease urinary retention when taking atropine
void before taking med
same for all muscarinic antagonists
Pt ed on constipation
increase dietary fiber and fluids and physical activity
contraindications for taking muscarinic antagonists
glaucoma due to increased iop intestinal Atony MI BPH - urinary retention urinary tract obstruction MG pt - can precipitate myasthenic crisis use caution in pt with preexisting tachycardia use caution in asthmatics
such as Atropine
Pt is taking a muscarinic antagonist. It is summer time and they have a trip planned with their family. What important education would you give
This can cause anhidrosis. Sweating is necessary for cooling and someone who cannot sweat is at risk for hyperthermia. Avoid activities that might lead to overheating
drug interactions for muscarinic antagonists due to their significant muscarinic blockade
tricyclic antidepressants (TCA)
antihistamines
phenothiazine antipsychotics
“Don’t feed anyone on Atropine TAPAs!”
muscarinic antagonist that is used for motion sickness
Scopolamine
Muscarinic antagonist (anticholinergic) used to treat asthma, COPD, rhinitis caused by allergies or the common cold
Ipratropium (Atrovent)
anticholinergic for IBS or hypermotility
Dicyclomine (Bentyl)
pneumonic/ way to remember Atropine or anticholinergic adverse effects
Can’t see, Can’t pee, Can’t Shit, Can’t Spit
blurred vision/photophobia/elevated IOP urinary retention Constipation Xerostomia Anhidrosis
Tachycardia
Thickening of bronchial secretions and causes bronchial plugging
3 ways to reduce side effects for anticholinergics
1) using long acting formulas
2) using drugs that dont cross BBB
3) using drugs that are selective
highly selective M3 med for OAB
Darifenacin (Enablex)
Primarily M3 selective med for OAB
Oxybutynin
Solifenacin
Nonselective drugs for OAB
Fesoterodine
Tolterodine
Trospium
M1 affects what when activated/blocked
salivary glands - > salivation -> dry mouth
CNS ->enhanced cognition -> confusion/hallucinations
M2 affect what when activated/blocked
Heart - > Bradycardia ->tachycardia
M3 affects what when activated/blocked
Salivary glands -> Salivation->dry mouth
Bladder-> voiding ->urinary retention
GI smooth muscle -> increased tone/motility -> constipation
eyes -> miosis, accomodation, tearing ->mydriasis, blurred vision, dry eyes
what drug for OAB caused hallucinations and agitation that were prominent among pediatric and hallucinations, confusion and sedation with older adults pts
Oxybutynin (Ditropan XL, Gelnique, Oxytrol)
which two drugs for OAB has a side effect of Headache
Darifenacin and Solifenacin
Which drugs for OAB have the side effect of prolonging QT interval
Solifenacin
Tolterodine
which OAB drug is not metabolized by CYP enzymes
Trospium
Which OAB has the lowest bioavailability and lacks CNS effects
Trospium
Which OAB has been associated with angioedema of the face, lips, tongue and larynx
Solifenacin
which OAB drugs should be avoided in severe liver impairment
Darifenacin
Solifenacin
CYP3A4 inhibitors
azole antifungal drugs (ketoconazole, itraconazole)
certain protease inhibitors for HIV/AIDS (ritonavir, nelfinavir)
Macrolide abx such as Clarithromycin
drug interactions for Trospium
Trospium is eliminated by the kidneys, we can assume it may compete with other drugs that undergo renal tubular excretion.
Among these are Vancomycin Metformin Digoxin Procainamide
what is the only OAB drug not available in Extended release or long acting
Solifenacin
How is Solifenacin taken?
swallowed intact with liquid
with or without food
which 2 OAB drugs don’t effect CNS
Darifenacin (no effect on memory, reaction time, word recognition or cognition)
Trospium
antidote to antimuscarinic poisoning
physostigmine
how to differentiate between a true psychotic episode and antimuscarinic poisoning
a true psychotic episode is not associated with signs of excessive muscarinic blockade
-dry mouth
hyperthermia
dry skin, ect
Name that class Epinephrine Norepinephrine Isoproterenol Dopamine Dobutamine Phenylephrine Albuterol Ephedrine
Adrenergic Agonists
catecholamines and noncatecholamines
all are catecholamines except
Phenylephrine
Albuterol
Ephedrine
Catecholamines vs Noncatecholamines
Catecholamines
1) cant be taken orally (MAO and COMT)
2) Short duration of action
3) Do not act on CNS
what catecholamine is safe in pregnancy
Dobutamine
Which catecholamines/noncatecholamines has a adverse effect of hyperglycemia in diabetics and which receptor is responsible for this
Epinephrine
Isoproterenol
Albuterol
Ephedrine
B2
which catecholamine works on all 4 adrenergic receptors
Epinephrine
“The Es include everybody”
Which non-catecholamine works on all 4 adrenergic receptors
Ephedrine
“The Es include everybody”
What do you give for A1 adrenergic agonist extravates
phentolamine
what catecholamines can cause tissue necrosis if extravated
Epinephrine
norepinephrine
dopamine (if high doses)
Alpha1 receptors cause
Vasoconstriction of blood vessels
Mydriasis
Alpha2 receptors cause
Reduction in sympathetic outflow to heart and blood vessels
Severe pain
Beta1 receptors affect
Heart
Kidney
Beta2 receptors affect
Lungs
Uterus
Liver and skeletal muscle – glycogenolysis which can cause hyperglycemia in DM II patients
Dopamine receptors
Dilation of renal vasculature
what drugs interact with catecholamines
MAO inhibitors (inactivates epi)
Tricyclic antidepressants -block uptake and prolong epi effects
several inhalation anesthetics - tachydysrhythmias
noncatecholamine that is used to reduce nasal congestion, raise BP and dilate the eyes. Also used coadministered with local anesthetics to delay anesthetic absorbtion
Phenylephrine
Adverse effects of Albuterol in high doses
why?
Tremors
Tachycardia
high doses affect B1 in addition to B2
adverse effect that Ephedrine has but Epinephrine does not share
insomnia due to Ephedrine crossing CNS and Epinephrine not
Alpha adrenergic antagonists approved in children
OraVerse - agent for reversal of local anesthesia following dental surgery
phentolamine for prevention of tissue damage post extravation of iv vasopressors
Alpha Adrenergic antagonists approved during pregnancy
There are 3 but they are only approved for BPH so irrelevant. no others are approved
older adults are esp vulnerable to what side effect of alpha blockers
first dose effect.
Beers criteria specifically identifies what a1 blockers as innapropriate for older adults
doxazosin
prazosin
terazosin
due to high incidence of orthostatic hyypotension
Alpha blockers are associated with worsening of what in women and increases what for both genders in older adults?
urinary incontinence
syncope
what is the most significant adverse effect associated with A2 blockade
reflex tachycardia
Phenoxybenzamine
Phentolamine
nonselective A adrenergic blockers
Alfuzosin Doxazosin Prazosin Silodosin Tamsulosin Terazosin
A1 selective adrenergic blockers
Carteolol Nadolol Pindolol Propanolol Sotalol Timolol
1st gen nonselective B Blockers
Carvedilol
Labetalol
Vasodilating B Blockers
acts on B1, B2, A1
Acebutolol Atenolol Betaxolol Bisoprolol Esmolol Metoprolol Nebivolol
2nd gen B1 selective Blockers
Prazosin is approved only for
HTN and BPH
which A blockers (adrenergic antagonists) have the first dose effect as an adverse effect
Prazosin
Terazosin
Doxazosin
These 3 also have orthostatic hypotension, reflex tachycardia and nasal congestion listed
what 3 A blockers are approved for HTN and BPH
Prazosin
Terazosin
Doxazosin
what are the 3 A blockers that are only approved for BPH
Tamsulosin (Flomax)
Alfuzosin (Uroxatral)
Silodosin (Rapaflo)
Max benefits of Tamsulosin develop within
2 weeks
What A blocker approved only for BPH does not interfere with ejaculation
Alfuzosin
What A blocker approved only for BPH can prolong QT
Alfuzosin with doses four times greater than recommended
first dose effects need to know
1% of pt lose consciousness 30-60 min after pt receiving initial dose. To minimize initial dose should be small (no more than 1mg in Prazosin). Subsequent doses gradually increased with little risk for fainting. Pt who are starting treatment should avoid driving or other hazardous activities 12 -24 hrs. Take first dose right before going to bed.
drug interaction for Alfuzosin
CYP3A4 inhibitors such as erythromycin, clarithromycin, itraconazole, ketoconazole, nefazodone, HIV protease inhibitors such as ritonavir
drug interaction for Tamsulosin
combined with cimetidine increases drug levels
combined with hypotensive drugs such as PDE-5 inhibitors (Viagra)
B Blockers for Heart failure
Carvedilol
Bisoprolol
metoprolol
Propanolol is contraindicated in
AV heart block Heart failure bradycardia Asthma COPD dangerous in diabetics - use with caution history of anaphylaxis
B Blockers in pregnancy -
other than labetalol may put neonate at risk for 3-5 days Bradycardia resp distress hypoglycemia
3 antihypertensives save in pregnancy
labetalol
methyldopa
nifedipine
What antihypertensive should be avoided in pt with history of anaphyhlaxis
Propanolol
blocks epinephrine being able to help in anaphylaxis
Drug interactions Propanolol
Verapamil and diltiazem - cardiac effects are identical to propanolol so can cause excessive cardiosuppression
what b blocker is safer for diabetics, asthmatics and for pt with history of anaphylaxis
Metoprolol
bc its a selective B1
2 B blockers that block A Adrenergic receptors in addition to B1 and B2
Labetalol
Carvedilol
B Blockers considered safest in pregnancy and which is drug of choice
Lebetalol - DoC
acebutolol
pindolol
sotalol
which b blocker is most secreted in Breastmilk
Betaxolol
Black box for Sotalol (Betapace)
When starting or restarting solalol, pt should be in a facility that can provide continuous EkG monitoring and CPR for min of 3 days
What lab needs to be ordered prior to starting Sotalol
Creatinine clearance
how are Sotalol and Esmolol different from the other B Blockers
very short half life of 15 min
used for emergency treatment of SVT
Esmolol
B blocker approved for ventricular dysrhythmias and maintenance of NSR in pt with prev a-fib or A flutter
Sotalol
partial agonist that produces a limited degree of receptor activation while preventing strong agonists from binding to that receptor to cause full activation
keeps resting heart rate from not being reduced like a regular B Blocker
Intrinsic sympathomimetic activity
Pindolol
The abrupt discontinuation of these b blockers may cause exacerbation of angina and increase risk for MI
Atenolol
Metoprolol
Nadolol
Timolol
Use all B Blockers with caution in Pt with a history of
Depression and in pt taking CCBs
abrupt withdrawal of B blockers can cause
tachycardia
ventricular dysrhythmias
taper off gradually
B Blocking A adrenergic receptors, carvedilol and lebetalol can cause
postural hypotension.
move slowly when changing from a supine or sitting to a upright position
lie down if feel lightheaded
B1 blockade can mask early signs and symptoms of
hypoglycemia by preventing common tachycardia, tremors and perspiration. Pt need to rely on other indicators such as hunger and poor concentration to identify hypoglycemia
B2 blockade can prevent what in diabetics
glycogenolysis which is an emergency means of increasing blood glucose. Pt may need to reduce insulin dosage.
signs and symptoms of Heart failure
shortness of breath
night coughs
swelling of extremities
notify provider if occur while taking B Blockers
Clonidine class and what it is approved for
centrally acting A2 agonist
HTN
ADHD
Severe pain
Clonidine patch pt ed
apply patch to hairless, intact skin on the upper arm or torso
apply a new patch every 7 days
Contain metal and must be removed prior to MRI
How can someone minimize daytime sedation with Clonidine
Take the major portion of daily dose at bedtime
Pt monitoring for clonidine
have pt record BP daily and call clinic if hypotension develops
Pt ed on Clonidine
do not abruptly discontinue drug - may cause tachycardia and other dysrhythmias
carry an adequate supply of meds and a copy of prescription
Possible CNS depression. Avoid hazardous activities if alertness is reduced
Dry mouth can be significant. Use pt ed for dry mouth
Potential for rebound hypertension. Refill script promptly so they dont run out of medication. Warn them not to d/c without talking to PCP first
net result of cardiac suppression and vasodilation is
decreased BP (orthostatic hypotension is not a concern)
Hypotensive responses to clonidine begin when
30-60 min after administration
can you take clonidine while pregnant
no
what central acting A2 agonist has high abuse potential
Clonidine
Clonidine Tablet prep is called
Catapres
Clonidine in an extended release tablet used for mgmt of ADHD
Kapvay
A2 agonist used for HTN and ADHD
Guanfacine (Intuniv)
What med is an indirect A2 agonist?
Methyldopa bc it has to be converted to methylnorpinephrine to be a alpha 2 agonist
The principal mechanism of methyldopa is
vasodilation, not cardiosupression.
what A2 agonist does not decrease HR or Cardiac output
Methyldopa
How is methyldopa used in pregnancy
treatment of preeclampsia
what are the two most severe adverse effects for methyldopa
Hemolytic anemia and Hepatotoxicity
What labs need to be done for methyldopa before and periodically thereafter
Coombs
CBC for blood counts (Hgb, HCT, Red cell count)
LFTs
A coombs test should be performed before treatment and
6-12 months later
if a coombs test turns positive it usually occurs
6-12 mos later. Of those pts only 5% of those pts develop hemolytic anemia. If they do not develop hemolytic anemia, they can continue the drug.
If a pt taking Methyldopa develops hemolytic anemia
Melthyldopa should be withdrawn. it resolves after withdrawal. Coombs test may remain positive for months
can you use Central acting alpha blockers in older adults
no, beers says nobody over 65
most potent diuretic
Loop diuretics
Furosemide (Lasix)
which diuretic can promote diuresis even when renal blood flow and GFR are low
Furosemide (Lasix)
if treatment with furosemide alone is insufficient, what can be added?
Thiazide Diuretic
Furosemide can promote excessive loss of
sodium, chloride and water (dehydration)
what medication acts on the thick segment of the ascending loop of Henle
Furosemide (Lasix)
what diuretic works on the early distal convoluted tubule
Thiazides
What diuretic in the late distal convoluted tubule and collecting duct (distal nephron)
Spironolactone
adverse effects of loop diuretics and thiazides
Hyponatremia Hypochloremia dehydration Hypokalemia Hypotension Ototoxicity Hyperglycemia Hyperuricemia reduction of HDL Increase in LDL and triglycerides
Rarely, loop diuretics cause hearing impairment. With _____, deafness is transient. With ______, irreversible hearing loss may occur
Furosemide
Ethacrynic acid
diuretics and pregnancy
no
Diuretics and Breastfeeding
decrease milk production
no data on drug transmission
Older adults and diuretics
most common cause of adverse med reactions and interactions in older adults. Monitor closely for dehydration and cardiac dysrhythmias
when taking Digoxin, what can increase risk for ventricular dysrhythmias
Hypokalemia
To reduce risk of dysrhythmias for pt taking Digoxin and a diuretic
Add a potassium sparing diuretic or potassium supplement
monitor Potassium levels
The risk for furosemide induced hearing loss is increased by concurrent use of
other ototoxic drugs, esp aminoglycoside antibiotics (gentamycin). Combined use should be avoided
ethacrynic acid (Edecrin)
torsemide (Demadex)
Bumetanide (Burinex)
other loop diuretics
like furosemide (Lasix)
what 2 loop diuretics are approved for HTN
Furosemide (Lasix)
Torsemide (Demadex)
Drug interactions for loop and thiazide diuretics
Digoxin Ototoxic drugs Potassium sparing diuretics lithium antihypertensive agents NSAIDS
NSAIDS and loop diuretics
reduce sodium excretion and blunt diuretic effects of loop diuretics which exacerbate edema.
thiazide diuretics and gout
can make gout worse bc promotes elevated serum uric acid levels