Term
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Definition
DIRECT AGONIST OF ACH (MUSCARINIC)
Urecholine/Duvoid
increase smooth muscle tone and motility of detrusor muscle in bladder
-helps empty bladder
-treatment of GERD
-given orally or subQ
-never give IM or IV due to extreme cholinergic side effects
-10-50 mg 1 hr before meals |
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Term
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Definition
DIRECT AGONIST OF ACH (MUSCARINIC)
Glaucoma (cause miosis and drop in IOP)
activates pupillary sphincter and canal of Schlemn |
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Term
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Definition
DIRECT AGONIST OF ACH (MUSCARINIC)
glaucoma (cause miosis and drop in IOP)
relieve xerostomaia in Sjorgen Syndrome
emergency management of malignant glaucoma |
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Term
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Definition
(Evoxac) DIRECT AGONIST OF ACH (MUSCARINIC)
Increases salivation, indicated for xerostomia in Sjorgen Syndrome
Could have patient put a marble or piece of sugarless candy in mouth if they don't want the side effects of the drug |
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Term
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Definition
Hydergine REVERSIBLE ACH INHIBITOR
potent vasoconstrictor
treatment of vascular headache
improved cerebral circulation
uncertain positive effects with AD (won't prescribe to patients) |
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Term
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Definition
Tacrine REVERSIBLE AChE INHIBITOR
Mild to moderate dementia of AD type
first developed and approved
hepatotoxicity
have to take 4 times a day |
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Term
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Definition
Aricept REVERSIBLE ACHE INHIBITOR
mild to moderate dementia
once daily dosing, no liver toxicities
CYP450 Substrate |
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Term
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Definition
Exelon REVERSIBLE ACHE INHIBITOR
mild to moderate dementia AD
difficult to titrate due to GI SE
no benefits over donepezil but available in a liquid |
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Term
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Definition
Reminyl REVERSIBLE ACHE INHIBITOR
mild to moderate dementia AD
CYP 450 metabolism
GI SE similar to rivastigmine |
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Term
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Definition
Namenda
NMDA receptor antagonist
binds N-methyl-D-aspertase receptors
moderate to severe dementia AD
inhibits glutaminergig neurodegeneration
SE's: GI, dizziness, confusion, HTN, hallucinations, long T1/2 |
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Term
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Definition
IsoptoEserine REVERSIBLE ACHE INHIBITOR
increases peristalsis of the bladder or gut
can enter the CNS: convulsions, bradycardia, and paralysis of skeletal muscle
meiosis when topically applied to the eye (glaucoma therapy)
given by injection to counteract toxicities associated with anticholingergic drugs like atropine: specifically tertiray muscarinic antagonists (administered IV) |
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Term
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Definition
Prostigmin REVERSIBLE ACHE INHIBITOR+ DIRECT ACTING AGONIST
bladder and GI stimulant (agent of choice for tx of paralytic ileus or urinary bladder atony form surgery)
antidote for tubocurarine overdose
Myastenia gravis therapy
does NOT enter CNS
Cholinergic side effects: N&V&D hypotension
used to treat poisoning with quaternary muscarinic antagonists |
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Term
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Definition
Mestinon-oral
Regonol-IM/IV
REVERSIBLE ACHE INHIBITOR
treatment of myasthenia gravis
diagnosed using tensilon test |
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Term
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Definition
Reversol, Enlon, Tensilon
REVERSIVLE ACHE INHIBITOR
used in dx of myasthenia gravis: to differentiate cholinergic crisis from MG
If patient's strength improves after IV dose= MG, if no improvement= cholinergic crisis
antidote for NM blockade (similar to Neostigmine, yet more rapidly absorbed and short duration) |
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Term
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Definition
REVERSIBLE/IRREVERSIBLE ACHE INHIBITOR (ORGANOPHOSPHATES)
treatment of head lice (malathion): not toxic to humans
insecticide (both)
Parathion: causes most deaths associated with organophosphates |
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Term
Isoflurophate (floropryl opth)
Echothiophate (phospholine iodide) |
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Definition
IRREVERSIBLE ACHE INHIBITORS (ORGANOPHOSPHATES)
both used as second line agents to treat glaucoma
Floropryl (isoflurophate): long lasting treatment of glaucoma; used to treat open angle glaucoma and accommodative congergent strabismus (child that is farsighted-bring one eye inward to accommodate) |
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Term
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Definition
IRREVERSIBLE HCHE INHIBITORS (ORGANOPHOSPHATES)
Nerve gas
causes cholinergic intoxication
usually die of respiratory failure
-maintain respiration and decontaminate
-administer atropine
-administer PAM |
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Term
| Toxicities of AChE inhibitors DUMBELS |
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Definition
Diarrhea
Urination
Miosis
Bronchoconstriction
Excitation: skeletal muscles, CNS
Lacrimation
Salivation, Sweating |
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Term
| Current uses of Antimuscarinic Agents |
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Definition
-parkinson's disease
-overactive bladder
-tx neuroleptic-induced drug SE's
-COPD
-motion sickness/nausea
-glaucoma |
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Term
| Anti-Muscarinic Categories: |
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Definition
Tertiary amines: more widespread, cross BBB, lipophilic
Quat. amines: less widespread, don't cross BBB, hydrophilic |
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Term
|
Definition
ANTICHOLINERGIC
treat bradycardia
dilate pupil on exam
Gi antispasmodic
antidote for organophosphate poisioning
detrusor antispasmodic
Crosses BBB
as antispasmodic rarely used alone due to potent anti-secretory effect
SEs: delirious
dilate pupils: hard to see
flushing
dry skin
overheating |
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Term
| Atropine Sulfate Kinetics |
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Definition
Administration: endotracheal, Im, IV, PO, SC, and ophthalmic
Distribution: well distributed, crosses BBB
Metabolism: hepatic
Eliminated: parent drug and metabolites in urine |
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Term
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Definition
Isopto Hyoscine Transderm-Scop ANTICHOLINERGIC prevention of motion sickness by blocking muscarinic receptors in the vestibular system and CNS
and N&V
pre op amnesia and reduction of respiratory and salivary secretions
crosses BBB
higher CNS penetration than atropine
amnestic and sedative properties |
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Term
| Anticholinergic toxicites: avoid in elderly |
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Definition
mad as a hatter: delirious
blind as a bat: dilate pupils of eye
red as a beet: flushing common SE
dry as a bone: dry skin
hot as a hare: cause overheating and hyperthermia |
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Term
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Definition
ANTICHOLINERGIC
Librax
antispasmodic in GI tract
treatment of peptic ulcer disease and IBS
used in combination with Chlordiaxepoxide 5mg (librium) |
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Term
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Definition
ANTICHOLINERGIC
bentyl
GI Antispasmodic, IBS
IM injection twice as bioavailable as oral dose
requires higher dose rate than what is approved
only oral dose clearly shown to be effective is 160 mg/ day divided in 4 equal doses |
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Term
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Definition
Anticholinergic
Urispas
inhibits spasm of urinary tract
available orally 100 mg tablet
indicated for symptomatic relief of dysuria, urgency, nocturia, suprapubic pain, frequency, and incontinence |
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Term
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Definition
Anticholinergic
Detrol
Tx of overactive bladder
rapidly absorbed orally
food intake increases bioavailability
pharmacologically active metabolite
reduce dose in pt with reduced hepatic function (should not receive doses greater than 1mg twice daily) |
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Term
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Definition
Anticholinergic
Atrovent
bronchodilator
anti-secretory in COPD (relaxes smooth M and prevents contraction of smooth muscle)
given by inhalation
not as effective as B agonist
very few antimuscarinic effects outside of the lungs because poorly absorbed and rapidly metabolized |
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Term
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Definition
Anticholinergic
Enablex
antispasmodic: tx overactive bladder
caution with CYP 450 inhibitors
SE: xerostomia, constipation, pregnancy category C
caut: glaucoma, urinary retention, GI retention, obstruction, MG, hot environment |
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Term
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Definition
Anticholinergic
VESIcare
Tx of overactive bladder
pay attention to pts CrCl
same SEs as darifenacin + QT prolongation, and angioedema
can cause ventricular arrhythmia
more expensive |
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Term
|
Definition
Anticholinergic
Sanctura
treatment of overactive bladder
take on empty stomach |
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Term
|
Definition
Anectine
NM blocking drug
depolarizing nicotinic cholinergic agonist
occupying and activating nicotinic receptor for a prolonged period of time, leading to blockade
-induce brief paralysis in short surgical procedures such as tracheal intubation (does not relieve pain or produce sedation)
rapid onset and short duration of action
abnormally prolonged action causes apnea |
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Term
| Mivacurium, Rapacuronium, Atracurium, Cisatracurium, Rocuronium, Vercuronium, Doxacurium, Tubocurarine, Gallamine, Metocurarine, Pancuronium, Pipecuronium |
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Definition
NM blockers, nondepolarizing, nicotinic anticholinergic
flaccid paralysis, short acting-long acting
intubation surgery |
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Term
| Botulinium Toxin Type A (Botox) |
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Definition
anticholinergic: inhibit ACh release at NC junction
muscle relaxing drug: tx spasticity in children, injected IM to produce partial chemical denervation of muscle
onset of action 3-5 days after injection, lasts up to 3 months post injection
SEs: dyphagia, pregnancy category C |
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Term
|
Definition
A2 agonist
tx of hypertension
prevent release of NE form adrenergic nerve endings
in anesthesia: reduced dose of IV hypnotic needed for anaesthetic induction and orotracheal intubation
Classic tx for opioid withdrawal and alcoholic withdrawal |
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Term
|
Definition
INDIRECT A2 AGNIST
Increases release of NE from the nerve ending vesicles thus potentiating the effects of natural amine
other effect of stimulating CNS, increased HR and increased BP |
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Term
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Definition
Mixed action: direct acting A and B agonist + indirect agonist
CNS stimulant effect and used by people to keep them alert
bronchodialtor and decongestant (removed from OTC products by FDA b/c can be used to make meth)
Long half life |
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Term
|
Definition
Aramine
Mixed action: acting A and B agonist + indirect agonist
increases both systolic and diastolic blood pressure
positive iontropic effect on heart
peripheral vasoconstriction action
Begins 1-2 min after IV infusion
10 min after IM injection
5-20 min after sub Q injection
effects last 20 min to 1 hr |
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Term
|
Definition
Drug of choice for immediate tx of anaphylactic shock
acts both A and B receptors but most prominent actions are on B receptors of the HEART, VASCULATURE AND OTHER SMOOTH M.
given IV, intracardiac or via endotracheal tube
not effective orally
minimal CNS penetration
baroreceptor reflex will not affect this |
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Term
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Definition
activates both B1 and A receptors
increases TP and diastolic BP
increase MAP and systolic BP
has direct stimulant effect on heart rate (overcome by baroreceptor mediated vagal bradycardia)
rarely used therapeutically
synthesized from DOPA
stored in vesicles
released into synapse and binds to receptor
metabolized by CMOT or restored |
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Term
| Dopamine (intropin, dopastat) |
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Definition
used for severe heart failure, easier to titrate than epi
activated peripheral B receptors to increase HR and contractility (+ chromotrope, +inotrope)
activates dopamine receptors in renal , coronary and splanchnic vessels to reduce arterial resistance and increase blood flow
no oral activity
found in basal ganglia and adrenal medulla
low dose positive inotropic effect and increase systolic BP (w/ little effect on diastolic bp or mean bp)
high dose activated A receptors that cause vasoconstriction with reflex heart rate |
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Term
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Definition
increases CO and lowers TPR
high dose increases HE and BP
B1 selective
no effect on dopamine receptors
given IV infusion
short T1/2 (2 min)
clinically for shock and heart failure |
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Term
|
Definition
Direct acting B agonist
dilates bronchial smooth m
increases HR and increases contractility
causes vasodilation
decreases TPR and decreases diastolic BP
activates B 1,2 receptors with little A activity
poor oral activity
given orally, IV, SL, inhalation |
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Term
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Definition
Direct acting B agonist
dilates bronchial smooth m
increases HR and increases contractility
causes vasodilation
decreases TPR and decreases diastolic BP
activates B 1,2 receptors with little A activity
poor oral activity
given orally, IV, SL, inhalation |
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Term
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Definition
Direct acting B agonist
dilates bronchial smooth m
increases HR and increases contractility
causes vasodilation
decreases TPR and decreases diastolic BP
activates B 1,2 receptors with little A activity
poor oral activity
given orally, IV, SL, inhalation |
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Term
Metaproterenol
(metaperl, alupent) |
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Definition
DIRECT ACTIN B2 AGONIST
relax bronchial smooth m with fewer cardiac effects and longer duration of action that epi
slow onset
intermediate duration (1hr/4hrs) |
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Term
Albuterol
(proventil, ventolin) |
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Definition
Direct acting B2 agonist
relax bronchial smooth m with fewer cardiac effects and longer duration than epi
rapid acting |
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Term
|
Definition
Direct acting B2 agonist
relax bronchial smooth m with fewer cardiac effects and longer duration than epi
rapid onset
short duration |
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Term
Tetrabutaline
(brethine, bricanyl)
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|
Definition
Direct acting B2 agonist
Tx of bronchospasm + used to suppress premature labor (inhibits uterine contractions, causes relaxation of the uterus) |
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Term
|
Definition
Direct acting B2 agonist
tx of bronchospasm + used to suppress premature labor (inhibits contractions of the uterus, causes relaxation) |
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Term
Phenylephrine
(NeoSynephrine) |
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Definition
A1 agonist
topical application to nasal mucosa for vasoconstriction and ocular application for mydriasis |
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Term
|
Definition
A1 antagonist
Tx of hypertension (relaxation of atrial and venous smooth m.)
BPH: relaxation of bladder neck muscle
Have little CV activity (no A2)
SEs: first dose orthostasis- best to give first dose at bedtime (HS) |
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Term
|
Definition
A1 antagonist
Tx of hypertension (relaxation of atrial and venous smooth m.)
BPH: relaxation of bladder neck muscle
Have little CV activity (no A2)
SEs: first dose orthostasis- best to give first dose at bedtime (HS)
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Term
|
Definition
A1 antagonist
Tx of hypertension (relaxation of atrial and venous smooth m.)
BPH: relaxation of bladder neck muscle
Have little CV activity (no A2)
SEs: first dose orthostasis- best to give first dose at bedtime (HS)
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Term
|
Definition
Direct A1 antagonist
BPH only (not for HTN)
relaxes smooth m. improving urine flow
r/o prostate ca. prior to therapy
caution with inhibitors of CYP-450
dosage 0.4 mg QD 30 min after meal daily
interactions with Viagra, Levitra and Cialis: potential orthostasis |
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Term
|
Definition
A2 antagonist
used primarily for research applications
treat erectile dysfunction |
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Term
|
Definition
A2 antagonist
used primarily for research applications |
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Term
| Phentolamine (Regitine, Vasomax) |
|
Definition
Non selective A antagonist reversible short acting
tx for HTN emergencies associated with pheochromocytosis
increases vasodilation
tx for Raynaud's syndrome
prevention of dermal necrosis after etravasatioin of damaging chemicals into soft tissue
tx of ED
blocks vasoconstriction to increase tissue perfusion in pts with shock
lowers BP and decreases TPR: accompanied by reflex tachycardia (due to decreased vascular tone with may be exaggerated secondary to A2 receptor blockade on cardiac cell membranes
Given IV or IM
lasts 4 hrs after administration
causes epi reversal
SEs: dizziness, orthostatic hypotension, myocardial ischemia, darrhea, nasal stuffiness, severe sinus tachycardia, pirapism |
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Term
|
Definition
| NONSELECTIVE A AGONIST REVERSIBLE AND SHORT ACTING |
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Term
| Phenooxybenzamine (dibenzyline) |
|
Definition
NONSELSECTIVE A AGONIST, irreversible, long acting (non-competitive)
treatment of phemochromocytoma (an adrenergic secreting adrenal gland tumor can cause severe HTn and tachycardia)
hypertensive crisis: blocks effects of exogenous and endogenous catecholamines
has been used to treat premature ejaculation
has 15-20 hr blockade: depending on ho long the body takes to make new receptor sites not bound by the drug
SEs: enters CNS causing sedation and fatigue, orthostatic hypotension, reflex tachycardia, angina (myocardial ischemia) |
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Term
|
Definition
B1 antagonist
tx of HTN
cardiac arrhythmias |
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Term
|
Definition
B1 antagonists
tx of HTN, angina pectoris, acute MI |
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Term
|
Definition
B1 antagonists
no tx for HTN
sinus tachycardia: not intended for use in chronic setting use inta and post op tachycardia and HTN
cardiac arrhythmias, SVT |
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Term
|
Definition
B1 antagonists/ B1 blocker (cardioselective BB)
Lopressor
Tx of HTN, angina pectoris, acute MI and CHF (XL formulation only) |
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Term
|
Definition
Nonselective B blocker
Tx HNT
angina pectoris
Half life of 20-24 hrs
dose interval must be adjusted for CrCl
overdose : bronchospasm, HF, bradycardia, hypotension |
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Term
| Propranolol (prototypical non selective B Blocker) |
|
Definition
Nonselective B blocker
Tx HTN, angina pectoris, hypertropic subaortic stenosis, cardiac arrhythmias, SVT arrhythmias, tachyarrhythmias of digitalis intoxication
MI, pheochromocytoma (after primary treatment with alpha adrenergic blocking agent)
migraine, essential tremor with Parkinsons
SE: brohchoconstriction, potentially lethal when administered to an asthmatic
drug-drug interactions: potentiate effects (cimetidine, furosemide, chloropromazine) inhibit effects (barbiturates, phenytoin, rifampin) |
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Term
|
Definition
Nonselective B blockers
tx HTN, MI, migraine |
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Term
| Labetalol (Normodyne, Trandate) |
|
Definition
B1, 2 and A 1 blocking properties
NTN A1 blocker reduces peripheral vascular resistance
contraindications: asthma, 2nd 3rd degree heart block, overt cardiac failure, monitor liver fct and d/c with first sign of liver toxicity |
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Term
|
Definition
A/B adrenergic blocker
HTN and CHF (in conjunction with digoxin, diuretics, ACEIs)
SE: orthostasis A and bradycardia B |
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Term
|
Definition
B1 blocker (low ISA)
HTN and arrhythmias
active metabolite 8-13 hrs |
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Term
|
Definition
B1 blocker
HTN, angina, acute MI
no active metabolite |
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Term
|
Definition
B1 blocker
approved for HNT |
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Term
|
Definition
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Term
|
Definition
B1 blocker
SVT and sinus tach
metabolized by RBCs
must keep IV dripping because fast metabolism |
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Term
|
Definition
partial agonist at B receptors
mitigate lipid and CHO metabolic effects seen with B blockers
without albuterol on board: 100% binding
with albuterol on board: albuterol effect is mitigated and as the pindolol concentration decreases the albuterol effect increases
given orally |
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